The protective effect of spizofurone (AG-629) on the rat gastric mucosa was studied in the presence of various stimuli. Spizofurone given orally markedly inhibited gastric lesions induced by ethanol (ED50 = 6.5 mg/kg). Spizofurone inhibited ethanol-induced gastric lesions even when administered intraperitoneally (i.p.), but the onset of action after oral administration was shorter. Spizofurone given orally or i.p. in a dose range of 25-200 mg/kg inhibited indomethacin-induced gastric antral ulcers in re-fed rats. Furthermore, spizofurone potentiated the inhibitory effect of prostaglandin E2 on indomethacin-induced gastric antral ulcers. Spizofurone given i.p. prevented a decrease in potential difference and the formation of gastric lesions induced by intragastric instillation of 30 mM aspirin in 0.1 N HCl. Spizofurone given i.p. inhibited the increase in net fluxes of H+ and Na+ caused by intragastric instillation of 15% ethanol in 0.1 N HCl. These findings indicate that spizofurone, like prostaglandin E2, exerts gastric mucosal protection and even potentiates the anti-ulcer effect of prostaglandin E2. The gastric mucosal protection by spizofurone is ascribed in part to preservation of the mucosal barrier.

Animals↗

PubMed1985

Detection of different blood flow patterns in the true and false lumina with aortic root dissection by pulsed Doppler echocardiography.

We report a 53-year-old man with aortic dissection, in whom pulsed Doppler echocardiography showed two different flow patterns within the dilated aorta. Although two-dimensional echocardiography has been successful in making the diagnosis of aortic root dissection, several conditions producing false positives have also been noted. Simultaneous recording of pulsed Doppler echocardiography may be useful to provide additional diagnostic clues in selected cases.

Aortic Dissection↗

PubMed1985

Isoproterenol-induced desensitization to the positive inotropic effect of isoproterenol in ventricular strips isolated from carp heart (Cyprinus carpio).

Whether the positive inotropic effect of isoproterenol in ventricular strips of carp heart is altered by previous exposure to the agonist was studied. Isoproterenol produced a concentration-dependent positive inotropic effect in these preparations which was competitively antagonized by propranolol. Isoproterenol dose-response curves were shifted significantly downward and to the right after previous treatment with and removal of isoproterenol. The desensitization could be demonstrated after 5 min incubation and near maximal desensitization was observed after 30 min exposure to 1000 nM isoproterenol. The responsiveness was only partially recovered after 180 min incubation in drug-free medium. Isoproterenol produces a rapidly developing desensitization to inotropic effects of the beta-adrenergic agonist. This phenomenon may be mediated by alterations in beta-adrenergic receptors, adenylate cyclase and/or the beta receptor-adenylate cyclase coupling mechanism.

Animals↗

PubMed1985

Antibiotic susceptibilities of Staphylococcus aureus strains derived from furuncle and bullous impetigo.

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Ampicillin↗

PubMed1985

Exaggerated posterior aortic wall excursion. A new echocardiographic feature of atrial septal defect with left to right shunt?

In 32 adult patients with a secundum type atrial septal defect (ASD) and normal pulmonary vascular resistance, the posterior aortic wall excursion (AoE) was measured using M-mode echocardiography, before, 16.2 +/- 4.5 days after, and 2.4 +/- 1.1 years after operative repair of the ASD. This parameter was also measured in 50 control subjects. The AoE index (AoE corrected for body surface area) in patients with ASD was significantly greater than in disease-free subjects (0.81 vs 0.59 cm, p less than 0.01). When the AoE index was plotted against the pulmonary to systemic blood flow ratio (Qp/Qs) obtained by the Fick method, a single linear relationship was evident (r = 0.65, p less than 0.01). The index normalized within 1 month after the operation; left ventricular dimension index became normal only 1 year after the operation. The right ventricular dimension index remained enhanced even 1 year after the operation. We suggest that exaggerated AoE might be another echocardiographic feature of ASD with normal pulmonary vascular resistance.

Adolescent↗

PubMed1985

Effects of insulin, amino acids and fasting on myofibrillar protein degradation in perfused hindquarters of rats.

The rate of 3-methylhistidine (3-MH) release from rat perfused hindquarters was measured to investigate the effects of insulin, amino acids and fasting on myofibrillar protein degradation. Since release of 3-MH into the perfusate increased linearly and the pool of free 3-MH in the perfused muscle did not change significantly during 2 h of perfusion, it was concluded that 3-MH release reflected the rate of myofibrillar protein degradation. Tyrosine release in the presence of cycloheximide represented the degradation rate of total muscle protein. Insulin suppressed the net release of tyrosine in normal rats, but did not affect the rate of release of 3-MH and tyrosine in the presence of cycloheximide. 3-MH release was not influenced by perfusate amino acid concentrations at zero to 5 times the normal plasma levels. When rats were fasted for one and two days, 3-MH release increased 1.7 and 2.6 times, respectively, compared with the fed rats, which showed that the rate of degradation of myofibrillar protein in skeletal muscle rose just after the beginning of fasting.

Amino Acids↗

PubMed1985

Conversion of cloxacillin into a progressive inhibitor of beta-lactamases by sulfonation and its activity against various types of these enzymes.

