scholarly journals Propafenone analogue with additional H‐bond acceptor group shows increased inhibitory activity on P‐glycoprotein

2020 ◽  
Vol 353 (3) ◽  
pp. 1900269
Author(s):  
Anna Cseke ◽  
Theresa Schwarz ◽  
Sankalp Jain ◽  
Simon Decker ◽  
Kerstin Vogl ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
P Glycoprotein ◽  
Acceptor Group

scholarly journals Quantitative Structure–Activity Relationships for the Flavonoid-Mediated Inhibition of P-Glycoprotein in KB/MDR1 Cells

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1661 ◽  
Author(s):  
Mengmeng Xia ◽  
Yajing Fang ◽  
Weiwei Cao ◽  
Fuqiang Liang ◽  
Siyi Pan ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Qsar Model ◽  
Quantitative Structure Activity Relationship ◽  
Quantitative Structure ◽  
Glycoprotein P ◽  
Chemotherapy Drugs ◽  
Structure Activity ◽  
P Glycoprotein ◽  
Daily Diet ◽  
Low Toxicity

P-glycoprotein (P-gp) serves as a therapeutic target for the development of inhibitors to overcome multidrug resistance (MDR) in cancer cells. In order to enhance the uptake of chemotherapy drugs, larger amounts of P-gp inhibitors are required. Besides several chemically synthesized P-gp inhibitors, flavonoids as P-gp inhibitors are being investigated, with their advantages including abundance in our daily diet and a low toxicity. The cytotoxicity of daunorubicin (as a substrate of P-gp) to KB/MDR1 cells and the parental KB cells was measured in the presence or absence of flavonoids. A two-dimensional quantitative structure–activity relationship (2D-QSAR) model was built with a high cross-validation coefficient (Q2) value of 0.829. Descriptors including vsurf_DW23, E_sol, Dipole and vsurf_G were determined to be related to the inhibitory activity of flavonoids. The lack of 2,3-double bond, 3′-OH, 4′-OH and the increased number of methoxylated substitutions were shown to be beneficial for the inhibition of P-gp. These results are important for the screening of flavonoids for inhibitory activity on P-gp.

P-Glycoprotein Inhibitory Activity of Lipophilic Constituents of Echinacea pallida Roots in a Human Proximal Tubular Cell Line

Planta Medica ◽  
2008 ◽  
Vol 74 (3) ◽  
pp. 264-266 ◽  
Author(s):  
Nadia Romiti ◽  
Federica Pellati ◽  
Paola Nieri ◽  
Stefania Benvenuti ◽  
Barbara Adinolfi ◽  
...  
Keyword(s):  
Cell Line ◽  
Inhibitory Activity ◽  
Proximal Tubular Cell ◽  
Tubular Cell ◽  
P Glycoprotein ◽  
Echinacea Pallida ◽  
Proximal Tubular

scholarly journals From Taxuspine X to Structurally Simplified Taxanes with Remarkable P-Glycoprotein Inhibitory Activity

2010 ◽  
Vol 1 (8) ◽  
pp. 416-421 ◽  
Author(s):  
Daniele Castagnolo ◽  
Lorenzo Contemori ◽  
Giorgio Maccari ◽  
Stanislava I. Avramova ◽  
Annalisa Neri ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
P Glycoprotein

scholarly journals Euryops pectinatus L. Flower Extract Inhibits P-glycoprotein and Reverses Multi-Drug Resistance in Cancer Cells: A Mechanistic Study

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 647 ◽  
Author(s):  
Wafaa M. Elkady ◽  
Iriny M. Ayoub ◽  
Yousra Abdel-Mottaleb ◽  
Mohamed F. ElShafie ◽  
Michael Wink
Keyword(s):  
Molecular Docking ◽  
Multidrug Resistance ◽  
Cancer Cells ◽  
Inhibitory Activity ◽  
In Silico ◽  
Chemotherapeutic Agents ◽  
Selective Cytotoxicity ◽  
Flower Extract ◽  
P Glycoprotein ◽  
In Silico Molecular Docking

