RESUMO
New 5'-alkyl ethoxy- and aminocarbonylphosphonates of 3'-azido-3'-deoxythymidine (AZT) were synthesized, and their antiviral properties in HIV-1-infected cell cultures and stability to chemical hydrolysis were studied. The AZT 5'-aminocarbonylphosphonates were shown to be significantly more stable in phosphate buffer (pH 7.2) than the corresponding ethoxycarbonylphosphonates. The therapeutic (selectivity) index of some of the compounds exceeded that of the parent AZT due to their higher antiviral activity. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2004, vol. 30, no. 3; see also http://www.maik.ru.
Assuntos
Fármacos Anti-HIV/síntese química , Foscarnet/análogos & derivados , HIV-1/efeitos dos fármacos , Zidovudina/análogos & derivados , Fármacos Anti-HIV/farmacologia , Células Cultivadas , Humanos , Compostos Organofosforados/síntese química , Compostos Organofosforados/farmacologiaRESUMO
Phage display was used to obtain peptides mimicking a HIV-1 gp41 conserved epitope recognized by virus-neutralizing monoclonal antibodies (MCA) 2F5. Rabbits and mice were immunized with the peptides exposed on the surface of filamentous bacteriophages. Antibodies to gp41 were detected in the sera of immunized animals. The virus-neutralizing activity of the sera was examined.
Assuntos
Anticorpos Monoclonais/imunologia , Epitopos/imunologia , Proteína gp41 do Envelope de HIV/imunologia , HIV-1/imunologia , Mimetismo Molecular/imunologia , Peptídeos/imunologia , Sequência de Aminoácidos , Animais , Bacteriófagos/imunologia , Epitopos/química , Feminino , Soros Imunes , Imunização , Camundongos , Camundongos Endogâmicos C57BL , Dados de Sequência Molecular , Peptídeos/química , CoelhosRESUMO
The immunostimulating activity of triterpenes of vegetable origin and their derivatives was studied. The study revealed that glycyrrhizic and betulonic acids, as well as derivatives of ursolic and glycyrrhetinic acids, enhanced the level of specific antibodies to bovine serum albumin in mice.
Assuntos
Adjuvantes Imunológicos/farmacologia , Plantas/química , Triterpenos/farmacologia , Animais , Formação de Anticorpos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Soroalbumina Bovina/imunologiaAssuntos
Adjuvantes Imunológicos/farmacologia , Triterpenos/farmacologia , Adjuvantes Imunológicos/química , Animais , Formação de Anticorpos/efeitos dos fármacos , Linfócitos B/imunologia , Relação Dose-Resposta Imunológica , Imunidade Celular/efeitos dos fármacos , Técnicas Imunoenzimáticas , Masculino , Camundongos , Soroalbumina Bovina/imunologia , Triterpenos/química , Ácido UrsólicoRESUMO
Progesterone and glucocorticoid receptor levels were assayed in breast tumor. The progesterone levels in tumor were 1.2-2.5 times those in normal tissue sampled from the same patients. The binding of glycyrrhizic acid (GA) to cytoplasmic proteins (GA "receptor" levels) was studied using procedures for glucocorticoid receptor assay. The "receptor" concentrations in tumor tissue were 1.5-5 times that in normal one. The "receptors" were detected only in 5.9% of normal breast tissue samples. The Kd of GA-protein complex was ca.7 x 10(-8) M. GA seems to offer significant advantage as a drug-carrier involved in therapy of glucocorticoid-dependent breast cancer.
Assuntos
Neoplasias da Mama/química , Mama/química , Ácido Glicirrízico/análise , Receptores de Glucocorticoides/análise , Receptores de Progesterona/análise , Citoplasma , Feminino , Ácido Glicirrízico/metabolismo , Humanos , Ligação ProteicaRESUMO
A chronically HIV-1-infected culture of continuous human monocytes producing infectious virus during long-term continuous cultivation (over 200 passages) without the addition of noninfected cells was generated. HIV-1 produced by this culture had typical morphology and complete set of virus-specific proteins. This cell line is proposed for use as an additional model for the evaluation of antiviral effects of various drugs.