二氯荧光素二丙烯酸酯的合成与抗肿瘤活性研究

合成了化合物二氯荧光素二丙烯酸酯(Ⅰ),用元素分析、IR、1HNMR、UV、荧光光谱对它进行了表征。测试了Ⅰ对小鼠白血病L1210细胞生长曲线的影响和对人体胃腺癌SGC-7901的抗肿瘤活性。结果表明,Ⅰ对体外培养肿瘤细胞L1210有很强的瞬时杀伤作用〔在ρ(Ⅰ)=0 1μg mL时,24h对其杀死率几乎为100%〕;对人体胃腺癌SGC-7901有很强的细胞增殖的抑制作用〔在ρ(Ⅰ)=0 1μg mL时,克隆数约为(3±1.1)%,集落形成率=0 15%,存活率=0 4%〕。是有希望的脂溶性、带荧光的抗肿瘤药学化合物。

双功能化合物—二氯荧光素二丙烯酸酯的合成与生物活性

In this paper 2,7Dichloro3,6Acrylate Fluorescin Ester has been prepared and characterized by elementary analysis,IR,UV,1HNMR,Flourensence spectra.Afterwards,its antitumor activity was tested.The results showed that it has good flourensence and antitumor activity and it is a prospective antitumor agent.Then,use it to pigmentate broad bean farian.The results show that it has good determination function for broad bean cells vitality.So it is a selective determination agent for broad bean cell

D113丙烯酸系弱酸性阳离子交换树脂的应用及特性

论述了近年来国内开发的Ｄ１１３大孔丙烯酸系弱酸性阳离子交换树脂在热电厂水处理与环保等行业的用途和应用特性．介绍了该树脂的质量鉴别方法和使用中的注意事项。

P(HPMA-FMA)荧光探针制备、细胞毒性评估及细胞吞噬示踪检测

以甲基丙烯酰氯、三乙胺和荧光素反应得到荧光素甲基丙烯酸酯（FMA），将其与聚N-（2-羟丙基）甲基丙烯酰胺（HPMA）以物质的量之比1∶10混合并通过引发剂偶氮二异丁腈（AIBN）引发聚合反应，生成带有荧光探针的聚合物P（HPMA-FMA）。采用台盼蓝排染法评估了该聚合物的细胞毒性，荧光显微镜和流式细胞仪观察和检测了全反式维甲酸（ATRA）诱导HL-60细胞分化过程中，P（HPMA-FMA）被细胞吞噬后的荧光示踪效应。 结果表明：P（HPMA-FMA）的细胞毒性极低，当P（HPMA-FMA）的质量浓度为4～16 mg/mL时对细胞增殖无影响；当其质量浓度为30 μg/mL时即可满足荧光显微镜定性示踪观察和流式细胞术定量检测所需要的荧光强度。

深海环境通用自清洁防污涂层的研究

针对我国深海防污研究与应用刚起步且防污涂料产业技术及工艺落后的现状,该项目从我国南海资源勘查开发的迫切需求出发,优选出了综合性能优良的4种防污涂料基础材料——2种含辣素功能结构的丙烯酸金属盐树脂和2种二硫代二丙酰胺防污剂,并优化了其制备工艺,实现了规模化生产;针对南海的应用环境,通过复配技术优化防污涂料配方体系,研发了具有通用技术特性的自清洁防污涂料,并实现了规模化生产,在潜标、船舶等设施上进行了示范应用,效果良好;从防污性能加速评价方法和具有协同防污作用的防污涂料复配技术方面完善防污涂料理论与技术体系,探索深海环境防污涂层技术体系及其应用。

Graft Copolymerization of Ethyl Acrylate onto Hydroxypropyl Methylcellulose Using Potassium Persulfate as Initiator

With potassium persulfate (KPS) as initiator, graft copolymerization of ethyl acrylate (EA) onto water-soluble hydroxypropyl methylcellulose (HPMC) was investigated in aqueous medium. Effects of monomer concentration, initiator concentration, matrix concentration, and reaction temperature on the percentage of grafting (G) and grafting efficiency (G_E) were studied. The results show that G and G_E values both increase with the the increase of EA concentration and KPS concentration; when raising HPMC concentration from 0.12 mmol/L to 0.47 mmol/L, G decreases, while G_E increases;and when raising reaction temperature from 50 ℃ to 65 ℃,G increases, but G_E decreases. In addition, the graft copolymers were characterized by Fourier transform infrared (FTIR) spectra and transmission electron microscopy (TEM) methods.

