溶剂极性对沙棘渣提取物组成及体外降血糖、降血脂活性的影响

为探讨溶剂极性对沙棘渣提取物组成及体外降糖降脂活性影响，以沙棘果渣和籽渣为原料，采用不同极性溶剂经超声波辅助提取，评价沙棘渣中活性成分含量及其体外降血糖和降血脂能力，结合超高效液相色谱串联四极杆静电场轨道阱高分辨质谱(UPLC-Q-Orbitrap HRMS)对沙棘渣中活性成分进行鉴定。结果表明，溶剂极性对多酚类化合物的提取效率、降血糖、降血脂能力有显著影响，其中60%乙醇提取物具有最高的粗提物得率，果渣的60%乙醇提取物中总酚含量（11.08 mg/g）、总黄酮含量（6.49 mg/g）和原花青素含量（6.18 mg/g）最高。籽渣的80%乙醇提取物中总酚含量（25.70 mg/g）最高，丙酮提取物中总黄酮含量（14.23 mg/g）、原花青素含量（16.87 mg/g）最高。沙棘果渣和籽渣丙酮提取物具有最好的α-葡萄糖苷酶与α-淀粉酶活性抑制能力。籽渣80%乙醇提取物、果渣60%乙醇提取物具有最好的甘氨胆酸钠和牛磺胆酸钠结合能力。原花青素是籽渣提取物体外降血脂、降血糖活性主要贡献者。果渣提取物中的总多酚与降血脂能力显著相关。从沙棘渣提取物中共鉴定出37种化合物，主要为黄酮和萜类成分。沙棘籽渣提取物具有很强的体外降血糖、降血脂活性，有望用于特膳食品和功能性食品基料的研发。     

不同品种松树皮活性成分及其提取影响因素

本研究选择华南地区五种松树品种,通过活性成分含量和抗氧化活性复合响应值筛选最佳的松树品种,并分析不同提取条件(提取时间、提取温度、溶剂浓度、液料比和提取次数)对原花青素提取率和清除自由基活性的影响。试验结果表明:不同品种松树树皮活性物质的含量差异显著,马尾松树皮的总多酚含量、总黄酮含量、原花青素和水溶性多糖含量最高,分别为(107.5±6.31)mg/g、(81.1±4.67)mg/g、(36.8±2.31)mg/g和(24.9±3.17)mg/g。通过马尾松树皮原花青素含量和清除DPPH自由基能力复合响应值分析,不同的提取条件对其影响显著,最佳影响因素为乙醇浓度为60%,提取温度50℃,提取时间90 min,液料比25∶1。     

黑果腺肋花楸有效物质的提取及抗氧化和降糖活性研究

以黑果腺肋花楸多酚含量、黄酮含量及出膏率为考察指标,采用单因素实验和正交实验并通过多指标综合评分法优化黑果腺肋花楸多酚和黄酮的提取工艺;通过对DPPH的清除能力评价其抗氧化活性;并通过建立肝细胞高糖损伤模型,比较提取物组与模型组葡萄糖消耗量评价其降糖活性。结果表明,黑果腺肋花楸多酚和黄酮的最佳提取工艺为:超声功率120 W、提取时间10 min、乙醇体积分数50%、液料比10∶1(mL∶g)、提取温度40℃;黑果腺肋花楸提取物的IC_(50)值(60.350μg·mL~(-1))与VC的相近,具有较强的抗氧化活性;黑果腺肋花楸提取物溶液(1 000～3.125μg·mL~(-1))无肝细胞毒性,且与模型组相比,提取物组葡萄糖消耗量显著提升,由5.59 mmol·L~(-1)·(24 h)~(-1)升至8.29 mmol·L~(-1)·(24 h)~(-1),具有较强的降糖活性。     

