• Applied Biological Chemistry
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• v.38 no.5
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• pp.478-483
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• 1995

To investigate the constituents of antimutagenic factor from brown rice, methanol extracts were fractionated into ether, ethylacetate, buthanol and aqueous fractions. The ether fractions showed distinct antimutagenic effect and active spot were selected by silica gel chromatography. The specific activity of active spot decreased with isolation of the active components from the methanol extract. Qualitative analyses of the active spot by using various spraying reagents revealed that ninhydrin and orcinol did not develop colored reactions. But, ferric chloride, 2,7-dichlorofluorescein, antimony pentachloride, phosphomolybdic acid, bromothymol blue and rhodamine 6G led to colored reactions. These results suggested that the consitituents of active material were neither polar nor nitrogen-containing compounds and that they may contain phenolic compounds and fatty acid derivatives. Main compounds of the active spot were analyzed to be o-hydroxy benzyl alcohol(saligenin), octanoic acid(caprylic acid), 9,12-cis-octadecadienoic acid(linoleic acid), 11-cis-octadecenoic acid(oleic acid), hexadecanoic acid(palmitic acid), 1H-indole-2-carboxylic acid and 1,2-benzenedicarboxylic acid(phthalate) in GC/Mass spectrum, and antimutagenicity of these active compounds using standard regeant was reconfirmed in S. typhimurium reversion assay.

• YAKHAK HOEJI
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• v.42 no.4
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• pp.437-446
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• 1998

The distribution, metabolism and excretion of CKD-602{20(S)-7-[2-(N-Isopropylamino)ethyl]camptothecin HCI), a new camptothecin derivative, were investigated in rats after a sing le administration of CKD-602. 1. The tissue levels of CKD-602 given to mice by the intravenous route at a dose of 20mg/kg were the highest in intestine, followed in descending order by kidney, liver, stomach,lung, heart, spleen and plasma. The concentrations of CKD-602 after 24hrs decreased to less than 2% of the peak level in most tissues except the skin. The urinary and fecal excretion of CKD-602 were 47.6% and 44.4% of the administered dose, respectively, with 0.7% remaining in the rinse. 2. After administration of CKD-602 at 10mg/kg in rats, metabolism of this compound was examined in plasma, urine, and feces. The plasma samples were collected for 24hr, urinary and fecal samples for 72hr. While any peak of CKD-602 in HPLC chromatograms was not detected from plasma and urine it was detected in feces (peaks, 9.8 min). However, additional peak area was about 0.5% of the peak area of parent CKD-602. Therefore, CKD-602 may be eliminated with the parent form and rarely metabolized in the body. 4. After I.v. administration of CKD-602 at 10mg/kg in rats, urinary and fecal excretions were examined for 72hrs post dose period. 87% of total urinary excretion of CKD-602 was excreted within 8hr after administration, 53%, and 32% of total fecal excreted amounts were determined in 0-24 hr and 24-48hr periods, respectively. The total excretion amounts of CKD-602 into urine and feces were 94% of the administered dose.

• Korean Journal of Food Science and Technology
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• v.30 no.6
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• pp.1273-1278
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• 1998

Conditions for enzyme-protein binding assay (EPBA) were established in order to detect biotin more rapidly and reproducibly than traditional microbiological assay (MBA). EPBA with streptavidin and biotin-KLH conjugate showed cross-reactivities on biocytin, a derivative with biotin activity, at the rate of 109% $(IC_{50}=0.3\;ppb)\;and\;197%\;(IC_{50}=0.8\;ppb)$, respectively, but not on other derivatives with no biotin activities, such as desthiobiotin, diaminobiotin and 2-iminobiotin. Detection ranges of biotin by EPBA with streptavidin and biotin-KLH conjugates were $0.01{\sim}30\;ng/mL\;and\;0.01{\sim}1.0\;ng/mL(ppb)$, respectively. In the spike test with milk, fruit flake and pine-carrot juice, the correlation coefficience between MBA and EPBA with biotin-KLH conjugates was r=0.994. But MBA showed cross-reactivities both on biocytin and desthiobiotin at the rate of 80.1% and 66.7%, respectively. Detection range of biotin by MBA was $0.1{\sim}0.5\;ng/mL(ppb)$. These results strongly suggest that EPBA is efficient for biotin detection in sensitivity, detection range, cross-reactivity and time consuming.

