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

Author(s)

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

Affiliation

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

• Document type: Journal article
• Source: JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY; v. 175, p. 89-98, OCT 2017.
• Web of Science Citations: 3

Abstract

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)

• FAPESP's process: 13/25155-7 - Obtaining and in vitro biological study of hypericin derivatives for use as photosensitizers in photodynamic therapy
• Grantee: Gislaine Patricia de Andrade
• Support Opportunities: Scholarships in Brazil - Doctorate
• FAPESP's process: 14/18527-8 - Phthalocyanines and Naphthalocyanines: synthesis and characterization of amphiphilic macrocyles for photodynamic therapy
• Grantee: Anderson Orzari Ribeiro
• Support Opportunities: Regular Research Grants