1,2,3‐Triazole hybrids with anti‐HIV‐1 activity Feng, Lian‐Shun; Zheng, Man‐Jie; Zhao, Feng ...
Archiv der Pharmazie (Weinheim),
January 2021, 2021-Jan, 2021-01-00, 20210101, Letnik:
354, Številka:
1
Journal Article
Recenzirano
The human immunodeficiency virus type 1 (HIV‐1) is the major etiological agent responsible for the acquired immunodeficiency syndrome (AIDS), which is a serious infectious disease and remains one of ...the most prevalent problems at present. Currently, combined antiretroviral therapy is the primary modality for the treatment and management of HIV/AIDS, but the long‐term use can result in major drawbacks such as the development of multidrug‐resistant viruses and multiple side effects. 1,2,3‐Triazole is the common framework in the development of new drugs, and its derivatives have the potential to inhibit various HIV‐1 enzymes such as reverse transcriptase, integrase, and protease, consequently possessing a potential anti‐HIV‐1 activity. This review covers the recent advances regarding the 1,2,3‐triazole hybrids with potential anti‐HIV‐1 activity; it focuses on the chemical structures, structure–activity relationship, and mechanisms of action, covering articles published from 2010 to 2020.
This review covers the recent advances in the field of 1,2,3‐triazole hybrids with potential anti‐HIV‐1 activity; it focuses on the chemical structures, structure–activity relationship, and mechanisms of action, covering articles published between 2010 and 2020.
The design and synthesis of solar steam generation materials is a green and promising approach to produce freshwater from seawater or contaminated water. Here, we develop a highly efficient and ...stable bilayer evaporator by assembling WO3-x nanorods (WO3-x NRs) onto a wood surface. Due to the broad-band absorption of the WO3-x NRs and the multiscatter of the incident light caused by the wood, the prepared solar evaporator with unique light trapping structures shows a high solar absorption (~94.0%). Additionally, combining with the merits of rapid water transport and heat localization, the energy conversion efficiency of the evaporator reaches as high as 82.5% under one sun irradiation and shows a stable water generation capability during long-term illumination cycles, which is one of the best performance compared with other wood-based materials and oxygen-defected tungsten oxide. The evaporator also shows great performance towards the evaporation of seawater and contaminated water, indicating great potential application. This work can provide reference for designing other high photothermal conversion system.
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•A bilayer evaporator by assembling WO3-x nanorods onto the wood surface was designed for solar steam generation.•The solar evaporator has 94.0% solar absorptance.•The energy conversion efficiency can reach at 82.5% under one sun.•The evaporator shows great performance toward water evaporation from seawater and contaminated water.
The use of arctigenin (ARG), a traditional medicine with many pharmacological activities, has been restricted due to its poor solubility in water. Five amino acid derivatives of ARG have been ...synthesized using glycine, o-alanine, valine, leucine, and isoleucine, which have t-butyloxy carbonyl (BOC) as a protective group. In this study, we examined the effects of removing these protective groups. The results showed that the amino acid derivatives have better solubility and nitrite-clearing ability than ARG. Among the compounds tested, the amino acid derivatives without protective group were the best. Based on these results, ARG and its two amino acid derivatives without protective group (ARG8, ARG10) were selected to evaluate their anti-tumor activity in vivo at a dosage of 40 mg/kg. The results indicated that ARG8 and ARG10 both exhibit more anti-tumor activity than ARG in H22 tumor-bearing mice. The tumor inhibition rates of ARG8 and ARG10 were 69.27 and 43.58%, which was much higher than ARG. Furthermore, the mice treated with these compounds exhibited less damage to the liver, kidney and immune organs compared with the positive group. Furthermore, ARG8 and ARG10 improved the serum cytokine levels significantly compared to ARG. In brief, this study provides a method to improve the water solubility of drugs, and we also provide a reference basis for new drug development.
