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Ethnopharmacological Relevance: Nocardiosis is an uncommon infectious disease that bears certain similarities to tuberculosis, with a continuous increase in its incidence and a poor prognosis. In traditional Chinese medicine, the leaves of Cajanus cajan (L.) Millsp. are employed to treat wounds, malaria, coughs, and abdominal pain., Aim of the Study: In this study, we investigated the effects and mechanisms of longistylin A (LGA), a natural stilbene isolated from C. cajan, as a potential antibiotic against nocardiosis., Materials and Methods: LGA was isolated from the leaves of C. cajan and assessed using a minimum bactericidal concentration (MBC) determination against Nocardia seriolae. Multi-omics analysis encompassing genes, proteins, and metabolites was conducted to investigate the impact of LGA treatment on N. seriolae. Additionally, quantitative analysis of 40 cytokinins in N. seriolae mycelium was performed to assess the specific effects of LGA treatment on cytokinin levels. Cryo-scanning electron microscopy was utilized to examine morphological changes induced by LGA treatment, particularly in the presence of exogenous trans-zeatin-O-glucoside (tZOG). The therapeutic effect of LGA was investigated by feeding N. seriolae-infected largemouth bass., Results: LGA exhibited significant efficacy against N. seriolae, with MBC value of 2.56 μg/mL. Multi-omics analysis revealed that LGA disrupted glycerophospholipid metabolism and hormone biosynthesis by notably reducing the expression of glycerol-3-phosphate dehydrogenase and calmodulin-like protein. Treatment with LGA markedly disrupted 12 distinct cytokinins in N. seriolae mycelium. Additionally, the addition of exogenous tZOG counteracted the inhibitory effects of LGA on filamentous growth, resulting in mycelial elongation and branching. Furthermore, LGA treatment improved the survival rate of largemouth bass infected with N. seriolae., Conclusions: We found for the first time that LGA from C. cajan exhibited significant efficacy against N. seriolae by interfering with glycerophospholipid metabolism and cytokinin biosynthesis., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier B.V. All rights reserved.)

Scleral lenses (SLs) are large-diameter rigid contact lenses that are a mainstay treatment for eyes with corneal irregularities. In recent years, there has been increased interest in the role of managing dry eye disease (DED) with SLs, as many patients with DED have reported symptomatic relief with SL wear. The role of SLs for DED management when there are associated corneal irregularities is supported by individual case reports and studies. This has prompted practitioners to begin advocating using SLs in DED cases, even in the absence of associated corneal irregularities and other ocular surface diseases (OSDs). There have also been discussions on potentially placing SLs earlier in the treatment hierarchy of DED, where it currently sits at a more advanced level of intervention (Step 3) in the TFOS DEWS II Report. This review will present the currently available, albeit sparse, evidence that supports and suggests this practice, as well as ancillary evidence supporting the purported benefits of SL wear in DED. The advantages of SL wear, such as corneal healing, absence of tear evaporation and contact lens dehydration, and improved visual acuity with associated increased wear comfort, and how this will benefit DED patients will be explored. Conversely, the challenges associated with fitting SLs in DED patients, including increased midday fogging, poor wettability, and subjective patient satisfaction, will also be presented, as well as a discussion on the key considerations for SL fitting in this population. Overall, while more research is needed to support the use of SLs in DED patients without associated corneal irregularities and other forms of OSD, the use of these lenses may prove to have a potentially wider role given their reported ancillary benefits in these populations.

Bioassay-guided purification of the xanthine oxidase (XOD) inhibitory extract of the roots of Ampelopsis japonica resulted in the isolation of two new triterpenoids ( 1-2 ), designated Ampejaponoside A and B, along with sixteen known compounds ( 3-18 ). The structures of Ampejaposide A and B were elucidated by comprehensive analysis of spectroscopic data with the structures of the known compounds 3-18 confirmed by comparison the spectral data with corresponding values reported in literatures. All the isolates were evaluated for their XOD inhibitory activity in vitro . As a result, compounds 2 , 8 , and 14-16 displayed significant XOD inhibitory effect, particularly 16 being the most potent with an IC 50 value of 0.21  μ M, superior to positive substance allopurinol (IC 50 1.95  μ M). Molecular docking uncovered a unique interaction mode of 16 with the active site of XOD. The current study showed that the triterpenoids and polyphenols from A. japonica could serve as new lead compounds with the potential to speed up the development of novel XOD inhibitors with clinical potential to treat hyperuricaemia and gout.

Four novel new isocoumarins, cajanolactone B, C, D1 and D2 (1-4), were isolated from ethanolic extracts of the leaves of Cajanus cajan . The structural elucidation has been completed mainly depending on extensive spectroscopic analysis including UV, IR, NMR (1D and 2D), HRESIMS and chiral analysis. Notably, all these new isocoumarins were found to exist in racemic forms, among which compounds 3 and 4 share the same planar structure. This finding suggests that at least the biosynthesis of isocoumarin in C. cajan is chiral tolerant. A plausible biogenetic pathway of compounds 1-4 is proposed., Competing Interests: The authors declare no conflict of interest that could have appeared to influence the work reported in this paper., (This journal is © The Royal Society of Chemistry.)

