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Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology II

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (1 August 2021) | Viewed by 51850

Special Issue Editors


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Guest Editor
Department for the Innovation in Biological, Agrofood and Forestal Systems, Tuscia University, 01100 Viterbo, Italy
Interests: plant compounds; biological activities; cellular biology; microscopy assays
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Department for the Innovation in Biological, Agrofood and Forestal Systems, Università degli Studi della Tuscia Viterbo, Viterbo, Italy
Interests: natural compounds and their characterization and application; mammalian cell cultures
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We are pleased to invite you to submit short communications, research, or review articles to a Special Issue entitled “Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology II”.

Natural compounds are secondary metabolites produced by plants, animals, and microorganisms with defending or adapting purposes. For thousands of years, humans have used these molecules as healing agents and still nowadays natural compounds are an important source in the research of new drugs. Therefore, this Special Issue is focused on the latest findings and advancements on the studies in new drugs covering different aspects such as the isolation, chemical analysis, biological activities and biotechnological applications of extracts or molecules from natural sources. Also, research on semisynthetic modifications of natural compounds is welcome.

Dr. Elisa Ovidi
Prof. Dr. Antonio Tiezzi
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Natural products
  • Drug discovery
  • Chemistry of natural compounds
  • Biology of natural compounds
  • Drug discovery biotechnology

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Published Papers (15 papers)

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Research

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14 pages, 3511 KiB  
Article
Anticancer Activity of Continentalic Acid in B-Cell Lymphoma
by Byeol-Eun Jeon, Chan-Seong Kwon, Ji-Eun Lee, Keumok Moon, Jaeho Cha, Inmyoung Park, Sara Koh, Myunghee Yoon, Sang-Woo Kim and Jeong Nam Kim
Molecules 2021, 26(22), 6845; https://doi.org/10.3390/molecules26226845 - 12 Nov 2021
Cited by 2 | Viewed by 1882
Abstract
Aralia continentalis has been used in Korea as a folk remedy for arthralgia, rheumatism, and inflammation. However, its anti-lymphoma effect remains uncharacterized. Here, we demonstrate that A. continentalis extract and its three diterpenes efficiently kill B-lymphoma cells. Our in vitro and in vivo [...] Read more.
Aralia continentalis has been used in Korea as a folk remedy for arthralgia, rheumatism, and inflammation. However, its anti-lymphoma effect remains uncharacterized. Here, we demonstrate that A. continentalis extract and its three diterpenes efficiently kill B-lymphoma cells. Our in vitro and in vivo results suggest that the cytotoxic activities of continentalic acid, a major diterpene from A. continentalis extract, are specific towards cancer cells while leaving normal murine cells and tissues unharmed. Mechanistically, continentalic acid represses the expression of pro-survival Bcl-2 family members, such as Mcl-1 and Bcl-xL. It dissociates the mitochondrial membrane potential, leading to the stimulation of effector caspase 3/7 activities and, ultimately, cell death. Intriguingly, this agent therapeutically synergizes with roflumilast, a pan-PDE4 inhibitor that has been successfully repurposed for the treatment of aggressive B-cell malignancies in recent clinical tests. Our findings unveiled that A. continentalis extract and three of the plant’s diterpenes exhibit anti-cancer activities. We also demonstrate the synergistic inhibitory effect of continentalic acid on the survival of B-lymphoma cells when combined with roflumilast. Taken in conjunction, continentalic acid may hold significant potential for the treatment of B-cell lymphoma. Full article
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14 pages, 4501 KiB  
Article
Strawberry Juice Powders: Effect of Spray-Drying Conditions on the Microencapsulation of Bioactive Components and Physicochemical Properties
by César Leyva-Porras, María Zenaida Saavedra-Leos, Laura Araceli López-Martinez, Vicente Espinosa-Solis, Yolanda Terán-Figueroa, Alberto Toxqui-Terán and Isaac Compeán-Martínez
Molecules 2021, 26(18), 5466; https://doi.org/10.3390/molecules26185466 - 08 Sep 2021
Cited by 12 | Viewed by 2662
Abstract
The drying of fruit juices has advantages such as easy handling of powders, reduction in volume, and preservation of the characteristics of the fruit. Thus, in this work, the effect of the spray drying conditions of strawberry juice (SJ) with maltodextrin (MX) as [...] Read more.
