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Lee, Sojung,Chae, Mee Ree,Lee, Byoung-Cheol,Kim, Yong-Chul,Choi, Jae Sue,Lee, Sung Won,Cheong, Jae Hoon,Park, Chul-Seung American Society for Pharmacology and Experimental 2016 Molecular pharmacology Vol.90 No.2
<P>The large-conductance calcium-activated potassium channel (BKCa channel) plays critical roles in smooth muscle relaxation. In urinary bladder smooth muscle, BKCa channel activity underlies the maintenance of the resting membrane potential and repolarization of the spontaneous action potential triggering the phasic contraction. To identify novel BKCa channel activators, we screened a library of natural compounds using a cell-based fluorescence assay and a hyperactive mutant BKCa channel (Lee et al., 2013). From 794 natural compounds, kurarinone, a flavanone from Sophora flavescens, strongly potentiated BKCa channels. When treated from the extracellular side, this compound progressively shifted the conductance-voltage relationship of BKCa channels to more negative voltages and increased the maximum conductance in a dose-dependent manner. Whereas kurarinone strongly potentiated the homomeric BKCa channel composed of only the a subunit, its effects were much smaller on heteromeric channels coassembled with auxiliary beta subunits. Although the activation kinetics was not altered significantly, the deactivation of BKCa channels was dramatically slowed by kurarinone treatment. At the single-channel level, kurarinone increased the open probability of the BKCa channel without affecting its single-channel conductance. Kurarinone potently relaxed acetylcholine-induced contraction of rat bladder smooth muscle and thus decreased the micturition frequency of rats with overactive bladder symptoms. These results indicate that kurarinone can directly potentiate BKCa channels and demonstrate the therapeutic potentials of kurarinone and its derivatives for developing antioveractive bladder medications and supplements.</P>
Gene transfer of the K<sub>ATP</sub> channel restores age-related erectile dysfunction in rats
So, Insuk,Chae, Mee Ree,Lee, Sung Won BLACKWELL SCIENCE 2007 BJU INTERNATIONAL Vol.100 No.5
<P>OBJECTIVE</P><P>To determine if gene transfer of the ATP-sensitive potassium (K<SUB>ATP</SUB>) channel can reverse age-related erectile dysfunction in the rat, as the K<SUB>ATP</SUB> channel is an important subtype of potassium channels regulating smooth muscle tone.</P><P>MATERIALS AND METHODS</P><P>In an <I>in vitro</I> study, gene were transferred using cDNA of the K<SUB>ATP</SUB> channel in cultured human corporal smooth muscle (CSM) cells and human embryonic kidney (HEK) cells. After gene transfer, the activities of transferred channels were assessed by the patch-clamp technique. In an <I>in vivo</I> study, 15 old rats were used for groups of gene therapy and nine young adult rats were used as normal controls. The old rats were divided into three groups, i.e. controls and two gene-transfer groups (Kir6.1 + SUR2B and Kir6.2 + SUR2B). The intracavernosal pressure (ICP) response to cavernosal nerve stimulation was assessed after intracorporal injection with naked cDNA of the K<SUB>ATP</SUB> channel. The transgene expression of the K<SUB>ATP</SUB> channel was examined by reverse transcription-polymerase chain reaction (RT-PCR) in rats transfected with cDNA of Kir 6.1 and 6.2.</P><P>RESULTS</P><P>The transferred gene of the K<SUB>ATP</SUB> channel was functionally active and appropriate for gene transfer. The mean (<SMALL>SEM</SMALL>) ratio of ICP to systemic blood pressure in the gene-transfer groups, at 79.4 (1)% and 76.5 (2.6)% (both eight rats) was significantly higher than that in age-matched control rats, at 59.4 (3.3)% (eight), and similar to that in the young control rats, at 77.1 (2.7)% (nine). The RT-PCR showed expression of Kir6.1 and 6.2 genes in the transfected groups.</P><P>CONCLUSION</P><P><I>In vivo</I> gene transfer of the K<SUB>ATP</SUB> channel can physiologically restore erectile function in aged rats, and might be applicable to the development of new forms of therapy for treating human erectile dysfunction.</P>
Effect of Testosterone on Potassium Channel Opening in Human Corporal Smooth Muscle Cells
Han, Deok Hyun,Chae, Mee Ree,Jung, Jae Hun,So, Insuk,Park, Jong Kwan,Lee, Sung Won Elsevier 2008 The journal of sexual medicine Vol.5 No.4
<P>INTRODUCTION: In humans, the role of testosterone in sexual functions, including sexual desire, nocturnal penile erections, and ejaculatory volume, has been relatively well established. However, the effects of testosterone on intrapenile structure in humans remains controversial. AIM: We assessed the direct effects of testosterone on potassium channels in human corporal smooth muscle cells, in an effort to understand the mechanisms inherent to the testosterone-induced relaxation of corporal smooth muscle cells at the cellular and molecular levels. Methods. We conducted electrophysiologic studies using cultured human corporal smooth muscle cells. We evaluated the effects of testosterone on potassium channels-BK(Ca) and K(ATP) channels-by determining the whole-cell currents and single-channel activities. For the electrophysiologic recordings, whole-cell and cell-attached configuration patch-clamp techniques were utilized. MAIN OUTCOME MEASURES: Changes in whole-cell currents and channel activities of BK(Ca) and K(ATP) channels by testosterone. Results. Testosterone (200 nM) significantly increased the single-channel activity of calcium-activated potassium (BK(Ca)) channels and whole-cell K(+) currents by 443.4 +/- 83.4% (at +60 mV; N = 11, P < 0.05), and this effect was abolished by tetraethylammonium (TEA) (1 mM), a BK(Ca) channel blocker. The whole-cell inward K(+) currents of the K(ATP) channels were also increased by 226.5 +/- 49.3% (at -100 mV; N = 7, P < 0.05). In the presence of a combination of vardenafil (10 nM) and testosterone (200 nM), the BK(Ca) channel was activated to a significantly higher degree than was induced by testosterone alone. CONCLUSIONS: The results of patch-clamp studies provided direct molecular evidence that testosterone stimulates the activity of BK(Ca) channels and K(ATP) channels. An understanding of the signaling mechanisms that couple testosterone receptor activation to potassium channel stimulation will provide us with an insight into the cellular processes underlying the vasorelaxant effects of testosterone.</P>
Lee, Jun Ho,Chae, Mee Ree,Sung, Hyun Hwan,Ko, Mikyeong,Kang, Su Jeong,Lee, Sung Won Blackwell Pub 2013 The journal of sexual medicine Vol.10 No.7
<P>Rubus coreanus is a perennial shrub native to the southern part of the Korean peninsula. Although it is known that R. coreanus has a dose-dependent relaxation effect on rabbit corpus cavernosum (CC), the exact mechanism of action by which R. coreanus work is not fully known.</P>
Gene transfer of TRPC6 (dominant negative) restores erectile function in diabetic rats.
