• Korean Journal of Plant Resources
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• 제24권2호
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• pp.236-242
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• 2011

In this present study, we investigated the anti-oxidant activity, the inhibition ability of lipid peroxidation, and the protective effect of cow pulmonary epithelium (CPAE) cells under oxidative stress using green tea and 3 types of fermented teas of Jeju Island. To compare the physiological activity of non-fermented and 3 types of fermented teas, the fermented time was controlled with 0 hr. (non fermented tea, G), 12 hrs. (20% fermented tea, F20), 17 hrs. (50% fermented tea, F50) and 24 hrs. (80% fermented tea, F80), respectively. Scavenging ability on DPPH radicals of 80 ${\mu}g/mL$ concentration of F20 was similar to that of 50 ${\mu}M$ epigallocatechin gallate (EGCG) but it was stronger than those of G, F50 and F80. All extracts tested inhibited LDL oxidation but G and F20 inhibited LDL oxidation 25~30% more than F50 and F80 at 40 ${\mu}g/mL$ concentration which was similar to that of 50 ${\mu}M$ EGCG. We observed that the CPAE cells treated with the tea extracts had a significant increase in cell viability, especially the cells under oxidative stress with 1 mM $H_2O_2$ as compared with the control group (no treatment with tea extracts). These findings suggested that all tea extracts containing fermented tea had a protective effect on oxidative stressed CPAE cells through their free radical scavenging activity. It can be concluded that F20 extracted from 20% fermented tea has the most significant antioxidative effects that inhibit lipid peroxidation and protect the CPAE cells under oxidative stress.

• Journal of Pharmaceutical Investigation
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• 제30권3호
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• pp.191-199
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• 2000

Genomics is providing targets faster than we can validate them and combinatorial chemistry is providing new chemical entities faster than we can screen them. Historically, the drug discovery cascade has been established as a sequential process initiated with a potency screening against a selected biological target. In this sequential process, pharmacokinetics was often regarded as a low-throughput activity. Typically, limited pharmacokinetics studies would be conducted prior to acceptance of a compound for safety evaluation and, as a result, compounds often failed to reach a clinical testing due to unfavorable pharmacokinetic characteristics. A new paradigm in drug discovery has emerged in which the entire sample collection is rapidly screened using robotized high-throughput assays at the outset of the program. Higher-throughput pharmacokinetics (HTPK) is being achieved through introduction of new techniques, including automation for sample preparation and new experimental approaches. A number of in vitro and in vivo methods are being developed for the HTPK. In vitro studies, in which many cell lines are used to screen absorption and metabolism, are generally faster than in vivo screening, and, in this sense, in vitro screening is often considered as a real HTPK. Despite the elegance of the in vitro models, however, in vivo screenings are always essential for the final confirmation. Among these in vivo methods, cassette dosing technique, is believed the methods that is applicable in the screening of pharmacokinetics of many compounds at a time. The widespread use of liquid chromatography (LC) interfaced to mass spectrometry (MS) or tandem mass spectrometry (MS/MS) allowed the feasibility of the cassette dosing technique. Another approach to increase the throughput of in vivo screening of pharmacokinetics is to reduce the number of sample analysis. Two common approaches are used for this purpose. First, samples from identical study designs but that contain different drug candidate can be pooled to produce single set of samples, thus, reducing sample to be analyzed. Second, for a single test compound, serial plasma samples can be pooled to produce a single composite sample for analysis. In this review, we validated the issue whether the second method can be applied to practical screening of in vivo pharmacokinetics using data from seven of our previous bioequivalence studies. For a given drug, equally spaced serial plasma samples were pooled to achieve a 'Pooled Concentration' for the drug. An area under the plasma drug concentration-time curve (AUC) was then calculated theoretically using the pooled concentration and the predicted AUC value was statistically compared with the traditionally calculated AUC value. The comparison revealed that the sample pooling method generated reasonably accurate AUC values when compared with those obtained by the traditional approach. It is especially noteworthy that the accuracy was obtained by the analysis of only one sample instead of analyses of a number of samples that necessitates a significant man-power and time. Thus, we propose the sample pooling method as an alternative to in vivo pharmacokinetic approach in the selection potential lead(s) from combinatorial libraries.

