新型单羰基姜黄素类似物的合成及抗肿瘤活性研究

采用氮烷基化、羟基保护、醛酮缩合三步反应合成了8个新型单羰基姜黄素类似物,结构经质谱、核磁共振氢谱和核磁共振碳谱等手段进行确认。并采用MTT染色法体外检测所合成的8个单羰基姜黄素类似物对人肺癌细胞H1299,结肠癌细胞HT-29,人体胰腺癌细胞BxPC-3和人前列腺癌细胞PC-3的抗癌活性。半数抑制浓度IC50值结果显示:所合成的8个姜黄素类似物对四种细胞均有较强的抑制作用,其中化合物A6在四种细胞中的半数抑制浓度IC50均在0.65 μM以下,抗癌活性比姜黄素提高了40倍以上。     

2-氨基喹啉衍生物的合成及抗肿瘤药物VU-WS113的制备

为了找到适合大规模生产2-氨基喹啉类化合物的合成方法,以对硝基苄溴和相应的仲胺为原料,经过取代、还原、酰胺化、关环、溴代、叠氮化、还原等反应制备了5个2-氨基喹啉类化合物,并以IR,1HNMR,13CNMR和MS对所制备的化合物结构进行了表征.以6-(吗啉甲基)-2-氨基喹啉和2,5-二甲基-1-苯基-1H-吡咯-3-羧酸为原料,合成了抗肿瘤药物VU-WS113.分别考察了加料顺序、催化剂、反应时间等多个因素对反应的影响.实验结果表明,该方法具有操作简单、反应条件温和以及产率较高等特点,具有大规模制备的前景.     

异位妊娠的临床治疗进展

异位妊娠是早期妊娠妇女死亡的主要原因之一,近年来其发病率逐年上升,并且趋于年轻化,要求保留生育功能的患者明显增加,为此,异位妊娠的治疗也发生了相应的变化,由以往主要采用手术治疗,逐渐转为采用保守治疗的过程,尤其是药物保守治疗成为目前研究的热点。对异位妊娠的不同治疗方法进行综述,目的是探索更为合理,安全,有效,最大限度保留生育功能的异位妊娠的治疗方法。     

基于电磁加热效应的恶性肿瘤治疗

介绍了常规恶性肿瘤的治疗方法及其特点,重点阐述了肿瘤热疗的原理和现有的热疗方法。肿瘤热疗的核心问题是在有机体内定点、定域和可控地造成温度场(即只在恶性肿瘤范围内加热,不损伤周边正常组织),温度场对肿瘤组织的作用是宏观的,热力学的,在温度场内的所有细胞均受到作用。现有的肿瘤热疗方法难以做到定点定域加热。借鉴工业电磁加热技术,重点探讨了通过电磁加热效应实现定点定域,从而用于恶性肿瘤治疗的可行性和治疗技术路线。     

New strategies for the repair of spinal cord injury

Spinal cord injury （SCI） leads to several neu- rologic damages to patients with sensory and motor func- tion loss. Although some inspiring results were reported in animal, even in non-human primate models, the clinical translation of these research achievements barely move forward for the SCI patients. This review mainly focused on the pathogenesis of the primary and secondary injury, the clinical therapies and the new technologies in spinal cord injury. Moreover, the key scientific issues on this field were discussed in the review. Finally, some suggestions were proposed for the scientific and clinical researches.     

