• Title/Summary/Keyword: anti-platelet effects

Search Result 190, Processing Time 0.027 seconds

Comparison of Piperacillin/Tazobactam Dosing (13.5 g/day vs. 18 g/day) for the Treatment of Hospital-Acquired Pneumonia and Ventilator-associated Pneumonia in Intensive Care Unit (중환자실 내 병원성 폐렴 치료를 위한 Piperacillin/Tazobactam의 용량에 따른 효과와 안전성 비교)

  • Kang, Jeung Yun;Lee, Kyung A;Kim, Jae Song;Kim, Soo Hyun;Son, Eun Sun
    • Korean Journal of Clinical Pharmacy
    • /
    • v.28 no.3
    • /
    • pp.167-173
    • /
    • 2018
  • Background: In July 2016, the Infectious diseases society of america and the american thoracic society (IDSA & ATS) published a guideline recommending piperacillin/tazobactam (Pip/Tazo) 18 g/day as the anti-pseudomonal dose for the treatment of pathogenic pneumonia. After the guideline was published, the Pip/Tazo dose used for the treatment of pathogenic pneumonia was changed from 13.5 g/day to 18 g/day in a superior general hospital intensive care unit (ICU). In this study, we analyzed the effectiveness and safety of the new dose. Methods: Adult patients aged ${\geq}19years$ who were diagnosed with pneumonia in ICU and who received Pip/Tazo for 7 days or more from September 1, 2015 to May 31, 2017 were included in the study. The electronic medical record (EMR) was retrospectively analyzed. Results: At baseline, there was a significant difference between 44 patients treated with 13.5 g/day and 31 patients treated with 18 g/day of Pip/Tazo. The 18 g/day-treatment group comprised more elderly patients than the 13.5 g/day-treatment group (p=0.028). The results of the treatment-effects analysis showed no significant difference between the two groups. In case of safety data, there were significant differences in two parameters related to blood count, namely hemoglobin (p=0.016) and platelet count (p=0.011). Conclusion: Based on the significant difference in baseline age, there is a possibility that high-dose Pip/Tazo showed improved therapeutic effect. However, when high-dose Pip/Tazo was used, the blood cell count was found to drop from the reference value more frequently. Therefore, blood cell count should be monitored carefully when high-dose Pip/Tazo is administered.

Pharmacokinetics Interaction between Cardiotonic Pills and Cilostazol in Rats (렛트를 이용한 심적환과 cilostazol에 관한 상호작용 연구)

  • Kim, Ekyune
    • Journal of Life Science
    • /
    • v.26 no.1
    • /
    • pp.123-128
    • /
    • 2016
  • The object of this study was to obtain accurate information about the co-administration effects of cardiotonic pills on the pharmacokinetics of cilostazol were observed as a process of the comprehensive and integrative medicine. Cilostazol is a synthetic anti-platelet and vasodilator agent developed for the treatment of intermittent claudication resulting from peripheral arterial disease. By increasing intracellular cyclic adenosine monophosphate (cAMP), cilostazol induces the activation of protein kinase A, which activates endothelial nitric oxide synthase. In order to evaluate the effect of a single or repeated cardiotonic pill dose on the pharmacokinetics of cilostazol, a single dose of pure_distilled water or a colloidal suspension of distilled water and cardiotonic pills were administered to the control and test groups, respectively. After 30 min, both groups were administered cilostazol. Plasma was collected 30min before administration, and 0.25, 0.5, 0.45, 1, 2, 4, 6, 8, and 24h after the end of cilostazol treatment. We then evaluated the pharmacokinetic changes observed with cilostazol between the control and test groups. No statistically significant differences were observed. These findings demonstrated that a single dose of cardiotonic pills did not affect the pharmacokinetics of cilostazol. The results obtained in this study suggest that co-administration of cardiotonic pills and cilostazol may not affect the bioavailability of cilostazol as a potential drug interaction.