• Journal of Ginseng Research
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• 제23권3호
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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.

• Proceedings of the Plant Resources Society of Korea Conference
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• 한국자원식물학회 2018년도 춘계학술발표회
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• pp.3-3
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• 2018

For centuries, Panax ginseng Meyer (Korean ginseng) has been widely used as a medicinal herb in Korea, China, and Japan. Ginsenosides are a class of triterpene saponins and recognized as the bioactive components in Korean ginseng. Ginsenosides, which can be classified broadly as protopanaxadiols (PPD), protopanaxatriols (PPT), and oleanolic acids, have been shown to flaunt a vast array of pharmacological activities such as immune-modulatory, anti-inflammatory, anti-tumor, anti-diabetic, and antioxidant effects. In recent years, a number of ginseng and ginsenoside researches have increasingly gained wide attention owing to its unique pharmacological properties. Although good efficacies of ginsenosides have been reported, lack of target specific delivery into tumor sites, low solubility, and low bioavailability due to modifications in gastro-intestinal environments limit their biomedical application in clinical trials. As a result to this major challenge, nanotechnology and drug delivery techniques play a significant role to solve this problematic issue. Thus, we reported the preparation of poly-ethylene glycol (PEG) and glycol chitosan (GC) functionalized to ginsenoside (Compound K and PPD) conjugates via hydrolysable ester bonds with improved aqueous solubility and pH-dependent drug release. In vitro cytotoxicity assays revealed that PEG-CK, and PPD-CK conjugates exhibited lower cytotoxicity compared to bare CK and PPD in HT29 cells. However, GC-CK conjugates exhibited higher and similar cytotoxicity in HT29 and HepG2 cells. Furthermore, GC-CK-treated RAW264.7 cells did not exhibit significant cell death at higher concentration of treatment which supports the biocompatibility of the polymer conjugates. They also inhibited nitric oxide production in lipopolysaccharide (LPS)-induced RAW64.7 cells. In addition to polymer-ginsenoside conjugates, silver (AgNps) and gold nanoparticles (AuNps) have been successfully synthesized by green chemistry using different m. The biosynthesized nanoparticles demonstrated antimicrobial efficacy, anticancer, anti-inflammatory, antioxidant activity, biofilm inhibition, and anticoagulant effect. Special interest on the effective delivery methods of ginsenoside to treatment sites is the focus of metal nanoparticle research.In short, nano-sizing of ginsenoside results in an increased water solubility and bioavailability. The use of nano-sized ginsenoside and P. ginseng mediated metallic nanoparticles is expected to be effective on medical platform against various diseases in the future.

• Nuclear Medicine and Molecular Imaging
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• 제41권6호
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• pp.561-565
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• 2007

Purpose: Lipophilic cations including tetraphenylphosphonium (TPP) salts penetrate the hydrophobic barriers of the plasma and mitochondrial membranes, resulting in accumulation in mitochondria in response to the negative inner transmembrane potentials. The development of radiolabeled phosphonium cations as a noninvasive imaging agent may serve as a new molecular "voltage sensor" probe to investigate the role of mitochondria in the pathophysiology and diagnosis of cancer. Materials and Methods: We have synthesized a reference compound (4-fluorophenyl)triphenylphosphonium (TPP) and a labeled compound $[^{18}F]$TPP via two step nucleophilic substitution of no-carrier-added $[^{18}F]$fluoride with the precursor, 4-iodophenyltrimethylammonium iodide, in the presence of Kryptofix-2.2.2 and $K_2CO_3$. Result: The reference compound (4-fluorophenyl)triphenylphosphonium (TPP) was synthesized in 60% yield. The radiolabeled compound $[^{18}F]$TPP was synthesized in $10\sim15%$ yield. The radiochemical purity of the $[^{18}F]$TPP was $95.57{\pm}0.51%$ (n=11). Conclusion: $[^{18}F]$TPP was successfully synthesized that might have a potential to be utilized as a novel myocardial or cancer imaging agent for PET. However, it is required to improve the radiochemical yield to apply $[^{18}F]$TPP in preclinical or clinical researches.

