The influence of 8-prenylnaringenin on the activity of voltage-gated kv1.3 potassium channels in human jurkat t cells

Gąsiorowska, Justyna; Teisseyre, Andrzej; Uryga, Anna; Michalak, Krystyna

doi:10.2478/s11658-012-0029-0

Cited by 10 publications

(17 citation statements)

References 27 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…It was concluded that the antiproliferative effect of these compounds could be, at least partially, related to the inhibition of Kv1.3 channels (Teisseyre and Michalak 2005 , 2006 ; Teisseyre et al 2009 ). Our previous studies also showed that a plant-derived prenylated flavonoid 8-prenylnaringenin—in contrast to its precursor—naringenin was an effective inhibitor of Kv1.3 channels both in normal human TL and in a human cancer T cell line—Jurkat (Gąsiorowska et al 2012 ). The estimated value of a half-blocking concentration (EC 50 ) was about 2.5 μM.…”

Section: Introductionmentioning

confidence: 90%

Inhibition of Kv1.3 Channels in Human Jurkat T Cells by Xanthohumol and Isoxanthohumol

et al. 2015

Self Cite

View full text Add to dashboard Cite

Using whole-cell patch-clamp technique, we investigated influence of selected compounds from groups of prenylated chalcones and flavonoids: xanthohumol and isoxanthohumol on the activity of Kv1.3 channels in human leukemic Jurkat T cells. Obtained results provide evidence that both examined compounds were inhibitors of Kv1.3 channels in these cells. The inhibitory effects occurred in a concentration-dependent manner. The estimated value of the half-blocking concentration (EC50) was about 3 μM for xanthohumol and about 7.8 μM for isoxanthohumol. The inhibition of Kv1.3 channels by examined compounds was not complete. Upon an application of the compounds at the maximal concentrations equal to 30 μM, the activity of Kv1.3 channels was inhibited to about 0.13 of the control value. The inhibitory effect was reversible. The application of xanthohumol and isoxanthohumol did not change the currents’ activation and inactivation rate. These results may confirm our earlier hypothesis that the presence of a prenyl group in a molecule is a factor that facilitates the inhibition of Kv1.3 channels by compounds from the groups of flavonoids and chalcones. The inhibition of Kv1.3 channels might be involved in antiproliferative and proapoptotic effects of the compounds observed in cancer cell lines expressing these channels.

show abstract

Section: Introductionmentioning

confidence: 90%

Inhibition of Kv1.3 Channels in Human Jurkat T Cells by Xanthohumol and Isoxanthohumol

et al. 2015

Self Cite

View full text Add to dashboard Cite

show abstract

“…In contrast to what was observed earlier in the case of genistein and resveratrol, the inhibitory effect of 8-prenylnaringenin was complete. A complete inhibition of Kv1.3 channels occurred at concentrations higher than 10 mM [39]. The inhibitory effect of 8-prenylnaringenin was reversible.…”

Section: Polycyclic Compounds As Inhibitors Of Kv13 Channelsmentioning

confidence: 89%

“…Other studies showed that 8-prenylnaringenin could also inhibit cell proliferation and induce apoptosis in the breast cancer cell line MCF-7 [40]. The results of electrophysiological studies indicate that 8-prenylnaringenin inhibits Kv1.3 channels in a concentration-dependent manner [39]. The estimated EC 50 value is about 3 μM.…”

Section: Polycyclic Compounds As Inhibitors Of Kv13 Channelsmentioning

confidence: 93%

“…Studies performed recently provide evidence that a prenyl-derivative of naringenin --8-prenylnaringenin -inhibits Kv1.3 channels both in normal human T lymphocytes and in human T cell line Jurkat when applied at low micromolar concentrations [39]. This compound is a natural derivative of naringenin that is isolated from common hops (Humulus lupulus).…”

Section: Polycyclic Compounds As Inhibitors Of Kv13 Channelsmentioning

confidence: 99%

“…8-prenylnaringenin is the most potent inhibitor of the Kv1.3 channels of the naringenin derivatives tested to date. The potency of the inhibition may be due to the presence of a prenyl group in the molecule of this flavonoid [39].…”

Section: Polycyclic Compounds As Inhibitors Of Kv13 Channelsmentioning

confidence: 99%

See 2 more Smart Citations

Voltage-Gated Ptassium Channels Kv1.3 - Potentially New Molecular Target in Cancer Diagnostics and Therapy

