The α‐amylase inhibition has been considered as an effective therapeutic approach against chronic Type 2 Diabetes mellitus (DM). In the present study, a series of biphenylcarbonitrile‐thiazolidinedione conjugates have been synthesized and evaluated for their antidiabetic activity viaα‐amylase inhibition. It was found that most of the conjugates (14 a–j) exhibited significant α‐amylase inhibition activity compared to the standard drug Acarbose. Off these, compound 14 b,14 c and 14 dwere most potent with IC50 value 0.13 μM, 0.15 μM and0.13 μM respectively. To ascertain ligand‐receptor interactions, the in silico molecular docking studies of these conjugates (14 a–j) have been carried out into the Acarbose active site of barley (malt) α‐amylase enzyme. The results have shown fair corroboration between significant α‐amylase inhibition activity of 14 b, 14 c and 14 d and their docking scores compared to the standard drug Acarbose. This study demonstrated that biphenylcarbonitrile‐thiazolidinedione conjugate could be a plausible pharmacophore for targeting α‐amylase for the treatment of Type 2 Diabetes mellitus.
Background:Plumbago zeylanica plant belongs to Plumbaginaceae. The plant is reported for many pharmacological activities.
Aim: The objective of the study was to identify fatty acids and non-polar chemical compounds in Plumbago zeylanica leaves.
Materials and methods: Petroleum ether extract was prepared using soxhlet apparatus. Saponifiable and unsaponifiable matter was separated with saponification process. To identify fatty acids in saponifiable matter further esterification was performed. Gas chromatography and mass spectrometry analysis was performed of both saponifiable and unsaponifiable fractions. All the fatty acid methyl esters and non-polar chemical compounds were identified using NIST library data.
Results: A total of 14 compounds were identified with comparison of NIST data. From that, 8 fatty acid methyl esters and 6 non-polar chemical compounds were identified. Here we have analyzed fatty acids and non-polar chemical compounds by the same GC-MS method.
Conclusions: The present analysis showed that Plumbago Zeylanica leaves contain 8 fatty acids and 6 non-polar chemical compounds. Principal determination of the research was development of efficient method to identify non-polar compound from plant by single injection using chromatographic technique.
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