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( Sabina Shrestha ),( Ji Hae Park ),( Dae Young Lee ),( Jin Gyeong Cho ),( Do Gyeong Lee ),( Moon Hee Cho ),( Tae Sook Jeong ),( Hee Cheol Kang ),( Nam In Baek ) 한국응용생명화학회 2011 Journal of Applied Biological Chemistry (J. Appl. Vol.54 No.1
The bark of Machilus thunbergii was extracted with 80% aqueous methanol (MeOH), and the concentrated extract was partitioned using ethyl acetate (EtOAc), butanol (n-BuOH), and H2O, successively. From the EtOAc fraction, five lignans were isolated through the repeated silica gel, octadecyl silica gel (ODS) and, Sephadex LH-20 column chromatography. Based on nuclear magnetic resonance (NMR), mass spectroscopy (MS), and infrared spectroscopy (IR) spectroscopic data, the chemical structures of the compounds were determined to be machilin A (1), machilin F (2), licarin A (3), nectandrin A (4), and nectandrin B, (5). This study presents comparative account of five lignans from M. thunbergii bark contributing inhibition of low density lipoprotein (LDL), ACAT-1, and ACAT-2. Compounds 2-5 showed varied degree of antioxidant activity on LDL with IC50 values of 2.1, 11.8, 15.3, and 4.1 μM. Compounds 1, 2, and 3 showed inhibition activity on ACAT-1 with values 63.4±6.9% (IC50=66.8 μM), 53.7±0.9% (IC50=109.2 μM), and 78.7±0.2% (IC50= 40.6 μM), respectively, at a concentration of 50 mg/mL, and on ACAT-2 with values 47.3±1.5% (IC50=149.7 μM), 39.2±0.2% (IC50=165.2 μM), and 52.1±1.0% (IC50=131.0 μM), respectively, at a concentration of 50 mg/mL.
Baek, Mi-Young,Cho, Jin-Gyeong,Lee, Dae-Young,Ahn, Eun-Mi,Jeong, Tae-Sook,Baek, Nam-In The Korean Society for Applied Biological Chemistr 2010 Applied Biological Chemistry (Appl Biol Chem) Vol.53 No.3
The dried stem bark of Albizia julibrissin was extracted in 70% aqueous EtOH, and concentrated extracts were partitioned with EtOAc, n-BuOH, and $H_2O$, successively. From the EtOAc fraction, three triterpenoids were isolated through repeated silica gel and octadecyl silica gel column chromatography. Based on nuclear magnetic resonance spectrometry (NMR), mass spectrometry, and infrared spectroscopy spectroscopic data, the chemical structures of the compounds were determined to be lupeol (1), betulinic acid (2), and oleanolic acid (3). This was the first report in which compounds 1, 2, and 3 were isolated from the stem bark of A. julibrissin. Since the NMR data for some compounds have been incorrectly or incompletely identified in previous literature, the NMR were revised on the basis of 2-D NMR experiments. Compounds 1, 2, and 3 showed inhibition activity on ACAT-1 with values of $89.3{\pm}3.7%$, $61.2{\pm}3.4%$, and $52.5{\pm}0.7%$, respectively, at a concentration of $50\;{\mu}g/mL$ and on ACAT-2 with values of $44.3{\pm}2.1%$, $55.5{\pm}0.3%$, and $22.0{\pm}2.6%$, respectively, at a concentration $50\;{\mu}g/mL$.
( Mi Young Baek ),( Jin Gyeong Cho ),( Dae Young Lee ),( Eun Mi Ahn ),( Tae Sook Jeong ),( Nam In Baek ) 한국응용생명화학회 2010 Applied Biological Chemistry (Appl Biol Chem) Vol.53 No.3
The dried stem bark of Albizia julibrissin was extracted in 70% aqueous EtOH, and concentrated extracts were partitioned with EtOAc, n-BuOH, and H2O, successively. From the EtOAc fraction, three triterpenoids were isolated through repeated silica gel and octadecyl silica gel column chromatography. Based on nuclear magnetic resonance spectrometry (NMR), mass spectrometry, and infrared spectroscopy spectroscopic data, the chemical structures of the compounds were determined to be lupeol (1), betulinic acid (2), and oleanolic acid (3). This was the first report in which compounds 1, 2, and 3 were isolated from the stem bark of A. julibrissin. Since the NMR data for some compounds have been incorrectly or incompletely identified in previous literature, the NMR were revised on the basis of 2-D NMR experiments. Compounds 1, 2, and 3 showed inhibition activity on ACAT-1 with values of 89.3±3.7%, 61.2±3.4%, and 52.5±0.7%, respectively, at a concentration of 50 μg/mL and on ACAT-2 with values of 44.3±2.1%, 55.5±0.3%, and 22.0±2.6%, respectively, at a concentration 50 μg/mL.
