RESUMO
The antibiotic acetomycin was active in vitro against HCT-8 human colon adenocarcinoma cells (IC50, 1.5 microgram/ml) and L1210 murine leukemia cells (IC50, 2.2 micrograms/ml). Acetomycin also had marked activity in the human tumor stem cell assay, with a 33% overall response rate (less than or equal to 30% survival) against 49 primary tumors. However, acetomycin was inactive in four in vivo tumor assay systems (L1210 and P388 leukemias, B16 melanoma and the MX-1 mammary xenograft system). This lack of in vivo activity may result from metabolic inactivation of acetomycin.
Assuntos
Antibióticos Antineoplásicos/uso terapêutico , Leucemia L1210/tratamento farmacológico , Adenocarcinoma , Animais , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Neoplasias do Colo , Furanos/farmacologia , Furanos/uso terapêutico , Humanos , Camundongos , Ensaio Tumoral de Célula-TroncoRESUMO
The isolation and characterization of the title antibiotics, which are produced by the same Streptomyces sp., is described. The potent antitumor agent, PD 124,895, is an analog of hydroxyelactocin (PD 114,721). PD 124,966 is a new member of the depsipeptide family of antibiotics.
Assuntos
Antibióticos Antineoplásicos/isolamento & purificação , Peptídeos Cíclicos , Animais , Antibióticos Antineoplásicos/farmacologia , Fenômenos Químicos , Química , Ácidos Graxos Insaturados/isolamento & purificação , Ácidos Graxos Insaturados/farmacologia , Espectroscopia de Ressonância Magnética , Camundongos , Peptídeos/isolamento & purificação , Peptídeos/farmacologia , Streptomyces/metabolismoRESUMO
Two antibiotics were isolated from culture broths of a Streptomyces sp. and identified as 8"-hydroxypactamycin and 7-deoxypactamycin. The latter antibiotic was shown to be identical to cranomycin. An additional compound, 8"-hydroxypactamycate, was also isolated.
Assuntos
Antibióticos Antineoplásicos/isolamento & purificação , Pactamicina/isolamento & purificação , Antibióticos Antineoplásicos/farmacologia , Fenômenos Químicos , Química , Pactamicina/análogos & derivados , Streptomyces/metabolismoRESUMO
A new, highly substituted phenazine with antitumor activity was isolated from the culture broth of a Streptomyces sp. This compound, whose structure was determined by spectroscopic methods and verified by X-ray diffraction analysis, was found to be methyl 6-formyl-4,7,9-trihydroxy-8-methyl-1-phenazinecarboxylate.
Assuntos
Antibióticos Antineoplásicos , Antibióticos Antineoplásicos/farmacologia , Fenômenos Químicos , Química , Espectroscopia de Ressonância Magnética , Modelos Estruturais , Fenazinas/farmacologia , Difração de Raios XAssuntos
Antibióticos Antineoplásicos/isolamento & purificação , Adenocarcinoma/tratamento farmacológico , Animais , Antraquinonas/isolamento & purificação , Antraquinonas/uso terapêutico , Antibióticos Antineoplásicos/uso terapêutico , Fenômenos Químicos , Química , Neoplasias do Colo/tratamento farmacológico , Humanos , Leucemia L1210/tratamento farmacológicoRESUMO
The isolation and properties of PD 118,576, a new cytotoxic antibiotic obtained from the culture broth of a Streptomyces sp., are described. The structure of this compound was established by spectral analyses of the parent compound and its tri-O-acetyl derivative. PD 118,576 proved to be related to the bafilomycins and therefore is a new member of this recently discovered family of macrolide antibiotics.
Assuntos
Antibacterianos , Antibióticos Antineoplásicos/isolamento & purificação , Macrolídeos , Streptomyces/metabolismo , Acetilação , Fenômenos Químicos , Química , Cetonas/isolamento & purificação , Espectroscopia de Ressonância MagnéticaRESUMO
A new antibiotic, PD 113,876, was isolated from the culture broth of a Streptomyces sp. and was shown by X-ray diffraction analysis to be the N-7 oxide of guanine. This novel antimetabolite is very active in vivo against L1210 lymphocytic leukemia.
Assuntos
Antibióticos Antineoplásicos/isolamento & purificação , Guanina/análogos & derivados , Streptomyces/metabolismo , Animais , Antibióticos Antineoplásicos/farmacologia , Fermentação , Guanina/isolamento & purificação , Leucemia L1210/tratamento farmacológico , Camundongos , Difração de Raios XRESUMO
A dry column chromatographic procedure is described. It allows for the rapid concentration of biologically active materials in natural products fractionation. The potential value of the technique is described, utilizing as an example the separation of an anticancer active fraction obtained from Euphorbia cyparissias.
