• Biomolecules & Therapeutics
• /
• 제24권2호
• /
• pp.178-183
• /
• 2016

Naturally occurring coumarin compounds have received substantial attention due to their pharmaceutical effects. Esculetin is a coumarin derivative and a polyphenol compound that is used in a variety of therapeutic and pharmacological strategies. However, its effect on aldose reductase activity remains poorly understood. In this study, the potential beneficial effects of esculetin on lenticular aldose reductase were investigated in galactose-fed (GAL) rats, an animal model of sugar cataracts. Cataracts were induced in Sprague-Dawley (SD) rats via a 50% galactose diet for 2 weeks, and groups of GAL rats were orally treated with esculetin (10 or 50 mg/kg body weight). In vehicle-treated GAL rats, lens opacification was observed, and swelling and membrane rupture of the lens fiber cells were increased. Additionally, aldose reductase was highly expressed in the lens epithelium and superficial cortical fibers during cataract development in the GAL rats. Esculetin reduced rat lens aldose reductase (RLAR) activity in vitro, and esculetin treatment significantly inhibited lens opacity, as well as morphological alterations, such as swelling, vacuolation and liquefaction of lens fibers, via the inhibition of aldose reductase in the GAL rats. These results indicate that esculetin is a useful treatment for galactose-induced cataracts.

• 항공우주기술
• /
• 제10권2호
• /
• pp.133-145
• /
• 2011

본 논문은 2008년 8월초부터 2010년 6월 10일 KSLV-I 2차 발사까지 수행된 나로우주센터의 추진제 및 고압가스 품질 관리 결과를 정리한 것이다. 품질관리는 나로우주센터에서 사용되는 모든 고압가스(Air, GHe, $GN_2$) 및 액화가스(LOX, $LN_2$)를 대상으로 관련 발사대 및 조립동 모든 장비에 대해 자율시험(AT), 인증시험(QT), 비행시험(FT) 모든 단계에서 수행하였다. 결과로써 총 428회의 간이검사(check analysis), 111회의 전항목검사(full analysis)를 수행하였다.

• Archives of Pharmacal Research
• /
• 제24권4호
• /
• pp.323-326
• /
• 2001

Previous studies have demonstrated that CW252053, a quinazoline antifolate, exhibits potent inhibitory activity against thymidylate synthase (TS) as well as cytotoxic activity against tumor cell lines in vitro. In this studys, we evaluated the in vivo antitumor efficacy of CW252053 in the mouse tumor model. Female B6D2F$_1$ mice were injected with LY3.7. 2C TK-/- (thymidine kinase deficient mouse Iymphoma) cells into the gastrocnemius muscle. Then, CW252053 was administered twice daily by intraperitoneal injection for 10 days, and tumor growth was monitored daily by leg diameter measurement. All animals in the vehicle, 5-FU, and low dose (30mgmg/kg CW252053 treated groups died between days 12 and 23 because of the tumor burden. In contrast, dosing with 60 mg/kg of CW252053 produced a cure rat against tumor growth of 37.5% and a survival rate of 50%. Even more significantly, a higher dose of CW252053 (120 mg/kg) elicited both a 100% cure rate and a 100% survival rate at the termination of the study, confirming that this compound has very potent in vivo antitumor activity against tumor growth. During the experimental period of this study no signs of toxicity were observed even at the high CW252053 dosage rate of 120 mg/kg.

• Molecules and Cells
• /
• 제21권2호
• /
• pp.213-217
• /
• 2006

Although AIMP1 (previously known as p43) is one of three auxiliary proteins bound to a macromolecular aminoacyl tRNA complex, it is also secreted as a cytokine controlling both angiogenesis and immune responses. Here we show that systemically administered purified recombinant human AIMP1 had anti-tumor activity in mouse xenograft models. In Meth A-bearing Balb/c mice, tumor volume increased about 28 fold in the vehicle treatment group, while an increase of about 16.7 fold was observed in the AIMP1-treated group. We also evaluated the anti-tumor activity of AIMP1 in combination with a sub-clinical dose of the cytotoxic anti-tumor drug, paclitaxel. The growth of NUGC-3 human stomach cancer cells was suppressed by 84% and 94% by the combinations of 5 mg/kg paclitaxel + 25 mg/kg AIMP1 (p = 0.03), and 5 mg/kg paclitaxel + 50 mg/kg AIMP1 (p = 0.02), respectively, while 5 mg/kg paclitaxel alone suppressed growth by only 54% (p = 0.02). A similar cooperative effect of AIMP1 and paclitaxel was observed in a lung cancer xenograft model. These results suggest that AIMP1 may be useful as a novel anti-tumor agent.

