Proteinaceous microspheres of BSA (Bovine Serum Albumin) containing an anticancer drug, Taxol (paclitaxel) were fabricated using a sonochemical procedure and then assayed for chemical and biological activity. The sonochemical reaction did not compromise the drug, which became encapsulated in the BSA microspheres. The amount of the anticancer drug in the microspheres was determined by HPLC. Anticancer activity of the proteinaceous microspheres encapsulating the Taxol was tested on Mouse Multiple Myeloma cell line MPC-11. The influence of the Taxol microspheres on the cancer cells was different from pristine Taxol. It was found that Taxol in combination with the organic solvent causes the death of cancer cells. 相似文献
Electrochemistry combined with mass spectrometry represents an emerging analytical technique used to study the oxidation pathway of various drugs and in vivo occurring compounds, continuously showing a capability to generate many known metabolites or new oxidation products. An on‐line HPLC/EC/HR ESI‐MS method had been used to investigate the oxidation of selected cytokinin compounds. This setup allowed rapid identification and general structure elucidation of the obtained products. An electrochemical oxidation of isopentenyladenine resulted in five products, including hydroxylated and dehydrogenated products, which correlates very well with its in vivo metabolism. Electrochemical conversion of trans‐zeatin revealed six products, with two dehydrogenation products corresponding to its in vivo occurring metabolites. cis‐Zeatin oxidation in the electrochemical cell gave rise to eight products, resembling similarity to trans‐zeatin oxidation. All three compounds underwent a complete turnover mainly through two oxidation reactions occurring in the electrochemical cell? dehydrogenation and a less typical aliphatic hydroxylation. The resulting products are in correlation with their known in vivo metabolism. 相似文献
Journal of Thermal Analysis and Calorimetry - The main aim of this article was to describe the methodology for the measurement of specific heat using the laser flash apparatus. The obtained values... 相似文献
Nucleotides, their analogues, and other phosphate esters and phosphoramidates often contain the triethylammonium cation as a counterion. We found that this may be lost during chromatographic purification or concentration of solutions, yielding products in acidic forms or containing sub-stoichiometric amounts of the counterion. This in turn may be detrimental, e.g., due to possible decomposition of a compound or inaccurate sample preparation. Correlations between the structure of studied compounds and their susceptibility for cation loss were analyzed. Modifications in preparative techniques were developed to obtain the studied compounds with stoichiometric anion to cation ratios.
Graphical Abstract Triethylammonium salts of phosphate esters and phosphoramidates may lose the cationic component during chromatography or evaporation of solvent
Hirshfeld surfaces and two‐dimensional fingerprint plots are used to analyse the intermolecular interactions in two new phosphorothioic triamide structures, namely N,N′,N′′‐tris(3,4‐dimethylphenyl)phosphorothioic triamide acetonitrile hemisolvate, P(S)[NHC6H3‐3,4‐(CH3)2]3·0.5CH3CN or C24H30N3PS·0.5CH3CN, (I), and N,N′,N′′‐tris(4‐methylphenyl)phosphorothioic triamide–3‐methylpiperidinium chloride (1/1), P(S)[NHC6H4(4‐CH3)]3·[3‐CH3‐C5H9NH2]+·Cl− or C21H24N3PS·C6H14N+·Cl−, (II). The asymmetric unit of (I) consists of two independent phosphorothioic triamide molecules and one acetonitrile solvent molecule, whereas for (II), the asymmetric unit is composed of three components (molecule, cation and anion). In the structure of (I), the different components are organized into a six‐molecule aggregate through N—H...S and N—H...N hydrogen bonds. The components of (II) are aggregated into a two‐dimensional array through N—H...S and N—H...Cl hydrogen bonds. Moreover, interesting features of packing arise in this structure due to the presence of a double hydrogen‐bond acceptor (the S atom of the phosphorothioic triamide molecule) and of a double