• The Korean Journal of Physiology and Pharmacology
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• v.13 no.2
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• pp.71-78
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• 2009

(S)-Carbamic acid 2-[4-(4-fluoro-benzoyl)-piperidin-1-yl]-1-phenyl-ethyl ester hydrochloride (YKP1447) is a novel "atypical" antipsychotic drug which selectively binds to serotonin (5-$HT_{2A}$, Ki=0.61 nM, 5-$HT_{2C}$, Ki=20.7 nM) and dopamine ($D_2$, Ki=45.9 nM, $D_3$, Ki=42.1 nM) receptors with over $10\sim100$-fold selectivity over the various receptors which exist in the brain. In the behavioral studies using mice, YKP1447 antagonized the apomorphine-induced cage climbing ($ED_{50}$=0.93 mg/kg) and DOI-induced head twitch ($ED_{50}$=0.18 mg/kg) behavior. In the dextroamphetamine-induced hyperactivity and conditioned avoidance response (CAR) paradigm in rats, YKP1447 inhibited the hyperactivity induced by amphetamine ($ED_{50}$=0.54 mg/kg) and the avoidance response ($ED_{50}$=0.48 mg/kg); however, unlike other antipsychotic drugs, catalepsy was observed only at much higher dose ($ED_{50}$=68.6 mg/kg). Based on the CAR and catalepsy results, the therapeutic index (TI) value for YKP1447 is over 100 (i.p.). These results indicate that YKP1447 has an atypical profile and less undesirable side effects than currently available drugs.

• Journal of Microbiology and Biotechnology
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• v.31 no.7
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• pp.1022-1027
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• 2021

Three compounds were isolated from marine-derived Streptomyces sp. CNQ-031, and their inhibitory activities against monoamine oxidases (MAOs), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-secretase (BACE-1) were evaluated. Compound 1 (5,7-dihydroxy-2-isopropyl-4H-chromen-4-one) was a potent and selective inhibitor of MAO-A, with a 50% inhibitory concentration (IC₅₀) of 2.70 µM and a selectivity index (SI) of 10.0 versus MAO-B. Compound 2 [5,7-dihydroxy-2-(1-methylpropyl)-4H-chromen-4-one] was a potent and low-selective inhibitor of MAO-B, with an IC₅₀ of 3.42 µM and an SI value of 2.02 versus MAO-A. Compound 3 (1-methoxyphenazine) did not inhibit MAO-A or MAO-B. All three compounds showed little inhibitory activity against AChE, BChE, and BACE-1. The K_i value of compound 1 for MAO-A was 0.94 ± 0.28 µM, and the K_i values of compound 2 for MAO-A and MAO-B were 3.57 ± 0.60 and 1.89 ± 0.014 µM, respectively, with competitive inhibition. The 1-methylpropyl group in compound 2 increased the MAO-B inhibitory activity compared with the isopropyl group in compound 1. Inhibition of MAO-A and MAO-B by compounds 1 and 2 was recovered by dialysis experiments. These results suggest that compounds 1 and 2 are reversible, competitive inhibitors of MAOs and can be considered potential therapies for neurological disorders such as depression and Alzheimer's disease.

• Journal of Ginseng Research
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• v.43 no.1
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• pp.1-9
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• 2019

