Carvedilol is an antihypertensive and antianginal compound that combines nonselective beta-adrenoceptor blocking and vasodilation properties and is devoid of intrinsic sympathomimetic activity. The purpose of the present study was to evaluate the bioequivalence of two carvedilol tablets, $Dilatrend^{TM}$ (Chong Kun Dang Pharmaceutical Co., Ltd.) and $Carvelol^{TM}$ (Dae Won Pharmaceutical Co., Ltd.), according to the prior and revised guidelines of Korea Food and Drug Administration (KFDA). The carvedilol release from the two carvedilol tablets in vitro was tested using KP VII Apparatus II method with various different kinds of dissolution media (pH 1.2, 4.0, 6.8 buffer solution, water and blend of PSB80 into water). Eighteen normal male volunteers, $24.22{\pm}1.86$ years in age and $64.81{\pm}4.56\;kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After one tablet containing 25 mg of carvedilol was orally administered, blood was taken at predetermined time intervals and the concentrations of carvedilol in serum were determined using HPLC method with fluorescence detector. The dissolution profiles of two carvedilol tablets were very similar at all dissolution media. Besides, the 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 using non-transformed and logarithmically transformed $AUC_t$ and $C_{max}$. The results showed that the differences in $AUC_t$, $C_{max}$ and $T_{max}$ between two tablets based on the $Dilatrend^{TM}$ were 2.23%, -2.00% and 0.00%, respectively. Minimum detectable differences $({\Delta})$ at ${\alpha}=0.05$ and $1-{\beta}=0.8$ were less than 20% (e.g., 13.55% and 17.61% for $AUC_t$ and $C_{max}$, respectively). The powers $(l-{\beta})$ at ${\alpha}=0.05$, ${\Delta}=0.2$ for $AUC_t$ and $C_{max}$ were 98.08% and 88.81%, respectively. The 90% confidence intervals were within ${\pm}20%$ (e.g., $-5.69{\sim}10.16$ and $-12.30{\sim}8.30$ for $AUC_t$ and $C_{max}$, respectively). There were no sequence effect between two tablets in logarithmically transformed $AUC_t$ and $C_{max}$. The 90% confidence intervals using logarithmically transformed were within the acceptance range of log(0.8) to log(1.25) (e.g., $0.95{\sim}1.11$ and $0.89{\sim}1.09$ for $AUC_t$ and $C_{max}$, respectively). Two parameters met the criteria of prior and revised KFDA guideline for bioequivalence, indicating that $Carvelol^{TM}$ tablet is bioequivalent to $Dilatrend^{TM}$ tablet.
In this study, we investigated the antioxidant activities, inhibition activity against ACE (angiotensin converting enzyme) and antitumor activity of extract from Acanthopanax senticosus HARMS fruits for development novel functional resources. In order to understand the factors responsible for the potent antioxidant and antihypertensive ability of fruits in A. senticosus, it has been evaluated for anti-oxidative activity using Fenton's reagent/ethyl linoleate system and for free radical scavenging activity using the l,l-diphenyl-2-picryl hydrazyl free radical generating system. The fruits extract of A. senticosus showed higher antioxidant activities than positive control, ${\alpha}$-tocopherol at all concentrations, while fruits extract of A. senticosus showed same degree of radical scavenging activity with positive control, ${\alpha}$-tocopherol. The ability of fruit extracts from A. senticosus to influence the inhibitory activity of angiotensin converting enzyme (ACE) and xanthine oxidase (XOase) has also been discussed. The activity of growth-inhibitory of fruit extracts of A. senticosus was screened by SRB (sulphorhodamine B) method on diverse cancer cells representing different types of cancers. The fruit extracts of A. senticosus showed moderate inhibition on proliferation of LNCaP and MOLT-4F cells and did not inhibit the proliferation of other cancer cells. The fruit extracts of A. senticosus inhibited the proliferation of cancer cells with $GI_{50}$ values ranging from 5 to $10{\mu}g/mL$. This result revealed that the fruit extracts of A. senticosus was expected to be good candidate for development into source of free radical scavengers, antihypertentive, and anti-tumor agent.
