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

a 2019

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

DRABINOVÁ, Martina, Martina ČARNECKÁ, Otakar HUMPA, Iva SLANINOVÁ, Jiří SLANINA et. al.

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

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

References:

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

Abstract

V originále

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

Citovat

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.

@proceedings{1558936,
   author = {Drabinová, Martina and Čarnecká, Martina and Humpa, Otakar and Slaninová, Iva and Slanina, Jiří},
   booktitle = {20. ročník Školy hmotnostní spektrometrie},
   keywords = {liquid chromatography; mass spectrometry; lignans; bioactivity; isomerism; Schizandra},
   language = {eng},
   isbn = {978-80-88195-14-6},
   title = {SYNTHESIS AND EVALUATION OF ACETYL DERIVATIVES OF DIBENZOCYCLOOCTADIENE LIGNANS AS P-GLYCOPROTEIN INHIBITORS},
   url = {http://www.skolams.cz/},
   year = {2019}
}

TY  - CONF
ID  - 1558936
AU  - Drabinová, Martina - Čarnecká, Martina - Humpa, Otakar - Slaninová, Iva - Slanina, Jiří
PY  - 2019
TI  - SYNTHESIS AND EVALUATION OF ACETYL DERIVATIVES OF DIBENZOCYCLOOCTADIENE LIGNANS AS P-GLYCOPROTEIN INHIBITORS
SN  - 9788088195146
KW  - liquid chromatography
KW  - mass spectrometry
KW  - lignans
KW  - bioactivity
KW  - isomerism
KW  - Schizandra
UR  - http://www.skolams.cz/
L2  - http://www.skolams.cz/
N2  - 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.
ER  -

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 \textit{20. ročník Školy hmotnostní spektrometrie}. 2019. ISBN~978-80-88195-14-6.

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