Authors: A Yajima, H Higashiiwai, A Sato...

Among the 95 cases of ovarian cancer treated by us between May, 1975 and August, 1978, only 33 were suitable for complete resection. The remaining 62 cases underwent incomplete resection, followed by F.Q.C. combination chemotherapy (1-(2-tetrahydrofuryl)-5-fluorouracil, carbazilquinone, cytosine arabinoside); 54.8% showed an antitumor response. The median survival time of the responders was 13.2 months, whereas it was 7.4 months for the non-responders. The survival rate after 24 months, however, was 13% and 4%, respectively. Side effects of the drugs, including leucopenia, thrombocytopenia, nausea and vomiting, were found in roughly one half of the cases.

Topics: Antineoplastic Agents; Carbazilquinone; Cytarabine; Drug Therapy, Combination; Female; Humans; Ovarian Neoplasms; Tegafur

PubMed: 6777904
DOI: 10.1620/tjem.132.225

Clinical Trial

Authors: T Takenaka, K Maruyama, T Kinoshita...

The standard management of primary gastric lymphoma (PGL) (stage II) has not been established despite the use of various treatment modalities. The present prospective trial of combined surgery and chemotherapy for the treatment of PGL (stage II) included 25 consecutive patients treated between July 1978 and December 1993. Twenty-one patients were treated with total gastrectomy and four with partial gastrectomy; this was followed by post-operative chemotherapy with m-VEPA (vincristine, cyclophosphamide, prednisolone and doxorubicin), followed by consolidation chemotherapy with VEMP (vindesine, cyclophosphamide, methotrexate and prednisolone) or VQEP (vindesine, carbazilquinone, cyclophosphamide and prednisolone). Twenty-one of the 25 patients who completed post-operative chemotherapy were free of relapse 26-203 (median 94) months after the gastrectomy. Of the four patients who did not complete the projected chemotherapy, two relapsed and died of lymphoma. Another patient with recurrent lymphoma died in an accident, and the fourth patient was in remission at 54 months after surgery. The post-operative overall and disease-free survival rates at 10 years for the 25 evaluable patients were 81.6% and 92.0% respectively. Major surgical complications and treatment-related death after chemotherapy were not observed. PGL (stage II) appears to be curable when treated with gastrectomy and adjuvant chemotherapy.

Topics: Adult; Aged; Aged, 80 and over; Antineoplastic Combined Chemotherapy Protocols; Carbazilquinone; Chemotherapy, Adjuvant; Combined Modality Therapy; Cyclophosphamide; Doxorubicin; Female; Humans; Lymphoma, B-Cell, Marginal Zone; Lymphoma, Non-Hodgkin; Male; Methotrexate; Middle Aged; Neoplasm Staging; Prednisolone; Prognosis; Prospective Studies; Stomach Neoplasms; Vincristine; Vindesine

PubMed: 9400946
DOI: 10.1038/bjc.1997.582

Authors: Qinsi Zheng, Steffen Jockusch, Gabriel G Rodríguez-Calero...

Bright, long-lasting and non-phototoxic organic fluorophores are essential to the continued advancement of biological imaging. Traditional approaches towards achieving photostability, such as the removal of molecular oxygen and the use of small-molecule additives in solution, suffer from potentially toxic side effects, particularly in the context of living cells. The direct conjugation of small-molecule triplet state quenchers, such as cyclooctatetraene (COT), to organic fluorophores has the potential to bypass these issues by restoring reactive fluorophore triplet states to the ground state through intra-molecular triplet energy transfer. Such methods have enabled marked improvement in cyanine fluorophore photostability spanning the visible spectrum. However, the generality of this strategy to chemically and structurally diverse fluorophore species has yet to be examined. Here, we show that the proximal linkage of COT increases the photon yield of a diverse range of organic fluorophores widely used in biological imaging applications, demonstrating that the intra-molecular triplet energy transfer mechanism is a potentially general approach for improving organic fluorophore performance and photostability.

Topics: Carbazilquinone; Carbocyanines; Cyclization; Energy Transfer; Fluorescent Dyes; Oxazines; Photolysis; Photons; Polyenes; Rhodamines

PubMed: 26700693
DOI: 10.1039/c5pp00400d

Comparative Study

Authors: N Saijo, E Shimizu, M Shibuya...

The effect of chemotherapy on natural killer (NK) activity and antibody-dependent cell-mediated cytotoxicity (ADCC) in 15 advanced carcinomas of the lung was examined with regard to the drug, dose, route and timing of administration. The relationship between the effect of chemotherapy on the prognosis for the patients, and the changes in NK activity and ADCC, was also analysed. The NK activity and ADCC in patients with poor prognosis were significantly subnormal, even before treatment. The NK activity and ADCC began to decrease 2 weeks after the initiation of treatment and reached the lowest level during the 3rd or 4th week in all patients. Thereafter, they returned to the pretreatment level in 8 patients with stabilized disease. In contrast, they were not restored in 7 patients with progressive disease and poor prognosis. In 4 patients it was found that the effect of chemotherapy with pepleomycin and carbazilquinone on NK activity and ADCC differed according to the drug used. From this pilot study it is suggested that NK activity and ADCC are valuable prognostic factors in patients with advanced carcinoma of the lung, and that detailed analysis of the effect of each anticancer agent on NK activity and ADCC is desirable for the establishment of better treatment regimens for advanced carcinoma of the lung.

