Inhibitory effects of 3,3',4,5'-tetrahydroxystilbene and 3,3',4,5'-tetrahydroxybibenzyl, the constituents of Cassia garrettiana on antigen-induced histamine release in vitro.
3,3',4,5'-Tetrahydroxystilbene (I) and 3,3',4,5'-tetrahydroxybibenzyl (II), isolated from the heartwood of Cassia garrettiana Craib (Leguminosae), showed inhibitory effects on antigen-induced histamine release from rat peritoneal mast cells in vitro. The inhibitory effect of I (IC50 = 30.2 microM) was much stronger than that of II (greater than 100 microM). Compound II, as well as I (IC50 = 7.3 microM) reported previously, also inhibited the histamine release from human peripheral basophils induced by anti-immunoglobulin E (IgE) in vitro, and its IC50-value was 68.0 microM. These results suggest that the trans-olefin structure in the molecule may be necessary for I to have an inhibitory effect on histamine release. Considering that disodium cromoglycate did not show any significant inhibitory effect on anti-IgE-induced histamine release from human basophils, the strong inhibitory effects of I in both tests are of considerable interest.
Inamori
Y
Y
Osaka University of Pharmaceutical Sciences, Japan.
Ogawa
M
M
Tsujibo
H
H
Baba
K
K
Kozawa
M
M
Nakamura
H
H
D000818:Animals; D000941:Antigens / Q000276:immunology*; D001491:Basophils / Q000187:drug effects / Q000378:metabolism; D001632:Bibenzyls / Q000494:pharmacology*; D002366:Cassia / Q000737:chemistry*; D006633:Histamine Antagonists / Q000494:pharmacology*; D006636:Histamine Release / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D008407:Mast Cells / Q000187:drug effects / Q000378:metabolism; D010946:Plants, Medicinal; D051381:Rats; D011919:Rats, Inbred Strains; D013267:Stilbenes / Q000494:pharmacology*
D000941:Antigens; D001632:Bibenzyls; D006633:Histamine Antagonists; D013267:Stilbenes; C074505:3,3',4,5'-tetrahydroxybibenzyl; C041525:3,3',4,5'-tetrahydroxystilbene