Yinglan Jin,노문철,Kondaji Gajulapati,Hwa Young Jung,Shanthaveerappa K. Boovanahalli,이지현,Jung Ho Choi,김영국,Kyeong Lee,Yongseok Choi 대한화학회 2009 Bulletin of the Korean Chemical Society Vol.30 No.6
A novel series of imidazo[1,2-α]pyridines was designed, synthesized, and tested for their ability to inhibit acyl- CoA:cholesterol acyltransferase. Preliminary lead optimization efforts resulted in the identification of ACAT inhibitors represented by analogues 5b, 5c, 6a, 6c, 7b, and 7c. The ACAT inhibitory activity of these compounds was further established by potent inhibition of cholesteryl ester formation in HepG2 cells by a representative analogue 7b.
Mi Young Baek,Jin Gyeong Cho,Dae Young Lee,Eun Mi Ahn,Tae Sook Jeong,Nam In Baek 한국응용생명화학회 2010 Journal of Applied Biological Chemistry (J. Appl. Vol.53 No.3
The dried stem bark of Albizia julibrissin was extracted in 70% aqueous EtOH, and concentrated extracts were partitioned with EtOAc, n-BuOH, and H2O, successively. From the EtOAc fraction, three triterpenoids were isolated through repeated silica gel and o
Jin, Ying-Lan,Rho, Mun-Chual,Gajulapati, Kondaji,Jung, Hwa-Young,Boovanahalli, Shanthaveerappa K.,Lee, Jee-Hyun,Song, Gyu-Yong,Choi, Jung-Ho,Kim, Young-Kook,Lee, Kyeong,Choi, Yong-Seok Korean Chemical Society 2009 Bulletin of the Korean Chemical Society Vol.30 No.6
A novel series of imidazo[1,2-$\alpha$]pyridines was designed, synthesized, and tested for their ability to inhibit acyl- CoA:cholesterol acyltransferase. Preliminary lead optimization efforts resulted in the identification of ACAT inhibitors represented by analogues 5b, 5c, 6a, 6c, 7b, and 7c. The ACAT inhibitory activity of these compounds was further established by potent inhibition of cholesteryl ester formation in HepG2 cells by a representative analogue 7b.
고콜레스테를 조건으로 배양한 Hep G2세포의 콜레스테를 함량변동과 Acyl CoA : Cholesterol Acyltransferase의 활성에 미치는 인삼성분의 영향
박성출,노연희,구자현,Park, Song-Chul,Noh, Yun-Hee,Koo, Ja-Hyun 고려인삼학회 1995 Journal of Ginseng Research Vol.19 No.3
A human hepatoma cell line, hep G2, was used to investigate the mechanism of serum cholesterol reduction by ginseng total saponin, ginsenoside-$Rb_1$, - $Rb_2$, and non-saponin fraction (ether extraction). Hep G2 cells were incubated in 10 $\mu\textrm{g}$/ml of cholesterol containing serum free-RPMl1640 medium with various concentration of ginseng components. The amounts of cholesterol in Hep G2 cells were decreased to maximum 51% in total saponin or two ginsenoside-treated groups while there was 137% increase in cholesterol level of control group as compared with that of normal group. Nonsaponin groups did not show the same effect. In order to elucidate the observed changes in the amount of cholesterol, the activity of amyl CoA : cholesterol acyltransferase (ACAT) in groups showing remarkable reduction in cholesterol amount, i.e., total saponin 10-6%, ginsenoside-$Rb_1$ $10^{-4}$%, ginsenoside-$Rb_2$, $10^{-4}$%, and non-saponin fraction $10^{-4}$%, was assayed using [1-$^{-14}C$%]oleic acid as enzyme substrate. The activity of ACAT was increased in all groups tested as compared with that of control group except for non-saponin group cultured in water soluble cholesterol containing medium. The serum cholesterol lowering effects of ginseng components can partially be attributed to the increased hepatocellular ACAT activity.
임치환,김종민,백승화,Lim, Chi-Hwan,Kim, Jong-Min,Baek, Seung-Hwa 대한예방한의학회 2008 대한예방한의학회지 Vol.12 No.3
80% MeOH extract of black rices fractionated with n-hexane, EtOAc, and n-BuOH. Copper-induced LDL oxidation inhibition assay and ACAT inhibition assay examined with fractions. n-Hexane and EtOAc fractions showed high inhibition activity. We divided n-hexane fraction into three sub-layers(H1 - H3) and EtOAc into eight sub-layers(E1 - E8). H1, H2, E6, and E7 are showed higher inhibition activity than standard in Lp-PLA2 inhibition assay and H1 and E6 are showed higher ACAT inhibition activity than standard.