School of Medicine, Nantong University, 19 Qi Xiu Road, Nantong 226001, PR China.
School of Pharmaceutical Engineering & Life Science, Changzhou University, 1 Gehu Road, Changzhou 213164, PR China.
Fitoterapia. 2013 Dec;91:256-260. doi: 10.1016/j.fitote.2013.09.019. Epub 2013 Oct 3.
The biotransformation of 20(S)-protopanaxadiol (1) by Aspergillus niger AS 3.1858 was conducted. Seven metabolites 26-hydroxyl-20(S)-protopanaxadiol (2); 23, 24-en-25-hydroxyl-20(S)-protopanaxadiol (3); 25, 26-en-20(S)-protopanaxadiol (4); (E)-20, 22-en-25-hydroxyl-20(S)-protopanaxadiol (5); 25, 26-en-24(R)-hydroxyl-20(S)-protopanaxadiol (6); 25, 26-en-24(S)-hydroxyl-20(S)-protopanaxadiol (7); and 23, 24-en-25-ethoxyl-20(S)-protopanaxadiol (8) were afforded. Among them, 6, 7, and 8 are new compounds. The chemical structures of these metabolites were elucidated based on extensive spectral data including 2D NMR and HRMS. In addition, the cytotoxicity of substrate and all transformed products was evaluated by MTT assay using a panel of seven human tumor cell lines (Du-145, Hela, K562, K562/ADR, SH-SY5Y, HepG2, and MCF-7 cells) and one normal cell line Vero.
黑曲霉 AS 3.1858 对 20(S)-原人参二醇（1）进行了生物转化。分离得到 7 种代谢产物 26-羟基-20(S)-原人参二醇（2）；23,24-烯-25-羟基-20(S)-原人参二醇（3）；25,26-烯-20(S)-原人参二醇（4）；（E）-20,22-烯-25-羟基-20(S)-原人参二醇（5）；25,26-烯-24(R)-羟基-20(S)-原人参二醇（6）；25,26-烯-24(S)-羟基-20(S)-原人参二醇（7）；23,24-烯-25-乙氧基-20(S)-原人参二醇（8）。其中，化合物 6、7 和 8 为新化合物。这些代谢产物的化学结构是基于广泛的光谱数据，包括 2D NMR 和 HRMS 来阐明的。此外，采用 MTT 法，用 7 个人类肿瘤细胞系（Du-145、Hela、K562、K562/ADR、SH-SY5Y、HepG2 和 MCF-7 细胞）和一个正常细胞系 Vero 评估了底物和所有转化产物的细胞毒性。
