Pipersarmenoids, new amide alkaloids from Piper sarmentosum.

A chemical investigation of the aerial parts of Piper sarmentosum resulted in the isolation and identification of 14 amide alkaloids, including three new amide alkaloids, pipersarmenoids A - C (1-3), three new natural amide alkaloids, pipersarmenoids D - F (4-6), and 8 known analogues, N-p-coumaroyltyramine (7), piperlotine C (8), piperlotine D (9), pellitorine (10), sarmentine (11), aurantiamide acetate (12), 1-cinnamoyl pyrrolidine (13) and sarmentamide B (14). Their structures were determined by spectroscopic analysis including HRESIMS and 1D and 2D NMR. The cytotoxicity, neuroinflammation-inhibiting and acetylcholinesterase (AChE) inhibitory activities of those compounds were tested. Compounds 1, 2 and 12 inhibited NO production induced by LPS in BV2 cells with IC50 values of 9.36, 12.53 and 10.77 µM, respectively. Moreover, 1, 2, 7 and 11 showed moderate inhibitory activity on AChE with IC50 values ranging from 37.56 to 48.84 µM.

Design, synthesis, in vitro and in vivo evaluation and molecular docking study of novel pleuromutilin derivatives as antibacterial agents.

14 novel pleuromutilin derivatives were designed and synthesized as inhibitors against Staphylococcus aureus (S. aureus). The modification was focused on the C22 position of pleuromutilin. We conducted the characterization, in vitro and in vivo biological assessment of the compounds. Compound 18 exhibited the best antibacterial effect against MRSA (MIC = 0.015 µg/mL, MBC = 0.125 µg/mL). Compound 18 was further studied by time-kill kinetic and post-antibiotic effect (PAE) approaches. Besides, most compounds exhibited low cytotoxicity to RAW 264.7 cells. Compound 18 displayed decent bactericidal activity in vivo (-0.51 log10 CFU/mL). Molecular docking study indicated that compound 18 could be located stably at the ribosome (ΔGb = -7.30 kcal/mol). The results revealed that compound 18 might be further developed into a novel antibiotic.

Cobalt based bimetallic catalysts for heterogeneous electro-Fenton adapting to vary pH for HEDP and MIT degradation.

Most of the materials studied as catalysts in the electro-Fenton system are variants of iron oxide or iron hydroxide. However, iron-based catalysts often exhibit weak catalytic capabilities under neutral and alkaline conditions. In this work, we synthesized three cobalt based bimetallic oxides, Co2CuOx, Co2AlOx, and Co2NiOx, using hydrothermal method and evaluated them as catalysts for the heterogeneous electro-Fenton system to remove 1-hydroxyethylidene-1,1-diphosphonic acid (HEDP) and Methylisothiazolinone [2-methyl-4-isothiazolin-3-one] (MIT). Co2NiOx has the highest catalytic degradation activity for HEDP, and Co2CuOx has the best catalytic degradation effect for MIT. Based on characterization results of the catalysts, the reasons for the differences in the pollutant removal efficiency were analysed, and the optimal pH for the three cobalt based oxides to remove HEDP and MIT was investigated. The results showed that the optimal pH values of the three cobalt based bimetallic oxides are not only influenced by the second metal type, but also by the properties of pollutants. Therefore, suitable cobalt based catalysts can be selected based on the different properties of pollutants, or the composition of cobalt based catalysts can be adjusted to meet the different pH requirements of target wastewater. The three cobalt based bimetallic oxides exhibited good degradation of HEDP and MIT under neutral conditions, which to some extent solved the problem of narrow pH range in the practical application of the electro-Fenton process.

Toxicity effects and mechanism of micro/nanoplastics and loaded conventional pollutants on zooplankton: An overview.

Micro/nanoplastics in aquatic environments is a noteworthy environmental problem. Zooplankton, an important biological group in aquatic ecosystems, readily absorb micro/nanoplastics and produce a range of toxic endpoints due to their small size. This review summarises relevant studies on the effects of micro/nanoplastics on zooplankton, including combined effects with conventional pollutants. Frequently reported adverse effects include acute/chronic lethal effects, oxidative stress, gene expression, energetic homeostasis, and growth and reproduction. Obstruction by plastic entanglement and blockage is the physical mechanism. Genotoxicity and cytotoxicity are molecular mechanisms. Properties of micro/nanoplastics, octanol/water partition coefficients of conventional pollutants, species and intestinal environments are important factors influencing single and combined toxicity. Selecting a wider range of micro/nanoplastics, focusing on the aging process and conducting field studies, adopting diversified zooplankton models, and further advancing the study of mechanisms are the outstanding prospects for deeper understanding of impacts of micro/nanoplastics on aquatic ecosystem.

