| 摘要: | 本研究利用抑制一氧化氮生成的活性分析平台來篩選真菌培養株，期能找出具有抗發炎活性的真菌株，發現所篩選的53株真菌中，8株真菌株的醱酵培養液或菌絲體萃出物，對於RAW264.7 細胞的生成一氧化氮具有顯著的抑制作用或對於 RAW264.7 細胞具強的細胞毒性，後續選定Bipolaris sp. #NTOU799 及 Pseudallescheria boydii #NTOU2362 兩菌株進行其醱酵液成分研究。
在擴大培養後，針對所含代謝產物進行分析、分離、純化與鑑定，計獲得14個化合物，分別為﹕boydone A (1)、boydone B (2)、fusidilactones A (3)、L-mevalonolactone (4)、lactic acid (5)、ovalicin (6)、botryorhodine C (7)、botryorhodine G (8)、botryorhodine F (9)、N-(2-phenylethyl)-acetamide (10)、N-(4-hydroxyphenethyl)-acetamide (11)、bipopeptide A (12)、L-ornithine, 4-hydroxy-N5-L-phenylalanyl (13) 和 Cyclo (glycyl-L-proline) (14)，其中化合物1、2、8、9 及 12為新化合物。在生物活性上，化合物 2 及 6對於肺腺癌A549細胞的生長相較於正控制組 (5-FU，GI50 = 3.6 μM)，分別具中等及強的抑制活性，其生長半抑制濃度 (GI50) 分別為41.34 及 4.07 μM。
In the preliminary biological screening, the fermented mycelia or broths of 8 out of 53 tested fungal strains were found to exhibited significant bioactivities. Among them, the EtOAc extracts of the fermented broths of Bipolaris sp. #NTOU799 and Pseudallescheria boydii #NTOU2362 exhibited significant both inhibitory activities of NO production and cytotoxicities in RAW264.7 cells.
A series of extraction, separation and purification of chemical entities from these fermented broths were thus carried out, which have resulted in the isolation and identification of fourteen compounds 1-14.
Their structures were elucidated to be boydone A (1), boydone B (2), fusidilactones A (3), L-mevalonolactone (4), lactic acid (5), ovalicin (6), botryorhodine C (7), botryorhodine G (8), botryorhodine F (9), N-(2-phenylethyl)-acetamide (10), N-(4-hydroxyphenethyl)-acetamide (11), bipopeptide A (12), L-ornithine, 4-hydroxy-N5-L-phenylalanyl (13), and cyclo (glycyl-L-proline) (14).
Of these compounds identified, 1, 2, 8, 9, and 12 were novel. Compounds 2 and 6 showed moderate to potent cytotoxicities against A549 lung cancer cell line when compared with 5-FU, and the GI50 values were determined to be 41.34 and 4.07 μM, respectively. |
