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1.
J Pharm Pharmacol ; 49(2): 216-22, 1997 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-9055199

RESUMO

The anti-tumour activity of acriflavine in combination with guanosine has been evaluated in solid or ascitic tumour-implanted animal models. Guanosine is known to potentiate the anti-tumour effects of some chemotherapeutic agents. Administration of acriflavine (15 mg kg-1 day-1, i.m., 14 days) to ICR mice subcutaneously implanted with Ehrlich carcinoma resulted in approximately 30% inhibition in tumour growth. In contrast, minor tumour growth inhibition was observed in animals treated with guanosine at the same daily dose. Treatment of animals with both acriflavine and guanosine (AG60, 1:1, w/w) at 30 mg kg-1 resulted in approximately 65% inhibition in tumour growth rate. Whereas treatment with acriflavine or guanosine resulted in 70% or 30% decrease in tumour weight, respectively, treatment of tumour-implanted mice with AG60 (30 mg kg-1) resulted in a 96% decrease in tumour weight, relative to control, 14 days after tumour-cell implantation. Dose-related inhibition in tumour growth rate was also observed in animals treated with AG60, with maximum (65%) inhibition noted at a dose of 30 mg kg-1 (ED50 23 mg kg-1). Suppression of body weight increase and elevated plasma glucose levels by acriflavine or AG60 indicated that glucose utilization might be impaired. The anti-tumour effect of AG60 was also determined in CDF1 mice intraperitoneally implanted with Ehrlich ascitic tumour. Ehrlich ascitic tumour proliferation was completely suppressed by AG60 (30 mg kg-1, i.p.). Microscopic analyses of intraperitoneal touch-prints revealed that AG60 was more effective in suppressing tumour proliferation than acriflavine alone. Fluorescent microscopic examinations demonstrated that acriflavine avidly bound with Yac-1 cell plasma membrane, leading to morphological changes in the cells, such as bleb formations, swelling and ballooning. The time-related changes in tumour cell morphology by acriflavine or AG60 might represent energy depletion, followed by osmotic lysis as a result of cationic influx. Enhanced anti-tumour activity of acriflavine in combination with guanosine might be explained by the blocking of nutrient transport through selective acriflavine binding with plasma membrane and by concomitant guanosine perturbation of cellular ATP production. This study demonstrates that guanosine enhances the anti-tumour effects of acriflavine against a variety of cancer cells without serious adverse effects, providing a preclinical basis for potential application of this combination against cancer proliferation.


Assuntos
Acriflavina/farmacologia , Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico , Guanosina/uso terapêutico , Acriflavina/administração & dosagem , Animais , Glicemia/efeitos dos fármacos , Carcinoma de Ehrlich/tratamento farmacológico , Relação Dose-Resposta a Droga , Sinergismo Farmacológico , Guanosina/administração & dosagem , Leucemia P388 , Masculino , Camundongos , Camundongos Endogâmicos ICR , Células Tumorais Cultivadas/efeitos dos fármacos
2.
Artigo em Inglês | MEDLINE | ID: mdl-705420

RESUMO

A total of 107 cases of trichomonas vaginitis were treated with different regimens of ornidazole. The overall success rate of the treatment assessed by wet smear and clinical signs after three days in 68 cases was 98.5%. The side effects were mild and of short duration. These were noted in 14.7% of the assessable cases. No significant differences were seen in the success rate between the three drug regimens and the preliminary conclusions of the trial are that ornidazole is safe and effective in the treatment of trichomonas vaginitis in Korean women with an oral dose of 1.0 gm, 1.0 gm plus 0.5 gm intravaginally or 2.0 gm given in a single day.


Assuntos
Nitroimidazóis/administração & dosagem , Ornidazol/administração & dosagem , Vaginite por Trichomonas/tratamento farmacológico , Adulto , Esquema de Medicação , Feminino , Humanos , Pessoa de Meia-Idade , Vaginite por Trichomonas/microbiologia
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