• Journal of Pharmaceutical Investigation
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• 제25권3호spc1호
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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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• 제18권2호
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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.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1993년도 학술대회지
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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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• 제8권4호
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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.

• 한국염색가공학회지
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• 제24권2호
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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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• 제22권1호
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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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• 제14권1호
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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.

• 약학회지
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• 제36권4호
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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.

• 대한화장품학회지
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• 제40권3호
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• pp.227-236
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• 2014

본 연구에서는 친수성 계면활성제와 친유성 계면활성제가 조합된 다양한 HLB (Hydrophilic Lipophilic Balance) 값을 갖는 유화 시스템의 조건에서, required HLB 값이 각기 다른 오일들을 적용하여 제조한 O/W 및 W/S 에멀젼들의 특성 및 유화 안정성을 조사해 보았다. 그 결과 O/W 에멀젼은 유화제의 HLB 값이 낮을수록 점도가 높고, 유화입자는 작고 조밀한 경향을 나타내었으며, 원심분리에서도 더 안정한 경향을 나타내었다. W/S 에멀젼은 유화제의 HLB 값이 높을수록 유화입자는 작고 조밀해지는 경향을 나타내었으며, 원심분리에서도 더 안정한 경향을 나타내었다. 그러나 W/S 에멀젼은 시간이 경과할수록 모든 유화제의 HLB 조건에서 점도가 낮아지는 경향이 나타나 장기 안정도에서는 불안정한 특성을 나타내었다. 이번 연구의 결과는 O/W 에멀젼은 HLB 값이 높은 비이온 계면활성제의 적용이 적합하며 W/S 에멀젼은 HLB 값이 낮은 비이온 계면활성제의 적용이 적합하다는 기본 이론과 상반되는 결과로서 앞으로의 화장품 연구 개발 시 유용한 연구 자료가 될 것으로 사료된다.

• Journal of Ginseng Research
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• 제23권3호
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• pp.182-189
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• 1999

본 연구에서 홍삼의 항산화 효과를 알아보기 위하여 생쥐에 홍삼의 총사포닌 분획, 수용성 추출물, 알코올 추출물, 지용성 분획과 ascorbic acid를 투여(200mg/kg/0.1ml)한 후 paraquat(PQ) 100mg/kg을 복강투여 하였을 때 활성산소 라디칼의 생성을 촉진시킨 후 간에서 $H_2O_2$ 함량, SOD, catalase, GP의 량을 측정한 결과 총사포닌 투여군을 제외한 홍삼추출물 투여 후 PQ투여군 치가 PQ 단독 처리군에 비하여 $H_2O_2$ 생성량이 유의성(p<0.01) 있게 감소 억제되었다. 한편 항산화효소의 활성은 PQ단독 처리군에 비하여 SOD는 홍삼추출물 투여 모든 군에서 유의성있는 증가를 하였고, catalase는 수용성 추출물과 지용성 분획 투여군에서 증가하였으며, CP는 지용성 분획에서 유의성(p<0.01)있는 증가를 보였다. 그리고 지질과산화에서 PQ처리는 지질과산화 경향 MDA량이 증가되는 것을 볼 수 있었고, 홍삼추출물 투여는 PQ단독 처리군에 비하여 지질과산화 경향에서 MDA량은 억제되는 경향을 보였다.