Preparation of 111In-DTPA morpholino oligomer for low abdominal accumulation

An ability to quantitate the beta cell mass by noninvasive nuclear imaging will be very useful in the prevention, diagnosis, and treatment of diabetes. However, to be successful, radioactivity from the pancreas must not be obscured by the background radioactivity in the abdomen. Pretargeting offers the promise of achieving high target organ to normal tissue ratios. In preparation for pancreas imaging studies by pretargeting using morpholino oligomers (MORF/cMORF), it was necessary to develop a simple and efficient method to radiolabel the cMORF effector. Because we have shown that labeling the cMORF with ¹¹¹In via DTPA reduces excretion into the intestines compared to labeling with ^99mTc via MAG₃, the conjugation of DTPA to cMORF was investigated for ¹¹¹In labeling. The amine-derivatized cMORF was conjugated with DTPA using 1-ethyl-3(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC) as an alternative to the conventional cyclic anhydride. The conjugation efficiency (represented by the number of DTPA groups attached per cMORF) was investigated by changing the EDC, DTPA, and cMORF molar ratios. Different open columns were considered for the purification of DTPA–cMORF. Before conjugation, each cMORF molecule was confirmed to have an amine by trinitrobenzene sulfonic acid (TNBS) assay using the ω-amino butyric acid as positive standard and the non-amine derivatized cMORF as negative standard. The average number of DTPA groups per cMORF was 0.15–0.20 following the conjugation over a cMORF/DTPA molar ratio of 0.5–5 and over a cMORF/EDC molar ratio of 20–60. The conjugation efficiency was lower than expected probably due to steric hindrance. A 1×50 cm P-4 column using ammonium acetate as eluting buffer provided an adequate separation of DTPA–cMORF from free DTPA. The ¹¹¹In labeling efficiency by transchelation from acetate exceeded 95%, thus avoiding the need for postlabeling purification. Despite the lower than expected conjugation efficiency in which no more than one-fifth of the cMORF were DTPA-derivatized, a specific radioactivity of at least 300 μCi/μg or 1.90 Ci/μmol of cMORF was achieved. In conclusion, a protocol is described for ¹¹¹In-DTPA–cMORF that provides the high specific activity favorable to beta cell imaging because of the low mass fraction of beta cells in pancreas (1–2%) and obviates the need for postlabeling purification.     

Glomerular Capillary Hemorrhage Induced in Rats by Diagnostic Ultrasound with Gas–Body Contrast Agent Produces Intratubular Obstruction

Glomerular capillary hemorrhage (GCH) induced by ultrasonic cavitation during diagnostic imaging represents a unique contrast agent–related nephron injury. Consequences of GCH during 1.5-MHz diagnostic ultrasound with contrast agent were examined by histologic methods in rats. Definity was infused at 10 μl/kg/min for 5 min at the start of 8 min of intermittent image-exposure, with 2.3 MPa in situ peak rarefactional pressure amplitude. Kidney samples were taken for histology at 5 min, 30 min, 4 h, 2 d, 1 week and 4 weeks post exposure. In addition, samples were taken at 4 h from groups treated with heparin or aminocaproic acid. GCH was found in 61% of glomeruli in the center of the scan plane 5 min after exposure, which declined (p < 0.05) to 36.3% after 4 h. The width of Bowman's space was significantly increased for glomeruli with GCH relative to glomeruli without GCH (p < 0.05), consistent with tubular obstruction. Antibody staining revealed fibrin clotting in Bowman's space in 4-h samples and this persisted in the 2-d samples. Heparin reduced and aminocaproic acid increased the GCH seen in 4-h samples. Tubular dilation was evident with injury to the epithelium after 2 d. After one week, areas of inflammatory cell infiltration were present. After four weeks, areas of interstitial fibrosis were revealed by Masson's trichrome stain. The consequences of GCH induced by diagnostic ultrasound with contrast agents include rupture of glomerular capillaries, procoagulant activity resulting in intratubular obstruction, and the potential for progression of the resulting tubular injury toward interstitial fibrosis. (E-mail: douglm@umich.edu)     

基于模糊数学形态学及免疫智能的旋转机械状态参数图形识别方法

以旋转机械振动多维图形为对象，研究了直接提取和挖掘图形特征信息的模糊形态学方法，提出了基于模糊数学形态学及免疫智能的旋转机械振动参数图形识别方法。利用模糊形态滤波方法实现图形滤波，研究了模糊形态边缘检测算子，并结合旋转机械振动参数图形进行形态学梯度的边缘纹理特征提取，最后利用人工免疫算法对图形特征进行诊断识别。在600MW模化汽轮机转子试验台上进行了转子正常、转子不平衡故障、转子不对中故障及汽流激振故障的试验，诊断结果表明本文所提出的方法可以获得较高的诊断精度，为旋转机械故障诊断探索了一条新路。     

牛蒡子提取物中牛蒡苷和牛蒡苷元的含量测定研究

目的建立牛蒡子提取物中牛蒡苷及其苷元的含量测定方法.方法采用HPLC,以牛蒡甘、牛蒡苷元为含量测定指标,测定了牛蒡了提取物中牛蒡苷和牛蒡苷元的含量.色谱柱为Kromasil C18 100A(150mm×4.6mm,51μm).流动相甲醇-水(采川梯度洗脱的方式0～7min,35%～45%甲醇;7～9[Bin,45%～48%甲醇;9～15min,48%～53%甲醇;15～24min,53%～80%甲醇;24～30min,80%～100%甲醇);检测波长为280nm.结果牛蒡苷及牛蒡苷元的平均回收率分别为97.7%,96.9%.RSD分别为1.3%,0.9%(n=5);线性方程分别为Y=782.6X-64.11(r=0.999 8).y=1 220.217X-35.26(r=0.999 8).结论该方法快速准确,可同时测定牛蒡提取物中牛蒡苷和牛蒡苷元的含量,可用作牛蒡子提取物的质量控制方法.     

