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二肽基肽酶-4抑制剂对结肠癌抗癌作用的评估——一项体外研究

Evaluation of Anti Cancer Effects of DPP-4 Inhibitors in Colon Cancer- An Invitro Study.

作者信息

Amritha C A, Kumaravelu Punnagai, Chellathai D Darling

机构信息

Postgraduate Student, Department of Pharmacology, Sri Ramachandra Medical College & Research Institute , Porur, Chennai, India .

Associate Professor, Department of Pharmacology, Sri Ramachandra Medical College & Research Institute , Porur, Chennai, India .

出版信息

J Clin Diagn Res. 2015 Dec;9(12):FC14-6. doi: 10.7860/JCDR/2015/16015.6979. Epub 2015 Dec 1.

Abstract

INTRODUCTION

Among the oral anti-diabetic drugs, Dipeptidyl peptidase - 4(DPP-4) inhibitor is an emerging class of drugs. Inhibitors of DPP-4 enzyme like Sitagliptin and Vildagliptin have shown Anti-oxidant properties in many studies, both invivo and invitro. It has also been characterized as an apoptotic agent on pancreatic cancer cells. In the following study, Anticancer effect of DPP 4 inhibitors on colon cell lines (HT-29) using MTT assay- {3 -4, 5-dimethyl (thiazol - 2 -yl) -3, 5- dimethyl tetrazolium bromide} assay was elucidated.

AIM

To elucidate and compare the anticancer potential of two DPP 4 inhibitors using in-vitro MTT assay on colorectal cell lines (HT-29).

MATERIALS AND METHODS

We treated HT-29 cell lines with two DPP 4 inhibitors. HT-29 cells were incubated at 37(0)C and drug samples were added in various concentrations and incubated for 24 hours. MTT dye was added to the sample and it was incubated for 4 hours. One ml of DMSO was added Using an Ultraviolet-Spectrophotometer, measurement of absorbance was done at 570nm following which the half maximal inhibitory concentration was graphically estimated in relation to the percentage of viability of the cell and the sample concentration.

RESULTS

We found that both the drugs have shown anticancer activity starting from low to high concentrations when compared with the control using MTT assay. The IC 50 value of Sitagliptin is 31.2 mcg/ml and Vildagliptin is 125 mcg/ml.

CONCLUSION

From this study, we found that the drugs have significant Anti-Cancer property, which would probably play a role as cytotoxic agent in tumour cells. Sitagliptin was found to be more potent than Vildagliptin in colon cancer cell lines.

摘要

引言

在口服抗糖尿病药物中,二肽基肽酶-4(DPP-4)抑制剂是一类新兴药物。西他列汀和维格列汀等DPP-4酶抑制剂在许多体内和体外研究中均显示出抗氧化特性。它还被表征为胰腺癌细胞的凋亡剂。在以下研究中,使用MTT法(3-4,5-二甲基(噻唑-2-基)-3,5-二甲基四氮唑溴盐法)阐明了DPP 4抑制剂对结肠细胞系(HT-29)的抗癌作用。

目的

使用体外MTT法阐明并比较两种DPP 4抑制剂对结肠直肠细胞系(HT-29)的抗癌潜力。

材料与方法

我们用两种DPP 4抑制剂处理HT-29细胞系。HT-29细胞在37℃孵育,加入不同浓度的药物样品并孵育24小时。向样品中加入MTT染料并孵育4小时。加入1ml二甲基亚砜,使用紫外分光光度计在570nm处测量吸光度,然后根据细胞活力百分比和样品浓度以图形方式估算半数最大抑制浓度。

结果

我们发现,与对照组相比,使用MTT法时,两种药物从低浓度到高浓度均显示出抗癌活性。西他列汀的IC50值为31.2 mcg/ml,维格列汀的IC50值为125 mcg/ml。

结论

从这项研究中,我们发现这些药物具有显著的抗癌特性,可能在肿瘤细胞中作为细胞毒性剂发挥作用。在结肠癌细胞系中,西他列汀比维格列汀更有效。

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