• Bulletin of the Korean Chemical Society
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• 제13권5호
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• pp.486-491
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• 1992

The rate constants for the reactions of p-nitrophenyl acetate with 6 different aryloxides and 2 benzohydroxamates have been measured spectrophotometrically in water containing various concentrations of cetyltrimethylammonium bromide (CTAB). The reactivity of the nucleophiles has been demonstrated to be significantly enhanced as the concentration of the surfactant increases up to a certain point. When the basicities of the aryloxides are comparable, the rate enhancement is more prominent for the aryloxide having larger binding constant to the micellar aggregate. Benzohydroxamates exhibitis significantly large ${\alpha}$-effect in the absence of the surfactant, although, the ${\alpha}$-effect nucleophiles are considered to be more solvated in water than the corresponding normal nucleophile. Thus, the solvation effect does not appear to be solely responsible for the ${\alpha}$-effect. Interestingly, the large ${\alpha}$-effect disappears in the presence of the surfactant. Therefore, one might attribute the disappearance of the ${\alpha}$-effect to solvent effect. However, a structural change of the reactive ${\alpha}$ -effect nucleophile into unreactive ones would also be considered to be responsible for the absence of the ${\alpha}$-effect in the present system.

• 약학회지
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• 제25권2호
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• pp.57-64
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• 1981

The antihypertensive effect of $\alpha-Methyldopa$ administered concurrently with timolol or labetalol were studied with spontaneously hypertensive rats (SHR). Every drugs were administered orally once a day after prechecking the systolic blood pressure and heart rate of SHR. The blood pressure and heart rate of SHR were significantly decreased in groups of combination while those of non-combination groups were fallen slightly. Compared with control group, the significant changes of blood pressure was obseved in group of $\alpha-methyldopa$ with timolol(100mg+2mg/kg)and $\alpha-methyldopa$ with labetalol (100mg+12.5mg/kg). The group of $\alpha-methyldopa$ with timolo 1 (100mg + 1.0mg/kg) reduced blood Pressure in similar degree as manifested in group of $\alpha-methyldopa$ with labetalol (100mg + 50mg/kg). In the group that $\alpha-methyldopa$ was administered concurrently with timolol, the maximum antihypertensive effect and heart rate decreasing effect were appeared after 3hr and 1hr of administration respectively and those effects in group of $\alpha-methyldopa$ with labetalol were appeared after 6hr of administration. The acute oral toxicity test was performed using albino mice with $\alpha-methyldopa$ alone, $\alpha-methyldopa$ with timolol (100:1) and $\alpha-methyldopa$ with labetatol (4:1), and was found that the $LD_{50}$ of $\alpha-methyldopa$ alone was 1104 mg/kg, $\alpha-methyldopa$ with timolol (100:1) was 1115 mg/kg and $\alpha-methyldopa$ with labetalol (4:1) was 354mg/kg.

• Bulletin of the Korean Chemical Society
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• 제13권6호
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• pp.642-647
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• 1992

Second-order rate constants have been measured spectrophotometrically for the reactions of substituted phenyl acetates with butane-2,3-dione monoximate and p-chlorophenoxide anions in MeCN-H$_2$O mixtures of varying compositions. The reaction rate, unexpectedly, decreased remarkably upon initial additions of MeCN to H$_2$O up to 30-40 mole ${\%}$ MeCN, and followed by a gradual increase upon further additions of MeCN. The change in solvent composition also influenced the magnitude of the ${\alpha}$-effect, i.e., the ${\alpha}$-effect increased as the mole ${\%}$ MeCN increased. The solvent dependent ${\alpha}$-effect for the present system appears to indicate that the differential solvation between the ${\alpha}$-effect nucleophile and the corresponding normal nucleophile is not solely responsible but the difference in the transition-state stabilization is also responsible for the ${\alpha}$ -effect in organic solvent-rich region.

• Bulletin of the Korean Chemical Society
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• 제13권6호
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• pp.632-636
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• 1992

Second-order rate constants have been determined spectrophotometrically for nucleophilic substitution reactions of p-nitrophenyl benzoate with various anionic nucleophiles including 6 ${\alpha}$ -effect nucleophiles. The logarithmic second-order rate constants for the aryloxides give a good Bronsted correlation with the respective basicity while the ones for p-chlorothiophenoxide and hydroxide exhibit significantly positive and negative deviations, respectivity, from the Bronsted linear line. The deviations are attributed to a solvation effect rather than a change in the reaction mechanism. The ${\alpha}$-effect nucleophiles except highly basic ones demonstrate significantly higher nucleophilicity (the ${\alpha}$ -effect) than would be predicted from the respective basicity. The effect of solvation and polarizability appears to be important for the ${\alpha}$-effect as well as for the reaction rate.

