estatins

The beneficial effects of atorvastatin are based on both cholesterol-dependent and independent mechanisms. The latter probably include the ability of the estatin to enhance the expression of endothelial nitric oxide synthase (eNOS) and to cause a vasodilatation. In turn, the antioxidant and anti-inflammatory actions of melatonin are related to its vascular protection. In the present study, we investigated the efficacy of the combination of melatonin plus atorvastatin against endothelial cell damage induced by inflammation and oxidative stress injury...

New cysteine protease inhibitors, named cathestatin A and B, have been discovered as metabolites of Penicillium citrinum. Cathestatins were found to be decarbamidoyl analogs of estatins and showed a specific inhibition for cysteine proteases. Cathestatins suppressed parathyroid hormone (PTH)-stimulated 45Ca release in organ cultures of chick embryonic calvaria.

Ten adult patients with severe atopic dermatitis were treated for three months with estatin, which is a metabolite of Streptomyces olivoreticuli. Bestatin has been shown to increase tumor resistance in mice, augment a variety of immune responses and to reduce the level of IgE in non-atopic healthy persons. During bestatin therapy we were not able to see any clinical change of the atopic dermatitis. No influence was found on the concentration of IgE in serum and the number of eosinophils in blood. The percentage of T lymphocytes and the Con A-induced suppressor cell activity was not changed...

New thiol protease inhibitors, estatins A and B, were isolated from the culture filtrate of Myceliophthora thermophila M4323. The basic, water-soluble inhibitors were characterized as having an agmatine, trans-epoxysuccinic acid and L-phenylalanine or L-tyrosine moieties in the structure. The molecular formulas C18H25N5O5 and C18H25N5O6 for A and B were indicated by elemental analysis and fast atom bombardment MS. Estatins were specific inhibitors against thiol proteases such as papain, ficin and bromelain...