Affiliation:
1. College of Pharmacy Pusan National University Busan 46241 Republic of Korea
2. Research Institute for Drug Development Pusan National University Busan 46241 Republic of Korea
3. Institute of Marine Drugs Guangxi University of Chinese Medicine Nanning 530200 P.R. China
4. College of Pharmacy Kyung Hee University Seoul 02447 Republic of Korea
Abstract
AbstractIn our search for peroxisome proliferator‐activated receptor (PPAR) agonists, five undescribed compounds, namely two acyclic diterpenes (1 and 2; cladopsol A and cladopsol B), two sesquiterpenes (3 and 4; cladopsol C and cladopsol D), and one C21‐ecdysteroid (5; cladopsol E), and 15 known compounds were isolated from the jellyfish‐derived fungus – Cladosporium oxysporum. The structures of the undescribed compounds were defined using UV, NMR, HR‐ESI‐MS, and electronic circular dichroism (ECD) spectroscopy and a modified Mosher's method. Luciferase reporter assay and docking analysis suggested that cladopsol B may function as a PPAR‐γ partial agonist with a potential antidiabetic lead which may evade the side effects of full agonists. Moreover, cladopsol B stimulated glucose uptake in HepG2 cells with an efficacy comparable to that of rosiglitazone, but with less side effect induced by lipid accumulation in 3T3‐L1 cells. Therefore, cladopsol B could serve as a molecular skeleton in a study of advanced antidiabetic lead with less side effect.
Funder
National Research Foundation of Korea
Subject
Molecular Biology,Molecular Medicine,General Chemistry,Biochemistry,General Medicine,Bioengineering