Celastrol: A Spectrum of Treatment Opportunities in Chronic Diseases.
Celastrol: A Spectrum of Treatment Opportunities in Chronic Diseases.
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DOI：
10.3389/fmed.2017.00069
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发表时间：
2017
影响因子：
3.9
通讯作者：
Moita LF
中科院分区：
文献类型：
--
作者：
Cascão R;Fonseca JE;Moita LF
近年来，从药用植物中鉴定具有显著治疗特性的新生物活性化合物引起了人们的极大兴趣。这就是雷公藤（TW）的情况，雷公藤是一种用于中药的草药。迄今为止，使用其根提取物进行的临床试验显示出令人印象深刻的治疗特性，但也显示出大量的胃肠道副作用。从TW中获得的最有前途的生物活性化合物是雷公藤红素。在过去的十年中，越来越多的研究发表强调雷公藤红素在不同临床领域的药用价值。在这里，我们系统地审查了雷公藤红素的作用机制和治疗性质的炎症性疾病，即，类风湿性关节炎，系统性红斑狼疮，炎症性肠病，骨关节炎和过敏，以及在癌症，神经退行性疾病和其他疾病，如糖尿病，肥胖症，动脉粥样硬化和听力损失。我们还将关注雷公藤红素制剂的毒理学特征和局限性，即溶解度、生物利用度和剂量问题，这些问题仍然限制了其进一步的临床应用和有用性。
The identification of new bioactive compounds derived from medicinal plants with significant therapeutic properties has attracted considerable interest in recent years. Such is the case of the Tripterygium wilfordii (TW), an herb used in Chinese medicine. Clinical trials performed so far using its root extracts have shown impressive therapeutic properties but also revealed substantial gastrointestinal side effects. The most promising bioactive compound obtained from TW is celastrol. During the last decade, an increasing number of studies were published highlighting the medicinal usefulness of celastrol in diverse clinical areas. Here we systematically review the mechanism of action and the therapeutic properties of celastrol in inflammatory diseases, namely, rheumatoid arthritis, systemic lupus erythematosus, inflammatory bowel diseases, osteoarthritis and allergy, as well as in cancer, neurodegenerative disorders and other diseases, such as diabetes, obesity, atherosclerosis, and hearing loss. We will also focus in the toxicological profile and limitations of celastrol formulation, namely, solubility, bioavailability, and dosage issues that still limit its further clinical application and usefulness.