Effects of Curcuma spp. on P-glycoprotein function

Ampasavate, Chadarat; Sotanaphun, Uthai; Phattanawasin, Panadda; Piyapolrungroj, Nusara

doi:10.1016/j.phymed.2009.09.004

Cited by 47 publications

(44 citation statements)

References 24 publications

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“…14 The individual effects of C, DMC, and BDMC on P-gp expression and function were tested in limited studies. 16,17 One study focused on the characterization of C, DMC, and BDMC effects on P-gp function using KB-V1 and KB-3-1 cells, which were multidrug resistance and drug sensitive cervical carcinoma cells, respectively. 17 Their results demonstrated that The IC 50 values of the inhibitory effect of C, DMC, and BDMC on rhodamine 123 efflux by P-gp were 5.8 ± 0.32, 1.56 ± 0.13, and 3.08 ± 0.19 μM, respectively, indicating that DMC possessed the most potent effect on rhodamine 123 efflux by P-gp.…”

Section: ■ Discussionmentioning

confidence: 99%

“…Recently, limited studies reported that the isolated curcumin, demethoxycurcumin, and bisdemethoxycurcumin may diversely contribute to the influence of P-gp expression and function. 16,17 However, inconsistent results have been obtained among different studies, and kinetic mechanisms of interactions between P-gp and the three major curcuminoids were not investigated.…”

Section: ■ Introductionmentioning

confidence: 99%

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Demethoxycurcumin Modulates Human P-Glycoprotein Function via Uncompetitive Inhibition of ATPase Hydrolysis Activity

Teng

Hsieh

Hung

et al. 2015

J. Agric. Food Chem.

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Curcuminoids are major components of Curcuma longa L., which is widely used as spice in food. This study aimed at identifying whether curcumin, demethoxycurcumin, and bisdemethoxycurcumin could modulate efflux function of human P-glycoprotein and be used as chemosensitizers in cancer treatments. Without altering P-glycoprotein expression levels and conformation, the purified curcuminoids significantly inhibited P-glycoprotein efflux function. In rhodamine 123 efflux and calcein-AM accumulation assays, demethoxycurcumin demonstrated the highest inhibition potency (inhibitory IC50 = 1.56 ± 0.13 μM) among the purified curcuminoids, as well as in the fold of reversal assays. Demethoxycurcumin inhibited P-glycoprotein-mediated ATP hydrolysis under concentrations of <1 μM and efficiently inhibited 200 μM verapamil-stimulated ATPase activity, indicating a high affinity of demethoxycurcumin for P-glycoprotein. These results suggested that demethoxycurcumin may be a potential additive natural product in combination with chemotherapeutic agents in drug-resistant cancers.

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Section: ■ Discussionmentioning

confidence: 99%

Section: ■ Introductionmentioning

confidence: 99%

Demethoxycurcumin Modulates Human P-Glycoprotein Function via Uncompetitive Inhibition of ATPase Hydrolysis Activity

Teng

Hsieh

Hung

et al. 2015

J. Agric. Food Chem.

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“…Curcumin and demethoxy curcumin inhibit P-gp, but not bisdemethoxy curcumin Ampasavate et al (2010) Curcuma longa Ramified curcumin hydrolyzed K562/A02 leukemia Downregulation of P-gp and MDR1 expression, increased sensitivity to anticancer drugs Huang et al (2010) Scutellaria baicalensis Baicalin Rats Involvement of P-gp in active baicalin efflux into bile. P-gp inhibitors cyclosporin A and quinidine promoted active baicalin transport into bile and reduced drug levels in the blood, but had no effect on blood-brain barrier passage of baicalin Tsai and Tsai (2004b) …”

Section: Caco-2 Intestinal Cells Llc-ga5-col300mentioning

confidence: 99%

P-glycoprotein and its inhibition in tumors by phytochemicals derived from Chinese herbs

Eichhorn

Efferth

2012

Journal of Ethnopharmacology

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“…Increase sensitivity to anticancer drugs by inhibition of MDR1 expression [61] In vitro Inhibition of P-gp function [62] Marsdenia tenacissima Cancer, asthma In vitro Inhibition of P-gp function [63] Paeonia alba Menstrual disorders, heat rashes, stops bleeding In vitro Induction of intestinal P-gp expression [64] Paeonia lactiflora Reduces fever and pain, prevents infection In vitro Inhibition of P-gp efflux function [65] Peucadanum praeruptorum…”

Section: In Vitromentioning

confidence: 99%

The effect of herbal materials on the p-glycoprotein activity and function

et al. 2013

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S u m m a r y P-glycoprotein (P-gp) encoded by the MDR1 (multidrug resistance 1) gene is ATP-dependent transporting protein which is localizated in the cell membrane. P-gp is expressed REVIEW ARTICLE Unauthenticated Download Date | 6/7/19 11:36 AM 130 A. Bogacz, D. Deka-Pawlik, J. Bartkowiak-Wieczorek, M. Karasiewicz, R. Kujawski, A. Kowalska, A. Chałas, B. Czerny, E.Grześkowiak, P. M. Mrozikiewicz mainly in organs with the secretory functions and its physiological role concerns tissue protection against xenobiotics. P-glycoprotein is involved in the permeability barriers of the blood-brain, blood-placenta directly protecting these organs. It participates in the transport of many drugs and other xenobiotics affecting their absorption, distribution, metabolism and excretion. The high P-gp activity in the cell membranes of cancer tissue is a major cause of lack of effectiveness of chemotherapy. Hence, the methods which could increase the sensibility of these pathological cells to cytostatics are still being searched.In the experimental studies it was shown that natural plant substances may have an effect on the expression level and activity of P-glycoprotein. Hypericum perforatum, ginkgo biloba and Camellia sinensis increase P-gp activity while curcumin from Curcuma longa, piperine and silymarin inhibit this protein. Taking into account a wide substrate spectrum of P-gp, application of our knowledge on interactions of herbals and synthetic drugs should be considered in order to improve drug impact on different tissues.

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Effects of Curcuma spp. on P-glycoprotein function

Cited by 47 publications

References 24 publications

Demethoxycurcumin Modulates Human P-Glycoprotein Function via Uncompetitive Inhibition of ATPase Hydrolysis Activity

Demethoxycurcumin Modulates Human P-Glycoprotein Function via Uncompetitive Inhibition of ATPase Hydrolysis Activity

P-glycoprotein and its inhibition in tumors by phytochemicals derived from Chinese herbs

The effect of herbal materials on the p-glycoprotein activity and function

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