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Role of Natural Compounds in Human Health and Disease

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

Deadline for manuscript submissions: 26 December 2024 | Viewed by 1512

Special Issue Editors


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Guest Editor
Department of Biochemistry, Kosin University College of Medicine, Busan 49267, Republic of Korea
Interests: natural product

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Guest Editor
Natural Product Research Center, Korea Institute of Science & Technology, Gangneung 25451, Republic of Korea
Interests: natural product

Special Issue Information

Dear Colleagues,

Natural Compounds have been used for a long time in traditional medicine to treat different illnesses. Recently, there has been more interest in these natural compounds because they might have health benefits and fewer side effects compared to synthetic drugs. Their antioxidant, anti-inflammatory, antimicrobial, and immunomodulatory properties offer a wide range of therapeutic applications, including anti-cancer, anti-cardiovascular disease, anti-neurodegenerative diseases, and anti-metabolic disorders. For example, curcumin has been extensively studied for its ability to inhibit tumor growth and metastasis. Omega-3 fatty acids from fish oil, flavonoids from dark chocolate, and polyphenols from red wine have been shown to improve heart health by reducing blood pressure, improving lipid profiles, and enhancing endothelial function. Ginkgo biloba is believed to improve cognitive function and slow the progression of neurodegenerative diseases due to its antioxidant and anti-inflammatory properties. Berberine, found in several plants, has been shown to regulate glucose and lipid metabolism, making it a potential treatment for type 2 diabetes.

This special issue explores the role of natural compounds in promoting human health and fighting diseases, highlighting their mechanisms of action, therapeutic potential, and the challenges associated with their use.

Importantly, the exact active ingredient of natural origin extract must be reported in the submitted research manuscript, since papers describing the effects of mixed extraction from natural origin are not in the scope of the journal.

Dr. Jaewon Shim
Dr. Wook-bin Lee
Guest Editors

Manuscript Submission Information

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Keywords

  • natural compound
  • therapeutic applications
  • action mechanisms of natural compounds
  • traditional medicine

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Published Papers (2 papers)

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Research

13 pages, 1876 KiB  
Article
Development and Evaluation of ABI-171, a New Fluoro-Catechin Derivative, for the Treatment of Idiopathic Pulmonary Fibrosis
by Gian Luca Araldi, Yu-Wen Hwang and Ganesh Raghu
Int. J. Mol. Sci. 2024, 25(21), 11827; https://doi.org/10.3390/ijms252111827 - 4 Nov 2024
Viewed by 560
Abstract
The persistent challenge of idiopathic pulmonary fibrosis (IPF), characterized by disease progression and high mortality, underscores the urgent need for innovative therapeutic strategies. We have developed a novel small molecule—catechin derivative ABI-171—selectively targeting dual-specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) and proviral integration site for [...] Read more.
The persistent challenge of idiopathic pulmonary fibrosis (IPF), characterized by disease progression and high mortality, underscores the urgent need for innovative therapeutic strategies. We have developed a novel small molecule—catechin derivative ABI-171—selectively targeting dual-specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) and proviral integration site for Moloney murine leukemia virus 1 (PIM1) kinases, crucial in the pathogenesis of fibrotic processes. We employed the Bleomycin-induced (intratracheal) mouse model of pulmonary fibrosis (PF) to evaluate the therapeutic efficacy of ABI-171. Mice with induced PF were treated QD with ABI-171, either prophylactically or therapeutically, using oral and intranasal routes. Pirfenidone (100 mg/kg, TID) and Epigallocatechin gallate (EGCG, 100 mg/kg, QD), a natural catechin currently in a Phase 1 clinical trial, were used as reference compounds. ABI-171, administered prophylactically, led to a significant reduction in hydroxyproline levels and fibrotic tissue formation compared to the control group. Treatment with ABI-171 improved body weight, indicating mitigation of disease-related weight loss. Additionally, ABI-171 demonstrated anti-inflammatory activity, reducing lymphocyte and neutrophil infiltration. In the therapeutic setting, ABI-171, administered 7 days post-induction, reduced mortality rates (p = 0.04) compared with the bleomycin and EGCG control groups. ABI-171 also ameliorated the severity of lung injuries assessed by improved Masson’s trichrome scores when administered both orally and intranasally. ABI-171 significantly decreases bleomycin-induced PF and improves survival in mice, showcasing promising therapeutic potential beyond current medications like pirfenidone and EGCG for patients with IPF. Based on these results, further studies with ABI-171 are ongoing in preclinical studies. Full article
(This article belongs to the Special Issue Role of Natural Compounds in Human Health and Disease)
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14 pages, 2454 KiB  
Article
Vitex agnus castus Extract Ze 440: Diterpene and Triterpene’s Interactions with Dopamine D2 Receptor
by Jakob K. Reinhardt, Lukas Schertler, Hendrik Bussmann, Manuel Sellner, Martin Smiesko, Georg Boonen, Olivier Potterat, Matthias Hamburger and Veronika Butterweck
Int. J. Mol. Sci. 2024, 25(21), 11456; https://doi.org/10.3390/ijms252111456 - 25 Oct 2024
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Abstract
Pre-clinical studies suggest that extracts prepared from the fruits of Vitex agnus castus (VAC) interact with dopamine D2 receptors, leading to reduced prolactin secretion. In previous experiments, dopaminergic activity was mostly evaluated using radioligand binding assays or via the inhibition of prolactin release [...] Read more.
Pre-clinical studies suggest that extracts prepared from the fruits of Vitex agnus castus (VAC) interact with dopamine D2 receptors, leading to reduced prolactin secretion. In previous experiments, dopaminergic activity was mostly evaluated using radioligand binding assays or via the inhibition of prolactin release from rat pituitary cells. Diterpenes featuring a clerodadienol scaffold were identified as major active compounds, but no conclusive data regarding their potency and intrinsic activity are available. Utilising advances in chromatography, we re-examined this topic using HPLC-based tracking of bioactivity via microfractionation of the VAC extract Ze 440. Using a cAMP-based assay, we measured dopaminergic activity in CHO-K1 cells that overexpress the human D2 receptor. Six diterpenes were isolated from two active HPLC microfractions. Viteagnusin I emerged as the most potent diterpene (EC50: 6.6 µM), followed by rotundifuran (EC50: 12.8 µM), whereas vitexilactone was inactive (EC50: >50 µM). Interestingly, triterpenes were also identified as active, with 3-epi-maslinic acid being the most active compound (EC50: 5.1 µM). To better understand these interactions at the molecular level, selected diterpenes and triterpenes were analysed through molecular docking against D2 receptor structures. Our data show that the dopaminergic activity of VAC diterpenes seems to depend on the configuration and on ring substitution in the side chain. This study also highlights for the first time the dopaminergic contribution of triterpenes such as 3-epi-maslinic acid. Full article
(This article belongs to the Special Issue Role of Natural Compounds in Human Health and Disease)
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