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提取物显示具有抗高血糖活性,可逆转氧化应激,并对链脲佐菌素诱导的糖尿病大鼠的肝损伤具有保护作用。

Extract of Shows Antihyperglycemic Activity, Reverses Oxidative Stress, and Protects against Liver Damage in Streptozotocin-induced Diabetic Rats.

作者信息

Elbanna Ahmed H, Nooh Mohammed M, Mahrous Engy A, Khaleel Amal E, Elalfy Taha S

机构信息

Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

Department of Biochemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

出版信息

Pharmacogn Mag. 2017 Oct;13(Suppl 3):S607-S612. doi: 10.4103/pm.pm_4_17. Epub 2017 Oct 11.

Abstract

BACKGROUND

Several studies have affirmed the effectiveness of some plants as antihyperglycemic agents.

OBJECTIVE

We investigated the possible effect of leaves extract in reducing hyperglycemia and reversing signs of organ damage associated with diabetes in streptozotocin (STZ) rat model.

MATERIALS AND METHODS

Both polar fraction of the leaves (defatted ethanolic extract [DEE]) and nonpolar fraction (-hexane extract) were evaluated for α-glucosidase inhibition and 2,2-diphenyl-1-picrylhydrazyl radical scavenging potential. DEE was selected for further studies and was administered at two doses, i.e., 150 or 300 mg/kg to STZ-diabetic rats for 4 weeks.

RESULTS

Only DEE exhibited antioxidant and antihyperglycemic activities and its oral administration at both dose levels resulted in significant reduction in fasting blood glucose and glycated hemoglobin. Furthermore, signs of oxidative stress as indicated by hepatic reduced glutathione, nitric oxide, and malondialdehyde levels were completely reversed. In addition, histopathological examination and measurement of serum aspartate transaminase and alanine transaminase levels showed that DEE protected the liver from signs of liver pathogenesis when compared to diabetic untreated animals and those treated with metformin. Phytochemical analysis of DEE showed high flavonoids content with quercitrin as the major constituent along with other quercetin glycosides.

CONCLUSION

This study strongly highlights the possible beneficial effect of leaves extract in relieving hyperglycemia and liver damage in STZ-diabetic rats and recommends further investigation of the value of quercetin derivatives in controlling diabetes and ameliorating liver damage associated with it.

SUMMARY

The polar fraction of the leaves (defatted ethanolic extract [DEE]) exhibited both antioxidant activity in 2,2-diphenyl-1-picrylhydrazyl scavenging assay and strong α-glucosidase inhibition while the nonpolar fraction (-hexane extract) failed to show any activity in both assays. DEE was further investigated in streptozotocin-induced diabetic rat model where oral administration of DEE at 2 doses (150 and 300 mg/kg) for 4 weeks resulted in significant reduction in fasting blood glucose and glycated hemoglobin and reversal of oxidative stress signs as indicated by measurement of hepatic reduced glutathione, nitric oxide, and malondialdehyde levels. In addition, histopathological examination and measurement of serum aspartate transaminase and alanine transaminase levels showed that DEE protected the liver from signs of pathogenesis observed in diabetic untreated rats. Phytochemical analysis of DEE showed high flavonoid content with quercitrin as the major constituent (62.9 ± 0.18 mg/mg). ALT: Alanine transaminase, AST: Aspartate transaminase, DEE: Defatted ethanol extract, DPPH: 2,2-diphenyl-1-picrylhydrazyl, FBG: Fasting blood glucose, GAE: Gallic acid equivalent, GSH: Reduced glutathione, Hb1Ac: Glycated hemoglobin, HE: Hexane extract MDA: Malondialdehyde, QE: Quercetin equivalent, STZ: Streptozotocin, TAC: Total antioxidant capacity.

摘要

背景

多项研究证实了某些植物作为抗高血糖药物的有效性。

目的

我们在链脲佐菌素(STZ)诱导的大鼠模型中,研究了[植物名称]叶提取物在降低高血糖以及逆转与糖尿病相关的器官损伤体征方面的潜在作用。

材料与方法

评估了[植物名称]叶的极性部分(脱脂乙醇提取物[DEE])和非极性部分(正己烷提取物)对α - 葡萄糖苷酶的抑制作用以及对2,2 - 二苯基 - 1 - 苦基肼自由基的清除能力。选择DEE进行进一步研究,并以150或300 mg/kg这两种剂量给予STZ诱导的糖尿病大鼠,持续4周。

结果

只有DEE表现出抗氧化和抗高血糖活性,以两种剂量水平口服DEE均能显著降低空腹血糖和糖化血红蛋白。此外,肝脏中还原型谷胱甘肽、一氧化氮和丙二醛水平所表明的氧化应激体征完全得到逆转。另外,组织病理学检查以及血清天冬氨酸转氨酶和丙氨酸转氨酶水平的测量结果表明,与未治疗的糖尿病动物和用二甲双胍治疗的动物相比,DEE保护肝脏免受肝脏病变体征的影响。DEE的植物化学分析显示黄酮类化合物含量高,以槲皮苷为主要成分,还有其他槲皮素糖苷。

结论

本研究强烈突出了[植物名称]叶提取物在缓解STZ诱导的糖尿病大鼠高血糖和肝脏损伤方面可能具有的有益作用,并建议进一步研究槲皮素衍生物在控制糖尿病及改善与之相关的肝脏损伤方面的价值。

总结

[植物名称]叶的极性部分(脱脂乙醇提取物[DEE])在2,2 - 二苯基 - 1 - 苦基肼清除试验中表现出抗氧化活性,并对α - 葡萄糖苷酶有较强抑制作用,而非极性部分(正己烷提取物)在这两种试验中均未表现出任何活性。在链脲佐菌素诱导的糖尿病大鼠模型中对DEE进行了进一步研究,以150和300 mg/kg这两种剂量口服DEE 4周,导致空腹血糖和糖化血红蛋白显著降低,并且通过测量肝脏中还原型谷胱甘肽、一氧化氮和丙二醛水平表明氧化应激体征得到逆转。此外,组织病理学检查以及血清天冬氨酸转氨酶和丙氨酸转氨酶水平的测量结果表明,DEE保护肝脏免受未治疗糖尿病大鼠中观察到的病变体征的影响。DEE的植物化学分析显示黄酮类化合物含量高,以槲皮苷为主要成分(62.9±0.18 mg/mg)。ALT:丙氨酸转氨酶,AST:天冬氨酸转氨酶,DEE:脱脂乙醇提取物,DPPH:2,2 - 二苯基 - 1 - 苦基肼,FBG:空腹血糖,GAE:没食子酸当量,GSH:还原型谷胱甘肽,Hb1Ac:糖化血红蛋白,HE:正己烷提取物,MDA:丙二醛, QE:槲皮素当量,STZ:链脲佐菌素,TAC:总抗氧化能力

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1eb/5669104/21e6bc809331/PM-13-607-g004.jpg

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