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Natural Products and Synthetic Compounds for Drug Development: 3rd Edition

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: closed (20 April 2025) | Viewed by 1561

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Special Issue Information

Dear Colleagues,

Nature is a rich source of bioactive compounds that have been explored as alternative therapies over the years, exhibiting interesting pharmacological properties and paving the way for the isolation and characterization of biologically active substances, as well as the development of molecular hybrids or small molecules for treating various diseases.

Nature plays a crucial role as a source of drug structures for the development of novel, effective, and safe drugs. Medicinal chemistry develops active compounds through structural simplification, hybridization, or mimicking derivatives to interact with different targets and treat a variety of human diseases. This field of research has demonstrated tremendous practicality, increasing target affinity, and addressing a range of issues affecting candidate drugs.

The theme of this Special Issue is "Natural Products and Synthetic Compounds for Drug Development", and we welcome original articles and broad reviews covering natural products, their derivatives, and synthetic compounds. Topics of interest include oxidative stress-related conditions, reactive oxygen species, oxidative damage, and inflammatory stimulation. Furthermore, we will consider applications to different human diseases, including cancer, infectious diseases, cardiovascular, and neurological diseases. We aim to provide the latest findings on the pharmacological and clinical characteristics of specific molecular compounds, the pharmacology of natural compounds, and the roles of bioactive natural products in human health and disease.

This Special Issue is supervised by Prof. Dr. Guan-Jhong Huang and assisted by our Guest Editor’s Assistant Editor Dr. Xingkang Wu (Modern Research Center for Traditional Chinese Medicine, the Key Laboratory of Chemical Biology and Molecular Engineering of Ministry of Education, Shanxi University).

Prof. Dr. Guan-Jhong Huang
Guest Editor

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Keywords

  • reactive oxygen
  • anti-inflammation
  • cancer
  • infectious diseases
  • liver diseases
  • lung disease
  • kidney disease
  • cardiac disease
  • neuro disease

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Published Papers (2 papers)

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Research

14 pages, 1974 KiB  
Article
9-Hydroxyaristoquinolone: A New Indole Alkaloid Isolated from Aristotelia chilensis with Inhibitory Activity of NF-κB in HMC-3 Microglia Cells
by Rebeca Pérez, Viviana Burgos, Jaime R. Cabrera-Pardo, Leandro Ortiz, Antoni Camins, Miren Ettcheto, Bernd Schmidt, Vaderament-A. Nchiozem-Ngnitedem and Cristian Paz
Int. J. Mol. Sci. 2025, 26(6), 2419; https://doi.org/10.3390/ijms26062419 - 7 Mar 2025
Viewed by 605
Abstract
Neurodegenerative diseases are characterized by a progressive process of degeneration and neuronal death in the nervous system, with neuroinflammation being one of the main factors contributing to the progression of these diseases. Aristotelia chilensis (Maqui) is a native tree of Chile used in [...] Read more.
Neurodegenerative diseases are characterized by a progressive process of degeneration and neuronal death in the nervous system, with neuroinflammation being one of the main factors contributing to the progression of these diseases. Aristotelia chilensis (Maqui) is a native tree of Chile used in the Mapuche folk medicine for wounds and digestive treatment. It produces edible black berries with the highest antioxidant capacity among berries, and the Mapuche people used it for producing an alcoholic beverage. The leaves of Maqui contain indole alkaloids with different pharmacological properties that suggest neuroprotective effects. Here, the isolation and chemical characterization of a new alkaloid, named 9-hydroxyaristoquinolone, and the evaluation of its anti-inflammatory activity in the microglial cell line HMC-3, treated with LPS, are reported. 9-Hydroxyaristoquinolone protects microglia from LPS-induced morphological changes at concentrations as low as 1 µM, with a reduction in IKBα-P levels and inhibition of the NF-κB pathway, which was assessed by THP-1 NF-κB dual cell reporter and Western blot in HMC-3 cells. In silico studies suggest that 9-hydroxyaristoquinolone does not induce hepatotoxicity or genotoxicity and exhibits BBB permeability. Full article
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10 pages, 1174 KiB  
Article
Bisabolane Sesquiterpenes with Anti-Chlamydial Activity Isolated from Ligularia narynensis
by Na Gao, Yi-Lin He, Hui-Ming Qi, Hong-Ying Yang, Guo-Li Li, Zhao-Cai Li and Tong Shen
Int. J. Mol. Sci. 2025, 26(3), 1388; https://doi.org/10.3390/ijms26031388 - 6 Feb 2025
Viewed by 587
Abstract
Chlamydia are obligate intracellular bacterial pathogens affecting humans and animals, causing miscarriage, stillbirth, or weak fetuses in the late stages of pregnancy of goats and sheep. Because there is no commercial vaccine for chlamydia in animals, drug treatment has become the most effective [...] Read more.
Chlamydia are obligate intracellular bacterial pathogens affecting humans and animals, causing miscarriage, stillbirth, or weak fetuses in the late stages of pregnancy of goats and sheep. Because there is no commercial vaccine for chlamydia in animals, drug treatment has become the most effective curative method. Natural products, also known as secondary metabolites, are becoming one of the main sources used in new drug development because of their structural diversity and biodiversity. In natural products, plant sources play a major role in the development process of new drugs. In this study, five undescribed highly oxygenated bisabolane sesquiterpenes (Pararubin W, Pararubin X, Pararubin Y., Pararubin Z, and Pararubin AA) were isolated from whole plants of Ligularia narynensis. Their chemical structures were determined via analyses of HRESIMS, IR, 1D, and 2D NMR data, along with the assignment of their relative configurations. These compounds were tested for their anti-chlamydial activity. The results show that compounds 1 and 5 inhibited the growth of Chlamydia abortus in host cells in a dose-dependent manner. Full article
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