The drying of fruit juices has advantages such as easy handling of powders, reduction in volume, and preservation of the characteristics of the fruit. Thus, in this work, the effect of the spray drying conditions of strawberry juice (SJ) with maltodextrin (MX) as a carrying agent on the microencapsulation of bioactive compounds and physicochemical properties was studied. The content of phenolic compounds and antioxidant activity showed higher values at low concentrations of MX, while the effect of drying temperature was negligible. The thermal characterization showed that the low molecular weight sugars in the juice decreased the glass transition temperature (Tg). The morphological analysis by scanning electron microscopy (SEM) indicated that at low concentrations of MX, the particles agglomerated, while at intermediate and high concentrations, the particles were observed as well separated. Through microstructural analysis by X-ray diffraction (XRD), the presence of amorphous state was confirmed in all the samples, which is beneficial for preventing chemical and biochemical reactions, and promoting the conservation of the microencapsulated bioactive compounds. Full article
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10 pages, 6142 KiB  
Article
Urease Inhibitory Kinetic Studies of Various Extracts and Pure Compounds from Cinnamomum Genus
by Manoj Kumar, Neha Sikri, Sulekha Chahal, Jitender Sharma, Bhavna Sharma, Poonam Yadav, Monika Bhardwaj, Divya Vashishth, Pooja Kadyan, Sudhir Kumar Kataria and Sunita Dalal
Molecules 2021, 26(13), 3803; https://doi.org/10.3390/molecules26133803 - 22 Jun 2021
Cited by 8 | Viewed by 2254
Abstract
Urease is an enzyme that plays a significant role in the hydrolysis of urea into carbonic acid and ammonia via the carbamic acid formation. The resultant increase in pH leads to the onset of various pathologies such as gastric cancer, urolithiasis, hepatic coma, [...] Read more.
Urease is an enzyme that plays a significant role in the hydrolysis of urea into carbonic acid and ammonia via the carbamic acid formation. The resultant increase in pH leads to the onset of various pathologies such as gastric cancer, urolithiasis, hepatic coma, hepatic encephalopathy, duodenal ulcers and peptic ulcers. Urease inhibitors can reduce the urea hydrolysis rate and development of various diseases. The Cinnamomum genus is used in a large number of traditional medicines. It is well established that stem bark of Cinnamomum cassia exhibits antiulcerogenic potential. The present study evaluated the inhibitory effect of seven extracts of Cinnamomum camphora, Cinnamomum verum and two pure compounds Camphene and Cuminaldehyde on urease enzyme. Kinetic studies of potential inhibitors were carried out. Methanol extract (IC50 980 µg/mL) of C. camphora and a monoterpene Camphene (IC50 0.147 µg/mL) possess significant inhibitory activity. The Lineweaver Burk plot analysis suggested the competitive inhibition by methanol extract, hexane fraction and Camphene. The Gas Chromatography-Mass Spectroscopy (GC–MS) analysis of hexane fraction revealed the contribution of various terpenes. The present study targets terpenes as a new class of inhibitors that have potential therapeutic value for further development as novel drugs. Full article
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10 pages, 2605 KiB  
Article
Observation of Intact and Proteolytically Cleaved Amyloid-Beta (1–40)-Oleuropein Noncovalent Complex at Neutral pH by Mass Spectrometry
by Ioana Cezara Caba, Raluca Ştefănescu and Bogdan Ionel Tamba
Molecules 2021, 26(11), 3261; https://doi.org/10.3390/molecules26113261 - 28 May 2021
Cited by 1 | Viewed by 3071
Abstract
Mass spectrometry analyses carried out on mass spectrometers equipped with soft ionization sources demonstrated their utility in the assessment of the formation of noncovalent complexes and the localization of the binding sites. Direct analyses by mass spectrometry of the noncovalent complex formed in [...] Read more.
