• Journal of Korean Neurosurgical Society
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• 제59권2호
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• pp.154-157
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• 2016

A continuous electroencephalography (cEEG) can be helpful in detecting vasospasm and delayed cerebral ischemia in aneurysmal subarachnoid hemorrhage (SAH). We describe a patient with an aneurysmal SAH whose symptomatic vasospasm was detected promptly by using a real-time cEEG. Patient was immediately treated by intraarterial vasodilator therapy. A 50-year-old woman without any significant medical history presented with a severe bifrontal headache due to acute SAH with a ruptured aneurysm on the anterior communicating artery (Fisher grade 3). On bleed day 6, she developed a sudden onset of global aphasia and left hemiparesis preceded by cEEG changes consistent with vasospasm. A stat chemical dilator therapy was performed and she recovered without significant neurological deficits. A real-time and protocol-based cEEG can be utilized in order to avoid any delay in detection of vasospasm in aneurysmal SAH and thereby improve clinical outcomes.

• 한국임상약학회지
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• 제2권1호
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• pp.1-9
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• 1992

Protective effect of urokinase on reperfusion were studied followed by global ischemia in the isolated perfused rat heart. Separately, anti-platelet aggregation effect of urokinase also investigated. Urokinase exhibited positive effect for the protection of rat heart function by increasing the LV dp/dt, coronary flow(CF) and the Tate pressure product(RPP), and by decreasing the LVEDP on reperfusion. Urokinase also decreased arrhythmia by $74.7\%(P<0.05) induced by global ischemia in the rat heart. In the platelet aggregation study, urokinase did not show the inhibitory effect of ADP or collagen induced platelet aggregation inviuo and exvivo.

• 한국임상약학회지
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• 제7권1호
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• pp.33-39
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• 1997

Cardiac and antihypertensive effects of BMS-180448, a cardiac-selective ATP-sensitive potassium channel opener, and its newly synthesized derivatives KR-31281, KR-31282 and KR-31299 were evaluated in isolated perfused rat hearts (25 min global ischemia/30 min reperfusion) and conscious rats. Three new compounds $(10\;{\mu}M)$ induced positive inotropism as evidenced by increased LVDP (left ventricular developed pressure) and RPP (Rate-Pressure Product) in nonischemic rat heart. HR-31299 increased CF (coronary flow) and HR (heart rate) but the other two had no effects. KR-31282, KR-31281 and HR-31299 had a tendency to increase reperfusion LVDP and RPP compared with vehicle, while the latter two significantly reduced reperfusion EDP with a tendency to inclose TTC (time to contracture). All three KR-compounds had very weak effects on MBP and HR in conscious rats. These results indicate that KR-31281 and HR-31299 may have some cardioprotective effects, although weaker than BMS-180448, and their mode of action different from that of BMS-180448, despite the similarity in major structural moeity.

• Archives of Pharmacal Research
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• 제26권10호
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• pp.800-804
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• 2003

The effects of KR-31378, a neuroprotective agent for ischemia-reperfusion damage, on liver microsomal cytochrome P450s (CYPs) were investigated in male Sprague Dawley rats. When rats were treated orally with KR-31378 for 7 consecutive days, CYP3A-selective erythromycin N-demethylase (ERDM) activity was significantly induced in a dose-dependent manner. In Western immunoblotting, CYP 3A proteins were clearly induced by treatment with KR-31378. Within 24 h after treatment with 80 mg/kg of KR-31378, ERDM activity was induced in liver microsomes in accompanied by induction of the level of CYP 3A proteins. The present results suggest that KR-31378 might modulate the expression of CYP 3A enzymes in humans.

• 한국생물공학회:학술대회논문집
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• 한국생물공학회 2003년도 생물공학의 동향(XIII)
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• pp.164-166
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• 2003

본 연구에서는 손상된 심근의 재생을 위하여 골수단핵세포를 피브린 고분자와 함께 SD 래트에 이식하였고 8주 후에 신생혈관의 형성과 더불어 심장의 기능이 향상되었음을 확인할 수 있었다. 이 연구는 세포이식을 통한 조직 재생시 세포 이식용 매트릭스의 중요성을 보여준다. 환자 자신의 골수세포를 사용한다면 면역 문제가 없어서, 이 방법이 심부전 환자의 치료에 쉽게 이용될 수 있을 것이다.

• 약학회지
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• 제41권1호
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• pp.117-125
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• 1997

The pharmacological effects of benzopyran potassium channel openers (lemakalim, KR-30450 and KR-30818) on the occlusion/reperfusion-induced myocardial infarction were investigat ed. In anesthetized rats, subjected to 45-min occlusion of the left anterior descending coronary artery (LAD) followed by 90-min reperfusion, the infarct size was measured by calculating the ratio of infarct zone to area at risk (IZ/AAR) with the Evans blue/TTC technique. Rats were intravenously given vehicle (1% DMSO), lemakalim, KR-30450, and KR-30818 alone or in combination with a selective K$_{ATP}$ blacker glibenclamide, 30 min prior to coronary occlusion. Compared to vehicle, lemakalim (30 ${\mu}$g/kg i.v.), the active enantiomer of cromakalim, had a tendancy to decrease infarct size. KR-30450(30 ${\mu}$g/kg, i.v.). the newly synthetized potassium channel openers (PCOs), caused a reduction of infarct size (from 70${\pm}$4%to 57${\pm}$5%). but KR-30818 (30 ${\mu}$g/kg, i.v.), a metabolite of KR-30450. did not modify infarct size. It seem ed likely that glibenclamide (0.3mg/kg, i.v.), given in combination, reduced the effects of these PCOs, especially KR-30450 (30 ${\mu}$g/kg, i.v.) on the infarct size. These results indicate that. in the coronary occluded rat model of ischemia, lemakalim and KR-30450 may exert cardioprotective activity through a reduction of infarct size, the effect being considered related to the opening of K$_{ATP}$ channel.

