• 생명과학회지
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• 제12권1호
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• pp.106-112
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• 2002

췌장에서 분비되는 콜레스테롤 에스터레이즈(pCEase)와 소장의 acyl coenzyme A:cholesterol acyltransferase (ACAT)는 흡수된 콜레스테롤을 다시 ester화하는데 관여한다. 한방재료 중 순환촉진작용 및 건위작용 등을 가지는 계피(Cinnamomi cortex)의 에탄올 추출물이 in vitro에서 pCEase 활성에 대하여 강한 저해작용을 보였으며 에탄올 추출물의 용매분획 중 클로로포름분획이 다른 분획들, 즉 에틸 아세테이트분획, 부탄올분획 및 물 분획보다 저해활성이 강하였다. 계피의 클로로포름분획이 고콜레스테롤식 이를 섭취시킨 rat에서 혈중 콜레스테롤치를 저하시키는 효과가 있는지 측정한 실험에서 클로로포름분획을 150 mg/kg 섭취시켰을 경우 고콜레스테롤식이만은 투여한 대조군에 비하여 총cholesterol 함량이 25.1% 감소하였으며, HDL-cholesterol 함량도 33.4$\pm$1.82 g/dl로 정상군 수준으로 회복되었고 동맥경화지수 역시 현저하게 감소된 것으로 나타났다. 콜레스테롤 생합성에 관여하는 효소인 HMG-CoA reductase 활성을 측정한 결과, 고콜레스테롤 식이에 의해 감소되었던 활성이 계피 클로로포름분획의 투여량을 증가시킬수록 증가하였으나 150 mg/kg 투여군 에서도 정상군에 비하여 유의적인 감소를 보였다. 또한 계피 클로로포름분획의 독성검사 결과, mouse에서 LD$_{50}$ 은 1,300 mg/kg으로 산출되었다.

• Food Science and Biotechnology
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• 제18권1호
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• pp.95-102
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• 2009

The aerial parts of garland (Chrysanthemum coronarium L.) were extracted in 80% aqueous methanol (MeOH) and the concentrated extract was then partitioned using ethyl acetate (EtOAc), n-butanol (n-BuOH), and $H_2O$, successively. EtOAc and n-BuOH fractions resulted in 4 glycerides with the application of octadecyl silica gel and silica gel column chromatography. The chemical structures of the glycerides were determined using several spectroscopic methods, including nuclear magnetic resonance (NMR) and mass spectrometry (MS) as (2S)-1-O-palmitoyl-sn-glycerol (1), (2S)-1-O-oleoyl-2-O-oleoyl- 3-O-$\beta$-D-galactopyranosyl-sn-glycerol (2), (2S)-1-O-palmitoyl-2-O-linoleoyl-3-O-phosphorouscholine-sn-glycerol (3), and (2S)-1-O-linolenoyl-2-O-palmitoyl-3-O-[$\alpha$-D-galactopyrasyl-($1{\rightarrow}6$)-$\beta$-D-galactopyranosyl]-sn-glycerol (4). The free fatty acids of these glycerides were determined with gas chromatography (GC)-MS analysis following alkaline hydrolysis and methylation. These glycerides demonstrated an inhibitory effect on acyl-CoA: cholesterol acyltransferase (ACAT, compound 1: $45.6{\pm}0.2%$ at $100{\mu}g/mL$), diacylglycerol acyltransferase (DGAT, compound 1: $59.1{\pm}0.1%$ at $25{\mu}g/mL$), farnesyl protein transferase (FPTase, compound 2: $98.0{\pm}0.1%$; compound 3: $55.2{\pm}0.1%$ at $100{\mu}g/mL$), and $\beta$-secretase ($IC_{50}$, compound 4: $2.6{\mu}g/mL$) activity. This paper is the first report on the isolation of these glycerides from garland and their inhibitory activity on ACAT, DGAT, FPTase, and $\beta$-secretase.

• 한국식품과학회지
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• 제32권1호
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• pp.200-205
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• 2000

췌장에서 분비되는 cholesterol esterase(CEase)와 소장의 acyl coenzyme A: cholesterol acyltransferase(ACAT)는 흡수된 콜레스테롤을 다시 ester화하는데 관여한다. 한방재료 중 건위, 진토 및 수렴지사작용 등을 가지는 초두구(Alpiniae Katusumadaii Semen)의 에탄올 추출물이 in vitro에서 cholesterol esterase활성에 대하여 강한 저해작용을 보였으며 에탄올추출물의 용매분획 중 클로로포름분획이 다른 분획들, 즉 에틸 아세테이트분획, 부탄올분획 및 물 분획보다 강하였다. 초두구의 클로로포름분획이 고 콜레스테롤식이를 섭취시킨 rat에서 혈중 콜레스테롤치를 저하시키는 효과가 있는지 측정한 실험에서 chloroform분획을 100 mg/kg 및 150 mg/kg 섭취시켰을 경우 각각 총cholesterol 함량이 11.8% 및 20.8% 감소하였으며 HDL-cholesterol 함량 및 동맥경화지수는 정상군에 가깝게 회복된 것으로 나타났다. 또한 초두구 chloroform분획의 독성검사 결과 mouse에서 $LD_{50}$은 1,625mg/kg으로 산출되었다.

