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  • apoptotic cell
  • A 1.5-fold higher apoptotic effect compared with melphalan was induced by 120 μg/mL of the 50% ethanol-water extract of CF. The apoptotic cell death in HepG2 cells occurred via extrinsic and intrinsic caspase-dependent pathways in dose- and time-dependent manners by significantly increasing the activities of caspase 3/7, 8, and 9, decreasing the mitochondrial membrane potential, and causing apoptotic body formation and DNA fragmentation. (biomedcentral.com)
  • Combining 4-HC with either F-ara-A or Cl-F-ara-A produced more than additive apoptotic cell death than the sum of each alone. (aacrjournals.org)
  • tumors
  • Cyclic imides such as N-substituted alkyl ethers, thioethers, sulfoxides, sulfones and related derivatives were potent agents against human single cell tumors and selected solid tumor growths, eg adenocarcinoma of the colon and glloma. (ovid.com)
  • Although administration of bLF and P-B alone suppressed DMBA-induced HBP tumors, combined administration of bLF and P-B was more effective in inhibiting HBP carcinogenesis by inhibiting oxidative DNA damage, carcinogen activation, cell proliferation, invasion, and angiogenesis. (cognizantcommunication.com)
  • Increased activity of GSH/GSTs in comparison to normal tissues has been found in several tumor tissues comprising, for instance, gastrointestinal tumors (including esophageal, gastric, colon, hepatocellular and pancreatic), uterine and ovarian cancers, head and neck cancer, lung and NSCL carcinomas as well as met static liver tumors originating from the colon, stomach and bladder [Cancer Res. (allindianpatents.com)
  • The drug shows high potency and activity in various experimental models including P-gp- and MRP1-expressing multidrug resistant tumors as well as tumors resistant to platinum derivatives, alkylating agents and topoisomerase I and II inhibitors. (aacrjournals.org)
  • Etoposide was approved by FDA in 1983 for use in patients with refractory testicular tumors, small-cell lung cancer, nonlymphocytic leukemias, and non-Hodgkins lymphoma (424). (quackwatch.org)
  • enzyme
  • when cytosine arabinoside or deoxyguanosine was used as the substrate, the kinase activity in the extracts from the dGuo-R cells was only 10% of the enzyme activity in the extracts from the wild-type cells. (ecu.edu)
  • The apoptosis induction mechanisms were investigated through nuclear morphological changes, DNA fragmentation, mitochondrial membrane potential alterations, and caspase enzyme activities. (biomedcentral.com)
  • The activities associated with this enzyme include an NADP-dependent dehydrogenase, a cyclohydrolase and a synthetase. (aspetjournals.org)
  • resistance
  • The dGuo-R cell line showed an increased level of resistance to 2-fluoro-2'-deoxyadenosine and 2-fluoroadenine arabinoside (11-14-fold), but essentially no increase in resistance to deoxyadenosine or adenine arabinoside. (ecu.edu)
  • Chronic lymphocytic leukemia (CLL) lymphocytes respond to DNA alkylation by excision repair, with the extent of repair increasing as the cells acquire resistance to alkylating agents. (aacrjournals.org)
  • The first of them involved studies in which elevated levels or expression and activity of GSH/GSTs were correlated with increased levels of drug resistance. (allindianpatents.com)
  • This approach also included modulation of GSH/GSTs activity by means of GSH inhibitors such as BSO (buthionine sulphoximine), in order to circumvent or reverse drug resistance. (allindianpatents.com)
  • Recently, the role of GSH in dmg resistance has been linked to the regulation of the activity of the multi-drug resistance-associated proteins (IVIRP) which confer resistance to different cytotoxics including anthracyclines (e.g. doxorubicin, idarubicin, epirubicin and donatives thereof), epidophyllotoxins (e.g. etoposide and teniposide), Vince alkaloids (e.g. vinblastine and vincrisdne) and tisanes (e.g. paclitaxel and docetaxel) [Eur. (allindianpatents.com)
  • Studies are in progress to determine the methylation status of the XPG gene in the nemorubicin-resistant cell line.In conclusion, these results further corroborate the unique mechanism of action of nemorubicin and identify a novel mechanism of drug resistance through the genetic silencing of a DNA repair gene. (aacrjournals.org)
  • Moreover, a growing body of evidence implies that a variety of miRNAs suppress malignant phenotypes of pancreatic cancer cells including drug resistance through the down-regulation of RUNX2. (beds.ac.uk)
  • compounds
  • Keywords: Boron, anti-neoplastic, leukemia, topoisomerase 11, RNA polymerase, DNA polymerases, acute toxicity INTRODUCTION There is rapidly growing interest in the biological activity of boron compounds in animals, including humans. (docme.ru)
  • Lastly, boron compounds have been found to possess potent pharmacological activity (e.g. anti-inflammatory, analgesic, hypolipidemic, etc.) in animal model studies. (docme.ru)
  • Boron compounds, ranging from analogs of the a-amino-acids, peptides, neurotransmitters (e.g. acetylcholine) to boronated DNA, have been prepared and tested for their biological In view of this promising pharmacological activity, we have been carrying out studies on select compounds to establish further their mode of action and acute toxicity. (docme.ru)
