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Natural Products: Biological and Pharmacological Activity

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

Deadline for manuscript submissions: closed (30 April 2023) | Viewed by 12441

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Prof. Dr. Luisa Tesoriere

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Department of Biological, Chemical and Pharmaceutical Sciences and Technologies, University of Palermo, 90123 Palermo, Italy
Interests: nutraceuticals; bioactivity of natural products; betalain pigments; biochemistry
Special Issues, Collections and Topics in MDPI journals

Dr. Alessandro Attanzio

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Department of Biological, Chemical and Pharmaceutical Sciences and Technologies, University of Palermo, 90123 Palermo, Italy
Interests: biochemistry and methodologies; Sicilian foods; bioactive compounds; phytochemicals; bioactivity; cell cultures; chemoprevention; oxidative stress; apoptosis; eryptosis
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleague,

Dietary phytochemicals are widely investigated in the fields of chemistry, biology, pharmacology and medicine for their potential health-promoting effects. Indeed, many in vitro and in vivo studies provide evidence that a number of these compounds may affect redox-sensitive bio-signaling cell pathways involved in the pathogenesis of chronic disorders such as cancer and cardiovascular diseases, which could finally contribute to their prevention and/or control. On the other hand, numerous data have been collected showing a correlation between the onset of diseases characterized by inflammatory etiology and lower intake of fruit and vegetables, highlighting how natural dietary molecules could play a crucial role in the prevention of chronic degenerative diseases.

In this scenario, extracts from natural products and/or from agri-food waste represent a source of phytochemicals that could act as drugs or be used in combination with them, preventing or modifying metabolic and pathological disorders.

In light of these considerations, discovering the activity of natural molecules at the level of specific pathways is now considered the basis to suggest either preventive dietary strategies or eventually therapeutic interventions. Among these strategies, a healthy lifestyle and the consumption of functional foods have been described as having beneficial effects in the fight against cellular aging and its related disorders.

This Special Issue aims to collect original research and reviews on the biological and pharmacological activity of natural products that act on organ well-being and on the prevention of diseases.

Potential topics include, but are not limited to, the following:

Potential synergistic antitumor, anti-inflammatory and antieryptotic activity in vitro and in vivo;
Regulation of metabolic disorders in vitro and in vivo;
Recovery and enhancement of waste agri-food products.

Prof. Dr. Luisa Tesoriere
Dr. Alessandro Attanzio
Guest Editors

Manuscript Submission Information

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Keywords

antioxidants
phytochemicals
nutraceutical
lifestyle
phytomedicine
medicinal plants
plant extracts
natural drugs
chemoprevention
combotherapy
age-related diseases
metabolism
inflammaging
therapeutic strategies

Published Papers (7 papers)

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Research

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18 pages, 3221 KiB

Open AccessArticle

Characterization and Inhibitory Effects of Essential Oil and Nanoemulsion from Ocotea indecora (Shott) Mez in Aspergillus Species

by Leonardo de Assunção Pinto, Francisco Paiva Machado, Ricardo Esteves, Victor Moebus Farias, Felipe Braz Nielsen Köptcke, Eduardo Ricci-Junior, Leandro Rocha and Luiz Antonio Moura Keller

Molecules 2023, 28(8), 3437; https://doi.org/10.3390/molecules28083437 - 13 Apr 2023

Cited by 2 | Viewed by 1215

Abstract

The Aspergillus genus, the etiological agent of aspergillosis, is an important food contaminant and mycotoxin producer. Plant extracts and essential oils are a source of bioactive substances with antimicrobial potential that can be used instead of synthetic food preservatives. Species from the Lauraceae family and the Ocotea genus have been used as traditional medicinal herbs. Their essential oils can be nanoemulsified to enhance their stability and bioavailability and increase their use. Therefore, this study sought to prepare and characterize both nanoemulsion and essential oil from the Ocotea indecora’s leaves, a native and endemic species from the Mata Atlântica forest in Brazil, and evaluate the activity against Aspergillus flavus RC 2054, Aspergillus parasiticus NRRL 2999, and Aspergillus westerdjikiae NRRL 3174. The products were added to Sabouraud Dextrose Agar at concentrations of 256, 512, 1024, 2048, and 4096 µg/mL. The strains were inoculated and incubated for up to 96 h with two daily measurements. The results did not show fungicidal activity under these conditions. A fungistatic effect, however, was observed. The nanoemulsion decreased the fungistatic concentration of the essential oil more than ten times, mainly in A. westerdjikiae. There were no significant changes in aflatoxin production. Full article

