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The hot deformation behavior of AZ42 alloy was observed using thermal compression tests at a temperature scope of 250–400 °C and strain rate scope of 0.001–1 s−1. True stress-strain curves exhibited a combination of work hardening and dynamic softening features. A Northern Goshawk algorithm (NGO)-optimized artificial neural network (ANN) model was proposed. The established NGO-ANN model demonstrated impressive prediction accuracy, achieving a high determination coefficient of 0.991, a mean absolute percentage error of 3.51 %, and a root mean square error of 2.73. Subsequently, three-dimensional (3D) hot processing map based on the dynamic material model (DMM) theory was created. There were three different regions within the processing maps: the flow instability region (region A: 250–260 °C, 0.02–1 s−1, and region B: 300–400 °C, 0.01–0.1 s−1), high-power dissipation coefficient region (region C: 350–400 °C, 0.001–0.02 s−1, and region D: 300–350 °C, 0.5–1 s−1), and low power dissipation efficiency safety region (region E: the rest ones). Microstructural analysis revealed significant local plastic flow features in the flow instability region and a combination of coarse initial deformation grains and fine dynamic recrystallization (DRX) grains in the low power dissipation efficiency safety region. Fine and uniform grains were observed in the high-power dissipation efficiency region with DRX degree VDRX as high as 85.6 %, resulting in the best mechanical properties. Based on the established 3D hot processing map, the optimal process domains were determined.

Ultra-Wideband (UWB) technology is crucial for indoor localization systems due to its high accuracy and robustness in multipath environments. However, Non-Line-of-Sight (NLoS) conditions can cause UWB signal distortion, significantly reducing positioning accuracy. Thus, distinguishing between NLoS and LoS scenarios and mitigating positioning errors is crucial for enhancing UWB system performance. This research proposes a novel 1D-ConvLSTM-Attention network (1D-CLANet) for extracting UWB temporal channel impulse response (CIR) features and identifying NLoS scenarios. The model combines the convolutional neural network (CNN) and Long Short-Term memory (LSTM) architectures to extract temporal CIR features and introduces the Squeeze-and-Excitation (SE) attention mechanism to enhance critical features. Integrating SE attention with LSTM outputs boosts the model’s ability to differentiate between various NLoS categories. Experimental results show that the proposed 1D-CLANet with SE attention achieves superior performance in differentiating multiple NLoS scenarios with limited computational resources, attaining an accuracy of 95.58%. It outperforms other attention mechanisms and the version of 1D-CLANet without attention. Compared to advanced methods, the SE-enhanced 1D-CLANet significantly improves the ability to distinguish between LoS and similar NLoS scenarios, such as human obstructions, enhancing overall recognition accuracy in complex environments.

In this study, to improve the fatigue strength of the LDED (laser-directed energy deposition) 316L stainless steel, an in situ ultrasonic rolling technology is developed to assist the laser-directed energy deposition process (LDED-UR). The microstructural characteristics and fatigue behavior are comprehensively discussed. The results show that the average size of pores of the LDED-UR alloy is about 10.2 μm, which is much smaller than that of the LDED alloy (34.1 μm). Meanwhile, the density of the LDED alloy is also enhanced from 98.26% to 99.27% via the in situ ultrasonic rolling. With the application of the in situ ultrasonic rolling, the grains are transformed into fully equiaxed grains, and their average grain size is greatly reduced from 84.56 μm to 26.93 μm. The fatigue limit of the LDED-UR alloy is increased by 29% from 210 MPa (LDED alloy) to 270 MPa, which can be ascribed to the decreased porosity and the fine grains. In particular, the crack initiation site of the LDED alloy is located at the surfaces, while it is nucleated from the sub-surface for the LDED-UR alloy. This is mainly attributed to the compression residual stress induced by the in situ ultrasonic rolling. This research offers a valuable understanding of the failure mechanisms in additively manufactured metals, guiding the development of effective strategies to improve their fatigue threshold under severe operating conditions.

