台灣株Theissenia cinerea醱酵液之生物活性成分研究

Studies on the bioactive constituents of the fermented broth of Theissenia cinerea isolated in Taiwan

李亮欣(Liang-Hsin Lee)

指導教授 ： 李宗徽

臺北醫學大學/藥學院/生藥學研究所/碩士(2010年)

https://doi.org/10.6831/TMU.2010.00161

摘要

在曹 (2009) 的研究中，利用抑制一氧化氮合成酶 （inducible nitric oxide synthase, iNOS）的活性平台來篩選單離自本土的真菌，藉以找尋出具有抗發炎活性的真菌株，發現Theissenia cinerea (#89091602) 的醱酵培養液，對於離體RAW264.7細胞產生一氧化氮的活性，具有顯著的抑制作用。後續本研究中選擇以麥芽抽取物 (malt extract) 為培養基加以擴大培養後，針對醱酵液所含代謝產物進行一系列的分析、分離、純化與結構解析，計分離出9個化合物，分別為：theissenoic acid (1)、theissenoxide (2)、theissenolactone A (3)、theissenolactone B (4)、theissenolactone C (5)、5-hydroxymethylfurfural (6)、bis-2,5-hydroxymethylfuran (7)、succinic acid (8) 和tyrosol (9)，其中1 - 5是過去未曾報導過的新化合物。在細胞毒殺活性上，4和5對於A549肺腺癌細胞具有中等強度的毒殺作用，其GI50分別為14.90與47.92 μM，此外，在iNOS的抑制實驗中，在100 ?慊/mL的濃度下，同樣發現4與5對RAW264.7有100%的毒殺作用，至於其劑量與活性間的相關性有待進一步探究。

關鍵字

真菌 ； 誘導型一氧化氮合成酶Theissenia cinerea ； theissenoic acid ； theissenoxide ； theissenolactone A ； theissenolactone B ； theissenolactone C

並列摘要

In our preview studies, it was found that 13 strains of 34 tested fungus species exhibited significant anti-iNOS activity. Based on this findings, Theissenia cinerea (#89091602) was selected to investigate its bioactive constituents. A series of bioassay-guided chemical examination on the fermented broth of this fungus was carried out, which resulted in the isolation of five new compounds along with four known ones. Their structures were elucidated to be theissenoic acid (1)、 theissenoxide (2)、theissenolactone A (3)、theissenolactone B (4)、theissenolactone C (5)、5-hydroxymethylfurfural (6)、bis-2,5-hydroxymethylfuran (7)、succinic acid (8) and tyrosol (9) on the basis of spectroscopic analysis. Of these compounds identified, compounds 1-5 were new chemical entities. The bioactivities of all the pure isolates were further evaluated. Compounds 4 and 5 exhibited moderate cytotoxicities against A549 lung cancer cell line with GI50 values of 14.90 and 47.92 μM, respectively.

並列關鍵字

iNOS ； Theissenia cinere ； theissenoic acid ； theissenoxide ； theissenolactone A ； theissenolactone B ； theissenolactone C ； cytotoxicitycytotoxicity

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