• Natural Product Sciences
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• v.19 no.3
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• pp.201-205
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• 2013

Thirteen phenolic compounds, 1,4-dimethoxybenzene (1), 3,4-dihydroxybenzaldehyde (2), (2E)-3-(4-hydroxy-3,5-dimethoxyphenyl)acrylaldehyde (3), 3,7-dihydroxy-4H-chromen-4-one (4), 2,3-dihydroxy-1-(3,4-dihydroxyphenyl)propan-1-one (5), 4-hydroxy-3-methoxybenzoic acid (6), 4-hydroxy-3,5-dimethoxybenzoic acid (7), methyl 3,4-dihydroxybenzoate (8), 4-hydroxy-3,5-dimethoxybenzaldehyde (9), 3,4-dihydroxybenzoic acid (10), 3-hydroxy-1-(4-hydroxy-3-methoxyphenyl)propan-1-one (11), 2,4,6-trihydroxybenzaldehyde (12) and benzene-1,2,4-triol (13) were isolated from the heartwood of Caesalpinia sappan. Their anti-inflammatory activity was evaluated against LPS-induced NO production in macrophage RAW264.7 cells. Among them, compounds 3 and 8 showed strong inhibitory activities toward the LPS-induced NO production in macrophage RAW264.7 cells with $IC_{50}$ values of 14.5 and 21.5 ${\mu}M$, respectively.

• Korean Journal of Veterinary Research
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• v.47 no.1
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• pp.67-75
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• 2007

Environmental mastitis has increased particularly in well-managed or low somatic cell countherds that have successfully controled contagious pathogens. Major pathogens of environmental mastitisare Escherichia coli (E. coli) and Streptococcus uberis. The present study was conducted to investigate1,865 quaters of 241 Korean dairy farms from 2001 to 2004. Prevalence of major gram-negative bacteriaisolated from mastitis milk were E. coli (22.7%) and Enterobacter spp. (16.3%) in coliforms and Pseudomoassp. (10.3%) and Serratia spp. (7.9%) in non-coliforms. The results on antibiotic susceptibility by agardifusion test against these pathogens were 86.7% in piperaciliin, 94.6% in cefepime, 85.5% in amikacin,87.7% in gentamicin and so on. In contrast, the susceptibility against ampicillin (41.9%), cephalothin (9.9%),streptomycin (39.9%) and tetracycline (46.7%) appeared to be below 50%. Gram-negative bacteria showed(96.8%). Acording to year, distribution of high $256{\sim}64{\mu}g/ml$ on cephalothin get increased, but the othersare diferent. These findings demonstrate that major gram-negative bacteria were E. coli and Enterobacterspp. isolates, and often encountered the diverse antibiotic resistant patterns.

• Journal of Nutrition and Health
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• v.52 no.4
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• pp.323-331
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• 2019

Purpose: Glucocorticoids (GCs) are implicated in secondary osteoporosis, and the resulting fractures cause significant morbidity. Polyunsaturated fatty acids (PUFAs) play a vital role in bone metabolism. However, few trials have studied the impact of omega-3 PUFA-containing oils against GC-induced osteoporosis. Therefore, the present study was undertaken to determine whether supplementation with omega-3 PUFA-containing dietary oils such as fish oil, flaxseed oil or soybean oil can impede the development of GC-induced osteoporosis. Methods: The fatty acids (FAs) content of oils was determined using gas chromatography. Male rats were subdivided into 5 groups (8 rats each): normal control (balanced diet), prednisolone control (10 mg/kg prednisolone daily), soybean oil (prednisolone 10 mg/kg + soybean oil 7% w/w), flaxseed oil (prednisolone 10 mg/kg + flaxseed oil 7% w/w), and fish oil (from cod liver; prednisolone 10 mg/kg + fish oil 7% w/w). Results: The study data exhibited a significant depletion in bone mineral density (BMD) and femur mass in the prednisolone control compared to the normal control, accompanied with a marked decrease in the levels of plasma calcium and 1,25-$(OH)_2$-vitamin $D_3$, and elevated levels of C-terminal telopeptide (CTX), tumor necrosis factor-alpha (TNF-${\alpha}$) and malondialdehyde (MDA). Supplementation with fish oil, soybean oil or flaxseed oil helped to improve plasma calcium levels, and suppress oxidative stress and inflammatory markers. Additionally, bone resorption was suppressed as reflected by the decreased CTX levels. However, fish oil was more effective than the other two oils with a significant improvement in BMD and normal histological results compared to the normal control. Conclusion: This study demonstrated that supplementation with dietary oils containing omega-3 PUFAs such as fish oil, soybean oil or flaxseed oil can play a role in the prevention of bone loss and in the regulation of bone metabolism, especially fish oil which demonstrated a greater level of protection against GC-induced osteoporosis.

