• 제목/요약/키워드: 14-3-$3{\beta}$

검색결과 1,348건 처리시간 0.029초

아세클로페낙(100mg) 제제인 세나펜 정과 에어할 정의 생물학적동등성 평가 (Bioequivalence Evaluation of Senafen Tablet and Airtal Tablet Containing Aceclofenac 100 mg)

  • 박은우;송우헌;차영주;최영욱
    • Biomolecules & Therapeutics
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    • 제6권4호
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    • pp.423-428
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    • 1998
  • Aceclofenac is an orally effective non-steroidal anti-inflammatory agent of the phenylacetic acid derivative. Bioequivalence study of two aceclofenac preparations, the test drug (Senafe $n_{R}$: Daewon Phar-maceutical Company) and the reference drug (Airta $l_{R}$: Daewoong Pharmaceutical Company), was conducted according to the guidelines of Korea Food and Drug Administration (KFDA). Sixteen healthy male volunteers, 24$\pm$4 years old and 63.9$\pm$6.9 kg of body weight in average, were divided randomly into two groups and administered the drug orally at the dose of 100 mg as aceclofenac in a 2$\times$2 crossover study. Plasma concentrations of aceclofenac were monitored by HPLC method for 12 hr after administration. AU $Co_{-12h}$ (area under the plasma concentration-time curve from initial to 12 hr) was calculated by the linear trapezoidal method. $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{msx}$) were compiled directly from the plasma drug concentration-time data. Student's t-test indicated no significant differences between the formulations in these parameters. Analysis of variance (ANOVA) revealed that there are no differences in AU $Co_{12h}$, $C_{max}$ and $T_{max}$ between the formulations. The apparent differences between the formulations were far less than 20% (e.g., 0.25, 0.01 and 7.32 for AU $Co_{-12h}$, $C_{max}$. and $T_{max}$, respectively). Minimum detectable differences (%) between the formulations at $\alpha$=0.05 and 1-$\beta$=0.8 were less than 20% (e.g., 14.65, 12.47 and 15.46 for AU $Co_{-l2h}$, $C_{max}$ and $T_{max}$, respectively). The 90% confidence intervals for these parameters were also within $\pm$ 20% (e.g.,-10.19~10.68, -8.87~8.89 and -3.69~ 18.33 for AU $Co_{-12h}$, $C_{msx}$ and $T_{max}$, respectively). These results satisfy the bioequivalence criteria of KFDA guidelines, indicating that two formulations of aceclofenac are bioequivalent.quivalent.ivalent.ent.t.ent.

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Inhibition of inflammatory responses elicited by urban fine dust particles in keratinocytes and macrophages by diphlorethohydroxycarmalol isolated from a brown alga Ishige okamurae

  • Fernando, I.P. Shanura;Kim, Hyun-Soo;Sanjeewa, K.K. Asanka;Oh, Jae-Young;Jeon, You-Jin;Lee, Won Woo
    • ALGAE
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    • 제32권3호
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    • pp.261-273
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    • 2017
  • Fine dust (FD) particles have become a major contributor to air pollution causing detrimental effects on the respiratory system and skin. Although some studies have investigated the effects of FD on the respiratory system, their possible effects on the skin remain under-explored. We investigated the FD mediated inflammatory responses in keratinocytes, present in the outer layers of skin tissues and the transfer of inflammatory potential to macrophages. We further evaluated the anti-inflammatory effects of the polyphenolic derivative, diphlorethohydroxycarmalol (DPHC) isolated from Ishige okamurae against FD-induced inflammation. Size distribution of FD particles was analyzed by scanning electron microscopy. FD particles induced the production of cyclooxygenase-2, prostaglandin E2 ($PGE_2$), interleukin (IL)-$1{\beta}$, and IL-6 in HaCaT keratinocytes and the expression of nitric oxide (NO), inducible nitric oxide synthases (iNOS), $PGE_2$, tumor necrosis factor-${\alpha}$ expression in RAW 264.7 macrophages. Further, we evaluated the inflammatory potential of the culture medium of inflammation-induced HaCaT cells in RAW 264.7 macrophages and observed a marked increase in the expression of NO, iNOS, $PGE_2$, and proinflammatory cytokines. DPHC treatment markedly attenuated the inflammatory responses, indicating its effectiveness in suppressing a broad range of inflammatory responses. It also showed anti-inflammatory potential in in-vivo experiments using FD-stimulated zebrafish embryos by decreasing NO and reactive oxygen species production, while eventing cell death caused by inflammation.

