• 한국미생물·생명공학회지
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• 제20권4호
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• pp.422-429
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• 1992

Maltosy-$\beta$-cyclodextrin는 $\beta$-cyclodextrin에 maltose가 $\Alpha$-1,6 glycosidic bond로 결합된 분지환상결합체로서 pullulanase의 역반응(축합반응)을 이용하여 $\beta$-cyclodextrin과 maltose로부터 합성된다. Maltosyl-$\beta$-cycloextrin의 합성수율을 증가시키기 위하여 각종 water activity depressor인 각종 polyol, sugar 그리고 polyethylene glycol(PEG)등의 첨가의 영향을 검토하였다. 가장 적절한 water activity depressor는 PEG 6000로서, 첨가량 10%(w/w)의 경우 maltosyl-$\beta$-cyclodextrin 생성량과 합성수율은 크게 증가하여 3.02g/100ml 와 55.9%(w/w)로서, 첨가하지 않았을 경우보다 약 1.3배 증가하였다. Water activity는 PEG 6000을 20%(w/w) 첨가할 때 원래의 0.966에서 0.914로 감소하였으며, maltosyl-$\beta$-cyclodextrin 합성수율은 water activity에 반비례하여 증가하였다. Pullulanase의 역반응을 이용한 maltosyl-$\beta$-cyclodextrin 합성반응의 각종 열역학적 상수를 평가하였으며, $\Delta$H는 36.788kJ/mol, $\Delta$S는 0.067kJ/moleK, 그리고 $\Delta$G는 14.433kJ/mole이였다. PEG 6000의 분리회수에 적절한 ultrafiltration membrane의 pore size는 3K dalton이었으며, 여과액과 농축액의 적정 분획비는 1.0 : 9.0였다. Maltosyl-$\beta$-cyclodextrin 합성수율의 증가는 첨가한 PEG가 water activity를 감소시켜 합성된 maltosyl-$\beta$-cyclodextrin이 재분해되는 pullulanase이 정반응인 hydrolysis reaction을 억제하여 equilbrium state에 변화를 주기 때문인 것으로 유추된다.

• Journal of Pharmaceutical Investigation
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• 제9권3호
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• pp.27-38
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• 1979

This study was attempted to investigate the pharmacological action, especially depressor action of Phellodendri cortex and to elucidate the mechanism of its action, making use of Phellodendri cortex methanol extract (PCME) because its hypotensive action is not clear. Influence of PCME on the blood pressure of the rabbits and cats were observed in this study. PCME, when given intravenously in the rabbits and cats, elicited the hypotensive action, but intraventricular PCME in the rabbits did not show depressor action. Accumulation and tachyphylaxis by PCME administered into the ear-vein of the rabbits were not shown. Depressor effect of PCME in the rabbits was attenuated significantly by pretreatment with phentolamine, guanethidine, chorisondamine and atropine, but not by propranolol, diphenhydramine, cyproheptadine and vagotomization. The pressor activity of angiotensin was unimpaired after injection of maximal hypotensive doses (100mg/kg) of PCME, but the pressor activity of norepinephrine and carotid occlusion was abolished markedly. In addition, PCME given into jugular vein of the cats weakened norepinephrine pressor responses and caused the reversal of epinephrine pressor responses. These results suggest that the hypotensive action of PCME may be due to dual mechanisms by interference with peripheral sympathetic function, alpha adrenoceptor blocking action, and peripheral parasympathomimetics action, muscarinic action.

• 대한두개안면성형외과학회지
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• 제12권2호
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• pp.125-128
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• 2011

Purpose: Asymmetric crying facies is caused by agenesis or hypoplasia of the depressor anguli oris muscle and is often associated various anomalies. Several static and dynamic surgical interventions have been reported, but their effects are unreliable. We report on the successful use of botulinum toxin A in an asymmetric crying facies patient. Methods: A 4-year-old girl presented with a facial asymmetry on crying or smiling. Physical examination revealed that her face had no asymmetry at rest. However, the patient showed characteristic asymmetry when smiling, crying, and with other normal facial movements. Asymmetric crying facies was clinically suspected and the weakness of left depressor anguli oris was present on electrophysiology study. Fifteen units of botulinum toxin type A were injected to the right depressor anguli oris muscle. Results: The patient showed the prominent improvement in the facial symmetry without significant complication and the effect persisted until 3 months post injection. Conclusion: Asymmetric crying facies was treated successfully with botulinum toxin A and this method was easy and noninvasive.

