title: Antidiabetic activities of triterpenoids isolated from bitter melon associated with activation of the AMPK pathway.
abstract: Four cucurbitane glycosides, momordicosides Q, R, S, and T, and stereochemistry-established karaviloside XI, were isolated from the vegetable bitter melon (Momordica charantia). These compounds and their aglycones exhibited a number of biologic effects beneficial to diabetes and obesity. In both L6 myotubes and 3T3-L1 adipocytes, they stimulated GLUT4 translocation to the cell membrane--an essential step for inducible glucose entry into cells. This was associated with increased activity of AMP-activated protein kinase (AMPK), a key pathway mediating glucose uptake and fatty acid oxidation. Furthermore, momordicoside(s) enhanced fatty acid oxidation and glucose disposal during glucose tolerance tests in both insulin-sensitive and insulin-resistant mice. These findings indicate that cucurbitane triterpenoids, the characteristic constituents of M. charantia, may provide leads as a class of therapeutics for diabetes and obesity.
authors: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China.
authors: Min-Jia
authors: MJ
authors: Tan
authors: Ji-Ming
authors: JM
authors: Ye
authors: Nigel
authors: N
authors: Turner
authors: Cordula
authors: C
authors: Hohnen-Behrens
authors: Chang-Qiang
authors: CQ
authors: Ke
authors: Chun-Ping
authors: CP
authors: Tang
authors: Tong
authors: T
authors: Chen
authors: Hans-Christoph
authors: HC
authors: Weiss
authors: Ernst-Rudolf
authors: ER
authors: Gesing
authors: Alex
authors: A
authors: Rowland
authors: David E
authors: DE
authors: James
authors: Yang
authors: Y
authors: Ye
mesh_terms: D041721:3T3-L1 Cells; D055372:AMP-Activated Protein Kinases; D017667:Adipocytes / Q000187:drug effects / Q000378:metabolism / Q000648:ultrastructure; D000818:Animals; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D005227:Fatty Acids / Q000378:metabolism; D005947:Glucose / Q000378:metabolism; D051275:Glucose Transporter Type 4 / Q000378:metabolism; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D007328:Insulin / Q000378:metabolism; D051379:Mice; D029777:Momordica charantia / Q000737:chemistry*; D009097:Multienzyme Complexes / Q000378:metabolism*; D018485:Muscle Fibers, Skeletal / Q000187:drug effects / Q000378:metabolism / Q000648:ultrastructure; D010084:Oxidation-Reduction / Q000187:drug effects; D010766:Phosphorylation / Q000187:drug effects; D017346:Protein Serine-Threonine Kinases / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects*; D013729:Terpenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*
chemical_list: D005227:Fatty Acids; D051275:Glucose Transporter Type 4; D007004:Hypoglycemic Agents; D007328:Insulin; D009097:Multienzyme Complexes; D013729:Terpenes; D017346:Protein Serine-Threonine Kinases; D055372:AMP-Activated Protein Kinases; D005947:Glucose