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土木香内酯:一种具有多种药理作用的倍半萜内酯。

Alantolactone: A sesquiterpene lactone with diverse pharmacological effects.

机构信息

Eye Center, The Second Hospital of Jilin University, Changchun, China.

Department of Rehabilitation Medicine, The Second Hospital of Jilin University, Changchun, China.

出版信息

Chem Biol Drug Des. 2021 Dec;98(6):1131-1145. doi: 10.1111/cbdd.13972. Epub 2021 Oct 13.

Abstract

Alantolactone (Ala) is a sesquiterpene lactone that can be isolated from many herbal plants belonging to Asteraceae. Besides the antimicrobial activities against bacteria, fungi and viruses, Ala has also demonstrated significant anti-inflammatory effects in various models by inhibiting NF-κB and MAPKs to decrease the pro-inflammatory cytokines such as IL-1β, IL-6 and TNF-α. The antitumor effects of Ala have been demonstrated in vitro and in vivo via inducing intrinsic apoptosis, oxidative stress, ER stress, cell cycle arrest and inhibiting autophagy and STAT3 phosphorylation, which are also involved in its combination or synergy with other antitumor drugs. Ala also has neuroprotective activity through attenuating oxidative stress and inflammation, besides its modulation of glucose and lipid metabolism. This review summarizes the recent advances of the pharmacological effects of Ala, including anti-inflammatory, antitumor, antimicrobial, neuroprotective activities, as well as the underlying mechanisms. Ala might be employed as a potential lead to develop drugs for multiple diseases.

摘要

土木香内酯(Ala)是一种倍半萜内酯,可从菊科的多种草本植物中分离得到。除了具有抗细菌、真菌和病毒的活性外,Ala 还通过抑制 NF-κB 和 MAPKs 减少促炎细胞因子(如 IL-1β、IL-6 和 TNF-α),在各种模型中表现出显著的抗炎作用。通过诱导细胞内凋亡、氧化应激、内质网应激、细胞周期停滞和抑制自噬和 STAT3 磷酸化,Ala 在体外和体内显示出抗肿瘤作用,这也与其与其他抗肿瘤药物的联合或协同作用有关。Ala 还通过减轻氧化应激和炎症具有神经保护活性,此外还能调节葡萄糖和脂质代谢。本文综述了 Ala 的药理作用的最新进展,包括抗炎、抗肿瘤、抗菌、神经保护活性以及潜在的机制。Ala 可能被用作开发多种疾病药物的潜在先导化合物。

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