全蝎白术白头翁组合发酵品不同醇浓度提取物的活性成分分析及体外药理研究

评价全蝎白术白头翁组合发酵品(SAPZFP)不同醇浓度提取物的活性成分含量及体外抗肿瘤活性差异。分别测定SAPZFP不同醇浓度提取物的醇溶性总蛋白、总多糖、总黄酮的含量,并采用MTT法检测不同醇浓度提取物抑制肿瘤细胞体外增殖的能力。SAPZFP不同醇浓度提取物均具有体外抗肿瘤活性,其中75%醇提物抑制乳腺癌细胞株MCF-7、肺腺癌细胞株A549体外增殖的能力最强,IC50分别为0.066、0.022 mg·mL-1。综上所述,SAPZFP的25%、50%、75%醇提物均具有体外抗肿瘤活性,且75%醇提物效果最优。     

瓜馥木抗肿瘤活性研究

目的研究瓜馥木和黄酮化合物抗肿瘤活性。方法以半数抑制浓度(IC50)为评价抗肿瘤活性强度的指标,采用MTT法测定瓜馥木提取物和黄酮化合物体外抗肿瘤活性。结果 5,6,7,8-四甲氧基黄酮、石油醚、氯仿和乙酸乙酯的提取物均能显著抑制SPCA-1肺腺癌细胞、SGC-7901胃癌细胞、BEL-7402肝癌细胞和K562白血病细胞增殖;水提取物只对K562白血病细胞有抑制作用。结论瓜馥木具有抗肿瘤活性。     

虫草花总黄酮,总氨基酸含量测定及其抗氧化活性研究

目的对4个不同产地虫草花的总黄酮、总氨基酸的含量分别进行测定,并对4个不同产地的虫草花的提取物进行抗氧化活性研究。方法采用Al(NO)_3-NaNO_2-NaOH比色法测定总黄酮含量;采用茚三酮比色法测定总氨基酸的含量。结果 4个不同产地虫草花的总黄酮、总氨基酸含量存在一定差异;虫草花提取物对DPPH和超氧阴离子两种自由基清除能力较好,清除率与浓度呈量效关系。结论不同产地虫草花的总黄酮、总氨基酸含量存在差异,同时实验证明虫草花具有良好的抗氧化活性。     

黄蜀葵花提取物中总黄酮与总多酚含量测定及体外抑菌与抗氧化活性研究

采用比色法测定了不同产地黄蜀葵花提取物(Abelmoschi corolla extracts, ACE)中的总黄酮和总多酚含量,通过琼脂打孔法和微量稀释法研究了ACE的体外抑菌活性,并通过DPPH法、ABTS法和FRAP法评价了ACE的抗氧化活性。结果表明：不同产地ACE中总黄酮和总多酚含量差别不大,安徽ACE中的总黄酮含量最高,为(4.68±0.37)mg·g^-1,陕西ACE中的总多酚含量最高,为(1.48±0.11) mg·g^-1;ACE具有一定的体外抑菌活性,能显著抑制变异链球菌的生长,且呈浓度依赖性,最低抑菌浓度(MIC)和最低杀菌浓度(MBC)分别为3 mg·mL^-1和6 mg·mL^-1;ACE具有一定的抗氧化活性,能够清除DPPH、ABTS等自由基,且在一定浓度范围内呈量效关系。     

龙眼叶丙酮部位抗氧化活性研究

采用丙酮为溶剂,通过浸泡龙眼叶的方法得到龙眼叶丙酮提取物。以没食子酸为对照品测定该提取物的总酚含量,并采用ABTS体系评价眼叶丙酮提取物的抗氧化活性,探讨抗氧化活性和总酚含量之间的关系。龙眼叶丙酮提取物在较低药液浓度时即对ABTS自由基表现出一定的清除能力,且该清除能力与药液浓度呈正相关的关系。在最高药液浓度时,龙眼叶丙酮提取物对ABTS自由基的清除率达到74. 94%。此外,龙眼叶丙酮提取物具有良好的还原能力。     

