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Natural Products with Biological and Therapeutic Activity

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

Deadline for manuscript submissions: closed (31 October 2022) | Viewed by 21240

Special Issue Editors


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Guest Editor
Department of Chemical Sciences, University of Catania, Viale A. Doria 6, 95125 Catania, Italy
Interests: organic synthesis; natural product chemistry; NMR spectroscopy; enzyme inhibition; antioxidant activity

E-Mail Website
Guest Editor
Department of Chemical Sciences, University of Catania, Viale A. Doria 6, 95125 Catania, Italy
Interests: mass spectrometry; NMR; chromatographic separation; natural products chemistry; proteomics; food analysis; organic chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Extracts from plants have been used for thousands of years as medicines. Although much is known about the biological properties of natural products, the actual biological target(s) and precise mechanism of action are often unexplored.

Nature offers an astonishing structural variety of compounds, and secondary metabolites such as terpenoids, polyphenols, and alkaloids have a plethora of biological properties, including antioxidant, antimicrobial, anti-inflammatory, antidiabetic, anti-obesity, and antitumor activity. Thus, knowledge around the role of the above-cited metabolites on human health could be employed for new food supplements, over-the-counter medications, or even effective drugs with low side effects.

The issue is dedicated to bioactive natural products extracted from edible and non-edible plants and fruits, and from the waste of agri-food industry processes, with emphasis on novel biological targets and pharmacological studies (both in vitro and in vivo). Works employing innovative and green extraction/isolation methodologies, bioassay guided approaches, and metabolomics methods are much appreciated.

Biological and pharmacological studies involving biopolymers and natural products/natural extracts-based biopolymers are also welcome. Reviews investigating the state of the art related to extracts from “medicinal plants” or to a single class of natural products and their biological and therapeutic activities will be considered.

Dr. Nunzio Cardullo
Dr. Vera Muccilli
Guest Editors

Manuscript Submission Information

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Keywords

  • natural products
  • medicinal plants
  • natural-based extracts
  • bioactive metabolites
  • phytochemical analysis
  • biological assays
  • pharmacological activity
  • metabolomics

Published Papers (8 papers)

