海洋珍珠生物提取液对人宫颈癌Siha细胞增殖与凋亡作用的影响

为探讨海洋珍珠生物提取液对宫颈癌Siha细胞株增殖和凋亡的影响,采用MTT法检测了细胞增殖情况,在流式细胞仪用Annexin V和PI双染检测了细胞的凋亡率,PI单染法测定了细胞周期,Hoechst 33258/PI荧光染色法观测了Siha细胞的形态学改变,RT-PCR法测定了宫颈癌Siha细胞株内Bcl-2,Bax基因表达。结果表明,海洋珍珠生物提取液在一定质量浓度范围内,以浓度依赖性的方式抑制宫颈癌Siha细胞的生长(P0.05);以0,6,30和60μg/mL海洋珍珠生物提取液处理细胞24 h,Siha细胞早期凋亡率分别为5%,7.1%,32.25%和31.95%,晚期凋亡比例为0.45%,2.85%,8.55%和23.2%;荧光显微镜下细胞呈现典型的凋亡性改变;RT-PCR显示海洋珍珠生物提取液处理后宫颈癌Siha细胞内的Bcl-2 mRNA表达降低,Bax mRNA表达升高。提示海洋珍珠生物提取液以浓度依赖性的方式抑制宫颈癌Siha细胞增殖,并通过降低Bcl-2 mRNA,升高Bax mRNA来诱导细胞凋亡。     

负载顺铂的泊洛沙姆温敏凝胶用于小鼠宫颈癌的局部化疗

为了探讨载有顺铂的温敏凝胶对小鼠宫颈癌的局部化疗作用,制备了载有顺铂的泊洛沙姆温敏凝胶,并通过流变学、体外溶蚀、体外释放等技术手段表征其结构和性能,采用鼠源宫颈癌U14细胞制备了原位宫颈/阴道癌模型,将载药凝胶灌注入荷瘤鼠阴道,评价载药凝胶对小鼠宫颈/阴道癌的抑制作用。结果表明,载有顺铂的泊洛沙姆温敏凝胶经阴道给药后对小鼠宫颈/阴道癌的抑瘤率可达到63.1%,可有效抑制小鼠宫颈癌的生长,而系统安全性则远远高于静脉注射顺铂。因此,载有顺铂的温敏凝胶有可能成为一种新型的宫颈癌治疗剂型。     

姜黄素联合顺铂对卵巢癌细胞COC1的体外抗肿瘤作用

利用MTT比色法研究了姜黄素(Cur)联合顺铂（DDP）对卵巢癌COC1细胞的抑制作用。 结果表明,当ρ(DDP)为2.5~10 mg/L,ρ(Cur)=5 mg/L时,与DDP相比,二者联合用药对卵巢癌COC1细胞可产生协同抑制作用;ρ(Cur)=5 mg/L就可明显增强COC1细胞对顺铂的敏感性,增敏倍数为2.66倍;光学显微镜观察发现,药物作用后COC1细胞的形态发生了改变,细胞折光度下降,大小不一、形态各异、排列疏散和胞浆空泡化严重。 为探讨姜黄素协同顺铂抑制肿瘤的机制,本研究采用高效液相色谱法测定姜黄素辅助用药前后细胞内DDP含量的变化。 结果表明,在加入姜黄素前后,COC1细胞内顺铂含量虽然略有下降,但差异无统计学意义（P＞0.05）。 由此可见,姜黄素与顺铂联合用药对人卵巢癌COC1细胞增殖具有协同抑制作用,且姜黄素可同时增加COC1细胞对顺铂的敏感性,但姜黄素可能并未明显改变顺铂在细胞内的含量,即姜黄素可能不是通过影响顺铂进入细胞的通路而起协同抑制作用的。     

C-13位烷氧基赤霉素衍生物的合成与抗肿瘤活性研究

设计并合成了系列C-13位为醚结构且在A环和D环有两个α,β-不饱和酮结构的赤霉素衍生物.采用噻唑蓝(MTT)法评价了其对人肺腺癌细胞(A549)、人肝癌细胞(HepG2)、人胃癌细胞(MKN28)以及结肠癌细胞(HT29)的体外生长抑制作用,结果表明:此类化合物都有较强的体外抗肿瘤活性,其中化合物27的活性最强(对人胃癌细胞MKN28的IC50=0.21μmol·L-1),优于阳性对照药物顺铂(DDP).     

