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Volume 25
Issue 8
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Molecules, Volume 25, Issue 8 (April-2 2020) – 244 articles

Cover Story (view full-size image): The research of noble metals containing polyoxometalates is a challenging field that combines smart synthetic approaches and nontrivial reactivity with wide perspectives for different catalytic applications. The unique combination of ruthenium and polyoxoanions creates a new generation of water oxidation and organic substrates activation catalysts. In this report, we summarized our studies of Ru-atom reactivity inside the POM backbone towards azide. Two reaction pathways result in i) azide-acetonitrile click reaction and ii) azide decomposition. The first pathway produces coordinated tetrazole and the second generates a novel POM complex with a coordinated N2 molecule. Such reactivity is important for the transformation of organic substrates and N2 activation. View this paper.

 

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11 pages, 1043 KiB  
Article
Extraction of Protein from Four Different Seaweeds Using Three Different Physical Pre-Treatment Strategies
by Jack O’ Connor, Steve Meaney, Gwilym A. Williams and Maria Hayes
Molecules 2020, 25(8), 2005; https://doi.org/10.3390/molecules25082005 - 24 Apr 2020
Cited by 46 | Viewed by 6749
Abstract
Seaweeds are a rich source of protein and can contain up to 47% on the dry weight basis. It is challenging to extract proteins from the raw biomass of seaweed due to resilient cell-wall complexes. Four species of macroalgae were used in this [...] Read more.
Seaweeds are a rich source of protein and can contain up to 47% on the dry weight basis. It is challenging to extract proteins from the raw biomass of seaweed due to resilient cell-wall complexes. Four species of macroalgae were used in this study-two brown, Fucus vesiculosus and Alaria esculenta, and two red, Palmaria palmata and Chondrus crispus. Three treatments were applied individually to the macroalgal species: (I) high-pressure processing (HPP); (II) laboratory autoclave processing and (III) a classical sonication and salting out method. The protein, ash and lipid contents of the resulting extracts were estimated. Yields of protein recovered ranged from 3.2% for Fucus vesiculosus pre-treated with high pressure processing to 28.9% protein recovered for Chondrus crispus treated with the classical method. The yields of protein recovered using the classical, HPP and autoclave pre-treatments applied to Fucus vesiculosus were 35.1, 23.7% and 24.3%, respectively; yields from Alaria esculenta were 18.2%, 15.0% and 17.1% respectively; yields from Palmaria palmata were 12.5%, 14.9% and 21.5% respectively, and finally, yields from Chondrus crispus were 35.2%, 16.1% and 21.9%, respectively. These results demonstrate that while macroalgal proteins may be extracted using either physical or enzymatic methods, the specific extraction procedure should be tailored to individual species. Full article
(This article belongs to the Special Issue Bioactives and Functional Ingredients in Foods and Beverages)
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8 pages, 741 KiB  
Article
Synthetic Kavalactone Analogues with Increased Potency and Selective Anthelmintic Activity against Larvae of Haemonchus contortus In Vitro
by H.M.P. Dilrukshi Herath, Aya C. Taki, Nghi Nguyen, José Garcia-Bustos, Andreas Hofmann, Tao Wang, Guangxu Ma, Bill C.H. Chang, Abdul Jabbar, Brad E. Sleebs and Robin B. Gasser
Molecules 2020, 25(8), 2004; https://doi.org/10.3390/molecules25082004 - 24 Apr 2020
Cited by 3 | Viewed by 2473
Abstract
Kava extract, an aqueous rhizome emulsion of the plant Piper methysticum, has been used for centuries by Pacific Islanders as a ceremonial beverage, and has been sold as an anxiolytic agent for some decades. Kavalactones are a major constituent of kava extract. [...] Read more.
Kava extract, an aqueous rhizome emulsion of the plant Piper methysticum, has been used for centuries by Pacific Islanders as a ceremonial beverage, and has been sold as an anxiolytic agent for some decades. Kavalactones are a major constituent of kava extract. In a previous investigation, we had identified three kavalactones that inhibit larval development of Haemonchus contortus in an in vitro-bioassay. In the present study, we synthesized two kavalactones, desmethoxyyangonin and yangonin, as well as 17 analogues thereof, and evaluated their anthelmintic activities using the same bioassay as employed previously. Structure activity relationship (SAR) studies showed that a 4-substituent on the pendant aryl ring was required for activity. In particular, compounds with 4-trifluoromethoxy, 4-difluoromethoxy, 4-phenoxy, and 4-N-morpholine substitutions had anthelmintic activities (IC50 values in the range of 1.9 to 8.9 µM) that were greater than either of the parent natural products—desmethoxyyangonin (IC50 of 37.1 µM) and yangonin (IC50 of 15.0 µM). The synthesized analogues did not exhibit toxicity on HepG2 human hepatoma cells in vitro at concentrations of up to 40 µM. These findings confirm the previously-identified kavalactone scaffold as a promising chemotype for new anthelmintics and provide a basis for a detailed SAR investigation focused on developing a novel anthelmintic agent. Full article
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14 pages, 4930 KiB  
Article
Combretum quadrangulare Extract Attenuates Atopic Dermatitis-Like Skin Lesions through Modulation of MAPK Signaling in BALB/c Mice
by Ju-Hyoung Park, Min Hee Hwang, Young-Rak Cho, Seong Su Hong, Jae-Shin Kang, Won Hee Kim, Seung Hwan Yang, Dong-Wan Seo, Joa Sub Oh and Eun-Kyung Ahn
Molecules 2020, 25(8), 2003; https://doi.org/10.3390/molecules25082003 - 24 Apr 2020
Cited by 17 | Viewed by 3670
Abstract
Atopic dermatitis (AD) is a chronic inflammatory disease. Combretum quadrangulare (C. quadrangulare) is used as a traditional medicine to improve various pathologies in Southeast Asia. In this study, we investigated the effects of C. quadrangulare ethanol extract (CQ) on 1-chloro-2,4-dinitrobenzene (DNCB)-induced [...] Read more.
Atopic dermatitis (AD) is a chronic inflammatory disease. Combretum quadrangulare (C. quadrangulare) is used as a traditional medicine to improve various pathologies in Southeast Asia. In this study, we investigated the effects of C. quadrangulare ethanol extract (CQ) on 1-chloro-2,4-dinitrobenzene (DNCB)-induced AD like skin lesions in BALB/c mice. After administration with CQ (100, 200, and 400 mg/kg) for 6 weeks, AD symptoms, protein expression, immunoglobulin E (IgE), thymus and activation-regulated chemokine (TARC), and ceramidase level were measured in skin lesions of DNCB-induced BALB/c mice. CQ group improved the dermatitis score, skin pH, transepidermal water loss (TEWL), and skin hydration. Furthermore, histological analysis revealed that CQ attenuated the increased epidermal thickness and infiltration of mast cells caused by DNCB. CQ also increased the expression of filaggrin, and reduced the expression of ceramidase, serum IgE level, and the number of eosinophils. CQ effectively inhibited cytokines and chemokines such as interleukin (IL)-6, IL-13, TARC, and thymic stromal lymphopoietin (TSLP) at the mRNA levels, as well as the activation of mitogen-activated protein kinase (MAPK), including extracellular signal-regulated kinase (ERK), c-jun N-terminal kinase (JNK), and p38 in the skin lesions. Taken together, these findings demonstrate that CQ may be an effective treatment of AD-like skin lesions by inhibiting the expression of inflammatory mediators via the MAPK signaling pathways. Full article
(This article belongs to the Special Issue New Biologically Active Substances from Plants and Animals of the Pacific Region)
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15 pages, 5098 KiB  
Article
Metallurgical Preparation of Nb–Al and W–Al Intermetallic Compounds and Characterization of Their Microstructure and Phase Transformations by DTA Technique
by Tomas Cegan, Daniel Petlak, Katerina Skotnicova, Jan Jurica, Bedrich Smetana and Simona Zla
Molecules 2020, 25(8), 2001; https://doi.org/10.3390/molecules25082001 - 24 Apr 2020
Cited by 9 | Viewed by 2643
Abstract
The possibilities of metallurgical preparation of 40Nb-60Al and 15W-85Al intermetallic compounds (in at.%) by plasma arc melting (PAM) and vacuum induction melting (VIM) were studied. Both methods allow easy preparation of Nb–Al alloys; however, significant evaporation of Al was observed during the melting, [...] Read more.
