Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry and Computational Chemistry

Abstract

Preclinic study of Bgl2 ligand as component of mix antibiofilm toward Candida albicans on mucous intestinal biofilm preinduced Rattus novergicus

Author(s): Afaf Baktir, Masfufatun and Sofijan Hadi

Candida biofilms are difficult to be penetrated by drug molecules and resistant to almost all types of antifungal (multi drug resistance), included fluconazole. The successfull of Candida treatment is determined by eradication of extracellular matrix of Candida biofilms, especially which attach in the gastrointestinal tract of patients. In the previous studies it was successfully eradicated Candida biofilms in vitro using novel biomaterials that are in the process of patent, those are the combination of hydrolase enzyme and ligand Bgl2 used to hydrolyze the extracell matrix and to prevent the matrix regeneration respectively. The effects were proved by increasing of fluconazole activity as much as 61.14%. The purpose of this research were determining the effectiveness and ED50of ligand Bgl2 as the antibiofilm candidate toward Candida biofilm extracellular matrix in mice as the animal models. Research methods includedthe formation of Candida albicansbiofilms on the mucous membran of gastrointestinal tract of mice, followed byhealing it using mix antibiofilm: hydrolase enzymesand ligand Bgl2, to elevate the action of fluconazole. The concentration of Bgl2 ligand were variedand procent inhibition of biofilm formation was determinated for each dose.The reduction of the biofilm as responds to the treatments were analyzed to determine the ED50.The biofilm were analyzed by determinating of Candida viability (CFU) in faecal and intestinal tissue samples for several weeks of biofilm induction, and SEM analysis of the biofilm sample. The elevated doses of Bgl2 ligand 0, 5, 10, 15, 17,5 and 20 mg/kg body weight gave the percent inhibition of biofilm formation 0, 31, 54, 93, 100 and 69 % respectively, from which was calculated the ED50of Bgl2 ligand for C. albicans eradication was 8,57 mg /kg body weight. Hydrolase enzymes and ligand Bgl2 effectively enhanced the fluconazole activity on two weeks treatment. ED50 Bgl2 ligand value of 8,57 mg / kg body weight is smaller thanthose LD50 reported 17.5 mg / kg body weight. This means that biofilm eradication using combination of antibiofilm found in this research to eradicate C.albicans biofilm does not cause side effects. The conclusions were: (1) ED50 of Bgl2 ligand was 8,57 mg/ kg body weight on using in combiantion with hydrolase enzymes and fluconazol (mix antibiofilm) (2) Hydrolase enzymes and ligand Bgl2 effectively increased the fluconazole activity.


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