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排序方式: 共有421条查询结果,搜索用时 15 毫秒
101.
Emmanuel T. Oluwabusola Nursheena Parveen Katermeran Wee Han Poh Teo Min Ben Goh Lik Tong Tan Oluwatofunmilayo Diyaolu Jioji Tabudravu Rainer Ebel Scott A. Rice Marcel Jaspars 《Molecules (Basel, Switzerland)》2022,27(5)
Natural products derived from marine sponges have exhibited bioactivity and, in some cases, serve as potent quorum sensing inhibitory agents that prevent biofilm formation and attenuate virulence factor expression by pathogenic microorganisms. In this study, the inhibitory activity of the psammaplin-type compounds, psammaplin A (1) and bisaprasin (2), isolated from the marine sponge, Aplysinella rhax, are evaluated in quorum sensing inhibitory assays based on the Pseudomonas aeruginosa PAO1 lasB-gfp(ASV) and rhlA-gfp(ASV) biosensor strains. The results indicate that psammaplin A (1) showed moderate inhibition on lasB-gfp expression, but significantly inhibited the QS-gene promoter, rhlA-gfp, with IC50 values at 14.02 μM and 4.99 μM, respectively. In contrast, bisaprasin (2) displayed significant florescence inhibition in both biosensors, PAO1 lasB-gfp and rhlA-gfp, with IC50 values at 3.53 μM and 2.41 μM, respectively. Preliminary analysis suggested the importance of the bromotyrosine and oxime functionalities for QSI activity in these molecules. In addition, psammaplin A and bisaprasin downregulated elastase expression as determined by the standard enzymatic elastase assay, although greater reduction in elastase production was observed with 1 at 50 μM and 100 μM. Furthermore, the study revealed that bisaprasin (2) reduced biofilm formation in P. aeruginosa. 相似文献
102.
Hailong Zhang Shiqi Hong Sarah Si Kai Tan Tao Peng Lucas Yuan Hao Goh Kwan Hang Lam Keat Theng Chow Rajeev Gokhale 《Molecules (Basel, Switzerland)》2022,27(19)
Polysorbates (PS 20 and PS 80) are the most widely used surfactants in biopharmaceutical formulations to protect proteins from denaturation, aggregation, and surface adsorption. To date, around 70% of marketed therapeutic antibodies contain either PS 20 or PS 80 in their formulations. However, polysorbates are chemically diverse mixtures, which are prone to degradation by oxidation and hydrolysis to produce peroxides and fatty acids, which, in turn, induce protein oxidation, aggregation, and insoluble particle formation. These will negatively impact protein quality and stability. Thus, polysorbate degradation has emerged as one of the major challenges in the development and commercialization of therapeutic protein products. KLEPTOSE® HPβCD (hydroxypropyl beta-cyclodextrin), a new multifunctional excipient, has been shown to provide protein stabilization functions in biopharmaceutical downstream processes and in their final formulations. This study aims to evaluate HPβCD, a new molecule of its class, against polysorbates as a stabilizer in biologics formulations. In this study, the chemical stability of KLEPTOSE® HPβCDs is compared with polysorbates (20 and 80) under various stress conditions. When subjected to heat stress, HPβCDs show little change in product recovery (90.7–100.7% recovery for different HPβCDs), while polysorbates 20 and 80 show significant degradation, with only 11.5% and 7.3% undegraded product remaining, respectively. When subjected to other chemical stressors, namely, autoclave, light, and oxidative stresses, HPβCD remains almost stable, while polysorbates show more severe degradation, with 95.5% to 98.8% remaining for polysorbate 20 and 85.5% to 97.4% remaining for polysorbate 80. Further, profiling characterization and degradation analysis reveal that chemical structures of HPβCDs remain intact, while polysorbates undergo significant hydrolytic degradation and oxidation. Lastly, the physicochemical stability of monoclonal antibodies in formulations is investigated. When subjected to light stress, adalimumab, as a model mAb, formulated in the presence of HPβCD, shows a significant decrease in protein aggregation, and superior monomer and total protein recovery compared to PS 80-containing formulations. HPβCD also reduces both agitation and thermal stress-induced protein aggregation and prevents subvisible particle formation compared to PS 80. 相似文献
103.
Noresah Said Kar Chun Wong Woei Jye Lau Ying Siew Khoo Yin Fong Yeong Nur Hidayati Othman Pei Sean Goh Ahmad Fauzi Ismail 《Molecules (Basel, Switzerland)》2022,27(23)
Most researchers focused on developing highly selective membranes for CO2/CH4 separation, but their developed membranes often suffered from low permeance. In this present work, we aimed to develop an ultrahigh permeance membrane using a simple coating technique to overcome the trade-off between membrane permeance and selectivity. A commercial silicone membrane with superior permeance but low CO2/CH4 selectivity (in the range of 2–3) was selected as the host for surface modification. Our results revealed that out of the three silane agents tested, only tetraethyl orthosilicate (TEOS) improved the control membrane’s permeance and selectivity. This can be due to its short structural chain and better compatibility with the silicone substrate. Further investigation revealed that higher CO2 permeance and selectivity could be attained by coating the membrane with two layers of TEOS. The surface integrity of the TEOS-coated membrane was further improved when an additional polyether block amide (Pebax) layer was established atop the TEOS layer. This additional layer sealed the pin holes of the TEOS layer and enhanced the resultant membrane’s performance, achieving CO2/CH4 selectivity of ~19 at CO2 permeance of ~2.3 × 105 barrer. This performance placed our developed membrane to surpass the 2008 Robeson Upper Boundary. 相似文献
104.
