Gold nanoparticles (AuNPs) were prepared by reducing HAuCl4 with pear juice as reducing and protecting agent, which was rapid and environmentally friendly. AuNPs were characterized by scanning electron microscopy (SEM), Fourier Transform Infra-Red (FT-IR) and ultraviolet-visible (UV-Vis) spectroscopy. Compared with AuNPs prepared using citrate sodium as reducing agent, AuNPs synthesized by pear juice were more stable. AuNPs were used for colorimetric detection of vitamin C. When this as-prepared AuNPs mixed with AgNO3 and vitamin C, AgNO3 was reduced to Ag by vitamin C and deposited on the surface of AuNPs to form Ag/AuNPs , which was accompanied by a color change , as well as the increase of the Ag/AuNPs peak absorbance at 432 nm monitored by UV-Vis detection. Vitamin C could be analyzed qualitatively by the naked eyes according to the color change and quantitatively by UV-Vis detection. The main factors influencing detection of vitamin C were investigated in detail, including the volume of AgNO3, the pH value and the incubate time. When the concentration of vitamin C was 0.8 mg/L, the solution could be observed from red to brown with naked eyes. The linear range of vitamin C was from 0.4 mg/L to 40 mg/L and from 40 mg/L to 80 mg/L, the relative standard deviation (RSD) was 1.6% (n=8 , C-Vc =8 mg/L) and the limit of detection (LOD) was 0.17 mg/L. This method had good selectivity and specificity and was applied to detect vitamin C in vitamin C tablets with recoveries ranging from 89.5% to 110.0%.

A novel series of 4, 6-disubstituted pyrimidines derivatives were designed, synthesized, and evaluated as epidermal growth factor receptor (EGFR) inhibitors for non-small cell lung cancer(NSCLC). 4, 6-disubstituted pyrimidines as core structure was utilized to substitute the lead structure AZD3759 of the quinazoline basic skeleton via an approach involving scaffold hopping. It was found that compound Yfq07 exhibited the best inhibitory effect compared with AZD3759 in vitro and in vivo: Yfq07 exhibited a competitive ATP inhibitory effect, multiple target effects, and further featured a stronger activity against H3255, A431, HCC827, PC-9 and H1975 compared to AZD3759. Moreover, a stronger pro-apoptotic effect, inhibition of cell G2/M phase on A431, H3255, HCC827 and H1975 could also be observed. In this study, the ultimate goal was changing the core structure to improve other epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) properties while retaining the overall potency. Yfq07 was further explored as an effective 4, 6-pyrimidine anticancer agent for the treatment of human NSCLC.

BACKGROUND:Thienopyrimidinone is a newly designed, selective fibroblast growth factor receptor 1 (FGFR1) inhibitor with an excellent anticancer effect.OBJECTIVE:The goal of the present study was to design and synthesize better FGFR1 inhibitors through modifications of the lead compound thienopyrimidinone.METHODS:In the present study, a series of C-2 substituted derivatives of thienopyrimidinone, namely L1-L16, were synthesized, and their inhibitory effects on FGFR1 were evaluated. The anti-proliferative activities of these compounds were assessed by MTT assay.RESULTS:Among the novel derivatives, L11 was found to exert remarkable FGFR1 inhibitory activity (79.93% at 10 µM) and anti-proliferative activity, with IC50 values of 2.1, 2.5, and 3.5 .M in the FGFR1-overexpressing cell lines, H460, HT-1197, and B16F10, respectively.CONCLUSION:Our newly synthesized thienopyrimidinone derivatives may be candidate FGFR1 inhibitors for future development as novel anticancer agents.

Curcumol is the effective component of traditional Chinese medicine curcuma and modem Chinese medicine zedoary oil.The medicinal research related to curcumol is worth to be carried out by pharmaceutical scientists,for curcumol has many important bioactivities,such as antitumor,anti-reproduction,anti-inflammatory and so on.This review discussed the progresses of curcumol in pharmacology,toxicology,pharmacokinetics and pharmacodynamics.

Several derivatives of γ‐aminopropyl silatrane containing acyclovir in their molecular structure were synthesized and evaluated for their immunomodulatory and antiviral activities. The structures of all these derivatives were confirmed by mass spectra, IR, and 1H NMR. Based on WST‐1 assay in vitro, these compounds could stimulate proliferation of splenic lymphocytes at certain concentrations. Furthermore, compound 3d could also potentiate the expression of IFN‐γ, IL‐2, CD4+, CD8+, and CD4+/CD8+ in vivo. Our results show that these derivatives possess antiviral activity against herpes simplex viruses with a similar potency to acyclovir without a cellular immune response.

