Prediction of in vivo Bioavailibility by in vitro Characterization of Ethylenediamine Dipropanoic Acid Derivatives with Cytotoxic Activity
Апстракт
O,O'-diethyl-(S, S)-ethylenediamine-N, N'-di-2-(3-cyclohexyl) propanoate (DE-EDCP) is novel substance with cytotoxic activity in human leukemic cells. The aim of this study has been to predict in vivo bioavailability of the DE-EDCP and its potential metabolite (S, S)-ethylenediamine-N, N'-di-2-(3-cyclohexyl) propanoic acid (EDCP) by in vitro characterization which includes determination of lipophilicity and passive membrane permeability. There has also been evaluated inter-laboratory reproducibility of the bio-analytical method which was previously developed and validated for non-clinical study of the DE-EDCP and EDCP. Distribution coefficient n-octanol/water was 1.68 and 0.03, and apparent permeability coefficient was 4 x 10(-4) cm/s and 20 x 10(-4) cm/s, for the DE-EDCP and EDCP, respectively. Observed results have shown that the DE-EDCP is more lipophilic with better membrane retention, but the EDCP has better pass through the membrane. Also, there has been demonstrated a reproducib...ility and robustness of the proposed bio-analytical method.
Кључне речи:
Transfer of the UHPLC-MS/MS / cross validation / (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl) propanoic acid esters / membrane permeability / lipophilicityИзвор:
Acta Chimica Slovenica, 2018, 65, 1, 59-64Издавач:
- Slovensko Kemijsko Drustvo, Ljubljana
Финансирање / пројекти:
DOI: 10.17344/acsi.2017.3477
ISSN: 1318-0207
PubMed: 29562114
WoS: 000428179900006
Scopus: 2-s2.0-85044361213
Институција/група
PharmacyTY - JOUR AU - Tubić, Biljana AU - Vladimirov, Sandra AU - Marković, Bojan AU - Sabo, Tibor PY - 2018 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3156 AB - O,O'-diethyl-(S, S)-ethylenediamine-N, N'-di-2-(3-cyclohexyl) propanoate (DE-EDCP) is novel substance with cytotoxic activity in human leukemic cells. The aim of this study has been to predict in vivo bioavailability of the DE-EDCP and its potential metabolite (S, S)-ethylenediamine-N, N'-di-2-(3-cyclohexyl) propanoic acid (EDCP) by in vitro characterization which includes determination of lipophilicity and passive membrane permeability. There has also been evaluated inter-laboratory reproducibility of the bio-analytical method which was previously developed and validated for non-clinical study of the DE-EDCP and EDCP. Distribution coefficient n-octanol/water was 1.68 and 0.03, and apparent permeability coefficient was 4 x 10(-4) cm/s and 20 x 10(-4) cm/s, for the DE-EDCP and EDCP, respectively. Observed results have shown that the DE-EDCP is more lipophilic with better membrane retention, but the EDCP has better pass through the membrane. Also, there has been demonstrated a reproducibility and robustness of the proposed bio-analytical method. PB - Slovensko Kemijsko Drustvo, Ljubljana T2 - Acta Chimica Slovenica T1 - Prediction of in vivo Bioavailibility by in vitro Characterization of Ethylenediamine Dipropanoic Acid Derivatives with Cytotoxic Activity VL - 65 IS - 1 SP - 59 EP - 64 DO - 10.17344/acsi.2017.3477 ER -
@article{ author = "Tubić, Biljana and Vladimirov, Sandra and Marković, Bojan and Sabo, Tibor", year = "2018", abstract = "O,O'-diethyl-(S, S)-ethylenediamine-N, N'-di-2-(3-cyclohexyl) propanoate (DE-EDCP) is novel substance with cytotoxic activity in human leukemic cells. The aim of this study has been to predict in vivo bioavailability of the DE-EDCP and its potential metabolite (S, S)-ethylenediamine-N, N'-di-2-(3-cyclohexyl) propanoic acid (EDCP) by in vitro characterization which includes determination of lipophilicity and passive membrane permeability. There has also been evaluated inter-laboratory reproducibility of the bio-analytical method which was previously developed and validated for non-clinical study of the DE-EDCP and EDCP. Distribution coefficient n-octanol/water was 1.68 and 0.03, and apparent permeability coefficient was 4 x 10(-4) cm/s and 20 x 10(-4) cm/s, for the DE-EDCP and EDCP, respectively. Observed results have shown that the DE-EDCP is more lipophilic with better membrane retention, but the EDCP has better pass through the membrane. Also, there has been demonstrated a reproducibility and robustness of the proposed bio-analytical method.", publisher = "Slovensko Kemijsko Drustvo, Ljubljana", journal = "Acta Chimica Slovenica", title = "Prediction of in vivo Bioavailibility by in vitro Characterization of Ethylenediamine Dipropanoic Acid Derivatives with Cytotoxic Activity", volume = "65", number = "1", pages = "59-64", doi = "10.17344/acsi.2017.3477" }
Tubić, B., Vladimirov, S., Marković, B.,& Sabo, T.. (2018). Prediction of in vivo Bioavailibility by in vitro Characterization of Ethylenediamine Dipropanoic Acid Derivatives with Cytotoxic Activity. in Acta Chimica Slovenica Slovensko Kemijsko Drustvo, Ljubljana., 65(1), 59-64. https://doi.org/10.17344/acsi.2017.3477
Tubić B, Vladimirov S, Marković B, Sabo T. Prediction of in vivo Bioavailibility by in vitro Characterization of Ethylenediamine Dipropanoic Acid Derivatives with Cytotoxic Activity. in Acta Chimica Slovenica. 2018;65(1):59-64. doi:10.17344/acsi.2017.3477 .
Tubić, Biljana, Vladimirov, Sandra, Marković, Bojan, Sabo, Tibor, "Prediction of in vivo Bioavailibility by in vitro Characterization of Ethylenediamine Dipropanoic Acid Derivatives with Cytotoxic Activity" in Acta Chimica Slovenica, 65, no. 1 (2018):59-64, https://doi.org/10.17344/acsi.2017.3477 . .