The possibilities of metallurgical preparation of 40Nb-60Al and 15W-85Al intermetallic compounds (in at.%) by plasma arc melting (PAM) and vacuum induction melting (VIM) were studied. Both methods allow easy preparation of Nb–Al alloys; however, significant evaporation of Al was observed during the melting, which affected the resulting chemical composition. The preparation of W–Al alloys was more problematic because there was no complete re-melting of W during PAM and VIM. However, the combination of PAM and VIM allowed the preparation of W–Al alloy without any non-melted parts. The microstructure of Nb–Al alloys consisted of Nb2Al and NbAl3 intermetallic phases, and W–Al alloys consisted mainly of needle-like WAl4 intermetallic phase and Al matrix. The effects of melting conditions on chemical composition, homogeneity, and microstructure were determined. Differential thermal analysis was used to determine melting and phase transformation temperatures of the prepared alloys. Full article
(This article belongs to the Special Issue Intermetallics: Synthesis, Structure, Function)
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21 pages, 1065 KiB  
Review
Induced Pluripotent Stem Cell (iPSC)-Based Neurodegenerative Disease Models for Phenotype Recapitulation and Drug Screening
by Chia-Yu Chang, Hsiao-Chien Ting, Ching-Ann Liu, Hong-Lin Su, Tzyy-Wen Chiou, Shinn-Zong Lin, Horng-Jyh Harn and Tsung-Jung Ho
Molecules 2020, 25(8), 2000; https://doi.org/10.3390/molecules25082000 - 24 Apr 2020
Cited by 69 | Viewed by 11426
Abstract
Neurodegenerative diseases represent a significant unmet medical need in our aging society. There are no effective treatments for most of these diseases, and we know comparatively little regarding pathogenic mechanisms. Among the challenges faced by those involved in developing therapeutic drugs for neurodegenerative [...] Read more.
Neurodegenerative diseases represent a significant unmet medical need in our aging society. There are no effective treatments for most of these diseases, and we know comparatively little regarding pathogenic mechanisms. Among the challenges faced by those involved in developing therapeutic drugs for neurodegenerative diseases, the syndromes are often complex, and small animal models do not fully recapitulate the unique features of the human nervous system. Human induced pluripotent stem cells (iPSCs) are a novel technology that ideally would permit us to generate neuronal cells from individual patients, thereby eliminating the problem of species-specificity inherent when using animal models. Specific phenotypes of iPSC-derived cells may permit researchers to identify sub-types and to distinguish among unique clusters and groups. Recently, iPSCs were used for drug screening and testing for neurologic disorders including Alzheimer’s disease (AD), amyotrophic lateral sclerosis (ALS), spinocerebellar atrophy (SCA), and Zika virus infection. However, there remain many challenges still ahead, including how one might effectively recapitulate sporadic disease phenotypes and the selection of ideal phenotypes and for large-scale drug screening. Fortunately, quite a few novel strategies have been developed that might be combined with an iPSC-based model to solve these challenges, including organoid technology, single-cell RNA sequencing, genome editing, and deep learning artificial intelligence. Here, we will review current applications and potential future directions for iPSC-based neurodegenerative disease models for critical drug screening. Full article
(This article belongs to the Special Issue Phenotypic Drug Discovery)
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11 pages, 2459 KiB  
Article
Effect of Saturated Steam Heat Treatment on Physical and Chemical Properties of Bamboo
by Qiuyi Wang, Xinwu Wu, Chenglong Yuan, Zhichao Lou and Yanjun Li
Molecules 2020, 25(8), 1999; https://doi.org/10.3390/molecules25081999 - 24 Apr 2020
Cited by 63 | Viewed by 3231
Abstract
The aim of this study was to investigate the effects of the heat treatment time and initial moisture content of bamboo on the corresponding chemical composition, crystallinity, and mechanical properties after saturated steam heat treatment at 180 °C. The mechanism of saturated steam [...] Read more.
The aim of this study was to investigate the effects of the heat treatment time and initial moisture content of bamboo on the corresponding chemical composition, crystallinity, and mechanical properties after saturated steam heat treatment at 180 °C. The mechanism of saturated steam heat treatment of bamboo was revealed on the micro-level, providing a theoretical basis for the regulation of bamboo properties and the optimization of heat treatment process parameters. XRD patterns of the treated bamboo slices were basically the same. With the increase in the initial moisture content of bamboo, the crystallinity of bamboo increased first and then decreased after treatment. Due to the saturated steam heat treatment, the content of cellulose and lignin in bamboo slices increased while the content of hemicellulose decreased, but the content of cellulose in bamboo with a 40% initial moisture content increased first and then decreased. The shear strength of treated bamboo changed little within 10 min after saturated steam heat treatment, and then decreased rapidly. During the first 20 min with saturated steam heat treatment, the compressive strength, flexural strength, and flexural modulus of elasticity of the treated bamboo increased, and then decreased. Full article
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20 pages, 1380 KiB  
Review
Antimicrobial Peptides as Probes in Biosensors Detecting Whole Bacteria: A Review
by Éric Pardoux, Didier Boturyn and Yoann Roupioz
Molecules 2020, 25(8), 1998; https://doi.org/10.3390/molecules25081998 - 24 Apr 2020
Cited by 26 | Viewed by 4843
Abstract
Bacterial resistance is becoming a global issue due to its rapid growth. Potential new drugs as antimicrobial peptides (AMPs) are considered for several decades as promising candidates to circumvent this threat. Nonetheless, AMPs have also been used more recently in other settings such [...] Read more.
Bacterial resistance is becoming a global issue due to its rapid growth. Potential new drugs as antimicrobial peptides (AMPs) are considered for several decades as promising candidates to circumvent this threat. Nonetheless, AMPs have also been used more recently in other settings such as molecular probes grafted on biosensors able to detect whole bacteria. Rapid, reliable and cost-efficient diagnostic tools for bacterial infection could prevent the spread of the pathogen from the earliest stages. Biosensors based on AMPs would enable easy monitoring of potentially infected samples, thanks to their powerful versatility and integrability in pre-existent settings. AMPs, which show a broad spectrum of interactions with bacterial membranes, can be tailored in order to design ubiquitous biosensors easily adaptable to clinical settings. This review aims to focus on the state of the art of AMPs used as the recognition elements of whole bacteria in label-free biosensors with a particular focus on the characteristics obtained in terms of threshold, volume of sample analysable and medium, in order to assess their workability in real-world applications. Full article
(This article belongs to the Special Issue Antimicrobial Peptides: From Synthesis to Application)
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21 pages, 2386 KiB  
Review
Viral Hepatitis and Iron Dysregulation: Molecular Pathways and the Role of Lactoferrin
by Romina Mancinelli, Luigi Rosa, Antimo Cutone, Maria Stefania Lepanto, Antonio Franchitto, Paolo Onori, Eugenio Gaudio and Piera Valenti
Molecules 2020, 25(8), 1997; https://doi.org/10.3390/molecules25081997 - 24 Apr 2020
Cited by 33 | Viewed by 5189
Abstract
The liver is a frontline immune site specifically designed to check and detect potential pathogens from the bloodstream to maintain a general state of immune hyporesponsiveness. One of the main functions of the liver is the regulation of iron homeostasis. The liver detects [...] Read more.
