Evaluation of ethnomedical claim III: anti-hyperglycemic activities of Gongronema latifolium root and stem.

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.