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손건호,정근영,도재철,Son, Kun-Ho,Jung, Keun-Young,Do, Jae-Chul 한국생약학회 1993 생약학회지 Vol.24 No.3
Three compounds were isolated from the rhizomes of Dioscorea quinqueloba and identified as $diosgenin\;3-O-{\alpha}_-L-rhamnopyranosyl(1{\rightarrow}2)-{\beta}-_D-glucopyranoside$, dioscin and gracillin by chemical and spectroscopic means.
손건호,김소희,정근영,장현욱,Son, Kun-Ho,Kim, So-Hee,Jung, Keun-Young,Chang, Hyeun-Wook 한국생약학회 1994 생약학회지 Vol.25 No.2
The platelet activating factor (PAF) is a newly discovered chemical mediator, the chemical structure of which is 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine. Since PAF has potent and broad activities, its pathophysiological roles have received much attention. To develope a new PAF antagonist from medicinal plants, extracts of twenty medicinal herb were screened using PAF receptor binding, $[^{14}C]$ serotonin release and platelet aggregation.
플라보노이드 화합물로부터 HMG-CoA reductase 저해 활성 물질 탐색
손건호(Kun Ho Son),이주연(Ju Yeon Lee),이정순(Jeong Soon Lee),강삼식(Sam Sik Kang),손호용(Ho Yong Sohn),권정숙(Chong Suk Kwon) 한국생명과학회 2018 생명과학회지 Vol.28 No.2
심혈관계 질환은 질환별 사망률 순위에 있어서 세계에서는 1위이며, 우리나라에서는 2위인 질병이다. 심혈관계질환 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 μg/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, IC50값을 계산한 결과, sophoraflavanone G가 7.3 μg/ml로 가장 낮았으며 morin과 kuraridin은 각각 13.3 μg/ml과 87.4 μg/ml으로 확인되어, 향후 고콜레스테롤혈증 예방 및 치료제의 가능성을 제시하였다. 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 μg/ml, and the IC50 values were calculated to 13.31 μg/ml and 7.26 μg/ml respectively.
페놀 화합물로부터 HMG-CoA reductase 저해 활성 물질 탐색
손건호(Kun Ho Son),이주연(Ju Yeon Lee),이정순(Jeong Soon Lee),강삼식(Sam Sik Kang),손호용(Ho Yong Sohn),권정숙(Chong Suk Kwon) 한국생명과학회 2017 생명과학회지 Vol.27 No.3
심혈관계 질환은 질환별 사망률 순위에 있어서 세계에서는 1위이며, 우리나라에서는 2위인 질병이다. 심혈관계질환 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 71종의 페놀 및 그와 관련된 화합물들을 대상으로 10 ug/ml 농도에서 HMG-CoA reductase 저해 활성을 탐색하였다. 그 결과, 1,4-naphthoquinone의 HMG-CoA reductase 저해율이 99.4%로 가장 높았고, 다음으로 plumbagin 91.4%, pentagalloyl β-D-glucose 46.6%, 2,4-dihydroxybenzoic acid 40.9%, shikonin 37.7%, 1,2-naphthoquinone 36.6%, trans-cinnamic acid 32.0%, acetonylgeraniin 30.2%, benzoic acid 28.5%, geraniin 28.3%, gentisic acid 22.3%의 순이었다. IC50값을 계산한 결과, 1,4-naphthoquinone가 2.1 μg/ml로 가장 낮았으며, plumbagin과 pentagalloyl β-D-glucose은 각각 5.8 μg/ml과 13.1 μg/ml으로 나타났다. 1,4-naphthoquinone과 plumbagin의 경우, 5 μg/ml에서도 각각 90.3%와 43.3%의 저해율을 나타내었다. High level of plasma cholesterol is strongly associated with the development of atherosclerosis and coronary heart disease. Clinical trials designed to reduce plasma cholesterol level by diet or pharmacological intervention have resulted in marked reduction of disease incidence. The enzyme 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase which reduces cholesterol biosynthesis in the liver is the key enzyme of the mevalonate pathway that produces cholesterol. In this study, 71 naturally occurring phenolic compounds were tested for inhibitory activities against HMG-CoA reductase. Eleven compounds out of 71 showed inhibitory activities: three hydrolyzable tannin (geraniin, acetonyl geraniin and pentagalloyl β-D-glucose), four benzoic acid derivatives (benzoic acid, trans-cinnamic acid, 2,4-dihydroxybenzoic acid and 2,5-dihydroxybenzoic acid), and four naphthoquinone derivatives (1,2-naphthoquinone, 1,4-naphthoquinone, plumbagin and shikonin). At the concentration of 10 μg/ml, 1,4-naphthoquinone inhibited HMG-CoA reductase by 99.4%, and then plumbagin 91.4%, pentagalloyl β-D-glucose 46.6%, 2,4-dihydroxybenzoic acid 40.9%, shikonin 37.7%, 1,2-naphthoquinone 36.6%, trans-cinnamic acid 32.0%, acetonyl geraniin 30.2%, benzoic acid 28.5%, geraniin 28.3% and 2,5-dihydroxybenzoic acid 22.3%, respectively. IC50 values of 1,4-naphthoquinone and plumbagin was 2.1 μg/ml and 5.8 μg/ml, respectively. Antioxidant activities;Microphthalmia-associated transcription factor;Sesamum indicum L.;tyrosinase related protein-1;tyrosinase related protein-2;Tyrosinase