hydrogen‐bond donor (the N—H unit of the cation). For both (I) and (II), the full fingerprint plot of each component is asymmetric as a consequence of the presence of three fragments. These analyses reveal that H...H interactions [67.7 and 64.3% for the two symmetry‐independent phosphorothioic triamide molecules of (I), 30.7% for the acetonitrile solvent of (I), 63.8% in the phosphorothioic triamide molecule of (II) and 62.9% in the 3‐methylpiperidinium cation of (II)] outnumber the other contacts for all the components in both structures, except for the chloride anion of (II), which only receives the Cl...H contact. The phosphorothioic triamide molecules of both structures include unsaturated C atoms, thus presenting C...H/H...C interactions: 17.6 and 21% for the two symmetry‐independent phosphorothioic triamide molecules in (I), and 22.7% for the phosphorothioic triamide molecule of (II). Furthermore, the N—H...S hydrogen bonds in both (I) and (II), and the N—H...Cl hydrogen bonds in (II), are the most prominent interactions, appearing as large red spots on the Hirshfeld surface maps. The N...H/H...N contacts in structure (I) are considerable, whereas for (II), they give a negligible contribution to the total interactions in the system. 相似文献
3‐Hydroxyquinoline‐2,4‐diones react with KSCN in the presence of the NH$\rm{{_{4}^{+}}}$ ions to generate 2,3‐dihydro‐3‐thioxoimidazo[1,5‐c]quinazolin‐5(6H)‐ones, 2,3‐dihydro‐2‐thioxo‐1H‐imidazo[4,5‐c]quinolin‐4(5H)‐ones, and products of molecular rearrangement of the 3‐aminoquinolinedione intermediates. Starting compounds with a benzyl (Bn) group at C(3) afford 3‐aminoquinolinediones, even when only AcONH4 is used. The results of the reaction between 3‐hydroxyquinoline‐2,4‐diones and KSCN in the presence of BuNH2 show that replacing a OH group with a secondary NH2 group is also possible. 相似文献
This study proposes changes to the design and evaluation of the CO2 headspace test, which is used as a simple method for assessment of the complete biodegradability of surfactants. It presents a modified equation for the calculation of biodegradation. It is proposed that the solution of 7 mol L?1 sodium hydroxide commonly used in the process involving alkalinisation of the vial contents be replaced with 15 mol L?1 sodium hydroxide. The use of the higher hydroxide concentration leads to a significant reduction in the value of the blank CO2 headspace test. 相似文献
The unit‐cell size and pore diameter as functions of temperature are investigated in the syntheses of FDU‐12 silicas with face‐centered cubic structure templated by Pluronic (PEO‐PPO‐PEO) block copolymer micelles swollen by toluene. The temperature range in which the unit‐cell size and pore size strongly increase as temperature decreases is correlated with the critical micelle temperature (CMT) of the surfactant. While Pluronic F127 affords a wide range of unit‐cell parameters (28–51 nm) and pore diameters (16–32 nm), it renders moderately enlarged pore sizes at 25 °C. The use of Pluronic F108 with higher CMT affords FDU‐12 with very large unit‐cell size (~49 nm) and large pore diameter (27 nm) at 23 °C. Large unit‐cell size (40–41 nm) and pore size (22 nm) were obtained even at 25 °C. The application of Pluronics F87 and F88 with much smaller molecular weights and higher CMTs also allows one to synthesize FDU‐12 with quite large unit‐cell parameters and pore sizes at room temperature. The present work demonstrates that one can judiciously select Pluronic surfactants with appropriate CMT to shift the temperature range in which the pore diameter is readily tunable. 相似文献
Here it is reported that crystals of an enantiopure [7]helquat salt undergo reversible thermal solid–solid phase transition at 404 K. Differential scanning calorimetry (DSC), capillary electrophoresis (CE), and X‐ray diffraction analysis were used to unravel the mechanistic details of this process. The single‐crystal‐to‐single‐crystal course enabled direct monitoring of the structural changes by in situ variable‐temperature X‐ray diffraction, thus providing the first direct evidence of a solid phase transition in a helicene‐like compound. 相似文献