[Prospects of using miramistin for individual prevention of sexual HIV transmission].

For more than 20 years cationic surfactant Miramistin has been used in Russia and Ukraine as an antiseptic mean for individual prophylaxis of venereal diseases and for the treatment of genitourinary tract and other systems infections. Complete inhibition of HIV-1 activity in vitro by Miramistin in concentrations higher than 0.0075%, has been demonstrated, that allows to consider this detergent as a potent first-generation vaginal microbicide for the prevention of HIV transmission. Higher anti-HIV effect of Miramistin than of nonoxynol-9 and low local toxicity show good prospects of using Miramistin for individual prevention of HIV transmission.

[Synthesis and biological activity of anomeric muramoyldipeptide butylglycosides]. / Sintez i biologicheskaia aktivnost anomernykh butilglikozidov muramoildipeptida.

The synthesis of anomeric butyl glycosides of muramyl dipeptide was reported. alpha-Butyl glycoside of N-acetyl-D-glucosamine was 4,6-O-benzylidenated and the benzylidene derivative was 3-O-alkylated by the Williamson reaction with sodium (S)-2-chloropropionate. The resulting protected alpha-butyl glycoside of muramic acid was then condensed with L-Ala-D-iGln-OBzl by the DCC-HOSu method. Mild acidic hydrolysis and subsequent catalytic hydrogenolysis of the resulting glycopeptide yielded the target alpha-butyl glycoside of N-acetyl-L-alanyl-D-isoglutamine. In the synthesis of beta-butyl glycoside of N-acetylmuramyl-L-alanyl-D-isoglutamine, 2-acetamido- 4,6-di-O-acetyl-2-deoxy-3-O-[(R)-1-(methoxycarbonyl)ethyl]-alpha- D-glucopyranose, a 1-OH derivative of muramic acid, was the key compound. Its interaction with the excess thionyl chloride resulted in the corresponding glycosyl halide, which was condensed with n-butanol according to Helferich. O-Deacetylation, 4,6-isopropylidenation, and subsequent alkaline hydrolysis of the resulting compound gave the protected beta-butyl glycoside of muramic acid. Its activation and condensation with L-Ala-D-iGln-OBzl and the subsequent removal of protective groups were performed in the same manner as the reactions in the synthesis of alpha-butyl glycoside of N-acetyl-L-alanyl-D-isoglutamine. The adjuvant activity of the butyl glycosides to HIV proteins rgp160 and rgp120 and their ability to affect in vitro HIV replication and the proliferation of mouse spleen T-cells were examined. The biological activity of anomeric muramyl dipeptides was shown to depend essentially on the configuration of their anomeric center.

[Effect of saponins from Hedera taurica Carr. and modified muramylpeptides on replication of human immunodeficiency virus in vitro]. / Vliianie saponinov iz Hedera taurica Carr. i modifitsirovannykh muramilpeptidov na reproduktsiiu virusa immunodefitsita cheloveka in vitro.

The effects of muramyldipeptide (MDP), several new MDP derivatives, and saponins derived from Hedera taurica Carr, on the in vitro replication of HIV-1 were studied. The coefficient of alteration of the rate of HIV replication was used to compare these reagents' effects on virus replication in Jurkat-tat cells. This coefficient was calculated as the ratio of concentrations of HIV p24 in supernatants to the amount of viable cells. Muramylpeptides boosted HIV replication. Only one modified muramylpeptide alpha-butyl-MDP and tauroside H2 were not capable of boosting HIV-1 antigen production.

[The effect of fetal calf serum on the anti-HIV properties of miramistin]. / Vliianie émbrional'noi syvorotki korov na anti-VICh-svoistva miramistina.

The anti-HIV activity of an antiseptic miramistin in the presence of fetal calf serum (FCS) was studied. It has been recently shown that cation detergent miramistin at a concentration of 100 micrograms/ml prevented HIV-1 replication in MT-4 cells when these cells were cocultivated with MT-4 cells previously infected and treated with the detergent in a protein-free medium. Under such conditions 50 micrograms of miramistin per ml delayed HIV propagation in MT-4 cells by 14 days. Detergent-dependent arrest of HIV development was abolished by addition of FCS at a final concentration of 50%. Miramistin in a dose of 100 micrograms/ml prevents HIV-1 replication in Jurkat-tat cells when they are cocultivated with the cells of the same line previously infected and treated by the detergent in the presence of 5% FCS. FCS in concentrations from 12.5 to 75% prevents the anti-HIV activity of miramistin in a dose of 100 micrograms/ml.

[The use of the Soviet detergents dezintegron-O and dezintegron-B for the solubilization of influenza virus glycoproteins]. / Ispol'zovanie otechestvennykh detergentov dezintegrona-O i dezintegrona-B dlia soliubilizatsii glikoproteidov virusa grippa.

Native detergents, desintegron-O-and desintegron-B, solubilize hemagglutinins of the influenza virus as intensively, as foreign drugs (mulgophen, zwittergent and sodium sarcozyl) do. This permits recommending desintegrons for quantitative determination of hemagglutinin of the influenza virus in virus-containing materials by means of the reaction of single radial immunodiffusion. Desintegron-O and desintegron-B permit extracting enzymatically active neuraminidase from influenza A viruses with 44.6-83.4% yield.

[An immunological analysis of the hemagglutinin from the influenza A virus (H1N1) isolated by using various detergents]. / Immunologicheskii analaiz gemaggliutinina virusa grippa A (H1N1), vydelennogo s pomoshch'iu razlichnykh detergentov.

Immunogenic properties of influenza virus hemagglutinin, isolated by new detergents O-14 (desintegron-O) and B-14 (desintegron-B) have been studied. Hemagglutinin isolated by desintegron-O has been found to be more immunogenic than virions. It has been shown that hemagglutinin isolated by desintegron-B induces a lower humoral immune response than the influenza virus.