• 대한치과교정학회지
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• 제23권3호
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• pp.415-425
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• 1993

Fluoride is one of the most potent stimulators of bone formation in vivo. But its direct effects on osteoblast is not yet clear This study was to investigate the effects of Sodium fluoride on alkaline phosphatase(ALP) activity, cAMP formation responsive to parathormone(PTH) and type I $\alpha$ 2 collagen ribonucleic acid (mRNA) level in Murin osteoblast-like (MC3T3-E1) cells. The cells were cultured in $\alpha-Minimal$ essential medium $(\alpha-MEM)$ supplemente with $10\%$ fetal bovine serum (FBS) and then changed to $0.1\%$ FBS with various concentration of Sodium fluoride. The ALP activity was assayed by the method of Lowry with disodium phenyl phosphated as substrate. cAMP formation was measured by Radioimmuno Assay(RIA). Type I $\alpha$ 2 collagen ribonucleic acid(mRNA) expression was studied by Nothern blot analysis. The results were as follows: 1. cAMP level was increased by PTH in MC3T3-E1 cells. 2. Sodium fluoride showed the tendency of inhibitory effects on cAMP responsiveness to PTH in MC3T3-E1 cells. 3. Sodium fluoride increased ALP activity at cocentration of $2{\mu}M,\;4{\mu}M,\;and\;10{\mu}M$ significantly different from control at the 0.001 level. ALP activity revealed maximum value at $10{\mu}M$ in this study. 4. Nothern blot analysis of Sodium fluoride treated cells, using Type I $\alpha$ 2 collagen prove, revealed significant increase at $10{\mu}M$ in MC3T3-E1 cells.

• Toxicological Research
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• 제17권1호
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• pp.41-47
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• 2001

In order to test the effects of hyperbaric oxygen (HBO) and $\alpha$-tocopherol on full-thickness skin grafts in rats, we peeformed full-thickness skin grafts bilaterally on rats. After surgery, we analyzed the tissue-concentrations of superoxide dismutase (SOD), catalase, and glutathione peroxidase(GPx)/reductase(GPr) on days 0, 2, 4, 7, 10, 14, 21 and 28. The four groups had similar patterns of change in SOD, catalase, GPx and GPr values. SOD increased initially, and was significantly increased at day 7, returning to the preoperative activity level on day 14 (control, HBO, and $\alpha$-tocopherol treated alone) and 28 (HBO plus $\alpha$-tocopherol). Catalase had a similar pattern of change as the SOD enzyme activity, except for the surgical control on day 2. Glutathione peroxidase/reductase activity in the four groups had a similar pat-tern of enzyme activity, with a significant increase from preoperative level on day 4, peaking during days 7 to 10, and returning to preoperative level on day 21(surgical control, HBO, and $\alpha$-tocopherol-treated alone) and 28 (HBO plus $\alpha$-tocopherol treated group). Hence, the clinical use of HBO and $\alpha$-tocopherol mixture can be recommended as an adjunctive treatment for free skin grafts in rats. But, the antioxidant used, its dose, and the timing of its administration, as well as, the exposure time and the pressure of HBO, should be the subject of further research.

• 한국식품영양과학회지
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• 제38권12호
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• pp.1672-1678
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• 2009

유자씨 종피와 배유부분에 대한 n-hexane 및 ethanol 추출물에 대한 항산화활성, ACE 저해활성, $\alpha$-glucosidase 억제활성 및 항암활성을 살펴보았다. 항산화활성은 종피 nhexane 추출물(CSH1), 배유 n-hexane 추출물(CSH2), 종피 70% ethanol 추출물(CSE1) 및 배유 70% ethanol 추출물(CSE2) 가운데 CSE1이 가장 높은 활성을 나타내었으며, CSE1의 용매분획물 가운데 ethylacetate 층이 2 mg/mL의 농도에서 라디칼소거능이 73.81% 그리고 총항산화력이 56.64 mg AA eq/g으로 우수한 항산화활성을 나타내었다. 또한 ACE 저해활성과 $\alpha$-glucosidase 억제활성도 CSE1이 각각 31.63% 및 45.17%로 가장 높은 활성을 나타내었다. 각각의 추출물에 대한 유방암, 간암, 폐암, 대장암 및 전립선암 세포에 대한 증식억제효과는 모든 암세포에 대하여 5mg/mL의 농도에서 종피 ethanol 추출물(CSE1)이 가장 높은 암세포 증식억제효과를 보였다.

