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Natural Products and Their Derivatives: Synthesis, Structural Modification, and Biological 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 December 2023) | Viewed by 1955

Special Issue Editors

School of Biotechnology and Health Sciences, Wuyi University, Jiangmen City, China
Interests: natural product; synthesis; structural modification; biological activity; mechanism study
School of Pharmacy & State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, China
Interests: pharmaceutical chemistry; synthesis; structural modification; biological activity; natural product
Department of Chemical Biology, Ernest Mario School of Pharmacy, Ruters University, Piscataway, NJ, USA
Interests: natural product; biological activity; mechanism study; inflammation; tumour

Special Issue Information

Dear Colleagues,

In recent years, the research community has witnessed significant advances in the design and synthesis of bioactive molecules, the discovery of novel natural product, total synthesis of natural product, development of synthetic methodology basing on synthesis of bioactive scaffolds. Accordingly, we hope to be able to summarize and display the latest developments in the synthesis strategies of active natural products and analogs, as well as their biological activities through the collection of this album, and provide new methods and template molecules for the subsequent development of innovative drug molecules.

Dr. Xuetao Xu
Prof. Dr. Shao-Hua Wang
Prof. Dr. Xi Zheng
Guest Editors

Manuscript Submission Information

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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

  • chemical biology
  • drug research
  • bioactive molecules
  • natural product
  • total synthesis
  • synthetic methodology
  • synthetic strategy development

Published Papers (2 papers)

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Research

11 pages, 3156 KiB  
Article
Microwave-Promoted Total Synthesis of Puniceloid D for Modulating the Liver X Receptor
by Young Jin Jung, Narges Hosseininasab, Jungjin Park, Soonsil Hyun, Jae-Kyung Jung and Jae-Hwan Kwak
Molecules 2024, 29(2), 416; https://doi.org/10.3390/molecules29020416 - 15 Jan 2024
Viewed by 509
Abstract
A growing global health concern is metabolic syndrome, which is defined by low HDL, diabetes, hypertension, and abdominal obesity. Nuclear receptors are attractive targets for treatment of diseases associated with metabolic syndrome. Liver X receptors (LXRs) have become one of the most significant [...] Read more.
A growing global health concern is metabolic syndrome, which is defined by low HDL, diabetes, hypertension, and abdominal obesity. Nuclear receptors are attractive targets for treatment of diseases associated with metabolic syndrome. Liver X receptors (LXRs) have become one of the most significant pharmacological targets among nuclear receptors. Multiple research studies emphasize the essential function of the liver X receptor (LXR) in the pathophysiology of metabolic syndrome. Puniceloid D, among natural products, demonstrated promising effects on LXRα. However, attempts at the total synthesis of natural products were faced with challenges, including long synthetic steps and low yields, requiring a more efficient approach. In this study, for the first time, we successfully synthesized puniceloid D through a seven-step process and conducted docking studies to gain a comprehensive understanding of the interactions involved in the binding of puniceloid D to LXR within different heterodimeric contexts. Our understanding of the pathophysiology of metabolic syndrome could be improved by these findings, which might assist with the development of novel treatment strategies. Full article
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19 pages, 3451 KiB  
Article
Synthesis, Anti-Tyrosinase Activity, and Spectroscopic Inhibition Mechanism of Cinnamic Acid–Eugenol Esters
by Jianping Li, Xiaofeng Min, Xi Zheng, Shaohua Wang, Xuetao Xu and Jinbao Peng
Molecules 2023, 28(16), 5969; https://doi.org/10.3390/molecules28165969 - 09 Aug 2023
Cited by 3 | Viewed by 1041
Abstract
Tyrosinase plays crucial roles in mediating the production of melanin pigment; thus, its inhibitors could be useful in preventing melanin-related diseases. To find potential tyrosinase inhibitors, a series of cinnamic acid–eugenol esters (c1~c29) was synthesized and their chemical structures [...] Read more.
Tyrosinase plays crucial roles in mediating the production of melanin pigment; thus, its inhibitors could be useful in preventing melanin-related diseases. To find potential tyrosinase inhibitors, a series of cinnamic acid–eugenol esters (c1~c29) was synthesized and their chemical structures were confirmed by 1H NMR, 13C NMR, HRMS, and FT-IR, respectively. The biological evaluation results showed that all compounds c1~c29 exhibited definite tyrosinase inhibitory activity; especially, compound c27 was the strongest tyrosinase inhibitor (IC50: 3.07 ± 0.26 μM), being ~4.6-fold stronger than the positive control, kojic acid (IC50: 14.15 ± 0.46 μM). Inhibition kinetic studies validated compound c27 as a reversible mixed-type inhibitor against tyrosinase. Three-dimensional fluorescence and circular dichroism (CD) spectra results indicated that compound c27 could change the conformation and secondary structure of tyrosinase. Fluorescence-quenching results showed that compound c27 quenched tyrosinase fluorescence in the static manner with one binding site. Molecular docking results also revealed the binding interactions between compound c27 and tyrosinase. Therefore, cinnamic acid–eugenol esters, especially c27, could be used as lead compounds to find potential tyrosinase inhibitors. Full article
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