Discovery of Natural Product Derived Labdane Appended Triazoles as Potent Pancreatic Lipase Inhibitors.

ABSTRACT: Obesity contributes to the genesis of many metabolic disorders including dyslipidemia, coronary heart disease (CHD), nonalcoholic fatty liver, type 2 diabetes, etc. Pancreatic lipase plays a vital role in food fat digestion and absorption. Therefore, to control obesity, inhibition of pancreatic lipase is the active therapy. Thus, novel natural product derived labdane appended triazoles with pancreatic lipase inhibition potential were designed and synthesized. Among these hybrids, 6b and 6f exhibited excellent inhibitory activity (IC₅₀ 0.75 ± 0.02 ?M and 0.77 ± 0.01 ?M), slightly better than that of the positive control Orlistat (IC₅₀ 0.8 ± 0.03 ?M). Compounds 6c, 6e, and 6g-j inhibited the PL comparable to that of positive control. Interestingly none of the compounds showed cytotoxicity (Hep G2) in the concentration range from 0.5 to 100 ?M. Overall results reveal the potential of labdane appended triazoles as antiobesity agents.

SUBMITTER: Jalaja R 

PROVIDER: S-EPMC6047173 | biostudies-literature | 2018 Jul

REPOSITORIES: biostudies-literature