Preparation of dummy template‐imprinted polymers for the rapid extraction of nonsteroidal anti‐inflammatory drugs residues in aquatic environmental samples

A molecularly imprinted polymer was synthesized and applied as a sorbent in the solid‐phase extraction device. The imprinted polymer was characterized by fourier‐transform infrared spectroscopy and scanning electron microscope. The results revealed that imprinted polymer possess sensitive selectivity and reliable adsorption properties for five NSAIDs. The imprinted polymer was successfully applied to the pre‐concentration for five NSAIDs in different water samples prior to UPLC‐MS/MS. In the early studies, several factors were investigated, including pH adjustment, the kind of elution solvent and the volume of elution solvent. Finally, we found that the pH 5 and an aliquot of 2 mL methanol were suitable for the water samples. The limits of detection and limits of quantitation of five nonsteroidal anti‐inflammatory drugs varied from 0.007 to 0.480 μg L⁻¹ and 0.03 to 1.58 μg L⁻¹, respectively. The spiking recoveries of the target analytes were 50.33‐127.64% at the levels of 0.2 μg L⁻¹, 2 μg L⁻¹ and 5 μg L⁻¹. The precision and accuracy of this method showed a great increase compared with traditional solid‐phase extraction. The developed method was successfully applied to extraction and analysis of NSAIDs in different water samples with satisfactory results which could help us better understand their environmental fate and risk to ecological health.     

Synthesis,spectroscopic characterization,thermal behaviour,in vitro antimicrobial and anticancer activities of novel ruthenium tricarbonyl complexes containing monodentate V‐shaped Schiff bases

The interaction of Ru₃(CO)₁₂ with a novel family of monodentate V‐shaped Schiff base ligands (L^1–4; L¹: (E)‐1‐(4‐((4‐bromobenzylidene)amino)phenyl)ethanone, L²: (E)‐1‐(3‐(4‐(dimethylamino)benzylideneamino)phenyl)ethanone, L³: (E)‐1‐(4‐(4‐(dimethylamino)benzylideneamino)phenyl)ethanone, L⁴: (E)‐1‐(3‐(3,4‐dimethoxybenzylideneamino)phenyl)ethanone) in air under atmospheric pressure afforded the novel complexes [Ru(CO)₃(L^1–4)₂]. The parent ligands and their complexes were characterized using elemental analyses and spectroscopic techniques. In addition, the structure of the representative ligand L¹ was determined using single‐crystal X‐ray analysis. The stereochemistry and theoretical optimization of the three‐dimensional geometry of the ligands and their complexes were justified. In vitro antimicrobial screening against bacterial stains Escherichia coli and Staphylococcus aureus and fungus Candida albicans was conducted. Cytotoxicity of the compounds as anti‐tumour agents was evaluated against liver carcinoma (HepG2), breast carcinoma (MCF7) and colon carcinoma (HCT‐116) cell lines relative to cisplatin and doxorubicin. The complexes showed variable in vitro cytotoxic activities against the three studied cell lines, with IC₅₀ values less than those of cis‐platin, and thus appear to be building blocks for promising anti‐tumour agents.     

Stability of Antimicrobial Drug Molecules in Different Gravitational and Radiation Conditions in View of Applications during Outer Space Missions

The evolution of different antimicrobial drugs in terrestrial, microgravity and hypergravity conditions is presented within this review, in connection with their implementation during human space exploration. Drug stability is of utmost importance for applications in outer space. Instabilities may be radiation-induced or micro-/hypergravity produced. The antimicrobial agents used in space may have diminished effects not only due to the microgravity-induced weakened immune response of astronauts, but also due to the gravity and radiation-altered pathogens. In this context, the paper provides schemes and procedures to find reliable ways of fighting multiple drug resistance acquired by microorganisms. It shows that the role of multipurpose medicines modified at the molecular scale by optical methods in long-term space missions should be considered in more detail. Solutions to maintain drug stability, even in extreme environmental conditions, are also discussed, such as those that would be encountered during long-duration space exploratory missions. While the microgravity conditions may not be avoided in space, the suggested approaches deal with the radiation-induced modifications in humans, bacteria and medicines onboard, which may be fought by novel pharmaceutical formulation strategies along with radioprotective packaging and storage.     