  • Furthermore, whereas many agents currently entering clinical trials are said to be cytostatic, the data to be presented show that many if not all of these compounds possess cytotoxic activity that is at least as important if not more so than any cytostatic property. (aacrjournals.org)
  • neoplastic cells
  • Pubmed ID: 24778021 Sonodynamic therapy (SDT) is a form of ultrasound therapy in which chemotherapeutic agents known as sonosensitizers are administered to increase the efficacy of ultrasound's preferential damage to neoplastic cells. (jove.com)
  • There is abundant evidence of critical cytoskeletal differences involving microfilaments between normal and neoplastic cells, and a variety of natural products and semi-synthetic derivatives are available to exploit these differences in vitro. (jove.com)
  • potent
  • One analogue, LY354899, was a potent inhibitor of the dehydrogenase activity isolated from porcine liver (IC 50 = 100 nM), but was less active against the synthetase and cyclohydrolase activities. (aspetjournals.org)
  • In this study, we confirm that LY354899 is a potent inhibitor of C1-synthase dehydrogenase, but is only weakly antiproliferative toward CCRF-CEM lymphocytic leukemia cells. (aspetjournals.org)
  • topoisomerase
  • F14512 combines an epipodophyllotoxin core-targeting topoisomerase II with a spermine moiety introduced as a cell delivery vector. (topogen.com)
  • cytotoxic effects
  • Prolonged time to progression and improved overall survival have been recently reported using novel targeted therapies, and it has been argued that this effect is totally or partially mediated by cancer cell cytostasis without direct cytotoxic effects. (aacrjournals.org)
  • protein
  • The iL3 peptide fusion protein (iL3-L12-h b 2 m) was developed based on the mutant iL3 peptide, derived from the L3 ribosomal protein, and expressed in the mutagenized murine fibroblastic tumor cell line, BCA34. (cognizantcommunication.com)
  • The iL3-L12- b 2 m and a negative control fusion protein utilizing the H-2K d -restricted NP (147-155) influenza peptide (NPL12-h b 2 m) were both produced in E. coli for exogenous antigen presentation by dendritic cells. (cognizantcommunication.com)
  • In vitro, the iL3-L12-h b 2 m protein was found to stabilize H-2K d over time on the surface of H-2K d -expressing target cells and sensitized them to peptide-specific CTL-mediated lysis. (cognizantcommunication.com)
  • molecular analysis of these defects highlighted XPG as a crucial gene, being expressed at the protein level in L1210 wild type cells but not in the nemorubicin-resistant subline. (aacrjournals.org)
  • molecular
  • Molecular mechanisms of cytostasis will be analyzed, including interference with the cell cycle as well as putative links with necrosis and autophagy. (aacrjournals.org)
  • Therefore, it is urgent to develop novel treatment options against pancreatic cancer, and also to understand the precise molecular mechanisms how pancreatic cancer cells could acquire and maintain GEM-resistant phenotype. (beds.ac.uk)
  • Since p53, which monitors and ensures the genomic integrity, is an essential molecular barrier against carcinogenesis [ 8 , 9 ], it is possible that loss of function mutation of p53 leads to the accumulation of genetic damage within pancreatic cancer cells, and thus they might acquire GEM-resistant property as well as metastatic potential. (beds.ac.uk)
  • extracts
  • the Km values for deoxycytidine and cytosine arabinoside were increased in the extracts from the dGuo-R cells. (ecu.edu)
  • By use of high-performance liquid chromatography, the kinase activities in the extracts from the wild-type and resistant cells could be resolved. (ecu.edu)
  • analogues
  • Because incorporation of nucleotide analogues into the repair patches elicits death signals in quiescent cells, the increased capacity for excision repair in alkylator-resistant cells could facilitate incorporation of nucleotide analogues. (aacrjournals.org)
  • We hypothesized that the mechanism-based interaction of nucleoside analogues with alkylating agents could elicit greater than additive killing of CLL cells. (aacrjournals.org)
  • Recently, purine nucleoside analogues have been shown to be efficacious in the therapy of CLL and other indolent B-cell malignancies. (aacrjournals.org)
  • kinase
  • There was the specific loss of kinase activity toward cytosine arabinoside and deoxyguanosine as substrates. (ecu.edu)
  • These data indicate that the dGuo-R cells have decreased levels of a specific deoxyribonucleoside kinase activity. (ecu.edu)
  • IC50
  • The IC50 values for araC and araG were increased, but only 10-12-fold in the dGuo- R cells when compared with the wild-type cells. (ecu.edu)
  • serum
  • Serum effect on cellular uptake of spermidine, spergualin, 15-deoxyspergualin, and their metabolites by L5178Y cells. (semanticscholar.org)
  • Addition of calf serum stimulated uptake of [3H]spermidine into the cells in a serum concentration-dependent manner. (semanticscholar.org)
  • assay
  • In addition, these cells are not able to repair UV-induced damage on transfected DNA (host -cell reactivation assay), suggesting that the NER system might be involved in mediating the cytotoxic activity of nemorubicin. (aacrjournals.org)