• Title/Summary/Keyword: SHR

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Antihypertensive Effects of Enantiomers of Amlodipine Camsylate, a Novel Salt of Amlodipine

  • Oh, Kwang-Seok;Kim, Maeng-Sup;Lee, Byung-Ho
    • Biomolecules & Therapeutics
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    • v.15 no.1
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    • pp.40-45
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    • 2007
  • The vascular relaxant effects on isolated rat aorta of amlodipine camsylates (S-, R-enantiomer, and R/S-racemate), were evaluated and compared with that of S-amlodipine besylate. Furthermore, antihypertensive effects were measured in spontaneously hypertensive rat (SHR). The S-amlodipine camsylate concentration-dependently inhibited $Ca^{2+}$-induced contraction of rat aorta with a very slow onset of action (reached its maximum at 3.5h; $ED_{50}:\;1.50\;{\pm}\;0.24$ nM), having a potency 2-fold higher than those of R/S-amlodipine camsylate $(ED_{50}:\;3.36\;{\pm}\;0.91\;nM)$ and similar to those of S-amlodipine besylate $(ED_{50}:\;1.44\;{\pm}\;0.14\;nM)$, whereas the R-amlodipine camsylate has 590-fold lower vasorelaxant activity $(ED_{50}:\;886.4\;{\pm}\;49.7\;nM)$. In SHR, orally administered S-amlodipine camsylate produced a dose-dependent and long-lasting (>>10 h) antihypertensive effect $(ED_{20}:\;0.89\;mg/kg)$, with a potency 2-fold higher than those of R/S-amlodipine camsylate $(ED_{20}:\;1.82\;mg/kg)$ and similar to those of S-amlodipine besylate $(ED_{20}:\;0.71\;mg/kg)$. In contrast, the R-amlodipine camsylate has no effect even-though administrated high concentration 10 mg/kg. These results suggest that S-amlodipine camsylate has the potency and long-lasting antihypertensive activity as single enantiomer drug, and its antihypertensive effect is not significantly different to that of S-amlodipine besylate.

Study on pharmacological activities of the roots of Cicorium intibus

  • Yim, Dong-sool;Kim, Kwang-sub;Cheong, Jae-hoon;Lee, Sook-yeun
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1997.04a
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    • pp.74-74
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    • 1997
  • Chicory is used popularly. We use leaves of the plant as ordinary mea1, and roots as a substitute of tea materials. It also has been asserted that it has clinical effects on weakness, hepatic disease, diabetes, etc. However, experimental evidences are so insufficient that we started these studies. For antiinflammatory activity, MeOH Ex. was orally administered to rats, and decreased amounts of paw edema induced by carrageenan injection were measured. For bile secretion increament, rats were administered total MeOH, EtOAc fraction, and BuOH fraction Ex. respectively. One hour later, bile ducts were cannulated, and we collected bile every 20 minutes for 4 hours. For hepatoprotective activity, CCl$_4$-intoxicated mouse were treated with MeOH Ex., then s-GPT, S-GOT, and liver weight were measured. For antidiabetic activity, rats were induced diabetes by streptozocin 45mg/kg(i.v) injection. One week later, 1000mg/kg of total MeOH Ex. of chicory root was orally administered. We divided rats into three groups. Group 1 rats were administered only once, group 2 ones once a day for one week, and group 3 ones for three weeks. The concentrations of serum glucose were measured before and after administration. For antihypertensive activity, SHR were administrated total MeOH Ex. of chicory once a day for 8 days, and were measured blood pressure on 1st, 3rd, 6th and 8th day. Total MeOH, EtOAc fraction, and BuOH fraction Ex. increased bile secretion in rats, and decreased liver toxicity induced by CCl$_4$ in mouse. Total MeOH, Ex. of chicory roots has antiinflammatory effect, and decreased blood glucose concentration in group 2 and 3 rats. It was revealed not lowering blood pressure significantly in SHR.

