Synthesis and anticancer activities of 5,6,7-trimethylbaicalein derivatives

The aim of this study was to develop potential anticancer agents based on a naturally occurring baicalein, a flavonoid from Scatellariae radix. Cinnamic acid derivatives were converted to corresponding chlorides and then condensed with 3,4,5-trimethoxyphenol in the presence of BF(3) x Et(2)O to give chalcones. Intramolecular cyclization of these intermediates by the actions of DMSO/I(2) afforded the desired trimethylbaicalein derivatives. Cell viability after treatment with the tested compound for 2 d was determined by a colorimetric MTT assay. The results indicated that most of the derivatives showed improved inhibition of proliferation of Hep G2 cells. Compound 9 was the most potent, in which the cell viability was reduced to <2% at the 25 microM level. In the case of Hep 3B cells, 8a, 8b and 8f showed moderate inhibition of their proliferation and 25 microM was required to reduce the viability to ca. 30%. On the other hand, prostate DU145 cells were more resistant. Most of the derivatives caused a 60% inhibition of DU145 cells only at a concentration of 100 microM or above.     

Reactions of unsaturated aldehydes with cyclopentadiene in solvents of various polarities

The rate constants of cycloaddition of cyclopentadiene to unsaturated aldehydes in different solvents cannot be correlated with a single parameter, in particular, the Brownstein parameter. The data set can be fitted only by multiparameter equations in which the decisive factor increasing the reaction rate is the capability of a solvent for electrophilic solvation. The same parameter also governs the ratio of the endo and exo isomers of the addition product.     

Chemically enhanced alpha-energy spectroscopy in liquids

Summary The determination of transuranic (TRU) content in nuclear wastes, reactor materials, process solutions, and various other matrices is required in support of material assessment, environmental restoration, and waste processing activities. We have found that direct measurement of TRU is possible using surface passivated ion implanted planar silicon diode detectors. The performance and durability of modern silicon diodes enables direct detection of alpha-particles, with retention of some spectral information, through small air gaps or under direct contact with liquid or solid samples. We will present results on the performance of silicon diode detectors for the determination of TRU in liquids.     

镧对Rhizoctonia solani的毒力及其致病酶活性的影响

采用琼脂平板生长速率法及液体培养基培养测定了La对立枯丝核病菌(Rhizoctoniasolani)的抑制作用和毒力,并测定了其对病菌胞外的果胶酶、蛋白酶和纤维素酶等几种致病酶的活性的影响。结果表明,随着La浓度升高,对病菌菌丝生长的抑制作用增强,固体培养上所测定的对病菌的EC50和EC95分别为171.9和667.7mg·L-1;在液体培养基中所测定的EC50和EC95分别为111 4和500 7mg·L-1。在一定浓度范围内,La提高了单位量菌丝所产生3种致病酶的活性,但由于对菌丝生长量的强烈抑制,使病菌胞外3种致病酶的总量或总活性受到抑制,减低了病菌的致病力。     

倒数示波计时电位法在合金样品测定中的应用

应用倒数示波计时电位法，在含有吸附络合物的溶液中，采用桂汞电极作为极化电极，测定了Ｃｕ＾２＋、Ｎｉ＾２＋、Ｃｄ＾２＋、Ｐｂ＾２＋等几种金属离子的检测下限，并通过沿（ｄＥ／ｄｔ）－１￣Ｅ曲线上的峰高对合金样品进行定量分析，得到满意结果。实现了示波分析由常量到微量的飞跃。     

One-pot enantioselective formation of eight-membered rings from alkenyl Fischer carbene complexes and ketone enolates

Eight-membered carbocycles with up to five new stereogenic centers are enantioselectively obtained following a one-pot procedure that involves the coupling of three components: an alkenyl Fischer carbene complex, a ketone enolate, and allyl lithium.     

Fluorescence studies on the interactions of barbaloin with bovine serum albumin

The fluorescence quenching reactions of barbaloin with bovine serum albumin (BSA) in pH 7.20 Tris-HCl buffer solution were studied. The quenching mechanism of BSA by barbaloin was interpreted using the Stern-Volmer (S-V) mechanism. The binding constant K values were 2.78 x 10(5) (293 K), 1.87 x 10(5) (310 K), 1.25 x 10(5) (318 K), and the number of binding sites (n) were 1.18, 1.14, and 1.09, respectively. In addition, the thermodynamic functions enthalpy (deltaH degrees ) and entropy (deltaS degrees ) for the reaction were also calculated according to Vant's Hoff equation were -23.7 kJ/mol and 23.6 J/mol, respectively. Plausible explanations of the quenching mechanism are discussed on the basis of a hydrophobic interaction between barbaloin and BSA.     

氯过氧化物酶的手性催化活性在有机合成中的应用

氯过氧化物酶（CPO）作为过氧化物酶家族中的一员对多种有机底物表现出了广泛的催化活性。自上世纪60年代被发现以来，CPO在有机合成中的应用一直是一个研究热点。它作为一种生物催化剂能催化广泛的底物合成手性化合物，且有高的产率和高的对映选择率。本文综述了氯过氧化物酶在手性有机合成中的应用，重点关注了卤化、醇氧化、羟基化、环氧化、磺化氧化等反应，并讨论了目前在该领域所面临的问题及今后的发展趋势。     

Calix[4]arenes containing benzodiazepinone fragments at the lower rim

A series of p-tert-butylcalix[4]arene derivatives containing 1,4(1,5)-benzodiazepinone fragments as substituents were prepared. The biological activity of the compounds, namely, their antispasmodic activity in mice, was evaluated by antagonism with a spasmodic agent, Corazol, upon transdermal administration. According to the data obtained, benzodiazepine derivatives of calixarenes show higher antispasmodic activity compared to 3-hydroxyphenazepam, taking into account their considerably higher molecular weight.     

磷酸钡钙∶铈、锰红色荧光粉的研制

采用高温固相反应合成了磷酸钡钙∶铈、锰红色荧光粉。借助TG,XRD,荧光粉相对亮度仪、荧光分光光度仪等手段系统研究了合成过程中原料化学组成及配比、合成条件对磷酸钡钙∶铈、锰发光性能的影响。结果表明,荧光粉基质(BaxCa1-x)3(PO4)2具有畸变的Ca3(PO4)2结构。该荧光粉中Ce3+是助激活剂,Mn2+是激活剂,由Ce3+→Mn2+的能量传递使Mn2+激发产生650 nm左右的发射,当Ce3+和Mn2+浓度相等且都为0.15时,荧光粉有最高的红色发射亮度。