Synthesis and in vitro-Anti-hepatitis B Virus Activities of Several Ethyl 5-Hydroxy-1H-indole-3-carboxylates

A series of ethyl 5-hydroxyindole-3-earboxylates 6a-10r was designed and synthesized. The structures of all the compounds were confirmed by IR, ^1H NMR, and MS and their anti-hepatitis B virus （HBV） activities were evaluated in 2.2.15 cells. Among them, compound 7g { ethyl 5-hydroxy-2- [ （ 3-methoxyphenylsulfinyl ） methyl ] -1-methyl-4- [ （4-methylpiperazin-1-yl） methyl ]-1H-indole-3-carboxylate} displays a significant anti-HBV activity, which is more potent than the positive control lamivudine.

Effects of a rumen protected B vitamin blend substituted for biotin upon milk production and component yield in lactating dairy cows

Results from 4 switchback field trials involving 608 cows were combined to assess the effects of a protected B vitamin blend (BVB) vs 10 mg of unprotected biotin upon milk yield (kg), fat %, protein %, fat yield (kg) and protein yield (kg) in primiparous and multiparous cows. Trials consisted of 3 DHIA periods executed in the order control-test-control. Cows from 45 to 300 days in milk (DIM) at the start of the experiment that were available for all 3 periods were included in the analysis. No diet changes other than the substitution of 3 grams/cow/day of the BVB for 10 mg of biotin during the test period occurred. Results from the two control periods were compared to results obtained during the test period by individual cow using a paired T test. Results for all cows showed that the provision of the BVB resulted in increased (P < 0.05) milk, fat percentage (%), protein %, fat yield and protein yield. Analysis by age revealed that milk production and milk protein yield were only improved in mature cows. Milk production had a negative effect upon the magnitude of the increase in milk components. The change in milk yield was greatest in early lactation and declined with DIM. Protein % and fat % increased with DIM in mature cows, but not in first lactation cows. Differences in fat yields between test and control feeding periods did not change with DIM, but the improvement in protein yield in mature cows declined with DIM. These results indicate that the BVB provided economically important advantages throughout lactation beyond those witnessed with biotin, but expected results would vary with cow age and stage of lactation.

Effect of malaria components on blood mononuclear cells involved in immune response

During malaria infection,elevated levels of pro-inflammatory mediators and nitric;oxide production have been associated with pathogenesis and disease severity.Previous in vitro and in vivo studies have proposed that both Plasmodium falciparum hemozoin and glycosylphosphatidylinositols are able to modulate blood mononuclear cells,contributing to stimulation of signal transduction and downstream regulation of the NF-KB signaling pathway,and subsequently leading to the production of pro-inflammatory cytokines,chemokines,and nitric oxide.The present review summarizes the published in vitro and in vivo studies that have investigated the mechanism of intracellular signal transduction and activation of the NF-KB signaling pathway in blood mononuclear cells after being inducted by Plasmodium falciparum malaria components.Particular attention is paid to hemozoin and glycosylphosphatidylinositols which reflect the important mechanism of signaling pathways involved in immune response.

A METHOD OF LEUKOCYTE SEGMENTATION BASED ON S COMPONENT AND B COMPONENT IMAGES

A leukocyte segmentation method based on S component and B component images is proposed.Threshold segmentation operation is applied to get two binary images in S component and B component images.The samples used in this study are peripheral blood smears.It is easy tofind from the two binary images that gray values are the same at every corresponding pixels in theleukocyte cytoplasm region,but opposite in the other regions.The feature shows that "IMAGEAND"operation can be employed on the two binary images to segment the cytoplasm region ofleukocyte.By doing"IMAGE XOR"operation between cytoplasn region and nucleus region,theleukocyte segment ation can be retrieved effectively.The segmentation accuracy is evaluated by comparing the segmentation result of the proposed method with the manual segmentation by ahematologist.Experiment results show that the proposed method is of a higher segmentationaccuracy and it also performs well when leukocytes overlap_with erythrocytes.The averagesegmentation accuracy of the proposed method reaches 97.7%for segmenting five types ofleukocyte.Good segmentation results provide an important foundation for leukocytes aut omaticrecognition.

