Disposition kinetics, plasma protein binding, metabolism in vitro and in vivo of curcubitacins in rats

• Grant number: 12/14408-9
• Support type: Scholarships in Brazil - Doctorate
• Effective date (Start): September 01, 2012
• Effective date (End): August 31, 2016
• Field of knowledge: Health Sciences - Pharmacy - Pharmacognosy
• Principal researcher: Norberto Peporine Lopes
• Grantee: Giovana Maria Lanchoti Fiori
• Home Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil
• Associated research grant: 09/51812-0 - Development of a platform for the study of in vitro and in vivo metabolism of natural products, a need for pre-clinical testing system, AP.BTA.TEM
• Associated scholarship(s): 14/18095-0 - Species-dependent binding of cucurbitacin E and cucurbitacin I to albumin: optical biosensor and circular dichroism study, BE.EP.DR

Abstract

Cayaponia tayuya (Vell.) Cogn of Cucurbitaceae family, native of throughout Brazil, has vast pharmacologycal potential scientifically proven as anti-tumor, anti-inflammatory and anti cancer due to the presence of cucurbitacines in roots of this plant.The species C. Tayuya have not established safety and efficacy and prolonged use or the use of high doses must be avoided until pharmacokinetic and toxicological studies are carried out. Pharmacokinetic preclinical evaluation aims to describe the parameters of absorption, distribution, metabolism and excretion of drugs in order to guide the design of clinical studies. The investigation of the biotransformation products in studies performed in vitro and in vivo aimed to predict the behavior of the drug candidate in humans, seeking to ensure greater security to the volunteers of studies clinical Phase I.Thus, the cucurbitacines drugs candidate should be evaluated as to the pre-clinical pharmacokinetic aspects, pharmacodynamic and toxicological tests, which form the basis of the expected effects in humans. The objectives of this project are to contribute in the development of drug candidates cucurbitacines through the characterization of preclinical pharmacokinetics, including research in models of metabolism in vitro and in vivo.

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)

LANCHOTI FIORI, GIOVANA MARIA; D'AGATE, SALVATORE; ROCHA, ADRIANA; SOARES PEREIRA, ANA MARIA; DELLA PASQUA, O.; LOPES, NORBERTO PEPORINE. Development and validation of a quantification method for cucurbitacins E and I in rat plasma: Application to population pharmacokinetic studies. Journal of Pharmaceutical and Biomedical Analysis, v. 144, n. SI, p. 99-105, SEP 10 2017. Web of Science Citations: 3.

Academic Publications

(References retrieved automatically from State of São Paulo Research Institutions)

FIORI, Giovana Maria Lanchoti. Population pharmacokinetics and plasma protein binding of cucurbitacin E and its metabolite cucurbitacin I in rats. 2016. Doctoral Thesis - Universidade de São Paulo (USP). Faculdade de Ciências Farmacêuticas de Ribeirão Preto Ribeirão Preto.