• The Korean Journal of Physiology
• /
• 제25권2호
• /
• pp.147-158
• /
• 1991

The effects of noradrenaline on the spontaneous contraction recorded from a strip of mucosa-free antral circular muscle were studied in the guinea-pig stomach, and the changes in slow waves and membrane resistance were analyzed in order to elucidate the mechanism for the excitatory response to noradrenaline. Electrical responses of circular muscle cells were recorded using glass microelectrodes filled with 3 M KCI. Electrotonic potentials were produced to estimate membrane resistance by the partition stimulating method. All experiments were performed in tris-buffered Tyrode solution which was aerated with 100% $O_2$ and kept at $35^{\circ}C$. The results obtained were as follows: 1) The spontaneous contractions were potentiated dose-dependently by the application of noradrenaline. 2) Through the experiments using adrenoceptor-blockers, the strong excitatory effect via $[\alpha}-adrenoceptors$ and the weak inhibitory efffect via ${\beta}-adrenoceptors$ were noted. 3) Noradrenaline produced hyperpolarization of membrane potential, and increases in the amplitude and the maximum rate of rise of slow waves. 4) In the presence of apamin, Ca-dependent K channel blocker, the characteristic hyperpolarization was not developed. However, the excitatory effect of noradrenaline on spontaneous contraction remained. 5) Membrane resistance was reduced during the hyperpolarized state by the application of noradrenaline, and the change of membrane resistance and the hyperpolarized state were completely abolished by apamin. From the above results, following conclusions could be made: Excitatory responses to noradrenaline result from the dominant ${\alpha}-excitatory$, and the weak ${\beta}-inhibitory$ action of noradrenaline. Hyperpolarization of membrane potential by noradrenaline is due to the activation of Ca-dependent K channel.

• The Korean Journal of Physiology and Pharmacology
• /
• 제2권1호
• /
• pp.95-100
• /
• 1998

The conductance change evoked by step depolarization was studied in primarily cultured rat adrenal chromaffin cells using patch-clamp and capacitance measurement techniques. When we applied a depolarizing pulse to a chromaffin cell, the inward calcium current was followed by an outward current and depolarization-induced exocytosis was accompanied by an increase in conductance trace. The slow inward tail current which has the same time course as the conductance change was observed in current recording. The activation of slow tail current was calcium-dependent. Reversal potentials agreed with Nernst equation assuming relative permeability of $Cs^+\;to\;K^+$ is 0.095. The outward current and tail current were blocked by apamin (200 nM) and d-tubocurarine (2 mM). The conductance change was blocked by apamin and did not affect membrane capacitance recording. We confirmed that conductance change after depolarization comes from the activation of the SK channel and can be blocked by application of the SK channel blockers. Consequently, it is necessary to consider blocking of the SK channel during membrane capacitance recording.

• Journal of Acupuncture Research
• /
• 제34권1호
• /
• pp.31-38
• /
• 2017

Objectives : The purpose of this study was to analyze the components of the clinically used bee venom (BV) pharmacopuncture. Methods : Two kinds of bee venom pharmacopuncture (BV-I and II), three kinds of separate purification BV (SPBV) pharmacopuncture (SPBV-I, II, and III), and apitoxin were investigated in this study. We performed a component analysis of melittin, apamin, and phospholipase $A_2$ using high-performance liquid chromatography (HPLC). Results :1. BV-I contained approximately 40% more melittin than BV-II did. 2. In the three separate purification BV pharmacopuncture, SPBV-I, SPBV-II, and SPBV-III, phospholipase $A_2$ content decreased remarkably. 3. The melittin content in SPBV-I increased by 5% compared to that in BV-I. 4. The amount of melittin in apitoxin was similar to that in SPBV-I. Conclusion : The compositions of the BV pharmacopuncture and separate purification BV pharmacopuncture changed depending on the collection method and concentration. Therefore, it is necessary to choose the most suitable BV for each specific medical treatment target. Furthermore, research into the composition of BV may be needed for its safe and effective use.