A novel synthesis of pyrazolo[3,4-b]pyridine derivatives through multi-component reaction in ionic liquid

An efficient and novel procedure for the preparation of pyrazolo[3,4-b]pyridine derivatives through multi-component reaction of aldehyde, 5-amino-3-methyl-1-phenylpyrazole and malononitrile or cyanoacetate in [bmim][BF4] is described in this paper. Advantages of the method presented here include mild conditions, high yields together with a green nature and ease of recovery and reuse of the reaction medium.

Effects of UV-B radiation intensity and timing on epidemiological components of wheat stripe rust

Stripe rust caused by Puccinia striiformis f. sp. tritici is an important wheat disease worldwide that is greatly influenced by environmental conditions. Ultraviolet B(UV-B) radiation is one important environmental factor affecting the occurrence and epidemiology of wheat stripe rust. Investigating UV-B radiation effects on the epidemiology of stripe rust may be conducive to monitoring and predicting this disease. In this study, wheat seedlings were exposed to UV-B radiation during different periods under laboratory conditions and radiation effects on epidemiological components of wheat stripe rust were investigated. Results showed that incubation period was shortened, and the infection efficiency, sporulation quantity and disease index increased when UV-B radiation was performed only pre-inoculation. When the UV-B radiation was performed only postinoculation or both pre-and post-inoculation, the incubation period was prolonged, and the infection efficiency, sporulation quantity and disease index were reduced. When healthy wheat seedlings were inoculated using urediospores collected from wheat leaves irradiated by UV-B only post-inoculation or both pre-and post-inoculation, infection efficiency, sporulation quantity and disease index were also reduced. However, in the latter, the disease incubation period did not differ under varying UV-B radiation intensities compared to that when wheat leaves were not treated with UV-B radiation. Overall, the effects of direct exposure of wheat plants to UV-B radiation with different intensities in different periods on epidemiological components of wheat stripe rust were systematically explored, and the results suggest that the effects of UV-B radiation increased gradually with the increase of UV-B radiation intensity. This information provides a basis for monitoring and predicting this disease as well as for conducting further studies on pathogen virulence variation.

Is there a need for universal double reflex testing of HBsAg-positive individuals for hepatitis D infection?

Hepatitis D virus(HDV)can infect HBsAg-positive individuals,causing rapid fibrosis progression,early decompensation,increased hepatocellular carcinoma risk,and higher mortality than hepatitis B virus(HBV)mono-infection.Most countries lack high-quality HDV prevalence data,and the collection techniques employed often bias published data.In recent meta-analyses,HDV prevalence in HBsAg-positive patients reaches 5%-15%and is even significantly higher in endemic areas.Since HBV vaccination programs were implemented,HDV prevalence has decreased among younger populations.However,owing to immigrant influx,it has increased in some Western countries.The current practice of HDV screening in HBsAg-positive individuals is stepwise,based on physician’s discretion,and limited to at-risk populations and may require numerous visits.Double reflex testing,which includes anti-HDV testing in all HBsAg-positive individuals and then HDV RNA testing for anti-HDV-positive ones,is uncommon.Reflex testing can identify more HDV infection cases and link identified patients to further care and follow-up.Moreover,laboratory-based double reflex screening is less biased than physician-led testing.Therefore,health-care providers should learn about reflex testing,and federal and provincial hepatitis control programs should implement laboratory-based double reflex testing to obtain reliable HDV prevalence estimates.The test’s cost-effectiveness depends on the number of HBV-positive patients screened to identify one HDV-positive patient.Such testing may be viable in areas with low HBsAg but high HDV prevalence.However,its economic impact on areas with low HDV prevalence needs further study.