• Biomolecules & Therapeutics
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• 제8권4호
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• pp.325-331
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• 2000

The present study was designed to assess the role of spinal adenosine $A_2$ receptor in the regulation of cardiovascular functions such as mean arterial pressure (MAP) and heart rate (HR) in male Sprague-Dawley rats. Rats (250~300 g) were anesthetized with urethane and paralyzed with d-tubocurarine and artificially ventilated. blood pressure and HR were continuously monitored via a femoral catheter connected to a pressure transducer and a polygraph. Drugs were administered intrathecally using injection cannula through guide cannula which was inserted inthrathecally at lower thoracic level through a puncture of an atlantooccipital mombrane. Intrathecal injection of an adenosine $A_2$ receptor agonist, 5'-(N-cyclopropyl)-carboxamaidoadenosine (CPCA; 1, 2 and 3 nmol, respectively), produced a dose-dependent decrease in MAP and HR. Pretreatment with $N^{G}$-nitro-L-arginine methyl ester (L-NAME), a nitric oxide synthase inhibitor or 10 nmol of MDL-12,330, an adenylate cyclase inhibitor blocked significantly the depressor and bradycardic effect of 2 nmol of CPCA. But, Pretreatment with 3 nmol of bicuculline, gamma-aminobutyric acid A (GAB $A_{A}$) receptor antagonist, or 50 nmol of 5-aminovaleric acid, GAB $A_{B}$ receptor antagonist did not inhibit the depressor and bradycardic effect of 2 nmol of CPCA. These results indicate that adenosine $A_2$ receptor in the spinal cord plays an inhibitory role in the regulation of cardiovascular function and that the depressor and bradycardic action of adonosine $A_2$ receptor are mediated via the synthesis of nitric oxide and the activation of adenylate cyclase in the spinal cord of rats.s.s.s.

• Archives of Pharmacal Research
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• 제3권1호
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• pp.23-30
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• 1980

Berberine, when administered into a ear-vein of the rabbit anesthetized with urethane, produced a long-lasting, dose related fall in blood pressure, but intraventricular berberline did not elicit the hypotensive response. This hypotensive activity of berberine was not influenced by pretreatment of vagotomization and atropine. Depressor responses induced by berberine were not impaired by diphenhydramine, chlorisondamine, guanethidine and propranolol, but reduced significantly by phentolamine pretreatment. Berberine attenuated markedly prossor responses of norepinephrine and epinephrine. These results suggest that berberine causes the hypotensive activity that is attributable to alpha adrenoceptor blockade, but not to a direct relaxant effect upon vascular smooth muscle.

• 대한약리학회지
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• 제1권1호
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• pp.63-65
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• 1965

Rabbit blood pressure showed gradual fall by intraventricular guanethidine (5mg). The pressure rise by carotid occlusion was markedly inhibited or abolished by the guanethidine, while it was enhanced by small dose (2mg). The intraventricular guanethidine did not affect norepinephrine pressor effect, but caused marked inhibition or abolishment of depressor action of serotonin.

• 대한약리학회지
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• 제22권2호
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• pp.115-122
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• 1986

Urethane 마취 가토에서 뇌내 alpha-1및 alpha-2 adrenoceptor의 작용에 미치는 calcium antagonist의 영항을 알아보고자 뇌실내 methoxamine과 clonidine의 혈압및 심박수 변동에 미치는 diltiazem, nifedipine의 영향을 조사한 결과, 1). 뇌실내 methgramine(1mg)은 혈압상승및 심박수 감소를 일으켰고, 뇌실내 clonidine$(30{\mu}g)$은 혈압하강및 심박수 감소를 일으켰다. 2). 뇌실내 diltiazem과 nifedipine은 dose-dependent한 혈압하강을 일으켰으며 심박수 감소를 일으켰다. Diltiazem에 비하여 nifedipine은 혈압하강 효과는 크고 심박수 감소효과는 작았다. 뇌실내 diltiazem$(400{\mu}g)$, nifedipine$(35{\mu}g)$의 혈압하강 작용은 완만하고 지속적이었으나 같은 양의 정맥내 투여효과는 일과성이었다. 3). 뇌실내 diltiazem$(400{\mu}g)$이나 nifedipine$(35,\;350{\mu}g)$ 처리 후에 methoxamine(1mg)의 혈압상승 효과는 영향받지 않았으나 심박수감소 효과는 유의하게 감약되었다. 4). Clonidine의 혈압하강 작용은 뇌실내 diltiazem$(400{\mu}g)$이나 nifedipine$(35,\;350{\mu}g)$ 처리 후에 감약되었으나 정맥 내 diltiazem$(200{\mu}g/kg)$이나 nifedipine$(30{\mu}g/kg)$ 후에는 영향받지 않았다. Clonidine의 심박수 감소작용은 .뇌실내및 정맥내 diltiazem이나 nifedipine 처리후에 감약되었다. 5). 뇌실내 clonidine$(30{\mu}g)$ 처 리후 뇌실내 diltiazem$(400{\mu}g)$과 nifedipine$(350{\mu}g)$의 혈압하강및 심박수 감소효과는 영향 받지 않고 그대로 나타났다. 이상의 결과로 diltiazem과 nifedipine은 가토뇌내에서 methoxamine에 의한 혈압상승의 작용점인 alrfia-1 adrenoceptor의 흥분에는 영향을 미치지 못하나 clonidine의 작용점인 alpha-2 adrenoceptor의 흥분에 의한 혈압하강및 심박수 감소효과는 억제한다고 추론하였다.

