📜乙酰紫草素置于4-二甲氨基吡啶,Sodium Hydroxide,1-(3-二甲基氨基丙基)-3-乙基碳二亚胺体系中,用 甲醇,二氯甲烷 作为反应溶剂,化学反应生成 异戊酰紫草素
参考文献:Human Acat Inhibitory Effects Of Shikonin Derivatives From Lithospermum Erythrorhizon
标题:Human Acat Inhibitory Effects Of Shikonin Derivatives From Lithospermum Erythrorhizon
摘要:Three Naphthoquinones Were Isolated By Bioassay-Guided Fractionation From The Chcl3 Extracts Of Roots Of Lithospermum Erythrorhizon. They Were Identified As Acetylshikonin (1),Isobutyrylshikonin (2),And (3-Hydroxyisovalerylshikonin (3) On The Basis Of Their Spectroscopic Analyses. The Compounds 1-3 Were Tested For Their Inhibitory Activities Against Human Acat-1 (Hacat-1) Or Human Acat-2 (Hacat-2). Compound 2 Preferentially Inhibited Hacat-2 (Ic50 = 57.5 Wm) Than Hacat-1 (32% At 120 Mu M),Whereas Compounds 1 And 3 Showed Weak Inhibitory Activities In Both Hacat-1 And-2. To Develop More Potent Hacat Inhibitor,Shikonin Derivatives (5-11) Were Synthesized By Semi-Synthesis Of Shikonin (4),Which Was Prepared By Hydrolysis Of 1-3. Among Them,Compounds 5 And 7 Exhibited The Strong Inhibitory Activities Against Hacat-1 And-2. Furthermore,We Demonstrated That Compound 7 Behaved As A Potent Acat Inhibitor In Not Only In Vitro Assay System But Also Cell-Based Assay System. (C) 2006 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2006.11.024