• Food Science and Preservation
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• v.11 no.2
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• pp.221-226
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• 2004

This study was carried out to determine the antimutagenic and anticancer effects of Allium victoriolis using Ames test and cytotoxicity. Allium victorialis extracted with ethanol and then further fractionated to chloroform, ethyl acetate and water. The inhibition rate of ethanol extract (200 $\mu\textrm{g}$/plate) of Allium victorialis in the Salmonella typhimurium TA100 strain showed 88.2% against the mutagenesis induced by N-methyl-N'-nitro-N-nitrosoguanidine(MNNG). The suppression ratio against 4-nitroquinoline-1-oxide(4NQO) in the Salmonella typhimurium TA98 and TA100 strains showed 76.4% and 83.0%, respectively. The cytotoxicity effects of Allium victorialis extract against the cell lines with human lung carcinoma (A549), human breast adenocarcinoma (MCF-7) and human gastric cacinoma (KATOIII) were inhibited with the increase of extract concentration. The treatment of 0.5 $\mu\textrm{g}$/plate Allium victorialis of ethanol extract showed strong cytotoxicities of 74.2%, 71.3% and 67.4% against A549, MCF-7 and KATOIII, respectively.

• Journal of the korean academy of Pediatric Dentistry
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• v.36 no.2
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• pp.217-226
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• 2009

Allyl isothiocyanate (AIT), the principle ingredient of antimicrobial ingredients from horseradish root, can be prepared from extracts of horseradish root or synthetic method. It is reported that the horseradish root extract has the antimicrobial effect against various oral microorganisms, while there is no further study about the antimicrobial effect against the oral microorganisms of synthetic AIT derived from synthetic method. The aim of the study is to compare the difference of the antimicrobial effect between horseradish root extracts and synthetic AIT. To evaluate the antimicrobial effect, we measured the minimum inhibitory concentration(MIC) and minimum bactericidal concentration (MBC), and the results are like following. 1. The MIC of horseradish root extract against 7 kinds of oral pathogenic microorganisms is about 117$\sim$1,750 ppm(0.0117$\sim$0.175%), and the MIC of the synthetic AIT is about 344$\sim$3,000 ppm(0.0344$\sim$0.3%), which have the antimicrobial effects against all kinds of microorganisms. 2. The MBC of the horseradish root extracts against the 7 kinds of oral microorganisms is about 625.2$\sim$6,000 ppm(0.06252$\sim$0.6%), and the MBC of the synthetic AIT is about 1,750$\sim$7,000 ppm(0.175$\sim$0.7%), which have the antimicrobial effects against all kinds of microorganisms.

• Journal of Ginseng Research
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• v.34 no.3
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• pp.246-253
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• 2010

Ginsenoside $Rg_3$ ($Rg_3$), one of the active ingredients in Panax ginseng, attenuates NMDA receptor-mediated currents in vitro and antagonizes NMDA receptors through a glycine modulatory site in rat cultured hippocampal neurons. In the present study, we examined the neuroprotective effects of $Rg_3$ on 24-hydroxycholesterol (24-OH-chol)-induced cytotoxicity in vitro. The results showed that $Rg_3$ treatment significantly and dose-dependently inhibited 24-OH-chol-induced cell death in rat cultured cortical neurons, with an $IC_{50}$ value of $28.7{\pm}7.5\;{\mu}m$. Furthermore, the $Rg_3$ treatment not only significantly reduced DNA damage, but also dose-dependently attenuated 24-OH-chol-induced caspase-3 activity. To study the mechanisms underlying the in vitro neuroprotective effects of $Rg_3$ against 25-OH-chol-induced cytotoxicity, we also examined the effect of $Rg_3$ on intracellular $Ca^{2+}$ elevations in cultured neurons and found that $Rg_3$ treatment dose-dependently inhibited increases in intracellular $Ca^{2+}$, with an $IC_{50}$ value of $40.37{\pm}12.88\;{\mu}m$. Additionally, $Rg_3$ treatment dose-dependently inhibited apoptosis with an $IC_{50}$ of $47.3{\pm}14.2\;{\mu}m$. Finally, after confirming the protective effect of $Rg_3$ using a terminal deoxynucleotidyl transferase-mediated dUTP nick end-labeling assay, we found that $Rg_3$ is an active component in ginseng-mediated neuroprotection. These results collectively indicate that $Rg_3$-induced neuroprotection against 24-OH-chol in rat cortical neurons might be achieved via inhibition of a 24-OH-chol-mediated $Ca^{2+}$ channel. This is the first report to employ cortical neurons to study the neuroprotective effects of $Rg_3$ against 24-OH-chol. In conclusion, $Rg_3$ was effective for protecting cells against 24-OH-chol-induced cytotoxicity in rat cortical neurons. This protective ability makes $Rg_3$ a promising agent in pathologies implicating neurodegeneration such as apoptosis or neuronal cell death.