Serovar and sequence type distribution and phenotypic and genotypic antimicrobial resistance of Salmonella originating from pet animals in Chongqing, China.

A total of 334 Salmonella isolates were recovered from 6,223 pet rectal samples collected at 50 pet clinics, 42 pet shops, 7 residential areas, and 4 plazas. Forty serovars were identified that included all strains except for one isolate that did not cluster via self-agglutination, with Salmonella Typhimurium monophasic variant, Salmonella Kentucky, Salmonella Enteritidis, Salmonella Pomona, and Salmonella Give being the predominant serovars. Fifty-one sequence types were identified among the isolates, and ST198, ST11, ST19, ST451, ST34, and ST155 were the most common. The top four dominant antimicrobials to which isolates were resistant were sulfisoxazole, ampicillin, doxycycline, and tetracycline, and 217 isolates exhibited multidrug resistance. The prevalence of ß-lactamase genes in Salmonella isolates was 59.6%, and among these isolates, 185 harbored blaTEM, followed by blaCTX-M (66) and blaOXA (10). Moreover, six PMQR genes, namely, including qnrA (4.8%), qnrB (4.2%), qnrD (0.9%), qnrS (18.9%), aac(6')-Ib-cr (16.5%), and oqxB (1.5%), were detected. QRDR mutations (76.6%) were very common in Salmonella isolates, with the most frequent mutation in parC (T57S) (47.3%). Furthermore, we detected six tetracycline resistance genes in 176 isolates, namely, tet(A) (39.5%), tet(B) (8.1%), tet(M) (7.7%), tet(D) (5.4%), tet(J) (3.3%), and tet(C) (1.8%), and three sulfonamide resistance genes in 303 isolates, namely, sul1 (84.4%), sul2 (31.1%), and sul3 (4.2%). Finally, we found 86 isolates simultaneously harboring four types of resistance genes that cotransferred 2-7 resistance genes to recipient bacteria. The frequent occurrence of antimicrobial resistance, particularly in dogs and cats, suggests that antibiotic misuse may be driving multidrug-resistant Salmonella among pets.IMPORTANCEPet-associated human salmonellosis has been reported for many years, and antimicrobial resistance in pet-associated Salmonella has become a serious public health problem and has attracted increasing attention. There are no reports of Salmonella from pets and their antimicrobial resistance in Chongqing, China. In this study, we investigated the prevalence, serovar diversity, sequence types, and antimicrobial resistance of Salmonella strains isolated from pet fecal samples in Chongqing. In addition, ß-lactamase, QRDR, PMQR, tetracycline and sulfonamide resistance genes, and mutations in QRDRs in Salmonella isolates were examined. Our findings demonstrated the diversity of serovars and sequence types of Salmonella isolates. The isolates were widely resistant to antimicrobials, notably with a high proportion of multidrug-resistant strains, which highlights the potential direct or indirect transmission of multidrug-resistant Salmonella from pets to humans. Furthermore, resistance genes were widely prevalent in the isolates, and most of the resistance genes were spread horizontally between strains.

Biological characteristics and pathogenicity comparison of Nocardia seriolae isolated from Micropterus salmoides and Channa argus.

Nocardia seriolae is the primary pathogen causing nocardiosis in various fish species, leads to significant economic losses in the aquaculture industry. In this study, 10 bacterial strains isolated from Micropterus salmoides and Channa argus infected with nocardiosis, were identified as N. seriolae by physiological and biochemical identification, as well as 16S rDNA sequencing. Moreover, the key virulence-related genes such as ESX-1, T7SS-2, T7SS-3, EspG1, sodC, sod2 and ESAT6 were all positive, and showing high homology among different strains. Pathogenicity testing revealed mortality rates ranging from 70 to 100%, accompanied by the presence of white nodules in the viscera of deceased fish. The drug sensitivity test demonstrated that LY21811, the most lethal strain, exhibited high sensitivity to nine types of antibiotics, including azithromycin, doxycycline, florfenicol and compound sulfamethoxazole, yet showed complete resistance to ß-lactam antibiotics. Additionally, the tannic acid also demonstrated potent inhibitory effects against LY21811, with a minimum inhibitory concentration of 0.0625 mg/mL. These results showed that N. seriolae originated from M. salmoides and C. argus in Zhejiang Province were highly conserved, demonstrating a high homogeneity in genetic characteristics, pathogenicity and antimicrobial susceptibilities. These results provide a foundation for further research on the pathogenic characteristics and disease prevention of N. seriolae infections.

