RESUMEN
Novel 2alpha-substituted 1alpha,25-dihydroxyvitamin D3 analogues were efficiently synthesized and their biological activities were evaluated. 2alpha-Methyl-1alpha,25-dihydroxyvitamin D3 (2), whose unique biological activities were previously reported, was modified to 2alpha-alkyl (ethyl and propyl) and 2alpha-hydroxyalkyl (hydroxymethyl, hydroxyethyl, and hydroxypropyl) analogues 3-7 by elongation of the alkyl chain and/or introduction of a terminal hydroxyl group. 2alpha-Hydroxypropyl-1alpha,25-dihydroxyvitamin D3 (7) exhibited an exceptionally potent calcium-regulating effect and a unique activity profile.
Asunto(s)
Calcitriol/química , Colecalciferol/análogos & derivados , Bioquímica/métodos , Calcitriol/metabolismo , Calcitriol/farmacología , Agonistas de los Canales de Calcio/química , Agonistas de los Canales de Calcio/metabolismo , Agonistas de los Canales de Calcio/farmacología , Diferenciación Celular/efectos de los fármacos , Colecalciferol/química , Colecalciferol/metabolismo , Colecalciferol/farmacología , Evaluación Preclínica de Medicamentos , Células HL-60/efectos de los fármacos , Humanos , Receptores de Calcitriol/metabolismo , Estereoisomerismo , Relación Estructura-Actividad , Vitamina D/análogos & derivados , Vitamina D/química , Proteína de Unión a Vitamina D/metabolismoRESUMEN
A 59-year-old man was hospitalized for rectal bleeding. Barium enema and proctoscopy revealed an elevated tumor, completely stenosing the rectum. The microscopic features of the specimens obtained by proctoscopic biopsy of the tumor comprised aggregations of histiocytes with intracytoplasmic inclusions (von Hansemann cells and Michaelis-Gutmann bodies). Rectal malacoplakia was diagnosed. In the course of laparotomy, the tumor was found to be strongly infiltrated to the pelvis. Thus, radical surgery was not performed, and an artificial anus was made. Excisional biopsy from the tumor tissue revealed the features of well-differentiated adenocarcinoma and malacoplakia. Forty-three cases of malacoplakia of the gastrointestinal tract from a review of the literature including ours were collected and discussed.
Asunto(s)
Adenocarcinoma/complicaciones , Malacoplasia/complicaciones , Enfermedades del Recto/complicaciones , Neoplasias del Recto/complicaciones , Adenocarcinoma/patología , Humanos , Malacoplasia/patología , Masculino , Persona de Mediana Edad , Enfermedades del Recto/patología , Neoplasias del Recto/patologíaRESUMEN
The macrophage inhibition test was carried out using colostral macrophages obtained from PPD sensitive and measles and mycoplasma pneumoniae antigen insensitive woman. The macrophage migration was inhibited by PPD but neither by measles nor by mycoplasma pneumoniae antigen. Human colostral macrophages can be used as indicator cells in migration inhibition tests.