In-vitro antidiabetic activity of a Bistorta officinalis Delarbre root extract can not be confirmed in the in-vivo models hen's egg test and Drosophila melanogaster.

IF 2 4区 医学 Q3 PHYSIOLOGY
I Bauer, G Rimbach, S Nevermann, C Neuhauser, B Schwarzinger, C Schwarzinger, J Weghuber, K Luersen
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引用次数: 0

Abstract

The potential of plant bioactives for the prevention and therapy of diabetes is increasingly being recognized. In the present study we investigated the antidiabetic properties of an aqueous Bistorta officinalis Delarbre extract (BODE) by employing both in-vitro assays and in-vivo models. Multiple targets in glucose homeostasis which are involved in the regulation of the blood glucose level were affected by BODE in-vitro. The extract exhibited inhibitory activities towards the intestinal carbohydrate-hydrolysing enzymes α-amylase and α-glucosidase with IC50 values of 81.5 μg/mL and 8.4 μg/mL, respectively. Furthermore, moderate reduction of the dipeptidyl peptidase-4 (DPP4) enzyme activity was evident when tested in the presence of 1.0 mg/mL BODE. A significant inhibition of the intestinal glucose transporter sodium-dependent glucose transporter 1 (SGLT1) in response to 1.0 mg/mL BODE was shown for Caco-2 cells mounted in Ussing chambers. High performance liquid chromatography-mass spectrometry analyses of the BODE revealed several plant bioactives including gallotannins, catechins and chlorogenic acid. Although our in-vitro data were promising, BODE-supplementation in the model organism Drosophila melanogaster lacked to confirm the antidiabetic effect of the extract in-vivo. Moreover, BODE failed to reduce blood glucose levels in chicken embryos (in-ovo). Hence, BODE is probably not a suitable candidate for developing a pharmaceutical against diabetes mellitus.

马齿苋根提取物的体外抗糖尿病活性在体内模型、鸡蛋试验和黑腹果蝇试验中未得到证实。
植物生物活性物质在预防和治疗糖尿病方面的潜力日益被人们所认识。在本研究中,我们通过体外实验和体内模型研究了水相巴戟天提取物(BODE)的抗糖尿病特性。BODE对体外葡萄糖稳态中参与血糖水平调节的多个靶点产生影响。提取物对肠道糖水解酶α-淀粉酶和α-葡萄糖苷酶具有抑制作用,IC50值分别为81.5 μg/mL和8.4 μg/mL。此外,当1.0 mg/mL BODE存在时,二肽基肽酶-4 (DPP4)酶活性明显降低。在Ussing室中,小肠葡萄糖转运体钠依赖性葡萄糖转运体1 (SGLT1)对1.0 mg/mL BODE有明显的抑制作用。高效液相色谱-质谱联用分析显示其含有没食子单宁、儿茶素和绿原酸等多种植物活性成分。尽管我们的体外实验数据很有希望,但在模式生物黑腹果蝇中补充bode还不能证实该提取物在体内的抗糖尿病作用。此外,BODE不能降低鸡胚胎(卵内)的血糖水平。因此,BODE可能不是开发抗糖尿病药物的合适候选者。
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来源期刊
CiteScore
4.00
自引率
22.70%
发文量
0
审稿时长
6-12 weeks
期刊介绍: Journal of Physiology and Pharmacology publishes papers which fall within the range of basic and applied physiology, pathophysiology and pharmacology. The papers should illustrate new physiological or pharmacological mechanisms at the level of the cell membrane, single cells, tissues or organs. Clinical studies, that are of fundamental importance and have a direct bearing on the pathophysiology will also be considered. Letters related to articles published in The Journal with topics of general professional interest are welcome.
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