A new antiinflammatory agent identified as 8-[C-beta-D-[2-O-(E)-cinnamoyl]glucopyranosyl]-2- [(R)-2-hydroxypropyl]-7-methoxy-5-methylchromone (1) has been isolated from Aloe barbadensis Miller. At a dose of 200 microg/mouse ear, 1 exhibited topical antiinflammatory activity equivalent to 200 microg/ear of hydrocortisone. There was no reduction in thymus weight caused by treatment with 1 for any of the doses tested, while 200 microg/ear of hydrocortisone resulted in a 50% decrease in thymus weight.
The results suggest that RBx 7,796, a novel chemotype, is an orally efficacious inhibitor of 5-lipoxygenase enzyme that is effective against both neutrophilic and eosinophilic airway inflammation and shows potent inhibition with once daily administration.
Centchroman [dl-3,4-trans-2,2-dimethyl-3-phenyl-4-[p-(beta-pyrrolidinoethoxy)phenyl] - 7-methoxychroman hydrochloride], an antifertility agent under clinical evaluation, has been resolved into its optical enantiomers. The cytosol estrogen receptor binding affinity and estrogenic, antiestrogenic and antiimplantation activities of the two enantiomers have been determined. The enantiomers display a 7-fold difference in receptor affinity, and a corresponding difference in stimulation of the uterine growth and antiimplantation activity was observed in rats.
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