Radioiodinated progesterone derivative for progesterone receptor targeting with enhanced nucleus uptake via phenylboronic acid conjugation

A novel ¹³¹I‐radiolabeled probe with aromatic boronate motif (¹³¹I‐EIPBA) was designed to target progesterone receptor (PR)–positive breast cancer with enhanced nucleus uptake. Acetylene progesterone was conjugated with pegylated phenylboronic acid via click reaction and radiolabeled with ¹³¹I to afford ¹³¹I‐EIPBA. Meanwhile, ¹³¹I‐EIPB without boronate was prepared as control agent. After determination of the lipophilicity and stability of these tracers, in vitro cell uptake studies and in vivo biodistribution in rats were performed to verify the enhanced nucleus uptake and PR targeting ability of ¹³¹I‐EIPBA. ¹³¹I‐EIPBA was obtained with moderate radiochemical yield (40.35 ± 3.52%) and high radiochemical purity (>98%). As expected, the high binding affinity (39.58 nM) of ¹³¹I‐EIPBA for PR was determined by cell binding assay. The internalization ratio of ¹³¹I‐EIPBA was remarkably higher than that of ¹³¹I‐EIPB in PR‐positive MCF‐7 cells. Furthermore, the enhanced nucleus uptake of ¹³¹I‐EIPBA (0.59 ± 0.02%) was found to be significantly higher than that of ¹³¹I‐EIPB (0.13 ± 0.01%) in MCF‐7 cells. A novel ¹³¹I‐EIPBA compound was developed for PR targeting with improved cellular nucleus uptake. Furthermore, the introduction of aromatic boronate motif provides a worthwhile strategy for enhancing the nuclear receptor targeting of tracers.     

复方茵柏合剂壳聚糖澄清工艺研究

目的研究壳聚糖澄清法用于复方茵柏合剂的除杂效果以及制备工艺的可行性。方法以绿原酸为评价指标，通过正交设计优选澄清条件，与原制备工艺比较，并进行稳定性试验。结果壳聚糖澄清法所制备样品中绿原酸含量、薄层色谱鉴别与原工艺比较均无显著差异，且澄清度和稳定性均优于原工艺。结论壳聚糖澄清法具有简化工艺、缩短生产周期、提高制剂稳定性等优点，可用于复方茵柏合剂的制备。     

计算机辅助鼻额区域影像解剖学研究

OBJECTIVE: To evaluate the value of Advantage Windows 3.1 (AW 3.1) software for anatomical study of nasofrontal region, and to study the CT characteristics of nasofrontal region which related to the frontal sinus surgery. METHODS: Eighty patients underwent axial consecutive computed tomography scans and these data were studied with AW 3.1 software which provided reconstructional imaging of continuous coronal, sagittal, axial sections. Some related structures of nasofrontal region were studied and measured. RESULTS: AW 3.1 software could identify and measure the following structures accurately: The diameter of frontal sinus was (22.5 +/- 8.6) mm in height, (16.3 +/- 6.8) mm in depth, (23.8 +/- 9.8) mm in breadth. The diameter of frontal sinus ostium: the anterior-posterior diameter was (7.3 +/- 1.7) mm, the transverse diameter was (8.5 +/- 1.9) mm. The width of nasal beak of frontal bone(5.9 +/- 1.4 ) mm. The distance of frontal sinus ostium to the floor of columella nasi and the corresponding angle to the nasal floor were (60.8 +/- 4.2) mm and (70.1 +/- 4.7) degrees. The superior attachment sites of the uncinate process were as follows: lamina papyracea 41%, posteromedial wall of agger nasi cell 11%, middle turbinate 19%, anterior skull base 16%, superior bifurcation 13%. The cells could impinge on the frontal recess to cause obstruction (terminal recess 38.8%, anterior ethmoid cell 27.6%, agger nasi cells 24.5%). The accessory cells could impinge on the frontal sinus (perifrontal cells 32.7%, superaorbital cells 38.8%, intersinus septal cells 32.0%). There was significant difference between two groups of characteristics of nasofrontal region. CONCLUSIONS: AW 3.1 software is a helpful and powerful new tool for anatomical study of nasofrontal region and for preoperative evaluation. The structures of nasofrontal region are complex and various, frontal sinusitis almost always results from the obstruction of frontal sinus outflow tract. These results of anatomical study of nasofrontal region are helpful in directing the functional endoscopic surgery in frontal sinus.     

