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染料木素和柚皮素分别为黄酮类天然活性分子,具有抗氧化和抗肿瘤等多种生物活性。以染料木素和柚皮素为母体,分别在染料木素7-位酚羟基和柚皮素4-位羰基上引入含氮的肟基和肟醚单元,合成了4个黄酮肟和6个黄酮肟醚,并通过核磁共振(1H NMR)及高分辨质谱(HR-MS)进行了结构表征。采用MTT法对胃癌细胞株SGC-7901体外抗肿瘤活性筛选。结果表明:含肟基的化合物活性优于肟醚,化合物3c对胃癌细胞株SGC-7901有较好的抑制作用。 相似文献
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根据拼合原理, 设计并合成了21个未见报道的新的二芳醚基哌嗪类衍生物, 其结构用1H NMR, ESI-MS, HRMS进行了确证, 初步生物活性测定实验证明部分目标化合物具有良好的细胞毒活性. 化合物4i分别对人食管癌(Eca109)细胞株和人鼻咽癌(CNE)细胞株的IC50为7.13和4.54 μmol8226;L-1, 与对照品顺铂(DDP)相近. 化合物5d对人鼻咽癌细胞株也表现较好的活性, 其IC50为8.49 μmol8226;L-1. 相似文献
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柚皮素、柚皮苷与溶菌酶相互作用的荧光光谱法研究 总被引:2,自引:0,他引:2
应用荧光光谱法研究了50%甲醇/水体系中柚皮素、柚皮苷与溶菌酶分子间的结合反应. 以Lineweaver-Burk双倒数方程和能量传递原理分别计算了两者与溶菌酶反应的结合常数(K)和结合距离(r): K柚皮素25 ℃=4.00×104, K柚皮苷25 ℃=3.48×104; r柚皮素=3.21 nm, r柚皮苷=3.30 nm, 以及由热力学参数的计算判断了两种分子与溶菌酶之间的作用力类型. 结果表明: 柚皮素、柚皮苷均能与溶菌酶以疏水作用相结合形成非共价化合物, 从而导致溶菌酶内在荧光的静态猝灭; 相对柚皮素, 柚皮苷与溶菌酶的结合距离增大, 作用强度减弱, 表明黄酮分子上多糖的取代不利于黄酮分子与蛋白之间的亲和作用. 根据Haslam等提出的多酚-蛋白质反应模型, 从分子水平初步探讨了糖取代对黄酮分子与蛋白相互作用减弱的原因. 相似文献
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以4-甲氧基苯甲醛与2-溴-4’-氟苯乙酮为原料,经缩合、取代反应后,再与α-溴代酮或α-溴代酯反应,合成得到8个查尔酮哌嗪衍生物(3a~3h),其结构经1H NMR、13C NMR和HRMS确证。采用MTT法初步测试了所合成化合物的体外细胞毒活性,结果表明,哌嗪环上含酮基取代的化合物对肿瘤细胞株A549和SGC7901均表现出良好的抑制活性,特别是化合物3a(IC50=0.28μmol/L,2.53μmol/L)活性最高,值得进一步深入研究。 相似文献
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LIU Yazhou HUANG Lan SUN Qianyun ZHANG Maosheng LI Tianlei LIANG Guangyi PAN Weidong 《高等学校化学研究》2014,30(6):937-940
A series of derivatives of tetrandrine and fangchinoline was designed and synthesized to find more active anti-cancer compounds. Their anti-cancer activities were tested against human hcpatocellular carcinoma BEL-7402 and PLC/PRF/5 cells, human lung adenocarcinoma A549 cells as well as human leukaemia K562 cells, and the structure-activity relationship(SAR) was also studied. All the compounds except BI exhibited superior inhibitory ac- tivities against PLC/PRF/5 cells with half maximal inhibitory conccntration(ICs0) values of less than 15 μmol/L, and compounds A2, A4, B2 and B4 showed IC50 values of less than 9 pmol/L. Compounds A2, A6, B2 and B4 showed potent anti-cancer activities against all the tested cells with 1C5o values of less than 10 pmol/L. The results show that terandrine and fangchinoline derivatives are potential suppressors to human cancer. 相似文献
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柚皮苷分子印迹传感器的制备与应用 总被引:4,自引:0,他引:4
以邻氨基酚为单体,无电化学活性的柚皮苷为模板分子,采用循环伏安法(扫速为100mV/s)在碳电极上往复扫描30次,电聚合出具有识别柚皮苷分子功能的敏感膜。以扫描电子显微镜(SEM)、X射线全反射(XRR)及电化学方法对该印迹传感器进行表征。结果表明,印迹传感器敏感膜与非印迹膜在形貌结构和电化学特性方面有明显的不同。此传感器对柚皮苷有较好的选择性,响应快(30s),在6.0×10-5~1.4×10-4mol/L范围内呈线性关系,且重现性好(RSD=1.8%,n=5);传感器对柚皮苷的检出限为1.6×10-5mol/L。 相似文献
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本文利用环糊精修饰毛细管胶束电动色谱法(CD-MEKC)同时分离检测橙皮苷和柚皮苷对映体。实验优化的条件为:以60mmol/L胆酸钠(SC)+30mmol/L羟丙基-β-环糊精(HP-β-CD)+20 mmol/L NaH2PO4-100 mmol/L NaOH(pH=9.0,97%(V/V))+3%(V/V)甲醇为运行缓冲液,分离电压25kV,紫外检测波长214nm。在上述最佳条件下,橙皮苷和柚皮苷对映体在9min内得到完全分离,橙皮苷对映体的检测限(S/N=3)分别为0.13μg/mL和0.25μg/mL;柚皮苷对映体的检测限(S/N=3)分别为0.14μg/mL和0.07μg/mL。将所建立的方法用于胃苏颗粒制剂中橙皮苷和柚皮苷的对映体测定,回收率在86.0%~113.2%之间。 相似文献
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固体表面延迟荧光测定中草药中有效成分柚皮甙 总被引:2,自引:0,他引:2
