Wahyuni Dwi Kusuma, Wacharasindhu Sumrit, Bankeeree Wichanee, Punapayak Hunsa, Putri Sastia Prama, Prasongsuk Sehanat
Plant Biomass Utilization Research Unit, Department of Botany, Faculty of Science, Chulalongkorn University, Bangkok, 10330, Thailand.
Department of Biology, Faculty of Science and Technology, Universitas Airlangga, Surabaya, East Java, 60115, Indonesia.
Sci Rep. 2025 Jul 1;15(1):21371. doi: 10.1038/s41598-025-06729-9.
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.
本研究的目的是利用黑曲霉（菌株UI X - 172）将源自大叶紫檀心材的紫檀素转化为美迪紫檀素，并在计算机模拟和体外实验中评估其抗氧化、抗疟和抗癌活性。本研究强调了通过去甲基化将紫檀素生物转化为美迪紫檀素。美迪紫檀素对2,2'-联氮-双(3-乙基苯并噻唑啉-6-磺酸)（ABTS，IC = 0.61±0.05μg/mL）和1,1-二苯基-2-苦基肼（DPPH，IC = 7.50±1.6μg/mL）表现出抗氧化活性，对恶性疟原虫3D7株表现出抗疟活性（IC = 0.45±0.35μg/mL），对肝细胞源性癌细胞系（Huh7it - 1细胞，IC = 34.32±5.56μg/mL）表现出抗癌功效。美迪紫檀素在计算机模拟中也显示出良好的抗氧化、抗疟和抗癌特性，其结合亲和力低于市售药物。这些结果突出了利用黑曲霉通过微生物转化绿色合成美迪紫檀素，其在体外和计算机模拟实验中显示出有前景的活性，然而，临床开发还需要进一步研究。