Depression Mediates the Association Between Burden and Quality of Life in Informal Caregivers of Stroke Survivors: Meta-analytic Structural Equation Modeling.

OBJECTIVE: This study aims to use Meta-analytical structural equation modeling (MASEM) to clarify the relationship between burden, depression, and quality of life in informal caregivers of stroke survivors. DATA SOURCES: The databases of PubMed, Cochrane Library, Embase, China Knowledge Resource Integrated Database, Wan Fang Database, and Chinese Biomedical Database were comprehensively searched before January 16, 2023. STUDY SELECTION: Two researchers performed an independent initial search by using a unified search strategy. Observational studies investigating the relation between burden, depression, and quality of life in informal caregivers of stroke survivors were included. The studies that met the inclusion criteria were appraised by "Quality Assessment and Validity Tool for Correlational Studies". DATA EXTRACTION: PRISMA guidelines were used for this study. Data extraction was performed independently by 2 researchers. The following data were extracted: study author, year of publication, country, language, sample size, age, sex (%women), the caregivers' relation with stroke survivor, measures, type of outcome reported in the study, study design, and main conclusion. DATA SYNTHESIS: The analysis included 18 articles that reported 23 effect sizes (N=3284). The MASEM findings showed that caregiver burden was positively associated with caregiver depression (ß=0.474, 95% CI [0.398, 0.550]), caregiver depression was negatively associated with caregiver quality of life (ß=-0.316, 95% CI [-0.545, -0.087]). Furthermore, the association between caregiver burden and quality of life was completely mediated by caregiver depression (ß=-0.150, 95% CI [-0.271, -0.041]). CONCLUSIONS: Using the MASEM approach, we observed that caregiver depression completely mediated the relation between burden and quality of life in informal caregivers of stroke survivors. Although the results did not allow for causal inference, this result suggested that for burdened stroke survivors' informal caregivers efforts should be made to their mental health to eliminate the internal barriers, then eventually improve their quality of life.

Nonreciprocal strong mechanical squeezing based on the Sagnac effect and two-tone driving.

We propose a scheme for generating nonreciprocal strong mechanical squeezing by using two-tone lasers to drive a spinning optomechanical system. For given driving frequencies, strong mechanical squeezing of the breathing mode in the spinning resonator can be achieved in a chosen driving direction but not in the other. The nonreciprocity originates from the Sagnac effect caused by the resonator's spinning. We also find the classical nonreciprocity and the quantum nonreciprocity can be switched by simply changing the angular velocity of the spinning resonator. We show that the scheme is robust to the system's dissipations and the mechanical thermal noise. This work may be meaningful for the study of nonreciprocal device and quantum precision measurement.

Glaucatotones A-I: Guaiane-type sesquiterpenoids from the roots of Lindera glauca with anti-inflammatory activity.

Glaucatotones A - I, nine new guaiane-type sesquiterpenoids, along with two reported compounds, namely (1ß,5ß)-1-hydroxyguaia-4(15),11(13)-dieno-12,5-lactone (10) and pseudoguaianelactone C (11), were isolated from the roots of Lindera glauca. The structures and absolute configurations of these compounds were elucidated by extensive spectroscopic analyses, single-crystal X-ray diffraction, and comparison of experimental and calculated electronic circular dichroism (ECD) data. Structurally, glaucatotone A (1) is characterized as a dihomosesquiterpenoid with an unprecedented 5/5/7/6 ring system. A pair of enantiomers, (±)-glaucatotone B (2a/2b), represent the first rearranged norsesquiterpenoid with a (cyclopentylmethyl)cyclohexane skeleton. 3 is defined as a dinorsesquiterpenoid possessing a 5/7/5 ring system. 4-6 are three guaiane-type norsesquiterpenoids. In vitro bioactivity, 2a selectively inhibited Bcap-37 with IC50 value of 5.60 µM, and 9 selectively inhibited Du-145 with IC50 value of 5.52 µM. The anti-inflammatory activity of 1-9 were tested, and of these compounds, 1, 2a, 2b and 7 exhibited potent inhibitory effects.

