研究动态
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从抗氧化剂和脑血管扩张剂到其抗癌潜力的研究。

Vincamine, from an antioxidant and a cerebral vasodilator to its anticancer potential.

发表日期:2023 Aug 09
作者: Yulin Ren, Kevin DeRose, Leyan Li, Judith C Gallucci, Jianhua Yu, A Douglas Kinghorn
来源: ANTIOXIDANTS & REDOX SIGNALING

摘要:

维奈明(Vincamine)是一种天然存在的吲哚类生物碱,展示了抗氧化活性,并且已被临床应用于脑血管疾病和供应不足的预防和治疗。 已有充分文件表明抗氧化剂可能有助于癌症治疗,因此最近对维奈明的潜在抗肿瘤活性进行了研究。 发现维奈明展示了对癌细胞的细胞毒性,并且调节了参与肿瘤生长的几种重要蛋白质,包括乙酰胆碱酯酶(AChE),丝裂原活化蛋白激酶(MAPK),核因子-κB(NF-κB),核因子红细胞2相关因子2(Nrf2)和T-box 3(TBX3)。 几种二吲哌生物碱,包括长春新碱和长春诺碱及其合成衍生物吉非替尼、芬法尼和诺雷波嗪,已被用作临床有效的癌症化学治疗药物。 在本综述中,总结了维奈明作为一种有价值的治疗剂的发现和开发,并描述了其抗氧化和抗肿瘤活性,并阐述了其抗癌潜力相关的抗氧化机制。 此外,还讨论了基于维奈明的可能抗肿瘤剂设计,这有助于发现进一步用于癌症治疗的新剂。 版权所有©2023 Elsevier Ltd. 保留所有权利。
Vincamine is a naturally occurring indole alkaloid showing antioxidant activity and has been used clinically for the prevention and treatment of cerebrovascular disorders and insufficiencies. It has been well documented that antioxidants may contribute to cancer treatment, and thus, vincamine has been investigated recently for its potential antitumor activity. Vincamine was found to show cancer cell cytotoxicity and to modulate several important proteins involved in tumor growth, including acetylcholinesterase (AChE), mitogen-activated protein kinase (MAPK), nuclear factor-κB (NF-κB), nuclear factor erythroid 2-related factor 2 (Nrf2), and T-box 3 (TBX3). Several bisindole alkaloids, including vinblastine and vincristine and their synthetic derivatives, vindesine, vinflunine, and vinorelbine, have been used as clinically effective cancer chemotherapeutic agents. In the present review, the discovery and development of vincamine as a useful therapeutic agent and its antioxidant and antitumor activity are summarized, with its antioxidant-related mechanisms of anticancer potential being described. Also, discussed herein are the design of the potential vincamine-based oncolytic agents, which could contribute to the discovery of further new agents for cancer treatment.Copyright © 2023 Elsevier Ltd. All rights reserved.