• 한국어병학회지
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• 제14권1호
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• pp.31-36
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• 2001

해수에 적응된 뱀장어, Anguilla japonica의 장 세포막으로부터 새로운 clonidine의 결합부위가 있음이 밝혀졌다. Clonidine의 특이적인 결합부위는 적어도 2개의 부위 (high affinity $K_d=1.4{\pm}0.3$ nMn= 5, low affinity $K_d=175{\pm}34$ nM)를 가지고 있었다. 2nM [$^3H$]clonidine의 특이적인 결합은 $20^{\circ}C$, pH 7.5에서 최적 결합능을 가지고 있었고, 라벨되지 않은 clonidine에 의해 가역적인 반응을 보였다. 이러한 결합은 adrenaline, yohimbine과 rauwolscine에 의한 저해능은 약하였다. 그리고 대부분의 결합부위는 $\alpha_2$-adrenoceptor와는 상이하였다. Clonidine의 특이적인 결합은 다양한 imidazoline/guanidinium약물에 의해 억제되었다. Competition 실험의 결과, 2nM[$^3H$]clonidine의 치환 rank order는 다음과 같다. guanabenz > cirazoline = naphazoline=UK14,304= ST587 $\geq$ clonidine $\geq$ idazoxan = RX821002 = tolazoline > ST93 = oxymetazoline = amiloride = ST91 > yohimbine = efaroxan = rauwolscine $\geq$ adrenaline = ST567 = histamine = agmatine. 이러한 순서는 포유류에 분류된 imidazoline receptorl($I_1$), imidazoline receptor 2($I_2$) 및 imidazoline/guanidinium receptive sites(IGRS)형태와는 틀리기 때문에 새로운 imidazoline receptor라고 생각된다. 지금까지 보고된 포유류의 세포와 조직에서 IGRS의 생리학적인 역할은 명확하지 않지만, 해수뱀장어 장은 IGRS의 세포에 있어서의 역할 그리고 IGRS의 내인성(內因性) ligand가 무엇인가에 대한 좋은 모델이 될 수 있다고 생각되어진다.

• Applied Microscopy
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• 제28권2호
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• pp.215-224
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• 1998

흰쥐 부신수질의 발생에 따른 미세구조적 변화를 관찰하기 위하여 임신 20일령, 출생직후, 출생후 7일, 15일 및 30일에 각각 조직을 채취하여 전자현미경적으로 관찰한 바, 흰쥐 부신 수질에서는 과립내용물의 전자밀도가 중등도 또는 낮고, 한계막에 싸여 있으며, 한계막과 과립 내용물간에 비교적 넓은 halo를 형성하거나 얇은 core를 형성하는 원형 내지 타원형의 소위 adrenaline 과립 $(123\sim200nm)$과 과립 내용물의 전자밀도가 adrenaline 과립보다 높고 한계막과 과립내용물간에 대체로 넓은 halo를 형성하는 부정형의 소위 noradrenaline 과립 (장경 $177\sim299nm$, 단경 $124\sim194nm$) 등 두 가지 형태의 과립이 관찰되었다. 이들 두 종류의 과립은 임신 후기 및 출생직후에서는 두종의 과립이 한 세포내에서 흔재하고 있었으나, 출생후 7일령에서부터 명확한 두종의 세포를 구별할 수 있었으며 과립의 크기와 수는 일령에 따라 다소 차이를 나타내었고, 핵내에서는 치밀체가 출현하였다.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1990년도 Proceedings of International Symposium on Korean Ginseng, 1990, Seoul, Korea
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• pp.196-200
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• 1990

the ginseng polypeptide (GPP) isolated from the root of Panax ginseng C.A. Meyer was demonstrated to decrease the levels of blood sugar and hepatic glycogen when injected intravenously to rats at a doses of 50-200mg/kg without affecting blood total lipid. When mice were injected subcutaneously daily at a dose of 50 and 100mg/kg for 7 successive days, GPP was also found to decreased blood sugar and hepatic glycoge. In addition, GPP was found to decrease various experimenta hyperglycemias induced by injection of adrenaline, glucose and alloxan. GPP exhibited inhibiting effect on the glycogen enhancement induced by glucose, but strengthening effect on the glycogen decrease induced by adrenaline. When the levels of blood total lipid and liver glycogen were increased by alloxan, GPP was shown to inhibit these changes except its lowering blood sugar. the toxicity of GPP is very low, its LD50 was found to be 1.62$\pm$0.130 g/kg for iv.