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
/
v.52
no.4
/
pp.447-452
/
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.
Kim, Ji-Young;Kim, Yun-Young;Kim, Hye-Rang;Yun, Sung-Seob;Kim, Wan-Sik;Yea, Hyun-Soo;Chung, Jin-Young;Lee, In-Hoe;Choue, Ryo-Won
Journal of the East Asian Society of Dietary Life
/
v.18
no.6
/
pp.918-926
/
2008
It is well known non-drug therapy for hypertension patients can reduce blood pressure. These types of therapy include maintaining ones ideal body weight, quitting smoking, consuming large amounts of fruits and vegetables consuming low levels of saturated fat and salt and regular exercise. Fermented milk protein derived biologically active peptides such as isoleucine-proline-proline_(IPP) or valine-proline-proline_(VPP) have been shown to lower blood pressure in hypertensive subjects. This study was conducted to investigate the antihypertensive effects of medical nutritional therapy _(MNT) in accordance with the consumption of fermented milk enriched with IPP and VPP. To accomplish this, we conducted a randomized case-controlled study of 43 subjects who had blood pressure levels greater than 120/80 mmHg. The subjects in the study group were randomly allocated into two groups, an MNT + fermented milk (100mL/day) group (n=21) and an MNT+L. helveticus fermented milk with tripeptides (IPP=2.2mg, VPP=2.6mg/100mL) group (n=22). The MNT included weight management, reduction of sodium, total fat and saturated fat intake, increased intake of fruits and vegetables, and increased intake of low fat dairy products. The treatments were administered for 12 weeks during which time no drug interventions were conducted. The daily intakes of total calories, fats, cholesterol and Na decreased significantly after 12 weeks of MNT in the control and the experimental groups. In addition, the systolic blood pressure de creased significantly in the control and experimental groups; however, the diastolic blood pressure only decreased significantly in the experimental group. Overall, the results of this study indicate that the intake of fermented milk containing IPP and VPP in conjunction with MNT exerted positive effects on the blood pressure of pre- and hypertensive subjects.
Jeon, Hyun Joo;Yu, Sun Nyoung;Kim, Sang Hun;Park, Seul Ki;Choi, Hyeun Deok;Kim, Kwang Yeon;Lee, Sun Yi;Chun, Sung Sik;Ahn, Soon Cheo
Journal of Life Science
/
v.24
no.8
/
pp.827-836
/
2014
There is a rising trend in obesity due to various factors, including changes in eating habits, lack of exercise, and genetic and psychological factors. Citrus peel has been reported to prevent obesity via antioxidative, antihypertensive, and LDL cholesterol-lowering effects. This study investigated the effects of citrus peel extract fermented with or without Aspergillus oryzae in a mouse model of diet-induced obesity. The animals were divided into four groups: a high-fat diet group (HFD), a normal fat diet (NFD) group, a citrus peel extract (CP) group, and a citrus peel extract fermented with A. oryzae (CPA) group. The citrus peel extract improved lipid metabolism and weight loss in the high-fat diet-induced obese mouse model. As expected, the body weight was higher in the HFD group compared with the NFD, CP, and CPA groups. However, the concentrations of total cholesterol (TG) and triglyceride (TC) in the serum and liver of the CP and CPA groups were lower than in the HFD group. There were no significant differences in the HDL cholesterol concentration among the groups. Taken together, our results suggest that extract of citrus peel biotransformed with A. oryzae had more antiobesity activity than citrus peel not transformed by A. oryzae through the fermentation of metabolites.
