• Title/Summary/Keyword: 항고

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Preparation of (S)-(+)-Pranidipine by Optical Resolution (광학 분할에 의한 (S)-(+)-Pranidipine의 제조방법)

  • Baek, Du-Jong;Yoon, Ji Hye;Kim, Moon-Sik
    • Journal of the Korean Chemical Society
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    • v.59 no.6
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    • pp.488-492
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    • 2015
  • In this study, the effective preparation method of (S)-(+)-pranidipine, the active component of antihypertensive drug as a calcium channel blocker, was developed using optical resolution. The racemic monocarboxylic acid 5 obtained by the hydrolysis of (±)-pranidipine was mixed with optically active quinidine to form salts, and the insoluble diastereomeric salt was collected and successive treatment with base and acid furnished (R)-(-)-carboxylic acid 7. (S)-(+)-Pranidipine was prepared by esterification of this acid with cinnamyl alcohol, and the analysis by chiral HPLC showed 100% enantiomeric excess (ee). This process would be industrially very useful to prepare chiral (S)-(+)-pranidipine, since the use of strong base and anhydrous solvents, and ultra-low temperature condition were excluded in this process.

Screening New Antihypertensive Angiotensin I-Converting Enzyme Inhibitor -Producing Yeast and Optimization of Production Condition (항고혈압성 안지오텐신 전환효소 저해제를 생산하는 새로운 효모의 선별 및 저해물질 최적 생산조건)

  • Kang, Min-Gu;Kim, Ha-Kun;Yi, Sung-Hun;Lim, Sung-Il;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.39 no.3
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    • pp.194-197
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    • 2011
  • Forty eight strains of yeast were cultured in potato dextorse(PD) broth at $30^{\circ}C$ for 24 hr and centrifuged with 12,000 rpm for 20 min. After concentrated the cultures, antihypertensive angiotensin I-converting enzyme(ACE) inhibitory activities of its concentrates were investigated. Among them, the concentrates from Saccharomyces cerevisiae Y183-3 showed the highest ACE inhibitory activity of 71.8%. The ACE inhibitor from Saccharomyces cerevisiae Y183-3 was maximally produced when Saccharomyces cerevisiae Y183-3 cultured in PD broth at $30^{\circ}C$ for 36 hr.

Antimicrobial, Antihypertensive and Anticancer Activities of Garlic Extracts (마늘 추출물의 항균, 항고혈압 및 항암활성)

  • Kim, Ki-Ju;Do, Jeong-Ryong;Kim, Hyun-Ku
    • Korean Journal of Food Science and Technology
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    • v.37 no.2
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    • pp.228-232
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    • 2005
  • Antibacterial, antifungal, anticancer, and ACE inhibitory activities of methanol, ethyl acetate, chloroform, and hexane extracts of garlic were investigated. Methanol extract showed highest yield of 7.9-8.8 brix. Ethyl acetate and chloroform extracts showed strong antibacterial activities as determined by inhibition zone (8-16mm) against B. subtilis and P. aeruginosa, and good antifungal activities as determined by inhibition zone (8-30mm) against A. niger, M. miehei, and T. reesei. Wando, Banyans, Chinese, and Seosan garlic methanol extracts showed 65.6, 60.4, 70.1, and 55.3% ACE inhibitory activities, 42.3, 53.8, 50.4, and 54.5% anticancer activities against SNU-1, and 11.3, 20.2, 36.6, and 30.5% anticancer activities against HeLa, respectively.

Manufacture and Characteristics of Functional Drink Using Pear-Strawberry Fermentative Concentrates from Fermentation by Saccharomyces cerevisiae C-2 (Saccharomyces cerevisiae C-2로 발효시킨 배-딸기 발효 농축물을 이용한 기능성 음료의 제조 및 특성)

  • Jang, Jeong-Hoon;Na, Kwang-Chul;Kim, Wal-Soo;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.38 no.2
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    • pp.189-191
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    • 2010
  • Mixed juice of pear and strawberry was fermented by commercial Saccharomyces cerevisiae C-2 at $25^{\circ}C$ for 7 days and obtained the pear-strawberry fermentative concentrates (PSFC). The PSFC showed high ACE inhibitory activity of 70.8%. The PSFC drink was prepared by using PSFC and by-materials including amylopeptide, and determined changes of quality and ACE inhibitory activity during storage of $20^{\circ}C$ and $40^{\circ}C$. PSFC drink was very stable at storage of $20^{\circ}C$ for 8 weeks without any quality and ACE inhibitory activity.

