摘要
背景:斑蝥素在中医药中被列为高毒物。但斑rid素可以有效治疗不同类型的疾病,如传染性软疣。尽管斑蝥素很有用,但不幸的是,由于其副作用,越来越多的法规限制了这种有用的治疗选择。斑蝥素的毒性作用已导致它在大多数合法的医疗用途中被滥用。尽管斑蝥素会产生效应,并且必须实现其优点。最近,癌症越来越影响人们的生活。因为斑蝥素可以治疗一些癌症,所以必须使用溶液来减少副作用。这篇综述旨在描述一些类似物,几种有效的方法来抑制斑蝥素和斑蝥素的药物基因组学的副作用。 方法:我们通过输入数据库搜索关于斑蝥素的研究。然后对这些论文进行评估并分析其创建,解决方案,机制等,并针对性地筛选出与研究内容相关的论文,并根据解决方案,机制研究等内容对其进行整理。最后,这些内容被统一到一个框架中。 结果:发现一些斑蝥素的类似物显示出与斑rid素类似的功能,我们发现去甲斑蝥素,酰基硫脲衍生物,斑蝥素酰胺,酸酐修饰的衍生物和其他衍生物具有较小的副作用。修饰的斑rid素类似物减少肝细胞的毒性。斑蝥素由六环和五环组成,六环和酸酐部分上的氧部分表现出生化活性。蛋白磷酸酶与许多细胞过程有关,包括细胞凋亡,细胞周期进程等。斑蝥素可引起细胞凋亡和DNA双链断裂。斑蝥素和去甲斑蝥素能有效抑制哺乳动物和植物蛋白磷酸酶1(PP1)和蛋白磷酸酶2A(PP2A)的活性。斑蝥素在纳摩尔水平抑制PP5,IC50值为600 nM。 PP5可以控制哺乳动物的细胞存活,死亡,增殖和其他一些细胞内生物活性。斑蝥素处理后,EtPP5 mRNA表达水平下调。它们也可用于抑制谷胱甘肽S转移酶(GSTs),血管生成和A549人肺癌细胞的表达,触发弓形虫诱导膀胱癌细胞凋亡。我们发现使用维生素C和人参皂甙并将斑蝥素转化为纳米颗粒可以减少斑蝥素在患者中的副作用。 结论斑蝥素可抑制多种肿瘤细胞系。斑蝥素引起DNA单链和双链断裂并诱导细胞凋亡。虽然斑蝥素对人体有一定的毒性,但应该认真对待它的抗癌作用。几种可行的方法可以帮助解决这个问题。斑蝥素最重要的药物基因组学是斑蝥素可以抑制PPs,因为PPs与许多细胞过程有关。这个前景非常广阔,需要继续研究。
关键词: 斑蝥素,癌症,毒性,抑制,类似物,蛋白磷酸酶。
Current Medicinal Chemistry
Title:Overview of Cantharidin and its Analogues
Volume: 25 Issue: 17
关键词: 斑蝥素,癌症,毒性,抑制,类似物,蛋白磷酸酶。
摘要: Background: Cantharidin has been categorized as highly toxicant in Chinese medicine. But cantharidin can efficiently treat different types of diseases, such as molluscum contagiosum. While cantharidin is quite useful, unfortunately, due to its side effects, increasing regulations have limited access to this useful therapeutic option. Cantharidin's toxic effects have caused it to fall into disuse for most legitimate medical purposes. Although cantharidin generates effects and its advantages must be realized. Recently, cancer affects people’s life more and more. Because cantharidin can treat some cancers, so solutions must be used to reduce side effects. This review aims to describe some its analogues, several efficient methods to inhibit the side effects of cantharidin and pharmacogenomics of cantharidin.
Methods: We searched for research about cantharidin by entering the database. Then evaluated these papers and analyzed their founding, solution, mechanism, etc., and targeted to screen the papers related to the content of our research, and then sorted them out in accordance with the solution, mechanism research and other content. Finally, these content was unified into a framework.
Results: Some cantharidin's analogues were found that they show some similar functions to cantharidin and we found that norcantharidin, acylthiourea derivatives, cantharidinamides, anhydride-modified derivatives and other derivatives have less side effects. The modified cantharidin analogues reduce toxicity in hepatocytes. Cantharidin consists of a six-ring and a five-ring, the moiety of oxygen on the six-ring and the anhydride section exhibit biochemical activity. Protein phosphatases are associated with many cellular processes including apoptosis, cell cycle progression and so on. Cantharidin can cause apoptosis and double-stand breakage of DNA. Cantharidin and norcantharidin can efficiently inhibit the activity of mammalian and plant protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) in vivo. Cantharidin inhibits PP5 at the nanomolar level with an IC50 value of 600 nM. PP5 can manage the cellular survival, death, proliferation and other some intracellular biological activities in mammals. After cantharidin’s treatment, the level of EtPP5 mRNA expression was downregulated. Their also can be used to inhibit the Glutathione S-transferases (GSTs), angiogenesis and the expression of A549 human lung cancer cells, trigger eryptosis and induced bladder cancer cell apoptosis. We found that using Vitamin C and ginsenosides and translating cantharidin into nanoparticles can minimize the cantharidin side effects in the patients.
Conclusion: Cantharidin can inhibit various tumor cell lines. Cantharidin causes both DNA single- and double- strand breaks and induces apoptosis. Although cantharidin shows some toxicity for human, its anti-cancer effects should be taken seriously. Several viable methods can help solve this problem. The most important pharmacogenomics of cantharidin is that cantharidin can inhibit PPs, because PPs are associated with many cellular processes. This prospect is very broad and needs to continue studying.
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Cite this article as:
Overview of Cantharidin and its Analogues, Current Medicinal Chemistry 2018; 25 (17) . https://dx.doi.org/10.2174/0929867324666170414165253
DOI https://dx.doi.org/10.2174/0929867324666170414165253 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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