• 대한한방내과학회지
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• 제25권1호
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• pp.28-45
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• 2004

Objectives : The main purpose of this study is to evaluate the effect of Injinchunggan-tang on $TNF-{\alpha}$ signal transmission system. Materials and Methods : We analyzed the following with quantitative RT-PCR method; the effect of Injinchunggan-tang on secretion of $TNF-\alpha$ mRNA/protein and stability, the effect on gene revelation that consists of signal transmission system (TRAIL, NIK, A20, TRADD, RAIDD, RIP TNFR-I, TNFR-II, TRAF1, TRAF2, FADD), the one on activation of p38, Erk1/2 MAPK and the rate of nuclear $NF-{\kappa}B/cytosolic\;NF-{\kappa}B$ in HepG2 cell. We also analyzed the inhibitory effect of Injinchunggan-tang on the apoptosis of HepG2 cell that $TNF-{\alpha}$ induces and the $NF-{\kappa}B$ restraint effected by transfection of $I{\kappa}B{\Delta}N$ through tryphan blue exclusion assay. Results : Injinchunggan-tang prohibits revelation of $TNF-{\alpha}$ mRNA in HepG2 cell and the creation of protein. However, it has no effect on the stability of $TNF-{\alpha}$ mRNA. While it did not have any effect on the generation of TRAIL, NIK, A20, TRADD, RAIDD and RIP genes, Injinchunggan-tang reduces the revelation of TNFR-I, TNFR-II, TRAF1, TRAF2 and FADD genes. It has been confirmed that Injinchunggan-tang restraints the revelation of $TNF-{\alpha}$ mRNA that is promoted by ethanol, acetaldehyde, lipopolysaccharide, in proportion to the treatment density and time. It activated $NF-{\kappa}B$ of HepG2 cell and promoted activation of $NF-{\kappa}B$ that is occurred by $TNF-{\alpha}$. It has been observed that the restraint effect against the $TNF-{\alpha}$ inducing apoptosis is lost when it is intercepted the function of $NF-{\kappa}B$ in HepG2 cell. Conclusion: It has been confirmed that Injinchunggan-tang has restraining effect against the revelation of $TNF-{\alpha}$ and mRNA that is constituent element of TNF-a signal transmission system. It also has been revealed that it restraints the activation of p38, Erk1/2 by $TNF-{\alpha}$. Through this prohibiting effect, it is inferred that it restraints signal transmission among various cells that are related to inflammation reaction. Meanwhile, Injinchunggan-tang protects liver cell from apoptosis that is caused by $TNF-{\alpha}$, by maintaining the activating function for $NF-{\kappa}B$.

• Archives of Pharmacal Research
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• 제13권1호
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• pp.64-68
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• 1990

The stabilization effect of .alpha.-tocopherol incorporated into liposomal phospholipid membrane was investigated by fluorospectrophotometry and UV-visible spectretarded by the presence of .alpha.-tocopherol in the bilayer of liposomal phospholipid membrane relative to cholesterol-containing liposomes and pure phospholipid liposomes. .alpha.-tocopherol-containing liposomes prolonged the oxidation of liposomes-embedded heme as those of cholesterol-containing liposomes and pure phospholipid liposomes. Thus .alpha.-tocopherol-containing liposomes may be useful for the carrier systems of nutrients and drugs to phospholipid bilayer and stabilized liposomes.

• Applied Biological Chemistry
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• 제48권1호
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• pp.103-108
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• 2005

${\alpha}-Amylase$ 저해제는 소장에서 전분의 소화를 저해하여 포도당의 흡수를 지연시킴으로써 혈당 조절 목적으로 이용된다. 따라서 본 연구에서는 ${\alpha}-amylase$ 저해제를 탐색할 목적으로 국내 자생 목본류 약 1400여종의 70% ethanol 추출액을 대상으로 ${\alpha}-amylase$ 저해제 분포를 검색하였다. 수종의 목본류에서 ${\alpha}-amylase$ 저해제가 분포하고 있음이 확인되었으며, 그 중 활성이 비교적 높은 말채나무 기원의 저해제를 대상으로 연구를 진행하였다. 기원별 효소에 따른 저해 활성도를 살펴보면 salivary와 pancreatic ${\alpha}-amylase$, 미생물 기원의 ${\alpha}-glucosidase$에는 탁월한 저해 활성을 보인 반면 돼지 기원의 ${\alpha}-glucosidase$ 저해제에 대해서는 매우 낮은 저해 활성을 보였다. ${\alpha}-Amylase$와 ${\alpha}-glucosidase$의 kinetic을 분석하면 salivary와 pancreatic 두 효소에 모두 경쟁적 저해제로, 효모의 ${\alpha}-glucosidase$에는 비경쟁적과 반경쟁적의 혼합형 저해제로 나타났다. 또한 열과 산성에 대한 안정성을 확인한 결과 비교적 안정적인 것으로 나타났다. 본 추출물의 식이 섭취에 따른 혈당 강하 효과와 체중에 미치는 영향에서는 혈당과 체중 상승을 억제하는 효과가 확인되었고, mRNA수준에서 대퇴근 세포에 있어서 GLUT4의 발현이 증가됨을 확인하였다.

