The chlorite-based drug solution WF has been successfully applied to dampen strong inflammatory disease states and to improve wound healing processes. However, the molecular mechanisms of this drug are not well understood. This study is directed to investigate how WF and its components affect the expression of surface markers and sulphated proteoglycans and glycosaminoglycans in proinflammatorystimulated monocytes and macrophages.Human blood-derived macrophages were cultivated from monocytes in the presence of U/ml granulocyte-macrophage colony-stimulating factor and activated by a mixture of ng/ml lipopolysaccharide LPS and ng/ml interferon γ IFNγ . These cells were identified and characterised by their specific cell-surface receptors CD , CD , CD , CD , CD , and CD using flow cytometry approaches. The sulphation level of proteoglycans and glycosaminoglycans was assessed by the Blyscan™ dye-binding assay. The expression of the surface marker CD , a proteoglycan with sulphated glycosaminoglycan side chains, was followed by antibodies against CD . The binding of fluorescence-labelled hyaluronan to CD was also investigated by flow cytometry. All analyses were performed after incubation of monocytes and macrophages with WF or with its main components chlorite and chlorate.The drug substance WF inhibited the activation of LPS/IFNγ-stimulated human monocyte-derived macrophages. Among them are the diminished expression of proinflammatory surface markers, the inhibition of the expression of the hyaluronan receptor CD , and the binding of hyaluronan to CD . Further, the overall amount of sulphated proteoglycans and glycosaminoglycans was down-regulated by WF . These in vitro experiments indicate that WF is able to inhibit the proinflammatory activation of macrophages. The results suggested that chlorite is the active principle in WF as chlorite caused principally the same changes in targets as WF . The WF component chlorate inhibited only the overall sulphation level of proteoglycans and glycosaminoglycans and the binding of hyaluronan to CD .