• Proceedings of the Korea Society of Environmental Toocicology Conference
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• 2003.05a
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• pp.183-184
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• 2003

Sophoricoside was isolated as the inhibitor of IL-5 bioactivity from Sophora japonica (Leguminosae). It has been reported to have an anti-inflammatory effect on rat paw edema model. To develop as an anti-allergic drug, genotoxicity of sophoricoside was investigated in bacterial and mammalian cell system such as Ames bacterial test, chromosomal aberration assay, Comet assay and MOLY assay. In Ames test, sophoricoside of 5000 ∼ 313 $\mu\textrm{g}$/plate concentrations was not shown significant mutagenic effect in Salmonella typhimurium TA98, TA100, TA1535 and TA1537 strains. The cytotoxicity (IC$\_$50/ and IC$\_$20/) of sophoricoside was determined above the concentration of 5000 $\mu\textrm{g}$/ml in Chinese hamster lung (CHL) fibroblast cell and L5178Y mouse lymphoma cell line. At concentrations of 5000, 2500 and 1250 $\mu\textrm{g}$/ml, this compound was not induced chromosomal aberration in CHL fibroblast cell in the absence and presence of S-9 metabolic activation system. Also in comet assay, DNA damage was not observed in L5178Y cell line. Also in MOLY assay, sophoricoside of 5000 ∼ 313 $\mu\textrm{g}$/ml concentrations was not shown significant mutagenic effect in absence of S-9 metabolic activation system. However, the higher concentration of 5000 and 2500 $\mu\textrm{g}$/ml of sophoricoside induced the increased mutation frequency (MF) in the presence of S-9 metabolic activation system. From these results, no genotoxic effects of sophoricoside observed in bacterial systems whereas, genotoxic effects observed in mammalian cell systems in the presence of metabolic activation system. These results suggested that the metabolite(s) of sophoricoside can cause some genotoxic effects in mammalian cells.

• Environmental Mutagens and Carcinogens
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• v.21 no.2
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• pp.99-105
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• 2001

Sophoricoside was isolated as the inhibitor of IL-5 bioactivity from Sophora japonica (Leguminosae). It has been reported to has an anti-inflammatory effect on rat paw edema model. To develope as an anti-allergic drug, genotoxicity of sophoricoside was investigated in bacterial and mammalian cell system such as Ames bacterial reversion test, chromosomal aberration assay and single cell gel electrophoresis (Comet) assay. As results, in the range of 1,250~40 $\mu\textrm{g}$/plate sophoricoside concentrations was not shown significant mutagenic effects in Salmonella typhimurium TA 98, TA 100, TA 1535 and TA 1537 strains in Ames test. The 80% cell growth inhibition concentration (IC/SUB 80/) of sophoricoside was determined as above 5,000 $\mu\textrm{g}$/$m\ell$ in Chinese hamster lung (CHL) fibroblast cell and L5178Y mouse lymphoma cell line for the chromosomal aberration and comet assay, respectively. Sophoricoside was not induced chromosomal aberration in CHL fibroblast cell at concentrations of 700, 350 and 175 $\mu\textrm{g}$/$m\ell$ or 600, 300 and 150 $\mu\textrm{g}$/$m\ell$ in the absence or presence of S-9 metabolic activation system, respectively. Also, in the comet assay, the induction of DNA damage was not observed in L5178Y mouse lymphoma cell line both in the absence or presence of S-9 metabolic activation system. From these results, no genotoxic effects of sophoricoside were observed in bacterial and mammalian cell systems used in these experiments.

• Proceedings of the Korea Society of Environmental Toocicology Conference
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• 2003.05a
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• pp.189-189
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• 2003

Sophoricoside was isolated as the inhibitor of IL-5 bioactivity from Sophora japonica (Leguminosae). To develope as novel anti-allergic drug, kinetic study was performed in rats. Serum concentration of sophoricoside was measured by gas chromatography-mass spectrometry (GC/MS) in male Sprague-Dawley rat (250${\pm}$10g, n=5) after oral administration of sophoricoside (100mg/kg). The recovery of sophoricoside after extraction and concentration was above 95 % from rat serum. Between-day precision(relative standard deviation 2.2-2.8%) and within-day precision(2.0-12.1%) were determined from replicate analysis of a spiked control and incurred serum sample. The detection limits of sophoricoside in this serum was approximately 0.1 ng/mL. The Pharmacokinetic parameters were derived from the noncompartmental analysis. The C$\_$max/(3.56${\pm}$0.34 $\mu\textrm{g}$/mL) value for sophoricoside in male rat was observed at 7.6 h. The elimination half-life(t$\_$1/2/) of sophoricoside was approximately 4.47 h, the mean residence time (MRT) averaged 10.75 h, the total body clearance (Cl) averaged 0.0042 mL/min/kg. and the area under the serum concentration-time curve (AUC$\_$0-$\infty$/) was 24.93 $\mu\textrm{g}$$.$hr/mL.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.314.2-315
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• 2003

Sophoricoside was isolated as the inhibitor of IL-5 bioactivity from Sophora japonica (Leguminosae). To develope as novel anti-allergic drug. kinetic study was performed in rats. Serum concentration of sophoricoside was measured by gas chromatography-mass spectrometry (GC/MS) in male Sprague-Dawley rat (250${\pm}$10g, n=5) after oral administration of sophoricoside (100mg/kg). (omitted)

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.320.2-320.2
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• 2002

