Latest ArticlesInfectious diseases become one of the leading causes of human death. Traditional treatment based on classical antibiotics could not provide enough antibacterial activity to combat bacterial infections due to low bioavailability, even leading to antibiotic resistance. In recent years, biomimetic delivery systems have been developed to improve drug therapy for various diseases, such as malignant tumor and cardiovascular disease. In this work, we designed virus-inspired nanodrugs (VNDs) through co-assembly of amphiphilic lipopeptide dendrons and poly(lactic-co-glycolic acid) polymers for high-efficiency antibiotic delivery. These VNDs had well-defined and stable nanostructures for tetracycline encapsulation and delivery. The VNDs were capable of promoting antibiotic internalization and enhancing their antibacterial effects against Gram-negative Escherichia coli and Gram-positive Staphylococcus aureus. Additionally, no obvious cytotoxicity of VNDs was observed to human cell lines. This work successfully demonstrated the virus-mimetic nanoparticles served as promising and applicable antibiotic delivery platform for antibacterial treatment.
Thermotherapy and chemotherapy have received extensive attention to tumor treatment. However, thermal tolerance and drug resistance severely limit clinical effect of tumor therapy owing to endoplasmic reticulum (ER) stress. Reducing thermal tolerance and drug resistance of tumors is an urgent challenge to be solved. In this work, we design a nanoplatform of PBA-Dtxl@MIL-101 as an ER inhibitor. Amino functionalized Fe-metal organic framework (MIL-101) nanoparticles are synthesized as pH and microwave (MW) dual stimuli-responsive drug delivery system. Then, the chemical chaperones of 4-phenylbutyric acid (PBA) and antineoplastic drug Docetaxel (Dtxl) were successfully loaded into MIL-101 nanoparticles to form PBA-Dtxl@MIL-101 nanoparticles. Furthermore, PBA-Dtxl@MIL-101 nanoparticles exhibit inhibitor effect of ER stress through upregulating caspase 9 proteins and reduce thermal tolerance by downregulating HSP 90. It was demonstrated that the therapy sensitized by PBA-Dtxl@MIL-101 nanoparticles obviously destroyed tumor cells, showing simultaneously enhanced thermo-chemo therapy.
Monoamine oxidase A (MAO-A) is a prominent myocardial source of reactive oxygen species (ROS), and its expression and activity are strongly increased in failing hearts. Therefore, accurate evaluation of MAO-A activity in cardiomyocytes is of great importance for understanding its biological functions and early diagnosing the progression of heart failure. However, so far, there is no report on the fluorescent diagnosis of heart failure by a specific probe for MAO-A. In this work, two far-red emissive fluorescent turn-on probes (KXS-M1 and KXS-M2) for the highly selective and sensitive detection of MAO-A were fabricated. Both probes exhibit good response to MAO-A, one of which, KXS-M2, performs better than the other one in terms of a fluorescence increment and sensitivity. Using the pioneering probe KXS-M2, specific fluorescence imaging of MAO-A in glucose-deprived H9c2 cardiac cells, zebrafish and isoprenaline-induced failing heart tissues was achieved, proving that KXS-M2 can serve as a powerful tool for the diagnosis and treatment of heart failure.
The enantioselective epoxidation of olefin by MnⅡ(R,R-PMCP)(OTf)2, H2O2 and H2SO4 was explored by DFT calculations and experiments. Theoretical results suggest that [MnⅤ(O)(R,R-PMCP)(SO4)]+ species with a triplet ground spin state serves as the active species for the olefin epoxidation. It can be generated by the H2SO4 assisted O-O heterolysis of MnⅢ(OOH) species. MnⅢ-persulfate is also involved in this system, but it cannot promote the olefin epoxidation directly, preferring instead to transform into MnⅤ(O). Actually, the asymmetric epoxidation reactions with H2O2/H2SO4 or Oxone provide similar enantioselectivity in the presence of manganese catalyst. These observations further support the transformation of MnⅢ-persulfate to MnⅤ(O) species.
An electrochemically promoted decarboxylative borylation reaction is reported. The reaction proceeds under mild conditions in an undivided cell without use of transition metal- or photo-catalysts. The key feature of the reaction is the compatibility of diboron reagents with the electrochemical conditions. This reaction exhibits broad substrate scope, good functional group tolerability, and easy scalability.
