{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,30]],"date-time":"2026-04-30T23:14:20Z","timestamp":1777590860240,"version":"3.51.4"},"reference-count":28,"publisher":"Oxford University Press (OUP)","issue":"10","license":[{"start":{"date-parts":[[2006,10,1]],"date-time":"2006-10-01T00:00:00Z","timestamp":1159660800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/academic.oup.com\/journals\/pages\/open_access\/funder_policies\/chorus\/standard_publication_model"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2006,10,1]]},"abstract":"<jats:title>Abstract<\/jats:title>\n               <jats:p>The phenoxyacetic acid derivatives 1\u20136 [2-methoxy-4-(2-propenyl)phenoxyacetic acid (1); 2-methoxy-5-nitro-4-(2-propenyl)phenoxyacetic acid (2); methyl 2-methoxy-4-(2-propenyl)phenoxyacetate (3); ethyl 2-methoxy-4-(2-propenyl)phenoxyacetate (4); methyl 2-methoxy-5-nitro-4-(2-propenyl)phenoxyacetate (5); ethyl 2-methoxy-5-nitro-4-(2-propenyl)phenoxyacetate (6)] related to \u03b1-asarone have been reported previously as hypolipidaemic agents in diet-induced hyperlipidaemic mice. We have aimed to expand the pharmacological profile of these derivatives by investigating their hypolipidaemic activity in rats and mice under different experimental conditions. The antiplatelet activity was tested also in-vitro from blood derived from consenting healthy volunteers. In normolipidaemic rats, compounds 2, 3 and 5 at oral doses of 40 and 80 mg kg\u22121 significantly decreased total cholesterol and LDL-cholesterol levels. Moreover, analogues 3 and 5 administered to hypercholesterolaemic rats at the same doses for seven days also produced a reduction in the content of these same lipoproteins. In neither case were the high-density lipoprotein cholesterol and triglyceride concentrations affected. However, practically all tested compounds were found to be hypocholesterolaemic agents, and were shown to effectively lower low-density lipoprotein cholesterol and triglyceride levels in Triton-induced hyperlipidaemic mice at oral doses of 50 and 100 mg kg\u22121. In all tests, all animals appeared to be healthy throughout the experimental period in their therapeutic ranges. Triton-induced hypercholesterolaemic mice appeared to be a desirable model for this class of hypolipidaemic drugs. On the other hand, compounds 1, 2, 4 and 5 significantly inhibited ADP-induced aggregation in-vitro. These findings indicated that all of these compounds appeared to be promising for the treatment of human hyperlipidaemia and thrombotic diseases.<\/jats:p>","DOI":"10.1211\/jpp.58.10.0007","type":"journal-article","created":{"date-parts":[[2006,10,9]],"date-time":"2006-10-09T23:02:16Z","timestamp":1160434936000},"page":"1343-1349","source":"Crossref","is-referenced-by-count":11,"title":["Hypolipidaemic and antiplatelet activity of phenoxyacetic acid derivatives related to \u03b1-asarone"],"prefix":"10.1093","volume":"58","author":[{"given":"Ricardo","family":"P\u00e9rez-Past\u00e9n","sequence":"first","affiliation":[{"name":"Area Acad\u00e9mica de Farmacia, Instituto de Ciencias de la Salud, Universidad Aut\u00f3noma del Estado de Hidalgo ,","place":["M\u00e9xico"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rosa Virginia","family":"Garc\u00eda","sequence":"additional","affiliation":[{"name":"Departamento de Farmacia, Escuela Nacional de Ciencias Biol\u00f3gicas, Instituto Polit\u00e9cnico Nacional , M\u00e9xico D.F.,","place":["M\u00e9xico"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Leticia","family":"Gardu\u00f1o","sequence":"additional","affiliation":[{"name":"Departamento de Farmacia, Escuela Nacional de Ciencias Biol\u00f3gicas, Instituto Polit\u00e9cnico Nacional , M\u00e9xico D.F.,","place":["M\u00e9xico"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Elba","family":"Reyes","sequence":"additional","affiliation":[{"name":"Departamento de Morfolog\u00eda, Escuela Nacional de Ciencias Biol\u00f3gicas, Instituto Polit\u00e9cnico Nacional , M\u00e9xico D.F.,","place":["M\u00e9xico"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Fernando","family":"Labarrios","sequence":"additional","affiliation":[{"name":"Departamento de Qu\u00edmica Org\u00e1nica, Escuela Nacional de Ciencias Biol\u00f3gicas, Instituto Polit\u00e9cnico Nacional , M\u00e9xico D.F.,","place":["M\u00e9xico"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Joaqu\u00edn","family":"Tamariz","sequence":"additional","affiliation":[{"name":"Departamento de Qu\u00edmica Org\u00e1nica, Escuela Nacional de Ciencias Biol\u00f3gicas, Instituto Polit\u00e9cnico Nacional , M\u00e9xico D.F.,","place":["M\u00e9xico"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Germ\u00e1n","family":"Chamorro","sequence":"additional","affiliation":[{"name":"Departamento de Farmacia, Escuela Nacional de Ciencias Biol\u00f3gicas, Instituto Polit\u00e9cnico Nacional , M\u00e9xico D.F.,","place":["M\u00e9xico"]}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"286","published-online":{"date-parts":[[2006,10,1]]},"reference":[{"key":"2024103109340250500_cit1","doi-asserted-by":"crossref","first-page":"927","DOI":"10.1038\/194927b0","article-title":"Aggregation of blood platelets by adenosine diphosphate and its reversal","volume":"194","author":"Born","year":"1962","journal-title":"Nature"},{"key":"2024103109340250500_cit2","first-page":"597","article-title":"Farmacolog\u00eda y Toxicolog\u00eda de Guatteria gaumeri y \u03b1-asarone","volume":"45","author":"Chamorro","year":"1993","journal-title":"Rev. Inv. Clin."},{"key":"2024103109340250500_cit3","doi-asserted-by":"crossref","first-page":"71","DOI":"10.1016\/S0378-4274(98)00041-1","article-title":"Dominant lethal study of \u03b1-asarone in male mice","volume":"99","author":"Chamorro","year":"1998","journal-title":"Toxicol. Lett."},{"key":"2024103109340250500_cit4","first-page":"587","article-title":"High hypolipidemic activity of saturated side-chain \u03b1-asarone analogs","volume":"10","author":"Cruz","year":"2001","journal-title":"Med. Chem. Res."},{"key":"2024103109340250500_cit5","doi-asserted-by":"crossref","first-page":"186","DOI":"10.1002\/ddr.10281","article-title":"Hypolipidemic activity of new phenoxyacetic derivatives related to \u03b1-asarone with minimal pharmacophore features","volume":"60","author":"Cruz","year":"2003","journal-title":"Drug Dev. Res."},{"key":"2024103109340250500_cit6","first-page":"27","article-title":"Statins, platelet aggregation and coronary heart disease","volume":"13","author":"Dajani","year":"2002","journal-title":"J. Assoc. Acad. Minor Phys."},{"key":"2024103109340250500_cit7","first-page":"101","article-title":"Synthesis and hypolipidemic activity of some alpha-asarone analogs","volume":"3","author":"D\u00edaz","year":"1993","journal-title":"Med. Chem. Res."},{"key":"2024103109340250500_cit8","doi-asserted-by":"crossref","first-page":"266","DOI":"10.1016\/0005-2760(79)90028-6","article-title":"Effects on ML-236B on cholesterol metabolism in mice and rats: lack of hypocholesterolemic activity in normal animals","volume":"575","author":"Endo","year":"1979","journal-title":"Biochim. Biophys. Acta."},{"key":"2024103109340250500_cit9","doi-asserted-by":"crossref","first-page":"2024","DOI":"10.1016\/0031-9422(80)83029-9","article-title":"Propenylbenzenes from Guatteria gaumeri","volume":"19","author":"Enr\u00edquez","year":"1980","journal-title":"Phytochemistry"},{"key":"2024103109340250500_cit10","doi-asserted-by":"crossref","first-page":"499","DOI":"10.1093\/clinchem\/18.6.499","article-title":"Estimation of the concentration of low-density lipoprotein cholesterol in plasma without use of preparative ultracentrifuge","volume":"18","author":"Friedwald","year":"1972","journal-title":"Clin. Chem."},{"key":"2024103109340250500_cit11","doi-asserted-by":"crossref","first-page":"161","DOI":"10.1016\/S0378-8741(96)01492-4","article-title":"Hypolipidemic activity of \u03b1-asarone in mice","volume":"55","author":"Gardu\u00f1o","year":"1997","journal-title":"J. Ethnopharmacol."},{"key":"2024103109340250500_cit12","first-page":"279","article-title":"Effet de l'\u03b1-asarone sur l'hypercholest\u00e9rolemie et la chol\u00e9lithiase exp\u00e9rimentales","volume":"21","author":"G\u00f3mez","year":"1987","journal-title":"Plantes M\u00e9d. Phytoth\u00e9r."},{"key":"2024103109340250500_cit13","doi-asserted-by":"crossref","first-page":"956","DOI":"10.1002\/jps.2600730724","article-title":"Hypolipidemic activity of 3-N-(1\u2032, 8\u2032-napthalimido) propionic acid in rodents","volume":"73","author":"Hall","year":"1984","journal-title":"J. Pharm. Sci."