• Proceedings of the Korean Society of Applied Pharmacology
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• 1998.11a
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• pp.178-178
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• 1998

We reported that the hexane fraction of Torilis Fructus have an anti-inflammatory and analgesic effect. Therefore, in order to isolate the active compound, the hexan fraction of Torilis Fructus was chromatographed on silica gel column. The subfraction of hexane fraction was crystallized as colorless stout needles. The chemical structure of this compound was verified to be torilin through m.p., UV, IR, GC-MS, and NMR spectral data. In pharmacological tests, torilin exhibited strong anticarrageenan activity at the dose of 90 and 270 mg/kg, p.o. in rats, and it had inhibitory effect on the vascular permeability at the dose of 30 and 90 mg/kg, p.o. in mice. Torilin showed potent inhibition of leucocyte emigration in CMC-pouch at the dose of 3 and 9 mg/rat, s.c. Torilin have the analgesic effect at the dose of 30, 90 and 270 mg/kg, p.o. in both of the acetic acid- and phenyl-p-benzoquinone-induced writhing syndrome. It also increased the pain threshold at the dose of 30, 90 and 270 mg/kg, p.o. in the tail pressure method and the Randall-Selitto method. Torilin did not show a hypothermic action at the dose of 30 and 90 mg/kg, p.o. in mice. The acute toxicity of torilin was very weak: the LD$\_$50/ value was more than 5000 mg/kg, p.o. and 2000 mg/kg, Lp. in mice. From the above mentioned results, it was suggested that torilin had potent anti-inflammatory and analgesic activities in animals.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1998.11a
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• pp.89-94
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• 1998

Marine sponges are recognized as a plentiful source of diverse biologically active secondary metabolites. Recently, we have initiated a research to discover antitumor constituents from the marine sponges collected from Korean Waters. Marine sponges collected from the South Sea of Korea were screened for several biological activities including such as brine shrimp lethality and cytotoxicity. Significant brine shrimp lethality was detected in the crude extract of a two-sponge association of Poecillastra sp. and Jaspis sp. A cross-section of this sample showed two layers of morphologically distinct sponges. The thin and dirty yellow outer layer was identified as Poecillastra sp. (Pachastrellidae), the surface of which was very rough. The light-grey inner layer was identified as Jaspis sp. (Jaspidae), the surface of which was smooth. This two-sponge association appears to be consistent as these sponges were always found in associated form regardless of collection site or collection period. Investigation of the bioactive constituents monitored by brine shrimp lethality assay led to the isolation of pectenotoxin II (PTX2) and psammaplin A as causative compounds for the brine shrimp lethality. $^1$H- and $\^$13/C-nmr signals of PTX2 was fully assigned utilizing TOCSY, HETCOR, Long-range HETCOR, and Homonuclear J-resolved 2D experiments. PTX2 displayed very potent and selective cytotoxicities in the 60 cell line panel antitumor assay at the NCI. PTX2 has progressed to acute toxicity determination and in vivo antitumor assay at the NCI (Table 1). However, significant in vitro antitumor activity of PTX2 can not be affirmed in the in vivo assay.

• Journal of Chest Surgery
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• v.39 no.11 s.268
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• pp.854-857
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• 2006

The patient was an eight-year-old female. She was diagnosed as dilated cardiomyopathy. She was supported with bi-ventricular assist because of heart failure for 15 days. After 7 days, she was suffered from prerenal type ARF and support with continuous veno-veno hemodyalisis(CVVHD). And then heart transplantation was performed, heart donor's blood type was A. Immune suppressants were used after due consideration for renal toxicity. ARF was resolved on post operative $14^{th}$ day. She was discharged on post operative $52^{nd}$ day without any specific post operative complication. She has been followed up without any immune rejection reaction upto 14 months.

• Journal of Pharmaceutical Investigation
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• v.22 no.3
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• pp.185-196
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• 1992

To assess its suitability as a prodrug of 5-fluorouracil (5-FU), 1-glycyloxymethyl-5-FU HCl (GFU), a 5-fluorouracil derivative having a glycyloxymethyl group at the N-l position was synthetized. Its physicochemical properties and hydrolysis kinetics, in aqueous solution of pH $1{\sim}10$ and in the presence of human plasma or rat liver homogenate were studied. Its acute toxicity and antitumor activity against sarcoma 180 were also examined, GFU showed higher lipid/water partition coefficient than 5-FU. The calculated $pK_{\alpha}$ values of 5-FU and GFU were 8.02 and 7,20, respectively. The decomposition rates of GFU in aqueous solution showed a pH-dependence over the pH range used, which could be ascribed to solvent catalysed hydrolysis reaction at pH lower than 4,16 and to specific hydroxide ion hydrolysis reaction at pH higher than 4,16, The half-life of GFU was 6,9 min in 80% human plasma solution and less than 3 min in rat liver homogenate at $37^{\circ}C$, The $LD_{50}$ value of 5-FU was 240 mg/kg while that of GFU was 440.6 mg/kg (226 mg as 5-FU). Both of 5FU and GFU showed a strong antitumor activity, Therapeutic ratios of 5-FU and GFU were 3.07 and 3.55, respectively.

