Preliminary evaluation of the toxicity of some synthetic furan derivatives in two cell lines and Artemia salina.
This study describes the preliminary toxicity evaluation of five new furan derivatives, 2-[2-acetylamino-2-[(benzothiazolyl-substituted)aminocarbonyl]vinyl]-5-nitro furane (compounds A, B, D and E) and 2-[2-phenylamino-2-[benzothiazolylaminocarbonyl]vinyl]furane (compound C). Cytotoxicity was determined using the MTT (tetrazolium salt) method over BHK21 (Syrian baby hamster kidney) and Hep-2 (human larynx carcinoma) cells, which had previously been used to evaluate the cytotoxicity of the 5-nitrofuran derivatives. The lethal concentration 50 (LC(50)) was determined using brine shrimp (Artemia salina) bioassay. Nitrofurantoin was used as reference compound. The results demonstrate that BHK21 cells are more sensitive than Hep-2 cells. This structurally related serial of compounds shows a differential toxicity, which is an indication that the toxicity naturally arising from the nitro group can be modulated by the substituents over the furan ring. Additionally, compound C, the only derivative with no nitro group, was least toxic to Hep-2, but exhibits toxicity to BHK21 cells and brine shrimp. The LC(50 )brine shrimp test (BST) bioassay results were as follows: A, 654.2 microg ml(-1); B, 50.0 microg ml(-1); C, 533.4 microg ml(-1); D, 172.1 microg ml(-1); E, 76.4 microg ml(-1), and NF, >1000 microg ml(-1).
Amaro
María I
MI
Unidad de Química Medicinal, Facultad de Farmacia, Universidad Central de Venezuela. Apartado 40-109, Caracas 1040 A, Venezuela. amaroisabel2003@yahoo.com
Monasterios
Melina
M
Avendaño
Milagros
M
Charris
Jaime
J
D000818:Animals; D001156:Artemia / Q000187:drug effects*; D001681:Biological Assay; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006224:Cricetinae; D004305:Dose-Response Relationship, Drug; D005663:Furans / Q000737:chemistry / Q000145:classification / Q000633:toxicity*; D006801:Humans; D008647:Mesocricetus; D021281:Quantitative Structure-Activity Relationship; D013778:Tetrazolium Salts / Q000378:metabolism; D013844:Thiazoles / Q000378:metabolism; D018675:Toxicity Tests
D005663:Furans; D013778:Tetrazolium Salts; D013844:Thiazoles; C022616:thiazolyl blue