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Published on: April 17, 2012
Effects of Medium Molecular Weight Heparinyl Phenylalanine on Type I Hypersensitivity
Seiichi Takeda1, Takao Toda2, Kazuki Nakamura3
1Research and Development Center, Fuso Pharmaceutical Industries Ltd, Osaka, Japan sei-takeda@fuso-pharm.co.jp.
Background/Aim:
We investigated the inhibitory action of medium molecular weight heparinyl phenylalanine (MHF) on type I hypersensitivity in comparison with medium molecular weight heparinyl arginine (MHR).
Materials And Methods:
MHF and MHR were synthesized from heparin (HE) to decrease the side-effect of HE based on its anticoagulant action and used in this study.
Results:
MHF demonstrated a significant inhibitory action on 48-h homologous passive cutaneous anaphylaxis in rats. Although MHF did not affect the death of mice injected with a lethal dose of histamine, it significantly prolonged the survival time of mice administered a lethal dose of compound 48/80. On the other hand, MHR did not inhibit type I hypersensitivity.
Conclusion:
The inhibitory action of MHF on the type I allergic reaction was due to a reduction or delay in histamine release from mast cells. MHF may be a potent anti-allergic agent.
Insights
Medium molecular weight heparinyl phenylalanine (MHF) effectively inhibits type I hypersensitivity reactions by reducing histamine release. This compound shows potential as a potent anti-allergic agent, unlike MHR.
Area of Science:
- Immunology
- Pharmacology
- Allergy Research
Background:
- Heparin (HE) derivatives were synthesized to mitigate side effects associated with anticoagulant action.
- Medium molecular weight heparinyl phenylalanine (MHF) and medium molecular weight heparinyl arginine (MHR) were developed from heparin.
Purpose of the Study:
- To investigate the inhibitory effects of MHF and MHR on type I hypersensitivity.
- To compare the anti-allergic potential of MHF and MHR.
Main Methods:
- Synthesis of MHF and MHR from heparin.
- Evaluation of MHF and MHR in a rat model of homologous passive cutaneous anaphylaxis.
- Assessment of MHF and MHR effects on histamine and compound 48/80-induced reactions in mice.
Main Results:
- MHF significantly inhibited 48-hour homologous passive cutaneous anaphylaxis in rats.
- MHF prolonged survival time in mice treated with lethal compound 48/80 but did not affect histamine-induced mortality.
- MHR demonstrated no inhibitory effect on type I hypersensitivity.
Conclusions:
- MHF's anti-allergic action is attributed to reduced or delayed histamine release from mast cells.
- MHF exhibits potential as a powerful anti-allergic therapeutic agent.
- MHF offers a promising alternative for managing type I allergic reactions.
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