Jina Pharmaceuticals Inc., 28100 N. Ashley Circle, Libertyville, IL 60048, USA.
Chem Phys Lipids. 2010 May;163(4-5):362-6. doi: 10.1016/j.chemphyslip.2010.02.004. Epub 2010 Feb 25.
Two guggullipid derivatives, Z-guggulsulfate [4,17(20)-pregnadiene-3-one-16beta-sulfate] sodium salt and Z-guggullaurate [4,17(20)-pregnadiene-3-one-16beta-laurate], have been synthesized and evaluated for liposomal drug delivery system. Its precursor, Z-guggulsterol [4,17(20)-pregnadiene-3-one-16beta-ol], is also synthesized in gram scale starting from guggulsterone using the novel combination of known reactions in fewer steps and with higher yield than previously reported synthesis. These new synthetic guggullipid derivatives were also used in the preparation of liposomes. This new class of lipid molecules will be a useful tool in the development of nanosomal or liposomal drug delivery system.
两种古柯脂衍生物，Z-古柯脂硫酸盐[4,17(20)-孕二烯-3-酮-16β-硫酸盐]钠盐和 Z-古柯脂月桂酸酯[4,17(20)-孕二烯-3-酮-16β-月桂酸酯]，已被合成并评估用于脂质体药物传递系统。其前体 Z-古柯甾醇[4,17(20)-孕二烯-3-酮-16β-醇]也从古柯甾酮开始，以克为单位规模合成，使用新的已知反应组合，步骤更少，收率高于以前报道的合成。这些新的合成古柯脂衍生物也用于制备脂质体。这种新型脂质分子将成为纳米或脂质体药物传递系统开发的有用工具。
