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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Govaniadine Evaluation of Cytotoxicity and Permeability in Cell Culture

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Author(s):
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]
Total Authors: 8
Affiliation:
[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
Total Affiliations: 5
Document type: Journal article
Source: REVISTA BRASILEIRA DE FARMACOGNOSIA-BRAZILIAN JOURNAL OF PHARMACOGNOSY; v. 30, n. 3 MAY 2020.
Web of Science Citations: 0
Abstract

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)

FAPESP's process: 15/02592-8 - Evaluation of the cytotoxicity of the alkaloid govaniadine in human cell lines
Grantee:Lucas Maciel Mauriz Marques
Support type: Scholarships abroad - Research Internship - Doctorate
FAPESP's process: 13/16496-5 - In vitro, in vivo metabolism and pharmacokinetic profile evaluation of the alkaloid govaniadine
Grantee:Lucas Maciel Mauriz Marques
Support type: Scholarships in Brazil - Doctorate