Background: Korean ginseng is an important cash crop in Asian countries. However, plant yield is reduced by pathogens. Among the Ilyonectria radicicola-species complex, I. mors-panacis is responsible for root-rot and replant failure of ginseng in Asia. The development of new methods to reveal the existence of the pathogen before cultivation is started is essential. Therefore, a quantitative real-time polymerase chain reaction method was developed to detect and quantify the pathogen in ginseng soils. Methods: In this study, a species-specific histone H3 primer set was developed for the quantification of I. mors-panacis. The primer set was used on DNA from other microbes to evaluate its sensitivity and selectivity for I. mors-panacis DNA. Sterilized soil samples artificially infected with the pathogen at different concentrations were used to evaluate the ability of the primer set to detect the pathogen population in the soil DNA. Finally, the pathogen was quantified in many natural soil samples. Results: The designed primer set was found to be sensitive and selective for I. mors-panacis DNA. In artificially infected sterilized soil samples, using quantitative real-time polymerase chain reaction the estimated amount of template was positively correlated with the pathogen concentration in soil samples ($R^2=0.95$), disease severity index ($R^2=0.99$), and colony-forming units ($R^2=0.87$). In natural soils, the pathogen was recorded in most fields producing bad yields at a range of $5.82{\pm}2.35pg/g$ to $892.34{\pm}103.70pg/g$ of soil. Conclusion: According to these results, the proposed primer set is applicable for estimating soil quality before ginseng cultivation. This will contribute to disease management and crop protection in the future.

• Parasites, Hosts and Diseases
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• v.57 no.1
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• pp.1-8
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• 2019

There is no effective treatment modality available against different forms of leishmaniasis. Therefore, the aim of this study was to improve the penetration and efficacy of selenium and glucantime coupled with niosomes and compared them with their simple forms alone on in vitro susceptibility assays. In this study, the niosomal formulations of selenium and in combination with glucantime were prepared. The size and morphology of the niosomal formulations were characterized and the effectivity of the new formulation was also evaluated using in vitro MTT assay, intra-macrophage model, and gene expression profile. From the results obtained, no cytotoxicity effect was observed for niosomal and simple forms of drugs, as alone or in combination. Niosomal formulations of the drugs significantly showed more inhibitory effects ($P{\leq}0.001$) than the simple drugs when the selectivity index was considered. The gene expression levels of Interleukin (IL-10) significantly decreased, while the level of IL-12 and metacaspase significantly increased ($P{\leq}0.001$). The results of the present study showed that selenium plus glucantime niosome possess a potent anti-leishmanial effect and enhanced their lethal activity as evidenced by the in vitro experiments.

• Journal of Applied Biological Chemistry
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• v.66
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• pp.165-170
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• 2023

Isolation of the culture broth of a marine-derived Acremonium sp. CNQ-049 guided by HPLC-UV yielded compound 1 (3-phenethyl-2-phenylquinazolin-4(3H)-one), and its inhibitory activities against monoamine oxidases (MAOs), cholinesterases (ChEs), and β-secretase 1 (BACE1) were evaluated. Compound 1 was an effective selective MAO-B inhibitor with an IC₅₀ value of 9.39 µM and a selectivity index (SI) value of 4.26 versus MAO-A. In addition, compound 1 showed a potent selective butyrylcholinesterase (BChE) inhibition with an IC₅₀ value of 7.99 µM and an SI value of 5.01 versus acetylcholinesterase (AChE). However, compound 1 showed weak inhibitions against MAO-A, AChE, and BACE1. The Ki value of compound 1 for MAO-B was 5.22±1.73 µM with competitive inhibition, and the Ki value of compound 1 for BChE was 3.00±1.81 µM with mixed-type inhibition. Inhibitions of MAO-B and BChE by compound 1 were recovered by dialysis experiments. These results suggest that compound 1 is a dual-functional reversible inhibitor of MAO-B and BChE, that can be used as a treatment agent for neurological disorders.

• Korean Journal of Ecology and Environment
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• v.37 no.1 s.106
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• pp.130-136
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• 2004