永存原始玻璃体增生症与先天性纤维血管瞳孔膜临床特征的比较

目的：分析永存原始玻璃体增生症(PHPV)和先天性纤维血管瞳孔膜(CFPM)的临床特征异同。

方法：回顾性分析2006-03/2021-12在空军军医大学西京医院眼科接受手术治疗的PHPV(PHPV组)和CFPM患儿(CFPM组)的眼部生物测量参数、临床表现、病变的形态学特点。

结果：纳入PHPV患儿56例61眼,CFPM患儿24例25眼; PHPV和CFPM的发病年龄相似、无性别差异,均以单眼患病为主,其占比分别为91%和96%。PHPV合并白内障患眼可有多种并发症和眼发育异常,CFPM主要为不同程度的瞳孔区堵塞及形态异常。PHPV组和CFPM组单眼患病患儿患眼前房深度(ACD)均小于对侧眼,手术年龄≤24月龄患儿患眼眼轴长度(AL)均小于对侧眼(P<0.05); PHPV组单眼患病患儿患眼角膜直径(CD)小于对侧眼、眼压高于对侧眼(均P<0.05); CFPM组单眼患病患儿患眼与对侧眼CD、IOP比较均无显著差异(P>0.05)。PHPV组患儿患眼ACD小于CFPM组患眼(P<0.05)。术中发现PHPV纤维血管膜组织位于晶状体后、玻璃体腔内,而CFPM纤维血管膜位于虹膜与晶状体前囊膜之间,很少累及晶状体。

结论：PHPV和CFPM有非常相似的临床特点,提示PHPV和CFPM可能是永存胚胎血管(PFV)的不同表现形式,但PHPV病变范围更广、病情更复杂。     

视网膜母细胞瘤患者RB1基因突变筛选

目的：了解视网膜母细胞瘤患RBl基因的突变特点。方法：应用PCR-SSCP技术筛奄RB患白细胞基因组DNA，测序分析确定突变。结果：在RB患10例中，确定双眼RB患1例第8外显子37位核苷酸A-T突变，引起12位谷氨酸变为天门冬酰氨酸(G12A)。其母亲同样为第8外显子36位核苷酸A-T突变，引起12位谷氨酸变为天门冬酰氨酸(G12A)。结论：本组双眼RB患1例为遗传性，其RB1基因突变为微小突变，其母亲为突变基因携带，本研究为遗传咨询提供一些有价值的资料。     

柱前手性衍生化反相高效液相色谱法拆分地佐西平对映异构体的研究

用乙酰葡萄糖异硫氰酸酯(GITC)作柱前手性衍生化试剂,以反相高效液相色谱法成功地拆分了地佐西平对映异构体。在此基础上建立了地佐西平对映异构体纯度和血药浓度测定方法。已用于测定右旋地佐西平的光学纯度和小鼠血药浓度。     

复方丹参肠黏附微丸中龙脑含量测定方法的建立及不同剂型龙脑溶出度的研究

通过将冰片进行β-CD包合,制备成复方丹参肠黏附微丸,建立复方丹参肠黏附微丸中龙脑的含量测定方法,考察其体外溶出度,并与市售复方丹参片的溶出度进行对比,评价剂型设计的合理性。利用气相色谱法测定复方丹参肠黏附微丸中龙脑的含量,采用溶出度测定法第一法,分别测定复方丹参肠黏附微丸中龙脑在人工肠液的溶出度及复方丹参片中龙脑在人工胃液、人工肠液的溶出度。在该方法下测得复方丹参肠黏附微丸中龙脑的质量分数为0.79%,其体外溶出12 h内累积溶出量近70%;复方丹参片中龙脑的质量分数为0.80%,在人工肠液中,20 min内累积溶出量达60%,40 min累积溶出量达90%以上;在人工胃液中,40 min内累积溶出量不足20%,但在40~150 min累积溶出量达80%以上。结果表明,利用气相色谱法可有效测得复方丹参肠黏附微丸中龙脑的含量,与市售复方丹参片相比,复方丹参肠黏附微丸中的龙脑具有明显的缓释作用。在复方丹参肠黏附微丸中将冰片进行了包合,并制备成肠溶型制剂,在一定程度上降低了冰片对胃、肠黏膜的刺激作用,提高了药物的安全性。     

健脾益肾法治疗慢性疲劳综合征验案举隅

慢性疲劳综合征(CFS)是一组以长期慢性或反复发作的极度疲劳为主要表现的综合征,属于中医学的"虚劳"范畴。慢性疲劳综合征与脾肾两脏亏虚关系密切。脾虚运化功能失常,气血生化无源,四肢肌肉失养,五脏六腑不充,而产生疲劳乏力,肾虚髓海失充,脑窍空虚,清窍失养可见头晕头痛,注意力不集中,记忆力下降,睡眠障碍等,故治慢性疲劳综合征,脾肾同调,健脾益肾,相得益彰。     

DCC基因转染对卵巢癌细胞HO-8910生长及化疗药物敏感性的影响

结直肠癌缺失(deleted in colorectal carcinoma, DCC)基因是于1990年确定并命名的重要的肿瘤抑癌基因,定位于人染色体18q21.3.DCC蛋白具有跨膜分子特征,其胞外部分氨基酸排序与神经细胞黏附分子相似.细胞黏附分子介导细胞间、细胞与基质间的相互作用,促进细胞与细胞间的黏附,是维持细胞生长的重要条件之一.有研究表明,良性卵巢肿瘤组织中DCC基因的表达缺失率为20%,恶性卵巢肿瘤组织中DCC基因的表达缺失率为56%,两者比较差异有显著意义.在临床分期晚、组织分化差、盆腹腔有转移的卵巢恶性肿瘤中DCC基因表达缺失率更高.