Synthesis and in vitro Anti-hepatitis B Virus Activity of Some Ethyl 5-Hydroxy-4-substituted Aminomethyl-2-sulfinylmethyl-1H-indole-3-carboxylates

A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-lH-indole-3-carboxylates 8a--8j and 11e--11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus（HBV） activity and cytotoxicity. Among them, six compounds showed more potent inhibitory activity than lamivudine. Compound 8e exhibited the most significant anti-HBV activity with an IC50 value of 1.62 μmol/L, which was 33-times more potent than the reference drug lamivudine（IC50=54.78μmol/L）.

INVARIANT SUBSPACES AND GENERALIZED FUNCTIONAL SEPARABLE SOLUTIONS TO THE TWO-COMPONENT b-FAMILY SYSTEM

Invariant subspace method is exploited to obtain exact solutions of the two- component b-family system. It is shown that the two-component b-family system admits the generalized functional separable solutions. Furthermore, blow up and behavior of those exact solutions are also investigated.

UI组件库在B端界面设计中的应用

随着互联网的快速发展,企业对于业务效率和管理需求的不断提高,企业级系统的复杂性和规模不断增加,传统的开发方式已经无法满足快速迭代和定制化需求的要求。B端(Business-to-Business)产品的发展对各行各业的发展越来越关键。为了提高开发效率、降低维护成本、增强系统的灵活性,人们开始探索更加灵活和可复用的开发方式,于是UI组件化设计应运而生。一个好的UI组件库可以有助于改善用户体验,提高用户满意度。

核酸外切体成分4在初治弥漫大B细胞淋巴瘤患者中的表达及临床意义

目的:探讨初治弥漫大B细胞淋巴瘤(DLBCL)患者组织中核酸外切体成分4(EXOSC4)的表达情况及其临床意义。方法:采用免疫组织化学染色方法检测181例初治DLBCL患者组织中EXOSC4蛋白的表达情况;收集临床资料,并分析初治DLBCL患者组织中EXOSC4蛋白表达与临床特征的相关性及其预后意义。结果:181例初治DLBCL患者组织中,EXOSC4蛋白表达阳性率为68.51%;将患者分为高表达组44例和低表达组137例,两组患者年龄、性别、B症状、血清乳酸脱氢酶(LDH)水平、美国东部肿瘤协作组(ECOG)评分、Ann Arbor分期、结外侵犯、国际预后指数(IPI)评分、国家综合癌症网络IPI(NCCN-IPI)评分、细胞起源等特征的差异均无统计学意义(P>0.05)。Cox多因素回归分析结果显示,组织EXOSC4蛋白高表达是初治DLBCL患者OS和PFS的独立不良预后因素(均P<0.05)。K-M生存分析结果显示,组织中EXOSC4蛋白高表达初治DLBCL患者总生存期和无进展生存期较低表达患者显著缩短(均P<0.05)。结论:初治DLBCL患者组织EXOSC4蛋白高表达是影响生存的独立不良预后因素。

C1QB在恶性肿瘤中的临床研究进展

补体C1QB作为经典途径的重要组成部分,能有效清除死亡细胞及免疫复合物,维持体内环境平衡,一直被认为是抑制肿瘤的因素之一。近年发现,C1QB等补体系统及其激活产物不仅是诱导炎症的主要驱动力,参与补体的活化,亦可能通过非经典补体途径(如血管生成、细胞黏附),改变肿瘤微环境,参与肿瘤细胞的侵袭和迁移。因此,深入探讨C1QB等补体在不同肿瘤中免疫学及肿瘤生物学中的功能及作用,可为临床恶性肿瘤的诊断、治疗及预后的新靶点提供依据。

Hepatitis D virus dual-infection among Chinese hepatitis B patient related to hepatitis B surface antigen,hepatitis B virus DNA and age

