Optimization of anti-allergic activity bioassay using cyclodextrins as carriers of flavonoids

• Grant number: 12/03151-7
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: May 01, 2012
• End date: December 09, 2015
• Field of knowledge: Health Sciences - Pharmacy
• Principal Investigator: Rose Mary Zumstein Georgetto Naal
• Grantee: Marcia Andreia Bertoz
• Host Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil

Abstract

Allergic diseases such as asthma, rhinitis, food allergy, and others have been accentuated in recent years and subjecting allergic individuals to low quality of life and leading them to death. For most people, the strategies used to treat the symptoms, or prevent the disease, have proved inefficient and impractical which emphasizes the need for the discovery of new drugs and new alternatives that may be involved in immune responses more efficiently. In this context, natural products play a fundamental role and have been the subject of considerable investigation in the search for new therapeutic agents. Some classes of substances are potent inhibitors of mast cell degranulation, among which are the flavonoids naturally present in many foods and beverages. Many of these substances are poorly soluble in water and easily oxidized or photodegraded, which reduces the absorption in the body and impedes the performance of biological assays. Moreover, due to the low solubility, the application of these compounds intravenously is impractical which enables the studies related to drug carrier systems. The incorporation of flavonoids such as quercetin, rutin, and mangiferin on cyclodextrins (CD) can alleviate these problems and increase the bioavailability of the drugs and the efficiency of biological assays aimed at finding new alternatives to medical therapy. In this work, we intend to invest in the behavior of mangiferin and compare the anti-allergic activity of the bioactive free and associated with CD. To achieve these objectives, the inclusion complexes of mangiferin to CD will be prepared, in the absence and presence of cholesterol, and such complexes will be used in the assay of anti-allergic activity, under different conditions such as varying the stoichiometric ratio drug: CD, time of exposure of cells to the inclusion complexes, cholesterol concentration, and cytotoxicity.(AU)