A COMPOSITION COMPRISING SYNTHETIC PROTOBIOSIDE DERIVATIVES THAT EXHIBIT THE HYPOLIPIDEMIC PROPERTIES
Creators: name: Alkoclar, Erdal Can
Publisher: name: Zenodo
Year: 2020
Subjects: Protobioside CYP17A1 Cholesteryl Ester Hydrolase

description: The invention relates to a composition formed for exhibiting hypolipidemic character. <strong>State of the Art</strong> Hypolipidemics are various types of medications used as the lipid-lowering agents in the treatment of the elevated lipid levels in the blood. They are also referred to as hypolipidemic drugs or antihyperlipidemic drugs. The lipid lowering medications may be categorized into several classes. They differ in terms of side effects and their actions on the cholesterol profile. Some reduce LDL cholesterol known as “bad cholesterol”, while others increase HDL cholesterol known as “good cholesterol”. In clinical use, the patient’s cholesterol level, cardiovascular risk status and the liver and kidney functions are checked in order to determine which drug the patient is to take, and these are assessed along with the risks and the benefits of the drug. According to the state of the art, the invention no. TR1998/00444 with classification "C07H 17/00" entitled "Hypolipidemic 1,4-benzothiazepine-1,1-dioxides" relates to novel hypolipidemic compositions, novel processes and novel intermediate compounds for preparing the same, pharmacological compositions comprising the same and the uses of the same in medicine, particularly for the prophylaxis and treatment of the hyperlipidemic stares such atherosclerosis. The compounds of the formula (I) wherein R1 through R10 and X are as defined herein. Further, the invention no. WO 2000/020410 entitled "Propanolamine derivatives substituted with heterocyclic compounds, their production, medicaments, use" relates to heterocyclically substituted propanolamine derivatives and their pharmaceutically acceptable salts and functional derivatives. The invention describes compounds of formula (I), wherein the radicals have the meanings thus cited, as well as their physiologically acceptable salts, physiologically functional derivatives and methods for the production thereof. The compounds are suitable as, for example, hypolipidemic agents. Further, the invention no. EP1414439B1 entitled "Novel pyrroles having hypolipidemic hypocholesteremic activities, process for their preparation and pharmaceutical compositions containing them and their use in medicine" provides methods for the preparation of the novel compounds defined in the general formula (I), their tautomeric forms, their derivatives, their analogs, their stereoisomers, their pharmaceutically acceptable salts and their pharmaceutically acceptable solvates. This invention also relates to the process for preparing such compounds, a composition containing such a compound and the use of such a compound and composition in medicine. The compounds lower the triglyceride levels in the blood and may be useful in the treatment of obesity, hyperlipidemia, hypercholesteremia, syndrome X and diabetes. As a result, the presence of the need for a composition for exhibiting hypolipidemic character and the inadequacy of the existing solutions have made it necessary to perform an improvement in the relevant art. <strong>Object of the Invention</strong> In order to eliminate the disadvantages of the state of the art, an object of the invention is to establish BAR (bile acid receptor) antagonistic function. Another object of the invention is to trigger an increase in the CYP7A1 expression. Another object of the invention is to trigger an increase in the expression of cholesteryl ester hydrolase. In order to achieve the aforesaid advantages, the invention is a composition for exhibiting hypolipidemic character, said composition being obtained by the components selected from the group comprising <strong>3,20-dimethyl-1,2,21,22-tetradehydro-2,3,20,21-protobioside,</strong> <strong>17,20-dimethyl-1,2,21,22-tetradehydro-2,3,20,21-protobioside </strong>that are used individually or in combinations. The structural and characteristic features and all the advantages of the invention will become more clearly understood from the detailed description provided below and therefore, the evaluation must be made taking this detailed description into consideration. <strong>Detailed Description of the Invention</strong> The invention is a composition comprising synthetic protobioside derivatives formed for exhibiting hypolipidemic character. Said invention establishes BAR (bile acid receptor) antagonistic function, triggers an increase in the CYP7A1 expression, and triggers an increase in the expression of cholesteryl ester hydrolase. The composition according to the invention contains <strong>3,20-dimethyl-1,2,21,22-tetradehydro-2,3,20,21-protobioside,</strong> <strong>17,20-dimethyl-1,2,21,22-tetradehydro-2,3,20,21-protobioside</strong>. Said composition is obtained by a mixture of the aforesaid components according to the following ratios by weight: <strong>1-99% 3,20-dimethyl-1,2,21,22-tetradehydro-2,3,20,21-protobioside,</strong> <strong>99-1% 17,20-dimethyl-1,2,21,22-tetradehydro-2,3,20,21-protobioside. </strong> The composition is obtained from the aforesaid components selected from the aforesaid group and used according to the mentioned weight ratio ranges individually or in combinations. Said invention also encompasses the use of said composition for exhibiting hypolipidemic character and the manufacture thereof for this purpose. <strong>CLAIMS</strong> A composition for exhibiting hypolipidemic character, said composition being obtained by the components selected from the group comprising <strong>3,20-dimethyl-1,2,21,22-tetradehydro-2,3,20,21-protobioside,</strong> <strong>17,20-dimethyl-1,2,21,22-tetradehydro-2,3,20,21-protobioside </strong>that are used individually or in combinations. A composition according to Claim 1 characterized in that it comprises 1-99% by weight <strong>3,20-dimethyl-1,2,21,22-tetradehydro-2,3,20,21-protobioside</strong>. A composition according to Claim 1 characterized in that it comprises 99-1% by weight <strong>17,20-dimethyl-1,2,21,22-tetradehydro-2,3,20,21-protobioside</strong>. Use of the components according to Claims 1 to 3 obtained individually or in combinations selected from the group consisting of <strong>3,20-dimethyl-1,2,21,22-tetradehydro-2,3,20,21-protobioside,</strong> <strong>17,20-dimethyl-1,2,21,22-tetradehydro-2,3,20,21-protobioside </strong>for the manufacture of a composition for exhibiting hypolipidemic character.