In the present study, prey preference of juvenile fishes was examined using an experimental approach. Zooplankton composition, as a prey of the fish, was evaluated by taking into account the species as well as body size of juveniles in the aquarium. The predation of juvenile fishes is known to be an important factor in changes of zooplankton communities. In some previous studies at the regulated Nakdong River, the collapse of large cladcoerans and an increase in the rotifer population by selective predation during spring and summer were observed. This study focused on the predation of juvenile fishes such as Hyporhamphus sajori, Rhinogobius brunneus, and Opsariichtys uncirostris amurensis on zooplankton community structure in mesocosm scale experiments. These fishes selected the cladoceran Moina micrura with highest individual preference value (Manly/Chesson index)among zooplankton prey in the experimental aquarium. When the size-selective prey preferences of the juvenile fish were compared, both small (body size <2 cm) and large (body size >2cm) juveniles of O. uncirostris positively selected M. micrura. In the outdoor experimental tanks, juvenile fishes consumed the cladoceran M. micrura, resulting in an high abundance of the rotifer, Polyarthra spp. The results suggest that juvenile fish predation may play an important role in regulating the zooplankton community structure by reducing the cladoceran density and increase of rotifers in the Nakdong River during spring and summer.

• Korean Journal of Fisheries and Aquatic Sciences
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• v.35 no.3
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• pp.223-230
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• 2002

Investigations were made on catch composition, sex ratio, relationships between carapace length, body weight and fecundity and spawning season of major target shrimps (Acetes chinensis, A. japonicus) in the shrimp fishing areas of south-western coastal waters, accounting for about $45\%$ of annual shrimp landings in Korea. Catches were collected monthly in the fishing areas from March 2000 to February 2001, using single pocket-walled fishing gear, Total 59 species (shrimps 14, fishes 34, other crustaceans 8 and cephalopods 3 species) occurred. During the study period the bycatch-to-shrimp ratio of shrimp fishery was 2.42 in April 2000 and less than 1 for all months except for August 2000 and Febuary 2001. Compared with shrimp fishery of other areas and nations, these results indicate that effect of the fishing gear on catches of other species is minor, suggesting higher gear selectivity for shrimps. Of shrimps, there were two dominant species (A. chinensis, A. japonirus). Average sex ratio was 1.44 $\pm$ 0.42 for A. japonicus and 1,44 $\pm$ 0.43 for A. chinensis, which are dominant females in August. Average fecundity was 4,812 $\pm$ 1,511 for A. japonicus and 5,561 $\pm$ 1,900 for A. chinensis. In the two species mature females were found in the period from May to August. Similarly, the gonadosomatic index (GSI) was higher in July and August, with a peak in July, These results indicate that their main spawning season was summer.

• Journal of the Korean Society of Food Science and Nutrition
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• v.44 no.3
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• pp.356-362
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• 2015

Prickly pear cactus cladodes were extracted with hot water and 70% ethanol, followed by fractionation with n-hexane (HF), ethyl acetate (EF), n-butanol (BF), and distilled water. Total phenolics and total flavonoid contents as well as antioxidative and anti-inflammatory activities were then measured. Total phenolic contents were 784, 452, and 220 mg gallic acid equivalents (GAE)/g, whereas total flavonoid contents were 214, 76, and 113 mg quercetin equivalents (QE)/g in EF, BF, and HF, respectively. DPPH and ABTS radical scavenging activities ($IC_{50}$) were 103 and $105{\mu}g/mL$ in EF, 359 and $379{\mu}g/mL$ in BF, and 469 and $605{\mu}g/mL$ in HF, respectively. Oxygen radical absorbance capacity was highest at $391{\mu}M$ TE in EF (in decreasing order of $117{\mu}M$ TE in BF and $64{\mu}M$ TE in HF), whereas superoxide anion radical scavenging activity ($IC_{50}$) was highest at $40{\mu}g/mL$ in EF (in decreasing order of $69{\mu}g/mL$ in BF and $98{\mu}g/mL$ in 70% ethanol extract). Inhibitory activity ($IC_{50}$) of nitric oxide (NO) production induced by LPS-activated RAW264.7 cells was highest at $62{\mu}g/mL$ in HF (in decreasing order of $104{\mu}g/mL$ in EF and $465{\mu}g/mL$ in BF). The selectivity index (ratio of inhibitory activity of NO production to cell cytotoxicity) was highest at 4.63 in EF (in decreasing order of 3.37 in HF and 2.14 in BF). In conclusion, EF showed potent antioxidant and anti-inflammatory effects with high phenolic and flavonoid contents.