槐花α-葡萄糖苷酶抑制活性研究

用体外α-葡萄糖苷酶抑制模型,对槐花乙酸乙酯、石油醚、正丁醇、丙酮水总提取物进行活性筛选,对提取物浓度与抑制活性关系进行了研究,并对强活性的3种浸膏进行了抑制动力学研究。槐花总提取物(IC50=50.56 mg.L-1)、乙酸乙酯部位(IC50=1.25 mg.L-1)、正丁醇部位(IC50=16.14 mg.L-1)。活性远高于对照Acarbose(IC50=1 081.27 mg.L-1);并全部属于非竞争性抑制类型(Ki值分别为4.53、652.5 mg.L-1和62.38mg.L-1);从乙酸乙酯部位得到活性成分槲皮素(IC50=8.86 mg.L-1)和山奈酚(IC50=73.69 mg.L-1)。结果表明,槐花乙酸乙酯部位可作为降血糖活性部位进行体内研究。该文报道的新颖性已为河南大学图书馆2009年6月24日出具的第CX200906242号《科技查新报告》所证实。     

树上虾乙酸乙酯部位抗氧化活性研究

测定树上虾乙酸乙酯提取物的总酚含量,并测定其抗氧化能力,研究其抗氧化活性和总酚含量之间的关系。采用乙酸乙酯为提取溶剂得到树上虾提取物,并采用ABTS体系和还原能力体系研究其抗氧化效果。结果表明,树上虾乙酸乙酯提取物的总酚含量为43. 9 mg/g,其对ABTS自由基的最高清除率为96. 2%。树上虾乙酸乙酯提取物具有较高的总酚含量,其优异的抗氧化性能可能与其所含酚类物质有关。     

Prenylated Flavonoids with Potential Antimicrobial Activity: Synthesis,Biological Activity,and In Silico Study

Prenylated flavonoids are an important class of naturally occurring flavonoids with important biological activity, but their low abundance in nature limits their application in medicines. Here, we showed the hemisynthesis and the determination of various biological activities of seven prenylated flavonoids, named 7–13, with an emphasis on antimicrobial ones. Compounds 9, 11, and 12 showed inhibitory activity against human pathogenic fungi. Compounds 11, 12 (flavanones) and 13 (isoflavone) were the most active against clinical isolated Staphylococcus aureus MRSA, showing that structural requirements as prenylation at position C-6 or C-8 and OH at positions C-5, 7, and 4′ are key to the antibacterial activity. The combination of 11 or 12 with commercial antibiotics synergistically enhanced the antibacterial activity of vancomycin, ciprofloxacin, and methicillin in a factor of 10 to 100 times against drug-resistant bacteria. Compound 11 combined with ciprofloxacin was able to decrease the levels of ROS generated by ciprofloxacin. According to docking results of S enantiomer of 11 with ATP-binding cassette transporter showed the most favorable binding energy; however, more studies are needed to support this result.     

超声波对木瓜蛋白酶的活性及动力学和热力学参数的影响

高活性的木瓜蛋白酶有助于降低其在食品和医药工业中的应用成本。研究了超声波对木瓜蛋白酶活性的影响,并从动力学和热力学参数的变化分析了酶活性变化机理。结果表明,超声波对木瓜蛋白酶活性的影响较显著,在超声波功率40 W处理5 min时,木瓜蛋白酶活性提高最大,比对照组提高了9.0%,随着处理时间的延长,木瓜蛋白酶活性开始下降,9 min时酶活性比对照组降低了14.5%。当超声处理温度从20℃增加到40℃时,木瓜蛋白酶的反应速率常数从0.0628增加到0.0753。而热力学参数Ea、.H、.S和.G经过超声波处理后分别降低了14.9%、16.2%、7.3%和0.1%。由动力学和热力学参数的变化可见,木瓜蛋白酶经过一定功率的超声处理一定时间后,其催化的反应更容易进行。     

