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Probing Pharmacological and Biological Performance of Synthetic and Natural Compounds—2nd Edition

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

Deadline for manuscript submissions: 31 May 2025 | Viewed by 10914

Special Issue Editor

Prof. Dr. Chia-che Chang

E-Mail Website
Guest Editor
Institute of Biomedical Sciences, National Chung Hsing University, Taichung 402204, Taiwan
Interests: anticancer natural products; cancer stem cells; drug resistance
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Compounds from natural sources and their synthetic derivatives have been considered a gold mine in the discovery and development of novel therapeutics for human ailments, including cancer, cardiovascular disorders, and infectious diseases, along with the application of their beneficial effects to promote health, prevent aging, and in cosmetics’ development. An in-depth understanding of the biological activities and of the underlying mechanisms of action is fundamental to translate the pharmacological potentials of natural compounds and their synthetic derivatives to benefit human wellness. Along this line, this Special Issue of Molecules aims to include original articles with novel discoveries and insightful reviews on the pharmacological and biological performance of synthetic and natural compounds, with the hope of enhancing our knowledge of the health-beneficial potentials of these natural materials. 

Prof. Dr. Chia-che Chang
Guest Editor

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 and synthetic compounds
  • aging
  • cancer
  • cardiovascular diseases
  • metabolic syndromes
  • inflammation
  • oxidative stress
  • regulated cell death

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Related Special Issue

Published Papers (5 papers)

