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Seven photoaffinity-based and sixteen biotin-based berberine (BBR) probes were constructed and screened for their effects on c-Jun N-terminal protein kinases (JNK) phosphorylation (p-JNK) suppressi...

The phosphatidylinositol 3-kinase-Akt signaling pathway plays an essential role in regulating cell proliferation and apoptosis. Akt kinase is at the center of this signaling pathway and interacts with a variety of proteins. Akt is overexpressed in almost 80% of tumors. However, inhibiting Akt has serious clinical side effects so is not a suitable treatment for cancer. During recent years, Akt scaffold proteins have received increasing attention for their ability to regulate Akt signaling and have emerged as potential targets for cancer therapy. In this paper, we categorize Akt kinase scaffold proteins into four groups based on their cellular location: membrane-bound activator and inhibitor, cytoplasm, and endosome. We describe how these scaffolds interact with Akt kinase, how they affect Akt activity, and how they regulate the specificity of Akt signaling. We also discuss the clinical application of Akt scaffold proteins as targets for cancer therapy.

The bacterium Vibrio cholerae can colonize the human intestine and cause cholera, but spends much of its life cycle in seawater. The pathogen must adapt to substantial environmental changes when moving between seawater and the human intestine, including different availability of carbon sources such as fructose. Here, we use in vitro experiments as well as mouse intestinal colonization assays to study the mechanisms used by pandemic V. cholerae to adapt to these environmental changes. We show that a LacI-type regulator (FruI) and a fructose/H+ symporter (FruT) are important for fructose uptake at low fructose concentrations, as those found in seawater. FruT is downregulated by FruI, which is upregulated when O2 concentrations are low (as in the intestine) by ArcAB, a two-component system known to respond to changes in oxygen levels. As a result, the bacteria predominantly use FruT for fructose uptake under seawater conditions (low fructose, high O2), and use a known fructose phosphotransferase system (PTS, Fpr) for fructose uptake under conditions found in the intestine. PTS activity leads to reduced levels of intracellular cAMP, which in turn upregulate virulence genes. Our results indicate that the FruT/FruI system may be important for survival of pandemic V. cholerae in seawater.

The C-terminal of G protein-coupled receptors is now recognized as being important for G protein activation and signaling function. To detect the role of C-terminal tail in receptor activation, we used the α1b-AR, which has a long C-terminal of 164 amino acids. We constructed the intramolecular FRET sensors, in which the C-terminal was truncated to 10 (∆C-10), 20 (∆C-20), 30 (∆C-30), 50 (∆C-50), 70 (∆C-70), or 90 (∆C-90). The truncated mutants of ∆C-10, ∆C-20, or ∆C-30 cannot induce FRET signal changes and downstream ERK1/2 phosphorylation. However, the truncated mutants of ∆C-50, ∆C-70, or ∆C-90 induce significant FRET signal changes and downstream ERK1/2 phosphorylation, especially ∆C-90. This is particularly true in the case of the ∆C-90, ∆C-70, or ∆C-50 which retained the potential phosphorylation sites (Ser401, Ser404, Ser408, or Ser410). The ∆C-90 showed an increase in agonist-induced FRET signal changes and ERK1/2 phosphorylation in PKC- or endocytosis-dependent and EGFR-, src-, or β-arrestin2-independent.

The hydrogenation of CO2 to CH4 can realize the utilization of CO2, which has an important implications to both the energy and environment. As a result of the low catalytic activity of the supported Ni/SiO2 catalyst, the ZrO2 is added to improve its catalytic performance by the impregnation method. The experimental results show that ZrO2 is an effective promoter to enhance the low-temperature catalytic activity of Ni/SiO2 catalyst.

The soil fertility index (SFI) is an indicator that is commonly used to evaluate the soil fertility in the rice paddy regions of China. However, calculating an SFI requires the laboratory measurement of multiple soil properties, which adds to the costs and complexity of conventional methods. Visible and near-infrared (vis-NIR, 400-2,500 nm) spectra might offer opportunities to cost-effectively and rapidly assess soil properties and the SFI. In this study, we evaluated soil fertility properties and their derived SFIs for paddy fields in southern China using vis-NIR spectra with the partial least-squares regression model. The results showed very good prediction accuracy of vis-NIR spectroscopy for soil organic matter, clay and sand contents, with the former two having an apparent spectral response in the near-infrared range. A good predictive ability was obtained for total nitrogen, silt, available nitrogen and total potassium. In contrast, the prediction accuracy was only moderate for cation exchange capacity and available phosphorus, and it was poor for the pH, total phosphorus and available potassium without apparent spectral responses. A bootstrapped partial least squares regression model predicted the SFI directly from the vis-NIR spectra accurately (R-2 of 0.80 and ratio of performance to interquartile range of 3.12), whereas SFI computed from vis-NIR estimates of the individual indicators was less accurate. This shows that vis-NIR spectroscopy can improve the efficiency of soil fertility assessments within the cultivated paddy rice regions of southern China. Highlights Soil fertility index (SFI) can be predicted directly with spectroscopy. Prediction accuracy of vis-NIR spectroscopy was good for SOM, TN and clay. SFI estimated directly from vis-NIR spectra was superior to SFI calculated from predicted individual indicator. Successful prediction of SFI from vis-NIR spectra can be attributed to the high significance of SOM and TN.

