In this study, we isolated nine compounds from the acid hydrolysate of the flower buds of Lonicera fulvotomentosa Hsu et S. C. Cheng and characterized their chemical structures using 1H-NMR, 13C-NMR, and electron ionization mass spectroscopy (EI-MS). These compounds were identified as β-sitosterol (1), 5,5′-dibutoxy-2,2′-bifuran (2), nonacosane-10-ol (3), ethyl (3β)-3,23-dihydroxyolean-12-en-28-oate (4), oleanolic acid (5), ethyl caffeate (6), caffeic acid (7), isovanillin (8), and hederagenin (9), with 4 as a new triterpene compound. Inhibitory activity against human immunodeficiency virus (HIV) protease was also evaluated for the compounds, and only ethyl caffeate, caffeic acid, and isovanillin (6, 7, and 8) exhibited inhibitory effects, with IC50 values of 1.0 μM, 1.5 μM, and 3.5 μM, respectively. Molecular docking with energy minimization and subsequent molecular dynamic (MD) simulation showed that ethyl caffeate and caffeic acid bound to the active site of HIV protease, while isovanillin drifted out from the active site and dissociated into bulk water during MD simulations, and most of the binding residues of HIV protease have been previously identified for HIV protease inhibitors. These results suggest that caffeic acid derivatives may possess inhibitory activities towards HIV protease other than previously reported inhibitory activities against HIV integrase, and thus ethyl caffeate and caffeic acid could be used as lead compounds in developing potential HIV protease inhibitors, and possibly even dual-function inhibitors against HIV.
Abstract Space exploration has captured the imagination of humanity for generations. From the first steps on the moon to the recent Mars rover and Artemis lunar exploration missions, space travel has always been an ambitious goal for humanity. However, as we venture further into space and prepare for long-term missions to other planets, the physiological and health risks associated with prolonged space travel are becoming more prominent. Most current research on astronaut health focuses on identifying individual genes or pathways for specific symptoms astronauts face. The human system is complex and delicate, and the effects of microgravity, radiation, and isolation on astronaut health during long-duration spaceflight are still not fully understood. This study used a novel ranking and analysis methodology to combine space omics data from multiple datasets in the NASA OSDR repository. The data was used to generate a multi-omic, integrative bioinformatics analysis pipeline, which identified and characterized a genome-wide spaceflight gene expression correlation loss as a central biosignature for astronaut health on the International Space Station (ISS). Our findings indicate that genome-wide correlation loss corresponds to a breakdown in gene synchronization and cooperation, showcasing the systemic symptoms spaceflight induces and their genomic roots.
Bovine mastitis is one of the major infectious diseases in dairy cattle, resulting in large economic loss due to decreased milk production and increased production cost to the dairy industry. Antibiotics are commonly used to prevent/treat bovine mastitis infections. However, increased antibiotic resistance and consumers' concern regarding antibiotic overuse make it prudent and urgent to develop novel therapeutic protocols for this disease.
Purpose To explore the changes of plasma LL-37 in the bloodstream infected children. Methods 40 patients with bloodstream infection were included in case group,they visited the Capital Institute of Pediatrics Affiliated to Children's Hospital between May 30th and January 1st, 2015. Double blood cultures from different parts were positive in these children. 40 normal children with matched age and gender were control groups.We determine plasma LL-37 content of two groups by enzyme-linked immunosorbent,and observed evolution and prognosis of the disease. Results Case group can be divided into MODS group and …
Ni-doped copper nitride films have been prepared by co-sputtering of Ni and Cu targets. The addition of Ni to Cu 3 N films reduced the intensity of the (111) diffraction peak, and lead a little angular shifts of the peaks. The films showed a large difference in reflectance in the infrared and visible before and after thermal decomposition, which is applicable to optical recording media. The films change from a semiconductor to a conductor with the increased ratio of Ni in Cu 3 N films.