• Journal of Ginseng Research
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• 제14권2호
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• pp.338-342
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• 1990

The ginseng Polypeptide (GPP) Isolated from the root of Panax ginseng C.A. Meyer was domonstrated to decrease the levels of blood sugar and hepatic glycogen when injected intravenoilsly to rats at a doses of 50-200 mg/kg without affecting blood total lipid. When mice were injected slibclitaneollsly daily at a dose of 50 and 100 mg/kg for 7 successive days. GPP was also found to decrease blood sligar and hepatic glycogen. In addition, GPP was found to decrease variolls experimental hypergly cemias induced by injection of adrenaline, glilcose and alloxan. GPP exhibited inhibiting effect on the glut rogen enhancement indllced by glucose, but strenthening effect on the glycogen decrease indliced by adrenaline. When the levels of blood total lipid and lilrer glycogen were increased by T alloxan. GPP was shown to inhibit these changes except its lowering blood sugar. The toxicity of GPP is very low, LD50 was found to be 1.62 $\pm$ 0.130 g/kg for iv.

• Bulletin of the Korean Chemical Society
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• 제32권2호
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• pp.455-458
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• 2011

In previous report, with the aid of receptor-oriented pharmacophore-based in silico screening, we characterized three novel hPNMT inhibitors (YPN010, YPN016, and YPN017) and proposed that the hydrogen bonding interaction between inhibitors and side chain of Lys57 is very important to inhibitory activity of hPNMT. To confirm the importance of Lys57, mutant with substitution of Lys57 with Ala was cloned and binding study was performed for a K57A mutant of hPNMT using STD-NMR and fluorescence experiments. The binding constants for three novel inhibitors with mutant hPNMT were dramatically decreased compared to those with wild-type protein. K57A mutant-induced conversion of noradrenaline to adrenaline was suppressed about 95 % compared to wild-type hPNMT. Mutagenic analysis using a K57A mutant confirmed the importance of the Lys57 residue in binding of the inhibitor candidate to hPNMT as well as enzymatic activity of hPNMT, implying that these results are consistent with our binding model.

• 대한약리학회지
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• 제24권1호
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• pp.63-70
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• 1988

문맥 고혈압 동물에서 내장장기의 혈류역동학적 변동으로서 문맥압의 증가와 동반하여 장간의 혈류량 증가와 혈관저항의 감소뿐만 아니라 전신 혈관저항의 감소가 특징적으로 야기된다. 문맥고혈압에 있어서 propranolol이 beta 1과 beta 2 수용체의 봉쇄작용으로 문맥고혈압을 저하시킨다는 점에서 사용되기도 한다. 본 실험에서는 흰쥐에서 문맥을 부분적으로 결찰하여 문맥고혈압을 야기하고 10일 후에 내장장기의 혈류역동학적 변동과 혈관 수축성 약물에 대한 반응성의 변동을 관찰하였다. 동시에 이에 대한 propranolol의 효과도 검토하였다. 문맥 결찰 후에는 비 펄프압의 증가와 동반하여 내장장기의 혈류량과 모세혈관압 증가가 야기되었고 동시에 모세혈관 전 저항(Ra)과 모세혈관 후 저항(Rv)은 저하되었다. Noradrenaline에 대한 Rv의 증가반응, adrenaline에 대한 Ra와 Rv의 증가반응, 및 phenylephrine에 대한 상장간막 동맥압, Ra및 Rv의 증가반응이 특징적으로 문맥결찰군에서 대조군에 비하여 현저히 약화되었다. Propranolol 처치군(PPL-3)에서 장간막 혈류량의 감소가 초래되었고, 문맥결찰군에서 저하된 Ra와 Rv가 propranolol투여로 대조군 수치로 회복되 었다. 이러한 성적의 결과로 문맥 결찰에 의하여 장간막 혈류량 증가와 동반된 Ra와 Rv의 저하는 비 펄프압 증가로 야기된 것으로 추측되며 내장장기 혈류역동학적 및 혈관 반응도의 변동은 장기적인 propranolol 처치로 효과있게 교정되는 점으로 미루어 내장장기의 과혈류역동은 내장장기 혈관의 아드레나린성 수용체의 기능변동과 밀접한 관련이 있다고 사료되었다.

• 한국미생물생명공학회:학술대회논문집
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• 한국미생물생명공학회 1978년도 춘계학술대회
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• pp.98.2-98
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• 1978

호기성 발효에 있어서, 산소와 charge transfer complex를 형성할 수 있는 phenol 유도체인 guai-acol, vanillin, O-v-anillin 등과 catechol 유도체인 resorcine, adrenaline, dopamin 등이 산소와의 반응에 의하여 효과적인 산소공급 촉진제로서 이용될 수 있는가를 알아보기 위하여 합성배지중에서 나타내는 산소이동계수(KLQ)를 측정 비교하여 발효공학에의 응용가능성을 검토하였다.

