Background: The insulinotropic activity of the combined root and stem of Gongronema latifolium (Asclepiadaceae) was evaluated to justify its African ethnomedicinal use in the management of diabetes.
Methods: A methanolic extract and its chromatographic fractions (A1 -A6 ) were tested for glucose-reducing and in vitro insulin-stimulating abilities using glucose-loaded rats and INS-1 cells, respectively. In vivo insulin-releasing activities for the significantly (P<0.05) active antihyperglycemic A5 and A6 and in vitro insulinotropic activity of the C1 fraction and its isolated constituents were also similarly determined.
Results: The extract (100 mg/kg) had higher in vivo antihyperglycemic activity than the individual A1 -A6 , indicating a synergistic effect of the plant constituents. Higher in vivo insulin release in response to A5 (100 mg/kg) than A6 , agreed with their in vivo antihyperglycemic activities and confirmed insulin release as a mechanism of action of the plant. Compared with 5.6 mmol/L glucose (negative control), the extract and the A3 , A6 , and C1 (all at 100.0 μg/mL) elicited significantly higher in vitro insulin release that was similar to that of glibenclamide (1.0 μg/mL; P>0.05). Fraction C1 yielded a 1:1 mixture of α-amyrin and β-amyrin cinnamates (1a:1b), lupenyl cinnamate (2), lupenyl acetate (3), and two unidentified triterpenoids, Y and Z. The 1a:1b mixture (100.0 μg/mL) demonstrated the highest insulinotropic activity that was comparable (P>0.05) to that of glibenclamide (1.0 μg/mL).
Conclusions: The results confirm pancreatic activity as a mechanism underlying the antidiabetic action of G. latifolium and justify its ethnomedical use.
Keywords: Gongronema latifolium; antihyperglycemic; insulin release; α-amyrin cinnamate; β-amyrin cinnamate; 降糖药，Gongronema latifolium，胰岛素释放作用，α-肉桂香树脂醇，β-肉桂香树脂醇.
© 2013 Wiley Publishing Asia Pty Ltd and Ruijin Hospital, Shanghai Jiaotong University School of Medicine.