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저자: 업로드:2017-09-18 조회수:
The coralberry could offer new hope for asthmatics. An international team of scientists says they have extracted a new type of active pharmaceutical ingredient from coralberry leaves to combat asthma, a widespread respiratory disease. The leaves contain a substance named FR900359 and it inhibited the contraction of the airways in mice. The plant itself is not exotic: it can be found in any well-stocked garden center.
Their study
("Targeted Inhibition of Gq Signaling Induces Airway Relaxation
in Mouse Models of Asthma") is published in Science
Translational Medicine.
"We...hypothesized that pharmacological Gq inhibition could serve as a central mechanism to achieve efficient therapeutic bronchorelaxation. We found that the compound FR900359 (FR), a membrane-permeable inhibitor of Gq, was effective in silencing Gq signaling in murine and human airway smooth muscle cells. Moreover, FR both prevented bronchoconstrictor responses and triggered sustained airway relaxation in mouse, pig, and human airway tissue ex vivo," write the investigators. "Inhalation of FR in healthy wild-type mice resulted in high local concentrations of the compound in the lungs and prevented airway constriction without acute effects on blood pressure and heart rate. FR administration also protected against airway hyperreactivity in murine models of allergen sensitization using ovalbumin and house dust mite as allergens. Our findings establish FR as a selective Gq inhibitor when applied locally to the airways of mice in vivo and suggest that pharmacological blockade of Gq proteins may be a useful therapeutic strategy to achieve bronchorelaxation in asthmatic lung disease."
Researchers at the
Institutes of Physiology I, Pharmaceutical Biology, and Pharmaceutical
Chemistry at the University of Bonn, and asthma specialists from Nottingham in the U.K., report
that FR appears to be more effective and has a more prolonged method of
action in relieving bronchial spasms than salbutamol.
"We have so far only tested the substance in asthmatic mice," explains junior professor Daniela Wenzel, Dr. Med., who is the study leader doing research in respiratory diseases at the Institute of Physiology I at the University of Bonn. "This compound inhibits critical signaling molecules in our cells, the Gq proteins," which are involved in key functions in many processes in the body, including control of the airway tone.