• Journal of Veterinary Clinics
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• 제32권6호
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• pp.519-522
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• 2015

A 6-year-old castrated male Shih-Tzu was admitted to the Gyeongsang Animal Medical Center with hematuria and vomiting. Serum chemistry indicated increases in blood urea nitrogen and creatinine values. Radiography showed radiopaque materials attached to the ventralis of the inner bladder wall. Penile urethra also was filled with radiopaque materials. Ultrasonography revealed bilateral perineal effusion in the kidney, thinned bladder wall, and materials with acoustic shadowing at the caudal extremity of the os penis. Because urination was not identified by urinary obstruction, cystocentesis was performed. Hematuria was diagnosed by urinalysis, but clear crystals were not identified. Owing to failure of securing patency to the bladder using retrohydropropulsion, cystotomy and urethrotomy with retrohydropropulsion were performed. In this report, we describe the clinical and radiographic findings of urethral plugs in a male Shih-Tzu dog, wherein the urethral plugs were treated successfully with hydropropulsion, cystotomy, and urethrotomy. It provides an option for the treatment of urethral plugs in a dog.

• Journal of the Korean Applied Science and Technology
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• 제38권3호
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• pp.651-661
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• 2021

Eruca sativa, called arugula, is a perennial plant in the Brassicaceae family, an edible plant commonly used in Italian cuisine. To study as a cosmetic material application E. sativa was extracted with 70% ethanol (ES). Then ES was fractionated using n-hexane, chloroform, ethyl acetate, n-butyl alcohol and water (EHex, EEA, ECHCl₃, EBuOH and EDW). EEA showed mushroom tyrosinase inhibitory activity. ES, EEA and EBuOH showed inhibition of tyrosinase activity. As a result, ES is expected to have skin whitening efficacy. ES was applied to 0.05, 0.1% the toner and emulsion formulation to test the stability. The anti-microbial activity of eight bacteria and fungi including Staphylococcus aureus and Propionibacterium acnes which cause dermatitis and acne was evaluated. EEA showed effects in all of microorganisms. The toner and emulsion containing ES with 0.05, 0.1% were passed in the challenge test. At -20, 4, 25, 55 ℃ and daylight, there was no significant change on pH, viscosity for 4 months. However, emulsions had phase separation phenomenon at 55 ℃, so the base formulation needs improvement. In addition, through the skin penetration test, EEA penetrated 0.058% in 6 hr, predicting the clinical efficacy. This means that E. sativa can contribute whitening agent and the synergistic effect of preservatives.

• Journal of Applied Biological Chemistry
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• 제53권2호
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• pp.65-70
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• 2010

Medium-chain fatty acids (MCFA) are composed of 8-12 carbon atoms, and are found in coconut, cuphea, and palm kernel oil. MCFA were introduced into clinical nutrition in the 1950s for dietary treatment of malabsorption syndromes because of their rapid absorption and solubility. Recently, MCFA have been applied to Gastrointestinal Permeation Enhancement Technology (GIPET), which is one of the most important parts in drug delivery system in therapeutics. Therefore, to accumulate the MCFA in seed oil of rapeseed, much effort has been conducted by classical or molecular breeding. Laurate can be successfully accumulated up to 60 mol% in the seed oil of rapeseed by the expression of bay thioesterase (Uc FatB1) alone or crossed with a line over-expressing the coconut lysophosphatidic acid acyltransferase (LPAAT) under the control of a napin seed-storage protein promoter. Also, caprylate and caprate were obtained 7 mol% and 29 mol%, respectively, from plants over-expressing of the medium-chain specific thioesterase (Ch FatB2) alone or together with the chain-length-specific condensing enzyme (Ch KASIV). Despite the success of some research in utilizing parallel classical and molecular breeding to produce MCFA, commercially available seed oils have for the most part, not been realized. Recent research in the field of developing MCFA-enriched transgenic plants has established that there is no single rate-limiting step in the production of the target fatty acids. The purpose of this article is to review some of the recent progress in understanding the mechanism and regulation of MCFA production in seed oil of rapeseed.

