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Verfasst von:Tajima, Yasuhiro [VerfasserIn]   i
 Nakagawa, Hiroshi [VerfasserIn]   i
 Tamura, Ai [VerfasserIn]   i
 Kadioglu, Onat [VerfasserIn]   i
 Satake, Kazuhiro [VerfasserIn]   i
 Mitani, Yuji [VerfasserIn]   i
 Murase, Hayato [VerfasserIn]   i
 Regasini, Luis Octavio [VerfasserIn]   i
 Silva Bolzani, Vanderlan [VerfasserIn]   i
 Ishikawa, Toshihisa [VerfasserIn]   i
 Fricker, Gert [VerfasserIn]   i
 Efferth, Thomas [VerfasserIn]   i
Titel:Nitensidine A, a guanidine alkaloid from Pterogyne nitens, is a novel substrate for human ABC transporter ABCB1
Verf.angabe:Yasuhiro Tajima, Hiroshi Nakagawa, Ai Tamura, Onat Kadioglu, Kazuhiro Satake, Yuji Mitani, Hayato Murase, Luis Octavio Regasini, Vanderlan da Silva Bolzani, Toshihisa Ishikawa, Gert Fricker, Thomas Efferth
Jahr:2014
Jahr des Originals:2013
Umfang:10 S.
Fussnoten:Online 14 October 2013 ; Gesehen am 01.10.2020
Titel Quelle:Enthalten in: Phytomedicine
Ort Quelle:München [u.a.] : Elsevier, 1994
Jahr Quelle:2014
Band/Heft Quelle:21(2014), 3, Seite 323-332
ISSN Quelle:1618-095X
Abstract:The Pterogyne nitens (Fabaceae) tree, native to South America, has been found to produce guanidine alkaloids as well as bioactive flavonols such as kaempferol, quercetin, and rutin. In the present study, we examined the possibility of interaction between human ATP-binding cassette (ABC) transporter ABCB1 and four guanidine alkaloids isolated from P. nitens (i.e., galegine, nitensidine A, pterogynidine, and pterogynine) using human T cell lymphoblast-like leukemia cell line CCRF-CEM and its multi-drug resistant (MDR) counterpart CEM/ADR5000. In XTT assays, CEM/ADR5000 cells were resistant to the four guanidine alkaloids compared to CCRF-CEM cells, although the four guanidine alkaloids exhibited some level of cytotoxicity against both CCRF-CEM and CEM/ADR5000 cells. In ATPase assays, three of the four guanidine alkaloids were found to stimulate the ATPase activity of ABCB1. Notably, nitensidine A was clearly found to stimulate the ATPase activity of ABCB1 as strongly as the control drug, verapamil. Furthermore, the cytotoxic effect of nitensidine A on CEM/ADR5000 cells was synergistically enhanced by verapamil. Nitensidine A inhibited the extrusion of calcein by ABCB1. In the present study, the possibility of interaction between ABCB1 and two synthetic nitensidine A analogs (nitensidine AT and AU) were examined to gain insight into the mechanism by which nitensidine A stimulates the ATPase activity of ABCB1. The ABCB1-dependent ATPase activity stimulated by nitensidine A was greatly reduced by substituting sulfur (S) or oxygen (O) for the imino nitrogen atom (N) in nitensidine A. Molecular docking studies on human ABCB1 showed that, guanidine alkaloids from P. nitens dock to the same binding pocket as verapamil. Nitensidine A and its analogs exhibit similar binding energies to verapamil. Taken together, this research clearly indicates that nitensidine A is a novel substrate for ABCB1. The present results also suggest that the number, binding site, and polymerization degree of the isoprenyl moiety in the guanidine alkaloids and the imino nitrogen atom cooperatively contribute to their stimulation of ABCB1's ATPase activity.
DOI:doi:10.1016/j.phymed.2013.08.024
URL:Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.

Volltext ; Verlag: https://doi.org/10.1016/j.phymed.2013.08.024
 Volltext: http://www.sciencedirect.com/science/article/pii/S0944711313003279
 DOI: https://doi.org/10.1016/j.phymed.2013.08.024
Datenträger:Online-Ressource
Sprache:eng
Sach-SW:ABCB1
 ATP-binding cassette (ABC) transporter
 Guanidine alkaloid
 P-glycoprotein
K10plus-PPN:1734273666
Verknüpfungen:→ Zeitschrift

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