Inhibition of P-glycoprotein-mediated transport by extracts of and monoterpenoids contained in Zanthoxyli Fructus

Yoshida, Naoko; Takagi, Akiyoshi; Kitazawa, Hidenori; Kawakami, Junichi; Adachi, Isao

doi:10.1016/j.taap.2005.04.001

Cited by 52 publications

(39 citation statements)

References 22 publications

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“…Previously, we investigated possible interactions between Japanese traditional herbal medicines and conventional medicines (Kawakami et al, 2002) and reported that an extract of Zanthoxyli Fructus and some terpenoids can inhibit P-gp-mediated efflux transport in vitro and in vivo (Yoshida et al, 2005(Yoshida et al, , 2006b. In the present study, the inhibitory effects of seven terpenoids (Fig.…”

mentioning

confidence: 52%

“…In our preliminary experiments for the present report, MRP2-or BCRP-mediated transport was attempted to be evaluated by the whole cell-based assay such as the intracellular accumulation and transcellular transport studies as shown in our previous reports (Yoshida et al, 2005(Yoshida et al, , 2006a. However, an active efflux via these transporters was not shown probably because of the high hydrophilicity of the specific substrate used ([ 3 H]E 2 17␤G).…”

Section: Discussionmentioning

confidence: 99%

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Inhibitory Effects of Terpenoids on Multidrug Resistance-Associated Protein 2- and Breast Cancer Resistance Protein-Mediated Transport

Yoshida¹,

Takada²,

Yamamura³

et al. 2008

Drug Metabolism and Disposition

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ABSTRACT:The possibility of interactions between natural products/supplements and conventional prescription medicines is one of the most important issues in pharmacotherapeutic safety. Recently, we reported that some terpenoids such as (R)-(؉)-citronellal and glycyrrhetic acid, which are present in herbal medicines, can act as inhibitors of P-glycoprotein (MDR1/ABCB1). In the present study, the effects of seven terpenoids on multidrug resistance-associated protein 2 (MRP2/ABCC2) and breast cancer resistance protein (BCRP/ ABCG2)-mediated transport were investigated in vitro. Membrane vesicles were prepared from MRP2 cDNA transfected Sf9 cells derived from pupal ovarian tissue of Spodoptera frugiperda, a fall armyworm, and BCRP cDNA transfected LLC-PK1 cells derived from porcine kidney. MRP2-or BCRP-mediated efflux transport was measured as ATP-dependent accumulation of [ 3 H]estradiol 17-␤-D-glucuronide (E 2 17␤G) into membrane vesicles collected by a rapid filtration technique. The effects of (R)-(؉)-citronellal, (S)-(؊)-␤-citronellol, ␣-terpinene, terpinolene, (؊)-␤-pinene

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mentioning

confidence: 52%

Section: Discussionmentioning

confidence: 99%

Inhibitory Effects of Terpenoids on Multidrug Resistance-Associated Protein 2- and Breast Cancer Resistance Protein-Mediated Transport

Yoshida¹,

Takada²,

Yamamura³

et al. 2008

Drug Metabolism and Disposition

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“…Furthermore, the component monoterpenoids of the essential oil of Zanthoxyli fructus, demonstrate a strong inhibition of P-glycoprotein (25). TPL is a diterpenoid triepoxide derived from the herb Tripterygium wilfordii, and is proposed to have a similar molecular structure to the monoterpenoids.…”

Section: Discussionmentioning

confidence: 99%

Modulation of P-glycoprotein expression by triptolide in adriamycin-resistant K562/A02 cells

Hui

et al. 2011

Oncology Letters

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Abstract. Multidrug resistance is a serious obstacle encountered in leukemia treatment. Previous studies have found drug resistance in human leukemia is mainly associated with overexpression of the multidrug resistance gene 1 (MDR1). The aim of the present study was to investigate the modulation of P-glycoprotein expression by triptolide in adriamycin-resistant K562/A02 cells. The reverse effects of triptolide on drug resistance in K562/A02 cells were assessed by 3-[4,5-dimethylthiazol-2-yl]-2, 5-diphenyl-tetrazolium bromide (MTT) assay. The percentage of apoptotic cells was obtained from annexin V/fluorescein isothiocyanate (FITC) and propridium iodide (PI) double-staining. The effects of triptolide on P-glycoprotein activity were evaluated by measuring intracellular adriamycin accumulation. The expression of P-glycoprotein was determined by flow cytometry. A luciferase reporter gene assay was used to detect the transcriptional activity of the MDR1 promoter. Results revealed that triptolide decreased the degree of resistance of K562/A02 cells, and significantly inhibited P-glycoprotein expression and drug-transport function, and increased the accumulation of adriamycin in K562/A02 cells as measured by flow cytometry. A luciferase reporter gene assay demonstrated that triptolide was capable of inhibiting the transcriptional activity of the MDR1 promoter. Triptolide may effectively reverse the adriamycin resistance in K562/A02 cells via modulation of the P-glycoprotein expression and by increasing intracellular adriamycin accumulation.

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“…25 In a previous study in vitro, we found an extract of and some monoterpenoids in Zanthoxyli Fructus and some other citrus herbs (Rutaceae) inhibited the P-gpmediated efflux of [ 3 H]digoxin in P-gp-transfected LLC-PK1 cells. 26 We found that (R)-(þ)-citronellal ( Fig. 1), a monoterpenoid with a relatively lower molecular weight (&150) and no aromatic ring, contained in the essential oil of Zanthoxyli Fructus can be a potent P-gp inhibitor.…”

Section: Introductionmentioning

confidence: 83%

Effects of citronellal, a monoterpenoid in Zanthoxyli Fructus, on the intestinal absorption of digoxin in vitro and in vivo

Yoshida

Takagi

Kitazawa

et al. 2006

Journal of Pharmaceutical Sciences

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Inhibition of P-glycoprotein-mediated transport by extracts of and monoterpenoids contained in Zanthoxyli Fructus

Cited by 52 publications

References 22 publications

Inhibitory Effects of Terpenoids on Multidrug Resistance-Associated Protein 2- and Breast Cancer Resistance Protein-Mediated Transport

Inhibitory Effects of Terpenoids on Multidrug Resistance-Associated Protein 2- and Breast Cancer Resistance Protein-Mediated Transport

Modulation of P-glycoprotein expression by triptolide in adriamycin-resistant K562/A02 cells

Effects of citronellal, a monoterpenoid in Zanthoxyli Fructus, on the intestinal absorption of digoxin in vitro and in vivo

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