一个双核锌配合物[Zn2(cttb)Cl4]·DMF的合成、结构和抗肿瘤活性

以顺,顺,顺,顺-环戊烷-1,2,3,4-四甲酸和邻苯二胺为原料,合成了顺,顺,顺,顺-2,2',2',2'-环戊烷四苯并咪唑(cttb)及其双核锌配合物[Zn_2(cttb)Cl_4]·DMF,通过元素分析、红外光谱、核磁共振氢谱和X-ray单晶衍射对其结构进行了表征。该配合物晶体属于三斜晶系,P-1空间群,每个中心Zn~(2+)离子分别与两个Cl~-离子和配体中的两个N原子配位,形成四配位的四面体几何构型。MTT测试表明,锌配合物及其配体对人食管癌细胞Eca109均有抑制作用,其半抑制浓度IC50值分别为33.34μM和34.54μM,小于阳性对照物顺铂的IC50值43.99μM。     

顺铂温敏载药粒子的制备表征

制备了顺铂温敏载药纳米粒子，表征其相关性质并考察不同温度下对体外肿瘤细胞的生长抑制作用。制备的两亲嵌段聚合物在水溶液中自发形成胶束结构并包裹顺铂，测定顺铂载药粒子的结构、形态、粒径及包封率、载药量、晶体状态等特性，并对顺铂的体外释放以及不同细胞系体外毒性也做了研究。载药粒子粒径为83.3 ± 4.3 nm，载药量为37.8%，包封率为77.8%。血清中相变温度39.3 ℃。载药颗粒在单纯化疗时细胞抑制率较小，加热后抑制作用明显增加(P<0.01)，与游离药物相近(P>0.5)。顺铂载药纳米粒子具有较好的温控特性，为顺铂在肿瘤热靶向治疗中的应用提供了一条新的途径。     

二肽类膦酸酯衍生物的合成与抗肿瘤活性

为了寻找抗肿瘤活性化合物,以前期研究的含一个氨基酸结构单元的膦酸酯衍生物为基础,设计合成了15个二肽类膦酸酯衍生物(Ⅲa-Ⅲo)。采用溴化噻唑蓝四氮唑(MTT)法进行体外抗肿瘤活性测试。结果表明:该类化合物对人肺癌细胞(A-549)、人胃癌细胞(SGC-7901)和人食管癌细胞(EC-109)有潜在增殖抑制作用。其中,化合物Ⅲf对A-549和EC-109的半数抑制浓度(IC 50)分别为(6.9±1.2)和(6.3±1.0)μmol/L,化合物Ⅲn对SGC-7901和EC-109的IC 50分别为(6.7±1.0)和(6.1±1.0)μmol/L,与对照药顺铂接近。     

3-芳基噻唑烷-4-酮-2-酰胺的合成及其抗肿瘤活性研究

合成了系列新的3-芳基噻唑烷-4-酮-2-酰胺衍生物,并测试了化合物抑制肿瘤细胞增殖活性.部分化合物对A-549和Hela肿瘤细胞有弱的细胞毒性,而对BGC-823没有抑制作用,表现出一定的选择性.其中,化合物7ad对A-549有较强的抑制活性(IC50=21.0μmol·L-1),与阳性对照顺铂的抑制活性(IC50=19.4μmol·L-1)相当.初步的构效关系表明化合物的立体结构可能对其抗肿瘤活性影响较大.     

红花黄色素抗氧化活性研究

通过考察红花黄色素(SY)及其主要化学成分对羟基自由基介导2-脱氧核糖氧化降解的抑制作用,以及对1,1-二苯基-2-苦肼基自由基(DPPH·)的清除能力,探究SY的体外抗氧化活性及其抗氧化的主要有效成分.通过Fenton反应产生羟基自由基,用紫外分光光度计检测了SY及其主要化学成分对2-脱氧核糖降解的抑制作用和对DPPH·的清除能力,同时对红花黄色素B(SYB)抑制2-脱氧核糖降解的作用机制做了初步研究.结果表明SY抑制Fenton反应对2-脱氧核糖的氧化降解的IC50为256.79 μg/mL,对DPPH·清除的IC50值为27.15μg/mL.羟基红花黄色素A(HSYA)和SYB是SY中抗氧化的两个有效成分,抑制2-脱氧核糖的氧化降解的IC50分别为220.68 μg/mL和207.01μg/mL;对DPPH·清除的IC50值分别为55.81 μg/mL和41.25μg/mL.SYB对2-脱氧核糖氧化降解的抑制作用机理研究表明,SYB除了对Fenton反应产生的羟基自由基具有直接清除作用外,又可通过与Fe2+离子的络合作用而阻断Fenton反应产生羟基自由基.由此可知SY具有明显的体外抗氧化活性,SYB和HSYA为其主要抗氧化活性成分.     

