title: A small molecule IFB07188 inhibits proliferation of human cancer cells by inducing G2/M cell cycle arrest and apoptosis.
abstract: A small molecule, 15b-β-hydroxy-5-N-acetylardeemin (IFB07188), was previously isolated from the fungi Aspergillus terreus. However, the toxicological features of this natural product have never been investigated. In present study, we described the anticancer activities of IFB07188. We found that IFB07188 can decrease the viability and invasive potency of multiple cancer cell lines. Further mechanistic investigation demonstrates that cell cycles are arrested at G2/M phase and the arrest is induced by deregulated cell cycle proteins. A concomitant flow cytometric analysis also shows that IFB07188 can trigger massive apoptosis in a dose-dependent manner. The proapoptotic effect of IFB07188-treated cancer cells is characterized by depolarization of mitochondria membrane potential (Δψ(m)) and positive Hochest staining. Finally, results from invasion assay suggest that IFB07188 can suppress tumor cell invasion independent of apoptosis. Collectively, these data establish that IFB07188 can effectively inhibit cancer cell growth and invasiveness, prompting its potential use in cancer chemotherapy.
authors: State Key Laboratory of Pharmaceutical Biotechnology and Model Animal Research Center, Nanjing University, Nanjing, China.
authors: Tingzhe
authors: T
authors: Sun
authors: Wei
authors: W
authors: Zheng
authors: Hui
authors: H
authors: Peng
authors: Aihua
authors: A
authors: Zhang
authors: Yongjun
authors: Y
authors: Chen
authors: Renxiang
authors: R
authors: Tan
authors: Pingping
authors: P
authors: Shen
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D001230:Aspergillus / Q000737:chemistry; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D005260:Female; D005434:Flow Cytometry; D059565:G2 Phase Cell Cycle Checkpoints / Q000187:drug effects; D006801:Humans; D026121:Indole Alkaloids / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D059566:M Phase Cell Cycle Checkpoints / Q000187:drug effects; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects; D009361:Neoplasm Invasiveness
chemical_list: C579037:15b-beta-hydroxy-5-N-acetylardeemin; D000972:Antineoplastic Agents, Phytogenic; D026121:Indole Alkaloids