Synthesis of dammarenolic acid derivatives with a potent α-glucosidase inhibitory activity

AbstractDammarenolic acid (DA) is an A-seco-dammarane triterpenoids, isolated fromDipterocarpus alatus resin. DA was modified including reactions of esterification and amination with heterocyclic amines andl-amino acids. The structures of new compounds were confirmed by MS,1H NMR, and13C NMR spectroscopic analyses and their activities againstα-glucosidase and acetylcholinesteras were studied. The cytotoxic activity of DA was screened using a broad panel of 60 human cancer cell lines and it has cytotoxic effect for a variety of human tumor cell lines (leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, breast cancer). All A-seco-dammarane derivatives exhibited very low or no activity against achetylcholinesterase. The majority of new compounds demonstrated higher antidiabetic activity againstα-glucosidase compared with starting dammarenolic acid. The methyl dammarenoloate determined as a lead compound with the IC50 value of 0.037  μM being about 4800-fold more active than acarbose and 108-fold more active than the native DA with the IC50 value of 4.0  μM.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research

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