期刊
JOURNAL OF PHARMACY AND PHARMACOLOGY
卷 70, 期 9, 页码 1242-1252出版社
OXFORD UNIV PRESS
DOI: 10.1111/jphp.12952
关键词
artocarpanone; artocarpin; Artocarpus heterophyllus; immunosuppression; phagocytosis
资金
- Universiti Kebangsaan Malaysia [AP2014-023]
ObjectivesTo investigate the effects of flavonoids isolated from Artocarpus heterophyllus. heartwood on chemotaxis, phagocytosis, reactive oxygen species (ROS) production and myeloperoxidase (MPO) activity of human phagocytes. MethodsChemotaxis was evaluated using a modified Boyden chamber and phagocytosis was determined by flowcytometer. Respiratory burst was investigated by luminol-based chemiluminescence assay while MPO activity was determined by colorimetric assay. Key findingsArtocarpanone and artocarpin strongly inhibited all steps of phagocytosis. Artocarpanone and artocarpin showed strong chemotactic activity with IC50 values of 6.96 and 6.10 m, respectively, which were lower than that of ibuprofen (7.37 m). Artocarpanone was the most potent compound in inhibiting ROS production of polymorphonuclear leucocytes and monocytes with IC50 values comparable to those of aspirin. Artocarpin at 100 g/ml inhibited phagocytosis of opsonized bacteria (28.3%). It also strongly inhibited MPO release with an IC50 value (23.3 m) lower than that of indomethacin (69 m). Structure-activity analysis indicated that the number of hydroxyl group, the presence of prenyl group and variation of C-2 and C-3 bonds might contribute towards their phagocytosis. ConclusionsArtocarpanone and artocarpin were able to suppress strongly the phagocytosis of human phagocytes at different steps and have potential to be developed into potent anti-inflammatory agents.
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