[Modification of antitumor effect of vincristine by natural avermectins].

The effect of avermectins (aversectin C, aversectin C1 and avermectin B1) on the vincristine antitumor action with respect to murine transplantable tumors was studied. It was shown that both the natural avermectins mixtures and the individual avermectin B1 potentiated the antitumor action of vincristine on Ehrlich carcinoma, melanoma B16 and P388 lymphoid leukemia, including the vincristine resistant strain P388. Such an effect of the avermectins was observed only when they were administered after vincristine.

[Effect of avermectns on Ca(2+)-dependent chloride currents in plasmalemma of Chara corallina cells].

A natural complex of avermectins, aversectin C, and a component of this complex, avermectin A1, were shown to change the conductivity of Ca(2+)-dependent chloride channels of plasmalemma of Chara corallina cells by acting only from the outer side of the cellular membrane. Low concentrations of aversectin C and avermectin A1 increased the chloride current: K1/2 = 3.5 x 10(-5) mg/ml for the whole complex and K1/2 = 2.

[Selective cytostatic and cytotoxic effects of avermectins].

A natural avermectin complex, aversectin C, was shown to be capable of exerting selective cytostatic effect. It killed proliferating neuroblastoma B 103 cells but was non-toxic for differentiated cells of this culture. The activity of aversectin C was related neither to activation of the GABA alpha-receptors nor to their blocking and was at a large extent due to the action of avermectin A1, a component of aversectin C.

[Acute toxicity of aversectin C : various routes of administration and dosage forms].

The acute oral, cutaneous, and inhalation toxicity of aversectin C was studied on white unbred rats and mice. The compound was less toxic for rats than for mice, the LD50 for oral administration being 90 and 33 mg/kg, respectively. Aversectin C exhibited a maximum acute toxicity upon the inhalation in rats (LD50 = 40 mg/kg), while a minimum toxicity level was observed for the cutaneous application in rats (1700 mg/kg).