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杨叶肖槿金属配合物作为潜在过氧化物酶体增殖物激活受体-γ激动剂的分离、表征及临床前研究

The isolation, Characterization and Preclinical Studies of Metal Complex of Thespesia populnea for the Potential Peroxisome Proliferator-activated Receptors-γ Agonist Activity.

作者信息

Phanse Mohini Ashok, Patil Manohar Janardhan, Abbulu Konde

机构信息

Department of Pharmacognosy, Modern College of Pharmacy, Nigdi, India.

Department of Pharmacognosy, Maratha Mitramandal College of Pharmacy, Kalewadi, Pune, Maharashtra, India.

出版信息

Pharmacogn Mag. 2015 Oct;11(Suppl 3):S434-8. doi: 10.4103/0973-1296.168984.

DOI:10.4103/0973-1296.168984
PMID:26929578
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4745214/
Abstract

BACKGROUND

Diabetes mellitus is an international public health problem since ancient days. The condition is predominantly more severe in developing countries like India where, life is more sedentary due to the even changing lifestyles in this fast-paced global scenario. Thespesia populnea is widely used in the ayurvedic system of medicine for treatment of diabetes mellitus in India for years. The aim of this work is to explore the anti-diabetic activity of the isolated compound.

MATERIALS AND METHODS

The sesquiterpene isolated from hexane fraction of bark of T. populnea modified synthetically then identified by using analytical techniques such as electron paramagnetic resonance spectra for confirmation and the anti-diabetic activity was evaluated by anti-hyperglycemic, hypoglycemic potential.

RESULT

In the present work, we have studied the anti-hyperglycemic and hypoglycemic activity of the vanadium complex in glucose loaded and normal animals were shown significantly decreased in plasma blood glucose level. The results derived from preclinical studies confirm the potential of new sesquiterpene.

CONCLUSION

The findings could provide evidence regarding the anti-diabetic potential of T. populnea by lowering blood glucose level.

SUMMARY

Thespesia populnea is widely used in the ayurvedic system of medicine for treatment of diabetes in India. Present study aimed to explore the anti diabetic potential of isolated compound. Isolation of sesquiterpene from hexane fraction of bark of Thespesia populnea and modified synthetically then authenticated by using analytical techniques such as electron paramagnetic resonance spectra for confirmation. The modified complex was further assessed for its anti diabetic property in glucose loaded rats. Vanadium complex demonstrated significant reduction in plasma blood glucose level in glucose loaded animals. The results derived from preclinical studies confirm the potential of new sesquiterpene. The present findings conclude that anti diabetic potential of Thespesia populnea could be due to lowering blood glucose level by acting on PPAR-γ receptor.

摘要

背景

糖尿病自古以来就是一个国际公共卫生问题。在印度等发展中国家,这种疾病尤为严重,在这个快节奏的全球环境中,生活方式不断变化,人们的生活更加久坐不动。多年来,杨叶肖槿在印度阿育吠陀医学体系中被广泛用于治疗糖尿病。这项工作的目的是探索分离出的化合物的抗糖尿病活性。

材料与方法

从杨叶肖槿树皮的己烷馏分中分离出倍半萜,然后进行合成修饰,通过电子顺磁共振光谱等分析技术进行鉴定以确认其结构,并通过抗高血糖、降血糖潜力评估其抗糖尿病活性。

结果

在本研究中,我们研究了钒配合物在葡萄糖负荷动物和正常动物中的抗高血糖和降血糖活性,结果显示血浆血糖水平显著降低。临床前研究的结果证实了新倍半萜的潜力。

结论

这些发现可以为杨叶肖槿通过降低血糖水平而具有抗糖尿病潜力提供证据。

总结

杨叶肖槿在印度阿育吠陀医学体系中被广泛用于治疗糖尿病。本研究旨在探索分离出的化合物的抗糖尿病潜力。从杨叶肖槿树皮的己烷馏分中分离出倍半萜并进行合成修饰,然后通过电子顺磁共振光谱等分析技术进行鉴定以确认其结构。进一步评估修饰后的配合物在葡萄糖负荷大鼠中的抗糖尿病特性。钒配合物在葡萄糖负荷动物中显示出血浆血糖水平显著降低。临床前研究的结果证实了新倍半萜的潜力。目前的研究结果表明,杨叶肖槿的抗糖尿病潜力可能是由于通过作用于PPAR-γ受体降低血糖水平。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/76e8/4745214/da315c88b6db/PM-11-434-g007.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/76e8/4745214/d35555e2e946/PM-11-434-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/76e8/4745214/2b0e11455282/PM-11-434-g002.jpg
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