title: Conjugation of substituted ferrocenyl to thiadiazine as apoptosis-inducing agents targeting the Bax/Bcl-2 pathway.
abstract: Ferrocene compounds are a class of biologically active compounds that has antitumour and antifungal properties. This study investigated the induction of apoptosis in human fibrosarcoma cells (HT1080) after treatment with a series of 6-ferrocenyl-3-subsituted7H-1,2,4-triazolo[3,4-b]- 1,3,4-thiadiazine (FTFs). We found that FTFs could suppress the viability of HT1080 cells. Cell cycle analysis showed that proliferative inhibition of HT1080 cells occurred through apoptosis, as the cells were blocked in G1 phase. Moreover, mitochondrial membrane staining assay demonstrated that FTFs exposure significantly decreased mitochondrial membrane potential. Finally, under the stress of FTFs, Bax/Bcl-2 ratio in HT1080 cells was significantly increased. These results suggested that FTFs-induced apoptosis in HT1080 cells may work dependent on a Bax/Bcl-2 pathway.
authors.affiliation: School of Life Sciences, Lanzhou University, Lanzhou 730000, PR China.
authors.forename: Ruidong
authors.initials: R
authors.lastname: Miao
authors.forename: Juan
authors.initials: J
authors.lastname: Wei
authors.forename: Minghua
authors.initials: M
authors.lastname: Lv
authors.forename: Yan
authors.initials: Y
authors.lastname: Cai
authors.forename: Yuping
authors.initials: Y
authors.lastname: Du
authors.forename: Xinping
authors.initials: X
authors.lastname: Hui
authors.forename: Qin
authors.initials: Q
authors.lastname: Wang
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D005354:Fibrosarcoma / Q000188:drug therapy; D006801:Humans; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects; D013829:Thiadiazines / Q000737:chemistry* / Q000494:pharmacology*; D051028:bcl-2-Associated X Protein / Q000378:metabolism*
chemical_list: D000970:Antineoplastic Agents; D019253:Proto-Oncogene Proteins c-bcl-2; D013829:Thiadiazines; D051028:bcl-2-Associated X Protein