The liver is a frontline immune site specifically designed to check and detect potential pathogens from the bloodstream to maintain a general state of immune hyporesponsiveness. One of the main functions of the liver is the regulation of iron homeostasis. The liver detects changes in systemic iron requirements and can regulate its concentration. Pathological states lead to the dysregulation of iron homeostasis which, in turn, can promote infectious and inflammatory processes. In this context, hepatic viruses deviate hepatocytes’ iron metabolism in order to better replicate. Indeed, some viruses are able to alter the expression of iron-related proteins or exploit host receptors to enter inside host cells. Lactoferrin (Lf), a multifunctional iron-binding glycoprotein belonging to the innate immunity, is endowed with potent antiviral activity, mainly related to its ability to block viral entry into host cells by interacting with viral and/or cell surface receptors. Moreover, Lf can act as an iron scavenger by both direct iron-chelation or the modulation of the main iron-related proteins. In this review, the complex interplay between viral hepatitis, iron homeostasis, and inflammation as well as the role of Lf are outlined. Full article
(This article belongs to the Collection Molecular Medicine)
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15 pages, 2787 KiB  
Article
Potential Antimicrobial and Anticancer Activities of an Ethanol Extract from Bouea macrophylla
by Ngoc Hong Nguyen, Thuy Trang Nguyen, Phu Cuong Ma, Qui Thanh Hoai Ta, Thuc-Huy Duong and Van Giau Vo
Molecules 2020, 25(8), 1996; https://doi.org/10.3390/molecules25081996 - 24 Apr 2020
Cited by 28 | Viewed by 5442
Abstract
Bouea macrophylla is a tree widely grown throughout South East Asia. It is used in folk medicine for the treatment of various illnesses. The present study aimed to identify the chemical constituents and to test the antimicrobial and anticancer activities of an ethanol [...] Read more.
Bouea macrophylla is a tree widely grown throughout South East Asia. It is used in folk medicine for the treatment of various illnesses. The present study aimed to identify the chemical constituents and to test the antimicrobial and anticancer activities of an ethanol extract from B. macrophylla leaves. The extract exhibited excellent antibacterial properties against 9 out of 10 target microorganisms. including four Gram-negative bacteria (Escherichia coli, Shigella flexneri, Vibrio cholera, and Pseudomonas aeruginosa) and four Gram-positive bacteria (Staphylococcus aureus, Listeria monocytogenes, Enterococcus faecalis, and Bacillus cereus), as well as a fungus (Candida albicans). In addition, the extract was also tested on HeLa and human colorectal carcinoma (HCT116) cells to evaluate its cytostatic effects. The ethanol extract was able to inhibit the proliferation of HeLa and HCT116 cells, showing IC50 = 24 ± 0.8 and 28 ± 0.9 µg/mL, respectively, whereas the IC50 values of doxorubicin (standard) were 13.6 ± 1.3 and 15.8 ± 1.1 µg/mL respectively. Also, we identified various bioactive compounds in the extract such as polyphenols, flavonoids, caryophyllene, phytol, and trans-geranylgeraniol by GC-MS, which could contribute to the extract’s biological activities. Therefore, our findings strongly indicate that the constituents of the B. macrophylla ethanol extract could be active against the tested bacteria and fungi as well as cancer cells. Further investigation is needed to understand the mechanisms mediating the antimicrobial and anticancer effects and identify signaling pathways that could be targeted for therapeutic application. Full article
(This article belongs to the Special Issue Biological Activities of Medicinal Plants)
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21 pages, 5874 KiB  
Article
Fluorescent Biaryl Uracils with C5-Dihydro- and Quinazolinone Heterocyclic Appendages in PNA
by Ali Heidari, Arash Ghorbani-Choghamarani, Maryam Hajjami and Robert H. E. Hudson
Molecules 2020, 25(8), 1995; https://doi.org/10.3390/molecules25081995 - 24 Apr 2020
Cited by 6 | Viewed by 3033
Abstract
There has been much effort to exploit fluorescence techniques in the detection of nucleic acids. Canonical nucleic acids are essentially nonfluorescent; however, the modification of the nucleobase has proved to be a fruitful way to engender fluorescence. Much of the chemistry used to [...] Read more.
There has been much effort to exploit fluorescence techniques in the detection of nucleic acids. Canonical nucleic acids are essentially nonfluorescent; however, the modification of the nucleobase has proved to be a fruitful way to engender fluorescence. Much of the chemistry used to prepare modified nucleobases relies on expensive transition metal catalysts. In this work, we describe the synthesis of biaryl quinazolinone-uracil nucleobase analogs prepared by the condensation of anthranilamide derivatives and 5-formyluracil using inexpensive copper salts. A selection of modified nucleobases were prepared, and the effect of methoxy- or nitro- group substitution on the photophysical properties was examined. Both the dihydroquinazolinone and quinazolinone modified uracils have much larger molar absorptivity (~4–8×) than natural uracil and produce modest blue fluorescence. The quinazolinone-modified uracils display higher quantum yields than the corresponding dihydroquinazolinones and also show temperature and viscosity dependent emission consistent with molecular rotor behavior. Peptide nucleic acid (PNA) monomers possessing quinazolinone modified uracils were prepared and incorporated into oligomers. In the sequence context examined, the nitro-substituted, methoxy-substituted and unmodified quinazolinone inserts resulted in a stabilization (∆Tm = +4.0/insert; +2.0/insert; +1.0/insert, respectively) relative to control PNA sequence upon hybridization to complementary DNA. All three derivatives responded to hybridization by the “turn-on” of fluorescence intensity by ca. 3-to-4 fold and may find use as probes for complementary DNA sequences. Full article
(This article belongs to the Special Issue Advances in Nucleoside/Nucleotides and Nucleic Acid Chemistry: A Theme Issue in Honor of Prof. Dr. Piet Herdewijn)
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12 pages, 919 KiB  
Brief Report
Nanoparticle-Mediated Gene Silencing for Sensitization of Lung Cancer to Cisplatin Therapy
by Daniel P. Feldmann, Joshua Heyza, Christoph M. Zimmermann, Steve M. Patrick and Olivia M. Merkel
Molecules 2020, 25(8), 1994; https://doi.org/10.3390/molecules25081994 - 24 Apr 2020
Cited by 10 | Viewed by 3735
Abstract
Platinum-based chemotherapy remains a mainstay treatment for the management of advanced non-small cell lung cancer. A key cellular factor that contributes to sensitivity to platinums is the 5′-3′ structure-specific endonuclease excision repair cross-complementation group 1 (ERCC1)/ xeroderma pigmentosum group F (XPF). ERCC1/XPF is [...] Read more.