Corosolic acid의 유방암세포 증식 및 전이에 미치는 영향
손건호(Kun Ho Son),황진현(Jin-hyeon Hwang),김동하(Dong-ha Kim),조영은(Young-Eun Cho) 한국영양학회 2020 Journal of Nutrition and Health Vol.53 No.2
본 연구는 인간 유래 유방 암세포 MDA-MB-231를 대상으로 CA에 의한 세포사멸, 세포 이동 및 침윤 효과를 조사하였다. 암세포의 증식 억제 효과는 CA 농도 의존적으로 증식률이 감소하는 것을 확인하였다. CA에 의한 apoptosis 양성 세포를 확인하기 위해 DAPI stain를 진행한 결과, CA 농도 의존적으로 죽은 세포를 확인하였다. MDA-MB-231 세포에서 CA에 의한apoptosis marker 단백질 발현 증가와 ROS production증가를 확인할 수 있었다. 또한 CA에 의한 MDAMB-231의 세포 이동률이 유의적으로 감소하는 것을 확인하였다. 마지막으로 세포의 이동과 전이 능력 또한 CA를 처리한 군에서 통계적으로 감소하는 것을 확인하였다. 본 연구 결과를 통해서 CA의 암세포 증식률 억제, 세포사멸 증가, 그리고 세포 이동 및 전이 억제 효과가 나타나는 것을 확인했으며, 이 결과를 통해서 향후 유방암에 대한 항암제로 개발될 수 있는 가능성을 가지고 있는 것으로 사료된다. Purpose: Corosolic acid (CA), also known as 2α-hydroxyursolic acid, is present in numerous plants, and is reported to exhibit anti-cancer and anti-proliferative activities in various cancer cells such as osteosarcoma, hepatocellular carcinoma, lung adenocarcinoma, and colon cancer. However, the anti-cancer activity of CA on human breast cancer cells and the underlying mechanisms remain to be elucidated. The present study aimed to investigate the anticancer effects of CA in the human breast cancer cell line, MDA-MB-231. Methods: Cell viability, reactive oxygen species (ROS) production, apoptosis marker protein expression, migration, invasion rate, and vascular endothelial growth factor (VEGF) levels were assessed by treating MDA-MB-231 cells to increasing concentrations of CA. Results: The results showed that CA significantly inhibited the cell proliferation of MDAMB-231 cells in a dose-dependent manner. To assess the effect of CA on apoptosis, nuclei of MDA-MB-231 cells were stained with DAPI solution. Chromatin condensation, which indicates apoptosis, was observed to increase dose-dependently. In addition, western-blot analysis revealed elevated levels of the apoptosis marker proteins (Bax and cleaved caspase 3) subsequent to MDA-MB-231 exposure to CA. ROS production was also increased in the CA-induced apoptosis in MDA-MB-231 treated cells. Interestingly, CA exposure resulted in significantly decreased migration and invasion rates in the MDA-MB-231 cells. Data further revealed that exposure to CA markedly decreased the VEGF concentration, thereby contributing to a reduction in angiogenesis. Conclusion: Our results determined that exposure to CA induces anti-proliferation, apoptosis, and ROS production, and suppresses cell migration and invasion rate in MDAMB-231 cells. Taken together, these results indicate the potential of CA to be applied as an effective chemotherapeutic agent for treating breast cancer.
멍석딸기뿌리의 성분에 관한 연구(Ⅰ). : (-)-Epicatechin의 분리
손건호(Kun Ho Son),강삼식(Sam Sik Kang),도재철(Jae Chul do) 한국생약학회 1988 생약학회지 Vol.19 No.3
(-)-Epicatechin, mp 234∼6°, was isolated from the fresh roots of Rubus parvifolius together with a sterol mixture, which was found to be a mixture of β-sitosterol (major), stigmasterol and campesterol.
손건호(Kun Ho Son),김주선(Ju sun Kim),강삼식(Sam Sik Kang),김현표(Hyun Pyo Kim),장현욱(Hyeun Wook Chang) 한국생약학회 1994 생약학회지 Vol.25 No.1
Two flavonoids, diosmetin 7-O-glucoside and lonicerin, and an iridoid, vogeloside have been isolated from the aerial parts of Lonicera japonica (Caprifoliaceae). The structures of these isolates have been detekmined by chemical transformations and interpretation of the spectral data. This is the first report of the isolation of diosmetin 7-O-glucoside from this plant.