Investigations of interaction mechanism and conformational variation of serum albumin affected by artemisinin and dihydroartemisinin

In this work, binding interactions of artemisinin (ART) and dihydroartemisinin (DHA) with human serum albumin (HSA) and bovine serum albumin (BSA) were investigated thoroughly to illustrate the conformational variation of serum albumin. Experimental results indicated that ART and DHA bound strongly with the site I of serum albumins via hydrogen bond (H-bond) and van der Waals force and subsequently statically quenched the intrinsic fluorescence of serum albumins through concentration-dependent manner. The quenching abilities of two drugs on the intrinsic fluorescence of HSA were much higher than the quenching abilities of two drugs on the intrinsic fluorescence of BSA. Both ART and DHA, especially DHA, caused the conformational variation of serum albumins and reduced the α-helix structure content of serum albumins. DHA with hydrophilic hydroxyl group bound with HSA more strongly, suggesting the important roles of the chemical polarity and the hydrophilicity during the binding interactions of two drugs with serum albumins. These results reveal the molecular understanding of binding interactions between ART derivatives and serum albumins, providing vital information for the future application of ART derivatives in biological and clinical areas.     

谷子不育系及其相应可育系小孢子发育的细胞学观察

以谷子2个品种的不育系及其保持系为材料,对其小孢子发育的细胞形态学进行了观察研究。结果表明:昭盟A花药的外部形态及花粉母细胞的发育过程与昭盟B相似,能形成外观正常的三核花粉,但其花药不能开裂散粉。石炮A表现出了败育时间和方式的多样性,且不育系与保持系间在花药长度上有显著差异。此外,两种不育系的维管束都表现出不同程度的发育不良。不良程度与药囊退化程度相关。     

Phytoconstituents of Selaginella effusa Alston and Their α-Glucosidase as well as Urease Inhibitory Activities

Three new compounds ( 1 – 2 , 14 ), as well as 22 known compounds ( 3 – 13 , 15 – 25 ), were extracted for the first time from the Selaginella effusa Alston (S. effusa). For the unknown compounds, the planar configurations were determined via NMR and by high-resolution mass spectrometry, while their absolute configurations were determined by calculated electronic circular dichroism (ECD), and the configuration of the stereogenic center of biflavones 4 – 5 were established for the first time. The pure compounds ( 1 – 25 ) were tested in vitro to determine the inhibitory activity of the enzyme-catalyzed reactions. Compounds 1 – 9 inhibited α-glucosidase with IC₅₀ values ranging from 0.30±0.02 to 4.65±0.04 μM and kinetic analysis of enzyme inhibition indicated that biflavones 1 – 3 were mixed-type α-glucosidase inhibitors. Compounds 12 – 13 showed excellent inhibitory activity against urease, with compound 12 (IC₅₀=4.38±0.31 μM) showing better inhibitory activity than the positive control drug AHA (IC₅₀13.52±0.61 μM). In addition, molecular docking techniques were used to simulate inhibitor-enzyme binding and to estimate the binding posture of the α-glucosidase and urease catalytic sites.     

ent-Pimarane Diterpenes from the Aerial Parts of Siegesbeckia pubescens

Five new ent-pimarane diterpenes ( 1 – 5 ) and five known analogs ( 6 – 10 ) were isolated from the aerial parts of Siegesbeckia pubescens. Their structures, including absolute configurations, were determined by comprehensive spectroscopic methods especially 1D and 2D NMR and quantum chemical electronic circular dichroism calculations. All the isolated compounds were evaluated for their cytotoxicity against human BT549, A549 and H157 cancer cell lines. Among them, compounds 1 and 2 showed mild cytotoxicity against lung cancer cell lines H157 with IC₅₀ values of 16.35±2.59 and 18.86±4.83 μM, respectively.     

