丹皮酚曼尼希碱衍生物的合成及抗血小板聚集活性

以丹皮酚和不同的有机胺为原料,利用曼尼希反应合成系列丹皮酚曼尼希碱衍生物,合成得到5个丹皮酚曼希尼碱衍生物.目标化合物的结构经过核磁共振氢谱(¹H NMR)和质谱(HR-MS)确证.采用Born比浊法,对5个目标化合物进行了以ADP为诱导剂的体外抗血小板聚集的活性试验;结果表明,目标化合物2a～2e(AIR:46.35%～85.39%)的活性均强于阳性对照药阿司匹林(AIR:35.08%),其中化合物2d(AIR:35.08%)的抗血小板聚集活性最强,具有进一步的研究价值.     

基于系统药理学探讨抗病毒口服液治疗COVID-19分子机制

目的:基于网络药理学与分子对接技术探索抗病毒口服液在治疗新型冠状病毒肺炎(COVID-19)的作用机制.方法:使用TCMSP数据库对抗病毒口服液的中药活性成分进行检索并根据条件筛选.使用OM IM和Gene Cards数据库对疾病靶点进行筛选,构建活性成分-靶点网络图.将筛选得到的靶点用String数据库得到蛋白互作网络图.运用GO和KEGG富集分析,得到靶点-信号通路网络图.结果:共筛选得到中药活性成分靶点226个,疾病靶点256个,关联靶点21个,富集于22个生物过程及80条信号通路.根据中药-化合物-靶点网络图分析,得到排名前5的活性成分分别为槲皮素、β-谷甾醇、山奈酚、木犀草素和汉黄芩素.分子对接结果显示抗病毒口服液的核心化合物与疾病靶点SARS-CoV-23CL水解酶和血管紧张素转化酶Ⅱ(ACE2)能较好的结合.结论:抗病毒口服液中的主要活性成分通过与SARS-CoV-23CL和ACE2结合,作用于IL-6、PPARG、VEGFA等靶点,影响免疫调节、抗病毒、抗炎等途径发挥对C O V ID-19的治疗作用.     

一种噻二唑类杂环化合物抗K562肿瘤活性研究

研究噻二唑类杂环化合物对人白血病K562癌细胞的体外抗肿瘤活性筛选。方法:利用MTT法间接测定各化合物对肿瘤细胞后的生长情况,并计算出肿瘤细胞的抑制率,选择抑制率较高的化合物进行深入研究,计算其半数抑制浓度(IC50),并考察其浓度-生长率线性关系。结果:大部分化合物均显示了较好的人白血病K562癌细胞抑制活性,化合物1抑制率达92.01%,IC50为7.07×10-5mol/L,浓度-生长率R2=0.986。结论:噻二唑类杂环化合物具有较好的抗肿瘤活性。     

构树的化学特性和药理作用研究进展

综述了国内外对构树(Broussonetia papyrifera)化学成分和药理作用的研究进展,现代研究表明:从构树中分离得到的化合物对超氧化物歧化酶显示出较高的抑制活性,能够抑制酪氨酸酶的活性,具有强烈抑制类脂氧化作用,桦木醇和桦木酸对抗疼痛和抗炎效果较好,对凝血酶引起的血小板凝聚亦有强烈的抑制作用,具有很强的抗真菌作用,可显著抑制ⅡA和v型sPLA2s的活性,且对HepG2细胞有较高的细胞毒作用,还有些化合物对α-葡萄糖苷酶的抑制活性检测结果具有较好的α-葡萄糖苷酶抑制活性.该属植物中已发现的各类化学成分及其药理作用可为开发新药提供依据.     

