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Cytotoxicity of Calpain Inhibitor KR‐180
Author(s) -
Alzahrani Roba,
Baashirah Azzah,
Myles Ebert,
Donkor Isaac,
Boadi William,
Wang Xiaofei
Publication year - 2016
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.30.1_supplement.833.2
Subject(s) - calpain , viability assay , cytotoxicity , programmed cell death , proteases , apoptosis , cell culture , chemistry , cancer research , cell , pharmacology , medicine , microbiology and biotechnology , biology , biochemistry , in vitro , enzyme , genetics
Calpains are calcium dependent, non‐lysosomal cysteine proteases. They are expressed ubiquitously in mammals and many other organisms. Excessive activities of calpain have been associated with various diseases, including Alzheimer's disease (AD), cancer, neurological injury, ischemia/reperfusion injury, atherosclerosis, and diabetes and cataract formation. Thus calpain inhibitors are used to treat these diseases. A newly synthesized proprietary compound KR‐180 was investigated for its cytotoxicity in this preliminary study. We tested cell viability after treatment of cells for 24 h with KR‐180 at 1 mM 100 μM, 10 uM, 1 uM, 100 nM, 10 nM. Cell viability was measured by the alamarBlue colorimetric assay. For 3T3‐L1 cells, the KR‐180 treatment at 1 mM reduced cell viability by 80%, while treatment at lower KR‐180 concentrations did not affect 3T3‐L1 viability. The similar effect was observed for lung cancer cell line (A549) where a significant reduction (about 40%) in cell viability was seen at the 1 mM dose. For colon cancer cell line (SW620) and prostate cancer cell line (PC3), all tested KR‐180 concentrations did not cause any significant reduction in viability. In summary, preliminary results suggest that the compound has low cytotoxicity, since it could cause cell death at high concentration 100 μM or higher.