• 한국식품조리과학회지
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• 제14권5호
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• pp.560-565
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• 1998

The purpose of this study was to investigate any differences in the efficiency of various antioxidants for the three types of substrates such as corn oil in water (O/W) emulsion, water in com oil (W/O) emulsion, and bulky corn oil. ${\alpha}$-Tocopherol (${\alpha}$-Toc) at 0.01 or 0.02%, ascorbic acid (AsA), ascorbyl palmitate (AP), and BHT at 0.02% were added separately to the prepared O/W emulsion, W/O emulsion, and bulk oil, and their antioxidative effects were compared. The mixture of ${\alpha}$-Toc ind AsA or AP at the level of 0.02% also was tested to observe any synergistic effect. Oxidation was made by storing at 42${\pm}$1$^{\circ}C$ for 25 days and the oxidative stability was determined by peroxide value and conjugated dienoic acid with time fluctuation of storage. The results were as follows: 1. In case of O/W emulsion, the order of antioxidative effect was AP> ${\alpha}$-Toc+AP>${\alpha}$-Toc+AsA>AsA>BHT. 2. In case of W/O emulsion, the order of antioxidative effect was AsA>AP>${\alpha}$-Toc+AsA>BHT. ${\alpha}$-Toc+AP mixture showed the prooxidant effect rather than synergistic effect. 3. In case of bulk oil, the order of antioxidative effect was AsA>AP>${\alpha}$-Toc+AsA>${\alpha}$-Toc+AP\ulcornerBHT. Therefore, AsA, a hydrophilic antioxidant, was more effective in W/O emulsion system than in O/W emulsion system, while the opposite trend was found in AP, a lipophilic antioxidant. AsA, a hydrophilic antioxidant, was more efficient in bulk oil of anhydrous substrate. ${\alpha}$-Toc showed prooxidant effects in all substrates.

• 약학회지
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• 제41권5호
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• pp.547-553
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• 1997

The purpose of this investigation was to determine the inhibition on $Na^+,\;K^+$-ATPase, cyclic AMP phosphodiesterase and platelet activation by marine sterols isolated from octocorals. Three marine polyhydroxysterols, 7${\alpha},\;8{\alpha}-epoxy-3b{\beta},\;5{\alpha},\;6{\alpha}-trihydroxycholestane (1),\;24-methyl-7{\alpha},\;8{\alpha}-epoxy-3{\beta},\;5{\alpha},\;6{\alpha}-trihydroxycholest-22-ene (2),\;and\;7{\alpha},\;8{\alpha}-epoxy-3{\beta},\;5{\alpha},\;6{\alpha}-trihydroxycholest-22-ene (3)$, were isolated from the Gorgonian Acabaria undulata. Five marine sterols(compound 4, 5, 6, 7, 8) were isolated from the soft coral Alcyonium gracillimum. Three marine polyhydroxysterols (1, 2, 3) and pregna-1. 20-diene-3-one (8) exhibit a potent inhibitory effect on rabbit platelet aggregation induced by collagen and thrombin. Those polyhydroxysterols also exhibit a potent inhibitory effect on cyclic AMP phosphodiesterase. Compound 6 with an unusual cyclic enolether exhibit a inhibitory effect on $Na^+,\;K^+$-ATPase.

• The Korean Journal of Physiology and Pharmacology
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• 제18권3호
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• pp.233-239
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• 2014

The present study was designed to investigate the effect Hypericum Perforatum (HP), on behavioral changes, corticosterone, TNF-${\alpha}$ levels and tryptophan metabolism and disposition in bilateral ovariectomized rats compared to $17{\alpha}$-ethinylestradiol. Behavioral analysis by measuring immobility time in forced swimming test and open field test, serum and hippocampal corticosterone and TNF-${\alpha}$ along with hippocampal kynurenine/tryptophan ratio were determined in mature ovariectomized rats treated orally either by HP at three different doses 125, 250, and 500 mg/kg/day or by $17{\alpha}$-ethinylestradiol $30{\mu}g/kg/day$ for 30 days. Ovariectomized rats showed significant increase in immobility time in the forced swimming test. Along with elevation in serum and hippocampal TNF-${\alpha}$ and corticosterone levels associated with significant increase in hippocampal kynurenine/tryptophan ratio. Immobility time in the forced swimming test was decreased in rats treated by different doses of HP in a dose dependent manner and $17{\alpha}$-ethinylestradiol with no concomitant changes in the open field test. Only Rats treated with HP exhibited significant decrease in the elevated serum and hippocampal TNF-${\alpha}$ and corticosterone, which couldn't explain the associated insignificant effect on hippocampaus kynurenine/tryptophan ratio in comparison to ovariectomized untreated rats. It is concluded that increased tryptophan metabolism toward kynurenine secondary to elevated corticosterone and TNF-${\alpha}$ might be one of the pathohphysiological mechanisms that could explain depression like state observed in this rat model. Further, the observed attenuating effect of HP on TNF-${\alpha}$ and corticosterone could contribute in its antidepressant effect in this animal model by other ways than their effects on tryptophan-kynurenine metabolism pathway.