A Pair of New Spirocyclic Alkaloid Enantiomers with TrxR Inhibitory Activities Were Isolated from Marine-Derived Aspergillus ruber TX-M4-1  

作　　者：WANG Cong WANG Yufei SUN Jian WANG Shiyi DU Weisheng ZHOU Liman KONG Fandong 

机构地区：[1]Key Laboratory of Chemistry and Engineering of Forest Products,State Ethnic Affairs Commission,Guangxi Key Laboratory of Chemistry and Engineering of Forest Products,Guangxi Minzu University,Nanning 530006,China [2]Guangxi Collaborative Innovation Center for Chemistry and Engineering of Forest Products,Key Laboratory of Universities in Guangxi for Excavation and Development of Ancient Ethnomedicinal Recipes,Guangxi Minzu University,Nanning 530006,China

出　　处：《Journal of Ocean University of China》2023年第6期1677-1682,共6页中国海洋大学学报（英文版）

基　　金：supported by the National Natural Science Foundation of China(No.82204276);the Guangxi Natural Science Foundation(No.2021GXNSFBA075036);the Specific Research Project of Guangxi for Research Bases and Talents(Nos.AD22035018,AD20297036);the 2021 University-Level Scientific Research Projects of Guangxi Minzu University(No.2021MDKJ003);the Talent Scientific Research Initiation Project of Guangxi Minzu University(No.2021KJQD09);the Xiangsi Lake Youth Innovation Team Project of Guangxi Minzu University(No.2021 RSCXSHQN01);the Guangxi Scholarship Fund of Guangxi Education Department.

摘　　要：One new spirocyclic alkaloid,5-isopentenyl-cryptoechinuline D(1),along with 11 known compounds(2–12),were iso-lated from a marine fungus Aspergillus ruber TX-M4-1.The structures of compounds 1–12 were elucidated by spectroscopic evi-dences.Compound 1 was initially isolated as an enantiomer,and further separation of 1 by chiral HPLC afforded a pair of enantio-mers,including(-)-5-isopentenyl-cryptoechinuline D(1a)and(+)-5-isopentenyl-cryptoechinuline D(1b).Their absolute configura-tions were elucidated by ECD spectroscopic data.Compounds 1a,5 and 10 could inhibit thioredoxin reductase(TrxR)activity with IC50 values of 6.2,36.3 and 18.6μmol L^(-1),respectively.Surface plasmon resonance(SPR)study also demonsrated the interactions between compounds 6,8 and Niemann-Pick C1 Like 1(NPC1L1)respectively,which indicate that compounds 6 and 8 are potential NPC1L1 inhibitors.

关 键 词：Aspergillus ruber TX-M4-1 spirocyclic alkaloid TrxR inhibitory activity 

分 类 号：R915[医药卫生—微生物与生化药学]