• Advances in Traditional Medicine
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• 제8권3호
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• pp.302-310
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• 2008

Azadirachta indica A. Juss (N.O. Meliaceae), popularly known, as 'Neem' is an indigenous tree widely available in India. Almost every part of the tree has long been used in Unani system of medicine for the treatment of a variety of human ailments. The flowers have been mentioned as a remedy useful in controlling diabetes mellitus. The present study had been designed to investigate the hypoglycemic/anti-hyperglycemic effects of the methanolic extract of the flowers of A. indica (Gule-Neem) and its different fractions on normal, glucose fed hyperglycemic, adrenaline induced hyperglycemic and alloxan induced diabetic rats. The methanolic extract was resolved into water soluble and water insoluble fractions. Water soluble portion of the methanolic extract was found to possess significant blood sugar lowering effect in glucose-fed and adrenaline-induced hyperglycemic rats but it did not show such effect in normal and alloxan induced mild and severe diabetic rats. Water-soluble portion was fractionated by employing the polarity criterion with ethyl acetate and butanol. The ethyl acetate fraction was further fractionated into phenolic and non-phenolic fractions. Hypoglycemic effect of these fractions was also evaluated. The results suggest that the flowers of A. indica contain at least two different constituents, responsible for the said activity. These investigations validate the use of flowers of A. indica in diabetes by Unani physicians.

• Natural Product Sciences
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• 제5권1호
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• pp.25-32
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• 1999

The pharmacological actions of ambrein were investigated alone or in combination as a pretreatment with agonists (adrenaline, noradrenaline, acetylcholine, histamine, nicotine), antagonists (atropine, atenolol) and calcium channel blocker (verapamil) in vivo in anaesthetized SWR rats using blood pressure, heart rate and myocardial contractility as parameters. Ambrein in the dose range of 50-200 mg/kg to the normotensive anaesthetized rats demonstrated negative chronotropic effect and increased the myocardial contractility significantly. At the mid dose (100 mg/kg) this increase in contractile force was 36% and 44% above the normal at 30 min and 60 min intervals post-treatment, respectively. Both of the lower and high doses (50 mg/kg and 200 mg/kg) had similar effects. Furthermore, this contractile response was dose related. Also, this compound produced a considerable increase in myocardial contractility when used as a pretreatment with some agonists and antagonists. The results on blood pressure did not show a considerable change when ambrein was used alone. However, ambrein pretreatment at the dose of 100 mg/kg did not block the effects of adrenaline, noradrenaline, isoprenaline and acetylcholine on heart rate and blood pressure. On the other hand, this pretreatment attenuated the sympathoadrenal effects of nicotine significantly. Chronotropic and blood pressure changes produced by histamine were also inhibited by ambrein pretreatment. This pretreatment significantly reversed the effects of atenolol but failed to demonstrate any change in the negative chronotropic, inotropic and hypotensive responses induced by verapamil. It is concluded that ambrein induced nonselective dose dependent antagonism of the effects of some agonists and antagonists require contribution of some neuromediators. However, the positive isotropic effects of ambrein possibly involve the enhancement of slow Ca channels and/or activation of ${\beta}-adrenergic$ receptors in the heart. At this moment it is difficult to explain the exact mode of action of ambrein and the studies dealing with Ca channel blocker and adrenergic blocker followed by ambrein may help to define the factors which contribute to its positive inotropic effects.

• The Korean Journal of Physiology
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• 제19권2호
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• pp.113-125
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• 1985

Electrophysiological difference of the central and peripheral area of the sinoatrial node in the rabbit was studied by glass microelectrode technique. Effects of $K^+,\;Na^+,\;Cs^+,$ adrenaline and ouabain on the action potential of the two areas were investigated, and transient hyperpolarization ($K^+-induced$ hyperpolarization) which developed following readmission of potassium after having pre-treated with $K^+-free$ Tyrode solution for 10 minutes was analyzed. The results obtained were as follows ; 1) The frequency of the spontaneous action potential recorded in the periphery of the SA node was faster than the central area. Reduction by $Cs^+$ and increase by O mM $K^+$, $10^{-6}M$ adrenaline and $10^{-6}M$ ouabain in the frequency of action potential were noticed more prominently in the peripheral than the central area. On the contrary, the frequency in the central area was more decreased than the Peripheral area by 13 mH $K^+$ and 1 mM $Co^{2+}$. 2) The amplitude of the K+_induced hyperpolarization was very small in the central area but large in the peripheral area. Transient hyperpolarization was abolished by ouabain and low sodium, and decreased by cooling the tissue $(17^{\circ}C)$. 3) By changing the concentration of $Ca^{2+}$ in the perfusate, the amplitude and the rate of transient hyperpolarization were increased in the high $Ca^{2+}$ concentration. It could be concluded that the central area of the SA node is less susceptible to the inhibition of Na-Pump and more susceptible to Ca-blocker and high concentration of $K^+$. The Na-Pump activity of the central area measured by means of transient hyperpolarization is found to be much less active than that of the peripheral area.