Anticancer Activity of (±)-Kusunokinin Derivatives towards Cholangiocarcinoma Cells
Issued Date
2022-12-01
Resource Type
eISSN
14203049
Scopus ID
2-s2.0-85143618029
Pubmed ID
36500383
Journal Title
Molecules
Volume
27
Issue
23
Rights Holder(s)
SCOPUS
Bibliographic Citation
Molecules Vol.27 No.23 (2022)
Suggested Citation
Rattanaburee T., Sermmai P., Tangthana-umrung K., Thongpanchang T., Graidist P. Anticancer Activity of (±)-Kusunokinin Derivatives towards Cholangiocarcinoma Cells. Molecules Vol.27 No.23 (2022). doi:10.3390/molecules27238291 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/83511
Title
Anticancer Activity of (±)-Kusunokinin Derivatives towards Cholangiocarcinoma Cells
Other Contributor(s)
Abstract
This study aimed to investigate the cytotoxicity and anticancer activity of (±)-kusunokinin derivatives ((±)-TTPG-A and (±)-TTPG-B). The cytotoxicity effect was performed on human cancer cells, including breast cancer, cholangiocarcinoma, colon and ovarian cancer-cells, compared with normal cells, using the MTT assay. Cell-cycle arrest and apoptosis were detected using flow-cytometry analysis. We found that (±)-TTPG-B exhibited the strongest cytotoxicity on aggressive breast-cancer (MDA-MB-468 and MDA-MB-231) and cholangiocarcinoma (KKU-M213), with an IC50 value of 0.43 ± 0.01, 1.83 ± 0.04 and 0.01 ± 0.001 µM, respectively. Interestingly, (±)-TTPG-A and (±)-TTPG-B exhibited less toxicity than (±)-kusunokinin (9.75 ± 0.39 µM) on L-929 cells (normal fibroblasts). Moreover, (±)-TTPG-A predominated the ell-cycle arrest at the S phase, while (±)-TTPG-B caused cell arrest at the G0/G1 phase, in the same way as (±)-kusunokinin in KKU-M213 cells. Both (±)-TTPG-A and (±)-TTPG-B induced apoptosis and multi-caspase activity more than (±)-kusunokinin. Taken together, we conclude that (±)-TTPG-A and (±)-TTPG-B have a strong anticancer effect on cholangiocarcinoma. Moreover, (±)-TTPG-B could be a potential candidate compound for breast cancer and cholangiocarcinoma in the future.