RESUMO
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.
Assuntos
Analgésicos/uso terapêutico , Dor/tratamento farmacológico , Animais , Modelos Animais de Doenças , Mucosa Gástrica/efeitos dos fármacos , Masculino , Camundongos , Naloxona/uso terapêutico , Dor/fisiopatologia , Medição da Dor/métodosRESUMO
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.
Assuntos
Acorus/química , Antineoplásicos Fitogênicos/administração & dosagem , Antígeno B7-H1/metabolismo , Carcinoma Pulmonar de Lewis/tratamento farmacológico , Molécula de Adesão da Célula Epitelial/metabolismo , Animais , Antígeno B7-H1/genética , Carcinoma Pulmonar de Lewis/metabolismo , Carcinoma Pulmonar de Lewis/patologia , Linhagem Celular Tumoral , Molécula de Adesão da Célula Epitelial/genética , Feminino , Camundongos Endogâmicos C57BL , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Ratos , Carga Tumoral , Ensaios Antitumorais Modelo de XenoenxertoRESUMO
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.
Assuntos
Analgésicos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Carragenina/toxicidade , Flavonoides/uso terapêutico , Inflamação/tratamento farmacológico , Lychnis/química , Ácido Acético/toxicidade , Animais , Diclofenaco/uso terapêutico , Feminino , Histamina/toxicidade , Inflamação/induzido quimicamente , Masculino , Camundongos , Serotonina/toxicidadeRESUMO
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.
Assuntos
Carcinoma Pulmonar de Lewis/tratamento farmacológico , Carcinoma Pulmonar de Lewis/enzimologia , Inibidores Enzimáticos/uso terapêutico , Janus Quinase 3/antagonistas & inibidores , Animais , Inibidores Enzimáticos/farmacologia , Feminino , Camundongos , Camundongos Endogâmicos C57BL , Células-Tronco Neoplásicas/efeitos dos fármacos , Células-Tronco Neoplásicas/metabolismoRESUMO
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.
Assuntos
Antiulcerosos/farmacologia , Cichorium intybus/química , Mucosa Gástrica/efeitos dos fármacos , Fitoterapia , Extratos Vegetais/farmacologia , Úlcera Gástrica/tratamento farmacológico , Animais , Antiulcerosos/isolamento & purificação , Carbacol/farmacologia , Cães , Famotidina/farmacologia , Feminino , Fístula Gástrica , Suco Gástrico/química , Suco Gástrico/efeitos dos fármacos , Suco Gástrico/metabolismo , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patologia , Masculino , Extratos Vegetais/isolamento & purificação , Raízes de Plantas/química , Ratos , Ratos Sprague-Dawley , Estações do Ano , Estômago/efeitos dos fármacos , Estômago/patologia , Úlcera Gástrica/patologiaRESUMO
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.
Assuntos
Antiulcerosos/farmacologia , Ecdisteroides/análise , Lychnis/química , Extratos Vegetais/farmacologia , Silene/química , Úlcera Gástrica/prevenção & controle , Animais , Etanol , Feminino , Camundongos , Espectrofotometria Ultravioleta , Estatísticas não ParamétricasRESUMO
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.
Assuntos
Carcinoma Pulmonar de Lewis/tratamento farmacológico , Ciclofosfamida/uso terapêutico , Polissacarídeos/uso terapêutico , Animais , Carcinoma Pulmonar de Lewis/patologia , Sinergismo Farmacológico , Feminino , Camundongos , Camundongos Endogâmicos C57BL , Peso MolecularRESUMO
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.
Assuntos
Alginatos/uso terapêutico , Animais , Carcinoma de Ehrlich/tratamento farmacológico , Carcinoma Pulmonar de Lewis/tratamento farmacológico , Feminino , Ácido Glucurônico/uso terapêutico , Ácidos Hexurônicos/uso terapêutico , Masculino , Transplante de NeoplasiasRESUMO
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.
Assuntos
Antineoplásicos/farmacologia , Carcinoma Pulmonar de Lewis/tratamento farmacológico , Citostáticos/farmacologia , Ginsenosídeos/farmacologia , Animais , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Melanoma/tratamento farmacológico , CamundongosRESUMO
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.
Assuntos
Alginatos/uso terapêutico , Materiais Biocompatíveis/uso terapêutico , Esvaziamento Gástrico/efeitos dos fármacos , Pectinas/uso terapêutico , Polissacarídeos/uso terapêutico , Úlcera Gástrica/tratamento farmacológico , Administração Oral , Alginatos/administração & dosagem , Animais , Antidiarreicos/administração & dosagem , Antidiarreicos/uso terapêutico , Materiais Biocompatíveis/administração & dosagem , Modelos Animais de Doenças , Portadores de Fármacos , Feminino , Ácido Glucurônico/administração & dosagem , Ácido Glucurônico/uso terapêutico , Ácidos Hexurônicos/administração & dosagem , Ácidos Hexurônicos/uso terapêutico , Masculino , Camundongos , Pectinas/administração & dosagem , Polissacarídeos/administração & dosagem , Ratos , Ratos Wistar , Úlcera Gástrica/fisiopatologia , Resultado do TratamentoRESUMO
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.