Latent class analysis of symptoms of depression and anxiety among older women.

OBJECTIVES: This cross-sectional study aims to consider the potential classification of depression and anxiety symptoms among older women, and identify the influencing factors of this classification. METHODS: This study examines Chinese women aged 65 years and older. Latent class analysis was used to explore the mental health subgroups of older women, and multivariate logistic regression was employed to examine the influencing factors based on the health ecological model among these subgroups. RESULTS: The results helped classify this population under three subgroups: the coexistence of depression and anxiety group, dominated depression group, and the low symptoms group. Moreover, class differences in terms of age, residence, education, income, assessment of current life and health status, sleep duration, and health behaviors, such as alcohol use and exercise were noted. CONCLUSIONS: These findings explain the heterogeneity among older women, and help illuminate their unique aspects of mental health. Accordingly, they are significant for scholars and policymakers to understand depression and anxiety among older women.

Latent profile analysis of the symptoms of depression and activities of daily living impairment among older adults.

BACKGROUND: With the aging population, depressive symptoms and impaired Activities of Daily Living have increased medical costs and mortality, generating severe public health issues. This study reconsiders the potential classification of depressive symptoms and ADL impairment in older adults and identifies various factors that may affect classifications. METHODS: This study focused on 6270 Chinese adults aged 65 years or older. We used latent profile analysis to explore depressive symptoms and ADL impairment (basic ADLs and instrumental ADLs) in various subgroups of older adults. We used Chi-square analysis and multivariate logistic regression to examine the determinants of depressive symptoms and ADL impairment among subgroups. RESULTS: The study's results classified older adults into three subgroups: those with high level depressive symptoms and BADLs and IADLs impairment, those with moderate level depressive symptoms and IADLs impairment, and those with no to low level depressive symptoms and without BADLs and IADLs impairment. Illiterate, having fallen in the past year, as well as having hearing difficulties all predicted high level depressive symptoms and severe BADLs and IADLs impairment. In contrast, regular exercise, contact with friends, playing cards/mahjong, participating in organized social activities, and visiting siblings predicted moderate level depressive symptoms and IADLs impairment. CONCLUSION: This paper discusses what is known about the various subgroups as well as the treatment of depressive symptoms and ADL impairment in older populations. It also gives policy and practice recommendations for the future that may help rehabilitate and maintain the mental health and ADLs independence of older adults. (PsycInfo Database Record (c) 2024 APA, all rights reserved).

Imaging investigation of cervicocranial artery dissection by using high resolution magnetic resonance VWI and MRA: qualitative and quantitative analysis at different stages.

BACKGROUND: To explore the value of magnetic resonance angiography (MRA) and high resolution magnetic resonance vessel wall imaging (HRMR-VWI) in cervicocranial artery dissection (CCAD) for the disease diagnosis, course staging and treatment. On the basis of qualitative evaluation, this study also extract the changes of different stages in vessel wall in different vessel segments to identify imaging indicators for the quantitative evaluation of CCAD. METHODS: We retrospectively enrolled 34 patients with CCAD (38branches) with conventional MRA and HRMR-VWI examinations. Two radiologists independently analyzed imaging features of vessel wall and lumen in the different stages, and the typical sign detection of artery dissection were compared between MRA and HRMR-VWI. Then the parameters of vessel wall was quantitatively evaluated by the post-processing software (Vesselmass, Leiden University Medical Center, Leiden, The Netherlands. RESULTS: HRMR-VWI revealed typical sign detection of artery dissection in all patients in the acute and subacute stage. Among them, the intimal flap/double lumen sign ditection were more common than the MRA, there was significant difference (P = 0.012). MRA revealed typical sign detection of artery dissection in more than half the patients, and the detection was no significant difference at the chronic stage between MRA and HRMR-VWI (P = 1.000/1.000/0.761). In the acute and subacute stage, the typical sign detection of intramural hematoma and Grade II enhancement revealed by HR-MRI was higher than the observations in the chronic stage (P = 0.000/0.000/0.016), while there was no significant difference by MRA (P = 0.902). The values of wall thickness, relative signal intensity of vessel wall enhancement, relative signal intensity of intramural hematoma (IMH), and percentage of stenosis in CCAD decreased from acute to subacute and then to chronic stages. Each quantitative parameter in patients with CCAD in the early stages (i.e., acute and subacute stages) was significantly different from that in patients with CCAD in the recovered group at chronic stage (P < 0.05). Wall thickness and relative signal intensity of vessel wall enhancement in patients with CCAD in the early stages were not significantly different from those in patients with CCAD in the incompletely recovered group at chronic stage (P > 0.05). CONCLUSIONS: As the only noninvasive imaging technology, HRMR-VWI displays the structure of the vessel wall in vivo, showing not only excellent performance in the early diagnosis of CCAD, but also describing the changes of different stages in the qualitative and quantitative characteristics of vessel wall. It also helps to guide the diseasediagnosis, course staging and treatment of CCAD. Although the diagnostic efficacy of MRA was not as good as HRMR-VWI, it should be the first choice of method for routine examination in evaluating CCAD, especially at the chronic stage of CCAD.

