• 대한한방부인과학회지
• /
• 제28권1호
• /
• pp.13-28
• /
• 2015

Objectives: To observe the in vitro anti-inflammatory effects of Hyunbulikyung-tang aqueous extracts (HBLKT) and the possible synergic combination effects with a nonsteroidal anti-inflammatory drug, piroxicam. Methods: Anti-inflammatory effects of HBLKT (yield=16.17%) were observed on LPS activated raw 264.7 cells based on $ED_{50}$ to cell viability, NO, $PGE_2$, $TNF-{\alpha}$, $IL-1{\beta}$ and IL-6 productions as compared with piroxicam, in the present study. In addition, the combination effects of HBLKT with piroxicam were observed after treatment of HBLKT 1/4 $ED_{50}$ + piroxicam 1/4 $ED_{50}$, 1/8 $ED_{50}$, 1/16 $ED_{50}$, 1/32 $ED_{50}$ and 1/64 $ED_{50}$ concentrations, respectively. Results: Significant (p<0.01 or p<0.05) increases of cell viabilities and decreases of NO, $PGE_2$, $TNF-{\alpha}$, $IL-1{\beta}$ and IL-6 cytokine releases were detected in HBLKT 1/4 $ED_{50}$ + piroxicam 1/4 $ED_{50}$, 1/8 $ED_{50}$, 1/16 $ED_{50}$ and 1/32 $ED_{50}$ concentration co-treatment as compared with each of single 1/4 $ED_{50}$ concentration of piroxicam and HBLKT treatments, respectively. Although significant (p<0.01 or p<0.05) increases of cell viabilities and decreases of NO, $PGE_2$, $TNF-{\alpha}$, $IL-1{\beta}$ and IL-6 cytokine releases were also demonstrated in piroxicam 1/64 $ED_{50}$ + HBLKT 1/4 $ED_{50}$ co-treatment as compared with LPS control, no significant changes were detected as compared with each of single 1/4 $ED_{50}$ concentration of piroxicam and HBLKT treatments, in this experiment. Conclusions: Hyunbulikyung-tang showed cell protective and anti-inflammatory effects against LPS activated raw 264.7 cells. It, therefore, expected that HBLKT will be showed favorable effects to relieve dysmenorrhea related to over expressed inflammatory cytokines, and it also expected that the clinical dosages of piroxicam can be reduced as 1/8 levels as combination with HBLKT.

• Journal of Yeungnam Medical Science
• /
• 제6권2호
• /
• pp.207-215
• /
• 1989

Minaprine의 말초 항콜린 작용 유무를 판별하기 위하여 백서를 단두 사혈하여 적출된 십이지장, 상행결장, 방광으로부터의 평활근 절편을 사용하여 atropine의 bethanechol 작용 차단 능력을 기준으로 하여 minaprine의 차단 능력을 비교하여 다음과 같은 결과를 얻었다. 십이지장 절편에서 atropine $10^{-8}M$ 존재하에서의 bethanechol에 대한 ED50는 대조군에 비하여 유의한 차이를 보였으나(P<0.01), minaprine $10^{-8}M$ 및 $10^{-7}M$ 존재하의 bethanechol에 대한 ED50는 대조군에 비하여 유의한 차이가 없었다. 상행결장 절편에서 atropine $10^{-8}M$ 존재하에서의 bethanechol에 대한 ED50는 대조군에 비하여 유의한 차이를 보였으나(P<0.01), minaprine $10^{-8}M$ 및 $10^{-7}M$ 존재하의 bethanechol에 대한 ED50는 대조군에 비하여 유의한 차이가 없었다. 방광 절편에서 atropine $10^{-8}M$ 존재하에서의 bethanechol에 대한 ED50는 대조군에 비하여 유의한 차이를 보였으며(P<0.01), minaprine $10^{-8}M$ 및 $10^{-7}M$ 존재하의 bethanechol에 대한 ED50는 대조군에 비하여 유의한 차이를 보였다.(P<0.01) 그러나 minaprine $10^{-8}M$ 존재하의 bethanechol에 대한 ED50는 atropine $10^{-8}M$ 존재하의 bethanechol에 대한 ED50에 비해 유의한 차이를 보였다.(P<0.05)

