• 한국식품과학회지
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• 제30권6호
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• pp.1476-1479
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• 1998

키토산 올리고당이 ACE 저해활성과 SHR의 혈압에 미치는 영향을 검토하였다. 키토산 올리고당은 모두 ACE 저해활성을 나타내었다. ACE 저해활성$(IC_{50})$은 3량체가 $0.9\;{\mu}mole$로 가장 우수하였고 2량체의 경우에는 $2.4\;{\mu}mole$, 그 외의 올리고당은 모두 $>100\;{\mu}mole$였다. 강력한 ACE 저해제인 Captopril(2-D-mercaptopropanoyl-L-proline)의 인체 투여량을 기준으로 3량체 키토산 올리고당 2.14 mg/kg을 SHR에 강제 경구투여한 바, 4시간 경에 8주령 및 21주령 SHR모두 최저혈압을 보였고 이 때의 혈압 강하는 8주령 SHR $27{\pm}4.8\;mmHg$, 21주령 SHR $36{\pm}4.3\;mmHg$로 나타났다. 따라서 3량체 키토산 올리고당은 2량체 키토산 올리고당과 함께 향후 고혈압 치료제로서 응용가능함이 시사되었다.

• Childhood Kidney Diseases
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• 제3권1호
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• pp.42-47
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• 1999

목 적 : ACE inhibitor는 주로 항고혈압제제로 사용되고 있으나 정상 혈압을 가진 신질환 환자에서 단독으로 쓰일 경우 단백뇨를 감소시키고 신기능을 보호하는 효과가 있음이 보고되었다. 그러나 소아 신증후군에서 스테로이드와 병합 투여할 경우 단백뇨 소실에 상승작용이 있는지에 대해서는 별로 알려진 바가 없다. 이에 저자들은 신증후군 환아에서 스테로이드와 ACE inhibitor인 Inhibace의 병합투여가 단백뇨 소실에 미치는 영향을 관찰하기 위하여 본 연구를 시행하였다. 방 법 : 원발성 신증후군으로 내원한 환아를 대상으로 치료방법에 따라 Prednisolone 2mg/kg/day를 단독으로 투여한 환아(대조군)와 Prednisolone 및 Inhibace 2.5mg/day를 같이 투여한 환아(Inhibace군)로 구분하였으며 이 중 치료에 반응을 보인 45명(대조군 29명, Inhibace군 16명)을 대상으로 치료결과를 비교하였다. 결 과 : 두 군간의 평균연령 및 남녀비는 유의한 차이가 없었다. 발병시 24시간 요중 단백량은 대조군 $699.6{\pm}1396.6 mg/m^2/hr$, Inhibace군 $624.9{\pm}275.1\;mg/m^2/hr$로 유의한 차이는 없었다. 스테로이드 투여 후 단백뇨 소실까지의 기간은 Inhibace군에서 $10.9{\pm}2.0$일로 대조군의 $13.6{\pm}4.0$일보다 유의하게 짧았고 (P<0.05) 성별 및 연령에 따른 차이는 없었다. 치료 전후의 혈청 콜레스테롤 농도는 대조군과 Inhibace군 간에 유의한 차이가 없었으며 Inhibace군에서 치료 전후에 크레아티닌 청소율의 유의한 변화는 없었다. 혈압의 변화는 두 군간에 유의한 차이는 없었으며 Inhibace 군에서 저혈압의 소견은 보이지 않았다. 결 론 : 소아 신증후군에서 스테로이드와 ACE inhibitor의 병합투여는 스테로이드 단독 투여에 비해 완해에 이르는 기간을 단축시키는 효과가 있는 것으로 사료되며 앞으로 장기간의 ACE inhibitor의 투여가 재발율 및 관해 유지에 미치는 영향에 대한 연구가 더 필요할 것으로 생각된다.

• 생명과학회지
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• 제20권6호
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• pp.838-844
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• 2010

토양에서 생육하는 Streptomyces corcohrussi의 혈전용해효소가 DEAE-Sephadex A-50 그리고 Sephadex G-50 젤 여과를 이용한 크로마토그라피 방법에 의해 순수분리 되었다. SDS-PAGE 분석결과, 분리된 효소는 단일 단백질이고, 그 분자량은 약 34 kDa 이라는 것을 알 수 있었다. 순수분리된 효소의 혈전용해활성은 plasminogen-rich fibrin plate에서 0.8 U/ml 이었으나, plasminogen-free fibrin plate 에서의 그 효소활성은 0.36 U/ml 이하이었다. 이러한 결과로, 순수 분리된 효소가 plasminogen activator 로 작용한다는 것을 알 수 있었다. 단백질 저해제인 $\varepsilon$-ACA, t-AMCHA 와 mercuric chloride의 존재시에 그 혈전용해활성은 24% 이하이었는데, 이러한 결과는 이들 plasmin 저해제 그리고(혹은) fibrinogen을 fibrin으로 전환시키는 과정과 관련된 fibrinogen 저해제에 의해 이 효소가 조절될 수 있음을 나타낼 수 있다. 한편으로, 중금속 이온인 $Zn^{2+}$은 그 활성을 58% 감소시켰다. 순수 분리된 효소의 최적 온도는 약 $50^{\circ}C$ 이었고, 그 효소활성의 92% 이상은 pH 5.0과 8.0 사이에서 유지되었다. 그러므로, 이러한 결과들은 하나의 강력한 혈전용해효소를 제공해서, S. corcohrussi 유래 새로운 혈전용해제의 개발에 기여하도록 한다.