On the assumption of the theory that the sulfone of a penam derivative should effectively act as a suicide substrate against beta-lactamases to which the parent compound is a poor substrate, the action of cloxacillin sulfone on four different types of beta-lactamases was studied. As we expected, cloxacillin sulfone showed strong mechanism-based irreversible inactivation against type Ib penicillinase and Proteus vulgaris cephalosporinase whereas it showed no progressive inactivation against cloxacillin-hydrolyzing type II penicillinase. However, an unexpected result was that cloxacillin sulfone could not inactivate Citrobacter freundii cephalosporinase which itself could hardly hydrolyze the parent cloxacillin. The number of hydrolytic events which occurred before inactivation of type Ib penicillinase, and P. vulgaris cephalosporinase, by the inactivator was 190 and 13, respectively. These values indicate that cloxacillin sulfone is far more effective as a suicide substrate against the two types of beta-lactamases than penam sulfones so far reported. The inactivation proceeded via the formation of an irreversible enzyme-inhibitor complex which could be detected by isoelectric focusing.

Cloxacillin↗

PubMed1985

7-Hydroxyguanine, a novel antimetabolite from a strain of Streptomyces purpurascens. II. Physico-chemical properties and structure determination.

The molecular formula of a new antimetabolite produced by Streptomyces purpurascens was determined to be C5H5N5O2 by elemental analysis, FD-MS and 13C NMR. Reduction of this antimetabolite with Raney nickel yielded guanine. The antimetabolite was distinguishable from known N-hydroxyguanines by comparison of their UV spectra. The structure of the antimetabolite was finally established to be 7-hydroxyguanine by X-ray crystallography.

Antimetabolites, Antineoplastic↗

PubMed1985

[Studies on CA 125, CA 19-9, TPA and IAP as tumor markers in patients with ovarian cancer].

CA 125, CA 19-9, TPA and IAP were useful for diagnosis of ovarian cancer. CA 125 was localized immunohistochemically in the surface and cytoplasma of cancer cells of serous cystadenocarcinomas, clear cell carcinomas, endometrioid carcinomas and undifferentiated carcinomas and CA 19-9 localized in mucinous cystadenocarcinomas and endometrioid carcinomas. When the cut off value of CA 125 was set by 35 U/ml in the control group, the patients with serous cystadenocarcinoma showed positive in 81%, resulting by 1,766.5 U/ml as an average value. As for CA 19-9 having set by 37 U/ml as the cut off value, patients suffering from mucinous cystadenocarcinoma who revealed positive by 60%, were 194 U/ml in an average value. It is considered that measuring values of CA 125 and CA 19-9 are valuable not only to diagnose as ovarian cancers but also to evaluate their prognosis.

Adenocarcinoma, Mucinous↗

PubMed1985

[Multiple primary cancers observed after surgery of lung cancer, and their countermeasures].

Multiple primary cancers were found after surgery in 80 (2.5%) of 3,154 patients with lung cancer. Patients with squamous cell carcinoma most frequently suffered from multiple primary cancers. The period up to discovery of the second primary cancers was within two years in 78.8% of the patients. Second primary cancers were most frequently observed in the lung, followed by the stomach, colon and rectum. Second primary cancers were found in the lung in 26 patients, 14 of these (53.8%) having squamous cell carcinoma. Multiple primary cancers were noted in 2.8% of 1,210 lung cancer patients who underwent stage I curative operation and 2.4% of the remaining 1,944 cases. As to prognosis, 14 patients survived for more than three years after the second primary cancers were found.

Adenocarcinoma↗

PubMed1985

Differentiation between idiopathic pulmonary fibrosis and interstitial pneumonia associated with collagen vascular diseases by comparison of the ratio of OKT4+ cells and OKT8+ cells in BALF T lymphocytes.

Idiopathic pulmonary fibrosis (IPF) and interstitial pneumonia associated with collagen vascular disease have been shown to be difficult to differentiate by clinical, roentgenological, pathological and immunological findings. We have applied the analysis of BALF T cell phenotypes to these two groups by enumerating the cell populations of OKT4+ and OKT8+ cells in BALF and, as a result, have been able to discern a clear and meaningful differentiating point between the two groups. In all 9 patients with IPF were examined in whom OKT4+ cells outnumbered OKT8+ cells in BALF T cell subsets, while 13 patients with collagen vascular disease were tested (3 SLE, 6 RA, 2 Sjögren's syndrom and 2 MCTD) in whom OKT8+ cells were more numerous than OKT4+ cells. No difference was observed in blood T lymphocytes between these two groups. These results provide us with a means of differentiation between these groups, especially in clinically borderline cases.

Adrenal Cortex Hormones↗

PubMed1985

Electron microscopic observations of cell wall and cytoplasmic membrane in murine and human leprosy bacilli.

The cell wall and the cytoplasmic membrane of Mycobacterium lepraemurium in murine lepromas and M. leprae in human skin lepromas were studied in ultrathin serial sections at the electron microscopic level. The cell wall in M. lepraemurium was composed of three layers: an innermost electron-dense layer, an intermediate electron-transparent zone, and a thin outermost electron-dense layer. The fine structure of the cell wall in M. leprae was slightly different. In general, the cytoplasmic membrane of M. lepraemurium and M. leprae seemed to have a similar structure.

Animals↗

PubMed1985

Electron microscopic observations of acid-fast bacilli in nasal mucosal biopsies of lepromatous leprosy patients.

The fine structure of acid-fast bacilli in nasal mucosal lepromas of lepromatous leprosy patients was studied in ultrathin sections by the electron microscope. The cell envelope of the bacilli was the main point of these observations. The electron microscopic examination of some of the bacilli revealed the envelope to be multilaminate. Some of the cellular matter was filled with an electron-less-dense, amorphous substance, surrounded with a membrane-like structure, and was adherent to the outermost layer of the bacillary cell envelope.

Adult↗