• Journal of Life Science
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• v.28 no.2
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• pp.247-256
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• 2018

3-Hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors (statins) are widely used drugs for lowering blood lipid levels and preventing cardiovascular diseases. HMG-CoA reductase is a key enzyme to control the biosynthesis of cholesterol. We have tested HMG-CoA reductase-inhibitory activity on the flavonoids of 98 species in vitro. The anti-hypercholesterolemic activities of flavonoids were studied using an HMG-CoA reductase assay equipped with a 96-well UV plate. This assay was based on the spectrophotometric measurement of the decrease in absorbance, which represents the oxidation of NADPH by the catalytic subunit of HMG-CoA reductase in the presence of the substrate HMG-CoA. Among the clinically available statins, pravastatin was used as a positive control. Among the tested compounds, kuraridin, morin and sophoraflavanone G showed strong inhibition activities. In particular, morin and sophoraflavanone G inhibited HMG-CoA reductase by 45.0% and 54.6% at a concentration of $10{\mu}g/ml$, and the $IC_{50}$ values were calculated to $13.31{\mu}g/ml$ and $7.26{\mu}g/ml$ respectively.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.151.2-151.2
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• 2003

For the purpose of the development of a skin-whitening agent, Sophora flavescens was evaluated for tyrosinase inhibitory activity and its active principles were identified followed activity-guided isolation. The ethanol extract and dichloromethane fraction from S. flavescens showed significant inhibition of mushroom tyrosinase. From the dichloromethane fraction, three known prenylated flavonoids, sophoraflavanone G, kuraridin, and kurarinone, were isolated. Compared with kojic acid ($IC_50$=20.5 $\mu$M), these compounds possessed more potent tyrosinase inhibitory activity. (omitted)

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.197.3-197.3
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• 2003

From the EtOAc fraction of the MeOH extract of Albizzia julibrissin (Leguminosae), a rare 5-deoxy flavone (geraldone), a 3',4',7,8-tetrahydroxyflavanone, an isoflavone (daidzein), and five prenylated flavonoids (sophoflavescenol, kurarinone, kurarinol, kuraridin and kuraridinol) were isolated and identified based on the analysis of spectral data.(omitted)

• Archives of Pharmacal Research
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• v.27 no.6
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• pp.593-599
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• 2004

From the EtOAc fraction of the MeOH extract of Albizzia julibrissin (Leguminosae）, a rare 5-deoxyflavone (geraldone, 1）, isookanin (2）, luteolin (3）, an isoflavone (daidzein, 4）, five prenylated flavonoids ［soph6f1avescenol (5）, kurarinone (6）, kurarinol (7）, kuraridin (8） and kuraridinol (9）］, a cerebroside (soya-cerebroside I, 10）, and $(-)-syringaresinol-4-O-{\beta}-D-glucopyranoside$ (11） were isolated and characterized on the basis of spectral data. Compounds 2, 3, and 11, showed 1, 1-diphenyl-2-picrylhydrazyl radical scavenging activity.

• Microbiology and Biotechnology Letters
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• v.34 no.3
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• pp.265-272
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• 2006

Acne is a chronic inflammatory follicular disorder of the skin, occurring in specialized pilosebaceous units on the face, and Propionibacterium acnes, a strict anaerobic pathogen, plays an important role in the pathogenesis of acne. To develop a reliable and effective anti-acne agent, we have evaluated antibacterial activity of 500 plant extracts, prepared from 335 plants, against P. acnes. Based on the results of disc-paper method, 25 plant extracts, including the extracts of Chloranthus japonicus (aerial part), Sophora flavescens (radix), Evodia officinalis (fructus), Ginko biloba (semem), Morus alba (root bark), Aralia continentalis (whole) and Reynoutria elliptica (radix), were selected as possible sources of anti-acne agent. Among them, the extract of S. flavescens (radix) was finally selected and kuraridin and kurarinone were identified as major active compounds of S. flavescens. These results suggested that medicinal and wild plants could be the potential source of anti-acne agent.