增材制造制备Zn–Nd合金的成形质量、力学性能及抗炎活性（英文）

目的:锌具有良好的降解性能和生物相容性,被视为一种很有前途的骨修复材料。然而,锌金属作为骨植入物时的力学强度难以满足承重骨修复的需求,并存在炎症反应的风险。本文旨在探讨稀土钕合金化对锌骨植入物激光成形质量的影响,为改善锌合金的成形质量、提高力学性能及增加抗炎活性提供理论依据。创新点:1.在增材制造过程中,添加钕能够有效改善锌基合金的成形质量;2.稀土钕提高了锌基合金的力学性能,同时也赋予了抗炎活性。方法:1.通过实验对比锌钕合金的表面形貌,计算出相应的致密度,并分析钕对锌基合金成形质量的影响(图2);2.基于不同实验对比锌钕合金的微观组织结构及力学强度的变化,并探讨稀土钕提高力学性能的原因(图3～5和表1);3.通过电化学实验和浸泡实验,分析稀土钕对降解性能的影响(图6和7);4.基于体外生物学实验,对比分析钕对抗炎活性和细胞活性的影响(图8和9)。结论:1.稀土钕提高了激光增材制造锌合金的成形质量,并使其致密化率高达98.71%;2.钕合金化有助于晶粒细化和第二相强化,使极限抗拉强度提高到了(119.3±5.1) MPa;3.钕合金化能抑制促炎因子的释放,促进抗炎因子的释放,进而使锌钕部分具有良好的抗炎活性,而细胞培养试验也表明其具有良好的生物相容性。     

花生肽体外抗氧化活性的研究

花生肽是花生蛋白质经过控制性的水解、精制以后得到的一类活性肽。本文对通过Alcalase碱性蛋白、Protamex复合蛋白酶和Neutrase中性蛋白酶水解花生分离蛋白制备的花生肽的体外抗氧化活性进行研究。采用亚油酸-硫氰酸钾方法、脱氧核糖方法和邻苯三酚方法测定花生肽的抗亚油酸过氧化能力、清除羟自由基能力和清除超氧阴离子的能力,从而对花生肽的体外抗氧化活性进行评价。结果表明用Alcalase碱性蛋白酶水解得到得花生肽抗氧化活性最强。     

NDV感染体外诱导胃癌细胞BGC-823的凋亡

目的 :研究新城疫病毒在体外抗胃癌细胞活性及其与细胞凋亡的关系。方法 :应用倒置显微镜观察细胞形态、MTT法测NDV在体外对BGC - 82 3的抑制和杀伤作用 ,同时用流式细胞术检测胃癌细胞凋亡情况及细胞分裂周期各时象的变化。结果 :NDV在体外可使BGC - 82 3胃癌细胞形成明显的细胞病变效应、细胞生长抑制及细胞凋亡 ,且细胞凋亡率与感染时间呈正相关。G2、S期细胞减少 ,增殖指数 (PI)降低 ,与阴性对照组比较有显著性差异 (P<0 .0 1)。结论 :NDV具有显著的抗BGC - 82 3胃癌细胞活性。     

花椒挥发油作为天然经皮促透剂的细胞毒性及促透活性(英文)

研究目的:研究花椒挥发油作为天然经皮促透剂的促透活性及其促透机制,同时评价其皮肤细胞毒性。创新要点:首次评价了花椒挥发油的皮肤细胞毒性、经皮促透活性及其作用机制。研究方法:利用表皮角质形成细胞(HaCaT)和真皮成纤维细胞(CCC-ESF-1)评价花椒挥发油的细胞毒性;采用亲水性及亲脂性模型药测定挥发油促透活性的基础上研究其促透作用机制。重要结论:花椒挥发油具有良好促透活性并具有较低皮肤细胞毒性。     

电化学法测定西维因水解速率参数

使用现代电化学分析方法,通过监测水解产物的生成情况,研究了本身无电化学活性的西维因(甲萘威)在水中的水解情况,在pH=7.0的BR缓冲液环境中西维因水解产物检测的灵敏度最高.考察了环境酸度以及环境温度对水解的影响,并测定了不同条件下的水解速率常数.发现西维因的水解过程符合一级反应方程,其水解受pH值、温度的影响.在酸性介质中西维因仍有一定的水解,但是水解的速率明显低于碱性介质中的水解速率.同时,环境温度也会影响水解速率,在较高温度下,不论环境酸度值为碱性或者酸性,西维因的水解速率均有所升高.     

