Antimicrobial triterpenes from Debregeasia salicifolia

New triterpene, 3beta-(trans-cinnamoyloxy)-19alpha-hydroxy-urs-12-ene (1) has been isolated from the methanolic fraction of Debregeasia salicifolia, along with uvaol (2), 3beta,19alpha-dihydroxy-urs-12-ene (3), ursolic acid (4), pomolic acid (5), pomolic acid methyl ester (6) and tormentic acid (7) reported for the first time from this species. The compounds (1), (3) and (6) showed significant antimicrobial activity. The structure elucidation was made with the help of extensive 2D NMR spectroscopic techniques.     

Screening of urban aerosol particulate composites for selected metal distribution and their dependence on meteorological parameters

Local atmospheric aerosol particulate samples, collected as composites on daily 6-12 hour basis, at Quaid-i-Azam University campus, Islamabad, Pakistan, using high volume sampling technique, were analysed for Pb, Na, K, Fe, Mn, Cd, Cr, Ni, Zn and Co by FAAS method. The monitoring period ran from October, 2001 through March, 2002, with a total of 105 samples collected on cellulose filters, treated in part with the HNO3-based wet digestion method for metal quantification, and for particle size distribution separately. The metal content of the aerosols was examined in relation to dependence on meteorological parameters, such as temperature, relative humidity, wind speed, sun shine and pan evaporation. Statistical correlation analysis was conducted for multiple metal pairs in aerosols, and the data were examined in relation to meteorological parameters and relevant aerosol particle size fractions. The study revealed no viable strong correlation between the meteorological parameters and metal levels; in general, however, a significant positive correlation was found for temperature. A strong positive correlation was observed for PM<25 and PM2.5-10. For coarse particles (PM10-100 and PM>100), however, a negative correlation was observed. The levels of Na, K, Fe and Zn were found in the range of 1-5 microg/m3 while those for the rest of the metals in the sub microg/m3 range. Principal component analysis and cluster analysis were performed on dataset for source identification and appointment. Largest contribution (33%) was shown by the industrial emissions followed by traffic/road dust (16.7%).     

Exploring the Potential of Metallodrugs as Chemotherapeutics for Triple Negative Breast Cancer

This review focuses on studies of coordination and organometallic compounds as potential chemotherapeutics against triple negative breast cancer (TNBC) which has one of the poorest prognoses and worst survival rates from all breast cancer types. At present, chemotherapy is still the standard of care for TNBC since only one type of targeted therapy has been recently developed. References for metal-based compounds studied in TNBC cell lines will be listed, and those of metal-specific reviews, but a detailed overview will also be provided on compounds studied in vivo (mostly in mice models) and those compounds for which some preliminary mechanistic data was obtained (in TNBC cell lines and tumors) and/or for which bioactive ligands have been used. The main goal of this review is to highlight the most promising metal-based compounds with potential as chemotherapeutic agents in TNBC.     

Siloxyaluminate and Siloxygallate Complexes as Models for Framework and Partially Hydrolyzed Framework Sites in Zeolites and Zeotypes

Anionic molecular models for nonhydrolyzed and partially hydrolyzed aluminum and gallium framework sites on silica, M[OSi(OtBu)₃]₄⁻ and HOM[OSi(OtBu)₃]₃⁻ (where M=Al or Ga), were synthesized from anionic chlorides Li{M[OSi(OtBu)₃]₃Cl} in salt metathesis reactions. Sequestration of lithium cations with [12]crown-4 afforded charge-separated ion pairs composed of monomeric anions M[OSi(OtBu)₃]₄⁻ with outer-sphere [([12]crown-4)₂Li]⁺ cations, and hydroxides {HOM[OSi(OtBu)₃]₃} with pendant [([12]crown-4)Li]⁺ cations. These molecular models were characterized by single-crystal X-ray diffraction, vibrational spectroscopy, mass spectrometry and NMR spectroscopy. Upon treatment of monomeric [([12]crown-4)Li]{HOM[OSi(OtBu)₃]₃} complexes with benzyl alcohol, benzyloxide complexes were formed, modeling a possible pathway for the formation of active sites for Meerwin–Ponndorf–Verley (MPV) transfer hydrogenations with Al/Ga-doped silica catalysts.     

