Key result
Lindera erythrocarpa extract reduces HERG channel maximum conductance by ~60%.
Why the study?
The effects of Lindera erythrocarpa on the HERG channel, important in cancer progression and cardiac action potential duration, were not well characterized.
p-value: p=<0.05
Lindera erythrocarpa extracts demonstrate voltage-dependent blockade of HERG channels, suggesting a mechanism for potential cardiac arrhythmogenic side effects.
May confer proarrhythmic risk via HERG inhibition; leaves open clinical translation and safety in humans.
Lindera erythrocarpa Makino (Lauraceae) is used as a traditional medicine for analgesic, antidote, and antibacterial purposes and shows anti-tumor activity. We studied the effects of Lindera erythrocarpa on the human ether-a-go-go-related gene (HERG) channel, which appears of importance in favoring cancer progression in vivo and determining cardiac action potential duration. Application of MeOH extract of Lindera erythrocarpa showed a dose-dependent decrease in the amplitudes of the outward currents measured at the end of the pulse (I(HERG)) and the tail currents of HERG (I(tail)). When the BuOH fraction and H(2)O fraction of Lindera erythrocarpa were added to the perfusate, both I(HERG) and I(tail) were suppressed, while the hexane fraction, CHCl(3) fraction, and EtOAc fraction did not inhibit either I(HERG) or I(tail). The potential required for half-maximal activation caused by EtOAc fraction, BuOH fraction, and H(2)O fraction shifted significantly. The BuOH fraction and H(2)O fraction (100 microg/mL) decreased g(max) by 59.6% and 52.9%, respectively. The H(2)O fraction- and BuOH fraction-induced blockades of I(tail) progressively decreased with increasing depolarization, showing the voltage-dependent block. Our findings suggest that Lindera erythrocarpa, a traditional medicine, blocks HERG channel, which could contribute to its anticancer and cardiac arrhythmogenic effect.
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Hong et al. (2009) studied HERG channel function (in vitro). Lindera erythrocarpa extract vs. Control (normal Ringer's solution) was evaluated on HERG channel maximum conductance (gmax) and half-maximal activation potential (V1/2) (p=<0.05). Lindera erythrocarpa extracts, specifically the BuOH and H2O fractions at 100 μg/mL, significantly decreased the maximum conductance of HERG channels by 59.6% and 52.9%, respectively.
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