• 약학회지
• /
• 제48권2호
• /
• pp.117-121
• /
• 2004

Ranunculin, a potent cytotoxic component of P. koreana, was synthesized by reacting (s)-(-)-5-(hydroxymethyl)-2(5H)-furanone with 2,3,4,6-tetra-O-acetyl-$\alpha$-D-glucopyranosyl bromide and successive removal of the acetyl protecting group by 0.5 M HCl/MeOH. A new deacetylation process of the intermediate tetraacetylranunculin was deviced giving a yield of 83% of ranunculin. Protoanemonin, the cytotoxic structural moiety of ranunculin, was synthesized by dehydration of (s)-(-)-5-hydroxymethyl-2(5H)-furanone. Ranunculin showed a moderate cytototoxic activity against A-549 (ED$_{50}$=7.53 $\mu\textrm{g}$/$m\ell$), NIH3T (ED$_{50}$=13.6$\mu\textrm{g}$/$m\ell$), and SK-OV-3 (ED$_{50}$=17.5 $\mu\textrm{g}$/$m\ell$). Meanwhile, protoanemonin also exhibited moderate cytotoxicity against A-549 (ED$_{50}$=9.38 $\mu\textrm{g}$/$m\ell$), NIH3T (ED$_{50}$=13.8 $\mu\textrm{g}$/$m\ell$), and SK-OV-3 (ED$_{50}$=15.1 $\mu\textrm{g}$/$m\ell$). It was found that both of the synthetic products showed a potenter cytotoxicity against A-549.ainst A-549.

• The Korean Journal of Pain
• /
• 제7권2호
• /
• pp.181-187
• /
• 1994

The MAC($ED_{50}$)values of enflurane, fentanyl, and nalbuphine-enflurane under 65% $N_2O$ were determined in 76 Sprague-Dawley rats using the tail-clamp technique to compare the equipotent effects of intravenous and inhaled anesthetics. The rats were divided into 3 groups: enfluarne, fentanyl, and nalbuphine-enflurane. Results were as follows: 1) The MAC value of enflurane under 65% $N_2O$ was $1.160{\pm}0.05%$ and after subcutaneous nalbuphine 20 mg/kg injection, the values were 1.08% at 60min and 0.99% at 90min. 2) The lowest $ED_{50}$ for fentanyl was 26.8 ${\mu}g$/kg at 15 min, and the $ED_{50}$, 30, 45, and 60min after the injection were 36.2, 39.7, and 44.7 ${\mu}g$/kg, respectively. 3) On arterial blood gas analysis under 65% $N_2O$-1MAC($ED_{50}$), fentanyl and nalbuphine-enflurane groups showed mild increase in $PaCO_2$, but there were no significant differences among 3 groups. Fentanyl group showed significant difference in pH compared with enfluarane and nalbuphine-enflurane groups. 4) Rats injected with high dose fentanyl(above $40{\mu}g$) displayed rigidity and respiratory depression.

