title: Diasteltoxins A-C, Asteltoxin-Based Dimers from a Mutant of the Sponge-Associated Emericella variecolor Fungus.
abstract: Three novel asteltoxin-bearing dimers namely diasteltoxins A-C (1-3) along with asteltoxin were isolated from a mutated strain of a sponge-derived fungus Emericella variecolor XSA-07-2. Their structures were determined by extensive spectroscopic analyses including the computed electronic circular dichroism (ECD) data for the configurational assignment. The biogenetic formation of the dimers through [2 + 2] cycloaddition of asteltoxin was postulated. Diasteltoxins 1-3 exerted inhibitory effects against the tumor cell lines H1299 and MCF7 and exhibited significant inhibition against thioredoxin reductase (TrxR).
authors: State Key Laboratory of Natural and Biomimetic Drugs, Peking University , Beijing 100191, P. R. China.
authors: Hailin
authors: H
authors: Long
authors: State Key Laboratory of Natural and Biomimetic Drugs, Peking University , Beijing 100191, P. R. China.
authors: Zhongbin
authors: Z
authors: Cheng
authors: State Key Laboratory of Natural and Biomimetic Drugs, Peking University , Beijing 100191, P. R. China.
authors: Wei
authors: W
authors: Huang
authors: State Key Laboratory of Natural and Biomimetic Drugs, Peking University , Beijing 100191, P. R. China.
authors: Qi
authors: Q
authors: Wu
authors: State Key Laboratory of Natural and Biomimetic Drugs, Peking University , Beijing 100191, P. R. China.
authors: Xiaodan
authors: X
authors: Li
authors: State Key Laboratory of Natural and Biomimetic Drugs, Peking University , Beijing 100191, P. R. China.
authors: Jingrong
authors: J
authors: Cui
authors: Institute of Pharmaceutical Biology and Biotechnology, Heinrich-Heine University , 40225 Duesseldorf, Germany.
authors: Peter
authors: P
authors: Proksch
authors: State Key Laboratory of Natural and Biomimetic Drugs, Peking University , Beijing 100191, P. R. China.
authors: Wenhan
authors: W
authors: Lin
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D019281:Dimerization; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D032842:Emericella / Q000235:genetics*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D057809:HEK293 Cells; D006801:Humans; D061986:MCF-7 Cells; D008968:Molecular Conformation; D009154:Mutation; D011161:Porifera / Q000382:microbiology*; D011753:Pyrones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013880:Thioredoxin-Disulfide Reductase / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011753:Pyrones; C030923:asteltoxin; D013880:Thioredoxin-Disulfide Reductase