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硫代卡巴肼衍生物在炎症性疾病中的治疗观点:体外/体内研究综述。

Therapeutic perspective of thiosemicarbazones derivatives in inflammatory pathologies: A summary of in vitro/in vivo studies.

机构信息

Environmental Health Research Lab (EHRL), Faculty of Sciences V, Lebanese University, Nabatieh, Lebanon.

出版信息

Int Immunopharmacol. 2021 Jul;96:107778. doi: 10.1016/j.intimp.2021.107778. Epub 2021 May 24.

Abstract

Following induction of inflammation, the nuclear factor kappa B (NF-κB) in activated macrophages induces the transcription of pro-inflammatory cytokines such as tumor necrosis factor-alpha (TNF-α), interleukin-1β (IL-1β), interleukin-6 (IL-6), and cyclooxygenase (COX), an inflammatory enzyme implicated in the synthesis of prostaglandins (PGs). The latter are involved in the transition and the maintenance of chronic inflammation underling various chronic disorders that require treatment. Concerning this, many anti-inflammatory drugs are available to treat the inflammatory disorders, but their therapeutic use is associated with a variety of side effects. Therefore, the discovery of new safer and potential anti-inflammatory drugs is necessary. In this regard, thiosemicarbazones (TSC) compounds and their metals complexes attracted high interest due to their wide range of biological activities, interestingly, the anti-inflammatory activity. They are formed by the action of thiosemicarbazide on an aldehyde or ketone, and contain a sulfur atom in place of the oxygen atom. Their ability to form a stable complex with transition metal is known to enhances the biological activity and reduces the side effects of the parent compound. Thus, this review article describes the inflammatory response mediated by NF-κB-COX-PGs and summarizes the anti-inflammatory activity of different thiosemicarbazones derivatives synthesized in research area.

摘要

在炎症诱导后,激活的巨噬细胞中的核因子 kappa B(NF-κB)诱导促炎细胞因子的转录,如肿瘤坏死因子-α(TNF-α)、白细胞介素-1β(IL-1β)、白细胞介素-6(IL-6)和环氧化酶(COX),COX 是一种参与前列腺素(PGs)合成的炎症酶。后者参与各种慢性疾病的转变和慢性炎症的维持,这些疾病需要治疗。关于这一点,有许多抗炎药物可用于治疗炎症性疾病,但它们的治疗用途与各种副作用有关。因此,有必要发现新的更安全和有潜力的抗炎药物。在这方面,硫代氨基甲脒(TSC)化合物及其金属配合物因其广泛的生物活性而引起了极大的兴趣,有趣的是,它们具有抗炎活性。它们是由硫代氨基甲脒对醛或酮的作用形成的,其中一个硫原子取代了氧原子。已知它们与过渡金属形成稳定配合物的能力可增强生物活性并降低母体化合物的副作用。因此,本文描述了由 NF-κB-COX-PGs 介导的炎症反应,并总结了研究领域中合成的不同硫代氨基甲脒衍生物的抗炎活性。

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