• The Korean Journal of Physiology
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• 제24권1호
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• pp.171-180
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• 1990

In 19 cats anesthetized with ${\alpha}-chloralose$ effects of taurine and ${\beta}-alanine$ on the responses of wide dynamic range (WDR) cells to mechanical, chemical and thermal stimuli were investigated in the lumbar spinal cord of the cat. Also studied was an interaction of strychnine with taurine in affecting the activities of WDR cells. Following intravenous administration of taurine, the responses of WDR cells to all types of mechanical stimuli were markedly enhanced, demonstrating that the response to pressure was most sensitive to taurine action. When the receptive field was exposed to thermal stimuli ($50^{\circ}C$) for 20 sec. taurine increased activity of WDR cell to 169.5% of the control value. The $K^{+}$-induced activation of WDR cells was invariably suppressed after taurine administration. Intravenously administered strychnine remarkably reduced the enhanced response of WDR cell to natural stimuli resulting from intravenous administration of taurine. Also ${\beta}-alanine$ markedly activated the response of spinal dorsal horn cell to natural mechanical stimuli. These findings suggest that neutral amino acid and its derivative such as ${\beta}-alanine$ and taurine can enhance the response of WDR cells to different stimuli in cats.

• Asian-Australasian Journal of Animal Sciences
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• 제17권1호
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• pp.146-152
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• 2004

Ghrelin is an acylated peptide recently identified as the endogenous ligand for the growth hormone (GH) secretagogues receptor 1a (GHS-R1a) and is involved in a novel system for regulating GH release. To understand the long-term effects of ghrelin, here we constructed six myogenic expression vectors containing the cDNA of swine mature ghrelin (pGEM-wt-sGhln, pGEM-wt-hGhln), ghrelin mutant of $Ser^3$ with $Trp^3$ (pGEM-mt-sGhln, pGEM-mt-hGhln) and truncated ghrelin derivative (pGEM-tmtsGhln, pGEM-tmt-hGhln) encompassing the first 7 residues of ghrelin (including $Ser^3$ substituted with $Trp^3$) and adding a basic amino acid, Lys (K) in the C-terminus. The constructs, pGEM-wt-sGhln, pGEM-mt-sGhln and pGEM-tmt-sGhln were linked with the ghrelin leader sequence, while the pGEM-wt-hGhln, pGEM-mt-hGhln and pGEM-tmt-hGhln were linked with a leader sequence from the human growth hormone releasing hormone (hGHRH). Intramuscular injection of 200 ${\mu}g$ pGEM-wt-sGhln or pGEM-tmt-sGhln augmented growth over 3 weeks in normal rats and peaked at day 21 or 14 post-injection respectively, whose body weight gains were on average approximately 6% or 19% heavier over controls. However, other injectable vectors had no such enhanced growth effects. Our results suggested that the efficacy of the ghrelin leader sequence was more effective than that of hGHRH in our system. Moreover, the results indicated that skeletal muscle might have the ability to posttranslationally modify the in vivo expressed ghrelin. And the most strikingly, the short ghrelin analog seems to mimic the biological effects more efficiently when compared with the full-length ghrelin.

• Molecular & Cellular Toxicology
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• 제2권3호
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• pp.151-158
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• 2006

Khal was a synthetic congener of halocidin, a heterodimeric peptide consisting of 19 and 15 amino acid residues detected in Halocynthia aurantium. This compound was considered a candidate for the development of a novel peptide antibiotic. The genotoxicity of Khal was subjected to high throughput toxicity screening (HTTS) because they revealed strong antibacterial effects. Mouse lymphoma thymidine kinase ($tk^{+/-}$) gene assay (MOLY), single cell gel electrophoresis (Comet) assay and chromosomal aberration assay in mammalian cells and Ames reverse mutation assay in bacterial system were used as simplified, inexpensive, short-term in vitro screening tests in our laboratory. These compounds are not mutagenic in S. typhimurium TA98 and TA100 strains both in the presence and absence of metabolic activation. Before performing the comet assay, $IC_{20}$ of Khal was determined the concentration of $25.51\;{\mu}/mL\;and\;21.99\;{\mu}g/mL$ with and without S-9, respectively. In the comet assay, Khal was not induced DNA damage in mouse lymphoma cell line. Also, the mutation frequencies in the Khal-treated cultures were similar to the vehicle controls. It is suggests that Khal is non-mutagenic in MOLY assay. And no clastogenicity was observed in Khal-treated Chinese hamster lung cells. The results of this battery of assays indicate that Khal has no genotoxic potential in bacterial or mammalian cell systems. Therefore, we suggest that Khal, as the optimal candidates with both no genotoxic potential and antibacterial effects must be chosen.