Bioactive peptides derived from proteins found in various foods provide significant health benefits, including regulating blood sugar levels by inhibiting carbohydrate-hydrolyzing enzymes. Hydrolysates of peanut protein were prepared using alcalase (AH) or trypsin (TH) to generate antidiabetic peptides with high activity against α-amylase (IC 50 of 6.46 and 5.71 mg/mL) and α-glucosidase (IC 50 of 6.30 and 5.57 mg/mL), as well as antiradical activity to scavenge DPPH • (IC 50 of 4.18 and 3.12 mg/mL) and ABTS •+ (IC 50 of 2.87 and 2.56 mg/mL), respectively. The bioactivities of hydrolysates were greatest in the ultrafiltration-generated F3 fraction (< 3 kDa). The most active fraction was TH-F3, which was purified by gel filtration chromatography to generate sub-fractions (SF). With IC 50 values of 1.05 and 0.69 mg/mL, the F3-SF8 fraction was the most effective at inhibiting the activity of α-amylase and α-glucosidase, respectively. This fraction was further purified using RP-HPLC to generate sub-subfractions (SSF), the most active of which were F3-SF8-SSF9 and SSF10. The peptide sequences F3-SF8-SSF9 and SSF10 were determined using LC-MS/MS. Two novel antidiabetic peptides with the potential to inhibit α-amylase and α-glucosidase were identified, with the sequences Asp-Trp-Arg (476.22 Da, IC 50 of 0.78, and 0.35 mg/mL) and Phe-Tyr (329.15 Da, IC 50 of 0.91, and 0.41 mg/mL). These results suggest that peptides derived from peanut protein are attractive natural ingredients for diabetes management applications., (© 2023. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.)

Three new stilbenoids, namely two rare plant-derived phenanthrenes denominated Cajananthrenes A and B ( 1 , 2 ) and one bibenzyl named Cajanbenzyl ( 3 ), together with a diphenyl ether derivative designated Cajanether ( 4 ), as well as five other known compounds ( 5 - 9 ) were isolated from the ethanolic extract of the leaves of Cajanus cajan . Their structures were determined through extensive spectroscopic analysis including UV, IR, NMR (1D and 2D) and HRESIMS as well. A plausible biogenesis pathway was proposed for the biosynthesis of compounds 1 - 3 . Compounds 1 and 2 displayed moderate anti-inflammatory activity as evident from the inhibitory effect on NO production in LPS-stimulated RAW 264.7 macrophages with IC 50 values of 73.6 and 44.6 μM respectively.

Immunogenic cell death (ICD), one of cell-death types through release of damage-associated molecular patterns from dying tumor cells, activates tumor-specific immune response and elicits anti-tumor immunity by traditional radiotherapy and chemotherapy. However, whether natural products could induce ICD in leukemia is not elucidated. Here, we report dietary γ-mangostin eradicates murine primary leukemic cells and prolongs the survival of leukemic mice. As well, it restrains primary leukemic cells and CD34 + leukemic progenitor cells from leukemia patients. Strikingly, γ-mangostin attenuates leukemic cells by inducing ICD as characterized by expression of HSP90B1, ANXA1 and IL1B. Additionally, γ-mangostin accelerates cytoplasmic chromatin fragments generation, promoting DNA damage response, and enhances cGAS activation, leading to up-regulation of chemokines. Meanwhile, it induces HDAC4 degradation and acetylated histone H3 accumulation, which promotes chemokines transcription. Ultimately, CD8 + T cell is activated and recruited by γ-mangostin-induced chemokines in the microenvironment. Our study identifies γ-mangostin triggers ICD and activates cGAS signaling through DNA damage response and epigenetic modification. Therefore, dietary γ-mangostin would act as a potential agent to provoke anti-tumor immunity in the prevention and treatment of leukemia., Competing Interests: Declaration of Competing Interest The authors declare no competing financial interest., (Copyright © 2023 The Authors. Published by Elsevier Ltd.. All rights reserved.)

Coronaviruses, as enveloped positive-strand RNA viruses, manipulate host lipid compositions to enable robust viral replication. Temporal modulation of the host lipid metabolism is a potential novel strategy against coronaviruses. Here, the dihydroxyflavone pinostrobin (PSB) was identified through bioassay that inhibited the increment of human coronavirus OC43 (HCoV-OC43) in human ileocecal colorectal adenocarcinoma cells. Lipid metabolomic studies showed that PSB interfered with linoleic acid and arachidonic acid metabolism pathways. PSB significantly decreased the level of 12, 13- epoxyoctadecenoic (12, 13-EpOME) and increased the level of prostaglandin E2. Interestingly, exogenous supplement of 12, 13-EpOME in HCoV-OC43-infected cells significantly stimulated HCoV-OC43 virus replication. Transcriptomic analyses showed that PSB is a negative modulator of aryl hydrocarbon receptor (AHR)/cytochrome P450 (CYP) 1A1signaling pathway and its antiviral effects can be counteracted by supplement of FICZ, a well-known AHR agonist. Integrative analyses of metabolomic and transcriptomic indicated that PSB could affect linoleic acid and arachidonic acid metabolism axis through AHR/CYP1A1 pathway. These results highlight the importance of the AHR/CYP1A1 pathway and lipid metabolism in the anti-coronavirus activity of the bioflavonoid PSB., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 Elsevier B.V. All rights reserved.)

Control of Aspergillus flavus is beneficial for the agricultural economy and food safety. Stilbenes exhibit antifungal properties through an unknown mechanism. Here, six stilbenes isolated from Cajanus cajan were screened for anti- A. flavus activity. Among them, pinosylvin monomethyl ether (PME) showed the strongest anti- A. flavus activity and has a broad antifungal spectrum with negligible hemolysis within the concentration range measured. PME inhibited the spore germination of A. flavus and the accumulation of aflatoxin B1. Mechanistic studies showed that PME could bind the cell membrane phospholipids, resulting in increased permeability and decreased fluidity. Further metabolic analysis showed that PME caused the lysis of cell membranes and subsequent collapse of spores, which resulted in a cell wall autolysis-like phenotype. Structure-activity relationship analysis revealed the importance of maintaining amphiphilicity harmony by substituent groups for the antifungal activity of stilbenes. Together, natural stilbenes are promising antifungal lead compounds worthy of further exploration and research for potential application in the food, pharmaceutical, and agricultural industries.