• Archives of Pharmacal Research
• /
• 제19권5호
• /
• pp.416-422
• /
• 1996

Twenty one phenylacetylshikonin analogues were synthesized from various subsitituted phenyl acetic acids and their cytotoxicity values against A549, K562 and L1210 cell lines and antitumor action in mice bearing S-180 cells were measured. All of phenylacetylshikonin analogues expressed a potent cytotoxicity $(ED_{50}, 0.1-1.80{\mu}g/ml)$ against L1210 and K562 cells. L1210 cells were the most sensitive to shikonin analogues among these cells. Except 4-methosyphenylacetylshikonin $(0.098 {\mu}g/ml)$, and a-acetoxyphenylacetylshikonin $(0.10 {\mu}g/ml)$, all other shikonin derivatives sshowed higher $ED_{50}$ values than phenylacetylshikonin $(0.13{\mu}g/ml)$, in L1210. In K562 cell, a-substitution of phenylacetylshikonin $(0.1{\mu}g/ml)$, while other subsitutions increased it slightly; 4-methoxyphenylacetylshikonin $(0.033{\mu}g/ml)$ showed a exceptionally good cytotoxicity against K562 cell. 4-Halogenation tended to decrease the cytotoxic effect on L1210 cells, while it enhanced the effect on K562; 4-bromophenylacetyl $$[ED_{50};(L1210)=1.76{\mu}g/ml, ;ED_{50};(K 562)=0.32 {\mu}g/ml]$$ and 4-chlorophenylacetyl shikonin $$[ED_{50};(L1210)=1.64 {\mu}g/ml, ;ED_{50};(K562)=0.32 {\mu}g/ml]$$. In contrast, A549 cells were much less sensitive to these shikonin analogues which showed $ED_{50}$ values of$1.5-1.35 {\mu}g/ml)$.Most of phenylacetylshikonin derivatives showed good antitumor activity in mice bearing S-180 cells. a-A-cetoxyphenylacetylshikonin and 4-dimethylaminophenylacetylshikonin showed highest T/C value (192-195%), implying that introduction of a-acetyl or of 4-dimethylamino group enhanced the antitumor activity as shown for 4-dimethylaminophenylacetylshikonin (T/C, 192%). It might be due to improvement of water solubility by dimethylamino group in the molecule.

• Journal of Plant Biotechnology
• /
• 제39권4호
• /
• pp.281-287
• /
• 2012

본 연구에서는 용암해수가 지닌 독특한 미네랄 구성을 바탕으로 자란의 생육에 적합한 농도를 규명하기 위해 실험을 수행하였다. 자란의 기내배양용 고체배지구성을 위해 30 g/L sucrose와 3.0과 8.0 g/L의 gelrite 및 plant agar를 동일하게 처리한 MS 배지와 RO(Reverse Osmosis) 탈염수, ED(Electrodialsis) 탈염수 배지를 각각 제조하여 배지경도를 측정한 결과, plant agar가 첨가된 MS, RO, 및 ED 배지의 경도는 각각 60,000, 40,000 및 $38,000g/cm^2$의 경도가 측정되었다. 하지만 gelrite가 첨가된 배지는 MS를 제외한 RO, ED배지는 $2,000g/cm^2$ 내외의 경도를 보였다. 제조된 배지에서 식물체의 생육을 확인한 결과, RO 탈염수 0%에서는 88%, RO 50%에서는 57%, RO 100%에서는 31%의 생존율을 보였다. 하지만 잎 길이, 엽폭은 모두 RO 탈염수 100%에서 높았다. ED배지는 ED 100%를 제외한 배지에서 모두 양호한 생장을 보였다. 엽록소 함량 분석을 통한 생리적 건전도를 측정한 결과, 대조구에서는 총엽록소 함량이 66.3 ug/ml인데 비해 RO 10%, RO 50%, RO 100%, ED 10%, ED 50%, ED 100%에서는 각각 77.3, 69.3, 76.4, 79.0, 75.7, 74.4 ug/ml로 모두 대조구보다 높은 총엽록소 함량을 나타냈다. 또한 용암해수 내 유용성분의 식물체내로의 축적은 스토론튬, 바나듐, 셀레늄 등이 원활하게 이루어짐을 확인한 바, 용암해수를 이용한 식물조직배양용 배지로의 산업적 이용가치가 높을 것으로 보이고 더 나아가 용암해수가 원예작물뿐만 아니라 유용성분 함유 약용작물의 생산에도 충분히 활용 가능할 것으로 사료된다.

• 한국미생물·생명공학회지
• /
• 제10권1호
• /
• pp.53-58
• /
• 1982

천연물 가운데서 항암물질을 얻을 목적으로 동양에서 오랫동안 암이나 암에 비슷한 질병의 치료에 씌여온 한약재를 물이나 유기용매로서 추출하여 검색하였다. Fischer배지에 자라는 L1210 세포에 추출물을 첨가한 다음 48시간 후에 세포수를 헤아려 생장을 50% 억제할 수 있는 추출물의 농도를 나타내는 ED$_{50}$값을 측정하였다. 물로서 추출한 38종의 한약재 가운데서 6종이 낮은 ED$_{50}$값을 나타냈다. 이들을 다시 유기용매로서 추출하므로써 ED$_{50}$값이 더욱 떨어져 NCI의 품질관리범위 치역내에 들어갔다. 항암제원으로 유망시되는 한약재로서 Cinnamomum cassia, Citrus trifoliata, Coptis japonica, Panax ginseng, Phellodendron amurense, Scutellaria baikalensis를 들 수가 있다.

