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黄芩苷和黄芩素增强阿霉素和多西紫杉醇对 MCF-7 乳腺癌细胞的细胞毒性、促凋亡活性和遗传毒性。

Baicalin and Baicalein Enhance Cytotoxicity, Proapoptotic Activity, and Genotoxicity of Doxorubicin and Docetaxel in MCF-7 Breast Cancer Cells.

机构信息

Department of Oncobiology and Epigenetics, Faculty of Biology and Environmental Protection, University of Lodz, Pomorska 141/143 Str., 90-236 Lodz, Poland.

Department of Medical Biophysics, Faculty of Biology and Environmental Protection, University of Lodz, Pomorska 141/143 Str., 90-236 Lodz, Poland.

出版信息

Molecules. 2024 May 25;29(11):2503. doi: 10.3390/molecules29112503.

DOI:10.3390/molecules29112503
PMID:38893380
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11173533/
Abstract

Breast cancer is a major health concern and the leading cause of death among women worldwide. Standard treatment often involves surgery, radiotherapy, and chemotherapy, but these come with side effects and limitations. Researchers are exploring natural compounds like baicalin and baicalein, derived from the plant, as potential complementary therapies. This study investigated the effects of baicalin and baicalein on the cytotoxic, proapoptotic, and genotoxic activity of doxorubicin and docetaxel, commonly used chemotherapeutic drugs for breast cancer. The analysis included breast cancer cells (MCF-7) and human endothelial cells (HUVEC-ST), to assess potential effects on healthy tissues. We have found that baicalin and baicalein demonstrated cytotoxicity towards both cell lines, with more potent effects observed in baicalein. Both flavonoids, baicalin (167 µmol/L) and baicalein (95 µmol/L), synergistically enhanced the cytotoxic, proapoptotic, and genotoxic activity of doxorubicin and docetaxel in breast cancer cells. In comparison, their effects on endothelial cells were mixed and depended on concentration and time. The results suggest that baicalin and baicalein might be promising complementary agents to improve the efficacy of doxorubicin and docetaxel anticancer activity. However, further research is needed to validate their safety and efficacy in clinical trials.

摘要

乳腺癌是一个主要的健康问题,也是全球女性死亡的主要原因。标准治疗通常包括手术、放疗和化疗,但这些治疗方法都有副作用和局限性。研究人员正在探索黄芩素和黄芩苷等天然化合物,这些化合物来源于植物,可能是潜在的辅助治疗方法。本研究调查了黄芩素和黄芩苷对阿霉素和多西紫杉醇(常用于乳腺癌的化疗药物)的细胞毒性、促凋亡和遗传毒性活性的影响。分析包括乳腺癌细胞(MCF-7)和人内皮细胞(HUVEC-ST),以评估对健康组织的潜在影响。我们发现,黄芩素和黄芩苷对两种细胞系均表现出细胞毒性,黄芩苷的作用更强。两种黄酮类化合物,黄芩素(167µmol/L)和黄芩苷(95µmol/L),协同增强了阿霉素和多西紫杉醇在乳腺癌细胞中的细胞毒性、促凋亡和遗传毒性活性。相比之下,它们对内皮细胞的影响是混合的,取决于浓度和时间。研究结果表明,黄芩素和黄芩苷可能是提高阿霉素和多西紫杉醇抗癌活性疗效的有前途的辅助剂。然而,需要进一步的临床试验来验证它们的安全性和疗效。

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2
Doxorubicin and other anthracyclines in cancers: Activity, chemoresistance and its overcoming.多柔比星和其他蒽环类药物在癌症中的应用:活性、化学耐药性及其克服。
Mol Aspects Med. 2023 Oct;93:101205. doi: 10.1016/j.mam.2023.101205. Epub 2023 Jul 27.
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Baicalein sensitizes triple negative breast cancer MDA-MB-231 cells to doxorubicin via autophagy-mediated down-regulation of CDK1.
黄芩苷和黄芩素在乳腺癌中的治疗潜力:机制与疗效的系统评价
Curr Issues Mol Biol. 2025 Mar 11;47(3):181. doi: 10.3390/cimb47030181.
黄芩素通过自噬介导的 CDK1 下调使三阴性乳腺癌 MDA-MB-231 细胞对阿霉素敏感。
Mol Cell Biochem. 2023 Jul;478(7):1519-1531. doi: 10.1007/s11010-022-04597-9. Epub 2022 Nov 21.
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Baicalin regulates TLR4/IκBα/NFκB signaling pathway to alleviate inflammation in Doxorubicin related cardiotoxicity.黄芩苷通过调控 TLR4/IκBα/NFκB 信号通路减轻蒽环类药物相关性心脏毒性的炎症反应。
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