Experiment teaching of pharmacy specialty can effectively improve the ability of students'exper-imental practice.It is very important that evaluation system of experiment achivement to reflect the the ex-perimental teaching effect will be established.By analysis of the defects of achievement evaluation for the traditional experimental teaching,the paper proposes that the evaluation system of experiment achivement based on platform of laboratory admittance should be established.This system provides preliminary work for the reform of pharmacy professional experiment teaching.

Several derivatives of -aminopropyl silatrane containing acyclovir in their molecular structure were synthesized and evaluated for their immunomodulatory and antiviral activities. The structures of all these derivatives were confirmed by mass spectra, IR, and H-1 NMR. Based on WST-1 assay in vitro, these compounds could stimulate proliferation of splenic lymphocytes at certain concentrations. Furthermore, compound 3d could also potentiate the expression of IFN-, IL-2, CD4(+), CD8(+), and CD4(+)/CD8(+)in vivo. Our results show that these derivatives possess antiviral activity against herpes simplex viruses with a similar potency to acyclovir without a cellular immune response.

Using curcumol that was extracted from the volatile oil of Rhizoma Curcumae as the raw material, its derivatives were synthesized and purified. The structures of these compounds were confirmed by 1H, 13C NMR, and mass spectral data. The test compounds were evaluated for their in vitro anti-tumor activity against gastric cancer cell lines SGC-7901 and lung carcinoma cell line H460 by methyl thiazolyl tetrazolium chromatometry. Distinct structure–activity relationships of these curcumol derivatives were also revealed for inhibiting cell proliferation. Presence of electron-withdrawing groups or amino could increase the activity significantly, whereas esterification of 8-hydroxy diminished the anti-tumor activity. Many of the tested candidates exhibited higher inhibition efficiency than curcumol, suggesting that structural modifications could enhance its activity effectively.

Curcumol reacts under the Woodward-Prevost conditions providing not usual products but several unexpected derivatives A~C. The structures of compounds A~C were determined by MS, NMR and X-ray diffraction analysis. A plausible mechanism involved in their formation was discussed.

Objective:To explore the emmetropia intervention on the prevention and treatment of the myopia in early days.Methods: 200 cases of visual acuity above 1.0,refraction at 0~+0.75 D,the age at 4~7 year old,were divided into control and intervention group,each 100 cases.The control had never given any processing,the intervention was given Atropine sulfate eye ointment/week or given the Tropicamide eye drops to sleep before drop an eye/day,reexamine visual acuity and refraction annually,continuously for 5 years.The difference of group was tested with four space watch card square examination.Results: With the Visual acuity decreased below 1.0,the control group was 47 people,account for 47.5%,the intervention group was 21 people,account for 21.4%.The control group showed the specific value higher(χ2=14.78,P0.01).The refraction decreased below-0.25 D,the control group was 49 people,account for 49.5%,the intervention group was 24 people,account for 24.5%.The control group showed specific value higher(χ2=13.2,P0.01).Conclusion: It has the clinical meaning to start the intervention of the emmetropia in early days.

Objective:To improve the synthetic technique of isoflavone derivatives.Methods:Eight different isoflavone derivatives were synthesized through F-C acylation,cylization,and/or hydrolysation using resorcinol and arylacetic acids as raw materials.Results:The structures were confirmed by 1H-NMR,IR and MS.Conclusion:This synthetic route has mild reaction condition,convenient disposition,and good yield.

The isomers of 10,14-epoxycurcumol derivatives were separated by the ionic liquid [BMIm]BF4, in which there is a difference in the solubility of the complexes formed with the isomers and [BMIm]BF4. The yield 22% of (10R)-10,14-epoxycurcumol (E1) with 99% ee and the yield 49% of (10S)-10,14-epoxycurcumol (E2) with 92% ee were obtained respectively in the resolution. The ionic liquid could be recovered easily and used again with the same separation effect.

Objective:To synthesize three target compounds in order to explore the growth regulating activity on radishes and corns.Methods:Triisopropanolamine and γ-aminopropyltriethoxysilane were used as raw materials to obtain the new target compounds through silylation and acylation.Method of plating test was used to examine growth regulating activity of target compounds on radishes of amphibrya and corns of dicotyledon under the concentration of 20,50,100 ppm.Results:The stucture of target compounds were identified by 1H-NMR,MS,IR and elemental analysis.The test results showed that all compounds have definite plant growth regulating activity.The optimal concentration of target compounds for promoting plant growth was 50 ppm.Conclusion:The target compounds have definite growth regulating function for the radish seeds and corn seeds.

