Korean Journal of Pharmacognosy (생약학회지)

The Korean Society of Pharmacognosy (한국생약학회)
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Screening of Acyl-CoA:Cholesterol Acyltransferase(ACAT) Inhibitors from Natural Sources

천연자원으로부터 아실코에이: 콜레스테롤아실 전달효소 저해제의 탐색

  • Kim, Mi-Kyung (Cardiovascular Research Laboratory Korea Research Institute of Bioscience & Biotechnology) ;
  • Kwon, Byoung-Mog (Antibiotics Research Laboratory Korea Research Institute of Bioscience & Biotechnology) ;
  • Bae, Ki-Hwan (College of Pharmacy, Chungnam National University) ;
  • Choi, Don-Ha (Lab. of Natural Products Chemistry, Forestry Research Institute) ;
  • Lee, Hak-Ju (Lab. of Natural Products Chemistry, Forestry Research Institute) ;
  • Kim, Hong-Eun (College of Agriculture, Chungbuk National University) ;
  • Kim, Young-Kook (Cardiovascular Research Laboratory Korea Research Institute of Bioscience & Biotechnology)
  • 김미경 (생명공학연구소 항순환기질환물질연구실) ;
  • 권병목 (생명공학연구소 항생물질연구실) ;
  • 배기환 (충남대학교 약학대학) ;
  • 최돈하 (임업연구소 천연물화학연구실) ;
  • 이학주 (임업연구소 천연물화학연구실) ;
  • 김홍은 (충북대학교 농과대학) ;
  • 김영국 (생명공학연구소 항순환기질환물질연구실)
  • Published : 1999.12.30
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Abstract

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 $100\;{\mu}g/ml$.

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