蒈烷-3, 4-二醇的除草活性

采用平皿培养法考察蒈烷-3, 4-二醇在水溶液中对一年生黑麦草和油菜根、茎伸长的抑制作用, 探讨其作为水基除草剂的应用潜力。结果表明: 蒈烷-3, 4-二醇微溶于水, 可在少量亲水性有机溶剂和表面活性剂作用下配制成浓度大于20mmol/L水乳液, 能够抑制黑麦草和油菜根、茎的伸长, 表现与浓度相关的除草活性, 对黑麦草的根、茎伸长的半数抑制浓度(IC₅₀)分别达到1.12和1.73mmol/L, 而对油菜根、茎伸长的IC₅₀分别达到1.23和2.12mmol/L。其除草活性明显高于天然单萜二醇对孟烷-3, 8-二醇, 而稍低于商业除草剂草甘膦, 有望进一步研究开发作为水基植物源除草剂。     

Synthesis,Characterization, and Biological Activity Evaluation of Magnetite-Functionalized Eugenol

This work reports the magnetite-functionalization and biological evaluation of eugenol by the co-precipitation method employed only Fe²⁺ under mild conditions and control from the amount of the incorporated magnetite. Magnetic nanoparticles were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), Fourier transform infrared (FTIR), hydrodynamic size distribution (Zetasizer), and vibrating sample magnetometer (VSM). SEM images showed that EUG·Fe₃O₄ similar in shape to a nanoflower. The FTIR spectrum confirmed the presence of characteristic EUG and Fe₃O₄ bands in the EUG·Fe₃O₄ sample, the XRD analysis showed that the magnetite functionalization with eugenol slightly affected the Fe₃O₄ crystal structure, while the VSM measurements demonstrate that EUG·Fe₃O₄ 1:1 shows a superparamagnetic behavior, suggesting small non-interacting particles. The in vitro safety profile and cytotoxicity of free eugenol, magnetite pristine, EUG·Fe₃O₄ 1:1, EUG·Fe₃O₄ 1:5, and EUG·Fe₃O₄ 1:10 was investigated using human cell lines (keratinocytes and melanoma). The results demonstrate the high biocompatibility of EUG·Fe₃O₄ in HaCat cells and the greater specificity for the A375 cell line. Furthermore, the magnetite-functionalization with eugenol decreased the toxic effects of free eugenol on healthy cells. Antibacterial tests were performed in different bacterial strains. The experimental data showed that among the magnetic compounds, the microorganisms were only sensitive to treatment with EUG·Fe₃O₄ 1:1. Regarding the antibiofilm activity assay, it can be observed that only the EUG·Fe₃O₄ caused a significant decrease in biomass when compared to the positive control. Finally, it can be concluded that EUG·Fe₃O₄ proves to be a potential candidate for future studies for drug delivery of cancer and bacterial infections treatments.

Graphical Abstract

     

纤维结合蛋白的提纯、定量、活性检测及抗体制备

采用重复两次亲和层析法从血浆中提取纤维结合蛋白(简称FN)可达到电泳纯;免疫家兔,抗FN血清平均效价可达16~x;经吸收得单特异抗血清;再经(NH_4)_1SO_4沉淀、DE-AE-HW离子交换可制出高纯度抗FN IgG;建立了两种FN的定量测定方法:1.火箭电泳法,检查了89份健康人血浆,平均含量为293±45μg/ml;2.免疫浊度法,检测了20份血浆,平均值为344±52μg/ml。最后建立了促进BHK细胞伸展活性的检测法,敏感度可达5μg/ml,并初步应用于稳定性和热变性试验,为开展FN的应用提供了质控指标。对比了我们精制的FN与SIGMA试剂公司的FN,二者成分相同,活性也很相似。     

