30170-00-4Relevant academic research and scientific papers
GUGGULPHOSPHOLIPID METHODS AND COMPOSITIONS
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Page/Page column 54, (2008/12/05)
The present invention relates to the methods for preparing synthetic guggulphospholipids, their fatty acid analogues and other bioactive molecules. The present invention relates to E-guggulsterone and Z-guggulsterone or mixture of E- and Z-guggulsterones; and E-guggulsterol and Z-guggulsterol or mixture of E- and Z-guggulsterols synthetically modified to guggulphospholipids and analogues and salts thereof, fatty acid analogues of guggulsterols, guggulsulfate and salts thereof, guggulphosphate and salts thereof; and guggulsterols conjugated with drugs for use as prodrugs. Also the present invention provides a novel method for the preparation of E-guggulsterol and Z-guggulsterol or mixture of E-and Z-guggulsterols from a mixture of E- and Z-guggulsterones. The present invention further relates to guggulphospholipids and other bioactive molecules incorporated into complexes such as liposomes, complexes, emulsions, vesicles, micelles, and mixed micelles, which can include other active agents, such as hydrophobic or hydrophilic drugs for use, e.g., in treatment of human and animal diseases.
Total synthesis of perdeuterated phospholipids
Bersch, B.,Starck, J. P.,Milon, A.,Nakatani, Y.,Ourisson, G.
, p. 575 - 583 (2007/10/02)
A general method for the total synthesis of various perdeuterated phospholipids (DMPA, DMPG, DMPE, DMPC) is described.Starting from simple and easily obtainable deuterated precursors, perdeuterated phosphatidic acid (DMPA-d59) was synthesized.DMPA-d59 was coupled to various perdeuterated alcohols in the presence of alkylsulfonyl chlorides as condensing agents.The preparation of the perdeuterated alcohols is also presented.The major advantage of this method lies in the independent synthesis of DMPA and the alcohol moieties, allowing the transformation to the desired phospholipid class in the final reaction step.The reaction scheme presented here can also be used for the synthesis of selectively deuterated phospholipids.Keywords - perdeuterated phospholipids / phosphatidic acid-d59 / phosphatidylglycerol-d64 / phosphatidylcholine-d72 / phopshatidylethanolamine-d63 / total synthesis