溴氰菊酯对大鼠小脑皮质组织中HO和ATPase活性的影响

目的:研究溴氰菊酯(DM)对SD大鼠小脑皮质组织中血红素加氧酶(HO)的活性和ATPase活性的影响。方法:(1)成年雄性SD大鼠共40只,其中20只用于血红素加氧酶(HO)的活性的测定,另20只用于ATPase活力测定,均随机分为对照组和DM染毒实验组,实验组中大鼠72小时内给溴氰菊酯(1/20LD50)三次,对照组为相同剂量的玉米油,分别检测小脑皮质组织HO活性和ATPase活性。(2)成年雄性SD大鼠30只,同样方法取出小脑皮质,制成切片,随机分为对照组(相同剂量的玉米油)和5个不同浓度的DM染毒试验组(2×10-7mmol/L、2×10-6mmol/L、2×10-5mmol/L、2×10-4mmol/L、2×10-3mmol/L),测定ATPase活性。结果:整体染毒小脑皮层组织HO活性为对照组的240.39%(p﹤0.05),Na+,K+-ATPase活性为对照组的131.47%(p﹤0.05),Ca2+-ATPase活性增加没有统计学意义,Mg2+-ATPase有显著的抑制作用(P<0.05),为对照组的79.91%。体外试验发现只有达到10-3mmol/L数量级的DM对温育小脑皮质切片组织中的Mg2+-ATPase活性才有显著的抑制作用(P<0.05);且无论何种浓度均未发现上述体内染毒时对Na+,K+-ATPase活性的增加作用。结论:DM可增加大鼠小脑皮质的HO活性,体内体外染毒DM对三种ATPase活性的影响并不一致。     

卡思卡特城堡

It is worthy of noting that, whilst Crookston Castle witnessed the earlier and happier portion of Mary's variegated life,     

不同的吃喝玩乐

一、吃和喝吃苹果 eat an apple, 吃药 take medicine,吃糖 have some sweets,吃饭 have one's meals,吃馆子 dine out,吃惊 be surprised/     

漏洞百出的教育

Many college freshmen arrive woefully unprepared to do college work, and as disadvantaged populations continue to grow, the share of the American work force that has made it through college is expected to plummet. Many experts blame that educational failure not just on high schools but also on colleges. School & College, a special report by The Chronicle, looks at efforts to fix the system. What reforms would better prepare students for college? What should schools and colleges be doing differently? How should state and federal officials help?     

Western and Eastern culture differences in commercial field

The communication of people partially is the communication of cultures. Culture has a direct effect on international commercial activities in all aspects. Different conceptions about time, space, equality, law and the like, lead people to deal with things in different ways. So to know cultures of the counterpart is to facil-itate our enterprises so as to have a smooth and successful communication in commercial activity.     

只要努力,不要后悔

There are numbers of crossroads on our long and unpredictable life journey where we totally have no idea about which direction to choose. No matter what our decision is, we should not turn back, but face the music and go ahead instead. I am this kind of girl who always does try without regretting, one example is how I dealt with my love.     

浅谈移民问题

Migration occurs behind a variety of reasons and has a great effect on the whole world. People may migrate in order to improve their economic situation, or in order to escape civil strife, persecution, and environmental disasters. The impact of migration is complex, bringing both benefits anddisadvantages. This paper briefly talks about the causes of migration, the allocation of benefits, and the ways in which individual countries and the international community deal with this important subject.     

Sister Carrie, an Adherent of Desires

Sister Carrie is one of the most controversial characters in American literature.Thought as a "fallen woman" firstly,she was defined as a "new woman" by some critics later. However, by digging into the motivaton behind the whole process of Carrie's "success", the relationship between Carrie and her creator (the author), the social conditions of then American, it can be found that Carrie has never been free-standing on her thought and she has never found her real-sdf even after becoming a famous actress. In a society dominated by mass consumerism Carrie is only an adherent of her own desires. She also is a representative of all those country girls flooded into cities, a symbol and a sacrifice of the urbanization of America in a time countryside was overcome by cities.     

Improvement of one-cycle controller by use of proportional integral differential controller

1.IntroductionOne-cyclecontrolmethod,whichwasproposedaboutonedecadeago[1],hasbecomeanattractivemethodinspecialfieldssuchaspowerfactorcorrection[2-6],switchingamplifiers[7,8],etc.Themainideaofthiscontrollerisbasedonintegrationofdiodevoltageinone-cycleandforcesittobeexactlyequaltothereferencevalue.Themainadvantageofthiscontrollerisitsrealtimeabilitytorejectthevariationofinputvoltage[1].Despitethisgreatability,ithasnogoodperformancesinrejectingofloaddisturbanceandfollowingreferencecommands.Espec…     

风的曲线

Rosco and I wait for the fishermen to return.I sit at a wooden bench near the store at Mt.Baker Resort and watch the clouds change shape. Rosco has my belt around his neck and an eight foot tow chain hooked to a tree. Dogs must be on a leash. Ducks and rabbits are loose.