Platinum-based chemotherapy remains a mainstay treatment for the management of advanced non-small cell lung cancer. A key cellular factor that contributes to sensitivity to platinums is the 5′-3′ structure-specific endonuclease excision repair cross-complementation group 1 (ERCC1)/ xeroderma pigmentosum group F (XPF). ERCC1/XPF is critical for the repair of platinum-induced DNA damage and has been the subject of intense research efforts to identify small molecule inhibitors of its nuclease activity for the purpose of enhancing patient response to platinum-based chemotherapy. As an alternative to small molecule inhibitors, small interfering RNA (siRNA) has often been described to be more efficient in interrupting protein–protein interactions. The goal of this study was therefore to determine whether biocompatible nanoparticles consisting of an amphiphilic triblock copolymer (polyethylenimine-polycaprolactone-polyethylene glycol (PEI-PCL-PEG)) and carrying siRNA targeted to ERCC1 and XPF made by microfluidic assembly are capable of efficient gene silencing and able to sensitize lung cancer cells to cisplatin. First, we show that our PEI-PCL-PEG micelleplexes carrying ERCC1 and XPF siRNA efficiently knocked down ERCC1/XPF protein expression to the same extent as the standard siRNA transfection reagent, Lipofectamine. Second, we show that our siRNA-carrying nanoparticles enhanced platinum sensitivity in a p53 wildtype model of non-small cell lung cancer in vitro. Our results suggest that nanoparticle-mediated targeting of ERCC1/XPF is feasible and could represent a novel therapeutic strategy for targeting ERCC1/XPF in vivo. Full article
(This article belongs to the Special Issue Nanocarriers for Diagnostics, Imaging, and Drug Delivery: Critical Perspectives on Materials, Technologies, in Vivo Fate)
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14 pages, 3105 KiB  
Article
The Cytotoxic and Apoptotic Effects of the Brown Algae Colpomenia sinuosa are Mediated by the Generation of Reactive Oxygen Species
by Reem Al Monla, Zeina Dassouki, Achraf Kouzayha, Yahya Salma, Hala Gali-Muhtasib and Hiba Mawlawi
Molecules 2020, 25(8), 1993; https://doi.org/10.3390/molecules25081993 - 24 Apr 2020
Cited by 18 | Viewed by 4501
Abstract
Brown algae are a novel resource of biogenic molecules, however few studies have been conducted in the Mediterranean to assess the cytotoxic mechanisms of algal-derived compounds. This study focuses on the antineoplastic activity of extracts from non-investigated algae of the Lebanese coast, Colpomenia [...] Read more.
Brown algae are a novel resource of biogenic molecules, however few studies have been conducted in the Mediterranean to assess the cytotoxic mechanisms of algal-derived compounds. This study focuses on the antineoplastic activity of extracts from non-investigated algae of the Lebanese coast, Colpomenia sinuosa. Extracts’ antineoplastic activities were evaluated by MTT and trypan blue on different tumorigenic cells. Results indicated that the most potent extract was obtained by soxhlet using dichloromethane:methanol solvent (DM soxhlet) against HCT-116. Wound healing assay confirmed that this extract decreased the migration potential of HCT-116 cells with minimal effects on non-tumorigenic cells. It also induced an increase in the subG1 population as determined by flow cytometry. Western blot analysis demonstrated that apoptosis in treated HCT-116 cells was induced via upregulation of p21 protein and downregulation of the anti-apoptotic Bcl 2, which led to caspases activation. The latter, catalyzes the degradation of PARP-1, and thus suppresses cancer proliferation. Morphological alterations, further confirmed apoptosis. A strong pro-oxidant activity evidenced by the enhanced generation of reactive oxygen species (ROS) was observed in HCT-116 treated cells. Interestingly, a strong antioxidant effectively blocked effect induced by the extract. These results indicate that C. sinuosa is a source of bioactive compounds possessing pro-apoptotic and anti-migratory efficacy. Full article
(This article belongs to the Special Issue Algae and Microalgae and Their Bioactive Molecules for Human Health)
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15 pages, 1815 KiB  
Article
Membrane Phospholipids and Polyphosphates as Cofactors and Binding Molecules of SERPINA12 (vaspin)
by Catherine A. Tindall, Sebastian Dommel, Veronika Riedl, David Ulbricht, Stefanie Hanke, Norbert Sträter and John T. Heiker
Molecules 2020, 25(8), 1992; https://doi.org/10.3390/molecules25081992 - 24 Apr 2020
Cited by 4 | Viewed by 3378
Abstract
Visceral adipose tissue derived serine protease inhibitor (vaspin) is a member of the serpin family and has been shown to have beneficial effects on glucose tolerance, insulin stability as well as adipose tissue inflammation, parameters seriously affected by obesity. Some of these effects [...] Read more.
Visceral adipose tissue derived serine protease inhibitor (vaspin) is a member of the serpin family and has been shown to have beneficial effects on glucose tolerance, insulin stability as well as adipose tissue inflammation, parameters seriously affected by obesity. Some of these effects require inhibition of target proteases such as kallikrein 7(KLK7) and many studies have demonstrated vaspin-mediated activation of intracellular signaling cascades in various cells and tissues. So far, little is known about the exact mechanism how vaspin may trigger these intracellular signaling events. In this study, we investigated and characterized the interaction of vaspin with membrane lipids and polyphosphates as well as their potential regulatory effects on serpin activity using recombinant vaspin and KLK7 proteins and functional protein variants thereof. Here, we show for the first time that vaspin binds to phospholipids and polyphosphates with varying effects on KLK7 inhibition. Vaspin binds strongly to monophosphorylated phosphatidylinositol phosphates (PtdInsP) with no effect on vaspin activation. Microscale thermophoresis (MST) measurements revealed high-affinity binding to polyphosphate 45 (KD: 466 ± 75 nM) and activation of vaspin in a heparin-like manner. Furthermore, we identified additional residues in the heparin binding site in β-sheet A by mutating five basic residues resulting in complete loss of high-affinity heparin binding. Finally, using lipid overlay assays, we show that these residues are additionally involved in PtdInsP binding. Phospholipids play a major role in membrane trafficking and signaling whereas polyphosphates are procoagulant and proinflammatory agents. The identification of phospholipids and polyphosphates as binding partners of vaspin will contribute to the understanding of vaspins involvement in membrane trafficking, signaling and beneficial effects associated with obesity. Full article
(This article belongs to the Special Issue Protein-Peptide and Protein-Small Molecule Interactions)
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21 pages, 3275 KiB  
Article
Effects of Graphene Oxide Nanofilm and Chicken Embryo Muscle Extract on Muscle Progenitor Cell Differentiation and Contraction
by Jaśmina Bałaban, Mateusz Wierzbicki, Marlena Zielińska, Jarosław Szczepaniak, Malwina Sosnowska, Karolina Daniluk, Dominik Cysewski, Piotr Koczoń, André Chwalibog and Ewa Sawosz
Molecules 2020, 25(8), 1991; https://doi.org/10.3390/molecules25081991 - 23 Apr 2020
Cited by 11 | Viewed by 3631
Abstract
Finding an effective muscle regeneration technique is a priority for regenerative medicine. It is known that the key factors determining tissue formation include cells, capable of proliferating and/or differentiating, a niche (surface) allowing their colonization and growth factors. The interaction between these factors, [...] Read more.
Finding an effective muscle regeneration technique is a priority for regenerative medicine. It is known that the key factors determining tissue formation include cells, capable of proliferating and/or differentiating, a niche (surface) allowing their colonization and growth factors. The interaction between these factors, especially between the surface of the artificial niche and growth factors, is not entirely clear. Moreover, it seems that the use of a complex of complementary growth factors instead of a few strictly defined ones could increase the effectiveness of tissue maturation, including muscle tissue. In this study, we evaluated whether graphene oxide (GO) nanofilm, chicken embryo muscle extract (CEME), and GO combined with CEME would affect the differentiation and functional maturation of muscle precursor cells, as well as the ability to spontaneously contract a pseudo-tissue muscle. CEME was extracted on day 18 of embryogenesis. Muscle cells obtained from an 8-day-old chicken embryo limb bud were treated with GO and CEME. Cell morphology and differentiation were observed using different microscopy methods. Cytotoxicity and viability of cells were measured by lactate dehydrogenase and Vybrant Cell Proliferation assays. Gene expression of myogenic regulatory genes was measured by Real-Time PCR. Our results demonstrate that CEME, independent of the culture surface, was the main factor influencing the intense differentiation of muscle progenitor cells. The present results, for the first time, clearly demonstrated that the cultured tissue-like structure was capable of inducing contractions without externally applied impulses. It has been indicated that a small amount of CEME in media (about 1%) allows the culture of pseudo-tissue muscle capable of spontaneous contraction. The study showed that the graphene oxide may be used as a niche for differentiating muscle cells, but the decisive influence on the maturation of muscle tissue, especially muscle contractions, depends on the complexity of the applied growth factors. Full article
(This article belongs to the Section Medicinal Chemistry)
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15 pages, 1478 KiB  
Article
Protective Effects of Vitamin K Compounds on the Proteomic Profile of Osteoblasts under Oxidative Stress Conditions
by Marta Muszyńska, Ewa Ambrożewicz, Agnieszka Gęgotek, Grzegorz Grynkiewicz and Elżbieta Skrzydlewska
Molecules 2020, 25(8), 1990; https://doi.org/10.3390/molecules25081990 - 23 Apr 2020
Cited by 9 | Viewed by 2834
Abstract
Oxidative stress, which accompanies the pathogenesis of many bone diseases, contributes to the reduction of osteoblast activity, resulting in the inhibition of differentiation. This study aimed to assess the effect of vitamins K1 and K2 (MK4 and MK7) on the proteomic profile of [...] Read more.
