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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.
천연자원으로부터 아실코에이: 콜레스테롤아실 전달효소 저해제의 탐색
김미경,권병목,배기환,최돈하,이학주,김홍은,김영국,Kim, Mi-Kyung,Kwon, Byoung-Mog,Bae, Ki-Hwan,Choi, Don-Ha,Lee, Hak-Ju,Kim, Hong-Eun,Kim, Young-Kook 한국생약학회 1999 생약학회지 Vol.30 No.4
Acyl-CoA: Cholesterol Acyltransferase (ACAT) is a key enzyme responsible for cholesteryl ester formation in atherogenesis and in cholesterol absorption from the intestines. In addition under pathological conditions, formation and accumulation of cholesteryl ester as lipid droplets by ACAT within macrophages constitute a characteristic feature of early lesions of atherosclerotic plaques. ACAT inhibitors are expected to be effective for treatment of atherosclerosis and hypercholesterolemia. ACAT inhibitors of natural origin have been rarely reported. In our screening program for ACAT inhibitors, 303 plants were extracted with methanol or ethanol, and screened for the inhibitory activity against ACAT from the rat liver microsome. Extracts of 13 plants including Quercus aliena, Diospyros kaki, Platycarya strobilacea and Hibiscus syriacus inhibited more than 90% of ACAT activity and 43 samples in alcohol extracts such as Magnolia obovata and Panax ginseng also inhibited more than 70% of ACAT activity at a concentration of $100\;{\mu}g/ml$.
식용식물자원으로부터 활성물질의 탐색-XXII. 사자발쑥 (Artemisia princeps PAMPANINI)의 지상부로부터 Triterpenoid의 분리
백남인,방면호,조진경,송명종,이대영,한민우,정해곤,정태숙,이경태,최명숙 한국응용생명화학회 2008 Journal of Applied Biological Chemistry (J. Appl. Vol.51 No.3
The aerial parts of Sajabalssuk (Artemisia princeps PAMPANINI, Sajabalssuk) was extracted with 80% aqueous MeOH, and the concentrated extract was partitioned with EtOAc, n-BuOH and H2O, successively. From the EtOAc fraction, three cycloartane-type triterpnoids and one ursanetype triterpenoid were isolated through the repeated silica gel, ODS and Sephadex LH-20 column chromatographies. From the results of physico-chemical data including NMR, MS and IR, the chemical structures of the triterpenoids were determined as wrightial (1), wrightial acetate (2), 27- norcycloart-20(21)-ene-25-al-3β-ol acetate (3) and ursolic acid (4). No report has been found for isolation of compound 3 in the literature so far, and compounds 1, 2 and 3 were the first to be isolated from Sajabalssuk (Artemisia princeps PAMPANINI, Sajabalssuk). Also, compound 1 showed Acyl-CoA:Cholesterol acyltransferase (hACAT-1) and hACAT-2 inhibitory activity with the IC50 values of 33.0 and 45.0 μg/ml, respectively. Compounds 2 and 3 inhibited hACAT-1 activity with the IC50 values of 12.0 and 16.0 μg/ml, respectively. The aerial parts of Sajabalssuk (Artemisia princeps PAMPANINI, Sajabalssuk) was extracted with 80% aqueous MeOH, and the concentrated extract was partitioned with EtOAc, n-BuOH and H2O, successively. From the EtOAc fraction, three cycloartane-type triterpnoids and one ursanetype triterpenoid were isolated through the repeated silica gel, ODS and Sephadex LH-20 column chromatographies. From the results of physico-chemical data including NMR, MS and IR, the chemical structures of the triterpenoids were determined as wrightial (1), wrightial acetate (2), 27- norcycloart-20(21)-ene-25-al-3β-ol acetate (3) and ursolic acid (4). No report has been found for isolation of compound 3 in the literature so far, and compounds 1, 2 and 3 were the first to be isolated from Sajabalssuk (Artemisia princeps PAMPANINI, Sajabalssuk). Also, compound 1 showed Acyl-CoA:Cholesterol acyltransferase (hACAT-1) and hACAT-2 inhibitory activity with the IC50 values of 33.0 and 45.0 μg/ml, respectively. Compounds 2 and 3 inhibited hACAT-1 activity with the IC50 values of 12.0 and 16.0 μg/ml, respectively.
이대영,정태숙,류하나,방면호,홍윤희,이윤형,백남인 한국약용작물학회 2008 한국약용작물학회지 Vol.16 No.5
Cholesterol acyltransferase (ACAT) catalyzes the acylation of cholesterol to cholesteryl ester with long chain fatty acids and ACAT inhibition is a useful strategy for treating hypercholesterolemia or atherosclerosis. Inhibitory effects on ACAT of the MeOH extracts prepared from 163 edible plants were evaluated. 15 species out of 163 species exhibited higher than 50% of inhibition on the hACAT-1 and 9 species exhibited higher than 50% of inhibition on the hACAT-2 activity at their concentration of 100 μg/mL.
식용식물자원으로부터 활성물질의 탐색-XXII. 사자발쑥 (Artemisia princeps PAMPANINI)의 지상부로부터 Triterpenoid의 분리
방면호 ( Myun Ho Bang ),조진경 ( Jin Gyeong Cho ),송명종 ( Myoung Chong Song ),이대영 ( Dae Young Lee ),한민우 ( Min Woo Han ),정해곤 ( Hae Gon Chung ),정태숙 ( Tae Sook Jeong ),이경태 ( Kyung Tae Lee ),최명숙 ( Myung Sook Choi 한국응용생명화학회(구 한국농화학회) 2008 Applied Biological Chemistry (Appl Biol Chem) Vol.51 No.3