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Shuqin Han Yuji Kanematsu Kazuyuki Hattori Hideki Nakashima Takashi Yoshida 《Journal of polymer science. Part A, Polymer chemistry》2009,47(3):913-924
A new anhydro disaccharide monomer, 1,6‐anhydro‐2,3‐di‐o‐benzyl‐4‐o‐(2′,3′,4′,6′‐tetra‐o‐benzyl‐β‐D ‐galactopyranosyl)‐β‐D ‐glucopyranose (benzylated 1,6‐anhydro lactose (LSHBE)), was synthesized from D ‐lactose to investigate the polymerizability and biological activities of the resulting branched polysaccharides. The ring‐opening polymerization of LSHBE was carried out with phosphorus pentafluoride as a catalyst under high vacuum to give a stereoregular benzylated (1 → 6)‐α‐D ‐lactopyranan. The molecular weights of poly(LSHBE)s increased with an increase in the amount of CH2Cl2 solvent, and polymerization temperatures were affected in both molecular weights and yields of the polymers. The copolymerization of LSHBE with benzylated 1,6‐anhydro‐β‐D ‐glucopyranose (LGTBE) gave the corresponding copolysacchrides having different proportions of lactose and glucose units in good yields. After debenzylation to recover hydroxyl groups and then sulfation, sulfated homopoly(lactose)s and copoly(lactose and glucose)s were obtained. Sulfated homopoly(lactose)s had moderate anti‐HIV (EC50 = 5.9 and 1.3 μg/mL) and blood anticoagulant activities (AA = 18 and 13 unit/mg), respectively. Sulfated copoly(lactose and glucose) having 15 mol % lactose units gave high anti‐HIV and blood anticoagulant activities of 0.3 μg/mL and 54 unit/mg, respectively. These biological results suggest that the distance between branched units on the main chain plays an important role in the anti‐HIV and blood anticoagulant activities. © 2008 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 47: 913–924, 2009 相似文献
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《中国化学》2018,36(8):731-736
A series of novel 3,4‐dichloroisothiazole based 1,2,4‐triazole derivatives were rationally designed and synthesized. Their structures were confirmed by 1H NMR, 13C NMR, HRMS or elemental analysis; the typical crystal structure was determined by X‐ray diffraction for validation. All target compounds were evaluated for their in vitro fungicidal and in vivo anti‐TMV activities. The bioassay results indicated that compound 6b , namely 1‐(3,4‐dichloroisothiazol‐5‐yl)‐1‐(4‐fluorophenyl)‐2‐(1H‐1,2,4‐triazol‐1‐yl)ethanol, exhibited excellent growth inhibition against B. cinerea, C. arachidicola and P. piricola with median effective concentrations (EC50) of 6.98, 2.73 and 3.07 μg/mL, respectively, and good in vivo anti‐TMV activity of over 60% of inactivation and induction activity at 100 μg/mL. These data demonstrate that compound 6b is both a fungicide and an anti‐TMV lead, deserving further studies. 相似文献
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Flavonoids Isolated from Heat‐Processed Epimedium koreanum and Their Anti‐HIV‐1 Activities 下载免费PDF全文
Hong‐Mei Li Cheng Zhou Chin‐Ho Chen Rong‐Tao Li Kuo‐Hsiung Lee 《Helvetica chimica acta》2015,98(8):1177-1187
Systematic phytochemical investigation on heat‐processed Epimedium koreanum led to the isolation of 13 flavonoids, including five new prenyl‐flavonol glycosides, koreanosides A–E ( 1 – 5 , resp.). Their structures were elucidated on the basis of detailed analysis of the 1D‐ and 2D‐NMR spectroscopic data and chemical reactions. Apigenin ( 11 ) exhibited moderate anti‐HIV‐1 activity with an EC50 value of 12.8±3.27 μg/ml. 相似文献
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A series of N‐(3‐amino‐3,4‐dihydro‐4‐oxopyrimidin‐2‐yl)‐4‐chloro‐2‐mercapto‐5‐methylbenzenesulfonamide derivatives 10‐17 have been synthesized as potential anti‐HIV agents. The in vitro anti‐HIV‐1 activity of these compounds has been tested at the national Cancer Institute (Bethesda, MD), and the structure‐activity relationships are discussed. The selected N‐[3‐amino‐3,4‐dihydro‐6‐(tert‐butyl)‐4‐oxothieno[2,3‐e]pyrimidin‐2‐yl]‐4‐chloro‐2‐metcapto‐5‐methylbenzenesulfonamide ( 14 ) showed good anti‐HIV‐1 activity with 50% effective concentration (EC50) value of 15 μM and weak cytotoxic effect (IC50 = 106 μM). 相似文献
