Squalene synthase plays an important role in the cholesterol biosynthetic pathway. Inhibiting this enzyme in hypercholesterolemia can lower not only plasma cholesterol but also plasma triglyceride levels. A squalene synthase inhibitor was screened from Prunus mume fruit, and then purified via sequential processes of ethanol extraction, HP-20 column chromatography, ethyl acetate extraction, silica gel column chromatography, and crystallization. The squalene synthase inhibitor was identified as chlorogenic acid with a molecular mass of 354 Da and a molecular formula of C16H18O9 based on UV spectrophotometry, 1H and 13C NMRs, and mass spectrometry. Chlorogenic acid inhibited the squalene synthase of pig liver with an IC50 level of 100 nM. Since chlorogenic acid was an effective inhibitor against the squalene synthase of an animal source, it may be a potential therapeutic agent for hypercholesterolemia.
Download full-text PDF |
Source |
|---|
Publication Analysis
Top Keywords
Similar Publications
Synthetic inhibition of SREBP2 and the mevalonate pathway blocks rhabdomyosarcoma tumor growth in vitro and in vivo and promotes chemosensitization.
Mol Metab
December 2024
Department of Molecular and Translational Medicine, University of Brescia, Brescia, Italy. Electronic address:
Article Synopsis
- The study aimed to explore the effects of targeting the mevalonate pathway (MVP) in rhabdomyosarcoma (RMS), a common soft tissue tumor in young individuals.
- In silico analyses showed that higher levels of MVP-related genes correlated with poorer patient survival, while in vitro tests revealed that MVP inhibitors significantly reduced RMS cell growth, migration, and survival.
- In vivo experiments demonstrated the effectiveness of MVP inhibition in RMS xenografts, highlighting the potential of these inhibitors as a therapeutic strategy against RMS.
Discovery and Functional Identification of 2,3-Oxidosqualene Cyclases and Cytochrome P450s in Triterpenoid Metabolic Pathways of .
J Agric Food Chem
December 2024
Guangdong Engineering Research Center of Biosynthesis and Metabolism of Effective Components of Chinese Medicine, International Institute for Translational Chinese Medicine, School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, P. R. China.
Article Synopsis
- * The study identified key enzyme genes involved in the triterpenoid metabolic pathways using transcriptome sequencing and synthetic biology, particularly focusing on two 2,3-oxidosqualene cyclases and two cytochrome P450s.
- * Researchers successfully reconstructed the biosynthetic pathway for ursane and oleanane-type triterpenoids in a yeast host, detailing the enzymatic reactions necessary for producing important compounds like ursolic acid and oleanolic acid.
Structure-based virtual screening to identify hypocholesterolemic phytochemicals as potent inhibitors of squalene synthase a potential target for hypercholesterolemia.
J Biomol Struct Dyn
December 2024
Laboratory of Biology and Health, Faculty of Sciences Ben M'Sick, Health and Biotechnology Research Centre, Hassan II University of Casablanca, Casablanca, Morocco.
Squalene synthase (SQS) plays a crucial role in the cholesterol biosynthetic pathway. Its distinctive strategic position makes it a promising candidate for targeting and developing new anti-hypercholesterolemic agents. To uncover novel phytochemical scaffolds as potential inhibitors of SQS, we employed a structure-based virtual screening approach that involves screening 545 phytochemicals collected from Moroccan aromatic and medicinal plants and filtering them based on RMSD values and their affinity towards the target enzyme.
View Article and Find Full Text PDFEffects of water stress on secondary metabolism of Panax ginseng fresh roots.
PLoS One
November 2024
Department of Pharmacognosy, Heilongjiang University of Chinese Medicine, Harbin, Heilongjiang, China.
Article Synopsis
- Panax ginseng, a commonly used herbal medicine in Asia, relies on its roots and rhizomes, which contain ginsenosides, the main active compounds that enhance its adaptability to ecological stress.
- A study involved applying water spray to create a short-term water stress scenario for 5-year-old P. ginseng roots, revealing significant increases in oxidative stress indicators and enzyme activities linked to ginsenoside production.
- The water stress treatment resulted in notable boosts in various ginsenosides (e.g., Rg1 and Rb1) and a 40.1% increase in total saponins, highlighting the potential for water management to enhance the medicinal properties of P. ginseng.
Estrogen Enhances Expression in Theca Cells of Chicken Hierarchical Ovarian Follicles by Increasing LSD1Ser54p Level Through GSK3β Phosphorylation at 216th Tyrosine.
Biomolecules
October 2024
College of Animal Science and Technology, Shandong Agricultural University, Tai'an 271017, China.
Article Synopsis
- The study investigates how estrogen influences the development of chicken ovarian follicles by regulating the phosphorylation of specific proteins, particularly lysine demethylase 1A (LSD1) and glycogen synthase kinase 3 beta (GSK3β).
- It was found that estrogen increases the phosphorylation of GSK3β, enhancing its interaction with LSD1, which in turn boosts levels of LSD1Ser54p.
- The research indicates that this process promotes the upregulation of a gene involved in cholesterol biosynthesis, potentially increasing estrogen production in chicken ovarian cells.
Want 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!