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阿扎诺尔,一种强效的微粒体前列腺素E合酶-1抑制剂:新型抗炎药。

Arzanol, a potent mPGES-1 inhibitor: novel anti-inflammatory agent.

作者信息

Kothavade Pankaj S, Nagmoti Dnyaneshwar M, Bulani Vipin D, Juvekar Archana R

机构信息

Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai 400 019, India.

出版信息

ScientificWorldJournal. 2013 Oct 1;2013:986429. doi: 10.1155/2013/986429. eCollection 2013.

Abstract

Arzanol is a novel phloroglucinol α -pyrone, isolated from a Mediterranean plant Helichrysum italicum (Roth) Don ssp. microphyllum which belongs to the family Asteraceae. Arzanol has been reported to possess a variety of pharmacological activities. However, anti-inflammatory, anti-HIV, and antioxidant activities have been studied in some detail. Arzanol has been reported to inhibit inflammatory transcription factor NF κB activation, HIV replication in T cells, releases of IL-1 β , IL-6, IL-8, and TNF-α , and biosynthesis of PGE₂ by potentially inhibiting mPGES-1 enzyme. Diversity of mechanisms of actions of arzanol may be useful in treatment of disease involving these inflammatory mediators such as autoimmune diseases and cancer. This review presents comprehensive information on the chemistry, structure-activity relationship, and pharmacological activities of arzanol. In addition this review discusses recent developments and the scope for future research in these aspects.

摘要

阿扎诺醇是一种新型的间苯三酚α-吡喃酮,从属于菊科的地中海植物小叶蜡菊(Helichrysum italicum (Roth) Don ssp. microphyllum)中分离得到。据报道,阿扎诺醇具有多种药理活性。然而,对其抗炎、抗HIV和抗氧化活性进行了较为详细的研究。据报道,阿扎诺醇可通过潜在抑制mPGES-1酶来抑制炎症转录因子NFκB的激活、T细胞中的HIV复制、IL-1β、IL-6、IL-8和TNF-α的释放以及PGE₂的生物合成。阿扎诺醇作用机制的多样性可能有助于治疗涉及这些炎症介质的疾病,如自身免疫性疾病和癌症。本文综述了阿扎诺醇的化学、构效关系和药理活性的全面信息。此外,本文还讨论了这些方面的最新进展以及未来研究的范围。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a365/3807707/48b0791086b4/TSWJ2013-986429.001.jpg

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