Effect of stressors on family adaptation in stroke patients: A parallel multivariable mediation model.

AIMS: The mechanisms underlying how stressors affect family adaptation are unclear. This study determined the relationship between stressors and family adaptation among stroke patients, particularly the parallel mediating role of family function and family resilience. METHODS AND RESULTS: The study was conducted in the neurology ward of a tertiary hospital in China. A total of 335 stroke inpatients were interviewed face-to-face from August 2020 to March 2021. A questionnaire was administered that included demographic characteristics, the Family Inventory of Life Events and Changes, Family Apgar Index Scale, Family Hardiness Index Scale, and Family Adaptation Scale. The demographic data and correlations among the research variables were analyzed. A bootstrap method using the SPSS PROCESS macro was employed to test a mediation model. Family adaptation was negatively related to stressors (r = -0.291, p < 0.01) and positively related to family function (r = 0.531, p < 0.01) and family resilience (r = 0.393, p < 0.01). Furthermore, family function and family resilience played parallel mediating roles between stressors and family adaptation. CONCLUSIONS: This study elaborated how stressors interacted with family adaptation through the mediation of family function and family resilience. The findings suggest that enhancement of family function and family resilience may help to improve family adaptation among stroke patients.

Identification of Solid and Liquid Materials Using Acoustic Signals and Frequency-Graph Features.

Material identification is playing an increasingly important role in various sectors such as industry, petrochemical, mining, and in our daily lives. In recent years, material identification has been utilized for security checks, waste sorting, etc. However, current methods for identifying materials require direct contact with the target and specialized equipment that can be costly, bulky, and not easily portable. Past proposals for addressing this limitation relied on non-contact material identification methods, such as Wi-Fi-based and radar-based material identification methods, which can identify materials with high accuracy without physical contact; however, they are not easily integrated into portable devices. This paper introduces a novel non-contact material identification based on acoustic signals. Different from previous work, our design leverages the built-in microphone and speaker of smartphones as the transceiver to identify target materials. The fundamental idea of our design is that acoustic signals, when propagated through different materials, reach the receiver via multiple paths, producing distinct multipath profiles. These profiles can serve as fingerprints for material identification. We captured and extracted them using acoustic signals, calculated channel impulse response (CIR) measurements, and then extracted image features from the time-frequency domain feature graphs, including histogram of oriented gradient (HOG) and gray-level co-occurrence matrix (GLCM) image features. Furthermore, we adopted the error-correcting output code (ECOC) learning method combined with the majority voting method to identify target materials. We built a prototype for this paper using three mobile phones based on the Android platform. The results from three different solid and liquid materials in varied multipath environments reveal that our design can achieve average identification accuracies of 90% and 97%.

Reactive oxygen species-mediated endoplasmic reticulum stress contributes to osteocyte death induced by orthodontic compressive force.