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Research

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26 pages, 4780 KiB  
Article
Synthesis, Structural Properties and Biological Activities of Novel Hydrazones of 2-, 3-, 4-Iodobenzoic Acid
by Izabela Czyżewska, Liliana Mazur, Anna Biernasiuk, Anna Hordyjewska and Łukasz Popiołek
Molecules 2024, 29(16), 3814; https://doi.org/10.3390/molecules29163814 - 11 Aug 2024
Viewed by 1933
Abstract
Nowadays, searching for novel antimicrobial agents is crucial due to the increasing number of resistant bacterial strains. Moreover, cancer therapy is a major challenge for modern medicine. Currently used cytostatics have a large number of side effects and insufficient therapeutic effects. Due to [...] Read more.
Nowadays, searching for novel antimicrobial agents is crucial due to the increasing number of resistant bacterial strains. Moreover, cancer therapy is a major challenge for modern medicine. Currently used cytostatics have a large number of side effects and insufficient therapeutic effects. Due to the above-mentioned facts, we undertook research to synthesize novel compounds from the acylhydrazone group aimed at obtaining potential antimicrobial and anticancer agents. As a starting material, we employed hydrazides of 2-, 3- or 4-iodobenzoic acid, which gave three series of acylhydrazones in the condensation reaction with various aldehydes. The chemical structure of all obtained compounds was confirmed by IR, 1H NMR, and 13C NMR. The structure of selected compounds was determined by single-crystal X-ray diffraction analysis. Additionally, all samples were characterized using powder X-ray diffraction. The other issue in this research was to examine the possibility of the solvent-free synthesis of compounds using mechanochemical methods. The biological screening results revealed that some of the newly synthesized compounds indicated a beneficial antimicrobial effect even against MRSA—the methicillin-resistant Staphylococcus aureus ATCC 43300 strain. In many cases, the antibacterial activity of synthesized acylhydrazones was equal to or better than that of commercially available antibacterial agents that were used as reference substances in this research. Significantly, the tested compounds do not show toxicity to normal cell lines either. Full article
(This article belongs to the Special Issue Probing Pharmacological and Biological Performance of Synthetic and Natural Compounds—2nd Edition)
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20 pages, 5306 KiB  
Article
Anticancer Activity and Molecular Mechanisms of Acetylated and Methylated Quercetin in Human Breast Cancer Cells
by Kozue Sakao, Shihomi Hamamoto, Daigo Urakawa, Ziyu He and De-Xing Hou
Molecules 2024, 29(10), 2408; https://doi.org/10.3390/molecules29102408 - 20 May 2024
Cited by 1 | Viewed by 1897
Abstract
Quercetin, a flavonoid polyphenol found in many plants, has garnered significant attention due to its potential cancer chemoprevention. Our previous studies have shown that acetyl modification of the hydroxyl group of quercetin altered its antitumor effects in HepG2 cells. However, the antitumor effect [...] Read more.
Quercetin, a flavonoid polyphenol found in many plants, has garnered significant attention due to its potential cancer chemoprevention. Our previous studies have shown that acetyl modification of the hydroxyl group of quercetin altered its antitumor effects in HepG2 cells. However, the antitumor effect in other cancer cells with different gene mutants remains unknown. In this study, we investigated the antitumor effect of quercetin and its methylated derivative 3,3′,4′,7-O-tetramethylquercetin (4Me-Q) and acetylated derivative 3,3′,4′,7-O-tetraacetylquercetin (4Ac-Q) on two human breast cancer cells, MCF-7 (wt-p53, caspase-3-ve) and MDA-MB-231 (mt-p53, caspase-3+ve). The results demonstrated that 4Ac-Q exhibited significant cell proliferation inhibition and apoptosis induction in both MCF-7 and MDA-MB-231 cells. Conversely, methylation of quercetin was found to lose the activity. The human apoptosis antibody array revealed that 4Ac-Q might induce apoptosis in MCF-7 cells via a p53-dependent pathway, while in MDA-MB-231 cells, it was induced via a caspase-3-dependent pathway. Furthermore, an evaluation using a superoxide inhibitor, MnTBAP, revealed 4Ac-Q-induced apoptosis in MCF-7 cells in a superoxide-independent manner. These findings provide valuable insights into the potential of acetylated quercetin as a new approach in cancer chemoprevention and offer new avenues for health product development. Full article
(This article belongs to the Special Issue Probing Pharmacological and Biological Performance of Synthetic and Natural Compounds—2nd Edition)
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21 pages, 3390 KiB  
Article
Total Content and Composition of Phenolic Compounds from Filipendula Genus Plants and Their Potential Health-Promoting Properties
by Ekaterina Sokolova, Tatiana Krol, Grigorii Adamov, Yulia Minyazeva, Dmitry Baleev and Nikolay Sidelnikov
Molecules 2024, 29(9), 2013; https://doi.org/10.3390/molecules29092013 - 27 Apr 2024
Cited by 3 | Viewed by 1680
Abstract
This current article was dedicated to the determination of the composition of phenolic compounds in extracts of four species of the genus Filipendula in order to establish a connection between the composition of polyphenols and biological effects. A chemical analysis revealed that the [...] Read more.
This current article was dedicated to the determination of the composition of phenolic compounds in extracts of four species of the genus Filipendula in order to establish a connection between the composition of polyphenols and biological effects. A chemical analysis revealed that the composition of the extracts studied depended both on the plant species and its part (leaf or flower) and on the extractant used. All four species of Filipendula were rich sources of phenolic compounds and contained hydrolyzable tannins, condensed tannins, phenolic acids and their derivatives, and flavonoids. The activities included data on those that are most important for creating functional foods with Filipendula plant components: the influence on blood coagulation measured by prothrombin and activated partial thromboplastin time, and on the activity of the digestive enzymes (pancreatic amylase and lipase). It was established that plant species, their parts, and extraction methods contribute meaningfully to biological activity. The most prominent result is as follows: the plant organ determines the selective inhibition of either amylase or lipase; thus, the anticoagulant activities of F. camtschatica and F. stepposa hold promise for health-promoting food formulations associated with general metabolic disorders. Full article
(This article belongs to the Special Issue Probing Pharmacological and Biological Performance of Synthetic and Natural Compounds—2nd Edition)
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15 pages, 2743 KiB  
Article
Neuroprotective Effects of Aldehyde-Reducing Composition in an LPS-Induced Neuroinflammation Model of Parkinson’s Disease
by Sora Kang, Youngjin Noh, Seung Jun Oh, Hye Ji Yoon, Suyeol Im, Hung Taeck Kwon and Youngmi Kim Pak
Molecules 2023, 28(24), 7988; https://doi.org/10.3390/molecules28247988 - 7 Dec 2023
Cited by 2 | Viewed by 2545
Abstract
Parkinson’s disease (PD) is a complex neurodegenerative disease in which neuroinflammation and oxidative stress interact to contribute to pathogenesis. This study investigates the in vivo neuroprotective effects of a patented yeast extract lysate in a lipopolysaccharide (LPS)-induced neuroinflammation model. The yeast extract lysate, [...] Read more.
Parkinson’s disease (PD) is a complex neurodegenerative disease in which neuroinflammation and oxidative stress interact to contribute to pathogenesis. This study investigates the in vivo neuroprotective effects of a patented yeast extract lysate in a lipopolysaccharide (LPS)-induced neuroinflammation model. The yeast extract lysate, named aldehyde-reducing composition (ARC), exhibited potent antioxidant and anti-aldehyde activities in vitro. Oral administration of ARC at 10 or 20 units/kg/day for 3 days prior to intraperitoneal injection of LPS (10 mg/kg) effectively preserved dopaminergic neurons in the substantia nigra (SN) and striatum by preventing LPS-induced cell death. ARC also normalized the activation of microglia and astrocytes in the SN, providing further evidence for its neuroprotective properties. In the liver, ARC downregulated the LPS-induced increase in inflammatory cytokines and reversed the LPS-induced decrease in antioxidant-related genes. These findings indicate that ARC exerts potent antioxidant, anti-aldehyde, and anti-inflammatory effects in vivo, suggesting its potential as a disease-modifying agent for the prevention and treatment of neuroinflammation-related diseases, including Parkinson’s disease. Full article
(This article belongs to the Special Issue Probing Pharmacological and Biological Performance of Synthetic and Natural Compounds—2nd Edition)
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Review

