Govaniadine Evaluation of Cytotoxicity and Permeability in Cell Culture

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]}

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

• 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 Opportunities: 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 Opportunities: Scholarships in Brazil - Doctorate