The deformation mechanism and static recrystallization (SRX) behavior of an Ni-based single-crystal superalloy are investigated. Indentation tests were performed to investigate the effects of crystal orientation and external stress on SRX behavior. Following solution heat treatment, the depth of the SRX layer below the indentation increases with a deviation angle (β) from the [001] orientation. The slip analysis indicates that an increased deviation angle leads to an increase in the resolved shear stress on the slip plane and a decrease in the number of active slip systems. In addition, the variation pattern of the SRX layer depth with the deviation angle is consistent for different external stresses. The depth of the SRX layer also increases with external stress. The coarse γ′ phases and residual γ/γ′ eutectics obviously enhance the pinning effects on the expansion of recrystallized grain boundaries, resulting in slower growth rates of the recrystallized grains in interdendritic regions than those in dendrite core regions.

High-temperature tensile tests were developed to explore the flow features of an Al-Zn-Mg-Cu alloy. The fracture characteristics and microstructural evolution mechanisms were thoroughly revealed. The results demonstrated that both intergranular fractures and ductile fractures occurred, which affected the hot tensile fracture mechanism. During high-temperature tensile, the second phase (Al2CuMg) at the grain boundaries (GBs) promoted the formation and accumulation of dimples. With the continual progression of high-temperature tensile, the aggregation/coarsening of dimples along GBs appear, aggravating the intergranular fracture. The coalescence and coarsen of dimples are reinforced at higher tensile temperatures or lower strain rates. Considering the impact of microstructural evolution and dimple formation/coarsening on tensile stresses, a physical mechanism constitutive (PMC) equation is herein proposed. According to the validation and analysis, the predictive results were in preferable accordance with the testing data, showing the outstanding reconfiguration capability of the PMC model for high-temperature tensile features in Al–Zn–Mg–Cu alloys.

The Arctic sea ice plays a significant role in climate-related processes and has a considerable effect on humans, however accurately predicting the Arctic sea ice concentration is still challenging. Recently, with the rise and development of artificial intelligence, big data technology, machine learning has been widely used in the field of sea ice prediction. In this study, we utilized a sea ice concentration dataset obtained from satellite remote sensing and applied the k-nearest-neighbors (Ice-kNN) machine learning model to forecast the summer Arctic sea ice concentration and extent on 122 days prediction. Based on the physical characteristics of summer sea ice, different algorithms are employed to optimize the prediction model. A drift-ice correction algorithm is designed to address the unrealistic drift ice around the sea ice edge, and a distance function combined with the spatial pattern is proposed to enhance similarity detection. Deseasonalized and detrended sea ice datasets and an expanded training library are also utilized to improve model performance. Furthermore, sensitivity analysis reveals a positive impact of net surface heat flux on sea ice prediction. The modified Ice-kNN model outperforms climatological and anomaly persistence predictions, demonstrating its applicability to predicting summer Arctic sea ice. The September sea ice extent hindcasts of the modified Ice-kNN model are compared to a variety of models submitted to the Sea Ice Prediction Network, underscoring its potential to improve predictive skill for Arctic sea ice.

Recently, severe plastic deformation of alloys under cold conditions has been experimentally investigated to develop refined microstructures. The present study proposed to demonstrate the feasibility of applying cold deformation to a β-solution treated near β-Ti alloy. To be specific, the evolution of microstructure and mechanical properties of a β-solution treated near β-Ti alloy subjected to unidirectional 20% cold rolling were investigated. Results showed that long cracks formed in the 20% cold rolled sample. Meanwhile, two types of deformation-inducted α′ martensite have been observed in cold-rolled β matrix, namely, acicular α′ martensite with an orientation relationship of (12¯10)α′//(111)β with β matrix, and deformed (irregular shape) α′ martensite without coordinating orientation relationship. The formation of cracks was mainly related to the pre-existing α′ plate, and the micro-crack was prone to occur in α′ plates and propagate to β matrix. The microstructure characteristics result in poor ductility and low ultimate strength in the cold-rolled sample. Lastly, the lattice distortion and {101¯2}1¯011 α′-twinning were also characterized in the deformed α′ plates.