• Journal of the Society of Cosmetic Scientists of Korea
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• 제34권4호
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• pp.275-286
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• 2008

In this study, we investigated the anti-oxidative, anti-wrinkle and whitening effects of Platycarya strobilacea bark extracts. The free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activity ($FSC_{50}$) of extract / fractions of Platycarya strobilacea was in the order: 50% ethanol extract ($6.75{\mu}g/mL$) < deglycosylated aglycone fraction ($6.62{\mu}g/mL$) < ethyl acetate fraction ($4.15{\mu}g/mL$). Reactive oxygen species (ROS) scavenging activities ($OSC_{50}$) of some Platycarya strobilacea extracts on ROS generated in $Fe^{3+}$-EDTA/$H_2O_2$ system were investigated using the luminol-dependent chemiluminescence assay. The order of ROS scavenging activity was ethyl acetate fraction (OSC50, $0.56{\mu}g/mL$) < 50% ethanol extract ($0.02{\mu}g/mL$) < deglycosylated aglycone fraction ($0.01{\mu}g/mL$). The deglycosylated aglycone fraction showed the most prominent scavenging activity. The protective effects of extract / fractions of Platycarya strobilacea on the rose-bengal sensitized photohemolysis of human erythrocytes were investigated. The ethanol extract (50%) suppressed photohemolysis in a concentration dependent manner, particularly ethyl acetate fraction exhibited the most prominent cellular protective effect (${\tau}_{50}$, 717.27 min at $10{\mu}g/mL$). The inhibitory effect of Platycarya strobilacea extracts on tyrosinase were investigated to assess their whitening efficacy. Finally, their anti-elastase activities were measured to predict the anti-wrinkle efficacy in the human skin. The inhibitory effect ($IC_{50}$) on tyrosinase of some Platycarya strobilacea extracts was 50% ethanol extract ($243.98{\mu}g/mL$) < ethyl acetate fraction ($153.87{\mu}g/mL$) < deglycosylated aglycone fraction ($137.53{\mu}g/mL$). Also, The inhibitory effect of elastase ($IC_{50}$) of some Platycarya strobilacea extracts was 50% ethanol extract ($31.01{\mu}g/mL$) < ethyl acetate fraction ($14.42{\mu}g/mL$) < deglycosylated aglycone fraction ($1.48{\mu}g/mL$). The cream containing the ethyl acetate fraction of Platycarya strobilacea extracts was formulated. The skin hydration, transepidermal water loss, and the whitening effects were investigated after topical application of the cream. The skin hydration of cream containing extract was increased by $2{\sim}8%$ than the placebo cream, transepidermal water loss was decreased. The cream containing extract suppressed the melanogenesis of skin by 9.55% than the placebo cream. These results indicate that extract / fractions of Platycarya strobilacea can function as antioxidants in biological systems, particularly skin exposed to UV radiation by anti-oxidative activity and protect cellular membranes against ROS. The inhibitory effect on elastase and tyrosinase, and the increase of skin hydration and the whitening effect of the cream containing extract could be applicable to new functional cosmetics for antiaging.

• Journal of Veterinary Clinics
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• 제20권2호
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• pp.237-241
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• 2003

A case of juvenile onset generalized demodicosis of one year old, intact female Japanese Chin dog weighing 3.1kg was presented to the Small Animal Clinic of the College of Veterinary Medicine of Kyungpook National University. The diagnosis was made based on the physical examination, deep skin scrapings, hematology, serum chemistry, endocrinologic evaluation and bacterial culture. Numerous D. canis mites of various stages were observed in multiple skin scraping samples. CBC, serum chemistry, $T_3$, $T_4$ and free $T_4$ values were within normal range and Staphylococcus intermedius was isolated in bacterial culture of pustules. The dog was healthy other than skin lesions at the presentation. The three different treatment protocols were tried for the case. No clinical improvement was observed during 13 weeks of orally given daily basis ivermectin therapy at 600ug/kg and 2 weeks of spot-on weekly basis selamectin therapy at 30 mg/kg with cephalexin given orally twice a day at 25 mg/kg. However, a remarkable remission was seen by 0.1% amitraz dip on weekly basis with 4% chlorhexidine bath given twice a week. The secondary staphylococcal infection and accompanied pruritus was almost disappeared in two weeks and she was recovered clinically normal in 9 weeks of therapy. The therapy was continued for 4 more weeks to prevent relapse. The dog is clinically normal and being monitored for development of any abnormal dermatological signs for the time being.