菝葜中黄酮和芪类成分的研究

目的：为阐明百合科植物菝葜的有效成分,对其根茎进行了化学成分研究。方法：运用层析手段和波谱方法分离并鉴定了5个酚性化合物。结果：它们的结构为二氢山奈酚(dihydrokaempferol,1),3,5,4′—三羟基芪(3,5,4′-trihydroxystilbene,2),3,5,2′,4′—四羟基芪(3,5,2′,4′-tetrahydroxystilbene,3),二氢山奈酚3—O-α—L—鼠李糖等(黄杞苷,dihydrokaempferol 3-O-α-L-rhamnoside,engletin,4),槲皮素4′—0-β—D—葡萄糖等(quercetin4′—O-β—D—glucoside,5)。结论：5个化合物均为首次从菝葜中得到,其中化合物1,4,5为首次从菝葜属植物中得到。     

人肝微粒体中西尼地平及其代谢物的HPLC测定法及代谢动力学

目的　建立人肝微粒体中西尼地平及其脱氢代谢物的 HPLC测定法 ,并用本法研究西尼地平在人肝微粒体中代谢的动力学。方法　色谱柱为 Hypersil C1 8柱 (2 5 0 mm× 4.6mm ID,5μm) ,流动相为乙腈 -甲醇 -0 .0 1 mol/ L四丁基溴化铵溶液 (5 5∶ 5∶ 40 ,V/ V/ V) ,柱温 5 0℃ ,检测波长 UV 2 3 8nm,样品用乙醚 -正己烷 (1∶ 1 ,V/ V)提取。用人肝微粒体研究西尼地平的代谢。结果　本法的回收率为 90 .62 %～ 1 0 9.90 % ,西尼地平和其脱氢代谢物的日间、日内 RSD分别为 4.70 %～ 8.3 5 %和 3 .88%～ 8.1 1 % ,西尼地平及其脱氢代谢物的浓度分别在 0 .77μg/ ml～ 98.2 4μg/ ml和 0 .1 3 μg/ ml～ 5 .3 6μg/ ml范围内与峰面积呈良好的线性相关性。在温孵时间为1 0～ 60 min,微粒体蛋白浓度为 1 mg/ ml时 ,西尼地平呈线性消除 ,而其脱氢代谢物呈线性增加。结论　西尼地平在人肝微粒体内被迅速代谢 ,人肝 P45 0酶参与了西尼地平的脱氢氧化     

腰椎退行性疾病患者行后路腰椎融合手术的疗效影响因素

目的 探讨腰椎退行性疾病患者行后路腰椎融合手术的疗效影响因素,以期为临床提供借鉴.方法 收集2016年1月～2019年12月本院行后路手术治疗的127例腰椎退行性病变患者资料,分析性别、年龄、融合节段、体质量指数、ASA分级、手术时间、手术出血量、伤口感染、基础疾病、术后并发症、非计划再次手术等因素对手术疗效的影响.采...     

立体定向穿刺引流联合32P囊内注射治疗囊性脑转移瘤

目的 观察立体定向穿刺引流联合32P囊内注射治疗囊性脑转移瘤的疗效.方法 研究设3个组:A组25例,采用立体定向穿刺引流联合32P囊内注射治疗;B组21例,采用立体定向穿刺引流联合X刀治疗;C组26例,单纯采用X刀治疗.结果 A组、B组和C组总有效率分别为76.0%、66.7%和7.7%,A组和B组总有效率显著高于C组(χ2＝24.163,P＝0.000).1年、2年生存率A组分别为52.0%、16.0%,B组为42.8%、14.3%,C组为19.2%、0,A组和B组1年生存率显著高于C组(χ2＝6.116,P＝0.047).A组1例患者出现癫痫小发作,B组2例患者出现头痛、1例患者出现脑水肿,C组3例患者出现脑水肿.未见其他严重并发症.结论 立体定向穿刺引流联合32P囊内注射治疗囊性脑转移瘤有较好的临床疗效.     

Inhibition of STAT3 signaling and induction of SHP1 mediate antiangiogenic and antitumor activities of ergosterol peroxide in U266 multiple myeloma cells

Background  

Ergosterol peroxide (EP) derived from edible mushroom has been shown to exert anti-tumor activity in several cancer cells. In the present study, anti-angiogenic activity of EP was investigated with the underlying molecular mechanisms in human multiple myeloma U266 cells.     

Erratum: Analysis of Infections Occurring in Breast Cancer Patients after Breast Conserving Surgery Using Mesh

[This corrects the article on p. 328 in vol. 14, PMID: 22323921.].     

