Injectable Micromotor@Hydrogel System for Antibacterial Therapy

The drug delivery system based on nano/micromotors has become a research hot spot in recent years. However, naked micromotors may be ruptured or passivated under the complex biological environment, which will result in the leakage of drugs in advance or limited self-propulsion performance. Herein, an injectable micromotor@hydrogel drug delivery system to protect micromotors from the external environment is proposed. The micromotors were prepared through layer-by-layer assembly technology. The asymmetric decomposition of hydrogen peroxide catalyzed by the locally distributed platinum nanoparticles enabled efficient propulsion of the micromotors in low concentration of hydrogen peroxide. In order to protect micromotors, they were loaded into the Schiff base hydrogel. The micromotor@hydrogel system can be injected directly into the lesion to release micromotors in response to the environment, reducing external influence on micromotors and improving the sustained-release effect. Erythromycin (Ery) loaded into the micromotors and the micromotor@hydrogel system demonstrated excellent antibacterial effect. Micromotors released from the hydrogel underwent enhanced diffusion in the surroundings of bacteria without addition of exogenous hydrogen peroxide, which was manifested by their appearance in edge of the inhibition zone. The proposed micromotor@hydrogel drug delivery system offers a new strategy for the treatment of bacterial infections.     

Synthesis and evaluation of the anticancer activity of the water-dispersible complexes of 4-acylaminoisoxazole derivative with biocompatible nanocontainers based on Ca2+ (Mg2+) cross-linked alginate

Water-dispersible complexes of 4-methyl-N-[5-methyl-3-(3,4,5-trimethoxyphenyl)isoxazol-4-yl]benzamide possessing anticancer activity were prepared by its immobilization with biocompatible polymer nanocontainers based on sodium alginate cross-linked with Ca²⁺ and Mg²⁺ ions. It was found that this isoxazole derivative retains its structure during immobilization. Colloidal stable nanocontainers filled with this compound exhibit toxicity toward the colon carcinoma (HCT116) tumor cell line.     

Fruit waste (Pulp) decorated CuO NFs as promising platform for enhanced catalytic response and its peroxidase mimics evaluation

Herein, we report for the first time, an eco-compatible hydrothermal route for the synthesis of carbon enriched mesoporous material (CuO NFs@MP) using fruit waste (Pulp) obtained from Citrus limetta’s (Mausambi) decorated irregular shaped CuO nanoflakes (NFs). The CuO NFs@MP nanocomposite was fully characterized through several spectroscopic-cum-analytical techniques such as TEM and XPS, which further confirmed the presence of CuO NFs. CuO NFs@MP could serve as an excellent catalyst for N-Arylation reaction and also paves promising peroxidase mimic activity. The preliminary results indicated that CuO NFs@MP shows the catalytic advantage of higher yields, shorter reaction time and greener conditions. Simultaneously, the oxidation of colorless TMB with H₂O₂ into blue-green colored ox-TMB was also observed in 60 s with CuO NFs@MP. The present nanocomposite is easy to synthesize, economical, retrievable and a reusable catalyst for synthesizing a varied range of N-Arylated products and could also mimic peroxidase without significant loss of activity.     

Engineering nanostructures of CuO-based photocatalysts for water treatment: Current progress and future challenges

Nowadays, increasing extortions regarding environmental problems and energy scarcity have stuck the development and endurance of human society. The issue of inorganic and organic pollutants that exist in water from agricultural, domestic, and industrial activities has directed the development of advanced technologies to address the challenges of water scarcity efficiently. To solve this major issue, various scientists and researchers are looking for novel and effective technologies that can efficiently remove pollutants from wastewater. Nanoscale metal oxide materials have been proposed due to their distinctive size, physical and chemical properties along with promising applications. Cupric Oxide (CuO) is one of the most commonly used benchmark photocatalysts in photodegradation owing to the fact that they are cost-effective, non-toxic, and more efficient in absorption across a significant fraction of solar spectrum. In this review, we have summarized synthetic strategies of CuO fabrication, modification methods with applications for water treatment purposes. Moreover, an elaborative discussion on feasible strategies includes; binary and ternary heterojunction formation, Z-scheme based photocatalytic system, incorporation of rare earth/transition metal ions as dopants, and carbonaceous materials serving as a support system. The mechanistic insight inferring photo-induced charge separation and transfer, the functional reactive radical species involved in a photocatalytic reaction, have been successfully featured and examined. Finally, a conclusive remark regarding current studies and unresolved challenges related to CuO are put forth for future perspectives.     

A immunosuppressive triterpenoid saponin from the stems of Epigynum griffithianum

Abstract

Chemical investigation of the stems of Epigunum griffithianum led to the isolation and identification of a new triterpenoid saponin (1) and two known compounds (epigynosides A (2) and B (3)). These structures were elucidated by means of spectroscopic analysis (1D and 2D NMR, MS, UV, IR) as well as comparison with the reported data. Compound 1 was evaluated in vitro for the immunosuppressive activities on proliferation of mice splenocyte and displayed significant immunosuppressive activities compared to the positive control (dexamethasone) with the concentration at 25?μM.     

