Peptide bioconjugates with anti-Leishmania activity

• Grant number: 22/07966-7
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: October 01, 2022
• End date: September 30, 2024
• Field of knowledge: Biological Sciences - Biochemistry - Chemistry of Macromolecules
• Principal Investigator: Eduardo Maffud Cilli
• Grantee: João Victor Marcelino de Souza
• Host Institution: Instituto de Química (IQ). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil

Abstract

Leishmaniasis is a neglected disease caused by the protozoan of the genus Leishmania, presenting in visceral and cutaneous forms. Leishmaniasis is characterized by symptoms such as high fever and weakness, in the case of skin infection, there is the appearance of lesions under the skin. As for the visceral, there may be swelling of the abdominal region, due to a condition called visceromegaly. The drugs used for the treatment of leishmaniasis have been suffering a reduction in effectiveness due to the resistance action mechanisms. In addition, the current compounds have low selectivity towards the pathogen and several side effects, such as chills, fever, nausea, and headache, among others. In this way, the use and development of new compounds is a way to overcome the resistance and cytotoxicity problems of current drugs on the market. Therefore, in the present study, the feasibility of using peptides conjugated to guanidinium molecules will be analyzed, in which previous tests carried out by our study group showed good leishmanicidal activity. The proposed peptides have proven ability and affinity for the cell membrane, allowing the molecule coupled to it to be easily transported into the cell, in order to improve activity against the protozoan and increase selectivity against the disease-causing agent.(AU)