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Synthesis, Anticonvulsant Activity and Cytotoxicity of Novel Valproic Acid Derivatives 新型丙戊酸衍生物的合成、抗惊厥活性及细胞毒性研究
Pub Date : 2017-04-01 DOI: 10.9790/5736-1004013745
T. A. Sheha, T. Ibrahim, Nader E Abo-Dya, M. Tantawy, M. El-nagar, Zakaria K M Abdel-Samii
Objective: The aim of this work was to construct novel hydrazones and thiosemsicarbazide derivatives of valproic acid. The new targets will be evaluated for their anticonvulsant activity and cytotoxicity effects. Methods: Targets 7a-k, 10. 11 were synthesized starting from valproic acid using benzotriazole activation and hydrazide and thiosemicarbazide chemistry. The anticonvulsant activity was evaluated by pentylenetetrazoleinduced seizures modes using sodium valproate as a standard for comparison of the activity. The compounds with high anticonvulsant activity were subsequently examined for cytotoxicity against HepG2 by MTT assay. Results: The new targets were characterized using 1 HNMR and 13 CNMR and their purity were authenticated by elemental analysis. Four compounds 7e, 7j, 10 and 11 exhibited the most potent anticonvulsant activity associated with low cytotixicity. Conclusion: Compounds 11 exhibited a moderate anticonvulsant activity and a significantly lower cytotoxicity than valproic acid and 5-fluorouracile suggesting that it could be used as a lead for the development of better anticonvulsant drug candidates.
目的:构建丙戊酸的新型腙和硫代氨基脲衍生物。新的靶点将被评估其抗惊厥活性和细胞毒性作用。方法:目标7a-k, 10。其中11种以丙戊酸为起始原料,采用苯并三唑活化、肼和硫代氨基脲化学合成。采用戊四唑诱导的癫痫发作模式,以丙戊酸钠作为比较活动的标准来评估抗惊厥活性。随后用MTT法检测具有高抗惊厥活性的化合物对HepG2的细胞毒性。结果:用1hnmr和13cnmr对新靶点进行了表征,并通过元素分析对其纯度进行了验证。其中化合物7e、7j、10和11表现出较强的抗惊厥活性,且细胞毒性较低。结论:化合物11具有中等的抗惊厥活性,且细胞毒性明显低于丙戊酸和5-氟尿嘧啶,可作为开发更好的抗惊厥候选药物的先导。
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引用次数: 1
Kinetic Modeling of Vitamin C (Ascorbic Acid) Degradation in Blanched Commonly Consumed Salad Vegetables Using Computer Simulation Analysis 用计算机模拟分析热漂后常见沙拉蔬菜中维生素C(抗坏血酸)降解的动力学模型
Pub Date : 2017-04-01 DOI: 10.9790/5736-1004015966
E. Awagu, E. Ekanem, A. M. Kolo, M. Adamu
Vitamin C (ascorbic acid) is one of the most important and popular vitamins, and is contained in most fruits and vegetables; the problem with vitamin C is its easy degradation during processing. In this study, the degradation kinetics of vitamin C was determined in Lettuce and Cabbage, and the processing treatment considered was blanching at 70 0 C of water differently for 5, 10, 15, 20,25,30,35 and 40 minutes. Samples were dried in mild temperature (15–20 0 C) and ground to find dust and High Pressure liquid chromatographic (HPLC) was used for determination of the AA of vegetable salad samples which consisted of an isocratic elution procedure with UV-Visible detection at 245nm. The rate constants were calculated for both vegetable salad samples under the same processing method using the integrated law method; half-life was also calculated. Degradation of ascorbic acid in Lettuce and Cabbage under the same pretreatment procedure followed the firstorder kinetic model, as the coefficient of determination (R 2 -value) were 0.8981 and 0.9785 respectively. The rate constant of ascorbic acid degradation for Lettuce and Cabbage under the same blanching conditions were 0.099 min-1 and 0.088 min-1 respectively. The half-life of Lettuce and Cabbage were 420.0892 and 472.6004 seconds respectively. The most appropriate vegetable salad under the blanching pretreatment procedure is the cabbage because its rate constant depicted from the model equations was lower, and the half life longer, hence, slower rate of degradation. The first order forecast (Ln(C)), was 0.657964 for Lettuce and 1.330017 for Cabbage, which further authenticate that blanched Lettuce degradation was higher than Cabbage under the same pretreatment conditions.