During orthodontic tooth movement (OTM), osteocytes, the most mechanosensitive cells in alveolar bone, suffer the heavy orthodontic force and initiate alveolar bone resorption on the compression side. However, the inherent mechanisms of compressive force-induced osteocyte death are not fully understood. In this study, we established an OTM model on Sprague-Dawley rats by inserting coil springs to investigate osteocyte damage on the compression side of alveolar bone. We then applied compressive force on the MLO-Y4 osteocyte-like cell line in vitro to explore whether the reactive oxygen species (ROS)-mediated endoplasmic reticulum stress (ERS) pathway is involved in compressive force-induced osteocyte death. We found that the orthodontic force caused apparent alveolar bone loss, osteocyte death, and elevated serum sclerostin and receptor activator of NF-κB ligand (RANKL) levels in rats. In vitro, compressive force inhibited cell viability but increased the LDH leakage and loss of mitochondrial membrane potential in MLO-Y4 cells. Simultaneously, it activated protein kinase RNA-like endoplasmic reticulum kinase (PERK), eukaryotic translation initiation factor 2 (eIF2α), and their downstream pro-apoptotic ERS signaling proteins and caused significant osteocyte apoptosis, which can be blocked by ERS inhibitor salubrinal. Moreover, the compressive force elevated intracellular ROS levels, while the ROS scavenger N-acetyl-L-cysteine (NAC) alleviated ERS and apoptosis in loaded osteocytes. These results suggest that the orthodontic compressive force induced osteocyte apoptosis via the ROS-mediated ERS pathway. This study first proposes the ERS pathway as a new potential pathway for regulating the rate of OTM based on osteocyte death. RESEARCH HIGHLIGHTS: The orthodontic force increases osteocyte death in rat alveolar bone. The compressive force causes osteocyte apoptosis by the endoplasmic reticulum stress (ERS) pathway in vitro. The ROS scavenger NAC blocked compressive force-induced ERS and osteocyte apoptosis.

Discrimination of Polygonati Rhizoma Species: An Investigation Utilizing High-Performance Liquid Chromatography Fingerprints and Chemometrics.

Polygonati Rhizoma has been a famous traditional Chinese medicine (TCM) for two thousand years. It is increasingly being used not just as a traditional herbal medicine but also as a popular functional food. In this study, qualitative and quantitative analysis of PR from three different origins were initially performed using chemical fingerprint and chemometrics methods. Hierarchical cluster analysis (HCA) and Principal component analysis (PCA) were used to classify 60 PR samples from three different origins. The results revealed that the PR samples fell into three clusters related to the origins. In addition, pairwise comparison of varying PR and obtaining chemical markers between different species through the establishment of partial least squares discriminant analysis. Finally, chemical markers 9,13 and 17 were identified by LC/MS as disporopsin, 5,7-dihydroxy-3-(4'-hydroxybenzyl)-6,8-dimethylchroman-4-one and (3R)-5,7-dihydroxy-3-(4'-hydroxybenzyl)-6-methylchroman-4-one or isomer, respectively. In conclusion, these methods can be applied to identify and distinguish the quality of PR with other original plants and provide novel ideas for evaluating herbal products used in TCM.

Design, Synthesis and Biological Evaluation of Novel Pleuromutilin Derivatives Containing 6-Chloro-1-R-1H-pyrazolo[3,4-d]pyrimidine-4-amino Side Chain.

Two series of pleuromutilin derivatives were designed and synthesized as inhibitors against Staphylococcus aureus (S. aureus). 6-chloro-4-amino-1-R-1H-pyrazolo[3,4-d]pyrimidine or 4-(6-chloro-1-R-1H-pyrazolo[3,4-d]pyrimidine-4-yl)amino-phenylthiol were connected to pleuromutilin. A diverse array of substituents was introduced at the N-1 position of the pyrazole ring. The in vitro antibacterial activities of these semisynthetic derivatives were evaluated against two standard strains, Methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300, Staphylococcus aureus (S. aureus), ATCC 29213 and two clinical S. aureus strains (144, AD3) using the broth dilution method. Compounds 12c, 19c and 22c (MIC = 0.25 µg/mL) manifested good in vitro antibacterial ability against MRSA which was similar to that of tiamulin (MIC = 0.5 µg/mL). Among them, compound 22c killed MRSA in a time-dependent manner and performed faster bactericidal kinetics than tiamulin in time-kill curves. In addition, compound 22c exhibited longer PAE than tiamulin, and showed no significant inhibition on the cell viability of RAW 264.7, Caco-2 and 16-HBE cells at high doses (≤8 µg/mL). The neutropenic murine thigh infection model study revealed that compound 22c displayed more effective in vivo bactericidal activity than tiamulin in reducing MRSA load. The molecular docking studies indicated that compound 22c was successfully localized inside the binding pocket of 50S ribosomal, and four hydrogen bonds played important roles in the binding of them.

