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黄芩苷介导的癌症关键信号通路调控。

Baicalin mediated regulation of key signaling pathways in cancer.

作者信息

Singh Shilpi, Meena Abha, Luqman Suaib

机构信息

Bioprospection and Product Development Division, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow, 226015, Uttar Pradesh, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, Uttar Pradesh, India.

Bioprospection and Product Development Division, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow, 226015, Uttar Pradesh, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, Uttar Pradesh, India.

出版信息

Pharmacol Res. 2021 Feb;164:105387. doi: 10.1016/j.phrs.2020.105387. Epub 2020 Dec 19.

Abstract

Baicalin has been widely investigated against different types of malignancies both at the cellular and molecular levels over the past few years. Due to its remarkable anti-proliferative potential in numerous cancer cell lines, it has created immense interest as a potential chemotherapeutic modality compared to other flavonoids. Thus, this review focuses on the recent accomplishments of baicalin and its limitations in cancer prevention and treatment. Further, combination studies and nanoformulations using baicalin to treat cancer along with the metabolism, bioavailability, toxicity, and pharmacokinetics have been discussed. The present review explains biological source, and anti-proliferative potential of baicalin against cancers including breast, colon, hepatic, leukemia, lung, and skin, as well as the relevant mechanism of action to modulate diverse signaling pathways including apoptosis, cell cycle, invasion, and migration, angiogenesis, and autophagy. The anticancer mechanism of baicalin in orthotropic and xenograft mice models have been deliberated. The combination studies of baicalin in novel therapies as chemotherapeutic adjuvants have also been summarized. The low bioavailability, fast metabolism, and poor solubility, and other significant factors that limit the clinical use of baicalin have been examined as a challenge. The improvement in the pharmacokinetics and pharmacodynamics of baicalin with newer approaches and the gaps are highlighted, which could establish baicalin as an effective and safe compound for cancer treatment as well as help to translate its potential from bench to bedside.

摘要

在过去几年中,黄芩苷已在细胞和分子水平上针对不同类型的恶性肿瘤进行了广泛研究。由于其在众多癌细胞系中具有显著的抗增殖潜力,与其他黄酮类化合物相比,它作为一种潜在的化疗药物引起了极大的关注。因此,本综述重点关注黄芩苷在癌症预防和治疗方面的最新成果及其局限性。此外,还讨论了使用黄芩苷治疗癌症的联合研究和纳米制剂,以及其代谢、生物利用度、毒性和药代动力学。本综述解释了黄芩苷的生物来源及其对乳腺癌、结肠癌、肝癌、白血病、肺癌和皮肤癌等癌症的抗增殖潜力,以及调节包括凋亡、细胞周期、侵袭和迁移、血管生成和自噬等多种信号通路的相关作用机制。还探讨了黄芩苷在原位和异种移植小鼠模型中的抗癌机制。还总结了黄芩苷作为化疗佐剂在新型疗法中的联合研究。低生物利用度、快速代谢、低溶解度以及其他限制黄芩苷临床应用的重要因素已被视为一项挑战。强调了采用新方法改善黄芩苷药代动力学和药效学方面的进展以及存在的差距,这可能使黄芩苷成为一种有效且安全的癌症治疗化合物,并有助于将其潜力从实验室转化为临床应用。

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