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Natural Bioactive Compounds for Human Health 2.0

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A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: 28 June 2024 | Viewed by 8007

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Special Issue Editors

Prof. Dr. Chun-Tao Che

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Guest Editor

Department of Pharmaceutical Sciences, College of Pharmacy, University of Illinois Chicago, Chicago, IL 60612, USA
Interests: pharmacognosy; natural products; traditional medicine; plant chemistry; dietary supplements; natural drug discovery and development
Special Issues, Collections and Topics in MDPI journals

Prof. Dr. Hongjie Zhang

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Guest Editor

School of Chinese Medicine, Hong Kong Baptist University, Hong Kong 999077, China
Interests: natural products drug discovery from natural resources; development of botanical dietary supplements from herbal medicines, traditional herbal medicines against different disease targets such as cancer; HIV; HCV; bird flu
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The submission of manuscripts is invited for the Special Issue “Natural Bioactive Compounds for Human Health”, which will contain a selection of papers dealing with health-related bioactive substances from plant sources. Original research reports, review articles and commentaries are welcome.

Natural plant products have been used for a long time as medicines to treat a variety of diseases, although recently, the mainstream pharmaceutical market has been dominated by synthetic drugs. However, we have witnessed the advent of a global interest in complementary and alternative medicine, as well as non-synthetic pharmaceutical products. Substances of natural plant origin have attracted the attention of the pharmaceutical community as a viable source offering benefits for disease management and health maintenance. As a result, many biologically active natural plant products (such as flavonoids, terpenoids, phenolics, and alkaloids) have been discovered, many of which are in different stages of development.

This Special Issue aims to cover all aspects of natural bioactive plant products, including, but not limited to, chemical characterization, in vitro and in vivo activities, clinical effects, mechanisms of action, structure–activity relationships, and pharmacokinetic/pharmacodynamic properties. Papers dealing with the product development of natural nutraceuticals and dietary supplements are also welcome.

Prof. Dr. Chun-Tao Che
Prof. Dr. Hongjie Zhang
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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. 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 bioactive plant products
biological and pharmacological activity
natural plant drug discovery and development
nutraceuticals
botanical dietary supplement

Published Papers (6 papers)

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Research

Jump to: Review

29 pages, 9067 KiB

Open AccessArticle

The Antitumoral Effect In Ovo of a New Inclusion Complex from Dimethoxycurcumin with Magnesium and Beta-Cyclodextrin

by Marco A. Obregón-Mendoza, William Meza-Morales, Karla Daniela Rodríguez-Hernández, M. Mirian Estévez-Carmona, Leidys L. Pérez-González, Rosario Tavera-Hernández, María Teresa Ramírez-Apan, David Barrera-Hernández, Mitzi García-Olivares, Brian Monroy-Torres, Antonio Nieto-Camacho, María Isabel Chávez, Rubén Sánchez-Obregón and Raúl G. Enríquez

Int. J. Mol. Sci. 2024, 25(8), 4380; https://doi.org/10.3390/ijms25084380 - 16 Apr 2024

Viewed by 620

Abstract

Breast cancer is one of the leading causes of death in the female population because of the resistance of cancer cells to many anticancer drugs used. Curcumin has cytotoxic activities against breast cancer cells, although it has limited use due to its poor bioavailability and rapid metabolic elimination. The synthesis of metal complexes of curcumin and curcuminoids is a relevant topic in the search for more active and selective derivatives of these molecular scaffolds. However, solubility and bioavailability are concomitant disadvantages of these types of molecules. To overcome such drawbacks, the preparation of inclusion complexes offers a chemical and pharmacologically safe option for improving the aqueous solubility of organic molecules. Herein, we describe the preparation of the inclusion complex of dimethoxycurcumin magnesium complex (DiMeOC-Mg, (4)) with beta-cyclodextrin (DiMeOC-Mg-BCD, (5)) in the stoichiometric relationship 1:1. This new inclusion complex’s solubility in aqueous media phosphate buffer saline (PBS) was improved by a factor of 6x over the free metal complex (4). Furthermore, 5 affects cell metabolic rate, cell morphology, cell migration, induced apoptosis, and downregulation of the matrix metalloproteinase-2 (MMP-2) and matrix metalloproteinase-9 (MMP-9), interleukin-6 (IL-6), and signal transducer and activator of transcription-3 (STAT3) expression levels on MD Anderson metastasis breast-231 cancer (MDA-MB-231) cell lines. Results of an antitumor assay in an in ovo model showed up to 30% inhibition of tumor growth for breast cancer (MDA-MB-231) when using (5) (0.650 mg/kg dose) and 17.29% inhibition with the free homoleptic metal complex (1.5 mg/kg dose, (4)). While the formulation of inclusion complexes from metal complexes of curcuminoids demonstrates its usefulness in improving the solubility and bioavailability of these metallodrugs, the new compound (5) exhibits excellent potential for use as a therapeutic agent in the battle against breast cancer. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds for Human Health 2.0)