Lack of Effects of Recombinant Human Bone Morphogenetic Protein-2 on Angiogenesis in Oral Squamous Cell Carcinoma Induced in the Syrian hamster Cheek Pouch

  • Zaid, Khaled Waleed;Nhar, Bander Mossa;Alanazi, Salman Mohammed Ghadeer;Murad, Rashad;Domani, Ahmad;Alhaf, Awadh Jamman
    • Asian Pacific Journal of Cancer Prevention
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    • 제17권7호
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    • pp.3527-3531
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    • 2016
  • Recombinant human bone morphogenetic protein-2 (rhBMP-2 ), a member of the TGF-${\beta}$ family, has been used widely in recent years to regenerate defects of the maxillary and mandible bones. Such defects are sometimes caused by resection of oral squamous cell carcinoma (OSCC) yet the biologic effects of rhBMP-2 on these carcinomas are not fully clear. The objective of this study was to determine histologically whether rhBMP-2 produces adverse effects on angiogenesis during induction of OSCC, a biologic process critical for tumor formation in an experimental model in the buccal pouch of golden Syrian hamsters. Buccal cavities were exposed to painting with 0.5% DMBA in liquid paraffin three times a week for 14 weeks, then biopsies were taken. Division was into 2 groups: a study group of 10 hamsters receiving $0.25{\mu}g/ml$ of rhBMP-2 in the $3^{rd}$ and $6^{th}$ weeks; and a control group of 10 hamsters which did not receive any additional treatment. VEGF expression and microvessel density were measured but no differences were noted between the two groups. According to this study, rh-BMP-2 does not stimulate angiogenesis during induction of OCSSs.

Effects of α-tocopherol on hemolysis and oxidative stress markers on red blood cells in β-thalassemia major

  • Sovira, Nora;Lubis, Munar;Wahidiyat, Pustika Amalia;Suyatna, Franciscus D.;Gatot, Djajadiman;Bardosono, Saptawati;Sadikin, Mohammad
    • Clinical and Experimental Pediatrics
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    • 제63권8호
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    • pp.314-320
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    • 2020
  • Background: The accumulation of unpaired α-globin chains in patients with β-thalassemia major may clinically create ineffective erythropoiesis, hemolysis, and chronic anemia. Multiple blood transfusions and iron overload cause cellular oxidative damage. However, α-tocopherol, an antioxidant, is a potent scavenger of lipid radicals in the membranes of red blood cells (RBCs) of patients with β-thalassemia major. Purpose: To evaluate the effects of α-tocopherol on hemolysis and oxidative stress markers on the RBC membranes of patients with β-thalassemia major. Methods: Forty subjects included in this randomized controlled trial were allocated to the placebo and α-tocopherol groups. Doses of α-tocopherol were based on Institute of Medicine recommendations: 4-8 years old, 200 mg/day; 9-13 years old, 400 mg/day; 14-18 years old, 600 mg/day. Hemolysis, oxidative stress, and antioxidant variables were evaluated before and after 4-week α-tocopherol or placebo treatment, performed before blood transfusions. Results: Significant enhancements in plasma haptoglobin were noted in the α-tocopherol group (3.01 mg/dL; range, 0.60-42.42 mg/dL; P=0.021). However, there was no significant intergroup difference in osmotic fragility test results; hemopexin, malondialdehyde, reduced glutathione (GSH), or oxidized glutathione (GSSG) levels; or GSH/GSSG ratio. Conclusion: Use of α-tocopherol could indirectly improve hemolysis and haptoglobin levels. However, it played no significant role in oxidative stress or as an endogen antioxidant marker in β-thalassemia major.

Purification and Characterization of a New Fibrinolytic Enzyme of Bacillus licheniformis KJ-31, Isolated from Korean Traditional Jeot-gal

  • Hwang, Kyung-Ju;Choi, Kyoung-Hwa;Kim, Myo-Jeong;Park, Cheon-Seok;Cha, Jae-Ho
    • Journal of Microbiology and Biotechnology
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    • 제17권9호
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    • pp.1469-1476
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    • 2007
  • Jeot-gal is a traditional Korean fermented seafood and has long been used for seasoning. We isolated 188 strains from shrimp, anchovy, and yellow corvina Jeot-gal, and screened sixteen strains that showed strong fibrinolytic activities on a fibrin plate. Among those strains, the strain that had the largest halo zone was chosen and identified as Bacillus licheniformis by using 16S rDNA sequencing and an API CHB kit. The fibrinolytic activity of Bacillus licheniformis was characterized and designated as bpKJ-31. The active component of bpKJ-31 was identified as a 37 kDa protein, designated bacillopeptidase F, by internal peptide mapping and N-terminal sequencing. The optimum activity of bpKJ-31 was shown at pH 9 and $40^{\circ}C$, with a chromogenic substrate for plasmin. It had high degrading activity for the $B{\beta}$-chain and $A{\alpha}$-chain of fibrin(ogen), and also acted on thrombin, but not skim milk and casein. The amidolytic activity of bpKJ-31 was inhibited by 1 mM phenylmethanesulfonyl fluoride, but 1 mM EDTA did not affect the enzyme activity, indicating that bpKJ-31 is an alkaline serine protease, like a plasmin. The bpKJ-31 showed approximately 14.3% higher fibrinolytic activity than the plasmin. These features of bpKJ-31 make it attractive as a health-promoting biomaterial.

