A series of amide tethered 4-aminoquinoline-naphthalimide hybrids has been synthesized to assess their in vitro antiplasmodial potential against chloroquine-susceptible (3D7) and ...chloroquine-resistant (W2) strains of Plasmodium falciparum. The most active and noncytotoxic compound had an IC50 value of 0.07 μM against W2 strain and was more active than standard antimalarial drugs, including chloroquine, desethylamodiaquine, and quinine, particularly for drug resistant malaria. The promising scaffold, when subjected to heme binding and molecular modeling studies, was identified as a possible potent inhibitor of hemozoin formation and P. falciparum chloroquine resistance transporter (PfCRT), respectively, and, therefore, could act as a dual function antiplasmodial.
The internal organs of vertebrates show distinctive left-right asymmetry. Leftward extracellular fluid flow at the node (nodal flow), which is generated by the rotational movement of node cilia, is ...essential for left-right patterning in the mouse and other vertebrates. However, the identity of the pathways by which nodal flow is interpreted remains controversial as the molecular sensors of this process are unknown. In the current study, we show that the medaka left-right mutant abecobe (abc) is defective for left-right asymmetric expression of southpaw, lefty and charon, but not for nodal flow. We identify the abc gene as pkd1l1, the expression of which is confined to Kupffer's vesicle (KV, an organ equivalent to the node). Pkd1l1 can interact and interdependently colocalize with Pkd2 at the cilia in KV. We further demonstrate that all KV cilia contain Pkd1l1 and Pkd2 and left-right dynein, and that they are motile. These results suggest that Pkd1l1 and Pkd2 form a complex that functions as the nodal flow sensor in the motile cilia of the medaka KV. We propose a new model for the role of cilia in left-right patterning in which the KV cilia have a dual function: to generate nodal flow and to interpret it through Pkd1l1-Pkd2 complexes.
Leveraging a recent method for spectrally-shaped random FM (RFM) waveform generation, in conjunction with a particular implementation of spread-spectrum signaling, a multi-user form of dual-function ...radar/communication (DFRC) is proposed that seeks to balance the disparate requirements of each function. Using a radar-amenable spread-spectrum multiple-access signaling scheme, receive dynamic range for sensing is preserved by exploiting high-dimensional (and thus separable) waveforms, which are specifically structured to convey encoded information in a manner that can be readily decoded at a communication receiver.
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There is no study on food-derived peptide with both anticoagulant and angiotensin I-converting enzyme inhibitory (ACEI) activities yet. In this work, the anticoagulant and ACEI ...activities of the casein hydrolysates released by pepsin digestion were evaluated for the first time to the best of our knowledge. Results indicated that the casein hydrolysate exhibited potent anticoagulant activity by prolonging the thrombin time (TT) and the activated partial thromboplastin time (APTT). Compared with control samples, at 10mg/mL, the TT and APTT of casein hydrolysate were 186.0 % ± 6.6 % and 163.5 % ± 7.4 %, respectively. The casein hydrolysate also showed a strong ACEI activity with an IC50 value of 1.775mg/mL. The components of the bioactive casein hydrolysate were analyzed by nanoscale liquid chromatography quadrupole time-of-flight tandem mass spectrometry (NanoLC-Q-TOF-MS/MS). Total of 115 peptides were identified, among which 34, 9, 55 and 17 peptides were derived from αs1-, αs2-, β-, and κ-casein, respectively. The results of PeptideRanker and PepSite 2 analysis showed that 6 peptides (FRQFYQL, NENLLRF, NPWDQVKR, PVVVPPFLQ, PVRGPFPIIV, and ARHPHPHLSF) have both ACEI and anticoagulant activities by binding to the active sites of ACE and thrombin. This study indicated that casein is a potential functional food supplement that can be used for medical purposes.
In this letter, we develop a new framework to design optimal waveform in a radar-communication system for maximizing its communication performance subject to a constraint on its detection ...performance. The novelty of our newly developed framework lies in that our detection constraint is expressed as the radar detection probability being greater than or equal to a specific value for a given false alarm probability, while this constraint was directly put on the waveform. Our framework can significantly outperform two benchmark schemes in terms of achieving a higher average sum rate subject to guaranteeing the same detection performance.