Zn–Ca–Al mixed oxide as efficient catalyst for synthesis of propylene carbonate from urea and 1,2-propylene glycol

A series of Zn–Ca–Al oxides with different CaO and ZnO contents have been prepared and evaluated in the synthesis of propylene carbonate(PC) from 1,2-propylene glycol(PG) and urea in a batch reactor. The effect of catalyst composition, basicity and reaction process parameters such as temperature, catalyst dose, molar ratio of PG to urea, purge gas flow and reaction time has been studied to find suitable reaction conditions for the PC synthesis. The PC selectivity and yield under the desired conditions could reach 98.4% and 90.8%, respectively. The best performing catalyst also exhibited a good reusability without appreciable loss in the PC selectivity and yield after five consecutive reaction runs. In addition, a stepwise reaction pathway involving a 2-hydroxypropyl carbamate intermediate was proposed for the urea alcoholysis to PC in the presence of Zn–Ca–Al catalysts, according to the time dependences of reaction intermediates and products.

ADSORBENTS USED IN THE CLEARANCE OF ENDOTOXIN

A series of modified poly (methyl methacrylate, PMMA) resins were prepared and compared their adsorption abilities to endotoxin. The results showed that adsorbents, which were grafted with tertiary amine and long spacing arms, had the best adsorption capacities and good blood compatibility. It is hopeful to be used as adsorbent in hemoperfusion for clinical clearance of endotoxin. The influence of original concentration of endotoxin on adsorption and the adsorption mechanism were also investigated.

雷公藤内酯醇衍生物对肝癌细胞增殖、凋亡的作用研究

目的研究新型雷公藤内酯醇(Triptolide,TPL)衍生物对正常肝细胞的毒性以及对肝癌细胞的增殖、凋亡作用。方法通过对TPL进行化学修饰,获得2种新型衍生物:雷公藤内酯三醇(TP-3-OH)和丙烯酸雷公藤甲素酯(TPO)。通过体外培养人胚胎肝细胞LO2和肝癌细胞Hep G2、Hep3B、SMMC-7721,分为DMSO对照组,TPL/TP-3-OH/TPO低、中、高浓度组(25、50、100 nmol·L^(-1))。通过检测培养上清中乳酸脱氢酶(LDH)的活性来评价TP-3-OH、TPO对肝细胞的毒性;采用MTT实验检测细胞增殖情况;采用流式细胞术及Western Blot法检测细胞凋亡及凋亡通路相关蛋白表达情况;采用划痕实验检测细胞迁移能力。结果与TPL组比较,50、100 nmol·L^(-1)浓度条件下TP-3-OH、TPO组的LO2细胞培养上清中的LDH活性明显降低(P<0.05,P<0.01)。与DMSO对照组比较,TPO中、高浓度(50、100 nmol·L^(-1))组的LO2细胞增殖抑制率明显升高(P<0.05,P<0.01),TPO低、中、高浓度(25、50、100 nmol·L^(-1))组的Hep G2、Hep3B、SMMC-7721肝癌细胞增殖抑制率均明显升高(P<0.05,P<0.01);TPO高浓度(100 nmol·L^(-1))组的LO2、Hep G2和SMMC-7721细胞的早期、晚期细胞凋亡率均明显升高(P<0.05,P<0.01);TPO中、高浓度(50、100 nmol·L^(-1))组SMMC-7721、Hep G2细胞的cleaved-Caspase-3、cleaved-PARP蛋白表达显著上调(P<0.01);TPO中浓度(50 nmol·L^(-1))组SMMC-7721细胞的24 h迁移率明显降低(P<0.05)。结论经化学修饰获得的2种新型TPL衍生物对肝细胞的毒性降低,其中TPO具有抑制肝癌细胞增殖、促进肝癌细胞凋亡的作用。

