• Title/Summary/Keyword: ACAT inhibitory activity

Search Result 27, Processing Time 0.02 seconds

Development of Biologically Active Compounds from Edible Plant Sources XXII. Triterpenoids from the Aerial Parts of Sajabalssuk (Artemisia princeps PAMPANINI) (식용식물자원으로부터 활성물질의 탐색-XXII. 사자발쑥(Artemisia princeps PAMPANINI)의 지상부로부터 Triterpenoid의 분리)

  • Bang, Myun-Ho;Cho, Jin-Gyeong;Song, Myoung-Chong;Lee, Dae-Young;Han, Min-Woo;Chung, Hae-Gon;Jeong, Tae-Sook;Lee, Kyung-Tae;Choi, Myung-Sook;Baek, Nam-In
    • Applied Biological Chemistry
    • /
    • v.51 no.3
    • /
    • pp.223-227
    • /
    • 2008
  • 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 $H_2O$, successively. From the EtOAc fraction, three cycloartane-type triterpnoids and one ursane-type 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-3${\beta}$-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 $IC_{50}$ values of 33.0 and 45.0 ${\mu}g/ml$, respectively. Compounds 2 and 3 inhibited hACAT-1 activity with the $IC_{50}$ values of 12.0 and 16.0 ${\mu}g/ml$, respectively.

The Effects of Gangzitongmaekeum on Antioxidation Activity and Dietary Hyperlipidemia-induced Mice (강지통맥음(降脂通脈飮)이 항산화 활성과 고지혈(高脂血) 유발(誘發) 백서(白鼠)에 미치는 영향(影響))

  • Cha, Kwan-Bae;An, Joung-Jo;Jo, Hyun-Kyung;Yoo, Ho-Rhyong;Kim, Yoon-Sik;Seol, In-Chan
    • The Journal of Internal Korean Medicine
    • /
    • v.29 no.3
    • /
    • pp.703-715
    • /
    • 2008
  • This experiments was performed to determine the effects of Gangzitongmaekeum(降脂通脈飮 : GTE) on antioxidation activity and hyperlipidemia induced by hypercholesterolemic diet in mice. The results obtained were as follows : 1. GTE showed a safety in cytotoxicity and toxicity of human fibroblast cells and liver. 2. GTE showed DPPH scavenging activity, superoxide dismutase (SOD)-like activity and inhibitory effect on reactive oxygen species (ROS). 3. GTE treated mice showed body and liver weight decrease, compared to the hyperlipidemia-induced control group. 4. GTE decreased total cholesterol and LDL cholesterol levels significantly, but HDL cholesterol levels not significantly. 5. GTE decreased triglyceride levels significantly. 6. Glucose levels in GTE treated mice significantly decreased compared to the hyperlipidemia-induced control group. 7. Albumin levels in GTE treated mice were similar with the hyperlipidemia-induced control group. 8. The lipophagy in liver compared with the control group tended to be decreased in GTE treated mice. In the change of aorta, the cell was regular and boundary of vessel wall was clear, compared to the hyperlipidemia-induced control group. 9. TBARS levels in GTE treated mice significantly decreased compared to the hyperlipidemia-induced control group. 10. The change of SOD and catalase activity significantly increased compared to the hyperlipidemia-induced control group. 11. ACAT mRNA level and HMG-CoA reductase mRNA levels in GTE treated mice significantly decreased compared to the hyperlipidemia-induced control group. Conclusion : These results suggest that Gangzitongmaekeum is effective in antioxidation activity and dietary hyperlipidemia-induced mice.

