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越南海星Protoreaster nodosus的抗炎成分。

Anti-inflammatory components of the Vietnamese starfish Protoreaster nodosus.

作者信息

Thao Nguyen Phuong, Luyen Bui Thi Thuy, Koo Jung Eun, Kim Sohyun, Koh Young Sang, Cuong Nguyen Xuan, Nam Nguyen Hoai, Van Kiem Phan, Kim Young Ho, Van Minh Chau

出版信息

Biol Res. 2015 Feb 20;48(1):12. doi: 10.1186/s40659-015-0002-2.

DOI:10.1186/s40659-015-0002-2
PMID:25762127
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4347916/
Abstract

BACKGROUND

In the present study, we examined the inhibitory effects of a methanolic extract, dichloromethane fraction, water layer, and polyhydroxylated sterols (1-4) isolated from the Vietnamese starfish Protoreaster nodosus on pro-inflammatory cytokine (IL-12 p40, IL-6, and TNF-α) production in LPS-stimulated bone marrow-derived dendritic cells (BMDCs) using enzyme-linked immunosorbent assays (ELISA).

RESULTS

The methanolic extract and dichloromethane fraction exerted potent inhibitory effects on the production of all three pro-inflammatory cytokines, with IC50 values ranging from 0.60 ± 0.01 to 26.19 ± 0.64 μg/mL. Four highly pure steroid derivatives (1-4) were isolated from the dichloromethane fraction and water layer of P. nodosus. Potent inhibitory activities were also observed for (25S) 5α-cholestane-3β,4β,6α,7α,8β,15α,16β,26-octol (3) on the production of IL-12 p40 and IL-6 (IC50s = 3.11 ± 0.08 and 1.35 ± 0.03 μM), and for (25S) 5α-cholestane-3β,6α,8β,15α,16β,26-hexol (1) and (25S) 5α-cholestane-3β,6α,7α,8β,15α,16β,26-heptol (2) on the production of IL-12 p40 (IC50s = 0.01 ± 0.00 and 1.02 ± 0.01 μM). Moreover, nodososide (4) exhibited moderate inhibitory effects on IL-12 p40 and IL-6 production.

CONCLUSION

This is the first report of the anti-inflammatory activity from the starfish P. nodosus. The main finding of this study is the identification oxygenated steroid derivatives from P. nodosus with potent anti-inflammatory activities that may be developed as therapeutic agents for inflammatory diseases.

摘要

背景

在本研究中，我们使用酶联免疫吸附测定法（ELISA）检测了从越南海星瘤海星（Protoreaster nodosus）中分离得到的甲醇提取物、二氯甲烷馏分、水层和多羟基化甾醇（1 - 4）对脂多糖刺激的骨髓来源树突状细胞（BMDCs）中促炎细胞因子（IL - 12 p40、IL - 6和TNF -α）产生的抑制作用。

结果

甲醇提取物和二氯甲烷馏分对所有三种促炎细胞因子的产生均具有显著抑制作用，IC50值范围为0.60±0.01至26.19±0.64μg/mL。从瘤海星的二氯甲烷馏分和水层中分离出四种高纯度甾体衍生物（1 - 4）。（25S）5α - 胆甾烷 - 3β，4β，6α，7α，8β，15α，16β，26 - 辛醇（3）对IL - 12 p40和IL - 6的产生也表现出显著抑制活性（IC50分别为3.11±0.08和1.35±0.03μM），（25S）5α - 胆甾烷 - 3β，6α，8β，15α，16β，26 - 己醇（1）和（25S）5α - 胆甾烷 - 3β，6α，7α，8β，15α，16β，26 - 庚醇（2）对IL - 12 p40的产生表现出显著抑制活性（IC50分别为0.01±0.00和1.02±0.01μM）。此外，瘤海星苷（4）对IL - 12 p40和IL - 6的产生表现出中等抑制作用。

结论

这是关于瘤海星抗炎活性的首次报道。本研究的主要发现是从瘤海星中鉴定出具有显著抗炎活性的氧化甾体衍生物，这些衍生物可能被开发为炎症性疾病的治疗药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2185/4347916/f204c023a308/40659_2015_2_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2185/4347916/877b6a696ee8/40659_2015_2_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2185/4347916/0b3c03b8798c/40659_2015_2_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2185/4347916/a597b301c992/40659_2015_2_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2185/4347916/f204c023a308/40659_2015_2_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2185/4347916/877b6a696ee8/40659_2015_2_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2185/4347916/0b3c03b8798c/40659_2015_2_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2185/4347916/a597b301c992/40659_2015_2_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2185/4347916/f204c023a308/40659_2015_2_Fig4_HTML.jpg

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