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从柘树中分离出的一种异戊烯基呫吨酮——柘树异戊烯基呫吨酮A，通过抑制BV2小胶质细胞中的NF-κB和p38 MAPK信号通路来抑制脂多糖诱导的神经炎症。

A Prenylated Xanthone, Cudratricusxanthone A, Isolated from Cudrania tricuspidata Inhibits Lipopolysaccharide-Induced Neuroinflammation through Inhibition of NF-κB and p38 MAPK Pathways in BV2 Microglia.

作者信息

Yoon Chi-Su, Kim Dong-Cheol, Quang Tran Hong, Seo Jungwon, Kang Dae Gill, Lee Ho Sub, Oh Hyuncheol, Kim Youn-Chul

机构信息

Institute of Pharmaceutical Research and Development, College of Pharmacy, Wonkwang University, Iksan 54538, Korea.

Institute of Marine Biochemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Caugiay, Hanoi 100000, Vietnam.

出版信息

Molecules. 2016 Sep 16;21(9):1240. doi: 10.3390/molecules21091240.

DOI:10.3390/molecules21091240
PMID:27649130
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6272989/
Abstract

Cudrania tricuspidata Bureau (Moraceae) is an important source of traditional Korean and Chinese medicines used to treat neuritis and inflammation. Cudratricusxanthone A (1), a prenylated xanthone, isolated from C. tricuspidata, has a variety of biological and therapeutic activities. The goal of this study was to examine the effects of compound 1 on neuroinflammation and characterize its mechanism of action in lipopolysaccharide (LPS)-stimulated BV2 microglia. Cudratricusxanthone A (1) suppressed the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 enzymes and decreased the production of iNOS-derived nitric oxide and COX-2-derived prostaglandin E2 in LPS-stimulated mouse BV2 microglia. The compound also decreased tumor necrosis factor-α, interleukin (IL)-1β, and IL-12 production; inhibited the phosphorylation and degradation of IκB-α; and blocked the nuclear translocation of p50 and p65 in mouse BV2 microglia induced by LPS. Cudratricusxanthone A (1) had inhibitory effects on nuclear factor kappa B DNA-binding activity. Additionally, it inhibited the p38 mitogen-activated protein kinase signaling pathway. Our data suggests that cudratricusxanthone A (1) may be a useful therapeutic agent in the treatment of neurodegenerative diseases caused by neuroinflammation.

摘要

柘树（桑科）是用于治疗神经炎和炎症的传统韩药和中药的重要来源。从柘树中分离出的一种异戊烯基黄酮——柘树黄酮A（1），具有多种生物学和治疗活性。本研究的目的是研究化合物1对神经炎症的影响，并阐明其在脂多糖（LPS）刺激的BV2小胶质细胞中的作用机制。柘树黄酮A（1）抑制了诱导型一氧化氮合酶（iNOS）和环氧化酶（COX）-2的表达，并减少了LPS刺激的小鼠BV2小胶质细胞中iNOS衍生的一氧化氮和COX-2衍生的前列腺素E2的产生。该化合物还降低了肿瘤坏死因子-α、白细胞介素（IL）-1β和IL-12的产生；抑制了IκB-α的磷酸化和降解；并阻断了LPS诱导的小鼠BV2小胶质细胞中p50和p65的核转位。柘树黄酮A（1）对核因子κB DNA结合活性有抑制作用。此外，它还抑制了p38丝裂原活化蛋白激酶信号通路。我们的数据表明，柘树黄酮A（1）可能是治疗由神经炎症引起的神经退行性疾病的有效治疗剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6db/6272989/b65d5089050f/molecules-21-01240-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6db/6272989/b85f467ac33e/molecules-21-01240-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6db/6272989/c12a72e63d50/molecules-21-01240-g003.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6db/6272989/99ff4e61dcaf/molecules-21-01240-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6db/6272989/b65d5089050f/molecules-21-01240-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6db/6272989/b85f467ac33e/molecules-21-01240-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6db/6272989/ddfe4f12ec5f/molecules-21-01240-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6db/6272989/c12a72e63d50/molecules-21-01240-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6db/6272989/8d6f83c7d2f8/molecules-21-01240-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6db/6272989/99ff4e61dcaf/molecules-21-01240-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c6db/6272989/b65d5089050f/molecules-21-01240-g006.jpg

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