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Development of anti-allergics against antianaphylaxis type by lead-optimization

Research Project

Project/Area Number 12680591
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field Bioorganic chemistry
Research InstitutionHIROSHIMA UNIVERSITY

Principal Investigator

OHTANI Kazuhiro  Faculty of Medicine, Hiroshima University, Associate Professor, 医学部, 助教授 (20203820)

Co-Investigator(Kenkyū-buntansha) KOIKE Tohru  Faculty of Medicine, Hiroshima University, Professor, 医学部, 教授 (90186586)
Project Period (FY) 2000 – 2001
Project Status Completed (Fiscal Year 2001)
Budget Amount *help
¥2,700,000 (Direct Cost: ¥2,700,000)
Fiscal Year 2001: ¥1,200,000 (Direct Cost: ¥1,200,000)
Fiscal Year 2000: ¥1,500,000 (Direct Cost: ¥1,500,000)
KeywordsAnti-allergics / RBL-2H3 cells / mast cells / basophils / microphyllone / calcium chanell / アレルギー / RBL-2113細胞 / ラット腹腔マスト細胞 / ヒト好塩基球 / 酸化還元電位
Research Abstract

Microphyllone isolated from Ehretia microphylla has the inhibitory activity on exocytosis in RBL-2H3 cells at _□M concentration. We have determined the physicochemical and biological characters of microphyllone as a novel anti-allergic compound. Microphyllone inhibited exocytosis not only in RBL-2H3 cells but also in rat mast cells, and human basophiles with various stimuli. Microphyllone inhibited an increase in concentration of intracellular calcium ion by stimulation, which is due to inhibition of calcium influx through calcium release-activated calcium (CRAC) channel. We, furthermore, determine the effects of microphyllone in the following allergic models. Microphyllone suppressed passive cutaneous anaphylaxis reaction and immediate phase of ascaris-induced biphasic skin allergic reaction. On the other hand, microphyllone has no effect on type-IV allergic modes such as late phase of ascaris-induced biphasic skin allergic reaction and oxazolone-induced contact type delayed cutaneous reaction. Microphyllone can be a new type of anti-allergics and/or a lead compound for new class anti-allergics against acute allergic reactions.

Report

(3 results)
  • 2001 Annual Research Report   Final Research Report Summary
  • 2000 Annual Research Report

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Published: 2000-04-01   Modified: 2016-04-21  

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