目的:合成两个新的化合物γ-(甲基取代苯氨基甲酰胺基)-丙基-2,8,9-三氧杂-5-氮杂 -1-硅杂三环[3,3,3,01,5]十一碳烷3a和3b,并对其抗炎活性进行研究.方法:先合成γ-氨丙基杂氮硅三环,对其氨丙基上氨基进行异氰酸酯化得到.通过环氧化酶(COX)抑制剂体外试剂盒,设40、80、160μg/mL三个浓度对化合物进行抗炎实验.结果:合成的目标物结构经IR、MS、1H-NMR及元素分析验证确认;对COX -1抑制活性最高的是化合物3a在160μg/mL时,抑制率为33.34%;抑制活性最低的是3b在40 μg/mL时,抑制率为1.67%;对COX-2抑制活性最高的是化合物3a在160 μg/mL时,抑制率为20.22%,抑制活性最低的是3b在40μg/mL时,抑制率为1.78%.结论:化合物3a具有一定的COX抑制活性,在三个浓度条件下, 随浓度的升高而活性增强.

Objective:To explore the antitumor activity of the compound 1-[3-[2-[1-(5-fluorouracil)]acetamide]propyl]-2,8,9-trioxa-5-azal-1-silicontricyclo[3,3,3,01,5]undecane on Hela,SW480 and A549.Methods:The concentration of the compound was prepared as 25,50,100,200,400 mg/L using culture media.The antitumor activity on Hela,SW480 and A549 was analyzed with MTT method.Results:The compound showed no inhibitive effect in vitro on Hela and the inhibition ratio depended on the increasing concentration.The inhibitive effect on SW480 was the highest,which was up to 50.2% under the 400 mg/L concentration.Conclusion:The compound shows an elective antitumer activity.

<正>1-取代-2,8,9-三氧杂-5-氮杂-1-硅三环[3.3.3.01,5]十一烷,简称杂氮硅三环,是一类具有特殊分子结构和显著生物活性的有机硅化合物。随着对其结构与生物活性的研究深入,越来越多的新发现证明了这是一种拥有广阔应用前景的化合物。笔者现对杂氮硅三环的生物活性研究进展作一些

The m-difluorobenzene was brominated,and the composition and structure of products were analyzed by Gas Chromatography/Mass Spectrometer(GC/MS).The optimum preparation conditions were selected with orthogonal design combined with multi-index test.According to Z-score result,the optimum conditions for preparation of 1-bromo-2,4-difluorobenzene was: carbon tetrachloride as solvent,reaction molar ratio of 2∶1,reaction temperature at 5℃ and reaction time at 12 h.The results showed that the product purity prepared under the optimum conditions was higher than 99.50%.

Objective:To synthesize the target compound γ-(3,4-dichlorobenzoyl) aminopropyl-3,7,10-trimethy1-2,8,9-trioxa-5-azal-1-silicontricyclo[3,3,3,01,5] undecane and to explore the growth regulating activity on radishes and corns.Methods:Triisopropanolamine and γ-aminopropyl triethoxysilane were used as raw materials to obtain the new target compound through silylation and acylation.Plating method test was used to examine growth regulating activity of compound I and II on radishes of amphibrya and corns of dicotyledon under the the concentration of 20,50,100 ppm.Results and Conclusion:The stucture of compound I and II were confirmed by 1H-NMR,IR and elemental analysis.The test of their biological activity shows that compound II has good plant growth regulating activity and is better than I.The optimal concentration of I and II for promoting plant growth is 50 ppm.

We carried out a series of reforms on the teaching of medical chemistry experiments.It includes the content of course,the teaching methods,and the inspection methods.We combined theory with practice and the students'initiative and comprehensive qualities have been greatly increased.

Carmofur was obtained by the one-pot method based on the reaction of 5-fluorouracil with n-hexylamine using triphosgene as the acylating agent.The technological conditions of synthesis were preliminary explored.The optimum reaction conditions were obtained as follows:pyridine was used as the solvent and catalyst,the ratio of n(triphosgene):n(5-fluorouracil) was equal to 1.2,the reaction temperature was 50 ℃,and the reaction time was 2 h,with the product yield reaching 92.7%.