• 약학회지
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• 제29권2호
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• pp.62-69
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• 1985

The isomeric intermediates, $3{\alpha}$and $3{\beta}-amino-5{\alpha}-cholestane required for the synthesis of N-nitrosoureas, N-(2-chloroethyl)-N-nitrosocarbamoyl-$3{\alpha}-amino-5{\alpha}$-cholestane (9), N-methyl-N-nitrosocarbamoyl-3${\alpha}-amino-5{\alpha}-cholestane$ (10), N-(2-chloroethyl)-N-nitrosocarbamoyl-$3{\beta}-amino-5{\alpha}-cholestane$: (7), and N-methyl-N-nitrosocarbamoyl-$3{\beta}-amino-5{\alpha}-cholestane$ (8) were obtained through the $LiAlH_{4}$ reduction of $5{\alpha}$-cholestan-3-one oxime, followed by the chromatographic separation: the assignment of the stereochemistry of both isomers were based on the shape and chemical shift of $C_{3}$-proton resonances on their NMR spectra and on the elution mobility on the TLC. The urea intermediates, N-(2-chloroethyl) carbamoyl-3.alpha.-amino-5.alpha.-cholestane (13), N-methylcarbamoyl-$3{\alpha}-amino-5{\alpha}-cholestane$ (14), N-(2-chloroethyl) carbamoyl-$3{\beta}-amino-5{\alpha}-cholestane (11) and N-methyl-$3{\beta}-amino-5{\alpha}$-cholestane (12) were prepared by the treatment of each isomers ($3{\alpha}$-amino-and $3{\beta}-amino-5{\alpha}$-cholestane) with alkyl isocyanates in anhydrous $CHCl_{3}$, and the corresponding nitrosoureas, 7-10 were obtained by the nitrosation of the ureas, 11-14, with AcOH (or HCOOH)/$NaNO_{2}$ in ice-cold condition. The inhibitory activity of the nitrosoureas, 7-10, and their intermediates, 12-14 towards the growth of L1210 murine leukemia cells, were examined. Among them, the compounds 9 and 10 exhibited high activity having $ED_{50}$ to be 5.5g/ml and 6.1g/ml, respectively.

• 한국식품영양과학회지
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• 제38권10호
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• pp.1331-1335
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• 2009

본 연구에서는 유전적으로 제2형 당뇨를 가진 Goto-Kakizaki 흰쥐의 간 세포액에 함유된 당 이용 대사 관련 주요 효소인 glucokinase(GK)와 acetyl CoA carboxylase (ACC)에 약용 식물 물 추출물들이 어떤 영향을 미치는지 알아보았다. $\alpha$-Glucosidase 저해제는 제2형 당뇨 치료와 예방을 위해 사용되어져 오고 있다. 따라서 약용식물 물 추출물들의 $\alpha$-glucosidase 저해 활성을 알아보았다. Goto-Kakizaki 흰쥐의 간 세포액 분획물을 GK과 ACC 활성을 알아보기 위해 사용하였다. 본 실험에 사용된 약용 식물들은 Lycium chinense(JGP), Discorea japonica Thunb.(SY), Pyrus pyrifolia(YSB), Cornus officinalis(SSY), Paeonia suffruticosa ANDR.(MDP), Cordyceps militaris(DCH) 그리고 Acanthopanax senticosus(GSO)였다. 지골피(JGP), 산약(SY), 야생배(YSB) 그리고 산수유(SSY) 물 추출물들은 GK 활성을 증가시켰고, 실험에 사용된 모든 약용식물 물추출물들은 간 ACC 활성을 증가시켰다. 야생배(YSB), 산수유(SSY), 목단피(MDP) 그리고 가시오가피(GSO) 물 추출물들은 대조군보다 현저히 높은 $\alpha$-glucosidase 활성 억제를 보여주었다. $\alpha$-Glucosidase 활성을 가장 억제시킨 것은 GSO 물 추출물이었고, 그 억제율은 $\alpha$-glucosidase 치료제인 acarbose보다 높았다. 따라서 제2형 당뇨에서 지골피 (JGP), 산약(SY), 야생배(YSB) 그리고 산수유(SSY) 물 추출물들은 글루코스 대사과정을 활성화시켜 항당뇨 효과를 나타내는 천연 소재일 것으로 생각되고 야생배(YBS), 목단피(MDP) 그리고 가시오가피(GSO)는 천연 $\alpha$-glucosidase 저해제로써 사용될 수 있을 것이다. 약용식물 물 추출물에 의한 증가된 ACC 활성은 더해진 항당뇨 효과를 나타낼 것이다.

