A New Sesquiterpene-Coumarin Ether and a New Abietane Diterpene and their Effects as Inhibitors of P-Glycoprotein

Madureira, AM; Molnár, Annamária; Abreu, Pedro; Molnár, Joséph; Ferreira, Maria José U.

doi:10.1055/s-2004-827231

Cited by 40 publications

(35 citation statements)

References 13 publications

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“…The reversal of this resistance, via inhibition of drug efflux mechanisms, is a promising research area. In this regard, extensive studies have been performed in order to obtain new effective resistance modifiers from plants (11). The use of these natural bacterial resistance modifiers, including…”

Section: Galbanic Acid As An Inhibitor Of S Aureusmentioning

confidence: 99%

“…1. B), a sesquiterpene coumarin ether compound, showed a significant effect in inhibiting the efflux pump activity mediated by pglycoprotein as compared with that of verapamil, a known resistance inhibitor (11). In the present study, we described the effect of galbanic acid, a major plant sesquiterpene coumarin present in Ferula szowitsiana on antimicrobial activity of antibiotics against S. aureus (18), as a modulator of antibiotic resistance on clinical isolates of S. aureus, and its possible inhibitory effect on MDR pumps.…”

Section: Galbanic Acid As An Inhibitor Of S Aureusmentioning

confidence: 99%

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Effect of galbanic acid, a sesquiterpene coumarin from Ferula szowitsiana, as an inhibitor of efflux mechanism in resistant clinical isolates of Staphylococcus aureus

Bazzaz¹,

Memariani²,

Khashiarmanesh³

et al. 2010

Braz. J. Microbiol.

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Galbanic acid, a sesquiterpene coumarin from Ferula szowitsiana roots, was investigated for its potentiating effect on the antimicrobial activity of antibiotics as well as ethidium bromide, in 6 multidrug resistance (MDR) clinical isolates of Staphylococcus aureus. Galbanic acid had inhibitory effect on none of the isolated bacteria tested (up to 800 µg /ml). The MIC range of ciprofloxacin, tetracycline and ethidium bromide, against all tested S. aureus were 10-80, 10-80 and 4-16 µg/ml, respectively. These were reduced to 2.5-5, 2.5-5 and 0.5-2 µg/ml in the presence of galbanic acid (300 µg /ml) or verapamil (100 µg /ml). The rate of ethidium bromide (2 µg /ml) accumulation in clinical isolates was enhanced with galbanic acid (300 µg /ml). There is also a decrease in loss of ethidium bromide from bacteria in the presence of galbanic acid. Similar results were obtained when verapamil (100 µg /ml) was used as an efflux pump inhibitor. Galbanic acid, like verapamil, a typical inhibitor of efflux pump, reduced the MIC of ethidium bromide and tested antibiotics. Since efflux is the only known reported mechanism for ethidium bromide resistance, the reduction in ethidium bromide MIC and enhanced accumulation as well as decreased efflux of ethidium bromide in the presence of galbanic acid, can be attributed to this efflux inhibitory properties.

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Section: Galbanic Acid As An Inhibitor Of S Aureusmentioning

confidence: 99%

Section: Galbanic Acid As An Inhibitor Of S Aureusmentioning

confidence: 99%

Effect of galbanic acid, a sesquiterpene coumarin from Ferula szowitsiana, as an inhibitor of efflux mechanism in resistant clinical isolates of Staphylococcus aureus

Bazzaz¹,

Memariani²,

Khashiarmanesh³

et al. 2010

Braz. J. Microbiol.

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“…It has been shown that sesquiterpenes from the Celastraceae and Euphorbiaceae families could act as reversal agents (Spivey et al, 2002;Madureira et al, 2004). The probable mechanism of feselol action could be its interaction with and inhibition of the function of the MRP2.…”

Section: Discussionmentioning

confidence: 99%

“…Sesquiterpene coumarins of the drimane type (diportlandin, conferone, mogoltacin, and feselol, Fig. 1) can increase the accumulation and effectiveness of several anticancer agents (Madureira et al, 2004;Barthomeuf et al, 2006;Neshati et al, 2009;Behnam Rassouli et al, 2009;Rassouli et al, 2011a;Mollazadeh et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

Feselol Enhances the Cytotoxicity and DNA Damage Induced by Cisplatin in 5637 Cells

Mollazadeh

Matin

Bahrami

et al. 2011

Zeitschrift Für Naturforschung C

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Transitional cell carcinoma (TCC), which is the most common type of bladder cancer, shows resistance to chemotherapeutic agents due to the overexpression of drug effl ux pumps. In this study, the effects of feselol, a sesquiterpene coumarin extracted from Ferula badrakema, on cisplatin cytotoxicity were investigated in 5637 cells, a TCC subline. Cell viability and DNA lesion were evaluated by thiazolyl blue tetrazolium bromide and comet assays, respectively. Feselol had no signifi cant cytotoxic effect in 5637 cells but at 32 μg/mL it increased the cytotoxicity of 1 μg/mL cisplatin by 37% after 24 h. Furthermore, the comet assay revealed that DNA damage induced by cisplatin in 5637 cells is enhanced by 31% when used in combination with feselol. Therefore, feselol might be considered as an effective reversal agent for future in vivo and clinical studies.

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“…A new sesquiterpene-coumarin ether (5 0 b, Figure 4, Table 5) was isolated and characterized from the Me 2 CO extract of whole dried plant of Euphorbia portlandica 105 . Examined for its effects on the reversal of MDR on mouse lymphoma cells (L5178), sesquiterpene-coumarin ether proved to be more active than the verapamil.…”

Section: Coumarinsmentioning

confidence: 99%

Advances in plant-based inhibitors of P-glycoprotein

Zhou

James

et al. 2016

Journal of Enzyme Inhibition and Medicinal Chemistry

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Multidrug resistance (MDR) has emerged as the main problem in anti-cancer therapy. Although MDR involves complex factors and processes, the main pivot is the expression of multidrug efflux pumps. P-glycoprotein (P-gp) belongs to the family of adenosine triphosphate (ATP)-binding cassette (ABC) transporters. It functions in cellular detoxification, pumping a wide range of xenobiotic compounds out of the cell. An attractive therapeutic strategy for overcoming MDR is to inhibit the transport function of P-gp and thus, increase intracellular concentration of drugs. Recently, various types of P-gp inhibitors have been found and used in experiments. However, none of them has passed clinical trials due to their high side-effects. Hence, the search for alternatives, such as plant-based P-gp inhibitors have gained attention recently. Therefore, we give an overview of the source, function, structure and mechanism of plant-based P-gp inhibitors and give more attention to cancer-related studies. These products could be the future potential drug candidates for further research as P-gp inhibitors.

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A New Sesquiterpene-Coumarin Ether and a New Abietane Diterpene and their Effects as Inhibitors of P-Glycoprotein

Cited by 40 publications

References 13 publications

Effect of galbanic acid, a sesquiterpene coumarin from Ferula szowitsiana, as an inhibitor of efflux mechanism in resistant clinical isolates of Staphylococcus aureus

Effect of galbanic acid, a sesquiterpene coumarin from Ferula szowitsiana, as an inhibitor of efflux mechanism in resistant clinical isolates of Staphylococcus aureus

Feselol Enhances the Cytotoxicity and DNA Damage Induced by Cisplatin in 5637 Cells

Advances in plant-based inhibitors of P-glycoprotein

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