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J Antibiot (Tokyo) ; 2019 Dec 12.
Artigo em Inglês | MEDLINE | ID: mdl-31831870


To find novel polymycin analogues with high antimicrobial activities and low toxicity, 36 novel polymyxin analogues were synthesized, and in which TZ40-J and TZ40-K were evaluated for their antimicrobial activities using broth microdilution method and for their haemolytic toxicity with sterile sheep blood. Preliminary safety assessments of those two compounds were carried out via the MTT cell viability assay in vitro and acute toxicity assay in vivo. Experimental data demonstrated that TZ40-J and TZ40-K were less toxic and indicate higher activities against Pseudomonas aeruginosa than polymyxin B.

Curr Pharm Des ; 2019 Dec 27.
Artigo em Inglês | MEDLINE | ID: mdl-31880242


BACKGROUND: Ghrelin (GHRL) is a polypeptide, which can specifically bind to the GHSR. The expression of GHSR has significant differences in human normal and prostate cancer tissues. It is meaningful to find an effective diagnostic method for the diagnosis and prognosis of invasive/neuroendocrine prostate cancer. METHODS: GHRL and GHSR mRNAs level were determined by quantitative real-time polymerase chain reaction in PC tissues. The expression of GHRL and GHSR proteins were assessed respectively by western blot and immunohistochemistry. GHRL polypeptide probe was synthesized through standard solid-phase synthesis of polypeptide, and labeled with Alexa Fluor 660. Confocal microscope was used to capture fluorescence images. Living imaging analysis show tumor areas of different invasiveness in mice models. RESULTS: The level of GHRL and GHSR copy number amplification and mRNA expression were increased in invasive/neuroendocrine prostate cancer, and the protein expression of GHRL and GHSR were similarly boosting in NEPC. The GHRL polypeptide probe could effectively bind to GHSR. In PC3, we found that GHRL probe specifically bind to GHSR on cell membrane and accumulated in cells through internalization after binding. Living imaging in mice models showed that there were different signal intensities in tumor areas of different invasiveness. CONCLUSION: The GHSR and GHRL might be used to the molecular imaging diagnosis for invasive/neuroendocrine prostate cancer in future.

J Antibiot (Tokyo) ; 72(4): 210-217, 2019 04.
Artigo em Inglês | MEDLINE | ID: mdl-30635615


To find novel amphotericin B (AmB) derivatives with high therapeutic potential, low toxicity, and water solubility, a series of nine N-substituted AmB derivatives were evaluated for their antifungal activity using the broth dilution method and for their hemolytic toxicity with sterile defibrinated sheep blood. Qualitative screening of the effect of the derivatives on two reference Candida albicans strains and of their solubility was performed based on the value of n (n is a positive integer), resulting in the identification of an optimal compound, NH2-(AEEA)5-AmB (DMR005; AEEA is 8-amino-3,6- dioxaoctanoic acid). Preliminary safety assessments of DMR005 were carried out via the MTT cell viability assay in vitro and acute toxicity assay in vivo. In general, DMR005 not only has higher water solubility and less toxicity than the parent polyene but also retains antifungal potency.

Anfotericina B/síntese química , Anfotericina B/farmacologia , Antifúngicos/síntese química , Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Anfotericina B/análogos & derivados , Anfotericina B/toxicidade , Animais , Antifúngicos/toxicidade , Sobrevivência Celular , Técnicas Citológicas , Modelos Animais de Doenças , Eritrócitos/efeitos dos fármacos , Células HEK293 , Hemólise/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Envenenamento/patologia , Ovinos , Solubilidade