• Journal of Dairy Science and Biotechnology
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• 제16권2호
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• pp.98-105
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• 1998

Various peptides derived from food are among the most potent physiologically active agents known, and include anticancer peptides, angiotensin converting enzyme(ACE) inhibitor exhibiting antihypertension action, opioid peptides, antithrombotic peptides, hypocholesterolemic peptides, immunomodulators, calcium absorption enhancers, and other peptides. Hydrophobic peptides extracted from a Cheddar-type cheese slurry were fractionated by gel chromatography and repeated HPLC. A peptide fraction from HPLC showed high cytotoxicity on the tumor cell lines such as a human colon carcinoma, and comprised of Tyr, Ser, Leu, Gly, and others. Hypocholesterolemic peptides were isolated from peptic hydrolyzates of casein and soy proteins. Macropeptides of 1,000${\sim}$5,000 dalton were effective on reducing the cholesterol level of mouse serum. Peptides showing high Krigbaum hydrophobicity and ANS surface hydrophobicity resulted in high hypocholesterolemic effect and fecal steroid concentrations. Caseinomacropeptides(CMP) were isolated from whey powder and treated with soluble and immobilized trypsin to obtain antithrombotic peptides. One fraction from the CMP hydrolyzed with immobilized trypsin for 24h exhibited high antithrombotic activity with 52.5% inhibition of platelet aggregation. These result suggested that peptides from various milk products could be utilized as a good bioactive agents for developing health functional foods.

• 약학회지
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• 제34권2호
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• pp.88-101
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• 1990

Captopril, angiotensin converting enzyme (ACE) inhibitor, when given intravenously in dog, elicited the diuretic action along with the increases of glomerular filtration rates (GFR), renal plasma flow (RPF) and osmolar clearances (Cosm) with no changes of free water clearnces ($C_{H_2O}$), and then captopril produced the enlargement of excretion rates of electrolytes in urine and the reduction of reabsorption rates of electrolytes in renal tubles. Captopril, when given into a renal artery, exhibited no changes of renal function in the experinental kidney, whereas diuretic action with the same mechanism as shown in intravenous captopril in control kidney. Captopril, when injected into a carotid artery, showed increases in rates of urine flow in a small does which did not affect on renal action when it was administered intravenusly. Diuretic action induced by captopril was not influenced by renal artery denervation, propranolol and angiotensin II inhibiters. Above results suggest that captopril produced diuretic action along with renal hemodynamic changes by slight contraction of vas efferense and reduction of reabsorption rate of electrolytes in renal tubules, especilly distal tubules, that may be mediatedby endogenous substances.

• 한국임상약학회지
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• 제27권3호
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• pp.136-142
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• 2017

Background: Dementia is one of important social and economic healthcare issues in the aging age. Therefore, it signifies to analyze the relationship between chronic disease or cardiovascular drug use and the incidence of dementia to establish a basis for increasing or preventing the risk of dementia. The purpose of this study was to investigate the correlation between the prevalence of chronic diseases and the use of cardiovascular drugs in patients diagnosed with dementia. Methods: In this study, we used data from sample of elderly patients from the Health Insurance Review and Assessment Service. We analyzed by logistic regression analysis with age, gender, and medication as covariates. KCD-7 was used to diagnosis of the disease, and drugs were analyzed using ATC codes and Korean standardized drug classification codes. Results: A total of 1,276,331 patients were analyzed in the sample of the elderly population, of which 532,075 (41.7%) were male and 744,256 (58.3%) were female. The patients have the higher risk of dementia in the older, women, and lower socioeconomically status. Cerebral infarction and ischemic heart disease increases risk of dementia. Patients taking statins, angiotensin converting enzyme inhibitor (ACEI) or angiotensin II receptor antagonists (ARB) showed low incidence of dementia. Conclusion: This study has been shown that ACEI, ARB, and statin drugs may associate with lower incidence of Alzheimer's and other dementia except vascular dementia.