Oxidative stress, which accompanies the pathogenesis of many bone diseases, contributes to the reduction of osteoblast activity, resulting in the inhibition of differentiation. This study aimed to assess the effect of vitamins K1 and K2 (MK4 and MK7) on the proteomic profile of human osteoblasts cell line under oxidative conditions induced by hydrogen peroxide (H2O2). The analysis was performed using QExactiveHF mass spectrometer with a nanoelectrospray ionization source. The osteoblast protein exposed to oxidative stress and vitamin K was compared with the proteome of cells exposed only to oxidative stress. Our proteomic analysis identified 1234 proteins changed after 5 days, 967 after 15 days, and 1214 after 20 days of culture. We observed the most frequent changes in the expression of proteins with catalytic activity or protein/DNA binding properties (45% and 40%, respectively). Significant changes were also observed in proteins with transcription/translation regulator activity (2–6%), regulators of molecular functions (5–6%), signal transducers (1–4%), transporters (4–6%), and structural molecules (3–5%). Our results clearly show that vitamins K protect cells from H2O2-induced changes in protein expression, primarily through their effects on transcriptional regulators and transporter proteins. As a result, vitamins K can support the formation, remodeling, and mineralization of bone tissue. Full article
(This article belongs to the Collection Molecular Medicine)
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11 pages, 2748 KiB  
Article
MnO2/rGO/CNTs Framework as a Sulfur Host for High-Performance Li-S Batteries
by Wei Dong, Lingqiang Meng, Xiaodong Hong, Sizhe Liu, Ding Shen, Yingkai Xia and Shaobin Yang
Molecules 2020, 25(8), 1989; https://doi.org/10.3390/molecules25081989 - 23 Apr 2020
Cited by 27 | Viewed by 3317
Abstract
Lithium-sulfur batteries are very promising next-generation energy storage batteries due to their high theoretical specific capacity. However, the shuttle effect of lithium-sulfur batteries is one of the important bottlenecks that limits its rapid development. Herein, physical and chemical dual adsorption of lithium polysulfides [...] Read more.
Lithium-sulfur batteries are very promising next-generation energy storage batteries due to their high theoretical specific capacity. However, the shuttle effect of lithium-sulfur batteries is one of the important bottlenecks that limits its rapid development. Herein, physical and chemical dual adsorption of lithium polysulfides are achieved by designing a novel framework structure consisting of MnO2, reduced graphene oxide (rGO), and carbon nanotubes (CNTs). The framework-structure composite of MnO2/rGO/CNTs is prepared by a simple hydrothermal method. The framework exhibits a uniform and abundant mesoporous structure (concentrating in ~12 nm). MnO2 is an α phase structure and the α-MnO2 also has a significant effect on the adsorption of lithium polysulfides. The rGO and CNTs provide a good physical adsorption interaction and good electronic conductivity for the dissolved polysulfides. As a result, the MnO2/rGO/CNTs/S cathode delivered a high initial capacity of 1201 mAh g−1 at 0.2 C. The average capacities were 916 mAh g−1, 736 mAh g−1, and 547 mAh g−1 at the current densities of 0.5 C, 1 C, and 2 C, respectively. In addition, when tested at 0.5 C, the MnO2/rGO/CNTs/S exhibited a high initial capacity of 1010 mAh g−1 and achieved 780 mAh g−1 after 200 cycles, with a low capacity decay rate of 0.11% per cycle. This framework-structure composite provides a simple way to improve the electrochemical performance of Li-S batteries. Full article
(This article belongs to the Special Issue Electrochemistry of Low Dimensional and Nanostructured Carbon Materials: Applications in Sensing and Energy Storage)
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12 pages, 2578 KiB  
Article
Mechanical and Thermal Properties of Polyether Polytriazole Elastomers Formed by Click-Chemical Reaction Curing Glycidyl Azide Polymer
by Liming He, Jun Zhou, Yutao Wang, Zhongliang Ma and Chunlin Chen
Molecules 2020, 25(8), 1988; https://doi.org/10.3390/molecules25081988 - 23 Apr 2020
Cited by 9 | Viewed by 2651
Abstract
Energetic binders are a research hot-spot, and much emphasis has been placed on their mechanical properties. In this study, propargyl-terminated ethylene oxide-tetrahydrofuran copolymer (PTPET) was synthesized. Then, PTPET and low-molecular-weight ester-terminated glycidyl azide polymer (GAP) were reacted by the click reaction without using [...] Read more.
Energetic binders are a research hot-spot, and much emphasis has been placed on their mechanical properties. In this study, propargyl-terminated ethylene oxide-tetrahydrofuran copolymer (PTPET) was synthesized. Then, PTPET and low-molecular-weight ester-terminated glycidyl azide polymer (GAP) were reacted by the click reaction without using catalysts to obtain a polyether polytriazole elastomer. Through tensile tests, where R = 0.5, the tensile strength reached 0.332 MPa, with an elongation at break of 897.1%. Swelling tests were used to measure the cross-linked network and showed that the cross-linked network regularity was reduced as R increased. The same conclusions were confirmed by dynamic mechanical analysis (DMA). In DMA curves, Tg was around −70 to −65 °C, and a small amount of crystallization appeared at between −50 and −30 °C, because locally ordered structures were also present in random copolymers, thereby forming localized crystals. Their thermal performance was tested by Differential Scanning Calorimeter (DSC) and Thermal Gravimetric Analyzer (TG), and the main mass loss occurred at around 350 to 450 °C, which meant that they were stable. In conclusion, the polyether polytriazole elastomer can be used as a binder in a composite propellant. Full article
(This article belongs to the Special Issue Advanced Chemistry of Energetic Materials)
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20 pages, 4051 KiB  
Review
Type 2 Diabetes Mellitus: A Review of Multi-Target Drugs
by Angelica Artasensi, Alessandro Pedretti, Giulio Vistoli and Laura Fumagalli
Molecules 2020, 25(8), 1987; https://doi.org/10.3390/molecules25081987 - 23 Apr 2020
Cited by 214 | Viewed by 24315
Abstract
Diabetes Mellitus (DM) is a multi-factorial chronic health condition that affects a large part of population and according to the World Health Organization (WHO) the number of adults living with diabetes is expected to increase. Since type 2 diabetes mellitus (T2DM) is suffered [...] Read more.
Diabetes Mellitus (DM) is a multi-factorial chronic health condition that affects a large part of population and according to the World Health Organization (WHO) the number of adults living with diabetes is expected to increase. Since type 2 diabetes mellitus (T2DM) is suffered by the majority of diabetic patients (around 90–95%) and often the mono-target therapy fails in managing blood glucose levels and the other comorbidities, this review focuses on the potential drugs acting on multi-targets involved in the treatment of this type of diabetes. In particular, the review considers the main systems directly involved in T2DM or involved in diabetes comorbidities. Agonists acting on incretin, glucagon systems, as well as on peroxisome proliferation activated receptors are considered. Inhibitors which target either aldose reductase and tyrosine phosphatase 1B or sodium glucose transporters 1 and 2 are taken into account. Moreover, with a view at the multi-target approaches for T2DM some phytocomplexes are also discussed. Full article
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16 pages, 2023 KiB  
Review
Interactions of Tea-Derived Catechin Gallates with Bacterial Pathogens
by Peter W. Taylor
Molecules 2020, 25(8), 1986; https://doi.org/10.3390/molecules25081986 - 23 Apr 2020
Cited by 14 | Viewed by 3592
Abstract
Green tea-derived galloylated catechins have weak direct antibacterial activity against both Gram-positive and Gram-negative bacterial pathogens and are able to phenotypically transform, at moderate concentrations, methicillin-resistant Staphylococcus aureus (MRSA) clonal pathogens from full β-lactam resistance (minimum inhibitory concentration 256–512 mg/L) to complete susceptibility [...] Read more.