Characterization of Homocysteine ${\gamma}$-Lyase from Submerged and Solid Cultures of Aspergillus fumigatus ASH (JX006238)

  • El-Sayed, Ashraf S.;Khalaf, Salwa A.;Aziz, Hani A.
    • Journal of Microbiology and Biotechnology
    • /
    • v.23 no.4
    • /
    • pp.499-510
    • /
    • 2013
  • Among 25 isolates, Aspergillus fumigatus ASH (JX006238) was identified as a potent producer of homocysteine ${\gamma}$-lyase. The nutritional requirements to maximize the enzyme yield were optimized under submerged (SF) and solid-state fermentation (SSF) conditions, resulting in a 5.2- and 2.3-fold increase, respectively, after the last purification step. The enzyme exhibited a single homogenous band of 50 kDa on SDS-PAGE, along with an optimum pH of 7.8 and pH stability range of 6.5 to 7.8. It also showed a pI of 5.0, as detected by pH precipitation with no glycosyl residues. The highest enzyme activity was obtained at $37-40^{\circ}C$, with a $T_m$ value of $70.1^{\circ}C$. The enzyme showed clear catalytic and thermal stability below $40^{\circ}C$, with $T_{1/2}$ values of 18.1, 9.9, 5.9, 3.3, and 1.9 h at $30^{\circ}C$, $35^{\circ}C$, $40^{\circ}C$, $50^{\circ}C$, and $60^{\circ}C$, respectively. Additionally, the enzyme $K_r$ values were 0.002, 0.054, 0.097, 0.184, and 0.341 $S^{-1}$ at $30^{\circ}C$, $35^{\circ}C$, $40^{\circ}C$, $50^{\circ}C$, and $60^{\circ}C$, respectively. The enzyme displayed a strong affinity to homocysteine, followed by methionine and cysteine when compared with non-S amino acids, confirming its potency against homocysteinuria-related diseases, and as an anti-cardiovascular agent and a specific biosensor for homocysteinuria. The enzyme showed its maximum affinity for homocysteine ($K_m$ 2.46 mM, $K_{cat}\;1.39{\times}10^{-3}\;s^{-1}$), methionine ($K_m$ 4.1 mM, $K_{cat}\;0.97{\times}10^{-3}\;s^{-1}$), and cysteine ($K_m$ 4.9 m M, $K_{cat}\;0.77{\times}10^{-3}\;s^{-1}$). The enzyme was also strongly inhibited by hydroxylamine and DDT, confirming its pyridoxal 5'-phosphate (PLP) identity, yet not inhibited by EDTA. In vivo, using Swiss Albino mice, the enzyme showed no detectable negative effects on platelet aggregation, the RBC number, aspartate aminotransferase, alanine aminotransferase, or creatinine titer when compared with negative controls.

Simultaneous determination and acute toxicity study of Fructus mume extracts in ICR mice (오매(烏梅)의 다성분동시분석 및 마우스를 이용한 경구 단회투여 급성독성시험)

  • Lee, In-Sun;Han, Chang-Hyun;Lee, Chul;Hwang, Bang-Yeon;Jung, Sang-Hyeok;Lee, Young-Joon;Jeon, Won-Kyung
    • Journal of Society of Preventive Korean Medicine
    • /
    • v.15 no.1
    • /
    • pp.37-47
    • /
    • 2011
  • Objectives : Previous studies have shown that Fructus mume (FM) has anti-platelet effects. The present study was performed to determine the acute oral toxicity and quality control of a crude extract of FM in ICR mice. Methods : We investigated the in vivo single dose acute toxicity of FM 95% ethanol extract. This test was orally administered once by gavage to 20 male and 20 female mice at dose levels of 0 (control group), 1250, 2500 and 5000mg/kg body weight, respectively. Mortalities, clinical findings, autopsy findings and body weight changes were monitored daily for the 14 days following the administration. HPLC analysis was performed for the simultaneous determination of ursolic acid and p-hydroxycinnamic acid in FM. Reverse-phase chromatography using a C18 column and photodiode array detection at 211 nm was used for quantification of the two maker components. The mobile phase for gradient elution consists of water and acetonitrile. Results : We observed survival rates, general toxicity, change of body weight, and autopsy. The mice did not die after single oral administration of maximum dose of FM. Autopsy of animal revealed no abnormal gross finding. Therefore, $LD_{50}$ value of FM for ICR mice was more than 5000mg/kg on oral route. The HPLC analysis showed that ursolic acid and p-hydroxycinnamic acid amounts to 9.75- and 0.12% in the extract with the retention times of 47.99- and 15.38 minutes, respectively. Conclusions : These results suggest that no toxic dose level of FM in mice is considered to be more than 5000mg/kg. Consequently, it was concluded that FM have no effect on acute toxicity and side effect in ICR mice. For the quality control of FM extract, simultaneous determination of ursolic acid and p-hydroxycinnamic acid was established.

