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Screening of Nine Herbs with Biological Activities on ACE Inhibition, HMG-CoA Reductase Inhibition, and Fibrinolysis (9종의 허브류로부터 ACE 저해활성, HMG-CoA reductase 저해활성 및 혈전용해활성에 대한 검색)

  • Kwon, Eun-Kyung;Kim, Young-Eon;Lee, Chang-Ho;Kim, Hae-Yeong
    • Korean Journal of Food Science and Technology
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    • v.38 no.5
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    • pp.691-698
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    • 2006
  • The purpose of this study was to investigate how herb extracts may improve blood circulation. Twenty-six extracts from nine different herbs (marjoram, lavender, dill, rosemary, hyssop, rose, lemon balm, pineapple sage, and echinacea) were evaluated for their anti-hypertensive effects via angiotensin I converting enzyme (ACE) inhibition. Their cholesterol-lowering effects via hydroxy-methyl-glutaryl coenzyme A (HMG-CoA) reductase inhibition and their fibrinolytic activity via fibrin-plate method were also evaluated. Both water extraction of rose flowers and 70% EtOH extraction of pineapple sage leaves effectively reduced the ACE activity with inhibition rates of 133.8% and 91.2%, respectively. Similarly, both water and 70% EtOH extracts of rose flowers strongly inhibited the enzymatic activity of HMG-CoA reductase by 48.9% and 80.5%, respectively. Water and 70% EtOH extracts of rose flowers also showed relatively high fibrinolytic activity. Based on these observations, rose flower extracts can be developed as a functional tool for use in the improvement of blood circulation.

Analytical study of circle tunnel Load considering Dilatancy Effect (Dilatancy 효과를 고려한 원형 터널 이완하중에 대한 해석적 연구)

  • Park, Shin-Young;Han, Heui-Soo
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.21 no.9
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    • pp.626-633
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    • 2020
  • This study examined the behavior of the ground by comparing the methods using the results of the Terzaghi formula and the ground investigation data and method considering the dilatancy effect for a circular tunnel using the finite element method. In the case of the Terzaghi formula, the tunnel load can be overestimated and cause overdesign. The method using the results of the ground investigation data cannot be applied when a reasonable coefficient of earth pressure is not determined. This is because it behaves completely differently from the actual behavior, and unexpected problems can occur. In the case of the method considering the dilatancy effect, however, both the strength enhancement effect can be considered through the dilatancy angle and relative density. Therefore, the tunnel load was calculated most reasonably using the method considering dilatancy. Finite element analysis using the geotechnical survey results showed that the tensile stress acts at the top of the tunnel when the upper soil of the tunnel is shallow. On the other hand, additional verification is necessary, such as a comparison with the field measurement results. Through additional research, if normalized, the tunnel load can be calculated reasonably at the time of tunnel design, and safe and economical design is possible.

Bioequivalence of Cardil Tablet to Cardura Tablet (Doxazosin 2 mg) (카두라 정(독사조신 2 mg)에 대한 카르딜 정의 생물학적 동등성)