Synthesis and Property Studies of Transparent Resins Containing Rare Earth Complex Eu(Ⅲ) (TTA)_2(MA)_2 Phen·H_2O

A new rare earth complex Eu（III） （TTA）2（MA）2Phen · H2O was synthesized and characterized by element analysis, FTIR, UV, thermal analysis, and fluorescence spectra. The strong fluorescence and high thermal stability of Eu（III） （TTA）2（MA）2Phen · H2O were used to modify resin. The copolymer containing europium was prepared by copolymerization of Eu（III） and styrene/α- methylacrylic acid, and characterized by FTIR and fluorescence spectra. The fluorescence spectra showed that the copolymer was a sort of materials with good fluorescence property, and the higher fluorescence intensity came from the higher europium content.

Antinociceptive activity of transient receptor potential channel TRPV1, TRPA1, and TRPM8 antagonists in neurogenic and neuropathic pain models in mice

The aim of this research was to assess the antinociceptive activity of the transient receptor potential （TRP） channel TRPV1, TRPM8, and TRPA1 antagonists in neurogenic, tonic, and neuropathic pain models in mice. For this purpose, TRP channel antagonists were administered into the dorsal surface of a hind paw 15 min before capsaicin, allyl isothiocyanate （AITC）, or formalin. Their antiallodynic and antihyperalgesic efficacies after intraperitoneal ad- ministration were also assessed in a paclitaxel-induced neuropathic pain model. Motor coordination of paclitaxel- treated mice that received these TRP channel antagonists was investigated using the rotarod test. TRPV1 antagonists, capsazepine and SB-366791, attenuated capsaicin-induced nociceptive reaction in a concentration-dependent manner. At 8 pg/20 pl, this effect was 51% （P〈0.001） for capsazepine and 37% （P〈0.05） for SB-366791. A TRPA1 antagonist, A-967079, reduced pain reaction by 48% （P〈0.05） in the AITC test and by 54% （P〈0.001） in the early phase of the formalin test. The test compounds had no influence on the late phase of the formalin test. In paclitaxel-treated mice, they did not attenuate heat hyperalgesia but N-（3-aminopropyl）-2-{[（3-methylphenyl）methyl]oxy}-N-（2-thienylmethyl） benzamide hydrochloride salt （AMTB）, a TRPM8 antagonist, reduced cold hyperalgesia and tactile allodynia by 31% （P〈0.05） and 51% （P〈0.01）, respectively. HC-030031, a TRPA1 channel antagonist, attenuated tactile allodynia in the von Frey test （62%; P〈0.001）. In conclusion, distinct members of TRP channel family are involved in different pain models in mice. Antagonists of TRP channels attenuate nocifensive responses of neurogenic, tonic, and neuropathic pain, but their efficacies strongly depend on the pain model used.

Ricinus communis agglutinin I functionalisation of poly(methyl methacrylate) (PMMA) as a substrate for microfluidic device

We report a functionalisation strategy which is able to generate Ricinus communis agglutinin 1 （RCA 120） modified PMMA microfluidic device for binding and culturing living cells. The functionalisation is achieved by standard aminealdehyde （Schiff base） reaction through the crosslinker, glutaraldehyde. To prove the ability of the RCA 120 modified PMMA surface, the PC 12 cell line （rat pheochromocytoma ceils） has been captured and cultured by the microfluidic device. In the presence of tunicamycin, the dose/timedependence on decreasing of binding affinity of RCA 120 modified device with PC 12 cell is also observed. The experimental results demonstrate that the lectin-functionalized microfluidic device can be employed as efficient cell culturing platform, and has a great promise of being used as a powerful tool for monitoring the interaction of drug with living cell.