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Effects of the Korean Mistletoe Hot-Water Extract on the Lipid Components and Blood Pressure Level in Spontaneously Hypertensive Rats (한국산 겨우살이 열수추출액이 본태성 고혈압쥐의 지질성분 및 혈압 저하에 미치는 영향)

  • Kim, Han-Soo
    • Korean Journal of Pharmacognosy
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    • v.37 no.3
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    • pp.169-176
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    • 2006
  • This study was designed to observe the effects of Korean mistletoe(Viscum album L. var. coloratum Ohwi) hot-water extract administration on the improvement on the lipid components, apolipoprotein and blood pressure level in spontaneously hypertensive rats (SHR, Wistar strain, male) fed the experimental diets for 33 days. Concentrations of total cholesterol, triglyceride (TG), LDL-cholesterol, free cholesterol and atheroscieotic index in serum were significantly lower in the Korean mistletoe extract administration group [group KM(Korean mistletoe 10.0 g% hot-water extract)] than those in the control group. In the ratio of HDL-cholesterol concentration Korean mistletoe 10.0% hot-water extract administration group were higher percentage than in the control group. However, concentrations of total cholesterol and TG in liver and brain were significantly lower in the group KM than those in the control group. But the components of apolipoprotein (Apo) A-I and Apo A-II in serum were significantly higher in the KM group than in the control group. However, components of Apo C-II, Apo C-III, Apo E and ratio of Apo B to Apo A-I in serum were fairly reduced in the group KM than in the control group. The levels of systolic and diastolic blood pressure were significantly lower in KM cup than control group. From these results, Korean mistletoe hot-water extract administration were effective on the improvement of the lipid components, coronary heart disease and hypertension in spontaneously hypertensive rats. And particularly, Korean mistletoe extract administration were more effective as a therapeutic regimen for the control of blood pressure in hypertension.

Experimental study on the effects of Guibitanggamibang on blood pressure and hyperlipidemia (귀비탕가미방(歸脾湯加味方)이 고혈압(高血壓) 및 고지혈증(高脂血症)에 미치는 영향(影響))

  • Roh, Jin-Hwan;Moon, Sang-Kwan;Ko, Chang-Nam;Cho, Ki-Ho;Kim, Young-Suk;Bae, Hyung-Sup;Lee, Kyung-Sup
    • The Journal of Korean Medicine
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    • v.18 no.2
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    • pp.245-266
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    • 1997
  • In order to study the effects of Guibitanggamibang on blood pressure and hyperlipidemia, experimental study were performed on hypertension in normal and SHR rats, and on hyperlipidemia induced by Triton WR-1339 in normal rats. Also the level of total cholesterol, triglyceride, LDL-cholesterol, HDL-cholesterol, phospholipid and transaminase(GOT, GPT) were measured. The results are summarized as follows: 1. After Guibitanggamibang was given to normal rats, the results showed that inhibitory effects on blood pressure and heart beat were not statistically significant. 2. After Guibitanggamibang was given to SHR rats, the results showed that inhibitory effects on blood pressure were statistically significant. 3. In the model of hyperlipidemia induced by 2% cholesterol food, Guibitanggarrubang had significantly-decreasing effects on total cholesterol, triglyceride, HDL-cholesterol, LDL-choleste rol, Transaminase(GOT, GPT) level in serum. 4. In the model of hyperlipidemia induced by Triton WR-1339, Guibitanggamibang had significantly-decreasing effects on total cholesterol, triglyceride, LDL-cholesterol, phospholipid, Transaminase(GOT, GPT) level in serum. 5. In the model of hyperlipidemia induced by Triton WR-1339, Guibitanggamibang had no significant effects on HDL-cholesterol level in serum. These results show that Guibitanggamibang(歸脾湯加味方) has significant inhibitory effects on blood pressure and hyperlipidemia and that it could be clinically applied for hypertension and hyperlipidemia.

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Differential changes of nicotinamide adenine dinucleotide phosphate-diaphorase, neuropeptide Y and vasoactive intestinal peptide in the cerebral cortex of the rat after repeated electroacupuncture

  • Kim, Yong-Suk;Kim, Jong-In;Kim, Chang-Hwan;Yoo, Jin-Hwa;Huh, Young-Buhm
    • Journal of Acupuncture Research
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    • v.22 no.2
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    • pp.13-18
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    • 2005
  • This study was undertaken to investigate the effects of electroacupuncture(EA) on Choksamni(ST36), a well-known acupuncture site, on nicotinamide adenine dinucleotide phosphate-diaphorase(NADPH-d), neuropeptide Y(NPY) and vasoactive intestinal peptide(VIP) in the cerebral cortex of spontaneously hypertensive rats(SHR). EA on Choksamni was applied using 2Hz electrical biphasic pulses of 10min, 3 times a week for a total of 10 sessions. Thereafter we evaluated changes in NADPH-d-positive neurons histochemically and changes in NPY and VIP-positive neurons immunohistochemically. The optical density of NADPH-d-positive neurons in the Choksamni group was significantly lower in all areas of the cerebral cortex than in the control group. However, the optical density of NPY-positive neurons in the Choksamni group was similar to that of the controls in most areas of the cerebral cortex, with the exception of the primary motor and visual cortices. The optical density of VIP-positive neurons in the Choksamni group was significantly decreased as compared to the control group in most areas of the cerebral cortex, with the exception of the cingulate cortex. The present results demonstrated that EA on Choksamni changes the activity of the NO system, and that stimulation at the same level, causes selective changes within the peptidergic system in the cerebral cortex of SHR.