The screening practices for hepatitis D virus(HDV)are diverse and nonstandardized worldwide,and the exact prevalence of HDV is uncertain.AIM To estimate HDV prevalence and investigate viral marker quantity trends in patients with hepatitis D.METHODS We collected 5594 serum samples from patients with hepatitis B in Jilin Province,China(3293 males and 2301 females,age range of 2 to 89 years).We then conducted tests for hepatitis B surface antigen(HBsAg),hepatitis B Virus(HBV)DNA,anti-hepatitis D antigen(HDAg),and HDV RNA.RESULTS We found that the prevalence of anti-HDAg and HDV RNA among hepatitis B patient were 3.6%(3.2-4.2%)and 1.2%(0.9-1.5%),respectively,87.69%of hepatitis D patients were 51-70 years old.HDV infection screening positive rate of patients with HBV DNA levels below 2000 IU/mL(2.0%)was higher than those above 2000 IU/mL(0.2%).Among anti-HDAg positive patients,the HDV RNA positive rate was positively correlated with the HBsAg level and anti-HDAg level.There was a weak correlation between HBsAg and anti-HDAg levels among hepatitis D patients.CONCLUSION Our study highlights the importance of considering multiple factors when assessing the severity of HDV infection,comprehensive evaluation of patients’clinical and laboratory parameters is necessary for proper diagnosis and treatment.

多组元Fe-W-B合金本构方程及热加工图的研究

为解决铸造高硼合金难热加工以及硼化物呈网状分布的问题,本文以多组元Fe-W-B合金为例,采用Gleeble-3500热模拟实验机研究了其在变形温度800℃~1150℃、应变速率0.01s-1~10s-1条件下的高温流变行为。结果表明,多组元Fe-W-B合金的高温流变应力状态主要受温度和应变速率影响,具体表现为流变应力随着应变速率降低和变形温度升高而减小,真应力一应变曲线表现出动态回复型和动态再结晶型特征。本文还构建了Arrhenius型热变形本构方程并对其准确性进行了验证;根据热加工图确定了多组元Fe-W-B合金最佳热加工窗口并进行锻造验证。锻后,多组元Fe-W-B合金中的网状硼化物被有效破碎并且力学性能大幅提升。

基于转录组数据分析的六味地黄方活性组分LWD-b抗补体作用的发现与验证

目的 基于转录组数据分析发现与验证六味地黄方活性组分的抗补体作用,并研究其可能的作用途径。方法 人恶性黑素瘤细胞A375用DMEM/F12高糖培养基培养,分为细胞对照、六味地黄苷糖LW-AFC、寡糖组分CA-30、多糖组分LWB-B和糖苷组分LWD-b组(终浓度均为100 mg·L^(-1)),培养6 h后用L1000技术采集细胞转录组数据,采用Cosine相似度算法和特征方向法对各组转录组数据进行相似性比对和差异表达分析,采用基因富集分析算法进行KEGG通路富集分析。采用实时荧光定量PCR(RT-qPCR)测定补体通路基因C3和C5 m RNA表达。采用基于补体经典途径的溶血活性实验测定相对溶血率,观察LWAFC,CA-30,LWB-B和LWD-b(终浓度均为1,10和100 mg·L^(-1))及LWD-b中各主要成分莫诺苷、芍药苷、獐牙菜苷、马钱苷、马钱苷酸和丹皮酚原苷(终浓度均为1和100μmol·L^(-1))的抗补体活性。采用补体成分(C1q,C2,C3,C4,C5和C9)缺失血清法测定LWD-b的补体作用靶点。结果 转录组数据分析结果显示,LWD-b下调的基因显著富集于补体级联激活通路(P<0.01),而LW-AFC,CA-30和LWB-B此作用不明显。RT-qPCR结果表明,与细胞对照组相比,LWD-b 100 mg·L^(-1)组补体C3和C5 mRNA表达明显降低(P<0.01)。抗补体活性测定结果表明,与补体组相比,LWD-b各浓度组及LW-AFC 10和100 mg·L^(-1)组相对溶血率均明显降低(P<0.01),但仅LWD-b组相对溶血抑制率>20%,提示LWD-b具有抗补体活性,LW-AFC,CA-30和LWB-B此作用不明显。LWD-b中主要成分的抗补体活性筛选结果表明,与补体组相比,莫诺苷1和100μmol·L^(-1)组及芍药苷100μmol·L^(-1)组相对溶血率均明显降低(P<0.01),且相对溶血抑制率均>20%;獐牙菜苷、马钱苷、马钱苷酸和丹皮酚原苷组相对溶血率虽也明显降低(P<0.01),但其相对溶血抑制率均<20%;提示莫诺苷和芍药苷具有显著抗补体活性,而其余成分抗补体活性较弱。补体成分缺失血清法测定结果表明,分别与补体C1q,C2,C3,C5和C9缺失血清组相比,LWD-b 100 mg·L^(-1)处理后相对溶血率变化均<5%,提示LWD-b降低溶血能力与其作用于上述补体成分相关。结论 基于转录组数据分析发现并验证了六味地黄方活性组分LWD-b具有抗补体激活作用,莫诺苷和芍药苷可能是其发挥该作用的主要活性成分。LWD-b可能通过作用于补体成分C1q,C2,C3,C5和C9发挥作用。

