Xiao Yina, Lee Ik-Soo
College of Pharmacy, Chonnam National University, Gwangju 61186, Korea.
Foods. 2022 Feb 14;11(4):543. doi: 10.3390/foods11040543.
Microbial transformation is an alternative method for structural modification. The current study aimed at application of microbial transformation for discovering new derivatives and investigating the structure-activity relationship of isobavachalcone (), 4-hydroxyderricin (), and xanthoangelol () isolated from the herb . In the initial screening process, - were incubated with microbes using a two-stage fermentation method and analyzed through TLC monitoring. The screening results showed that and were able to transform and , respectively. Additionally, and var. were able to transform . Following scale-up fermentation, four new (, , , and ) and five known (, , , , and ) metabolites were produced. Cytotoxicity of all the compounds (-) was investigated using three human cancer cell lines including A375P, HT-29, and MCF-7 by MTT method. Meanwhile, the tyrosinase inhibitory activity of - was evaluated using l-tyrosine as a substrate. Overall, and displayed the highest cytotoxicity, and and exhibited the most potent tyrosinase inhibitory activity with relatively low cytotoxicity. This allowed us to postulate that the introduction of 4'--glucopyranosyl group led to the reduction in cytotoxicity and improvement in tyrosinase inhibitory activity.
微生物转化是一种结构修饰的替代方法。当前的研究旨在应用微生物转化来发现新的衍生物，并研究从该草药中分离出的异补骨脂查尔酮（）、4-羟基德里辛（）和花椒毒素（）的构效关系。在初步筛选过程中，使用两阶段发酵法将 - 与微生物一起孵育，并通过薄层色谱监测进行分析。筛选结果表明，和分别能够转化和。此外，和变种能够转化。经过放大发酵，产生了四种新的（、、、和）和五种已知的（、、、、和）代谢产物。使用MTT法，利用包括A375P、HT-29和MCF-7在内的三种人类癌细胞系研究了所有化合物（ - ）的细胞毒性。同时，以L-酪氨酸为底物评估了 - 的酪氨酸酶抑制活性。总体而言，和表现出最高的细胞毒性，而和表现出最强的酪氨酸酶抑制活性，且细胞毒性相对较低。这使我们推测，4'- - 吡喃葡萄糖基的引入导致细胞毒性降低和酪氨酸酶抑制活性提高。