Hypericum kouytchense Lévl is a semi-evergreen plant of the Hypericaceae family. Its roots and seeds have been used in a number of traditional remedies for antipyretic, detoxification, anti-inflammatory, antimicrobial and antiviral functions. However, to date, no bioactivity compounds have been characterized from the insect gall of H. kouytchens. In this study, we evaluated the antiviral activities of different extracts from the insect gall of H. kouytchen against cathepsin L, HIV-1 and renin proteases and identified the active ingredients using UPLC-HRMS. Four different polar extracts (HW, H30, H60 and H85) of the H. kouytchense insect gall exhibited antiviral activities with IC50 values of 10.0, 4.0, 3.2 and 17.0 µg/mL against HIV-1 protease; 210.0, 34.0, 24.0 and 30.0 µg/mL against cathepsin L protease; and 180.0, 65.0, 44.0 and 39.0 µg/mL against human renin, respectively. Ten compounds were identified and quantified in the H. kouytchense insect gall extracts. Epicatechin, eriodictyol and naringenin chalcone were major ingredients in the extracts with contents ranging from 3.9 to 479.2 µg/mg. For HIV-1 protease, seven compounds showed more than 65% inhibition at a concentration of 1000.0 µg/mL, especially for hypericin and naringenin chalcone with IC50 values of 1.8 and 33.0 µg/mL, respectively. However, only hypericin was active against cathepsin L protease with an IC50 value of 17100.0 µg/mL, and its contents were from 0.99 to 11.65 µg/mg. Furthermore, we attempted to pinpoint the interactions between the active compounds and the proteases using molecular docking analysis. Our current results imply that the extracts and active ingredients could be further formulated and/or developed for potential prevention and treatment of HIV or SARS-CoV-2 infections.
Mesoporous anatase TiO2 nanomaterials (MATNs) with both large specific surface areas and structural coherence are highly desirable to achieve excellent physicochemical properties for photovoltaic applications, but the existing synthesis methods either need templates or cause pollution. Herein we report a simple, template-free, and green approach to synthesize MATNs consisting of interconnected nanoparticles. The Ti-complex intermediates were first prepared using titanium isopropoxide and acetic acid in a solvothermal reaction, which went through a morphology transformation sequence of nanowires, microspheres, and microflowers with a prolonged reaction time. Then the Ti-complex intermediates were cracked into MATNs under annealing, which were applied in dye-sensitized solar cells (DSSCs) and hole-conductor-free perovskite solar cells (HPSCs). The mesoporous anatase TiO2 nanowire-based DSSCs achieved a high power conversion efficiency (PCE) up to 7.78% because of both a high dye-adsorption capacity and long charge-transfer channels, while the PCE based on the P25 photoelectrodes is 6.61%. The further application of mesoporous anatase TiO2 nanowires in HPSCs achieved an improved PCE of 8.52%, compared to 6.78% for cells prepared using the P25 electrodes.
Over the past few decades, it has been well established that gut microbiota-derived metabolites can disrupt gut function, thus resulting in an array of diseases. Notably, phenylacetylglutamine (PAGln), a bacterial derived metabolite, has recently gained attention due to its role in the initiation and progression of cardiovascular and cerebrovascular diseases. This meta-organismal metabolite PAGln is a byproduct of amino acid acetylation of its precursor phenylacetic acid (PAA) from a range of dietary sources like egg, meat, dairy products, etc. The microbiota-dependent metabolism of phenylalanine produces PAA, which is a crucial intermediate that is catalyzed by diverse microbial catalytic pathways. PAA conjugates with glutamine and glycine in the liver and kidney to predominantly form phenylacetylglutamine in humans and phenylacetylglycine in rodents. PAGln is associated with thrombosis as it enhances platelet activation mediated through the GPCRs receptors α2A, α2B, and β2 ADRs, thereby aggravating the pathological conditions. Clinical evidence suggests that elevated levels of PAGln are associated with pathology of cardiovascular, cerebrovascular, and neurological diseases. This Review further consolidates the microbial/biochemical synthesis of PAGln and discusses its role in the above pathophysiologies.
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