• The Journal of Korean Obstetrics and Gynecology
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• v.28 no.1
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• pp.13-28
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• 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
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• v.6 no.2
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• pp.207-215
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• 1989

The authors studied ED50 of bethanechol on the contractilities of the smooth muscles isolated from various organs of rat under the presence of atropine(a classical competitive blocker of cholinergic muscarinic receptor) or minaprine(a newly developed antidepressant drug) to investigate the pheripheral anticholinergic effect of minaprine. The results were as follows ; 1) There was no significant difference between ED50 of bethanechol in the control group and that under the presence of minaprine $10^{-8}M$ and $10^{-7}M$ in the smooth muscles isolated from the duodenum. 2) There was no significant difference between ED50 of bethanechol in the control group and that under the presence of minaprine $10^{-8}M$ and $10^{-7}M$ in the smooth muscles isolated from the ascending colon. 3) There was significant difference between ED50 of bethanechol in the control group and that under the presence of minaprine $10^{-8}M$ and $10^{-7}M$ in the smooth muscles isolated from the urinary bladder(P<0.01). 4) There was significant difference between ED50 of the atropine $10^{-8}M$ and minaprine ($10^{-8}M$) in the smooth muscles isolated from the urinary bladder(P<0.05).

• YAKHAK HOEJI
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• v.48 no.2
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• pp.117-121
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• 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
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• v.7 no.2
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• pp.181-187
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• 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
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• v.19 no.5
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• pp.416-422
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• 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
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• v.39 no.4
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• pp.281-287
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• 2012

This experiment was conducted to investigate the effect of various type of Magma seawater (MSW) concentrations on plant growth and useful mineral contents in Bletilla striata. In the RO (Reverse Osmosis) and ED (Electronic Distal) treatment, hardness of medium was poored in 3.0 g/L gelrite but increased in 8.0 g/L plant agar, 38,000 and $2,000g/cm^2$ respectably. We analyzed the morphological and physiological characteristics differences of B. striata treated various MSW. Survival frequency of plant and growth (shoot length, shoot diameter, root length, root diameter, shoot/root ratio) were significantly increased in RO and ED treatment at 50% and 10%, especially. Chlorophyll contents in ED treatments were higher than those in control and RO treatment. The content of strontium (Sr) in 20, 50, 75, 100% ED treatment, were higher than those in the control and RO, ED 1, 5, 10% treatment. These results showed that treatment of ED with the range of 20~100% could be used to supply the strontium enriched orchid plant. It is considered that MSW may be applied for use in Magma seawater to promotion of growth and produced functional plant.

• Microbiology and Biotechnology Letters
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• v.10 no.1
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• pp.53-58
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• 1982

In order to obtain anticancer substances from natural products, extracts of dry herbs, which have long been used to treat cancer or canter-like diseases in oriental countries, were screened. Extracts were made with hot water and/or organic solvents. With the extracts we treated murine leukemic L1210 cells growing in Fischer's medium. After 48 hours of incubation, cells were counted and concentrations of dry extracts to achieve 50 percent inhibition of the control growth, ED$_{50}$ values, were determined. Among the 38 species of medicinal plants tested, water extracts of six species showed ED$_{50}$ values of substantially low. Further extraction with organic solvents could reduce their ED$_{50}$ values within the range of the NCI quality control limit. The promising species as potential sources of anti-cancer substances included Cinnamomum cassia, Citrus trifoliata, Coptis japonica, Panax ginseng, Phellodendron amurense, and Scutellaria baikalensis.

• Archives of Pharmacal Research
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• v.9 no.4
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• pp.215-217
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• 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
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• v.15 no.1
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• pp.40-45
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• 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.

• Korean Journal of Fisheries and Aquatic Sciences
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• v.50 no.4
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• pp.366-371
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• 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.