维生素C(抗坏血酸)是最重要和最受欢迎的维生素之一,大多数水果和蔬菜中都含有维生素C;维生素C的问题在于它在加工过程中容易降解。在本研究中,测定了生菜和卷心菜中维生素C的降解动力学,并考虑了在70 - 0℃的水下分别焯水5、10、15、20、25、30、35和40 min的加工处理。样品在15-20℃的温和温度下干燥,研磨以寻找粉尘,采用高压液相色谱法(HPLC)测定蔬菜沙拉样品中的AA,该方法采用等温洗脱法,紫外可见检测波长为245nm。采用积分律法计算了两种蔬菜沙拉样品在相同处理方法下的速率常数;还计算了半衰期。在相同的预处理条件下,生菜和白菜中抗坏血酸的降解符合第一种动力学模型,决定系数(r2值)分别为0.8981和0.9785。在相同的焯水条件下,生菜和白菜抗坏血酸降解速率常数分别为0.099 min-1和0.088 min-1。生菜和卷心菜的半衰期分别为420.0892和472.6004秒。在焯水预处理条件下,白菜的速率常数较低,半衰期较长,降解速度较慢,是最合适的蔬菜沙拉。生菜的一级预测Ln(C)为0.657964,大白菜的一级预测Ln(C)为1.330017,进一步证明在相同预处理条件下,焯水生菜的降解率高于大白菜。
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引用次数: 11
Synthesis, Characterization and Performance Evaluation of Poly Octadecyl Methacrylate and Poly Octadecyl Methacrylate-CoMethylmethacrylate as an Additive for Lubricating Oil 聚甲基丙烯酸十八酯及聚甲基丙烯酸十八酯-甲基丙烯酸乙酯润滑油添加剂的合成、表征及性能评价
Pub Date : 2017-04-01 DOI: 10.9790/5736-1004015058
Mohammad R. Ahmed, A. A. Mohammed, Maysoon. A.hamad
Methacrylate polymers are widely used as additives in lubricating oils, as pour point depressants and viscosity index improvers. In this study, homopolymer of Octadecyl methacrylate and Octadecyl methacrylate_co_methylmethacrylate with molar ratios of 30:70, 50:50 and 70:30 were synthesized and characterized. The free radical polymerization was carried out at 70 °C in toluene solvent and 2, 2′azobisisobutyronitrile (AIBN) as initiator. All products were characterized by FTIR, 1 H-NMR and gel permeation chromatography (GPC). The obtained results showed the efficacy of the additives as viscosity index improvers, pour point depressants. The pour points of most base oils containing each polymer decreased compared to that of the pure base oil. 70% octadecyl methacrylate units showed a 15C o reduction in their pour points, thus establishing the large efficiency of the products synthesized in this work. The efficiencies of the prepared compounds as viscosity index improvers were investigated. It was found that the efficiency of the prepared compound as viscosity index improvers increases with increasing the concentration of additives.
甲基丙烯酸酯聚合物被广泛用作润滑油添加剂、降凝剂和粘度指数改善剂。本文合成了摩尔比为30:70、50:50和70:30的甲基丙烯酸十八酯和甲基丙烯酸十八酯-辅酶-甲基丙烯酸甲酯均聚物,并对其进行了表征。以2,2′偶氮二异丁腈(AIBN)为引发剂,在70℃甲苯溶剂下进行自由基聚合。所有产物均通过FTIR、1h - nmr和凝胶渗透色谱(GPC)进行了表征。结果表明,添加剂具有改善粘度指数、降低凝点的作用。与纯基础油相比,含有每种聚合物的大多数基础油的倾点都降低了。70%甲基丙烯酸十八烷基酯单元的倾点降低了15℃,从而建立了本工作合成产品的高效率。考察了所制备的化合物作为粘度指数改进剂的效率。结果表明,随着添加剂浓度的增加,所制备的化合物作为粘度指数改进剂的效率提高。
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引用次数: 6
Profiling of Zn2+ Ion Sorption in Modeled Aqueous Solutions by different Parts of Maize Biomass 玉米生物量不同部位对模拟水溶液中Zn2+离子的吸附特性
Pub Date : 2017-04-01 DOI: 10.9790/5736-1003017075
C. Duru, I. Duru, F. Ibe, M. C. Enedoh
The efficiency of the husk, stalk, cob and seed chaff from maize biomass in the removal of Zn ions from solution under different conditions was studied and compared. Fourier Transform Infrared spectra of the different biomass parts before and after adsorption of metal ions showed that the husk and cob had more available functional groups and as such active sites for the adsorption of Zn 2+ ions than the seed chaff and stalk. Percentage removal of Zn 2+ ions from solution increased with increase in the studied pH range for all the parts. This value also increased with increase in biomass load for the husk and cob but showed an alternating increase and decrease in Zn 2+ ions removal as biomass load increased when the seed chaff and stalk were studied. At optimum pH and biomass load for the studied parts the maize husk gave the best removal efficiency of 72.8 %, making it a promising green packing material for industrial scale water treatment application.
