Tranilast, an orally active anti-allergic drug, up-regulates the anti-inflammatory heme oxygenase-1 expression but down-regulates the pro-inflammatory cyclooxygenase-2 and inducible nitric oxide synthase expression in RAW264.7 macrophages

Tranilast: A review of its therapeutic applications

“…These results suggest that tranilast-mediated suppression of microglial iNOS activity induced by IFN-␥ involves the inhibition of NF-B-dependent iNOS expression [17,175]. It also inhibited the release of NO from activated macrophages [63] and corrected eNOS and iNOS synthase expression in macrophages [18]. Therefore, tranilast could alter NO metabolism and bioavailability.…”

“…Furthermore, studies have revealed the importance of mast cells in the pathogenesis of inflammatory arthritis [43]. On the other hand, since tranilast inhibited the expression of many cytokines [18,40], chemokines [22,23] and proteases [28,29] from various cell types, including fibroblasts, lymphocytes, macrophages and neutrophils, it may be advantageous in the treatment of arthritis [43]. In addition, tranilast, by inhibiting angiogenesis and VEGF-induced effects [76], had suppressive effects in autoimmune disease models [7].…”

“…It also inhibited PGD synthetase in spleen [34] and brain [35]. On the other hand, tranilast increased the expression of anti-inflammatory cytokines, confirming its role in regulating anti-allergic responses; it induced heme oxygenase (HO)-1 expression and activity [18,36], and it also increased production of IL-4 and IL-10 [7].…”

“…The suppressive effects and cells include: histamine release from mast cells [2,15], COX-2 expression in fibroblasts [16], iNOS expression in microglia cells [17], COX-2 and iNOS expression in macrophages [18], IL-6 secretion in endothelial cells [19], IL-8 from monocytes [20], IL-5 in lung and spleen cells [21], eotaxin-1 production from conjunctival fibroblasts [22], and MCP-1 in mesangial cells [23]. In addition, it also inhibits the surface expression of VCAM-1 in fibroblasts [19,24], expression of ICAM-1 from monocytes [25], release of IL-2 and IL-1␤ from monocytes and macrophages [26], release of TGF-␤1 from fibroblasts [17,26] also from mast cells and basophils [27], MMP-2 and -9 production from fibroblasts and neutrophils [28,29] as well as INF-␥ and TNF-␣ production [7].…”

Evaluation of the effect of tranilast on rats with spinal cord injury

“…It is also known to inhibit fibrotic scar formation and fibrosis [9,30]. Additionally, tranilast has anti-inflammatory effects [12,20,23,25,26].…”