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Orbitides from Croton antisyphiliticus and c. sphaerogynus (Euphorbiaceae), chemical-biological characterization and synthesis: rational prospection of low molecular weight peptides with antitumor potential

Grant number: 17/12326-9
Support type:Scholarships in Brazil - Master
Effective date (Start): October 01, 2017
Effective date (End): February 28, 2019
Field of knowledge:Physical Sciences and Mathematics - Chemistry
Principal Investigator:Vanderlan da Silva Bolzani
Grantee:Jhennifer Priscila Nastri
Home Institution: Instituto de Química (IQ). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil
Associated research grant:13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery, AP.CEPID

Abstract

Orbitides are peptides composed of a few units of amino acids (5-11), which are synthesized in nature by the ribosomal route and characterized by N-±-C type amide bonds, common in the cyclic peptides or miniproteins. It is a class of natural products that has been attracting great interest from strategic sectors such as pharmaceuticals, cosmetics and agricultural pest control. Despite this finding, research on orbitides isolated from plant species of brazilian biodiversity is still very modest. The orbitides from vegetal origin occur only in some taxa, being important molecular models for research in the chemistry of natural products. In this sense, scientific research with this class of substances has been emerging in the world's leading research centers because they are important models in the study of new drugs. In Brazil, there are still very few studies on this class of peptides and NuBBE has been consolidating in the study on peptides of plant species from our biodiversity. There are reports that species of the genus Croton biosynthesize these compounds, in addition, some important pharmacological properties were recorded in the literature, which justifies the present study. There are many chemical and biological studies with species of the genus, most report the occurrence of terpenes of the class of phorbols, highly cytotoxic. Therefore, it is interesting to investigate the accumulated orbitides are responsible for the reported activities, including the antitumor. The line of research in peptides in the NuBBE has been growing in recent years and aims to identify novel peptides, of great interest as prototypes of antitumor drugs. Cancer is a serious pathology on the world stage, so the search for therapies with greater effectiveness and less toxicity has become the target and challenge for many researchers. In this project, a priori, the isolation, identification and characterization of orbitides from the species Croton antisyphiliticus and Croton sphaerogynus are proposed. Subsequently, the naturally occurring compounds and their synthesized analogs will be tested for inhibition of tumor migration in vitro and cell proliferation.

Academic Publications
(References retrieved automatically from State of São Paulo Research Institutions)
NASTRI, Jhennifer Priscila. Orbitídeos de Euphorbiaceae, caracterização química e síntese : prospecção racional de peptídeos cíclicos com potencial antitumoral. 2019. 87 f. Master's Dissertation - Universidade Estadual Paulista "Júlio de Mesquita Filho" Instituto de Química..

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