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Through the l - to d - type amino acid substitution and attachment of solubilizing tags, the novel proteolysis-resistant and water-soluble fluorescent probes were developed, which could achieve the sensitive "turn on" sensing of heparin. [Display omitted] • The first systematic structural optimizations were conducted on the promising fluorescent probe TPE-1 for heparin sensing. • The novel d -type peptide based fluorescent probes were developed for the highly sensitive "turn on" sensing of heparin. • The representative heparin probe XH-6 was demonstrated to possess extremely high proteolytic stability and good solubility. Developing "turn on" fluorescent probes was desirable for the detection of the effective anticoagulant agent heparin in clinical applications. Through combining the aggregation induced emission (AIE) fluorogen tetraphenylethene (TPE) and heparin specific binding peptide AG73, the promising "turn on" fluorescent probe TPE-1 has been developed. Nevertheless, although TPE-1 could achieve the sensitive and selective detection of heparin, the low proteolytic stability and undesirable poor solubility may limit its widespread applications. In this study, seven TPE-1 derived fluorescent probes were rationally designed, efficiently synthesized and evaluated. The stability and water solubility were systematically estimated. Especially, to achieve real-time monitoring of proteolytic stability, the novel Abz/Dnp-based "turn on" probes that employ the internally quenched fluorescent (IQF) mechanism were designed and synthesized. Moreover, the detection ability of synthetic fluorescent probes for heparin were systematically evaluated. Importantly, the performance of d -type peptide fluorescent probe XH-6 indicated that d -type amino acid substitutions could significantly improve the proteolytic stability without compromising its ability of heparin sensing, and attaching solubilizing tag 2-(2-aminoethoxy) ethoxy) acid (AEEA) could greatly enhance the solubility. Collectively, this study not only established practical strategies to improve both the water solubility and proteolytic stability of "turn on" fluorescent probes for heparin sensing, but also provided valuable references for the subsequent development of enzymatic hydrolysis-resistant d -type peptides based fluorescent probes. [ABSTRACT FROM AUTHOR]

Extracellular vesicles are composed of loaded soluble substances and lipid bilayers; these include apoptotic bodies, exosomes, and microvesicles. Extracellular vesicles, as carriers of biological information between cells, have been recognized for their role in the diagnosis and treatment of cardiovascular diseases. The biogenesis of extracellular vesicles is closely related to autophagy. Moreover, extracellular vesicles further affect autophagy levels in target cells through their transmitted contents. Autophagy is a catabolic cell process that maintains cell homeostasis by eliminating misfolded proteins and damaged organelles. Existing studies have revealed that extracellular vesicles and autophagy share molecular mechanisms with notable crosstalk, including, perspectives such as amphisomes and "secretory autophagy." In this review, we first introduce the biogenesis of extracellular vesicles and the classic views of autophagy before moving onto the crosstalk between extracellular vesicles and autophagy. Finally, we discuss the research progress of extracellular vesicles and autophagy in cardiovascular pathophysiology. [ABSTRACT FROM AUTHOR]

Graphical abstract Abstract Inspired by steaming bread, a novel three dimensional N and S co-doped reduced graphene oxide (3D NS-rGO) foam is fabricated via a gas foaming method similar to steaming bread procedure, in which (NH 4) 2 S 2 O 3 is selected as the foaming agent as well as N and S source. Such cross-linked 3D structure not only has the high specific surface area also enable more transport channels for electrons/ions transport. Furthermore, introducing of N and S-containing functional groups creates lattice defects in graphene, which provides more active sites where the Faradaic pseudocapacitance occurs. Consequently, the electrochemical test of 3D NS-rGO sample in a three-electrode system demonstrates a high specific capacity of 306.3 F g−1 at 1 A g−1, two times higher than that of rGO prepared at the same temperature. Moreover, 3D NS-rGO sample reveals the superb cycling stability with less than 2% capacitance loss after 10,000 cycles and it exhibits potential application for high performance supercapacitors. [ABSTRACT FROM AUTHOR]

