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1.
Biomed Khim ; 63(1): 75-80, 2017 Jan.
Artigo em Russo | MEDLINE | ID: mdl-28251954

RESUMO

Melatonin is a pineal hormone that has a capacity to lower intraocular pressure; it exhibits neuroprotective and antioxidant properties that make it possible to use melatonin in the therapy of glaucoma. Analogs of melatonin having affinity to melatonin receptors are promising candidates for application as antiglaucomatous drugs. Chemical modification of the melatonin structure can in-crease efficiency, bioavailability and selectivity of these analogs. We have designed and synthe-sized a number of new 2-oxindole derivatives - ligands of melatonin MT3 subtype receptors that displayed ability to lower intraocular pressure in normotensive rabbits and high antioxidant activity against hydroxyl radical and superoxide anion-radical. The antioxidant activity of new ligands was several times higher than one of melatonin that makes them prospective therapeutic tools for the diseases that include oxidative stress. The maximal hypotensive effect of analogs was comparable to that of melatonin itself but prolonged. Combination of these properties gives an opportunity of using the presented melatonin analogs in complex therapy of glaucoma.


Assuntos
Antioxidantes/farmacologia , Glaucoma/prevenção & controle , Pressão Intraocular/efeitos dos fármacos , Melatonina/farmacologia , Fármacos Neuroprotetores/farmacologia , Hipertensão Ocular/tratamento farmacológico , Receptores de Melatonina/agonistas , Animais , Antioxidantes/síntese química , Desenho de Fármacos , Expressão Gênica , Glaucoma/metabolismo , Glaucoma/fisiopatologia , Indóis/química , Ligantes , Masculino , Melatonina/análogos & derivados , Melatonina/síntese química , Fármacos Neuroprotetores/síntese química , Hipertensão Ocular/metabolismo , Hipertensão Ocular/fisiopatologia , Oxirredução , Oxindóis , Estudos Prospectivos , Ligação Proteica , Coelhos , Receptores de Melatonina/genética , Receptores de Melatonina/metabolismo , Relação Estrutura-Atividade
2.
Radiobiologiia ; 27(2): 171-6, 1987.
Artigo em Russo | MEDLINE | ID: mdl-3575661

RESUMO

The monolayer technique, the methods of electron microscopy and IR-spectroscopy were used to study isolated nuclear membranes of calf thymus cells. The data obtained permitted to study the relationship between structural disorders induced by irradiation of membranes, the changes in their functional status, and the role played by a lipid component of membranes in these processes.


Assuntos
Núcleo Celular/efeitos da radiação , Membranas Intracelulares/efeitos da radiação , Animais , Núcleo Celular/fisiologia , Núcleo Celular/ultraestrutura , Fenômenos Químicos , Físico-Química , Membranas Intracelulares/fisiologia , Membranas Intracelulares/ultraestrutura , Lipídeos de Membrana/efeitos da radiação , Microscopia Eletrônica , Fosfolipídeos/efeitos da radiação , Espectrofotometria Infravermelho , Termodinâmica
3.
Radiobiologiia ; 25(5): 603-6, 1985.
Artigo em Russo | MEDLINE | ID: mdl-2999865

RESUMO

A comparative study was made of the effect of X-radiation on the membrane-bound glucoso-6-phosphatase of the nuclear membrane and microsomal fraction of calf thymus cells. Dose- and concentration-dependencies of inactivation of glucoso-6-phosphatase are indicative of a higher radiosensitivity of glucoso-6-phosphatase of nuclear membranes than that of microsomes. This difference in radiosensitivity is associated with the peculiarities of the composition and structural organization of these two membrane systems of a cell.


Assuntos
Glucose-6-Fosfatase/efeitos da radiação , Membranas Intracelulares/metabolismo , Animais , Bovinos , Núcleo Celular/metabolismo , Glucose-6-Fosfatase/metabolismo , Técnicas In Vitro , Microssomos/metabolismo , Tolerância a Radiação , Timo/ultraestrutura
4.
Radiobiologiia ; 24(6): 743-7, 1984.
Artigo em Russo | MEDLINE | ID: mdl-6515006

RESUMO

A study was made of the effect of X-radiation on nuclear membranes. Good resolution spectra of nuclear membrane of equal effective thickness were obtained by the method of internal reflection spectroscopy in the infrared region. The experiment indicated the presence of major characteristic bands of protein and phospholipid molecular groups of non-irradiated nuclear membranes. Conformational changes in the samples of the exposed (100 and 1000 Gy) lipoprotein complex resulted in some quantitative changes in the absorption intensities of the molecular groups of membranes. These data are consistent with the behaviour of nuclear membranes on the interphase, studied by the Langmur monolayer technique, and with the changes in the membrane morphology observed with the electron microscope.


Assuntos
Membrana Nuclear/efeitos da radiação , Animais , Bovinos , Técnicas In Vitro , Lipídeos de Membrana/efeitos da radiação , Proteínas de Membrana/efeitos da radiação , Conformação Proteica/efeitos da radiação , Espectrofotometria Infravermelho , Timo/citologia
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