Bee venom (BV) is used in folk medicine to treat arthritis. It has antiinflammatory effects in animal models of rheumatic disease. We have studied the effects of BV on human neutrophil production of superoxide (O2-) and hydrogen peroxide, finding potent, nontoxic, dose-dependent production inhibition. Melittin, the major fraction of BV (50-70%) shows high-affinity calmodulin binding (Kd 3 nM). Drugs which bind calmodulin, such as trifluoperazine, inhibit O2- production by human neutrophils. For these reasons we have investigated the effect of melittin and other BV peptides on O2- production by human peripheral blood leukocytes. We show that melittin inhibited O2- production both pre- and poststimulation in contrast to other BV fractions which were without effect. Oxygen radicals and their derivatives from inflammatory cells are implicated in the tissue damage occurring during inflammation. The inhibition is due to a direct effect on cells, and not indicator medium, dismutation, toxic or scavenging effects. We propose that melittin may serve as a prototype small (mol wt 1280), cationic, amphipathic, calmodulin-binding, membrane-active, superoxide-production-inhibiting peptide, providing a model for peptides which could have a role in in vivo regulation of radical production.
Summary
A double‐blind crossover study has compared intra‐nasal sodium cromoglycate (SCG) with beclomethasone dipropionate (BDP), and both drugs with placebo, in fifty‐two chronic perennial rhinitis patients, BDP was significantly more effective in relieving symptoms than SCG (76.9% and 50% of the patients improved respectively, P<0.01). Both drugs were more active than placebos but while BDP was very clearly more effective (P<0.0005) SCG was only marginally better than its placebo (P<0.05, Fisher; P=0.068, χ2). BDP was selected by 56% of the patients as the best agent for continuing therapy at the end of the trial. By contrast SCG was preferred by the same number of patients as chose the two placebos (11.5%).
Investigation of the antiinflammatory properties of bee venom demonstrates that it inhibits production of superoxide anion by human neutrophils in a potent, selective, nontoxic, dose-dependent fashion, both pre- and poststimulation by particulate and soluble activators of the neutrophil oxidative metabolism burst. The effect is not due to receptor competition, superoxide dismutase, and/or catalase activity, scavenging, or indicator media effects. These findings may explain the antiinflammatory effects of whole bee venom in experimental systems, its widespread use in folk medicine, and lead to the development of potent, new antiinflammatory substances for therapeutic use in man.
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