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Astragaloside IV reversed the autophagy and oxidative stress induced by the intestinal microbiota of AIS in mice.黄芪甲苷通过逆转肠道菌群诱导的 AIS 小鼠自噬和氧化应激发挥作用。
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ADME/toxicity prediction and antitumor activity of novel nitrogenous heterocyclic compounds designed by computer targeting of alkylglycerone phosphate synthase.通过计算机靶向烷基甘油磷酸合酶设计的新型含氮杂环化合物的ADME/毒性预测及抗肿瘤活性
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Therapeutic Monoclonal Antibodies Delivery for the Glioblastoma Treatment.治疗性单克隆抗体在脑胶质母细胞瘤治疗中的应用。
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Computer-aided design of temozolomide derivatives based on alkylglycerone phosphate synthase structure with isothiocyanate and their pharmacokinetic/toxicity prediction and anti-tumor activity .基于磷酸烷基甘油合酶结构并带有异硫氰酸酯的替莫唑胺衍生物的计算机辅助设计及其药代动力学/毒性预测和抗肿瘤活性
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Tumor response of temozolomide in combination with morphine in a xenograft model of human glioblastoma.替莫唑胺联合吗啡在人胶质母细胞瘤异种移植模型中的肿瘤反应
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甲酰胺衍生物可诱导U251胶质瘤细胞系发生凋亡。

Carboxamide derivatives induce apoptosis in the U251 glioma cell line.

作者信息

Yan Tao, Zhuang Junxue, He Lu

机构信息

Department of Pharmacy, Tianjin Huanhu Hospital, Tianjin 300350, P.R. China.

Department of Pharmacy, Tianjin Baodi Hospital, Baodi Clinical College of Tianjin Medical University, Tianjin 301800, P.R. China.

出版信息

Oncol Lett. 2019 Aug;18(2):1409-1414. doi: 10.3892/ol.2019.10434. Epub 2019 Jun 4.

DOI:10.3892/ol.2019.10434
PMID:31423205
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6607392/
Abstract

Glioma is a malignant tumor that is frequently treated using chemotherapy. The aim of the present study was to examine the antitumor activity of two novel carboxamide derivatives in glioma, and investigate the underlying mechanisms. Two previously designed and synthesized carboxamide derivatives were selected and their effects on glioma cells were evaluated. Specifically, assays to evaluate proliferation, apoptosis, oxidation, caspase-3, -8 and -9 activity, and the expression of Bcl-2 and surviving in glioma cells were conducted. The carboxamide derivatives were revealed to inhibit proliferation, as well as to induce apoptosis and oxidative damage in glioma U251 cells. In addition, the carboxamide derivatives increased the activity of caspase-3, -8 and -9, and suppressed the expression of Bcl-2 and survivin. These findings demonstrate that the carboxamide derivatives displayed antitumor activity against glioma , which may have been mediated via the induction of oxidative damage and apoptosis.

摘要

神经胶质瘤是一种常采用化疗进行治疗的恶性肿瘤。本研究的目的是检测两种新型羧酰胺衍生物对神经胶质瘤的抗肿瘤活性，并探究其潜在机制。选择了两种先前设计并合成的羧酰胺衍生物，并评估了它们对神经胶质瘤细胞的作用。具体而言，进行了评估神经胶质瘤细胞增殖、凋亡、氧化、半胱天冬酶-3、-8和-9活性以及Bcl-2和存活蛋白表达的实验。结果显示，羧酰胺衍生物可抑制神经胶质瘤U251细胞的增殖，并诱导其凋亡和氧化损伤。此外，羧酰胺衍生物可增加半胱天冬酶-3、-8和-9的活性，并抑制Bcl-2和存活蛋白的表达。这些发现表明，羧酰胺衍生物对神经胶质瘤具有抗肿瘤活性，其机制可能是通过诱导氧化损伤和凋亡来介导的。