• 한국버섯학회지
• /
• 제20권3호
• /
• pp.93-101
• /
• 2022

Cordyceps militaris mycelium extracts containing high amounts of cordycepin were evaluated in vitro for their anti-inflammatory and tumor cell growth-inhibitory activities. All extracts dose dependently inhibited the increased production of inflammatory mediators including reactive oxygen species (ROS), nitric oxide (NO), and 𝛽-hexosaminidase in lipopolysaccharide (LPS)-stimulated inflammatory cells. All extracts were evaluated for anti-proliferative activity against normal RBL-2H3 cells and diverse types of cancer cell lines, including HCT, MC5-7, U-87MG, AGS, and A549 cells. The extract showed the strongest growth inhibition (IC₅₀ = 28.13 ㎍/mL) relative to vehicle-treated control cells against fibrosarcoma (MC5-7). We have demonstrated anti-inflammatory activity of C. militaris via inhibition of NO, ROS production, and 𝛽-hexosaminidase release in activated cells. C. militaris mycelium extract was also evaluated mechanistically and found to exert six types of anti-cancer activity, confirming its pharmacological potential. Our study suggests C. militaris use as a potential source of anti-inflammatory and anti-cancer agents. C. militaris may also be considered a functional food.

• 대한교통학회지
• /
• 제30권1호
• /
• pp.31-43
• /
• 2012

한국이 UN 자동차 법규 표준화 기구(WP29) 주관의 소형차 배출가스 시험방법 국제 표준화(WLTP/DHC) 연구에 참여하게 됨에 따라 우리나라의 도로 종류 별, 주행 시간대 별 주행패턴 측정이 요구되었다. 이에 본 연구에서는 WP29에서 제안한 주행패턴 표준화 방법을 토대로, 우리나라의 도로 교통 특성을 반영한 실 도로 주행패턴을 측정하고, 대표성을 갖는 도로 종류 별 주행 시간대별 총 7가지 유형의 주행패턴을 분석하였다. 이를 위해 이동식 차량활동도 모니터링 장비(PAMS)를 이용하여 35,410km의 실주행자료를 수집하였으며, 각 유형별로 분석된 주행패턴은 서로 유의한 차이가 있는 것으로 나타났다.

• The Korean Journal of Physiology and Pharmacology
• /
• 제19권2호
• /
• pp.183-189
• /
• 2015

Foeniculum vulgare Mill. (fennel) is used to flavor food, in cosmetics, as an antioxidant, and to treat microbial, diabetic and common inflammation. No study to date, however, has assessed the anti-inflammatory effects of fennel in experimental models of inflammation. The aims of this study were to investigate the anti-inflammatory effects of fennel in model of lipopolysaccharide (LPS)-induced acute lung injury. Mice were randomly assigned to seven groups (n=7~10). In five groups, the mice were intraperitoneally injected with 1% Tween 80-saline (vehicle), fennel (125, 250, $500{\mu}l/kg$), or dexamethasone (1 mg/kg), followed 1 h later by intratracheal instillation of LPS (1.5 mg/kg). In two groups, the mice were intraperitoneally injected with vehicle or fennel ($250{\mu}l/kg$), followed 1 h later by intratracheal instillation of sterile saline. Mice were sacrificed 4 h later, and bronchoalveolar lavage fluid (BALF) and lung tissues were obtained. Fennel significantly and dose-dependently reduced LDH activity and immune cell numbers in LPS treated mice. In addition fennel effectively suppressed the LPS-induced increases in the production of the inflammatory cytokines interleukin-6 and tumor necrosis factor-alpha, with $500{\mu}l/kg$ fennel showing maximal reduction. Fennel also significantly and dose-dependently reduced the activity of the proinflammatory mediator matrix metalloproteinase 9 and the immune modulator nitric oxide (NO). Assessments of the involvement of the MAPK signaling pathway showed that fennel significantly decreased the LPS-induced phosphorylation of ERK. Fennel effectively blocked the inflammatory processes induced by LPS, by regulating pro-inflammatory cytokine production, transcription factors, and NO.

