Analgesic Activity of Hexaazaisowurtzitane Derivatives.

Pronounced analgesic activity of the innovative compound 4-(3,4-dibromthiophencarbonyl)-2,6,8,12-tetraacethyl-2,4,6,8,10,12hexaazatetracyclo[5,5,0,03, 11,05, 9] dodecane (thiowurtzine) was observed in the thermal nociceptive hot plate test and in the acute visceral and somatic deep pain model (acetic acid writhing test). In these experimental models, naloxone-sensitive thiowurtzine-induced analgesia was revealed. The absence of tropism to peripheral opioid receptors in the acetic acid writhing test was demonstrated using naloxone methiodide. Course administration of low-toxic thiowurtzine in effective doses was not associated with ulcerogenic damage to the gastric mucosa in experimental animals.

Effect of Acorus calamus L. Polysaccharide on CD274 and CD326 Expression by Lewis Lung Carcinoma Cells in Mice.

Tumor cells can maintain their growth via immunosuppression and escape from host antitumor immunity by controlling the PD-1/PD-L1 system. Expression of PD-L1 (CD274) is an inhibitory signal for T cells, while the increase in CD326 expression in the tumor tissue correlates with metastasis development. The experimental preparation on the basis of α(1,2)-L-rhamno-α(1,4)-D-galactopyranosyluronan from Acorus calamus L. produces an antitumor effect: it reduces tumor node size and the number and area of metastases after transplantation of Lewis lung carcinoma. Using flow cytometry, we demonstrated a decrease in the population of tumor cells expressing surface CD274 (PD-L1) and CD326 antigens after 20-day course of α(1,2)-L-rhamno-α(1,4)-D-galactopyranosyluronan.

Anti-Inflammatory and Analgesic Activities of the Complex of Flavonoids from Lychnis chalcedonica L.

Anti-inflammatory and analgesic activities of the complex of flavonoids from Lychnis chalcedonica L. were studied in the models of acute aseptic inflammation induced by carrageenan, histamine, and serotonin and acetic acid-induced painful chemical stimulation. It is demonstrated that course treatment with flavonoids derived from Lychnis chalcedonica L. produced a stable pharmacological effect comparable with that of the reference anti-inflammatory drug diclofenac.

Antitumor Effects of JAK3 Inhibitor on the Model of Transplantable Lewis Lung Carcinoma and Mechanisms of Their Development.

Mice with Lewis lung carcinoma were used to study the antitumor and antimetastatic effects of JAK3 inhibitor. The study revealed no effect of JAK3 inhibitor on the growth of primary tumor node, but found a pronounced inhibition of hematogenous spread of the pathologic process into the lungs. In vitro blockade of JAK3 in cultured Lewis lung carcinoma produced no effect on the count of the stem tumor cells and stimulated functions of committed elements. In addition, blockade of JAK3 significantly elevated maturation index of the tumor tissue.

Effects of Cichorium Intybus L. Root Extract on Secretory Activity of the Stomach in Health and Ulcer Disease.

Gastroprotective effect of Cichorium intybus L. root extract is demonstrated on H. Shay's model of experimental ulcer in rats. The effect is attributed to the antisecretory activity of the plant and stimulation of defense barrier function of the gastric mucosa. The regulatory effect of the phytocomplex on seasonal characteristics of the gastric secretory and defense functions in dogs with Basov's fistula is detected.

Antiulcer activity of extracts of ecdysteroid-containing plants of genera Lychnis and Silene of the Caryophyllaceae family.

We studied antiulcer activity of the extracts of ecdysteroid-containing plants of the Caryophyllaceae family: Lychnis chalcedonica L., Silene viridiflora L.Sp.Pl., and Silene frivaldszkyana Hampe. Experiments on the model of neurogenic and aspirin-induced ulcerogenesis showed unidirectional and pronounced gastroprotective effects of S. viridiflora and L. chalcedonica extracts comparable to the efficacy of famotidine. In these models, a course of intragastric treatment with the extracts reduced ulcerative lesions of all types.

Effects of nonstarch polysaccharides with different molecular weights on the development of Lewis lung carcinoma in mice and efficiency of cytostatic therapy.

The effects of nonstarch polysaccharides with different molecular weights on the development of Lewis' lung carcinoma and efficiency of cyclophosphamide therapy in mice were studied. Treatment with these substances with low molecular weights (<30 kDa) caused no changes in the primary tumor growth, but inhibited its metastasizing, while nonstarch polysaccharides with high molecular weights (>400 kDa) inhibited the growth of Lewis' lung carcinoma node. Antimetastatic effects of cyclophosphamide were stimulated by low and high molecular weight polysaccharides.

Comparative evaluation of the efficiency of various alginate forms under conditions of an oncological experiment.

The effects of various alginate forms on the development of transplanted tumors in mice and efficiency of cytostatic therapy were studied. High-molecular-weight Ca and Na alginates, acid-soluble hydrolysate, and sodium alginate fraction inhibited the growth of Ehrlich adenocarcinoma. The use of acid-insoluble sodium alginate in chemotherapy protocol improved the treatment efficiency. All alginate forms inhibited metastasizing of Lewis pulmonary carcinoma; in combination with cyclophosphamide they potentiated its antimetastatic effect.

[Effect of ginsenoside Rh2 on the development of transferred tumors and chemotherapy efficiency].

