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The Effects of Eupatilin (Stillen$^{(R)}$) on Motility of Human Lower Gastrointestinal Tracts

  • Ryoo, Seung-Bum;Oh, Heung-Kwon;Yu, Sung A;Moon, Sang Hui;Choe, Eun Kyung;Oh, Tae Young;Park, Kyu Joo
    • The Korean Journal of Physiology and Pharmacology
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    • v.18 no.5
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    • pp.383-390
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    • 2014
  • Gastrointestinal motility consists of phasic slow-wave contractions and the migrating motor complex (MMC). Eupatilin (Stillen$^{(R)}$) has been widely used to treat gastritis and peptic ulcers, and various cytokines and neuropeptides are thought to be involved, which can affect gastrointestinal motility. We performed a study to identify the effects of eupatilin on lower gastrointestinal motility with electromechanical recordings of smooth muscles in the human ileum and colon. Ileum and colon samples were obtained from patients undergoing bowel resection. The tissues were immediately stored in oxygenated Krebs-Ringer's bicarbonate solution, and conventional microelectrode recordings from muscle cells and tension recordings from muscle strips and ileal or colonic segments were performed. Eupatilin was perfused into the tissue chamber, and changes in membrane potentials and contractions were measured. Hyperpolarization of resting membrane potential (RMP) was observed after administration of eupatilin. The amplitude, AUC, and frequency of tension recordings from circular and longitudinal smooth muscle strips and bowel segments of the ileum and colon were significantly decreased after admission of eupatilin. Eupatilin elicited dose-dependent decreases during segmental tension recordings. In conclusion, eupatilin (Stillen$^{(R)}$) showed inhibitory effects on the human ileum and colon. We propose that this drug may be useful for treating diseases that increase bowel motility, but further studies are necessary.

Effect of Dopamine on the $Ca^{2+}\;-dependent\;K^+\;currents$ in Isolated Single Gastric Myocytes of the Guinea-pig

  • Rhee, Poong-Lyul;Lee, Sang-Jin;Kim, Sung-Joon;So, In-Suk;Hwang, Sang-Ik;Kim, Ki-Whan
    • The Korean Journal of Physiology
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    • v.27 no.2
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    • pp.139-150
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    • 1993
  • We have reported that dopamine potentiates spontaneous contractions dose-dependently in guinea-pig antral circular muscle strips (Hwang et al, 1991). To clarify the underlying excitatory mechanism of dopamine on the gastric smooth muscle, the effects of dopamine on voltage-dependent $Ca^{2+}\;currents\;and\;Ca^{2+}\;-dependent\;K^+\;currents$ were observed in enzymatically dispersed guinea-pig gastric myocytes using the whole-cell voltage-clamp technique. Experiments were also done using isometric tension recording and conventional intracellular microelectrode techniques. 1) The effect of dopamine on the spontaneous contraction of antral circular muscle strips of the guinea-pig was excitatory in a dose-dependent manner, and was blocked by phentolamine, an ${\alpha}-adrenoceptor$ blocker. 2) The slow waves were not changed by dopamine. 3) The voltage-operated inward $Ca^{2+}$ current was not influenced by dopamine. 4) The $Ca^{2+}\;-dependent\;K^+$ outward current, which might reflect the changes of intracellular calcium concentration, was enhanced by dopamine. This effect was abolished by phentolamine. 5) The enhancing effect of dopamine on the $Ca^{2+}\;-dependent\;K^+$ current disappeared with heparin which is known to block the action of $InsP_3$. From these results, it is suggested that dopamine acts via $InsP_3-mediated\;Ca^{2+}$ mobilization from intracellular stores and such action potentiates the spontaneous contraction of guinea-pig gastric smooth muscle.

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Role of $Na^+\;-K^+$ Pump on Endothelium-dependent Relaxation

  • Sung, Sang-Hyun;Roh, Joon-Ryang;Park, Tae-Sic;Suh, Suk-Hyo;Hwang, Sang-Ik;Kim, Ki-Whan
    • The Korean Journal of Physiology
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    • v.27 no.2
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    • pp.199-207
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    • 1993
  • To study the underlying mechanism through which the endothelium-dependent relaxation is inhibited by blocking the $Na^+\;-K^+$ pump, the effects of $Na^+\;-K^+$ pump blockade on the release of EDRF and its relaxing activity were examined, using organ bath study, bioassay technique, and cGMP measurement. Endothelium-dependent relaxation was attenuated by blocking the $Na^+\;-K^+$ pump in the vascular ring with intact endothelium. In bioassay experiment EDRF release was decreased with the blockade of the $Na^+\;-K^+$ pump in the EDRF donor strip. Endothelium-dependent increase of cGMP level was suppressed by inhibiting the $Na^+\;-K^+$ pump in the test strips. The magnitude of relaxation of test strip which was induced by the perfusate that had passed through the EDRF donor strip was decreased with the blockade of the $Na^+\;-K^+$ pump in the test strip. Therefore, it could be suggested that the attenuation of endothelium-dependent relaxation caused by inhibiting $Na^+\;-K^+$ pump activity is due to both the decreased release of EDRF from endothelial cells and the decreased sensitivity of the smooth muscle cells to EDRF.

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