Choline acetyltransferase (CAT) and muscarinic cholinergic receptor (MCR) activities are markedly reduced in aged as compared with young-adult rat brain. Nicergoline was found to correct these reduced activities in most regions of the brain, especially in the cerebral cortex and hippocampus. Chronic administration of nicergoline had no effect on CAT activity or MCR binding in young-adult rat brain. Nicergoline thus appears to have a specific therapeutic effect on cholinergic functions in aged rat brain, where it acts both pre-synaptically and post-synaptically.

Journal Article↗

PubMedDate not supplied

Specific genomic alterations in rat renal cell carcinomas induced by N-ethyl-N-hydroxyethylnitrosamine.

To characterize genetic alterations occurring in renal tumorigenesis, EHEN-induced renal cell tumors were examined using restriction landmark genomic scanning (RLGS) analysis, an electrophoretic separation technique that detects gene amplifications and deletions. Comparison of DNAs from tumor against those from corresponding nontumorous kidney and/or EHEN-treated kidney without development of renal tumors yielded specific alterations in terms of both amplified and reduced DNA spots. Two amplified spots were detected only in renal cell tumors and an additional four spots were frequent in EHEN-treated kidneys. One reduced spot was common to all tumor samples, and another was frequently detected in the tumors analyzed but not in EHEN-treated kidneys. A subset of the altered spots thus appeared to be specific for EHEN-induced renal tumorigenesis.

Animals↗

PubMedDate not supplied

Comparison of in vitro antimicrobial activity of AM-1155 with those of tosufloxacin and fleroxacin against clinical isolates of Neisseria gonorrhoeae harboring quinolone resistance alterations in GyrA and ParC.

The in vitro antimicrobial activities of AM-1155, a new fluoroquinolone, tosufloxacin and fleroxacin were tested against 55 clinical isolates of Neisseria gonorrhoeae using the agar dilution method. In our previous study, all the strains had been examined for mutations in the region corresponding to the quinolone-resistance determining region of the Escherichia coli gyrA gene and the analogous region of the parC gene, and tested for susceptibility to ciprofloxacin. In this study, the 55 isolates of N. gonorrhoeae were assigned to one of three categories based on the presence or absence of alterations in GyrA and ParC. In each category, the antimicrobial activity of AM-1155 against the isolates was compared with those of tosufloxacin and fleroxacin. The MICs of AM-1155 for 11 highly fluoroquinolone-resistant isolates with alterations in both GyrA and ParC ranged from 0.06 to 1.0 microgram/ml. The MICs inhibiting 50% (MIC50) and 90% (MIC90) of these isolates were 0.125 and 1.0 microgram/ml, respectively. The MICs of AM-1155 for 20 moderately fluoroquinolone-resistant isolates with alterations only in GyrA ranged from 0.03 to 0.25 microgram/ml (MIC50, 0.06 microgram/ml; MIC90m, 0.125 microgram/ml). The MICs of AM-1155 for 24 of the quinolone-susceptible isolates without alterations in either GyrA or ParC ranged from 0.004 to 0.03 microgram/ml (MIC50, 0.008 microgram/ml. MIC90, 0.015 microgram/ml). There were significant differences between the MIC distribution of AM-1155 and each corresponding MIC distribution of tosufloxacin and fleroxacin in these three categories to which the 55 isolates were assigned (p < 0.05). Based on the MIC90S of the tested fluoroquinolones, AM-1155 was two- and eightfold more active against the highly fluoroquinolone-resistant isolates than tosufloxacin and fleroxacin, respectively. Against the moderately fluoroquinolone-resistant isolates, AM-1155 was four- and sixteenfold more active than tosufloxacin and fleroxacin, respectively. Against the quinolone-susceptible strains, AM-1155 was also two- to fourfold more active than the other fluoroquinolones. Overall, AM-1155 exhibited more potent in vitro activity against both quinolone-resistant and quinolone-susceptible isolates of N. gonorrhoeae than tosufloxacin and fleroxacin. In ciprofloxacin treatment failures of gonorrhea at single doses of 500 mg. MICs for the causative organisms have ranged from 1.0 to 16.0 micrograms/ml. The MICs of AM-1155 for the isolates harboring quinolone resistance-associated genetic alterations, including strains exhibiting ciprofloxacin MICs of 2.0 and 8.0 micrograms/ml, still ranged from 0.03 to 1.0 microgram/mL A single-dose study in humans has demonstrated higher peak serum concentrations and longer half-lives of AM-1155, resulting in the AUC0-00 values of AM-1155, which are threefold greater than those of ciprofloxacin at the single doses of 400 and 600 mg. Because of its potent in vitro antimicrobial activity and advantageous pharmacokinetic behavior, AM-1155 may be a clinically useful agent for treating gonorrhea including that caused by quinolone-resistant strains.

Anti-Infective Agents↗

PubMedDate not supplied

Mycoplasma genitalium in non-gonococcal urethritis.

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Adult↗

PubMedDate not supplied

Clinical assay of serum SCC-Ag in urothelial cancers.

Serum squamous cell carcinoma related antigen (SCC-Ag) values were determined in 86 patients with urothelial cancers. Mean +/- standard deviation for serum SCC-Ag, was 3.4 +/- 0.98 ng/ml and positive values (greater than 2.0 ng/ml) were found in 27%. Neither pathological stage nor cell grade of the urothelial cancer showed any relation to serum SCC-Ag. Serum SCC-Ag. changed parallel to the clinical course. These results suggest that, as there is no specific tumor marker in urothelial cancer, serum SCC-Ag. may be a useful aid in diagnosing cancer and monitoring these patients. Used together with another non-specific marker, an increase in the accuracy of diagnosis of these malignancies can be expected.

Adenocarcinoma↗

PubMedDate not supplied

Treatment of metastatic gastric cancer by combined radiation and hyperthermia (report of two cases).

Two patients with metastatic carcinoma of the stomach on the abdominal wall were treated by radiotherapy using cobalt-60 gamma-ray or megavoltage electrons combined with hyperthermia induced with a Thermotron (8 MHz). The total dosage was 44 Gy fractionated into 11 doses (twice a week), by cobalt-60 gamma-ray and 10 hyperthermia treatments for patient 1, and 32 Gy fractionated into eight doses (twice a week) given by megavoltage electrons and five hyperthermia treatments for patient 2. In patient 1, the shrinkage of the tumor was more than 50%. No tumor cells were observed histologically at the end of treatment. In patient 2, the tumors completely disappeared. These results encourage us in the use of radiotherapy combined with hyperthermia for rather radioresistant adenocarcinoma.

Abdominal Muscles↗