小剂量奈达铂同步放疗对中晚期宫颈癌作用

目的对小剂量奈达铂与顺铂周疗方案同步放疗治疗中晚期宫颈癌的临床疗效及毒副反应进行分析。方法收集2012年7月至2015年12月中晚期宫颈癌患者(均为鳞状细胞癌)86例随机分两组。顺铂组采用顺铂周疗方案同步放疗治疗,奈达铂组采用小剂量奈达铂周疗方案同步放疗治疗。比较两组患者中晚期宫颈癌治疗总有效率,毒副作用发生率,治疗前和治疗后患者生存质量评分以及KPS评分的差异。结果奈达铂组患者中晚期宫颈癌治疗总有效率和顺铂组无显著差异,P0.05;奈达铂组肾脏毒性、恶心呕吐等毒副作用发生率低于顺铂组,而血液毒性反应明显高于顺铂组,P0.05。治疗前两组生存质量评分以及KPS评分比较无显著差异,P0.05;治疗后奈达铂组生存质量评分以及KPS评分改善幅度更大,P0.05。结论小剂量奈达铂周疗方案同步放疗治疗中晚期宫颈癌的临床疗效确切,优于顺铂周疗方案同步放疗治疗,可有效改善病情,减少肾脏毒性、恶心呕吐等毒副作用的发生,但也增加了血液毒性,需引起注意。     

Highly stable core-surface-crosslinked nanoparticles as cisplatin carriers for cancer chemotherapy

Cisplatin is a potent anticancer drug with low solubility in water. A new type of highly stable polymer micelles, namely core-surface-crosslinked nanoparticles (SCNPs) made from amphiphilic brush copolymers, were evaluated as the carrier of cisplatin. Cisplatin could be loaded in the SCNPs with poly(varepsilon-caprolactone) (PCL) cores and hydrophilic poly(ethylene glycol) (PEG) or poly[2-(N,N-dimethylamino)ethyl methacrylate] (PDMA) shells with high loading efficiency (approximately 90%). In vitro cellular uptake experiments indicated that both SCNPs could be easily taken up by SKOV-3 ovarian cancer cells. Both cell proliferation assay and IC50 measurements indicated that cisplatin encapsulated in the SCNPs had much enhanced cytotoxicity to the cancer cells compared to free cisplatin. The positive charges on the PCL/PDMA SCNPs promoted the cellular internalization of the nanoparticles, resulting in higher cytotoxicity of cisplatin in these SCNPs. The IC50 of the cisplatin encapsulated in PCL/PDMA SCNPs was as low as 0.01 microg/mL, lower than that of cisplatin in PCL/PEG SCNPs and free cisplatin.     

Chemical composition and bioactivity of Citrus medica L. cv. Diamante essential oil obtained by hydrodistillation, cold-pressing and supercritical carbon dioxide extraction

The chemical composition of the essential oil of Citrus medica L. cv. Diamante peel obtained by hydrodistillation, cold-pressing and supercritical carbon dioxide extraction techniques was determined by GC/MS analysis. Forty-six components were fully characterised. Limonene and γ-terpinene were the major components of the oils obtained by hydrodistillation (HD) and cold-pressing (CP), while citropten was the major constituent in the oil obtained by supercritical carbon dioxide extraction (SFE). Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities were evaluated. The essential oil obtained by hydrodistillation exerted the highest inhibitory activity against BChE (IC?? value of 154.6 μg mL?1) and AChE (IC?? value of 171.3 μg mL?1. Interestingly, the oil obtained by cold-pressing exhibited a selective inhibitory activity against AChE. The essential oils have also been evaluated for the inhibition of NO production in LPS induced RAW 264.7 macrophages. The oil obtained by hydrodistillation exerted a significant inhibition of NO production with an IC?? value of 17 μg mL?1 (IC?? of positive control 53 μg mL?1).     

离子色谱法测定盐酸贝那普利片的含量

建立离子色谱法测定盐酸贝那普利片含量的方法。实验中选定了最佳的色谱条件为淋洗液:甲烷磺酸(6mmol/L)-乙腈(35%),流速:1.0mL/min,柱温:25℃,进样量:7μL。实验表明,贝那普利在0.5~25μg/mL范围内线性关系良好,相关系数r为0.999 9,检测限为0.089μg/mL,加标回收率为97.96%。方法操作简单,灵敏度高、准确、重现性好,可用于盐酸贝那普利片含量的测定。     

气相色谱-质谱法测定当归粉、当归原药材中的邻苯二甲酸二丁酯

建立了气相色谱-质谱法测定当归粉和当归原药材中邻苯二甲酸二丁酯（DBP）的方法。在国家标准的基础上,通过单因素试验,优化了提取方法和提取溶剂,确定了以正己烷为提取剂从水中液液萃取的方法。方法学试验结果表明,DBP浓度在0．01～1．00μg／mL范围内与色谱峰面积呈良好的线性关关系,线性相关系数r^2=0．9995,检出限为0．05μg／g（全扫描）,不同水平的加标回收率在90％～100％之间,测定结果的相对标准偏差小于5％（n=3）。该方法适合当归粉和当归原药材中DBP的日常检测。     

Synthesis and biological evaluation of glyco-GA compounds as anticancer agents

A series of novel glyco-gambogic acid（GA） compounds were synthesized and evaluated for their in vitro anti-proliferative activity against human hepatocellular carcinoma（HCC） cells.All compounds showed much better aqueous solubility（0.92- 1.89 mg/mL） than GA（0.013 mg/mL）,and displayed potent inhibition on HCC cells(IC₅₀:0.21-12.23μmol/L) and little affects on non-tumor liver cells(IC₅₀:42.56-86.43μmol/L),suggesting that glyco-GA compounds selectively inhibit HCC proliferation,and may be promising candidates for further intensive study.     