Green tea-derived galloylated catechins have weak direct antibacterial activity against both Gram-positive and Gram-negative bacterial pathogens and are able to phenotypically transform, at moderate concentrations, methicillin-resistant Staphylococcus aureus (MRSA) clonal pathogens from full β-lactam resistance (minimum inhibitory concentration 256–512 mg/L) to complete susceptibility (~1 mg/L). Reversible conversion to susceptibility follows intercalation of these compounds into the bacterial cytoplasmic membrane, eliciting dispersal of the proteins associated with continued cell wall peptidoglycan synthesis in the presence of β-lactam antibiotics. The molecules penetrate deep within the hydrophobic core of the lipid palisade to force a reconfiguration of cytoplasmic membrane architecture. The catechin gallate-induced staphylococcal phenotype is complex, reflecting perturbation of an essential bacterial organelle, and includes prevention and inhibition of biofilm formation, disruption of secretion of virulence-related proteins, dissipation of halotolerance, cell wall thickening and cell aggregation and poor separation of daughter cells during cell division. These features are associated with the reduction of capacity of potential pathogens to cause lethal, difficult-to-treat infections and could, in combination with β-lactam agents that have lost therapeutic efficacy due to the emergence of antibiotic resistance, form the basis of a new approach to the treatment of staphylococcal infections. Full article
(This article belongs to the Special Issue Catechins in Human Health 2020)
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12 pages, 5647 KiB  
Article
N-Acetylation of Amines in Continuous-Flow with Acetonitrile—No Need for Hazardous and Toxic Carboxylic Acid Derivatives
by György Orsy, Ferenc Fülöp and István M. Mándity
Molecules 2020, 25(8), 1985; https://doi.org/10.3390/molecules25081985 - 23 Apr 2020
Cited by 6 | Viewed by 7254
Abstract
A continuous-flow acetylation reaction was developed, applying cheap and safe reagent, acetonitrile as acetylation agent and alumina as catalyst. The method developed utilizes milder reagent than those used conventionally. The reaction was tested on various aromatic and aliphatic amines with good conversion. The [...] Read more.
A continuous-flow acetylation reaction was developed, applying cheap and safe reagent, acetonitrile as acetylation agent and alumina as catalyst. The method developed utilizes milder reagent than those used conventionally. The reaction was tested on various aromatic and aliphatic amines with good conversion. The catalyst showed excellent reusability and a scale-up was also carried out. Furthermore, a drug substance (paracetamol) was also synthesized with good conversion and yield. Full article
(This article belongs to the Special Issue Small Molecules: Structure and Activity - Theme Issue Honoring Prof. Kalevi Pihlaja on His 80th Birthday)
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12 pages, 3074 KiB  
Article
Hematite Nanoparticles from Unexpected Reaction of Ferrihydrite with Concentrated Acids for Biomedical Applications
by Afanasy V. Lunin, Anna A. Lizunova, Elizaveta N. Mochalova, Maria N. Yakovtseva, Vladimir R. Cherkasov, Maxim P. Nikitin and Eugene L. Kolychev
Molecules 2020, 25(8), 1984; https://doi.org/10.3390/molecules25081984 - 23 Apr 2020
Cited by 15 | Viewed by 4325
Abstract
The development of synthetic ways to fabricate nanosized materials with a well-defined shape, narrow-sized distribution, and high stability is of great importance to a rapidly developing area of nanotechnology. Here, we report an unusual reaction between amorphous two-line ferrihydrite and concentrated sulfuric or [...] Read more.
The development of synthetic ways to fabricate nanosized materials with a well-defined shape, narrow-sized distribution, and high stability is of great importance to a rapidly developing area of nanotechnology. Here, we report an unusual reaction between amorphous two-line ferrihydrite and concentrated sulfuric or other mineral and organic acids. Instead of the expected dissolution, we observed the formation of new narrow-distributed brick-red nanoparticles (NPs) of hematite. Different acids produce similar nanoparticles according to scanning (SEM) and transmission electron microscopy (TEM), selected area electron diffraction (SAED), X-ray diffraction (XRD), infrared spectroscopy (FTIR), and energy-dispersive X-ray spectroscopy (EDX). The reaction demonstrates new possibilities for the synthesis of acid-resistant iron oxide nanoparticles and shows a novel pathway for the reaction of iron hydroxide with concentrated acids. The biomedical potential of the fabricated nanoparticles is demonstrated by the functionalization of the particles with polymers, fluorescent labels, and antibodies. Three different applications are demonstrated: i) specific targeting of the red blood cells, e.g., for red blood cell (RBC)-hitchhiking; ii) cancer cell targeting in vitro; iii) infrared ex vivo bioimaging. This novel synthesis route may be useful for the development of iron oxide materials for such specificity-demanding applications such as nanosensors, imaging, and therapy. Full article
(This article belongs to the Special Issue Complex Multifunctional Organic/Inorganic Nanocarriers)
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18 pages, 2454 KiB  
Article
Structure–Activity Relationships and Biological Evaluation of 7-Substituted Harmine Analogs for Human β-Cell Proliferation
by Kunal Kumar, Peng Wang, Ethan A. Swartz, Susmita Khamrui, Cody Secor, Michael B. Lazarus, Roberto Sanchez, Andrew F. Stewart and Robert J. DeVita
Molecules 2020, 25(8), 1983; https://doi.org/10.3390/molecules25081983 - 23 Apr 2020
Cited by 10 | Viewed by 3545
Abstract
Recently, we have shown that harmine induces β-cell proliferation both in vitro and in vivo, mediated via the DYRK1A-NFAT pathway. We explore structure–activity relationships of the 7-position of harmine for both DYRK1A kinase inhibition and β-cell proliferation based on our related previous structure–activity [...] Read more.
Recently, we have shown that harmine induces β-cell proliferation both in vitro and in vivo, mediated via the DYRK1A-NFAT pathway. We explore structure–activity relationships of the 7-position of harmine for both DYRK1A kinase inhibition and β-cell proliferation based on our related previous structure–activity relationship studies of harmine in the context of diabetes and β-cell specific targeting strategies. 33 harmine analogs of the 7-position substituent were synthesized and evaluated for biological activity. Two novel inhibitors were identified which showed DYRK1A inhibition and human β-cell proliferation capability. The DYRK1A inhibitor, compound 1-2b, induced β-cell proliferation half that of harmine at three times higher concentration. From these studies we can draw the inference that 7-position modification is limited for further harmine optimization focused on β-cell proliferation and cell-specific targeting approach for diabetes therapeutics. Full article
(This article belongs to the Section Medicinal Chemistry)
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14 pages, 3605 KiB  
Article
Technetium-Radiolabeled Mannose-Functionalized Gold Nanoparticles as Nanoprobes for Sentinel Lymph Node Detection
by Oscar J. Estudiante-Mariquez, Andrés Rodríguez-Galván, David Ramírez-Hernández, Flavio F. Contreras-Torres and Luis A. Medina
Molecules 2020, 25(8), 1982; https://doi.org/10.3390/molecules25081982 - 23 Apr 2020
Cited by 11 | Viewed by 2930
Abstract
Gold nanoparticles (AuNPs) are considered valuable nanomaterials for the design of radiolabeled nanoprobes for single-photon emission computed tomography (SPECT) imaging. Radiolabeled and functionalized AuNPs could improve lymphatic mapping by enhancing the radioactive signaling of individual particles in the sentinel node. In this study, [...] Read more.
