Rui Ma, Xu-Yao Feng, Jiang-Jiang Tang, Wei Ha, Yan-Ping Shi
{"title":"从大叶桉树中提取的 5α-Epoxyalantolactone 可减轻东莨菪碱诱导的阿尔茨海默病小鼠模型的认知缺陷。","authors":"Rui Ma, Xu-Yao Feng, Jiang-Jiang Tang, Wei Ha, Yan-Ping Shi","doi":"10.1007/s13659-024-00462-y","DOIUrl":null,"url":null,"abstract":"<div><p>Alzheimer’s disease (AD) is a complex neurodegenerative condition. 5<i>α</i>-epoxyalantolactone (5<i>α</i>-EAL), a eudesmane-type sesquiterpene isolated from the herb of <i>Inula macrophylla</i>, has various pharmacological effects. This work supposed to investigate the improved impact of 5<i>α</i>-EAL on cognitive impairment. 5<i>α</i>-EAL inhibited the generation of nitric oxide (NO) in BV-2 cells stimulated with lipopolysaccharide (LPS) with an EC<sub>50</sub> of 6.2 μM. 5<i>α</i>-EAL significantly reduced the production of prostaglandin E2 (PGE<sub>2</sub>) 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 5<i>α</i>-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 5<i>α</i>-EAL on cognitive impairment in vivo. After the mice were pretreated with 5<i>α</i>-EAL (10 and 30 mg/kg per day, <i>i.p.</i>) for 21 days, the behavioral experiments indicated that the administration of the 5<i>α</i>-EAL could alleviate the cognitive and memory impairments. 5<i>α</i>-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 5<i>α</i>-EAL as a potential bioactive compound for attenuating cognitive deficits in AD due to its pharmacological profile.</p><h3>Graphical Abstract</h3>\n<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"14 1","pages":""},"PeriodicalIF":4.8000,"publicationDate":"2024-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11219692/pdf/","citationCount":"0","resultStr":"{\"title\":\"5α-Epoxyalantolactone from Inula macrophylla attenuates cognitive deficits in scopolamine-induced Alzheimer’s disease mice model\",\"authors\":\"Rui Ma, Xu-Yao Feng, Jiang-Jiang Tang, Wei Ha, Yan-Ping Shi\",\"doi\":\"10.1007/s13659-024-00462-y\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>Alzheimer’s disease (AD) is a complex neurodegenerative condition. 5<i>α</i>-epoxyalantolactone (5<i>α</i>-EAL), a eudesmane-type sesquiterpene isolated from the herb of <i>Inula macrophylla</i>, has various pharmacological effects. This work supposed to investigate the improved impact of 5<i>α</i>-EAL on cognitive impairment. 5<i>α</i>-EAL inhibited the generation of nitric oxide (NO) in BV-2 cells stimulated with lipopolysaccharide (LPS) with an EC<sub>50</sub> of 6.2 μM. 5<i>α</i>-EAL significantly reduced the production of prostaglandin E2 (PGE<sub>2</sub>) 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 5<i>α</i>-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 5<i>α</i>-EAL on cognitive impairment in vivo. After the mice were pretreated with 5<i>α</i>-EAL (10 and 30 mg/kg per day, <i>i.p.</i>) for 21 days, the behavioral experiments indicated that the administration of the 5<i>α</i>-EAL could alleviate the cognitive and memory impairments. 5<i>α</i>-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 5<i>α</i>-EAL as a potential bioactive compound for attenuating cognitive deficits in AD due to its pharmacological profile.</p><h3>Graphical Abstract</h3>\\n<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>\",\"PeriodicalId\":718,\"journal\":{\"name\":\"Natural Products and Bioprospecting\",\"volume\":\"14 1\",\"pages\":\"\"},\"PeriodicalIF\":4.8000,\"publicationDate\":\"2024-07-02\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11219692/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Natural Products and Bioprospecting\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://link.springer.com/article/10.1007/s13659-024-00462-y\",\"RegionNum\":3,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Natural Products and Bioprospecting","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1007/s13659-024-00462-y","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
5α-Epoxyalantolactone from Inula macrophylla attenuates cognitive deficits in scopolamine-induced Alzheimer’s disease mice model
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.
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Natural Products and Bioprospecting serves as an international forum for essential research on natural products and focuses on, but is not limited to, the following aspects:
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