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血根碱、小檗碱及升麻和珊瑚菜提取物对造血系统癌细胞系的细胞毒性和促凋亡作用。

Cytotoxic and Proapoptotic Activity of Sanguinarine, Berberine, and Extracts of L. and DC. toward Hematopoietic Cancer Cell Lines.

机构信息

Chair and Department of Biology and Genetics, Medical University of Lublin, 4a Chodźki St., 20-093 Lublin, Poland.

Chair and Department of Medicinal Chemistry, Medical University of Lublin, 4 Jaczewskiego St., 20-090 Lublin, Poland.

出版信息

Toxins (Basel). 2019 Aug 23;11(9):485. doi: 10.3390/toxins11090485.

Abstract

Isoquinoline alkaloids belong to the toxic secondary metabolites occurring in plants of many families. The high biological activity makes these compounds promising agents for use in medicine, particularly as anticancer drugs. The aim of our study was to evaluate the cytotoxicity and proapoptotic activity of sanguinarine, berberine, and extracts of L. and DC. IC10, IC50, and IC90 doses were established toward hematopoietic cancer cell lines using trypan blue staining. Alterations in the expression of 18 apoptosis-related genes in cells exposed to IC10, IC50, and IC90 were evaluated using real-time PCR. Sanguinarine and L. extract exhibit significant cytotoxicity against all studied cell lines. Lower cytotoxic activity was demonstrated for berberine. DC. extract had no influence on cell viability. Berberine, sanguinarine, and L. extract altered the expression of apoptosis-related genes in all tested cell lines, indicating the induction of apoptosis. The presented study confirmed the substantial cytotoxicity and proapoptotic activity of sanguinarine, berberine, and L. extract toward the studied hematopoietic cell lines, which indicates the utility of these substances in anticancer therapy.

摘要

异喹啉生物碱属于存在于许多科植物中的毒性次生代谢物。这些化合物具有很高的生物活性,因此有望被用作药物,特别是抗癌药物。我们的研究旨在评估血根碱、小檗碱和白屈菜、DC 的提取物的细胞毒性和促凋亡活性。使用台盼蓝染色法确定了针对造血癌细胞系的 IC10、IC50 和 IC90 剂量。使用实时 PCR 评估了暴露于 IC10、IC50 和 IC90 的细胞中 18 个与凋亡相关基因的表达变化。血根碱和白屈菜提取物对所有研究的细胞系均表现出显著的细胞毒性。小檗碱的细胞毒性较低。DC. 提取物对细胞活力没有影响。小檗碱、血根碱和白屈菜提取物改变了所有测试细胞系中与凋亡相关基因的表达,表明诱导了细胞凋亡。本研究证实了血根碱、小檗碱和白屈菜提取物对研究中的造血细胞系具有显著的细胞毒性和促凋亡活性,这表明这些物质在抗癌治疗中的应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bb5/6784183/64039416cd41/toxins-11-00485-g001.jpg

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