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有機陰離子轉(zhuǎn)運多肽1B1對2型糖尿病藥物治療的影響

發(fā)布時間:2019-07-21 11:58
【摘要】:目的:了解有機陰離子轉(zhuǎn)運多肽1B1(OATP1B1)對2型糖尿病藥物治療的影響。方法:查閱近年來國內(nèi)外相關(guān)文獻,就OATP1B1的影響機制、對那格列奈和瑞格列奈等藥物的影響、其他基因組信息進行歸納和總結(jié)。結(jié)果:OATP1B1對那格列奈和瑞格列奈的體內(nèi)過程影響明顯,人類OATP1B1編碼基因(SLCO1B1)521TC位點的突變對那格列奈藥動學(xué)和藥效學(xué)的影響與野生型對照組比較,差異有統(tǒng)計學(xué)意義;OATP1B1對瑞格列奈藥動學(xué)影響呈劑量依賴關(guān)系。SLCO1B1 388AG位點的突變對2型糖尿病藥物的體內(nèi)過程影響不明顯。結(jié)論:OATP1B1作為攝入型轉(zhuǎn)運體在糖尿病的藥物治療中起重要作用;颊叩幕蚪M信息將成為2型糖尿病患者臨床合理用藥的重要參考因素,有必要對OATP1B1進行更深入、系統(tǒng)的研究。
[Abstract]:Objective: to investigate the effect of organic anion transport polypeptide 1B1 (OATP1B1) on drug therapy of type 2 diabetes mellitus (T2DM). Methods: the influence mechanism of OATP1B1, the influence of nateglinide and repaglinide and other genomic information on nateglinide and repaglinide were summarized by reviewing the relevant literature at home and abroad in recent years. Results: the effect of OATP1B1 on the in vivo process of nateglinide and repaglinide was obvious. The effect of mutation of human OATP1B1 coding gene (SLCO1B1) 521TC site on the pharmacokinetics and pharmacokinetics of nateglinide was significantly different from that of wild type control group. The effect of OATP1B1 on the pharmacokinetics of repaglinide was dose-dependent. The mutation of SLCO1B1 388AG site had no significant effect on the in vivo process of type 2 diabetic drugs. Conclusion: OATP1B1, as an ingestion transporter, plays an important role in the drug treatment of diabetes mellitus. The genomic information of patients will become an important reference factor for clinical rational drug use in patients with type 2 diabetes mellitus. It is necessary to study OATP1B1 more deeply and systematically.
【作者單位】: 皖南醫(yī)學(xué)院附屬弋磯山醫(yī)院臨床藥學(xué)部;
【基金】:國家自然科學(xué)基金資助項目(No.81173134)
【分類號】:R587.1


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