ABSTRACT
Three new pregnane glycosides, drevoluosides O-Q (1-3) along with five known volubiloside C (4), dreageoside A11 (5), 17ß-marsdenin (6), stavaroside H (7), and hoyacarnoside G (8) were isolated from the methanol extract of the Dregea volubilis leaves. Their structures were elucidated by chemical and spectroscopic methods. Compounds 6-8 showed significant anti α-glucosidase activity with the inhibitory percentages ranging from 32.6 to 47.1% at the concentration of 200 µM. Compound 3 showed significant inhibitory α-amylase activity with IC50 value of 51.3 ± 2.1 µM.
Subject(s)
Glycoside Hydrolase Inhibitors , alpha-Glucosidases , Glycoside Hydrolase Inhibitors/pharmacology , Glycosides/pharmacology , Plant Extracts/pharmacology , Plant Leaves , Pregnanes/pharmacology , alpha-AmylasesABSTRACT
In our search for novel small molecules targeting histone deacetylases, we have designed and synthesized two series of novel N-hydroxybenzamides incorporating 2-oxoindolines (4a-g, 6a-g). Biological evaluation showed that these benzamides potently inhibited HDAC2 with IC50 values in sub-micromolar range. In three human cancer cell lines the synthesized compounds were up to 4-fold more cytotoxic than SAHA. Docking experiments indicated that the compounds tightly bound to HDAC2 at the active binding site with binding affinities much higher than that of SAHA. Our present results demonstrate that these novel and simple N-hydroxybenzamides are potential for further development as anticancer agents and further investigation of similarly simple N-hydroxybenzamides should be warranted to obtain more potent HDAC inhibitors.
