Letter: Bone-marrow response to endotoxin-stimulated nitroblue tetrazolium.
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Bone Marrow↗
Biomedical subjects
B Barbieri
Publications and source records attributed to B Barbieri.
[Study of the efficacy of l-sulpiride on dyspepsia and on the motor dynamics of the gallbladder. Controlled test versus domperidone].
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Adult↗
Synthesis, antitumor activity, and cardiac toxicity of new 4-demethoxyanthracyclines.
The new anthracycline glycosides 4-demethoxy-4'-deoxydaunorubicin and 4-demethoxy-4'-O-methyldaunorubicin, synthesized by coupling 4-demethoxydaunomycinone with 1-chloro-derivatives of protected 4-O-methyl and 4-deoxydaunosamine derivatives, have been converted into the corresponding doxorubicin analogs. The new compounds have been compared for antitumor effect with the parent drugs and with the previously described 4-demethoxydaunorubicin, 4-demethoxy-4'-epidaunorubicin, and their doxorubicin analogs. All of the new analogs were more cytotoxic against HeLa cells in vitro and were more toxic and more potent in mice than the parent drugs. Comparison at optimal antitumor doses showed that the new analogs were as active as the parent drugs against ascitic P388 leukemia and disseminated Gross leukemia. They were also active when administered orally. The new doxorubicin analogs were slightly more active than doxorubicin against ascitic L1210 leukemia and were markedly more active against disseminated L1210 leukemia. In a parallel activity-cardiotoxicity test in C3H mice repeatedly treated iv, 4-demethoxydoxorubicin, 4-demethoxy-4'-epidoxorubicin, 4-demethoxy-4'-O-methyldoxorubicin, and 4-demethoxy-4'-deoxydoxorubicin showed antitumor activity against mammary carcinoma without inducing the typical myocardial lesions observed after doxorubicin treatment, 4-Demethoxy-4'-O-methyldoxorubicin, because of its high antitumor effectiveness, lack of cardiac toxicity in mice, and activity by the oral route, deserves further study.
Animals↗
Possible relevance of N-trifluoroacetyladriamycin (AD 41) in the antitumoral activity of N-trifluoroacetyladriamycin-14-valerate (AD 32) in tumor-bearing mice. I. Pharmacokinetic evidence.
N-Trifluoroacetyladriamycin-14-valerate (AD 32) is an analog of doxorubicin whose chemico-physical characteristics are nontypical compared to the parent compound. Its most interesting feature is the lack of capacity to intercalate with DNA; thus, its mechanism of action as an antitumoral drug is still unknown. The N-trifluoroacetyl bond on the glycoside moiety is very stable and does not easily undergo enzymatic hydrolysis. Conversely, the valerate ester is split very rapidly by tissue and blood hydrolases. In this paper we present a kinetic study on AD 32, and we additionally follow the formation and disappearance of its metabolite, N-trifluoroacetyladriamycin (AD 41). Peak levels, areas under the curve, and beta-half-lives of AD 32 and AD 41 after an iv injection of 80 mg/kg of AD 32 to Lewis lung carcinoma-bearing mice are presented. The results indicated very rapid disappearance of AD 32 from blood and tissues, whereas AD 42 persisted for much longer. Moreover, all of the tissues taken into consideration were able to hydrolyze AD 32 to AD 41, suggesting that this compound plays an important role in the antitumoral activity of AD 32.
Animals↗