This paper aims at the problem of fast stability control of amphibious robot after state switch. A novel method named as generalized multivariable adaptive super-twisting algorithm (GMASTA) is proposed for the finite time attitude control of amphibious robot. In the proposed method, the standard multivariate super-twisting algorithm is improved by introducing a linear term and a higher power term, in order to reduce convergence time and chattering. In addition, the adaptive gain is employed based on a disturbance observer which can avoid a conservative overestimation of the disturbance. For the designed attitude controller, the finite time stability is proved by Lyapunov method. Two numerical examples were carried out. The results from the first example show that GMSTA is better than MSTA in convergence and robustness. The other example is used to illustrate that the disturbance observer based on the GMASTA can realize the accurate observation of the integrated interference. Compared with PID, the proposed method based on GMASTA can converge faster and has better robustness.

High-temperature forming behaviors of a 7046-aluminum alloy were investigated by hot compression experiments. The microstructural evolution features with the changes in deformation parameters were dissected. Results indicated the formation of massive dislocation clusters/cells and subgrains through the intense DRV mechanism at low compression temperature. With an increase in deformation temperature, the annihilation of dislocations and the coarsening of subgrains/DRX grains became prominent, due to the collaborative effects of the DRV and DRX mechanisms. However, the growth of subgrains and DRX grains displayed the weakening trend at high strain rates. Moreover, two constitutive models involving a physically based (PB) model and a gate recurrent unit (GRU) model were proposed for predicting the hot compression features. By validation analysis, the predicted values of true stress perfectly fit with the experimental data, indicating that both the proposed PB model and the GRU model can accurately predict the hot compression behaviors of 7046-aluminum alloys.

Isothermal deformation experiments of the Hastelloy C276 alloy were executed using the Gleeble-3500 hot simulator at a temperature range of 1000–1150 °C and a strain rate range of 0.01–10 s−1. Microstructural evolution mechanisms were analyzed via transmission electron microscope (TEM) and electron backscatter diffraction (EBSD). Results reveal that the influences of hot compression parameters on the microstructure variation features and flow behaviors of the Hastelloy C276 alloy were significant. The intense strain hardening (SH) effects caused by the accumulation of substructures were promoted when the strain rates were increased, and true stresses exhibited a notable increasing tendency. However, the apparent DRV effects caused by the annihilation of substructures and the increasingly dynamic recrystallization (DRX) behaviors occurred at high compressed temperature, inducing the reduction in true stresses. In addition, a physical-based (PB) constitutive model and a long short-term memory (LSTM) model optimized using the particle swarm optimization (PSO) algorithm were established to predict the flow behavior of Hastelloy C276 alloy. The smaller average absolute relative error and greater relation coefficient suggest that the LSTM model possesses a higher forecasting accuracy than the PB model.

Near β-Ti alloys, a perfect candidate material for numerous applications in the aerospace, are expected to exhibit high temperature endurability. Here, in order to evaluate the high temperature oxidation mechanism of the near β-Ti alloy, detailed microstructural characterization was performed on a near β-Ti alloy, Ti-55511 alloy after isothermal heat treatment at 600 °C in a tube furnace. Parabolic oxidation kinetics was observed. The oxide layer consisted of Al2O3, TiO2, VO2, and Magnéli phases. Polymorphic phase transformations and Magnéli phases played critical roles in the oxide layer thickening. The formation of defects was highly correlated with the incorporation of oxygen into Al2O3 and VO2, which resulted in lattice distortion of the oxides. Continuous oxidation led to the formation of the higher-valence oxide V2O5 in VO2 particles.