• 한국식품과학회지
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• 제31권5호
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• pp.1378-1385
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• 1999

멸치액젓으로부터 항산화활성을 가지는 물질을 분리하기 위하여 용매추출 및 chromatography를 행하였다. 모든 용매분획들에 항산화활성이 있었으며 그 중 BuOH층과 수용액층이 소금을 함유하고 있었으나 항산화활성이 우수하였다. 수용액층을 투석막(MWCO 1000)으로 증류수에 대하여 투석하였을 때 투석막 내액의 항산화활성이 소실되었으므로 멸치액젓의 항산화성 물질은 분자량 1000이하의 분자량을 가진 것으로 추정하였다. Sephadex G-50 gel filtration chromatography에서 얻은 항산화물질 분획(tube No. 230-245)로 DE-52 anion exchange chromatography를 행한 결과 column에 결합하지 않고 흘러나온 분획(0 N NaCl용액) 및 0.05N NaCl용액으로 용출된 분획에서 항산화활성이 있었으나 $15\;{\mu}M$의 $Fe^{+++}\;ion$의 존재하에서 0 N NaCl 분획만 항산화활성이 유지되었다. Biogel P2 chromatography를 행한 결과 3번과 5번 분획의 항산화 활성이 특히 우수하였으며 TLC확인결과 아미노기가 풍부한 분자들임을 알 수 있었고 아미노산 조성을 분석하였을 때 다른 분획들보다 3번과 5번 분획에 소수성 아미노산이 많이 함유되어 있었다. TLC로 분리하여 항산화활성이 우수한 하나의 band를 HPLC의 C18 column으로 분석하였을 때 3개의 peak 중 항산화활성을 갖은 물질은 methionine 유도체이었으며 이는 멸치젓 수용액층의 많은 항산화물질 중 하나로 여러 아미노산 또는 oligopeptide의 유도체들의 상승효과가 멸치액젓의 항산화성을 유지하는 것으로 사료된다.

• 대한핵의학회지
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• 제33권6호
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• pp.527-536
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• 1999

목적: [C-11]flumazenil (RO 15-1788)은 벤조디아제핀 수용체 영상용 방사성 의약품으로 여러 가지신경, 정신 질환에서 양전자방출촬영(PET)용으로 연구되고 있다. 이 연구에서는2-amino 5-fluoroben-zoic acid를 출발물질로 사용하여 5단계에 걸쳐 플루마제닐 유도체를 합성한 후 F-18으로 표지하여 실험 동물에서의 성체 내 분포를 보았다. 대상 및 방법: 플루마제닐(c)의 합성은 F Hoffmann-La-Ro-che (Basle/CH)에서 보고된 방법에 의해 수정하여 합성하였다. 플루마제닐 유도체(d)는 플루마제닐(c)의 C-3 곁가지의 ethylester기를 tetrabutylammonium hydroxide와 반응하여 가수분해한 후 ditosylethane을 사용하여 tosyl기를 도입하여 합성하였다. 3-(2-[F-18]fluoro)flumazenil(e)의 합성은 TR-l3 사이클로트론에서 제조한 [F-18fluoride를 acetonitrile 용매하에서 플루마제닐 유도체(d)와 친핵성 치환반응으로 표지하였다. 표지된 플루마제닐 유도체는 TLC로 표지 효율을 측정하고, alumina-N과 $C_{18}$ Sep-pak으로 정제하였다. 3-(2-[F-18]fluoro)flumazenil의 생체 내 분포를 보기 위해 마우스(n=9)의 꼬31정맥으로 3-(2-[F-18]fluoro)flumazenil (0.37 MBq/0.1 mL)을 주사한 후 10, 30, 60분 후에 희생시켰다. 각 장기별 무게를 측정한 후 감마카운터로 방사능을 계수하였다. 투여한 방사능 양과 장기 내 방사능치를 구하여 시간에 따른 장기의 단위 무게별 주사량 대비 백분율(% ID/g)을 계산하였다. 결과: 플루마제닐 유도체 합성(d)의 전체 수득률은 40%였고, 플루마제닐 유도체의 F-18 표지효율은 66% 이상이었다. 마우스를 이용한 생체분포 실험에서 뇌의 섭취율은 10, 30, 60분에서 $2.5{\pm}0.4,\;2.2{\pm}0.3,\;2.1{\pm}0.1%ID/g$이었고, 혈액은 $3.7{\pm}0.4,\;3.3{\pm}0.1,\;3.3{\pm}0.09%ID/g$이었다. 결론: 새로운 벤조디아제 핀 수용체 영상용 방사성 의약품으로서 3-(2-[F-18]fluoro) flumazenil을 높은 표지 효율로 합성함으로서 PET와 SPECT 영상의 비교 연구에 이용될 수 있으며, F-18을 플루마제닐 유도체의 제각기 다른 위치에 치환함으로서 체내동태에 대한 연구에도 이용될 수 있다.

