Synthesis and antiviral activity of sulfonamidobenzophenone oximes and sulfonamidobenzamides

To find antiviral agents, various sulfonamidobenzophenone oximes (II) were synthesized from the appropriate m-sulfonamidobenzophenones by hydroxylamine reaction. The reaction products were generally obtained as syn/anti mixtures which were separable by fractional crystallization. The anti isomer had more potent antipoliovirus activity than the syn isomer. Various sulfonamidobenzamides (III) which were structurally related to II were synthesized by the reactions of amino-substituted benzamides with sulfuryl chloride or amines with (aminosulfonyl)benzoyl chloride. Antiviral activity was examined by the plaque-inhibition test. Compounds 5, 36, and 69 exhibited strong antipicornavirus activity. The structure-activity relationships are discussed.     

How can we make mass-screening of stomach cancer more efficient using epidemiological results?

From an observation of personnel we expect epidemiological studies make mass-screening of stomach cancer more efficient and suppose they should be done as to following aspects: (1) To decide the most efficient interval of mass-screening, investigating the frequency distribution of "Saving Duration" on many stomach cancers that is the duration when a stomach cancer is both detectably by screening and curable. (2) To decide who should undergo stomach examination quantifying cancer-risks of individuals with the use of epidemiological results. (3) To make epidemiological studies more sensitive and useful, classifying stomach cancers by microscopic pathological type, macroscopic one or "Saving Duration". (4) To settle a statistical standard of epidemiological results which is demanded for them to be useful in mass-screening.     

Effects of lumbar skin warming on gastric motility and blood pressure in humans

We examined the possibility that lumbar skin warming can increase gastrointestinal motility by investigating the electrogastrogram (EGG), blood pressure, and heart rate with psychometric ratings in healthy humans. Scores of mood state profiles showed that lumbar skin warming (42 degrees C, 20 min) decreased tension-anxiety, depression, anger-hostility, fatigue, and confusion of the participants. A multiple bandpass filter analysis of EGGs showed that a postural transition from orthostatic to supine for measurement caused an increase in dominant frequency of 25-29% towards the frequencies of the normal interdigestive migrating motor complex (IMC). The spectral power of the IMC band, 2.55-3.05 cycles/min, was increased by 20 min-warming, reflecting the increase in gastric contractility. No increase in the spectral power was observed in the time-matched control group without skin warming. Therefore, an increase in contractility is a characteristic of lumbar skin warming. The systolic blood pressure increased by 15% during warm stimulation. Interbeat intervals were not influenced by warm stimulation. An analysis of interbeat intervals by a fast Fourier transform method showed that the cardiac sympathetic and parasympathetic nerves did not play a major role in raising the blood pressure. Vasoconstriction of the mesenteric artery was therefore considered to cause a blood pressure increase during warming. It is hypothesized that vasoconstriction of the visceral arteries by lumbar skin warming increases the blood pressure and gastrointestinal contractility.     

Establishment and Characterization of Cell Lines from Human Adenovirus Type 12-induced Murine Tumors Producing Endogenous Virus Particles

Two cell lines designated IC KMS and D KMS were established from human adenovirus type 12 induced tumors of C3Hf/OK mouse. The cell lines retained the characteristics of the original tumor i.e., production of numerous C type and intracisternal A-type particles, integration of Adl2 El region DNA and amplification of the myc gene family. Chromosomal analysis revealed chromosome aberrations in both IC KMS and D KMS cells. The modal chromosome number of IC KMS cells was 54 and that of D-KMS cells was 48. Metacentric chromosomes and mini-chromosomes were found. Trisomy of chromosome 3, 7 and 12 was seen frequently in D KMS cells. Although DNA aneuploidy was revealed by flow cytometry, the DNA indices of these cells showed no relation to the copy number of integrated Adl2 DNA. These cells have been propagated by serial culture during the past 17 months. Production of endogenous virus particles is a unique characteristic of IC KMS and D KMS cells. These cell lines would be useful materials for examining the contribution of Adl2 carcinogenesis to activation of endogenous virus particles, and also the correlation between Adl2 carcinogenesis and cancer related genes. Acta Pathol Jpn 42: 242-248, 1992.     