The high-temperature compression characteristics of a Ti-55511 alloy are explored through adopting two-stage high-temperature compressed experiments with step-like strain rates. The evolving features of dislocation substructures over hot, compressed parameters are revealed by transmission electron microscopy (TEM). The experiment results suggest that the dislocations annihilation through the rearrangement/interaction of dislocations is aggravated with the increase in forming temperature. Notwithstanding, the generation/interlacing of dislocations exhibit an enhanced trend with the increase in strain in the first stage of forming, or in strain rates at first/second stages of a high-temperature compressed process. According to the testing data, an Informer deep learning model is proposed for reconstructing the stress–strain behavior of the researched Ti-55511 alloy. The input series of the established Informer deep learning model are compression parameters (compressed temperature, strain, as well as strain rate), and the output series are true stresses. The optimal input batch size and sequence length are 64 and 2, respectively. Eventually, the predicted results of the proposed Informer deep learning model are more accordant with the tested true stresses compared to those of the previously established physical mechanism model, demonstrating that the Informer deep learning model enjoys an outstanding forecasted capability for precisely reconstructing the high-temperature compressed features of the Ti-55511 alloy.

Active contour models (ACMs) have been widely applied in the field of image segmentation. However, it is still very challenging to construct an efficient ACM to segment images with intensity inhomogeneity. In this paper, a novel ACM guided by global and local signed energy-based pressure force (GLSEPF) is proposed. First, by computing the energy difference between the inner and outer energies of the evolution curve, a global signed energy-based pressure force (GSEPF) is designed, which can improve the robustness to initial curves. Second, a local signed energy-based pressure force (LSEPF) is introduced by computing the pixel-by-pixel energy difference within local neighborhood region, which can handle images with intensity inhomogeneity and noise. Finally, the global image information and the local energy information are used for the global and local force propagation functions, respectively. The global and local variances are used to automatically balance the weights of the GSEPF and the LSEPF, which can solve the problem of setting parameters. Meanwhile, a regularization term and a penalty term are applied to avoid the re-initialization process during iterations and smooth the level set function. Experimental results on different types of images demonstrate that the proposed model is more robust than the popular region-based and mixed ACMs for segmenting images with intensity inhomogeneity and noise. The code is available at: https://github.com/HuaxiangLiu/GLSEPF/.

This study aims to explore the effect of deformation parameters on microstructure evolution during the new two-stage annealing method composed of an aging treatment (AT) and a cooling recrystallization annealing treatment (CRT). Firstly, the hot compressive tests with diverse deformation parameters were finished for an initial aged deformed GH4169 superalloy. Then, the same two-stage annealing method was designed and carried out for the deformed samples. The results show that the deformation parameters mainly affect the grain microstructure during CRT by influencing the content, distribution and morphology of the δ phase after deformation. The reason for this is that there is an equilibrium of the content of the δ phase and Nb atom. When the deformation temperature is high, the complete dissolution behavior of the δ phase nuclei promotes the dispersion distribution of the δ phase with rodlike and needle-like shapes during AT. Thus, the fine and heterogeneous microstructure is obtained after annealing because the recrystallization nucleation is enhanced in those dispersed δ phases during CRT. However, when the retained content of δ phase nuclei is high after deformation, the clusters of intragranular δ phases will form during AT, resulting in the pinning of the motion for dislocation. The elimination of the mixed grain microstructure is slowed down due to the low static recrystallization (SRX) nucleation rate within the deformed grain.