Gold nanoparticles (AuNPs) are considered valuable nanomaterials for the design of radiolabeled nanoprobes for single-photon emission computed tomography (SPECT) imaging. Radiolabeled and functionalized AuNPs could improve lymphatic mapping by enhancing the radioactive signaling of individual particles in the sentinel node. In this study, an alternative method for functionalizing commercial AuNps with mannose is described. The chemical derivatization and biofunctionalization of AuNPs were performed with lipoic acid and mannose, respectively. Several levels of mannose were tested; the thiolate hydrazinonicotinamide-glycine-glycine-cysteine (HYNIC) molecule was also used for 99mTc radiolabeling. Physicochemical characterization of this system includes U-V spectroscopy, dynamic light scattering, Fourier-transform infrared spectroscopy, and transmission electron microscopy. The most stable nanoprobe, in terms of the aggregation, radiolabeling efficiency, and purity, was tested in a sentinel lymph node model in a rat by microSPECT/computed tomography (CT) imaging. The SPECT images revealed that 99mTc-radiolabeled AuNPs functionalized with mannose can track and accumulate in lymph nodes in a similar way to the commercial 99mTc-Sulfur colloid, commonly used in clinical practice for sentinel lymph node detection. These promising results support the idea that 99mTc-AuNPs-mannose could be used as a SPECT contrast agent for lymphatic mapping. Full article
(This article belongs to the Section Materials Chemistry)
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15 pages, 1159 KiB  
Article
Volatilome of Chill-Stored European Seabass (Dicentrarchus labrax) Fillets and Atlantic Salmon (Salmo salar) Slices under Modified Atmosphere Packaging
by Athanasios Kritikos, Ioanna Aska, Sotirios Ekonomou, Athanasios Mallouchos, Foteini F. Parlapani, Serkos A. Haroutounian and Ioannis S. Boziaris
Molecules 2020, 25(8), 1981; https://doi.org/10.3390/molecules25081981 - 23 Apr 2020
Cited by 25 | Viewed by 3820
Abstract
Fish spoilage occurs due to production of metabolites during storage, from bacterial action and chemical reactions, which leads to sensory rejection. Investigating the volatilome profile can reveal the potential spoilage markers. The evolution of volatile organic molecules during storage of European seabass ( [...] Read more.
Fish spoilage occurs due to production of metabolites during storage, from bacterial action and chemical reactions, which leads to sensory rejection. Investigating the volatilome profile can reveal the potential spoilage markers. The evolution of volatile organic molecules during storage of European seabass (Dicentrarchus labrax) fillets and Atlantic salmon (Salmo salar) slices under modified atmosphere packaging at 2 °C was recorded by solid-phase microextraction combined with gas chromatography-mass spectrometry. Total volatile basic nitrogen (TVB-N), microbiological, and sensory changes were also monitored. The shelf life of seabass fillets and salmon slices was 10.5 days. Pseudomonas and H2S-producing bacteria were the dominant microorganisms in both fish. TVB-N increased from the middle of storage, but never reached concentrations higher than the regulatory limit of 30–35 mg N/100 g. The volatilome consisted of a number of aldehydes, ketones, alcohols and esters, common to both fish species. However, different evolution patterns were observed, indicating the effect of fish substrate on microbial growth and eventually the generation of volatiles. The compounds 3-hydroxy-2-butanone, 2,3-butanediol, 2,3-butanedione and acetic acid could be proposed as potential spoilage markers. The identification and quantification of the volatilities of specific fish species via the development of a database with the fingerprint of fish species stored under certain storage conditions can help towards rapid spoilage assessment. Full article
(This article belongs to the Special Issue Food Traceability and Authenticity within Analytical Chemistry)
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17 pages, 7099 KiB  
Article
In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei
by Trong-Nhat Phan, Kyung-Hwa Baek, Nakyung Lee, Soo Young Byun, David Shum and Joo Hwan No
Molecules 2020, 25(8), 1980; https://doi.org/10.3390/molecules25081980 - 23 Apr 2020
Cited by 18 | Viewed by 3423
Abstract
Kinetoplastid parasites, including Leishmania and Trypanosoma spp., are life threatening pathogens with a worldwide distribution. Next-generation therapeutics for treatment are needed as current treatments have limitations, such as toxicity and drug resistance. In this study, we examined the activities of established mammalian target [...] Read more.
Kinetoplastid parasites, including Leishmania and Trypanosoma spp., are life threatening pathogens with a worldwide distribution. Next-generation therapeutics for treatment are needed as current treatments have limitations, such as toxicity and drug resistance. In this study, we examined the activities of established mammalian target of rapamycin (mTOR)/phosphoinositide 3-kinase (PI3K) inhibitors against these tropical diseases. High-throughput screening of a library of 1742 bioactive compounds against intracellular L. donovani was performed, and seven mTOR/PI3K inhibitors were identified. Dose-dilution assays revealed that these inhibitors had half maximal effective concentration (EC50) values ranging from 0.14 to 13.44 μM for L. donovani amastigotes and from 0.00005 to 8.16 μM for T. brucei. The results of a visceral leishmaniasis mouse model indicated that treatment with Torin2, dactolisib, or NVP-BGT226 resulted in reductions of 35%, 53%, and 54%, respectively, in the numbers of liver parasites. In an acute T. brucei mouse model using NVP-BGT226 parasite numbers were reduced to under the limits of detection by five consecutive days of treatment. Multiple sequence and structural alignment results indicated high similarities between mTOR and kinetoplastid TORs; the inhibitors are predicted to bind in a similar manner. Taken together, these results indicated that the TOR pathways of parasites have potential for the discovery of novel targets and new potent inhibitors. Full article
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21 pages, 5037 KiB  
Article
The Rheolaser Master™ and Kinexus Rotational Rheometer® to Evaluate the Influence of Topical Drug Delivery Systems on Rheological Features of Topical Poloxamer Gel
by Maria Chiara Cristiano, Francesca Froiio, Antonia Mancuso, Federica De Gaetano, Cinzia Anna Ventura, Massimo Fresta and Donatella Paolino
Molecules 2020, 25(8), 1979; https://doi.org/10.3390/molecules25081979 - 23 Apr 2020
Cited by 26 | Viewed by 4257
Abstract
Poloxamer 407 copolymer is a versatile and widely used thermo-reversible material. Its use has many advantages, such as bio-adhesion, enhanced solubilization of poorly water-soluble drugs and many applications fields like oral, rectal, topical, nasal drug administration. Hydrogels made up of Poloxamer 407 are [...] Read more.