Teisseyre¹,

Gąsiorowska²,

Michalak³

2015

Adv Clin Exp Med

Self Cite

View full text Add to dashboard Cite

Voltage-gated potassium channels, Kv1.3, which were discovered in 1984, are integral membrane proteins which are activated ("open") upon change of the cell membrane potential, enabling a passive flux of potassium ions across the cell membrane. The channels are expressed in many different tissues, both normal and cancer. Since 2005 it has been known that the channels are expressed not only in the plasma membrane, but also in the inner mitochondrial membrane. The activity of Kv1.3 channels plays an important role, among others, in setting the cell resting membrane potential, cell proliferation, apoptosis and volume regulation. For some years, these channels have been considered a potentially new molecular target in both the diagnostics and therapy of some cancer diseases. This review article focuses on: 1) changes of expression of the channels in cancer disorders with special regard to correlations between the channels' expression and stage of the disease, 2) influence of inhibitors of Kv1.3 channels on proliferation and apoptosis of cancer cells, 3) possible future applications of Kv1.3 channels' inhibitors in therapy of some cancer diseases. In the last section, the results of studies performed in our Laboratory of Bioelectricity on the influence of selected biologically active plant-derived compounds from the groups of flavonoids and stilbenes and their natural and synthetic derivatives on the activity of Kv1.3 channels in normal and cancer cells are reviewed. A possible application of some compounds from these groups to support therapy of cancer diseases, such as breast, colon and lymph node cancer, and melanoma or chronic lymphocytic leukemia (B-CLL), is announced (Adv Clin Exp Med 2015, 24, 3, 517-524).

show abstract

The Influence of 6-Prenylnaringenin and Selected Non-prenylated Flavonoids on the Activity of Kv1.3 Channels in Human Jurkat T Cells

et al. 2018

View full text Add to dashboard Cite

The influence of a prenylated flavonoid-6-prenylnaringenin (6-PR) and selected non-prenylated flavonoids: acacetin, chrysin, baicalein, wogonin, and luteolin on the activity of voltage-gated potassium channels Kv1.3 was investigated in human leukemic Jurkat T cells. Electrophysiological measurements were accompanied by studies on the cytotoxic effect of the examined compounds on Jurkat T cells. Electrophysiological studies were performed using the whole-cell patch-clamp technique. Cell viability was determined using the MTT assay. 6-PR inhibited Kv1.3 channels in Jurkat T cells in a concentration-dependent manner. The estimated value of the half-blocking concentration (EC) was about 5.76 µM. Among non-prenylated flavonoids, acacetin and chrysin inhibited Kv1.3 channels in Jurkat T cells when applied at the concentration of 30 µM, whereas baicalein, wogonin, and luteolin were ineffective at this concentration. The inhibitory effects of acacetin and chrysin on Kv1.3 channels were significantly less potent than the inhibition caused by 6-PR. All tested compounds inhibited growth of Jurkat T cells in a concentration-dependent manner. Wogonin and chrysin were the most cytotoxic flavonoids tested, whereas baicalein and 6-PR were the least cytotoxic compounds. In accordance to our hypothesis the prenylated flavonoid (6-PR) was much more effective inhibitor of Kv1.3 channels than non-prenylated compounds selected for this study. The inhibition of Kv1.3 channels by 6-PR, acacetin, and chrysin was not related to cytotoxicity of these compounds. The channels' inhibition might be involved in anti-proliferative and pro-apoptotic effects of 6-PR, acacetin and chrysin observed in cancer cell lines expressing these channels.

show abstract

The influence of 8-prenylnaringenin on the activity of voltage-gated kv1.3 potassium channels in human jurkat t cells

Cited by 10 publications

References 27 publications

Inhibition of Kv1.3 Channels in Human Jurkat T Cells by Xanthohumol and Isoxanthohumol

Inhibition of Kv1.3 Channels in Human Jurkat T Cells by Xanthohumol and Isoxanthohumol

Voltage-Gated Ptassium Channels Kv1.3 - Potentially New Molecular Target in Cancer Diagnostics and Therapy

The Influence of 6-Prenylnaringenin and Selected Non-prenylated Flavonoids on the Activity of Kv1.3 Channels in Human Jurkat T Cells

Contact Info

Product

Resources

About