ABSTRACT
A new superphane, featuring an aesthetically pleasing structure, was successfully obtained via one-pot synthesis of a hexakis-amine and m-phthalaldehyde in a [2+6] manner. It proved capable of entrapping a water dimer within its cavity as inferred from the mass spectroscopy, crystallographical analysis, NMR spectroscopy, and theoretical calculations.
Subject(s)
Aldehydes/chemical synthesis , Amines/chemical synthesis , Density Functional Theory , Water/chemistry , Aldehydes/chemistry , Amines/chemistry , Capsules , Dimerization , Magnetic Resonance Spectroscopy , Molecular StructureABSTRACT
Calix[4]pyrrole 1 can form host-guest complexes with certain thallium salts, for example, TlF, not only in the gas phase but also in solution and in the solid state. The complexation of TlF by calix[4]pyrrole 1 was found to promote self-assembly and the formation of well-defined and highly ordered fibrous supramolecular morphologies, as revealed by polarizing microscopy and scanning electron microscopy. The findings reported here serve to broaden the scope of cationic substrates that may be complexed as ion pairs by calix[4]pyrrole receptors while setting the stage for the development of new hosts for thallium(I) salts.
ABSTRACT
Two new naphthoate derivatives, including a symmetrical dimer (1) and a monomer (2), were separated from the roots of Morinda officinalis var. hirsuta. Their structures were characterized on the basis of spectroscopic means especially MS and NMR methods. Biological evaluations revealed that the two compounds did not show inhibition against both cholinesterases AChE and BChE, while the dimer (1) did exhibit moderate growth inhibitory activity toward one human osteosarcoma cell line U2OS with an IC50 value of 18.5 ± 1.1 µM.
Subject(s)
Morinda , Rubiaceae , Acetylcholinesterase , Cholinesterase Inhibitors/pharmacology , Humans , Molecular Structure , Plant RootsABSTRACT
Cadmium (Cd) is an established carcinogen that is involved in the progression of lung cancer. However, the mechanisms underlying this Cd-induced process have yet to be fully elucidated. The present study explored the potential roles of phosphorylated (p)-ERK in the Cd-induced migration and invasion of lung cancer cells. An MTT assay was performed to evaluate cell viability whilst western blot analysis and reverse transcription-quantitative PCR were used to detect the expression of protein and mRNA, respectively. Migration and invasion assays were performed to assess cell migratory and invasive abilities. The results demonstrated that exposure to Cd increased the expression of p-ERK in A549 cells. Cd also enhanced the migration and invasion of A549 cells, which could be blocked via U0126 treatment (an inhibitor of mitogen activated protein kinase). In addition, it was identified that Cd-induced expression of matrix metalloproteinases 2 mRNA was mediated by p-ERK. In conclusion, the present findings indicated that Cd induced A549 cell migration and invasion by activating ERK, and it was hypothesized that p-ERK could serve as a target in the clinical treatment of Cd-induced lung cancer.
ABSTRACT
Drug-resistant bacteria has been a threat to public life and property. We described the trends and changes in antibiotic resistance of important pathogens in a general hospital in Zhengzhou, China from 2011 to 2016, to control antimicrobial-resistant bacteria in hospital and provide support to clinicians and decision-making departments. Five dominant bacteria were enrolled based on the data from the general hospital during 6 years. The results of antimicrobial susceptibility testing were interpreted according to Clinical and Laboratory Standards Institute (CLSI). From 2011 to 2016, a total of 19,260 strains of bacteria were isolated, of which Klebsiella pneumoniae, Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Acinetobacter baumannii accounted for 51.98%. The resistance rate of K. pneumoniae and E. coli to carbapenem was less than 15%, but resistance of K. pneumoniae to carbapenems increased with time and resistance of E. coli to meropenem increased. The rate of extended-spectrum beta-lactamase (ESBL) production among K. pneumoniae and E. coli was decreasing. For most antibiotics, the resistance rate of ESBL-positive isolates was higher than that of ESBL-negative isolates, excluding carbapenems and cefoxitin. For S. aureus, the rate of methicillin-resistant S. aureus (MRSA) was stable. Resistance of S. aureus to mostly antibiotics decreased with time. Besides polymyxin B, P. aeruginosa and A. baumannii showed high resistance to other antibiotics. For A. baumannii, the resistance rate to mostly antibiotics was increasing. The bacteria showed high levels of resistance and multiple drug resistance. Continuous surveillance and optimizing the use of antibiotics are essential.Drug-resistant bacteria has been a threat to public life and property. We described the trends and changes in antibiotic resistance of important pathogens in a general hospital in Zhengzhou, China from 2011 to 2016, to control antimicrobial-resistant bacteria in hospital and provide support to clinicians and decision-making departments. Five dominant bacteria were enrolled based on the data from the general hospital during 6 years. The results of antimicrobial susceptibility testing were interpreted according to Clinical and Laboratory Standards Institute (CLSI). From 2011 to 2016, a total of 19,260 strains of bacteria were isolated, of which Klebsiella pneumoniae, Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Acinetobacter baumannii accounted for 51.98%. The resistance rate of K. pneumoniae and E. coli to carbapenem was less than 15%, but resistance of K. pneumoniae to carbapenems increased with time and resistance of E. coli to meropenem increased. The rate of extended-spectrum beta-lactamase (ESBL) production among K. pneumoniae and E. coli was decreasing. For most antibiotics, the resistance rate of ESBL-positive isolates was higher than that of ESBL-negative isolates, excluding carbapenems and cefoxitin. For S. aureus, the rate of methicillin-resistant S. aureus (MRSA) was stable. Resistance of S. aureus to mostly antibiotics decreased with time. Besides polymyxin B, P. aeruginosa and A. baumannii showed high resistance to other antibiotics. For A. baumannii, the resistance rate to mostly antibiotics was increasing. The bacteria showed high levels of resistance and multiple drug resistance. Continuous surveillance and optimizing the use of antibiotics are essential.
