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Your search keyword '"Zhongyong Zheng"' showing total 2 results
Start Over Author "Zhongyong Zheng" Topic 0104 chemical sciences
2 results on '"Zhongyong Zheng"'

1. A concise total synthesis and PPAR activation activity of hericerin from Hericium erinaceum

Author

Kai Wang, Baosong Chen, Zhongyong Zheng, Hongwei Liu, Li Bao, Zhengdi Wang, Liping Xie, and Changbin Guo

Subjects
0301 basic medicine, Hericium, Lactams, Stereochemistry, Peroxisome Proliferator-Activated Receptors, 030106 microbiology, Peroxisome proliferator-activated receptor, 01 natural sciences, Pparγ agonist, 03 medical and health sciences, chemistry.chemical_compound, Medicinal mushroom, Bromide, Cell Line, Tumor, Drug Discovery, Humans, Pharmacology, chemistry.chemical_classification, 010405 organic chemistry, Hericium erinaceum, Alkaloid, Total synthesis, Hep G2 Cells, 0104 chemical sciences, chemistry, Hepg2 cells, Agaricales, Transcriptome
Abstract

Hericerin is an isoindolinone meroterpenoid alkaloid isolated from medicinal mushroom Hericium erinaceum with some bioactivities. Herein, a concise total synthesis of hericerin was described, with four steps and 30% overall yield starting from commercially available methyl 3-hydroxy-5-methoxybenzoate and geranyl bromide. A comprehensive effect of hericerin on HepG2 cell line was observed and confirmed by transcriptomic analysis. Furthermore, hericerin was found to be a new PPARγ agonist.

Published
2020
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2. Structural Modification of Natural Product Ganomycin I Leading to Discovery of a α-Glucosidase and HMG-CoA Reductase Dual Inhibitor Improving Obesity and Metabolic Dysfunction in Vivo

Author

Hongwei Liu, Jinjin Zhang, Shuang-Jiang Liu, Nan Zhou, Zhongyong Zheng, Li Bao, Kai Wang, Chang Liu, Lifeng Wang, Mingfang Liao, Jun Wang, Yu-Jing Wang, and Wenzhao Wang

Subjects
0301 basic medicine, Male, Swine, Reductase, Pharmacology, Gut flora, 01 natural sciences, Rats, Sprague-Dawley, 03 medical and health sciences, chemistry.chemical_compound, Lactones, Insulin resistance, Drug Stability, In vivo, Drug Discovery, medicine, Animals, Glycoside Hydrolase Inhibitors, Obesity, Meroterpene, Metabolic Syndrome, biology, 010405 organic chemistry, Chemistry, Terpenes, alpha-Glucosidases, medicine.disease, biology.organism_classification, 0104 chemical sciences, Gastrointestinal Microbiome, Fatty Liver, Mice, Inbred C57BL, 030104 developmental biology, HMG-CoA reductase, biology.protein, Microsomes, Liver, Molecular Medicine, Female, Hydroxymethylglutaryl CoA Reductases, Anti-Obesity Agents, Steatosis, Metabolic syndrome, Hydroxymethylglutaryl-CoA Reductase Inhibitors
Abstract

It is a great challenge to develop drugs for treatment of metabolic syndrome. With ganomycin I as a leading compound, 14 meroterpene derivatives were synthesized and screened for their α-glucosidase and HMG-CoA reductase inhibitory activities. As a result, a α-glucosidase and HMG-CoA reductase dual inhibitor (( R, E)-5-(4-( tert-butyl)phenyl)-3-(4,8-dimethylnona-3,7-dien-1-yl)furan-2(5 H)-one, 7d) with improved chemical stability and long-term safety was obtained. Compound 7d showed multiple and strong in vivo efficacies in reducing weight gain, lowering HbAlc level, and improving insulin resistance and lipid dysfunction in both ob/ob and diet-induced obesity (DIO) mice models. Compound 7d was also found to reduce hepatic steatosis in ob/ob model. 16S rRNA gene sequencing, SCFA, and intestinal mucosal barrier function analysis indicated that gut microbiota plays a central and causative role in mediating the multiple efficacies of 7d. Our results demonstrate that 7d is a promising drug candidate for metabolic syndrome.

Published
2018

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