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大黄素:一种通过调节多个致癌靶点发挥抗肿瘤活性的代谢产物。

Emodin: A metabolite that exhibits anti-neoplastic activities by modulating multiple oncogenic targets.

机构信息

Department of Biotechnology, Maharishi Markandeshwar (Deemed to be University), Mullana-Ambala, Haryana 133207, India.

Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, USA.

出版信息

Toxicol In Vitro. 2021 Jun;73:105142. doi: 10.1016/j.tiv.2021.105142. Epub 2021 Mar 17.

DOI:10.1016/j.tiv.2021.105142
PMID:33722736
Abstract

Oncogenic transformation has been the major cause of global mortality since decades. Despite established therapeutic regimes, majority of cancer patients either present with tumor relapse, refractory disease or therapeutic resistance. Numerous drug candidates are being explored to tap the key reason being poor tumor remission rates, from novel chemotherapy agents to immunotherapy to exploring natural compound derivatives with effective anti-cancer potential. One of these natural product metabolites, emodin has present with significant potential to target tumor oncogenic processes: induction of apoptosis and cell cycle arrest, tumor angiogenesis, and metastasis to chemoresistance in malignant cells. Based on the present scientific excerpts on safety and effectiveness of emodin in targeting hallmarks of tumor progression, emodin is being promisingly explored using nanotechnology platforms for long-term sustained treatment and management of cancer patients. In this review, we summarize the up-to-date scientific literature supporting the anti-neoplastic potential of emodin. We also provide an insight into toxicity and safety profile of emodin and how emodin has emerged as an effective therapeutic alternative in synergism with established conventional chemotherapeutic regimes for management and treatment of tumor progression.

摘要

几十年来,致癌转化一直是全球死亡的主要原因。尽管有既定的治疗方案,但大多数癌症患者要么出现肿瘤复发、难治性疾病或治疗耐药性。正在探索大量的候选药物,主要原因是肿瘤缓解率低,从新型化疗药物到免疫疗法,再到探索具有有效抗癌潜力的天然化合物衍生物。这些天然产物代谢物之一,大黄素具有显著的靶向肿瘤致癌过程的潜力:诱导细胞凋亡和细胞周期停滞、肿瘤血管生成以及转移到恶性细胞的化疗耐药性。基于大黄素在靶向肿瘤进展标志方面的安全性和有效性的现有科学摘录,大黄素正在使用纳米技术平台进行探索,以实现癌症患者的长期持续治疗和管理。在这篇综述中,我们总结了支持大黄素抗肿瘤潜力的最新科学文献。我们还深入了解了大黄素的毒性和安全性概况,以及大黄素如何与既定的常规化疗方案协同作用,成为管理和治疗肿瘤进展的有效治疗替代方案。

相似文献

1
Emodin: A metabolite that exhibits anti-neoplastic activities by modulating multiple oncogenic targets.大黄素:一种通过调节多个致癌靶点发挥抗肿瘤活性的代谢产物。
Toxicol In Vitro. 2021 Jun;73:105142. doi: 10.1016/j.tiv.2021.105142. Epub 2021 Mar 17.
2
The distinct mechanisms of the antitumor activity of emodin in different types of cancer (Review).大黄素在不同类型癌症中抗肿瘤活性的独特机制(综述)。
Oncol Rep. 2013 Dec;30(6):2555-62. doi: 10.3892/or.2013.2741. Epub 2013 Sep 19.
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Safety of natural anthraquinone emodin: an assessment in mice.天然蒽醌大黄素的安全性:在小鼠中的评估。
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A Promising Emodin-Loaded Poly (Lactic-Co-Glycolic Acid)-d-α-Tocopheryl Polyethylene Glycol 1000 Succinate Nanoparticles for Liver Cancer Therapy.一种用于肝癌治疗的有前景的载大黄素聚(乳酸-乙醇酸)-d-α-生育酚聚乙二醇1000琥珀酸酯纳米颗粒。
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Combinatorial therapy of Thymoquinone and Emodin synergistically enhances apoptosis, attenuates cell migration and reduces stemness efficiently in breast cancer.姜黄素和大黄素联合治疗可协同增强乳腺癌细胞凋亡,有效抑制细胞迁移,降低肿瘤干细胞特性。
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Emodin inhibits angiogenesis in pancreatic cancer by regulating the transforming growth factor-β/drosophila mothers against decapentaplegic pathway and angiogenesis-associated microRNAs.大黄素通过调节转化生长因子-β/果蝇抗五聚体蛋白母系基因途径和血管生成相关的微小RNA来抑制胰腺癌中的血管生成。
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Emodin Sensitizes Hepatocellular Carcinoma Cells to the Anti-Cancer Effect of Sorafenib through Suppression of Cholesterol Metabolism.大黄素通过抑制胆固醇代谢增强索拉非尼对肝癌细胞的抗癌作用。
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Anti-tumor effect of emodin on gynecological cancer cells.大黄素对妇科癌细胞的抗肿瘤作用。
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Emodin enhances cisplatin-induced cytotoxicity in human bladder cancer cells through ROS elevation and MRP1 downregulation.大黄素通过提高活性氧水平和下调多药耐药相关蛋白1增强顺铂对人膀胱癌细胞的细胞毒性。
BMC Cancer. 2016 Aug 2;16:578. doi: 10.1186/s12885-016-2640-3.
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Emodin enhances cisplatin-induced cytotoxicity via down-regulation of ERCC1 and inactivation of ERK1/2.大黄素通过下调 ERCC1 和失活 ERK1/2 增强顺铂诱导的细胞毒性。
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引用本文的文献

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Advances in nano drug delivery systems for enhanced efficacy of emodin in cancer therapy.用于增强大黄素在癌症治疗中疗效的纳米药物递送系统的进展
Int J Pharm X. 2024 Dec 25;9:100314. doi: 10.1016/j.ijpx.2024.100314. eCollection 2025 Jun.
2
Mechanism of emodin in treating hepatitis B virus-associated hepatocellular carcinoma: network pharmacology and cell experiments.大黄素治疗乙型肝炎病毒相关性肝细胞癌的作用机制:网络药理学和细胞实验。
Front Cell Infect Microbiol. 2024 Sep 13;14:1458913. doi: 10.3389/fcimb.2024.1458913. eCollection 2024.
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Marine-Derived Leads as Anticancer Candidates by Disrupting Hypoxic Signaling through Hypoxia-Inducible Factors Inhibition.
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Mar Drugs. 2024 Mar 23;22(4):143. doi: 10.3390/md22040143.
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Emodin is a Potential Drug Targeting CD44-positive Hepatocellular Cancer.大黄素是一种针对 CD44 阳性肝癌的潜在药物靶点。
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Emodin exhibits anti-acne potential by inhibiting cell growth, lipogenesis, and inflammation in human SZ95 sebocytes.大黄素通过抑制人 SZ95 皮脂腺细胞的生长、脂肪生成和炎症反应发挥其抗痤疮潜力。
Sci Rep. 2023 Dec 7;13(1):21576. doi: 10.1038/s41598-023-48709-x.
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