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Biomedical subjects

F S Zarudiĭ

Publications and source records attributed to F S Zarudiĭ.

At least 19 recordsLinked to original sources

[Synthesis of the lupane group triterpenoids and there hepatoprotective activity].

Hemisuccinates, hemiphthalates, acetylsalicylates, cinnamates, and p-methoxycinnamates of lupeol, betulin, and 3-O-acetylbetulin were synthesized via interaction with corresponding acid anhydrides or acid chlorides. A number of betulin esters in position 3 and 28 were shown to exhibit a pronounced hepatoprotective effect similar to that of betulin and silibor. These experimental data were in a good agreement with the computer prediction of their biological activity. Betulin 3,28-bis-hemiphthalate was more effective than carsil in models of experimental hepatitis caused by carbon tetrachloride, tetracycline, and ethanol.

Animals↗

[Improvement of effectiveness of antibiotic therapy by pyrimidine derivatives in reparative regeneration of skin in rats].

It was shown on noninbred albino rats with various affections of the skin that pyrimidine derivatives stimulated the skin reparative regeneration and increased the efficacy of antibiotic therapy of Staphylococcus and Proteus infected wounds. The therapeutic effect of 2-methyl-4-amino-6-oxypyrimidine was much higher than that of oxymethyluracil or methyluracil. The pyrimidine derivatives proved to be universal accelerators for reparative regeneration, were compatible with antibiotics and increased their efficacy.

Animals↗

[Pyrimidine derivatives increase antibiotic therapy efficacy after ionizing irradiation].

Pyrimidine derivatives increased the antibiotic therapy efficacy in albino rats irradiated with RUM-7 apparatus for close-focus roentgenotherapy. 2-Methyl-4-amino-6-oxypyrimidine was twice as efficient as oxymethyluracil and 6 times as efficient as methyluracil in the stimulation of the skin reparative regeneration. When the total irradiation was performed with LUCH-1 apparatus in a dose of 6 Gy the pyrimidine derivatives also increased the antibiotic therapy efficacy. After the prophylactic use of the pyrimidine derivatives for 7 days prior to the total irradiation their therapeutic effect increased, the level of the exudative component lowered, the tissue epithelization increased, the terms of the wound healing decreased and the animal lifespan increased.

Administration, Topical↗

[Synthesis of triterpene 2,6-dideoxy-alpha-L-arabino-hexopyranosides from L-rhamnal. Their pharmacological properties].

Triterpene 2,6-dideoxy-alpha-L-arabino-hexopyranosides were synthesized by the glycosylation of oleanane triterpene alcohols with L-rhamnal acetate in the presence of cationite KU-2-8 and lithium bromide. 2,6-Dideoxy-alpha-L-arabino-hexopyranosides of allobetulin and methyl glycyrrhetinate showed pronounced antiulcerous activity; the latter also stimulated reparative skin regeneration in rats and was effective as a hepatoprotectant.

Animals↗

[Effect of 2-methyl-4-amino-6-hydroxypyrimidine on the effectiveness of antibiotic therapy in experimental staphylococcal infection in the context of immunosuppression].

The experiments on mice with Staphylococcus infection at the background of immune suppression due to the treatment with prednisolone or imuran showed that the use of 2-methyl-4-amino-6-oxypyrimidine, a derivative of pyrimidine, increased the animal survival, their lifespan and the efficacy of the tobramycin therapy.

Animals↗

[Transformations of glycyrrhizic acid. VIII. Synthesis of immunomodulating glycopeptides using tert-butyl amino acid esters].

Triterpene glycopeptides, derivatives of glycyrrhizic acid, were synthesized with the use of tert-butyl esters of L-amino acids. The condensation of glycoside with esters was carried out with N-hydroxysuccinimide--N,N-dicyclohexylcarbodiimide or N-hydroxybenzotriazol--N,N'-dicyclohexylcarbodiimide in the presence of a base (triethylamine, N-methyl- or N-ethylmorpholine). The protection groups were removed with the use of trifluoroacetic acid.

Adjuvants, Immunologic↗

[Synthesis and pharmacological activity of betulin dinicotinate].

The assignment of NMR resonances of lupane triterpenoids was refined by the example of 3,28-dinicotinoylbetulin, obtained by acylation of betulin. Hepatoprotective, untiulcer, antiinflammatory, reparative, and anti-HIV activities were found for the compound. In addition, it was demonstrated to have immunomodulatory activity, for the first time detected among lupane triterpenoids. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2002, vol. 28, no. 6; see also http://www.maik.ru.

Adjuvants, Immunologic↗

[Pharmacological properties of 11-deoxymisoprostol].

11-Deoxymisoprostol showed gastroprotector activity on the acute models of ulcers induced by acetylsalicylic acid and ethanol and produced curative effect on the chronic ulceration model induced by acetic acid. The positive effect is manifested by a decrease in the number of destructions and in the total area of chronic damage in the mucous membrane of the stomach. In addition, 11-deoxymisoprostol showed antiphlogistic activity on the acute edema models induced by carrageenan and formalin, by decreasing the model foot edema growth in experimental animals. The drug also decreased the level of lipid peroxidation in the rat blood serum on the background of acute ethanol ulceration.

Animals↗

[Study of pharmacological properties of betulin bishemiphthalate].

The results of pharmacological tests showed that betulin bishemiphthalate possesses hepatoprotector, antioxidant, and immunotropic properties. Administered in combination with hydroxymethyluracil, that betulin bishemiphthalate prevented the loss of experimental animals upon irradiation.

Acute Disease↗

[Some aspects of the antiarrhythmic effect of glialin].

The antiarrhythmic activity of allapinine and glialin (a complex of allapinin and glycyrrhizic acid) was studied on models of arrhythmias induced in rats and guinea pigs by intravenous administration of calcium chloride, aconitine, barium chloride, and strophanthin. The antiarrhythmic activity of glialin is qualitatively analogous to that of allapinine. The advantage of glialin over allapinin is its low toxicity, which is due to the presence of glycyrrhizic acid.

Aconitine↗

[The luteotropic and luteolytic properties of synthetic analogs of 11-deoxy-PGE1].

The luteotropic and luteolytic properties of synthetic analogues of 11-desoxy-PGE1 were studied. Compounds Nos. 1 and 2 depending on the dose exerted the opposite effect: in low doses--luteotropic, in high doses--luteolytic. Compounds Nos. 3, 4 and 5 in the whole range of doses exhibited only luteolytic properties. The ranges of doses of prostaglandin exerting the luteotropic effect depend on the structural modifications of prostaglandin molecule. The luteolytic effect of synthetic analogue No. 5 was suggested to be determined by its influence on the hypophysis through the change of contents of cyclic nucleotides and gonadotropic hormones. It was demonstrated that the luteolytic effect of compound No. 5 is realized through the central nervous system, in particular, through the hypophysis.

Alprostadil↗

[Device for measuring paw edema in rats and mice].

An unsophisticated highly precise mercuric electron-mechanic oncometer is proposed. It is intended for measuring paw edema in small laboratory animals during screening of new antiphlogistics. The device consists of two communicating vessels. The change in the mercury level after paw immersion transforms to the electrical signal by the induction technique. The controller of the displacement consists of a float, a ferromagnetic rod and a coil with windings. The movement of the rod changes mutual induction of the windings, amplitude modulation of the carrier frequency of the generator and unbalance of the differential diode bridge. The magnitude of the unbalance is recorded with the aid of appropriate units.

Animals↗