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Graphical abstract

8 pages, 2239 KiB

Open AccessCommunication

Guidongnins I–J: Two New 6,7-seco-7,20-Olide-ent-kaurene Diterpenes with Unusual Structures from Isodon rubescens

by Juan Zou, Jianghai Ye, Chenliang Zhao, Jingjie Zhang, Yahua Liu, Lutai Pan, Kang He and Hongjie Zhang

Int. J. Mol. Sci. 2023, 24(17), 13451; https://doi.org/10.3390/ijms241713451 - 30 Aug 2023

Viewed by 821

Abstract

Two undescribed ent-kaurene diterpenes, named guidongnins I (1) and J (2), were isolated from the medicinal plant Isodon rubescens. Compound 1 was determined to contain an unprecedented 23 carbons in the skeleton by bearing an extra isopropyl group at C-17 out of the diterpenoid parent structure, and compound 2 was the first example of 6,7-seco-7,20-olide-ent-kaurenes with two fused-tetrahydrofuran rings formed between C-6 and C-19/C-20 through oxygen bridges. Their structures, including their absolute configurations, were determined using the analyses of the spectroscopic and X-ray diffraction data. Guidongnins I (1) and J (2) were assessed for their anti-cancer activities against the growth of various cancer cell lines, and 2 displayed cytotoxic potency against HepG2 at IC₅₀ 27.14 ± 3.43 μM. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds for Human Health 2.0)

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8 pages, 767 KiB

Open AccessCommunication

Identification and Quantification of the Major Phenolic Constituents in Castanea sativa and Commercial Interspecific Hybrids (C. sativa x C. crenata) Chestnuts Using HPLC–MS/MS

by Aljaz Medic, Petra Kunc, Tilen Zamljen, Metka Hudina, Robert Veberic and Anita Solar

Int. J. Mol. Sci. 2023, 24(17), 13086; https://doi.org/10.3390/ijms241713086 - 23 Aug 2023

Viewed by 673

Abstract

Due to the lack of studies on chestnut metabolites, this study was conducted to identify and quantify the major phenolic constituents in chestnuts. Data were compared with the three most commonly grown interspecific hybrids of C. sativa and C. crenata (‘Bouche de Betizac’, ‘Marsol’, and ‘Maraval’) and three “native” accessions of C. sativa. High-performance liquid chromatography coupled with mass spectrometry was used to identify and quantify these compounds. Four dicarboxylic acid derivatives, five hydroxybenzoic acids, nine hydroxycinnamic acids, and three flavanols were identified and quantified, most of them for the first time. Hydroxybenzoic acids were the major phenolic compounds in all chestnut cultivars/accessions, followed by flavanols, dicarboxylic acid derivatives, and hydroxycinnamic acids. Of all the compounds studied, the (epi)catechin dimer was the most abundant in chestnut. The assumption that cultivars from commercial hybrids have a better and different metabolic profile than “native” accessions was refuted. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds for Human Health 2.0)

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14 pages, 6579 KiB

Open AccessArticle

Berberine Reduces Lipid Accumulation in Obesity via Mediating Transcriptional Function of PPARδ

by Jia-Wen Shou and Pang-Chui Shaw

Int. J. Mol. Sci. 2023, 24(14), 11600; https://doi.org/10.3390/ijms241411600 - 18 Jul 2023

