Search

Benzothiazole-piperazine derivatives prepared previously, 1h and 1j are potential anticancer agents. Since the mutagenic and genotoxic properties of anticancer drugs compose an essential issue to be researched, this study is focused on the analysis of the mutagenicity and genotoxicity of these molecules. The mutagenicity of 1h and 1j were determined by Ames test performed on Salmonella TA98 and TA100 strains. Sample 1j was mutagenic on TA98 bacterial strain. However, compound 1h was not mutagenic in bacterial strains TA98 and TA100 with and without S9 activation. The genotoxicity of 1h was evaluated by the chromosomal aberration assay on human lymphocytes. Compound 1h was also not genotoxic in human lymphocytes in vitro. All results revealed that, 1h was not mutagenic in the two Salmonella strains tested and was not genotoxic in chromosomal aberration assay. Therefore, results demonstrate that the described molecule is promising as a new anticancer drug without mutagenicity. Also, after performing Ames test with other recommended bacterial strains and in vivo experiments can be used safely for the development of new structures exhibiting anticancer activities. © 2017, Marmara University. All rights reserved.

ALC67 is an N-acylated thiazolidine compound with promising anticancer activity that led to the recent discovery of a series of 3-propionyl thiazolidine-4-carboxylic acid ethyl esters as a family of novel antiproliferative agents. Since the mutagenic and genotoxic properties of marketed anticancer molecules constitute a main issue to be addressed, this study focused on the analysis of the mutagenicity, antimutagenecity, and genotoxicity of this molecule. The mutagenicity and antimutagenicity of ALC67 were evaluated by Ames test performed on Salmonella TA98 and TA100 strains. The genotoxicity of this molecule was investigated in the chromosomal aberration assay on human lymphocytes. All results revealed that the analyzed structure is not mutagenic in the two Salmonella strains tested and was not genotoxic in human lymphocytes in vitro. On the other hand, it showed a weak antimutagenic effect in these two bacterial strains. The above results indicate that after performing some more mutagenicity assays using the other recommended strains, this compound can be safely used for the development of new structures exhibiting anticancer activities. © 2016 SAGE Publications.

Made available in DSpace on 2013-09-27T14:54:07Z (GMT). No. of bitstreams: 1 WOS000267218200032.pdf: 296807 bytes, checksum: 337a49e7688dc326d92b0bb1270102c4 (MD5) Previous issue date: 2008-01-01 Made available in DSpace on 2013-09-30T18:15:25Z (GMT). No. of bitstreams: 1 WOS000267218200032.pdf: 296807 bytes, checksum: 337a49e7688dc326d92b0bb1270102c4 (MD5) Previous issue date: 2008-01-01 Submitted by Vitor Silverio Rodrigues (vitorsrodrigues@reitoria.unesp.br) on 2014-05-20T13:31:44Z No. of bitstreams: 1 WOS000267218200032.pdf: 296807 bytes, checksum: 337a49e7688dc326d92b0bb1270102c4 (MD5) Made available in DSpace on 2014-05-20T13:31:44Z (GMT). No. of bitstreams: 1 WOS000267218200032.pdf: 296807 bytes, checksum: 337a49e7688dc326d92b0bb1270102c4 (MD5) Previous issue date: 2008-01-01 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Fundação de Amparo à Pesquisa do Estado de Minas Gerais (FAPEMIG) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Baccharis dracunculifolia de Candole (DC) ( Asteraceae) is indigenous throughout southeastern Latin America and is used by local people in traditional medicine. This plant is known to be the source of resin for the highly valued Brazilian green propolis. As no information is available on the safety of high doses of B. dracunculifolia extract, we evaluated the mutagenic potential of high doses of this plant extract in vivo on peripheral blood cells of Swiss mice using the comet assay and the micronucleus test. The extract was administered by gavage at doses of 1000, 1500 and 2000 mg/kg body weight. Peripheral blood cell samples were collected 4 and 24 h after treatment for the comet assay (genotoxicity assay), and at 48 and 72 h for the micronucleus test (clastogenicity assay). The B. dracunculifolia extract was devoid of clastogenic/genotoxic activity at all doses. Univ Estadual Paulista, Fac Filosofia & Ciencias, Dept Fonoaudiol, Marilia, SP, Brazil Univ Jose Rosario Vellano, Genet Lab, Alfenas, MG, Brazil Univ Fed Amapa, Lab Pesquisa Farmacos, Macapa, AP, Brazil Univ Estadual Paulista, Fac Filosofia & Ciencias, Dept Fonoaudiol, Marilia, SP, Brazil FAPESP: 06/57514-2 FAPEMIG: 1879/02 CNPq: 306544/2006-7