• 약학회지
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• 제52권4호
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• pp.299-305
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• 2008

Gabapentin, 1-(aminomethyl) cyclohexaneacetic acid, is a amino acid derivative, and is clinically effective in the treatment of neuropathic pain and partial seizures of epilepsy as a complementary therapy. The purpose of the present study was to evaluate the bioequivalence of two gabapentin tablets, $Neurontin^{R}$ tablet 800 mg (Pfizer Pharmaceuticals Co., Ltd.) and Gabapenin tablet 800 mg (Hanmi Pharm. Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of gabapentin from the two gabapentin formulations in vitro was tested using KP VIII Apparatus II method with 0.06 M HCI dissolution media. Twenty six healthy male subjects, $23.85{\pm}2.24$ years in age and $69.40{\pm}11.11$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ crossover study was employed. After a single tablet containing 800 mg as gabapentin was orally administered, blood samples were taken at predetermined time intervals and the concentrations of gabapentin in serum were determined using HPLC with fluorescence detector. The dissolution profiles of two formulations were similar in the tested dissolution media. 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 $AUC_{t}$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, $Neurontin^{R}$, were 1.28%, 0.63% and 0.62% for $AUC_{t}$, $C_{max}$ and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 (e.g., $log0.9097{\sim}log1.1598$ and $log0.8919{\sim}log1.1262$ for $AUC_{t}$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Gabapenin tablet 800 mg was bioequivalent to $Neurontin^{R}$ tablet 800 mg.

• 한국식품영양학회지
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• 제16권4호
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• pp.296-302
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• 2003

본 연구는 마늘속에 alliin을 크로마토그래피에 의하여 함량을 알고 이들이 에탄올추출물에 향균효과를 알아보기 위하여 연구했다. HPLC를 이용하기 위하여 메탄올로 Alliin을 추출하고 유해세균에 대한 향균활성을 알아보기 위하여 Alliin을 에탄을 추출물 시료를 조제하여 사용하였다. 마늘에는 alliin의 함량은 0.34 ∼0.73% fresh weight를 나타내고 에탄을 추출물의 시료에서 동결건조 시료수율이 가장 높았는데 이는 효소적 분해가 최소화되는 것으로 사료되며 에탄을 추출물의 향균효과는 Table 3에서 각 균주에 대하여 억제효과는 각 균주에서 50∼80% 효과를 보았고, 각종 균에 대한 억제차원에서 향균성을 달리하는 것을 알 수 있었으며 유해세균에 대한 향균작용이 마늘 추출물은 미생물의 발육저지력이 강하고 지속적으로 인체에 무해하므로 보존료 개발이 바람직함을 알았고, 독특한 향미를 주는 황화합물이 많아 산도의 증가와 관계없이 항균력이 강함을 보았고, 각종 균에 대한 항균성을 달리 하는 것을 알 수 있었다. 이로 인해 마늘성분중 선택적인 항균물질의 개발이 요구됨을 알았다.

• Journal of Pharmaceutical Investigation
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• 제27권4호
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• pp.287-293
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• 1997

To make a stable o/w emulsion, the effects of egg lecithin as an emulsifier and polyvinylpyrrolidone (PVP) as an auxiliary emulsifier on the physical stability of emulsion were investigated. The oil-in-water emulsion system was manufactured by microfluidizer and evaluated the physical stability. Average particle size and size distribution of emulsion was measured by dynamic light scattering analyzer and interfacial tension was measured. From the interfacial tension tested, critical micelle concentration of the egg lecithin was 0.1 %w/v and optimal concentration for the preparation of emulsion was 1.0 %w/v. The mean particle size was about $0.2\;{\mu}m$ which was suitable for injections. The short-term accelerated stability studies were conducted by centrifugation, freeze-thaw method and shaking of the emulsion samples. The addition of PVP was caused the reduction in the particle size and improved the physical stability of emulsion. These results suggested that a mixed interfacial film comprising the egg lecithin and PVP was formed at the o/w interface and it was effective in preventing phase separation under thermic or mechanical stress. We used antineoplaston A10 (A10) as a model drug which is peptide and amino acid derivative having a action to the living organism against the development of neoplastic growth by a nonimmunological progress. It has a poor solubility in water and there may be a difficulty in formulation of A10. Emulsion formulation study about A10 was performed. Solubility of A10 in emulsion was about five times as high as that in water. From the results of solubility and partition coefficient, almost A10 molecules in o/w emulsion exist in the interface between oil and water.

