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目的:以雷公藤甲素为原料,采用微生物转化法合成新型抗类风湿药物雷腾舒。方法:筛选10株小克银汉霉菌,采用HPLC法检测转化液中目标产物雷腾舒的浓度并计算产率,优化转化系统。结果:模型菌株雅致小克银汉霉ATCC36112在pH 4.5、底物浓度400μg.mL-1和转化10 d等条件下,雷腾舒产率>70%。结论:小克银汉霉ATCC36112转化雷公藤甲素,为活性代谢产物雷腾舒的合成开辟了一条新途径。
OBJECTIVE: To synthesize a new anti-rheumatoid drug Leitengshu using triptolide as raw material and microbial transformation method. Methods: Ten strains of Haemophilus kawakamii were screened, and the concentration of the target product Leitengshu was determined by HPLC. The yield of the target product was calculated and the transformation system was optimized. Results: The model strain Accutokolinia ATCC36112 had a yield of over 70% of Lentinulab at pH 4.5, substrate concentration of 400 μg.mL-1 and transformation time of 10 d. CONCLUSION: Transformation of triptolide ATCC36112 to Triptolide opens up a new way for the synthesis of active metabolite Leitengshu.