• Journal of Pharmaceutical Investigation
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• v.25 no.3
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• pp.43-51
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• 1995

The in vitro skin permeability of 16 drugs with a wide span of lipophilicity (log P ranging from -0,95 to 4.40) was evaluated with an ethanol/panasate 800 (tricaprylin, P-800) (40/60) lipophilic binary vehicle and an ethanol/water (60/40) hydrophilic binary vehicle with lauric acid, The skin permeability of the drugs was enhanced by the use of the ethanol/P-800 (40/60) binary vehicle or the ethanol/water (60/40) binary vehicle with lauric acid; permeation rate was increased and lag time' was decreased. The relationship between lipophilicity and skin permeation rate of the drugs showed parabolic shapes with their peaks at much greater hydrophilic range compared with other past references. In the in vivo skin absorption of theophylline using abdominal rat skin, the ethanol/P-800 (40/60)-7% (w/w) ethycellulose gel produced a good feature as a sustained-release preparation, and the ethanol/water (60/40)-3 % (w/w) HPMC gel with lauric acid showed the highest BA value. The results suggest that the lipophilicity of a drug is a main factor for prediction of the skin permeability of the drug and that the ethanol/P-800 (40/60) binary vehicle and ethanol/water (60/40) binary vehicle with lauric acid would be good candidates for clinical transdermal application of hydrophilic drugs.

• Journal of Ginseng Research
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• v.18 no.2
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• pp.108-112
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• 1994

Rats (Sprague Dawley, male, 200 g) were fed with 15% corn oil containing a large quantity of 18 2 (linoleic acid) for 3 weeks, and were followed by feeding the petroleum ether extracts from Korean red ginseng for 3 weeks. cGMP was produced more in platelets prepared from both 15% corn oil and petroleum ether extracts-fed group than in platelets only 15% corn oil-fed group, indicating that the production of cGMP is increased by feeding the petroleum ether extracts. When this platelet was stimulated by phorbol-12-myristate-13-acetate (PMA), the level of cGMP was decreased. However, the platelets in medium containing protein fraction (200 $\mu\textrm{g}$/ml) was stimulated by PMA, the production of cGMP inhibited by PMA was increased by 3 times or more. These results suggest that both the protein fraction and the petroleum ether extracts from Korean red ginseng are synergistic in the productiorl of cGMP, and they may have the antiplatelet effects.

• Proceedings of the Ginseng society Conference
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• 1993.09a
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• pp.94-101
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• 1993

Lipophilic fraction(LF) from Panax ginseng C.A. Meyer inhibited the aggregation of human platelets induced by th rombin(0.1u/$m{\ell}$). LF and Molsidomine(vasodilator) induced the stimulation of cGMP - elevation and 50KD - Phosphorylation. and then the inhibition of 20KD - Phosphorylation in human platelets activated by thrombin. LF also inhibited the $Ca^{2-}-influx$ into platelets. When rat(SD : male) was fed with LF, the level of cGMP was increased in rat platelets stimulated by collagen and thrombin. On the other hand. verapamil, $Ca^{2-}-antagonist$ increased cAMP level ;n platelet stimulated by thrombin. but LF does not affected. However LF potently inhibited the thromboxane $A_2(TXA_2)$ production. The results suggest that the inhibitory effects of LF are mediated by regulation the phosphorylatior. of 50KD via cGMP-elevation and depend upon the decrease of $TXA_2$ level.

• Biomolecules & Therapeutics
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• v.8 no.4
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• pp.293-298
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• 2000

