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Tripterygium wilfordii bioactive compounds as anticancer and anti-inflammatory agents

机译:雷公藤雷公藤生物活性化合物作为抗癌和抗炎药

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摘要

1. Bioactive compounds from medicinal plants with anticancer and anti-inflammatory effects have become key resources in drug discovery fields for the treatment of various malignancies and immunological disorders. 2. Tripterygium wilfordii (TW) is a medicinal plant that exhibits profound immunosuppressive effects and has been used in herbal regimens for the treatment of immunological diseases for thousand years in China. 3. Procedures for the isolation and characterization of TW bioactive compounds have been well established. Over the past three decades, more than 46 diterpenoids, 20 new triterpenoids, 26 alkaloids and other small molecules have been identified from TW. 4. Triptolide, celastrol and tripchlorolide are among the bioactive compounds conferring the immunosuppressive and anticancer activities of TW. Accumulated evidence suggests that the TW bioactive compounds exert their pharmacological actions by modulating the transcriptional activity of nuclear factor-κB signalling molecule. 5. Triptolide derivatives with improved water solubility have emerged as promising drug candidates. Clinical trials are being conducted on the derivatives to provide encyclopaedic knowledge on triptolide pharmacokinetics in patients.
机译:1.来自药用植物的具有抗癌和抗炎作用的生物活性化合物已成为药物开发领域中用于治疗各种恶性肿瘤和免疫疾病的关键资源。 2.雷公藤(TW)是一种具有深远的免疫抑制作用的药用植物,在中国已经有数千年的历史被用于治疗免疫疾病的草药疗法。 3. TW生物活性化合物的分离和表征方法已得到很好的建立。在过去的三十年中,TW已鉴定出46种以上的二萜,20种新的三萜,26种生物碱及其他小分子。 4.雷公藤内酯醇,Celastrol和三氯氯化物是赋予TW免疫抑制和抗癌活性的生物活性化合物。积累的证据表明,TW生物活性化合物通过调节核因子-κB信号分子的转录活性发挥其药理作用。 5.具有改善的水溶性的雷公藤内酯衍生物已成为有前途的候选药物。目前正在对该衍生物进行临床试验,以提供有关雷公藤内酯醇药物动力学的百科全书知识。

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