  • PDF

Screening of Biologically Active Compound from Edible Plant Sources-IX. Isolation and Identification of Sesquiterpene Lactons Isolated from the Root of Ixeris dentata forma albiflora; Inhibition Effects on ACAT, DGAT and FPTase Activity (식용식물자원으로부터 활성물질의 탐색-IX. 흰씀바귀(Ixeris dentata forma albiflora)뿌리에서 Sesquiterpene Lactone 화합물의 분리 및 구조 동정; ACAT, DGAT 및 FPTase 효소 활성의 저해)

  • Bang, Myun-Ho;Jang, Tae-O;Song, Myoung-Chong;Kim, Dong-Hyun;Kwon, Byoung-Mog;Kim, Young-Kuk;Lee, Hyun-Sun;Chung, In-Sik;Kim, Dae-Keun;Kim, Sung-Hoon;Park, Mi-Hyun;Baek, Nam-In
    • Applied Biological Chemistry
    • /
    • v.47 no.2
    • /
    • pp.251-257
    • /
    • 2004
  • The root of lxeris dentata forma albiflora was extracted with 80% aqueous MeOH and solvent fractionated with EtOAc, n-BuOH and water, successively. From the EtOAc and n-BuOH fractions, four sesquiterpene compounds were isolated through the repeated silica gel and ODS column chromatographies. The chemical structures were determined as zaluzanin C (1), $9{\alpha}-hydroxyguaian-4(l5),10(14),11(13)-triene-6,12-olide$ (2), $3{\beta}-O-{\beta}-D-glucopyranosyl-8{\alpha}-hydroxyguaian-4(15),10(14 )-diene-6,12-olide$ (3), and $3{\beta}-O-{\beta}- D-glucopyranosyl-8{\beta}hydroxyguaian-10(14)-ene-6,12-olide$ (4) through the interpretation of several spectral data including 2D-NMR. Some showed the inhibitory effects on DGAT (Diacylglycerol acyltransferase), ($IC_{50}$ values of 1, 2: 0.13, 0.10 mM), the catalyzing enzymes of the intracellular esterification of diacylglycerol and FPTase (Famesyl-protein transferase), ($IC_{50}$ values of 1, 2: 0.15, 0.18 mM), the farnesylation enzyme for Ras protein charge of cancer promotion.

Plasma Cholesterol-Lowering Effects of Alpiniae katsumadaii Extract as an Inhibiter of Pancreatic Cholesterol Esterase Activity (췌장 콜레스테롤 에스터레이즈 저해제인 초두구 추출물의 혈중 콜레스테롤 저해효과)

  • Kim, Hee-Sook;Kim, Ji-Young;Choi, Jong-Won;Huh, Young-Mi;Suh, Pann-Ghill;Ryu, Sung-Ho
    • Korean Journal of Food Science and Technology
    • /
    • v.32 no.1
    • /
    • pp.200-205
    • /
    • 2000
  • Ethanol extract of Alpiniae Katsumadaii semen inhibited potently cholesterol esterase activity in vitro. Chloroform fraction of ethanol extract showed the stronger inhibitory effect than other solvent fractions-ethylacetate fraction, butanol fraction, and aqueous fraction. The chloroform frac ion of Alpiniae katsumadaii semen were studied as a candidator of plasma cholesterol lowering material in high cholesterol-fed rats. In high cholesterol-fed rats, the diet with chloroform fraction of 100 mg/kg and 150 mg/kg lowered not only plasma neutral lipids contents 25.9% and 26.5% but also plasma total cholesterol level 11.8% and 20.8%, respectively. Plasma HDL-cholesterol level and Atherogenic Index(AI) in Alpiniae chloroform fraction-fed rats were recovered as those level of normal rats.

