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黄芩素在抗肿瘤作用及机制方面的最新进展。

The most recent progress of baicalein in its anti-neoplastic effects and mechanisms.

机构信息

The Second Clinical Medical College of Guangzhou University of Chinese Medicine, the Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, PR China.

The Second Clinical Medical College of Guangzhou University of Chinese Medicine, the Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, PR China.

出版信息

Biomed Pharmacother. 2024 Jul;176:116862. doi: 10.1016/j.biopha.2024.116862. Epub 2024 Jun 7.

Abstract

Problems, such as toxic side effects and drug resistance of chemoradiotherapy, target therapy and immunotherapy accompanying the current anti-cancer treatments, have become bottlenecks limiting the clinical benefit for patients. Therefore, it is urgent to find promising anti-cancer strategies with higher efficacy and lesser side effects. Baicalein, a flavonoid component derived from the Chinese medicine scutellaria baicalensis, has been widely studied for its remarkable anti-cancer activity in multiple types of malignancies both at the molecular and cellular levels. Baicalein exerts its anti-tumor effects by inhibiting angiogenesis, invasion and migration, inducing cell apoptosis and cell cycle arrest, as well as regulating cell autophagy, metabolism, the tumor microenvironment and cancer stem cells with no obvious toxic side effects. The role of classic signaling pathways, such as PI3K/AKT/mTOR, MAPK, AMPK, Wnt/β-catenin, JAK/STAT3, MMP-2/-9, have been highlighted as the major targets for baicalein exerting its anti-malignant potential. Besides, baicalein can regulate the relevant non-coding RNAs, such as lncRNAs, miRNAs and circ-RNAs, to inhibit tumorigenesis and progression. In addition to the mentioned commonalities, baicalein shows some specific anti-tumor characteristics in some specific cancer types. Moreover, the preclinical studies of the combination of baicalein and chemoradiotherapy pave the way ahead for developing baicalein as an adjunct treatment with chemoradiotherapy. Our aim is to summary the role of baicalein in different types of cancer with its mechanisms based on in vitro and in vivo experiments, hoping providing proof for baicalein serving as an effective and safe compound for cancer treatment in clinic in the future.

摘要

问题,如化学疗法和放射疗法、靶向治疗和免疫疗法伴随当前的抗癌治疗的毒副作用和耐药性,已成为限制患者临床获益的瓶颈。因此,迫切需要寻找更有效、副作用更小的有前途的抗癌策略。黄芩素是一种源自中药黄芩的黄酮类成分,已在多种类型的恶性肿瘤的分子和细胞水平上进行了广泛研究,具有显著的抗癌活性。黄芩素通过抑制血管生成、侵袭和迁移、诱导细胞凋亡和细胞周期停滞,以及调节细胞自噬、代谢、肿瘤微环境和癌症干细胞,发挥其抗肿瘤作用,且没有明显的毒副作用。经典信号通路的作用,如 PI3K/AKT/mTOR、MAPK、AMPK、Wnt/β-catenin、JAK/STAT3、MMP-2/-9,已被强调为黄芩素发挥其抗恶性潜能的主要靶点。此外,黄芩素可以调节相关的非编码 RNA,如 lncRNA、miRNA 和 circRNA,以抑制肿瘤发生和进展。除了上述共同特点外,黄芩素在某些特定类型的癌症中还表现出一些特定的抗肿瘤特性。此外,黄芩素与化学疗法和放射疗法联合的临床前研究为将黄芩素开发为化学疗法和放射疗法的辅助治疗铺平了道路。我们的目的是根据体外和体内实验总结黄芩素在不同类型癌症中的作用及其机制,希望为黄芩素在未来临床治疗癌症方面作为一种有效和安全的化合物提供证据。

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