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2.
J Nat Prod ; 84(2): 195-203, 2021 02 26.
Artigo em Inglês | MEDLINE | ID: mdl-33534559

RESUMO

Separating the immunosuppressive activity of FK506 (1) from its neurotrophic activity is required to develop FK506 analogues as drugs for the treatment of neuronal diseases. Two new FK506 analogues, 9-deoxo-36,37-dihydro-prolylFK506 (2) and 9-deoxo-31-O-demethyl-36,37-dihydro-prolylFK506 (3) containing a proline moiety instead of the pipecolate ring at C-1 and modifications at the C-9/C-31 and C-36-C-37 positions, respectively, were biosynthesized, and their biological activities were evaluated. The proline substitution in 9-deoxo-36,37-dihydroFK506 and 9-deoxo-31-O-demethyl-36,37-dihydroFK506 reduced immunosuppressive activity by more than 120-fold, as previously observed. Compared with FK506 (1), 2 and 3 exhibited ∼1.2 × 105- and 2.2 × 105-fold reductions in immunosuppressive activity, respectively, whereas they retained almost identical neurite outgrowth activity. Furthermore, these compounds significantly increased the strength of synaptic transmission, confirming that replacement of the pipecolate ring with a proline is critical to reduce the strong immunosuppressive activity of FK506 (1) while enhancing its neurotrophic activity.


Assuntos
Crescimento Neuronal/efeitos dos fármacos , Neurônios/efeitos dos fármacos , Tacrolimo/análogos & derivados , Animais , Células Cultivadas , Fermentação , Hipocampo/citologia , Imunossupressores , Camundongos Endogâmicos ICR , Estrutura Molecular , Ácidos Pipecólicos , Streptomyces/metabolismo
3.
Mitochondrial DNA A DNA Mapp Seq Anal ; 27(5): 3684-6, 2016 09.
Artigo em Inglês | MEDLINE | ID: mdl-26366825

RESUMO

We have determined the complete mitochondrial genome of Gekko japonicus, whose status as an endemic or invasive species is currently under debate in Korea. The total genome size is 16 544 bp and consists of 13 protein-coding genes, 2 rRNA (12S and 16S RNA) genes, 22 tRNAs and 2 non-coding regions. The A + T content of the genome is 55.8% (A, 31.2%; C, 29.4%; T, 24.6%; G, 14.9%). Phylogenetic analysis shows that G. japonicus has a close phylogenetic relationship with both G. swinhonis and G. chinensis. Our result will facilitate further genetic studies of this species to ascertain its species status.


Assuntos
Genoma Mitocondrial , Lagartos/genética , Animais , Composição de Bases , Códon de Iniciação , Códon de Terminação , Complexo IV da Cadeia de Transporte de Elétrons/genética , Evolução Molecular , Feminino , Proteínas Mitocondriais/genética , NADH Desidrogenase/genética , Filogenia , RNA Ribossômico/genética , RNA Ribossômico 16S/genética , RNA de Transferência/genética , Sequenciamento Completo do Genoma
4.
Zoolog Sci ; 30(11): 929-37, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24199858

RESUMO

To study the function of arginine vasotocin (AVT) in a specific courtship behavior (body undulation) in male Hynobius leechii, we injected various doses of AVT or an AVT V1a or V2 receptor antagonist into breeding and non-breeding males. After these injections, we placed the males alone or with breeding females in Petri dishes and measured the incidence and frequency of body undulation. Additionally, to test whether AVT modulates the olfactory response of males, we exposed breeding males that were injected with AVT to female odors and measured the same response. Both breeding and non-breeding males intraperitoneally injected with 50 or 100 µg of AVT exhibited body undulation. Additionally, breeding males intraperitoneally injected with 50 or 100 µg of AVT exhibited an increased frequency of body undulation when exposed to female odors. The intraperitoneal injection of 5, 25, or 50 µg of the AVT V1a or V2 receptor antagonist did not significantly decrease the incidence or frequency of body undulation of 100 µg AVT-injected breeding males. However, in a post-hoc experiment, the breeding males that were subcutaneously injected with 100 µg of the AVT V1a receptor antagonist exhibited a significant decrease in the frequency of body undulation, induced by exposure to females. Additionally, a central injection of 1 µg of AVT into the brain induced body undulation in breeding males. Our results show that AVT not only induces a specific courtship behavior in male H. leechii via AVT V1a receptors but also modulates the olfactory response.


Assuntos
Comportamento Sexual Animal/efeitos dos fármacos , Olfato/efeitos dos fármacos , Urodelos/fisiologia , Vasotocina/farmacologia , Animais , Encéfalo/efeitos dos fármacos , Encéfalo/fisiologia , Relação Dose-Resposta a Droga , Feminino , Masculino , Vasotocina/administração & dosagem
5.
Zoolog Sci ; 28(8): 593-9, 2011 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-21801000

RESUMO

To determine the habitat usage and movement patterns of the viviparous aquatic snake Oocatochus rufodorsatus (formerly Elaphe rufodorsata), we radio-tracked 21 snakes on agricultural lands during two active seasons in 2007 and 2008. Male and female snakes stayed close to aquatic habitats such as paddy fields and agricultural ponds during both breeding and non-breeding periods, except when the snakes moved to dry terrestrial areas to hibernate in late fall. The use of different structural features in the habitat, such as ground, tree, underground, and water, varied depending on the air and water temperatures, female's reproductive conditions, and the time of day. Male and female snakes moved about 17 m daily and postpartum females moved farther than antepartum females. The home ranges of males and females were 0.45 ha and 0.47 ha, respectively, and the year-round home range of this species was approximately 1.54 ha (95% fixed kernel). Thus, to conserve a population of O. rufodorsatus in our study area, areas including both aquatic and terrestrial habitats within a radius of 150 m from a core pond habitat must be preserved.


Assuntos
Ecossistema , Atividade Motora , Serpentes/fisiologia , Animais , Demografia , Feminino , Masculino , Estações do Ano , Caracteres Sexuais , Telemetria
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