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Research

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23 pages, 7413 KiB  
Article
Neuroprotective Effect of Quercetin and Memantine against AlCl3-Induced Neurotoxicity in Albino Wistar Rats
by Ratnakar Jadhav and Yogesh A. Kulkarni
Molecules 2023, 28(1), 417; https://doi.org/10.3390/molecules28010417 - 3 Jan 2023
Cited by 12 | Viewed by 2489
Abstract
Recent evidences indicate that there is a substantial increase in worldwide cases of dementia. Alzheimer’s disease is the leading cause of dementia and may contribute to 60–70% of cases. Quercetin is a unique bioflavonoid that has numerous therapeutic benefits such as anti-allergy, anti-ulcer, [...] Read more.
Recent evidences indicate that there is a substantial increase in worldwide cases of dementia. Alzheimer’s disease is the leading cause of dementia and may contribute to 60–70% of cases. Quercetin is a unique bioflavonoid that has numerous therapeutic benefits such as anti-allergy, anti-ulcer, anti-inflammatory, anti-hypertensive, anti-cancer, immuno-modulatory, anti-infective, antioxidant, acetylcholinesterase inhibitory activity, neuroprotective effects, etc. In the present study, we evaluated the neuroprotective effect of orally administered quercetin with memantine in albino Wistar rats after inducing neurotoxicity through AlCl3 (100 mg/kg, p.o.). Chronic administration of AlCl3 resulted in poor retention of memory and significant oxidative damage. Various behavioral parameters, such as locomotor activity, Morris water maze, elevated plus maze, and passive avoidance test, were assessed on days 21 and 42 of the study. The animals were euthanatized following the completion of the last behavioral assessment. Various oxidative stress parameters were assessed to know the extent of oxidative damage to brain tissue. Quercetin with memantine has shown significant improvement in behavioral studies, inhibition of AChE activity, and reduction in oxidative stress parameters. Histopathological studies assessed for cortex and hippocampus using hematoxylin and eosin (H&E), and Congo red stain demonstrated a reduction in amyloid-β plaque formation after treatment of quercetin with memantine. Immunohistochemistry showed that quercetin with memantine treatment also improved the expression of brain-derived neurotrophic factor (BDNF) and inhibited amyloid-β plaque formation. The present study results demonstrated protective effects of treatment of quercetin with memantine in the neurotoxicity linked to aluminum chloride in albino Wistar rats. Full article
(This article belongs to the Special Issue Natural Products with Biological and Therapeutic Activity)
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17 pages, 1551 KiB  
Article
Phytochemical Analysis and Anti-Cancer Properties of Extracts of Centaurea castriferrei Borbás & Waisb Genus of Centaurea L
by Joanna Kubik, Łukasz Waszak, Grzegorz Adamczuk, Ewelina Humeniuk, Magdalena Iwan, Kamila Adamczuk, Mariola Michalczuk, Agnieszka Korga-Plewko and Aleksandra Józefczyk
Molecules 2022, 27(21), 7537; https://doi.org/10.3390/molecules27217537 - 3 Nov 2022
Cited by 7 | Viewed by 2178
Abstract
The Centaurea L. (Asteraceae) genus includes many plant species with therapeutic properties. Centaurea castriferrei Borbás & Waisb is one of the least known and least described plants of this genus. The aim of the study was the phytochemical analysis of water and methanol–water [...] Read more.
The Centaurea L. (Asteraceae) genus includes many plant species with therapeutic properties. Centaurea castriferrei Borbás & Waisb is one of the least known and least described plants of this genus. The aim of the study was the phytochemical analysis of water and methanol–water extracts (7:3 v/v) obtained from the aerial parts of the plant as well as evaluation of their anticancer activity. Quantitative determinations of phenolic compounds and flavonoids were performed, and the antioxidant potential was measured using the CUPRAC method. The RP-HPLC/DAD analysis and HPLC-ESI-QTOF-MS mass spectroscopy were performed, to determine the extracts’ composition. The antiproliferative activity of the obtained extracts was tested in thirteen cancer cell lines and normal skin fibroblasts using MTT test. Regardless of the extraction method and the extractant used, similar cytotoxicity of the extracts on most cancer cell lines was observed. However, the methanol–water extracts (7:3 v/v) contained significantly more phenolic compounds and flavonoids as well as showing stronger antioxidant properties in comparison to water extracts. Centaurea castriferrei Borbás & Waisb is a rich source of apigenin and its derivatives. In all tested extracts, chlorogenic acid and centaurein were also identified. In vitro research revealed that this plant may be a potential source of compounds with anticancer activity. Full article
(This article belongs to the Special Issue Natural Products with Biological and Therapeutic Activity)
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15 pages, 1748 KiB  
Article
Phytochemical Analysis and Understanding the Antioxidant and Anticancer Properties of Methanol Extract from Litsea glutinosa: In Vitro and In Vivo Studies
by Shafia Shafiq, Ronok Zahan, Samina Yesmin, Alam Khan, Md. Sabbir Mahmud, Md Abu Reza, Sarah M. Albogami, Mohammed Alorabi, Michel De Waard, Hebatallah M. Saad, Jean-Marc Sabatier, Tarannum Naz and Gaber El-Saber Batiha
Molecules 2022, 27(20), 6964; https://doi.org/10.3390/molecules27206964 - 17 Oct 2022
Cited by 6 | Viewed by 2764
Abstract
Litsea glutinosa (L. glutinosa) is considered an evidence-based medicinal plant for the treatment of cancer, the leading cause of death worldwide. In our study, the in vitro antioxidant and in vivo anticancer properties of an essential ethno-medicinal plant, L. glutinosa, [...] Read more.