Expression, Purification, Crystallization and Preliminary X-Ray Crystallographic Analysis of CnrX from Cupriavidus metallidurans CH34

  • Kim, Kook-Han;Jung, Eun-Jung;Im, Ha-Na;Lelie, Daniel Van Der;Kim, Eunice Eun-Kyeong
    • Journal of Microbiology and Biotechnology
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    • 제18권1호
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    • pp.43-47
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    • 2008
  • The nickel and cobalt resistance of Cupriavidus metallidurans CH34 is mediated by the CnrCBA efflux pump encoded by the cnrYHXCBAT metal resistance determinant. The products of the three genes cnrYXH transcriptionally regulate expression of cnr. CnrY and CnrX are membrane-bound proteins, probably functioning as anti-sigma factors, whereas CnrH is a cnr-specific extracytoplasmic functions (ECF) sigma factor. The periplasmic domain of CnrX (residues 29-148) was cloned as a N-terminal His-tagged protein, expressed in Escherichia coli, and purified using affinity chromatography and gel filtration. The molecular mass was estimated to be about 13.6kDa by size exclusion chromatography, corresponding to a monomer. The tetragonal bipyramid crystals were obtained by mixing an equal volume of protein in 50mM Tris-HCl, pH 7.5, 1% glycerol, 100mM NaCl, 1mM DTT, and the reservoir solution of 15% w/v PEG 2000, 100mM lithium chloride at 277K in 2-4 days using hanging drop vapor diffusion. The protein concentration was 24mg/ml. The crystal that diffracted to $2.42{\AA}$ resolution belongs to space group $P4_1\;or\;P4_3$ with unit cell parameters of $a=b=32.14{\AA},\;c=195.31{\AA},\;{\alpha}={\beta}={\gamma}=90^{\circ}$, with one molecule of CnrX in the asymmetric unit.

생약의 여성호르몬 수용체 조절 활성 검색 (In vitro Screening of Medicinal Plants with Estrogen Receptor Modulation Activity)

  • 이창민;강세찬;오좌섭;최한;이설매;이재현;이미현;정의수;곽종환;지옥표
    • 생약학회지
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    • 제37권1호통권144호
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    • pp.21-27
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    • 2006
  • Yeast based estrogenicity assay is the simplest and useful for the assay and the discovery of novel estrogenic substances in natural specimens, The estrogen receptor(ER) modulation activity of 50% EtOH extracts of 101 traditional medicinal herbs was assessed using a recombinant yeast assay system with both a human estrogen receptor expression plasmid and a receptor plasmid. Among them, 14 species proved to be active. Pureariae Flos (flower of Puerraria thunbergiana BENTH.) had the highest estrogenic relative potency$(7.75{\times}10^{-3})$ $(EC_{50}=9.39\;{\mu}g/ml)$. The $EC_{50}$ value of $17{\beta}-estradiol$ used as the positive control was $0.073\;{\mu}g/ml)$ (Relative Potency=1.00). There results demonstrated that some of the traditional medical herb may be useful in the therapy of estrogen replacement.

콜라겐을 알긴산으로 교차 결합시킨 인공진피의 창상치유 효과 (The Wound Healing Effects of Alginate- crosslinked Collagen Dermal Substitute of Artificial Skin)

  • 장재훈;박대환;신정임;안기영;송철홍
    • Archives of Plastic Surgery
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    • 제33권1호
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    • pp.13-20
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    • 2006
  • Alginate, which is isolated from brown seaweed, is a bioabsorbable long chain polysaccharides, ${\beta}$-D-mannuronic acid and ${\alpha}$-L-guluronic acid. The authors produced alginates and alginate-colllagen as a disc form. Then, to evaluate the efficacy of alginate and alginate-collagen complex as a wound healing material, three full-thickness skin defects of 2 cm in diameter were made at the back of the New Zealand white rabbits. Three groups of dressing materials-alginate, alginate-collagen complex and vaseline gauze as control group - were applied on the wound and the results were evaluated grossly and histopathologically. The authors compared gross findings of sizes of healed wound, wound epithelization and wound contraction by tracing the remaining wound area at 5th, 10th, 15th, 20th, 25th day after wound introduction, and wound biopsy was performed at 3rd, 7th, 14th, 21st day, respectively. Alginate and alginate-collagen complex showed statistically higher percentage of wound contraction and wound healing compared to control group(p<0.05). Alginate-collagen complex showed statistically higher percentage of wound contraction, epithelization and wound healing compared to alginate alone. In conclusion, the result suggests that alginate has a good effect of wound healing and that alginate-collagen complex is more effective in wound healing than alginate alone.

