| 刘明香,许聪聪,李冉,等.海绵共附生真菌Nigrospora sp.的次级代谢产物及PD-1/PD-L1抑制活性研究[J].中国海洋药物,2020,39(3):1-6. |
| 海绵共附生真菌Nigrospora sp.的次级代谢产物及PD-1/PD-L1抑制活性研究 |
| Chemistry and PD-1/PD-L1 inhibitory activity of secondary metabolites from the sponge-associated fungus Nigrospora sp. |
| 投稿时间：2020-02-13 修订日期：2020-02-19 |
| DOI： |
| 中文关键词: 海绵共附生真菌 黑孢霉属 次生代谢产物 PD-1/PD-L1抑制活性 |
| English Keywords:Sponge-associated fungus Nigrospora sp. secondary metabolites PD-1/ PD-L1 inhibitory activity |
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| 中文摘要: |
| 目的 研究海绵Callyspongia sp.共附生真菌Nigrospora sp.中化学成分以及生物活性。 方法 利用正相硅胶柱层析、Sephadex LH-20凝胶柱层析和半制备型反相高效液相色谱(RPLC)等方法对该菌株乙酸乙酯提取物进行分离纯化；通过核磁共振谱(NMR)、质谱(MS)等技术并结合文献报道数据分析鉴定化合物结构；采用均相时间分辨荧光(HTRF)法检测化合物的PD-1/PD-L1结合抑制活性。结果 分离得到7个已知化合物,分别为punctaporonin D (1),punctaporonin E (2),punctaporonin F (3),desuccinoylpunctaporonin C (4),(20S, 22E, 24R)-麦角甾-7, 22-二烯-3β, 5α, 6β-三醇 (5),(22E, 24R)-麦角甾-3β-羟基-5α, 9α-环氧-7, 22-二烯-6-酮 (6),麦角甾-7, 22-二烯-6β-甲氧基-3β, 5α-二醇 (7)。在体外生物活性检测中,化合物6显示出PD-1/PD-L1结合抑制活性,其IC50值为22.5 μmol/L。结论 化合物4为新天然产物,化合物1-3和化合物6为首次从该属真菌中分离得到。化合物6显示PD-1/PD-L1结合抑制活性。 |
| English Summary: |
| Objective To investigate bioactive secondary metabolites of fungus Nigrospora sp. associated with the sponge Callyspongia sp. Methods The ethyl acetate extract of the strain was isolated and purified by normal phase silica gel column chromatography, gel Sephadex LH-20 and semi-preparative reversed phase liquid chromatography (RPLC). The structures of the compounds were identified by sereval modern spectral technologies including nuclear magnetic resonance (NMR) and mass spectrometry (MS). The PD-1/ PD-L1 binding inhibitory activity of the compounds were detected using homogenegous time resolved fluorescence (HTRF). Results Seven known compounds were isolated and identified as punctaporonin D (1), punctaporonin E (2), punctaporonin F (3), desuccinoylpunctaporonin C (4), (20S, 22E, 24R)-ergosta-7, 22-dien-3β, 5α, 6β-triol (5), 3β-hydroxy-5α, 9α-epoxy-(22E, 24R)-ergosta-7, 22-dien-6-one (6), ergost-7, 22-dien-6β-methoxy-3β, 5α-diol (7). Compound 6 showed PD-1/ PD-L1 binding inhibitory activity with IC50 of 22.5 μmol/L . Conclusion Compound 4 was reported as a new natural product while compounds 1-3 and 6 were reported from the Nigrospora sp. for the first time. Compound 6 showed a PD-1/ PD-L1 binding inhibitory activity in in vitro biotest. |
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