},{"key":"2024103109340250500_cit14","doi-asserted-by":"crossref","first-page":"138","DOI":"10.1097\/00041433-199706000-00003","article-title":"3-Hydoxy-3-methyglutaryl coenzyme A reductase inhibitors and hepatic apo lipoprotein B secretion","volume":"8","author":"Huff","year":"1997","journal-title":"Curr. Opin. Lipidol."},{"key":"2024103109340250500_cit15","doi-asserted-by":"crossref","first-page":"207","DOI":"10.1016\/0163-7258(87)90075-1","article-title":"Atherosclerosis risk factors","volume":"32","author":"Kannel","year":"1987","journal-title":"Pharm. Ther."},{"key":"2024103109340250500_cit16","doi-asserted-by":"crossref","first-page":"15","DOI":"10.1016\/S0021-9150(98)00141-5","article-title":"Lack of predictability of classical animal models for hypolipidemic activity: a good time for mice","volume":"140","author":"Krause","year":"1998","journal-title":"Atherosclerosis"},{"key":"2024103109340250500_cit17","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1211\/0022357991772015","article-title":"Synthesis and hypolipidemic evaluation of series of \u03b1-asarone analogues related to clofibrate in mice","volume":"51","author":"Labarrios","year":"1999","journal-title":"J. Pharm. Pharmacol."},{"key":"2024103109340250500_cit18","doi-asserted-by":"crossref","first-page":"115","DOI":"10.1055\/s-2006-959624","article-title":"\u03b1-Asarone toxicity in long term cultures of adult rat hepatocytes","volume":"59","author":"L\u00f3pez","year":"1993","journal-title":"Planta Med."},{"key":"2024103109340250500_cit19","doi-asserted-by":"crossref","first-page":"366","DOI":"10.1097\/01.hco.0000126582.27767.87","article-title":"Pharmacological elevation of high-density lipoproteins: recent insights on mechanism of action and atherosclerosis protection","volume":"19","author":"Meyers","year":"2004","journal-title":"Curr. Opin. Cardiol."},{"key":"2024103109340250500_cit20","doi-asserted-by":"crossref","first-page":"3671","DOI":"10.1021\/jm000905n","article-title":"Synthesis and hypolipidaemic and antiplatelet activities of \u03b1-asarone isomers in humans (in vitro), mice (in vivo), and rats (in vivo)","volume":"43","author":"Poplawski","year":"2000","journal-title":"J. Med. Chem."},{"key":"2024103109340250500_cit21","doi-asserted-by":"crossref","first-page":"397","DOI":"10.1078\/0944-7113-00274","article-title":"\u03b1-Asarone inhibits HMG-CoA reductase, lowers serum LDL-cholesterol levels and reduces biliary CSI in hypercholesterolemic rats","volume":"10","author":"Rodr\u00edguez-P\u00e1ez","year":"2003","journal-title":"Phytomedicine"},{"key":"2024103109340250500_cit22","first-page":"107","article-title":"The anticoagulant effect of beta-asarone in the mouse and the rat","volume":"34","author":"Rubio-Poo","year":"1991","journal-title":"Proc. West. Pharmacol. Soc."},{"key":"2024103109340250500_cit23","first-page":"3371","article-title":"Choosing drug therapy for patients with hyperlipemia","volume":"61","author":"Safeer","year":"2000","journal-title":"Am. Fam. Phys."},{"key":"2024103109340250500_cit24","first-page":"149","article-title":"Action t\u00e9ratogene de l'\u03b1-asarone chez la souris","volume":"12","author":"Salazar","year":"1992","journal-title":"J. Toxicol. Clin. Exp."},{"key":"2024103109340250500_cit25","first-page":"1694","article-title":"Hypolipidemic affects of S-methylmethionine (vitamin U) using various experimental procedures","volume":"30","author":"Seri","year":"1980","journal-title":"Arzneimittelforschung"},{"key":"2024103109340250500_cit26","doi-asserted-by":"crossref","first-page":"763","DOI":"10.1055\/s-2001-18360","article-title":"Effect of trans-dehydrocrotonin, a 19-nor-clerdone diterpene from Croton cajucara on experimental hypertriglyceridaemia and hypercholesterolaemia induced by triton WR 1339 (tyloxapol) in mice","volume":"67","author":"Silva","year":"2001","journal-title":"Planta Med."},{"key":"2024103109340250500_cit27","doi-asserted-by":"crossref","first-page":"6547","DOI":"10.1016\/j.bmc.2004.09.028","article-title":"Design, synthesis, and inhibition of platelet aggregation for some 1-o-chlorophenyl-1,2,3,4-tetrahydroisoquinoline derivatives","volume":"12","author":"Yang","year":"2004","journal-title":"Bioorg. Med. 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