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Biodistribution of enzymatically modified flavonoid: hydrolyzed rutin.

Grant number: 17/26010-3
Support type:Scholarships abroad - Research
Effective date (Start): March 04, 2018
Effective date (End): July 29, 2018
Field of knowledge:Health Sciences - Medicine
Principal Investigator:Denise Gonçalves Priolli
Grantee:Denise Gonçalves Priolli
Host: Maria Filomena Rabaca Roque Botelho
Home Institution: Universidade São Francisco (USF). Campus Bragança Paulista. Bragança Paulista , SP, Brazil
Local de pesquisa : Universidade de Coimbra (UC), Portugal  

Abstract

The most widely used therapy in colorectal cancer - which has great importance due to its high frequency and incidence - is the surgical resection added to adjuvant therapy. However, antineoplastic treatments have the potential to induce mutagenic effects in normal cells. Ideally, antineoplastics would lead to complete tumor remission and at the same time, provide protection to normal cells. Thus, the option of flavonoids as desirable antitumor agents arises, since, although their cellular and molecular mechanisms are partly unknown, they have demonstrated antitumor activity, as well as protective effects in normal cells. Possible protective activities are: antioxidant capacity, direct radical scavengers, metal ions chelating agents, inactivating carcinogens, while its antitumor activity seems to be related to gene expression modulation and DNA repair, hormonal modulation, inhibition of enzymes and apoptosis. It is known that the biological effects depend on the chemical structure of flavonoids, from which bioactive molecules are generated. The modification of the structure also influences the absorption efficiency and possibly its biodistribution. Quercetin-3-rutinoside can be transformed into quercetin-3-glycoside by the breakdown of the rhamnose molecule through alpha-L-rhamnosidase, resulting in a significant increase in its bioavailability, keeping its antitumoral action. Moreover, the radioligands development with radiotracer characteristics, justify their use in theranostic. By making the complexation of the hydrolyzed rutin with a radioisotope, such as 99mTc, we could add the antitumor effect to the neoplasia diagnostic capacity, a phenomenon that has been attracting attention in the field of oncology, the theranostic. The present study intends to investigate the hydrolyzed rutin biodistribution by complexation with 99mTc, demonstrating its capacity to reach neoplasia, not only to diagnosis but also in neoadjuvant effect, especially for human colorectal and glioblastoma cancer, in which the antitumor activity of this compound has already been demonstrated.