摘要
环孢素 A (CsA) 是一种环状十一肽,具有很强的免疫抑制效力。 CsA 于 80 年代中期首次上市,广泛用于移植,大大提高了实体器官移植后患者和移植物的存活率。不幸的是,由于其高毒性,CsA 给药可能会带来许多副作用。这些副作用严重限制了 CsA 的临床应用。因此,了解 CsA 在患者中的严重副作用非常重要,尤其是在移植中。在这篇综述文章中,总结了 CsA 的化学作用和最著名的毒性作用,包括肾毒性、肝毒性、神经毒性和心脏毒性作用。其现有的毒性数据(不同的物种,不同的给药途径),以前发表过,也进行了总结。此外,还详细讨论了 CsA 诱导毒性的分子途径。希望这篇综述有助于进一步了解 CsA 在患者中的来源、化学和临床应用,以及 CsA 诱导毒性的潜在机制。
关键词: 环孢菌素 A,肾毒性,肝毒性,神经毒性,心脏毒性,信号通路。
Current Medicinal Chemistry
Title:Cyclosporine A: Chemistry and Toxicity – A Review
Volume: 28 Issue: 20
关键词: 环孢菌素 A,肾毒性,肝毒性,神经毒性,心脏毒性,信号通路。
摘要: Cyclosporine A (CsA) is a cyclic undecapeptide with strong immunosuppressive potency. Firstly marketed in the mid-1980s, CsA was widely used in transplantation and greatly improved the survival rates of patients and grafts after solid-organ transplantation. Unfortunately, CsA administration can be associated with a number of side effects due to its high toxicity. These side effects seriously limited the clinical use of CsA. Therefore, it is important to understand the serious side effects of CsA in patients, especially in transplantation. In this review article, the chemistry and most known toxic effects of CsA, including the nephrotoxic, hepatotoxic, neurotoxic, and cardiotoxic effects, are summarized. Its available toxicity data (different species, different administration routes), published formerly, are also summarized. In addition, the molecular pathways of toxicity induced by CsA are also discussed in detail. It is hoped that this review will help to further understand the source, chemistry, and clinical application of CsA in patients as well as the potential mechanisms of CsA-induced toxicity.
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Cite this article as:
Cyclosporine A: Chemistry and Toxicity – A Review, Current Medicinal Chemistry 2021; 28 (20) . https://dx.doi.org/10.2174/0929867327666201006153202
DOI https://dx.doi.org/10.2174/0929867327666201006153202 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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