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Synergistic bioassay-guided isolation of the extracts of Artemisia rupestris L, which belongs to the family Asteraceae, afforded two acetylenic spiroketal enol ethers, namely rupesdiynes A (1) and B (2). Their structures were determined based on spectroscopic analysis and experimental and calculated ECD investigations. The two compounds exhibited synergistic activity and were able to reduce the minimum inhibitory concentration (MIC) of oxacillin four-fold, with a fractional inhibitory concentration index (FICI) of 0.5 in combination with oxacillin against the oxacillin-resistant EMRSA-16. Biofilm formation inhibitory and Ethidium bromide (EtBr) efflux assay were further employed to verify the possible mechanism of the synergistic antibacterial effect. Additionally, molecular docking studies were conducted to investigate the binding affinities of the two compounds with penicillin-binding protein 2a (PBP2a) of EMRSA-16. Taken together, rupesdiynes A (1) and rupesdiyne B (2) showed moderate synergistic activity against EMRSA-16 with oxacillin via inhibiting biofilm formation and efflux pump activity, respectively. [ABSTRACT FROM AUTHOR]

Sorafenib (SF), a multi‐kinase inhibitor, is the first FDA‐approved systemic chemotherapy drug for advanced hepatocellular carcinoma (HCC). However, its clinical application is limited by severe toxicity and side effects associated with high applied doses. Sophora alopecuroides L. is traditionally used as Chinese herbal medicine for treating gastrointestinal diseases, bacillary dysentery, viral hepatitis, and other diseases, and exerts an important role in anti‐tumor. Hence, we investigated the synergistic actions of seventeen flavonoids from this herb combined with SF against HCC cell lines and their primary mechanism. In the experiment, most compounds were found to prominently enhance the inhibitory effects of SF on HCC cells than their alone treatment. Among them, three compounds leachianone A (1), sophoraflavanone G (3), and trifolirhizin (17) exhibited significantly synergistic anticancer activities against MHCC97H cells at low concentration with IC50 of SF reduced by 5.8‐fold, 3.6‐fold, and 3.5‐fold corresponding their CI values of 0.49, 0.66, and 0.46 respectively. Importantly, compounds 3 or 17 combined with SF could synergistically induce MHCC97H cells apoptosis via the endogenously mitochondrial‐mediated apoptotic pathway, involving higher Bax/Bcl‐2 expressions with the activation of caspase‐9 and ‐3, and arrest the cell cycle in G1 phases. Strikingly, this synergistic effect was also closely related to the co‐suppression of ERK and AKT signaling pathways. Furthermore, compound 3 significantly enhanced the suppression of SF on tumor growth in the HepG2 xenograft model, with a 79.3% inhibition ratio at high concentration, without systemic toxicity, compared to either agent alone. These results demonstrate that the combination treatment of flavonoid 3 and SF at low doses exert synergistic anticancer effects on HCC cells in vitro and in vivo. [ABSTRACT FROM AUTHOR]

This study seeks to discover flavonoids from a traditional Chinese herb, Artemisia rupestris L., with synergistic antibacterial effects against multidrug-resistant Staphylococcus aureus. Five flavonoids, artemetin (1), chrysosplenetin (2), pachypodol (3), penduletin (4) and chrysoeriol (5) were obtained by various column chromatographic methods. Their chemical structures were determined on the basis of comprehensive spectroscopic analysis and comparison with literature data. Three of the compounds (2, 4 and 5) exhibited synergistic activity when combined with norfloxacin against SA1199B, an effluxing fluoroquinolone-resistant strain. The fractional inhibitory concentration indices (FICIs) of 2, 4 and 5 in combination with norfloxacin were 0.375, 0.079 and 0.266 respectively, suggesting synergy. Compound 5 also showed synergistic effects against EMRSA-15 and EMRSA-16 when combined with ciprofloxacin and oxacillin exhibiting FICIs of 0.024 and 0.375 respectively. Real time ethidium bromide (EtBr) efflux assay, qRT-PCR and molecular docking were employed to explore the mechanisms of the synergistic effects. [ABSTRACT FROM AUTHOR]

A novel optimised isolation method, TLC-bioautography, was evaluated and utilised in this research. Antibacterial compounds which were isolated from the dichloromethane extract of Ferula ferulioides (Steud.) Korovin were detected by means of the method. Their structures were elucidated by extensive spectral and chemical methods. Their antibacterial activities against drug-resistant Staphylococcus aureus (S. aureus) strains were evaluated with broth microdilution method, and the results proved that TLC-bioautography was an effective and highly efficient way to screen natural compounds from plant extracts against drug-resistant strains. [ABSTRACT FROM AUTHOR]

Providing XML data service in could environment attracts more and more attentions. By introducing existed XQuery engine (such as saxon) into cloud environment, a XML data query service framework was implemented. To improve the efficiency of XML data query in cloud environment, an optimization method based of XPath projection is applied in the procedure of splitting XML data, only leaving the data related to XQuery statements. Experiments show that the optimization method effectively reduces both the data size and the query processing time of XML data service. [ABSTRACT FROM AUTHOR]

