• Toxicological Research
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• 제20권2호
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• pp.159-166
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• 2004

Safety pharmacological properties of CJ-11555, an anti-cirrhotic agent, were investigated in experimental animals and in vitro test system. CJ-11555 had no effects on normal body temperature in rats, motor coordination, chemoshock induced by pentetrazol, electric shock induced by electric shocker and writhing syndromes in mice at dose levels of 100, 300 and 1,000 mg/kg. CJ-11555 inhibited intestinal activity and prolonged hexobarbital-induced sleeping time in mice at the dose level of 1,000 mg/kg. CJ-11555 affected on general activity and behaviour tests in SD rats, such as lacrimation, ptosis, piloerection, decreased body tone, abnormal dispersion within the cage, diarrhoea, red colored faeces, slight hypothermia and decreased grooming, at the dose level of 1,000 mg/kg in rats. CJ-11555 was effected on cardiovascular and respiratory system in anesthetized beagle dogs, such as tachycardia, increase of mean blood pressure and decrease of PR interval, decrease of respiratory rate and minute volume, at dose levels of 10 and 30 mg/kg. However, these effects were also observed in vehicle treated anesthetized beagle dogs. In in vitro experiments, CJ-11555 inhibited agonists (histamine, acetyl-choline or $BaCl_2$) induced contraction of isolated guinea-pig at the concentration of 30$\times$$10^6$ M. CJ-11555 was weekly inhibited hERG channel current at concentrations of 10 and 30$\times$$10^6$ M, and $IC_{50}$ was estimated to be higher than 30${\times}$$10^6$M. Based on these results, it was concluded that CJ-11555 affected on cardiovascular and respiratory system, general activity and behaviour and hexobarbital-induced sleeping time at the dose level of 1,000 mg/kg and contraction of the smooth muscle and hERG channel current at the concentration of 30$\times$$10^6$ M.

• 대한한의학회지
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• 제18권1호
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• pp.299-315
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• 1997

The present experiments were designed to investigate the effects of Samsaengyeum. water extracts on the Cardiovascular System in the Experimental Animals. Thus, the changes of blood pressure and heart rate were measured after oral administration. Measurement of Mortality rate was observed for measuring the effect of Samsaengyeum water extract Samsaengyeum water extract against pulmonary thromboembolism induced by collagen the mixture(0.1me/10g, 2mg/kg B.W) plus serotonin(5mg/kg B.W) in mouse. The effect of Samsaengyeiim water extract was examined by observing the change of collagen-induced platelet aggregation, coagulation activity, ex vivo and in vitro fibrinolytic activity of euglobulin fraction in rats. The results were summarized as followings. 1. Samsaengyeum dropped the blood pressure in spontaneous hypertensive rat. 2. The drug increased the auricular blood flow in rabbit. 3. The drug relaxed the artery contraction by pretreated norepinephrine in rat. 4. The drug inhibited the death rate of mouse which was led to thromboembolism by serotonin and collagen. 5. The drug inhibited the platelet aggregation in rat. 6. The drug prolonged the prothrombin time and activated partial thromboplastin time on the test of plasma coagulation factor activity in rat, but was not valuable. 7. The drug reduced the fibrinogen lyses time and increased the lyses area of rat. 8. Samsaengyeum reduced fibrinogen lyses time of rat in vitro assay. According to the above mentioned results, Samsaengyeum increased the blood flow and dropped the blood pressure by the dilation of blood vessel. And the drug inhibited the platelet aggregation.

• Mycobiology
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• 제33권4호
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• pp.206-209
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• 2005

Narceine methyl ester and narceine are potent alkaloids which were isolated from Corydalis longipes were found effective in vitro at very low concentration, i.e., $100{\sim}500\;ppm$ against spore germination of some test plant pathogenic fungi (Alternaria solani, A. tagetica, Cercospora abelmoschi, Curvularia maculans, Erysiphe cichoracearum, E. pisi, Fusarium udum, Helminthosporium oryzae, H. penniseti, Ustilago cynodontis). Among the test, phytopathogens the spores of F. udum, C. maculans and H. penniseti were highly sensitive at 200 ppm. However, spores of E. pisi, A. solani and A. tagetica were less sensitive at low concentration followed by other test fungi. Most of the fungi showed zero or nearly zero percent spore germination at 400 and 500 ppm.