Bergenin is a C-glucoside of 4-O-methyl gallic acid that has been isolated from the cortex of Mallotus japonicus (Euphorbiaceae). Acetylbergenin was synthesized by acetylation from bergenin to increase lipophilic and physiological activities. The therapeutic effects of bergenin and acetylbergenin were evaluated against carbon tetrachloride ($CCl_4$)-induced hepatotoxicity in rats. Bergenin and acetylbergenin were administered orally once daily for successive 5 days, after the intraperitoneal injection of a mixture 0.5 m1/kg of $CCl_4$ in olive oil (1:1). The substantially elevated serum enzymatic activities of alanine/aspartate aminotransferase, sorbitol dehydrogenase and ${\gamma}$-glutamyltransferase induced by $CCl_4$ were restored towards normalization by posttreatment with bergenin and acetylbergenin. Bergenin and acetylbergenin also significantly prevented the elevation of hepatic malondialdehyde formation and depletion of glutathione content induced by $CCl_4$ in a dose dependent fashion. In addition, the decreased activities of glutathione S-transferase and glutathione reductase were restored towards normalization. These results suggest that therapeutic effects of bergenin and acetylbergenin may be related complex mechanisms that involve prevention of lipid peroxidation and preservation of hepatic GSH. The results of this study clearly indicate that bergenin and acetylbergenin have potent hepatothrapeutic action against $CCl_4$-induced hepatotoxicity in rats. In addition, acetylbergenin 50 mgHg showed almost the same levels of hepatoprotective activity as those of bergenin 100 mgAg, indicating the fact that lipophilic acetylbergenin is more effective in the hepatoprotective action against $CCl_4$ than bergenin.

• Textile Coloration and Finishing
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• v.24 no.2
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• pp.138-144
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• 2012

Detergency and soil redeposition of wool fabric in 8 nonionic surfactants (Span 20, 40, 60, 80/Tween 20, 40, 60, 80) and 4 solvents (water, petroleum, perchloroethylene(PCE), decamethylcyclopentasiloxane($D_5$)) were studied. Detergency of wool fabric in water was very low with and without surfactants due to the low wetting and difficulty in penetration of water into the fabric. Lipophilic surfactants improved the detergency of wool fabric in petroleum solvent and PCE. The detergency of wool fabric in $D_5$ was similar to that in petroleum solvent without surfactants. When water was solubilized, Span 20 addition to petroleum solvent and PCE increased the detergency of wool fabric. The detergency for $D_5$ was improved with solubilized water, however, it was lowered when the surfactants were added to the system. Therefore, it is important to formulate appropriate detergents which have good solubility and affinity to silicone for $D_5$ charge system. Hydrophilic surfactants were effective for water and lipophilic surfactants were effective for petroleum solvent and PCE in soil redeposition prevention of wool fabric. The soil redeposition prevention effects are not found in $D_5$ with both Span 20 and Tween 20. The same tendency of results in soil redeposition of wool fabric is observed when water is solubilized.

• Journal of Ginseng Research
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• v.22 no.1
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• pp.1-10
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• 1998

In the present study, to determine whether the antioxidative components of Korean red ginseng protect against radiation damage and the possible relationship among the radioprotective effects and antioxidant actions, the effects of total saponin (200 mg/kg, ip) and lipophilic fraction (200 mg/kg, oral) preferment of mice on the survival ratio, major antioxidant enzymes (SOD, catalase and glutathione peroxidase) activities, glutathione levels and lipid peroxidation in the liver were exiled for 2 weeks after whole ${\gamma}$-body ${\gamma}$-irradiation (6.5 Gy). The 30-day survival ratio increased from 10% to 57% and 40% for mice treated with total saponin and lipophilic fraction, respectively. On day 14 after ${\gamma}$-irradiation, the ginseng total saponin pretreatment produced a slight increase of antioxidant enzymes activities and significantly Increased reduced glutathione (GSH) contents (p<0.05) in the liver compared with non-treated group. Pretreatment with ginseng total saponin significantly deceased GSSG/total GSH ratio (p<0.05) without change of GSSG in the liver and inhibited the radiation-induced incense in the hepatic malondialdehyde levels. (p<0.05) In these results, GSH plays an important role in the liver in several detoxifications and the reduction of lipid peroxides. Thus, it appears that total saponin of red ginseng exerts its radioprotective effect by accelerating the production of endogenous antioxidants, such as glutathione from radiation induced damages and thereby oxygen free radicals.