研究并比较了不同条件下玉米生物质的皮、茎、穗轴和谷壳对溶液中锌离子的去除效果。吸附金属离子前后不同部位的傅里叶变换红外光谱表明,壳和穗轴比谷壳和秸秆具有更多的有效官能团和吸附Zn 2+离子的活性位点。溶液中zn2 +离子的去除率随pH值的增加而增加。该值也随谷壳和穗轴生物量负荷的增加而增加,但在研究谷壳和秸秆时,Zn 2+离子去除率随生物量负荷的增加而交替增加和减少。在最佳pH和生物质负荷条件下,玉米壳的去除率最高,为72.8%,是一种很有前景的绿色包装材料,可用于工业规模水处理。
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引用次数: 11
Corn Silk as Corrosion Inhibitor for Mild Steel in 0.1M HCl Medium 玉米丝对低碳钢在0.1M HCl介质中的缓蚀作用
Pub Date : 2017-04-01 DOI: 10.9790/5736-1003015160
K. Orubite, N. Ngobiri
The effectiveness of corn silk water extract (CSWE) as corrosion inhibitor of mild steel in 0.5M HCl solution at 303K,313K and 323K was investigated in this work. Various concentrations of CSWE (5%v/v, 10%v/v, and 15% and 20% v/v) were prepared from dried corn silk. The study was carried out using weight loss and AAS analysis. The results of the AAS analysis collaborated weight loss measurements on the efficiency of CSWE as corrosion inhibitor. Inhibition efficiency of 77.7% and 72.0% was obtained respectively using both methods. Inhibition efficiency increased with increase in concentration of CSWE (5%v/v<10%v/v <15% < 20% v/v) while corrosion rate decreased as concentration increased. Increase in temperature reduced inhibition efficiency and CSWE was shown to be most effective at 303K than at 313K and 323K. Kinetic study of the process proposed a first order reaction type. From thermodynamic parameters, inhibition was attributed to the existence of a protective film on metal surface by interaction between inhibitor molecules and metal ions in solution..Reaction rate constant values calculated were 0.0234, 0.0818 and 0.104 for the blank solution and 0.0049, 0.0328, 0.0416 for the highest inhibitor concentration of 20% v/v respectively at the different temperatures studied.Data obtained were subjected to Langmuir, Temkin and Frendlich isotherms. Langmuir model was found to be most fitted of the three models. The utility of a waste material as corrosion inhibitor is once more reported.