Ethnopharmacological Relevance: The leaves of Eurya chinensis（Chinese Dagang Tea）have been consumed as herbal tea for centuries in Guangdong, China, and have also been used to prevent influenza and treat colds and fevers in traditional Chinese medicine. However, there are no reports on the chemical profile and efficacy of its leaves for the treatment of fever and viral infections., Materials and Methods: The chemical constituents of Eurya chinensis leaves were isolated and identified by phytochemical study and spectroscopic data, E. chinensis extracts and compounds were evaluated for their antiviral activities by cytopathic effect (CPE) reduction and antibody-based EC 50 assay. The antiviral effect of the main component was confirmed by immunofluorescence and transmission electron microscopy. Virtual screening and docking enzyme inhibition experiments were performed to analyze the anti-coronavirus mechanisms of the compounds from E. chinensis leaves., Results: In this study, we found for the first time that E. chinensis leaf extract exhibited inhibitory effects against coronaviruses HCoV-OC43 in vitro. Among 23 monomer compounds isolated from E. chinensis leaf extract, the triterpenoids (betulinic acid, α-amyrin) and the flavonoids (naringenin, eriodictyol and quercetin) showed marked antiviral activity. Microscopic optical analyses further demonstrated that betulinic acid can remove virus particles from HCoV-OC43 infected cells. Virtual screening and docking analysis towards the coronavirus in vogue revealed that betulinic acid was able to bind well to PLpro and Nsp14N7-MTase, and that the flavonoids prefer to bind with PLpro, Nsp3MES, NspP14N7-MTase, Nsp16GTA, and Nsp16SAM. The enzyme inhibition experiments demonstrated that betulinic acid (1) exhibited significant inhibition of PLpro and N7-MTase activity of SARS-CoV-2., Conclusion: This study proposes E. chinensis and its triterpenoids and flavonoids as promising potential treatments for coronaviruses., (Copyright © 2022. Published by Elsevier B.V.)

Optimization of the enzymolysis process for preparing peanut protein hydrolysates using alcalase and trypsin was performed by employing the central composite design (CCD) of response surface methodology (RSM). The independent variables were solid-to-liquid ratio (S/L), enzyme-to-substrate ratio (E/S), pH, and reaction temperature, while the response variables were degree of hydrolysate (DH), α -amylase, and α -glucosidase inhibitory activity. The highest DH (22.84% and 14.63%), α -amylase inhibition (56.78% and 40.80%), and α -glucosidase inhibition (86.37% and 86.51%) were obtained under optimal conditions, which were S/L of 1:26.22 and 1:30 w / v , E/S of 6% and 5.67%, pH of 8.41 and 8.56, and temperature of 56.18 °C and 58.75 °C at 3 h using alcalase (AH) and trypsin (TH), respectively. Molecular weight distributions of peanut protein hydrolysates were characterized by SDS-PAGE, which were mostly ˂10 kDa for both hydrolysates. Lyophilized AH and TH had IC 50 values of 6.77 and 5.86 mg/mL for α -amylase inhibitory activity, and 6.28 and 5.64 mg/mL for α -glucosidase inhibitory activity. The IC 50 of AH and TH against DPPH radical was achieved at 4.10 and 3.20 mg/mL and against ABTS radical at 2.71 and 2.32 mg/mL, respectively. The obtained hydrolysates with antidiabetic activity could be utilized as natural alternatives to synthetic antidiabetics, particularly in food and pharmaceutical products., Competing Interests: The authors declare no conflict of interest.

Two novel secondary metabolites, including one thujopsene-type sesquiterpene designated thujasutchin N ( 1 ) and one norlignan named thujasutchin O ( 2 ) were obtained from the ethanolic extract of the stems and roots of Thuja sutchuenensis . Among them, thujasutchin O ( 2 ) represents the first example of lignan sharing a unique carbon-reduced skeleton with novel acetal functionality. Their structures were unambiguously determined by means of extensively spectroscopic analysis including UV, IR, HRESIMS, NMR, and single crystal X-ray diffraction. Both of the isolates were evaluated for their in vitro cytotoxic and antibacterial activities.

Direct metal printing is a promising technique for manufacturing injection molds with complex conformal cooling channels from maraging steel powder, which is widely applied in automotive or aerospace industries. However, two major disadvantages of direct metal printing are the narrow process window and length of time consumed. The fabrication of high-density injection molds is frequently applied to prevent coolant leakage during the cooling stage. In this study, we propose a simple method of reducing coolant leakage for a direct-metal-printed injection mold with conformal cooling channels by combining injection mold fabrication with general process parameters, as well as solution and aging treatment (SAT). This study comprehensively investigates the microstructural evolution of the injection mold after SAT using field-emission scanning electron microscopy and energy-dispersive X-ray spectroscopy. We found that the surface hardness of the injection mold was enhanced from HV 189 to HV 546 as the Ni-Mo precipitates increased from 12.8 to 18.5%. The size of the pores was reduced significantly due to iron oxide precipitates because the relative density of the injection mold increased from 99.18 to 99.72%. The total production time of the wax injection mold without coolant leakage during the cooling stage was only 62% that of the production time of the wax injection mold fabricated with high-density process parameters. A significant savings of up to 46% of the production cost of the injection mold was obtained.

Inulin as a commercial prebiotic could selectively promote the growth of beneficial gut microbes such as lactic acid bacteria (LAB). Whether LAB in rabbit gut possesses the capability to metabolize and utilize inulin is little known. Therefore, this study recovered 94 LAB strains from neonate rabbits and found that only 29% (28/94) could metabolize inulin with both species- and strain-specificity. The most vigorous inulin-degrading strain, Lacticaseibacillus paracasei YT170, could efficiently utilize both short-chain and long-chain components through thin-layer chromatography analysis. From genomic analysis, a predicted fosRABCDXE operon encoding putative cell wall-anchored fructan β-fructosidase, five fructose-transporting proteins and a pts1BCA operon encoding putative β-fructofuranosidase and sucrose-specific IIBCA components were linked to long-chain and short-chain inulin utilization respectively. This study provides a mechanistic rationale for effect of inulin administration on rabbits and lays a foundation for synbiotic applications aimed at modulating the intestinal microbiota of young rabbits., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2021 Zhu, Yue, Li, Qiu, Xu, Wu, Yao, Zuo, Li and Li.)

