31 results about "Lysophosphatidyl choline" patented technology

A novel class of compounds to inactivate autotaxin enzymes is provided. Such compounds include mono- and di-fluoromethylphenyl C12-C18 phosphodiesters and exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds are non-cytotoxic, and can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of producing such novel compounds are encompassed within this invention as well as methods of inactivating autotaxin to certain degrees therewith.

Novel and optimized classes of pipemidic acid derivative compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes of compounds exhibit exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.

The invention discloses a metabolism marker for diagnosis of the acute coronary syndrome. The metabolism marker comprises one or more of phosphorylcholine, palmitoylethanolamine, lysophosphatidyl choline (16:0), phosphatidyl ceramide (d18:1 / 8:0), lysophosphatidyl choline (18:2), lysophosphatidyl choline (18:1) and phosphatidylinositol (18:3 / 0:0). When a single metabolism marker is used for diagnosis and distinguishing of acute coronary syndrome patients and coronary artery normal people, ROC area under the curve (AUC) is larger than 0.7 all the time, and clinical diagnosis significance is high; when several metabolism markers are combined to be used for diagnosis, AUC is further increased as the combination number increases and reaches the highest value 0.987 when all the seven metabolism markers are combined, and sensitivity and specificity are 99.1% and 98.9% respectively under the optimum cutoff value. The metabolism marker can be used for accurate diagnosis of the acute coronary syndrome and has high accuracy, sensitivity and specificity.

The invention discloses a method for preparing lysophosphatidyl choline by enzymatic alcoholysis, which comprises: adding phosphatidylcholine into low-carbon alcohol solution, uniformly stirring and mixing at a certain temperature, adding lipase, and allowing the lipase to catalyze the alcoholysis of phosphatidylcholine with constant-temperature stirring to obtain the lysophosphatidyl choline. The method has the advantages that: (1) the solubility of phosphatidylcholine, lysophosphatidyl choline serving as the product, and aliphatic ester, glycerophosphorylcholine and very small amount of fatty acid, which serve as byproducts, in the reaction system is improved, and the conversion rate of the lysophosphatidyl choline is high; (2) the aliphatic ester, a small amount of glycerophosphate and a very small amount of fatty acid are generated in an alcoholysis reaction process, but the pH value of the system is not changed, and the influence of the solvent on the activity of the lipase is relieved and the catalytic reaction activity of the lipase is high; (3) the properties of the fatty acid, the aliphatic ester and glycerophosphorylcholine, which are products of side reactions, are very different from those of the lysophosphatidyl choline, so the lysophosphatidyl choline product can be separated and purified very easily; and (4) the alcohol, which is the product of the reaction, can be removed easily.

The invention discloses an application of endogenous small molecular substances to rapid detection of early cardiotoxicity, wherein the endogenous small molecular substances refers to nine early cardiotoxicity biomarkers: L-carnitine, L-tryptophan, L-palmitoyl carnitine, 19-hydroxyl deoxycorticosterone, cholic acid, lysophosphatidyl choline (14: 0), lysophosphatidyl choline (22: 6), lysophosphatidyl choline (20: 2) and lysophosphatidyl choline (16: 0), and also refers to four early cardiotoxicity exclusive biomarkers: L-carnitine, 19-hydroxyl deoxycorticosterone, lysophosphatidyl choline (14: 0) and lysophosphatidyl choline (20: 2). According to the application of the endogenous small molecular substances to the rapid detection of the early cardiotoxicity, the screened early cardiotoxicity biomarkers are capable of giving rapid alarms to the toxicity before the heart tissues suffer pathological damages, so that the toxicity discovery time is early than the conventional biochemical detection indexes, more flexible judgement is carried out on the drug toxicity and diseases, and more time is provided for the early discovery and early treatment of the clinic cardiotoxicity.