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Tegshi Muschin Shuqin Han Taisei Kanamoto Hideki Nakashima Takashi Yoshida 《Journal of polymer science. Part A, Polymer chemistry》2011,49(15):3241-3247
To develop a biomaterial with an influenza virus‐adsorptive functionality, an alkyl curdlan sulfate was prepared by ionic interaction between a positively charged didodecyldimethyl ammonium bromide and a negatively charged sulfate group of curdlan sulfate, which has potent anti‐HIV activity, and then it was coated on a membrane filter with a 1‐μm pore size by hydrophobic interaction with the long alkyl groups in the curdlan sulfate. The alkyl curdlan sulfate with the degree of alkylation (DOA) of 0.03 (one didodecyldimethyl group/12 sugar residues with 36 hydroxyl or sulfate groups) showed potent anti‐HIV activity in a 50% effective concentration (EC50) as low as 0.87 μg/mL (standard curdlan sulfate EC50 = 0.3 μg/mL), and the activity decreased with increasing DOA. A DOA higher than 0.1 (one didodecyldimethyl group/three sugar residues with nine hydroxyl or sulfate groups) gave no anti‐HIV activity. Although both curdlan sulfate and alkyl curdlan sulfates did not inhibited infection of Madin‐Darby canine kidney cells by influenza viruses, the alkyl curdlan sulfate‐coated membrane filter was found to have a specific adsorptive functionality for influenza A virus in vitro. When 1.6 mg of the alkyl curdlan sulfate with the DOA of 0.03 was coated on a membrane filter (φ13 mm; pore size, 1 μm), three stacked alkyl curdlan sulfate‐coated membrane filters dramatically decreased hemagglutination to 1/4–1/32. However, the membrane filter did not effectively remove on influenza B viruses, and thus a membrane filter without alkyl curdlan sulfate was not effective against influenza viruses. These results can therefore be presumed to demonstrate that the alkyl curdlan sulfate‐coated membrane filter removed influenza A viruses by adsorption between the negatively charged sulfate groups and the positively charged envelope protein of the virus. © 2011 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem, 2011 相似文献
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Xiang‐Dong Qin Ze‐Jun Dong Ji‐Kai Liu Liu‐Meng Yang Rui‐Rui Wang Yong‐Tang Zheng Yang Lu Yun‐Shan Wu Qi‐Tai Zheng 《Helvetica chimica acta》2006,89(1):127-133
A novel benzofuran lactone, named concentricolide (= rel‐(6R)‐6‐ethylbenzo[2,1‐b:3,4‐c′]difuran‐8(6H)‐one; 1 ), was isolated along with four known compounds (friedelin, cytochalasin L‐696,474, armillaramide, and russulamide) from the fruiting bodies of the xylariaceous ascomycete Daldinia concentrica. The structure of 1 was established by spectroscopic methods and X‐ray crystallographic analysis. Its anti‐HIV‐1 activity was tested. Results showed that 1 inhibited HIV‐1 induced cytopathic effects. The EC50 value was 0.31 μg/ml. The therapeutic index (TI) was 247. Concentricolide exhibited the blockage (EC50 0.83 μg/ml) on syncytium formation between HIV‐1 infected cells and normal cells. 相似文献
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Hai‐Ying Tian Jun‐Jie Yan Di Wang Chen Gu Ye‐Zi You Xue‐Si Chen 《Macromolecular rapid communications》2011,32(8):660-664
New water‐soluble block copolymers of 2‐(2‐methoxyethoxy)ethyl methacrylate (MEO2MA), oligo(ethylene glycol) methacrylate (OEGMA), and N‐(3‐(dimethylamino) propyl) methacrylamide (DMAPMA) (poly(OEGMA‐co‐MEO2MA)‐b‐poly(DMAPMA)) were prepared via sequential reversible addition‐fragmentation chain transfer (RAFT) polymerization. Selective quaternization of poly(DMAPMA) block gives poly(OEGMA‐co‐MEO2MA)‐b‐poly((3‐[N‐(3‐methacrylamidopropyl)‐N,N‐dimethyl]ammoniopropane sulfonate)‐co‐N‐(3‐(dimethylamino) propyl) methacrylamide), such block copolymer exhibits double thermo‐responsive behavior in water, poly(MEO2MA‐co‐OEGMA) block shows a lower critical solution temperature (LCST), and poly((3‐[N‐(3‐methacrylamidopropyl)‐N,N‐dimethyl]ammoniopropane sulfonate)‐co‐N‐(3‐(dimethylamino) propyl) methacrylamide) block shows a upper critical solution temperature (UCST). Both of LCST and UCST can be controlled: LCST could be tuned by the fraction of OEGMA units in poly(OEGMA‐co‐MEO2MA), and UCST was found to be dependent on the degree of quaternization (DQ).
