Biotransformation of medicarpin from homopterocarpin by Aspergillus niger and its biological characterization.

The objective of this study was to convert homopterocarpin derived from Pterocarpus macrocarpus Kurz. heartwood to medicarpin using Aspergillus niger (strain UI X-172) and assess its antioxidant, antiplasmodial, and anticancer activities in silico and in vitro. This study highlighted biotransformation of homopterocarpin to medicarpin via demethylation. Medicarpin demonstrated antioxidant activity against 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS, IC = 0.61 ± 0.05 µg/mL) and 1,1-diphenyl-2-picrylhydrazyl (DPPH, IC = 7.50 ± 1.6 µg/mL), antiplasmodial activity against the Plasmodium falciparum strain 3D7 (IC = 0.45 ± 0.35 µg/mL), and anticancer efficacy against a hepatocyte-derived carcinoma cell line (Huh7it-1 cells, IC = 34.32 ± 5.56 µg/mL). Medicarpin also showed favorable antioxidant, antiplasmodial, and anticancer properties in silico with a binding affinity lower than commercial drugs. These results highlight the green synthesis of medicarpin by microbial transformation using A. niger, which demonstrates promising in vitro and computational activity, however, further studies are required for clinical development.