Mass spectrometry analyses carried out on mass spectrometers equipped with soft ionization sources demonstrated their utility in the assessment of the formation of noncovalent complexes and the localization of the binding sites. Direct analyses by mass spectrometry of the noncovalent complex formed in acidic and mildly acidic environments by amyloid beta (1–40) peptide and oleuropein have been previously described, and, in several studies, the absorption, metabolism, excretion, and the implications in the prevention and therapy of Alzheimer’s disease of oleuropein have been investigated. Our paper presents modifications of the method previously employed for noncovalent complex observation, namely, the amyloid beta (1–40) pretreatment, followed by an increase in the pH and replacement of the chemical environment from ammonium acetate to ammonium bicarbonate. The formation of noncovalent complexes with one or two molecules of oleuropein was detected in all chemical solutions used, and the amyloid beta (17–28) binding site was identified via proteolytic experiments using trypsin prior to and after noncovalent complex formation. Our results highlight the importance of further studies on the effect of oleuropein against amyloid beta aggregation. Full article
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16 pages, 6440 KiB  
Article
Protective Effects of Thymoquinone, an Active Compound of Nigella sativa, on Rats with Benzo(a)pyrene-Induced Lung Injury through Regulation of Oxidative Stress and Inflammation
by Mohammad A. Alzohairy, Amjad Ali Khan, Mohammed A. Alsahli, Saleh A. Almatroodi and Arshad Husain Rahmani
Molecules 2021, 26(11), 3218; https://doi.org/10.3390/molecules26113218 - 27 May 2021
Cited by 24 | Viewed by 2874
Abstract
Benzopyrene [B(a)P] is a well-recognized environmental carcinogen, which promotes oxidative stress, inflammation, and other metabolic complications. In the current study, the therapeutic effects of thymoquinone (TQ) against B(a)P-induced lung injury in experimental rats were examined. B(a)P used at 50 mg/kg b.w. induced lung [...] Read more.
Benzopyrene [B(a)P] is a well-recognized environmental carcinogen, which promotes oxidative stress, inflammation, and other metabolic complications. In the current study, the therapeutic effects of thymoquinone (TQ) against B(a)P-induced lung injury in experimental rats were examined. B(a)P used at 50 mg/kg b.w. induced lung injury that was investigated via the evaluation of lipid profile, inflammatory markers, nitric oxide (NO), and malondialdehyde (MDA) levels. B(a)P also led to a decrease in superoxide dismutase (SOD) (34.3 vs. 58.5 U/mg protein), glutathione peroxidase (GPx) (42.4 vs. 72.8 U/mg protein), catalase (CAT) (21.2 vs. 30.5 U/mg protein), and total antioxidant capacity compared to normal animals. Treatment with TQ, used at 50 mg/kg b.w., led to a significant reduction in triglycerides (TG) (196.2 vs. 233.7 mg/dL), total cholesterol (TC) (107.2 vs. 129.3 mg/dL), and inflammatory markers and increased the antioxidant enzyme level in comparison with the group that was administered B(a)P only (p < 0.05). B(a)P administration led to the thickening of lung epithelium, increased inflammatory cell infiltration, damaged lung tissue architecture, and led to accumulation of collagen fibres as studied through haematoxylin and eosin (H&E), Sirius red, and Masson’s trichrome staining. Moreover, the recognition of apoptotic nuclei and expression pattern of NF-κB were evaluated through the TUNEL assay and immunohistochemistry, respectively. The histopathological changes were found to be considerably low in the TQ-treated animal group. The TUNEL-positive cells increased significantly in the B(a)P-induced group, whereas the TQ-treated group showed a decreased apoptosis rate. Significantly high cytoplasmic expression of NF-κB in the B(a)P-induced group was seen, and this expression was prominently reduced in the TQ-treated group. Our results suggest that TQ can be used in the protection against benzopyrene-caused lung injury. Full article
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16 pages, 2760 KiB  
Article
Synthesis and Evaluation of Novel 2,2-Dimethylthiochromanones as Anti-Leishmanial Agents
by Seán Coll, Mohammad Alhazmi, Patrícia de Aguiar Amaral, Sandra Bourgeade-Delmas, Anne-Cécile Le Lamer and James W. Barlow
Molecules 2021, 26(8), 2209; https://doi.org/10.3390/molecules26082209 - 12 Apr 2021
Cited by 7 | Viewed by 1957
Abstract
Within this work, we describe the design and synthesis of a range of novel thiochromanones based on natural products reported to possess anti-leishmanial action, and their synthetic derivatives. All compounds were elaborated via the key intermediate 2,2,6-trimethoxythiochromanone, which was modified at the benzylic [...] Read more.