The aim of this study was to investigate the cytotoxic and apoptotic effects of Nephelium ramboutan-ake (pulasan) rind in selected human cancer cell lines. The crude ethanol extract and fractions (ethyl acetate and aqueous) of N. ramboutan-ake inhibited the growth of HT-29, HCT-116, MDA-MB-231, Ca Ski cells according to MTT assays. The N. ramboutan-ake aqueous fraction (NRAF) was found to exert the greatest cytotoxic effect against HT-29 in a dose-dependent manner. Evidence of apoptotic cell death was revealed by features such as chromatin condensation, nuclear fragmentation and apoptotic body formation. The result from a TUNEL assay strongly suggested that NRAF brings about DNA fragmentation in HT-29 cells. Phosphatidylserine (PS) externalization on the outer leaflet of plasma membranes was detected with annexin V-FITC/PI binding, confirming the early stage of apoptosis. The mitochondrial permeability transition is an important step in the induction of cellular apoptosis, and the results clearly suggested that NRAF led to collapse of mitochondrial transmembrane potential in HT-29 cells. This attenuation of mitochondrial membrane potential (Δψm) was accompanied by increased production of ROS and depletion of GSH, an increase of Bax protein expression, and induced-activation of caspase-3/7 and caspase-9. These combined results suggest that NRAF induces mitochondrial-mediated apoptosis. 相似文献
105.
Unprecedented Acid‐Promoted Polymerization and Gelation of Acrylamide: A Serendipitous Discovery 下载免费PDF全文
Siew Yin Chan Dr. Shermin S. Goh Dr. Qingqing Dou Benjamin Qi Yu Chan Dr. Wee Sim Choo Prof. David James Young Prof. Xian Jun Loh 《化学:亚洲杂志》2018,13(14):1797-1804
Dilute acid polymerizes degassed, aqueous acrylamide with concomitant gelation, without the need for added free radical initiator or cross‐linking agent. This reaction is accelerated by sonication or UV irradiation, but inhibited by adventitious oxygen or the addition of a free radical inhibitor, suggesting an acid‐accelerated free radical process. The resulting hydrogels are thixotropic in nature and partially disrupted by the addition of chaotropic agents, indicating the importance of hydrogen bonding to the 3D network. This discovery was made while trying to prepare pectin‐polyacrylamide hydrogels. We observed that pectin initiated the gelation of acrylamide, but only if the aqueous pectin samples had a pH lower than ca. 5. 相似文献
106.
Glen B. Deacon Prof. Dr. Lai Yoong Goh Prof. Dr. W. Roy Jackson Brian W. Skelton Wei Chen Allan H. White 《无机化学与普通化学杂志》2010,636(8):1478-1483
Monomeric manganese(II) complexes of bulky alkyl/ aryl‐substituted phenoxides, [Mn{C6HnRmO}2(DME)] [ 1 : R = C6H5, n = 3, m = 2 (2,6); 2 : R = Me3C, n = 3, m = 2 (2,6); 3 : R = Me3C, n = 2, m = 3 (2,4,6)] were prepared in yields of 37, 44 and 72 %, respectively, from the reaction of manganese powder, Hg(C6F5)2 and the corresponding phenol in the presence of a little mercury in dimethoxyethane (DME). The compounds were characterized spectroscopically and by magnetic measurements. The single crystal structures of 1 and 3 and also of the mixed phenoxide complex [Mn{(C6H3(C6H5)2‐2,6‐O}{C6H3(Me3C)2‐2,6‐O}(DME)] 4 are reported. 相似文献
107.
108.
109.
Jesus Felix Valenzuela Christopher Monterola Erika Fille Legara Xiuju Fu Rick Siow Mong Goh 《Complexity》2015,21(1):283-295
We examine the transmission of entities from the peripheries of scale‐free networks toward their centers when the nodes of the network have finite processing capabilities. We look at varying network utilization, U and find that clogging of the network sets in after a threshold value has been exceeded, and that the congestion sets in at the downstream nodes (those nearer to the collector) having large numbers of upstream neighbors. Investigation of the question of the degree of correlation of several characteristics of scale‐free networks (such as the average path length to the collector <l(min)> and the average clustering coefficient ) with the dynamics of centripetal flow in them reveals a negative answer: any correlation is indirect and will manifest in the number of producer nodes (which dictate the effective heaviness of the flow) and the interconnectedness of the feeder nodes, those nodes which are immediate neighbors of the collector node. An examination of reinforcement strategies shows dramatic improvements in both the finishing rate, and the average total transmission time, when the more centrally‐placed nodes are reinforced first, showing that the entities spend a large amount of their lifetime waiting in line at those nodes (which constitute the bottlenecks in the network) compared to the nodes in the periphery. Our results reinforce the importance of a network's hubs and their immediate environs, and suggest strategies for prioritizing elements of a network for optimization. © 2014 Wiley Periodicals, Inc. Complexity 21: 283–295, 2015 相似文献
110.
We provide a refined convergence analysis for the SAA (sample average approximation) method applied to stochastic optimization
problems with either single or mixed CVaR (conditional value-at-risk) measures. Under certain regularity conditions, it is
shown that any accumulation point of the weak GKKT (generalized Karush-Kuhn-Tucker) points produced by the SAA method is almost
surely a weak stationary point of the original CVaR or mixed CVaR optimization problems. In addition, it is shown that, as
the sample size increases, the difference of the optimal values between the SAA problems and the original problem tends to
zero with probability approaching one exponentially fast. 相似文献