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Nicky Chan Nathan Yee So Young An Jung Kwon Oh 《Journal of polymer science. Part A, Polymer chemistry》2014,52(14):2057-2067
New poly(ethylene oxide)‐based block copolymers (ssBCs) with a random copolymer block consisting of a reduction‐responsive disulfide‐labeled methacrylate (HMssEt) and a thermoresponsive di(ethylene glycol)‐containing methacrylate (MEO2MA) units were synthesized. The ratio of HMssEt/MEO2MA units in the random P(MEO2MA‐co‐HMssEt) copolymer block enables the characteristics of well‐defined ssBCs to be amphiphilic or thermoresponsive and double hydrophilic. Their amphiphilicity or temperature‐induced self‐assembly results in nanoaggregates with hydrophobic cores having different densities of pendant disulfide linkages. The effect of disulfide crosslinking density on morphological variation of disulfide‐crosslinked nanogels is investigated. In response to reductive reactions, the partial cleavage of pendant disulfide linkages in the hydrophobic cores converts the physically associated aggregates to disulfide‐crosslinked nanogels. The occurrence of in‐situ disulfide crosslinks provides colloidal stability upon dilution. © 2014 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2014 , 52, 2057–2067 相似文献
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N-甲基-2-单芳基苯并噻唑啉 (1) 在固体状态时可以稳定地储藏在空气中。但是,它们在不同溶剂中却表现出了不同的行为。在醇溶液或二甲亚砜-水的体系中,1相对稳定;而在其它有机溶剂如:丙酮,氯仿,二氯甲烷和乙酸乙酯等溶剂中,会发生自发偶联反应生成相应的邻-(N-芳酰基-N-甲氨基苯)-二硫化合物 (2)。对这些新的化合物 (1) 和 (2) 进行了体外人乳腺癌细胞 (MDA-MB-231) 血管内皮生长因子靶点筛选,大部分化合物都表现出了抑制活性。实验结果表明这两类化合物 (1) 和 (2) 作为血管内皮生长因子抑制剂值得进行深入研究。 相似文献
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Su Yue Ze‐Zhao Jiao Hong‐Xiang Sun Tian‐Yun Jin Lan Xiang 《Helvetica chimica acta》2015,98(7):961-966
A new tricyclic alkaloid named portulacatone ( 1 ), i.e., 5,6‐dihydro‐8,9‐dihydroxy‐11H‐pyrrolo[2,1‐b] [3]benzazepin‐11‐one, together with eight known compounds, methyl 4‐hydroxyphenylacetate ( 2 ), p‐hydroxybenzaldehyde ( 3 ), vanillin ( 4 ), protocatechualdehyde ( 5 ), p‐hydroxybenzoic acid ( 6 ), iseluxine ( 7 ), oleracein E ( 8 ), and (+)‐(R)‐feruloyl malate ( 9 ) were isolated from aerial parts of Portulaca oleracea L. Their structures were elucidated based on spectroscopic analyses. Among them, compounds 1 – 7 and 9 were isolated from this medicinal plant for the first time. Compounds 1 and 7 showed dose‐dependent scavenging activities against DPPH (2,2‐diphenyl‐1‐picryl‐hydrazyl) free radical, with EC50 values of 14.36 μM and 9.98 μM , respectively, more potent than the natural antioxidant vitamin C (EC50 20.72 μM ). 相似文献
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Guang‐Yu Yang Wei‐Lie Xiao Ying Chang Rui‐Rui Wang Jian‐Xin Pu Xue‐Mei Gao Chun Lei Yang Lu Yong‐Tang Zheng Han‐Dong Sun 《Helvetica chimica acta》2008,91(10):1871-1878
Three new highly oxygenated nortriterpenoids, wilsonianadilactones A–C ( 1 – 3 ), together with twelve known ones, i.e., 4 – 15 , were isolated from the leaves and stems of Schisandra wilsoniana. Their structures were established by means of extensive analysis of spectroscopic data, and compound 1 was further confirmed by X‐ray crystallographic diffraction. Compounds 1 – 3 showed weak anti‐HIV‐1 activity with EC50 values of 23.5, 55.5, and 66.4 μg/ml, respectively. 相似文献