Backgrounds: Liver hepatocellular carcinoma (HCC) is one of the most malignant tumors, of which prognosis is unsatisfactory in most cases and metastatic of HCC often results in poor prognosis. In this study, we aimed to construct a metastasis- related mRNAs prognostic model to increase the accuracy of prediction of HCC prognosis., Methods: Three hundred seventy-four HCC samples and 50 normal samples were downloaded from The Cancer Genome Atlas (TCGA) database, involving transcriptomic and clinical data. Metastatic-related genes were acquired from HCMBD website at the same time. Two hundred thirty-three samples were randomly divided into train dataset and test dataset with a proportion of 1:1 by using caret package in R. Kaplan-Meier method and univariate Cox regression analysis and lasso regression analysis were performed to obtain metastasis-related mRNAs which played significant roles in prognosis. Then, using multivariate Cox regression analysis, a prognostic prediction model was established. Transcriptome and clinical data were combined to construct a prognostic model and a nomogram for OS evaluation. Functional enrichment in high- and low-risk groups were also analyzed by GSEA. An entire set based on The International Cancer Genome Consortium(ICGC) database was also applied to verify the model. The expression levels of SLC2A1, CDCA8, ATG10 and HOXD9 are higher in tumor samples and lower in normal tissue samples. The expression of TPM1 in clinical sample tissues is just the opposite., Results: One thousand eight hundred ninety-five metastasis-related mRNAs were screened and 6 mRNAs were associated with prognosis. The overall survival (OS)-related prognostic model based on 5 MRGs (TPM1,SLC2A1, CDCA8, ATG10 and HOXD9) was significantly stratified HCC patients into high- and low-risk groups. The AUC values of the 5-gene prognostic signature at 1 year, 2 years, and 3 years were 0.786,0.786 and 0.777. A risk score based on the signature was a significantly independent prognostic factor (HR = 1.434; 95%CI = 1.275-1.612; P < 0.001) for HCC patients. A nomogram which incorporated the 5-gene signature and clinical features was also built for prognostic prediction. GSEA results that low- and high-risk group had an obviously difference in part of pathways. The value of this model was validated in test dataset and ICGC database., Conclusion: Metastasis-related mRNAs prognostic model was verified that it had a predictable value on the prognosis of HCC, which could be helpful for gene targeted therapy.

Binocular rivalry is the phenomenon that when two incompatible images are simultaneously presented, one to each eye, the two images compete with each other to be the dominant percept. Studying the underlying neural mechanisms of binocular rivalry is useful for understanding the mechanisms of interocular inhibition. Levelt's Propositions, a set of four propositions that were originally published over fifty years ago, are not only useful for characterizing the perceptual dynamics of binocular rivalry, but can also provide a metric for assessing the common or differential neural mechanisms of binocular rivalry when diverse stimulus types are used. In the present study, we conducted a series of psychophysics experiments, where we compared the rivalry dynamics of two quite different types of stimuli. Orthogonal gratings, a classic type of rivalry stimulus, were contrasted with luminance patches, a type of rivalry stimulus that is relatively less studied. Our results showed that, similar to the orthogonal gratings, the alternate percepts in luminance-only rivalry were described by the modified Levelt's Propositions, despite the clearly slower alternation rates for luminance patches. However, unlike the mixed percepts observed during transitions between oriented gratings, fusion percepts during luminance rivalry were common, could be lustrous, and obeyed the same Propositions, suggesting a regime of tri-stability. Overall, both types of rivalry are consistent with recent models that posit separate binocular and monocular channels embedded within neural circuits that also accomplish contrast normalization. Finally, luminance rivalry is discussed in the contexts of binocular summation and suppression, as well as Fechner's paradox., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2020 The Authors. Published by Elsevier Ltd.. All rights reserved.)

Three new pterocarpans, named abrusprecatins A-C ( 1-3 ), along with three known ones, namely medicarpin ( 4 ), maackiain ( 5 ), and 4-hydroxy-3-methoxy-8,9-methylenedioxypterocarpan ( 6 ) were isolated from the aerial parts of Abrus precatorius . The structures of these compounds were established by extensive analysis of mass spectrometric data, 1 D and 2 D NMR spectroscopic data. In addition, the absolute configurations were determined by a combination of single crystal X-ray diffraction analysis and circular dichroism spectroscopy.

Eight new sesquiterpenes with diverse skeletons involving four cuparenes, denominated thujasutchins F-I (1-4), one eudesmane and one cedrol, named thujasutchin J (5) and thujasutchin K (6), as well as two thujopsenes thujasutchins L-M (7-8) together with three known congener compounds (9-11) were isolated from EtOAc soluble fraction of ethanolic extract of the stems and roots of Thuja sutchuenensis. Their structures including absolute configurations were unambiguously established by extensive interpretation of the NMR and mass spectroscopic data, X-ray diffractions, and ECD measurements powered by molecular calculations. The biological assays disclosed that 5 and 9 displayed potent inhibitory effect against Staphylococcus. aureus (CMCC 26003), methicillin-resistant Staphylococcus aureus (JCSC 4744), Bacillus cereus (ATCC 10876), and Staphylococcus epidermidis (ATCC 12228) with MICs ranging from 6.25 to 25 μg/mL., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2020 Elsevier Inc. All rights reserved.)

A phytochemical investigation on the stems and leaves of Clausena lenis led to the isolation of a new furanocoumarin, clauselenisin A ( 1 ), together with five known analogues ( 2 - 6 ). The structure of 1 was elucidated by extensive spectroscopic methods and the known compounds were identified by comparisons with data reported in the literature. All known compounds ( 2 - 6 ) were isolated from C. lenis for the first time. All isolated compounds were evaluated for their their antiproliferative activities against five human cancer cell lines: HL-60, SMMC-7721, A-549, MCF-7 and SW480 in vitro . Compounds 1 - 6 showed significant antiproliferative effects with IC 50 values ranging from 0.36 to 16.48 μM.