丝裂霉素预防准分子激光屈光性角膜切削术后角膜混浊的临床研究

目的:探讨准分子激光屈光性角膜切削术中使用0.2g/L丝裂霉素(MMC)预防术后角膜上皮下混浊(haze)的安全性、有效性。方法:对120例(240眼)屈光不正的患者进行准分子激光屈光性角膜切削术,术中使用0.2g/L丝裂霉素,作用时间为20~90s,观察术后角膜上皮愈合时间、观察术后1,3,6,12mo时裸眼视力、矫正视力、屈光状态、haze形成情况及并发症、角膜内皮细胞计数等。结果:角膜上皮愈合时间为3.01±0.72d;手术前后角膜内皮细胞计数统计学上无显著性差异(P=0.62);术后1,3,6,12mo时裸眼视力、矫正视力、屈光状态统计学上无显著性差异;术后6mo0~0.5级haze218眼(90.8%),1级haze21眼(8.75%),2级haze1眼(0.83%),术后12mo1级haze12眼(5%);术后未见丝裂霉素毒性反应及并发症。结论:使用0.2g/L丝裂霉素预防准分子激光屈光性角膜切削术后角膜上皮下混浊安全、有效。     

硫酸镍与芪归解毒汤对人晶状体上皮细胞中HSP27表达的影响

目的:探讨硫酸镍损伤后人晶状体上皮细胞(lens epithelial cell,LECs)中热休克蛋白27(heat shock protein27,HSP27)表达情况,并给予芪归解毒汤干预,观察晶状体上皮细胞HSP27表达的变化。方法:体外培养正常人晶状体上皮细胞分为正常组,硫酸镍组和中药组,分别作用24h后,逆转录聚合酶链反应(RT-PCR)检测晶状体上皮细胞HSP27 mRNA的表达水平。结果:硫酸镍损伤可造成晶状体上皮细胞HSP27 mRNA表达水平上调(P<0.05),预先的中药干预能使HSP27 mRNA表达水平上调(P<0.05)。结论:硫酸镍损伤后晶状体上皮细胞HSP27mRNA表达水平上调,给予预先的中药干预可能通过提高HSP27的表达水平从而保护晶状体上皮细胞。     

“右江流域民族医药研究”刍议

首次提出“右江流域民族医药”概念，“右江流域民族医药”泛指右江流域少数民族地区所有少数民族医药，具体包括壮医药、瑶医药、苗医药、彝医药、仡佬医药、回族医药等少数民族医药；同时，“右江流域民族医药”又是对右江流域各种民族医药之间特殊关系的揭示，即“右江流域民族医药”应该是以壮医药为主体的多元化民族医药。多元化民族医药以及各民族医药之间的相关性是“右江流域民族医药”的特征。加强“右江流域民族医药”的研究，对丰富和发展壮医药和该区域其它民族医药的理论和实践，揭示右江流域各自民族医药之间的独特性及其相关性。建立起与本地少数民族地位相一致的民族医药学科体系，推动右江流域少数民族地区民族卫生事业以及社会经济的进步和发展，都具有重要意义。     

HPLC测定止泻保童颗粒中盐酸小檗碱的含量

目的:为控制止泻保童颗粒的质量,考察了高效液相色谱法测定止泻保童颗粒中盐酸小檗碱的含量。方法:色谱柱以十八烷基硅烷键合硅胶为填充剂,柱温25℃,以甲醇-磷酸三乙胺水溶液(30∶70)为流动相,检测波长为350nm。结果:盐酸小檗碱的加样回收率为97.1%,RSD=1.69%。结论:该法快速、简便、准确为制剂的质量控制提供了可行的分析方法。     

酸牛乳抑制1,2-二甲基肼诱发小鼠大肠癌的实验研究

106只小鼠随机分成5组,每组18至23只。1～3组小鼠皮下注射1,2-二甲基肼(DMH),剂量20mg/kg体重,每周一次,连续20周。实验结束前,动物分别自由饮用自来水(第一组),水加嗜酸乳酸杆菌酸牛乳(第二组)及水加牛乳(第三组)。第4组和第5组为对照组,动物分别皮下注射1mM EDTA和蒸馏水。 27周诱癌期后,对照组小鼠未发生肿瘤。DMH处理动物中,第2组的结肠癌发生率为44.4％,比第1组(80％)和第3组(100％)明显降低(P<0.05)。此外,实验期间第2组动物的存活率(100％) 比第1组(80％)和第3组(74％)都高。结论是喂饲嗜酸乳酸杆菌(Shahani株)制备的酸牛乳能显著降低DMH诱发的小鼠癌肿和死亡率,而单纯牛乳则能增加。本研究的资料提示,食物中添加活嗜酸乳酸杆菌可能有助于预防结肠癌。     

食管癌放射野外新病灶分析

自 1978年元月至 1981年 12月 ,放射治疗食管癌 112 8例 ,疗后发现放射野外新病灶 6 4例(5 .7% ) ,放射野上下缘新病灶发生率分别为 2 .9% ,1.6 %。第二段癌发生率占 1.2 % ,其中 5 4例进行了再程放疗 ,其 1,2 ,3,5年生存率分别为 5 3.7% ,2 4 .1% ,13.5 % ,5 .8%。结果表明此类病人与局部复发或未控制病例有较大区别 ,再程放疗在减少或避免重复照射的基础上 ,可给予根治性放疗 ,首次放疗时病变两端各延长 3cm的照射野是合理的。