New pyrene cholesterols useful for the study of the functional organization of the biological membranes, optionally in the presence of the external stimuli, e.g. temperature and pressure

摘要

Pyrene-cholesterols (I) are new. Pyrene-cholesterols of formula (I) are new. X = CH 2or O; and n = 2-10 (preferably 2-6). Independent claims are included for: (1) a process for implementing the method of detection, and optionally the photophysic measurement for the effects of given products on the biological membranes, comprises: screening of bioactive products being agonists or antagonists of receptors present in cellular membranes or on the surface of these membranes, the bioactive products are susceptible to be used for the preparation of drugs for the pathologic treatment in which the receptors intervene; in vitrodiagnosis of pathologies from cells of patients using the products as markers of these pathologies, or control of the orientation of therapeutic indication drugs comprising a bioactive product, by in vitrodetermination of agonist or antagonist effect of this drug on the patient cells to be treated by this drug; (2) a process for the study of the functional organization of the biological membranes, and implementing the method of detection, and optionally the measurement of external stimuli effects, e.g. temperature, pressure, modulation by the concentration of extrinsic agent in a lipid contained initially in the biological membranes, or the addition of a given product while influencing the organization of the biological membranes, comprises incorporation of (I) in the biological membranes, optionally application of external stimuli on the membranes, application on the biological membranes of a radiation of wavelength lambda maxat 330-350 nm i.e. characteristic absorption of pyrene, measurement of the intensity of fluorescence radiation emitted by the biological membranes to the wavelength of emission at 375-385 nm, characteristic the emission band-1 of pyrene, which intensity can be a function of polarity of the membrane, measurement of the intensity of at least any one of the two fluorescence radiation emitted by the biological membranes at 390-425 nm, characteristics the emission band 3 and 4 of pyrene, which intensity being a function of pyrene quantity, and thus (I) in the membranes, determination of the relationship between the intensity of the band 1 and that of band 3 and/or 4 with knowledge of ratios I1/I3 and/or I1/I4 and correlation between the ratio measured at the time of the previous stage, and the level of polarity of the membranes, which is related to their thickness, thus giving an indication on the functional organization of these membranes optionally in the presence of external stimuli; (3) a composition comprising (I), in mixture with a conveyor to exchange cholesterol or a phospholipid, naturally present in the membranes with (I); and (4) the preparation of (I). [Image].