Health & Environmental Research Online (HERO)


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8345980 
Journal Article 
Screening of leukotriene B4 receptor antagonist activity from the herbal drugs 
Lee, HJ; Ryu, JH 
2000 
31 
3 
273-279 
Korean 
Leukotriene B4 (LTB4) is a pro-inflammatory mediator synthesized in myeloid cells from arachidonic acid. Elevated levels of LTB4 have been found in a number of inflammatory diseases and levels are related to disease activity in some of these. Because LTB4 interacts with cells through specific cell surface receptors, LTB4 receptor blockade is the most specific approach to reduce the pathogenic role of LTB4. In order to find LTB4 receptor antagonist from plants, we screened the LTB4 receptor antagonistic activity of the methanol extract and solvent fractions of herbal drugs. The ability of samples to inhibit specific binding of [3H]-LTB4 to human peripheral neutrophils was used as assay to evaluate the antagonistic activity of plant materials. Among the tested methanol extracts of herbal drugs, Mori Radicis Cortex, Perillae Semen, Armeniacae Semen and Sophorae subprostratae Radix showed potent inhibitory activity above 70% at the concentration of 100 μg/ml. The inhibitory activities of LTB4 binding to human neutrophils were evaluated for several solvent fractions at three different concentrations. Especially, hexane soluble fractions of Anemarrhenae Rhizoma and Embeliae Radix, and ethyl acetate soluble fractions of Aristolochiae Fructus, Magnoliae Cortex and Zingiberis Rhizoma crudus showed moderate activity at 25 μg/ml. These fractions were promising candidates for the study of the activity-guided chromatographic purification of active compounds. Silica gel column chromatography of hexane soluble fractions of Anemarrhenae Rhizoma and Embeliae Radix gave very active sub-fractions, AA-4 and ES-4, and their inhibition activities of LTB4 binding to human neutrophil at 30 μg/ml were 78% and 62%, respectively. From these results we could anticipate new LTB4 receptor antagonist from herbal drugs, and the block of LTB4 effects may provide beneficial in neutrophil mediated diseases such as inflammation and bronchial asthma. 
Antagonist; Asthma; Inflammation; Leukotriene B4; Receptor; Screening