人前列腺生长因子的分离纯化及生物活性鉴定

从人良性增生前列腺组织中经硫酸铵沉淀和肝素－琼脂糖凝胶层析纯化出人前列腺生长因子（ｈＰＧＦ）,纯化倍数约１０００倍,ＳＤＳ－ＰＡＧＥ和等电聚焦电泳示分子量约为１７ｋＤ、等电点同标准ｂＦＧＦ,利用分离培养的人前列腺间质成纤维细胞进行活性鉴定,发现以１．３～１．７ｍｏｌ／ＬＮａＣｌ洗脱部分为ｈＰＧＦ,活性最高,对间质成纤维细胞有显著刺激增殖作用。     

四川55种鱼生活史型的研究

四川５５种鱼生活史型的研究刁晓明,罗一兵李波（西南农业大学水产系,重庆６３０７１６）（重庆大学计算机系,６３００００）ＬｉｆｅＨｉｓｔｏｒｙＰａｔｔｅｒｎｓｏｆ５５ＦｉｓｈＳｐｅｃｉｅｓｉｎＳｉｃｈｕａｎ￥ＤｉａｏＸｉａｏｍｉｎｇ;ＬｕｏＹｉｂｉｎｇ...     

重组白细胞介素-2纯化过程中影响活性的因素探讨

<正> 白细胞介素-2(Interleukin-2,IL-2)是一种重要的免疫调节剂,具有促进T细胞增殖和分化,调节NK细胞活性,诱导LAK等功能,在肿瘤治疗上有广泛的应用前景。我们的前文就重组菌中IL-2包含体的制备、性质及重组rIL-2的纯化进行了研究,本文就重组rIL-2纯化过程中影响其活性的有关因素进行了探讨。     

蝽卵金小蜂属一新种记述(小蜂总科:金小蜂科:柄腹金小蜂亚科)

本文记述金小蜂科柄腹金小蜂亚科蝽卵金小蜂属一新种,正模、配模、副模,采自北京市平谷县。     

兔出血症病毒核酸的某些理化性质的研究

本文对我国无锡分离的兔出血症病毒A_2R-3毒株核酸的某些理化性质进行了研究。采用孚尔根染色、二苯胺反应和核酸酶解实验证实病毒核酸为DNA类型。吖啶橙染色、甲醛反应、核酸酶S_1消化和核酸热变性实验表明病毒核酸为单链型。核酸电泳呈单一组分。电境观察显示核酸分子链呈线状,平均长度约为2.15μ。计算分子量约为2.1—2.5×10~6d。核酸碱基组盛为A25.34、T29.37、G23.85、C21.43、(G C)克分子百分比值为45.28。结合以前的报道、我们认为:兔出血症病毒可以归类于细小病毒科。     

The unprocessed C-terminal dipeptide of recombinant beta-nerve growth factor determines three stable forms with distinct biological activities.

The processing of polypeptide neurotrophins in the nervous system is poorly understood. In this paper, we provide information on the effects of C-terminal processing of nerve growth factor. Three forms of recombinant mouse beta-nerve growth factor (rNGF) were produced and isolated from insect cells infected with a recombinant baculovirus. The three purified forms of rNGF exhibited distinct biological activities and differed in their abilities to compete with high affinity binding of mouse beta-nerve growth factor (mNGF). However, they were chemically and structurally indistinguishable from each other. All three forms of rNGF differed from mature mNGF from mouse submaxillary gland in that the C-terminal Arg-Gly dipeptide had not been proteolytically removed. Removal of the C-terminal dipeptide by gamma-NGF peptidase treatment converted the three forms into a single form identical with mature mNGF. The above results demonstrate that a single polypeptide of rNGF, due to the presence of a C-terminal dipeptide, exhibits three stable dimeric protein conformations with distinct biological activities. The apparent lack of gamma-NGF peptidase in the nervous system raises the possibility that the biologically significant form of NGF may differ from mature mNGF; such a difference may be of physiological relevance.