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Synthesis of Curcuminoids and Evaluation of Their Cytotoxic and Antioxidant Properties

Curcumin (1) and ten derivatives (2–11) were synthesized and evaluated as cytotoxic and antioxidant agents. The results of primary screening by Sulforhodamine B assay against five human cancer cell lines (U-251 MG, glioblastoma; PC-3, human prostatic; HCT-15, human colorectal; K562, human chronic my...

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Detalles Bibliográficos
Autores principales: Lozada-García, María Concepción, Enríquez, Raúl G., Ramírez-Apán, Teresa O., Nieto-Camacho, Antonio, Palacios-Espinosa, Juan Francisco, Custodio-Galván, Zeltzin, Soria-Arteche, Olivia, Pérez-Villanueva, Jaime
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6154528/
https://www.ncbi.nlm.nih.gov/pubmed/28420097
http://dx.doi.org/10.3390/molecules22040633
Descripción
Sumario:Curcumin (1) and ten derivatives (2–11) were synthesized and evaluated as cytotoxic and antioxidant agents. The results of primary screening by Sulforhodamine B assay against five human cancer cell lines (U-251 MG, glioblastoma; PC-3, human prostatic; HCT-15, human colorectal; K562, human chronic myelogenous leukemia; and SKLU-1, non-small cell lung cancer) allowed us to calculate the half maximal inhibitory concentration (IC(50)) values for the more active compounds against HCT-15 and K562 cell lines. Compounds 2 and 10 were the most active against both cell lines and were more active than curcumin itself. Thiobarbituric acid reactive substances (TBARS) assay showed that 7 has potent activity; even stronger than curcumin, α-tocopherol, and quercetin.