The comparative study of effects of 5alpha-cholest-8(14)-en-15-on-3beta-ol (I), (22E)-5alpha-ergosta-8(14),22-dien-15-on-3beta-ol (II), (22S,23S)-22,23-oxido-5alpha-ergost-8(14)-en- 15-on-3beta-ol (III) and (22R,23R)-22,23-oxido-5alpha-ergost-8(14)-en-15-on-3beta-ol (IV) on HMG-CoA reductase, CYP27A1 and CYP3A4 genes expression in Hep G2 cells was performed. In the contrast to 15-ketocholestane derivative (I), 15-ketoergostane derivatives (II - IV) decreased the HMG- CoA reductase mRNA level; (22R,23R)-22,23-oxido-5alpha-ergost-8(14)-en-15-on-3beta-ol (IV) significantly increased CYP3A4 mRNA level (320% from control). Ketosterol (II) was found to be a more potent inhibitor of cholesterol biosynthesis in Hep G2 cells at a prolong incubation, compared with ketosterol (I). The side chain conformation of compounds (I) - (IV) was evaluated by computational modeling; the correlation between biological activity of these compounds and conformational flexibility of their side chains was found. The results obtained indicated that delta8(14)-15-ketoergostane derivatives may be used as a sterol biosynthesis and metabolism regulators in liver cells.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.18097/pbmc20105605576 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Sakuranetin Prevents Acetaminophen-Induced Liver Injury via Nrf2-Induced Inhibition of Hepatocyte Ferroptosis.
Drug Des Devel Ther
January 2025
Department of Hepatobiliary Surgery, Jingzhou Hospital Affiliated to Yangtze University, Jingzhou, Hubei, People's Republic of China.
Introduction: Oxidative stress is an important cause of acetaminophen (APAP)-induced liver injury (AILI). Sakuranetin (Sak) is an antitoxin from the cherry flavonoid plant with good antioxidant effects. However, whether sakuranetine has a protective effect on APAP-induced liver injury is not clear.
View Article and Find Full Text PDFVirtual screening and evaluation of bioactive peptides from as potential HMGCR inhibitors for hyperlipidemia treatment.
Front Nutr
December 2024
Key Laboratory of Cultivation and High-Value Utilization of Marine Organisms in Fujian Province, Fisheries Research Institute of Fujian, Xiamen, China.
Introduction: Hyperlipidemia remains a major disease threatening global public health. The morbidity and mortality associated with cardiovascular diseases have been increasing. The inhibition of 3-Hydroxy-3-methylglutaryl-coenzyme A reductase (HMGCR), a key enzyme in the cholesterol synthesis pathway, can effectively reduce cholesterol levels.
View Article and Find Full Text PDFRegulatory role of lnc-MAP3K13-3:1 on miR-6894-3p and SHROOM2 in modulating cellular dynamics in hepatocellular carcinoma.
BMC Cancer
January 2025
Jiangxi Provincial Key Laboratory of Child Development and Genetics, Jiangxi Provincial Children's Hospital, No. 122 of YangMing Road, DongHu District, NanChang, 330006, China.
Background: Hepatocellular carcinoma (HCC) is a prevalent primary liver malignancy and a leading cause of cancer-related mortality worldwide. Despite advancements in therapeutic strategies, the 5-year survival rate for individuals undergoing curative resection remains between 10% and 15%. Consequently, identifying molecular targets that specifically inhibit the proliferation and metastasis of HCC cells is critical for improving treatment outcomes.
View Article and Find Full Text PDFA novel cobalt oxide nanoparticle conjugated with ellagic acid arrests the cell cycle in human liver cancer cell line.
Sci Rep
January 2025
Department of Biology, Rasht Branch, Islamic Azad University, Rasht, Iran.
The current chemotherapy treatments for liver cancer have shown limited effectiveness. Therefore, there is an urgent need to develop new drugs to combat this disease more effectively. This study reports synthesis of cobalt oxide nanoparticles coated with glucose, and conjugated with Ellagic acid.
View Article and Find Full Text PDF[Berberine regulates glucose and lipid metabolism via clock-controlled genes to ameliorate insulin resistance of hepatocytes].
Zhongguo Zhong Yao Za Zhi
December 2024
Jiangxi Province Key Laboratory of Traditional Chinese Medicine Etiopathogenisis & Research Center for Differentiation and Development of Traditional Chinese Medicine Basic Theory, Jiangxi University of Chinese Medicine Nanchang 330004,China.
This study aims to investigate the mechanism of berberine in regulating the metabolism network via clock-controlled genes represented by brain and muscle arnt-like 1(BMAL1) to ameliorate insulin resistance(IR) of hepatocytes in vitro. The HepG2 cell model of dexamethasone-induced IR(IR-HepG2) was established and treated with 5, 10, and 20 μmol·L~(-1) berberine, respectively, for 24 h. The glucose oxidase method and cell counting kit-8(CCK-8) assay were employed to measure extracellular glucose concentration and cell viability, respectively.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!