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1、深海来源的微生物抗肿瘤活性筛选及次级代谢产物的初步研究蔡生新，赵博宇，朱天骄，顾谦群*，（教育部海洋药物重点实验室，中国海洋大学医药学院，青岛，266003)摘要：目的对来自深海的海水、海泥样品进行了微生物分离并通过抗肿瘤活性筛选获得活性菌株，并研究活性菌株6a的次级代谢产物。方法从样品中选择性分离得到真菌，采用SRB法对分离得到真菌的发酵产物进行抗肿瘤活性筛选；采用现代分离手段对菌株6a发酵产物进行了活性追踪分离，通过理化性质及波谱学手段进行化学结构鉴定。结果与结论从深海来源的样品中共分离获得29株真菌，其中7株具有细胞毒活性；从活性菌株6
2、a的发酵产物中分离得到10个单体化合物（1-10），其化学结构分别鉴定为8,9-dehydro-DesoxybrevianamideE(1)，8,9-dehydro-12,13-dehydro-DesoxybrevianamideE(2),8,9-dehydro-12-hydroxyl-DesoxybrevianamideE(3),8,9-dehydro-12-methoxyl-DesoxybrevianamideE(4),DesoxybrevianamideE(5),5-methoxysterigmatocystin(6),5,4’-dem
3、ethoxylsterigmatocystin(7),5,4’-demethoxyl-sterigmatocystinA(8),4’-methoxylsterigmatocystin(9),averufin(10),其中化合物1-4、7-9为新化合物。关键词：深海来源真菌；次级代谢产物；抗肿瘤活性AntitumorscreeningofdeepoceanwaterandsedimentsderivedfungiandprimaryinvestigationoftheirsecondarymetabolitesCAISheng-xin,ZHAO
4、Bo-yu,ZHUTian-jiao,GUQian-qun*(KeyLaboratoryofMarineDrugs,ChineseMinistryofEducation,SchoolofMedicineandPharmacy,OceanUniversityofChina,Qingdao266003,China)ABSTRACT:OBJECTIVEThecytotoxicmicrobialstrainsisolatedfromthedeepoceanwaterandsedimentswerescreened,andthesecondarymet
5、abolitesofactivefungus6awereinvestigated.METHODSActivemicrobialstrainswerescreenedusingchronicmedullaleucocythemia(K562)cellline.Bioactivefractionswereobtainedfromthecrudeextractof6athroughabioassay-guidedfractionationandthechemicalconstituentsofthefractionswereinvestigated
6、andpurifiedbythecombineduseofcolumnchromatographywithsilicagelandSephadexLH-20,thepreparativeHPLC.Theirstructureswereestablishedbyspectroscopicmethods.RESULTSANDCONCLUSIONTwentyninestrainsoffungiwereisolated.Amongthem,sevenstrainsshowedcytotoxicactivities.Tencompounds(1-10)
7、wereisolatedfromtheactivestrain6aandidentifiedas8,9-dehydro-DesoxybrevianamideE(1)，8,9-dehydro-12,13-dehydro-DesoxybrevianamideE(2),8,9-dehydro-12-hydroxyl-DesoxybrevianamideE(3),8,9-dehydro-12-methoxyl-DesoxybrevianamideE(4),DesoxybrevianamideE(5),5-methoxysterigmatocystin
8、(6),5,4’-demethoxylsterigmatocystin(7),5,4’-demethoxyl-sterigmatocystinA(8),84’-me