• Archives of Pharmacal Research
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• v.25 no.3
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• pp.329-335
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• 2002

Previously, several prenylated flavonoids having a C-8 lavandulyl moiety were found to inhibit cyclooxygenase-1 (COX-1) as well as 5-lipoxygenase (5-LOX), and sophoraflavanone G was the most potent inhibitor against these eicosanoid generating enzymes among 19 prenylated flavonoids tested. In this investigation, effects of sophoraflavanone G on COX-2 induction from RAW 264.7 cells and in vivo inflammatory response were studied. Sophoraflavanone G inhibited prostaglandin $E_2{\;}(PGE_2)$ production from lipopolysaccharide (LPS)-treated RAW cells by COX-2 down-regulation at 1-50 uM. Other prenylated flavonoids including kuraridin and sanggenon D also down-regulated COX-2 induction at 10-25 uM, while kurarinone and echinoisoflavanone did not. In addition, sophoraflavanone G showed in vivo anti-inflammatory activity against mouse croton oil-induced ear edema and rat carrageenan paw edema via oral (2-250 mg/kg) or topical administration (10-250 ug/ear). Although the potencies of inhibition were far less than that of a reference drug, prednisolone, this compound showed higher anti-inflammatory activity when applied topically, suggesting a potential use for several eicosanoidrelated skin inflammation such as atopic dermatitis.

• Proceedings of the Korean Society of Applied Pharmacology
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• 2001.11a
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• pp.82-82
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• 2001

Previously, several prenylated flavonoids having a C-8 lavandulyl moiety were found to inhibit cyclooxygenase-1 (COX-1) as well as 5-lipoxygenase (5-LOX), and sophoraflavanone G was the most potent inhibitor against these eicosanoid generating enzymes among the prenylated flavonoids tested. In this investigation, effects of sophoraflavanone G on COX-2 induction from RAW 264.7 cells and in vivo inflammatory response were studied. Sophoraflavanone G inhibited prostaglandin E$_2$(PGE$_2$) production from lipopolysaccharide (LPS)-treated RAW cells by COX-2 down-regulation without significantly affecting COX-2 activity at 1 50 $\mu$M. Other prenylated flavonoids including kuraridin and sanggenon D also down-regulated COX-2 induction at 10-25 $\mu$M, lirhile kurarinone and echinoisoflavanone did not. In addition, sophoraflavanone G shelved in vivo anti-inflammatory activity against mouse croton oil-induced ear edema and rat carrageenan paw edema via oral (2-250mg/kg) or topical administration (10 - 250 $\mu\textrm{g}$/ear). Although the potencies of inhibition were far less than that of a reference drug, prednisolone, this compound showed higher anti-inflammato교 activity when applied topically, suggesting a potential use for several eicosanoid-related skin inflammation such as atopic dermatitis.

• Archives of Pharmacal Research
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• v.28 no.5
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• pp.534-540
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• 2005

Activity-guided fractionation of the CH$_2Cl_2$-soluble fraction of the roots of Sophora flavescens furnished five 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scaveng ers: trans-hexadecyl ferulic acid (1) cis-octadecyl ferulic acid (2), trans-hexadecyl sinapic acid (3), (-)-4-hydroxy-3-methoxy-(6aR,11aR)-8, 9-methylenedioxypterocarpan (4) and desmethylanhydroicaritin (8), along with nine known inactive compounds: (-)-maackiain (5), xanthohumol (6), formononetin (7), (2S)-2'-methoxykurarinone (9), (2S)-3${\beta}$,7,4'-trihydroxy-5-methoxy-8-(${\gamma},{\gamma}$- imethylallyl )-flavanone (10), (2S)-7,4'-dihydroxy-5-methoxy-8- (${\gamma},{\gamma}$-dimethylallyl ) -flavanone (11), umbelliferone (12), kuraridin (13), and trifolirhizin (14). Compounds 1-4 and 8 exhibited DPPH free radical scavenging effects at IC$_{50}$ values of 33.01 ${\pm}$ 0.20, 57.06 ${\pm}$ 0.16, 39.84 ${\pm}$ 0.36, 35.83 ${\pm}$ 0.47, and 18.11 ${\pm}$ 0.04${\mu}$M, respectively. L-Ascorbic acid, when used as a positive control, exhibited an IC$_{50}$ value of 7.39 ${\pm}$ 0.01 ${\mu}$M. Compounds 1-4 and 8 also appeared to exert significant scavenging effects on authentic ONOO-, with IC$_{50}$ values of 5.76 ${\pm}$ 1.19, 15.06 ${\pm}$ 1.64, 8.17 ${\pm}$ 4.97, 1.95 ${\pm}$ 0.29 and 4.06 ${\pm}$ 2.41 ${\mu}$M, respectively. Penicillamine (IC$_{50}$= 2.36 ${\pm}$ 0.79${\mu}$M) was used as a positive control. In addition, compounds 2,4,6,8, and 10 were isolated from this plant for the first time.