A highly potent antiangiogenic activity of retinoids.
Four retinoids, i.e. retinol (vitamin A), retinoic acid, retinyl acetate and synthetic chalcone carboxylic acid (Ch 55), were examined for their effects on embryonic angiogenesis using 4.5-day chorioallantoic membranes of chick embryo. The effects of these retinoids were compared with that of antibiotic herbimycin A, which was the most powerful inhibitor of the angiogenesis reported previously. The four retinoids strongly inhibited embryonic angiogenesis; the order of inhibitory activity was Ch 55 greater than retinoic acid greater than herbimycin A greater than retinyl acetate based on the dose required for the half-maximal inhibitory effect. The present results suggest that retinoids are effective inhibitors of angiogenesis, and can be applied for the management of certain diseases accompanied by aberrant angiogenesis, particularly that which occurs during progressive growth of solid tumors.
Oikawa
T
T
Division of Cancer Therapeutics, Tokyo Metropolitan Institute of Medical Science, Japan.
Hirotani
K
K
Nakamura
O
O
Shudo
K
K
Hiragun
A
A
Iwaguchi
T
T
D000818:Animals; D016227:Benzoquinones; D002599:Chalcone / Q000494:pharmacology; D047188:Chalcones; D002642:Chick Embryo; D004224:Diterpenes; D004305:Dose-Response Relationship, Drug; D066298:In Vitro Techniques; D047029:Lactams, Macrocyclic; D009389:Neovascularization, Pathologic; D011809:Quinones / Q000494:pharmacology; D012176:Retinoids / Q000494:pharmacology*; D000084562:Retinyl Esters; D017828:Rifabutin / Q000031:analogs & derivatives; D014212:Tretinoin / Q000494:pharmacology; D014801:Vitamin A / Q000031:analogs & derivatives / Q000494:pharmacology
D016227:Benzoquinones; D047188:Chalcones; D004224:Diterpenes; D047029:Lactams, Macrocyclic; D011809:Quinones; D012176:Retinoids; D000084562:Retinyl Esters; D014801:Vitamin A; D017828:Rifabutin; C009166:retinol acetate; D014212:Tretinoin; D002599:Chalcone; C020754:herbimycin; C054189:3,5-di-tert-butylchalcone 4'-carboxylic acid