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Najim A. Al‐Masoudi Basil A. Saleh Nesreen Abdul Karim Ahmed Y. Issa Christoph Pannecouque 《Heteroatom Chemistry》2011,22(1):44-50
A series of new Cu(II), Pt(II), VO(II), Fe(II), and Co(II) complexes ( 1‐‐5 ) with 3‐methyl‐6,7‐diphenyllumazine are described. Similarly, complexes from 2‐thiouracil with Cu(II) ( 6,7 ) and Pt(II) ( 8 ) have been prepared and characterized by spectroscopic methods. All the complexes were assayed for their anti‐HIV‐1 and HIV‐2 activity by examination of their inhibition of HIV‐induced cytopathogenicity in MT‐4 cells. Compound 3 was found to be the most active inhibitor against HIV‐2 in cell culture (EC50 = >18.9 μ g/mL, selectivity index (SI) = 3), which provided a good lead for further optimization. Compounds 6 and 7 exhibited some activity (EC50 = >7.12 μ g/mL and >2.23 μ g/mL) against HIV‐1 and HIV‐2, but no selectivity was observed (SI <1). © 2010 Wiley Periodicals, Inc. Heteroatom Chem 22:44–50, 2011; View this article online at wileyonlinelibrary.com . DOI 10.1002/hc.20654 相似文献
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With the aim of discovering a lead compound for pyridine‐based fungicide bearing adamantane moiety, a series of novel O‐alkyl/benzyl‐1‐(adamantan‐1‐yl)‐2‐(pyridin‐3‐yl)ethan‐1‐one oximes were synthesized from 3‐methylpyridine, ethyl (adamantan‐1‐yl)carboxylate, and alkoxyamine or benzoxyamine hydrochloride. The in vitro antifungal activity against four pathogenic fungi was evaluated, and some compounds exhibited good antifungal activity. Compounds 3d and 3f demonstrated strong activity against Sclerotinia sclerotiorum, with EC50 values of 11.25 and 12.87 μg/mL, respectively; 3b , 3c, and 3k had notable activity against Botrytis cinerea, with EC50 values of 12.78, 12.57, and 11.97 μg/mL, respectively. For Rhizoctonia Solani, 3d and 3g showed sufficient activity with EC50 values of 9.66 and 8.90 μg/mL, respectively. In addition, 3d and 3g demonstrated moderate activity against Colletotrichum orbiculare, with EC50 values of 14.32 and 15.83 μg/mL, respectively. 相似文献
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Xiang Li Xiaojin Zhang Haopeng Sun Lei Zhang Yuan Gao Jinxin Wang Qinglong Guo Qidong You 《中国化学》2012,30(5):1083-1091
Gambogic acid (GA, 1 ), the most prominent representative of Garcinia natural products, has been reported to be a promising anti‐tumor agent. In order to further explore the structure‐activity relationship of GA and discover novel GA derivatives as anti‐tumor agents, 17 novel C‐37 modified derivatives of GA were synthesized and evaluated for their in vitro anti‐tumor activities against A549, HCT‐116, BGC‐823, HepG2 and MCF‐7 cancer cell lines. Among them, 11 compounds were found to be more potent than GA against some cancer cell lines. Notably, compound 8 was almost 5–10 folds more active than GA against A549 and BGC‐823 cell lines with the IC50 values of 0.12 µmol·L?1 and 0.57 µmol·L?1, respectively. Chemical modification at C‐37 position of GA by introducing of hydrophilic amines could lead to increased activity and improved drug‐like properties. These findings will enhance our understanding of the structure‐activity relationship (SAR) of GA and lead to the discovery of novel GA derivatives as potential anti‐tumor agents. 相似文献
