Evaluation of the antitumour activity of Rinvanil and Phenylacetylrinvanil on the cervical cancer tumour cell lines HeLa, CaSKi and ViBo
| Autor: | Jesús J. Alvarado-Sansininea, Patricia Demare, José M.V. Hernández-Vázquez, Ignacio Regla, Benny Weiss-Steider, Iván Monsalvo-Montiel, Hugo López-Muñoz, María L. Escobar, Luis Sánchez-Sánchez |
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| Rok vydání: | 2014 |
| Předmět: |
TRPV1
Antineoplastic Agents Apoptosis Pharmacology HeLa chemistry.chemical_compound Cell Line Tumor medicine Cytotoxic T cell Humans Fragmentation (cell biology) Cell Proliferation Phenylacetates biology Chemistry Caspase 3 Cancer biology.organism_classification medicine.disease Cell culture Capsaicin lipids (amino acids peptides and proteins) Female Drug Screening Assays Antitumor |
| Zdroj: | European journal of pharmacology. 758 |
| ISSN: | 1879-0712 |
| Popis: | Capsaicin is a potent inducer of apoptosis in tumourreceptor potential vanilloid 1 (TRPV1). The present study determined the IC50 and cytotoxic and apoptotic activities of the Capsaicin analogues Rinvanil and Phenylacetylrinvanil (PhAR) on three cervical cancer cell lines: HeLa, CaSKi and ViBo. These analogues possess an increased affinity for TRPV1 receptors. The IC50 obtained proved to be cytotoxic for all three cell lines; however, in the cells treated with Capsaicin both active caspase-3 and nuclear fragmentation were present. Capsaicin and its analogues also inhibited the normal proliferation of lymphocytes, suggesting that they are non-selective antitumour compounds. Finally, we discuss the possible loss of the relation between apoptosis and affinity to TRPV1, and the need for other strategies to synthesise Capsaicin analogues that can be useful in cancer treatments. |
| Databáze: | OpenAIRE |
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