  • Cho, Hea-Young;Kim, Soo-Jin;Shim, Young-Sun;Lim, Dong-Koo;Oh, In-Joon;Moon, Jai-Dong;Lee, Yong-Bok
    • Journal of Pharmaceutical Investigation
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    • v.30 no.1
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    • pp.61-65
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    • 2000
  • Doxazosin, a postsynaptic selective ${\alpha}1-adrenoceptor$ antagonist, is a potent antihypertensive agent which reduces peripheral resistance and blood pressure by vasodilatation of peripheral vessels. It is also used in the treatment of urinary obstruction by benign prostatic hypertrophy. The purpose of the present study was to evaluate the bioequivalence of two doxazosin tablets, $Cardura^{TM}$ (Pfizer Korea Ltd.) and $Cardil^{TM};$ (Kyungdong Pharmaceutical Co., Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). Sixteen normal male volunteers, $24.19{\pm}2.48$ years in age and $62.41{\pm}6.66$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After one tablet containing 2 mg of doxazosin was orally administered, blood was taken at predetermined time intervals and the concentrations of doxazosin in serum were determined with an HPLC method using spectrofluorometric detector. Pharmacokinetic parameters such as $AUC_t,\;C_{max}\;and\;T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters. The results showed that the differences in $AUC_t,\;C_{max}\;and\;T_{max}$ between two tablets were -1.54%, -1.51 % and 3.42%, respectively, when calculated against the $Cardura^{TM}$ tablet. The powers $(1-{\beta})$ for $AUC_t,\;C_{max}\;and\;T_{max}$ were all more than 99.00%. Minimum detectable differences $(\Delta)$ at ${\alpha}=0.05\;and\;1-{\beta}=0.8$ were all less than 20% (e.g., 12.73%, 12.84% and 13.01% for $AUC_t,\;C_{max}\;and\;T_{max}$, respectively). The 90% confidence intervals were all within :${\pm}20%$ (e.g., $-8.97{\sim}5.90,\;-9.01{\sim}6.00\;and\;-4.16{\sim}11.05\;for\;AUC_t,\;C_{max}\;and\;T_{max},\;respectively)$. All of the above para- meters met the criteria of KFDA for bioequivalence, indicating that $Cardil^{TM}$ tablet is bioequivalent to $Cardura^{TM}$ tablet.

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Pharmacological Characterization of KR-31125, a Novel Nonpeptide AT1 Receptor Antagonist (안지오텐신 수용체 길항제 KR-31125의 특성에 관한 연구)

  • Lee, Sung-Hou
    • Journal of Life Science
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    • v.20 no.6
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    • pp.831-837
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    • 2010
  • KR-31125 (2-butyl-5-dimethoxymethyl-6-phenyl-7-methyl-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-3H-imidazo[4,5-b]pyridine) is a potent inhibitor of angiotensin II type 1 ($AT_1$) receptors in human recombinant $AT_1$ receptors and rabbit aorta. These in vitro studies revealed that KR-31125 inhibited specific [$^{125}I$] [$Sar^1$, $Ile^8$]-angiotensin II binding to human recombinant $AT_1$ receptors in a concentration dependent manner with an $IC_{50}$ value of $19.72{\pm}2.65$ nM. However, no interaction with $AT_2$ receptors was detected as displayed by the competition binding of [$^{125}I$] CGP 42112A to human recombinant $AT_2$ receptor. The binding action was also confirmed as a competitive mode that was identical to the previously studied compound, losartan. In addition, KR-31125 caused a nonparallel shift to the right in the concentration response curves to angiotensin II with a 30-80% decrease in the maximum contractile responses ($pK_B$: 7.63). Compared to the previous studies with losartan that showed a parallel right shift in the maximum contractile responses to AII ($pA_2$: 7.59), KR-31125 presented a different mode of action with a similar potency to losartan. These results demonstrate that KR-31125 is a highly potent and $AT_1$ selective angiotensin II receptor antagonist that can be applied to the fields of new diagnostic and research tools with upcoming in vivo study results.

Pharmacological Profile of KR-31125, an Orally Active AT1 Receptor Antagonist (안지오텐신 수용체 리간드 KR-31125의 생체 내 활성에 관한 연구)

  • Lee, Sung-Hou
    • Journal of Life Science
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    • v.20 no.7
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    • pp.969-976
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    • 2010
  • In vivo studies of KR-31125 (2-butyl-5-dimethoxymethyl-6-phenyl-7-methyl-3-[[2'-(1H-tetrazol-5-yl) biphenyl-4-yl]methyl]-3H-imidazo[4,5-b]pyridine) were performed in pithed rats, conscious angiotensin II (AII) challenged normotensive rats, renal hypertensive rats (RHRs) and furosemide-treated beagle dogs. KR-31125 induced a non-parallel right shift in the dose-pressor response curve to AII ($ID_{50}$: 0.095 mg/kg) with a dose-dependent reduction in the maximum responses in pithed rats. Compared to losartan, this antagonistic effect was about 18 times more potent, presenting competitive antagonism. Other agonists such as norepinephrine and vasopressin did not alter the responses induced by KR-31125. Orally administered KR-31125 had no agonistic effect and dose-dependently inhibited the pressor response to AII with a slightly weaker potency ($ID_{50}$: 0.25 and 0.47 mg/kg, respectively) in the AII-challenged normotensive rat model, but with a more rapid onset of action than losartan (time to $E_{max}$: 30 min for KR-31125 and 6 hr for losartan). KR-31125 produced a dose-dependent antihypertensive effect with a higher potency than losartan in RHRs, and these effects were confirmed in furosemide-treated dogs where they presented a dose-dependent and long-lasting (>8 hr) antihypertensive effect with a rapid onset of action (time to $E_{max}$: 2-4 hr), as well as a 20-fold greater potency than losartan. These results suggest that KR-31125 is a potent, orally active $AT_1$ receptor antagonist that can be applied to the development of new diagnostic and research tools as an added exploratory potential of $AT_1$ receptor antagonist.

