title: In Silico and In Vitro Evaluation of Cytotoxic Activities of Farnesiferol C and Microlobin on MCF-7, HeLa and KYSE Cell Lines.
abstract: Background:Cancer is one of the leading causes of death worldwide. Despite certain advances in cancer therapy, still there is considerable demand for developing efficient therapeutic agents. Nowadays, there is a rising interest in the use of natural-based anti-cancer drugs. In this study, the cytotoxicity of farnesiferol C and microlobin isolated fromFerula szowitsianawas investigated against MCF-7, HeLa and KYSE cancer cell lines. In addition, the mechanism of binding of these compounds to apoptotic proteins (Bax, Bak and Bcl-2) was analyzed by anin silicomethod.Materials and methods:We used MTT assay in order to assess the cytotoxicity of compounds against cancer cell lines. Forin silicostudy, the AutoDock 4 was adopted.Results and discussion:According to thein vitrofindings, in general, farnesiferol C showed significant cytotoxicity at higher concentrations (>50 µM) following 48 and 72 h incubation with the selected cancer cells; however, microlobin exhibited almost no activity at concentrations up to 100 µM. Thein silicoresults revealed that both compounds could bind to Bax more efficiently rather than to Bcl-2 or Bak proteins.Conclusion:The results obtained by our preliminaryin vitroandin silicostudies suggest that these compounds might induce apoptosis through Bax activation; however further studies, eitherin vitroorin vivoare needed to clarify these activities.
authors.affiliation: Cellular and Molecular Research Center, Sabzevar University of Medical Sciences, Sabzevar, Iran.
authors.forename: L
authors.initials: L
authors.lastname: Aldaghi
authors.affiliation: Cellular and Molecular Research Center, Sabzevar University of Medical Sciences, Sabzevar, Iran.
authors.forename: A
authors.initials: A
authors.lastname: Rad
authors.affiliation: Biotechnology Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.
authors.forename: A
authors.initials: A
authors.lastname: Arab
authors.affiliation: Natural Products and Medicinal Plants Research Center, North Khorasan University of Medical Sciences, Bojnurd, Iran.
authors.forename: J
authors.initials: J
authors.lastname: Kasaian
authors.affiliation: Biotechnology Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.
authors.forename: M
authors.initials: M
authors.lastname: Iranshahi
authors.affiliation: Bioinformatics Research Center, Sabzevar University of Medical Sciences, Sabzevar, Iran.
authors.forename: A S
authors.initials: AS
authors.lastname: Sadr
authors.affiliation: Biotechnology Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.
authors.forename: F
authors.initials: F
authors.lastname: Soltani
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003374:Coumarins / Q000302:isolation & purification / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005309:Ferula / Q000737:chemistry; D006801:Humans; D062105:Molecular Docking Simulation; D011485:Protein Binding; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000378:metabolism; D012717:Sesquiterpenes / Q000302:isolation & purification / Q000494:pharmacology*; D050998:bcl-2 Homologous Antagonist-Killer Protein / Q000378:metabolism; D051028:bcl-2-Associated X Protein / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; C494772:BAK1 protein, human; D003374:Coumarins; D019253:Proto-Oncogene Proteins c-bcl-2; D012717:Sesquiterpenes; D050998:bcl-2 Homologous Antagonist-Killer Protein; D051028:bcl-2-Associated X Protein; C000618754:microlobin; C553326:farnesiferol C