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甜菊叶和钩藤提取物 GlucoMedix® 可降低大鼠模型的高血糖、高血脂和高血压,且无毒性:代谢综合征的治疗方法。

GlucoMedix®, an extract of Stevia rebaudiana and Uncaria tomentosa, reduces hyperglycemia, hyperlipidemia, and hypertension in rat models without toxicity: a treatment for metabolic syndrome.

机构信息

Department of Cellular and Molecular Sciences, Section of Pharmaceutical Sciences, Faculty of Sciences and Philosophy, Universidad Peruana Cayetano Heredia, Lima, Peru.

Quality Control Service, Research and Development Laboratories, Universidad Peruana Cayetano Heredia, Lima, Peru.

出版信息

BMC Complement Med Ther. 2022 Mar 8;22(1):62. doi: 10.1186/s12906-022-03538-9.

Abstract

BACKGROUND

The objective of this in vivo study is to evaluate in five rat models the pharmacologic effects and toxicity of a commercial hydro-alcoholic extract, GlucoMedix®, derived from Stevia rebaudiana and the pentacyclic chemotype of Uncaria Tomentosa (Willd.) DC, for use as a treatment for metabolic syndrome. The extract contains phytochemicals of Stevia (e.g., steviol glycosides) and Uncaria (e.g., pentacyclic oxindole alkaloids, but lacks tetracyclic oxindole alkaloids).

METHODS

The pharmacologic assessments in three rat models include reductions in chemically induced hyperglycemia, hyperlipidemia (cholesterol and triglycerides), and hypertension, all of which are comorbidities of metabolic syndrome. Acute toxicity and 28-day subacute toxicity were assessed in rat models at doses higher than those used in the efficacy models.

RESULTS

The acute oral toxicity was evaluated in Holtzman rats and the extract did not produce acute toxic effects or lethality, with the LD > 5000 mg/kg (extract wet weight). Furthermore, subacute oral toxicity was evaluated in rats for 28 days at daily doses as high as 2000 mg/kg without toxicity or abnormal clinical chemistry or hematological effects. Daily oral doses of 250 - 1000 mg/kg were used to evaluate the treatment effects in hyperglycemic (alloxan-induced and glibenclamide-controlled), hyperlipidemic (cholesterol-induced and atorvastatin-controlled), and hypertensive (L-NAME-induced and enalapril-controlled) rat models. Alloxan-induced hyperglycemia was reduced in a dose-dependent manner within 28 days or less. Cholesterol-induced hyperlipidemic rats exhibited dose-dependent reductions in cholesterol and triglycerides at 21 days. Furthermore, GlucoMedix® produced a dose-dependent decrease in systolic and diastolic arterial blood pressure in L-NAME-induced hypertensive rats at 28 days.

CONCLUSIONS

The five in vivo rat models revealed that the all-natural phytotherapy GlucoMedix® is a safe and effective treatment for hyperglycemia, hyperlipidemia, and hypertension. This extract is expected to affect multiple comorbidities of metabolic syndrome, without any acute or subacute oral toxicity in humans. Although multiple prescription drugs are well known for the treatment of individual comorbidities of metabolic syndrome, no drug monotherapy concurrently treats all three comorbidities.

摘要

背景

本体内研究的目的是在五种大鼠模型中评估一种商业性的水醇提取物 GlucoMedix®的药理作用和毒性,该提取物源自甜叶菊(Stevia rebaudiana)和钩藤(Uncaria Tomentosa(Willd.)DC)的五环化学型,用于治疗代谢综合征。该提取物含有甜菊(例如,甜菊糖苷)和钩藤(例如,五环吲哚生物碱,但缺乏四环吲哚生物碱)的植物化学物质。

方法

三种大鼠模型中的药理评估包括降低化学诱导的高血糖、高血脂(胆固醇和甘油三酯)和高血压,这些都是代谢综合征的合并症。在高于功效模型中使用的剂量下,在大鼠模型中评估急性毒性和 28 天亚急性毒性。

结果

在霍尔茨曼大鼠中评估了急性口服毒性,提取物没有产生急性毒性作用或致死作用,LD>5000mg/kg(提取物湿重)。此外,在大鼠中进行了为期 28 天的亚急性口服毒性评估,每日剂量高达 2000mg/kg,没有毒性或异常的临床化学或血液学效应。每日口服剂量为 250-1000mg/kg,用于评估在高血糖(均氧诱导和格列本脲控制)、高血脂(胆固醇诱导和阿托伐他汀控制)和高血压(L-NAME 诱导和依那普利控制)大鼠模型中的治疗效果。在 28 天或更短的时间内,均氧诱导的高血糖呈剂量依赖性降低。胆固醇诱导的高血脂大鼠在 21 天内表现出胆固醇和甘油三酯的剂量依赖性降低。此外,GlucoMedix®在 28 天内使 L-NAME 诱导的高血压大鼠的收缩压和舒张压呈剂量依赖性降低。

结论

五种体内大鼠模型表明,全天然植物疗法 GlucoMedix®是治疗高血糖、高血脂和高血压的安全有效方法。该提取物预计会影响代谢综合征的多种合并症,而不会对人类造成任何急性或亚急性口服毒性。虽然多种处方药因治疗代谢综合征的单个合并症而广为人知,但没有药物单一疗法同时治疗所有三种合并症。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6999/8905912/b163d67d0b62/12906_2022_3538_Fig1_HTML.jpg

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