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1.
Shiro Akinaga Tadashi Ashizawa Katsushige Gomi Hiroe Ohno Makoto Morimoto Chikara Murakata Masami Okabe 《Cancer chemotherapy and pharmacology》1992,29(4):266-272
Summary Novel derivatives of K-252a, (8R*,9S*,11S*)-(–)-9-hydroxy-9-methoxycarbonyl-8-methyl-2,3,9,10-tetrahydro-8, 11-epoxy-1H,8H,11H-2,7b,11a-triazadibenzo [a,g]-cycloocta[cde]trinden-1-one, an inhibitor of protein kinases and calmodulin-dependent phosphodiesterase, were synthesized and evaluated for their antitumor activity in vitro and in vivo. Of ten derivatives tested, four were active against the P388 murine leukemia i. p.-i. p. system, although K-252a was inactive. Among these derivatives, KT6124 was selected for further biological evaluation studies because its efficacy was the highest. KT6124 was also active against sarcoma 180 and B16 melanoma. It exerted a relatively broad spectrum of antiproliferative activity against 20 human tumor cell lines in vitro. To determine the mechanism(s) of action underlying the antitumor activity of KT6124, we tested the drug for inhibition of protein kinases, including Ca2+-and phospholipid-dependent protein kinase (PKC), in intact A431 human epidermoid carcinoma cells in comparison with the PKC-inhibitory activity of K-252a. KT6124 did not antagonize the action of phorbol 12-myristate 13-acetate (PMA) in A431 cells, whereas K-252a did, suggesting that KT6124 may not act on protein kinases in the cells. The interaction of KT6124 with DNA in living cells was examined by the alkaline elution method. KT6124 apparantly exhibited DNA scission both dose-and time-dependently in the target cells. The DNA breakage was dependent on proteinase K treatment, suggesting its possible interaction with DNA-related enzyme(s). These results indicate that KT6124 exerts antitumor activity by acting on DNA or on DNA-related enzyme(s) in tumor cells rather than via the inhibition of protein kinases. 相似文献
2.
Tadashi Kato 《Seishin shinkeigaku zasshi》2002,104(6):509-512
3.
Yutaka Okishio Tadayoshi Takeuchi Akikazu Fujita Kiyotaka Suenaga Kaori Fujinami Satoru Munakata Tadashi Takewaki Fumiaki Hata 《Journal of Smooth Muscle Research》2005,41(3):163-174
Recently an essential role of interstitial cells of Cajal (ICC) within myenteric plexus (ICC-MY) was suggested in ascending contraction and descending relaxation in the mouse ileum. The role of ICC in these neural reflexes was examined in the distal colonic segments prepared from the wild type and c-kit mutant, W/W(V) mice, in the present study. Localized distension of the segments from the wild type mice by using a small balloon resulted in ascending contraction and descending relaxation. In the segments from the mutant mice, localized distension also induced these neural reflexes similar to those observed in the wild type mice. Immunohistochemical examination demonstrated that ICC-MY and ICC present in muscle layers (ICC-IM) were severely disrupted in the mutant mouse, but only ICC, present within submucosal plexus (ICC-SMP), remained unchanged. In the small strips with ICC-SMP absent prepared from the mutant mouse, electrical field stimulation induced contraction or relaxation in the absence or presence of atropine, respectively. It was suggested that ICC have no important role in the ascending and descending neural reflexes in the mouse distal colon, this is in direct contrast to the role of ICC-MY in the ileum. 相似文献
4.
5.
Self-expandable metallic stent for unresectable malignant strictures in the esophagus and cardia 总被引:2,自引:0,他引:2
Shigeru Lee Harushi Osugi Taigo Tokuhara Masashi Takemura Masahiro Kaneko Yoshinori Tanaka Yushi Fujiwara Satoshi Nishizawa Hiroshi Iwasaki Shigefumi Suehiro 《The Japanese Journal of Thoracic and Cardiovascular Surgery》2005,53(9):470-476
Objective Self-expandable metallic stent (EMS) placement has been the first choice for dysphagia because of the certainty over its safety,
low invasiveness, and immediate efficacy. However, there still remain some problems in relation to the EMS placement site
and anticancer therapies before and after EMS placement. Methods: Consecutive 78 patients in whom EMS was placed due to the unresectable malignant stricture in the esophagus or cardia from
July 1995 to August 2003 in our department were studied. Results: Gastroesophageal reflux was found in 5 of 8 patients after placement of conventional EMS for the stricture in the gastroesophageal
junction. Meanwhile, acid and bile reflux into the esophagus were not detected by pH and bilirubin monitoring, respectively,
in 6 patients after placement of the EMS with an anti-reflux mechanism for the stricture in the gastroesophageal junction.
