Drug Designing: Open Access
Open Access

Highly potent glucosidase inhibitors from Pterocarpus indicus and molecular docking studies

28^th International Conference on Chemistry & Drug Designing

December 05-06, 2018 | Vancouver, Canada

Jirapast Sichaem

Thammasat University Lampang Center, Thailand

Posters & Accepted Abstracts: Drug Des

Abstract :

The phytochemical investigation of Pterocarpus indicus stems led to isolation of twelve compounds (1-12), including two major triterpenoids, lupeol (1) and canophyllol (2), one quinone derivative, 2,6-dimethoxy-p-benzoquinone (3), three phenolic derivatives, vanillic acid (4), trans-4-hydroxymellein (5) and cis-4-hydroxymellein (6), six flavonoids that can be classified into two pterocarpin derivatives, (6αR,11αR)-medicarpin (7) and (6αR,11αR)-3,8-dihydroxy-9-methoxy pterocarpan (8), together with four isoflavones, afromosin (9), formononetin (10), clycosin (11) and 8-O-methylretusin (12), by comparing their NMR spectral data to those formerly published and assured through co-TLC with authentic samples (Figure 1). Moreover, the X-ray crystal structure of 12 has been reported for the first time. A major active compound (1) was derivatized to one new analogue (1d) and five known derivatives (1a-1c and 1e-1f). All isolated compounds (1-12) and modified analogues (1a-1f) were evaluated for their α-glucosidase activity. In this regard, compounds 1 and 11 exhibited potent inhibitory activity towards yeast α-glucosidase when compared to the positive control (acarbose). In addition, the α-glucosidase (maltase and sucrase) inhibitory activity of all compounds (1-12 and 1a-1f) was also evaluated. Only compound 11 showed moderate inhibitory activity towards rat intestinal α-glucosidase. The experimental results were also confirmed by docking analysis. From this study, these compounds have emerged as promising molecules for diabetic therapy.

Biography :

Jirapast Sichaem has completed his PhD at the age of 26 years from Department of Chemistry, Faculty of Science, Chulalongkorn University, Thailand. He is a lecture at Department of Chemistry, Faculty of Science and Technology, Thammasat University, Thailand. He has his expertise in the field of cytotoxic, antioxidant, antidiabetic and anti-Alzheimer's compounds from Thai medicinal plants. He has published more than 30 papers in scientific journals.

E-mail: Jirapast.s@gmail.com