The O-antigen is the outermost component of the lipopolysaccharide layer in Gram-negative bacteria, and the variation of O-antigen structure provides the basis for bacterial serological diversity. Here, we determined the O-antigen structure of an Escherichia coli strain, LL004, which is totally different from all of the E. coli serogroups. The tetrasaccharide repeating unit was determined as →4)-β-d-Galp-(1→3)-β-d-GlcpNAc6OAc(~70%)-(1→3)-β-d-GalpA-(1→3)-β-d-GalpNAc-(1→ with monosaccharide analysis and NMR spectra. We also characterized the O-antigen gene cluster of LL004, and sequence analysis showed that it correlated well with the O-antigen structure. Deletion and complementation testing further confirmed its role in O-antigen biosynthesis, and indicated that the O-antigen of LL004 is assembled via the Wzx/Wzy dependent pathway. Our findings, in combination, suggest that LL004 should represent a novel serogroup of E. coli.

The serotonin receptor 5-HT1B is widely expressed in the central nervous system and has been considered a drug target in a variety of cognitive and psychiatric disorders. The anti-inflammatory effects of 5-HT1B agonists may present a promising approach for Alzheimer’s disease (AD) treatment. Herbal antidepressants used in the treatment of AD have shown functional overlap between the active compounds and 5-HT1B receptor stimulation. Therefore, compounds in these medicinal plants that target and stimulate 5-HT1B deserve careful study. Molecular docking, drug affinity responsive target stability, cellular thermal shift assay, fluorescence resonance energy transfer (FRET), and extracellular regulated protein kinases (ERK) 1/2 phosphorylation tests were used to identify emodin-8-O-β-d-glucopyranoside (EG), a compound from Chinese medicinal plants with cognitive deficit attenuating and antidepressant effects, as an agonist of 5-HT1B. EG selectively targeted 5-HT1B and activated the 5-HT1B-induced signaling pathway. The activated 5-HT1B pathway suppressed tumor necrosis factor (TNF)-α levels, thereby protecting neural cells against beta-amyloid (Aβ)-induced death. Moreover, the agonist activity of EG towards 5-HT1B receptor, in FRET and ERK1/2 phosphorylation, was antagonized by SB 224289, a 5-HT1B antagonist. In addition, EG relieved AD symptoms in transgenic worm models. These results suggested that 5-HT1B receptor activation by EG positively affected Aβ-related inflammatory process regulation and neural death resistance, which were reversed by antagonist SB 224289. The active compounds such as EG might act as potential therapeutic agents through targeting and stimulating 5-HT1B receptor for AD and other serotonin-related disorders. This study describes methods for identification of 5-HT1B agonists from herbal compounds and for evaluating agonists with biological functions, providing preliminary information on medicinal herbal pharmacology.

Intracerebral hemorrhage (ICH) is a devastating subtype of stroke that is associated with high morbidity and mortality. However, up to now, there are no effective prevention methods or specific therapies to improve its clinical outcomes. Herein, we explore preliminarily the efficacy of crocin, a carotenoid extracted from the stigma of saffron known for its anti-oxidation and free radical scavenging activities, in a mouse ICH model induced with collagenase infusion. Crocin or saline was administrated 6 h after ICH and then every 12 h for up to 7 days. Neurological scores were examined on days 1, 3, and 7 after ICH. Mice were sacrificed after1, 3, and 7 days of crocin treatment for examination of histology and immunohistochemistry. The results showed that oral administration of crocin attenuated the neurological deficits and reduced the myelin loss, neuron degeneration, iron deposition, reactive oxygen species (ROS) production and heme oxygenase-1 (HO-1) expression in the early stage of ICH, making it potential to be an ideal candidate for medical therapy of ICH in clinic.

Previous studies have reported the occurrence of a Redfield-type ratio (e.g., C/N/P, C/N, C/P, or N/P) between C, N, and P concentrations in marine and (in part) terrestrial ecosystems. Herein, we aimed to determine whether a similar Redfield-type ratio can occur in farmland soil, as well as to elucidate how the C, N, and P ratios change with farmland-use types, soil physicochemical properties, and environmental factors. The stoichiometric patterns of soil C, N, and P in farmland were analyzed based on 6150 samples (0–20 cm) collected in 2012 by the Soil Testing and Formulated Fertilization Project in the Poyang Lake region of Southern China. The average soil C/N/P ratio in farmland of the study region was 98.4:16:1, which was slightly lower than the Redfield ratio of 106:16:1. There was no significant correlation between the concentrations of C, N, and P, indicating the absence of Redfield-type C/N/P, C/P, and N/P ratios. In contrast, the correlation between the concentrations of C and N was significant, indicating the presence of a stable Redfield-type C/N ratio in farmland soil. The average soil C/N, C/P, and N/P ratios corresponding to various farmland-use types showed significant differences (p