Preparation and biological evaluation of tumor-specific Ara-C liposomal preparations containing RGDV motif

Arginine–glycine–aspartate (RGD) has been shown to be essential for the recognition of integrins overexpressed in tumor cells, especially during tumor invasion, angiogenesis, and metasis. In this study, a novel tetrapeptide, RGD–valine (RGDV), was designed and attached to the N position of 1-β-d-arabinofuranosylcytosine (Ara-C) at the valine end, as a homing device for the delivery of Ara-C to tumor cells. Furthermore, fatty acids of various chain lengths (C_nH_2n+1COOH, n = 7, 9, 11, 13, and 15) were attached to the arginine end of RGDV to form a series of C_nH_2n+1CO–RGDV–Ara-C compounds. The structures of C_nH_2n+1CO–RGDV–Ara-C compounds were confirmed using mass spectrometry and nuclear magnetic resonance. The liposomal preparations of the synthesized C_nH_2n+1CO–RGDV–Ara-C compounds were obtained using the film dispersion method in the presence of phospholipids. The particle size, zeta potential, and dispersity index of the liposomes formed were found to be approximately 215 nm (diameter), approximately ?30 mV, and <0.3, respectively. The antitumor activity of the liposomal preparations containing the respective C_nH_2n+1CO–RGDV–Ara-C compounds was evaluated in mice inoculated with sarcoma S₁₈₀. Liposomal Ara-C preparation, liposomal C₁₁H₂₃CO–V–Ara-C preparation, Ara-C, and C₁₁H₂₃CO–V–Ara-C sodium carboxymethyl cellulose (CMC-Na) suspensions were used as controls. C_nH_2n+1CO–RGDV–Ara-C containing liposomal preparations were shown with an enhanced antitumor activity, likely because of the targeting effect of RGDV.     

Characterization of protein rheology and delivery forces for combination products

Characterization of a protein–device combination product over a wide range of operating parameters defined by end-user requirements is critical for developing a product presentation that is convenient for patient use. In addition to the device components, several product attributes, such as product rheology and product–container interactions, govern the functionality of a delivery system. This article presents results from a characterization study conducted for a high-concentration antibody product in a prefilled syringe. Analytical models are used to study the rheological behavior and to estimate delivery forces over a broad design space comprising temperature, concentration, and shear stress. Data suggest that high-viscosity products may exhibit significant shear thinning under the shear rates encountered under desired injection times.     

国产和进口N-乙酰氨基己酸锌口服胶囊的人体药动学

 目的：测定乙酰氨基己酸锌在正常人体内的药动学过程。方法：试验在9个健康志愿者中进行，在分别给予po300，400和500mg乙酰氨基已酸锌后，抽取24h内不同时间的血样，并采用GC/MS法分别测定血清中N-乙酰氨基己酸含量；采用原子吸收光谱法测定血锌的浓度。结果：不同时间的血中乙酰氨基己酸的药动学过程符合一级吸收二室模型；而血锌药动学可能属于非线性类型。结论：本研究获得了有关乙酰氨基己酸锌的一系列药动学参数。包括c_max，t_peak和AUC等。     

川芎嗪对中波紫外线辐射后细胞光产物影响及其光保护作用机制的研究

目的观察中波紫外线(UVB)辐射后永生化角质形成细胞株(HaCaT细胞)中光产物环丁烷嘧啶二聚体(CPDs)的产生和清除情况,观察川芎嗪对UVB辐射后细胞光产物的影响并探讨其保护作用机制。方法采用30mJ/cm2UVB照射培养的HaCaT细胞,加入川芎嗪干预处理,采用免疫组织化学法检测CPDs,以RT-PCR法和Western blotting法检测各受试组中p53和增殖细胞核抗原(PCNA)的mRNA和蛋白的表达水平。结果UVB辐射后HaCaT细胞中CPDs生成,0.5h达高峰,辐射后4h内清除速率较快,4h后清除速率较慢直至辐射24h。川芎嗪处理UVB辐射的细胞中CPDs少于单纯照射组(P<0.05)。川芎嗪可下调p53(34.9%)和PCNA(30.9%)的mRNA表达,还可下调p53(23.1%)和PCNA(24.9%)的蛋白表达。结论HaCaT细胞对UVB照射所致光产物CPDs的清除存在快速期及慢速期;川芎嗪可降低光产物CPDs水平。川芎嗪的光保护作用可能与其下调修复相关调控分子p53和PCNA基因及蛋白表达有关。