  • PDF

Triterpenoids from the Fruits of Cornus kousa Burg. as Human Acyl-CoA: Cholesterol Acyltransferase Inhibitors

  • Lee, Dae-Young;Jung, La-Koon;Lyu, Ha-Na;Jeong, Tae-Sook;Lee, Youn-Hyung;Baek, Nam-In
    • Food Science and Biotechnology
    • /
    • v.18 no.1
    • /
    • pp.223-227
    • /
    • 2009
  • The fruits of Cornus kousa Burg. were extracted with 80% aqueous methanol (MeOH) and the concentrated extract was partitioned with ethyl acetate (EtOAc), n-butanol (n-BuOH), and $H_2O$. From the EtOAc traction, 5 triterpenoids were isolated through repeated silica gel ($SiO_2$), octadecyl silica gel (ODS), and Sephadex LH-20 column chromatography (c.c.). These compounds were determined to be ursolic acid (1), corosolic acid (2), taraxasterol (3), betulinic acid (4), and betulinic aldehyde (5) on the basis of their spectroscopic data including electronic ionization mass spectrometry, ultraviolet spectroscopy, infrared spectroscopy, and nuclear magnetic resonance. This is the first reported isolation of these compounds from this plant. Also, compounds 1, 3, 4, and 5 show a relatively high inhibitory activity against human acyl-CoA: cholesterol acyltransferase-1 (hACAT-1) with inhibition values of $52.8{\pm}0.7$, $91.1{\pm}0.4$, $93.0{\pm}0.7$, and $96.2{\pm}0.2%$ at a concentration of $100{\mu}M$, respectively.

Plasma Cholesterol-Lowering Effects of Cinnamomi cortex Extract as an Inhibitor of Pancreatic Cholesterol Esterase (췌장 콜레스테롤 에스터레이즈 저해제로서의 계피 추출물레 혈중 콜레스테롤 농도에 미치는 영향)

  • 김희숙;최종원;허영미;류성호;서판길
    • Journal of Life Science
    • /
    • v.12 no.1
    • /
    • pp.106-112
    • /
    • 2002
  • Ethanol extract of Cinnamomi cortex inhibited potently cholesterol esterase activity in vitro. Chloroform fraction of ethanol extract showed the stronger inhibitory effect than other solvent fractions - ethylacetate fraction, butanol fraction, and aqueous fraction. The chloroform fraction of Cinnamomi cortex was studied as a candidator of plasma cholesterol-lowering material using high cholesterol-fed rats. In high cholesterol-fed rats, the diet with chloroform fraction of 150 mg/kg lowered not only plasma neutral lipids contents 25.1% but also plasma total cholesterol level 49.6% than only high cholesterol diet. Plasma HDL-cholesterol level in Cinnamomi cortex chloroform fraction-fed rats was recovered as those level of normal rats. LD$_{50}$ of Cinnamomi chloroform extract was calculated as 1,300 mg/kg.

Biofunctional Activities of Citrus Flavonoids (감귤류 플라보노이드의 생리기능 활성)

  • Cha, Jae-Young;Cho, Young-Su
    • Applied Biological Chemistry
    • /
    • v.44 no.2
    • /
    • pp.122-128
    • /
    • 2001
  • This review showed a discussion on the biofunctional activities of citrus flavonoids. The major flavonoids of citrus species, hesperidin, hesperetin, naringin, and naringenin, were selected to evaluate their biological effects on the lipid metabolism in rats and hamsters, the proliferation of human hepatocyte HepG2 cells, and the antioxidative effect in lipid peroxidation models. These flavonoids showed hypotriglyceridemic effect in hamsters and hypochloesterolemic effect in rats. They also significantly inhibited the activities of phosphatidate phophohydrolase and acyl-CoA: cholesterol acyltransferase, which are key enzymes for biosynthesis of triglyceride and cholesterol, repectively, in vivo and in vitro experiments. These biofunctional activities by citrus flavonoids were shown more potent in the aglycone flavonoids, hespreretin and naringenin, than their corresponding glycoside flavonoids, hesperidin and naringin. These aglycone flavonoids also have inhibitory effects on proliferation of human hepatocyte cancer HepG2 cells. Hesperidin showed lowering activities of cellular triglyceride and cholesterol concentrations in HepG2 cells. Citrus flavonoids have significant importance in functional food industry as biofunctional active ingredients.

  • PDF