• 분석과학
• /
• 제27권6호
• /
• pp.277-283
• /
• 2014

한외여과법을 이용하여 봉독의 알러지 원인성분인 $PLA_2$를 제거하기 위하여 압력, 농도, 분자크기의 영향을 조사하였다. 봉독의 주요성분 분자량을 바탕으로 한외여과막의 투과크기를 선정하고 농도와 압력을 달리하였다. 그 결과, melittin과 apamin 함량은 유지되면서 $PLA_2$를 제거하는 최적조건(1 mg/mL, 20 psi, 10,000 dalton)을 찾았으며, 이를 HPLC와 SDS-PAGE로 확인하였다.

• 한국수정란이식학회지
• /
• 제21권1호
• /
• pp.35-43
• /
• 2006

이온 통로 및 이온 농도의 변화는 수정 현상을 포함한 다양한 세포 기능에 중요한 역할을 한다. 그러나 이러한 이온의 변화가 포유동물 배의 발달과정에 어떻게 관여하는지에 대해서는 알려진 바가 적다. 본 연구에서는 생쥐난자가 수정 이후 배 발달 과정을 거치는 동안 나타나는 칼슘과 포타슘 이온의 변화를 전기생리학적 실험 기법과 공초점 현미경을 이용하여 조사하였다. 수정 시에 나타나는 일시적인 세포내 칼슘 농도 변화는 활성 전류(수정 전류)와 함께 동반되었다. 그러나 수정과 같은 극적인 현상이나 자극이 없는 시기에는 세포내 칼슘 농도가 배 발달 시기와 상관없이 일정한 수준으로 유지되었다. 이것은 세포내외의 칼슘 농도의 보상현상으로도 설명할 수 있을 것이다. 배 발달이 진행됨에 따라 난관액의 포타슘 농도는 계속 증가하여 8세포기 배에서는 난자보다 26% 증가하였다. 상실배, 포배기에서는 포타슘 농도가 감소하였다. 배 발달이 진행됨에 따라 주로 포타슘 이온에 의해 조절되는 막 전압은 탈분극되고, 칼슘 이온의 세포 안으로의 유입은 점점 감소하였다. 생쥐 난자에 5 mM의 칼슘을 처리하였을 때 막 전압은 일시적인 과분극 현상을 보이다가 회복되었다. 칼슘 유입에 따른 막 전압 변화에 관여하는 포타슘 통로를 확인하기 위하여 포타슘 통로 차단제를 전 처리한 후 칼슘을 처리한 결과, 칼슘만을 단독으로 처리한 결과와 유의한 차이를 보이지 않았다. 막 전압의 과분극 현상은 잘 알려진 포타슘 통로 차단제인 TEA에 억제되지 않았다. 그리고 small conductance $Ca^{2+}$-activated 포타슘 통로 차단제 인 apamin에 의해서도 억제되지 않았다. 따라서 생쥐 난자에서 과분극을 유발시키는 포타슘 통로는 TEA와 apamin에 억제되지 않는 다른 포타슘 통로로 생각된다. 이상의 결과로부터 배 발달 동안 변화되는 칼슘과 포타슘 이온은 수정 및 초기 배 발달에 중요한 인자로써 작용할 것으로 생각되며, two-pore domain 포타슘 통로가 난자의 막 전압 조절에 관여할 가능성을 제시한다.

