P-glycoprotein inhibitors of natural origin as potential tumor chemo-sensitizers: A review.
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Abdallah HM, Al-Abd AM, El-Dine RS, El-Halawany AM
P-glycoprotein inhibitors of natural origin as potential tumor chemo-sensitizers: A review.
J Adv Res. 2015 Jan;6(1):45-62. doi: 10.1016/j.jare.2014.11.008. Epub 2014 Dec 1.
- PubMed ID
- 25685543 [ View in PubMed]
- Abstract
Resistance of solid tumors to treatment is significantly attributed to pharmacokinetic reasons at both cellular and multi-cellular levels. Anticancer agent must be bio-available at the site of action in a cytotoxic concentration to exert its proposed activity. P-glycoprotein (P-gp) is a member of the ATP-dependent membrane transport proteins; it is known to pump substrates out of cells in ATP-dependent mechanism. The over-expression of P-gp in tumor cells reduces the intracellular drug concentrations, which decreases the cytotoxicity of a broad spectrum of antitumor drugs. Accordingly, P-gp inhibitors/blockers are potential enhancer for the cellular bioavailability of several clinically important anticancer drugs such as, anthracyclines, taxanes, vinca alkaloids, and podophyllotoxins. Besides several chemically synthesized P-gp inhibitors/blockers, some naturally occurring compounds and plant extracts were reported for their modulation of multidrug resistance; however, this review will focus only on major classes of naturally occurring inhibitors viz., flavonoids, coumarins, terpenoids, alkaloids and saponins.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Emopamil P-glycoprotein 1 Protein Humans YesInhibitorDetails - Drug Transporters
Drug Transporter Kind Organism Pharmacological Action Actions Emopamil P-glycoprotein 1 Protein Humans UnknownInhibitorDetails Gallopamil P-glycoprotein 1 Protein Humans UnknownInhibitorDetails Naringenin P-glycoprotein 1 Protein Humans UnknownDownregulatorDetails