• 主题
高级搜索  >
历史搜索 清空历史
首页> 美国卫生研究院文献>Frontiers in Nutrition >Quercetin as an Emerging Anti-Melanoma Agent: A Four-Focus Area Therapeutic Development Strategy
【2h】

Quercetin as an Emerging Anti-Melanoma Agent: A Four-Focus Area Therapeutic Development Strategy

机译：槲皮素作为一种新兴的抗黑素瘤药物：四重点领域治疗发展战略

代理获取
本网站仅为用户提供外文OA文献查询和代理获取服务，本网站没有原文。下单后我们将采用程序或人工为您竭诚获取高质量的原文，但由于OA文献来源多样且变更频繁，仍可能出现获取不到、文献不完整或与标题不符等情况，如果获取不到我们将提供退款服务。请知悉。
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Replacing current refractory treatments for melanoma with new prevention and therapeutic approaches is crucial in order to successfully treat this aggressive cancer form. Melanoma develops from neural crest cells, which express tyrosinase – a key enzyme in the pigmentation pathway. The tyrosinase enzyme is highly active in melanoma cells and metabolizes polyphenolic compounds; tyrosinase expression thus makes feasible a target for polyphenol-based therapies. For example, quercetin (3,3′,4′,5,7-pentahydroxyflavone) is a highly ubiquitous and well-classified dietary polyphenol found in various fruits, vegetables, and other plant products including onions, broccoli, kale, oranges, blueberries, apples, and tea. Quercetin has demonstrated antiproliferative and proapoptotic activity in various cancer cell types. Quercetin is readily metabolized by tyrosinase into various compounds that promote anticancer activity; additionally, given that tyrosinase expression increases during tumorigenesis, and its activity is associated with pigmentation changes in both early- and late-stage melanocytic lesions, it suggests that quercetin can be used to target melanoma. In this review, we explore the potential of quercetin as an anti-melanoma agent utilizing and extrapolating on evidence from previous in vitro studies in various human malignant cell lines and propose a “four-focus area strategy” to develop quercetin as a targeted anti-melanoma compound for use as either a preventative or therapeutic agent. The four areas of focus include utilizing quercetin to (i) modulate cellular bioreduction potential and associated signaling cascades, (ii) affect transcription of relevant genes, (iii) regulate epigenetic processes, and (iv) develop effective combination therapies and delivery modalities/protocols. In general, quercetin could be used to exploit tyrosinase activity to prevent, and/or treat, melanoma with minimal additional side effects.
机译：为了成功治疗这种侵袭性癌症，用新的预防和治疗方法替代当前难治性的黑色素瘤治疗至关重要。黑色素瘤是由神经rest细胞发展而来的，神经cells细胞表达酪氨酸酶，酪氨酸酶是色素沉着途径中的关键酶。酪氨酸酶在黑色素瘤细胞中具有很高的活性，并能代谢多酚化合物。酪氨酸酶表达因此使基于多酚的疗法的靶标成为可行。例如，槲皮素（3,3'，4'，5,7-五羟基黄酮）是在各种水果，蔬菜和其他植物产品（包括洋葱，西兰花，羽衣甘蓝，橙子，蓝莓）中发现的普遍存在且分类良好的膳食多酚，苹果和茶。槲皮素已在多种癌细胞类型中显示出抗增殖和促凋亡活性。槲皮素很容易被酪氨酸酶代谢成各种化合物，从而增强抗癌活性。此外，鉴于酪氨酸酶表达在肿瘤发生过程中增加，并且其活性与早期和晚期黑素细胞病变中的色素沉着变化有关，这表明槲皮素可用于靶向黑色素瘤。在本综述中，我们探索并利用槲皮素作为抗黑素瘤药物的潜力，并从先前在各种人类恶性细胞系中进行的体外研究得出的证据进行推断，并提出了“四重点领域策略”来开发槲皮素作为靶向抗用作预防剂或治疗剂的黑色素瘤化合物。四个重点领域包括利用槲皮素来（i）调节细胞的生物还原潜力和相关的信号传导级联；（ii）影响相关基因的转录；（iii）调节表观遗传过程；（iv）开发有效的联合疗法和递送方式/方案。通常，槲皮素可用于利用酪氨酸酶活性来预防和/或治疗黑色素瘤，且副作用最小。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
代理获取

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号