• Bulletin of the Korean Chemical Society
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• v.14 no.1
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• pp.123-127
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• 1993

New lipophilic Crown-4 compounds of 16-membered rings containing furan (neutral carrier,I), tetrahydrofuran (neutral carrier,II) and lithium complex of the latter (neutral carrier,III) have been synthesized and tested as the active sensors for lithium ion in poly(vinyl chloride) (PVC) membrane electrode, in the presence and absence of an anion excluder, tetrakis(4-chloro-phenyl)borate (KTClPB), 2-nitrophenyl phenyl ether (NPPE), tris(2-ethylhexyl)phosphate (TEHP), o-nitrophenyl octyl ether (NPOE), dioctyl adipate (DOA), bis(2-ethylhexyl)adipate (BEHA), di-n-octylphenyl phosphonate (DOPP) were used as plasticizing solvent mediators. The electrode response function had a nearly Nernstian slope of 54-61 mV per decade (25$^{\circ}$C) within the concentration range of $10^{-1}-10^{-4}$ M LiCl and the detection limits for all electrodes were ca. $5{\times}10^{-4}$ M. The response time of the electrode was faster at the higher lithium concentration and the response of the electrode was stable for longer than 6 months. The sensor membranes exhibit improved response times and increased lifetimes as compared to the system described earlier.

• YAKHAK HOEJI
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• v.36 no.4
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• pp.326-333
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• 1992

A new series of methotrexate analogues was prepared in which the ${\beta}-position$ of the glutamic acid moiety is substituted by the aryl groups. The glutamic acid moiety was modified in order to enhance the lipophilic property. Reaction of N-acetylglicine ester[1] with ethyl 3-arylacrylate derivatives[2] produced trans-3-aryl-2-carboxy-5-pyrrolidone derivatives[3], which were hydrolyzed to give ${\beta}-aryl-glutamic$ acid derivatives[4]. The compounds[4] were treated with the p-aminobenzoic acid moiety and then with the pteridine ring moiety to give ${\beta}-arylmethotrexate$ derivatives[6,7]. These compounds were tested for antibacterial activity against Streptococcus faecium and for antitumor activity against murine leukemias and against human tumor cell lines in vitro. Several compounds showed significant antibacterial activity.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.40 no.3
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• pp.227-236
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• 2014

In this study, O/W and W/S emulsions were prepared by combining oils having different required hydrophilic lipophilic balance (HLB) values under the diverse conditions of HLB values composed of a hydrophilic surfactant and a lipophilic surfactant and their stability was investigated. Results showed that the higher the viscosity of O/W emulsions was as the lower the HLB value of emulsifier and emulsion particle showed a tendency to be a smaller and compact and stabler in centrifugal filtration. W/S emulsions also showed a similar tendency to be a smaller and compact as HLB values of emulsifier was higher and stabler in centrifugal filtration. However, the viscosity of W/S emulsion tended to get lower in HLB conditions of all emulsifiers as the time passed. This indicated that the emulsions had an unstable feature in long-term stability. In conclusion, the results showed opposite to the known theory that O/W emulsion is proper to be applied by nonionic surfactant with a high HLB value and W/S emulsion to be applied by nonionic surfactant with a low HLB value and provide useful information for the cosmetics research and related areas.

• Journal of Ginseng Research
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• v.23 no.3 s.55
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• pp.182-189
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• 1999

For the determination of anti oxidative effects of Korean red ginseng extracts, 100 mg/kg body weight of paraquat(1,1-dimethyl-4,4-bipyrimidinium dichloride) was injected to peritoneal cavity of 6 weeks 23-27 g of ICR mail mice which were pretreated with 200 mg/kg body weight of korean red ginseng extracts(total saponin, water extracts, alcohol extracts, lipophilic extracts) and ascorbic acid for 5 days. Most of mice died of paraquat toxicity within 4 days except only $30\%$ of ascorbic acid group. The hepatic total-SOD activity in liver was highest in ascorbic acid group and lipophilic ginseng extracts group next (p<0.0l). The level of hepatic hydroperoxide was lowest in the order of in alcohol extracts group, lipophilic extracts group and ascorbic acid group (p<0.0l). The highest catalase activity was induced by ascorbic acid followed by water extracts and lipophillic extracts (p<0.01). Finally, the lipid peroxidation level (malondialdehyde:MDA) was the lowest in water extracts group and ascorbic acid next (p<0.01). The highest MDA level was appeared in praquat group and next total saponin group next. In conclusion, the order of effectiveness of antioxidants was found to be ginseng water extracts> ascorbic acid> lipophillic extracts> other ginseng extracts. It was also found that any predominant antioxidant was not effective evenly to all of antioxidant test.