Prasad G Shyam, Govardhan P, Girisham S, Reddy S M
Department of Microbiology, Kakatiya University, Warangal-506009, Telangana, India.
Drug Metab Lett. 2014;8(2):88-95. doi: 10.2174/1872312808666140606103227.
Different fungi viz. Aspergillus niger NCIM 589, A.ochraceous NCIM 1140, Cunninghamella blakesleeana NCIM 687, C. echinulata NCIM 691, Rhizopus stolonifer NCIM 880, Mucor rouxi MTCC 386, Trichothecium roseum NCIM 1147 were screened for their potential to biotransform anti-hyperlipidemia and anti-hypertriglyceridemia drug, fenofibrate to fenofibric acid, the active metabolite and other mammalian metabolites. Among the fungi screened C. blakesleeana transformed fenofibrate to fenofibric acid and other three metabolites. HPLC, LC-MS/MS analysis and previous reports confirmed the transformation of fenofibrate and metabolites as fenofibric acid (M1), reduced fenofibric acid (M2), reduced fenofibric acid taurine conjugate (M3), reduced fenofibric acid ester glucuronide (M4), the mammalian metabolites reported previously. The results proved the potential of C.blakesleeana NCIM 687 in the production of mammalian phase I (M1 and M2) and phase II (M3 and M4) metabolites in large quantities and also as an in vitro model for drug metabolism studies.
对不同的真菌，即黑曲霉NCIM 589、赭曲霉NCIM 1140、布氏被孢霉NCIM 687、刺孢被孢霉NCIM 691、匍枝根霉NCIM 880、鲁氏毛霉MTCC 386、粉红单端孢霉NCIM 1147进行了筛选，以评估它们将抗高血脂和抗高甘油三酯药物非诺贝特生物转化为活性代谢物非诺贝特酸以及其他哺乳动物代谢物的潜力。在所筛选的真菌中，布氏被孢霉将非诺贝特转化为非诺贝特酸和其他三种代谢物。高效液相色谱法、液相色谱 - 串联质谱分析法以及先前的报告证实了非诺贝特的转化以及代谢物为非诺贝特酸（M1）、还原型非诺贝特酸（M2）、还原型非诺贝特酸牛磺酸共轭物（M3）、还原型非诺贝特酸酯葡萄糖醛酸苷（M4），这些都是先前报道的哺乳动物代谢物。结果证明了布氏被孢霉NCIM 687在大量生产哺乳动物I相（M1和M2）和II相（M3和M4）代谢物方面的潜力，以及作为药物代谢研究的体外模型的潜力。