The cytotoxic peptide LVTX-8, recently isolated from spider Lycosa vittata , is considered as a potential precursor for further anticancer drug development. In this study, a series of novel LVTX-8-based analogues and cytotoxic conjugates were rationally designed, synthesized, and systematically evaluated. Compared with the parent LVTX-8, peptides 825 and 827 not only possessed higher proteolytic stability, but also exhibited significantly improved anticancer durability and greatly reduced hemolysis. [Display omitted] • Ten spider toxin peptide LVTX-8-based analogues were designed and efficiently synthesized. • Their anticancer efficacy, serum stability, hemolytic activity, time-kill kinetics, anticancer mode of action, and subcellular localizations were evaluated systematically. • In particular, peptides 825 and 827 not only possessed higher proteolytic stability, but also exhibited significantly improved anticancer durability. • In addition, peptides 825 and 827 exhibited greatly reduced hemolysis, as well as higher selectivity to cancer cells than to human erythrocytes. Cytotoxic peptides derived from spider venoms have been considered as promising candidates for anticancer treatment. The novel cell penetrating peptide LVTX-8, which is a 25-residue amphipathic α-helical peptide isolated from spider Lycosa vittata , exhibited potent cytotoxicity and is a potential precursor for further anticancer drug development. Nevertheless, LVTX-8 may be easily degraded by multiple proteases, inducing the proteolytic stability problem and short half-life. In this study, ten LVTX-8-based analogs were rationally designed and the efficient manual synthetic method was established by the DIC/Oxyma based condensation system. The cytotoxicity of synthetic peptides was systematically evaluated against seven cancer cell lines. Seven of the derived peptides exhibited high cytotoxicity towards tested cancer in vitro , which was better than or comparable to that of natural LVTX-8. In particular, both N -acetyl and C-hydrazide modified LVTX-8 (8 2 5) and the conjugate methotrexate (MTX)-GFLG-LVTX-8 (8 2 7) possessed more durable anticancer efficiency, higher proteolytic stability, as well as lower hemolysis. Finally, we confirmed that LVTX-8 could disrupt the integrity of cell membrane, target the mitochondria and reduce the mitochondrial membrane potential to induce the cell death. Taken together, the structural modifications were conducted on LVTX-8 for the first time and the stability significantly improved derivatives 825 and 827 may provide useful references for the modifications of cytotoxic peptides. [ABSTRACT FROM AUTHOR]

Abstract: Molecular self-assembly has become a versatile approach to create complex and functional nanoarchitectures. In this work, the self-assembly behavior of an anionic surfactant (sodium dodecylbenzene sulfonate, SDBS) and a hydrotropic salt (benzylamine hydrochloride, BzCl) in aqueous solution is investigated. Benzylamine hydrochloride is found to facilitate close packing of surfactants in the aggregates, inducing the structural transformation from SDBS micelles into unilamellar vesicles, and multilamellar vesicles. The multilamellar vesicles can transform into macroscale fibers, which are long enough to be visualized by the naked eye. Particularly, these fibers are robust enough to be conveniently separated from the surfactant solution. The combined effect of non-covalent interactions (e.g., hydrophobic effect, electrostatic attractions, and π–π interactions) is supposed to be responsible for the robustness of these self-assembled aggregates, in which π–π interactions provide the directional driving force for one-dimensional fiber formation. [Copyright &y& Elsevier]

Abstract: Branched alkylbenzenesulfonate gemini surfactants: sodium 6,6′-(propane-1,3-diylbis(oxy))bis(3-(2-propylpentyl)benzenesulfonate) (C8BC3C8B), sodium 6,6′-(propane-1,3-diylbis(oxy))bis(3-(3,5,5-trimethylhexyl)benzenesulfonate) (C9BC3C9B), and sodium 6,6′-(propane-1,3-diylbis(oxy))bis(3-(2,4,4-trimethylpentan-2-yl)benzenesulfonate) (T-C8BC3C8B) have been synthesized. Their interfacial activity and aggregation behavior in aqueous solution were studied by surface/interface tension measurement, electrical conductivity, isothermal titration microcalorimetry, 1H NMR spectroscopy, dynamic light scattering, steady-state fluorescence and cryogenic transmission electron microscopy. The critical aggregation concentration (CAC) and the minimum average surface area/molecule (A min) decrease with the decrease of the branching factor, i.e., in the order of T-C8BC3C8B, C8BC3C8B and C9BC3C9B. Moreover, alkyl side chain branches generate much more significant increases in CAC and A min for the gemini surfactants than single-chain surfactants. However, the branching factor does not change the air/water surface tension at CAC regularly. Instead, the air/water surface tension decreases with the increase of the carbon number of the hydrocarbon chains. In addition, it is noted that the branched gemini surfactants display high efficiency in reducing toluene/water interfacial tension. Interestingly, the increase in the branching factor leads to much more endothermic enthalpy of aggregation. All these three surfactants form spherical vesicles in aqueous solution and may present a parallel-displaced structure with a directional arrangement of the benzene ring in the vesicles. [Copyright &y& Elsevier]