구절초 chrysanthemum sibiricum FISCHER의 성분 연구 (Studies on the consituents of Chrysanthemum sibiricum FISHER)

  • 이용주
    • 약학회지
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    • 제11권1_2호
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    • pp.7-16
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    • 1967
  • A yellowish microneedles, $C_{28}$ H$_{32}$ $O_{14}$ ${\cdot}$ I$_{1}$/$_2$, H$_{2}$O, m.p.262-$4^{\circ}$ , [${\alpha}$$_{D}^{20}$= -71,$43^{\circ}$(C = 0.42, pyridine), its acetate m.p.123-5.deg., were obtained in 0.3% yield from the leaves of Chrysanthemum sibiricum F$_{ISCHER}$. This substance is insoluble in water and the usual organic solvents except pyridine and ethylene glycol and, is not decomposed by dilute mineral acids but undergoes decomposition on being boiled in 60% H$_{2}$SO$_{4}$ or 35% HCl, giving one moel each of acacetin, glucose and rhamnose. It was not hydrolysed with a rhamnodiastase preparation obtained from the seeds of Rhamnus koraiensis. After permethylation of it, the uncrystallized product was hydrolysed and apigenin-5,4'-dimethyl ehter, m.p.$262^{\circ}$ was obtained, indicating that the disaccharide residue is at the 7 position of acacetin. Partial hydrolysis of this acacetin-7-rhamnoglucoside in cyclohexanol with formic acid gave acacetin-7-glucoside, m.p.246.deg. and rutinose, identifying them with authentic specimen on a paper chromatography. It was thus identified as linarin(acacetin-7-rutinoside) by means of mixed fusion, of paper partition chromatography and of its derivatives. Zemplen and Bognar suggested that the glucosidic linkage of linarin is .betha. by means of synthesis of this substance. But there is no evidence whether it is hydrolysed by emulsin or maltase or not. Linarin itself was not hydrolysed by an emulsin existing in the seed of Apricot or a maltase, but acacetin-7-glucoside(tilianin) which obtained from linarin gave acacetin and glucose on hydrolysis with the same emulsin and accordingly the glucosidic linkages of linarin and tilianin are thus regarded as ${\beta}$.

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우 난구세포의 공동배양과 CR1aa배양액이 체외생산된 우 수정란의 체외 발생에 미치는 영향 (Effects of Bovine Cumulus Cell Co-Culture and CR1aa Medium on In Vitro Development of In Vitro Produced Bovine Embryos)

  • 김동훈;정형민;박세필;이훈택;정길생
    • 한국가축번식학회지
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    • 제17권4호
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    • pp.271-278
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    • 1994
  • The aim of this study was to compare the two culture systems 1) co-culture with cumulus cells and 2) chemically defined medium supplemented with amino acids (CR1aa) and fetal calf serum (FCS) of in vitro produced bovine embryos from follicular oocytes in vitro. Bovine follicular oocytes were collected from ovaries of slaughtered cows and matured in TCM199 supplemented with 10% FCS and hormones (1$\mu\textrm{g}$/ml FSH-P and 1$\mu\textrm{g}$/ml oestradiol-17$\beta$)24 hours at 39$^{\circ}C$ under 5% CO2 in air. The capacitation of spermatozoa from ejaculated or frozen bull semen was induced by centrifugation through Percoll density gradient (45%, 90%). Then capacitated spermatozoa (1$\times$106/ml) were inseminated into 50${mu}ell$ droplet containing matured follicular oocytes and incubated for 40~42 hours. Cleaved embryos of 2~4cell stage were transferred to the co-culture with cumulus cells and/or CR1aa medium supplemented with FCS. In semen source, the developmental rates to the blastocyst and the hatched blastocyst stages were higher in ejaculated semen(27.6% and 14.9%) than those of frozen-thawed semen(18.3% and 11.8%), respectively. In two culture systems, the proportions of embryonic development upto the blastocysts and the hatched blastocysts were higher of CR1aa medium (22.1% and 12.1%) than those of cumulus cell co-culture (16.8% and 5.1%), respectively. The number of cells in exapnded blastocysts was slightly higher in cumulus cells co-culture (122.6$\pm$8.5) than that in CR1aa medium (117.9$\pm$5.9). The present results indicated that the early development of in vitro produced bovine embryos can be maintained efficiently in CR1aa medium as well as in co-culture with cumulus cells.

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