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首页> 外文期刊>RSC Advances >Molecular docking analysis and anti-hyperglycaemic activity of Synacinn (TM) in streptozotocin-induced rats
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Molecular docking analysis and anti-hyperglycaemic activity of Synacinn (TM) in streptozotocin-induced rats

机译：链脲佐菌素诱导大鼠Sysacinn（TM）的分子对接分析及抗高血糖活性

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摘要

Synacinn (TM) is a standardized polyherbal supplement formulated fromCinnamomum zeylanicumBlume,Curcuma zanthorrhizaRoxb.,Syzygium polyanthum(Wight) Walp.,Orthosiphon stamineusBenth. andAndrographis paniculata(Burm.f.) Nees. It is designed for the synergistic treatment of diabetes mellitus and its complications. Although the beneficial effects are yet to be verified scientifically, it is traditionally used to improve general health in patients with diabetes. This study aimed to evaluate the anti-hyperglycemic effects of Synacinn (TM) in a streptozotocin-induced type 1 diabetes rat model. Initially, Synacinn (TM) was used forin vivoacute oral toxicity tests and 14 day repeated dose toxicity tests to determine the toxicity levels. An efficacy study of Synacinn (TM) was carried outviathe oral administration of 10, 50, 100, 250, and 250 (b.i.d.) mg kg(-1)doses to streptozotocin-induced diabetic rats. After 28 days, blood serum was collected to measure the fasting blood glucose, triglyceride, cholesterol, alanine aminotransferase, alkaline phosphatase, creatinine, and uric acid levels. The liver, kidney, and pancreas structures were histopathologically analyzed.In silicobinding interaction studies of five phytochemicals in Synacinn (TM) identifiedviaHPLC with glucokinase were performed using molecular docking analysis. The results showed that although no mortality was observed during the acute oral toxicity tests, notable damage to the liver and kidney occurred during the 14 day repeated dose testing at Synacinn (TM) levels of 600 mg kg(-1)and 2000 mg kg(-1). Treatment with 250 mg kg(-1)(b.i.d.) Synacinn (TM) of the streptozotocin-induced type 1 diabetic rats significantly (p< 0.05) improved the fasting blood glucose (59%), triglyceride (58%), cholesterol (47%), alanine aminotransferase (60%), alkaline phosphatase (90%), and creatinine (32%) levels. Synacinn (TM) also improved the relative weights of liver (35%), kidney (36%), and pancreatic (36%) tissue. Histological analysis showed improvements in the conditions of the central vein of the liver, the kidney Bowman's capsule and glomerulus, and the pancreatic islets of Langerhans. HPLC analysis of a standardized extract identified five active phytochemicals: andrographolide (17.36 mg g(-1)), gallic acid (11.5 mg g(-1)), curcumin (2.75 mg g(-1)), catechin (3.9 mg g(-1)), and rosmarinic acid (5.54 mg g(-1)). Molecular docking studies with glucokinase showed that andrographolide yields the highest binding energy (-12.1 kcal mol(-1)), followed by catechin (-10.2 kcal mol(-1)), rosmarinic acid (-8.6 kcal mol(-1)), curcumin (-7.8 kcal mol(-1)), and gallic acid (-5.6 kcal mol(-1)). These current findings suggest that Synacinn (TM) at a dose of 250 mg kg(-1)was non-toxic to rats. A twice-daily 250 mg kg(-1)dose of Synacinn (TM) is an effective anti-hyperglycemic agent, lowering blood glucose, triglyceride, and cholesterol levels, and assisting the recovery of organ impairment caused by streptozotocin in type 1 diabetic rats.
机译：Synacinn（TM）是一种标准化的多草药补充剂制定fromCinnamomum zeylanicumBlume，莪术zanthorrhizaRoxb，蒲桃滇南（怀特）Walp，鸡脚参属stamineusBenth。 andAndrographis穿心莲（Burm.f）穿心莲。它是专为糖尿病及其并发症的协同治疗。虽然有益的影响还有待科学验证的，它是传统用来改善整体健康的糖尿病患者。这项研究的目的是评估Synacinn（TM）的在链脲佐菌素引起的1型糖尿病大鼠模型的抗高血糖作用。最初，Synacinn（TM）用于forin vivoacute口服毒性试验第14天反复给药毒性试验以确定的毒性水平。 Synacinn（TM）的功效研究进行的10，50，100，250，和250（b.i.d.的）outviathe口服给药毫克公斤（-1）剂量链脲佐菌素诱导的糖尿病大鼠。后28天，血收集血清以测量空腹血糖，甘油三酯，胆固醇，谷丙转氨酶，碱性磷酸酶，肌酐和尿酸水平。肝，肾，胰腺和结构是组织病理学五个植物化学物质analyzed.In silicobinding相互作用研究中Synacinn与葡萄糖激酶使用分子对接分析进行（TM）identifiedviaHPLC。结果表明，尽管在急性口服毒性试验中没有观察到死亡率，肝肾损害显着在2000年第14天重复剂量在Synacinn（TM）的600水平测试毫克公斤（-1）和毫克公斤发生（ -1）。治疗用250mg千克（-1）（BID）Synacinn的链脲佐菌素诱导的1型糖尿病大鼠（TM）显著（P <0.05）提高了空腹血糖（59％），甘油三酯（58％），胆固醇（47 ％），丙氨酸氨基转移酶（60％），碱性磷酸酶（90％），和肌酐（32％）的水平。 Synacinn（TM）也得到了改善肝脏（35％），肾（36％）和胰腺（36％）的组织的相对权重。组织学分析显示，在肝脏，肾脏肾小球囊和肾小球，和朗格汉斯胰岛的中央静脉条件的改善。一个标准化提取物确定了五个活性的植物化学物质的HPLC分析：穿心莲内酯（17.36毫克克（-1）），没食子酸（11.5毫克克（-1）），姜黄素（2.75毫克克（-1）），儿茶素（3.9毫克克（-1）），和迷迭香酸（5.54毫克克（-1））。与葡萄糖激酶分子对接研究表明，穿心莲内酯的产率最高的结合能量（千卡-12.1摩尔（-1）），其次是儿茶素（-10.2千卡摩尔（-1）），迷迭香酸（-8.6千卡摩尔（-1）） ，姜黄素（-7.8千卡摩尔（-1）），没食子酸（-5.6千卡摩尔（-1））。这些目前的研究结果表明，Synacinn（TM），剂量为250毫克公斤（-1）是无毒的大鼠。甲每日两次250mg的千克（-1）Synacinn（TM）的剂量是一种有效的抗高血糖剂，降血糖，甘油三酯和胆固醇水平，并协助在1型糖尿病大鼠引起菌素器官损伤的恢复。

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