Microbiological Transformation of L-Tyrosine to L-Dopa from Methanol Pretreated Biomass of a Novel Coriolus versicolor under Submerged Culture

The present study is concerned with the microbiological transformation of L-tyrosine to L-dopa by a newly isolated turkey tail mushroom Coriolus versicolor DOB-4. As tyrosinase (catechol oxidase, EC 1.10.3.1) is an extracellular enzyme, therefore biomass was used as an enzyme source in the reaction mixture. Biomass particles were pretreated with methanol and oven dried at 105 °C for 2 h. The optimal L-dopa production was achieved when 1.5 mg/ml L-tyrosine was used as the basal substrate. Thin layer chromatography and high-performance liquid chromatography analysis depicted that citric acid supports higher substrate conversion and product formation rates. A noticeable enhancement was observed when process parameters viz. L-tyrosine concentration (1.5 mg/ml), citric acid (1.5 mg/ml), time of incubation (50 min), and reaction temperature (60 °C) were optimized using Plackett–Burman design. The maximum production of L-dopa was found to be 0.872 mg/ml with L-tyrosine consumption of 1.002 mg/ml. The model terms were found highly significant (HS, p?≤?0.05), suggesting the potential commercial utility of the culture (df?=?3, LSD?=?0.342).     

Enhancement of electrical properties due to Cr substitution in Co-ferrite nanoparticles synthesized by two chemical techniques

Nanocrystalline cobalt ferrites with nominal composition CoCr_xFe_2−xO₄ ranging from x=0.0 to 0.5 with step increment of 0.25 were prepared by sol–gel auto combustion and chemical co-precipitation techniques. A comparative study of structural, electrical and magnetic properties of these ferrites has been measured using different characterization techniques. Structural and micro-structural studies were measured using X-ray diffraction, Fourier transform infra-red spectroscopy (FTIR), scanning electron microscopy and atomic force microscopy. Crystallite sizes of the series are within the range of 12–29±2 nm. Lattice parameters decrease by increasing Cr³⁺ concentration. FTIR confirms the presence of two lattice absorption bands. DC electrical resistivity increases to a value of ∼10¹⁰ Ω-cm with increase in Cr³⁺ concentration, but the most significant increase is in samples prepared by sol–gel combustion. Dielectric properties have been measured as a function of frequency at room temperature. Dielectric loss decreases to 0.1037 and 0.0108 at 5 MHz for chemical co-precipitation and sol–gel combustion, respectively. Impedance measurements further helped in analyzing the electrical properties and to separate the grain and grain boundary resistance effects using a complex impedance analysis. Magnetic parameters were studied using a vibrating sample magnetometer in the applied field of 10 kOe. The saturation magnetization decreased from 63 to 10.8 emu/gm with increase in Cr³⁺ concentration.     

A Facile Method to Prepare Double‐Layer Isoporous Hollow Fiber Membrane by In Situ Hydrogen Bond Formation in the Spinning Line

A double‐layer hollow fiber is fabricated where an isoporous surface of polystyrene‐block‐poly(4‐vinylpyridine) is fixed on a support layer by co‐extrusion. Due to the sulfonation of the support layer material, delamination of the two layers is suppressed without increasing the number of subsequent processing steps for isoporous composite membrane formation. Electron microscope‐energy‐dispersive X‐ray spectroscopy images unveil the existence of a high sulfur concentration in the interfacial region by which in‐process H‐bond formation between the layers is evidenced. For the very first time, our study reports a facile method to fabricate a sturdy isoporous double‐layer hollow fiber.

     

Fluoro-substituted ketones from nitriles using acidic and basic reaction conditions

Fluoro-substituted aliphatic nitriles are shown to undergo the Houben-Hoesch reactions with arenes in CF₃SO₃H to give fluoro-substituted ketones in good yields. The fluorine substituents appear to enhance the reactivities of the nitriles (and the nitrilium ion intermediates) compared to similar aliphatic nitriles. Fluoro-substituted ketones are also shown to be accessible through the reactions of organometallic reagents and fluoro-substituted nitriles.     

Facile one-pot synthesis,butyrylcholinesterase and α-glucosidase inhibitory activities,structure–activity relationship,molecular docking and DNA–drug binding analysis of Meldrum’s acid derivatives

Research on Chemical Intermediates - Meldrum’s acid derivatives were facile synthesized by one-pot condensation process and characterized by NMR (1H, 13C, DEPT-90 and DEPT-135) and EI-MS. The...