• 생명과학회지
• /
• 제28권2호
• /
• pp.247-256
• /
• 2018

심혈관계 질환은 질환별 사망률 순위에 있어서 세계에서는 1위이며, 우리나라에서는 2위인 질병이다. 심혈관계 질환 발생의 주 위험 요인인 콜레스테롤은 HMG-CoA reductase에 의해 간에서 신생합성이 조절된다. 현재 고콜레스테롤혈증 치료에 statin이 널리 사용되고 있지만 광범위한 부작용이 보고되고 있어서 이를 대체하거나 보조할 수 있는 천연물 유래의 기능성 물질 개발이 필요한 실정이다. 따라서 본 연구에서는 혈장 콜레스테롤 감소 활성을 가지는 물질을 발굴하고자 98종의 플라보노이드 및 그와 관련된 화합물들을 대상으로 $10{\mu}g/ml$ 농도에서 HMG-CoA reductase 저해 활성을 탐색하였다. 그 결과, sophoraflavanone G, morin, 및 kuraridin이 각각 54.6%, 45.04% 및 21.9%의 저해활성을 타내었으며, $IC_{50}$값을 계산한 결과, sophoraflavanone G가 $7.3{\mu}g/ml$로 가장 낮았으며 morin과 kuraridin은 각각 $13.3{\mu}g/ml$과 $87.4{\mu}g/ml$으로 확인되어, 향후 고콜레스테롤혈증 예방 및 치료제의 가능성을 제시하였다.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
• /
• pp.151.2-151.2
• /
• 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)

• 대한약학회:학술대회논문집
• /
• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
• /
• pp.197.3-197.3
• /
• 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
• /
• 제27권6호
• /
• pp.593-599
• /
• 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.

• 한국미생물·생명공학회지
• /
• 제34권3호
• /
• pp.265-272
• /
• 2006

피부 여드름 치료, 예방을 위한 천연물의 활성평가를 시도하였다. 335종의 약용 및 야생식물의 다양한 부위로부터 500종의 추출물을 조제하여, 여드름 원인세균인 Propionibacterium acnes에 대한 생육저지 활성을 평가한 결과, 21종 식물체에서 조제한 25종 추출물에서 활성을 확인하였다. 500종 추출물 중, 홀아비꽃대(지상부) 추출물에서 가장 강력한 활성이 나타났으며, 방기, 고삼, 오수유, 은행(씨), 상백피, 독활 및 호장근 추출물에서도 우수한 활성을 확인하였다. 특히 고삼, 상백피, 독활 등의 항여드름 활성은 기존 보고 및 민간요법과도 잘 일치하며, 홀아비꽃대 및 방기 추출물의 항여드름 균 활성은 본 연구에서 처음으로 확인하였다. 고삼을 대상으로 한 활성물질 분리결과, kuraridin과 kurarinone의 주요 활성물질임을 확인하였다. 본 연구결과는, 안정성이 확보된 식물추출물로부터 새로운 피부여드름 치료제 개발이 가능함을 제시하고 있으며, 현재 고삼 추출물 및 활성물질의 세포 독성 및 작용기전에 대한 연구가 진행중이다.

• Archives of Pharmacal Research
• /
• 제25권3호
• /
• pp.329-335
• /
• 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.

• 한국응용약물학회:학술대회논문집
• /
• 한국응용약물학회 2001년도 추계학술대회 및 정기총회
• /
• pp.82-82
• /
• 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
• /
• 제28권5호
• /
• pp.534-540
• /
• 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.