Luminescent PtII and PtIV Platinacycles with Anticancer Activity Against Multiplatinum-Resistant Metastatic CRC and CRPC Cell Models

Platinum-based chemotherapy persists to be the only effective therapeutic option against a wide variety of tumours. Nevertheless, the acquisition of platinum resistance is utterly common, ultimately cornering conventional platinum drugs to only palliative in many patients. Thus, encountering alternatives that are both effective and non-cross-resistant is urgent. In this work, we report the synthesis, reduction studies, and luminescent properties of a series of cyclometallated (C,N,N′)Pt^IV compounds derived from amine–imine ligands, and their remarkable efficacy at the high nanomolar range and complete lack of cross-resistance, as an intrinsic property of the platinacycle, against multiplatinum-resistant colorectal cancer (CRC) and castration-resistant prostate cancer (CRPC) metastatic cell lines generated for this work. We have also determined that the compounds are effective and selective for a broader cancer panel, including breast and lung cancer. Additionally, selected compounds have been further evaluated, finding a shift in their antiproliferative mechanism towards more cytotoxic and less cytostatic than cisplatin against cancer cells, being also able to oxidize cysteine residues and inhibit topoisomerase II, thereby holding great promise as future improved alternatives to conventional platinum drugs.     

Isatindolignanoside A,a glucosidic indole-lignan conjugate from an aqueous extract of the Isatis indigotica roots

A glucosidic indole-lignan conjugate with a novel carbon skeleton, named isatindolignanoside A (1), was isolated from an aqueous extract of the Isatis indigotica roots “ban lan gen”. Its structure was determined by comprehensive analysis of spectroscopic data, enzyme hydrolysis, and electronic CD calculations. Compound 1 is active against Coxsackie virus B3 and represents the first example of natural product having a structural feature of conjugation between indole and lignan, and its plausible biosynthetic pathway is postulated.     

Anti‐cancer potential of selenium‐ and tellurium‐containing species: opportunities abound!

An overview highlighting the anti‐cancer potential of (bio‐essential) selenium‐ and tellurium‐containing species, with an emphasis on biological targets and mechanisms of action, is presented. Studies thus far have focused on selenium(II) compounds (along with – to a lesser extent – inorganic selenium and selenium nanoparticles) which often successfully exploit the inherent anti‐oxidizing ability of selenium. Significantly less work has been conducted in developing anti‐cancer tellurium compounds, yet two tellurium(IV) species are proven, clinically, as anti‐cancer agents. Given the prevalence of the disease and the accumulated insights into mechanisms of action, the continued development of selenium‐ and tellurium‐containing molecules is an area deserving greater attention. Copyright © 2012 John Wiley & Sons, Ltd.     

Absolute configuration of Buagafuran:An experimental and theoretical electronic circular dichroism study

Buagafuran is a novel drug candidate derived from natural product.Its absolute configuration has been confirmed by electronic circular dichroism combined with modern quantum-chemical calculation using time-dependent density functional theory.The predicted UV absorbance peak is underestimated by several nanometers compared with the experimental data.The applicability of empirical rule for the C=C-C-O system in Buagafuran has also been discussed.Our results show that electronic circular dichroism could be a useful tool for the absolute configuration assignment of chiral drugs,especially for the oily or semisolid substances,whose crystal structures are impossible to obtain.     

超高效液相色谱串联质谱法同时快速测定牛奶中不同类型的11种兽药残留

建立了超高效液相色谱串联质谱测定牛奶中四环素类、青霉素类、磺胺类和泰乐菌素等11种兽药残留的检测方法。样品经乙腈超声提取后离心分离,上层清液稀释10倍后过0.2μm滤膜上机测定。在优化条件下,11种兽药在其线性范围内的相关系数均在0.998以上,定量下限(LOQ,S/N=10)为0.3～15μg/kg,在低、中、高3个水平下的加标回收率为81%～117%,相对标准偏差为0.6%～10.2%。方法用于实际牛奶样品中兽药残留量的测定,结果满意。     

Improvement of Nanoprecipitation Technique for Preparation of Gelatin Nanoparticles and Potential Macromolecular Drug Loading

An optimum nanoprecipitation technique for gelatin nanoparticles is established, based on aqueous gelatin solution and ethanolic solution containing stabilizer. Crosslinking with glutaraldehyde results in stable gelatine nanoparticles. Several factors such as the surfactant concentration, type of surfactant, type of nonsolvent and gelatin concentration are evaluated. Gelatin nanoparticles with 200–300 nm can be produced using 20–30 mg mL^?1 of gelatin and a minimum of 7% w/v stabilizer (Poloxamer 407 or 188). Furthermore, methanol and ethanol are good nonsolvents, whereas other nonsolvents such as acetone, isopropyl alcohol, and acetonitrile, result in phase separation and visible precipitates. The entrapment efficiency of fluorescein‐isothiocyanate (FITC)‐dextran as model drug was determined to 50% with no substantial effect on particle size. 80% of the drug is only released after enzymatic digestion.