The invention discloses a pancreatic ductal adenocarcinoma marker and a screening method thereof, which belongs to the field of clinical test and diagnosis. In view of the problem that the detection sensitivity and the detection specificity of the existing pancreatic ductal adenocarcinoma diagnosis marker are poor, serum of an early patient of early stage pancreatic duct adenocarcinoma is subjected to a trace metabolomics analysis by the high-performance liquid chromatography-tandem mass spectrometry technology, and different metabolites between normal human and the early stage pancreatic ductal adenocarcinoma patients are found. The different metabolites between normal human and pancreatic ductal adenocarcinoma patients are further analyzed by this technique to find the specific differentmetabolites C10:1 acyl carnitine and lysophosphatidyl choline LysoPC (14:0) of pancreatic ductal adenocarcinoma patients caused by cancer, i.e., the diagnostic molecules of the pancreatic ductal adenocarcinoma. According to the pancreatic ductal adenocarcinoma marker and the screening method thereof, the method can assist CA19-9 in diagnosing pancreatic duct adenocarcinoma patients, and can improve the diagnosis rate for the CA19-9 negative patients by 85%. The method is suitable for the screening of tumor markers.

The invention discloses a group of plasma metabolism micromolecular markers related to lung cancer early diagnosis and an application thereof. The plasma metabolism micromolecular markers comprise oneor more of the following markers: propionic acid, aspartic acid, furan glucoside, citric acid, allose, talose, galactopyranose, pyruvic acid, tryptophan, leucyl proline, glyceryl phosphoryl choline,oleoyl carnitine, lysophosphatidyl choline (18:3), lysophosphatidyl choline (18:2), lysophosphatidyl choline (18:1), lysophosphatidyl choline (22:6), lysophosphatidyl ethanolamine (20:0), lysophosphatidyl ethanolamine (18:2), and complex aminoacyl valine. Compared with the traditional protein biomarkers, the group of the provided markers has the stronger outcome relevance with diseases, and is stable, minimally invasive, and easy to detect, capable of greatly improving the sensitivity and the specificity of the related disease diagnosis, and suitable for the early clinical diagnosis and monitoring of lung cancer.

The invention discloses a medicament for treating tumors. The medicament consists of a histone deacetylase inhibitor and a lysophosphatidic acid suppressant, wherein the lysophosphatidic acid suppressant is a substance for inhibiting lysophosphatidic acid from bonding with a lysophosphatidic acid receptor or a substance for inhibiting the lysophosphatidic acid from generating. The medicament indicates that the histone deacetylase inhibitor (HDACi) can up-regulate autotaxin (ATX) expression by inhibiting the activity of HDAC3 and HDAC7 in multiple tumor cells. The ATX generated by the induction of the HDACi generates the lysophosphatidic acid (LPA) by catalyzing lysophosphatidyl choline (LPC) and weakens the killing effect of the HDACi on the tumor cells. If the ATX expression is inhibitedby a ribonucleic acid interference (RNAi) method or bromophosphonate-lysophosphatidic acid (BrP-LPA) serving as an ATX-LPA signal channel inhibitor is added to block an ATX-LPA signal, the killing effect of the HDACi on the tumor cells can be enhanced further. The study of the invention provides a new concept for treating the tumors by combing the lysophosphatidic acid suppressant and the HDACi. The medicament has wide application prospects in the treatment of the tumors.

The invention discloses a preparation method for polyene phosphatidyl choline for injection. The preparation method comprises the following steps: dissolving with a proper solvent by taking soyabean lecithin as a raw material, performing elution twice with a ternary mixed solvent consisting of multi-halogenated hydrocarbon, low carbon alcohol and water through column chromatography, and drying to obtain a product polyene phosphatidyl choline. The product obtained by the preparation method disclosed by the invention is high in phosphatidylcholine content (98.0%-99.9%, HPLC (high performance liquid chromatography) process), low in impurity content (less than 1.0% of lysophosphatidyl choline, less than 0.5% of phosphatidyl inositol, less than 0.5% of phosphatidyl ethanolamine, less than 0.2% of free fatty acid and less than 0.2% of triglyceride), and low in oxidative index (an acid value lower than 0.5, a peroxide value lower than 1.0 and methoxy phenylamine value lower than 5.0), so that the product quality reaches the quality standards of polyene phosphatidyl choline for injection.