| 冯妍,韩金媛,张翼,等.两株大白鲨鳃部来源青霉生物碱及其生物活性研究r*[J].中国海洋药物,2016,35(4):16-22. |
| 两株大白鲨鳃部来源青霉生物碱及其生物活性研究r* |
| Study on the Alkaloids from Two Great White Shark's Gill-derived Penicillium Strains and Their Bioactivity |
| 投稿时间：2016-02-01 修订日期：2016-03-08 |
| DOI： |
| 中文关键词: 鲨鱼 真菌 青霉 生物碱 细胞毒 |
| English Keywords:Sharks Fungi Penicillium Alkaloids Cytotoxicity. |
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| 中文摘要: |
| 目的 探索大白鲨鳃部共附生真菌菌株 Penicillium sp. BP2T2 和 Penicillium sp. TBG2-2 的次生代谢产物。方法 利用柱色谱和高效液相色谱对发酵产物进行分离纯化，综合运用质谱、一维与二维核磁共振谱、比旋光测定和圆二色谱来鉴定化合物结构，采用结晶紫法评价化合物细胞毒活性，采用改良的微孔板法评价卤虫 Artemia salina 致死活性，采用纸片法评价其抗菌活性。结果 从菌株 Penicillium sp. BP2T2 发酵产物中分离鉴定到 1 个生物碱 Meleagrin （1），从菌株 Penicillium sp. TBG2-2发酵产物中分离鉴定到3个生物碱，分别为fructigenine A （2）、（-）-cyclopenol （3） 和 viridicatol （4）。化合物 1、2 和 4 显示了对人结肠癌 HCT116 细胞株的细胞毒性，其半抑制浓度（IC50）分别为 5.1 μg/mL、40.5 μg/mL 和 59.0 μg/mL，并显示了对金黄色葡萄球菌或大肠埃希氏菌弱的抑菌活性，25 μg/片剂量下抑菌圈直径为7.5~8.0 mm。化合物 2 对卤虫的 24 h 半致死浓度为 125 μg/mL。结论 首次报道从鲨鱼鳃真菌中分离得到化合物 1~3 以及化合物 1、2 和 4 对 HCT116 细胞株的细胞毒性，鲨鱼鳃真菌作为研究较少的真菌资源在产生生物碱等次生代谢产物方面具有一定潜力。 |
| English Summary: |
| Objective To investigate the secondary metabolites from two symbiotic fungi Penicillium sp. BP2T2 and Penicillium sp. TBG2-2 isolated from the gill of the Carcharodon carcharias（the great white shark）. Methods The isolation and purification of compounds were performed by combined use of column chromatographies and HPLC. Their structures were elucidated by comprehensive analyses of MS，1D- and 2D-NMR，specific optical rotation，and ECD spectra. Their cytotoxicity was evaluated by crystal violet method，their brine shrimp lethality towards Artemia salina was tested by improved microwell test method，and their antimicrobial activity was assayed by paper disk diffusion method and micro-dilution method. Results One alkaloid meleagrin（1）was characterized from Penicillium sp.BP2T2，and 3 alkaloids fructigenine A（2），（-）-cyclopenol（3）and viridicatol（4）were characterized from Penicillium sp. TBG2-2. Preliminary studies showed that 1，2 and 4 showed moderate to weak cytotoxicity against HCT116 human colon cancer cell line with IC50 values of 5.1 μg/mL，40.5 μg/mL and 59.0 μg/ml，respectively. Besides，compounds 1，2 and 4 also displayed weak inhibition against Staphylococcus aureus or Escherichia coli with 7.5~8.0 mm inhibition zone at the doze of 25 μg/disk. Compound 2 was able to kill the brine shrimp larvae with 24 h-LC50 of 125 μg/mL. Conclusion It is the first time to report the isolation of compounds 1–3 from shark-derived fungi and the cytotoxictiy of compounds 1，2 and 4 towards HCT116 cell line. As a less explored resource，shark-derived fungi showed potential in producing secondary metabolites like alkaloids. |
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