• Bulletin of the Korean Chemical Society
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• 제35권7호
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• pp.2065-2071
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• 2014

${\beta}$-Secretase (beta-amyloid converting enzyme 1 [BACE1]) is involved in the first and rate-limiting step of ${\beta}$-amyloid ($A{\beta}$) peptides production, which leads to the pathogenesis of Alzheimer's disease(AD). Therefore, inhibition of BACE1 activity has become an efficient approach for the treatment of AD. Ligand-based and docking-based 3D-quantitative structure-activity relationship (3D-QSAR) studies of acyl guanidine analogues were performed with comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) to obtain insights for designing novel potent BACE1 inhibitors. We obtained highly reliable and predictive CoMSIA models with a cross-validated $q^2$ value of 0.725 and a predictive coefficient $r{^2}_{pred}$ value of 0.956. CoMSIA contour maps showed the structural requirements for potent activity. 3D-QSAR analysis suggested that an acyl guanidine and an amide group in the $R_6$ substituent would be important moieties for potent activity. Moreover, the introduction of small hydrophobic groups in the phenyl ring and hydrogen bond donor groups in 3,5-dichlorophenyl ring could increase biological activity.

• 한국유가공학회:학술대회논문집
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• 한국유가공기술과학회 1998년도 제46회 춘계 유가공 심포지움 - 우유 및 유제품의 기능성
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• pp.22-29
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• 1998

Various peptides derived from food are among the most potent physiologically active agents known, and include anticancer peptides, angiotensin converting enzyme(ACE) inhibitor exhibiting antihypertension action, opioid peptides, antithrombotic peptides, hypocholesterolemic peptides, immunomodulators, calcium absorption enhancers, and other peptides. Hydrophobic peptides extracted from a Cheddar-type cheese slurry were fractionated by gel chromatography and repeated HPLC. A peptide fraction from HPLC showed high cytotoxicity on the tumor cell lines such as a human colon carcinoma, and comprised of Tyr, Ser, Leu, Gly, and others. Hypocholesterolemic peptides were isolated from peptic hydrolyzates of casein and soy proteins. Macropeptides of 1,000${\sim}$5,000 dalton were effective on reducing the cholesterol level of mouse serum. Peptides showing high Krigbaum hydrophobicity and ANS surface hydrophobicity resulted in high hypocholesterolemic effect and fecal steroid concentrations. Caseinomacropeptides (CMP) were isolated from whey powder and treated with soluble and immobilized trypsin to obtain antithrombotic peptides. One fraction from the CMP hydrolyzed with immobilized trypsin for 24h exhibited high antithrombotic activity with 52.5% inhibition of platelet aggregation. These results suggested that peptides from various milk products could be utilized as a good bioactive agents for developing health functional foods.

• 약학회지
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• 제43권6호
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• pp.843-850
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• 1999

We investigated whether endothelium-derived NO and endothelin-1 might result enhanced vasoconstriction induced by administration of norepinephrien (NE) at the early stage of one-kidney, one-clip (1K1C) renal hypertensive rats. We also studied the relation ship of renin-angiotensin system (RAS) using rat aorta in this hypothesis. L-NMMA (30$\mu$M) and L-NAME(30${\mu}M$) enhanced vasoconstriction induced by NE in thoracic aorta of control rats. However angiotensin converting enzyme (ACE) inhibitor didn't. The aorta of 1KIC rats showed a singnificantly exaggerated contractile response to NE as compared with control rats. Rub-bing the endothelium abolished this difference. Ach and SNP-induced vasorelaxation show no significant difference between 1KIC and control rats. The treatment of phosphoramidon (10${\mu}M$) and oral administration of captopril (0.05, w/v%) abolished the exaggerated contractile response to NE at early stage of 1KIC rats. These results suggest that the increase of contractile response at the early phase in 1KIC rat is partially involved in the activation of ACE.

• 한국임상수의학회지
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• 제38권4호
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• pp.189-193
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• 2021

An 11-years old spayed female Persian chinchilla cat presented with acute onset of blindness from bilateral retinal detachment and systemic hypertension. On physical examination, the cat was tachycardic (240 beats/min) with a systolic blood pressure of around 250 mmHg. Clinical findings, blood works, urinalysis, thyroid function test, radiography, echocardiogram, and ultrasonography were performed to rule out underlying diseases. Organ injury induced by systemic hypertension including bilateral retinal detachment and left ventricular hypertrophy were confirmed by ultrasound. Based on these results, it was diagnosed as feline idiopathic hypertension with target organ damage (TOD). The cat was treated with a combination therapy using high doses of amlodipine, telmisartan, and atenolol. After the treatment, its hypertension and TOD were improved. This case showed that appropriate therapeutic management can help prevent TOD associated with feline hypertension.