Busca avançada
Ano de início
Entree
(Referência obtida automaticamente do Web of Science, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

Govaniadine Evaluation of Cytotoxicity and Permeability in Cell Culture

Texto completo
Autor(es):
Marques, Lucas M. M. [1, 2] ; Behrens, Matthias [1] ; Kalinina, Svetlana [1] ; Rottkord, Ulrike [1] ; Adhikari, Achyut [3] ; Shrestha, Ram L. S. [4] ; Humpf, Hans-Ulrich [1] ; Lopes, Norberto P. [2, 5]
Número total de Autores: 8
Afiliação do(s) autor(es):
[1] Westfalische Wilhelms Univ Munster, Inst Lebensmittelchem, Munster - Germany
[2] Univ Sao Paulo, Fac Pharmaceut Sci Ribeirao Preto, Dept BioMol Sci, Ribeirao Preto - Brazil
[3] Tribhuvan Univ, Cent Dept Chem, Kathmandu - Nepal
[4] Tribhuvan Univ, Amrit Sci Campus, Kathmandu - Nepal
[5] Shrestha, Ram L. S., Tribhuvan Univ, Amrit Sci Campus, Kathmandu, Nepal.Marques, Lucas M. M., Univ Sao Paulo, Fac Pharmaceut Sci Ribeirao Preto, Dept BioMol Sci, Ribeirao Preto - Brazil
Número total de Afiliações: 5
Tipo de documento: Artigo Científico
Fonte: REVISTA BRASILEIRA DE FARMACOGNOSIA-BRAZILIAN JOURNAL OF PHARMACOGNOSY; v. 30, n. 3 MAY 2020.
Citações Web of Science: 0
Resumo

Govaniadine (1), a tetrahydroprotoberberine-type alkaloid, is one of the main active constituent isolated fromCorydalis govanianaWall., Papaveraceae, with several biological activities: antinociceptive, anti-urease, and leishmanicidal. Some articles reporting tetrahydroprotoberberine and structurally related alkaloids cytotoxicity prompted us to evaluate the influence of compound1on cellular viability in two different cell lines: human hepatoma carcinoma (HepG2) and human embryonic kidney (HEK-293T) and its permeation across the human colon carcinoma cell line (Caco-2). Cellular viability reduction of compound1was observed between 30 and 100 mu M (HepG2) and between 70 and 100 mu M (HEK-293T). However, the effects were weaker than those in the positive controls (T-2 toxin and camptothecin). Prior to proceed the transport studies, a method for compound1quantification in Hank's Balanced Salt Solution medium was developed and validated by LC-MS/MS. The two calibration curves were linear over the concentration range of 6.3-200 nM and 0.2-10 mu M. The apparent permeability coefficient for absorptive transport was 20.6 +/- 3.9 x 10(-6) cm/s, indicating compound1crossed the cell monolayer by passive diffusion and it was not subjected to active efflux. (AU)

Processo FAPESP: 15/02592-8 - Avaliação da citotoxicidade do alcalóide govaniadina em linhagem de células humanas
Beneficiário:Lucas Maciel Mauriz Marques
Linha de fomento: Bolsas no Exterior - Estágio de Pesquisa - Doutorado
Processo FAPESP: 13/16496-5 - Avaliação do metabolismo in vitro, in vivo e do perfil farmacocinético do alcalóide govaniadina
Beneficiário:Lucas Maciel Mauriz Marques
Linha de fomento: Bolsas no Brasil - Doutorado