Species-dependent binding of cucurbitacin E and cucurbitacin I to albumin: optical biosensor and circular dichroism study

• Grant number: 14/18095-0
• Support Opportunities: Scholarships abroad - Research Internship - Doctorate
• Start date: January 05, 2015
• End date: May 04, 2015
• Field of knowledge: Health Sciences - Pharmacy - Pharmacognosy
• Principal Investigator: Norberto Peporine Lopes
• Grantee: Giovana Maria Lanchoti Fiori
• Supervisor: Carlo Bertucci
• Host Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil
• Institution abroad: Università di Bologna, Italy
• Associated to the scholarship: 12/14408-9 - Disposition kinetics, plasma protein binding, metabolism in vitro and in vivo of curcubitacins in rats, BP.DR

Abstract

This research project is devoted to the study of the albumin binding of some cucurbitacins. These natural products are already under investigation in Ribeirão Preto for their pharmacokinetics. The albumin binding study will give further information on the distribution parameters of these important compounds. The binding affinity will be determined to both rat albumin and human serum albumin, in order to give evidence of differences in the binding process to the two albumins. This should give an idea if the distribution data in rat can be extrapolated to man. Further the binding processes to the two albumins will be characterized by determining the kinetics parameters and by getting information on the binding mechanism(s). These studies will be carried out by using several spectroscopic and spectrometric techniques, but we will mainly use an optical biosensor and circular dichroism. The surface plasmon resonance (SPR) based optical biosensor will allow the determination of the binding parameters, both affinity and kinetics constants. Optical biosensors is a tool for early determination of absorption and distribution parameters of lead candidates and drugs, while circular dichroism study of protein bound cucurbitacins should allow having information on the binding mechanism and on the possible modulation of the protein secondary structure upon binding of the analysed natural compounds. (AU)

Scientific publications

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

FABINI, EDOARDO; LANCHOTI FIORI, GIOVANA MARIA; TEDESCO, DANIELE; LOPES, NORBERTO PEPORINE; BERTUCCI, CARLO. Surface plasmon resonance and circular dichroism characterization of cucurbitacins binding to serum albumins for early pharmacokinetic profiling. Journal of Pharmaceutical and Biomedical Analysis, v. 122, p. 166-172, APR 15 2016. (14/18095-0)