title: 2,4,5-trimethoxycinnamic acid: the major metabolite of alpha-asarone, retains most of the pharmacological properties of alpha-asarone.
abstract: 2,4,5-trimethoxycinnamic acid (TMC), the major and non toxic metabolite of alpha-asarone (2,4,5-trimethoxy-1-propenyl benzene), retains most of the pharmacological properties of alpha-asarone, since both substances, administered to hypercholesterolemic rats at 80 mg/kg body wt, decreased total serum cholesterol, lowered LDL-cholesterol levels and kept unaffected HDL-cholesterol levels. In addition, both substances increased bile flow, especially in hypercholesterolemic rats, by rising the secretion of bile salts, phospholipids and bile cholesterol. These drugs also reduced cholesterol levels of gallbladder bile, whereas phospholipids and bile salts concentrations were increased, decreasing the cholesterol saturation index (CSI). We also found that alpha-asarone was 20 times better inhibitor of HMG-CoA reductase than TMC. This effect on HMG-CoA reductase was the only property highly reduced in TMC in comparison with alpha-asarone, while the other pharmacological properties of alpha-asarone were retained by TMC. These experiments strongly suggest that TMC can be further studied as a possible hypocholesterolemic and cholelitholytic agent.
authors.affiliation: Departamento de Bioquímica, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Apartado Postal 4-129, Admon. 4, México City 06401, Mexico.
authors.forename: Javier
authors.initials: J
authors.lastname: Antunez-Solis
authors.forename: Fernando
authors.initials: F
authors.lastname: Hernández-Derramadero
authors.forename: Mayda
authors.initials: M
authors.lastname: Aquino-Vega
authors.forename: Selene
authors.initials: S
authors.lastname: Ibarra-Ramírez
authors.forename: Lorena
authors.initials: L
authors.lastname: Rodríguez-Páez
authors.forename: Isabel
authors.initials: I
authors.lastname: Baeza
authors.forename: Carlos
authors.initials: C
authors.lastname: Wong
mesh_terms: D000081248:Allylbenzene Derivatives; D000818:Animals; D000840:Anisoles / Q000378:metabolism* / Q000494:pharmacology*; D000924:Anticholesteremic Agents / Q000494:pharmacology*; D001646:Bile / Q000187:drug effects / Q000378:metabolism; D001647:Bile Acids and Salts / Q000097:blood / Q000378:metabolism; D002784:Cholesterol / Q000097:blood / Q000378:metabolism; D002934:Cinnamates / Q000494:pharmacology*; D006903:Hydroxymethylglutaryl CoA Reductases / Q000097:blood / Q000378:metabolism; D006937:Hypercholesterolemia / Q000378:metabolism; D000960:Hypolipidemic Agents / Q000494:pharmacology*; D008074:Lipoproteins / Q000097:blood / Q000378:metabolism; D008297:Male; D010743:Phospholipids / Q000097:blood / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar
chemical_list: C552680:2,4,5-trimethoxycinnamic acid; D000081248:Allylbenzene Derivatives; D000840:Anisoles; D000924:Anticholesteremic Agents; D001647:Bile Acids and Salts; D002934:Cinnamates; D000960:Hypolipidemic Agents; D008074:Lipoproteins; D010743:Phospholipids; C012195:asarone; D002784:Cholesterol; D006903:Hydroxymethylglutaryl CoA Reductases