Phosphorus (P) deficiency is an important factor that limits the agricultural production potential in acidic soils. The bacterial
gene encodes non-specific acid phosphatase (ACP), which participates ...in the mineralization of soil organic P and is therefore important for the improvement of soil P availability. However, the function and community population of
-harboring bacteria and their driving factors in acidic soil remain largely unknown. For this study, 51 soil samples and 207 plant samples were collected from four locations in the acidic soil region of southern China. Quantitative PCR and high-throughput sequencing were employed to analyze abundance and community composition of
-harboring bacteria. The results showed that soil P availability was the important nutrient element limiting the growth of both plants and soil bacteria. Soil ACP activity was clearly higher than alkaline phosphatase, indicating the important effect of
-harboring bacteria in acidic soils. ACP activity and
gene abundance showed a significant positive correlation, and both were closely related to soil available P, total carbon, and total nitrogen. The dominant genera of
-harboring bacteria involved
,
, and
. Compared to land-use pattern, sampling location, and soil parent material, soil property played a more important role in affecting
-harboring bacterial community structure, where N-related variables including soil NO
-N, NH
-N, and C/N ratio appeared to be the main factors. These findings suggest that
-harboring bacteria should provide an important contribution to soil P availability in acidic soil, and its function and community composition were strongly associated with soil nutrients.
► A new Si–O–C composite anode was prepared and exhibited good electrochemical performance. ► Mechanism of lithium storage in the composite anodes was suggested by comparing
29Si MAS NMR and Si (2p) ...XPS of the anodes at different potential state. ► Of the silicon species, SiOC
3 units are irreversible with lithium, but SiO
2C
2, SiO
3C, and SiO
4 units are reversible with lithium.
A Si–O–C composite material is prepared by pyrolyzing a copolymer of phenyl-substituted polysiloxane and divinylbenzene at 800
°C under a hydrogen atmosphere. The material has a high delithiation capacity about 965.3
mA
h
g
−1 in the first cycle and retains 660
mA
h
g
−1 after 40 cycles at 50
mA
g
−1. The differential capacity curves of the anode show that there are several reduction peaks between 0.2 and 0.6
V existing all the time during repeated cycles. By comparing
29Si nuclear magnetic resonance (
29Si MAS NMR), Si (2p) X-ray photoelectron spectroscopy (XPS) of the anode in the original, fully lithiated, and fully delithiated state, the reduction peaks are related to lithium reversible insertion into SiO
2C
2, SiO
3C, and SiO
4 units, respectively. The corresponding
29Si MAS NMR resonances shift to high field and their binding energies of the Si (2p) XPS peak increase in the fully lithiated state, and then both turn to the opposite direction in the fully delithiated state. The SiO
4 units decrease during repeated cycles. The remaining ones can reversibly transform to Li–silicate (Li
2SiO
3) when lithium is inserted, while the lost ones irreversibly transform to Li–silicate (Li
4SiO
4). However, the SiOC
3 units of the material are totally irreversible with lithium because they nearly disappear in the first discharge process, and lead to the formation SiC
4 units.
The additional local stress concentration caused by undercut and misaligned defects could lead to lower fatigue strength of welded joints. The paper aims to investigate the effects of undercuts and ...misalignments on fatigue performance and reliability of Load‐carrying Cruciform Welded Joint (LCWJ) quantitatively by probabilistic statistics theory and fracture mechanics theory. Firstly, the geometrical characteristics of undercut and misalignment are summarized from the literature and our experiments. Subsequently, the probabilistic distributions of material fracture properties, the configurations of geometries, and flaws were evaluated under specific loading conditions. The fatigue strengths are further estimated by the probabilistic reliability theory by combining the actual fatigue data. The results demonstrate a clear disparity of fatigue crack growth threshold and resistances for the tested data of base metal and weldment. The level of defects determines the interval of fatigue life, and the larger the dispersion accompanying earlier fatigue failure occurs.
Highlights
The effects of weld defects on fatigue strength and reliability were assessed quantitatively by the probabilistic method.
FCGRs of HAZ and U‐WM are more conservative than the base metal.
The SIFs in mismatched LCWJs were evaluated by the weight function theory.
