Comparative effect of leukotriene B4 and leukotriene B5 on calcium mobilization in human neutrophils.
Leukotriene B4 (LTB4) is reported to exert its biological activity in neutrophils through the increase in cytosolic free calcium that follows binding to its specific receptor. Leukotriene B5 has been shown to be far less active than LTB4. Therefore we compared the capacity of LTB4 and LTB5 to stimulate the rise in cytosolic free calcium using fura-2-loaded human neutrophils, to assess the relationship between the calcium mobilizing activity and biological potency of LTB4 and LTB5. At any concentration tested, LTB5 was less active than LTB4 in increasing cytosolic free calcium. ED50 for LTB4 and LTB5 were 5 X 10(-10) M and 5 X 10(-9) M, respectively. The difference in the binding affinities of LTB4 and LTB5 to the LTB4 receptor has been reported to explain the difference in their biological activities. In the present study we further demonstrated that the calcium mobilizing activity of LTB4 and LTB5 also correlates the different biological activity of the two compounds.
Seya
A
A
Second Department of Internal Medicine, School of Medicine, Chiba University, Japan.
Terano
T
T
Tamura
Y
Y
Yoshida
S
S
D002118:Calcium / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D015118:Eicosapentaenoic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology; D005453:Fluorescence; D006801:Humans; D007975:Leukotriene B4 / Q000494:pharmacology* / Q000031:analogs & derivatives; D009504:Neutrophils / Q000378:metabolism*
D007975:Leukotriene B4; C040212:leukotriene B5; D015118:Eicosapentaenoic Acid; D002118:Calcium