The co-injection of antioxidants with foot-and-mouth disease vaccination altered growth performance and blood parameters of finishing Holstein steers

  • Seo, Jakyeom;Song, Minho;Jo, Namchul;Kim, Woonsu;Jeong, Sinyong;Kim, Jongnam;Lee, Seyoung;Seo, Seongwon
    • Asian-Australasian Journal of Animal Sciences
    • /
    • v.32 no.6
    • /
    • pp.792-799
    • /
    • 2019
  • Objective: This study was conducted to evaluate whether the co-injection of antioxidants together with foot-and-mouth disease (FMD) vaccination has the potential to attenuate the negative effects caused by vaccination in Holstein finishing steers. Methods: A total of 36 finishing Holstein steers (body weight [BW]: $608{\pm}45.6kg$, 17 months old) were randomly allocated to one of three treatments: i) control (CON, only FMD vaccination without any co-injection), ii) co-injection of commercial non-steroidal anti-inflammatory drugs (NSAID) with FMD vaccination at a ratio of 10:1 (NSAID vol/FMD vaccine vol) as a positive control (PCON), iii) co-injection of commercial mixture of vitamin E and selenium with FMD vaccination (VITESEL) (1 mL of FMD vaccine+1 mL of antioxidants per 90 kg of BW). Changes in growth performance and blood parameters because of treatments were determined. Results: No significant difference in BW, average daily gain, and dry matter intake of the steers was observed among the treatments. The FMD vaccination significantly increased white blood cells (WBC), neutrophils, platelets, and mean platelet volume (p<0.01) in blood analysis. The count of lymphocyte tended to increase after vaccination (p = 0.08). In blood analysis, steers in VITESEL tended to have higher numbers of WBC, neutrophils, and platelets compared to that of other treatments (p = 0.09, 0.06, and 0.09, respectively). Eosinophils in VITESEL were higher than those in PCON (p<0.01). Among blood metabolites, blood urea nitrogen and aspartate transaminase were significantly increased, but cholesterol, alanine transferase, inorganic phosphorus, Mg, and albumin were decreased after FMD vaccination (p<0.01). Conclusion: The use of antioxidants in FMD vaccination did not attenuate growth disturbance because of FMD vaccination. The metabolic changes induced by vaccination were not controlled by the administration of antioxidants. The protective function of antioxidants was effective mainly on the cell counts of leukocytes.

Evaluation of in-vitro Antithrombosis Activity of Lees of Korean Traditional Wine (전통주 주박의 항혈전 활성 평가)