Litsea glutinosa (L. glutinosa) is considered an evidence-based medicinal plant for the treatment of cancer, the leading cause of death worldwide. In our study, the in vitro antioxidant and in vivo anticancer properties of an essential ethno-medicinal plant, L. glutinosa, were examined using non-toxic doses and a phytochemical analysis was executed using gas-chromatography–mass-spectrometry. The in vitro antioxidant study of the L. glutinosa methanolic extract (LGBME) revealed a concentration-dependent antioxidant property. The bark extract showed promising antioxidant effects in the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) assay. The strongest antioxidant activity was demonstrated at the maximum concentration (50 µg/mL). The IC50 values of the LGBME and BHT were 5.51 and 5.01 µg/mL, respectively. At the same concentration, the total antioxidant capacity of the LGBME was 0.161 µg/mL and the ferric reducing antioxidant power assay result of the LGBME was 1.783 µg/mL. In the cytotoxicity study, the LD50 of the LGBME and gallic acid were 24.93 µg/mL and 7.23 µg/mL, respectively. In the in vivo anticancer-activity studies, the LGBME, particularly at a dose of 150 mg/kg/bw, showed significant cell-growth inhibition, decreased tumor weight, increased mean survival rate, and upregulated the reduced hematological parameters in EAC (Ehrlich’s ascites carcinoma)-induced Swiss albino mice. The highest cell-growth inhibition, 85.76%, was observed with the dose of 150 mg/kg/bw. Furthermore, the upregulation of pro-apoptotic genes (p53, Bax) and the downregulation of anti-apoptotic Bcl-2 were observed. In conclusion, LGBME extract has several bioactive phytoconstituents, which confirms the antioxidant and anticancer properties of L. glutinosa. Full article
(This article belongs to the Special Issue Natural Products with Biological and Therapeutic Activity)
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21 pages, 4615 KiB  
Article
Chemico-Pharmacological Screening of the Methanol Extract of Gynura nepalensis D.C. Deciphered Promising Antioxidant and Hepatoprotective Potentials: Evidenced from in vitro, in vivo, and Computer-Aided Studies
by Nishan Chakrabarty, Hea-Jong Chung, Rashedul Alam, Nazim Uddin Emon, Safaet Alam, Mohammed Fazlul Kabir, Md. Minarul Islam, Seong-Tshool Hong, Tapas Sarkar, Md. Moklesur Rahman Sarker and Mohammad Manjur Rahman
Molecules 2022, 27(11), 3474; https://doi.org/10.3390/molecules27113474 - 27 May 2022
Cited by 8 | Viewed by 2902
Abstract
Gynura nepalensis D.C. (family: Asteraceae) has abundant uses in the alternative medicinal practice, and this species is commonly used in the treatment of diabetes, rheumatism, cuts or wounds, asthma, kidney stones, cough, urinary tract bleeding, gall bladder stones, hepatitis, diarrhea, hemorrhoids, constipation, vomiting, [...] Read more.
Gynura nepalensis D.C. (family: Asteraceae) has abundant uses in the alternative medicinal practice, and this species is commonly used in the treatment of diabetes, rheumatism, cuts or wounds, asthma, kidney stones, cough, urinary tract bleeding, gall bladder stones, hepatitis, diarrhea, hemorrhoids, constipation, vomiting, fertility problems, blood poisoning, septicemia, skin allergy, indigestion, high cholesterol levels, and so on. This study aims to investigate the hepatoprotective and antioxidant potential of the methanol extract of the Gynura nepalensis D.C. (GNME) along with chemical profiling with phytochemical screening. Moreover, prospective phytocompounds have been screened virtually to present the binding affinity of the bioactive components to the hepatic and oxidative receptors. In the hepatoprotective study, alanine transaminase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), total protein (TP), and lipid peroxidation (LP) and total bilirubin (TB) have been assessed, and in the antioxidant study, the DPPH free radical scavenging, total antioxidant flavonoid, and phenolic contents were determined. Moreover, the molecular binding affinity of the bioactive component of the plant has been analyzed using PyRx AutoDock Vina, Chimera, and Discovery Studio software. The plant extract showed dose-dependent hepatoprotective potential (p < 0.05, 0.01, 0.001) as well as strong antioxidant properties. Moreover, hepatoprotective and antioxidant molecular docking studies revealed a result varying from −2.90 kcal/mol to −10.1 kcal/mol. 4,5-dicaffeoylquinic acid and chlorogenic acid revealed the highest binding affinity among the selected molecules. However, the plant showed portent antioxidant and hepatoprotective properties in the in vitro, in vivo, and in silico models, and it is presumed that the hepatoprotective properties of the plant extract have occurred due to the presence of the vast bioactive chemical compounds as well as their antioxidant properties. Therefore, advanced studies are recommended to elucidate the pharmacological properties of the plant extracts. Full article
(This article belongs to the Special Issue Natural Products with Biological and Therapeutic Activity)
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14 pages, 6631 KiB  
Article
Impact of Electrospinning Parameters and Post-Treatment Method on Antibacterial and Antibiofilm Activity of Chitosan Nanofibers
by Viktoriia Korniienko, Yevheniia Husak, Julia Radwan-Pragłowska, Viktoriia Holubnycha, Yevhen Samokhin, Anna Yanovska, Julia Varava, Kateryna Diedkova, Łukasz Janus and Maksym Pogorielov
Molecules 2022, 27(10), 3343; https://doi.org/10.3390/molecules27103343 - 23 May 2022
Cited by 8 | Viewed by 2439
Abstract
Chitosan, a natural biopolymer, is an ideal candidate to prepare biomaterials capable of preventing microbial infections due to its antibacterial properties. Electrospinning is a versatile method ideally suited to process biopolymers with minimal impact on their physicochemical properties. However, fabrication parameters and post-processing [...] Read more.