A phytochemical investigation on the leaves of Callistemon viminalis resulted in the isolation of two unusual compounds, callistemonols A ( 1 ) and B ( 2 ). Callistemonol A ( 1 ) possesses a novel skeleton of a furan ring fusing both an α,β-triketone and a phloroglucinol unit, while callistemonol B ( 2 ) is an acylphloroglucinol derivative featuring two methyl substituents on a five-membered ring and an isovaleryl side chain. Their structures were fully characterized on the basis of extensive spectroscopic analysis, including 1D and 2D NMR parameters, as well as the IR and HRESIMS data. Callistemonol A ( 1 ) represents an example of a natural dibenzofuran with two phenyl moieties, and a plausible biogenetic pathway to generate this novel dibenzofuran through a C-C bond-forming radical SAM enzyme is proposed. Moreover, antimicrobial assays, in conjunction with time-killing and biophysical studies, revealed that 1 and 2 exert potent bactericidal activities against a panel of methicillin-resistant pathogenic microbes.

Two new polyketide metabolites, the 12-membered macrolides 4-hydroxy-12-methyloxacyclododecane-2,5,6-trione ( 1 ) and 12-methyloxacyclododecane-2,5,6-trione ( 2 ), were isolated from the endophytic fungal strain Cladosprium colocasiae A801 of the plant Callistemon viminalis , together with five known derivatives . Their structures were fully characterized by means of detailed spectroscopic analysis for new structures, and in comparison with published data for known compounds. The antibacterial, cytotoxic, and α-glucosidase inhibitory activities of the new compounds 1 and 2 were evaluated.

Three new prenylated stilbenes, named as cajanusins A-C (1-3), and one new natural product cajanusin D (4), along with six known derivatives (5-10) were isolated from the leaves of Cajanus cajan. Their structures were fully elucidated by means of extensive spectroscopic methods and comparison with data in the reported literatures. The new compounds of 1 and 2 were evaluated for in vitro cytotoxic activities against a panel of human cancer cell lines., (Copyright © 2019 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

Five new compounds including two stilbenes, designated thujasutchins A (1) and B (2), two phenolic compounds namely thujasutchins C (3) and D (4), as well as one sesquiterpene thujasutchin E (5), were isolated from the 95% ethanolic extract from the trunks and roots of Thuja sutchuenensis. Their structures were determined by means of extensively spectroscopic analysis including UV, IR, HRESIMS, 1 H and 13 C NMR (COSY, HSQC, HMBC). Moreover, compounds 1, 3-5 were evaluated for in vitro cytotoxic activities against SF-268, MCF-7, HepG-2, and A549 tumor cell lines., (Copyright © 2019 Elsevier B.V. All rights reserved.)

Two pairs of novel enantiomeric flavonoids (1a, 1b and 2a, 2b), along with one new lignan (3), were isolated from the aerial parts of Abrus precatorius. All of these enantiomeric flavonoids featured an unprecedented propylated flavonoid skeleton representing a new family of flavonoid, and the new lignan was found to have an attractive arachidate ester side chain. Their structures were extensively elucidated by means of detailed NMR and mass spectroscopic analysis. Moreover, biological evaluation of antibacterial activity for these compounds against Bacillus cereus and Escherichia coli were conducted., (Copyright © 2018 Elsevier B.V. All rights reserved.)

Ethnopharmacological Relevance: The leaves of Rhodomyrtus tomentosa are traditionally used in the treatment of infectious diseases such as wound infections in Chinese traditional medicine. The mechanisms of the activity of rhodomyrtosone B (RDSB), a natural acylphloroglucinol isolated from the leaves of Rhodomyrtus tomentosa, are still not understood. We provided a detailed investigation of the antibacterial action of RDSB against bacteria in vitro and in vivo., Materials and Methods: The antibacterial activity of RDSB was tested by the microdilution method against a panel of bacteria, and a time-killing assay was carried out according to CLSI guidelines. The cytotoxic potential of RDSB was evaluated against mammalian cells, and its haemolytic activity towards rabbit red blood cells (RBCs) was assessed. The mode of action of RDSB was investigated by targeting bacterial membranes, and its resistance was evaluated using a sequential passaging method. The antibacterial activities in vivo were assessed against MRSA in a mouse skin infection mode., Results: RDSB exhibited distinct antibacterial activities against selected Gram-positive pathogens responsible for serious infections, even including methicillin-resistant Staphylococcus aureus (MRSA) with a minimum inhibitory concentration (MIC) of 0.62-1.25 µg/mL and vancomycin-resistant Enterococcus faecium (VRE) with an MIC of 2.5 µg/mL. RDSB displayed much more rapid bactericidal activity against MRSA than that of vancomycin. The membrane-targeting experiments revealed that RDSB exhibited significant antibacterial activity with the perturbation of bacterial membrane potential and an increase in membrane permeability. In particular, RDSB had weak cytotoxicity to mammalian cells (IC 50 >14 µg/mL) and has advantageous specificity against selected Gram-positive bacterial membranes rather than RBCs. Notably, RDSB displayed in vitro antibacterial activities against MRSA without drug-resistance and profoundly attenuated the skin ulcer formation in a murine model of MRSA infection under a single dose of 40 µg RDSB per mouse., Conclusion: RDSB has profound antibacterial activity against drug-resistant bacteria (MRSA and VRE) and low cytotoxicity. It is bactericidal in nature, and an increase in membrane permeability resulting from membrane perturbation is one of its modes of action. RDSB represents a promising natural antibiotic to combat drug-resistant (MRSA and VRE) infections., (Copyright © 2018 Elsevier B.V. All rights reserved.)