• 한방안이비인후피부과학회지
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• 제23권3호
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• pp.11-32
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• 2010

Objective : The aim of this study is to determine the effects of Dendrobii herba extract and Punica granatum extract on skin disease and skin beauty. Methods : To investigate in vitro anti-oxidant activity assay, ethanol extracts of medicinal plants tested by DPPH radical, xanthine oxidase activity. In the next experiment, to investigate anti-inflammatory activity assay, examined by relations in NO synthesis, IL-$1{\beta}$, IL-6, TNF-${\alpha}$, NF-${\kappa}B$, COX-2, MAP kinase. To study Skin wrinkle formation effect, we were examined by tyrosinase activities, melanin synthesis in MNT-1 cell. Results : 1. In an anti-oxidant test, Dendrobii and Punica granatum extract showed high radical scavenging activity. 2. In an anti-inflammatory test, Dendrobii herba and Punica granatum extract weakly inhibited the lipopolysaccharide(LPS)-induced nitric oxide(NO) release from RAW 246.7 macrophage cells. Dendrobii herba and Punica granatum extract also inhibited LPS-induced IL-$1{\beta}$ and COX-2 expressions. The inhibitory effect of Dendrobii herba and Punica granatum extract on macrophage activation were via the inhibition of NF-${\kappa}B$, evidenced by transient transfection assay. however, Dendrobii herba and Punica granatum extract did not have any effects about activation of Jun-N-terminal kinase(JNK) and inhibition of p38 MAP kinase in RAW 264.7 cells. 3. In the skin wrinkle formation assay, Dendrobii herba and Punica granatum extract weakly inhibited collagenase and elastase, however it was not statistically significant. 4. In the skin whitening assay, Dendrobii herba and Punica granatum extract weakly inhibited tyrosinase activity, however, it was not statistically significant. They did not have any effect on melanin synthesis, indicating that they could not be applicable for skin whitening. Conclusion : Dendrobii herba extract and Punica granatum extract may play a significant role in skin disease and skin beauty.

• 대한화장품학회지
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• 제33권1호
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• pp.29-32
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• 2007

In vitro 및 in vivo에서 모두 효과를 나타내는 새로운 여드름 개선 성분을 개발하였다. 특히, in vitro에서 효과가 검증된 많은 원료들이 실제 여드름환자에게서 실질적인 효능을 나타내지 못하는 경우가 많아, 본 연구에서는 임상에서 실질적인 효과를 보일 수 있는 원료의 개발에 초점을 맞추었다. 우선적으로 여드름에 효과가 높은 것으로 알려져 있거나 여드름개선 효과가 기대되는 천연물질의 추출물을 대상으로 소규모의 예비임상시험을 통해 효능을 확인하였다. 여러 가지 후보물질 중에서 발아콩과 목련박피 2종의 추출물이 여드름 및 여드름에 의한 홍조현상과 흉터에 뚜렷한 효과를 나타내어 이 두 천연물의 혼합추출물을 SeleMix AN이라 명명하였다. 200여 명의 예비임상시험을 통해서 SeleMix AN의 임상적 효과를 확인한 후 상기 물질의 여드름 개선 작용기작을 규명하기 위한 in vitro 효능테스트를 실시하여 P. Acne 성장억제 효과(시료농도 0.0125%), 16.9%의 히스타민 분비저해효과와 함께, 인간유래 섬유아세포의 활성을 대조군 대비 57% 높여 주는 실험결과를 확인하였다. 최종적으로 분당 서울대병원과의 공동연구를 통해 23명의 여성여드름환자를 대상으로 한 임상평가를 실시하여 새로운 여드름 개선성분의 효능을 검증하였다. 여름에 실시된 최종임상에서 SeleMix AN이 함유된 시료는 피지분비량이 증가하고 여드름 발병율이 높아지는 계절적인 영향에도 불구하고 4주만에 특히, 염증성 병변을 대조군 대비 통계적으로 유의차 있게 감소시키는 뛰어난 여드름 개선 결과를 얻을 수 있었다.

• Journal of Pharmaceutical Investigation
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• 제31권4호
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• pp.233-239
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• 2001

Local drug delivery by using biocompatible polymers has been developed in the treatment of periodontitis for many years. In the field of dental therapy, doxycycline is usually a first choice because of its broad-spectrum antibiotic activity. The strip releases antibiotics for a week, and the polymer should be degradable after a week. In this study, we prepared and evaluated the chitosan strips and nanoparticle strips containing doxycycline hydrochloride, and studied their antiacterial activity, dissoultion, and degrability in vitro. The weight of cast strip containing a 5 mg of doxycycline hydrochloride and a 45 mg of chitosan polymer was $57.67{\pm}0.17\;mg$. The release rate of doxycycline hydrochloride from the strip was measured by HPLC. The drug released from chitosan strip and nanoparticle strip was shown to be $50\;{\mu}g/mL$ in first 24 hours. In antibacterial test showed growth inhibitory activity after 24 hrs anaerobic incubation. In vitro degradability showed demolished weight of $93.74{\pm}0.08%$ chitosan strip, $82.48{\pm}1.29%$ chitosan nanoparticle strip, $2.47{\pm}1.99%$ polycarprolactione strip (control). These results showed that, with this doxycycline hydrochloride strip, it is feasible to obtain a sustained release of the drug within the periodontal pocket for seven days which may be improve for local drug delivery system for treatment of periodontal disease.

