鬼臼毒素及其衍生物的瞬态粒子分析

分析了鬼臼毒素及其衍生物与还原性自由基(氢自由基、水合电子)作用、氧化性自由基羟基自由基和激光等作用后产生的各种瞬态粒子，对各粒子的生成和衰减过程进行跟踪，获得了各瞬态粒子的生成和衰减速率常数，进一步探讨了鬼臼毒素治疗肿瘤的构效关系。     

Antimycobacterial and anticancer activity of newly designed cinnamic acid hydrazides with favorable toxicity profile

A series of twelve novel hybrids of cinnamic acid and thiocarbohydrazones were designed, synthesized in high yield using a simple coupling strategy via acid chlorides, and evaluated for their impact against Mycobacterium tuberculosis (Mtb) and cancer cells survival. Among them, compound 3 demonstrated strong anti-Mtb activity by reducing bacilli survival for>90 % in all three treated Mtb isolates, whereas isoniazid and rifampicin did not. Moreover, compound 3 didn’t affect vitality of HepG-2 cells, implying on advantageous hepatotoxicity profile compared to current therapeutic options for tuberculosis. Compounds 2a and 3b displayed as strong inducers of apoptosis in A549 cells, both activating intrinsic caspase pathway and cell cycle arrest at the G0/G1 phase. Subsequent analyses disclosed differences in their activities, where 3b has ability to induce production of mitochondrial superoxide anions, while 2a significantly inhibited cellular mobility. More importantly, 3b considerably affected viability of HepG-2 and HaCaT cells, whereas 2a had moderate impact only on the later. Molecular modeling studies indicated high permeability and good absorption through the human intestine, and moderate aqueous solubility with poor blood–brain barrier permeability. In summary, our results reveal that novel compounds 3 and 2a represent promising agents for tuberculosis and cancer treatment, respectively, indicating that further investigation needs to be performed to clarify the mechanisms of their anti-Mtb and anticancer activity.     

Traditional uses,phytochemistry, pharmacology and other potential applications of Vitellaria paradoxa Gaertn. (Sapotaceae): A review

Vitellaria paradoxa Gaertn. is a multipurpose medicinal plant of the family Sapotaceae, and it has been widely used usually in the clinical traditional medicine as remedy for a wide range of diseases for several decades. In addition, the plant has also found applications in confectionery, cosmetics and soaps, and pharmaceuticals both locally and internationally. V. paradoxa, which has been identified with >150 phytoconstituents, is rich in oleanane-type triterpene acids and glycosides, such as paradoxosides A-E, tieghemelin A, parkiosides A-C, bassic acid, as well as flavonoids such as quercetin and catechin-type compounds. The extracts and the active constituents of V. paradoxa have been investigated for various pharmacological activities, including but not limited to anticancer, melanogenesis-inhibitory, antibacterial, anti-diabetic, antioxidant, anti-inflammatory, anti-diarrhoeal, and antifungal activities. Additionally, V. paradoxa has also been utilized in nanoparticles (NPs) synthesis. These NPs among other things have shown significant antinociceptive and antiedematogenic activities as well as environmental friendly adsorptive properties for the removal of pollutants from pharmaceutical effluents. Overall, this review comprehensively examines the traditional uses, phytochemistry, pharmacology, toxicology, clinical studies, and nanoparticles synthesized from V. paradoxa and their applications.     

水解聚合铝阳离子Al13和Al30的27Al核磁共振定量研究

采用不同磁场强度的NMR谱仪和不同测试温度,对水解聚合铝溶液中Keggin结构的聚合铝阳离子形态的定量分析方法进行了研究。检测结果表明,高场27A l NMR分析技术不仅能精确定量地检测出水解聚合铝溶液中具有Keggin结构的[A lO4A l12(OH)24(H2O)12]7 (简称A l13)聚合阳离子,而且还能定量地检测出[(A lO4)2A l28(OH)56(H2O)26]18 (简称A l30)聚合阳离子。提高测试温度,有利于降低A l30共振峰的线宽,增强其分辨率。在70℃测试温度下,采用高场27A lNMR分别对8种中、高浓度(0.1~2.0 mol/L)水解聚合铝溶液中的A l13和A l30形态分布进行了定量研究,证实了A l30形态是高浓度水解聚合铝溶液中的一种优势聚合形态。     

层状复合氧化物La4BaCu5-xMxO13(M=Mn, Co)的物化性质和结构中活性氧的研究

合成了一系列结构为层状ＡＢＯ３的复合氧化物Ｌａ４ＢａＣｕ５－ｘＭｘＯ１３（Ｍ＝Ｍｎ，Ｃｏ），并利用ＸＲＤ、Ｘ射线能谱、氧程序升温脱附和化学分析方法对它们的结构和活性氧种进行了研究。ＸＲＤ分析结果表明：它们的结构为五层的ＡＢＯ３结构。活性氧种的研究表明Ｌａ４ＢａＣｕ５Ｏ１３中掺杂Ｍｎ或Ｃｏ之后，样品中明显存在的ＭＣｕ（Ｍ＝Ｍｎ，Ｃｏ）之间的协同作用，并且ＣｕＭｎ之间协同作用明显比ＣｕＣｏ的强。     

Essential Oils of Nepeta Species Growing in Turkey

Essential oils from 22Nepetaspecies growing in Turkey have been studied. Results of GC/MS analyses of the essential oils have shown that four Nepeta species contain 4a-7-7a-nepetalactone as the major component. 4a-7-7a-Nepetalactone was the main constituent in N. racemosa. Seven Nepeta species contained caryophyllene oxide as the main constituent in their essential oils. 1,8-Cineole/linalool were the major components in the essential oils of six species. -Pinene,-terpineol,germacrene-D,and spathulenol were the main constituents in the essential oils fromN. phyllochlamys, N. viscida, N. sorgerae, andN. trachonitica, respectively.     