研究了玉米丝水提取物(CSWE)在303K、313K和323K的0.5M HCl溶液中对低碳钢的缓蚀效果。以干玉米丝为原料制备了不同浓度的CSWE (5%v/v、10%v/v、15%和20% v/v)。采用减重法和原子吸收光谱法进行研究。原子吸收光谱分析的结果与减重测量的结果一致,表明了CSWE作为缓蚀剂的效率。两种方法的抑菌率分别为77.7%和72.0%。随着CSWE浓度的增加,缓蚀效率增加(5%v/v<10%v/v <15% < 20% v/v),腐蚀速率随浓度的增加而降低。温度的升高降低了缓蚀效率,CSWE在303K时比313K和323K时最有效。动力学研究表明该反应为一级反应类型。从热力学参数上看,缓蚀剂分子与溶液中的金属离子相互作用在金属表面形成保护膜,在不同温度下,空白溶液的反应速率常数分别为0.0234、0.0818和0.104,最高缓蚀剂浓度为20% v/v时的反应速率常数分别为0.0049、0.0328和0.0416。所得数据采用Langmuir、Temkin和frenlich等温线。Langmuir模型是三种模型中最适合的。再一次报道了一种废料作为缓蚀剂的应用。
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引用次数: 5
Hydrogen Gas Production from Tannery Wastewater by Electrocoagulation of a Continuous Mode with Simultaneous Pollutants Removal 连续电凝法制备制革废水制氢,同时去除污染物
Pub Date : 2017-04-01 DOI: 10.9790/5736-1003014050
Abdalhadi Deghles, Uğur Kurt
The performance of a continuous electrocoagulation (EC) process was investigated for tannery wastewater treatment using aluminum and iron electrodes. The effects of the operating parameters, such as current density, pH of solution and inlet flow rate, on pollutants removal efficiency and recovery of hydrogen gas were investigated in order to optimize process performance. In the case of aluminum electrodes, The results showed that for tannery wastewater with an influent pH adjusted at about 6, the use of a current density of 14 mA/cm 2 , and an EC time of 125 min, gave access to pollutants (COD, Color, Cr, and NH3-N) removal efficiency 73, 94, 100 and 51%, respectively. The energy yield of harvested hydrogen was 16% of the electrical energy demand of the electrocoagulation process. However, in the case of iron electrodes, with effluent pH adjusted at about 7, , the use of a current density of 14 mA/cm 2 , and an EC time of 125 min, gave access to pollutants (COD, Color, Cr, and NH3-N) removal efficiency 67, 93, 100 and 46 %, respectively. And also, the energy yield of harvested hydrogen was 15 % of the electrical energy demand of the electrocoagulation process. Thus, the operating costs for two cases were found to be 0.675 $/m 3 wastewater. It could be seen that hydrogen gas production coupled with pollutants removal efficiency by EC continuous mode would be an effective approach for energy recovery and wastewater reutilization.
研究了连续电絮凝(EC)工艺处理铝、铁电极制革废水的性能。为了优化工艺性能,研究了电流密度、溶液pH、进口流量等操作参数对污染物去除效率和氢气回收率的影响。以铝电极为例,在pH值为6左右、电流密度为14 mA/ cm2、EC时间为125 min的条件下,对制革废水的COD、Color、Cr和NH3-N的去除率分别为73,94,100和51%。收获的氢气的能量产量为电凝过程电能需求的16%。然而,在铁电极的情况下,将出水pH调节为约7,使用14 mA/ cm2的电流密度,EC时间为125 min,对污染物(COD, Color, Cr和NH3-N)的去除效率分别为67%,93%,100%和46%。而且,收集的氢气的能量产量是电凝过程所需电能的15%。因此,两个案例的运营成本为0.675美元/立方米废水。由此可见,EC连续模式的产氢与污染物去除效率相结合,将是实现能源回收和废水回用的有效途径。
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引用次数: 9
Comparison of ground water quality between CEPZ industrial area and Hathazari non industrial area in Chittagong, Bangladesh 孟加拉国吉大港CEPZ工业区与Hathazari非工业区地下水水质比较
Pub Date : 2017-03-01 DOI: 10.9790/5736-1003010105
N. Islam, A. Morshed, D. Paul
Assessment of the quality of underground water is an important issue for the safety of mankind who uses this as drinking water and other purposes. For this reason, the present research activities have been focused on various essential physico-chemical parameters such as pH, electrical conductivity, total solids, total suspended solids, total dissolved solids, total hardness, turbidity, sulphate, nitrite, nitrate, phosphate, chloride, total alkalinity, arsenic, iron, manganese, chromium, nickel, cadmium, lead, magnesium, potassium, calcium, cobalt, mercury, copper and zinc of water samples from study area. In Chittagong Export Processing Zone (CEPZ) industrial area, most of the values of physico-chemical parameters for collected samples have exceeded the acceptable range of World Health Organization (WHO) and Bangladesh Standard and Testing Institute (BSTI). On the other hand, in Hathazari non-industrial area, almost all the values of both physical and chemical parameters as well as the trace metals have not crossed the acceptable limit according to WHO and BSTI.