Chitosan, a natural biopolymer, is an ideal candidate to prepare biomaterials capable of preventing microbial infections due to its antibacterial properties. Electrospinning is a versatile method ideally suited to process biopolymers with minimal impact on their physicochemical properties. However, fabrication parameters and post-processing routine can affect biological activity and, therefore, must be well adjusted. In this study, nanofibrous membranes were prepared using trifluoroacetic acid and dichloromethane and evaluated for physiochemical and antimicrobial properties. The use of such biomaterials as potential antibacterial agents was extensively studied in vitro using Staphylococcus aureus and Escherichia coli as test organisms. The antibacterial assay showed inhibition of bacterial growth and eradication of the planktonic cells of both E. coli and S. aureus in the liquid medium for up to 6 hrs. The quantitative assay showed a significant reduction in bacteria cell viability by nanofibers depending on the method of fabrication. The antibacterial properties of these biomaterials can be attributed to the structural modifications provided by co-solvent formulation and application of post-treatment procedure. Consequently, the proposed antimicrobial surface modification method is a promising technique to prepare biomaterials designed to induce antimicrobial resistance via antiadhesive capability and the biocide-releasing mechanism. Full article
(This article belongs to the Special Issue Natural Products with Biological and Therapeutic Activity)
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17 pages, 1443 KiB  
Article
Spaghetti Enriched with Inulin: Effect of Polymerization Degree on Quality Traits and α-Amylase Inhibition
by Nunzio Cardullo, Vera Muccilli, Vita Di Stefano, Sonia Bonacci, Lucia Sollima and Maria Grazia Melilli
Molecules 2022, 27(8), 2482; https://doi.org/10.3390/molecules27082482 - 12 Apr 2022
Cited by 7 | Viewed by 1956
Abstract
Inulin is considered a dietary fiber and represents a noteworthy ingredient for food biofortification due to its health effects and its neutral taste. The aim of the work was the evaluation of the quality of pasta produced using whole-meal flours of two ancient [...] Read more.
Inulin is considered a dietary fiber and represents a noteworthy ingredient for food biofortification due to its health effects and its neutral taste. The aim of the work was the evaluation of the quality of pasta produced using whole-meal flours of two ancient Sicilian landraces (Senatore Cappelli-CAP and Timilia—TIM) fortified with two types of inulin (long-chain topinambur inulin IT and low-chain chicory inulin IC), at two different levels of substitution (2 and 4%) to evaluate its possible effect on α-amylase inhibition. The color indices L* and a* were mainly influenced by cultivars, while IT improved the sensory attributes, mainly the elasticity sensation, and influenced less the other sensory attributes: adhesiveness, color, odor, taste, and Over Quality Score for both landraces. The cooking quality was linked mainly to the landrace used, due to the very different gluten matrix of CAP and TIM. IC and IT showed promising α-Amy inhibitory activity with comparable IC50 values of 0.45 ± 0.04 and 0.50 ± 0.06 mg/mL. The enrichment of spaghetti with inulin with an inhibitory effect on α-amylase determined the hypoglycemic properties of pasta, thus lowering the corresponding IC50 value. Full article
(This article belongs to the Special Issue Natural Products with Biological and Therapeutic Activity)
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14 pages, 5998 KiB  
Article
Anticancer Activity of Cordia dichotoma against a Panel of Human Cancer Cell Lines and Their Phytochemical Profiling via HPLC and GCMS
by Shilpa Raina, Vikas Sharma, Zahid Nabi Sheikh, Navneet Kour, Shashank K. Singh, Ali Zari, Talal A. Zari, Hesham F. Alharby and Khalid Rehman Hakeem
Molecules 2022, 27(7), 2185; https://doi.org/10.3390/molecules27072185 - 28 Mar 2022
Cited by 9 | Viewed by 2704
Abstract
The current study was conducted to examine the in vitro anticancer potential of Cordia dichotoma (bark, leaves, pulp and seed). The plant material was collected from UT of J&K and methodical bioassays were carried out on ten human cancer cell lines (Michigan Cancer [...] Read more.
The current study was conducted to examine the in vitro anticancer potential of Cordia dichotoma (bark, leaves, pulp and seed). The plant material was collected from UT of J&K and methodical bioassays were carried out on ten human cancer cell lines (Michigan Cancer Foundation-7 (MCF-7), M.D. Anderson-Metastatic Breast (MDA-MB-231), Neuroblastoma-2a (N2A), SH-SY5Y, U-251, HCT-116, SW-620, A-549, MIA PaCa-2, Panc-1) from five different origins (breast, CNS, colon, lung, pancreas) respectively. Methanolic extracts were produced and fractions were then obtained from the extracts and evaluated for cytotoxicity. Mechanistic assays, HPLC, and GCMS profiling were performed on the highest active fraction. The Sulforhodamine B (SRB) assay determined the in vitro cytotoxicity. The findings revealed that the bark portion had in vitro cytotoxicity against the A-549 human lung cancer cell line. To our knowledge, this is the first study to show that the plant’s bark has anticancer properties and induced chromatin condensation, confirmed cell death via ROS generation, and significantly decreased colony formation in A-549 cell line from lung origin in a dose-dependent manner. Furthermore, HPLC and GCMS investigations indicated the presence of a number of bioactive molecules such as gallic acid (144,969.86) uV*sec, caffeic acid (104.26) uV*sec, ferulic acid (472.87) uV*sec, vanillic acid (13,775.39) uV*sec, palmitic acid (18.34%), cis vaccenic acid (28.81%), etc. and one of the compounds was reported for the first time from the bark. As a result of its promising efficacy, it may become an essential cancer chemopreventive or chemotherapeutic medication for patients with lung carcinoma. Full article
(This article belongs to the Special Issue Natural Products with Biological and Therapeutic Activity)
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Review

