The anticancer activity of 3- and 10-bromofascaplysins is mediated by caspase-8, -9, -3-dependent apoptosis.
3- and 10-Bromofascaplysins was previously found to possess cytotoxic activity. In this study, we investigated their cancer preventive and proapoptotic properties. These effects were tested on mouse skin epidermal JB6 P(+) Cl41 cell line, its stable transfectants, and human tumor HL-60, THP-1, SNU-C4, SK-MEL-28, DLD-1, MDA-MB-231, and HeLa cells using a variety of assessments, including a cell viability (MTS) assay, flow cytometry, anchorage-independent soft agar assay, luciferase assay, mitochondrial permeability assay, and Western blotting. 3- and 10-Bromofascaplysins were effective at submicromolar concentrations as the anticancer agents, which exerted their action, at least in part, through the induction of caspase-8, -9, -3-dependent apoptosis.
Kuzmich
Alexandra S
AS
Pacific Institute of Bioorganic Chemistry, 159 Prospect 100-Let Vladivostoku, Vladivostok 690022, Russian Federation.
Fedorov
Sergey N
SN
Shastina
Valeria V
VV
Shubina
Larisa K
LK
Radchenko
Oleg S
OS
Balaneva
Nadezda N
NN
Zhidkov
Maxim E
ME
Park
Joo-In
JI
Kwak
Jong Y
JY
Stonik
Valentin A
VA
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D053148:Caspase 3 / Q000378:metabolism; D053181:Caspase 8 / Q000378:metabolism; D053453:Caspase 9 / Q000378:metabolism; D020169:Caspases / Q000378:metabolism*; D002460:Cell Line; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D051379:Mice; D008928:Mitochondria / Q000378:metabolism; D010539:Permeability / Q000187:drug effects; D012867:Skin / Q000166:cytology
D000970:Antineoplastic Agents; D053148:Caspase 3; D053181:Caspase 8; D053453:Caspase 9; D020169:Caspases