Cited by 2 | Viewed by 1395

Abstract

Obesity is defined as a dampness-heat syndrome in traditional Chinese medicine. Coptidis Rhizoma is an herb used to clear heat and eliminate dampness in obesity and its complications. Berberine (BBR), the main active compound in Coptidis Rhizoma, shows anti-obesity effects. Peroxisome proliferator-activated receptors (PPARs) are a group of nuclear receptor proteins that regulate the expression of genes involved in energy metabolism, lipid metabolism, inflammation, and adipogenesis. However, whether PPARs are involved in the anti-obesity effect of BBR remains unclear. As such, the aim of this study was to elucidate the role of PPARs in BBR treatment on obesity and the underlying molecular mechanisms. Our data showed that BBR produced a dose-dependent regulation of the levels of PPARγ and PPARδ but not PPARα. The results of gene silencing and specific antagonist treatment demonstrated that PPARδ is key to the effect of BBR. In 3T3L1 preadipocytes, BBR reduced lipid accumulation; in high-fat-diet (HFD)-induced obese mice, BBR reduced weight gain and white adipose tissue mass and corrected the disturbed biochemical parameters, including lipid levels and inflammatory and oxidative markers. Both the in vitro and in vivo efficacies of BBR were reversed by the presence of a specific antagonist of PPARδ. The results of a mechanistic study revealed that BBR could activate PPARδ in both 3T3L1 cells and HFD mice, as evidenced by the significant upregulation of PPARδ endogenous downstream genes. After activating by BBR, the transcriptional functions of PPARδ were invoked, exhibiting negative regulation of CCAAT/enhancer-binding protein α (Cebpα) and Pparγ promoters and positive mediation of heme oxygenase-1 (Ho-1) promoter. In summary, this is the first report of a novel anti-obesity mechanism of BBR, which was achieved through the PPARδ-dependent reduction in lipid accumulation. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds for Human Health 2.0)

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17 pages, 1854 KiB

Open AccessArticle

6-Oxofurostane and (iso)Spirostane Types of Saponins in Smilax sieboldii: UHPLC-QToF-MS/MS and GNPS-Molecular Networking Approach for the Rapid Dereplication and Biodistribution of Specialized Metabolites

by Bharathi Avula, Ji-Yeong Bae, Jongmin Ahn, Kumar Katragunta, Yan-Hong Wang, Mei Wang, Yongsoo Kwon, Ikhlas A. Khan and Amar G. Chittiboyina

Int. J. Mol. Sci. 2023, 24(14), 11487; https://doi.org/10.3390/ijms241411487 - 14 Jul 2023

Viewed by 1286

Abstract

Identifying novel phytochemical secondary metabolites following classical pharmacognostic investigations is tedious and often involves repetitive chromatographic efforts. During the past decade, Ultra-High Performance Liquid Chromatography-Quadrupole Time of Flight-Tandem Mass Spectrometry (UHPLC-QToF-MS/MS), in combination with molecular networking, has been successfully demonstrated for the rapid dereplication of novel natural products in complex mixtures. As a logical application of such innovative tools in botanical research, more than 40 unique 3-oxy-, 3, 6-dioxy-, and 3, 6, 27-trioxy-steroidal saponins were identified in aerial parts and rhizomes of botanically verified Smilax sieboldii. Tandem mass diagnostic fragmentation patterns of aglycones, diosgenin, sarsasapogenin/tigogenin, or laxogenin were critical to establishing the unique nodes belonging to six groups of nineteen unknown steroidal saponins identified in S. sieboldii. Mass fragmentation analysis resulted in the identification of 6-hydroxy sapogenins, believed to be key precursors in the biogenesis of characteristic smilaxins and sieboldins, along with other saponins identified within S. sieboldii. These analytes’ relative biodistribution and characteristic molecular networking profiles were established by analyzing the leaf, stem, and root/rhizome of S. sieboldii. Deducing such profiles is anticipated to aid the overall product integrity of botanical dietary supplements while avoiding tedious pharmacognostic investigations and helping identify exogenous components within the finished products. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds for Human Health 2.0)

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Review

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28 pages, 1771 KiB

Open AccessReview

Natural Compounds Targeting the Autophagy Pathway in the Treatment of Colorectal Cancer

by Yin-Xiao Du, Abdullah Al Mamun, Ai-Ping Lyu and Hong-Jie Zhang

Int. J. Mol. Sci. 2023, 24(8), 7310; https://doi.org/10.3390/ijms24087310 - 15 Apr 2023

Cited by 4 | Viewed by 2535

Abstract

Autophagy is a highly conserved intracellular degradation pathway by which misfolded proteins or damaged organelles are delivered in a double-membrane vacuolar vesicle and finally degraded by lysosomes. The risk of colorectal cancer (CRC) is high, and there is growing evidence that autophagy plays a critical role in regulating the initiation and metastasis of CRC; however, whether autophagy promotes or suppresses tumor progression is still controversial. Many natural compounds have been reported to exert anticancer effects or enhance current clinical therapies by modulating autophagy. Here, we discuss recent advancements in the molecular mechanisms of autophagy in regulating CRC. We also highlight the research on natural compounds that are particularly promising autophagy modulators for CRC treatment with clinical evidence. Overall, this review illustrates the importance of autophagy in CRC and provides perspectives for these natural autophagy regulators as new therapeutic candidates for CRC drug development. Full article

(This article belongs to the Special Issue Natural Bioactive Compounds for Human Health 2.0)

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