Two new ent-kaurane diterpenes (1-2), together with five known analogs, were isolated from the stems of Eurya chinensis. The structures of new compounds were established by extensive analysis of mass spectrometric and 1D and 2D NMR spectroscopic data. Compound 3 exhibited noticeable anti-inflammatory activity as denoted by inhibiting LPS-induced nitric oxide (NO) production in RAW264.7 cells with an IC 50 value of 7.82 μM. Compound 4 showed potent cytotoxic activity against human cancer cell lines NCI-H46, HepG2 and SW480 with IC 50 values ranging from 7.45 to 8.54 μM.

Methicillin-resistant Staphylococcus aureus (MRSA) infections are well-known as a significant global health challenge. In this study, twenty-two congeners of the natural antibiotic rhodomyrtosone B (RDSB) were synthesized with the aim of specifically enhancing the structural diversity through modifying the pendant acyl moiety. The structure-activity relationship study against various MRSA strains revealed that a suitable hydrophobic acyl tail in the phloroglucinol scaffold is a prerequisite for antibacterial activity. Notably, RDSB analogue 11k was identified as a promising lead compound with significant in vitro and in vivo antibacterial activities against a panel of hospital mortality-relevant MRSA strains. Moreover, compound 11k possessed other potent advantages, including breadth of the antibacterial spectrum, rapidity of bactericidal action, and excellent membrane selectivity. The mode of action study of compound 11k at the biophysical and morphology levels disclosed that 11k exerted its MRSA bactericidal action by membrane superpolarization resulting in cell lysis and membrane disruption. Collectively, the presented results indicate that the novel modified RDSB analogue 11k warrants further exploration as a promising candidate for the treatment of MRSA infections.

Three new dimeric kavalactones, designated as diyangonins A-C (1-3), along with two known analogs were isolated from the roots of Piper methysticum. Their structures were elucidated by means of extensive analysis of their 1D, 2D NMR, and mass spectroscopic data. All these dimers possess a skeleton featuring a cyclobutane ring connecting two kavalactone units in head-to-tail or head-to-head mode. Compounds 1-5 were evaluated for their cytotoxic activities against human tumor cell lines.

Two new stilbenoid dimers, cajanstilbenoids A (1) and B (2), were isolated from the leaves of Cajanus cajan. Planar structures of these compounds were verified by NMR (1D and 2D) and high-resolution electrospray ionization mass spectroscopy (HR-ESI-MS). Absolute configurations were assigned by comparing experimental and calculated electronic CD values. The cytotoxicity of 1 and 2 against human hepatoma (HepG2), human breast adenocarcinoma (MCF-7), and human lung cancer (A549) cells were evaluated in vitro. Compound 1 showed strong cytotoxicity against all the tested cell lines (IC 50 values: 2.14-2.56 µM), whereas compound 2 showed strong toxicity only against HepG2 (IC 50 value: 5.99 µM) and A549 cells (IC 50 value: 6.18 µM).

One new ent-kaurane diterpene derivative (1), along with four known diterpenes, was isolated from the stems of Eurya chinensis R.Br. The structure of the new compound was established by extensive analysis of mass spectrometric and 1D and 2D NMR spectroscopic data. Compound 1 showed moderate anti-inflammatory activities with IC 50 value of 8.12 μM. This is the first example of diterpenoids with 4-hydroxy-4-(2-hydroxyethyl)-1-hydroxyl-cyclohexanoyl substituent.

Three new kavalactone dimers, designated as yangonindimers A-C (1-3), along with one known analogue were isolated from the roots of Piper methysticum. Their structures were elucidated via extensive analysis of their 1D, 2D NMR and mass spectroscopic data. All these dimers possess a skeleton featuring a cyclobutane ring connecting two kavalactone units. Compounds 1-4 were evaluated for their cytotoxic activities against human tumour cell lines NCI-H46, SW480 and HepG2, but none showed significant activity.

Background: Few studies have investigated the association between puerperal women's living situation and postpartum depression. The aim of this study was to examine the association between living with parents or with parents-in-law and postpartum depression among Chinese puerperal women., Methods: A total of 1126 participants who completed questionnaire were included in our analysis. Postpartum depression status was assessed using the Edinburgh Postnatal Depression Scale. Logistic regression models were used to estimate the association between living with puerperal women's parents or with parents-in-law and risk of postpartum depression after adjustment for potential confounders., Results: The prevalence of postpartum depression among participants was 11.8%. Of the 1126 participants, 524 (46.5%) lived only with their husbands, 387 (34.4%) lived with their parents-in-law, and 215 (19.1%) lived with their parents. Compared with those living only with their husbands, puerperal women living with their parents-in-law had higher risk of postpartum depression after adjustment for potential confounders (OR=2.48; 95% CI: 1.20, 5.15). No association between living with puerperal women's parents and postpartum depression was found after adjustment for confounders (OR=1.05; 95%CI: 0.42, 2.65)., Limitations: Although we adjusted for a wide range of potential confounders, we cannot rule out the possibility of residual confounding by other unmeasured factors, such as breastfeeding, intimate partner violence, and marital relationship., Conclusions: Our findings suggest that living with parents-in-law may be a risk factor for postpartum depression among Chinese puerperal women. Future preventive interventions should include strategies that target the puerperal women who lived with parents-in-law., (Copyright © 2017 Elsevier B.V. All rights reserved.)

A new acylphloroglucinol with a novel architecture including an unprecedented dearomatic dibenzofuran core, named callistemenonone A (1), was isolated from the leaves of Callistemon viminalis (Myrtaceae). The structure was fully characterized on the basis of extensive spectroscopic analysis, including UV, HRESIMS, as well as 1D and 2D NMR spectral data (HSQC, HMBC, and ROESY). The deduced structure represents the first example of a natural dibenzofuran with two phenyl moieties coupling through tertiary hydroxy and ketal carbons. A plausible biogenetic pathway involving oxidative coupling and dearomatization as key steps is proposed to account for the biosynthesis of this novel class of dibenzofuran. Moreover, antimicrobial assays, in conjunction with the time-killing and biophysical studies, revealed that 1 exerted potent bactericidal activity against a panel of methicillin resistant pathogenic microbes with a unique mechanism.