Kim, Jung-Suk;Kim, Mi-Jeong;Park, Min-Hee;Ryu, Bog-Mi;Moon, Gap-Soon
Journal of the Korean Society of Food Science and Nutrition
/
v.37
no.1
/
pp.27-34
/
2008
This study investigated the anti-hypertensive effect of Phyllostachys pubescens culm extract (PCE) by examining its effects on renal angiotensin-converting enzyme (ACE) inhibition and blood pressure using the spontaneously hypertensive rat (SHR) system. Systolic blood pressure (SBP) and diastolic blood pressure (DBP) were measured weekly for 8 weeks. Also, total antioxidant capacity and protein oxidation of tissues were examined by plasma Trolox Equivalent Antioxidant Capacity assay (TEAC) and hepatic protein carbonyl values, respectively. Twenty male SHR were randomly divided into four groups: PCE50, PCE100, and PCE500 (50, 100, and 500 mg of PCE per kilogram bodyweight daily, respectively), and control group. At week 2, the SBP in all PCE groups appeared to be significantly lower than the control (p<0.05), whereas the DBP were not different until week 4 (p<0.05). At week 8, SBP in the PCE500 was lower by 20% than the control. PCE groups considerably suppressed ACE dose-dependently compared with the control. Plasma TEAC and hepatic protein carbonyl values indicated increased antioxidative activity due to the PCE feed. No adverse effect was observed on the liver of SHR as there was no difference for the GOT and GPT values among the groups. Results of this study suggest that ACE inhibition may be one possible mechanism for the blood pressure lowering effect of PCE; thus, long term consumption of PCE may be beneficial in preventing high blood pressure along with the increased antioxidative status.
No, Jae-Duck;Lee, Dae-Hyung;Lee, Dae-Hyoung;Choi, Shin-Yang;Kim, Na-Mi;Lee, Jong-Soo
Journal of the Korean Society of Food Science and Nutrition
/
v.35
no.8
/
pp.1025-1030
/
2006
In other to develop new functional doenjangs, two types of the isolated nuruk doenjangs were prepared with protease and amylase-producing Aspergillus oryzae D-2 and antihyperlipidemia Bacillus subtilis LK-12 and then changes of its quality and physiological functionalities were investigated during 2 months of fermentation and compared with those of the commercial nuruk doenjangs made by commercial Aspergillus oryzae and antihyperlipidemia Bacillus subtilis LK-12. ${\alpha}-Amylase$ activity of the isolated nuruk doenjangs during fermentation were decreased slightly, whereas proteases activities were increased significantly to $1.8{\sim}2.8$ Unit per mL after 1 month of fermentation. These ${\alpha}-amylase$ activities and proteases activities were similar with those of the commercial nuruk doenjangs. Amino-nitrogen content and reducing sugar content of the doenjangs after 2 months of fermentation were approximate $1.63{\sim}1.72\;mg%$ and $0.77{\sim}0.81%$, respectively. Antihypertensive angiotensin-Ⅰ converting enzyme inhibitory activities of the isolated nuruk doenjangs were slightly decreased from $85.6{\sim}87.2%$ to $84.0{\sim}85.1%$ after 2 months of fermentation and the commercial nuruk doenjangs were also significantly decreased from $85.7{\sim}88.0%$ to $69.1{\sim}79.7%$, lower than the isolated nuruk doenjangs. Fibrinolytic activity and HMG-CoA reductase inhibitory activity of the isolated nuruk doenjangs were very low and it were also similar with those of the commercial nuruk doenjangs. Antioxidant activity of the isolated nuruk doenjangs were showed $17{\sim}22%$, lower than that of the commercial nuruk doenjangs $(22{\sim}26%)$.
