根据药物设计原理,设计并合成了一系列二甲吡唑-1,3-硫氮杂茚衍生物(6a^6o),其结构经1 H NMR,13 C NMR,IR和MS(EI)表征。采用动物模型验证了6a^6o的活性。结果表明:当取代基为正丁基、正戊基、邻位氟取代苄基和2,6-二氯取代苄基时,化合...根据药物设计原理,设计并合成了一系列二甲吡唑-1,3-硫氮杂茚衍生物(6a^6o),其结构经1 H NMR,13 C NMR,IR和MS(EI)表征。采用动物模型验证了6a^6o的活性。结果表明:当取代基为正丁基、正戊基、邻位氟取代苄基和2,6-二氯取代苄基时,化合物表现出较好的抗癫痫活性。其中化合物6g的活性和保护指数均优于阳性对照药丙戊酸钠,并且在MTT实验中未见明显毒性。展开更多
Background Cathespin-B （cath-B） is an important proteolytic enzyme involved in the disease course of invasion in many types of cancer. Cath-B expression in subcutaneous heteroplastic pancreatic carcinoma in nude mic...Background Cathespin-B （cath-B） is an important proteolytic enzyme involved in the disease course of invasion in many types of cancer. Cath-B expression in subcutaneous heteroplastic pancreatic carcinoma in nude mice has not been studied. We investigated the role of cath-B in a model of heteroplastic pancreatic carcinoma in BALB/c nude mice. Methods Thirty-two six-week-old female BALB/c nude mice were equally divided into four groups. PANC-1 cells were inoculated subcutaneously in the left axillary region. Besides volume, weight of subcutaneous tumor, and change in body weight, cath-B expression in each group was measured by immunohistochemical staining, PCR and Western blotting. Its relationship to microvessel density （MVD）, CD44v6, and placenta growth factor （PLGF） was also examined. CA-074Me, a specific inhibitor of cath-B, was injected intraperitoneally （i.p.） at different stages of tumor growth in group B and C. Gemcitabine （GEM）, was also injected （i.p.） in group D to compare anti-tumor efficacy with CA-074Me. Results Expression of cath-B at different levels was related to tumor growth, MVD, and PLGF expression. In group A （control group）, cath-B expression was enhanced more than that seen in other groups. CA-074Me clearly inhibited cath-B expression and tumor growth in group B. There was no difference between group C and D with respect to anti-tumor effect. Conclusions Cath-B correlates with the growth and angiogenesis of tumors, but not with the adhesion induced by CD44v6. CA-074Me clearly inhibited cath-B expression and demonstrated an anti-neoplastic and anti-angiogenesis effect.展开更多
n contrast to the so-called intraocular pressure, which is .the transcomeal pressure difference, it is thetrans-lamina cribrosa pressure difference, which is of importance for physiology and pathophysiology of the opt...n contrast to the so-called intraocular pressure, which is .the transcomeal pressure difference, it is thetrans-lamina cribrosa pressure difference, which is of importance for physiology and pathophysiology of the optic nerve head. The trans-lamina cribrosa pressure difference is the difference between the pressure in the intraocular compartment （i.e., the so-called intraocular pressure） minus the retrobulbar pressure, which is formed by the orbital cerebrospinal fluid （CSF）I pressure and the retrobulbar optic nerve tissue pressure. This anatomical fact has been the basis for the speculation that some patients with so-called normal intraocular pressure glaucoma have an abnormally low orbital CSF pressure. Previous clinical studies have supported this hypothesis.2＇3 The purpose of this study is to report on a patient with low CSF pressure and co-existent open-angle glaucoma with normal intraocular pressure.展开更多
文摘根据药物设计原理,设计并合成了一系列二甲吡唑-1,3-硫氮杂茚衍生物(6a^6o),其结构经1 H NMR,13 C NMR,IR和MS(EI)表征。采用动物模型验证了6a^6o的活性。结果表明:当取代基为正丁基、正戊基、邻位氟取代苄基和2,6-二氯取代苄基时,化合物表现出较好的抗癫痫活性。其中化合物6g的活性和保护指数均优于阳性对照药丙戊酸钠,并且在MTT实验中未见明显毒性。
文摘Background Cathespin-B （cath-B） is an important proteolytic enzyme involved in the disease course of invasion in many types of cancer. Cath-B expression in subcutaneous heteroplastic pancreatic carcinoma in nude mice has not been studied. We investigated the role of cath-B in a model of heteroplastic pancreatic carcinoma in BALB/c nude mice. Methods Thirty-two six-week-old female BALB/c nude mice were equally divided into four groups. PANC-1 cells were inoculated subcutaneously in the left axillary region. Besides volume, weight of subcutaneous tumor, and change in body weight, cath-B expression in each group was measured by immunohistochemical staining, PCR and Western blotting. Its relationship to microvessel density （MVD）, CD44v6, and placenta growth factor （PLGF） was also examined. CA-074Me, a specific inhibitor of cath-B, was injected intraperitoneally （i.p.） at different stages of tumor growth in group B and C. Gemcitabine （GEM）, was also injected （i.p.） in group D to compare anti-tumor efficacy with CA-074Me. Results Expression of cath-B at different levels was related to tumor growth, MVD, and PLGF expression. In group A （control group）, cath-B expression was enhanced more than that seen in other groups. CA-074Me clearly inhibited cath-B expression and tumor growth in group B. There was no difference between group C and D with respect to anti-tumor effect. Conclusions Cath-B correlates with the growth and angiogenesis of tumors, but not with the adhesion induced by CD44v6. CA-074Me clearly inhibited cath-B expression and demonstrated an anti-neoplastic and anti-angiogenesis effect.
文摘n contrast to the so-called intraocular pressure, which is .the transcomeal pressure difference, it is thetrans-lamina cribrosa pressure difference, which is of importance for physiology and pathophysiology of the optic nerve head. The trans-lamina cribrosa pressure difference is the difference between the pressure in the intraocular compartment （i.e., the so-called intraocular pressure） minus the retrobulbar pressure, which is formed by the orbital cerebrospinal fluid （CSF）I pressure and the retrobulbar optic nerve tissue pressure. This anatomical fact has been the basis for the speculation that some patients with so-called normal intraocular pressure glaucoma have an abnormally low orbital CSF pressure. Previous clinical studies have supported this hypothesis.2＇3 The purpose of this study is to report on a patient with low CSF pressure and co-existent open-angle glaucoma with normal intraocular pressure.
