DSpace Coleção:http://repositorio.ufc.br/handle/riufc/3922026-04-16T01:18:03Z2026-04-16T01:18:03ZO uso de linhagens leucêmicas e a sua importância na oncologia experimentalSales, Lívia de OliveiraNogueira, Beatriz Maria DiasSilva, Emerson Lucena daMoraes, Maria Elisabete Amaral deMontenegro, Raquel CarvalhoMoreira-Nunes, Caroline de Fátima Aquinohttp://repositorio.ufc.br/handle/riufc/498902020-02-06T13:54:43Z2019-01-01T00:00:00ZTítulo: O uso de linhagens leucêmicas e a sua importância na oncologia experimental
Autor(es): Sales, Lívia de Oliveira; Nogueira, Beatriz Maria Dias; Silva, Emerson Lucena da; Moraes, Maria Elisabete Amaral de; Montenegro, Raquel Carvalho; Moreira-Nunes, Caroline de Fátima Aquino
Abstract: Experimental oncology is based on a model of study through cell culture, a
technique frequently used for the study of cancer biology and for tests of new anticancer
therapies. This model provides an appropriate system for researching the effects of
drugs and toxic compounds on cells, mutagenesis and carcinogenesis, in drug screening
and development. In addition the cell lines allows consistent and reproducible results,
becoming one of the main tools used in experimental oncology, with the advantage of
being derived from patients and easily manipulated in the laboratory. The use of cell
lines is fundamental in the research related to the study of new antineoplastic drugs for
the treatment of patients with chronic myeloid leukemia (CML) who are still refractory
to the currently available therapies. Thereby, the understanding of the mechanisms
of action and resistance and sensitivity patterns of these chemotherapies through the
use of these lineages can make cancer therapy more efficient and specific. Thus, we
highlight in this chapter the applications of cell lines as a study model for the various
biological aspects of cancer in Experimental Oncology.
Tipo: Capítulo de Livro2019-01-01T00:00:00ZAnálise in silico da farmacocinética e farmacodinâmica do composto benzotiazólico com potencial antitumoral contra linhagem de adenocarcinoma gástricoMesquita, Felipe PantojaLima, Luina BenevidesDaniel, Julio PaulinoPortilho, Adrhyann Jullyanne de SousaOliveira, Lais Lacerda Brasil deSilva, Emerson Lucena daChazin, liza de Lucas ChazinVasconcelos, Thatyana Rocha AlvesMoraes, Maria Elisabete Amaral deMontenegro, Raquel Carvalhohttp://repositorio.ufc.br/handle/riufc/498882020-02-06T13:54:07Z2019-01-01T00:00:00ZTítulo: Análise in silico da farmacocinética e farmacodinâmica do composto benzotiazólico com potencial antitumoral contra linhagem de adenocarcinoma gástrico
Autor(es): Mesquita, Felipe Pantoja; Lima, Luina Benevides; Daniel, Julio Paulino; Portilho, Adrhyann Jullyanne de Sousa; Oliveira, Lais Lacerda Brasil de; Silva, Emerson Lucena da; Chazin, liza de Lucas Chazin; Vasconcelos, Thatyana Rocha Alves; Moraes, Maria Elisabete Amaral de; Montenegro, Raquel Carvalho
Abstract: Gastric adenocarcinoma has high incidence and mortality rates
worldwide. The aim of this study was to evaluate the antitumor activity of benzothiazole
AFN01 against ACP03 gastric adenocarcinoma cell line. Furthermore, computational
prediction of the pharmacokinetics and pharmacodynamics of this molecule and the
molecular docking with the relevant pharmacological target found were performed. The
MTT assay was performed to evaluate the cytotoxic potential of the compound and
fluorescence microscopy was used to measure cell death induction with Fluorescein
Diacetate, Hoechst 33342 and Propidium Iodide fluorophores. The result of the
concentration-response curve obtained by MTT assay revealed a relevant cytotoxic
effect against the lineage with IC50 values around 17.24 μM at 24 h, 8.23 μM at 48
h and 1.39 μM at 72 h of exposure. AFN01 was able to induce apoptosis at 1 and 2
μM. Computational analyses identified relevant pharmacokinetic properties such as
positive intestinal absorption, inhibition of CYP1A2, CYP2C9 and CYP3A4, as well
as weak inhibition of hERG and class III acute oral toxicity. The pharmacodynamic
prediction identified molecular targets related to antitumor activity. The enzyme TDP1
was selected for molecular docking, indicating that benzothiazole has a binding energy
of -7.5 kcal/mol and important interactions with catalytic site residues of the enzyme.
In conclusion, the AFN01 benzothiazole compound is an excellent candidate for the
treatment of gastric adenocarcinoma, with good predicted pharmacokinetic parameters
and a potentially new molecular target.
Tipo: Capítulo de Livro2019-01-01T00:00:00Z