Tanshinones: sources, pharmacokinetics and anti-cancer activities.

Tanshinones: sources, pharmacokinetics and anti-cancer activities.
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Tanshinones:来源,药代动力学和抗癌活动。

DOI:
10.3390/ijms131013621
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发表时间:
2012-10-22
影响因子:
5.6
通讯作者:
Lü J
Lü J
中科院分区:
生物学2区
文献类型:
--
作者:
Zhang Y;Jiang P;Ye M;Kim SH;Jiang C;Lü J

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丹参酮是从丹参(丹参或丹参)中分离出来的一类松香烷二萜化合物,丹参是一种著名的中药(TCM)草药。自 20 世纪 30 年代首次发现以来,已从丹参中分离出 40 多种亲脂性丹参酮和结构相关化合物。近几十年来,人们进行了大量的研究来探讨丹参酮的分离、鉴定、合成和药理学。除了经过充分研究的心血管活性之外,最近还研究了丹参酮的体外和体内抗癌活性。在这篇综述中,我们更新了丹参酮的草药和替代来源,以及选定丹参酮的药代动力学。我们讨论抗癌特性并确定未来研究的关键问题。尽管之前的研究表明丹参酮的抗癌潜力会影响细胞培养模型中的多个细胞过程和分子靶标,但由于溶剂载体和给药途径缺乏统一性,临床前模型中体内效力评估实验的数据差异很大。为了解决丹参酮口服生物利用度差的问题,进行了化学修饰和新配方。到目前为止,为了支持丹参酮的抗癌适应症,人体临床试验的设计和执行还远远不够理想。
Tanshinones are a class of abietane diterpene compound isolated from Salvia miltiorrhiza (Danshen or Tanshen in Chinese), a well-known herb in Traditional Chinese Medicine (TCM). Since they were first identified in the 1930s, more than 40 lipophilic tanshinones and structurally related compounds have been isolated from Danshen. In recent decades, numerous studies have been conducted to investigate the isolation, identification, synthesis and pharmacology of tanshinones. In addition to the well-studied cardiovascular activities, tanshinones have been investigated more recently for their anti-cancer activities in vitro and in vivo. In this review, we update the herbal and alternative sources of tanshinones, and the pharmacokinetics of selected tanshinones. We discuss anti-cancer properties and identify critical issues for future research. Whereas previous studies have suggested anti-cancer potential of tanshinones affecting multiple cellular processes and molecular targets in cell culture models, data from in vivo potency assessment experiments in preclinical models vary greatly due to lack of uniformity of solvent vehicles and routes of administration. Chemical modifications and novel formulations had been made to address the poor oral bioavailability of tanshinones. So far, human clinical trials have been far from ideal in their design and execution for the purpose of supporting an anti-cancer indication of tanshinones.
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