A study on the child education experiences of married female students who left their children in their home countries for study abroad (모국에 자녀를 둔 기혼 여자유학생의 자녀교육 경험에 관한 연구)

  • Park, Misuk;Kalanova, Dilnoza
    • Asia-pacific Journal of Multimedia Services Convergent with Art, Humanities, and Sociology
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    • v.6 no.10
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    • pp.121-129
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    • 2016
  • The purpose of this study is to explore the child education experiences of married female students who left their children in their home countries. This study consists of two questions. First, what is the meaning of the child in home country for married female students to their foreign student's life? Second, how they do the child education? For this study data was collected from March to May, 2016 through in-depth interviews with 6 married female students who left their children in their home countries to further their studies in Korea. Then, the data was analyzed their cases were analyzed. First, for married female students their children are always in the first place during their life as a foreign student in Korea. Second, their children play a great role in their foreign student life. Third, the child makes them to be exemplary student in their foreign student's life. In addition, children's education is entrusted to those who are raising them in their home country. However, when big decisions have to be made, it is done by the mother. Also, because they feel sorry towards their children they actively reflect the views of the children. Moreover, they often check everything about their children through SNS. Through this study, we expect to less school life's difficulty of foreign married students and it will be helpful material for them to graduate their foreign students' life. The purpose of this study is to explore the child education experiences of married female students who left their children in their home countries.

The Preparation and Physicochemical Properties of Dipalmitoylphosphatidylcholine/Cholesterol/Fluorinated Surfactant Vesicle Incorporated Fatty Acid Salt (불소화지방산염 첨가에 의한 디팔미토일포스파티딜콜린/콜레스테롤/불소화계면활성제 베지클의 제조와 물성 측정 연구)

  • Park, Young Ju;Kwon, Kyung Ok;Kim, Myung Ja
    • Applied Chemistry for Engineering
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    • v.9 no.3
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    • pp.457-461
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    • 1998
  • The vesicle system of DPPC(dipalmitoylphosphaticylcholine)/Chol(Cholesterol) has been modified by incorporating various mole fractions of flourinated surfactant($C_8F_{17}(CH_2)_2OCO-CH_2CH(SO_3Na)COO(CH_2)_2C_8F_{17}$. Sodium bis(1H,1H,2H,2H-heptadecaflurododecyl)-2-sulfosuccinate, FS)/fluorinated fatty acid salt ($C_7F_{15}COONH_4$, ammoniumpentadecaflurooctyrate, FFS), and their physicochemical properties have been investigated in an attempt to enhance the stability of phospholipid vesicle system. The ${\zeta}$-potential measurement by use of Zetamaster sub-micron Particle Electrophoresis Analyzer (Malvern Co.) showed that a charged homogeneous DPPC/Chol/FS vesicle has been formed owing to the incorporated FFS effect on the membrane, playing a role as a cosurfactant in the bilayer between DPPC and FS components. With increase in the concentration of FFS, it was found that the particle size and also surface charge of the DPPC/Chol/FS vesicle decreased. The stability of DPPC/Chol/FS/FFS liposome was found to be enhanced significantly compared to that of DPPC/Chol/FS according to the dispersity change as a function of time. The release rate of dye molecule of Methylene Blue from the DPPC/Chol/FS/FFS vesicle was determined to be slower than that of DPPC/Chol/FS system, and it may be attributed to the increase in microviscosity of the hydrophobic region in the bilayer. The affinfinity of DPPC/Chol/FS/FFS vesicles to albumin was found to be slightly lowered compared to that of DPPC/Chol/FS. Based on these findings, it was confirmed that a more stable and homogeneous vesicle system of DPPC/Chol/FS could be prepared by addition of FFS, acting as a cosurfactant in the aggregate formation.