This study was conducted to investigate the effect of Makgeolli (MG) and Makgeolli GiGemi (MGG) on blood flow, serum lipid improvement in vivo, and inhibition of angiotensin converting enzyme (ACE) in vitro. The activities of serum AST and ALT were increased by ovariectomy. Serum AST levels were decreased to $77.71{\pm}13.97$ and $74.57{\pm}14.90\;unit/ml$ in the OVX-MG50 and OVX-MGG50 groups compared to the OVX-control group ($91.14{\pm}12.02\;unit/ml$). Serum ALT levels were decreased to $34.00{\pm}8.41$ and $30.43{\pm}3.60\;unit/ml$ in OVX-MG50 and OVX-MGG50 groups compared to the OVX-control group ($37.14{\pm}5.40\;unit/ml$). Serum total cholesterol and triglyceride contents decreased in the sham group compared with OVX-control group by ovariectomy. Six weeks feeding of MG and MGG resulted in a decrease to $116.14{\pm}36.02$ and $109.14{\pm}11.55\;mg/dl$ compared to the OVX-control group ($120.43{\pm}8.36\;mg/dl$) in serum total cholesterol, and triglyceride levels were decreased to $52.43{\pm}12.41$ and $47.29{\pm}12.08\;mg/dl$ in the OVX-MG50 and OVX-MGG50 groups compared to the OVX-control group ($58.57{\pm}5.47\;mg/dl$). The level of HDL-cholesterol in the OVX-control group was significantly reduced to $51.29{\pm}20.49\;mg/dl$ compared to the sham group ($72.29{\pm}10.29\;mg/dl$), but it was increased to $70.71{\pm}19.53$ and $62.00{\pm}20.20\;mg/dl$ with MG and MGG supplementation. Furthermore, the effect of the MG group was higher than the MGG group. Microscopic observation showed that whole blood passed smoothly through the micro channels in the MG and MGG supplemented groups. The platelet aggregation ability of the groups treated with MG and MGG was less than that of the OVX-control group. In vitro assay, the angiotensin converting enzyme (ACE) activity was significantly inhibited by MG and MGG (82.6% and 68.9% inhibition at 0.4 g/ml). These results suggest that the beneficial effects of MG and MGG may be used to improve on the lipid metabolic syndrome of menopausal women. In addition, MG and MGG might improve blood homeostasis mediated activities via antiplatelets and MG and MGG may be used as antihypertensive functional foods and nutraceuticals.
The goal of this study was to characterize the quality and physiological functionality of some traditional rice wines in Chungnam province, Korea. Non-sterilized and commercial sterilized traditional rice wines from five traditional rice wine factories of Chungnam province were collected and investigated for nutritional components, noxious compounds and physiological functionality. Ethanol content ranged from 16.1~18.3% and pH ranged from 3.27~4.76, and they also contained 0.15% to 0.55% of total acid. All traditional rice wines contained 10.15~139.9 mg% of amino nitrogen and 2.5~25.7% of total sugar. Among organic acids, lactic acid was contained 7.4~29.6 mg%, and succinic acid and propionic acid was also contained 0.2~2.7 mg% and 0.7~8.3 mg%, respectively. Antihypertensive angiotensin I-converting enzyme inhibitory activity were showed 37.0~86.0% in all rice wines, however, fibrinolytic activity, antioxidant activity, SOD-like activity and acetylcholinesterase inhibitory activity were low or not detected.
Purpose: The health risk of women increases after menopause. This study evaluated the effectiveness of a public health center-based nutrition education program for hypertension in women older than 50 years of age. Methods: The program included 8-week nutrition education and 8-week follow-up with keeping a health diary and nutrition counseling. The program was evaluated three times: before and after the nutrition education, and after the follow-up. The subjects were classified into hypertensives (n = 44) or normotensives (n = 71). Results: The rate of taking antihypertensive drugs in the hypertensive group was 86.4%. The systolic blood pressure decreased in the hypertensive and normotensive groups after nutrition education (p < 0.05). The body weight (p < 0.001), BMI (p < 0.001), waist circumference (p < 0.001), and percent body fat (p < 0.01) were also decreased after nutrition education in both groups. The hypertensive group showed an increase in HDL-cholesterol level (p < 0.001) and decreases in triglycerides (p < 0.01) and LDL-cholesterol (p < 0.05) levels after completion of the program. The normotensive group also displayed significant changes in HDL-cholesterol (p < 0.001) and triglycerides (p < 0.01). The dietary habits and nutrition knowledge on sodium and hypertension were improved in both groups (p < 0.001). The total score of dietary behavior related to the sodium intake was improved in the normotensive group (p < 0.001). The total score of the high sodium dish frequency questionnaire decreased in both groups after nutrition education and completion of the program compared to that before the program. Decreases in the consumption frequencies of noodles, pot stews and stews, Kimchi, and beverages were significant. The total self-efficacy score was increased in both groups by the program (p < 0.001). In particular, the hypertensive group showed improvement in all items. Conclusion: This public health center-based nutrition education program may contribute to the prevention and management of hypertension and chronic diseases in women over 50 years of age.
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