• Title/Summary/Keyword: active agent

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Anti-proliferative Effects of Water Extract of Agaricus blazei Murill in Human Lung Cancer Cell Line A549 (A549 인체폐암세포의 증식에 미치는 신령버섯 추출물의 영향에 관한 연구)

  • Choi, Woo-Young;Park, Cheol;Lee, Jae-Yun;Kim, Gi-Young;Park, Yeong-Min;Jeong, Yong-Kee;Lee, Won-Ho;Choi, Yung-Hyun
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.33 no.8
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    • pp.1237-1245
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    • 2004
  • Agaricus blazei Murill is a medicinal mushroom native to Brazil. It used to be a source of antitumor and immunoactive compounds and considered a health food in many countries. In the present study, it was examined the effects of water extract of A. blazei (WEAB) on the growth of human lung carcinoma cell line A549 in order to investigate the anti-proliferative mechanism by WEAB. Treatment of A549 cells to WEAB resulted in the growth inhibition, morphological change and induction of apoptotic cell death in a dose-dependent manner as measured by MTT assay and flow cytometric analysis. Flow cytometric analysis revealed that WEAB caused G2/M phase arrest of the cell cycle, which was associated with a down-regulation of cyclin A in both transcriptional and translational levels. WEAB treatment induced a marked up-regulation of cyclin-dependent kinase (Cdk) inhibitor p21, however, the levels of Cdk2, Cdc2, Wee1, Cdc25C and p53 expression were remained unchanged in WEAB treated cells. In addition, WEAB treatment inhibited the levels of cyclooxygenase (COX)-2 mRNA and protein without alteration of COX-l expression. Taken together, these findings suggest that WEAB may be a potential chemotherapeutic agent for the control of human lung carcinorma cells and further studies will be needed to identify the active compounds that confer the anti-cancer activity of WEAB. Once such compounds are identified, the mechanisms by which they exert their effects can begin to be characterized.

Bioequivalence of Terbinex Tablet to Lamisil Tablet (Terbinafine 125mg) (라미실 정(테르비나핀 125mg)에 대한 터비넥스 정의 생물학적동등성)

  • 고현철;홍정희;신인철
    • Biomolecules & Therapeutics
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    • v.11 no.1
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    • pp.65-71
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    • 2003
  • Terbinafine is a synthetic allylamine that is available in an oral formulation and is used at a dosage of 250mg/day. It is used as an active antifungal agent and inhibits the fungal enzyme squalene epoxidase, which leads to the accumulation of the sterol squalene, which is toxic to the organism. The purpose of the present study was to evaluate the bioequivalence of two terbinafine tablets, Lamisil (Novartis Korea Ltd.) and Terbinex (C-TRI Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). Eighteen normal male volunteers, 26.00$\pm$2.57 year in age and 70.51$\pm$9.36 kg in body weight, were divided into two groups and a randomized 2${\times}$2 cross-over study was employed. After one tablet containing 125 mg of terbinafine was orally administered, blood was taken at predetermined time intervals and the concentrations of terbinafine in plasma were determined using HPLC with UV detector. Pharmacokinetic parameters such as AUC, $C_{max}$ 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, $C_{max}$ and $T_{max}$ between two tablets were -4.191%, 5.223% and -25.720%, respectively when calculated against the Lamisil, tablet. The powers (1-$\beta$) for AUC, $C_{max}$ and $T_{max}$ were 81%, 87% and below 60%, respectively. Minimum detectable differences(.il) at alpha=O.1 and 1-/3=0.8 were less than 20% (e.g., 19.72% and 17.77% for AUC and $C_{max}$, respectively). But minimum detectable differences($\Delta$) at alpha=0.1 and 1-$\beta$=0.8 for $T_{max}$ were more than 20% (e.g., 26.25%). The 90% confidence intervals were within $\pm$20% (e.g., -17.440∼9.06 and -6.713∼17.160 for AUC and $C_{max}$ respectively). But 90% confidence intervals for $T_{max}$ were not within $\pm$20% (e.g., -43.346∼8.083). Another ANOVA test was conducted for logarithmically transformed AUC and $C_{max}$. These results showed that there are no significant differences in AUC and $C_{max}$ between the two formulations: The differences between the formulations in these log transformed parameters were all for less than 20% (e.g., -4.19% and 5.22% for AUC and $C_{max}$, respectively). The 90% confidence intervals for the log transformed data were not the acceptance range of log 0.8 to log 1.25 in AUC but the acceptance range of log 0.8 to log 1.25 in $C_{max}$ (e.g., log 1.13∼log 1.50 and log 0.94-log 1.22 for AUC and $C_{max}$ respectively). The major parameters, AUC and $C_{max}$ met the criteria of KFDA for bioequivalence although $T_{max}$ did not meet the criteria of KFDA (1998 year) for bioequivalence, indicating that Onfran tablet is bioequivalent to Zofran tablet. But in another ANOVA test AUC did not meet the criteria of KFDA (2002) for bioequivalence but $C_{max}$ met the criteria of KFDA (2002 year) for bioequivalence.or bioequivalence.equivalence.equivalence.equivalence.

