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芦丁和奥利司他通过抗氧化和凋亡作用产生抗肿瘤作用。

Rutin and orlistat produce antitumor effects via antioxidant and apoptotic actions.

机构信息

Department of Pharmacology & Toxicology, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt.

Department of Pharmacology & Toxicology, Faculty of Pharmacy, Sinai University, Ismailia, Egypt.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 2019 Feb;392(2):165-175. doi: 10.1007/s00210-018-1579-0. Epub 2018 Nov 21.

Abstract

Cancer is a broad term used to describe a large number of diseases characterized by uncontrolled cell proliferation that leads to tumor production. Cancer is associated with mutations in genes controlling proliferation and apoptosis, oxidative stress, fatty acid synthase (FAS) expression, and other mechanisms. Currently, most antineoplastic drugs have severe adverse effects and new effective and safe drugs are needed. This study aims to investigate the possible anticancer activity of rutin and orlistat which are both safely used clinically in humans against two breast cancer models (in vivo EAC and in vitro MCF7) and the pancreatic cancer cell line (PANC-1). Our results have shown that both rutin and orlistat exerted an in vivo anticancer activity as evidenced by the decrease in tumor volume, CEA level, cholesterol content, FAS, and the exerted antioxidant action (reduced MDA level and increased GSH content) and through histopathological examination. In addition, both were cytotoxic to MCF-7 and Panc-1 cell lines by promoting apoptosis. In conclusion, the anticancer activity of rutin and orlistat makes them promising candidates for cancer treatment alone or in combination with other anticancer drugs specially that they are used clinically with an acceptable safety profile.

摘要

癌症是一个广义的术语,用于描述大量以不受控制的细胞增殖为特征的疾病,这些疾病会导致肿瘤的产生。癌症与控制增殖和细胞凋亡、氧化应激、脂肪酸合酶 (FAS) 表达和其他机制的基因突变更相关。目前,大多数抗肿瘤药物都有严重的不良反应,因此需要新的有效和安全的药物。本研究旨在研究芦丁和奥利司他可能具有的抗癌活性,这两种药物在临床上都可安全用于人类,针对两种乳腺癌模型(体内 EAC 和体外 MCF7)和胰腺癌细胞系(PANC-1)。我们的研究结果表明,芦丁和奥利司他都具有体内抗癌活性,这一点可通过肿瘤体积、CEA 水平、胆固醇含量、FAS 的降低以及抗氧化作用(降低 MDA 水平和增加 GSH 含量)来证明,并且通过组织病理学检查也得到了证实。此外,芦丁和奥利司他对 MCF-7 和 Panc-1 细胞系都具有细胞毒性,可促进细胞凋亡。总之,芦丁和奥利司他的抗癌活性使它们成为单独或与其他抗癌药物联合治疗癌症的有前途的候选药物,特别是它们在临床上具有可接受的安全性。

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