1,721,044 research outputs found
Sattabacins and Sattazolins: new biologically active compounds with antiviral properties extraded from a Bacillus sp
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Karalicin, a new biologically active compound from Pseudomonas fluorescens/putida. I: production, physico-chemical properties and structure elucidation.
No full textPharmacological analysis of the methanolic extract and sorocein A, a new Diels-Alder compound isolated from the roots of Sorocea bonplandii bailon in the isolated rat uterus and guinea pig ileum
No full textThis study examines the effects of methanolic extract (ME) and its main constituent, sorocein A, isolated from the roots of Sorocea bonplandii on agonist-induced contractions in the rat uterus (RU) and in the guinea pig ileum (GPI) in vitro. ME (25-100 μg/ml), added to RU for 20 min, caused a graded and parallel shift to the right of bradykinin (BK)-mediated contractions with an apparent pA 2 value (-log g/ml) of 5.0. ME caused a rightward shift of the acetylcholine (ACh) and oxytocin-induced contractions associated with a marked depression of their maximal responses. In GPI, ME produced a non-competitive antagonism against BK-induced contraction, while responses to ACh and histamine were shifted to the right in a graded fashion, yielding pA 2 values (g/ml) of 5 in both cases. The purified compound sorocein A (15-60 μM) caused a parallel and graded rightward displacement of BK and ACh concentration-response curves in RU with pA 2 values (molar basis) of 4.9 and 5.2. Sorocein A also dose-dependently shifted to the right ACh and histamine-mediated contractions in GPI, yielding pA 2 values of 5.1 and 4.8, respectively. However, sorocein A antagonized in a non-competitive manner BK-induced contraction in GPI, characterized by a graded displacement to the right of the dose-response curve and progressive depression of the maximal contraction
Policondrite ricorrente e sindrome mieloproliferativa cronica in soggetto con spondilite anchilosante: effetto del trattamento con anti-TNF alpha.
No full textPossibile coinvolgimento di cellule T ad attività antiflogistica nella risposta al trattamento con infliximab nell'artrite reumatoide
No full textNovel hypotensive agents from Verbesina caracasana. Synthesis and pharmacology of Caracasanamide
No full textDiscovery of Mycobacterium tuberculosis protein tyrosine phosphatase B (PtpB) inhibitors from natural products
No full textProtein tyrosine phosphatase B (PtpB) is one of the virulence factors secreted into the host cell by Mycobacterium tuberculosis. PtpB attenuates host immune defenses by interfering with signal transduction pathways in macrophages and, therefore, it is considered a promising target for the development of novel anti-tuberculosis drugs. Here we report the discovery of natural compound inhibitors of PtpB among an in house library of more than 800 natural substances by means of a multidisciplinary approach, mixing in silico screening with enzymatic and kinetics studies and MS assays. Six natural compounds proved to inhibit PtpB at low micromolar concentrations (< 30 mu M) with Kuwanol E being the most potent with K-i = 1.6 +/- 0.1 mu M. To the best of our knowledge, Kuwanol E is the most potent natural compound PtpB inhibitor reported so far, as well as it is the first non-peptidic PtpB inhibitor discovered from natural sources. Compounds herein identified may inspire the design of novel specific PtpB inhibitors
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