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Effect of resveratrol on dipeptidyl peptidase-4 inhibitors pharmacokinetics: An in vitro and in vivo approach.
Chemico-Biological Interactions ( IF 5.1 ) Pub Date : 2019-11-28 , DOI: 10.1016/j.cbi.2019.108909
Shruti Surendran 1 , Rekha Sapkal 1 , David Paul 1 , Satheeshkumar Nanjappan 1
Affiliation  

Diabetes mellitus (DM) is a metabolic disorder with hyperglycemia being its hallmark symptom. The secondary symptom of DM is oxidative stress, which leads to the generation of free radicals. Diabetic nephropathy and neuropathy is the long-term effect of oxidative stress caused in DM, which leads to damage of kidneys and neurons respectively. Resveratrol (RES) is a phytochemical, found to be effective in the treatment of diabetic nephropathy and neuropathy. Due to its antioxidant property, it reduces the oxidative stress caused by DM. Dipeptidyl peptidase-4 (DPP-4) inhibitors are used for the treatment of type 2 DM. In vitro and in vivo data depicted that the metabolism of alogliptin (ALO), saxagliptin (SAX) and sitagliptin (SIT) were decreased in presence of RES while metabolism of teneligliptin (TEN) was not affected in presence of RES. The results show that the alteration of the pharmacokinetics of ALO, SAX and SIT was due to inhibition of CYP P450 by RES. Thus, there was a significant pharmacokinetic interaction between RES-ALO, RES-SAX and RES-SIT. Hence, a dose reduction is required when RES therapy is taken in combination with ALO, SAX and SIT as there is an increase in drug exposure, which might lead to toxicity.

中文翻译:

白藜芦醇对二肽基肽酶-4抑制剂药代动力学的影响:一种体外和体内方法。

糖尿病(DM)是一种代谢紊乱,高血糖症是其典型症状。DM的第二症状是氧化应激,其导致自由基的产生。糖尿病肾病和神经病是DM引起的长期氧化应激反应,分别导致肾脏和神经元的损害。白藜芦醇(RES)是一种植物化学物质,被发现可有效治疗糖尿病性肾病和神经病。由于其抗氧化性能,它减少了由DM引起的氧化应激。二肽基肽酶-4(DPP-4)抑制剂用于治疗2型DM。体外和体内数据表明,在RES存在下,阿格列汀(ALO),沙格列汀(SAX)和西他列汀(SIT)的代谢降低,而在RES存在下,teneligliptin(TEN)的代谢不受影响。结果表明,ALO,SAX和SIT的药代动力学改变是由于RES抑制CYP P450所致。因此,RES-ALO,RES-SAX和RES-SIT之间存在显着的药代动力学相互作用。因此,当RES治疗与ALO,SAX和SIT联合使用时,需要减少剂量,因为药物暴露会增加,这可能会导致毒性。
更新日期:2019-11-28
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