Heat shock protein 47 (HSP47), a collagen-specific molecular chaperone, is causally related to fibrotic diseases, including idiopathic pulmonary fibrosis. The identification of Compounds that interfere with the HSP47-collagen interaction is essential for the development of relevant therapeutics. Herein, we prepared human HSP47 as a soluble fusion protein expressed in E. coli and established an assay system for HSP47 inhibitor screening. We screened a natural and synthetic Compound library established at Nagasaki University. Among 1023 Compounds, 13 exhibited inhibitory activity against human HSP47, of which three inhibited its function in a dose-dependent manner. Epigallocatechin-3-O-gallate, one of these three Compounds, is a typical polyphenol Compound derived from tea leaves. Structurally related Compounds were synthesized and examined for their activity, revealing a hydroxyl group at A-ring position 5 as important for its activity. The present findings provide valuable insight for the development of natural product-derived therapeutics for fibrotic diseases, including idiopathic pulmonary fibrosis. 相似文献
Summary: Wear behavior correlations with morphology have been established from polytetrafluoroethylene (PTFE) drawn at 200, 327, and 375 °C with draw ratio about 4. The friction coefficient and wear rate for PTFE drawn at 327 °C are lower and the wear rate is lower than that of undrawn PTFE by about 30%. The structures of samples were characterized by scanning electron microscope (SEM), DSC, and wide angle X‐ray diffraction (WAXD). Results indicate that the debris morphologies of samples are different. The differences in the tribological behavior of undrawn and drawn samples were attributed to the improvement of the degree of the crystalline, fibrillation, and orderliness by drawing, especially, for PTFE drawn at 327 °C. The orderliness of molecular arrangement along the drawn direction is also higher for PTFE drawn at 327 °C than those of PTFE drawn at 200 and 375 °C, respectively. Therefore, the intensity of covalent bond along drawn direction is higher. The shear resistance and the deformability of the material are greatly improved and the size of the wear breakage unit decreases, which results in a good tribological property for PTFE drawn at 327 °C.
SEM morphology of fractured surface perpendicular to the draw direction for PTFE drawn at 327 °C. 相似文献
Ferromagnetic and perovskite-like thin films (<1m) of La1–xCaxMnO3+ have been routinely prepared by heat treatment of an amorphous La–Ca–Mn precursor. The precursor was electrodeposited cathodically in the absence of oxygen and water onto polished silver substrates from a nonaqueous solution of the components' nitrates. Analysis by X-ray diffraction and SQUID magnetometry shows these materials exhibit the appropriate structural and magnetic phases indicative of colossal magnetoresistance. 相似文献