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槲皮素及其衍生物:合成、药理用途,特别强调抗肿瘤特性以及具有增强生物利用度的前药。

Quercetin and its derivatives: synthesis, pharmacological uses with special emphasis on anti-tumor properties and prodrug with enhanced bio-availability.

作者信息

Hirpara Ketan V, Aggarwal Pawan, Mukherjee Amrita J, Joshi Narendra, Burman Anand C

机构信息

Chemical Research, Dabur Research Foundation, Ghaziabad, U.P. India.

出版信息

Anticancer Agents Med Chem. 2009 Feb;9(2):138-61. doi: 10.2174/187152009787313855.

Abstract

Cancer is one of the leading causes of death in the world. American Cancer Society reported 12 million new cases of malignancy diagnosed worldwide in 2007, with 7.6 million people dying from the disease. Plant-derived molecules have played an important role in cancer chemotherapy. Many cytotoxic plant-derived molecules such as vinblastine, vincristine, navelbine, etoposide, teniposide, taxol, taxotere, topotecan and irinotecan have been approved as anticancer drugs. Flavonoids, a plant-derived molecule has shown to regulate proliferation and cell death pathways leading to cancer. Some Flavonoids have already entered in clinical trials, among them Quercetin is emerging as prospective anticancer drug candidates and its prodrug QC12 has entered in phase-I clinical studies. In this review authors have tried to cover in brief but comprehensive way, the chemistry related to synthesis and uses of "Quercetin & its derivatives" with special emphasis on the anticancer properties.

摘要

癌症是全球主要的死亡原因之一。美国癌症协会报告称,2007年全球有1200万例新诊断的恶性肿瘤病例,其中760万人死于该疾病。植物来源的分子在癌症化疗中发挥了重要作用。许多具有细胞毒性的植物来源分子,如长春碱、长春新碱、诺维本、依托泊苷、替尼泊苷、紫杉醇、多西他赛、拓扑替康和伊立替康,已被批准作为抗癌药物。黄酮类化合物,一种植物来源的分子,已显示出可调节导致癌症的增殖和细胞死亡途径。一些黄酮类化合物已经进入临床试验,其中槲皮素正成为有前景的抗癌药物候选物,其前药QC12已进入I期临床研究。在这篇综述中,作者试图以简要但全面的方式涵盖与“槲皮素及其衍生物”的合成和用途相关的化学内容,并特别强调其抗癌特性。

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