Glutathione S-Transferase Highly Expressed in Holotrichia parallela Antennae Inactivates the Odorant Unsaturated Aldehyde Volatiles.

Odorant-degrading enzymes in insects play a vital role in maintaining olfactory sensitivity. However, the role and molecular mechanism of glutathione S-transferases (GSTs) in odorant inactivation has been rarely studied. In the present study, 31 GSTs were identified from the antennal transcriptome of Holotrichia parallela. HpGSTd1 possesses the highest transcriptome expression level. Recombinant HpGSTd1 showed degradation activity toward various unsaturated aldehyde volatiles. Furthermore, the metabolite of cinnamaldehyde was identified by high-resolution mass spectrometry (HRMS). The molecular docking analysis and site-directed mutagenesis revealed the key residues of HpGSTd1 in degrading odorants. In addition, the unsaturated aldehyde volatiles elicited the behavioral and electrophysiological responses of H. parallela. Taken together, our findings suggest that HpGSTd1 may play an essential role in inactivating odorants in H. parallela, which provides new insights for identifying molecular targets and exploring effective olfactory regulators for this underground pest.

An Improved YOLOv5-Based Underwater Object-Detection Framework.

To date, general-purpose object-detection methods have achieved a great deal. However, challenges such as degraded image quality, complex backgrounds, and the detection of marine organisms at different scales arise when identifying underwater organisms. To solve such problems and further improve the accuracy of relevant models, this study proposes a marine biological object-detection architecture based on an improved YOLOv5 framework. First, the backbone framework of Real-Time Models for object Detection (RTMDet) is introduced. The core module, Cross-Stage Partial Layer (CSPLayer), includes a large convolution kernel, which allows the detection network to precisely capture contextual information more comprehensively. Furthermore, a common convolution layer is added to the stem layer, to extract more valuable information from the images efficiently. Then, the BoT3 module with the multi-head self-attention (MHSA) mechanism is added into the neck module of YOLOv5, such that the detection network has a better effect in scenes with dense targets and the detection accuracy is further improved. The introduction of the BoT3 module represents a key innovation of this paper. Finally, union dataset augmentation (UDA) is performed on the training set using the Minimal Color Loss and Locally Adaptive Contrast Enhancement (MLLE) image augmentation method, and the result is used as the input to the improved YOLOv5 framework. Experiments on the underwater datasets URPC2019 and URPC2020 show that the proposed framework not only alleviates the interference of underwater image degradation, but also makes the mAP@0.5 reach 79.8% and 79.4% and improves the mAP@0.5 by 3.8% and 1.1%, respectively, when compared with the original YOLOv8 on URPC2019 and URPC2020, demonstrating that the proposed framework presents superior performance for the high-precision detection of marine organisms.

Structural characterization, antioxidant activity, and the effects of Codonopsis pilosula polysaccharides on the solubility and stability of flavonoids.

Codonopsis pilosula (CP) possesses properties related to nourishing the spleen and stomach, and tonifying Qi of the stomach and mind in traditional Chinese medicine (TCM). Codonopsis pilosula polysaccharides (CPPS), which are the primary active components of CP, are thought to be in charge of their extensive use. Rutin, quercetin, luteoloside, and luteolin, are common and pharmacologically significant flavonoids with many pharmacological activities, but their oral bioavailability is limited by poor solubility and stability. In this study, high-performance gel permeation chromatography (HPGPC) estimated the molecular weight of CPPS to be 9.7 × 105 Da. Sugar analysis revealed that CPPS is composed of D-mannose, D-glucose, and D-xylose with a molar ratio of 5.8:1.9:1.0. Moreover, the antioxidant test showed that CPPS had good antioxidant activity. It is worth noting that CPPS integrated the four flavonoids to form a spongy compound that significantly increased the solubilities and stabilities of flavonoids. The bonding constants of the CPPS and flavonoid-derived inclusion complexes ranged from 60 L mol-1 to 2,030,816 L mol-1, which demonstrated the capacity of CPPS to interact with flavonoids intermolecularly to form a drug complex system, resulting in potentially enhanced biopharmaceutical properties of flavonoids. This finding could provide a reference point for further applications of polysaccharides from herbal medicines.