The antiallergy and potential anticancer drug tranilast has been patented for treating Alzheimer's disease (AD), in which amyloid β-protein (Aβ) plays a key pathogenic role. We used solution NMR to determine that tranilast binds to Aβ40 monomers with ∼300 μM affinity. Remarkably, tranilast increases Aβ40 fibrillation more than 20-fold in the thioflavin T assay at a 1:1 molar ratio, as well as s...

PURPOSE The synthesis of chemokines and adhesion molecules by corneal fibroblasts contributes to the development of corneal lesions in severe ocular allergy. The effects of the antiallergy drug tranilast on the expression of such molecules were examined in human corneal fibroblasts. METHODS The release of chemokines into culture supernatants and the expression of vascular endothelial cell adh...

Results In LAD2 cells, both resveratrol and tranilast (10 ug/ml) inhibited degranulation induced by mast cell activators IgE/anti-IgE (39% and 19%, respectively; P<0.03), compound 48/80 (9% and 6%), and substance P (23% and 28%; P<0.03). This may be attributable to modulation of Ca levels, as resveratrol, and to a lesser extent tranilast, attenuated substance P-dependent increases in [Ca]i. Res...

BACKGROUND Anti-allergic drugs, such as tranilast and ketotifen, inhibit the release of chemokines from mast cells. However, we know little about their direct effects on the exocytotic process of mast cells. Since exocytosis in mast cells can be monitored electrophysiologically by changes in the whole-cell membrane capacitance (Cm), the absence of such changes by these drugs indicates their mas...

BACKGROUND Cancer stem cells (CSCs) have increased resistance to cancer chemotherapy. They can be enriched as drug-surviving CSCs (D-CSCs) by growth with chemotherapeutic drugs, and/or by sorting of cells expressing CSC markers such as aldehyde dehydrogenase-1 (ALDH). CSCs form colonies in agar, mammospheres in low-adherence cultures, and tumors following xenotransplantation in Scid mice. We hy...

it has been reported that cxcl12 binding to cxcr4 induces several intracellular signaling pathways, and enhances survival, proliferation, and migration of malignant cells. herein we examined the effects of anti-estrogen tamoxifen and anti-allergic tranilast drugs as a single or in combination on invasion by two in vitro invasion assays, wound-healing and matrigel invasion on mcf-7 and mda-mb-23...

It has been reported that CXCL12 binding to CXCR4 induces several intracellular signaling pathways, and enhances survival, proliferation, and migration of malignant cells. In the present study, we examined the effects of anti-estrogen tamoxifen and anti-allergic tranilast drugs as a single or in combination on invasion by two in-vitro invasion assays, wound-healing and matrigel invasion on MCF-...

Tranilast (N-[3,4-dimethoxycinnamoyl]-anthranilic acid; Rizaben®) is an anti-allergy drug approved for use in Japan and South Korea, also used against asthma, autoimmune diseases, and atopic and fibrotic pathologies. The antitumor potential of tranilast is attracting considerable interest. This review summarizes recent evidence concerning the effect of tranilast on different tumor types and dis...

N(3,4-dimethoxycinnamoyl) anthranilic acid (tranilast) prevents the synchronous upregulation of isoforms and receptors of the transforming growth factor (TGF)-beta system after arterial injury and reduces restenosis after human coronary angioplasty. However, the effects of tranilast and the importance of the TGF-beta system in stent restenosis, in which inward remodeling is unimportant but infl...

The purpose of this study was to determine the efficacy and the possible mechanism of action of a recently synthesized drug, TAS-301 [3-bis (4-methoxyphenyl)methylene-2-indolinone], on intimal formation in comparison with those of tranilast, the clinical efficacy of which was reported earlier. Rat carotid arteries were injured using a balloon catheter. Neointimal thickening, measured 14 days af...