• 대한임상검사과학회지
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• 제48권4호
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• pp.280-286
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• 2016

폴리페놀 성분은 심혈관질환에서 좋은 효과를 나타낸다고 보고되고 있다. 폴리페놀성 화합물인 3,4-다이하이드록시 하이드로시나믹산은 항산화 활성과 항암 활성을 나타낸다고 보고되었다. 이 연구의 목적은 3,4-다이하이드록시 하이드로시나믹산이 항동맥 경화 효과를 나타내는지를 뉴질랜드 흰 토끼에서 평가하는 것이다. 8주동안 고콜레스테롤 식이를 급여한 대조그룹 토끼의 광범위한 동맥 부위에서 동맥경화 초기병변이 형성되었다. 반면에 고콜레스테롤 식이를 급여하면서 3,4-다이하이드록시 하이드로시나믹산을 투여한 토끼에서는 대조 그룹의 토끼에 비해 동맥경화 병변 형성이 감소하였고, 병변 내로 침윤한 대식세포의 양도 감소하였다. 이러한 3,4-다이하이드록시 하이드로시나믹산의 효과에서 전신적으로나 국부적으로 독성이 관찰되지 않았다. 간의 아실-코엔자임 A: 콜레스테롤 아실트렌스페라제 활성이 고콜레스테롤 식이를 급여하면서 3,4-다이하이드록시 하이드로시나믹산을 투여한 토끼에서 대조 그룹의 토끼에 비해 22% 감소하였다. 이러한 연구 결과는 3,4-다이하이드록시 하이드로시나믹산이 토끼에서 아실-코엔자임 A: 콜레스테롤 아실트렌스페라제를 억제함으로써 항동맥경화 효과를 나타낸다는 것을 증명해 준다.

• Bulletin of the Korean Chemical Society
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• 제29권3호
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• pp.615-619
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• 2008

Eight triterpenoids, six lanostanes 1-6, one lupenane 7, and one oleanane 8, were isolated by bioactivity-guided fractionation of the ethylacetate extract from roots of Glycine max (L.) Merr. All isolated compounds were examined for their inhibitory activities against human ACAT-1 (hACAT-1) and human ACAT-2 (hACAT-2). Among them, three triterpenoids showed potent hACAT inhibitory activities, (24R)-ethylcholest-5-ene-3,7-diol (1) and 3b -hydroxylup-20(29)-en-28-oic acid (7) exhibited more potent inhibitory activity against hACAT-1 (1: IC50 = 25.0 1.2 and 7: IC50 = 11.5 0.4 m M) than hACAT-2 (1: IC50 = 102.0 5.4 and 7: IC50 = 33.9 3.7 m M), respectively. Interestingly, 5a ,8a -epidioxy-24(R)-methylcholesta-6,22-diene-3b -ol (4) has proven to be a specific inhibitor against hACAT-1 (IC50 = 38.7 0.8 m M) compared to hACAT-2 (IC50 >200). In conclusion, this is the first study to demonstrate that triterpenoids of G. max have potent inhibitory activities against hACAT-1 and hACAT-2.

• Preventive Nutrition and Food Science
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• 제5권2호
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• pp.109-113
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• 2000

In this study, a potential mechanism through which the hesperidin might work on the effect was examined in vivo. Male rats were fed a high cholesterol synthetic diet (1%, wt/wt) with hesperidin (0.1%, wt/wt) for 42 days. Activity of hepatic HMG-CoA reductase was significantly lowered by the hesperidin supplement compared to the control. Hesperidin did not significantly alter plasma or hepatic lipids, but tended to lower those lipid levels. Hesperidin also subsequently reduced the fecal neutral sterols compared to the control(253.3mg/d vs.521.9 mg/d). The inhibition of HMG-CoA reductase resulting from the hesperidin supplementation could count for the reduction in fecal neutral sterols that appears to compensate for the decreased cholesterol biosynthesis. The dose of hesperidin in a high choles-terol diet should apparently be more than 0.1% to exhibit the hypocholesterolemic response in these rats. It remains to be determined whether the observed alterations in cholesterol metabolism are specific to the rat or also could be applied to the humans.