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Comparison of Some Characteristics Relevant to Rice Bread made from Eight Varieties of Endosperm Mutants between Dry and Wet Milling Process (제분방법을 달리하여 제조한 8품종 변이체벼의 쌀빵가공성 비교)

  • Kang, Mi-Young;Han, Ji-Yeun
    • Korean Journal of Food Science and Technology
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    • v.32 no.1
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    • pp.75-81
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    • 2000
  • The processing properties for rice bread were examined using eight kinds of endosperm mutant rice. The varietal differences among eight kinds of endosperm mutant rice having the respective sugar contents and amylose contents were studied. The water absorptions of these eight cultivars were observed to have significant differences among the cultivars, revealing the water absorption ability of Shrunken(shr.) was 61.5%, and that of Punchilmi(fl) was 48.4%. In addition, the experiments using Whachungbyeo, Nampungbyeo and their mutant cultivars showed that the maximum water absorption was tend to be negatively correlated with the amylose content of each rice cultivars. This study also showed that the rice breads made by dry-milling was better in shape, mechanical properties(hardness, springiness, adhesiveness, chewiness) and texture tested using sensory evaluation than that made by wet-milling.

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Experimental study on the effects of Boyanghwanoh-tang(補陽還五湯) on blood pressure and hyperlipidemia (고혈압(高血壓) 및 고지혈증(高脂血症)에 대(對)한 보양환오탕(補陽還五湯)의 실험적(實驗的) 연구(硏究))

  • Jung, Woo-Sang;Ko, Chang-Nam;Cho, Ki-Ho;Kim, Young-Suk;Bae, Hyung-Sup;Lee, Kyung-Sup
    • The Journal of Internal Korean Medicine
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    • v.18 no.2
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    • pp.246-267
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    • 1997
  • In order to study the effects of Boyanghwanoh-tang(補陽還五湯) on blood pressure and hyperlipidemia, experimental study was performed on Hypertension in normal rats, SHR, and on Hyperlipidemia induced by Triton WR-1339 and 2% cholesterol Fed-diet in normal rats. Also the level of Total cholesterol, Triglyceride, LDL-cholesterol, HDL-cholesterol, Phospholipid were measured. The results are summarized as follows : 1. After Boyanghwanoh-tang(補陽還五湯) was given to normal rats and SHR, the results showed that inhibitory effects on blood pressure were not significant but exitory effects on heart beat were significant. 2. In the model of hyperlipidemia Rats induced by 2% Cholesterol Fed-Diet, Boyanghwanoh-tang(補陽還五湯) had significantly decreasing effects on Total cholesterol, Triglyceride, LDL-cholesterol, Phospholipid level in serum but no significantly increasing effects on HDL-cholesterol level in serum. 3. In the model of hyperlipidemia Rats induced by Triton WR-1339, Boyanghwanoh-tang(補陽還五湯) had significantly decreasing effects on LDL-cholesterol, Phospholipid level in serum and significantly increasing effects on HDL-cholesterol level in serum but there were not significantly decreasing effects on Total cholesterol, Triglyceride. These results show that Boyanghwanoh-tang(補陽還五湯) has significantly inhibitory effects on hyperlipidemia and thal it could be clinically applied for hyperlipidemia.

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Effect of Bangpoongtongsungsan on the Hypertention induced by L-NAME injection and SHR in Rats (방풍통성산(防風通聖散)이 L-NAME 유발 및 SHR 흰쥐의 고혈압에 미치는 영향)

  • Lee, Young-Hwa;Kim, Kyung-Chul;Lee, Yong-Tae
    • Journal of Oriental Physiology
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    • v.14 no.2 s.20
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    • pp.43-54
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    • 1999
  • In order to get the effect of Bangpoongtongsungsan (BPS) water extract on the blood pressure of every 5 group of rats (in normal state of after 3 hours of unanesthetized) was measured and following results were obtained. 1. BPS intraperitoneal injection was not recognized as having the effect of decreasing blood pressure compared with Control on hypertension induced by L-NAME in young rats. 2. BPS oral administration was recognized as having the effect of decreasing blood pressure compared with Control on hypertension induced by L-NAME in young rats. 3. BPS oral administration was recognized as having the effect of decreasing blood pressure compared with Control on hypertension induced by L-NAME's continual injection and BPS continual oral administration in young rats. 4. BPS oral administration was recognized as having the effect of decreasing blood pressure compared with Control on hypertension induced by L-NAME's in adult rats. 5. BPS oral administration was not recognized as having the effect of decreasing blood pressure compared with Control on spontaneous hypertension rats. According to the above results. it is known that BPS extract oral administration decreased the blood pressure of hypertension induced by and more effective to the youth.