Fast skin repair is critical for less infection, less pain and high quality of life, which is still limited with undesirable rehabilitation speed and side effects. Currently, laser-activated silk sealant agent without suture and gauze has been demonstrated promising for fast skin repair taking advantage of its structural transformation after heating. Nevertheless, more efficient healing effects and less side effects of laser-activated silk sealant agent remains challenging due to absence of suitable photo-thermal materials and robust/biomimetic protein materials. In this work, the marriage between silk protein and Rehmanniae radix preparata (a kind of the traditional Chinese herb) has been demonstrated as a novel and effective way to achieve an excellent healing effect for skin repair. The non-toxicity, high photothermal conversion efficiency and healing mechanism are systematically studied and proved. This new methodology might shed a new light for combining dark traditional Chinese medicine and silk fibroin for advanced wound healing technology.
The therapy of non-small lung cancer (NSCLC) is limited by wide metastasis and chemotherapy resistance, herein, we present a new cancer-targeting prodrug PBG with the integration of real-time fluorescence visualization. The potent anticancer drug Gefitinib conjugates a biotin recognition ligand yielding the prodrug PBG via a GSH-activatable disulfide bond linker. Once coupling a near-infrared azo-BODIPY fluorophore into the molecular structure of PBG, we obtain its fluorescent theranostic TBG. The prodrug PBG can sustain Gefitinib release by the high level of GSH in the pathophysiological milieu. We evaluate the drug delivery of the prodrug PBG using fluorescent TBG in PC9 cancer bearing nude mice models, which indicate that TBG can be utilized to monitor the in vivo drug release process. Prodrug PBG can be targeted to accumulate in the cancer lesion with a better and efficaciously therapeutic result compared with the single Gefitinib treatment in cells and in vivo. The fluorescence images also reveal that the targeting accumulation and longitudinal retention of anticancer drug in cancer lesions will contribute to the superior therapeutic effects. The above applications of our new prodrug PBG and its fluorescent theranostic TBG have the potential contribution to the research in biology and the clinical medicine.
It has been challenging to achieve multi-photochromic systems without affecting the individual photoswitching properties of the constituent units. Herein, we present the design and synthesis of a new family of platinum-acetylide dendrimers containing up to twenty-one photochromic dithienylethene (DTE) units that exhibit both high photochromic efficiency and individual switching properties. Upon irradiation with ultraviolet (UV) and visible (vis) light, the resultant metallodendrimers display high conversion yield and good fatigue resistance. More interestingly, cyclization-cycloreversion kinetics revealed that the photochromic property of each DTE unit in these metallodendrimers is unaffected by its neighbor and the full ring-closure of up to twenty-one DTE units in one single dendrimer has been achieved.
Oral drugs have been widely used in clinical therapy, but their developments were severely limited by the side effects of drug exposure as well as the multiple biological barriers. In this study, we constructed a "cluster bomb" oral drug delivery system (DOX@PFeL@L100) with core-shell structure to overcome the complex absorption barriers. The inner core termed as "bomb" that contains a lot of ultra-small diameter Fe3O4 nanoparticles (DOX@PFeL NPs) loaded with doxorubicin (DOX) and modified with l-valine, which can efficiently penetrate the epithelial cells via PePT1 receptor mediated endocytosis. The outer shell of this "cluster bomb" is a layer of pH-sensitive polymer (Eudragit®L100) that can be served as a pH-responsive switch and effectively control the "bomb" release in the intestinal microenvironment to improve the antitumor efficiency by the Fenton like reaction of DOX and Fe2+/Fe3+. This study demonstrates that the "cluster comb" oral drug delivery system can sequentially overcome the multiple biological barriers, providing a safe and effective approach for tumor therapy.
The process of selectively introducing a CF3 group into an organic molecule using inexpensive, stable, and solid sodium trifluoromethanesulfinate has rapidly advanced in recent years to become an eco-friendly method used by organic chemists to synthesize various natural and bioactive molecules. This review focuses on advances made within the last five years regarding C–H functionalisation, namely thermochemical C(sp2)–H (thio)trifluoromethylations, photochemical C(sp2)–H trifluoromethylations, and electrochemical C(sp2)–H trifluoromethylations, using Langlois' reagent (NaSO2CF3).
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