Multidrug-resistant Staphylococcus aureus , a Gram-positive bacterium that causes several difficult-to-treat human infections, is a considerable threat to global healthcare. We hypothesize that there exist inner responsive molecules (IRMs) which can function synergistically with antibiotics to restore the sensitivity of resistant bacteria to existing antibiotics without inducing new antibiotic resistance. An investigation of the extracts of the Chinese medicinal herb Piper betle L. led to the isolation of six benzoate esters, BO-1 - BO-6 . Among these, BO-1 as a distinct IRM displayed considerable synergism by potentiating antibacterial activity against five antibiotic-resistant S. aureus strains. Mechanistic studies demonstrated that BO-1 acted as a suppressing drug resistance IRM via inhibiting efflux activity. A combination of BO-1 with ciprofloxacin significantly inhibited resistance to this antibiotic and reversed its resistance in the S. aureus strain. Furthermore, BO-1 effectively enhanced the activity of ciprofloxacin against the efflux fluoroquinolone-resistant S. aureus strain SA1199B that caused infection in two animal models and significantly decreased the inflammatory factors IL-6 and C-reactive protein of the infected mice, thereby showing the practice utility of this approach.

A phytochemical investigation of an extract of the leaves of Piper betle , guided by a synergistic antibacterial screen, led to the isolation and structural elucidation of 10 new neolignans, Pibeneolignan A-J ( 1 - 10 ), together with 11 known compounds. The structures and absolute configurations of the new compounds were elucidated on the basis of spectroscopic data, single-crystal X-ray diffraction analysis, and experimental and calculated ECD investigations. Compounds 1 and 2 are new naturally occurring neolignan skeletons, based on the cyclohept-2-ene-1,4-dione framework. We propose that these natural products are biosynthetically formed from bicyclic [3.2.1] neolignans by oxidative cleavage and ring opening at C-1' and C-2'. Among these compounds, 9 , 13 , 15 , and 16 , in combination with norfloxacin against an effluxing S. aureus strain (SA1199B), exhibited significant synergistic activity with fractional inhibitory concentration indices (FICIs) of 0.078, 0.156, 0.125, and 0.25, respectively. Bacterial growth curves, ethidium bromide (EtBr) efflux, and qRt-PCR were further employed to verify their synergistic antibacterial mechanism. Furthermore, computational molecular modeling suggested the binding of compounds 14 - 17 and 19 to the active site of the modeled structure of the NorA efflux pump, which is the main efflux pump in SA1199B.

This study seeks to discover flavonoids from a traditional Chinese herb, Artemisia rupestris L., with synergistic antibacterial effects against multidrug-resistant Staphylococcus aureus . Five flavonoids, artemetin ( 1 ), chrysosplenetin ( 2 ), pachypodol ( 3 ), penduletin ( 4 ) and chrysoeriol ( 5 ) were obtained by various column chromatographic methods. Their chemical structures were determined on the basis of comprehensive spectroscopic analysis and comparison with literature data. Three of the compounds ( 2 , 4 and 5 ) exhibited synergistic activity when combined with norfloxacin against SA1199B, an effluxing fluoroquinolone-resistant strain. The fractional inhibitory concentration indices (FICIs) of 2, 4 and 5 in combination with norfloxacin were 0.375, 0.079 and 0.266 respectively, suggesting synergy. Compound 5 also showed synergistic effects against EMRSA-15 and EMRSA-16 when combined with ciprofloxacin and oxacillin exhibiting FICIs of 0.024 and 0.375 respectively. Real time ethidium bromide (EtBr) efflux assay, qRT-PCR and molecular docking were employed to explore the mechanisms of the synergistic effects.

To understand how soil texture and water content affect the mineralization of organic C in paddy soil, 3 selected soils (sandy loam, clay loam, and silty clay) were incubated (25 degrees C) with 14 C-labelled rice straw (1.0 g x kg(-1)) at water content varied from 45% to 105% of water holding capacity (WHC). Data indicated that, in the sandy loam and clay loam, the mineralization rate of 14 C-labelled rice straw reached the maximum at 75% WHC, as 53% and 58% of the straw C mineralized in the incubation period of 160 d, whereas in the silty clay, it increased gradually (from 41.8% to 49.0%) as water content increased up to 105% WHC. For all of the three soils, the mineralization rate of soil native organic C reached the maximum at 75% WHC, with 5.8% of the organic C mineralized in the same period for the sandy loam, and 8.0% and 4.8% for the clay loam and silty clay, respectively. As water content increased further, the mineralization rate of native organic C in the three soils significantly declined. The mineralization rate of added rice straw and native organic C in all the three soils, was well fitted with a conic curve. These results suggest that water-logging can decrease the mineralization of organic C in paddy soils.

An incubation test with three kinds of paddy soil (sandy loam, clay loam, and silty clay soils) in subtropical region was conducted at 10, 15, 20, 25 and 30 degrees C to examine the response of the mineralization of soil organic carbon (SOC) to temperature change. The results showed that during the period of 160 d incubation, the accumulative mineralized amount of SOC in sandy loam, clay loam, and silty clay soils at 30 degrees C was 3.5, 5.2 and 4.7 times as much as that at 10 degrees C, respectively. The mineralization rate was lower and relatively stable at lower temperatures (< or = 20 C), but was higher at the beginning of incubation and decreased and became stable as the time prolonged at higher temperatures (> or = 25 degrees C). During incubation, the temperature coefficient (Q10) of SOC mineralization in test soils fluctuated, with an average Q10 in sandy loam, clay loam, and silty clay soils being 1.92, 2.37 and 2.32, respectively. There was a positive exponential correlation between SOC mineralization constant k and temperature (P < 0.01), and the response of SOC mineralization to temperature change was in the order of clay loam soil > silty clay soil > sandy loam soil.