Design,Synthesis, and Immunosuppressive Activity of New Deoxybenzoin Derivatives

In the search for potential immunosuppressive agents with high efficacy and low toxicity, a series of new deoxybenzoins were synthesized and evaluated for their cytotoxicity and immunosuppressive activity. Among the synthesized compounds, four deoxybenzoin oximes (compounds 31 , 32 , 37 , and 38 ) exhibited lower cytotoxicity and higher inhibitory activity toward anti‐CD3/anti‐CD28 co‐stimulated T‐cell proliferation than other compounds. More significantly, compound 31 is >100‐fold less cytotoxic than cyclosporine A (CsA) and is also more potent ( 31 : SI>684.64, CsA: SI=235.44). The preliminary inhibition mechanism of compound 31 was also identified by flow cytometry, and this compound exerts immunosuppressive activity by inducing apoptosis in activated lymph node cells in a dose‐dependent manner. In addition, the mechanism of apoptosis was detected by western blot analysis.     

Sulfated and Oxygenated Imidazoline Derivatives: Synthesis,Antioxidant Activity and Light-Mediated Antibacterial Activity

Imidazoline derivatives with different exocyclic substituents were simply prepared from common starting materials. The procedures were carried out in an eco-friendly manner. The antioxidant activity of these derivatives was explored by different experimental assays, such as ABTS^.+ and DPPH^. scavenging assay, as well as reducing power assay. The structural differences are discussed in terms of the results. Sulfur analogs showed higher antioxidant activity than their oxygenated counterparts. The same tendency was observed in microbiological studies, in which the same imidazoline compounds were assayed for light-mediated activity against of Staphylococcus aureus and Escherichia coli strains. A light-enhanced activity was observed for almost all the sulfated imidazolines after exposure to UV-A (400-320 nm) light.     

Nanocobaltite: Preparation,Characterization, and their Catalytic Activity

Mixed transition metal oxides (MTMO) nanoparticles of 3rd‐series (NiCo₂O₄, CuCo₂O₄, and ZnCo₂O₄) were prepared by a co‐precipitation method. These were characterized by X‐ray diffraction (XRD) and transmission electron microscopy (TEM). The particle size was found to be in the order of 53.0, 43.4, and 21.2 nm, respectively. The thermolysis of ammonium perchlorate (AP), AP‐HTPB (hydroxyterminated polybutadiene) composite solid propellants (CSPs), and HTPB was found to be catalyzed with MTMOs and the burning rate of CSPs was also enhanced. TG and ignition delay study demonstrated that the higher temperature decomposition (HTD) of AP is catalyzed enormously by these catalysts and CuCo₂O₄ is the best candidate.     

Novel Heterobimetallic Radiotheranostic: Preparation,Activity, and Biodistribution

A novel Ru^II(arene) theranostic complex is presented. It is based on a 1,4,7,10‐tetraazacyclododecane‐1,4,7,10‐tetraacetic acid macrocycle bearing a triarylphosphine and can be tracked in vivo by using the γ emission of ¹⁵³Sm atoms. Notably, the heteroditopic ligand can be selectively metalated with ruthenium at the phosphorus atom despite the presence of other functionalities that are prone to metal coordination. Subsequent labeling with radionuclides such as ¹⁵³Sm can then be performed easily. The resulting heterobimetallic complex exhibits favorable solubility and stability properties in biologically relevant media. It also shows in vitro cytotoxicity in line with that expected for this type of metallodrug, and is nontoxic to the organism as a whole. As a proof of concept, initial studies in healthy mice were performed to obtain information about the uptake, biodistribution, and excretion of the radiolabeled complex.     

Synthesis,Thermal Properties and Antibacterial Activity of Polyketones

Abstract

Polyketones were prepared by the Friedel-Craft reaction from 1,3-dimethoxy benzene, chloroacetic acid and dichloroalkanes, i.e., dichloromethane and 1,2-dicholoroethane. The polyketones were characterized by IR spectra and vapour pressure osmometry. The thermal properties were studied by the thermogravimetry and differential scanning calorimetry. The kinetic parameters for the thermal decomposition reaction were evaluated by the methods of Broido and Doyle. The synthesized polylaketones shows antimicrobial properties against bacteria, fungi and yeast.