Within this work, we describe the design and synthesis of a range of novel thiochromanones based on natural products reported to possess anti-leishmanial action, and their synthetic derivatives. All compounds were elaborated via the key intermediate 2,2,6-trimethoxythiochromanone, which was modified at the benzylic position to afford various ester, amine and amide analogues, substituted by chains of varying lipophilicity. Upon testing in Leishmania, IC50 values revealed the most potent compounds to be phenylalkenyl and haloalkyl amides 11a and 11e, with IC50 values of 10.5 and 7.2 μM, respectively. Full article
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11 pages, 1287 KiB  
Article
Bioassay-Guided Identification of the Antiproliferative Compounds of Cissus trifoliata and the Transcriptomic Effect of Resveratrol in Prostate Cancer Pc3 Cells
by Luis Fernando Méndez-López, Pierluigi Caboni, Eder Arredondo-Espinoza, Juan J. J. Carrizales-Castillo, Isaías Balderas-Rentería and María del Rayo Camacho-Corona
Molecules 2021, 26(8), 2200; https://doi.org/10.3390/molecules26082200 - 11 Apr 2021
Cited by 3 | Viewed by 2434
Abstract
The bioassay-guided fractionation of a CHCl3-MeOH extract from the stems of Cissus trifoliata identified an active fraction against PC3 prostate cancer cells. The treatment for 24 h showed an 80% reduction in cell viability (p ≤ 0.05) by a WST-1 [...] Read more.
The bioassay-guided fractionation of a CHCl3-MeOH extract from the stems of Cissus trifoliata identified an active fraction against PC3 prostate cancer cells. The treatment for 24 h showed an 80% reduction in cell viability (p ≤ 0.05) by a WST-1 assay at a concentration of 100 μg/mL. The HPLC-QTOF-MS analysis of the fraction showed the presence of coumaric and isoferulic acids, apigenin, kaempferol, chrysoeriol, naringenin, ursolic and betulinic acids, hexadecadienoic and octadecadienoic fatty acids, and the stilbene resveratrol. The exposure of PC3 cells to resveratrol (IC25 = 23 μg/mL) for 24 h induced significant changes in 847 genes (Z-score ≥ ±2). The functional classification tool of the DAVID v6.8 platform indicates that the underlying molecular mechanisms against the proliferation of PC3 cells were associated (p ≤ 0.05) with the process of differentiation and metabolism. These findings provide experimental evidence suggesting the potential of C. trifoliata as a promising natural source of anticancer compounds. Full article
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13 pages, 5473 KiB  
Article
Physicochemical Properties and Antioxidant Activity of Spray-Dry Broccoli (Brassica oleracea var Italica) Stalk and Floret Juice Powders
by María Zenaida Saavedra-Leos, César Leyva-Porras, Alberto Toxqui-Terán and Vicente Espinosa-Solis
Molecules 2021, 26(7), 1973; https://doi.org/10.3390/molecules26071973 - 31 Mar 2021
Cited by 16 | Viewed by 2922
Abstract
This research presents the microencapsulation and conservation of antioxidants of broccoli juice processed by spray drying, and proposes the use of a by-product as a technological application. Broccoli juice (BJ) extracted from two sources, stalks and florets, was spray-dried employing maltodextrin (MX) as [...] Read more.