Topics: Aged; Antibiotics, Antineoplastic; Antibody-Dependent Cell Cytotoxicity; Azirines; Bleomycin; Carbazilquinone; Female; Humans; Killer Cells, Natural; Lung Neoplasms; Male; Middle Aged; Neoplasm Staging; Peplomycin; Pilot Projects; Prognosis; Time Factors

PubMed: 6185128
DOI: 10.1038/bjc.1982.182

Comparative Study

Authors: Sorana-Daniela Bolboacă, Lorentz Jäntschi

Quantitative structure-activity relationship (qSAR) models are used to understand how the structure and activity of chemical compounds relate. In the present study, 37 carboquinone derivatives were evaluated and two different qSAR models were developed using members of the Molecular Descriptors Family (MDF) and the Molecular Descriptors Family on Vertices (MDFV). The usual parameters of regression models and the following estimators were defined and calculated in order to analyze the validity and to compare the models: Akaike's information criteria (three parameters), Schwarz (or Bayesian) information criterion, Amemiya prediction criterion, Hannan-Quinn criterion, Kubinyi function, Steiger's Z test, and Akaike's weights. The MDF and MDFV models proved to have the same estimation ability of the goodness-of-fit according to Steiger's Z test. The MDFV model proved to be the best model for the considered carboquinone derivatives according to the defined information and prediction criteria, Kubinyi function, and Akaike's weights.

Topics: Animals; Carbazilquinone; Longevity; Mice; Molecular Structure; Quantitative Structure-Activity Relationship

PubMed: 19838601
DOI: 10.1100/tsw.2009.131

Authors: S Taniguchi, N T Kimura, T Baba...

To assess the effects of pH on the cytotoxicity of carboquone (CQ), use was made of the mouse tail skin and HeLa cells in culture. CQ had the most potent cytotoxic effect at pH 6 rather than at pH7 or 8. Regarding the interaction between 14C-CQ and HeLa cells, both the intracellular accumulation of free 14C-CQ and the ratio of bound 14C-CQ to total 14C-CQ uptake were enhanced at pH6. Among the fractionated biomolecules of DNA, RNA and protein, DNA was the most active in binding CQ, under the same conditions of pH. The 14C-CQ binding to nucleic acids at pH 6 was more apparent than was the binding to protein. Thus, the enhancement of CQ cytotoxicity at low pHs is probably due to an increase in the intracellular accumulation of free CQ as well as to an enhanced reactivity of CQ with DNA, within the ranges of a lower pH.

Topics: Animals; Azirines; Carbazilquinone; Cell Survival; Female; HeLa Cells; Humans; Hydrogen-Ion Concentration; In Vitro Techniques; Male; Mice; Nucleic Acids; Proteins; Skin

PubMed: 7311142
DOI: 10.1254/jjp.31.243

Authors: M Moriyama, Y Kubota, T Miura...

The effect of intravesical chemotherapy on superficial urinary bladder cancer was analysed. Fifty-nine patients with low-staged, low-grade bladder cancer were treated with intravesical instillation of three anticancer drugs (adriamycin, carbazilquinone and bleomycin). Complete response (CR) was observed in 15 out of 42 patients and partial response (PR) in 9 patients. Overall, a better response rate was observed with adriamycin and carbazilquinone than with bleomycin. Papillary tumors responded well to these intravesical chemotherapies compared to the non-papillary tumors . Intravesical recurrence of tumors was evaluated in 68 patients who received intravesical instillation of these three drugs after TUR of tumors. The actuarial recurrence rate of 68 patients was 11, 22 and 34% within 1, 2 and 3 years, respectively. These rates were significantly lower than that of TUR therapy alone. No serious side effect was seen in these patients. From these results, it is noted that intravesical chemotherapy is a useful approach for controlling superficial urinary bladder cancer.

Topics: Aged; Antineoplastic Combined Chemotherapy Protocols; Bleomycin; Carbazilquinone; Carcinoma, Papillary; Carcinoma, Transitional Cell; Doxorubicin; Drug Administration Schedule; Drug Evaluation; Drug Therapy, Combination; Female; Follow-Up Studies; Humans; Injections; Male; Middle Aged; Neoplasm Recurrence, Local; Urinary Bladder; Urinary Bladder Neoplasms

PubMed: 6203382
DOI: No ID Found

Authors: Yisaira Díaz-Espinosa, Carlos E Crespo-Hernández, Antonio E Alegría...

