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LYG-202 inhibits the proliferation of human colorectal carcinoma HCT-116 cells through induction of G1/S cell cycle arrest and apoptosis via p53 and p21(WAF1/Cip1) expression.
Biochem Cell Biol. 2011 Jun; 89(3):287-98.BC

Abstract

We recently established that LYG-202, a new flavonoid with a piperazine substitution, exerts an anti-tumor effect in vivo and in vitro. In the present study, we demonstrate that LYG-202 induces G1/S phase arrest and apoptosis in human colorectal carcinoma HCT-116 cells. Data showed that the blockade of the cell cycle was associated with increased p21(WAF1/Cip1) and Rb levels and reduced expression of cyclin D1, cyclin E, and CDK4. Moreover, PARP cleavage, activation of caspase-3, caspase-8, and caspase-9, and an increased ratio of Bax/Bcl-2 were detected in LYG-202-induced apoptosis. Additionally, activation of p53 resulted in the up-regulation of its downstream targets PUMA and p21(WAF1/Cip1), as well as the down-regulation of its negative regulator MDM2, suggesting that the p53 pathway may play a crucial role in LYG-202-induced cell cycle arrest and apoptosis. Furthermore, siRNA knockdown of p53 attenuated the G1 cell cycle arrest and apoptosis induced by LYG-202, as the effects of LYG-202 on up-regulation of p21(WAF1/Cip1) and down-regulation of Bcl-2 and pro-caspase-3 were partly inhibited in p53 siRNA transfected cells compared with control siRNA transfected cells. Collectively, these data indicate that LYG-202 exerts its anti-tumor potency by activating the p53-p21 pathway for G1/S cell cycle arrest and apoptosis in colorectal cancer cells.

Authors+Show Affiliations

Jiangsu Key Laboratory of Carcinogenesis and Intervention, China Pharmaceutical University, Tongjiaxiang, Nanjing, the People's Republic of China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

21491996

Citation

Liu, Wei, et al. "LYG-202 Inhibits the Proliferation of Human Colorectal Carcinoma HCT-116 Cells Through Induction of G1/S Cell Cycle Arrest and Apoptosis Via P53 and p21(WAF1/Cip1) Expression." Biochemistry and Cell Biology = Biochimie Et Biologie Cellulaire, vol. 89, no. 3, 2011, pp. 287-98.
Liu W, Dai Q, Lu N, et al. LYG-202 inhibits the proliferation of human colorectal carcinoma HCT-116 cells through induction of G1/S cell cycle arrest and apoptosis via p53 and p21(WAF1/Cip1) expression. Biochem Cell Biol. 2011;89(3):287-98.
Liu, W., Dai, Q., Lu, N., Wei, L., Ha, J., Rong, J., Mu, R., You, Q., Li, Z., & Guo, Q. (2011). LYG-202 inhibits the proliferation of human colorectal carcinoma HCT-116 cells through induction of G1/S cell cycle arrest and apoptosis via p53 and p21(WAF1/Cip1) expression. Biochemistry and Cell Biology = Biochimie Et Biologie Cellulaire, 89(3), 287-98. https://doi.org/10.1139/O10-162
Liu W, et al. LYG-202 Inhibits the Proliferation of Human Colorectal Carcinoma HCT-116 Cells Through Induction of G1/S Cell Cycle Arrest and Apoptosis Via P53 and p21(WAF1/Cip1) Expression. Biochem Cell Biol. 2011;89(3):287-98. PubMed PMID: 21491996.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - LYG-202 inhibits the proliferation of human colorectal carcinoma HCT-116 cells through induction of G1/S cell cycle arrest and apoptosis via p53 and p21(WAF1/Cip1) expression. AU - Liu,Wei, AU - Dai,Qinsheng, AU - Lu,Na, AU - Wei,Libin, AU - Ha,Jun, AU - Rong,Jingjing, AU - Mu,Rong, AU - You,Qidong, AU - Li,Zhiyu, AU - Guo,Qinglong, Y1 - 2011/04/14/ PY - 2011/4/16/entrez PY - 2011/4/16/pubmed PY - 2011/12/15/medline SP - 287 EP - 98 JF - Biochemistry and cell biology = Biochimie et biologie cellulaire JO - Biochem Cell Biol VL - 89 IS - 3 N2 - We recently established that LYG-202, a new flavonoid with a piperazine substitution, exerts an anti-tumor effect in vivo and in vitro. In the present study, we demonstrate that LYG-202 induces G1/S phase arrest and apoptosis in human colorectal carcinoma HCT-116 cells. Data showed that the blockade of the cell cycle was associated with increased p21(WAF1/Cip1) and Rb levels and reduced expression of cyclin D1, cyclin E, and CDK4. Moreover, PARP cleavage, activation of caspase-3, caspase-8, and caspase-9, and an increased ratio of Bax/Bcl-2 were detected in LYG-202-induced apoptosis. Additionally, activation of p53 resulted in the up-regulation of its downstream targets PUMA and p21(WAF1/Cip1), as well as the down-regulation of its negative regulator MDM2, suggesting that the p53 pathway may play a crucial role in LYG-202-induced cell cycle arrest and apoptosis. Furthermore, siRNA knockdown of p53 attenuated the G1 cell cycle arrest and apoptosis induced by LYG-202, as the effects of LYG-202 on up-regulation of p21(WAF1/Cip1) and down-regulation of Bcl-2 and pro-caspase-3 were partly inhibited in p53 siRNA transfected cells compared with control siRNA transfected cells. Collectively, these data indicate that LYG-202 exerts its anti-tumor potency by activating the p53-p21 pathway for G1/S cell cycle arrest and apoptosis in colorectal cancer cells. SN - 1208-6002 UR - https://www.unboundmedicine.com/medline/citation/21491996/LYG_202_inhibits_the_proliferation_of_human_colorectal_carcinoma_HCT_116_cells_through_induction_of_G1/S_cell_cycle_arrest_and_apoptosis_via_p53_and_p21_WAF1/Cip1__expression_ L2 - https://cdnsciencepub.com/doi/10.1139/o10-162?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub=pubmed DB - PRIME DP - Unbound Medicine ER -