Purification and Characteriztion of an Antifungal Antibiotic from Bacillus megaterium KL 39, a Biocontrol Agent of Red-Papper Phytophtora Blight Disease. (고추역병균 Phytophthora capsici를 방제하는 길항균주 Bacillus megaterium KL39의 선발과 길항물질)

  • 정희경;김상달
    • Microbiology and Biotechnology Letters
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    • v.31 no.3
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    • pp.235-241
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    • 2003
  • For the biological control of Phytophthora blight of red-pepper caused by Phytophthora capsici, an antibiotic-producing plant growth promoting rhizobacteria (PGPR) Bacillus sp. KL 39 was selected from a local soil of Kyongbuk, Korea. The strain KL 39 was identified as Bacillus megaterium by various cultural, biochemical test and API and Microlog system. B. megaterium KL 39 could produce the highest antifungal antibiotic after 40 h of incubation under the optimal medium which was 0.4% fructose, 0.3% yeast extract, and 5 mM KCl at 30 C with initial pH 8.0. The antifungal antibiotic KL 39 was purified by Diaion HP-20 column, silica gel column, Sephadex LH-20 column, and HPLC. Its RF value was confirmed 0.32 by thin-layer chromatography with Ethanol:Ammonia:Water = 8:1:1. The crude antibiotic KL39 was active against a broad range of plant pathogenic fungi, Rhizoctonia solani, Pyricularia oryzae, Monilinia fructicola, Botrytis cinenea, Alteranria kikuchiana, Fusarium oxysporum and Fusarium solani. The purified antifungal antibiotic KL39 had a powerful biocontrol activity against red-pepper phytophthora blight disease with in vivo pot test as well as the strain B. megaterium KL 39.

Cornu cervi pantotrichum Pharmacopuncture Solution Facilitate Hair Growth in C57BL/6 Mice

  • Lee, Seon-Yong;Lee, Dong-Jin;Kwon, Kang;Lee, Chang-Hyun;Shin, Hyun Jong;Kim, Jai Eun;Ha, Ki-Tae;Jeong, Han-Sol;Seo, Hyung-Sik
    • Journal of Pharmacopuncture
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    • v.19 no.2
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    • pp.122-128
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    • 2016
  • Objectives: Cornu cervi pantotrichum (CCP) has been widely used in Korean and China, as an anti-fatigue, anti-aging, and tonic agent to enhance the functions of the reproductive and the immune systems. Because CCP has various growth factors that play important roles in the development of hair follicles, we examined whether CCP pharmacopuncture solution (CCPPS) was capable of promoting hair growth in an animal model. Methods: One day after hair depilation, CCPPS were topically applied to the dorsal skin of C57BL/6 mice once a day for 15 days. Hair growth activity was evaluated by using macro- and microscopic observations. Dorsal skin tissues were stained with hematoxylin and eosin. Expressions of bromodeoxyuridine (BrdU), proliferating cell nuclear antigen (PCNA), and fibroblast growth factor (FGF)-7 were examined by using immunohistochemical staining. A reverse transcription polymerase chain reaction (RT-PCR) analysis was also conducted to measure the messenger RNA (mRNA) expression of FGF-7. Results: CCPPS induced more active hair growth than normal saline. Histologic analysis showed enlargement of the dermal papilla, elongation of the hair shaft, and expansion of hair thickness in CCPPS treated mice, indicating that CCPPS effectively induced the development of anagen. CCPPS treatment markedly increased the expressions of BrdU and PCNA in the hair follicles of C57BL/6 mice. In addition, CCPPS up regulated the expression of FGF-7, which plays an important role in the development of hair follicles. Conclusion: These results reveal that CCPPS facilitates hair re-growth by proliferation of hair follicular cells and up-regulation of FGF-7 and suggest that CCPPS can potentially be applied as an alternative treatment for patients with alopecia.