(This article belongs to the Special Issue Natural Products: Biological and Pharmacological Activity)

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20 pages, 7584 KiB

Open AccessArticle

Can Crude Oil Exploration Influence the Phytochemicals and Bioactivity of Medicinal Plants? A Case of Nigerian Vernonia amygdalina and Ocimum gratissimum

by Oluwatofunmilayo A. Diyaolu, Emmanuel T. Oluwabusola, Alfred F. Attah, Eric O. Olori, Adeshola A. Fagbemi, Gagan Preet, Sylvia Soldatou, Jones O. Moody, Marcel Jaspars and Rainer Ebel

Molecules 2022, 27(23), 8372; https://doi.org/10.3390/molecules27238372 - 30 Nov 2022

Viewed by 1447

Abstract

The Nigerian Niger-Delta crude oil exploration often results in spills that affect indigenous medicinal plant biodiversity, likely changing the phytochemical profile of surviving species, their bioactivity or toxicity. In crude oil-rich Kokori and crude oil-free Abraka, classic examples of indigenous plants occupying the medicine-food interface include Vernonia amygdalina (VAL) and Ocimum gratissimum leaves (OGL). These plants are frequently utilised during pregnancy and in anaemia. To date, no scientific investigation has been reported on the potential changes to the phytochemical or bioactivity of the study plants. To discuss the similarities and dissimilarities in antisickling bioactivity and phytochemicals in VAL and OGL collected from Kokori (VAL-KK and OGL-KK) and Abraka (VAL-AB and OGL-AB), in silico, in vitro and comparative UPLC-QTOF-MS analysis was performed. Nine unique compounds were identified in OGL-KK, which have never been reported in the literature, while differences in antisickling potentials were observed in VAL-KK, OGL-KK and, VAL-AB, OGL-AB. Our findings show that VAL-AB and OGL-AB are richer and more diverse in phytochemicals and displayed a slightly higher antisickling activity than VAL-KK and OGL-KK. Ligand-based pharmacophore modelling was performed to understand the potential compounds better; this study may provide a basis for explaining the effect of crude oil spills on secondary metabolites and a reference for further research. Full article

(This article belongs to the Special Issue Natural Products: Biological and Pharmacological Activity)

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22 pages, 5998 KiB

Open AccessArticle

Arteannuin-B and (3-Chlorophenyl)-2-Spiroisoxazoline Derivative Exhibit Anti-Inflammatory Effects in LPS-Activated RAW 264.7 Macrophages and BALB/c Mice-Induced Proinflammatory Responses via Downregulation of NF-κB/P38 MAPK Signaling

by Gifty Sawhney, Javeed Ur Rasool, Diksha Saroch, Mumin Ozturk, Frank Brombacher, Bilal Ahmad, Asha Bhagat, Asif Ali, Suraj P. Parihar and Zabeer Ahmed

Molecules 2022, 27(22), 8068; https://doi.org/10.3390/molecules27228068 - 20 Nov 2022

Cited by 3 | Viewed by 1749

Abstract

Host inflammatory responses are key to protection against injury; however, persistent inflammation is detrimental and contributes to morbidity and mortality. Herein, we demonstrated the anti-inflammatory role of Arteannuin-B (1) and its new spirocyclic-2-isoxazoline derivative JR-9 and their side effects in acute inflammatory condition in vivo using LPS-induced cytokines assay, carrageenan-induced paw edema, acetic acid-induced writhing and tail immersion. The results show that the spirocyclic-2-isoxazoline derivative is a potent anti-inflammatory agent with minimal cell toxicity as compared to Arteannuin-B. In addition, the efficacies of these compounds were also validated by flow cytometric, computational, and histopathological analysis. Our results show that the anti-inflammatory response of JR-9 significantly reduces the ability of mouse macrophages to produce NO, TNF-α, and IL-6 following LPS stimulation. Therefore, JR-9 is a prospective candidate for the development of anti-inflammatory drugs and its molecular mechanism is likely related to the regulation of NF-κB and MAPK signaling pathway. Full article