This research presents the microencapsulation and conservation of antioxidants of broccoli juice processed by spray drying, and proposes the use of a by-product as a technological application. Broccoli juice (BJ) extracted from two sources, stalks and florets, was spray-dried employing maltodextrin (MX) as a carrier agent at concentrations of 5, 7.5, and 10%, and inlet temperatures of 150 and 220 °C. The total phenolic content (TPC), and antioxidant activity (AA) of the BJ-MX powders were determined together with the physicochemical characteristics, including particle morphology, microstructure, and thermal properties. Based on the TPC and AA, the optimal processing conditions found were 5% of MX and a drying temperature of 220 °C. However, the florets showed higher TPC, while stalks presented higher AA under those processing conditions. The particles exhibited micrometric sizes and a mixture of spherical-shape particles and pseudo-spherical particles. The diffractograms indicated an amorphous microstructure in all samples. The glass transition temperature (Tg) was determined in the range of 50 °C for the samples dried at 150 °C and 55 °C for those dried at 220 °C. This suggested that powders might be stored at temperatures below the Tg without presenting any loss of antioxidants. Full article
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15 pages, 1058 KiB  
Article
The Inhibitory Effects of Plant Derivate Polyphenols on the Main Protease of SARS Coronavirus 2 and Their Structure–Activity Relationship
by Thi Thanh Hanh Nguyen, Jong-Hyun Jung, Min-Kyu Kim, Sangyong Lim, Jae-Myoung Choi, Byoungsang Chung, Do-Won Kim and Doman Kim
Molecules 2021, 26(7), 1924; https://doi.org/10.3390/molecules26071924 - 30 Mar 2021
Cited by 43 | Viewed by 4138
Abstract
The main protease (Mpro) is a major protease having an important role in viral replication of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the novel coronavirus that caused the pandemic of 2020. Here, active Mpro was obtained as a [...] Read more.
The main protease (Mpro) is a major protease having an important role in viral replication of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the novel coronavirus that caused the pandemic of 2020. Here, active Mpro was obtained as a 34.5 kDa protein by overexpression in E. coli BL21 (DE3). The optimal pH and temperature of Mpro were 7.5 and 37 °C, respectively. Mpro displayed a Km value of 16 μM with Dabcyl-KTSAVLQ↓SGFRKME-Edans. Black garlic extract and 49 polyphenols were studied for their inhibitory effects on purified Mpro. The IC50 values were 137 μg/mL for black garlic extract and 9–197 μM for 15 polyphenols. The mixtures of tannic acid with puerarin, daidzein, and/or myricetin enhanced the inhibitory effects on Mpro. The structure–activity relationship of these polyphenols revealed that the hydroxyl group in C3′, C4′, C5′ in the B-ring, C3 in the C-ring, C7 in A-ring, the double bond between C2 and C3 in the C-ring, and glycosylation at C8 in the A-ring contributed to inhibitory effects of flavonoids on Mpro. Full article
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20 pages, 4691 KiB  
Article
Optimization of Two Eco-Friendly Extractions of Black Medick (Medicago lupulina L.) Phenols and Their Antioxidant, Cosmeceutical, α-Glucosidase and α-Amylase Inhibitory Properties
by Lejsa Jakupović, Marko Kalvarešin, Karla Bukovina, Valentina Poljak, Lovorka Vujić and Marijana Zovko Končić
Molecules 2021, 26(6), 1610; https://doi.org/10.3390/molecules26061610 - 14 Mar 2021
Cited by 5 | Viewed by 2688
Abstract
Medicago lupulina is an ancient edible plant from the Fabaceae family. In this work, two eco-friendly methods for extraction of bioactive phenolics from M. lupulina were developed using mixtures of water with two non-toxic, skin- and environmentally-friendly polyol solvents: glycerol and polypropylene glycol. [...] Read more.
Medicago lupulina is an ancient edible plant from the Fabaceae family. In this work, two eco-friendly methods for extraction of bioactive phenolics from M. lupulina were developed using mixtures of water with two non-toxic, skin- and environmentally-friendly polyol solvents: glycerol and polypropylene glycol. Ultrasound-assisted extractions were optimized using a Box–Behnken design. The independent variables were the concentration of organic solvent in water (X1), extraction temperature (X2) and time (X3), while the response was phenolic content. The optimum conditions for extraction of polyphenols were (X1, X2, X3): (45%, 70 °C, 60 min) and (10%, 80 °C, 60 min) for glycerol and polypropylene glycol extraction, respectively. The extracts prepared at optimum conditions were rich in phenolic compounds, mainly derivatives of apigenin, kaempferol, luteolin, quercetin, caffeic and ferulic acid, as well as coumestrol. Their cosmeceutical and antidiabetic activity was tested. Both extracts demonstrated notable antioxidant, anti-lipoxygenase and anti-α-amylase activity. In addition to those activities, the glycerol extract efficiently inhibited protein coagulation, elastase and α-glucosidase activity. Glycerol present in the extract displayed enzyme-inhibiting activity in several assays and supported the action of the bioactive constituents. Thus, the optimized glycerol extract is a desirable candidate for direct incorporation in antidiabetic food supplements and cosmeceutical products. Full article
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12 pages, 1558 KiB  
Article
Structure Revision of Isocereulide A, an Isoform of the Food Poisoning Emetic Bacillus cereus Toxin Cereulide
by Veronika Walser, Markus Kranzler, Monika Ehling-Schulz, Timo D. Stark and Thomas F. Hofmann
Molecules 2021, 26(5), 1360; https://doi.org/10.3390/molecules26051360 - 04 Mar 2021
Cited by 5 | Viewed by 2077
Abstract
The emetic Bacillus cereus toxin cereulide presents an enormous safety hazard in the food industry, inducing emesis and nausea after the consumption of contaminated foods. Additional to cereulide itself, seven structurally related isoforms, namely the isocereulides A–G, have already been elucidated in their [...] Read more.