• The Korean Journal of Physiology
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• 제11권1호
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• pp.27-32
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• 1977

Diospyros Kaki Thunberg is the species of persimmon tree that grows in Korea. Although its fresh or dried fruits are often served as a desert, it has little been known if persimmon tree has any specific pharmacological action. The leaves and branches of persimmon tree has long been used as folk remedies for palsy and frostbite in the southern part of Korea and it is also in use for the treatment of hiccup and nocturnal enuresis in chinese herbal medicine. Recently it was reported that an intravenous administration of Diospyros Kaki Thunberg ethanol extract (KTEE) into the animals lowered arterial blood pressure. Lee concluded from his study on the mechanism of depressor action of KTEE that at least a part of depressor response he observed was caused by acetylcholine-like action of KTEE. On the other hand little study has been made on the effect of KTEE on the motility of isolated animal intestines. Therefore the present study was undertaken to investigate effect of KTEE and the mechanism of its action on the motility of isolated rabbit duodenum. Ethanol extract of Diospyros Kaki Thunberg was prepared by boiling 1 kg of dried branches of persimmon tree in 1 liter of ethanol and the motility of isolated rabbit duodenum was recorded on physiograph by means of force transducer connected with Magnus apparatus. Doses of KTEE used were $5{\times}10^{-4}gm/ml,\;1{\times}10^{-3}gm/ml,\;and\;2{\times}10^{-3}gm/ml$. And the isolated duodenum was separately pretreated with acetylcholine $(5{\times}10^{-7}gm/ml)$, pilocarpine $(2.5{\times}10^{-6}gm/ml)$, histamine $(5{\times}10^{-6}gm/ml)$ and barium chloride $(2.5{\times}10^{-5}gm/ml)$ in order to find out interactions of these drugs with KTEE. The results obtained are as follows: 1. At doses of $5{\times}10^{-4}gm/ml,\;1{\times}10^{-3}gm/ml$ KTEE reduced contractions of isolated duodenum, while tonus as well as contaction of duodenum were depressed with $2{\times}10^{-3}gm/ml$ of KTEE. 2. Since the inhibitory effect of KTEE on the intestinal motility was not blocked by pretreatment with acetylcholine, pilocarpine, and barium chloride, it was strongly suggested that the inhibitory action of KTEE on intestinal motility is mainly Caused by its antihistamine effect. 3. It is also concluded that the principal substance of KTEE responsible for inhibition of intestinal motility may also have a vasodilating activity and would not be an acetylcholine-like substance in case it is same substance as that cause depressor responses.

• 약학회지
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• 제22권3호
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• pp.163-174
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• 1978

차전자(Plantaginis Semen)은 우리나라 전국 각지의 원야와 노방의 자생하는 다년생 초목으로 Plantaginaceae(질경이과)에 속하는 Plantago major L. var. asiatica Decaisne 질경이의 종자를 말하며 그의 성분으로는 다량의 점액, 지방유, pentosan 및 galactan, succinic acid, plantanolic acid, adenine, choline. K-염등이 알려져 있다. 이 차전자는 한방과 민간에서 소염, 이뇨, 진해, 지사제로서 널리 사용되어 왔으며 그의 약리작용에 관해서는 이미 저자들이 가토를 이용한 실험에서 이의 methanol extract가 자궁수축작용, 호흡흥분작용, 혈압강하작용, 장관수축작용, 심장박동의 완제작용, 항이뇨작용이 있음을 보고한 바 있다. 그러나 그의 기전에 관해서는 거의 알려진 바가 없다. 따라서 저자들은 위의 여러가지 작용중 특히 혈압강하작용에 관한 본태를 파악하여 그의 실용성 여부를 구명코자 이 실험을 착수하였다.

• 생약학회지
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• 제7권3호
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• pp.215-220
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• 1976

1. Nepetae Herba water extract (NHW) produced a fall of blood pressure in the rabbit. 2. The depressor effect of NHW was inhibited by atropine, but was not affected by propranolol, hexamethonium and diphenhydramine. 3. NHW showed pressor response in the rabbit treated with atropine. 4. The pressor response in the atropine treated rabbit was inhibited by phentolamine and guanethidine.