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吡格列酮可提高肥胖、胰岛素抵抗恒河猴的全身胰岛素敏感性。

Pioglitazone increases whole body insulin sensitivity in obese, insulin-resistant rhesus monkeys.

作者信息

Tozzo Effie, Bhat Gowri, Cheon Kyeongmi, Camacho Raul C

机构信息

Department of Diabetes, Merck Research Laboratories, Kenilworth, New Jersey, United States of America.

Department of Molecular Biomarkers, Merck Research Laboratories, Kenilworth, New Jersey, United States of America.

出版信息

PLoS One. 2015 May 8;10(5):e0126642. doi: 10.1371/journal.pone.0126642. eCollection 2015.

Abstract

Hyperinsulinemic-euglycemic clamps are considered the "gold standard" for assessing whole body insulin sensitivity. When used in combination with tracer dilution techniques and physiological insulin concentrations, insulin sensitization can be dissected and attributed to hepatic and peripheral (primarily muscle) effects. Non-human primates (NHPs), such as rhesus monkeys, are the closest pre-clinical species to humans, and thus serve as an ideal model for testing of compound efficacy to support translation to human efficacy. We determined insulin infusion rates that resulted in high physiological insulin concentrations that elicited maximal pharmacodynamic responses during hyperinsulinemic-euglycemic clamps. These rates were then used with [U-13C]-D-glucose, to assess and document the degrees of hepatic and peripheral insulin resistance between healthy and insulin-resistant, dysmetabolic NHPs. Next, dysmetabolic NHPs were treated for 28 days with pioglitazone (3 mg/kg) and again had their insulin sensitivity assessed, illustrating a significant improvement in hepatic and peripheral insulin sensitivity. This coincided with a significant increase in insulin clearance, and normalization of circulating adiponectin. In conclusion, we have determined a physiological clamp paradigm (similar to humans) for assessing glucose turnover in NHPs. We have also demonstrated that insulin-resistant, dysmetabolic NHPs respond to the established insulin sensitizer, pioglitazone, thus confirming their use as an ideal pre-clinical translational model to assess insulin sensitizing compounds.

摘要

高胰岛素-正常血糖钳夹技术被认为是评估全身胰岛素敏感性的“金标准”。当与示踪剂稀释技术和生理胰岛素浓度联合使用时,胰岛素敏感性可被剖析并归因于肝脏和外周(主要是肌肉)效应。非人灵长类动物(NHPs),如恒河猴,是与人类最接近的临床前物种,因此是测试化合物疗效以支持向人类疗效转化的理想模型。我们确定了在高胰岛素-正常血糖钳夹期间能产生高生理胰岛素浓度并引发最大药效学反应的胰岛素输注速率。然后将这些速率与[U-13C]-D-葡萄糖一起使用,以评估和记录健康和胰岛素抵抗、代谢异常的NHPs之间肝脏和外周胰岛素抵抗的程度。接下来,对代谢异常的NHPs用吡格列酮(3mg/kg)治疗28天,再次评估其胰岛素敏感性,结果显示肝脏和外周胰岛素敏感性有显著改善。这与胰岛素清除率的显著增加以及循环脂联素的正常化相吻合。总之,我们确定了一种用于评估NHPs葡萄糖代谢的生理钳夹范式(类似于人类)。我们还证明了胰岛素抵抗、代谢异常的NHPs对既定的胰岛素增敏剂吡格列酮有反应,从而证实了它们作为评估胰岛素增敏化合物的理想临床前转化模型的用途。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/abd4/4425551/5a3f84cc3e3b/pone.0126642.g001.jpg

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