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16 pages, 986 KiB  
Review
Bioactive Peptides and Proteins from Centipede Venoms
by Yalan Han, Peter Muiruri Kamau, Ren Lai and Lei Luo
Molecules 2022, 27(14), 4423; https://doi.org/10.3390/molecules27144423 - 11 Jul 2022
Cited by 9 | Viewed by 2768
Abstract
Venoms are a complex cocktail of biologically active molecules, including peptides, proteins, polyamide, and enzymes widely produced by venomous organisms. Through long-term evolution, venomous animals have evolved highly specific and diversified peptides and proteins targeting key physiological elements, including the nervous, blood, and [...] Read more.
Venoms are a complex cocktail of biologically active molecules, including peptides, proteins, polyamide, and enzymes widely produced by venomous organisms. Through long-term evolution, venomous animals have evolved highly specific and diversified peptides and proteins targeting key physiological elements, including the nervous, blood, and muscular systems. Centipedes are typical venomous arthropods that rely on their toxins primarily for predation and defense. Although centipede bites are frequently reported, the composition and effect of centipede venoms are far from known. With the development of molecular biology and structural biology, the research on centipede venoms, especially peptides and proteins, has been deepened. Therefore, we summarize partial progress on the exploration of the bioactive peptides and proteins in centipede venoms and their potential value in pharmacological research and new drug development. Full article
(This article belongs to the Special Issue Natural Products with Biological and Therapeutic Activity)
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