  • Kim, Mi-Sun;Lee, Ye-Seul;Kim, Jong Sik;Shin, Woo-Chang;Sohn, Ho-Yong
    • Journal of Life Science
    • /
    • v.24 no.8
    • /
    • pp.865-872
    • /
    • 2014
  • In this study, ethanol and hot water extracts of lees from Korean traditional wine (J-B, J-S, J-Y, J-H, and J-W) were prepared, and their effects on blood coagulation, platelet aggregation, and hemolysis of human red blood cells (hRBCs) were investigated to develop functional food ingredients from lees. The pH and brix of the lees ranged from 3.90 to 4.29 and 5.0 to $27.0^{\circ}$, respectively, and there was a huge difference in the water and ethanol content among the lees. The nuruk and additives used affected the color and physicochemical properties of lees. The J-W takju made from only rice and traditional nuruk, which has $13^{\circ}$ brix and 1.8% of alcohol, has potential as functional food ingredient. With regard to the extraction yields of lees, higher yields were obtained from J-H, which contains different medicinal plants, in ethanol, followed by J-W, J-B, J-S, and J-Y. Higher extraction yields of lees were obtained from J-S in hot water, followed by J-B, J-W, J-H, and J-Y, respectively. The ethanol extract of J-H and the hot water extract of J-Y had the highest contents of total polyphenol and total flavonoids among the lees extracts. The 10 lees extracts did not show hemolysis activity against hRBCs up to 5 mg/ml. In an anticoagulation activity assay, the ethanol extracts of three yakju lees (J-B, J-S, and J-Y) and the hot water extract of J-W inhibited thrombin activity, whereas the hot water extract of J-B, J-S, and J-H inhibited blood coagulation factors. In an antiplatelet aggregation activity assay, only the J-W takju lees showed significant inhibition activity. Our results suggest that lees from traditional wine had high potential as a novel antithrombosis agent.

Protective effects of quality certified traditional Doenjang in Korea on TNF-α-induced vascular inflammation in human umbilical vein endothelial cells (혈관내피세포에서 TNF-α 자극에 의해 유도되는 혈관염증에 대한 전통식품 품질인증 된장의 효능 평가)

  • Kim, Eun-Ju;Jang, Yeon-Jeong;Kim, So-Young;Choi, Hye-Sun;Park, Shin-Young
    • Food Science and Preservation
    • /
    • v.23 no.3
    • /
    • pp.378-386
    • /
    • 2016
  • Anti-atherogenic effects in tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$)-stimulated human umbilical vein endothelial cells (HUVEC) are involved in the suppression of oxidative stress, cell adhesion molecules, and pro-inflammatory factors. This study investigated the vascular inflammation inhibitory activity of traditional Doenjang plays a key role in the pathogenesis and progression of atherosclerosis. The protective effects of Korean Deonjang was investigated on the expression of cell adhesion molecules (CAMs) in tumor necrosis factor (TNF)-${\alpha}$-induced human umbilical vascular endothelial cells (HUVECs). Deonjang extracts (20, 50, $100{\mu}g/mL$) decreased the expression of 20 ng/mL TNF-${\alpha}$-induced vascular cell adhesion molecule (VCAM)-1 intracellular adhesion molecule (ICAM)-1 proteins, and their corresponding mRNA levels. Nitric oxides (NO) produced by endothlial nitric oxides synthase (eNOS) dilated blood vessels, which had protective effects against platelet and leukocyte adhesion. While TNF-${\alpha}$-induced suppressed the production of nitric oxide in HUVECs, Doenjang restored NO production in HUVECs. In addition, Deonjang reduced the TNF-${\alpha}$-induced expression of inducible NO synthase (iNOS) and cyclooxygenase (COX)-2 mRNA levels. These results suggested that Doenjang can inhibited the production of cell adhesion molecules and inflammatory mediators, which could be a potential candidate for preventing atherosclerosis.

The Ability of Anti-tumor Necrosis Factor Alpha(TNF-${\alpha}$) Antibodies Produced in Sheep Colostrums