Antioxidant and Inhibition on Angiotensin Converting Enzyme Activity of Colored Potato Extracts (유색감자 추출물의 항산화 및 항고혈압 활성)

  • Park, Young-Eun;Cho, Huyn-Mook;Lee, Hyeon-Jin;Hwang, Young-Sun;Choi, Su-San-Na;Lee, Su-Jin;Park, Eun-Sun;Lim, Jung-Dae;Choung, Myoung-Gun
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.52 no.4
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    • pp.447-452
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    • 2007
  • This experiment was conducted to enhance the colored potatoes utilization and to determine the biological activity of colored potato extracts. In order to understand the factors responsible for the potent antioxidant and antihypertensive ability of colored potatoes, it has been evaluated for anti-oxidative activity using Fenton's reagent/ethyl linoleate system and for free radical scavenging activity using the 1,1-diphenyl-2-picryl hydrazyl free radical generating system. There were significant differences of antioxidant activities in $50{\mu}g/mL$ extracts treatment among different colored potatoes. About two-fold higher radical scavenging activity was found in 'Daegwan 1-102', 'Daegwan 1-104' and 'Jasim' compared to that in 'Superior'. Based on the flesh color tested, potatoes with purple tuber showed higher radical scavenging activity than red potatoes, while white potato showed the lowest radical scavenging activity. The ability of 80% ethanol extracts from colored potatoes to influence the inhibitory activity of angiotensin converting enzyme(ACE) and xanthine oxidase(XOase) has also been investigated. Expect 'Jasim', the high levels of inhibition activity of xanthine oxidase in two colored potatoes such as 'Daegwan 1-102' and 'Daegwan 1-104' were highly correlated to $IC_{50}$ values of ACE inhibition activity. The various therapeutic benefit claims in the new functional medicinal usage of colored potatoes ascribed to the phenolic compounds and anthocyanin. This result revealed that the extracts of colored potatoes are expected to be good candidate for development into source of free radical scavengers and anti-hypertentive agent.

Effects of Dietary Salt Restriction on the Development of Renal Failure in the Excision Remnant Kidney Model (식이 sodium 제한 및 식이 sodium 제한에 따른 항고혈압제의 투여가 만성신부전증의 진행에 미치는 영향에 관한 실험적 연구)

  • Kim Kee-Hyuk;Kim Sang-Yun;Kang Yong-Joo;Maeng Won-Jae;Kim Kyo-Sun
    • Childhood Kidney Diseases
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    • v.3 no.2
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    • pp.170-179
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    • 1999
  • Purpose: To evaluate whether or not sodium restriction had its own beneficial effect and increased the efficiency of the anti-hypertensive drugs on the progression of renal failure. Methods: We studied using the excision remnant kidney model. Treatment groups were as follows: 5/6 nephrectomy and a 0.49% (normal-high) sodium diet (NN); 5/6 nephrectomy and a 0.25% (normal-low) sodium diet (LN); 5/6 nephrectomy, a 0.49% sodium diet and enalapril (NNE); 5/6 nephrectomy, a 0.49% sodium diet and nicardipine (NNN); 5/6 nephrectomy, a 0.25% sodium diet and enalapril (LNE); 5/6 nephrectomy, a 0.25% sodium diet and nicardipine (LNN). Both diets were isocaloric and had the same content of protein, phosphorus and calcium. Proteinuria, remnant kidney weight, mesangial expansion scores, and glomerular volume were assessed. Results: Blood pressure tended to be lower in LN compared to NN (P<0.05). NN developed progressive hypertension. LNE, LU, NNE, and NNN reduced blood pressure. LNE, LNN, NNE, NNN, and LN had significantly less proteinuria than NN at 16 weeks (P<0.05). At 24 weeks, LN developed proteinuria (82 mg/day), which were lessened in LNE (54 mg/day) and not lessened in LNN (76 mg/day). Mesangial expansion scores were significantly less in LN rats compared to those in NN rats. Glomerular volumes at 24 weeks in LN rats were significantly less compared to those at 16 weeks in NN rats. Mesangial expansion scores and glomerular volumes at 4, weeks, 12 weeks, and 24 weeks were not different among LN, LNE, and LNN groups. Conclusion: Dietary salt restriction lessens renal damage, at least in part, by inhibiting compensatory renal growth and reducing blood pressure. Enalapril was particularly successful in reducing proteinuria and glomerular injury when combined with dietary salt restriction.

