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Curcumin down-regulates the multidrug-resistance mdr1b gene by inhibiting the PI3K/Akt/NF kappa B pathway
Byeong Hyeok Choi1, Chang Gun Kim, Yoongho Lim
1Department of Biomedical Science and Technology, IBST, Konkuk University, Seoul 143-701, Republic of Korea.
Abstract:
Curcumin, a constituent of turmeric, has anti-inflammatory, anti-carcinogenic, and chemopreventive effects in several animal tumor models. The expression of P-glycoprotein (P-gp), encoded by the mdr gene, is often associated with multidrug resistance (MDR) to unrelated chemotherapeutic drugs in cancer cells. Here, we demonstrate that curcumin down-regulates P-gp expression in multidrug-resistant L1210/Adr cells. Transfection with a series of 5'-deleted constructs of the mdr1b gene promoter indicated that a proximal region between -205 and +42 of the sequence was responsible for the suppression of promoter activity by curcumin. This response might be associated with the inhibition of the phosphatidyinositol 3-kinase (PI3K)/Akt/nuclear factor-kappa B (NF-kappa B) signaling pathway by curcumin. Moreover, curcumin reversed the MDR of the L1210/Adr cells. Thus, curcumin can contribute to the reversal of the MDR phenotype, probably due to the suppression of P-gp expression via the inhibition of the PI3K/Akt/NF-kappa B signaling pathway.
Insights
Curcumin, a turmeric compound, reduces P-glycoprotein expression in drug-resistant cancer cells. This action may reverse multidrug resistance by inhibiting key cellular signaling pathways.
Area of Science:
- Pharmacology
- Molecular Biology
- Cancer Research
Background:
- Curcumin, derived from turmeric, exhibits anti-inflammatory and anti-carcinogenic properties.
- P-glycoprotein (P-gp) expression, regulated by the mdr gene, is linked to multidrug resistance (MDR) in cancer.
- Multidrug resistance poses a significant challenge in cancer chemotherapy.
Purpose of the Study:
- To investigate the effect of curcumin on P-glycoprotein expression in multidrug-resistant cancer cells.
- To identify the specific gene promoter region responsible for curcumin's effect on P-gp expression.
- To explore the signaling pathways involved in curcumin-mediated suppression of P-gp.
Main Methods:
- Utilized multidrug-resistant L1210/Adr cells.
- Performed transfections with 5'-deleted constructs of the mdr1b gene promoter.
- Analyzed the involvement of the PI3K/Akt/NF-kappa B signaling pathway.
Main Results:
- Curcumin significantly down-regulates P-glycoprotein expression in L1210/Adr cells.
- A proximal region of the mdr1b gene promoter (between -205 and +42) mediates this suppression.
- Curcumin's action is associated with the inhibition of the PI3K/Akt/NF-kappa B signaling pathway.
- Curcumin treatment reversed the multidrug resistance phenotype in L1210/Adr cells.
Conclusions:
- Curcumin suppresses P-glycoprotein expression, a key factor in multidrug resistance.
- The PI3K/Akt/NF-kappa B signaling pathway is implicated in curcumin's MDR-reversal effects.
- Curcumin shows potential as a therapeutic agent to overcome multidrug resistance in cancer treatment.
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