• Applied Microscopy
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• v.36 no.4
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• pp.235-250
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• 2006

A protective effect of activated charcoal against the acute lead poisoning of kidney was studied in mile. Mice approximately 30 gm in weight were grouped into the control, lead acetate-treated, and activated charcoal-treated after lead acetate groups. Lead acetate (60 mg/kg) and activated charcoal (40mg/kg) were delivered orally. Serum AST, ALT and glucose were measured and the ultrastructural alteration of liver was examined by electron microscopy. Activated charcoal decreased the increase of serum AST, ALT and glucose levels induced by lead. Lead acetate-treated hepatic cells characterized by irregular nuclei, enlarged and reduced number of mitochodria, enlarged rough endoplasmic reticulum, loss of riboscomes. Cells treated with activated charcoal were similar to those of the control group. In conclusion, activated charcoal may protect the lead-induced toxicity on liver.

• Fisheries and Aquatic Sciences
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• v.12 no.1
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• pp.29-34
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• 2009

Fifty seven species of common seaweed from the coast of Korea were screened for antifungal activity against Malassezia species. Seaweeds as a source of bioactive compounds are able to produce a great variety of secondary metabolites with different activities. There are numerous reports on the biological activities of seaweeds against human pathogens, fungi, and yeasts, but only few contain data regarding inhibitory effects against Malassezia sp., a major cause of dandruff and seborrheic dermatitis. To help address this paucity of information, this work was carried out to examine the antifungal effects of seaweed extracts against M. furfur and M. restricta. Of the fifty seven species of marine algae screened for their potential antifungal activity, only 17 species (29.8%) exhibited inhibitory activity. In agar disc diffusion method, the ether extracts of Corallina pilulifera, Enteromorpha linza, Laminaria japonica, Symphyocladia latiuscula and Ulva sp. showed strong antifungal activity. To identify major constituents in seaweed extracts, four selected extracts were analyzed on' a GC-MS equipped with a flame ionization detector, and compared to spectral data from databases WILEY229.LIB and NIST107.LIB. Most constituents in seaweed extracts are fatty acid-related compounds. When we evaluated any acute toxicity, the ether extracts of the selected four species were not toxic in mice. According to these results, it can be suggested that these seaweed extracts are valuable for the development of therapeutic agents in treating dandruff and seborrheic dermatitis. Further investigations to determine its bioactive compound(s) are currently in progress.

• The Korea Journal of Herbology
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• v.26 no.3
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• pp.65-73
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• 2011

Objectives : The present study was evaluated the protective roles of Spatholobi Caulis in hepatotoxic rats due to APAP overdose. Methods : In experiments, rats were orally administrated with the aqueous extract of Spatholobi Caulis (SCE; 50, 100 mg/kg) for 4 days and then, orally gavage with APAP (1.2 g/kg) to induce acute liver damage. Results : Oral injection of APAP caused severe hepatic injury. Plasma ALT, AST and LDH levels were significantly elevated, but SCE significantly decreased ALT, AST and LDH to the normal level. In histopathological analysis, peripheral hemorrhage around portal triads and central necrosis around central veins were founded after APAP treatment. However, these histopathological changes were recovered by SCE pretreatment. SCE also decreased the percentage of generative hepatic regions (%/$mm^2$ hepatic parenchyma), the numbers of inflammatory cells (cells/$mm^2$ hepatic parenchyma) and the number of degenerative hepatic cells (N/100 hepatic cellls) which were significantly elevated after APAP injection. Furthermore, SCE down-regulated the contents of hepatic MDA and up-regulated hepatic GSH. SCE also inhibited the decrease in the expression of pro-caspase-3 by APAP treatment. Conclusions : Collectively, these data indicate that SCE protected APAP-induced hapatic damages through antioxidative and anti-apoptotic process. These findings the significant therapeutic potential of SCE during APAP-induced liver injury.

