Hypocholesterolemic activity of hesperetin derivatives

• Published in: Bioorganic & medicinal chemistry letters Vol. 13; no. 16; pp. 2663 - 2665
• Main Authors: Jeong, Tae-Sook, Kim, Eun Eai, Lee, Chul-Ho, Oh, Jung-Hoon, Moon, Surk-Sik, Lee, Woo Song, Oh, Goo-Taeg, Lee, Sangku, Bok, Song-Hae
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 18.08.2003; Elsevier
• Subjects: Animals; Anticholesteremic Agents - chemical synthesis; Anticholesteremic Agents - pharmacology; Biological and medical sciences; Body Weight; Cholesterol - blood; Cholesterol, Dietary - administration & dosage; Ethers - chemical synthesis; Ethers - pharmacology; General and cellular metabolism. Vitamins; Hesperidin - chemical synthesis; Hesperidin - chemistry; Hesperidin - pharmacology; Hypercholesterolemia - blood; Hypercholesterolemia - drug therapy; Medical sciences; Mice; Pharmacology. Drug treatments; Structure-Activity Relationship; Time Factors; Rodentia; Flavonoid; Cholesterol; Flavanone derivatives; Cis stereoisomer; Vertebrata; Polyphenol; Mammalia; Structure activity relation; Mouse; Animal; Phenols; Chemical synthesis; Antilipemic agent
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/S0960-894X(03)00574-2

Hesperetin ester and ether derivatives possessing a long alkyl chain were synthesized for examining their hypocholesterolemic activities in high cholesterol-fed mice. Hesperetin 7- O-lauryl ether ( 4b) and hesperetin 7- O-oleyl ether ( 4e) exhibited strong cholesterol-lowering effects. A series of hesperetin 7- O-esters 2 and hesperetin 7- O-ethers 4 were prepared and evaluated as hypocholesterolemic agents.