THE HALICYLINDRAMIDE EXTRACTED HALICHONDRIA SP., AND A MEDICINE CONTAINING THE SAME

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.