耐盐真菌Aspergillus variecolor B-17产生的烃基苯甲醛衍生物及其细胞毒活性

Alkyl Benzaldehyde Derivatives and Their Cytotoxicities from Halotolerant Fungus Aspergillus variecolor B-17

为从极端环境微生物中获得抗肿瘤药物先导化合物,作者从采自内蒙古盐湖的沉积物中分离了96株耐盐真菌。采用小鼠乳腺癌细胞株tsFT210和海虾(Artemia salina Leach)筛选抗肿瘤活性微生物,1株耐盐真菌AspergillusvariecolorB-17表现出明显的细胞毒活性和海虾致死活性。采用活性跟踪的分离方法,从该菌株的大量发酵产物的石油醚层提取物中分离得到了3个单体化合物。通过一维、二维超导核磁共振、质谱等波谱方法确定其结构分别为:2-(E-1-庚烯基)-3,6-二羟基-5-(3-甲基-2-丁烯基)苯甲醛(1)、2-庚基-3,6-二羟基-5-(3-甲基-2-丁烯基)苯甲醛(2)、2-(E,E-3,5-庚二烯基)-3,6-二羟基-5-(3-甲基-2-丁烯基)苯甲醛(3)。化合物1、2和3对P388、A549、HL-60和BEL-7402肿瘤细胞表现弱的细胞增殖抑制活性,IC50值分别为88,68,66,65μmol/L,9,99,110,84μmol/L以及77,147,93,203μmol/L。

In order to search for structurally novel and biologically active compounds from extreme microorganisms, 96 strains of halotolerant fungi were screened for their anti-tumor activities using brine shrimp, Artemia salina Leach, and the mouse temperature-sensitive p34^cdc2 mutant cell line tsFT210. The EtOAc extract of Aspergillus variecolor B-17 exhibited obvious cytotoxicity and lethality against tsFT210 cells and Artemia salina, respectively. Three alkyl benzaldehyde derivatives were isolated from the petroleum ether partition of the fermentation broth of A. variecolor B-17. By the spectroscopic method, their structures were identified as 2-（E-1-heptenyl）-3, 6-dihydroxy-5-（3-methyl-2-butenyl）benzaldehyde（1）, 2-heptyl-3, 6-dihydroxy-5- （3-methyl-2-butenyl） benzaldehyde （ 2 ）, 2- （ 3E, 5E-heptadienyl ）-3, 6-dihydroxy-5-（ 3-methyl-2- butenyl ） benzaldehyde（3）, respectively. Compounds 1-3 showed weak cytotoxicity against P388, A549, HL-60 and BEL-7402 cells with the IC50 values of 88, 68, 66 and 65μmol/L, 9, 99, 110 and 84μmol/L, and 77, 147, 93 and 203μmol/L, respectively.