• Journal of Acupuncture Research
• /
• 제19권2호
• /
• pp.65-77
• /
• 2002

Objective : This study was undertaken to determine which compound of Bee Venom for herb-acupuncture has cytotoxicity on mouse mast cell line. Methods : We compared crude bee venom and its compounds such as melittin, mast cell degranulating peptide (MCD peptide), apamin with control groups on cytotoxicity by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results & Conclusion : 1. Crude bee venom showed significant cytotoxic effect(p<0.01) in 1 hour treatment with $1{\mu}g/m{\ell}$ in comparison with control group in 1 hour treatment with low concentration of $10-4{\mu}g/m{\ell}$, $10-3{\mu}g/m{\ell}$, $10-2{\mu}g/m{\ell}$, $10-1{\mu}g/m{\ell}$ and $1{\mu}g/m{\ell}$, but it showed no significant cytotoxic effect in 6 hours treatment. 2. Melittin group showed no significant cytotoxic effect in comparison with control group in 1 and 6 hours treatment with low concentration of $10-4{\mu}g/m{\ell}$, $10-3{\mu}g/m{\ell}$, $10-2{\mu}g/m{\ell}$, $10-1{\mu}g/m{\ell}$ and $1{\mu}g/m{\ell}$. 3. MCD peptide and Apamin group showed no significant cytotoxic effect in comparison with control group in 1 and 6 hours treatment with low concentration of $10-4{\mu}g/m{\ell}$ $10-3{\mu}g/m{\ell}$, $10-2{\mu}g/m{\ell}$, $10-1{\mu}g/m{\ell}$ and $1{\mu}g/m{\ell}$. 4. Crude bee venom showed significant cytotoxic effect(p<0.01) in 1 and 6 hours treatment in comparison with control group in 1 and 6 hours treatment with high concentration of $10{\mu}g/m{\ell}$, $20{\mu}g/m{\ell}$ and $102{\mu}g/m{\ell}$. 5. Melittin group showed significant cytotoxic effect(p<0.01) in 1 hour treatment in comparison with control group in 1 hour treatment with high concentration of $10{\mu}g/m{\ell}$ but it showed no significant cytotoxic effect in 6 hours treatment. 6. Crude bee venom and its compounds have more cytotoxic effect in 1 hour treatment than in 6 hours treatment. It means cytotoxicity tends to decrease according to the treatment time.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
• /
• pp.151.2-152
• /
• 2003

Bee venom (BV) has been utilized to relieve pain and to treat inflammatory diseases such as rheumatoid arthritis (RA). BV contains a variety of different peptides including melittin, apamin, adolapin and mast cell degranulating (MCD) peptide. In addition, it also contains enzyme (i.e. phospholipase A2), biologically active amines and non-peptide components. (omitted)

• The Korean Journal of Physiology and Pharmacology
• /
• 제11권5호
• /
• pp.215-219
• /
• 2007

Small and large conductance $Ca^{2+}$-activated $K^+(SK_{Ca}\;and\;BK_{Ca})$ channels are implicated in the modulation of neuronal excitability. We investigated how changes in peripheral $K_{Ca}$ channel activity affect mechanical sensitivity as well as the afferent fiber type responsible for $K_{Ca}$ channel-induced mechanical sensitivity. Blockade of $SK_{Ca}$ and $BK_{Ca}$ channels induced a sustained decrease of mechanical threshold which was significantly attenuated by topical application of capsaicin onto afferent fiber and intraplantar injection of 1-ethyl-2-benzimidazolinone. NS1619 selectively attenuated the decrease of mechanical threshold induced by charybdotoxin, but not by apamin. Spontaneous flinching and paw thickness were not significantly different after $K_{Ca}$ channel blockade. These results suggest that mechanical sensitivity can be modulated by $K_{Ca}$ channels on capsaicin-sensitive afferent fibers.

• 한국독성학회:학술대회논문집
• /
• 한국독성학회 2003년도 추계학술대회
• /
• pp.117-117
• /
• 2003

Bee Venom (BV) has been treated in inflammatory diseases such as rheumatoid arthritis (RA). Bee venom contains several biologically active non-peptide substances as well as two major known peptides; the hemolytic peptide melittin (50%) and the neurotoxic peptide apamin, and a number of minor peptides.(omitted)

• 대한약학회:학술대회논문집
• /
• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
• /
• pp.93.1-93.1
• /
• 2003

Bee Venom (BV) has been treated in inflammatory diseases such as rheumatoid arthritis (RA). Bee venom contains several biologically active non-peptide substances as well as two major known peptides; the hemolytic peptide melittin (50%) and the neurotoxic peptide apamin, and a number of minor peptides. Previous our study showed that BV blocked LPS and SNP-induced production of NO and PG through inactivation of NF-kB which regulates expression of COX-2 and iNOS. (omitted)