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Epistatic Relationships among Genes Related to Endosperm Starch Synthesis in Rice

  • Lee, Joohyun;Koh, Hee-jong
    • Korean Journal of Breeding Science
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    • v.42 no.2
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    • pp.151-156
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    • 2010
  • The mutants of sugary-2 (su-2), floury (flo), shrunken-1 (shr-1), and dull-1 (du-1) were crossed to waxy (wx) to produce $F_2$ seeds. Chi-square analysis on the segregating ratio of the $F_2$ seeds revealed that flo, su-2, and shr-1 were independently transmitted with wx, while wx was epistatic over du-1. The floury and sugary-2 were crossed to Hwasunchalbyeo, a waxy variety, and then the $F_4$ of floury-waxy and sugary-2-waxy seeds were developed, respectively. As the parents phenotypes of sugary-2 and floury, the grains of these two lines showed lower hardness and grain weight than normal grain of Hwacheongbyeo. For alkali digestive value (AVD), the sugary-2-waxy showed lower ADV than Hwacheongbyeo. For the gel consistency of grain flours, the floury was medium like Hwacheongbyeo, while those of the sugary-2, floury-waxy, and sugary-2-waxy were soft like Hwasunchalbyeo. The amylose contents in the grains of the sugary-2 and floury were decreased to ~15% whereas that of Hwacheongbyeo was 19.1%. All the lines showing waxy endosperm (Hwasunchalbyeo, floury-waxy, and sugary-2-waxy) showed less than 4% amylose contents. Interestingly, the free sugar content in the brown rice was increased to 9.27% in the sugary-2-waxy, showing transgressive segregation phenomenon where the free sugar contents in its parents, sugary-2 and Hwasunchalbyeo, were 5.98% and 3.98% respectively. Also, the floury-waxy showed transgressive segregation phenomenon, containing 6.15% of free sugar content in the grains.

Changes of Bax, Bcl-2, CCR-2, MCP-1, and TGF-β1 genes in the left ventricle of spontaneously hypertensive rat after losartan treatment

  • Lee, Hyeryon;Kim, Kwan Chang;Hong, Young Mi
    • Clinical and Experimental Pediatrics
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    • v.62 no.3
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    • pp.95-101
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    • 2019
  • Purpose: Increased apoptosis was recently found in the hypertrophied left ventricle of spontaneously hypertensive rats (SHRs). Although the available evidence suggests that apoptosis can be induced in cardiac cells by various insults including pressure overload, cardiac apoptosis appears to result from an exaggerated local production of angiotensin in adult SHRs. Altered expressions of Bcl associated X (Bax), Bcl-2, chemokine receptor (CCR)-2, monocyte chemoattractant protein (MCP)-1, transforming growth factor $(TGF)-{\beta}1$, phosphorylated extracellular signal-regulated kinases (PERK), and connexin 43 proteins, and kallikrein mRNA were investigated to explore the effects of losartan on the SHR model. Methods: Twelve-week-old male rats were grouped as follows: control (C), SHR (hypertension: H), and losartan (L; SHRs were treated with losartan [10 mg/kg/day] for 5 weeks). Western blot and reverse transcription polymerase chain reaction assays were performed. Results: Expression of Bax, CCR-2, MCP-1, $TGF-{\beta}1$, PERK, and connexin 43 proteins, and kallikrein mRNA was significantly increased in the H group compared to that in the C group at weeks 3 and 5. Expression of Bax, CCR-2, MCP-1, $TGF-{\beta}1$, and connexin 43 proteins and kallikrein mRNA was significantly decreased after losartan treatment at week 5. PERK protein expression was significantly decreased after losartan treatment at weeks 3 and 5. Bcl-2 protein expression was significantly decreased in the H group compared to that in the C group at weeks 3 and 5. Conclusion: Losartan treatment reduced expression of Bax, CCR-2, MCP-1, $TGF-{\beta}1$, PERK, and connexin 43 proteins, and kallikrein mRNA in SHRs, along with decreased inflammation and apoptosis.