地下水的水质评价是人类饮用水和其他用水安全的重要问题。因此,目前的研究活动主要集中在研究区域水样的各种基本物理化学参数,如pH值、电导率、总固体、总悬浮固体、总溶解固体、总硬度、浊度、硫酸盐、亚硝酸盐、硝酸盐、磷酸盐、氯化物、总碱度、砷、铁、锰、铬、镍、镉、铅、镁、钾、钙、钴、汞、铜和锌。在吉大港出口加工区(CEPZ)工业区,所采集样品的理化参数值大多超出了世界卫生组织(世卫组织)和孟加拉国标准与检测研究所(BSTI)的可接受范围。另一方面,在哈扎扎里非工业地区,几乎所有的物理和化学参数值以及微量金属都没有超过世界卫生组织和BSTI规定的可接受限度。
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引用次数: 0
Evaluation of Minerals Content in SolaniumDubium Collected From White Nilein Central Sudan 苏丹中部白尼罗河中所采铀矿物含量的评价
Pub Date : 2017-03-01 DOI: 10.9790/5736-1002010111
A. Mohammed
Some plants of the family solanaceae such as Solanumdubium"Gubbain", which is a well-known wild plant, grow wildly in many regions in Sudan during the rainy season.Solanumdubiumis used in rural areas for milk coagulation. It is a bushy pubescent herb grown widely in northern, central and western Sudan along with other species such as S. innacum, S. esculentum, S. macrocarpon and S. melongena.Research on S. dubium was focused mainly on obtaining Solanum crude enzyme from the seeds in pure form and commercial production of the enzyme for cheese making. Solanaceous plants are known for their high alkaloidal content in all plant parts including the seeds, which are responsible for their antimicrobial activity in addition to other metabolites such as flavonoids and tannins. This study was conducted to determine the chemical composition of the seeds ofSolanumdubiumplant and its properties.Plant Solanumdubium have been used as milk coagulants in cheese making for centuries either as crude extracts or in purified form. These coagulants are an alternative to the calf rennet due to the limited availability and high price of rennet, religious factors, diet or ban on recombinant calf rennet in some countries. These enzymes are found in almost all kinds of plant tissues and can be obtained from their natural source or through in vitro culture to ensure a continuous supply of plant proteases. The excessive proteolytic nature of most plant coagulants haslimited their use in cheese manufacturing due to lower yields of cheese, bitter flavors and texture defects. The search for new potential milk-clotting enzymes from plants still continues in order to meet the increasing global demand for diversified and good quality cheese production. For the great important uses ofsolanum,the study aim’s to focus of the active chemicals component in solanum seeds. The seeds of Solanumdubium were blended and extracted using different types of buffers. The most reliable, quick, and efficient buffer was found to be 5% NaCl in acetate buffer (pH 5.0) which was used throughout the study. The extract was filtered and fractionated twice with ammonium sulphate. When compared with other plant enzymes, S. dubium enzyme was found to have higher clotting and proteolytic activities. The activity of the enzyme was steadily increased with enzyme and substrate concentration. The enzyme was found to be very stable against a wide range of pH values as well as a wide range of temperature (20–90 °C). The results of substrate specificity of the enzyme showed that the partially purified enzyme preferred both hydrophilic and hydrophobic amino acid residues at P1 position. The catalytic efficiency of the purified enzyme was enhanced by an aliphatic amino acids (Leu) compared to aromatic residue (Phe) at P1 position at the same site.And the morphology of solanum seeds was studied with scanning electron microscopy of mucilage at different magnification using Philips, Lancashire, XL-30 SEM and the result