• 한국잡초학회지
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• 제13권2호
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• pp.89-95
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• 1993

광합성 전자전달저해제의 탐색을 위한 biorational screening 방법으로 광합성 박테리아의 일종인 cyanobacteria의 표준형(wild type)과 $D_1$ 단백질의 구성 아미노산이 변환된 변이주 Di-1, G-264. Di-22 등 4종을 사용하여 신규합성 화합물에 대한 광합성 전자전달저해활성을 조사하여 구조-활성간의 특성을 검토하였고, 이들의 thermoluminescence band를 이용하여 결합부위를 비교하였다. 1. Phenol 화합물(E-series)들은 cyanobacteria를 이용한 광합성 전자전달 저해활성의 양상을 볼 때 diuron보다는 dinoseb과 비슷하였다. 2. 합성한 Phenol화합물에서 나타난 구조활성간의 특정으로는 치환기의 phenyl ring에 C1이 치환되지 않은 경우 Hill반응 저해활성이 나타나지 않았고, 화합물에 있는 두개의 ring을 연결하는 bridge의 길이가 길어질수록 Hill반응 저해활성은 약하게 나타났다. 3. Triazine 화합물(T-series)의 경우 T-27, T-28화합물은 대조약제 atrazine보다 각각 10, 30배 강한 저해활성을 나타내었고, 변이주 G-264에 대 한 저항성 비율이 atrazine보다 더욱 크게 나타나 이들 화합물들의 결합부위가 $D_1$ 단백질의 264번 위치와 깊은 관계가 있을 것으로 생각되었다. 4. Triazine 화합물에 있어서 치환기 -C-NH-는 전자전달계에 중요한 작용기로 생각되었다. 5. Thermoluninescence band를 이용하여 결합부위를 비교할 수는 있었지만, 명료하게 구분되지 않았다.

• 한국식품조리과학회지
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• 제28권6호
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• pp.805-811
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• 2012

This study was carried out in order to optimize the manufacturing condition of fried garlic flakes as well as to investigate the physicochemical properties of the flakes. Fried garlic flake samples were prepared as follows: garlic was sliced by a thickness of 1.5 mm, 2.0 mm, 2.5 mm, which were measured by a thickness gage. The samples were fried in vegetable oil under different temperatures of $140{\sim}150^{\circ}C$, $160{\sim}170^{\circ}C$ and $180{\sim}185^{\circ}C$. The compression strength depending on the height (h) was measured in order to find the thickness effect by the rheometer (force control: 50 N, h: 3.25 mm). Moreover, the sample with 1.5 mm thickness showed crisp phenomena of the split compared with the crush shape of the 2.0 mm and 2.5 mm thick samples. The result of strength for time dependence showed a sample with a thickness of 1.5 mm, which was measured 5~9 times more than the 2.0 mm and 2.5 mm thick samples. We thought the reason that the 1.5 mm sample had less response power equivalent to compression force than the other samples. Alliin has been found to affect the immune responses in the blood, it is a derivative of the amino acid cysteine and is also quite heat stable. The LC system with a UV detection at 210 nm consists of a separation on a Zorbax TMS column and isocratic elution with water and ACN as a mobile phase. The alliin contents of raw and fried garlic flake under $140{\sim}150^{\circ}C$, $160{\sim}170^{\circ}C$ and $180{\sim}185^{\circ}C$ were 18.10 mg/mL, 14.0 mg/mL, 11.6 mg/mL and 11.1 mg/mL, respectively. The decrement of alliin content under different temperature was a small quantity hence, we confirmed that the increasing manufacturing temperature was not affected by the alliin content. Examining for the particle structure of fried garlic flakes by a polarization microscope, the color of the sample treated at $160{\sim}170^{\circ}C$ was pure yellow. Furder, the fiber shaped particle, which has an effect on the tough texture, almost did not appear compared to the different temperature conditions. Finally, the sensory test for the preference of fried garlic flake under different conditions was carried out and the scores for various sensory characteristics were surveyed. According to the physicochemical measurements and sensory evaluation, we confirmed that the optimum manufacturing condition of fried garlic flake was 1.5 mm thick at a temperature of $160{\sim}170^{\circ}C$.