Changes in the emission fluorescence intensity of pheophorbide-a (PHEO) in the presence of carboquone (CARBOQ) were used to obtain the association constant, the number of CARBOQ molecules interacting with PHEO, and the fluorescence quantum yield of the complex. Excitation spectra of mixtures of PHEO and CARBOQ in ethanol (EtOH) show an unresolved doublet in the red-most excitation band of PHEO, indicating the formation of a loose ground-state complex. The 1:1 CARBOQ-PHEO complex shows a higher fluorescence quantum yield in EtOH (0.41 ± 0.02) than in buffer solution (0.089 ± 0.002), which is also higher than that of the PHEO monomer (0.28). Quenching of the PHEO fluorescence by DNA nucleosides and double-stranded oligonucleotides was also observed and the bimolecular quenching rate constants were determined. The quenching rate constant increase as the oxidation potential of the DNA nucleoside increases. Larger quenching constants were obtained in the presence of CARBOQ suggesting that CARBOQ enhances DNA photo-oxidation, presumably by inhibiting the back-electron-transfer reaction from the photoreduced PHEO to the oxidized base. Thus, the enhanced DNA-base photosensitized oxidation by PHEO in the presence of CARBOQ may be related to the large extent by which this quinone covalently binds to DNA, as previously reported.

Topics: Antineoplastic Agents, Alkylating; Carbazilquinone; Chlorophyll; DNA; Ethanol; Light; Photochemistry; Radiation-Sensitizing Agents; Spectrometry, Fluorescence

PubMed: 21138440
DOI: 10.1111/j.1751-1097.2010.00869.x

Authors: T Uchibayashi, H Hisazumi, T Asari...

Surgical tumor specimens from 67 urological malignancy patients were subjected to a human tumor clonogenic assay (HTCA) developed by Hamberger and Salmon. Appreciable growth of colonies was obtained in 20 of the 33 renal cancers, 20 of the 30 urothelial cancers and 1 of the 4 testicular cancers examined. Using HTCA, a plating efficiency ranging from 0.01 to 0.5% was obtained in these urologic malignancies. However, colonial growth adequate for chemosensitivity was obtained in 30 of these 67 patients. According to Von Hoff's definition, more than a 70% decrease in the plating efficiency after anticancer drug exposure was defined as susceptible. Susceptibility to vinblastine (VBL) was seen in 4 of the 11 patients with renal cancer. Susceptibility to cis-dichlorodiamine platinum (CDDP) was seen in 4 of the 15 patients with urothelial cancer, 1 of the 4 patients with renal cancer, and that to adriamycin (ADM) was seen in 3 of the 15 patients with urothelial cancer, 2 of the 10 patients with renal cancer and 1 patient with testicular cancer. For comparison, the ratio of IC90 to the peak plasma concentration of the drug tested was used as the "in vivo-in vitro therapeutic index (TI)". According to TI, susceptibility to VBL was seen in 3 of the 7 patients with renal cancer, and that to CDDP was seen in 2 of the 12 patients with urothelial cancer, and 1 of the 2 patients with renal cancer. Susceptibility to ADM was seen in 3 of the 15 patients with urothelial cancer, and 1 of the 6 patients with renal cancer.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Antineoplastic Agents; Carbazilquinone; Cisplatin; Colony-Forming Units Assay; Doxorubicin; Humans; Tumor Cells, Cultured; Tumor Stem Cell Assay; Urologic Neoplasms; Vincristine

PubMed: 3445845
DOI: No ID Found

Authors: K Tari, I Satake, S Kojima...

Sixteen patients with upper tract urothelial carcinoma underwent intravesical chemotherapy usually at 2 week intervals in the first year and at 4 week intervals in the second year after nephrouretectomy. For bladder instillation 10 mg mitomycin C in 20 ml saline was used on 7 patients, 5 mg carboquone and 100 mg cytosine arabinoside in 40 ml saline on 5 patients and 30 mg adriamycin in 40 ml saline on 4 patients. Two (12.5%) of the 16 patients developed bladder tumors within 2 years after surgery, but 11 (42.3%) of the 26 patients with upper tract urothelial carcinoma who did not receive intravesical chemotherapy suffered from bladder tumor within 2 years after surgery. Prophylactic intravesical chemotherapy reduced significantly (p less than 0.1) the incidence of bladder tumor after the surgery of renal pelvic and ureteral tumors.

Topics: Administration, Intravesical; Adult; Aged; Antineoplastic Combined Chemotherapy Protocols; Carbazilquinone; Carcinoma, Transitional Cell; Cytarabine; Doxorubicin; Female; Humans; Male; Middle Aged; Mitomycin; Mitomycins; Nephrectomy; Postoperative Period; Ureter; Urinary Bladder Neoplasms; Urologic Neoplasms

PubMed: 3118664
DOI: No ID Found