Abstract:
:The quassinoids bruceantin, brucein D, brucein E, bruceoside A, and brusatol significantly inhibited P-388 lymphocytic leukemic cell RNA and protein synthesis in tissue culture. However, DNA synthesis inhibition seemed to correlate more directly with the anti-neoplastic activity of these compounds in the in vivo P-338 survival system. In vitro, brusatol and bruceoside A marginally inhibited 10-day P-388 lymphocytic leukemia DNA polymerase, RNA polymerase, thymidylate synthetase, dihydrofolate reductase, phosphoribosyl pyrophosphate aminotransferase, and cathepsin protease activities. In vivo studies demonstrated similar inhibition and elevated cyclic AMP levels, correlating positively with the antineoplastic activity of individual compounds. Purine synthesis was inhibited drastically by brusatol in vivo, and one key inhibition site in purine synthesis was at phosphoribosyl pyrophosphate aminotransferase, the regulatory enzyme. Histone phosphorylation and ribonucleotide reductase activity also were inhibited marginally by brusatol.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Hall IH,Lee KH,Eigebaly SA,Imakura Y,Sumida Y,Wu RYdoi
10.1002/jps.2600680726subject
Has Abstractpub_date
1979-07-01 00:00:00pages
883-7issue
7eissn
0022-3549issn
1520-6017pii
S0022-3549(15)42734-0journal_volume
68pub_type
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