Assuntos
Antiulcerosos/uso terapêutico , Mucosa Gástrica/efeitos dos fármacos , Pectinas/uso terapêutico , Úlcera Gástrica/tratamento farmacológico , Acetatos , Hidróxido de Alumínio/uso terapêutico , Animais , Doença Crônica , Modelos Animais de Doenças , Combinação de Medicamentos , Mucosa Gástrica/patologia , Hidróxido de Magnésio/uso terapêutico , Masculino , Ratos , Ratos Wistar , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/patologiaRESUMO
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.
Assuntos
Antiulcerosos/imunologia , Antiulcerosos/uso terapêutico , Anticorpos/imunologia , Anticorpos/uso terapêutico , Histamina/imunologia , Úlcera Gástrica/tratamento farmacológico , Animais , Masculino , RatosRESUMO
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.
Assuntos
Mucosa Gástrica/efeitos dos fármacos , Pectinas/farmacologia , Úlcera Péptica/tratamento farmacológico , Animais , Antiulcerosos/farmacologia , Antiulcerosos/uso terapêutico , Etanol , Feminino , Mucosa Gástrica/patologia , Mucosa Intestinal/efeitos dos fármacos , Mucosa Intestinal/patologia , Masculino , Pectinas/uso terapêutico , Úlcera Péptica/induzido quimicamente , Ratos , Resultado do TratamentoRESUMO
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.
Assuntos
Antineoplásicos/uso terapêutico , Carcinoma de Ehrlich/tratamento farmacológico , Carcinoma de Ehrlich/cirurgia , Carcinoma Pulmonar de Lewis/tratamento farmacológico , Carcinoma Pulmonar de Lewis/cirurgia , Glycyrrhiza/química , Transplante de Neoplasias , Animais , Carcinoma de Ehrlich/patologia , Carcinoma Pulmonar de Lewis/patologia , Feminino , Ácido Glicirretínico/uso terapêutico , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Endogâmicos CBA , Metástase Neoplásica/tratamento farmacológico , Extratos Vegetais/uso terapêuticoRESUMO
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.
Assuntos
Antiulcerosos/uso terapêutico , Pectinas/uso terapêutico , Úlcera Gástrica/prevenção & controle , Animais , Feminino , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/patologia , Masculino , Camundongos , Ratos , Ratos Wistar , Úlcera Gástrica/etiologia , Úlcera Gástrica/patologiaRESUMO
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.
Assuntos
Antineoplásicos/uso terapêutico , Carcinoma Pulmonar de Lewis/tratamento farmacológico , Ciclofosfamida/uso terapêutico , Echinacea/química , Polissacarídeos/uso terapêutico , Animais , Antineoplásicos/isolamento & purificação , Feminino , Camundongos , Camundongos Endogâmicos C57BL , Extratos Vegetais/uso terapêutico , Polissacarídeos/isolamento & purificaçãoRESUMO
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.
Assuntos
Intestino Delgado/efeitos dos fármacos , Casca de Planta/química , Extratos Vegetais/uso terapêutico , Salicaceae/química , Úlcera Gástrica/tratamento farmacológico , Animais , Feminino , Trato Gastrointestinal/efeitos dos fármacos , Masculino , Camundongos , Camundongos Endogâmicos CBA , Extratos Vegetais/farmacologia , Reserpina/toxicidade , Úlcera Gástrica/induzido quimicamenteRESUMO
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.
Assuntos
Metabolismo dos Carboidratos , Hipertensão/metabolismo , Resistência à Insulina , Metabolismo dos Lipídeos , Síndrome Metabólica/metabolismo , Adulto , Idoso , Glicemia/análise , Feminino , Humanos , Insulina/sangue , Masculino , Síndrome Metabólica/diagnóstico , Pessoa de Meia-Idade , Obesidade/metabolismo , Índice de Gravidade de DoençaRESUMO
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.
Assuntos
Mucosa Gástrica/efeitos dos fármacos , Polissacarídeos/farmacologia , Substâncias Protetoras/farmacologia , Animais , Feminino , Mucosa Gástrica/patologia , Masculino , Ratos , Restrição Física , Caracteres Sexuais , Estresse PsicológicoRESUMO
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.