A cell-based screening identifies compounds from the stem of Momordica charantia that overcome insulin resistance and activate AMP-activated protein kinase.
Treatment of insulin resistance is a critical strategy in the prevention and management of type 2 diabetes. The crude extracts from all parts of Momordica charantia L. have been reported by many studies for the effective treatment of diabetes and related complications. However, the exact ingredients responsible for the hypoglycemic effect and the underlying mechanism of their actions have not been well characterized because of the lack of a proper assay and screening system. A new cell-based, nonradioactive, and nonfluorescent screening method was demonstrated in this study to screen for natural products from the stem of M. charantia, aiming to identify hypoglycemic components that can overcome cellular insulin resistance. The results suggest triterpenoids being potential hypoglycemic components of the plant and the mechanism underlying their action involving AMP-activated protein kinase.
Cheng
Hsueh-Ling
HL
Graduate Institute of Biotechnology, National Pingtung University of Science and Technology, Pingtung, Taiwan 91201. hlcheng@mail.npust.edu.tw
Huang
Hsin-Kai
HK
Chang
Chi-I
CI
Tsai
Chung-Pao
CP
Chou
Chang-Hung
CH
D055372:AMP-Activated Protein Kinases; D000818:Animals; D002460:Cell Line; D004789:Enzyme Activation / Q000187:drug effects; D005947:Glucose / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000494:pharmacology; D007333:Insulin Resistance; D008099:Liver; D051379:Mice; D029777:Momordica charantia / Q000737:chemistry*; D009097:Multienzyme Complexes / Q000378:metabolism*; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D018547:Plant Stems / Q000737:chemistry*; D017346:Protein Serine-Threonine Kinases / Q000378:metabolism*; D014409:Tumor Necrosis Factor-alpha / Q000494:pharmacology
D007004:Hypoglycemic Agents; D009097:Multienzyme Complexes; D010936:Plant Extracts; D014409:Tumor Necrosis Factor-alpha; D017346:Protein Serine-Threonine Kinases; D055372:AMP-Activated Protein Kinases; D005947:Glucose