Assessment of alternated cooling and heating treatment by US combined CEUS in the VX2 rabbit liver tumor model

Inoperable liver tumors are often treated by thermal ablation that destroys the tumor in situ and spares the adjacent hepatic tissue.Thermal–physical treatment has many advantages,but treatment by freezing or heating alone has some limitations.By taking the advantages and disadvantages of cryosurgery and thermotherapy into consideration,a new thermal technique that combines cryosurgery and radio frequency ablation has been proposed,thereby overcoming the disadvantages of each treatment strategy and improving therapeutic outcomes.This new approach remains to be systematically studied in the liver;therefore,this study was performed to estimate survival after alternated cooling and heating ablation therapy in a VX2 rabbit liver tumor model.Sixteen days after VX2 carcinoma implantation into the rabbit liver,tumors were treated with alternated cooling and heating ablation therapy.Rabbits were monitored for 6 months after treatment and assessed with ultrasound(US)and computed tomography at 1,7,14,and 30 days posttreatment.Untreated tumor-bearing animals served as the control group.Our results show that alternate freezing and heating ablation therapy resulted in a good recovery of VX2 rabbits.Compared with the control group,treated rabbits lived significantly longer(P\0.05),with 70%of treated animals surviving to 196 days posttreatment without metastasis or recurrence,while none of the controls did so.There was no local recurrence in the treatment group.All rabbits in the control group developed metastasis,while metastasis was only observed in 30% of treated rabbits.These results suggest that alternate cooling and heating ablation therapy can prolong the survival time of rabbits with VX2 liver tumors and is an effective method for tumor therapy.Furthermore,we also showed in this model that contrast enhanced US is a valid follow-up approach to assess treatment effectiveness.     

情侣软件 手机帮你融洽夫妻关系

在这个智能手机掌控生活的时代,即使是最私人的,最复杂的东西——爱情,都能找到方法变成应用软件。黄之燕在她一天的任何空闲时间都会下意识地掏出手机,那里有一个她和男友共同创造的虚拟的＂家＂,这是由一款名叫＂微爱＂的手机情侣应用软件提供的一项服务,情侣们可以根据自己的品位和喜好装饰一个房间,作为他们的私密空间。黄之燕承认她倾注了很大的心血,＂像回到了热恋期,用什么样的窗户,什么样的壁纸,每个细节都能够讨论很久。＂她说。她认为手机情侣应用确实提高了她和男友的亲密度。     

新型三氮唑Schiff碱衍生物的合成及抗肿瘤活性研究（英文）

以1-[二-(4-氟苯)甲基]哌嗪及氯乙酸乙酯为原料,经取代、肼解、环化制得3-[4-二-(4-氟苯)甲基哌嗪]-4-氨基-1,2,4-三氮唑-5-硫酮(5),5和取代芳香醛经缩合反应制得了22个Schiff碱6(a~v),其收率为73-85%。合成的22个目标化合物通过熔点测定和质谱、红外光谱、核磁共振氢谱分析、元素分析对其结构进行确证.经体外抗肿瘤活性测试表明除了化合物6(n,o)外,其余所有化合物均具有较好的活性,在化合物浓度为20ug/m L时,其抑制率高达99%。     

Nature Communications揭示乳腺癌患者对紫杉醇产生耐药的一种可能的机制

正来自复旦大学上海医学院的研究人员在新研究中证实,基因TEKT4所发生的遗传变化与对乳腺癌化疗药物紫杉醇(paclitaxel)抵抗有关,相关论文发表在5月13日的Nature Communications杂志上。复旦大学上海医学院的邵志敏教授和余科达副教授是这篇论文的共同通讯作者。紫杉醇是一种具有抗肿瘤活性的天然产物,它通过诱导和促进癌细胞中微管的生成,阻止微管正常生理聚集来抑制癌细胞有丝分裂和纺锤体形成,致使快速分裂的癌细胞被限制在有丝分     

神经营养因子联合治疗促进脊髓轴索再生的研究现状

神经营养因子（neurotrophic factors,NTFs）在急性脊髓损伤（spinal cord injury,SCI）后神经细胞的生长发育、保护和修复的过程中发挥重要作用。然而,单一的治疗尚不足以激活神经元内源性的再生程序;其次,再生抑制因子限制了NTFs对SCI后结构和功能恢复。因此,越来越多的学者选择以联合的方式探索NTFs对再生的促进作用。本文归纳了NTFs以联合的方式治疗轴索再生的基本原理和最新进展,旨在为联合治疗的进一步研究提供科学指导。