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RPF151, a novel capsaicin-like analogue: in vitro studies and in vivo preclinical antitumor evaluation in a breast cancer model.

Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine (2015-04-22)
Adilson Kleber Ferreira, Maurício Temotheo Tavares, Kerly Fernanda Mesquita Pasqualoto, Ricardo Alexandre de Azevedo, Sarah Fernandes Teixeira, Wilson Alves Ferreira-Junior, Ariane Matiello Bertin, Paulo Luiz de-Sá-Junior, José Alexandre Marzagão Barbuto, Carlos Rogério Figueiredo, Yara Cury, Mariana Celestina Frojuello Costa Bernstorff Damião, Roberto Parise-Filho

Capsaicin, the primary pungent component of the chili pepper, has antitumor activity. Herein, we describe the activity of RPF151, an alkyl sulfonamide analogue of capsaicin, against MDA-MB-231 breast cancer cells. RPF151 was synthetized, and molecular modeling was used to compare capsaicin and RPF151. Cytotoxicity of RPF151 on MDA-MB-231 was also evaluated by the 3-[4,5-dimethylthiazol-2-yl]-2,5diphenyltetrazolium bromide (MTT) assay. Cell cycle analysis, by flow cytometry, and Western blot analysis of cycle-related proteins were used to evaluate the antiproliferative mechanisms. Apoptosis was evaluated by phosphatidyl-serine externalization, cleavage of Ac-YVAD-AMC, and Bcl-2 expression. The production of reactive oxygen species was evaluated by flow cytometry. RPF151 in vivo antitumor effects were investigated in murine MDA-MB-231 model. This study shows that RPF151 downregulated p21 and cyclins A, D1, and D3, leading to S-phase arrest and apoptosis. Although RPF151 has induced the activation of TRPV-1 and TRAIL-R1/DR4 and TRAIL-2/DR5 on the surface of MDA-MB-231 cells, its in vivo antitumor activity was TRPV-1-independent, thus suggesting that RPF151 should not have the same pungency-based limitation of capsaicin. In silico analysis corroborated the biological findings, showing that RPF151 has physicochemical improvements over capsaicin. Overall, the activity of RPF151 against MDA-MB-231 and its lower pungency suggest that it may have a relevant role in cancer therapy.

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Product Description

Formaldehyde solution, ACS reagent, 37 wt. % in H2O, contains 10-15% Methanol as stabilizer (to prevent polymerization)
Formaldehyde solution, for molecular biology, 36.5-38% in H2O
Phenylmethanesulfonyl fluoride, ≥98.5% (GC)
Hydrocortisone, BioReagent, suitable for cell culture
Formaldehyde solution, for molecular biology, BioReagent, ≥36.0% in H2O (T)
Hydrocortisone, ≥98% (HPLC)
Formaldehyde solution, contains 10-15% methanol as stabilizer, 37 wt. % in H2O
Hydrocortisone, γ-irradiated, powder, BioXtra, suitable for cell culture
Phenylmethanesulfonyl fluoride, ≥99.0% (T)
Formaldehyde solution, meets analytical specification of USP, ≥34.5 wt. %
Formaldehyde solution, stabilized with methanol, ~37 wt. % in H2O, certified reference material
Tetramethylrhodamine ethyl ester perchlorate, suitable for fluorescence, ≥90% (HPCE)
Hydrocortisone, meets USP testing specifications
Formaldehyde-12C solution, 20% in H2O, 99.9 atom % 12C