Department of Microbiology, Kakatiya University, Warangal 506009, India.
J Microbiol Biotechnol. 2009 Sep;19(9):922-31. doi: 10.4014/jmb.0811.643.
Screening-scale studies were performed with 26 fungal cultures for their ability to transform the anti-inflammatory drug meloxicam. Among the different fungi screened, a filamentous fungus, Cunninghamella blakesleeana NCIM 687, transformed meloxicam to three metabolites in significant quantities. The transformation of meloxicam was confirmed by high-performance liquid chromatography (HPLC). Based on the liquid chromatography-tandem mass spectrometry (LC-MS/MS) data, two metabolites were predicted to be 5-hydroxymethyl meloxicam and 5-carboxy meloxicam, the major mammalian metabolites reported previously. A new metabolite was produced, which is not detected in mammalian systems. Glucose medium, pH of 6.0, temperature of 27 degrees , 5-day incubation period, dimethylformamide as solvent, and glucose concentration of 2.0%were found to be suitable for maximum transformation of meloxicam when studied separately. It is concluded that C. blakesleeana can be employed for biotransformation of drugs for production of novel metabolites.
采用 26 种真菌培养物进行了筛选规模的研究,以考察它们将抗炎药物美洛昔康转化的能力。在所筛选的不同真菌中,丝状真菌 Blakeslea cinerea NCIM 687 以显著量将美洛昔康转化为三种代谢物。美洛昔康的转化通过高效液相色谱(HPLC)得到确认。根据液相色谱-串联质谱(LC-MS/MS)数据,预测两种代谢物为 5-羟甲基美洛昔康和 5-羧基美洛昔康,这是先前报道的主要哺乳动物代谢物。产生了一种新的代谢物,在哺乳动物系统中未检测到。当分别研究时,发现葡萄糖培养基、pH 值 6.0、温度 27 度、5 天孵育期、二甲基甲酰胺作为溶剂和 2.0%的葡萄糖浓度最适合美洛昔康的最大转化。结论是,可以利用 Blakeslea cinerea 进行药物的生物转化,以生产新型代谢物。