• The Korean Journal of Physiology and Pharmacology
• /
• 제20권3호
• /
• pp.279-286
• /
• 2016

Caffeic acid phenethyl ester (CAPE), derived from honeybee hives, is a bioactive compound with strong antioxidant activity. This study was designed to test the neuroprotective effect of CAPE in 3-nitropropionic acid (3NP)-induced striatal neurotoxicity, a chemical model of Huntington's disease (HD). Initially, to test CAPE's antioxidant activity, a 2,2'-azino-bis-3-ethylbenzthiazoline-6-sulfonic acid (ABTS) antioxidant assay was employed, and CAPE showed a strong direct radical-scavenging effect. In addition, CAPE provided protection from 3NP-induced neuronal cell death in cultured striatal neurons. Based on these observations, the in vivo therapeutic potential of CAPE in 3NP-induced HD was tested. For this purpose, male C57BL/6 mice were repeatedly given 3NP to induce HD-like pathogenesis, and 30 mg/kg of CAPE or vehicle (5% dimethyl sulfoxide and 95% peanut oil) was administered daily. CAPE did not cause changes in body weight, but it reduced mortality by 29%. In addition, compared to the vehicle-treated group, robustly reduced striatal damage was observed in the CAPE-treated animals, and the 3NP-induced behavioral deficits on the rotarod test were significantly rescued after the CAPE treatment. Furthermore, immunohistochemical data showed that immunoreactivity to glial fibrillary acidic protein (GFAP) and CD45, markers for astrocyte and microglia activation, respectively, were strikingly reduced. Combined, these data unequivocally indicate that CAPE has a strong antioxidant effect and can be used as a potential therapeutic agent against HD.

• 비파괴검사학회지
• /
• 제32권1호
• /
• pp.1-6
• /
• 2012

본 연구에서는 광대역(100 kHz - 1 MHz) 탐촉자를 사용하여 자동차용 CNG연료탱크의 파열시험시 발생하는 음향방출신호의 분석을 통해 압력용기의 손상정도를 평가하였다. 압력이 420 bar까지 올라가기 전의 각 단계에서는 Kaiser 효과가 나타나고 creep 효과가 거의 나타나지 않으나, 420 bar 이상 상승시 creep 효과가 현저히 나타남으로써 용기가 손상을 입었다는 것을 알 수 있었으며, 480 bar 압력 상승 단계에서는 Kaiser 효과가 없어졌다. 540 bar의 압력 단계에서 공진형 탐촉자의 경우에서는 480 bar의 압력단계에 비하여 energy나 count 같은 activity가 감소하였으나 광대역 탐촉자의 경우 계속적으로 증가하였다. 또한 rise time이나 주파수 분석을 통해서 복합재료 압력용기의 손상 메카니즘을 관찰하기 위해서는 일반적으로 금속압력용기에서 많이 사용되는 공진형 탐촉자(150 kHz)보다 광대역 탐촉자가 효과적임을 알 수 있었다.

• Reproductive and Developmental Biology
• /
• 제35권2호
• /
• pp.159-165
• /
• 2011

To explore the role of histone deactylase (HDAC) activation in an in vivo model of hypertrophy, we studied the effects of Trichostatin A (TSA). TSA subjected to thoracic aortic banding (TAB)-induced pressure stress in mice. In histological observations, TAB in treated mice showed a significant hypertrophic response, whereas the sham operation remained nearly normal structure with partially blunted hypertrophy. TSA treatment had no effect (measured as HW/BW) on sham-operated animals. TAB animals treated with vehicle manifested a robust ~50% hypertrophic response (p<0.05 vs sham). TAB mice treated with 2 mg/kg/day TSA manifested a blunted growth responses, which was significantly diminished (p<0.05) compared with vehicle-treated TAB mice. TAB mice treated with a lower dose of TSA (0.5 mg/kg/day) manifested a similar blunting of hypertrophic growth (~25% increase in heart mass). Furthermore, to determine activity duration of TSA in vitro, 1 nM TSA was added to H9c2 cells. Histone acetylation was initiated at 4 hr after treatment, and it was peak up to 18 hr, then followed by significantly reduced to 30 hr. We also analyzed the expression of p53 following TSA treatment, wherein p53 expression was elevated at 4 hr, and it was maintained to 24 hr after treatment. ERK was activated at 8 hr, and maintained till 30 hr after treatment suggesting an intracellular signaling interaction between TSA and p53 expression Taken together, it is suggested that HDAC activation is required for pressure-overload growth of the heart. Eventually, these data suggest that histone acetylation may be a novel target for therapeutic intervention in pressure-overloaded cardiac hypertrophy.