title: Pyrophen Produced by Endophytic Fungi Aspergillus sp Isolated from Piper crocatum Ruiz and Pav Exhibits Cytotoxic Activity and Induces S Phase Arrest in T47D Breast Cancer Cells.
abstract: Ethyl acetate extracts obtained from culture of endophytic fungi Aspergillus sp isolated from Piper crocatum Ruiz and Pav, have been shown to possess cytotoxic activity against T47D breast cancer cells. Investigations were here conducted to determine bioactive compounds responsible for the activity. Bioassay guided fractionation was employed to obtain active compounds. Structure elucidation was performed based on analysis of LC-MS, 1H-NMR, 13C-NMR, COSY, DEPT, HMQC, HMBC data. Cytotoxity assays were conducted in 96 well plates against T47D and Vero cell lines. Bioassay guided isolation and chemical investigation led to the isolation of pyrophen, a 4-methoxy-6-(1'-acetamido-2'-phenylethyl)-2H-pyran-2-one. Further analysis of its activity against T47D and Vero cells showed an ability to inhibit the growth of T47D cells with IC50 values of 9.2 μg/mL but less cytotoxicity to Vero cells with an IC50 of 109 μg/mL. This compound at a concentration of 400 ng/mL induced S-phase arrest in T47D cells.
authors.affiliation: Pharmaceutical Biology Department, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta, Indonesia E-mail : puji_astuti@ugm.ac.id.
authors.forename: Puji
authors.initials: P
authors.lastname: Astuti
authors.forename: Willy
authors.initials: W
authors.lastname: Erden
authors.lastname: Wahyono
authors.forename: Subagus
authors.initials: S
authors.lastname: Wahyuono
authors.forename: Triana
authors.initials: T
authors.lastname: Hertiani
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects*; D001230:Aspergillus / Q000737:chemistry*; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology*; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D002522:Chlorocebus aethiops; D005260:Female; D006801:Humans; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000494:pharmacology; D031701:Piper / Q000737:chemistry*; D010936:Plant Extracts / Q000494:pharmacology*; D066244:Proton Magnetic Resonance Spectroscopy; D011753:Pyrones / Q000494:pharmacology*; D016196:S Phase / Q000187:drug effects*; D014407:Tumor Cells, Cultured; D014709:Vero Cells
chemical_list: D010936:Plant Extracts; D011753:Pyrones; C067225:pyrophen; D010649:Phenylalanine