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THE HALICYLINDRAMIDE EXTRACTED HALICHONDRIA SP., AND A MEDICINE CONTAINING THE SAME
专利权人:
发明人:
강헌중,최혁재,주문경
申请号:
KR1020050008588
公开号:
KR1012136570000B1
申请日:
2005.01.31
申请国别(地区):
KR
年份:
2012
代理人:
摘要:
In the present invention, among the halycillinamides (Halicylindramide) extracted from sponges of Halichondria ( Halichondria sp.), Its halycillin dramide A, halycillin dramide C and halycillin dramide F is a low-density lipoprotein (human) Antagonism of Farnesoid X Receptor (FXR), which is known to effectively lower LDL (low density lipoprotein) and cholesterol levels, and raises high density lipoprotein (HDL) and contains it as an active ingredient It relates to a hyperlipidemia treatment. To extract the material, the sponges halicondria are lyophilized to completely remove moisture, extracted with dichloromethane and methanol, and the solvent is evaporated under reduced pressure. The solvent is removed under reduced pressure from the methanol layer obtained by partition extraction of the residue into methanol and n-hexane. The residue is partitioned and extracted again with ethyl acetate and water, and the aqueous layer obtained is partitioned and extracted with n-butanol. After removal of the solvent of the n-butanol layer thus obtained under reduced pressure, the residue can be purified by resin column chromatography and two reverse phase semi-preparative HPLC to obtain the above substances.The halycillin dramide A and the halycillin dramide C and the novel marine natural halycillin dramide F isolated by the above method have excellent inhibitory activity against the panesoid orphan nuclear receptor involved in cholesterol metabolism, and have low cytotoxicity. see.본 발명은 해면동물 할리콘드리아(Halichondria sp.)로부터 추출된 할리실린드라마이드(Halicylindramide) 중, 그의 할리실린드라마이드 A, 할리실린드라마이드 C 및 할리실린드라마이드 F는 인간의 저밀도 지방단백질(LDL; low density lipoprotein) 및 콜레스테롤 수치를 효과적으로 낮추고, 고밀도 지방단백질(HDL; high density lipoprotein)을 높이는 것으로 알려진 파네소이드 고아 핵 수용체(FXR; Farnesoid X Receptor)의 길항작용과 이를 유효성분으로 함유하는 고지혈증 치료제에 관한 것이다. 상기 물질을 추출하기 위해서 해면동물 할리콘드리아를 동결 건조하여 수분을 완전히 제거하고, 디클로로메탄과 메탄올로 추출한 다음, 이 용매를 감압하에서 증발시킨다. 그 잔류물을 메탄올과 n-헥산으로 분배 추출하여 얻어진 메탄올층에서 용매를 감압하에 제거시킨다. 그 잔류물을 다시 에틸아세테이트와 물로 분배 추출하고, 여기서 얻어진 수
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