Macrophages activated by lipopolysaccharide (LPS) are known to induce several proinflammatory proteins including COX-2. iNOS and TNF which produce chemical mediators involved in inflammatory response. Sophoricoside and its analogs (genistin, genistein and orobol) from Sophora japonica (Leguminosae) showed differential inhibitory effects on COX-1 and 2 activities. Sophoricoside and genistin shwoed IC50 values of 4 uM and 6 uM on COX-2 activity and of 1,497 uM and 135 uM on COX-1 activity, respectively. Genistein and orobol showed IC50 values of 3 uM on COX-2 activity and of 28 uM and 18 uM on COX-1 activity. respectively. Therefore. the legume isoflavonoids to be selective COX-2 inhibitors. However. sophoricoside and its analogs did not show inhibitory effects of COX-2, iNos and TNF transcripts. which were identified by the RT-PCR.

• Proceedings of the Korean Society of Toxicology Conference
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• 2001.10a
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• pp.182-182
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• 2001

Sophoricoside was isolated as the inhibitor of IL-5 bioactivity from Sophora japonica (Leguminosae). It has been reported to have an anti-inflammatory effect on rat paw edema model. To develope as an anti-allergic drug, genotoxicity of sophoricoside was investigated in bacterial and mammalian cell system such as Ames bacterial test, chromosomal aberration assay and single cell gel electrophoresis (Comet) assay.(omitted)

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.177.1-177.1
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• 2003

Sophoricoside was isolated as the inhibitor of IL -5 bioactivity from Sophora japonica (Leguminosae). It has been reported to have an anti-inflammatory effect on rat paw edema model. To develope as an anti-allergic drug, genotoxicity of sophoricoside was investigated in bacterial and mammalian cell system such as Ames bacterial test and mouse lymphoma tk gene assay (MOLY). (omitted)

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.212.3-213
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• 2003

Polyphenolic compounds including flavonoids are wide spread in the plant kingdom, and interested recently because epidemiological studies have suggested correlations between the consumption of polyphenol-rich plant foods and the prevention of chronic diseases. Soy is a main source of isoflavonoids which are high dietary intake for the oriental population. In this study, anti-inflammatory action of sophoricoside, an isoflavone glycoside isolated from immature fruits of Sophora japonica (Leguminosae family), has been demonstrated. (omitted)

• Molecular & Cellular Toxicology
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• v.1 no.3
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• pp.179-188
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• 2005

To develop the novel anti-allergic drug, many sophoricoside derivatives were synthesized. Among these derivatives, JSH-II-3, VI-3, VII-3, VIII-3, VII-20 and VII-20 (sodium salt) were selected and subjected to high throughput toxicity screening (HTTS) because they revealed strong IL-5 inhibitory activity and limitation of quantity. Single cell gel electrophoresis (Comet) assay, mouse lymphoma thymidine kinase ($tk^{+/-}$) gene assay (MOLY), chromosomal aberration assay in mammalian cells and Ames reverse mutation assay in bacterial system were used as simplified, inexpensive, short-term in vitro screening tests in our laboratory. Through the primary screening using the comet assay, we could choose the first candidates of sophoricoside derivatives with no genotoxic potentials as JSH-VI-3, VII-3, VII-20 and VII-20 (sodium salt). Also JSH-VII-3, VII-20 and VII-20 (sodium salt) are non-mutagenic in MOLY assay, while JSH-II-3 is mutagenic at high concentration with the presence of metabolic activation system in both comet assay and MOLY assay. The selected derivatives (JSH-VI-3, VII-3, VII-20 and VII-20 (sodium salt) are not mutagenic in S. typhimurium TA98 and TA100 strains both in the presence and absence of metabolic activation. From results of chromosomal aberration assay, 6 h treatment of JSH-VI-3, VII-3 and VII-20 (sodium salt) were not revealed clastogenicity both in the presence and absence of S-9 mixture. Therefore, we suggests that JSH-VI-3, VII-3, VII-20 and VII-20 (sodium salt), as the optimal candidates with both no genotoxic potential and IL-5 inhibitory effects must be chosen. To process the development into new anti-inflammatory drug of these derivatives, further investigation will need.

• Natural Product Sciences
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• v.27 no.4
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• pp.284-292
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• 2021

Recently, a phytoestrogenic functional food has been developed using the fruits of Sophora japonica. Phytochemical investigation of fruits of S. japonica led to the isolation of eight flavonoid glycosides using various chromatographic techniques. The isolated compounds were identified as genistin (1), sophoricoside (2), genistein 7,4'-di-O-β-D-glucopyransoide (3), sophorabioside (4), genistein-7-O-β-D-glucopyranoside-4'-O-[(α-L-rhamnopyranosyl)-(1→2)-β-D-glucopyranoside] (5), sophoraflavonoloside (6), nicotiflorin (7) and kaempferol-3-O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranosyl-(1→3)-β-D-glucopyranoside (8), respectively, by comparison of their spectroscopic data with those reported in the literature. In addition, a new HPLC-DAD method for simultaneous determination of the isolated compounds was developed to quantitate the contents of flavonoids in S. japonica and S. flavescens. The method was validated in terms of limit of detection, limit of quantitation, specificity, linearity, precision and accuracy. The validated method was successfully applied to determine eight flavonoids in two Sophora species. The contents of eight flavonoids varied according to the parts and species. Particularly, it was found that only the fruits of S. japonica contained sophoricoside, a phytoestrogenic isoflavone.