Two new coumarins, named (±)-euryacoumarin A (1) and 6-demethylobtusinin (2), and one new natural coumarin, named euryacoumarin B (3), along with two known compounds, scopoletin (4) and obtusinol (5), were isolated from the stems of Eurya chinensis. Their structures were elucidated by means of extensive spectroscopic methods and comparison with data reported in the literatures. Compound 1 exhibited significant inhibition of LPS-induced nitric oxide (NO) production in RAW264.7 cells with IC 50 value of 35.64 ± 1.73 μM, and showed marginal antibacterial activities against Bacillus subtilis and B. cereus with MIC values of 50.59 ± 2.12 and 35.42 ± 0.96 μM, respectively.

Cytosporaphenones A-C, one new polyhydric benzophenone and two new naphtopyrone derivatives, along with eight known ones, were isolated from Cytospora rhizophorae, an endophytic fungus from Morinda officinalis. Their structures were fully characterized by means of detailed spectroscopic analysis and X-ray single crystal diffraction. To our knowledge, the three new compounds were the most highly oxygenated metabolites of their families discovered in nature. Moreover, all of the compounds were evaluated for in vitro cytotoxic activities against MCF-7, NCI-H460, HepG-2 and SF-268 tumor cell lines, and the new compound 1 exhibited weak growth inhibitory activity against the tumor cell lines MCF-7 and HepG-2 with IC 50 values of 70 and 60μM, respectively., (Copyright © 2016 Elsevier B.V. All rights reserved.)

Callviminols A-E (1-5), five rare phloroglucinols bearing a framework embodying a hexahydrodibenzo[b,d]furan or 2-phenylcyclohexanol nucleus derived from a phloroglucinol-monoterpene adduct, were isolated from the leaves of Callistemon viminalis. Their structures were established via extensive spectroscopic measurements, with the absolute configuration of 5 determined by electronic circular dichroism (ECD) calculations. The plausible biogenetic pathway suggested that a unique oxidative radical addition and classic cationic cyclization were key biosynthetic steps., (Copyright © 2016 Elsevier B.V. All rights reserved.)

A general and excellent acylation reagent, diacyl disulfide, was uncovered for efficient ester formation enabled by DMAP (4-(N,N-dimethylamino)pyridine) catalysis. This protocol offered a promising synthetic platform on site-selective acylation of phenolic and primary aliphatic hydroxyl groups, which greatly expanded the realm of protecting group chemistry. The importance of the reagent was also reflected by its excellent moisture tolerance, high efficiency, and potential in synthetic chemistry and biologically meaningful natural product modification.

A phytochemical study on the leaves of Callistemon viminalis, a widely distributed ornamental and medicinal plant of agricultural importance in China, resulted in the isolation of eleven acylphloroglucinols, including six new ones named callistenones F-K (1-6), as well as five known congeners. Their structures were fully characterized using spectral data interpretation for the new structures and compared to published data for the known ones. All the isolated compounds were evaluated for in vitro antimicrobial activity and growth inhibitory activity against four tumor cell lines (MCF-7, NCI-H460, SF-268 and HepG-2)., (Copyright © 2016 Elsevier B.V. All rights reserved.)

Two novel meroterpenoids, rhodomentones A and B bearing an unprecedented caryophyllene-conjugated oxa-spiro[5.8] tetradecadiene skeleton, were isolated from the leaves of Rhodomyrtus tomentosa. Their structures with unique NMR characteristics were determined by extensive spectroscopic analysis, single-crystal X-ray diffraction, quantum molecular calculation, chemical transformation as well as total synthesis.

Phytochemical study on the leaves of Rhodomyrtus tomentosa resulted in the isolation of fourteen compounds including a new acylphloroglucinol, named tomentosone C (1), and a new flavonol glycoside, namely myricetin-3,7,3'-trimethyl ether-5'-O-β-glucopyranoside (2). Their structures were characterized by spectral data interpretation for new structures and in comparison with published data for known compounds. The antimicrobial activity evaluation revealed that 1 and the known acylphloroglucinol rhodomyrtone (3) exhibited significant antimicrobial activity with MIC 3.66 and 1.83 μg ml(-1), respectively, toward Staphylococcus aureus, responsible for the antimicrobial activity observed with the n-hexane and EtOAc-soluble fraction of the ethanol extract of R. tomentosa leaves.

Objective: To study the chemical constituents from Mitrasacme pygmaea., Methods: The compounds were isolated and purified by column chromatography and their structure were identified by NMR and MS,and comparison spectral data with literature., Results: Eleven compounds were isolated and identified as tricin-7-O-β-D-glucopyranoside( 1),massonianoid A( 2),kaempferol( 3),cinnamic acid( 4),quercetin( 5),tiliroside( 6),tricin( 7),β-sitosterol( 8),adenosine( 9),α-tocopherolquinone( 10)and β-daucosterol( 11)., Conclusion: All the compounds are isolated from this genus for the first time.

Objective: To study the chemical constituents from Periploca forrestii., Methods: The constituents were separated by column chromatography and their structures were elucidated by spectroscopic methods., Results: Seven compounds were isolated from Periploca forrestii and identified as wogonin( 1),negletein( 2),vanilline( 3),isovanilline( 4),periplocoside L( 5),β-sitosterol( 6) and β-daucosterol( 7)., Conclusion: Compounds 1 and 2 are obtained from this genus for the first time,and compounds 3 ~ 5 are isolated from this plant for the first time.

A new natural halogen-containing stilbene derivative was isolated from the leaves of Cajanus cajan (L.) Millsp. and identified as 3-O-(3-chloro-2-hydroxyl-propanyl)-longistylin A by comprehensive spectroscopic and chemical analysis, and named cajanstilbene H (1). It is the first halogen-containing stilbene derivative found from plants. In human mesenchymal stem cells (hMSC) from bone marrow, 1 did not promote cell proliferation, but distinctly enhanced osteogenic differentiation of hMSC in time- and dose-dependent manners. In six human cancer cell lines, 1 showed a moderate inhibitory effect on cell proliferation, with IC50 values of 21.42-25.85 μmol·L(-1).