The emetic Bacillus cereus toxin cereulide presents an enormous safety hazard in the food industry, inducing emesis and nausea after the consumption of contaminated foods. Additional to cereulide itself, seven structurally related isoforms, namely the isocereulides A–G, have already been elucidated in their chemical structure and could further be identified in B. cereus contaminated food samples. The newly performed isolation of isocereulide A allowed, for the first time, 1D- and 2D-NMR spectroscopy of a biosynthetically produced isocereulide, revealing results that contradict previous assumptions of an l-O-Leu moiety within its chemical structure. By furthermore applying posthydrolytical dipeptide analysis, amino acid and α-hydroxy acid analysis by means of UPLC-ESI-TOF-MS, as well as MSn sequencing, the structure of previously reported isocereulide A could be corrected. Instead of the l-O-Leu as assumed to date, one l-O-Ile unit could be verified in the cyclic dodecadepsipeptide, revising the structure of isocereulide A to [(d-O-Leu-d-Ala-l-O-Val-l-Val)2(d-O-Leu-d-Ala-l-O-Ile-l-Val)]. Full article
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20 pages, 22449 KiB  
Article
A Contribution to the Solid State Forms of Bis(demethoxy)curcumin: Co-Crystal Screening and Characterization
by Steffi Wünsche, Lina Yuan, Andreas Seidel-Morgenstern and Heike Lorenz
Molecules 2021, 26(3), 720; https://doi.org/10.3390/molecules26030720 - 30 Jan 2021
Cited by 11 | Viewed by 2926
Abstract
Bis(demethoxy)curcumin (BDMC) is one of the main active components found in turmeric. Major drawbacks for its usage are its low aqueous solubility, and the challenging separation from other curcuminoids present in turmeric. Co-crystallization can be applied to alter the physicochemical properties of BDMC [...] Read more.
Bis(demethoxy)curcumin (BDMC) is one of the main active components found in turmeric. Major drawbacks for its usage are its low aqueous solubility, and the challenging separation from other curcuminoids present in turmeric. Co-crystallization can be applied to alter the physicochemical properties of BDMC in a desired manner. A co-crystal screening of BDMC with four hydroxybenzenes was carried out using four different methods of co-crystal production: crystallization from solution by slow solvent evaporation (SSE), and rapid solvent removal (RSR), liquid-assisted grinding (LAG), and crystallization from the melt phase. Two co-crystal phases of BDMC were obtained with pyrogallol (PYR), and hydroxyquinol (HYQ). PYR-BDMC co-crystals can be obtained only from the melt, while HYQ-BDMC co-crystals could also be produced by LAG. Both co-crystals possess an equimolar composition and reveal an incongruent melting behavior. Infrared spectroscopy demonstrated the presence of BDMC in the diketo form in the PYR co-crystals, while it is in a more stable keto-enol form in the HYQ co-crystals. Solubility measurements in ethanol and an ethanol-water mixture revealed an increase of solubility in the latter, but a slightly negative effect on ethanol solubility. These results are useful for a prospective development of crystallization-based separation processes of chemical similar substances through co-crystallization. Full article
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Review

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28 pages, 4928 KiB  
Review
Medicinal Plants, Phytochemicals, and Herbs to Combat Viral Pathogens Including SARS-CoV-2
by Arumugam Vijaya Anand, Balasubramanian Balamuralikrishnan, Mohandass Kaviya, Kathirvel Bharathi, Aluru Parithathvi, Meyyazhagan Arun, Nachiappan Senthilkumar, Shanmugam Velayuthaprabhu, Muthukrishnan Saradhadevi, Naif Abdullah Al-Dhabi, Mariadhas Valan Arasu, Mohammad Iqbal Yatoo, Ruchi Tiwari and Kuldeep Dhama
Molecules 2021, 26(6), 1775; https://doi.org/10.3390/molecules26061775 - 22 Mar 2021
Cited by 69 | Viewed by 11801
Abstract
The coronavirus disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome corona virus-2 (SARS-CoV-2), is the most important health issue, internationally. With no specific and effective antiviral therapy for COVID-19, new or repurposed antiviral are urgently needed. Phytochemicals pose a ray of [...] Read more.