• The Korean Journal of Physiology and Pharmacology
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• v.2 no.3
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• pp.323-330
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• 1998

Tetrahydroisoquinoline (THI) alkaloids can be considered as cyclized derivatives of simple phenylethylamines. Many of them, especially with 6,7-disubstitution, demonstrate a relatively high affinity for catecholamines. Present study examines the pharmacological action of limited series of THI, using rats' isolated atria and aorta. In addition, a $[^3H]$ prazosin displacement binding study with THI compounds was performed, using rat brain homogenates to investigate whether these probes have ?${\alpha}$-adrenoceptor affinity. We also compared the vascular relaxation potency of these probes with dobutamine. YS 49, YS 51, higenamine and dobutamine, concentration-dependently, relaxed endothelium-denuded rat thoracic aorta precontracted with phenylephrine (PE, 0.1 ${\mu}M$) in which $pEC_{50}$ were $5.56{\pm}0.32$ and $5.55{\pm}0.21$, $5.99{\pm}1.16$ and $5.57{\pm}0.34$, respectively. These probes except higenamine also relaxed KCl (65.4 mM)-contracted aorta. In isolated rat atria, all THIs and dobutamine increased heart rate and contractile force. In the presence of propranolol, the concentration response curves of YS 49 and YS 51 shifted to the right and resulted in $pA_2$ values of $8.07{\pm}0.84$ and $7.93{\pm}0.11$, respectively. The slope of each compound was not deviated from unity, indicating that these chemicals are highly competitive at the cardiac ?${\beta}-adrenoceptors$. YS 49, YS 51, and higenamine showed ?${\alpha)-adrenoceptor$ affinity in rat brain, in which the dissociation constant $(K_i)$ was 2.75, 2.81, and 1.02 ${\mu}M$, respectively. It is concluded, therefore, that THI alkaloids have weak affinity to ${\alpha)_1-adrenoceptor$ in rat aorta and brain, respectively, while these probes show relatively high affinity for cardiac ${\beta}-adrenoceptors$. Thus, these chemicals may be useful in the treatment of congestive heart failure.

• Journal of Life Science
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• v.19 no.2
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• pp.277-283
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• 2009

Biogenic amines are generally formed through the decarboxylation of specific free amino acids by exogenous decarboxylases released by microbial species associated with the fish products and fermented feeds. This study was conducted to investigate the properties of e tuna waste regarding the control of degradation of biogenic amines (histamine, tyramine, tryptamine, putrescine, and cadaverine) that might be related with the anti-nutritional factor of the tuna waste that is used for manufacturing domestic fish meal. The values of pH and the salt content were 6.51, 3.35% in tuna waste and 5.58 and 5.83% in tuna fish meal, respectively. The strains and dominant bacteria tested in the tuna waste sample were 9.20, 9.29, 5.67, 7.82 and 7.58 log CFU/g of total bacteria, aerobic plate count (APC), total coliform (TC), Lactobacillus spp. and Bacillus spp., respectively. The main histamine forming-bacteria (HFB) in tuna waste were detected by silica gel thin-layer chromatography (TLC) and 7 histamine-forming bacterial species were isolated among microbes grown in selective medium. The histamine concentration was determined by detection of fluorescence of ο-phthaldialdehyde (OPA) derivatives using HPLC and the date were used to reconfirm the identities of the amine-producing bacteria. The 15 histamine- forming bacteria strains grown in trypicase soy broth (TSB) supplemented with 1% L-histidine (TSBH) were identified as Lactococcus(L.) lactis subsp. lactis, Klebsiella pneummonlae, L. garvieae 36, Vibrio olivaceus, Hafnia alvei and L. garvieae which were main dominant amine - producing strains, and Morganella morganii identified by 16S ribosomal RNA (rRNA) sequencing with PCR amplification. A Phylogenetic tree generated from the 16S rRNA sequencing data showed different phyletic lines that could be readily classified as biogenic amine forming gram-positive and negative bacteria.