• Archives of Pharmacal Research
• /
• 제9권4호
• /
• pp.215-217
• /
• 1986

Steroidal nitrosoureas have been synthesized and their antitumor activity on L 1210 cells was evaluated, N-(2-Chloroethyl)-N-nitrosocarbamoyl-3-aza-A-homo-5$\alpha$-cholestane (5a) showed significantly low $ED_{50}$ value of 1.6 $\nu$g/ml whose activity is equivalent to that of methyl-CCNU ($ED_{50}$ = 1.7 mg/ml).

• Biomolecules & Therapeutics
• /
• 제15권1호
• /
• pp.40-45
• /
• 2007

The vascular relaxant effects on isolated rat aorta of amlodipine camsylates (S-, R-enantiomer, and R/S-racemate), were evaluated and compared with that of S-amlodipine besylate. Furthermore, antihypertensive effects were measured in spontaneously hypertensive rat (SHR). The S-amlodipine camsylate concentration-dependently inhibited $Ca^{2+}$-induced contraction of rat aorta with a very slow onset of action (reached its maximum at 3.5h; $ED_{50}:\;1.50\;{\pm}\;0.24$ nM), having a potency 2-fold higher than those of R/S-amlodipine camsylate $(ED_{50}:\;3.36\;{\pm}\;0.91\;nM)$ and similar to those of S-amlodipine besylate $(ED_{50}:\;1.44\;{\pm}\;0.14\;nM)$, whereas the R-amlodipine camsylate has 590-fold lower vasorelaxant activity $(ED_{50}:\;886.4\;{\pm}\;49.7\;nM)$. In SHR, orally administered S-amlodipine camsylate produced a dose-dependent and long-lasting (>>10 h) antihypertensive effect $(ED_{20}:\;0.89\;mg/kg)$, with a potency 2-fold higher than those of R/S-amlodipine camsylate $(ED_{20}:\;1.82\;mg/kg)$ and similar to those of S-amlodipine besylate $(ED_{20}:\;0.71\;mg/kg)$. In contrast, the R-amlodipine camsylate has no effect even-though administrated high concentration 10 mg/kg. These results suggest that S-amlodipine camsylate has the potency and long-lasting antihypertensive activity as single enantiomer drug, and its antihypertensive effect is not significantly different to that of S-amlodipine besylate.

• 한국수산과학회지
• /
• 제50권4호
• /
• pp.366-371
• /
• 2017

Six experimental diets for juvenile sea cucumbers Apostichopus japonicus were evaluated and compared with current commercial diets. Sea cucumbers (50 per tank; initial mean weight $2.3{\pm}0.1g$) in three replicates of seven groups were fed one of six experimental diets (ED1, 20% wild-harvested Sargassum thunbergii powder; ED2, 20% commercial S. thunbergii powder; ED3, 20% Undaria pinnatifida and Ascophyllum nodosum powders; ED4, 40% U. pinnatifida and A. nodosum powders; ED5, 10% brewer's yeast; and ED6, 10% sea shell powder) or a commercial diet (CD) for 28 weeks. The survival rate in all groups was 85-94%, with no significant difference among the experimental groups. The mean body weight of the sea cucumbers was significantly different among the experimental groups 6 weeks after the feeding trial. The final mean weight of the sea cucumbers was highest in ED1, ED3, and ED4, followed by ED6, ED5, ED2, and CD, in decreasing order. The results of this study suggest that U. pinnatifida and A. nodosum powders could provide a substitute for the S. thunbergii powder commonly used in commercial sea cucumber diets. Thus, the EP4 diet formulation, which contains no S. thunbergii, could be used as a practical feed for juvenile sea cucumbers.