Molecular insight for the role of key residues of calreticulin in its binding activities: A computational study

Calreticulin (CRT) is localized to and has functions in multiple cellular compartments, including the cell surface, the endoplasmic reticulum, and the extracellular matrix. Mutagenesis studies have identified several residues on a concave β-sheet surface of CRT critical for CRT binding to carbohydrate and other proteins/peptides. How the mutations of these key residues in CRT affect the conformation and dynamics of CRT, further influencing CRT binding to carbohydrates and other proteins to signal the important biological activities remain unknown. In this study, we investigated the effect of three key point mutations (C105A, C137A and W319A) on CRT conformation and dynamics via atomistic molecular dynamics simulations. Results show that these three key residues mutations induced the changes of CRT local backbone flexibility and secondary structure of CRT N-domain, which could further affect CRT’s binding activity. C137A mutation led to dramatic decrease of the overall size of CRT due to the P-domain fold back to the globular domain and formed new inter-domain contacts, which can cause blockage of CRT’s binding with other large substrates. Furthermore, for CRT concave β-strand surface patch containing lectin binding site, CRT C105A, C137A and W319A point mutation resulted in the changes in solvent accessible surface area, key residues’ side chain atom positions and dynamical correlated motions between residues. All these changes could directly affect CRT binding behavior. Results of this study provide molecular and structural insights into understanding the role of key residues of CRT in its binding behavior.     

Luminescent amphiphilic nanogels by terpyridine-Zn(II) complexation of polymeric micelles

In this work, we investigated terpyridine (tpy)/Zn(II) complexation for the crosslinking of polymeric micelles of the branched poly(ethylene oxide)–poly(propylene oxide) block copolymer Tetronic® 1107 (T1107) in water and produce physically stable amphiphilic luminescent nanogels. Nanoparticles displayed a size of 235 ± 25 and 318 ± 57 nm before and after Zn(II) crosslinking, respectively, as measured by dynamic light scattering. High-resolution scanning electron microscopy analysis revealed the multimicellar nature of the crosslinked nanoparticles. In addition, Zn(II) complexation prevented nanoparticle disassembly after extreme dilution below the critical micellar concentration and reduced the minimum concentration required for the reverse thermal gelation of concentrated aqueous T1107 systems. The cell compatibility and uptake were initially assessed in the murine macrophage cell line RAW 264.7. Results showed that complexation increases the cell compatibility of the nanoparticles with respect to the non-complexed counterparts. In addition, non-crosslinked nanoparticles accumulated in the cell membrane, while the complexed ones were internalized, as observed by confocal laser scanning fluorescence microscopy. Then, the antiproliferative activity of the crosslinked nanoparticles was confirmed in the rhabdomyosarcoma cell line Rh30; their inhibitory concentration 50 (IC₅₀) being 101 μg/mL (6.7 μM). Finally, the encapsulation and release of the hydrophobic antiretroviral efavirenz was characterized in vitro. Complexation slightly reduced the release kinetics with respect to the pristine nanoparticles. Overall results demonstrate the promise of this simple modification strategy to produce amphiphilic nanogels with a set of advantageous physicochemical, optical, and biological properties.     

Synthesis and biological activity of new derivatives with the preserved carane system

Abstract

Terpenoid derivatives, which contain a preserved carane system in their structure, exhibit a broad spectrum of biological activities. Among them, we can distinguish insecticides, structures with pharmacological application etc. In the presented paper, the substrate - (–)-cis-caran-trans-4-ol was transformed using the reactions of typical organic synthesis to obtain novel derivatives. Most importantly, bromolactone ((–)-(1R,4R,6S)-2'-(bromomethyl)-4,7,7-trimethylspiro[bicyclo[4.1.0]heptan-3,3'-furan]-5'(4'H)-one) with the preserved carane system was synthesized. This bromolactone was tested for antifeedant activity against the lesser mealworm, Alphitobius diaperinus Panzer, and peach potato aphid (Myzus persicae). In addition, its moderate antibacterial activity was observed against the Bacillus subtilis strain (with Minimal Inhibitory Concentration of 200 µg/mL).     

羟基对界面水分子的扰动与其对非离子型氢氟烃杂化表面活性剂聚集行为的改变

本文合成并比较了具有和不具有羟基的两种非离子型氢氟烃杂化表面活性剂，它们均表现出良好的热稳定性和优异的表面活性. 实验观察到羟基对改变其溶液的表面张力和所形成胶束的形态具有较大的影响. 该作用可归因于烷烃基团从空气/水表面上方到其下方的重排以及由羟基诱导的界面水结构的扰动. 本工作提供了一种通过修改界面处的取向结构来弱化碳氢链和碳氟链之间的不混溶性，从而利于设计具有不同界面性质表面活性剂的策略.     

Controllable Preparation of Plasmonic Gold Nanostars for Enhanced Photothermal and SERS Effects

Gold nanostars(Au NSs) are asymmetric anisotropic nanomaterials with sharp edge structure. As a promising branched nanomaterial, Au NS has excellent plasmonic absorption and scattering properties. In order to tune the plasmonic photothermal and surface-enhanced Raman scattering(SERS) activity of Au NSs to obtain the desired characteristics, the effects of reagents on the local surface plasmon resonance(LSPR) bands of Au NSs were studied and the morphology and size were regulated. Nanoparticles with different sharp edges were synthesized to make their local plasmon resonance mode tunable in the visible and near-infrared region. The effects of the number and sharpness of different tips under the control of AgNO₃ on the photothermal response of Au NSs and the SERS activity and their mechanism were discussed in detail. The results show that as the length of the branch tip becomes longer and the sharpness increases, the plasmonic photothermal effect of Au NSs is strengthened, and the photothermal conversion efficiency is the highest up to 40% when the length of Au NSs is the longest. Au NSs with high SERS activity are used for the Raman detection substrate. Based on this property, the quantitative detection of the pesticide thiram is achieved.