• Bulletin of the Korean Chemical Society
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• 제29권11호
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• pp.2287-2290
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• 2008

• Journal of Plant Biotechnology
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• 제29권1호
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• pp.63-68
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• 2002

상추의 기내 callus 배양으로부터 ACAT (Acyl-CoA: Cholesterol acyltransferase) 억제 활성물질로 알려진 phytol 의 생산가능성이 연구되었다. Callus는 0.5mg.L$^{-1}$ NAA가 첨가된 MS 배지에 4주간 치상된 자엽 절편체로부터 유도되었으며, 다양한 수준의 chlorophyll을 함유하고 있었다. Phytol이 chlorophyll분자를 구성하는 물질로 알려져 있음에 도 불구하고, phytol의 추출량은 녹색의 자엽에서 보다 callus 에서 높게 나타났다. GC 분석결과, phytol의 추출량은 callus의 chlorophyll 함량과 비례하지 않는 것으로 나타났으며, callus의 chlorophyll 함량수준은 callus의 형성능과 관련이 있는 것으로 사료되었다. 본 연구의 결과는 phytol의 기내생산에 있어서 상추의 callus 배양의 잠재성을 제시한다 하겠다.

• 대한본초학회지
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• 제20권2호
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• pp.91-102
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• 2005

Objectives : By examining the effects of Jwa Kum-Whan composed of Coptidis Rhizoma and Evodiae Fructus by the ratio of 6:1 the effects of Soo Ryeon-Whan and composed of Coptidis Rhizoma and Evodiae Fructus by the ratio of 1:1 on hyperlipidemia, the present study attempted to reveal the change of effects based on the ratio of combination. Methods : Jwa Kum-Whan and Soo Ryeon-Whan were injected to rats suffered from induced hyperlipidemia, and then its influence on lipid. During the cultivation of hepatocytes, Jwa Kum-Whan and Soo Ryeon-Whan were added to culture media, and the expression of the enzymes relevant to fat metabolism of hepatocytes was examined. Results : 1. Jwa Kum-Whan significantly decreased total cholesterol(Tc), triglyceride(TG), and LDL-cholesterol(LDLc) of rats suffering from hyperlipidemia induced by high cholesterol diet. Soo Ryeon-Whan decreased LDLc, but had no significant on Tc and TG. 2. Jwa Kum-Whan increased the expression of cholesterol esterase, LDL-receptor, diacylglycerol acyltransferase (DGAT), acylCoA-cholesterol-acyltransferase (ACAT), peroxisome proliferator activated receptor gamma $(PPAR{\gamma})$, peroxisome proliferator activated receptor alpha $(PPAR{\alpha})$ of cultivated hepatocytes. In addition, Soo Ryeon-Whan increased the expression of cholesterol esterase, LDL-Receptor, DGAT, $PPAR{\gamma},\;PPAR{\alpha}$ of cultivated hepatocytes, but had no significant effects on the expression of ACAT. Conclusion : Both Jwa Kum-Whan and Soo Ryeon-Whan were composed of Coptidis Rhizoma and Evodiae Fructus, but the fonner is more effective in hyperlipidemia.

• Nutrition Research and Practice
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• 제8권6호
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• pp.632-637
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• 2014

BACKGROUND/OBJECTIVES: The purpose of the current study was to investigate the effect of red pericarp glutinous rice rich in polyphenols (Jakwangchalbyeo, red rice) on serum and hepatic levels of cholesterol and hepatic protein expression linked to synthesis and degradation of cholesterol in a hypercholesterolemic mice diet as compared with brown rice. MATERIALS/METHODS: C57BL/6 male mice were randomly divided into four groups (n = 5 each), which were fed different diets for a period of 12 weeks: American Institute of Nutrition (AIN)-93G diet, AIN-93G diet with 2% cholesterol, brown rice with 2% cholesterol, or red rice with 2% cholesterol. RESULT: Consumption of red rice resulted in a significant decrease in serum level of low-density lipoprotein cholesterol and hepatic levels of triglyceride and total-cholesterol. Expression of acyl-coenzyme A cholesterol acyltransferase-2 (ACAT-2), sterol regulatory element binding protein-2 (SREBP-2), and 3-hydroxyl-3-methylglutaryl coenzyme A (HMG-CoA) reductase was decreased, while expression of phosphorylated adenosine monophosphate activated protein kinase (p-AMPK)/AMPK ratio, cholesterol 7-${\alpha}$-hydroxylase (CYP7a1), and sterol 12-${\alpha}$-hydroxylase (CYP8b1) was increased in mice fed red rice. Brown rice had similar effects on cholesterol metabolism, but the effect of red rice was significantly greater than that of brown rice. CONCLUSIONS: The current study suggested that red rice had a hypocholesterolemic effect by lowering hepatic cholesterol synthesis through ACAT-2, HMG-CoA reductase, and SREBP-2, and by enhancing hepatic cholesterol degradation through CYP7a1 and CYP8b1 in mice fed a hypercholesterolemic diet.