This study takes large size samples after hot-upsetting as research objects and aims to investigate the optimization double-stage annealing parameters for improving the mechanical properties of hot-upsetting samples. The double-stage annealing treatments and uniaxial tensile tests for hot-upsetting GH4169 superalloy were finished firstly. Then, the fracture mode was also studied. The results show that the strength of hot-upsetting GH4169 superalloy can be improved by the double-stage annealing treatment, but the effect of annealing parameters on the elongation of GH4169 alloy at high temperature and room temperature is not significant. The fracture mode of annealed samples at high-temperature and room-temperature tensile tests is a mixture of shear fracture and quasi-cleavage fracture while that of hot-upsetting sample is a shear fracture. The macroscopic expressions for the two fracture modes belong to ductile fracture. Moreover, it is also found that the improvement of strength by the double-stage annealing treatment is greater than the single-stage annealing treatment. This is because the homogeneity of grains plays an important role in the improvement of strength for GH4169 superalloy when the average grain size is similar. Based on a comprehensive consideration, the optimal annealing route is determined as 900 °C × 9–12 h(water cooling) + 980 °C × 60 min(water cooling).

Six new compounds with polyketide decalin ring, peaurantiogriseols A–F (1–6), along with two known compounds, aspermytin A (7), 1-propanone,3-hydroxy-1- (1,2,4a,5,6,7,8,8a-octahydro-2,5-dihydroxy-1,2,6-trimethyl-1-naphthalenyl) (8), were isolated from the fermentation products of mangrove endophytic fungus Penicillium aurantiogriseum 328#. Their structures were elucidated based on their structure analysis. The absolute configurations of compounds 1 and 2 were determined by 1H NMR analysis of their Mosher esters; the absolute configurations of 3–6 were determined by using theoretical calculations of electronic circular dichroism (ECD). Compounds 1–8 showed low inhibitory activity against human aldose reductase, no activity of inducing neurite outgrowth, nor antimicrobial activity.

Near β-Ti alloys with high strength and good ductility are desirable for application in aviation and aerospace industries. Nevertheless, strength and ductility are usually mutually exclusive in structural materials. Here we report a new thermo-mechanical process, that is, the alloy was cross-rolled in β field then aged at 600 °C for 1 h. By such a process, a high strength (ultimate tensile strength: 1480 MPa) and acceptable ductility (elongation: 10%) can be simultaneously achieved in the near β-Ti alloy, based on the microscale β matrix and nanoscale α phase. The microstructure evolution, mechanical properties and strengthening mechanisms have been clarified by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). The results showed that the grain size of the β phase progressively decreased with the increasing of rolling reduction. Moreover, dense dislocation structures and martensite phases distributed in the cross-rolled β matrix can effectively promote the precipitation of nanoscale α particles. TEM analyses confirmed that a heat-treatment twin was generated in the newly formed α lath during aging. These findings provide insights towards developing Ti alloys with optimized mechanical properties.

Multi-pass hot rolling was performed on bi-modal Ti-55511 alloy with 50% rolling reduction at 700 °C. Mechanical properties were evaluated by tensile test, and microstructure evolution was characterized by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). The results show that the Ti-55511 alloy with bi-modal microstructure exhibits good strength and high ductility (1102 MPa, 21.7%). Comparatively, after 50% hot rolling, an enhanced strength and decreased ductility were obtained. The refinement of α phases leads to the increased tensile strength, while the fragmentation of the equiaxed α phase results in a decreased ductility. The fragmentation process of equiaxed α phases followed the sequence of: elongation of α phases → formation of grooves and localized shear bands → the final fragmentation accomplished via deepening grooves.

Every year, hundreds of new compounds are discovered from the metabolites of marine organisms. Finding new and useful compounds is one of the crucial drivers for this field of research. Here we describe the statistics of bioactive compounds discovered from marine organisms from 1985 to 2012. This work is based on our database, which contains information on more than 15,000 chemical substances including 4196 bioactive marine natural products. We performed a comprehensive statistical analysis to understand the characteristics of the novel bioactive compounds and detail temporal trends, chemical structures, species distribution, and research progress. We hope this meta-analysis will provide useful information for research into the bioactivity of marine natural products and drug development.