• Proceedings of the Korean Environmental Health Society Conference
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• 2004.06a
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• pp.173-177
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• 2004

The acute toxicities of two major anti-pathogenic veterinary medicines, i.e., ciprofloxacin and enrofloxacin, and six benzimidazole anthelmintics, i.e., albendazole, thiabendazole, flubendazole, febantel, fenbendazole, and oxfendazole, were evaluated with a marine bacterium, Vibrio fischeri, and invertebrate Daphnia magna. These veterinary medical products have been widely used for farm animals, but their impact on aquatic fauna has seldom been investigated. In general, daphnids responded as much as 3 orders of magnitude more sensitively to the tested pharmaceuticals than the microbes. For Daphnia, the most toxic product among the tested anthelmintics was fenbendazole, followed by flubendazole > albendazole ${\approx}$ febantel > thiabendazole > oxfendazole. Daphnids' EC50 values obtained from 48 to 96 hrs of fenbendazole exposure ranged from 2.7 to 6.3 ug/L. The mixture toxicity of the test pharmaceuticals was generally additive in nature and was well predicted by a concentration addition model. Using the predicted no effect concentrations (PNECs) of the benzimidazole derivatives estimated from this study, and predicted environmental concentrations (PECs) of these pharmaceuticals, the risk quotients of each anthelmintics were calculated. Most of the test anthelmintic compounds resulted in risk quotients greater than 1. Especially, risk quotient for fenbendazole was 2,791, which strongly indicates this compound might cause severe ecological consequences, should no future action be taken. This study is the first report on the aquatic toxicities and potential ecological risk of major anthelmintic and antimicrobial veterinary products in Korea. The result of this study provides information necessary for conducting more detailed ecological risk assessment of pharmaceutical products in ambient water and guiding proper management decision.

• The Journal of Korean Medicine
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• v.29 no.5
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• pp.52-66
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• 2008

Objectives :Ginkgo-Chunghyul-dan (GCHD) is newly developed herbal medicine to prevent and treat stroke. In this study, we investigated whether the GCHD had antioxidant activity and anti-platelet aggregation effect in vitro and hypolipidemic activities in vivo. Methods :Anti-oxidant activity of GCHD was measured using the Blois method, anti-platelet effect of GCHD was assessed by the Born method, and hypolipidemic activities of GCHD were evaluated in corn oil- or Triton WR-1339-induced and cholesterol-fed rats. Results :GCHD showed anti-oxidant activity in the study inhibiting the formation of 1-diphenyl-2-picrylhydrazyl radicals and xanthine oxidase activity. GCHD had anti-platelet aggregation activity. GCHD significantly lowered total cholesterol (TC), triglyceride (TG), and low density lipoprotein cholesterol (LDL-C) in high cholesterol diet and Triton WR-1339 induced model TG in corn oil-induced model. GCHD had no acute toxicity at a single dosage. Conclusion : These results suggest that GCHD has the potential to treat hyperlipidemia and stroke.

• The Journal of Pediatrics of Korean Medicine
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• v.29 no.2
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• pp.26-36
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• 2015

Objectives In this study, effect of Geumsuyukgunjeon (GYJ) on the increase in airway epithelial mucosubstances of rats with acute bronchitis and EGF-induced MUC5AC mucin production from human airway epithelial cells were investigated. Materials and Methods Hypersecretion of airway mucus was induced by exposure of rats to SO2 during 3 weeks. Effect of orally-administered GYJ during 2 weeks on increase in airway epithelial mucosubstances from tracheal goblet cells of rats was assesed using histopathological analysis after staining the epithelial tissue with PAS-alcian blue. Possible cytotoxicity of GYJ was assessed by examining the potential damage of kidney and liver functions by measuring serum GOT/GPT activities and serum BUN and creatinine concentrations of rats and the body weight gain during experiment, after administering GYJ orally. Effect of GYJ on EGF-induced MUC5AC mucin production from human airway epithelial cells (A549) was investigated. Confluent A549 cells were pretreated for 30 min in the presence of GYJ and treated with EGF (25 ng/ml) for 24 hrs, to assess the effect of GYJ on EGF-induced MUC5AC mucin production using enzyme-linked immunosorbent assay (ELISA). Results (1) GYJ decreased the amount of intraepithelial mucosubstances of trachea of rats. (2) GYJ did not show kidney and liver toxicities and did not affect body weight gain of rats during experiment. (3) GYJ significantly inhibited EGF-induced MUC5AC mucin production from A549 cells. Conclusions The result from the present study suggests that GYJ might control both the mucus hypersecretion in vivo and do not show in vivo toxicity to liver and kidney functions after oral administration and the production of pulmonary mucin.