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Archive > Volume 11 Issue 1 > 2019,11(1):108-112. DOI:10.1016/j.chmed.2018.10.004 Prev Next

龍膽苦苷對(duì)炎癥靶點(diǎn)iNOS和COX-2抗炎活性研究

Original articles

Anti-inflammatory activities of gentiopicroside against iNOS and COX-2 targets

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    摘要:
    目的 本文旨在從中藥材黃管秦艽中分離出高純度龍膽苦苷化合物，并通過其對(duì)炎癥靶點(diǎn)的抑制作用來考察其抗炎活性。方法 采用HPLC、IR、NMR和MS等方法對(duì)龍膽苦苷的純度及分子結(jié)構(gòu)進(jìn)行了鑒定，并通過體內(nèi)、體外及分子對(duì)接實(shí)驗(yàn)考察其抗炎活性。結(jié)果 體外實(shí)驗(yàn)以小鼠巨噬細(xì)胞RAW264.7為研究對(duì)象，考察不同濃度的龍膽苦苷對(duì)脂多糖誘導(dǎo)的小鼠巨噬細(xì)胞產(chǎn)生NO以及釋放炎癥因子PEG2及1L-6的抑制狀況，結(jié)果表明，龍膽苦苷能夠明顯抑制NO及炎癥因子PEG2、1L-6產(chǎn)生和釋放。體內(nèi)實(shí)驗(yàn)以KM小鼠為研究對(duì)象，利用二甲苯致小鼠耳腫脹實(shí)驗(yàn)考察龍膽苦苷對(duì)急性炎癥的抑制活性，結(jié)果發(fā)現(xiàn)龍膽苦苷能有效的抑制小鼠耳腫脹且抑制率達(dá)34.17%。分子模擬對(duì)接實(shí)驗(yàn)發(fā)現(xiàn)龍膽苦苷中的糖片段能夠與炎癥靶點(diǎn)COX-2及iNOS中的氨基酸以氫鍵的形式有效的結(jié)合，進(jìn)而通過對(duì)二者的抑制作用表現(xiàn)出其生物活性。結(jié)論 龍膽苦苷是一種潛在的且對(duì)炎癥靶點(diǎn)COX-2及iNOS具選擇性的抑制劑，具有良好的抗炎活性。

    Abstract:
    Objective To isolate high-purity gentiopicroside from the Chinese herbal Gentiana officinalis and investigate its anti-inflammatory activity against iNOS and COX-2 targets. Methods The purity and structures of gentiopicroside was determined by HPLC, IR, NMR, and MS. We investigated the anti-inflammatory effects of gentiopicroside by in vivo， in vitro and molecular experiments. Results In vitro experiment results showed that gentiopicroside inhibited nitric oxide (NO), prostaglandin E2 (PGE2), and interleukin-6 (IL-6) production in mouse macrophages RAW 264.7 stimulated by lipopolysaccharide. In vivo experiment found xylene-induced mouse ear swelling was inhibited by gentiopicroside with an inhibition rate of 34.17%. Molecular docking of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) with gentiopicroside showed that hydrogen bonds (H-bonds) were formed between the sugar fragments in gentiopicroside structure with Tyr355, Ser353, Leu352, Ser530, Arg120, and His90 of COX-2, and Glu377, Asp382, Tyr373, Tyr347, Gln263, Asn370, and Gly371 of iNOS. Thus, gentiopicroside had a lower docking score and displayed satisfactory anti-inflammatory activities. Conclusion These results suggested that the mechanism of anti-inflammatory activity of gentiopicroside was associated with the downregulation of inflammatory cytokines, such as NO, PGE2, and IL-6, and the suppression of iNOS and COX-2. Therefore, gentiopicroside is a potential and selective iNOS and COX-2 inhibitor.

    關(guān)鍵詞:
    龍膽苦苷;抗炎活性;環(huán)氧合酶-2;一氧化氮合酶;炎癥靶點(diǎn)

    Keywords:


    Project Supported:
    We sincerely thank Lanzhou University Dr. Huan-xiang Liu gave us great help in molecular docking experiments. National Natural Science Foundation of China (No. 81660577, No. 21562001, and No. 81560716) and National Natural Science Foundation of Gansu Province (1506RJZA036).

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