KO-202125, a sauristolactam derivate, induces apoptosis to prevent KB human oral squamous carcinoma cells through inhibition of cyclooxygenase-2 expression
- Authors
- Leem, Dae-Ho; Choi, Kyeong-Hee; Han, Hye-Suk; Kim, Jun-Hee; Shin, Ji-Ae; Choi, Eun-Sun; Shim, Jung-Hyun; Kong, Gu; Min, Yong-Ki; Nam, Jeong-Seok; Oh, Seung Hyun; Kim, Kyoung-A; Kwon, Ki Han; Cho, Nam-Pyo; Cho, Sung-Dae
- Issue Date
- Jan-2010
- Publisher
- LIPPINCOTT WILLIAMS & WILKINS
- Keywords
- apoptosis; celecoxib; cyclooxygenase-2; KB human oral squamous carcinoma cells; KO-202125; PGE(2)
- Citation
- EUROPEAN JOURNAL OF CANCER PREVENTION, v.19, no.1, pp.23 - 30
- Indexed
- SCIE
SCOPUS
- Journal Title
- EUROPEAN JOURNAL OF CANCER PREVENTION
- Volume
- 19
- Number
- 1
- Start Page
- 23
- End Page
- 30
- URI
- https://scholarworks.bwise.kr/hanyang/handle/2021.sw.hanyang/175571
- DOI
- 10.1097/CEJ.0b013e328333d09e
- ISSN
- 0959-8278
- Abstract
- In a previous study, we demonstrated that cyclooxygenase-2 (COX-2) is overexpressed in Korean patients having oral cancer. The goal of this study was to study whether KO-202125 (KO), a sauristolactam derivative in KB human oral squamous carcinoma cells, inhibits the activity of COX-2 enzyme and induces apoptotic cell death. In this study, it was shown that KO inhibited COX-2 mRNA and protein and its catalytic activity (prostaglandin EA but not COX-1. The anti proliferative effect of KO on KB cells was also examined. The results showed that KO significantly decreased the number of viable cells and showed morphological changes in a concentration-dependent manner. The decrease in cell number was associated with apoptotic cell death evidenced by cleaved poly ADP ribose polymerase (PARP), nuclear fragmentation, sub-G, population and annexin V positivity. Interestingly, KO is more potent than celecoxib, which is a well-known selective COX-2 inhibitor, although more studies are needed to prove it. Altogether, these results show that KO can act as a potent antioral cancer drug candidate by regulating COX-2 activity.
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