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16 pages, 3206 KiB  
Review
Mechanism of Action of Dihydroquercetin in the Prevention and Therapy of Experimental Liver Injury
by Hewei Wei, Ting Zhao, Xinglong Liu, Qiteng Ding, Junran Yang, Xiaoyu Bi, Zhiqiang Cheng, Chuanbo Ding and Wencong Liu
Molecules 2024, 29(15), 3537; https://doi.org/10.3390/molecules29153537 - 27 Jul 2024
Cited by 3 | Viewed by 2200
Abstract
Liver disease is a global health problem that affects the well-being of tens of thousands of people. Dihydroquercetin (DHQ) is a flavonoid compound derived from various plants. Furthermore, DHQ has shown excellent activity in the prevention and treatment of liver injury, such as [...] Read more.
Liver disease is a global health problem that affects the well-being of tens of thousands of people. Dihydroquercetin (DHQ) is a flavonoid compound derived from various plants. Furthermore, DHQ has shown excellent activity in the prevention and treatment of liver injury, such as the inhibition of hepatocellular carcinoma cell proliferation after administration, the normalization of oxidative indices (like SOD, GSH) in this tissue, and the down-regulation of pro-inflammatory molecules (such as IL-6 and TNF-α). DHQ also exerts its therapeutic effects by affecting molecular pathways such as NF-κB and Nrf2. This paper discusses the latest research progress of DHQ in the treatment of various liver diseases (including viral liver injury, drug liver injury, alcoholic liver injury, non-alcoholic liver injury, fatty liver injury, and immune liver injury). It explores how to optimize the application of DHQ to improve its effectiveness in treating liver diseases, which is valuable for preparing potential therapeutic drugs for human liver diseases in conjunction with DHQ. Full article
(This article belongs to the Special Issue Probing Pharmacological and Biological Performance of Synthetic and Natural Compounds—2nd Edition)
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