The present study was designed to synthesize derivatives of E-resveratrol and evaluate their cytotoxic activity in vitro. Different functional groups were conjugated with the phenolic hydroxyl group of E-resveratrol, and the double bond of E-resveratrol was reduced. The in vitro cytotoxicity of the synthetic derivatives was evaluated against three tumor cell lines (A549, LAC, and HeLa) using the MTT assay. Twenty-six E-resveratrol derivatives were synthesized and their structures were confirmed by (1)H NMR, MS, IR, and elemental analyses. Compounds 1-6, 12, 15-21, and 23-26 were reported for the first time. Among them, Compounds 1, 2, 4, 5, and 9-11, showed significant cytotoxicity against tumor cells; especially, Compound 1 showed an IC50 value of 4.38 μmol · L(-1) in the A549 cells which was 15-fold more active than E-resveratrol; Compound 9 showed an IC50 value of 1.41 μmol · L(-1) in the HeLa cell line which was 90-fold more active than E-resveratrol, and close to adriamycin. The structure-activity relationships were also investigated. Compounds 1, 2 and 9-11 may serve as potential lead compounds for the discovery of new anticancer drugs., (Copyright © 2015 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

The present study was designed to identify potent anti-tumor compounds from a series of new longistylin C derivatives. Ten longistylin C derivatives were synthesized and their structures were confirmed by (1)H NMR, MS, and elemental analyses. Their cytotoxicity in vitro against three human cancer cell lines (A549, HepG2, and MCF-7) were evaluated by the MTT assay. Among these compounds, DT-6 and DT-9 displayed much better cytotoxicity against A549, HepG2, and MCF-7 cells, DT-1 exhibited selective cytotoxicity against HepG2, and the structure-activity relationships were investigated. In conclusion, Compounds DT-6 and DT-9 may serve as potential lead compounds for the discovery of new anti-cancer drugs., (Copyright © 2015 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

Natural products possessing anticancer activity have been extensively studied because of their low toxicity and potential effect. α-Mangostin, a component of Garcinia mangostana Linn, is a xanthone derivative shown to have antioxidant and antitumor properties. This study was carried out to investigate how to improve the anticancer effects of α-mangostin in chronic myeloid leukemia (CML) cell lines bearing wild-type BCR-ABL or BCR-ABL-T315I mutation. We showed that α-mangostin inhibited cell proliferation of K562, KBM5 and KBM5-T315I cells in both a time- and dose-dependent manner. Significantly, α-mangostin increased the number of apoptotic cells and induced DNA fragmentation compared to control cells. Moreover, α-mangostin selectively inhibited proliferation in primary CML cells, while showing limited lethality in normal hematopoietic progenitors. Additionally, α-mangostin induced not only apoptosis but also autophagy in CML cells. α-Mangostin dramatically increased the expression levels of LC-3II, an autophagosome marker in mammals, and the accumulation of autophagic vacuoles (AVs). Inhibition of autophagy by chloroquine enhanced α-mangostin-mediated cytotoxicity through increasing apoptosis. Taken together, our data suggest that targeting the autophagy pathway is a promising therapeutic strategy to enhance α-mangostin-induced apoptosis. Our study provides an approach for future studies to explore this combination for the treatment of CML.

Griffipavixanthone (GPX) is a dimeric xanthone which was isolated in a systematic investigation of Garcinia oblongifolia Champ. In this study, we investigate the effect of GPX on cell proliferation and apoptosis on human Non-small-cell lung cancer (NSCLC) cells in vitro and determine the mechanisms of its action. GPX inhibited the growth of H520 cells in dose- and time-dependent manners, with IC50 values of 3.03 ± 0.21 μM at 48 h. The morphologic characteristics of apoptosis and apoptotic bodies were observed by fluorescence microscope and transmission electron microscope. In addition, Annexin V/PI double staining assay revealed that cells in early stage of apoptosis were significantly increased upon GPX treatment dose-dependently. Rh123 staining assay indicated that GPX reduced the mitochondrial membrane potential. DCFH-DA staining revealed that intracellular ROS increased with GPX treatment. Moreover, GPX cleaved and activated caspase-3. In summary, this study showed that GPX inhibited H520 cell proliferation in dose- and time-dependent manner. Further mechanistic study indicated that GPX induced cell apoptosis through mitochondrial apoptotic pathway accompanying with ROS production. Our results demonstrate the potential application of GPX as an anti-non-small cell lung cancer agent.

A new prenylxanthone, garcimangostanol (1), was isolated from the EtOAc-soluble partition of the ethanol extract of the pericarp of Garcinia mangostana L., along with three known compounds, namely 8-deoxygartanin (2), 1-isomangostin (3), and garcinone C (4). The structure of compound 1 was elucidated on the basis of its 1D, 2D NMR and MS data. Compounds 1-4 exhibited either significant o r moderate cytotoxicity against MCF-7, A549, Hep-G2 and CNEhuman cancer cell lines in vitro with IC50 values from 4.0 +/- 0.3 to 23.6+/- 1.5 microM by MTT colorimetric assay.

A new isobenzofuranone, 4-(methoxymethyl)-7-methoxy-6-methyl-1(3H)-isobenzofuranone (1), together with seven known compounds, dilation (2), lumichrome (3), curvulari (4), 5,5'-oxy-dimethylene-bis(2-furaldehyde) (5), chromone (6), harman(1-methyl-β-carboline) (7), N9-methyl-1methyl-β-carboline (8), was isolated from the mangrove endophytic fungus, Penicillium sp. ZH58 obtained from the South China Sea coast. Their structures were determined by analysis of spectroscopic data. Compound 1 exhibited cytotoxicity against KB and KBV200 cells with IC50 values of 6 and 10 μg/mL, respectively.