Four new anthraquinone derivatives 1–4 were obtained along with seven known compounds 5–11 from the extracts of the fungal strain Alternaria sp. XZSBG-1 which was isolated from the sediments of the carbonate saline lake in Bange, Tibet, China. Their structures were determined by spectroscopic methods, mainly by 2D NMR spectra. Compound 1 is a novel tetrahydroanthraquinone with an epoxy ether bond between C-4a and C-9a. In the primary bioassays, compound 3 (alterporriol T) exhibited inhibition of a-glucosidase with a IC50 value 7.2 μM, and compound 9 showed good inhibitory activity against the HCT-116 and HeLa cell lines, with IC50 values of 3.03 and 8.09 μM, respectively.

A new alterporriol-type anthranoid dimer, alterporriol S (1), along with seven known anthraquinone derivatives, (+)-aS-alterporriol C (2), hydroxybostrycin (3), halorosellinia A (4), tetrahydrobostrycin (5), 9α-hydroxydihydrodesoxybostrycin (6), austrocortinin (7) and 6-methylquinizarin (8), were isolated from the culture broth of the mangrove fungus, Alternaria sp. (SK11), from the South China Sea. Their structures and the relative configurations were elucidated using comprehensive spectroscopic methods, including 1D and 2D NMR spectra. The absolute configurations of 1 and the axial configuration of 2 were defined by experimental and theoretical ECD spectroscopy. 1 was identified as the first member of alterporriols consisting of a unique C-10−C-2′ linkage. Atropisomer 2 exhibited strong inhibitory activity against Mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) with an IC50 value 8.70 μM.

Three new resveratrol derivatives, namely, resveratrodehydes A–C (1–3), were isolated from the mangrove endophytic fungus Alternaria sp. R6. The structures of these compounds were elucidated by analysis of their MS, 1D and 2D NMR spectroscopic data. All compounds showed broad-spectrum inhibitory activities against three human cancer cell lines including human breast MDA-MB-435, human liver HepG2, and human colon HCT-116 by MTT assay (IC50 < 50 μM). Among them, compounds 1 and 2 both exhibited marked cytotoxic activities against MDA-MB-435 and HCT-116 cell lines (IC50 < 10 μM). Additionally, compounds 1 and 3 showed moderate antioxidant activity by DPPH radical scavenging assay.

Parkinson’s disease (PD) is the second most common neurodegenerative disease affecting people over age 55. Oxidative stress actively participates in the dopaminergic (DA) neuron degeneration of PD. Xyloketals are a series of natural compounds from marine mangrove fungus strain No. 2508 that have been reported to protect against neurotoxicity through their antioxidant properties. However, their protection versus 1-methyl-4-phenylpyridinium (MPP+)-induced neurotoxicity is only modest, and appropriate structural modifications are necessary to discover better candidates for treating PD. In this work, we designed and synthesized 39 novel xyloketal derivatives (1–39) in addition to the previously reported compound, xyloketal B. The neuroprotective activities of all 40 compounds were evaluated in vivo via respiratory burst assays and longevity-extending assays. During the zebrafish respiratory burst assay, compounds 1, 9, 23, 24, 36 and 39 strongly attenuated reactive oxygen species (ROS) generation at 50 μM. In the Caenorhabditis elegans longevity-extending assay, compounds 1, 8, 15, 16 and 36 significantly extended the survival rates (p < 0.005 vs. dimethyl sulfoxide (DMSO)). A total of 15 compounds were tested for the treatment of Parkinson’s disease using the MPP+-induced C. elegans model, and compounds 1 and 8 exhibited the highest activities (p < 0.005 vs. MPP+). In the MPP+-induced C57BL/6 mouse PD model, 40 mg/kg of 1 and 8 protected against MPP+-induced dopaminergic neurodegeneration and increased the number of DA neurons from 53% for the MPP+ group to 78% and 74%, respectively (p < 0.001 vs. MPP+ group). Thus, these derivatives are novel candidates for the treatment of PD.

