Department of Pharmacology, All India Institute of Medical Sciences, New Delhi, India.
Department of Pharmacology, Khalsa College of Pharmacy, Amritsar, India.
J Pharm Pharmacol. 2023 Sep 1;75(9):1198-1211. doi: 10.1093/jpp/rgad043.
Diabetic cardiomyopathy (DC) is one of the severe secondary complications of diabetes mellitus in humans. Vinpocetine is an alkaloid having pleiotropic pharmacological effects. The present study is designed to investigate the effect of vinpocetine in DC in rats.
Rats were fed a high-fat diet for nine weeks along with single dose of streptozotocin after the second week to induce DC. The haemodynamic evaluation was performed to assess the functional status of rats using the Biopac system. Cardiac echocardiography, biochemical, oxidative stress parameters and inflammatory cytokine level were analysed in addition to haematoxylin-eosin and Masson's trichome staining to study histological changes, cardiomyocyte diameter and fibrosis, respectively. Phosphodiesterase-1 (PDE-1), transforming growth factor-β (TGF-β) and p-Smad 2/3 expression in cardiac tissues were quantified using western blot/RT-PCR.
Vinpocetine treatment and its combination with enalapril decreased the glucose levels compared to diabetic rats. Vinpocetine improved the echocardiographic parameters and cardiac functional status of rats. Vinpocetine decreased the cardiac biochemical parameters, oxidative stress, inflammatory cytokine levels, cardiomyocyte diameter and fibrosis in rats. Interestingly, expressions of PDE-1, TGF-β and p-Smad 2/3 were ameliorated by vinpocetine alone and in combination with enalapril.
Vinpocetine is a well-known inhibitor of PDE-1 and the protective effect of vinpocetine in DC is exerted by inhibition of PDE-1 and subsequent inhibition of the expression of TGF-β/Smad 2/3.
糖尿病心肌病（DC）是人类糖尿病的严重继发性并发症之一。长春西汀是一种具有多种药理作用的生物碱。本研究旨在探讨长春西汀对大鼠 DC 的作用。
大鼠在第 2 周后给予高脂肪饮食 9 周，并给予链脲佐菌素单次剂量，以诱导 DC。使用 Biopac 系统进行血流动力学评估，以评估大鼠的功能状态。此外，还进行了心脏超声心动图、生化、氧化应激参数和炎性细胞因子水平分析，以及苏木精-伊红和 Masson 三色染色，分别研究组织学变化、心肌细胞直径和纤维化。使用 Western blot/RT-PCR 定量心肌组织中的磷酸二酯酶-1（PDE-1）、转化生长因子-β（TGF-β）和 p-Smad 2/3 的表达。
与糖尿病大鼠相比，长春西汀治疗及其与依那普利联合治疗可降低血糖水平。长春西汀改善了大鼠的超声心动图参数和心脏功能状态。长春西汀降低了大鼠的心脏生化参数、氧化应激、炎性细胞因子水平、心肌细胞直径和纤维化。有趣的是，长春西汀单独和与依那普利联合使用可改善 PDE-1、TGF-β 和 p-Smad 2/3 的表达。
长春西汀是一种众所周知的 PDE-1 抑制剂，长春西汀在 DC 中的保护作用是通过抑制 PDE-1 以及随后抑制 TGF-β/Smad 2/3 的表达来实现的。