Ginseng (G) and Prepared Rehmannia Root (PRR) are commonly used in traditional Chinese medicine for blood supplementation. This study aimed to study G and PRR with different compatibility ratios ...changes in chemical composition and inhibition of cyclophosphamide-induced myelosuppression. HPLC was used to determine the chemical constituents of 13 ginsenosides, 5-hydroxymethylfurfural (5-HMF) and verbascoside in different proportions of G-PRR. Balb/c mice were injected intraperitoneally with cyclophosphamide (CTX) to induce bone marrow suppression. The effects of different proportions of G-PRR on peripheral blood, bone marrow nucleated cells, thymus and spleen index of myelosuppressed mice were analyzed. The results showed that the compatibility of G and PRR can promote the dissolution of ginsenosides, and the content of conventional ginsenosides decreased, and the content of rare ginsenosides increased. Different proportions of G-PRR increased the number of peripheral blood and bone marrow nucleated cells in cyclophosphamide-induced bone marrow suppression mice (p < 0.01), increased thymus index (p < 0.01), decreased spleen index (p < 0.01). Different proportions of G-PRR can improve the myelosuppression induced by cyclophosphamide in mice, and the combined effect of G-PRR is better than the single decoction of G and PRR. Among them, G-PRR 2 : 3 and G-PRR 1 : 2 were better than the other groups. These results indicate that different proportion of G-PRR can improve bone marrow suppression, and the combined decoction of G-PRR is better than the separate Decoction in improving bone marrow suppression. This improvement may be related to the changes of the substance basis and active ingredients of G-PRR.
MicroRNA-122 (miR-122) is the most abundant microRNA in hepatocytes and a central player in liver biology and disease. Herein, we report a previously unknown role for miR-122 in hepatocyte intrinsic ...innate immunity. Restoration of miR-122 levels in hepatoma cells markedly enhanced the activation of interferons (IFNs) in response to a variety of viral nucleic acids or simulations, especially in response to hepatitis C virus RNA and poly (I:C). Mechanistically, miR-122 downregulated the phosphorylation (Tyr705) of STAT3, thereby removing the negative regulation of STAT3 on IFN-signaling. STAT3 represses IFN expression by inhibiting interferon regulatory factor 1 (IRF1), whereas miR-122 targets MERTK, FGFR1 and IGF1R, three receptor tyrosine kinases (RTKs) that directly promote STAT3 phosphorylation. This work identifies a miR-122-RTKs/STAT3-IRF1-IFNs regulatory circuitry, which may play a pivotal role in regulating hepatocyte innate immunity. These findings renewed our knowledge of miR-122's function and have important implications for the treatment of hepatitis viruses.
The treatment of industrial wastewater with various organic compounds was essential for the source control of water pollution. Catalytic ozonation process was widely used in wastewater treatment due ...to its higher efficiency and easy operation. In this work, Ca2Fe2O5 was prepared by the sol–gel method and used as a catalyst to remove quinoline effectively by the catalytic ozonation process. The physical and chemical properties of the catalyst have been well characterized by X-ray diffraction, Fourier transform infrared spectroscopy, N2 physical adsorption–desorption profiles, transmission electron microscopy, and X-ray photoelectron spectroscopy. The results have shown that calcium iron oxide has sheet micromorphology and good crystal structure. In addition, the Ca2Fe2O5 catalyst has more oxygen vacancies than the Fe2O3 catalyst, which can promote the decomposition of ozone molecules to produce active free radicals effectively. In this study, the Ca2Fe2O5 catalyst has shown higher catalytic activity than the other reported catalysts, which can remove quinoline and other organics from an aqueous solution effectively. In the Ca2Fe2O5/O3 system, more ozone molecules decomposed to generate •OH radicals, which inhibited the direct reaction of ozone and quinoline to produce NH4 +-N. Meanwhile, •OH radicals generated in the catalytic ozonation process has increased the chemical oxygen demand removal rate efficiently. In addition, the intermediate products in the catalytic ozonation process were studied by electrospray ionization–mass spectrometry analysis. This research shows a promising way to prepare efficient catalysts for the treatment of quinoline by the catalytic ozonation process.
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