科研之友
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摘要
Lung cancer is known to be the leading reason for cancer-caused mortality in the world. Many chemotherapeutic drugs have been clinically used to treat lung cancer. Norfloxacin has been also used in the treatment of lung cancer for curing chemotherapy-induced infection of bacteria. This study aims to report potential drug-drug interaction (DDI) between norfloxacin and lung cancer treatment drugs based on the investigation of inhibition of norfloxacin towards on the activity of UGT2B7. In silico docking method was employed to evaluate the binding ability of norfloxacin with the activity cavity of UGT2B7. The chemical structure of norfloxacin can be well docked into the activity cavity of UGT2B7. The constitution of amino acids residues in the activity cavity contained Asn-283, Pro-289, Glu-291, Mse292, Ser-311, Phe-339, Asp-340, Gly-341, Trp-351, Leu-353, Tyr-354, Lys-355, Asn-360, Ala-377, Asn-378, Glu-382, Asp-398, Asp-401, Asn-402, and His-405. No hydrogen bonds were formed between norfloxacin and the activity cavity of UGT2B7. Hydrophobic interaction between norfloxacin and activity cavity of UGT2B7 significantly contributed to the strong binding between norfloxacin and UGT2B7. The involved amino acids residues in the hydrophobic interaction contained Tyr-354, Lys-355, Ala-377, Asp-398, Asp401, Asn-402, and His405. In conclusion, this study used in silico docking method to demonstrate the inhibition of norfloxacin on the activity of UGT2B7, indicating UGT2B7-mediated drug-drug interaction (DDI) between norfloxacin and anti-lung cancer drugs mainly undergoing UGT2B7-catalyzed glucuronidation metabolism.
- 出版日期2017
- 单位湖北医药学院