  • Yun, Sung-Seob
    • 한국유가공학회:학술대회논문집
    • /
    • 2007.09a
    • /
    • pp.49-58
    • /
    • 2007
  • Inflammatory process leads to the well-known mucosal damage and therefore a further disturbance of the epithelial barrier function, resulting abnormal intestinal wall function, even further accelerating the inflammatory process[1]. Despite of the records, etiology and pathogenesis of IBD remain rather unclear. There are many studies over the past couple of years have led to great advanced in understanding the inflammatory bowel disease(IBD) and their underlying pathophysiologic mechanisms. From the current understanding, it is likely that chronic inflammation in IBD is due to aggressive cellular immune responses including increased serum concentrations of different cytokines. Therefore, targeted molecules can be specifically eliminated in their expression directly on the transcriptional level. Interesting therapeutic trials are expected against adhesion molecules and pro-inflammatory cytokines such as TNF-${\alpha}$. The future development of immune therapies in IBD therefore holds great promises for better treatment modalities of IBD but will also open important new insights into a further understanding of inflammation pathophysiology. Treatment of cytokine inhibitors such as Immunex(Enbrel) and J&J/Centocor(Remicade) which are mouse-derived monoclonal antibodies have been shown in several studies to modulate the symptoms of patients, however, theses TNF inhibitors also have an adverse effect immune-related problems and also are costly and must be administered by injection. Because of the eventual development of unwanted side effects, these two products are used in only a select patient population. The present study was performed to elucidate the ability of TNF-${\alpha}$ antibodies produced in sheep colostrums to neutralize TNF-${\alpha}$ action in a cell-based bioassay and in a small animal model of intestinal inflammation. In vitro study, inhibitory effect of anti-TNF-${\alpha}$ antibody from the sheep was determined by cell bioassay. The antibody from the sheep at 1 in 10,000 dilution was able to completely inhibit TNF-${\alpha}$ activity in the cell bioassay. The antibodies from the same sheep, but different milkings, exhibited some variability in inhibition of TNF-${\alpha}$ activity, but were all greater than the control sample. In vivo study, the degree of inflammation was severe to experiment, despite of the initial pilot trial, main trial 1 was unable to figure out of any effect of antibody to reduce the impact of PAF and LPS. Main rat trial 2 resulted no significant symptoms like characteristic acute diarrhea and weight loss of colitis. This study suggested that colostrums from sheep immunized against TNF-${\alpha}$ significantly inhibited TNF-${\alpha}$ bioactivity in the cell based assay. And the higher than anticipated variability in the two animal models precluded assessment of the ability of antibody to prevent TNF-${\alpha}$ induced intestinal damage in the intact animal. Further study will require to find out an alternative animal model, which is more acceptable to test anti-TNF-${\alpha}$ IgA therapy for reducing the impact of inflammation on gut dysfunction. And subsequent pre-clinical and clinical testing also need generation of more antibody as current supplies are low.

  • PDF

Ototoxic Evaluation of Cis-platinum (Cis-Platinum의 이중독증에 관한 임상적 고찰)

  • 홍원표;정명현;오혜경;이경재
    • Proceedings of the KOR-BRONCHOESO Conference
    • /
    • 1982.05a
    • /
    • pp.17.1-17
    • /
    • 1982
  • In 1965, Rosenberg reported that platinum compounds not only inhibit growth and cell division of E. coli but also has anti-tumor activity. Since then, through animal and clinical experiments by Welsch(1971), Speer(1972), Rossof(1972), Hill(1974), and Wittes(1975), it was proved that Cis-platinum has excellent supressive effects on malignant tumor, especially on head and neck cancer. Accordingly, Cis-platinum is now widely used, sometimes without any other durg, or sometimes with Bleomycin and Methotrexate etc. Inspite of the strong anticancer effect, the use of Cis-platinum is quite often discouraged because of the reports that Cis-platinum causes auditory impairment at high frequencies above the speech range due to inner ear damage and irreversible change in the renal tubules. Since Kohonen et al(1965), Standnicki et al(1974) reported that Cisplatinum has toxic effects at the basal turn of the cochlea using guinea pig, many studies on ototoxicity after infusion of Cis-platinum have been carried out using animals. But the studies on ototoxicity in human beings can hardly be found except in reports by Piel et al(1974) and Hong et al (1979). So the authors did a study which tried to clarify the ototoxic effect by comparing the hearing level after infusion of Cis-plastinum with the hearing level before infusion of Cis-plastinum in 30 patients who was treated with Cis-platinum and admitted to the dept. of otolaryngology of Yonsei University Hospital during 2 years and a half from July. 1979 to March. 1982 and the following results were obtained. 1) The results of auditory evaluation, using the pure tone average, hearing loss of 4kHz and 8kHz, Speech Reception Threshold, PB score, SISI showed that the difference of dosage does not change the hearing level after infusion of Cis-platinum and before infusion of Cis-platinum. 2) Cis-platinum had no effect on the hearing level of patients with conductive hearing loss, or with sensorineural hearing loss, as well as with normal hearing level. 3) The infusion of Cis-platinum did not cause any change in creatinine clearance, creatinine, uric acid, but only one case showed that Cis-platinum caused severe nephrotoxicity. 4) The infusion of Cis-plastinum did not cause any change in hemoglobin, leukocyte count, platelet count and there was no correlation with the amount of infusion. 5) To see the side effect of hydration practiced with the infusion of Cis-platinum, the electrolytes, particularly the K level in the serum was measured. But the results did not show any change. 6) Judging from the results of this study mentioned above, ototoxicity caused by infusion of Cis-platinum can be prevented by sufficient hydration. Also the results might say that the appropriate method of infusion of Cis-platinum might be effective in the patients with head and neck cancer who had sensorineural hearing loss for whom the infusion of Cis-platinum has been absolutely cotraindicated.