Xyloketals, a new type of antioxidants from a marine mangrove fungus, have potential pharmacological properties. In this paper, the radical-scavenging activities of a series of synthetic xyloketals and related chromanes toward 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) were evaluated by absorption spectrometry. One of the compounds (compound 10) displayed significant antioxidative action against DPPH and ABTS. A structure-activity analysis showed that the reactive sites on these compounds correlated with a hydroxy-group and also with ketal or aromatic H substituents. Based in part on a density functional theory (DFT) calculation of compound 10, the antioxidant mechanism of this chromane was deduced as a possible radical-scavenging mechanism by a sequential proton loss electron-transfer (SPLET) process.

4-Deoxybostrycin is a natural anthraquinone compound isolated from the Mangrove endophytic fungus Nigrospora sp. collected from the South China Sea. Nigrosporin is the deoxy-derivative of 4-deoxybostrycin. They were tested against mycobacteria, especially Mycobacterium tuberculosis. In the Kirby-Bauer disk diffusion susceptibility test, they both had inhibition zone sizes of over 25 mm. The results of the absolute concentration susceptibility test suggested that they had inhibitory effects against mycobacteria. Moreover, 4-deoxybostrycin exhibited good inhibition which was even better than that of first line anti-tuberculosis (TB) drugs against some clinical multidrug-resistant (MDR) M. tuberculosis strains. The gene expression profile of M. tuberculosis H37Rv after treatment with 4-deoxybostrycin was compared with untreated bacteria. One hundred and nineteen out of 3,875 genes were significantly different in M. tuberculosis exposed to 4-deoxybostrycin from control. There were 46 functionally known genes which are involved in metabolism, information storage and processing and cellular processes. The differential expressions of six genes were further confirmed by quantitative real-time polymerase chain reaction (qRT-PCR). The present study provides a useful experiment basis for exploitation of correlative new drugs against TB and for finding out new targets of anti-mycobacterial therapy.

A series of new derivatives (5–29) of marine-derived bostrycin (1) were synthesized. The in vitro cytotoxic activities of all compounds were evaluated against MCF-7, MDA-MB-435, A549, HepG2, HCT-116 and MCF-10A cells using the MTT method. The compounds 7, 8, 22, 23, 25, 28 and 29 of the total showed comparable activity to epirubicin, the positive control, against the tested cancer cell lines. However, these compounds also exhibited cytotoxicity towards MCF-10A cells. The structure-activity relationship (SAR) of bostrycin derivatives was also discussed based on the obtained experimental data.

Breast cancer remains a major health problem worldwide. While chemotherapy represents an important therapeutic modality against breast cancer, limitations in the clinical use of chemotherapy remain formidable because of chemoresistance. The HER2/PI-3K/Akt pathway has been demonstrated to play a causal role in conferring a broad chemoresistance in breast cancer cells and thus justified to be a target for enhancing the effects of anti-breast cancer chemotherapies, such as adriamycin (ADR). Agents that can either enhance the effects of chemotherapeutics or overcome chemoresistance are urgently needed for the treatment of breast cancer. In this context, SZ-685C, an agent that has been previously shown, as such, to suppress Akt signaling, is expected to increase the efficacy of chemotherapy. Our current study investigated whether SZ-685C can override chemoresistance through inhibiting Akt signaling in human breast cancer cells. ADR-resistant cells derived from human breast cancer cell lines MCF-7, MCF-7/ADR and MCF-7/Akt, were used as models to test the effects of SZ-685C. We found that SZ-685C suppressed the Akt pathway and induced apoptosis in MCF-7/ADR and MCF-7/Akt cells that are resistant to ADR treatment, leading to antitumor effects both in vitro and in vivo. Our data suggest that use of SZ-685C might represent a potentially promising approach to the treatment of ADR-resistant breast cancer.

