Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, PR China.
Fitoterapia. 2011 Dec;82(8):1313-7. doi: 10.1016/j.fitote.2011.09.001. Epub 2011 Sep 17.
Biotransformation of ginsenoside-Rg₁ (1) by the fungus Absidia coerulea AS 3.2462 yielded five metabolites (2-6). On the basis of spectroscopic data analyses, the metabolites were identified as ginsenoside-F₁ (2), 6α,12β-dihydroxydammar-3-one-20(S)-O-β-D-glucopyranoside (3), 3-oxo-20(S)-protopanaxatriol (4), 3-oxo-7β-hydroxy-20(S)-protopanaxatriol (5), and 3-oxo-7β,15α-dihydroxy-20(S)-protopanaxatriol (6), respectively. Among them, 5 and 6 are new compounds. These results indicated that Absidia coerulea AS 3.2462 could catalyze the specific C-3 dehydrogenation of derivatives of ginsenoside-Rg₁, as well as hydroxylation at the 7β and 15α positions. Metabolites 2, 4 and 5 exhibited moderate reversal activity towards A549/taxol MDR tumor cells in vitro.
真菌斜卧青霉 AS 3.2462 对人参皂苷 Rg₁(1)的生物转化生成了五种代谢产物(2-6)。基于光谱数据分析,鉴定这些代谢产物分别为人参皂苷 F₁(2)、6α,12β-二羟基达玛-3-酮-20(S)-O-β-D-吡喃葡萄糖苷(3)、3-酮-20(S)-原人参三醇(4)、3-酮-7β-羟基-20(S)-原人参三醇(5)和 3-酮-7β,15α-二羟基-20(S)-原人参三醇(6)。其中,5 和 6 是新化合物。这些结果表明斜卧青霉 AS 3.2462 能够特异性地催化人参皂苷 Rg₁衍生物的 C-3 脱氢以及 7β 和 15α 位的羟化。代谢产物 2、4 和 5 在体外对 A549/taxol MDR 肿瘤细胞表现出中等的逆转活性。