以层析聚酰胺膜为基质,以LiAc作增强剂,建立了测定痕量中草药有效成分柚皮甙的固体表面延迟荧光法,该法聚样量少(2uL),线性范围宽(2.9~580.0ng/斑),检出限为0.033ng/斑。 相似文献
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Guzel Ziyatdinova Elvira Yakupova Endzhe Ziganshina Herman Budnikov 《Electroanalysis》2019,31(11):2130-2137
Carboxylated multi‐walled carbon nanotubes based glassy carbon electrodes (MWNT‐COOH/GCE) modified in situ with surfactants (sodium dodecyl sulfate (SDS), cetylpyridinium bromide (CPB) and Triton X100) have been tested for the naringin determination. The effect of surfactant nature and concentration on the voltammetric characteristics of naringin has been evaluated. Anionic 100 μM SDS shows the highest 2.7‐fold increase of the oxidation currents in comparison to MWNT‐COOH/GCE. The irreversible electrooxidation of naringin is surface‐controlled process with the one electron and one proton transfer. Under conditions of first order derivative linear sweep voltammetry in Britton‐Robinson buffer (BRB) pH 8.0, the analytical ranges of 0.75–25 and 25–100 μM with the LOD and LOQ of 0.14 and 0.46 μM, respectively, have been obtained. The electrode response is selective in the presence of ascorbic, gallic and p‐coumaric acids as well as quercetin, catechin and rutin. The method has been applied for the naringin quantification in grapefruit juices. 相似文献
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Squaric acid (dihydroxycyclobutenedione), the dianion of which may be regarded as a novel aromatic system, has recently become readily accessible by simple syntheses. The acidic character of squaric acid manifests itself in the formation of salts and of lower alkyl esters, which can be converted into the amides. Squaric acid dichloride shows in its reactions typical acyl chloride behavior. Condensation of squaric acid with pyrrole, phenol, and azulene derivatives yields cyclotrimethine dyes. 相似文献
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A novel compound 4-methyl-7-{[4-(2,2':6',2'-terpyridin-4'-yl)benzyl]amino}-2H-chromen-2-one(1) was synthesized, and its DNA-binding properties, cytotoxicity, and telomerase and Topo I inhibitory activities were evaluated. For comparison, the anti-proliferative and Topo I inhibitory activities of another two analogues 2 and 3 were also investigated. Compound 1 is able to stabilize the structures of human telomere(h-tert) and promoter(c-myc and c-kit2) G-quadruplexes and h-tert i-motif. The association constants(Kb) are about 106 L/mol for h-tert G-quadruplex and i-motif, while the values are about 105 L/mol for both promoter G-qaudruplexes and calf thymus DNA(ct-DNA). The binding of compound 1 induces the change of h-tert G-quadruplex from hybrid to antiparallel structure and exhibits 88.7% inhibition of telomerase activity at 8 mmol/L. Both compounds 1 and 3 inhibit significantly Topo I-mediated relaxation of pBR322 DNA. Compounds 1 and 2 show a high inhibitory efficacy on HepG2 and MCF-7 cancer cell lines with IC50 values of about 10-6 mol/L. The three compounds also induce a delay of cell cycle progression. The coumarin group is vital for improving the biological activity of terpyridine derivatives. 相似文献