• 한방안이비인후피부과학회지
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• 제16권2호
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• pp.96-118
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• 2003

The effect of Glycyrrhizae Radix water extract, known as depigmenting agent, on melanin biosynthesis was investigated in cellular level by using B16 mouse melanoma cells. The inhibitory effect of Glycyrrhizae Radix water extract on melanogenesis was determined by mushroom tyrosinase assay traditionally using in vitro screening test. To determine whether Glycyrrhizae Radix water extract suppress melanin synthesis in cellular level, B16 mouse melanoma cells were cultured in the presence of different concentrations of Glycyrrhizae Radix water extract. Effects on cell proliferation, melanin biosynthesis, tyrosinase activity, DOPAchrome tautomerase activity, and expression level of mRNA for tyrosinase were examined. The maximum concentration of Glycyrrhizae Radix water extract that was not inhibitory to growth of the cells was 2 mgml. At that concentration, melanin synthesis was significantly inhibited without cytotoxicity after 5 days, compared with untreated cells. The treatment with Glycyrrhizae Radix water extract reduced tyrosinase and DOPAchrome tautomerase activity in a dose-dependent manner. However, the treatment with Glycyrrhizae Radix water extract did not affect significantly mRNA levels for tyrosinase. These results suggest that the inhibitory effect of Glycyrrhizae Radix water extract on melanogenesis is correlated with the suppression of tyrosinase and DOPAchrome tautomerase activity more than altering mRNA levels of tyrosinase.

• 한국미생물·생명공학회지
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• 제22권3호
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• pp.322-328
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• 1994

Antitumor and immunoadjuvant activities of Bifidobacterium adolesentis ATCC-15703 were investigated against the ascites and solid forms of tumor induced by Sarcoma 180(S-180) in ICR mice. When 100 $\mu$g of the bacterium was intraperitonealy administered in the mice, the survival rate(T/C %) of the mice was 132% for 50 days after the inoculation of S-180, however the increment of their body weights was suppressed. When the 100 $\mu$g was subcutaneously adminis- tratered at the right grion, the suppresion rate of the tumor growth on the 21st day after inoculation of S-180 were 62.3%. Complete supression of the tumor growth was observed from 2 out of 8 test mice. The bacterium itself appeared to have noncytotoxic substance against the S-180 in vitro. The bacteria] administration markedly enhanced the activity of peritoneal macrophages. The num- ber of peritoneal macrophages at one day after the administration of the 100 $\mu$g increased about 8 times as much as that of the control, and the highest activity of acid phosphatase appeared at 2 days.

• 대한화학회지
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• 제54권1호
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• pp.77-87
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• 2010

40여년전에 보고된 이래 병원에서 유래한 메치실린-저항 Staphylococcus aureus (MRSA) 은 세계적으로 큰 문제가 되어왔다. 항균성의 가능성을 가지는 새로운 약품을 개발하기 위하여 N'-[(-3-substituted-4-oxo-1,3-thiazolidin-2-ylidene]-4-hydroxy benzohydrazide (4a-4.i)와 N'-[-(3,4-disubstituted)-1,3-thiazolidin-2ylidene)]-4-hydroxybenzohydrazide (5.a-5.i)~(10.a-10.i)을 적절한 합성방법을 사용하여 합성하였다. 이들 합성된 화합물들은 s. aureus 균주에 대해 생체외 조건에서 분석하였다. 시료 화합물과 표준 화합물에 대해 최소억제농도(MIC)를 결정하였다. 시험한 모든 화합물들은 2000 ${\mu}g$/mL 투여량까지는 독성이 없었고, 사용한 균주에 대해 상당한 항균성을 보였다. 특히 6.f, 7.g, 9.f 와 10.f, 10 i 들이 가장 항균성이 컸다. 이것으로 미루어 파라-히드록시벤조히드라자이드 고리와 치환된 싸이아졸린 고리는 항균성에 필수적임을 알 수 있었다. 3D-QSAR 분석결과로 파라-히드록시벤조히드라자이드의 활성자리에 대한 결합방식을 알게되었다.

• 대한예방한의학회지
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• 제13권1호
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• pp.59-67
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• 2009

Objectives : This research aimed to evaluate the effects of Rubus coreanus $M_{IQ}$. Methods: These extracts from fresh R. coreanus $M_{IQ}$. were investigated with radical scavenging activity, the content of total phenolics, ferric thiocyanate method and flavonoid contents Results: These results revealed that the ethyl acetate extract from fresh R. coreanus $M_{IQ}$. possesses remarkable radical scavenging activity. The content of total phenolics of the ethanol extract from dried R. coreanus $M_{IQ}$. ($IC_{50}$=155.87${\pm}$8.8${\mu}$g/mL) is the highest among all of the samples. The stronger radical-scavenging activity ($IC_{50}$=77.72${\pm}$2.1${\mu}$g/mL) of ethyl acetate extract from dried R. coreanus $M_{IQ}$. should be related to its phenolic content as measured by gallic acid test. Conclusion: These results suggest that dried R. coreanus $M_{IQ}$. may act as a potential antioxidant agent.