Abstract:
:In this study the activity of KW-2149 and two of its metabolites, M-16 and M-18, was measured against cell lines with different types of resistance. The influence of these metabolites and of the exposure time on the cytotoxic efficacy of KW-2149 was investigated. Against the human ovarian carcinoma cell lines, AOvC and A2780, KW-2149 was more active than mitomycin C (MMC), with an IC50 of, respectively, 3.4 nM and 9.82 microM for KW-2149 and 18.2 nM and 67.71 microM for MMC. Activity of M-18 was significant against both cell lines and was comparable with that of KW-2149. Against an MMC-resistant cell line, AOvCMMC, the resistance factor (RF) for KW-2149 was 3.1 versus 8.0 for MMC. Tested against a cisplatin-resistant cell line, AOvCCDDP, KW-2149 had a RF of 7.7 versus 2.4 for MMC. Increasing the exposure time from 1 to 8 h decreased the RF for KW-2149 from 7.7 to 3.0. In an MDR mediated resistant cell line, A2780mdr+, prolongation of exposure time increased RF for KW-2149 and MMC but decreased RF for M-18 from 7.0 at 1 h to 5.3 at 8 h. Tested against a rat colon carcinoma cell line CC531, KW-2149 and M-18 again demonstrated superior or equal activity compared with MMC, IC50 being, respectively, 0.6, 2.1 and 2.6. Here again M-18 showed an aberrant sensitivity pattern, as its activity decreased with mdr-1 expression in contrast to the other mitomycins. Our data confirm the activity of KW-2149 as an agent with equal or superior activity as compared with MMC. It is concluded that the metabolite M-18 can contribute to the activity of KW-2149. Efficacy of both KW-2149 and its metabolites increases with increasing exposure times. The increments of exposure time appeared even as a means to overcome resistance in some instances.
journal_name
Anticancer Drugsjournal_title
Anti-cancer drugsauthors
Dirix LY,Gheuens EE,van der Heyden S,van Oosterom AT,De Bruijn EAdoi
10.1097/00001813-199406000-00013subject
Has Abstractpub_date
1994-06-01 00:00:00pages
343-54issue
3eissn
0959-4973issn
1473-5741journal_volume
5pub_type
杂志文章abstract::Glucocorticosteroids (GC) play an important role in the treatment of neuro-oncologic patients. GC are used for the management of malignant brain tumors, either primary of secondary, neoplastic epidural spinal cord compression (NESC), as adjuvant chemotherapy of some central nervous system tumors and perioperatively in...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/00001813-199502000-00002
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