阿尔茨海默病（AD）是一种复杂的神经退行性疾病。 5α-环氧木香内酯 (5α-EAL) 是从旋覆花 (Inula macrophylla) 草本植物中分离出来的一种真香型倍半萜，具有多种药理作用。这项工作旨在研究 5α-EAL 对认知障碍的改善影响。 5α-EAL 抑制脂多糖 (LPS) 刺激的 BV-2 细胞中一氧化氮 (NO) 的产生，EC50 为 6.2 μM。 5α-EAL 显着减少前列腺素 E2 (PGE2) 和肿瘤坏死因子-α (TNF-α) 的产生，同时还抑制环氧合酶-2 (COX-2) 和诱导型一氧化氮合酶 (iNOS) 蛋白的产生。通过平行人工膜渗透测定证实了 5α-EAL 穿透血脑屏障 (BBB) 的能力。采用东莨菪碱 (SCOP) 诱导的 AD 小鼠模型来评估 5α-EAL 对体内认知障碍的改善影响。小鼠接受 5α-EAL（每天 10 和 30 mg/kg，腹腔注射）预处理 21 天后，行为实验表明给予 5α-EAL 可以减轻认知和记忆障碍。 5α-EAL 显着降低 SCOP 诱导的 AD 小鼠大脑中的 AChE 活性。总之，这些发现强调了天然产物 5α-EAL 作为一种潜在的生物活性化合物，由于其药理学特征，可减轻 AD 认知缺陷的有益作用。© 2024。作者。

Alzheimer's disease (AD) is a complex neurodegenerative condition. 5α-epoxyalantolactone (5α-EAL), a eudesmane-type sesquiterpene isolated from the herb of Inula macrophylla, has various pharmacological effects. This work supposed to investigate the improved impact of 5α-EAL on cognitive impairment. 5α-EAL inhibited the generation of nitric oxide (NO) in BV-2 cells stimulated with lipopolysaccharide (LPS) with an EC50 of 6.2 μM. 5α-EAL significantly reduced the production of prostaglandin E2 (PGE2) and tumor necrosis factor-α (TNF-α), while also inhibiting the production of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) proteins. The ability of 5α-EAL to penetrate the blood-brain barrier (BBB) was confirmed via a parallel artificial membrane permeation assay. Scopolamine (SCOP)-induced AD mice model was employed to assess the improved impacts of 5α-EAL on cognitive impairment in vivo. After the mice were pretreated with 5α-EAL (10 and 30 mg/kg per day, i.p.) for 21 days, the behavioral experiments indicated that the administration of the 5α-EAL could alleviate the cognitive and memory impairments. 5α-EAL significantly reduced the AChE activity in the brain of SCOP-induced AD mice. In summary, these findings highlight the beneficial effects of the natural product 5α-EAL as a potential bioactive compound for attenuating cognitive deficits in AD due to its pharmacological profile.© 2024. The Author(s).