The Antigluconeogenic Activity of Cucurbitacins from Momordica charantia

Abstract

Five new cucurbitacins, kuguacins II–VI (1–5), along with five known analogues (6–10), were obtained from the fruit of Momordica charantia. Structures of the new compounds were elucidated as 5β,19-epoxycucurbit-23-en-7-on-3β,25-diol (1), 5β,19-epoxycucurbit-7,23-dion-3β,25-diol (2), 5β,19-epoxycucurbit-6-en-19,23-dion-3β,25-diol (3), 5β,19-epoxy-23,24,25,26,27-pentanorcucurbit-6-en-7,19-dion-3β,22-diol (4), and cucurbit-5-en-7,23-dion-3β,19,25-triol (5) by extensive spectroscopic and single-crystal X-ray diffraction analyses. Some cucurbitane compounds from this species were screened for their potential antidiabetic properties in terms of antigluconeogenic activity. As a result, compounds 1, 10, 11, and 12 (at 25–100 µM) showed concentration-dependent inhibition on glucose production from liver cells. In addition, compounds 11 and 12 (at 100 µM) showed around 20–30 % inhibition on PEPCK activity.

Key words

Momordica charantia - Cucurbitaceae - cucurbitacin - kuguacins II–VI - antigluconeogenic activity - PEPCK activity

• References

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