(This article belongs to the Special Issue Natural Products: Biological and Pharmacological Activity)

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17 pages, 1193 KiB

Open AccessArticle

The Impact of Nitrile-Specifier Proteins on Indolic Carbinol and Nitrile Formation in Homogenates of Arabidopsis thaliana

by Eleanor C. M. Chroston, Annika Hielscher, Matthias Strieker and Ute Wittstock

Molecules 2022, 27(22), 8042; https://doi.org/10.3390/molecules27228042 - 19 Nov 2022

Cited by 1 | Viewed by 1219

Abstract

Glucosinolates, specialized metabolites of the Brassicales including Brassica crops and Arabidopsis thaliana, have attracted considerable interest as chemical defenses and health-promoting compounds. Their biological activities are mostly due to breakdown products formed upon mixing with co-occurring myrosinases and specifier proteins, which can result in multiple products with differing properties, even from a single glucosinolate. Whereas product profiles of aliphatic glucosinolates have frequently been reported, indole glucosinolate breakdown may result in complex mixtures, the analysis of which challenging. The aim of this study was to assess the breakdown of indole glucosinolates in A. thaliana root and rosette homogenates and to test the impact of nitrile-specifier proteins (NSPs) on product profiles. To develop a GC-MS-method for quantification of carbinols and nitriles derived from three prominent indole glucosinolates, we synthesized standards, established derivatization conditions, determined relative response factors and evaluated applicability of the method to plant homogenates. We show that carbinols are more dominant among the detected products in rosette than in root homogenates of wild-type and NSP1- or NSP3-deficient mutants. NSP1 is solely responsible for nitrile formation in rosette homogenates and is the major NSP for indolic nitrile formation in root homogenates, with no contribution from NSP3. These results will contribute to the understanding of the roles of NSPs in plants. Full article

(This article belongs to the Special Issue Natural Products: Biological and Pharmacological Activity)

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16 pages, 2087 KiB

Open AccessArticle

The Phytochemical Profile and Biological Activity of Malva neglecta Wallr. in Surgically Induced Endometriosis Model in Rats

by Esra Küpeli Akkol, Büşra Karpuz, Gizem Türkcanoğlu, Fatma Gül Coşgunçelebi, Hakkı Taştan, Michael Aschner, Anurag Khatkar and Eduardo Sobarzo-Sánchez

Molecules 2022, 27(22), 7869; https://doi.org/10.3390/molecules27227869 - 15 Nov 2022

Cited by 3 | Viewed by 1786

Abstract

Leaves and aerial parts of Malva neglecta Wallr. have been traditionally used in Anatolia for the treatment of pain, inflammation, hemorrhoids, renal stones, constipation, and infertility. This study investigated the effects of M. neglecta leaves in a rat endometriosis model. The dried plant material was extracted with n-hexane, ethyl acetate, and methanol, successively. Experimental endometriosis was surgically induced in six-week-old female, non-pregnant, Wistar albino rats by autotransplant of endometrial tissue to the abdominal wall. After twenty-eight days, rats were evaluated for a second laparotomy. Endometrial foci areas were assessed, and intraabdominal adhesions were scored. Rats were divided into five groups as control, n-hexane, ethyl acetate, methanol, and aqueous extracts, as well as reference. At the end of the treatment, all rats were sacrificed and endometriotic foci areas and intraabdominal adhesions were re-evaluated and compared with the previous findings. Moreover, peritoneal fluid was collected to detect tumor necrosis factor- α (TNF-α), vascular endothelial growth factor (VEGF), and interleukin-6 (IL-6) levels, and cDNA synthesis, and a quantitative real-time polymerase chain reaction (PCR) test was done. The phytochemical content of the most active extract was determined using High-Performance Liquid Chromatography (HPLC). Both endometrial volume and adhesion score decreased significantly in the group treated with methanol extract. In addition, significant decreases were observed in TNF-α, VEGF, and IL-6 levels in animals administered methanol extract. HPLC results showed that the activity caused by the methanol extract of M. neglecta was due to the polyphenols. Taken together, these novel findings indicate that M. neglecta may be a promising alternative for the treatment of endometriosis. Full article