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Liposome Formation and Active Ingredient Capsulation on the Supercritical Condition (초임계 상태에서 리포좀의 생성 및 약물봉입)

  • Mun, Yong-Jun;Cha, Joo-Hwan;Kim, In-Young
    • Journal of the Korean Applied Science and Technology
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    • v.38 no.6
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    • pp.1687-1698
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    • 2021
  • This study is to produce multiple layers of liposomes in a supercritical state and encapsulates active ingredients in order to stably encapsulate thermodynamically unstable active ingredients. In order to form a liposome in a supercritical state, a mixed surfactant development including vegetable-derived hydrogenated phosphatidyl choline and their delivative, hydrogenated sucrose distearate was synthesized as high purity. It describes a manufacturing method of injecting liquid carbon dioxide into a reactor to create a supercritical state and stirring to produce a giant liposome, and adding and loading genistein and quercetin. The HLB of the mixed lipid complex (SC-Lipid Complex) was 12.50, and multiple layers of liposome vesicles were formed even at very low concentrations. This surfactant had a specific odor with a pale yellow flake, the specific gravity was 0.972, and the acid value was 0.12, indicating that it was synthesized with high purity. As a result of the emulsifying capacity experiment using 20 wt% capric/capric triglyceride and triethylhexanoin using SC-Lipid Complex, it was found to have 96.2% emulsifying power. SC LIPOSOME GENISTEIN was confirmed that a multi-layer liposome vesicle was formed through a transmission electron microscope (Cryo-TEM) for the supercritical liposome encapsulated with genistein. The primary liposome particle size in which genistein was encapsulated was 253.9 nm, and the secondary capsule size was 18.2 ㎛. Using genistein as the standard substance, the encapsulation efficiency of supercritical liposomes was 99.5%, and general liposomes were found to have an efficiency of 93.6%. In addition, the antioxidant activity experiment in which quercetin was sealed was confirmed by the DPPH method, and it was found that the supercritical liposome significantly maintained excellent antioxidant activity. In this study, thermodynamically unstable raw materials were sealed into liposomes without organic solvents in a supercritical state. Based on these results, it is expected that it can be applied to various forms such as highly functional skincare cosmetics, makeup cosmetics, and scalp protection cosmetics.

Monitoring of Pesticide Residues on Herbs and Spices in the Incheon Metropolitan Area (인천 지역에 유통 중인 향신식물 및 향신료가공품 잔류농약 안전성 조사)

  • Yeo, Eun-young;Jung, Seung-Hye;Jang, Jin-Seob;Kwon, Sung-Hee;Park, Byung-Kyu;Lee, Soo-Yeon;Park, Jeong-Eun;Seo, Soon-Jae;Kim, Jung-Im;Kim, Meyong-Hee;Joo, Kwang-Sig;Hur, Myung-Je
    • Journal of Food Hygiene and Safety
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    • v.36 no.1
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    • pp.60-67
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    • 2021
  • In this study we investigated pesticide residues on herbs and spices disrtibuted in the Incheon Metropolitan area. A total of 112 samples were purchased from off-line and on-line markets from January to October 2020. In accordance with the implementation of the Positive List System (PLS), the proper usage of pesticides is now being enforced. It is assumed that unregistered pesticides are being used on herbs and spices due to the low number of registered pesticides in the agricultural industry. Pesticide residue levels were not detected in 99 samples but 11 kinds of pesticides in 6 samples (13 times) exceeded the MRLs. The pesticides that were used in accordance with the PLS were Diazinon, Diethofencarb and Pyridalyl. However, unregistered pesticides were on the herbs and spices. Therefore, it is necessary to educate producers of herbs and spices on the appropriate use of pesticides. It is also necessary to establish MRLs on herbs and spices.