Experiments on C57B1/6 mice showed that ginsenoside Rh2 inhibited the growth and metastasis process of Lewis lung tumor and increased the antitumor and antimetastatic effects of cyclophosphamide. On the model of transferred melanoma B-16, ginsenoside Rh2 showed a tendency to increase the antiblastome effect of the cytostatic drug.

[Anti-ulcerative effect of non-starch polysaccharides].

Standard models of experimental ulceration (of neurogenic origin, H. Shay ulcer, indomethacine-, ethanol-, prednisolone-, histamine- and acetate-induced ulcers) were used to demonstrate protective effect of non-starch polysaccharides (potassium alginate, potassium pectate, low-esterified pectin). Potassium pectate proved to be the most efficacious protector. Mechanism of its anti-ulcerative action is attributable to antacidic, cytoprotective, and reparative activity. It appeals to optimally stimulate the motor-evacuation function and, besides, exhibits marked anti-inflammatory activity.

[Antiulcer effect of calcium pectate on model of chronic gastric ulcer in rats].

Calcium pectate has been found to exhibit an antiulcer activity in rats with model of chronic ulcers. Course treatment of the experimental animals with calcium pectate (i) accelerated the repair of experimental damage due to better integrity and higher secretory activity of epithelium and (ii) decreased hemodynamic disorders in surrounding mucous and epithelial membranes. The maximum effect, which was achieved with calcium pectate in a dose of 50 mg/kg, exceeded the action of the reference drug maalox on both 14th and 21st days of experiment.

Effect of ultralow doses of antibodies to histamine on the development of chronic ulcerative process in the stomach of experimental animals.

Antiulcer activity of ultralow doses of antibodies to histamine was demonstrated on the model of chronic acetate-induced gastric ulcer in rats. Course therapy with the preparation accelerated healing of chronic experimental ulcer by correcting hemodynamic disturbances and stimulating mucus formation in the gastric wall.

Gastroprotective effect of nonstarch polysaccharide calcium pectate under experimental conditions.

Course prophylactic administration and single therapeutic treatment with calcium pectate improved resistance of rat gastroduodenal mucosa to ethanol-induced ulcers, prednisolone-induced ulcers, and H. Shay ulceration of the gastric mucosa.

Licorice preparations improve efficiency of chemotherapy and surgical treatment of transplanted tumors.

Experiments on animals with Lewis lung carcinoma and Ehrlich tumor showed that licorice (glycyrrhiza) extract and glyciram prepared from this plant improved the antitumor effect of cyclophosphamide. Glyciram reduced the toxic effect of the cytostatic on peripheral blood leukocytes. Licorice extract inhibited the growth of Ehrlich tumor and development of metastases in mice with Lewis lung carcinoma. Glyciram administered to mice after removal of Lewis lung carcinoma produced an antimetastatic effect and prevented relapses.

[Experimental evaluation of the antiulcer activity of calcium pectate].

Both chronic (prophylactic) and single administration of standardized calcium pectate considerably increased the resistance of rat stomach mucous membrane with respect to ulcerogenic factors of various etiology, including immobilized stress, indomethacin, ethanol, prednizolone, and histamine, according to H. Shay's model. The gastroprotective effect of this polysaccharide was comparable with or exceeded the action of famotidine, sea buckthorn oil, and maalox.

[Effect of Echinacea purpurea tincture and its polysaccharide complex on the efficacy of cytostatic therapy of transferred tumors].

Experiments on C57LB/6 mice with transplanted Luis lung carcinoma showed that the officinal Echinacea purpurea preparation did not influence the efficacy of cytostatic therapy. This echinacea preparation did not change the development of metastases and even stimulated the tumor growth. In contrast, a hydrophilic polysaccharide complex isolated from echinacea increased the antitumor and antimetastatic activity of cyclophosphamide.

[Effect of dry aspen bark extract on the motor function of gastrointestinal tract in mice].

Experiments on mice (both intact and those with reserpine induced gastric ulcers) showed that dry aspen bark (DAB) extract stimulated the motor gastric activity. The DAB preparation produced a moderate purgative effect.

[Carbohydrate and lipid metabolism in patients with metabolic syndrome].

The article presents results on the study on the state of carbohydrate and lipid metabolism in patients with arterial hypertension (AH) and a metabolic syndrome (MC), verified according to criteria NCEP ATP III (2001) in the presence of insulin resistance confirmed by HOMA-IR index Metabolic disorders were revealed both in patients with AH, and in patients with MC. These disorders have the unidirectional character and differ not qualitatively but quantitatively and according to the correlation and dispersive analysess, in many respects are defined by concomitant diseases of the digestive tract, hepatobiliary system, pancreas and nephropathy which is typical for patients with II stage AH.

Gastroprotective effect of natural non-starch polysaccharides.

Experiments on mice and rats with modeled neurogenic and indomethacin-induced injuries to the gastric mucosa showed that preventive courses of calcium alginate, calcium pectate, and low-esterified pectin improved the resistance of the gastroduodenal mucosa to the destructive effect of the above factors.

Non-starch polysaccharides as correctors in cytostatic therapy of experimental tumors.

We studied the effects of low-esterified pectin, calcium pectate, and alginate on the development of transplanted Ehrlich adenocarcinoma and Lewis pulmonary carcinoma and on the efficiency of cyclophosphamide treatment in mice.