The coronavirus disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome corona virus-2 (SARS-CoV-2), is the most important health issue, internationally. With no specific and effective antiviral therapy for COVID-19, new or repurposed antiviral are urgently needed. Phytochemicals pose a ray of hope for human health during this pandemic, and a great deal of research is concentrated on it. Phytochemicals have been used as antiviral agents against several viruses since they could inhibit several viruses via different mechanisms of direct inhibition either at the viral entry point or the replication stages and via immunomodulation potentials. Recent evidence also suggests that some plants and its components have shown promising antiviral properties against SARS-CoV-2. This review summarizes certain phytochemical agents along with their mode of actions and potential antiviral activities against important viral pathogens. A special focus has been given on medicinal plants and their extracts as well as herbs which have shown promising results to combat SARS-CoV-2 infection and can be useful in treating patients with COVID-19 as alternatives for treatment under phytotherapy approaches during this devastating pandemic situation. Full article
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21 pages, 4214 KiB  
Review
Peppers: A “Hot” Natural Source for Antitumor Compounds
by Micael Rodrigues Cunha, Maurício Temotheo Tavares, Thais Batista Fernandes and Roberto Parise-Filho
Molecules 2021, 26(6), 1521; https://doi.org/10.3390/molecules26061521 - 10 Mar 2021
Cited by 7 | Viewed by 3556
Abstract
Piper, Capsicum, and Pimenta are the main genera of peppers consumed worldwide. The traditional use of peppers by either ancient civilizations or modern societies has raised interest in their biological applications, including cytotoxic and antiproliferative effects. Cellular responses upon treatment with [...] Read more.
Piper, Capsicum, and Pimenta are the main genera of peppers consumed worldwide. The traditional use of peppers by either ancient civilizations or modern societies has raised interest in their biological applications, including cytotoxic and antiproliferative effects. Cellular responses upon treatment with isolated pepper-derived compounds involve mechanisms of cell death, especially through proapoptotic stimuli in tumorigenic cells. In this review, we highlight naturally occurring secondary metabolites of peppers with cytotoxic effects on cancer cell lines. Available mechanisms of cell death, as well as the development of analogues, are also discussed. Full article
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10 pages, 1981 KiB  
Review
Natural Products from the Marine Sponge Subgenus Reniera
by Xuelian Bai, Yang Liu, Hao Wang and Huawei Zhang
Molecules 2021, 26(4), 1097; https://doi.org/10.3390/molecules26041097 - 19 Feb 2021
Cited by 6 | Viewed by 3066
Abstract
Marine sponges are one of the prolific producers of bioactive natural products with therapeutic potential. As an important subgenus of Haliclona, Reniera sponges are mainly distributed in the Mediterranean Sea and Atlantic area, and had been chemically investigated for over four decades. [...] Read more.
Marine sponges are one of the prolific producers of bioactive natural products with therapeutic potential. As an important subgenus of Haliclona, Reniera sponges are mainly distributed in the Mediterranean Sea and Atlantic area, and had been chemically investigated for over four decades. By an extensive literature search, this review first makes a comprehensive summary of all natural products from Reniera sponges and their endozoic microbes, as well as biological properties. Perspectives on strengthening the chemical study of Reniera sponges for new drug-lead discovery are provided in this work. Full article
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