  • PDF

The Comparative Understanding between Red Ginseng and White Ginsengs, Processed Ginsengs (Panax ginseng C. A. Meyer) (홍삼과 백삼의 비교 고찰)

  • Nam, Ki-Yeul
    • Journal of Ginseng Research
    • /
    • v.29 no.1
    • /
    • pp.1-18
    • /
    • 2005
  • Ginseng Radix, the root of Panax ginseng C. A. Meyer has been used in Eastern Asia for 2000 years as a tonic and restorative, promoting health and longevity. Two varieties are commercially available: white ginseng(Ginseng Radix Alba) is produced by air-drying the root, while red ginseng(Ginseng Radix Rubra) is produced by steaming the root followed by drying. These two varieties of different processing have somewhat differences by heat processing between them. During the heat processing for preparing red ginseng, it has been found to exhibit inactivation of catabolic enzymes, thereby preventing deterioration of ginseng quality and the increased antioxidant-like substances which inhibit lipid peroxide formation, and also good gastro-intestinal absorption by gelatinization of starch. Moreover, studies of changes in ginsenosides composition due to different processing of ginseng roots have been undertaken. The results obtained showed that red ginseng differ from white ginseng due to the lack of acidic malonyl-ginsenosides. The heating procedure in red ginseng was proved to degrade the thermally unstable malonyl-ginsenoside into corresponding netural ginsenosides. Also the steaming process of red ginseng causes degradation or transformation of neutral ginsenosides. Ginsenosides $Rh_2,\;Rh_4,\;Rs_3,\;Rs_4\;and\;Rg_5$, found only in red ginseng, have been known to be hydrolyzed products derived from original saponin by heat processing, responsible for inhibitory effects on the growth of cancer cells through the induction of apoptosis. 20(S)-ginsenoside $Rg_3$ was also formed in red ginseng and was shown to exhibit vasorelaxation properties, antimetastatic activities, and anti-platelet aggregation activity. Recently, steamed red ginseng at high temperature was shown to provide enhance the yield of ginsenosides $Rg_3\;and\;Rg_5$ characteristic of red ginseng Additionally, one of non-saponin constituents, panaxytriol, was found to be structually transformed from polyacetylenic alcohol(panaxydol) showing cytotoxicity during the preparation of red ginseng and also maltol, antioxidant maillard product, from maltose and arginyl-fructosyl-glucose, amino acid derivative, from arginine and maltose. In regard to the in vitro and in vivo comparative biological activities, red ginseng was reported to show more potent activities on the antioxidant effect, anticarcinogenic effect and ameliorative effect on blood circulation than those of white ginseng. In oriental medicine, the ability of red ginseng to supplement the vacancy(허) was known to be relatively stronger than that of white ginseng, but very few are known on its comparative clinical studies. Further investigation on the preclinical and clinical experiments are needed to show the differences of indications and efficacies between red and white ginsengs on the basis of oriental medicines.