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

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 subli...

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Bibliographic Details
Published in:Human & experimental toxicology 2020-03, Vol.39 (3), p.262-275
Main Authors: Palko-Łabuz, A, Kostrzewa-Susłow, E, Janeczko, T, Środa-Pomianek, K, Poła, A, Uryga, A, Michalak, K
Format: Article
Language:English
Subjects:
Anticancer properties
Antitumor activity
Apoptosis
Biological activity
Biological effects
Cancer
Caspase-3
Cell cycle
Cell proliferation
Colon
Colon cancer
Colorectal cancer
Colorectal carcinoma
Cytotoxicity
DNA fragmentation
Doxorubicin
Toxicity
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Summary: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 flavokawain B to corresponding flavanone—5,7-dimetoxyflavanone—was shown to be more extensive in cancer than in non-cancer cells. We found that the cyclization of the chalcone was related to the significant decrease in the cytotoxicity. Cell proliferation and cell cycle progression were not impaired significantly in the studied cancer cells incubated with 5,7-dimethoxyflavanone. We did not observe apoptosis in the cells incubated with flavanone. The results from biological studies agreed with the theoretical activity that emerges from structural parameters.
ISSN:0960-3271
1477-0903
DOI:10.1177/0960327119882986