• Journal of Ginseng Research
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• 제41권3호
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• pp.373-378
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• 2017

Ocotillol-type saponins are one kind of tetracyclic triterpenoids, sharing a tetrahydrofuran ring. Natural ocotillol-type saponins have been discovered in Panax quinquefolius L., Panax japonicus, Hana mina, and Vietnamese ginseng. In recent years, the semisynthesis of 20(S/R)-ocotillol-type saponins has been reported. The biological activities of ocotillol-type saponins include neuroprotective effect, antimyocardial ischemia, antiinflammatory, antibacterial, and antitumor activities. Owing to their chemical structure, pharmacological actions, and the stereoselective activity on antimyocardial ischemia, ocotillol-type saponins are subjected to extensive consideration. In this review, we sum up the discovery, semisynthesis, biological activities, and metabolism of ocotillol-type saponins.

• Archives of Pharmacal Research
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• 제24권3호
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• pp.229-233
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• 2001

This Paper deals with the development of a technology for making a hydrophilic gel of Polyethylene oxide reception in which radiating ability is employed to cause cross-linking of Polymers in a water solution. The gel of polyethylene oxide was shown to be nontoxic contain 5-50% of polymer and be useful in composite medicinal forms along with biologically active substances including Bac. subtilis proteases. Proteases immobilized in the gel possess high thermal stability and proteolytic activity and are readily applied in medicine. The effect of immobilized proteolytic and glucolytic enzymes of Bac. subtillis (Immozimase) on the warm ischemia-reperfusion (I/R) which can cause hepatic and jejunum injury was also studied. These enzymes were immobilized on water-soluble polymer polyethylene glycol by means of an electron beam. The number of degraanulated mast cells as well as serum ALT after I/R in the group with Immozimase was decreased to almost half as compared with the control group. Pretreatment with Immozimase resulted in significant reduction of hepatic and gut neutrophil accumulation as compared with control animals. It was concluded that Immozimase has a protective effect for hepatic and gut ischemia/reperfusion, and this effect seems to be associated with prevention of leukocyte accumulation .

• Archives of Pharmacal Research
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• 제27권2호
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• pp.239-245
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• 2004

KR-31543, (2S,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(2 -methyl-2H-tetrazol-5-ylmethyl) amino]-3,4-dihydro-2-dimethoxymethyl-3-hydroxy-2-methyl-2H-1-benzopyran, is a new neuroprotective agent for preventing ischemia-reperfusion damage. This study was performed to identify the metabolic pathway of KR-31543 in human liver microsomes and to characterize cytochrome P450 (CYP) enzymes that are involved in the metabolism of KR-31543. Human liver microsomal incubation of KR-31543 in the presence of NADPH resulted in the formation of two metabolites, M1 and M2. M1 was identified as N-(4-chlorophenyl)-N-(2-methyl-2H-tetrazol-5-ylmethyl)amine on the basis of LC/MS/MS analysis with a synthesized authentic standard, and M2 was suggested to be hydroxy-KR-31543. Correlation analysis between the known CYP enzyme activities and the rates of the formation of M 1 and M2 in the 12 human liver microsomes have showed significant correlations with testosterone 6$\beta$-hydroxylase activity (a marker of CYP3A4). Ketoconazole, a selective inhibitor of CYP3A4, and anti-CYP3A4 monoclonal antibodies potently inhibited both N-hydrolysis and hydroxylation of KR-31543 in human liver microsomes. These results provide evidence that CYP3A4 is the major isozyme responsible for the metabolism of KR-31543 to M1 and M2.

• Journal of Chest Surgery
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• 제22권6호
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• pp.927-935
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• 1989

Using an isolated Rat heart preparation of the Sprague Dawley strain, the YUMC cardioplegic solution k the St. Thomas Hospital Cardioplegic Solution were compared in the non waking K working heart perfusion systems by evaluating the hemodynamics, [bio] chemical, and light microscopic finding The heart rate k coronary flow of the two groups in the 20 minutes post ischemic recovery time were 288.6*6.5 vs 283.7*12 and 21.3*1.0 vs 19.0*1.7 respectively with no statistical significance existing. However the aortic systolic pressure, aortic overflow, cardiac output which were 81.7[4.2 vs 78.4*1.8, 18.3*1.1 vs 13.0*2.5 and 36.9*0.9 vs 32.0*3.2 respectively with P < 0.01 indicate that the comparison of these three parameters is statistically meaningful. The amount of CPK extracted in the 20 minutes post 120 minutes of ischemia was compared for the two cardioplegic solution, the results of which turned out to be similar, light microscopic findings were also found to be similar. It is thought that the YUMC cardioplegic solution provided better results than the St. Thomas hospital solution because of the differing composition of the two solution such as glucose, mannitol, albumin were put only in the former solution enhancing osmolarity of the cardioplegic solution providing better hemodynamic results.