Free radical scavenging, antimicrobial and immunomodulatory activities of Orthosiphon stamineus

Orthosiphon stamineus is considered an important traditional folk medicine. In this study ethanol and aqueous extracts of O. stamineus were evaluated in vitro for their antioxidant, antimicrobial as well as for their immunomodulatory properties on human peripheral blood mononuclear cells (PBMCs). The DPPH radical scavenging method was used for the determination of antioxidant activity, while the antibacterial efficacy was investigated by both disc diffusion method and Minimum Inhibitory Concentration (MIC) against four bacterial strains (Gram-positive and Gram-negative). Furthermore, the immunomodulatory potential of the extracts was investigated through the MTT assay. Aqueous extract of O. stamineus exhibited significant free radical scavenging activity with IC?? 50 9.6 μg/mL, whereas the IC?? for the ethanol extract was 21.4 μg/mL. The best antimicrobial activity was shown by the aqueous extract of O. stamineus against Staphylococcus aureus, with inhibition zone of 10.5 mm and MIC value 1.56 mg/mL. Moreover, the results observed from the MTT assay showed that both plant extracts stimulated the PBMCs proliferation in vitro in a concentration-dependent manner, but the aqueous extract has remarkable activity against PBMCs. These findings indicate that O. stamineus showed high antioxidant activity and may be considered as an immunomodulatory agent.     

离子色谱法测定饮用水中痕量溴酸盐

建立了一种利用离子色谱法测定饮用水中痕量溴酸盐(BrO<,3><'->)的方法.色谱条件为:IonPac AS19(250mm x4 mm)色谱柱分离,KOH 梯度淋洗,流速1.0 mL/min,抑制电导检测,外标法定量.BrO<,3><'->浓度在2.0～100μg/L范围内有良好的线性,检出限为0.3 ng/mL,...     

Selective cytotoxicity of goniothalamin against hepatoblastoma HepG2 cells

Liver cancer has become one of the major types of cancer with high mortality and liver cancer is not responsive to the current cytotoxic agents used in chemotherapy. The purpose of this study was to examine the in vitro cytotoxicity of goniothalamin on human hepatoblastoma HepG2 cells and normal liver Chang cells. The cytotoxicity of goniothalamin against HepG2 and liver Chang cell was tested using MTT cell viability assay, LDH leakage assay, cell cycle flow cytometry PI analysis, BrdU proliferation ELISA assay and trypan blue dye exclusion assay. Goniothalamin selectively inhibited HepG2 cells [IC?? = 4.6 (±0.23) μM in the MTT assay; IC?? = 5.20 (±0.01) μM for LDH assay at 72 hours], with less sensitivity in Chang cells [IC?? = 35.0 (±0.09) μM for MTT assay; IC?? = 32.5 (±0.04) μM for LDH assay at 72 hours]. In the trypan blue dye exclusion assay, the Viability Indexes were 52 ± 1.73% for HepG2 cells and 62 ± 4.36% for Chang cells at IC?? after 72 hours. Cytotoxicity of goniothalamin was related to inhibition of DNA synthesis, as revealed by the reduction of BrdU incorporation. At 72 hours, the lowest concentration of goniothalamin (2.3 μL) retained 97.6% of normal liver Chang cells proliferation while it reduced HepG2 cell proliferation to 19.8% as compared to control. Besides, goniothalamin caused accumulation of hypodiploid apoptosis and different degree of G2/M arrested as shown in cell cycle analysis by flow cytometry. Goniothalamin selectively killed liver cancer cell through suppression of proliferation and induction of apoptosis. These results suggest that goniothalamin shows potential cytotoxicity against hepatoblastoma HepG2 cells.     

快速溶剂萃取-离子色谱法测定茶叶中的有机酸

建立了快速溶剂萃取-离子色谱法（ASE—IC）测定茶叶中的9种有机酸。优化了ASE苹取条件,以水为萃取溶剂,80℃下萃取5min,循环两次。采用Ionpac AS11HC柱分离,KOH溶液梯度洗脱,流速1,0mL／min,抑制电导检测。9种有机酸的检出限为0．009-0．160μg／mL,线性范围为0．5—10μg／mL,相关系数大于0．999,加标回收率为93．4％-99．2％,相对标准偏差为1．4％-4．1％。