Inhibition of Human Neutrophil Elastase by NSAIDs and Inhibitors, and Molecular Pharmacological Mechanism of the Inhibition (비스테로이드성 항염증제와 효소 억제제에 의한 사람 중성구 Elastase의 활성도 억제 및 분자약리학적 기전)

  • Kang, Koo-Il;Kim, Woo-Mi;Hong, In-Sik;Lee, Moo-Sang
    • The Korean Journal of Pharmacology
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    • v.32 no.3
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    • pp.425-431
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    • 1996
  • Human neutrophil elastases (HNElastase, EC 3.4.21.37), a causative factor of inflammatory diseases, are regulated by plasma proteinase inhibitors, alpha-proteinase inhibitor and ${\alpha}_2-macroglobulin$. Under certain pathological conditions, however, released enzymes or abnormal function of inhibitors may cause various inflammatory disease. NSAIDs have been clinically applied for treatment of inflammatory diseases. Inhibition of cyclooxygenase is a known mechanism of action of NSAIDs in the treatment of inflammatory disease. In in vitro experiments, HNElastase was inhibited by naproxen, phenylbutazone, and oxyphenbutazone, but ibuprofen, ketoprofen, aspirin, salicylic acid, and tolmetin did not inhibit elastase. HNElastase was also inhibited by chelating agents, EDTA & EGTA, and tetracyclines. Removal of divalent metal ions by EDTA caused inhibition of elastase, and reconstitution of the metal ions recovered the enzyme activity to a certain level. Frequencies and contours in the Raman spectra of various conditions of human neutrophil elastase undergo drastic changes upon partial removal and/or reconstitution of calcium and zinc ions. The metal ion content dependent activities and change of the contour of the Raman spectrogram suggest us that the mechanism of action of a chelator or chelator-like agents on neutrophil elastase may be related to the conformational change at/or near the active site, especially -C=O radical or -COOH radical.

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Bioequivalence of Flucona Capsule to Diflucan Capsule (Fluconazole 50 mg) (디푸루칸 캅셀(플루코나졸 50 mg)에 대한 플루코나 캅셀의 생물학적 동등성)

  • Cho, Hea-Young;Kang, Hyun-Ah;Lee, Suk;Oh, In-Joon;Lim, Dong-Koo;Moon, Jai-Dong;Lee, Yong-Bok
    • Journal of Pharmaceutical Investigation
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    • v.33 no.2
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    • pp.135-140
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    • 2003
  • Fluconazole is an orally active bis-triazole antifungal agent, which is used in the treatment of superficial and systemic candidiasis and in the treatment of cryptococcal infections in patients with the acquired immuno deficiency syndrome (AIDS). The purpose of the present study was to evaluate the bioequivalence of two fluconazole capsules, Diflucan (Pfizer Pharmaceuticals Korea Inc.) and Flucona (Korean Drug Pharmaceuticals Co., Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). The fluconazole release from the two fluconazole capsules in vitro was tested using KP VII Apparatus II method at 0.1 M hydrochloride dissolution media. Twenty normal male volunteers, $23.60{\pm}1.88$ years in age and $63.57{\pm}6.17\;kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After three capsules containing 50 mg as fluconazole was orally administered, blood was taken at predetermined time intervals and the concentrations of fluconazole in serum were determined using HPLC method with UV detector. The dissolution profiles of two fluconazole capsules were very similar at 0.1 M hydrochloride 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 logarithmically transformed $AUC_t$ and $C_{max}$ and untransformed $T_{max}$. The results showed that the differences in $AUC_t,\;C_{max}\;and\;T_{max}$ between two capsules based on the Diflucan were 4.96%, 5.65% and -13.76%, respectively. There were no sequence effects between two capsules in these parameter. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log(0.8) to log(1.25) $(e.g.,\;log(1.01){\sim}log(1.08)\;and\;log(1.00){\sim}log(1.12)\;for\;AUC_t\;and\;C_{max},\;respectively)$, indicating that Flucona capsule is bioequivalent to Diflucan capsule.