• Journal of Food Hygiene and Safety
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• v.25 no.2
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• pp.170-179
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• 2010

This study was conducted to investigate for mineral contents, total polyphenol compounds, betaine, choline and DPPH free radical scavenging activity of halophyte. The mineral concentrations of Salicornia herbacea (top part) were Na 100,006 mg/kg, K 1,385 mg/kg, Mg 6,263 mg/kg, Ca 2,750 mg/kg, Fe 90.4 mg/kg, Mn 98.9 mg/kg, Zn 33.3 mg/kg, Cu 3.4 mg/kg respectively. And Suaeda Japonica (top part) were Na 85,332 mg/kg, K 710 mg/kg, Mg 7,005 mg/kg, Ca 4,344 mg/kg, Fe 1,434.9 mg/kg, Mn 119.1 mg/kg, Zn 19.2 mg/kg, Cu 2.7 mg/kg respectively. The betaine contents of Salicornia herbacea (top part) were 15.09 mg/g and Suaeda Japonica (top part) were 14.64 mg/g. The choline contents estimated by the DBAP-choline derivatives of Salicornia herbacea (top part) were 20.9 mg/100 g, Salicornia herbacea (root) were 23.4 mg/100 g, Suaeda Japonica (top part) were 23.1 mg/100g and Suaeda Japonica (root) were 23.8 mg/100 g. Total polyphenol compounds of Salicornia herbacea (top part) were high 36.0 mg/g in growth phase. The DPPH radical scavenging activities of methanol extract Salicornia herbacea (top part) were high 90.1% in growth phase. The frozen dried powder of Salicornia herbacea (top part) 1 g was equal to Quercetin 30.26 mg, Rutin 42.65 mg, TBHQ 20.32 mg, BHA 25.86 mg, BHT 40.75 mg, Ascorbic acid 22.86 mg in DPPH radical scavenging activities.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.44 no.3
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• pp.239-247
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• 2018

Chronic inflammation is known to have effects on various diseases such as gout, cancer, dementia, atopic disease, and obesity. In addition, since some signal cascades involved in the development of inflammation are known to affect the damage and aging of the skin tissue, studies are being conducted actively to control the inflammation mechanism. In order to mitigate or prevent inflammatory response, a number of researches have been made to develop anti-inflammatory materials from some plants. In particular, Stevia rebaudiana produces steviol glycosides (SG), a natural sweetener with a distinctive flavor. Studies on some of SG have been shown to have anti-inflammatory activity. Researchers of this study expected that more SG also possess anti-inflammatory activity, besides stevioside, rebaudioside A, and steviol. In order to confirm this possibility, the researchers screened inhibition activity of various steviol glucosides for NO production in RAW 264.7 cell lines. As a result, steviol ${\beta}-glucopyranosyl$ ester (SGE) showed the highest inhibitory activity among steviol derivatives treated at the same molar concentration. In addition, we found that mRNA expression level of $interleukin-1{\alpha}$ ($IL-1{\alpha}$), $interleukin-1{\beta}$ ($IL-1{\beta}$), cyclooxygenase-2 (COX-2), nuclear factor kappa-light chain-enhancer of activated B cells ($NF-{\kappa}B$) and inducible nitric oxide synthase (iNOS) was also decreased in a dose-dependent manner. These results show that SGE inhibits anti-inflammatory activity and NO production in mouse macrophage RAW 264.7 cells. It was confirmed that SGE has potential to be applied as an anti-inflammatory material.

• The Korean Journal of Food And Nutrition
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• v.25 no.3
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• pp.564-569
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• 2012

Selenium was initially considered toxic to humans, but it was then discovered that selenium is essential for normal life processes. Selenium plays important roles in antioxidants. It is expected that chitosan microcapsules containing nano-selenium will be able to be used as a key material in bio-medical and cosmetic applications. The high concentration of chitosan derivatives guarantees increased antioxidative activity. Both inorganic and organic forms of selenium can be nutritional sources. The antioxidant properties of selenoproteins help prevent cellular damage from free radicals. The objective of this experiment was to study the antioxidative activity of chitosan nano-selenium. Our experiments were divided into five groups, in the presence of various concentrations(0.1%, 0.3%, 0.5%, 0.7%, and 0.9%) of chitosan. We performed an assessment of the antioxidant properties and cytotoxicity of respective concentrations of chitosan nano-selenium. The antioxidant activity was examined by the free radical scavenging activity on 1,1-diphenyl-2-picrylhydrazyl(DPPH) assay. The cytotoxicity effect was measured by means of 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay. As a result, the electron donating abilities of 0.1%, 0.3%, 0.5%, 0.7%, and 0.9% of chitosan nano-selenium exhibited effective andioxidant scavenging activity at 12.5 ${\mu}g/m{\ell}$ against DPPH radicals. 0.3% chitosan nano-selenium did not show cytotoxicity on human keratinocytes. In general, the cytotoxicity of 0.1% and 0.9% chitosan nano-selenium showed the lowest effects. Though low cytotoxicity of 0.5% and 0.7% chitosan nano-selenium exhibited 29.67% and 38.4% against human keratinocytes on adding 100 ${\mu}g/m{\ell}$ and 50 ${\mu}g/m{\ell}$, respectively, cell vitality was recovered with 200 ${\mu}g/m{\ell}$. These findings support the notion that chitosan nano-selenium may be useful as a new active ingredient source for bioactive compounds.

