A Comparative Study of the Anti-Allergic Effects of Disodium Baicalein 6-Phosphate (BPS) and Disodium Cromoglycate (DSCG)

Abstract

Abstract-A comparative study was carried out on the effects of a soluble derivative of baicalein, disodium baicalein 6-phosphate (BPS) and disodium cromoglycate (DSCG) on the immediate type allergic reactions.BPS not only inhibited reaginic antibody mediated reactions including antigen-induced mediator release from monkey lung, homologous PCA in rats, and reaginic antibody-mediated degranulation of mast cell, but also non-reaginic antibody-mediated reactions such as mediator release from guinea pig lung sensitized with ovalbumin and that from human lung caused by anti IgE. The agent, however, did not affect the mediator release from lung of rats sensitized with dinitrophynylated ascaris extract plus Bordetella pertussis. On the other hand, DSCG showed characteristic properties as an inhibitor of reaginic antibody-mediated reaction.It is thus assumed that the functional site of reaginic antibody is well fixed with DSCG at a definite distance between the two-chromone-nuclei while that of IgG is readily fixed with the two molecules of baicalein or BPS.Baicalein and baicalin are flavones contained in the radix of Scutellaria baicalensis GEORGI (Woogon), which from ancient times has often been used in Chinese medicine as a remedy for allergic diseases and inflammation. We (1-5) have already reported the anti allergic activity of baicalein and its derivatives, and these substances also have a potent protective action against active and passive anaphylaxis. These agents were also found to inhibit reagin-mediated reaction as well as disodium cromoglycate (DSCG). DSCG does inhibit reagin-mediated reaction with a fairly high specificity (6-12), however, inhibits not at all or only slightly non-reaginic antibody-mediated reactions (7-12) and the mediator release by specific antigen from the leucocytes of allergic patient (13).From the viewpoint of chemical structures, baicalein is a monochromone derivative while DSCG is a symmetric dichromone derivative, as shown in Fig. 1

Inhibition of homologous passive cutaneous anaphylaxis (PCA) by disodium cromoglycate-related compounds.

“…The present result appears to support the speculation described in a previous paper (1), in which the functional site of IgE highly interacts with the structure of DSCG at a definite distance between the two chromone-nuclei. In order to confirm this possibility, studies are now under way using the other experimental systems mediated by both IgE and IgG antibodies.…”

“…Conversely, DSCG showed characteristic properties as an inhibitor of IgE antibody-mediated reaction. From these findings, it was suggested that the functional site of IgE antibody appears to interact with DSCG, with a definite distance between the two chromone-nuclei ; while the site of the non-reaginic antibody, IgG, is shorter or longer than that of IgE antibody and is readily fixed with two molecules of BPS (1).…”

“…Such being the case, drugs with a mechanism similar to that of DSCG and are which effective when given orally are most feasible for treatment of patients with asthma, particularly children. Several reports on such drugs have been made (1,(3)(4)(5)(6)(7)(8)(9).…”

Antianaphylactic and Antipruritic Effects of the Flowers of Impatiens textori MIQ.

“…1A), compounds 1-3 (Fig. 1B) and DSCG, 13) a classical anti-degranulating agent, (Fig. 1C) all significantly inhibited BP decrease.…”

Antiallergic properties of an orally effective agent,((3-(1H-tetrazol-5-yl)-phenyl)amino) oxoacetic acid n-butyl ester.

“…The antiserum with the rat 3-hr PCA titer of 1 :64 did not induce 48-hr PCA. Rabbit anti-EA antiserum was prepared by the method of Koda et al (8). The rat 3-hr PCA titer was 1 :6.…”