《Table 5.Inhibitory effects of CNS, NS, and SF on UGT1A1, UGT1A4 and UGT2B7 in human livermicrosomes

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《三七-红花有效组分复方对人肝微粒体中UGT1A1、1A4和2B7活性抑制作用的研究（英文）》

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In our present study，etoposide[10]，trifluoperazine[11]and azidothymidine[12]were selected as the probe drugs to evaluate the effects of CNS，NS and SF on the activities of UGT1A1，1A4 and 2B7 in HLMs，respectively.There were two control groups（group A and group B）.Group A:probe drugs were incubated with HLMs in the absence of UDPGA；group B:probe drugs were incubated in the absence of HLMs.The probe drugs were stable in both control groups.Compared with the control group，4.4 mg/mL of CNS，4.8 mg/mL of NS and6.0 mg/mL of SF exhibited significant inhibition on UGT1A1，1A4 and 2B7 activities（P<0.05）with the IC50 values between 9.69±0.45 mg/mL to 27.66±2.14mg/mL in a concentration-dependent manner（Table 5）.Typically，UGT1A1 and 1A4 are believed to be the key enzymes for the metabolism of bilirubin and nitrogen compounds[2]，respectively.Meanwhile，UGT2B7 has been reported to be responsible for the glucuronidation of opioids，all C14，C16，C18，C20 saturated and unsaturated fatty acids[13].This finding above reminded us to focus on the HDI potency of CNS in clinic.