# US 2014/0194474 A1 · Composition for treating atherosclerosis and a preparation method thereof > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2014/0194474 A1 - Document ID: US20140194474A1 - Status: Published application - Kind: A1 - Application number: 14/202,564 - Filed: 2014-03-10 - Published: 2014-07-10 - Earliest claimed: 2011-08-10 - Assignees: Kaohsiung Medical University - Applicants: Kaohsiung Medical University - Inventors: Yang-Chang WU; Fang-Rong Chang; Tusty-Jiuan Hsieh; Suh-Hang Juo; An-Shen Lin; Ying-Chi Du - Web page: https://patentgrep.com/patent/US20140194474A1 ## CPC - A61K 31/12: Ketones - A61K 31/122: having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin - A61K 31/352: condensed with carbocyclic rings, e.g. methantheline {(cannabinoids A61K31/658)} - A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465) - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - C07C 49/835: having unsaturation outside an aromatic ring - C07C 49/84: containing ether groups, [IMAGE cpc-sch-C07C-0958.gif] groups,[IMAGE cpc-sch-C07C-0959.gif] groups, or[IMAGE cpc-sch-C07C-0960.gif] groups - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS ## Abstract Disclosed are a composition for preventing and treating atherosclerosis which includes chalcone compound. In particular, the chalcone compound bound with 2-hydroxyl in ring A and 4′-methyoxy in ring B has versatile therapeutic potentials on anti-atherosclerosis by acting as PPARγ inducer, p44/42 MAPK inhibitor and cell cycle blocker and does not show toxicity to human aortic smooth muscle cells (HASMCs). In addition, the chalcone compound exhibits synergistic effect with the PPARγ ligand (rosiglitazone) to inhibit cell proliferation and the upregulation of cyclin D1, cyclin D3, interleukin-1β (IL-1β) and interleukin-6 (IL-6) induced by oxidized low density lipoprotein (Ox-LDL). ## Claims ### Claim 1 A method to either prevent or treat an atherosclerosis of a subject, comprising a step of: administering to the subject an effective amount of a chalcone compound represented by Formula I: to either prevent or treat the atherosclerosis, wherein R1 is a first hydrogen, each of R2 to R5 is selected from a group consisting of a second hydrogen, a first hydroxide and a halogen, each of R6, R7, R9 and R10 is selected from a group consisting of a third hydrogen, a second hydroxide, a C1 to C20 alkoxy group and a benzyloxy group, and R8 is selected from a group consisting of a fourth hydrogen, a C1 to C20 alkyl group and a benzyl group. ### Claim 2 (depends on 1) The method according to claim 1 being effective in regulating a pathway by one of inhibiting a p44/42 mitogen-activated protein kinase (MAPK) phosphorylation and activating a peroxisome proliferator activated receptor gamma (PPARγ). ### Claim 3 (depends on 2) The method according to claim 2, wherein the p44/42 MAPK phosphorylation is effective in promoting an expression of at least one of an interleukin-6 (IL-6) and an interleukin-1beta (IL-1β). ### Claim 4 (depends on 2) The method according to claim 2, wherein the PPARγ is effective in inhibiting an expression of at least one of an interleukin-6 (IL-6) and an interleukin-1beta (IL-1β). ### Claim 5 (depends on 2) The method according to claim 2, wherein the PPARγ is effective in inhibiting an expression of at least one of a cyclin D1 and a cyclin D3. ### Claim 6 A method for increasing a reproduction of a peroxisome proliferator activated receptor gamma (PPARγ) in a subject, comprising a step of: administering to the subject an effective amount of a chalcone compound represented by Formula I: to increase the reproduction of the PPARγ, wherein R1 is a first hydrogen, each of R2 to R5 is selected from a group consisting of a second hydrogen, a first hydroxide and a halogen, each of R6, R7, R9 and R10 is selected from a group consisting of a third hydrogen, a second hydroxide, a C1 to C20 alkoxy group and a benzyloxy group, and R8 is selected from a group consisting of a fourth hydrogen, a C1 to C20 alkyl group and a benzyl group. ### Claim 7 (depends on 6) The method according to claim 6, wherein the PPARγ is translated from a messenger RNA, and the method is effective in increasing an expression of the messenger RNA. ### Claim 8 A method for inhibiting at least one of a cell proliferation of human aortic smooth muscle cells and an inflammation of a subject, comprising a step of: administering to the subject an effective amount of a chalcone compound represented by Formula I and a ligand of a peroxisome proliferator activated receptor gamma (PPARγ): to inhibit at least one of the cell proliferation of the human aortic smooth muscle cells and the inflammation, wherein R1 is a first hydrogen, each of R2 to R5 is selected from a group consisting of a second hydrogen, a first hydroxide and a halogen, each of R6, R7, R9 and R10 is selected from a group consisting of a third hydrogen, a second hydroxide, a C1 to C20 alkoxy group and a benzyloxy group, and R8 is selected from a group consisting of a fourth hydrogen, a C1 to C20 alkyl group and a benzyl group. ### Claim 9 A method for inhibiting an inflammation of a subject, comprising steps of: administering to the subject a first effective amount of a chalcone compound represented by formula II: and administering to the subject a second effective amount of an (RS)-5-[4-(2-[methyl(pyridin-2-yl)-amino]ethoxy)benzyl]thiazolidine-2,4-dione (rosiglitazone) to inhibit the inflammation. ### Claim 10 (depends on 9) The method according to claim 9, wherein the inflammation is a symptom of an atherosclerosis. ### Claim 11 A method for inhibiting a proliferation of a smooth muscle cell, comprising steps of: administering to the subject a first effective amount of a chalcone compound represented by formula II: and administering to the subject a second effective amount of a 2-(2-amino-3-methoxyphenyl)-chromen-4-one (PD98059) to inhibit the proliferation of the smooth muscle cell.