• Development and Reproduction
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• v.11 no.3
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• pp.187-193
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• 2007

Ethane 1,2-dimethane sulfonate(EDS), a Leydig cell specific toxicant, has been widely used to create the reversible testosterone withdrawal rat model. Though the maintenance of epididymal structure and function is highly dependent on the testosterone secreted from testis, its derivatives, dihydroxytestosterone(DHT) and estrogen, might have crucial roles. The aim of present study was to monitor the expression patterns of sex steroid receptors, cytochrome P450 aromatase(P450arom) and $5{\alpha}$-reductase in the rat epididymis up to 7 weeks after EDS injection. Adult male rats($350{\sim}400g$) were injected with a single does of EDS(75 mg/kg i.p.) and sacrificed on weeks 0, 1, 2, 3, 4, 5, 6 and 7. The transcriptional activities of the target genes were evaluated by semi-quantitative RT-PCRs. The transcript level of estrogen receptor alpha($ER{\alpha}$) in EDS group was significantly higher than control level on week 1(P<0.01). After week 2, there was no significant difference in $ER{\alpha}$ levels between EDS group and control. The transcript level of estrogen receptor beta($ER{\beta}$) in EDS group was significantly higher than control level on week 1(P<0.05), lowered on weeks 2 and 3(P<0.05 and P<0.01, respectively), fluctuated during weeks 4 and 6, and elevated on week 7(P<0.05). The androgen receptor (AR) message levels increased significantly week 2(P<0.01), then returned to control level on week 3. In contrast, expression of cytochrome P450 aromatase(P450arom) decreased sharply during weeks $1{\sim}3$(P<0.01 on weeks 1 and 2; P<0.05 on week 3), then went back to control level on week 4. The mRNA level of $5{\alpha}$-reductase type 2($5{\alpha}$-RT2) increased significantly on week 4(P<0.01), then returned to control level. The present study indicated that EDS administration could induce reversible alterations in the transcriptional activities of sex steroid hormone receptors and androgenconverting enzymes in rat epididymis. EDS injection model will be useful to clarify the regulation mechanism of mammalian epididymal physiology.

• Korean Chemical Engineering Research
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• v.49 no.3
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• pp.330-337
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• 2011

In this research, the preparation processes for making a series of $\omega$-mercapto alkylamine 1 and $\omega$-mercapto alkanoic acid 2 useful for studying of the self-assembled monolayer(SAM) are described. The preparation methods of the first goal materials, $\omega$-mercapto alkylamines 1 were carried out as follows: First, $\omega$-phthalimide alkanol 3 was synthesized from commercially available potassium phthalimide derivatives and $\omega$-bromoalkanol in DMF at $80{^{\circ}C}$ via substitution reaction. After refluxing $\omega$-phthalimide alkanol 3 with hydrazine hydrate in ethanol followed by treating with c-HCl, $\omega$-aminoalkanol 4 was obtained in 76-98% yield, accompanied with side-product 5. Bromination of hydroxyl moiety of $\omega$-aminoalkanol 4 using aqueous hydrobromic acid furnished $\omega$-bromoamine 6 in 34-97% yields. Substitution reaction 6 with thiourea in 95% ethanol gave $\omega$-aminoalkanthiuronium 7, which was treated with aqueous strong base and aqueous strong sulfuric acid gave desired products, $\omega$-mercapto alkylamines 1 through overall 5 steps. The second target material, $\omega$-mercapto alkanoic acid 2 was prepared via 2 steps. $\omega$-bromo alkanoic acid was reacted with thiourea to give $\omega$-thiourea alkanoic acid 7 in 69-85%, which was treated with aqueous strong base and strong acid to furnish $\omega$-mercapto alkanoic acid 2 in 50-98%. The fabricated long-chain alkylthiol(LCAT) can be used as linkers to immobilize protein, enzyme and various kinds of biomolecules on the surface of metallic materials(Au, Pt, Ti) by SAM, and can be useful chemical tools for the application study on the surface modification of metallic materials.