基于B/S模式的构件式酒店管理信息系统的设计与实现

主要介绍了基于B/S模式的酒店管理信息系统的设计与实现方法,包括设计目标、数据库的设计、系统功能设计、实现技术等,对系统中的关键技术如构件技术、B/S技术、网络安全技术等进行了较详细的阐述。

小麦A淀粉和B淀粉的比较

对实验室所制备的小麦A淀粉和B淀粉的组分、性质进行了研究。实验结果表明:B淀粉含有的蛋白质、脂肪、戊聚糖等成分明显高于A淀粉。A淀粉淀粉颗粒较大,颗粒形状主要为圆形,B淀粉中淀粉颗粒小,颗粒形状主要为椭圆形。A淀粉和B淀粉的结晶结构相似,都为A型。A淀粉的重量平均分子量(或重量平均聚合度)、数量平均分子量(或数量平均聚合度)、分散度都比B淀粉大。A淀粉的膨润力小于B淀粉,而蓝值、溶解度、粘度、相变温度和相变热焓均大于B淀粉。

增强UV-B辐射对烤烟主要香气前体物及化学成分的影响

为了探明影响特色优质烟叶香气风格形成和烤烟致香成分积累的原因,通过增强UV-B的方法,测定了光照中紫外线强度增大后烤烟的中上部烟叶质体色素(叶绿素、叶黄素、β-胡萝卜素)和多酚类物质(绿原酸、芸香苷)等香气前体物及总糖、还原糖、总氮、蛋白质、烟碱、钾等化学成分的含量。结果表明,增强UV-B辐射会抑制烤烟上部叶的质体色素合成,促进中部叶质体色素的合成,多酚受UV-B增强的影响表现与质体色素相反;增强UV-B辐射烤烟上部叶总糖、还原糖、总氮、蛋白质、烟碱含量降低,钾含量升高,中部叶总糖、还原糖含量降低,总氮、蛋白质、烟碱、钾含量升高。烤烟的主要香气前体物及化学成分与UV-B强度密切相关,适当增强UV-B有利于烤烟中部叶香气和品质的提高。

UV-B对烟草生长发育及次生代谢的影响

通过模拟UV-B辐射,探索不同紫外辐射强度、辐射方式对烟草幼苗生长发育、光合生理、色素及多酚、糖类、烟碱等代谢产物的影响,以期探讨烤烟品质形成的生态机理。结果表明:UV-B辐射可使烟苗矮化变粗,叶面积缩小,光合效率下降,但可恢复;UV-B处理叶绿素、糖、烟碱含量下降幅度与辐射强度正相关,但微量UV-B有利于成苗叶绿素含量提高;UV-B辐射可使与植物抗逆性有关的多酚含量得到显著提高,与处理时间、强度正相关;适宜强度的UV-B预处理可使烤烟叶绿素、总类胡萝卜素和总糖含量提高。