KINETICS STUDY ON MELT GRAFTING ACRYLIC ACID ONTO LLDPE USING REACTIVE EXTRUSION

The kinetics of melt grafting acrylic acid(AA)onto linear low density polyethylene(LLDPE)by using reactive extrusion was investigated.The polymeric peroxides(POOP and POOH)generated by electron beam irradiation were used to initiate the graft reaction.The samples taken out from the barrel at five ports along screw axis were analyzed by FTIR.The spectra show that both the graft copolymerization and homopolymerization proceed in two stages:the graft degree(or mass of homopolymer)increases linearly with the reaction time in the initial stage,and then gradually in the second stage.The rate of graft copolymerization R_g is always faster than that of homopolymerization R_h in the present system and the activation energy is 131 kJ·mol~(-1) for graft copolymerization and 127 kJ·mol~(-1) for homopolymeirzation.These results were interpreted in terms of solubility and diffusion of monomer,as well as the reactivity and the concentration of reactive species. The relationships between reaction rate and monomer concentration and peroxide concentration were found to he:R_g ∝ [M]~(1.46)[POOP+POOH]~(0.53) and R_h ∝[M]~(1.08)[POOH]~(0.51),which indicate that the addition of monomer to polymeric radicals is a slow step for the graft copolymerization.     

Light-assisted and remote delivery of carbon monoxide to malignant cells and tissues: Photochemotherapy in the spotlight

The recent discovery of the salutary effects of carbon monoxide (CO) in chronic obstructive pulmonary disease (COPD), ischemic perfusion damage, graft implantation, as well as its pro-apoptotic effects on hyper-proliferating cells has raised interest in delivering small doses of CO to biological targets under controlled conditions. In such attempts, photoactive metal carbonyl complexes (photoCORMs) have shown promise and several accounts of cancer cell eradication with light-triggered CO release from photoCORMs have been reported. CO releasing molecules (CORMs) and photoCORMs have been incorporated within biocompatible drug delivery vehicles such as carboxymethyl chitosan or mesoporous silica-based nanoparticles and the composite materials (photoCORs) have been successfully employed in controlled CO delivery to cancer cells to cause rapid CO-induced apoptosis. Fiber optic technology has also been utilized for remote delivery of CO to not easily accessible targets. Reports on all these therapeutic modalities for on-demand CO delivery to malignant targets in a highly localized fashion have opened up the possibility of phototherapy of cancer with the use of an unusual so-called “toxic” molecule. This review highlights the methodologies used in CO photochemotherapy reported so far along with analysis of their therapeutic outcomes, and possible improvements for better applicability.     

Transport of alkaline cation and neutral species through the α-Ni(OH)2/γ-NiOOH film electrode

The transport of alkaline cation and neutral species through the α-Ni(OH)₂/γ-NiOOH film electrode has been investigated during the hydrogen extraction from and injection into the film electrode in 0.1 M LiOH, KOH and CsOH solutions by using the electrochemical quartz crystal microbalance technique combined with the potentiostatic current transient technique and cyclic voltammetry. From the ohmic relationship between the initial current density and the applied potential step, it is suggested that the hydrogen transport through the film electrode is exclusively governed by "cell-impedance". On the basis of the "cell-impedance-controlled" hydrogen transport, the mass change measured indicates that during the hydrogen extraction, the alkaline cation is slowly inserted into the film electrode before the finish of the current plateau. After the period of current plateau has finished, it is drastically inserted at an exponential rate. By contrast, during the hydrogen injection, the extraction of alkaline cation is nearly completed before the finish of the current plateau. Most of the neutral species are incorporated into the film electrode during the immersion prior to the hydrogen extraction. The minority is not incorporated until the finish of the current plateau during the hydrogen injection. Electronic Publication     

CATALYTIC ACTIVE SITES OF YTTRIUM ORTHOVANADATE IN OXIDATIVE DEHYDROGENATION OF PROPANE

用ＥＳＲ、ＮＯＴＰＤ和１８Ｏ２同位素交换的方法研究了丙烷氧化脱氢催化剂正钒酸钇ＹＶＯ４的活性位。ＥＳＲ和ＮＯＴＰＤ结果证明催化剂中存在Ｖ４＋离子。１８Ｏ２同位素交换结果表明，Ｏ２是在Ｖ４＋及氧空位上活化的。氧的活化是催化剂在丙烷氧化脱氢中具有良好活性的原因。