Enzymatic Synthesis of Some Betulinic Acid Derivative: Enhance Their Bioactivity
Faujan B.H.Ahmad
Department of Chemistry, University Putra, Malaysia
Abstract:
Natural products played an important role in drug discovery and developments since it have been used to cure human diseases for thousands of years. Betulinic acid, a naturally occurring pentacyclic triterpenoid has attracted the science community attention for its medicinal value as anticancer and anti-HIV agents. In this work, the derivative of betulinic acid, 3-O-(3'',3''-dimethylsuccinyl)-betulinic acid was successfully synthesized by enzymatic method in organic solvent. The potential of this compound as anticancer agent was evaluated by MTT assay on cultured human T-promyelocytic leukemia (HL-60), human breast cancer (MCF-7), human cervical carcinoma cancer (HeLa) and mouse embryonic fibroblast normal cell line (3T3) cells lines. In particular, 3-O-(3'',3''-dimethylsuccinyl)-betulinic acid (DSB)showed nontoxic activity against human T-promyelocytic leukemia (HL-60) and human breast cancer (MCF-7) with IC50 > 30 mg/ml. However, it has better activity against human cervical carcinoma cancer (HeLa) (IC50 1.9 mg/ml) compared to betulinic acid (IC50 4.8 mg/ml). Interestingly, both compound were highly inactive against mouse embryonic fibroblast normal cell line (3T3) with IC50 > 30 mg/ml.
