Functional analysis of repositioned anilide derivatives as anticancer compounds

Off the different types cancers 40% of the population have been observed to be affected by leukemia. Contemporary therapeutics is focusing on generation of new synthetic analogues that can exert maximum positive physiological effect with minimum dosage and negligible deleterious side effects. New generation pharmacists are focusing on such promising effects of Imatinib (a potential anti-cancer drug molecule), Dasatinib, Pelitinib and Nilotinib. The present research study focuses on novel synthesized anilides derivative against BCR-ABL kinase as potential anti-leukemic agent. Validation of the compounds by molecular docking with specific BCR-ABL kinase confirmed their activity. Toxicity prediction of these compounds helped to identify sustainability as therapeutic molecules. The IC₅₀ values were calculated (211 ug, 175 ug, 272ug for compounds A, B, C resp.) and the mode of cell death was gauged by DNA laddering assay. The cells were observed to be induced for programmed cell death. By validating and in-vivo testing of three synthesized compounds, the compound B was observed to be more stable thermodynamically with a potentially vital active site and appears to be a promising anti-leukemic factor. The present research thus lays a preliminary platform in world of pharmaceutics, where these new analogues appear to be efficient, target specific and less toxic molecules.     

慢性支气管炎急性发作期病人血中微量元素的变化分析

为观察慢性支气管炎急性女作期血液中微量元素的变化，对１０１例慢性支气管炎急性发作期病人和３０例正常人全血中锌、铁、铜及钙进行检测。结果显示：慢性支气管炎急性发作期病人锌、铁、铜和钙４种元素均明显于正常人。提示患者血中微量元素总量减少，可能是慢性支气官炎易反复感染、加剧病变发展的原因之一。认为合理补充缺乏的微量元素，有助于疾病的防治。     

拉米夫定治疗慢性乙型肝炎YMDD变异的相关因素分析

目的分析拉米夫定治疗后慢性乙型肝炎酪氨酸(Y)、蛋氨酸(M)、天冬氨酸(D)、天冬氨酸(D)变异的相关因素.方法对169例经拉米夫定治疗12个月后的慢性乙型肝炎患者发生YMDD变异情况进行回顾性分析.采用荧光定量PCR和PCR产物测序等方法检测慢性乙型肝炎拉米夫定治疗前、治疗后HBV基因型、HBV DNA水平、HBeAg状态、ALT水平等指标.结果在169例患者中,基因型B共76例(44.97%),基因型C共93例(55.03%).拉米夫定治疗12个月后,46例(27.22%)患者发生YMDD变异,其中,基因型B变异27例(35.53%),基因型C变异19例(20.43%),两者有统计学差异(P<0.05).YMDD变异组患者治疗前HBV DNA水平显著高于YMDD未变异组[(7.26±0.58 vs6.44±0.65)log拷贝/ml,P<0.05].HBeAg阳性患者YMDD变异率显著高于HBeAg阴性患者(38.10%vs20.75%,P<0.05).YMDD变异组与未变异组在治疗前ALT水平上无明显差异[(136.09±28.21 vs 124.15±26.52)U/L,P>0.05].结论拉米夫定治疗慢性乙型肝炎发生YMDD变异与HBV基因型、HBV DNA水平、HBeAg状态等密切相关.拉米夫定治疗前,检测HBV基因型、HBV DNA水平,HBeAg状态等指标对慢性乙型肝炎抗病毒治疗具有重要意义.     

血清瘦素水平在评估慢性病毒性肝炎肝纤维化程度中的意义

目的探讨血清瘦素(LEP)水平与慢性乙肝（CHB）和慢性丙肝（CHC）患者肝纤维化程度之间的关系。方法采用ELISA方法检测65例CHB、41例CHC患者血清LEP浓度,同期25例健康体检者作为对照。所有入选患者均经肝脏穿刺病理学检查评估肝纤维化程度。结果与对照组相比,CHB与CHC患者LEP水平明显增高（P＜0.05或0.01）,CHB和CHC患者血清LEP水平在纤维化程度较高者均明显高于纤维化程度较低者（均P＜0.01）,且CHC组血清LEP水平显著高于相同纤维化分期CHB患者（P＜0.05或0.01）。结论血清LEP水平与慢性病毒性肝炎肝纤维化程度相关,血清LEP水平可作为慢性病毒性肝炎患者肝纤维化程度监测指标之一。     

