Effects of Dangkwisoo-San, Ginger and Curcumin on Transient Receptor Potential Melastatin 7 Channels
Objectives: Metabolic syndrome is correlated with increased cardiovascular risk and characterized by several factors, including visceral obesity, hypertension, insulin resistance, and dyslipidemia. Several members of a large family of nonselective cation entry channels, e.g., transient receptor potential (TRP) melastatin 7 (TRPM7) channels have been associated with the development of cardiovascular diseases. The purpose of this study was to investigate the effects of Dangkwisoo-san, ginger and curcumin on TRPM7 channel.
Methods: Human embryonic kidney (HEK) 293 cells stably transfected with the TRPM7 expression vectors were maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum (FBS), 1% penicillin/streptomycin, 5 µg/mL blasticidin, and 0.4 mg/mL zeocin in a humidified 20% O2/10% CO2 atmosphere at 37℃. Whole-cell patch clamp recordings were obtained using an Axopatch 700B amplifier and pClamp v.10.4 software, and signals were digitalized at 5 kHz using Digidata 1422A.
Results: Dangkwisoo-san extract (100, 200, 300, 400, and 500 µg/mL) inhibited the outward and inward TRPM7 whole-cell currents at dose dependent manner and the half maximal inhibitory concentration (IC)50 of Dangkwisoo-san was 218.3 µg/mL. Also, ginger extract (100, 200, 300, 400, and 500 µg/mL) inhibited the outward and inward of TRPM7 whole-cell currents in a dose dependent manner and the IC50 of ginger was 877.2 µg/mL. However, curcumin had no effects on TRPM7 whole-cell currents.
Conclusions: These results suggest that both Dangkwisoo-san and ginger have good roles to inhibit the TRPM7 channel, suggesting that Dangkwisoo-san and ginger are considered one of the candidate agents for the treatment of metabolic syndrome such as cardiovascular disease.