Chronic Administration of Baicalein Decreases Depression-Like Behavior Induced by Repeated Restraint Stress in Rats

  • Lee, Bombi;Sur, Bongjun;Park, Jinhee;Kim, Sung-Hun;Kwon, Sunoh;Yeom, Mijung;Shim, Insop;Lee, Hyejung;Hahm, Dae-Hyun
    • The Korean Journal of Physiology and Pharmacology
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    • v.17 no.5
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    • pp.393-403
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    • 2013
  • Baicalein (BA), a plant-derived active flavonoid present in the root of Scutellaria baicalensis, has been widely used for the treatment of stress-related neuropsychiatric disorders including depression. Previous studies have demonstrated that repeated restraint stress disrupts the activity of the hypothalamic-pituitary-adrenal (HPA) axis, resulting in depression. The behavioral and neurochemical basis of the BA effect on depression remain unclear. The present study used the forced swimming test (FST) and changes in brain neurotransmitter levels to confirm the impact of BA on repeated restraint stress-induced behavioral and neurochemical changes in rats. Male rats received 10, 20, or 40 mg/kg BA (i.p.) 30 min prior to daily exposure to repeated restraint stress (2 h/day) for 14 days. Activation of the HPA axis in response to repeated restraint stress was confirmed by measuring serum corticosterone levels and the expression of corticotrophin-releasing factor in the hypothalamus. Daily BA administration significantly decreased the duration of immobility in the FST, increased sucrose consumption, and restored the stress-related decreases in dopamine concentrations in the hippocampus to near normal levels. BA significantly inhibited the stress-induced decrease in neuronal tyrosine hydroxylase immunoreactivity in the ventral tegmental area and the expression of brain-derived neurotrophic factor (BDNF) mRNA in the hippocampus. Taken together, these findings indicate that administration of BA prior to the repeated restraint stress significantly improves helpless behaviors and depressive symptoms, possibly by preventing the decrease in dopamine and BDNF expression. Thus, BA may be a useful agent for the treatment or alleviation of the complex symptoms associated with depression.

Chemical Compositions and Nematicidal Activities of Essential Oils on Meloidogyne hapla (Nematoda: Tylenchida) Under Laboratory Conditions (식물정유의 당근뿌리혹선충(Meloidogyne hapla)에 대한 살선충활성 및 방향성성분 분석)

  • Jeon, Ju-Hyun;Ko, Hyoung-Rai;Kim, Se-Jong;Lee, Jae-Kook
    • The Korean Journal of Pesticide Science
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    • v.20 no.1
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    • pp.30-34
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    • 2016
  • To evaluate the efficacy of natural nematicides for the control of root-knot nematode in strawberry greenhouses, commercial essential oils were examined by 24-well culture plate bioassay for their nematicidal activities against second-stage juveniles and eggs of Meloidogyne hapla. Based on the mortality of M. hapla juveniles at a concentration of $125{\mu}g/mL$, the most active essential oil was Alpinia galanga (100%), followed by Carum carbi (22.3%), Eugenia caryophyllata (9.4%), Cinnamonum zeylanicum (7.2%), Mentha pulegium (2.4%), and Foeniculum vulgare (2.1%). Moreover, A. galanga significantly reduced hatching at 7, 14, and 21 days after treatment. The volatile constituents identified in the A. galangal oil were methyl cinnamate (87.4%), 1,8-cineole (4.4%), ${\beta}$-pinene (2.5%), ${\alpha}$-pinene (2.2%), and p-cymene (1.1%), as major constituents. Results of this study show that A. galangal essential oil and its major constituents may serve as an environmental friendly agent of a promising natural nematicide to control Meloidogyne spp.