• 약학회지
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• 제42권1호
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• pp.75-81
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• 1998

Effects of swainsonine (SW: 8${\alpha}$, ${\beta}$-indolizidine-1alpha, 2${\alpha}$, 8${\beta}$-triol from Locoweed) on the cellular and nonspecific immune responses of lipopolysaccharide (LPS) wer e studied in ICR mice. Mice were divided into 4 groups (10mice/group), and LPS was given to each mouse 1 hr after i.p. injection with 3.7mg/kg of SW by i.p. injection twice a week for 14 days at a dose of 2mg/kg. Immune responses of the delayed-type hypersensitivity response (DTH) to sheep red blood cells (s-RBC), phagocytic activity and natural killer (NK) cell activity were evaluated. LPS treatment didn`t affect NK cell activity, phagocytic activity, DTH to s-RBC compared with those in controls, and phagocytic activity of sareoma 180 tumor bearing mice. However, circulating leukocytes were significantly decreased. Combinaton of LPS and SW increased circulating leukocytes significantly compared vath that in LPS alone, and DTH to s-RBC, NK cell activity and phagocytic activities of normal and sarcoma tumor bearing mice were not affected. These findings indicate that SW didn`t affected the cellular immune responses suppressed by LPS but significantly increased circulating leukocytes.

• 한국연초학회지
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• 제20권1호
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• pp.71-79
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• 1998

Haemolyph carboxylesterases induced in diapausing pupae of Helicoverpa assulta Guenee were investigated. Increase in the activity of the electrophoresed isozyme bands were observed during the diapausing pupae. The isozymatic composition exhibited remarkable alterations represented as disappearance and induction of some isozyme bandsp which were identified as carboxylesterase (CE) on the basis of their specificities to inhibitors. Much higher activity of the induced CE was shown in reaction with $\beta$-naphthyl acetate ($\beta$-Na) than $\alpha$-naphthyl butyrate ($\alpha$-Nb), representing the high regioselectivity to $\beta$-naphthyl group. Optimal temperature for the enzyme activity was different to the substrates used 37$^{\circ}C$ in $\beta$-Na and 4$0^{\circ}C$ in $\alpha$-Nb, respectively. However, the optimal pH for the enzyme activity was the same as 7.5 regardless of the substrates used, and relatively high thermostability of the CE was demonstrated by showing the denaturation at high temperature (50~55$^{\circ}C$).

• 한국축산식품학회지
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• 제22권1호
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• pp.72-76
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• 2002

상업적으로 생산 판매되고 있는 여러 가지 유청 단백질을 이용하여 각종 암세포에 대한 세포독성을 조사한 결과, IgG, BSA, $\beta$-LG는 세포독성이 거의 없었으나, $\alpha$-LA가 강한 세포독성을 갖고 있음이 확인되었다. MKN45, HeLa, WiDr, 그리고 A498의 경우, $\alpha$-LA(1mg/ml)에 의해 세포성장이 95% 이상 억제되는 것으로 나타났다. HPLC를 이용하여 $\alpha$-LA에 혼입되어 있는 미량성분을 제거한 후, 세포독성을 조사한 결과, $\alpha$-LA이 나타내었던 세포독성이 대부분 없어지는 것으로 나타났다. 또한 $\alpha$-LA을 trypsin으로 부분 가수분해한 후, 각종 암세포에 대한 성장 억제효과를 검토한 결과, 암세포에 대한 독성을 상실하는 것으로 나타났으며, $\alpha$-LA를 EDTA로 처리할 경우, $\alpha$-LA의 세포독성이 대부분 상실되는 것으로 나타났다.

• Archives of Pharmacal Research
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• 제23권3호
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• pp.206-210
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• 2000

A new series of phosphonate side chain analogues of 1$\alpha$,25-dihydroxyvitamin $D_3$ (1) have been synthesized. Antiproliferative activities of theses analogues (8a,b and 9a,b) using human keratinocyte cell shows that analogues which have natural A-ring show higher activity than unnatural A-ring series and almost equally active to 1 $\alpha$,25-Dihydroxyvitamin $D_3$(1) at 1 $\mu$M level.

• 한국식품영양과학회지
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• 제43권2호
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• pp.318-322
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• 2014

본 연구에서는 울금(Curcuma longa L.)의 다양한 추출물을 대상으로 5-alpha reductase의 활성 저해 정도를 측정하였다. 5-Alpha reductase는 T에서 활성형 남성호르몬인 DHT로 전환을 담당하며, 전립선비대에서는 혈액에서 DHT 농도가 높다. Rat의 전립선조직 균질액과 5-alpha reductase를 과발현시킨 LNCaP 세포 균질액을 대상으로 측정한 결과, $100{\mu}g/mL$의 농도에서 울금의 열수추출물(CL-HW)과 20% 에탄올추출물(CL-E20)이 5-alpha reductase 활성을 효과적으로 저해하였다. 특히 CL-HW는 $100{\mu}g/mL$의 농도에서 80% 이상의 유의적 억제효과를 보였으며, CL-E20은 $50{\mu}g/mL$의 농도부터 80% 이상의 감소효과를 보였다. 이 같은 결과에서 CL-HW 및 CL-E20은 5-alpha reductase의 억제활성이 있으며, 이는 전립선비대 치료소재로 개발될 수 있는 가능성이 있음을 제안한다.