• The Korean Journal of Pesticide Science
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• v.4 no.2
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• pp.69-71
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• 2000

The herbicidal activities ($pI_{50}$) with alkoxy (RO-) groups on the azomethine nitrogen atom in 5-(2,3-dihydro-2,2-dimethylbenzothiophene-7-yl)-2-(1-(alkoxyimino)butyl)-3-hydroxy-2-cyclohexene-1-one derivatives against various weeds were measured in the flooded and in the paddy conditions. Particularly, i-propoxy subsutuent, 5 of them showed excellent herbicidal activity at a rate of 4kg/ha with pre-emergence against barnyard grass (Echinochloa crus-galli) with good selectivity on rice plant (Oryza sativa). The results of the structure-activity relationships (SAR) analyses are shown that the alkyl subsituents with higher hydrophobicity (logp>0) and electron donating (${\sigma}^*<0$) group as a new substrate rather than alkoxy substituents seems to be contribute to the herbicidal activity with pre-emergence.

• The Korean Journal of Pesticide Science
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• v.8 no.3
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• pp.168-174
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• 2004

In a course of the process for a lead optimization of 2-imino-l,3-thiazolines 1 which show a selective in vivo antifungal activity against rice blast, new compounds 2 in which C-5 was substituted by methyl group of the lead compound were synthesized and tested for the biological activity. Bromination of $\beta$-keto ester 7 followed by the reaction with thiourea and hydrolysis gave 2-imino-5-methyl-l,3-thiazoline carboxylic acid 3. Coupling reactions of 3 with aniline derivatives afforded 17 kinds of the corresponding 2-imino-5-methyl-l,3-thiazoline carboxanilides 2. Their in vivo antifungal activity against rice blast was weaker than that of 1, indicating that the in vivo antifungal activity of 2-imino-l,3-thiazolines was affected by the substituent at C-5. These results would be an important data for the molecular design in the lead optimization process of this series.

• BMB Reports
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• v.46 no.7
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• pp.370-375
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• 2013

Ischemia is characterized by oxidative stress and changes in the antioxidant defense system. Our recent in vitro study showed that 2-cyclopropylimino-3-methyl-1,3-thiazoline hydrochloride protects cortical astrocytes against oxidative stress. In the current study, we examined the effects of 2-cyclopropylimino-3-methyl-1,3-thiazoline hydrochloride on ischemia-induced neuronal damage in a gerbil ischemia/reperfusion models. Extensive neuronal death in the hippocampal CA1 area was observed 4 days after ischemia/reperfusion. Intraperitoneal injection of 2-cyclopropylimino-3-methyl-1,3-thiazoline hydrochloride (0.3 mg/kg body weight) significantly prevented neuronal death in the CA1 region of the hippocampus in response to transient forebrain ischemia. 2-Cyclopropylimino-3-methyl-1,3-thiazoline hydrochloride administration reduced ischemia-induced increases in reactive oxygen species levels and malondialdehyde content. It also attenuated the associated reductions in glutathione level and superoxide dismutase, catalase, and glutathione peroxidase activities. Taken together, our results suggest that 2-cyclopropylimino-3-methyl-1,3-thiazoline hydrochloride protects against ischemia-induced neuronal damage by reducing oxidative stress through its antioxidant actions.

• Natural Product Sciences
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• v.17 no.3
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• pp.245-249
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• 2011

Eight compounds, squalene (1), friedelin (2), ${\beta}$-sitosterol (3), ${\beta}$-sitosterol-3-O-glucoside (4), ${\alpha}$-tocopherol (5), betulinic acid (6), trilinolein (7) and 1-O-(9Z,12Z-Octadecadienoyl)-3-nonadecanoyl glycerol (8), were isolated from the barks of Tilia amurensis. Their chemical structures were identified by comparing their physicochemical and spectral data with those published in the literature. These isolated compounds were examined for their inhibitory activities against topoisomerase I and II. Compound 7 showed significant inhibition of DNA topoisomerase I and II activities, with percent decreases in activity of 87 and 95%, respectively at a concentration of $100\;{\mu}M$. Compound 6 exhibited cytotoxicity against the human colon adenocarcinoma cell line (HT-29), the human breast adenocarcinoma cell line (MCF-7) and the human liver hepatoblastoma cell line (HepG-2), with $IC_{50}$ values of 20, 59 and $16\;{\mu}M$, respectively.