Poloxamer 407 copolymer is a versatile and widely used thermo-reversible material. Its use has many advantages, such as bio-adhesion, enhanced solubilization of poorly water-soluble drugs and many applications fields like oral, rectal, topical, nasal drug administration. Hydrogels made up of Poloxamer 407 are characterized by specific rheological features, which are affected by temperature, concentration and presence of other compounds. A strategic approach in topical therapeutic treatments may be the inclusion of drug delivery systems, such as ethosomes, transfersomes and niosomes, into hydrogel poloxamer formulation. The evaluation of the interaction between colloidal carriers and the Poloxamer 407 hydrogel network is essential for a suitable design of an innovative topical dosage form. For this reason, the Rheolaser Master™, based on diffusing wave spectroscopy, and a Kinexus Rotational Rheometer were used to evaluate the influence of nanocarriers on the microrheological features of hydrogels. The advantages of the Rheolaser Master™ analyzer are: (i) its ability to determine viscoelastic parameter, without altering or destroying the sample and at rest (zero shear); (ii) possibility of aging analysis on the same sample. This study provide evidence that vesicular systems do not influence the rheological features of the gel, supporting the possibility to encapsulate an innovative system into a three-dimensional network. Full article
(This article belongs to the Special Issue Nanosystems in Pharmaceutical Technology)
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15 pages, 2066 KiB  
Article
In the Mists of a Fungal Metabolite: An Unexpected Reaction of 2,4,5-Trimethoxyphenylglyoxylic Acid
by Immo Serbian, Anne Loesche, Sven Sommerwerk, Phil Liebing, Dieter Ströhl and René Csuk
Molecules 2020, 25(8), 1978; https://doi.org/10.3390/molecules25081978 - 23 Apr 2020
Viewed by 2233
Abstract
The reactions of phenylglyoxylic acids during the synthesis and biological evaluation of fungal metabolites led to the discovery of hitherto unknown compounds with a p-quinone methide (p-QM) structure. The formation of these p-QMs using 13C-labelled starting materials revealed [...] Read more.
The reactions of phenylglyoxylic acids during the synthesis and biological evaluation of fungal metabolites led to the discovery of hitherto unknown compounds with a p-quinone methide (p-QM) structure. The formation of these p-QMs using 13C-labelled starting materials revealed a key-step of this reaction being a retro-Friedel–Crafts alkylation. Full article
(This article belongs to the Special Issue Exclusive Papers of the Editorial Board Members (EBMs) of the Bioorganic Chemistry Section of Molecules)
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15 pages, 271 KiB  
Article
Antimicrobial Testing of Schinus molle (L.) Leaf Extracts and Fractions Followed by GC-MS Investigation of Biological Active Fractions
by Giovanni Turchetti, Stefania Garzoli, Valentina Laghezza Masci, Carla Sabia, Ramona Iseppi, Pierluigi Giacomello, Antonio Tiezzi and Elisa Ovidi
Molecules 2020, 25(8), 1977; https://doi.org/10.3390/molecules25081977 - 23 Apr 2020
Cited by 11 | Viewed by 3047
Abstract
Schinus molle (L.) is a dioecious plant of the Anacardiaceae family, originating in South America and currently widespread in many regions throughout the world. In this work leaf extracts and derived low-pressure column chromatography (LPCC) fractions of S. molle L. male and female [...] Read more.
Schinus molle (L.) is a dioecious plant of the Anacardiaceae family, originating in South America and currently widespread in many regions throughout the world. In this work leaf extracts and derived low-pressure column chromatography (LPCC) fractions of S. molle L. male and female plants were investigated for the antimicrobial activity. Leaf extracts were tested on microbes Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Enterococcus faecalis, Candida albicans and Bacillus subtilis. Furthermore, the extracts showing antimicrobial activity were fractionated by LPCC and the obtained fractions tested on the same microorganism strains. Positive fractions were investigated by gas-chromatography/mass spectrometry (GC-MS) and were seen to be rich in sesquiterpenes, sesquiterpenoids and other terpens. The obtained effects highlighted the antimicrobial properties of S. molle (L.) leaf compounds and revealed their importance as a source of bioactive molecules of potential pharmaceutical interest. To our knowledge, this is the first paper reporting investigations on the chemical composition of the extracts and derived positive fractions from Schinus molle (L.) plants grown in central Italy Full article
(This article belongs to the Collection Qualitative and Quantitative Analysis of Bioactive Natural Products)
23 pages, 4327 KiB  
Article
Tailoring the Properties of Thermo-Compressed Polylactide Films for Food Packaging Applications by Individual and Combined Additions of Lactic Acid Oligomer and Halloysite Nanotubes
by Sandra Rojas-Lema, Luis Quiles-Carrillo, Daniel Garcia-Garcia, Beatriz Melendez-Rodriguez, Rafael Balart and Sergio Torres-Giner
Molecules 2020, 25(8), 1976; https://doi.org/10.3390/molecules25081976 - 23 Apr 2020
Cited by 29 | Viewed by 3623
Abstract
In this work, films of polylactide (PLA) prepared by extrusion and thermo-compression were plasticized with oligomer of lactic acid (OLA) at contents of 5, 10, and 20 wt%. The PLA sample containing 20 wt% of OLA was also reinforced with 3, 6, and [...] Read more.
In this work, films of polylactide (PLA) prepared by extrusion and thermo-compression were plasticized with oligomer of lactic acid (OLA) at contents of 5, 10, and 20 wt%. The PLA sample containing 20 wt% of OLA was also reinforced with 3, 6, and 9 parts per hundred resin (phr) of halloysite nanotubes (HNTs) to increase the mechanical strength and thermal stability of the films. Prior to melt mixing, ultrasound-assisted dispersion of the nanoclays in OLA was carried out at 100 °C to promote the HNTs dispersion in PLA and the resultant films were characterized with the aim to ascertain their potential in food packaging. It was observed that either the individual addition of OLA or combined with 3 phr of HNTs did not significantly affect the optical properties of the PLA films, whereas higher nanoclay contents reduced lightness and induced certain green and blue tonalities. The addition of 20 wt% of OLA increased ductility of the PLA film by nearly 75% and also decreased the glass transition temperature (Tg) by over 18 °C. The incorporation of 3 phr of HNTs into the OLA-containing PLA films delayed thermal degradation by 7 °C and additionally reduced the permeabilities to water and limonene vapors by approximately 8% and 47%, respectively. Interestingly, the highest barrier performance was attained for the unfilled PLA film plasticized with 10 wt% of OLA, which was attributed to a crystallinity increase and an effect of “antiplasticization”. However, loadings of 6 and 9 phr of HNTs resulted in the formation of small aggregates that impaired the performance of the blend films. The here-attained results demonstrates that the properties of ternary systems of PLA/OLA/HNTs can be tuned when the plasticizer and nanofiller contents are carefully chosen and the resultant nanocomposite films can be proposed as a bio-sourced alternative for compostable packaging applications. Full article
(This article belongs to the Special Issue Recent Trends in Active Food Packaging)
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13 pages, 6105 KiB  
Article
Kinetic Studies on Radical Scavenging Activity of Kaempferol Decreased by Sn(II) Binding
by Zhi-Yin Yang, Ling-Ling Qian, Yi Xu, Meng-Ting Song, Chao Liu, Rui-Min Han, Jian-Ping Zhang and Leif H. Skibsted
Molecules 2020, 25(8), 1975; https://doi.org/10.3390/molecules25081975 - 23 Apr 2020
Cited by 9 | Viewed by 2758
Abstract
Sn(II) binds to kaempferol (HKaem, 3,4′,5,7-tetrahydroxy-2-(4-hydroxyphenyl)-4H-1-benzopyran-4-one) at the 3,4-site forming [Sn(II)(Kaem)2] complex in ethanol. DPPH• scavenging efficiency of HKaem is dramatically decreased by SnCl2 coordination due to formation of acid inhibiting deprotonation of HKaem as ligands and [...] Read more.
Sn(II) binds to kaempferol (HKaem, 3,4′,5,7-tetrahydroxy-2-(4-hydroxyphenyl)-4H-1-benzopyran-4-one) at the 3,4-site forming [Sn(II)(Kaem)2] complex in ethanol. DPPH• scavenging efficiency of HKaem is dramatically decreased by SnCl2 coordination due to formation of acid inhibiting deprotonation of HKaem as ligands and thus reduces the radical scavenging activity of the complex via a sequential proton-loss electron transfer (SPLET) mechanism. Moderate decreases in the radical scavenging of HKaem are observed by Sn(CH3COO)2 coordination and by contact between Sn and HKaem, in agreement with the increase in the oxidation potential of the complex compared to HKaem, leading to a decrease in antioxidant efficiency for fruits and vegetables with Sn as package materials. Full article
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