SYNTHESIS AND EVALUATION OF ACETYL DERIVATIVES OF DIBENZOCYCLOOCTADIENE LIGNANS AS P-GLYCOPROTEIN INHIBITORS

DRABINOVÁ, Martina, Martina ČARNECKÁ, Otakar HUMPA, Iva SLANINOVÁ and Jiří SLANINA. SYNTHESIS AND EVALUATION OF ACETYL DERIVATIVES OF DIBENZOCYCLOOCTADIENE LIGNANS AS P-GLYCOPROTEIN INHIBITORS. In 20. ročník Školy hmotnostní spektrometrie. 2019. ISBN 978-80-88195-14-6.

Basic information

• Original name: SYNTHESIS AND EVALUATION OF ACETYL DERIVATIVES OF DIBENZOCYCLOOCTADIENE LIGNANS AS P-GLYCOPROTEIN INHIBITORS
• Authors: DRABINOVÁ, Martina (203 Czech Republic, belonging to the institution), Martina ČARNECKÁ (703 Slovakia, belonging to the institution), Otakar HUMPA (203 Czech Republic, belonging to the institution), Iva SLANINOVÁ (203 Czech Republic, belonging to the institution) and Jiří SLANINA (203 Czech Republic, guarantor, belonging to the institution).
• Edition: 20. ročník Školy hmotnostní spektrometrie, 2019.

Other information

• Original language: English
• Type of outcome: Conference abstract
• Field of Study: 30104 Pharmacology and pharmacy
• Country of publisher: Czech Republic
• Confidentiality degree: is not subject to a state or trade secret
• WWW: URL
• RIV identification code: RIV/00216224:14110/19:00110717
• Organization unit: Faculty of Medicine
• ISBN: 978-80-88195-14-6
• Keywords in English: liquid chromatography; mass spectrometry; lignans; bioactivity; isomerism; Schizandra
• Tags: rivok

Abstract

P-glycoprotein is typical ATP binding cassette (ABC) transporter responsible for the transportation out of cells of various xenobiotics including cytostatic compounds. A possible method for overcoming the resistance to anticancer drugs is the coadministration of compounds showing low toxicity and an ability to inhibit ABC transporters. Promising inhibitory activity has been discovered group of plant phenols, the dibenzocyclooctadiene lignans, from two plant genera Schisandra and Kadsura. The main source of these lignans are the fruits of Schisandra chinensis. In previous works three main structural features of dibenzocyclooctadiene lignans involved in P-glycoprotein inhibition were revealed: a 1,2,3-trimethoxy moiety, a 6- acyloxy group, and the absence of a 7-hydroxy group. To prepare more active derivatives, 7-hydroxy group was modified by acetylation.

Links

• MUNI/A/0976/2018, interní kód MU: Name: Příspěvek chemických a biochemických metodik ke studiu molekulární podstaty vybraných patologických stavů a onemocnění

Investor: Masaryk University, Category A