Govaniadine Evaluation of Cytotoxicity and Permeability in Cell Culture

Marques LMM, Behrens M, Kalinina S, Rottkord U, Adhikari A, (S) Shrestha RL, Humpf H, Lopes NP

Research article (journal)

Abstract

Govaniadine (1), a tetrahydroprotoberberine-type alkaloid, is one of the main active constituent isolated from Corydalis govaniana Wall., 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 compound 1 on 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 compound 1 was observed between 30 and 100μM (HepG2) and between 70 and 100μM (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 compound 1 quantification 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 6.3-200nM and 0.2-10μM. The apparent permeability coefficient for absorptive transport was 20.6 ± 3.9 × 10-6cm/s, indicating compound 1 crossed the cell monolayer by passive diffusion and it was not subjected to active efflux.

Details zur Publikation

Release year: 2020
Language in which the publication is written: English
Link to the full text: https://doi.org/10.1007/s43450-020-00066-wDO - 10.1007/s43450-020-00066-w