Novel furanic labdane diterpene compounds from Vitex rotundifolia L. fruit process for extraction and Acyl-CoA cholesterol acyltransferase inhibitors including thereof

PURPOSE: A composition containing rotundifuran and 6-epi-rotundifuran as a furanic labdane diterpene compound extracted from a fruit of Vitex rotundifolia Linne fil. is provided. Because the rotundifuran and 6-epi-rotundifuran specifically inhibits ACAT, it is effective in lowering blood cholesterol...

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Hauptverfasser: KIM, MI GYEONG, NOH, MUN CHEOL, SONG, HYE YEONG, LEE, HYEON SEON, LEE, SEUNG UNG, KIM, YEONG GUK
Format: Patent
Sprache:eng ; kor
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Zusammenfassung:PURPOSE: A composition containing rotundifuran and 6-epi-rotundifuran as a furanic labdane diterpene compound extracted from a fruit of Vitex rotundifolia Linne fil. is provided. Because the rotundifuran and 6-epi-rotundifuran specifically inhibits ACAT, it is effective in lowering blood cholesterol level and can be effectively used in prevention and treatment of cardiovascular disease caused by hypercholesterolemia. CONSTITUTION: ACAT(acyl-CoA:cholesterol acyltransferase) activity inhibitor contains a furanic labdane diterpene compound such as rotundifuran of formula(1) or 6-epi-rotundifuran of formula(2). The fruit of Vitex rotundifolia Linne fil. is soaked in methyl alcohol at room temperature for 3 days and concentrated under reduced pressure to produce a crude extract. The crude extract is fractioned with n-hexane, chloroform, ethyl acetate and water to concentrate a n-hexane layer and then separated by chromatography. 본 발명은 ACAT의 활성을 저해하는 퓨란성 랍단 디테르펜 화합물 및 이의 조성물에 관한 것으로서, 더욱 상세하게는 특이적으로 아실-코에이:콜레스테롤 아실트랜스퍼라제(Acyl-CoA:Cholesterol Acyltransferase, ACAT)를 저해하여 고콜레스테롤혈증에 기인하는 고지혈증, 동맥경화 등의 심혈관 질환 예방과 치료에 유용하게 사용할 수 있는 퓨란성 랍단 디테르펜(furanic labdane diterpene) 계열의 화합물인 로텐디퓨란(Rotundifuran)과 6-에피-로텐디퓨란(6-epi-rotundifuran), 이를 함유하는 조성물 및 순비기나무(L.)의 열매인 만형자(蔓荊子)로부터 퓨란성 랍단 디테르펜 화합물을 분리하는 방법에 관한 것이다.