國家衛生研究院 NHRI:Item 3990099045/6051

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Title:	Antiproliferative effects of N-heterocyclic indolyl glyoxylamide derivatives on human lung cancer cells
Authors:	Huang, TH;Chiu, SJ;Chiang, PH;Chiou, SH;Li, WT;Chen, CT;Chang, CA;Chen, JC;Lee, YJ
Contributors:	Institute of Biotechnology and Pharmaceutical Research
Abstract:	Background: N-Heterocyclic indolyl glyoxylamide compounds are derived from the antimicrotubule agent D-24851, which exhibits anticancer activity after oral administration. The actions of these compounds on lung cancer cells are still unknown. Here, we investigated the effects of two N-heterocyclic indolyl glyoxylamides, BPR0C259 and BPR0C123, on non-small human lung cancer cells. Materials and Methods: 3-[4,5-dimethylthiazol-2-yl]2,5-diphenyltetrazolium bromide (MTT) assay was used to determine the half maximal inhibitory concentration (IC(50)), cell viability and radiation response of A549 cells and H1299 cells. Apoptosis was determined by sub-G(1) ratio, colony formation assay and caspase-3 activation. Cell cycle distribution was detected using flow cytometry. Results: Both compounds were able to inhibit the viability of human lung cancer cells, although the IC(50) of BPR0C123 was lower than that of BPR0C259. Both compounds induced significant sub-G1 and caspase-3 activation as low as 0.1 mu M in both cell lines. These effects were independent of p53 activation because the level of serine-15 phosphorylated p53 was not affected after drug treatment. Furthermore, both compounds induced similar levels of G(2)/M phase arrest and radiosensitivity in these lung cancer cells. Conclusion: Current data suggest that N-heterocyclic indolyl glyoxylamides can suppress the proliferation of and potentially increase radiosensitivity of human lung cancer cells.
Date:	2011-10
Relation:	Anticancer Research. 2011 Oct;31(10):3407-3415.
Link to:	http://ar.iiarjournals.org/content/31/10/3407.full
JIF/Ranking 2023:	http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0250-7005&DestApp=IC2JCR
Cited Times(WOS):	https://www.webofscience.com/wos/woscc/full-record/WOS:000295667700039
Cited Times(Scopus):	http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=80054722088
Appears in Collections:	[Chiung-Tong Chen] Periodical Articles

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