茄科的一些植物,如著名的野生植物茄(Solanumdubium"Gubbain"),在雨季时在苏丹的许多地区疯狂生长。Solanumdubiumis用于农村地区的牛奶凝固。它是一种浓密的短柔毛草本植物,广泛生长在苏丹北部、中部和西部,与其他物种如S. inacum、S. esculentum、S. macrocarpon和S. melongena一起生长。对茄属植物的研究主要集中在从茄属植物种子中提取纯化的粗酶和用于奶酪生产的酶。众所周知,茄属植物包括种子在内的所有植物部位都含有很高的生物碱,除了黄酮类和单宁等其他代谢物外,生物碱还具有抗菌活性。对茄属植物种子的化学成分及其性质进行了研究。几个世纪以来,植物茄一直被用作奶酪制作中的牛奶凝固剂,无论是作为粗提取物还是纯化形式。这些凝血剂是小牛凝血酶的替代品,由于凝血酶的有限供应和高价格,宗教因素,饮食或在一些国家禁止重组小牛凝血酶。这些酶几乎存在于各种植物组织中,可以从其天然来源或通过离体培养获得,以确保植物蛋白酶的持续供应。大多数植物凝固剂的过度蛋白水解性质限制了它们在奶酪制造中的应用,因为奶酪产量低,味道苦,质地缺陷。从植物中寻找新的潜在凝乳酶仍在继续,以满足全球对多样化和高质量奶酪生产日益增长的需求。鉴于茄属植物的重要用途,本研究的重点是研究茄属植物种子中的活性化学成分。采用不同类型的缓冲液对茄属植物种子进行混合提取。发现最可靠、快速、有效的缓冲液是5% NaCl在醋酸缓冲液(pH 5.0)中,该缓冲液在整个研究中使用。提取液经过过滤,用硫酸铵进行两次分馏。与其他植物酶相比,dubium酶具有较高的凝血和蛋白水解活性。酶的活性随酶和底物浓度的增加而稳步增加。该酶在很宽的pH值范围内以及很宽的温度范围内(20-90°C)都非常稳定。底物特异性结果表明,部分纯化后的酶对P1位置的亲水和疏水氨基酸残基均有选择性。与同一位点P1位置的芳香族残基(Phe)相比,脂肪族氨基酸(Leu)提高了纯化酶的催化效率。用Philips、Lancashire、XL-30扫描电镜对不同倍率下的胶浆进行了形貌研究,结果见图5、6、7),并用红外光谱观察了胶浆结构的分异,见图8。在本研究中,测定了Mn、Cr、Cd、Zn等金属。在白尼罗州kenana地区采集的茄种子样品中,样品中最大允许含量分别为K、Cr、Fe、Cd、Zn、P等金属流和K、Mg、K、P等基本元素。表2和表3显示了茄种子中的金属浓度。研究结果表明,茄中重金属含量呈显著正相关。结果表明,在奶酪工业中使用的凝固剂类型对所研究的所有化学成分都没有显著影响。
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引用次数: 0
Partial Derivatives Involving Generalized I–Function of Two Variables 二变量广义i函数的偏导数
Pub Date : 2017-03-01 DOI: 10.9790/5736-1002012729
S. S. Dubey, S. Shrivastava
The aim of this paper is to derive partial derivatives involving generalized I–function of two variables.
本文的目的是推导涉及两变量广义i函数的偏导数。
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引用次数: 0
Nano Technology in Architecture: Exploring Possibilities. 纳米技术在建筑中的应用:探索可能性。
Pub Date : 2017-03-01 DOI: 10.9790/5736-1002014447
Anjali Acharya, S. Giri, V. Gokhale
The nano science and nano-engineering is also referred as nano modification, have come into common usage and describe two main avenues of application of nanotechnology in architectural application. Even though a huge and alluring potential of nanotechnology in architecture and civil engineering has been envisaged and enormous efforts throughout the world are being taken unto use nanotechnology in architectural applications, still few of grey areas need to be explored to make the technology more applicable. This paper presents the developments in the field of nanotechnology and nano science research in architectural development.
纳米科学和纳米工程也被称为纳米修饰,已经得到普遍应用,描述了纳米技术在建筑应用中的两种主要应用途径。尽管人们已经预见到纳米技术在建筑和土木工程方面具有巨大而诱人的潜力,并且全世界都在努力将纳米技术应用于建筑应用,但为了使这项技术更适用,还需要探索一些灰色地带。本文介绍了纳米技术和纳米科学在建筑发展中的研究进展。
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引用次数: 0
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IOSR Journal of Applied Chemistry
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