The median survival period of all patients after EMS placement was 123 days. The median survival period of 7 patients with
radiotherapy only after EMS placement was 138 days and that of 17 patients with radiotherapy before EMS placement was 60 days,
which was shorter than that of the former (p<0.05). On the other hand, the median survival period after hospital admission
due to dysphagia of these 7 patients was longer than that of 17 patients with radiotherapy only before EMS placement, although,
the difference was not significant. Conclusion: EMS with an antireflux mechanism is not commercially available in Japan and approval is urgently required. The indication
of radiotherapy associated with EMS placement is to be studied further. 相似文献
6.
Roberto Civitelli M.D. Eturo Ogata Louis V. Avioli Gary Stein Samuel Edelstein John A. Eisman Yasuho Nishii Hajime Orimo Jane Lian Takuo Fujita Yasufumi Hayashi Shigeaki Kato Tadashi Kobayashi Hirotoshi Morii Rikushi Morita Toshitaka Nakamura Yoshiki Seino Masataka Shiraki Tatsuo Suda Naoyuki Takahashi Hideaki Takahashi Tastuhiko Tanisawa Akifumi Tokita 《Calcified tissue international》1995,57(6):409-414
7.
8.
A. Robert Spitzer Shalom Stahl David Yarnitsky Ernest W. Johnson John R. Wilson R. A. C. Hughes Stefania Morino Giovanni Antonini Kiyotoshi Kaneko Yoji Ohnishi Tetsushi Atsumi Isao Hozumi Tadashi Miyatake Tetsuo Furukawa James P. Knochel Ikuo Mineo Seiichiro Tarui Francis O. Walker Andrew J. Gitter Walter C. Stolov Nicholas J. Capozzoli 《Muscle & nerve》1996,19(4):531-538
9.
Tamikuni Komatsu Masayuki Nomura Youzou Kakudate Syuzou Fujiwara R. B. Heimann 《Macromolecular chemistry and physics.》1995,196(9):3031-3040
Dehydrochlorinated poly(vinylidene chloride) proved to be a conjugated polyene-polyene polymer. Shock compression of the polymer formed a large portion of graphite and trace amounts of diamond and of an unknown carbon. The unknown carbon belongs to the hexagonal crystal system and possesses the cell dimension α0 = 0.338 nm. A comparison with known carbynes was made in terms of the crystalline parameters. 相似文献
10.
Diagnosis and treatment of thoracic outlet syndrome 总被引:2,自引:0,他引:2
Masataka Abe Tadashi Shimamura Jun Nishida Katsuaki Ichinohe 《Journal of orthopaedic science》1997,2(2):119-127
Patients who develop symptoms of thoracic outlet syndrome (TOS) have a predisposing anatomic abnormality. In most patients
with TOS, the symptoms are caused by entrapment of the brachial plexus and they do not arise from compression of the subclavian
artery, as was previously thought. The tests advocated for diagnosing this common syndrome (i.e., evaluating the positional
compression of the artery when the arms are raised, the neck is turned, or the shoulders are braced) cannot accurately diagnose
this syndrome. There are two reasons for this. The symptoms of TOS are not related to the compression of the artery in the
outlet in 98% of patients, and 75% of normal individuals without symptoms show diminished radial pulse on various provocation
tests. We employed four timed provocation tests (minute tests) to diagnose TOS: the timed Morley test, timed Wright test,
timed Eden test, and elevated arm stress exercise, all of which are very sensitive. In normal individuals without symptoms,
20% experience transitional symptoms such as slight pain and tiredness, on these tests indicating a subclinical state. TOS
is treated by keeping the thoracic outlet wide, this being done either conservatively or surgically. In 1993 and 1994, we
conservatively treated 418 of 422 patients with TOS by means of active exercise, a brace, and by block therapy. These measures
did not reduce the symptoms in 23 of these patients, so surgical treatment was indicated. In the remaining 4 of the 422 patients,
conservative treatment was not indicated and surgery was performed directly. All the patients showed significant clinical
improvement of varying degree.
Presented at the 69th Annual Meeting of the Japanese Orthopaedic Association, Tokyo, April 12, 1996 相似文献