Comparative in vitro study of photodynamic activity of hypericin and hypericinates in MCF-7 cells

Autor(es)

de Andrade, Gislaine Patricia ^[1] ; Manieri, Tania Maria ^[1] ; Nunes, Emilene Arusievicz ^[1] ; Viana, Gustavo Monteiro ^[1] ; Cerchiaro, Giselle ^[1] ; Ribeiro, Anderson Orzari ^[1]

Afiliação do(s) autor(es)

^[1] Univ Fed ABC, CCNH, Av Estados 5001, Santo Andre, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY; v. 175, p. 89-98, OCT 2017.
• Citações Web of Science: 3

Resumo

In this work we present a comparative in vitro study of photodynamic activity between hypericin (HYP) and some hypericinates (hypericin ionic pair with lysine or N-methylglucamine) in human mammary adenocarcinoma cells (MCF-7). The toxicity and phototoxicity of hypericin and hypericinates were compared, as well as their cellular uptake and localization and mutagenic, genotoxic and clonogenic capacity. Our results demonstrate that different cationic moieties promote differences in the hypericinate solubility in a biological environment, and can influence the cellular localization and the phototoxicity of the photosensitizer. It was verified that hypericinates have better efficiency to generate singlet oxygen than HYP, and a lower aggregation in biological medium. In vitro assays have shown that HYP and the hypericinates are able to permeate the MCF-7 cell membrane and accumulated in organelles near the nucleus. The difference in location, however, was not determinant to the cell death mechanism, and a higher prevalence of apoptosis for all studied compounds occurred. The photodynamic studies indicated that hypericinates were more effective than HYP and were able to inhibit the formation of cellular colonies, suggesting a possible ability to prevent the recurrence of tumors. It also appears that all compounds have relative safety for mutagenicity and genotoxicity, which opens up a further safe route for application in in vivo studies. (AU)

• Processo FAPESP: 13/25155-7 - Obtenção e estudo biológico in vitro de derivados de hipericina para aplicação como fotossensibilizadores em Terapia Fotodinâmica
• Beneficiário: Gislaine Patricia de Andrade
• Modalidade de apoio: Bolsas no Brasil - Doutorado
• Processo FAPESP: 14/18527-8 - Ftalocianinas e Naftalocianinas: síntese de macrociclos anfifílicos para aplicação em Terapia Fotodinâmica
• Beneficiário: Anderson Orzari Ribeiro
• Modalidade de apoio: Auxílio à Pesquisa - Regular