Latest ArticlesWe constructed a reaction-based near-infrared fluorescent probe (Niap) to specifically identify alkaline phosphatase (ALP) with fast red fluorescence enhancement. Based on the positive concentration-dependent manner between the fluorescent intensity of the Niap and ALP, probe Niap was used to study the ALP enrichment and variation in golden apple snails (Pomacea canaliculata) exposed to the molluscicide candidate PPU06. After treatment with different concentrations of PPU06 over various times, three organs of the surviving snails, liver, stomach and plantaris, were frozen and sectioned for fluorescent imaging experiments. With increased PPU06 concentration, red fluorescence substantially increased in the liver and reached a maximum within 24 h when the PPU06 concentration was 0.75 mg/L. No obvious changes in the stomach or foot plantaris were found. It showed PPU06 caused liver injury and stimulated the increase of ALP in the liver of P. canaliculata. This study demonstrates a rapid ALP fluorescent identification method that can be used to study the effects of PPU06 on P. canaliculata. It also provides optical evidence that may aid in the discovery of new chemistry for snail control.
Although the antitumor drug cabazitaxel shows great therapeutic potential, its high toxicity and poor water solubility limit its utility. However, the use of stimuli-responsive prodrugs is a promising strategy for overcoming these limitations. Herein, we report the synthesis of two highly water soluble, acid-sensitive PEGylated acyclic-ketal-linked cabazitaxel prodrugs (PKCs) with improved antitumor efficacy. In an acidic tumor microenvironment, the PKCs hydrolyzed rapidly to release the native drug, whereas they were stable in the normal physiological environment. Compared with cabazitaxel injection, the PKCs had much higher maximum tolerated doses; and in an MDA-MB-231 subcutaneous xenograft nude mouse model, the PKCs showed better antitumor efficacy and safety than cabazitaxel injection. The prodrug strategy reported herein could be useful for the development of other water soluble, acid-sensitive prodrugs with improved efficacy.
In the past few years, photo-crosslinkable hydrogels have drawn a great attention in tissue engineering applications due to their high biocompatibility and extracellular matrix (ECM)-like structure. They can be easily biofabricated through exposure of a photosensitive system composed of photo-crosslinkable hydrogels, photo-initiators and other compounds such as cells and therapeutic molecules, to ultraviolet or visible light. With the development of biofabrication methods, many researchers studied the biological applications of photo-crosslinkable hydrogels in tissue engineering, such as vascular, wound dressing and bone engineering. This review highlights the biomaterials for photo-crosslinkable hydrogels, biofabrication techniques and their biological applications in tissue engineering. Meanwhile, the challenges and prospects of photo-crosslinkable hydrogels are discussed as well.
Quaternary ammonium salts (QASs) are excellent candidates for treating stubborn bacterial infections caused by biofilms due to their high sterilization efficiency and potential inhibition of the development of drug resistance. However, the inherent toxicity of QASs, including cytotoxicity, protein absorption and hemolysis, severely limits their applications in vivo. Herein, a charge-convertible quaternary ammonium salt-based micelle (QAS-SL@CM) was constructed by co-assembly of two amphiphiles with opposite charges and shell cross-linking strategy. The toxicity of the QAS-SL@CM could be greatly reduced towards human cells contrast to the corresponding QASs. By response to the acidic environment at infection sites, the surface charge of QAS-SL@CM could be immediately changed to positive and then target to negatively charged bacteria. Furthermore, β-thiopropionate bonds on QAS-SL@CM could also be disintegrated under acid environment to release QASs to kill bacteria. Importantly, the QAS-SL@CM showed significant therapeutic effect in mice subcutaneous abscesses models without interference with normal cells. Therefore, a surface adaptive micelle constructed by charge-convertible strategy has been developed to overcome the cytotoxicity of QASs, and could intelligently respond to the microenvironment of infected wound for in vivo infection therapy, which shows promising application in clinic.
Since the discovery of left-handed G-quadruplex (L-G4) structure formed by natural DNA, there has been a growing interest in its potential functions. This study utilised it to catalyse enantioselective Diels-Alder reactions, considering its different optical rotation compared to an ordinary G4. It was determined that when L-G4 was used with a combination of copper(Ⅱ) ions, there was a good enantioselectivity (-52% ee) without further addition of ligands. When further consideration was given by adding G4 ligands, G4 was further stabilised, even obtaining a better enantioselectivity (up to -80% ee). Moreover, when using ligands that have regulatory effects on G4, the ee value can be adjusted. In this work, a minimal left-handed G4 was reported. A follow-up study was also conducted, which recovers that the minimal left-handed G4 remains its catalytic effect and enantioselectivity, but is not so effective as the former case. This indicates that a complete G4 structure is relatively conducive to chiral catalysis.
Nanomaterial based drug delivery system have received great attention in clinical application due to their high therapeutic efficacy and lower side effects than classical method, multi-functional nanomaterial also have shown the excellent performance at cancer theranostic and durg tracking in vivo and in vitro. However, most of these works are influenced by the bio-toxicity of applied nanomaterials, which could influence the diagnostic results and treatment effect. Therefore, we have prepared a high biocompatibility porous carbon nanospheres (PCNs) based nano-system (PCN-siRNA-DOX-FA) for targeted drug delivery and theranostic. The surface modifications have increased dispersion and stability of the PCNs, and folic acid (FA) had enhanced the active target ability for FA receptor positive cell lines. Moreover, through the siRNA structure and doxorubicin (DOX) loading, biological and chemical combined multi-therapy was achieved in cancerous cells. This constructed nano-system could positively improve the biotoxicity problem of nanomaterial and provide a potential platform for clinical cancer theranostic applications.
An efficient approach to sulfur-bridged imidazopyridines has been developed under metal-free conditions using inexpensive sulfur powder as the sulfur source. Most appealingly, the reaction can proceed smoothly without addition of any additives, ultimately decreasing the production of chemical waste. The inexpensive and green method should provide a useful strategy for constructing a library of novel and biological interesting heteroaromatic sulfides.
Based on 4-bromo-1, 8-naphthalic anhydride, one novel ratiometric fluorescence H2S-probe (IDNA) was designed and synthesized. Further studies indicate that IDNA can sensitively recognize H2S (detection limit of 7 μmol/L) with good selectivity and anti-interference ability. In addition, IDNA has satisfactory photostability in HeLa cells, ability of mitochondrial co-localization, and can be utilized in fluorescence imaging of H2S.
Autophagy plays a vital role in maintaining the balance of normal physiological state of living cells. In this paper, a polarity-specific two-photon fluorescent probe Lyso-NA based on naphthalimide was synthesized for the purpose of monitoring autophagy during biological research. The results of photophysical properties and theoretical calculation confirmed that different polarities of solvents mainly effected fluorescent intensities of probe. Fluorescent intensity, quantum yield and fluorescence lifetime of probe kept a good linear relationship with polarity respectively. In addition, due to its low toxicity and selective accumulation in lysosomes, Lyso-NA is suitable for detecting changes in lysosomal polarity of living cells. Compare with the imaging results of plasmid transfection, a better performed real-time long-term fluorescent visualization of autophagy in living cells was achieved. Probe Lyso-NA can work as an efficient and cost effective imaging tool for visualizing autophagy in living cells.
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