The nanoparticles of the hydrophobic drug of danazol with narrow size distribution are facilely prepared by controlled high-gravity anti-solvent precipitation （HGAP） process. Intensified micromixing and uniform nucl...The nanoparticles of the hydrophobic drug of danazol with narrow size distribution are facilely prepared by controlled high-gravity anti-solvent precipitation （HGAP） process. Intensified micromixing and uniform nucleation environment are created by the high-gravity equipment （rotating packed bed） in carrying out the anti-solvent precipitation process to produce nanoparticles. The average particle size decreases from 55 μm of the raw danazol to 190 nm of the nanoparticles. The Brunauer-Emmett-Teller （BET） surface area sharply increases from 0.66 m^2·g^-1 to 15.08 m^2·g^-l. Accordingly, the dissolution rate is greatly improved. The molecular state, chemical composition, and crystal form of the danazol nanoparticles remains unchanged after processing according to Fourier transform infrared （FTIR） and X-ray diffraction （XRD）, The high recovery ratio and continuous production capacity are highly appreciated in industry. Therefore, the HGAP method might offer a general and facile platform for mass production of hydrophobic pharmaceutical danazol particles in nanometer range.展开更多
Objective: To study the effect of danazol in vitro on the cytokine production of peritoneal macrophages in patients with endometriosis. Methods: Peritoneal macrophages were obtained from 14 cases of patients with endo...Objective: To study the effect of danazol in vitro on the cytokine production of peritoneal macrophages in patients with endometriosis. Methods: Peritoneal macrophages were obtained from 14 cases of patients with endometriosis. Danazol at concentration of 10 ng/ml and 100 ng/ml were added to the peritoneal macrophages cultures. The tumor necrosis factor a (TNFα)and interleukin 6 (IL-6) levels of peritoneal macrophage supernatant were detected by enzyme linked immunoassay. Results: Danazol at concentration of 100 ng/ml significantly inhibited TNFα and IL-6 production of peritoneal macrophages in patients with endometriosis. Conclusion: It is suggested that the immunomodulatory effect of danazol may contributed to the efficacy in the treatment of endometriosis.展开更多
There is scarce information about the effects of danazol and its derivatives at cardiovascular level. In addition, to date the cellular site and mechanism of action of danazol at the cardiovascular level is very confu...There is scarce information about the effects of danazol and its derivatives at cardiovascular level. In addition, to date the cellular site and mechanism of action of danazol at the cardiovascular level is very confusing. In order to clarify those phenomena in this study, a danazol derivative was synthesized with the objective of evaluating its activity on perfusion pressure and coronary resistance and comparing this phenomenon with the effect exerted by danazol. The Langendorff technique was used to measure changes on perfusion pressure and coronary resistance in an isolated rat heart model in the absence or presence of danazol and its derivative. Additionally, to characterize the molecular mechanism involved in the inotropic activity induced by danazol derivative was evaluated by measuring left ventricular pressure in the absence or presence of following compounds;flutamide, prazosin, metoprolol, indomethacin and nifedipine. The results showed that danazol derivative significantly increased the perfusion pressure and coronary resistance in comparison with the control conditions and danazol. Additionally, other data indicate that the danazol derivative increases left ventricular pressure in a dose-dependent manner;nevertheless, this phenomenon was significantly inhibited by flutamide. These data suggest that danazol derivative induces positive inotropic activity through of the activation androgen receptor.展开更多
基金Supported by the National High Technology Research and Development Program of China (2006AA030202)the Talent Training Program of Beijing (2007B022)
文摘The nanoparticles of the hydrophobic drug of danazol with narrow size distribution are facilely prepared by controlled high-gravity anti-solvent precipitation （HGAP） process. Intensified micromixing and uniform nucleation environment are created by the high-gravity equipment （rotating packed bed） in carrying out the anti-solvent precipitation process to produce nanoparticles. The average particle size decreases from 55 μm of the raw danazol to 190 nm of the nanoparticles. The Brunauer-Emmett-Teller （BET） surface area sharply increases from 0.66 m^2·g^-1 to 15.08 m^2·g^-l. Accordingly, the dissolution rate is greatly improved. The molecular state, chemical composition, and crystal form of the danazol nanoparticles remains unchanged after processing according to Fourier transform infrared （FTIR） and X-ray diffraction （XRD）, The high recovery ratio and continuous production capacity are highly appreciated in industry. Therefore, the HGAP method might offer a general and facile platform for mass production of hydrophobic pharmaceutical danazol particles in nanometer range.
文摘Objective: To study the effect of danazol in vitro on the cytokine production of peritoneal macrophages in patients with endometriosis. Methods: Peritoneal macrophages were obtained from 14 cases of patients with endometriosis. Danazol at concentration of 10 ng/ml and 100 ng/ml were added to the peritoneal macrophages cultures. The tumor necrosis factor a (TNFα)and interleukin 6 (IL-6) levels of peritoneal macrophage supernatant were detected by enzyme linked immunoassay. Results: Danazol at concentration of 100 ng/ml significantly inhibited TNFα and IL-6 production of peritoneal macrophages in patients with endometriosis. Conclusion: It is suggested that the immunomodulatory effect of danazol may contributed to the efficacy in the treatment of endometriosis.
文摘There is scarce information about the effects of danazol and its derivatives at cardiovascular level. In addition, to date the cellular site and mechanism of action of danazol at the cardiovascular level is very confusing. In order to clarify those phenomena in this study, a danazol derivative was synthesized with the objective of evaluating its activity on perfusion pressure and coronary resistance and comparing this phenomenon with the effect exerted by danazol. The Langendorff technique was used to measure changes on perfusion pressure and coronary resistance in an isolated rat heart model in the absence or presence of danazol and its derivative. Additionally, to characterize the molecular mechanism involved in the inotropic activity induced by danazol derivative was evaluated by measuring left ventricular pressure in the absence or presence of following compounds;flutamide, prazosin, metoprolol, indomethacin and nifedipine. The results showed that danazol derivative significantly increased the perfusion pressure and coronary resistance in comparison with the control conditions and danazol. Additionally, other data indicate that the danazol derivative increases left ventricular pressure in a dose-dependent manner;nevertheless, this phenomenon was significantly inhibited by flutamide. These data suggest that danazol derivative induces positive inotropic activity through of the activation androgen receptor.