Three new eremophilane sesquiterpenes (1–3) were isolated from the mangrove endophytic fungus Xylaria sp. BL321 together with 07H239-A (4), a known analogue of the new compounds. The structures of these compounds were elucidated by analysis of their MS, 1D and 2D NMR spectroscopic data. Compound 4 showed activation activity on α-glucosidase at 0.15 μM (146%), and then, 4 gradually produced inhibitory activity on α-glucosidase with increasing concentration, and the IC50 value is 6.54 μM.

Based on the natural isoprenyl phenyl ether from a mangrove-derived fungus, 32 analogues were synthesized and evaluated for inhibitory activity against influenza H1N1 neuraminidase. Compound 15 (3-(allyloxy)-4-hydroxybenzaldehyde) exhibited the most potent inhibitory activity, with IC50 values of 26.96 μM for A/GuangdongSB/01/2009 (H1N1), 27.73 μM for A/Guangdong/03/2009 (H1N1), and 25.13 μM for A/Guangdong/05/2009 (H1N1), respectively, which is stronger than the benzoic acid derivatives (~mM level). These are a new kind of non-nitrogenous aromatic ether Neuraminidase (NA) inhibitors. Their structures are simple and the synthesis routes are not complex. The structure-activity relationship (SAR) analysis revealed that the aryl aldehyde and unsubstituted hydroxyl were important to NA inhibitory activities. Molecular docking studies were carried out to explain the SAR of the compounds, and provided valuable information for further structure modification.

Two new sesquiterpenes, microsphaeropsisin B (1) and C (2), and two new de-O-methyllasiodiplodins, (3R, 7R)-7-hydroxy-de-O-methyllasiodiplodin (4) and (3R)-5-oxo-de-O-methyllasiodiplodin (5), together with one new natural product (6) and twelve known compounds (3, 7–17), were isolated from the co-cultivation of mangrove endophytic fungus Trichoderma sp. 307 and aquatic pathogenic bacterium Acinetobacter johnsonii B2. Their structures, including absolute configurations, were elucidated by extensive analysis of spectroscopic data, electronic circular dichroism, Mo2(AcO)4-induced circular dichroism, and comparison with reported data. All of the isolated compounds were tested for their α-glucosidase inhibitory activity and cytotoxicity. New compounds 4 and 5 exhibited potent α-glucosidase inhibitory activity with IC50 values of 25.8 and 54.6 µM, respectively, which were more potent than the positive control (acarbose, IC50 = 703.8 µM). The good results of the tested bioactivity allowed us to explore α-glucosidase inhibitors in lasiodiplodins.

Four new chromone derivatives, phomopsichins A–D (1–4), along with a known compound, phomoxanthone A (5), were isolated from the fermentation products of mangrove endophytic fungus Phomopsis sp. 33#. Their structures were elucidated based on comprehensive spectroscopic analysis coupled with single-crystal X-ray diffraction or theoretical calculations of electronic circular dichroism (ECD). They feature a tricyclic framework, in which a dihydropyran ring is fused with the chromone ring. Compounds 1–5 showed weak inhibitory activities on acetylcholinesterase as well as α-glucosidase, weak radical scavenging effects on 1,1-diphenyl-2-picrylhydrazyl (DPPH) as well as OH, and weak antimicrobial activities. Compounds 1–4 showed no cytotoxic activity against MDA-MB-435 breast cancer cells. Their other bioactivities are worthy of further study, considering their unique molecular structures.

In the crystal structure of the title compound, C11H11NO4, intramolecular O—H...O hydrogen bonding results in the formation of a planar five-membered ring, which is nearly coplanar with the quinoline group. Intermolecular N—H...O hydrogen bonds link the molecules into centrosymmetric dimers.

Research has been conducted on the xyloketals, metabolites isolated from the mangrove fungus Xylaria sp. from the South China Sea. The results of the spectroscopic and X-ray diffraction experiments elucidating these compounds' structures are described.