Subject(s)
Anti-Bacterial Agents/pharmacology , Bacteria/drug effects , Bacteria/isolation & purification , Bacterial Infections/microbiology , Drug Resistance, Bacterial , China , Hospitals, General , Humans , Microbial Sensitivity TestsABSTRACT
Seven new pentacyclic triterpenoids including six ursane-type, marinoids A-F (1-6), and one oleanane-type, marinoid G (7), along with five known analogues (8-12), were separated from the roots of Morinda officinalis var. officinalis. Their structures were assigned by spectroscopic means especially analysis of 2D NMR data, with the absolute configurations of 1 and 2 being determined via comparison of their experimental ECD spectra with the computed ones. Selective compounds displayed cytotoxic activity against two human osteosarcoma cell lines and also antibacterial effects against one Gram positive and one Gram negative strains.
Subject(s)
Anti-Bacterial Agents/pharmacology , Morinda/chemistry , Triterpenes/pharmacology , Anti-Bacterial Agents/isolation & purification , Cell Line, Tumor , China , Humans , Molecular Structure , Oleanolic Acid/analogs & derivatives , Oleanolic Acid/isolation & purification , Oleanolic Acid/pharmacology , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Plant Roots/chemistry , Triterpenes/isolation & purificationABSTRACT
Five new chromone derivatives, arthones Aâ»E (1â»5), together with eight known biogenetically related cometabolites (6â»13), were isolated from a deep-sea-derived fungus Arthrinium sp. UJNMF0008. Their structures were assigned by detailed analyses of spectroscopic data, while the absolute configurations of 1 and 5 were established by electronic circular dichroism (ECD) calculations and that of 2 was determined by modified Mosher ester method. Compounds 3 and 8 exhibited potent antioxidant property with DPPH and ABTS radical scavenging activities, with IC50 values ranging from 16.9 to 18.7 µM. Meanwhile, no compounds indicated obvious bioactivity in our antimicrobial and anti-inflammatory assays at 50.0 µM.
Subject(s)
Aquatic Organisms/chemistry , Chromones/pharmacology , Xylariales/chemistry , Animals , Bacteria/drug effects , Carbon-13 Magnetic Resonance Spectroscopy , Chromones/chemistry , Fungi/drug effects , Mice , Microbial Sensitivity Tests , Proton Magnetic Resonance Spectroscopy , RAW 264.7 CellsABSTRACT
Eight new 4-hydroxy-2-pyridone alkaloids arthpyrones Dâ»K (1â»8), along with two known analogues apiosporamide (9) and arthpyrone B (10), were isolated from a deep-sea-derived fungus Arthrinium sp. UJNMF0008. The structures of the isolated compounds were elucidated on the basis of spectroscopic methods with that of 1 being established by chemical transformation and X-ray diffraction analysis. Compounds 1 and 2 bore an ester functionality linking the pyridone and decalin moieties first reported in this class of metabolites, while 3 and 4 incorporated a rare natural hexa- or tetrahydrobenzofuro[3,2-c]pyridin-3(2H)-one motif. Compounds 3â»6 and 9 exhibited moderate to significant antibacterial activity against Mycobacterium smegmatis and Staphylococcus aureus with IC50 values ranging from 1.66â»42.8 µM, while 9 displayed cytotoxicity against two human osteosarcoma cell lines (U2OS and MG63) with IC50 values of 19.3 and 11.7 µM, respectively.