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Alumina doping and sulfation in hierarchically porous zirconia solid acids have been achieved simultaneously via one‐pot and bi‐surfactant‐assisted self‐assembly process, using aluminum sulfate as both Al and SO42? sources. The prepared composite solid acids showed much enhanced acidity and recycling catalytic activity for an esterification reaction compared with sulfated zirconia without alumina doping and Al‐doped sulfated zirconia without hierarchically porous structure. 相似文献
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Hankun Zhou Si Chen Ning Gan Tianhua Li Yuting Cao Qianli Jiang 《Electroanalysis》2013,25(10):2384-2393
A novel sandwich‐type electrochemiluminescence (ECL) immunosensor was developed to enable the sensitive detection of HIV‐1 antibodies. This system incorporated mesoporous silica (mSiO2) complexed with quantum dots (QDs) and nano‐gold particles, which were assembled to enhance signal detection. Magnetic beads were used by immobilizing the secondary anti‐IgG antibody. This was first employed to capture HIV‐1 antibody (Ab) to form a Fe3O4/anti‐IgG/Ab complex. A high loading and signal‐enhanced nanocomposite (hereafter referred to as Au‐mSiO2‐CdTe) was used as a HIV‐1 antigen label. The Au‐mSiO2‐CdTe nanocomposite was conjugated with the Fe3O4/anti‐IgG/Ab complex to form an immunocomplex (hereafter referred to as Fe3O4/anti‐IgG/Ab/HIV‐1/CdTe‐mSiO2‐Au). This complex could be further separated by an external magnetic field to produce ECL signals. Due to the large specific surface area and pore volume of mSiO2, the loading of the CdTe QDs was markedly increased. Thus, the loaded QDs released a powerful chemiluminescent signal with a concordantly increased sensitivity of the immunosensor. The immunosensor was highly sensitive, and displayed a linear range of responses for HIV‐1 antibody across a dilution range of 1 : 1500 through 1 : 50 with the detection limit of 1 : 4500. The immunoassay can be a promising candidate in early diagnosis of HIV infection. 相似文献
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Shi‐Fei Li Ying‐Tong Di Yue‐Hu Wang Cheng‐Jian Tan Xin Fang Yu Zhang Yong‐Tang Zheng Ling Li Hong‐Ping He Shun‐Lin Li Xiao‐Jiang Hao 《Helvetica chimica acta》2010,93(9):1795-1802
One new anthraquinone glycoside, 6‐O‐(α‐L ‐rhamnopyranosyl‐(1→6)‐β‐d‐ glucopyranosyl)emodin ( 1 ), and two new sesquilignans, seslignanoccidentaliols A ( 2 ) and B ( 3 ), were isolated from the whole plant of Cassia occidentalis. The structures of the new compounds were established by means of spectroscopic methods, especially 2D‐NMR data (1H,1H‐COSY, HMQC, HMBC, and ROESY), as well as HR‐ESI‐MS analysis. One previously reported sesquilignan, erythro‐guaiacylglycerol‐β‐O‐4′‐(5′)‐methoxylariciresinol, was revised to be seslignanoccidentaliol A ( 2 ). The 6‐O‐(α‐L ‐rhamnopyranosyl‐(1→6)‐β‐d‐ glucopyranosyl)emodin ( 1 ) exhibited moderate anti‐HIV‐1 activity with an EC50 value of 2.90 μg/ml and a therapeutic‐index (TI) value of 260. 相似文献
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Two new 4‐hydroxyisoflavanes, cordifoliflavanes A and B (1 and 2), were isolated from the roots of Codonopsis cordifolioidea. Their structures were elucidated by spectroscopic methods, including extensive 1D‐ and 2D‐NMR techniques. Compounds 1 and 2 were tested for their anti‐HIV‐1 activities and anti‐tobacco mosaic virus activities. The results showed that compounds 1 and 2 have modest anti‐HIV‐1 activities and anti‐tobacco mosaic virus activities, respectively. 相似文献