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Cyclization of flavokawain B reduces its activity against human colon cancer cells

Hum Exp Toxicol. 2020; 
Palko-?abuz A, Kostrzewa-Sus?ow E, Janeczko T, ?roda-Pomianek K, Po?a A, Uryga A, Michalak K.
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Recombinant Proteins (GenScript, Netherlands) The assay was based on the hydrolysis of a substrate DEVD-p-nitroaniline (pNA) by caspase 3 that led to the release of the pNA moiety. Get A Quote

摘要

Chalcones are naturally occurring compounds exhibiting biological activity through multiple mechanisms. Flavokawain B is one of chalcones found in kava plant. In our studies, we focused on the anticancer activity of flavokawain B in colorectal cancer cells LoVo and its resistant to doxorubicin subline-LoVo/Dx. Strong cytotoxic activity of flavokawain B and its ability to inhibit the proliferation in both cell lines was detected. These effects accompanied with induction cell cycle arrest in G2/M phase and the presence of SubG1 fraction. Flavokawain B at low concentration led to increase of caspase-3 activity. The chalcone-induced apoptosis was also confirmed by DNA fragmentation. In our work, the conversion of f... More

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