Jung, Jae Hun,Kim, Byung Joo,Chae, Mee Ree,Kam, Sung Chul,Jeon, Ju-Hong,So, Insuk,Chung, Ky Hyun,Lee, Sung Won Blackwell Pub 2010 JOURNAL OF SEXUAL MEDICINE Vol.7 No.3
<P>Transient receptor potential (TRP) channels play an important role in modulating intracellular Ca(2+) ([Ca(2+)](i)) levels.</P>
Tharaka Darshana Wijerathne,Ji Hyun Kim,Min Ji Kim,Chul Young Kim,Mee Ree Chae,Sung Won Lee,Kyu Pil Lee 대한약리학회 2019 The Korean Journal of Physiology & Pharmacology Vol.23 No.5
Sperm function and male fertility are closely related to pH dependent K+ current (KSper) in human sperm, which is most likely composed of Slo3 and its auxiliary subunit leucine-rich repeat-containing protein 52 (LRRC52). Onion peel extract (OPE) and its major active ingredient quercetin are widely used as fertility enhancers; however, the effect of OPE and quercetin on Slo3 has not been elucidated. The purpose of this study is to investigate the effect of quercetin on human Slo3 channels. Human Slo3 and LRRC52 were co-transfected into HEK293 cells and pharmacological properties were studied with the whole cell patch clamp technique. We successfully expressed and measured pH sensitive and calcium insensitive Slo3 currents in HEK293 cells. We found that OPE and its key ingredient quercetin inhibit Slo3 currents. Inhibition by quercetin is dose dependent and this degree of inhibition decreases with elevating internal alkalization and internal free calcium concentrations. Functional moieties in the quercetin polyphenolic ring govern the degree of inhibition of Slo3 by quercetin, and the composition of such functional moieties are sensitive to the pH of the medium. These results suggest that quercetin inhibits Slo3 in a pH and calcium dependent manner. Therefore, we surmise that quercetin induced depolarization in spermatozoa may enhance the voltage gated proton channel (Hv1), and activate non-selective cation channels of sperm (CatSper) dependent calcium influx to trigger sperm capacitation and acrosome reaction.
Effect of the novel BKCa channel opener LDD175 on the modulation of corporal smooth muscle tone.
Sung, Hyun Hwan,Choo, Seol Ho,Han, Deok Hyun,Chae, Mee Ree,Kang, Su Jeong,Park, Chul-Seung,So, Insuk,Park, Jong Kwan,Lee, Sung Won BLACKWELL PUBLISHING LTD 2015 JOURNAL OF SEXUAL MEDICINE Vol.12 No.1
<P>The BKCa channel has been reported to play an important role in erectile function. Recently, novel BKCa channel activator, LDD175, was introduced.</P>
Wijerathne, Tharaka Darshana,Kim, Ji Hyun,Kim, Min Ji,Kim, Chul Young,Chae, Mee Ree,Lee, Sung Won,Lee, Kyu Pil The Korean Society of Pharmacology 2019 The Korean Journal of Physiology & Pharmacology Vol.23 No.5
Sperm function and male fertility are closely related to pH dependent $K^+$ current (KSper) in human sperm, which is most likely composed of Slo3 and its auxiliary subunit leucine-rich repeat-containing protein 52 (LRRC52). Onion peel extract (OPE) and its major active ingredient quercetin are widely used as fertility enhancers; however, the effect of OPE and quercetin on Slo3 has not been elucidated. The purpose of this study is to investigate the effect of quercetin on human Slo3 channels. Human Slo3 and LRRC52 were co-transfected into HEK293 cells and pharmacological properties were studied with the whole cell patch clamp technique. We successfully expressed and measured pH sensitive and calcium insensitive Slo3 currents in HEK293 cells. We found that OPE and its key ingredient quercetin inhibit Slo3 currents. Inhibition by quercetin is dose dependent and this degree of inhibition decreases with elevating internal alkalization and internal free calcium concentrations. Functional moieties in the quercetin polyphenolic ring govern the degree of inhibition of Slo3 by quercetin, and the composition of such functional moieties are sensitive to the pH of the medium. These results suggest that quercetin inhibits Slo3 in a pH and calcium dependent manner. Therefore, we surmise that quercetin induced depolarization in spermatozoa may enhance the voltage gated proton channel (Hv1), and activate non-selective cation channels of sperm (CatSper) dependent calcium influx to trigger sperm capacitation and acrosome reaction.