Euryops pectinatus is a South African ornamental plant belonging to family Asteraceae. The present work evaluates the cytotoxic activity and phytochemical profile of the flower extract. Metabolite profiling was performed using HPLC-PDA-ESI-MS/MS. Total phenolics and flavonoids content were assessed. Cytotoxicity was evaluated against 6 different cancer cell lines using MTT assay. The possible underlying mechanism was proposed. We analyzed whether the extract could overcome the resistance of multidrug-resistant cancer cells for doxorubicin. The effect of combination of E. pectinatus with doxorubicin was also studied. Additionally, the potential inhibitory activity of the identified phytochemicals to PB1 protein was analyzed using in silico molecular docking. Twenty-five compounds were tentatively identified. Total phenolic and flavonoid contents represented 49.41 ± 0.66 and 23.37 ± 0.23 µg/mg dried flower extract, respectively. The extract showed selective cytotoxicity against Caco2 cells but its main effect goes beyond mere cytotoxicity. It showed strong inhibition of P-glycoprotein, which helps to overcome multidrug resistance to classical chemotherapeutic agents. In silico molecular docking showed that dicaffeoyl quinic acid, kaempferol-O-rutinoside, rutin, and isorhamnetin-O-rutinoside exhibited the most potent inhibitory activity to PB1 involved in tumor progression. Euryops pectinatus flower heads could have promising selective cytotoxicity alone or in combination with other chemotherapeutic agents to counteract multidrug resistance.

Secondary Metabolites from Endophytic Pestalotiopsis microspora and Their P-Glycoprotein Inhibitory Activity

2021 ◽  
Vol 57 (5) ◽  
pp. 924-926
Author(s):  
Yi-Xin Qian ◽  
Ji-Chuan Kang ◽  
Yi-Kai Luo ◽  
Xing-Bian Yang ◽  
Jun He ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Inhibitory Activity ◽  
P Glycoprotein ◽  
Pestalotiopsis Microspora

scholarly journals Inside Cover: 1-Cyclohexyl-4-(4-arylcyclohexyl)piperazines: Mixed σ and Human Δ8-Δ7 Sterol Isomerase Ligands with Antiproliferative and P-Glycoprotein Inhibitory Activity (ChemMedChem 1/2011)

ChemMedChem ◽  
2010 ◽  
Vol 6 (1) ◽  
pp. 2-2
Author(s):  
Carmen Abate ◽  
Mauro Niso ◽  
Marialessandra Contino ◽  
Nicola Antonio Colabufo ◽  
Savina Ferorelli ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
P Glycoprotein

Comparison of the inhibitory activity of anti-HIV drugs on P-glycoprotein

2007 ◽  
Vol 73 (10) ◽  
pp. 1573-1581 ◽  
Author(s):  
Caroline Henrike Storch ◽  
Dirk Theile ◽  
Heike Lindenmaier ◽  
Walter Emil Haefeli ◽  
Johanna Weiss
Keyword(s):  
Inhibitory Activity ◽  
P Glycoprotein ◽  
Hiv Drugs ◽  
Anti Hiv

scholarly journals The Inhibitory Activity of Curcumin on P-Glycoprotein and Its Uptake by and Efflux from LS180 Cells Is Not Affected by Its Galenic Formulation

Antioxidants ◽  
2021 ◽  
Vol 10 (11) ◽  
pp. 1826
Author(s):  
Sandra Flory ◽  
Romina Männle ◽  
Jan Frank
Keyword(s):  
Cell Culture ◽  
Inhibitory Activity ◽  
Important Determinant ◽  
Biological Activities ◽  
Intestinal Cells ◽  
Free Medium ◽  
Clear Effect ◽  
P Glycoprotein ◽  
Pre Treatment ◽  
Culture Supernatants

The biological activities of curcumin in humans, including its antioxidative and anti-inflammatory functions, are limited by its naturally low bioavailability. Different formulation strategies have been developed, but the uptake of curcumin from these galenic formulations into and efflux from intestinal cells, which may be critical processes limiting bioavailability, have not been directly compared. Furthermore, little is known about their effect on P-glycoprotein activity, an important determinant of the pharmacokinetics of potentially co-administered drugs. P-glycoprotein activity was determined in LS180 cells, incubated with 30 or 60 µmol/L of curcumin in the form of seven different formulations or native curcuma extract for 1 h. All formulations inhibited P-glycoprotein activity at both concentrations. Curcumin uptake, after 1 h incubation of LS180 cells with the formulations (60 µmol/L), showed significant variability but no consistent effects. After 1 h pre-treatment with the formulations and further 8 h with curcumin-free medium, curcumin in cell culture supernatants, reflecting the efflux, differed between individual formulations, again without a clear effect. In conclusion, curcumin inhibits P-glycoprotein activity independently of its formulation. Its uptake by and efflux from intestinal cells was not significantly different between formulations, indicating that these processes are not important regulatory points for its bioavailability.

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