(This article belongs to the Special Issue Natural Products: Biological and Pharmacological Activity)

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16 pages, 5224 KiB

Open AccessArticle

Isobavachalcone Induces Multiple Cell Death in Human Triple-Negative Breast Cancer MDA-MB-231 Cells

by Cheng-Zhu Wu, Mei-Jia Gao, Jie Chen, Xiao-Long Sun, Ke-Yi Zhang, Yi-Qun Dai, Tao Ma, Hong-Mei Li and Yu-Xin Zhang

Molecules 2022, 27(20), 6787; https://doi.org/10.3390/molecules27206787 - 11 Oct 2022

Cited by 5 | Viewed by 1931

Abstract

Standardized treatment guidelines and effective drugs are not available for human triple-negative breast cancer (TNBC). Many efforts have recently been exerted to investigate the efficacy of natural compounds as anticancer agents owing to their low toxicity. However, no study has examined the effects of isobavachalcone (IBC) on the programmed cell death (PCD) of human triple-negative breast MDA-MB-231 cancer cells. In this study, IBC substantially inhibited the proliferation of MDA-MB-231 cells in concentration- and time-dependent manners. In addition, we found that IBC induced multiple cell death processes, such as apoptosis, necroptosis, and autophagy in MDA-MB-231 cells. The initial mechanism of IBC-mediated cell death in MDA-MB-231 cells involves the downregulation of Akt and p-Akt-473, an increase in the Bax/Bcl-2 ratio, and cleaved caspases-3 induced apoptosis; the upregulation of RIP3, p-RIP3 and MLKL induced necroptosis; as well as a simultaneous increase in LC3-II/I ratio induced autophagy. In addition, we observed that IBC induced mitochondrial dysfunction, thereby decreasing cellular ATP levels and increasing reactive oxygen species accumulation to induce PCD. These results suggest that IBC is a promising lead compound with anti-TNBC activity. Full article

(This article belongs to the Special Issue Natural Products: Biological and Pharmacological Activity)

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Review

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28 pages, 2639 KiB

Open AccessReview

Phytochemistry and Biological Activities of Endophytic Fungi from the Meliaceae Family

by Yeni Mulyani, Siska Elisahbet Sinaga and Unang Supratman

Molecules 2023, 28(2), 778; https://doi.org/10.3390/molecules28020778 - 12 Jan 2023

Cited by 5 | Viewed by 2067

Abstract

Meliaceae plants are found worldwide in tropical or subtropical climates. They are important ethnobotanically as sources of traditional medicine, with 575 species and 51 genera. Previous research found that microorganisms are plant pioneers to produce secondary metabolites with diverse compound structures and bioactivities. Several plants of the Meliaceae family contain secondary metabolites isolated from endophytic fungi. Furthermore, related articles from 2002 to 2022 were collected from SciFinder, Google Scholar, and PubMed. About 276 compounds were isolated from endophytic fungi such as terpenoids, polyketides, lactones, pyrones, quinone, anthraquinones, xanthones, coumarines, isocoumarines, resorcylic acid lactones, cytochalasins, aromatics, ester, quinols, alkaloids, nitro compound, fatty acids, and sugars with bioactivities such as antioxidant, antibacterial, antifungal, anti-influenza, neuroprotective activities, anti-HIV, cytotoxic, allelopathic, anti-inflammatory, antifeedant effects, and BSLT toxicity. Meanwhile, secondary metabolites isolated from endophytic fungi were reported as one of the sources of active compounds for medicinal chemistry. This comprehensive review summarizes the ethnobotanical uses and secondary metabolites derived from Meliaceae endophytic fungi. Full article

(This article belongs to the Special Issue Natural Products: Biological and Pharmacological Activity)

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