A risk analysis based on a two-stage delayed diagnosis regression model with application to chronic disease progression

This paper presents a two-stage regression model for quantifying different stages of a disease progression with delayed diagnosis time and for identifying the risk factors associated with each stage. Conventional chronic disease progression studies reported replied on the assumption that the time of the confirmation of a disease state by diagnosis is the start time of this disease state. Clearly this will lead to biased estimates of progression since the disease state should have already occurred before the diagnosis, but the true occurrence time is unknown. This later confirmation is called the delayed diagnosis in this paper and a delay-time modelling procedure is developed for the identification of the unknown stages of progression. A hazard-based regression model is also proposed for a further risk analysis. We apply the developed methods to hepatitis C data and the analysis shows that considering the delayed diagnosis significantly improved the model fit in comparison with the conventional model. We also find that the risk factors associated with each stage are more significant, particularly in the second stage of progression, than those based on the conventional model. We conclude that such delayed phenomena in diagnosis should be taken into account when modelling the chronic disease progression process and conducting related risk analysis.     

Dynamical analysis of age-structured pertussis model with covert infection

An age-structured pertussis model with covert infection is proposed to understand the effect of covert infection on the recurrence of pertussis. It is found that vaccination only for young children does not have a decisive effect on whooping cough control. It is shown that although the vaccine coverage rate is relatively high, the model has a backward bifurcation for a larger covert infection rate. In addition, sufficient conditions for the disease-free steady state to be globally asymptotically stable are obtained.     

肾炎及肾衰患者血中金属元素含量的变化

用原子吸收法或极谱法测定了对例慢性肾炎病人（A组）和24例慢性肾衰病人(B组)及40名健康人（对照组，C组）全血中的Fe、Zn、Cu、Mn、Se、Pb和Ga含量。结果表明，A组与C组比较．血中Fe的含量A组明显低于C组（P＜0.05），Zn、Mn和Se的含量A组均非常明显低于C组（P＜0.01），Pb含量A组非常明显高于C组（P＜0．01），Cu和Ca含量两组间均无明显差异（P＞0.05）；B组与C组比较，Fe含量B组明显低于C组（P＜0.06），Se含量则B组明显高于C组（P＜0.05）；Zn、Mn、Cu、Ga含量B组均非常明显低于C组（P＜0.01），而Pb含量则B组非常明显高于C组（P＜0．01）。     

Isolation and Purification of Polysaccharides from Cordyceps minlitaris and Its Inhibition on the Proliferation of Rat Glomerular Mesangial Cells

The crude polysaccharide was obtained by means of the decolorization of porphyrized Cordyceps minlitaris stroma with organic solvent, extraction with hot water, precipitation in 80% ethanol, and protein removal with the Sevag method. After purification with Sephadex G-75, two of its components, CMP-1 and CMP-2, were obtained. Through the assay of gel chromatography and polarimetry, CMP-1 was identified as pure polysaccharide. The results demonstrated that CMP-1 had favorable oxidation resistance activity, which could scavenge not only oxygen-free radicals in the self-oxidation system of pyrogallic acid, but also the hydroxide-free radicals in the Fenton system. The study focused on the effects of low, medium, and high dosages of CMP-1 in rat blood serum on the proliferation of glomerular mesangial cells in vitro. Through MTT Colorimetric analysis, the activities were compared among the blank control group and the Niaoduqing positive control group CMP-1 and CMP-2. The results shows that CMP-1 was able to inhibit the proliferation of rat glomerular mesangial cells effectively. Therefore, CMP-1, one component of polysaccharides of Cordyceps minlitaris, was certainly a potential remedy for hyperplastic glomerular nephritis, whose antioxidant activity could slow down the process of chronic renal failure（CRF） to some extent.     

慢性支气管炎与17种元素的关系分析

采用ＩＣＰ－ＭＳ法对１３例慢性支气管炎急性发作期患者血清１７种元素进行测试，并与对照组比较，结果Ｓｒ，Ａｌ，Ｆｅ，Ｚｎ，Ｉ，Ｂ，Ｃａ等７种元素有显著差异，提示患者体内存在多种元素代谢紊乱，建议在治疗过程中注意纠正元素代谢紊乱，以利于改善病情。