The potassium salts of carboxylic acids are developed as efficient carboxylating agents through CO2 exchange. We describe these carboxylates as dual‐function reagents because they function as a ...combined source of CO2 and base/metalating agent. By using the salt of a commercially available carboxylic acid, this protocol overcomes difficulties when using CO2 gas or organometallic reagents, such as pressurized containers or strictly inert conditions. The reaction proceeds under mild conditions, does not require transition metals or other additives, and shows broad substrate scope. Through the preparation of several biologically important molecules, we show how this strategy provides an opportunity for isotope labeling with low equivalents of labeled CO2.
The potassium salt of triphenylacetic acid is developed as a combined source of CO2 and base/metalating agent. This method avoids specialized equipment and is used in the carboxylation of a range of compound classes. This provides a mechanistically distinct approach to carboxylation that has also been applied in carbon isotope labeling.
DY Gao solely or together with some of his collaborators applied his Canonical duality theory (CDT) for solving a class of unconstrained optimization problems, getting the so-called triality ...theorems. Unfortunately, the 'double-min duality' from these results published before 2010 revealed to be false, even if in 2003 DY Gao announced that 'certain additional conditions' are needed for getting it. After 2010 DY Gao together with some of his collaborators published several papers in which they added additional conditions for getting 'double-min' and 'double-max' dualities in the triality theorems. The aim of this paper is to treat rigorosly this kind of problems and to discuss several results concerning the 'triality theory' obtained up to now.
An integrated design consisting of a multiple-input-multiple-output (MIMO) antenna system for fourth generation applications and a planar connected array (PCA) for fifth generation applications is ...presented. The proposed design contains a 4-element printed-inverted-F antenna-based MIMO antenna system and a slot-based PCA. The antenna system is fabricated on a commercially available RO-4350 substrate with ${\rm \epsilon }_r$ ϵ r equal to 3.5. The dimensions of the board are 100 × 60 × 0.76 mm3 representing a typical smart phone backplane size. The antenna system covers 2.1 and 12.5 GHz frequency bands via its MIMO and PCA parts, respectively. The design is planar, low profile and compact in structure that is suitable for wireless handheld devices and mobile terminals. The PCA also serves as a defected ground structure at 2.1 GHz thus having two functions. Isolation is improved by at least 4 dB. The PCA consists of a 4 × 3 radiating slots fed via a corporate feed structure. The measured gain and efficiency values at the centre frequency are at least 3.4 dBi and 74%, respectively, for the MIMO antenna system and 8 dBi and 80% for the PCA. The envelope correlation coefficient did not exceed 0.2824 for all antennas showing good MIMO performance.
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•Hierarchical antibacterial surface was constructed via living SI-PIMP.•Antifouling and bactericidal functions were integrated in a hierarchical surface.•The pQAC layer was facilely ...adjusted to optimize the final performance.•Optimized hierarchical surface showed long-lasting antibacterial performance.
Bacterial infections are problematic in many healthcare-associated devices. Antibacterial surfaces integrating the strength of bacteria repellent and bactericidal functions exhibit an encouraging efficacy in tackling this problem. Herein, a hierarchical dual-function antibacterial polymer brush coating that integrates an antifouling bottom layer with a bactericidal top layer is facilely constructed via living photograft polymerization. Excellent resistance to bacterial attachment is correlated with the antifouling components, and good bactericidal activity is afforded by the bactericidal components, and therefore the hierarchical coating shows an excellent long-term antibacterial capability. In addition, due to the presence of the hydrophilic background layer, the hierarchical surface has the greatly improved biocompatibility, as shown by the suppression of platelet adhesion and activation, the inhibition of erythrocyte adhesion and damage, and low toxicity against mammalian cells. The hierarchical polymer brush system provides the basis for the development of long-term antibacterial and biocompatible surfaces.
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