Cationic polymerization of vinyl monomers with latent initiators, 3. 1-(p-methoxybenzyl)tetrahydrothiophenium hexafluoroantimonate as a new potent cationic initiator

Cationic polymerization of styrene in the presence of 1-(p-methoxybenzyl)tetrahydrothiophenium hexafluoroantimonate ( 3 ) as an efficient cationic initiator was investigated. 3 was synthesized in an excellent yield by the reaction of p-methoxybenzyl bromide with tetrahydrothiophene and the subsequent exchange of bromide ions for hexafluoroantimonate ions. In the polymerization of styrene, 3 acted as a potent thermally latent initiator which initiates the polymerization at a slightly higher temperature than room temperature, although no polymerization occurs at room temperature for 30 min. 3 is a much more active initiator than the previously reported benzylsulfonium salt 1 . The enhanced activity of 3 was also confirmed in the polymerization of glycidyl^b phenyl ether.     

ISCHEMIC ENTEROCOLITIS WITHOUT ARTERIO–OCCLUSIVE LESION

Four cases of Ischemic enterocolitis without arterio–occlusive lesion were described. Three cases were associated with sigmoid colon carcinomas. Ischemic lesions developed anal to the carcinomas in two cases, and oral to sigmoidostomy to relieve intestinal obstruction by carcinoma in one case. One other case was associated with inguinal hernia. Grossly, ischemic lesions involved relatively short intestinal segments, and the ischemic colonic lesions were not related to teniae coli. Extensive veno–occlusive lesions were discovered in a case of ischemic stricture of the ileum, which had been incarcerated in the right inguinal hernia. Reversible mechanical occlusion of the intestinal vessels caused by transient or recurrent intestinal strangulation is the most probable cause of these ischemic lesions., ACTA PATHOL. JPN. 33: 249–256, 1983.     

Social isolation stress augments angiogenesis induced by colon 26-L5 carcinoma cells in mice

We have previously shown that tumor necrosis factor-α (TNF-α), which is an important angiogenesis-related factor, was over-secreted in male BALB/c mice under social isolation stress as compared with the control, and closely associated with a remarkable elevation of tumor invasion and metastasis of colon 26-L5 carcinoma cells. In the present study, we explored the effect of isolation stress on the angiogenesis caused by colon 26-L5 carcinoma cells in vivo and in vitro. Social isolation lead to the enhancement of tumor growth after intrahepatic implantation with a fragment of colon 26-L5 tumor. Angiogenic response (number of vessels oriented towards tumor mass) and tumor growth (size) were significantly increased in the socially isolated mouse relative to that in the group-housed mice. Furthermore, higher protein level of hepatic TNF-α was found in the stressed mice than that in the control. Expression of mRNA for vascular endothelial growth factor (VEGF) and hepatocyte growth factor (HGF) were also elevated in the tumor regions and liver tissues of the stressed mice in comparison with that in group-housed mice. On the other hand, hepatic sinusoidal endothelial (HSE) cells treated with TNF-α exhibited a marked promotion of the migration, invasion, expression of mRNA for matrix metalloproteinase (MMP)-9, and tube-like formation, but no cytotoxicity against the cells in vitro. The above data suggest that the social isolation stress augmented the tumor-induced angiogenesis probably by up-regulating the angiogenesis-related factors, including TNF-α, VEGF and HGF, and consequently mediating the functions of endothelial cells such as migration, invasion, and tube-like formation.     

Relationship between immediate hypersensitive reactions by buckwheat ingestion and specific IgE for rice in subject with positive IgE-RAST for buckwheat]

IgE-mediated mechanisms are important in immediate hypersensitive reactions (IHR) to buckwheat. However, a part of subjects with high IgE for buckwheat show no IHR to buckwheat ingestion. Inspite of cross-allergenicity between buckwheat and rice, rice ingestion rarely induces IHR even in subjects with high IgE for rice unlike buckwheat-induced IHR. We speculated that there were some relationships between the presence of IHR to buckwheat and recognition of cross-allergenic determinants on buckwheat components with rice components. We examined IgE-RAST for rice in 58 subjects with positive IgE-RAST for buckwheat. IgE-RAST for Dermatophagoides pteronyssinus (Dp), egg white and cow's milk as unrelated antigens with rice were also assessed for a comparison. Subjects (n = 33) without IHR to buckwheat showed higher IgE-RAST values for rice than those (n = 25) with IHR, whereas there were no differences in IgE-RAST values for Dp, egg white and cow's milk between two groups with and without IHR. IgE-RAST values for buckwheat showed significant close correlations to those for rice in subjects without IHR to buckwheat but not in those with IHR. There were no significant correlations between IgE-RAST values for buckwheat and for Dp, egg white or cow's milk in both groups with and without IHR. These results suggested that the IgE from subjects without IHR to buckwheat recognized cross-allergenic determinants with rice on the buckwheat components.