The Effect of Enhancer on the Penetration of Indapamide through Hairless Mouse Skin (경피흡수촉진제의 영향에 따른 인다파마이드의 피부투과)

  • Seo, Hui;Jeung, Sang-Young;Park, Ji-Seon;Shin, Byung-Cheol;Hwang, Sung-Joo;Cho, Sun-Hang
    • Journal of Pharmaceutical Investigation
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    • v.37 no.4
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    • pp.237-242
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    • 2007
  • The chemical formula of indapamide is 3-(aminosulfonyl)-4-chloro-N-(2,3-dihydro-2-methyl-1H-indol-l-yl)-benzamide, Indapamide is an oral antipertensive diuretic agent indicated for the treatment of hypertensive and edema. Indapamide inhibits carbonic anhydrase enzyme. Transdermal drug delivery systems, as compared to their corresponding classical oral or injectable dosage form counterparts, offer many advantages. The most important advantages are improved systemic bioavailability of the pharmaceutical active ingredients (PAI), because the first-pass metabolism by the liver and digestive system are avoided; and the controlled, constant drug delivery profile (that is, controlled zero-order absorption). Also of importance is the reduced dose frequency compared to the conventional oral dosage forms (that is, once-a-day, twice-a-week or once-a-week). Other benefits include longer duration of therapeutic action from a single application, and reversible action. For example, patches can be removed to reverse any adverse effects that may be caused by overdosing. In order to evaluate the effects of vehicles and penetration enhancers on skin permeation of Indapamide, the skin permeation rates of Indapamide from vehicles of different composition were determined using Franz cells fitted with excised hairless skins. Solubility of Indapamide in various solvents was investigated to select a vehicle suitable for the percutaneous absorption of Indapamide, The solvents used were Tween80, Tween20, Labrasol, Lauroglycol90 (LG90) and Peceol. Lauroglycol90 increase the permeability of indapamide approximately 3.75-fold compared with the control. Tween80, Tween20, Labrasol, Lauroglycol90 (LG90) and Peceol showed flux of $0.06ug/cm^2/hr,\;0.4ug/cm^2/hr,\;0.21ug/cm^2/hr,\;0.72ug/cm^2/hr,\;0.29ug/cm^2/hr$, respectively.

Impact of the Customer Orientation and Job Satisfaction as a Result of the Consultant's Emotional Exhaustion at the Call Center (콜센터 상담원의 감정소진이 고객지향성 및 직무만족에 미치는 영향)

  • Cho, Sang-Eun;Yang, Hae-Sool
    • The Journal of the Korea Contents Association
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    • v.10 no.6
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    • pp.386-403
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    • 2010
  • This research studied the impact of the customer orientation and job satisfaction by lowering the desire of the kind for customers and the desire for fulfillment as a result of emotional exhaustion of the consultant who performs emotion labor at the call center. This research sets study model and hypothesis to verify that call center consultant's emotional exhaustion how to effect customer orientation and job satisfaction. We took questionnaires from 157 call center(financial institutes) consultant's in Seoul for the verification of the hypothesis. I show that the consultant's emotional exhaustion had negatively affected the customer orientation and job satisfaction. In this paper proposed the importance that the experience of the consultant's emotional exhaustion who is the main agent of the performance should be minimized by removing ad improving the factors to lower emotion exhaustion through lowering time pressure in the work performance reduce the consultant's emotional exhaustion, granting work autonomy and authority, and active support of relevant departments and the ongoing communication between the managers and consultant This study makes a significant meaning in that it proposed the consultant's emotional exhaustion was negative factor on the customer orientation and job satisfaction factor in operating call center worker.