Insulin releasing effect of some pure compounds from Moringa oleifera on mice islets

AbstractThe anti-diabetic activity of extracts, fractions and compounds ofMoringa oleifera have been reported; however, several constituents from this well known medicinal plant are not yet screened for bio-perspecting role for diabetes. Current studies demonstrated the anti-diabetic properties of five chemical constituents of the plant viz, 4-hydroxyphenylacetonitrite (1), fluoropyrazine (3), methyl-4-hydroxybenzoate (4), vanillin (5), and 4- α-L-rhamnopyranosyloxybenzyl isothiocyanate (6) along with one related compound 3,4-dihydroxy benzonitrile (2) for the first time in vitro and in vivo. Furthermore, the mechanism of action of compounds was predicted by utilizing molecular docking with protein kinase A (PKA) and exchange protein activated by cAMP (Epac2A). The structure of compounds was elucidated by UV, IR, MS, and1H NMR. The compounds1,3–5 induced significant insulin secretion at stimulatory (16.7  mM) glucose, but not at basal (3 mM) glucose concentration, and compound3 seems to be the most active. Compounds1,3–5 showed dose-dependent insulin secretory activity with optimum response at 200  μM. In silico studies revealed that compound3 has a noticeable electrostatic and hydrophobic interaction with protein kinase A (PKA). In vitro studies also showed that there was significant reduction of compounds1–3 mediated insulin secretion in the presence of PKA inhibitor suggesting that there is a possible role of PKA signaling pathway on insulin secretion. Upon o...
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research