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Effects of Dietary Protein on the Progression of Early Chronic Renal Failure in Subtotally Nephrectomizid Rats (저단백식이의 투여가 만성신부전증의 진행에 미치는 영향에 관한 실험적 연구)

  • Kim, Kyo-Sun;Kim, Kee-Hyuk;Kim, Sang-Yun;Kang, Yong-Joo;Maeng, Won-Jae
    • Childhood Kidney Diseases
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    • v.3 no.1
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    • pp.64-71
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    • 1999
  • Purpose : The protective effects of dietary protein on the progression of renal failure were studied in subtotally nephrectomized rats. Methods : Treatment groups were as follows; 5/6 nephrectomy and a normal protein ($18.5\%$) diet (NP); 5/6 nephrectomy and a low protein ($6\%$) diet (LP): 5/6 nephrectomy, a normal protein diet and converting enzyme inhibitor, enalapril (NPE): 5/6 nephrectomy, a low protein diet and enalapril (LPE). Both diets were isocaloric and had the same phosphorus content. Proteinuria, remnant kidney weight, mesangial matrix expansion score and glomerular volume were assessed at 4, 12 and 16 weeks after renal ablation. Results : LP and NP developed progressive hypertension. Eight weeks after surgery, LPE and NPE controlled hypertension. LP, LPE, and NPE had significantly less proteinuria than NP at 16 weeks (P<0.05). Kidney weight in LP were markedly less enlarged than NP (P<0.05). There was no difference in kidney weight between LPE and NPE. At 12 and 16 weeks the mesangial matrix expansion score was significantly less in LP, LPE, and NPE compared to NP (P<0.05). At 12 and 16 weeks mean glomerular volume was significantly less in LP compared to NP (P<0.05). At 12 and 16 weeks mean glomerular volume in LPE was significantly less compared to NPE. Conclusion : Dietary protein restriction afforded considerable protection from renal injury in the rat remnant kidney model. During the enalapril treatment, there was no additional protective effect of dietary protein restriction against the development of renal lesions.

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Concanamycin B, Active substance Against Phytophthora capsici Produced by Streptomyces neyagawaensis 38D10 Strain (Streptomyces neyagawaensis 38D10 균주가 생산하는 concanamycin B의 항고추역병 활성)

  • Kim, Chang-Jin;Lee, In-Kyoung;Yun, Bong-Sik;Yoo, Ick-Dong
    • Microbiology and Biotechnology Letters
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    • v.21 no.4
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    • pp.322-328
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    • 1993
  • During the screening of antifungal compounds from microbial secondary metabolites to control phytophthora blight of red pepper caused by Phytophthora capsici, a soil isolate, strain 38D10 was selected. Based on taxonomic studies, this strain was identified as Streptomyces neyagawaensis. The antifungal compound was purified from culture broth by HP-20 column chromatography, ethyl acetate extraction, silica gel column chromatography, HPLC and identified as concanamycin B by UV. $^1H$-NMR, $^{13}C$-NMR, SIMS analysis. Concanamycin B has strong antifungal activity against some phytopathogenic fungi but not antivacterial activity and preventive value were 50% and 100% at 125ppm and 250ppm in pot assay.

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Antihyperlipidemic Effects of Bupleuri Radix, padix and Uncariae Ramulus et Uncus on Experimental Hyperlipidemia in rats (고지혈증 랫트를 이용한 시호, 작약, 조구등의 항고지혈 효과)

  • 노환성;고우경;박건구;조영환;박형섭
    • Biomolecules & Therapeutics
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    • v.5 no.1
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    • pp.43-47
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    • 1997
  • Effects of Bupleuri Radix, Paeonie Radix or Uncariae Ramulus et rncus on experimental yperlipidemia were studied. Hyperlipidemia was induced on male Wistar rats by feeding them on high holesterol diet for one week, as previously described by the authors. Blood lipid profile was verified on these ats by measuring total cholesterol(TC), triglyceride(TG), high density lipoprotein cholesterol(HDL) and low ensity lipoprotein cholesterol(LDL). Then, the rats were followed by feeding normal diet. At the same time, ethanol extracts of the three individual herb medicines were orally administered to the rats for 4 weeks and the parameters above mentioned were monitored. Methanol extract of 5Bupleuri radix reduced the TC value significantly at 2 week point and Paeoneae Radix reduced the TC value at 4 week point in compare to control group, suggesting the antihyperlipidemic effect of the two herbal medicines in vivo. The extract of Uncariae Ramulus et Uncus however did not show antihyperlipidemic effect in our experiment.

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