Oligochitosan (OCHI) is known to have some specific biological activities. However, its interactions with blood components and related correlation with molecular structures remains to be clarified due to its growing use in biomedical areas. Herein, a series of OCHI were prepared by hydrogen peroxide induced degradation combined fractionation in ethanol solutions and their molecular structures were characterized by GPC, FTIR, 1H and 13C NMR, and then the interactions of the prepared OCHI with blood components, including red blood cells (hemolysis, deformability, and aggregation), coagulation system, complement (C3a, and C5a activation), and platelet (activation, and aggregation), were investigated. For red blood cells, OCHI has a quite low risk of hemolysis in a dose- and MW-dependent manner and the deformability and aggregation were observed in its high MW fraction. The coagulation tests revealed that OCHI is capable of a mild anticoagulation through blocking the intrinsic pathway and the anticoagulation corresponding MW was identified. In terms of complement, OCHI could inhibit C3a in a dose-dependent manner and activate C5a with its high MW fraction. In addition, there is no significant effect of OCHI on platelet activation and aggregation. Based on above results, the interactions related mechanism was discussed and proposed.

The synergistic effect of hierarchically porous zeolites on the fire retardancy and fire toxicity of ammonium polyphosphate (APP) treated wood composites was studied in this work. Hierarchically porous 4A (H4A) zeolite and 4A zeolite were hydrothermally synthesized and characterized. Several groups of wood composites containing APP as fire retardant and H4A/4A zeolites as synergists were fabricated. Thermogravimetric (TG) results showed that H4A zeolite increased the char formation and enhanced the thermal stability of APP treated wood at higher temperature. Cone calorimetry test results suggested that H4A zeolite reduced the heat release rate (HRR) and decreased CO produce rate (COPR) of APP treated wood composites. Moreover, H4A also exhibited better smoke suppression than 4A zeolite when the APP content was small. These results demonstrated that H4A zeolites may be a promising synergistic component for improving the fire retardancy and reducing the fire toxicity of APP treated wood composites.

O-polysaccharide (O-antigen) was isolated from the lipopolysaccharide of Vibrio cholerae O100 and studied by component analyses and 1D and 2D NMR spectroscopy. The following structure of the O-polysaccharide was established: →3)-β- d -QuipNAc4N(dHh)-(1 → 3)-α- d -Fucp4N(RHb)-(1 → 3)-α- l -FucpNAc-(1→ where Hb and dHh indicate 3-hydroxybutanoyl and 3,5-dihydroxyhexanoyl, respectively. The O-antigen gene cluster of V. cholerae O100 has been sequenced. The gene functions were tentatively assigned by comparison with sequences in the available databases and found to be in agreement with the OPS structure.

Due to the irreversibility of heavy metal pollution, the presence of heavy metals in farmland soil is associated with severe ecological risks that endanger both the environment and human health. Cadmium (Cd) and mercury (Hg) are two toxic heavy metals found widely in polluted soil. Cd is not readily fixed in the soil and is therefore easily accumulated by plants, while Hg has a wide range of pollution sources. The aims of this study were to explore the spatial variation in Cd and Hg concentrations in farmland soil in Poyang Lake Plain, China, and to assess their potential ecological risks as influenced by natural and human factors. A total of 283 soil samples were obtained from Fengcheng city, central Jiangxi Province. Data were then analyzed using geostatistics, the potential ecological risk index, Pearson’s correlation analysis, and Geodetector. The results showed moderate variation in soil Cd and Hg concentrations, with a remarkable difference in their spatial distribution. Cd concentrations in the northwest and northeast of Fengcheng were below the regional background level in Jiangxi; in most remaining areas, Cd concentrations were between the regional background level and national risk screening value. Areas with Hg concentrations lower than the regional background level were largely concentrated in the south, east and north of Fengcheng, and gradually increased towards the central, where they exceeded the regional background level but were below the national risk screening value. Overall, the potential ecological risk level of Cd was predominantly low, while that of Hg was moderate. The comprehensive potential ecological risk was low in most areas for both Cd and Hg, with some scattered areas of moderate risk. Moreover, the comprehensive potential ecological risk index of both Cd and Hg was significantly correlated with soil pH, total phosphorous, elevation, distance from a river (p < 0.01), and distance from a road (p < 0.05). The most significant factor influencing the comprehensive potential ecological risk index of these two heavy metals was soil pH of 5.2–5.6, followed by total p ≤ 0.52 mg kg−1. In conclusion, moderate pollution of Cd and Hg occurred in farmland soil in Poyang Lake Plain where their comprehensive potential ecological risk level was generally low and mainly influenced by soil pH and total phosphorous.

Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a secreted protein and its deficiency markedly enhanced the survival rate of patient with cardiovascular diseases (CVDs). Forty berberine (BBR) derivatives were synthesized and evaluated for their activities on down-regulating the transcription of PCSK9 in HepG2 cells, taking BBR as the lead. Structure–activity relationship (SAR) analysis revealed that 2,3-dimethoxy moiety might be beneficial for activity. Among them, 9k displayed the most potent activity with IC50 value of 9.5 ± 0.5 μM, better than that of BBR. Also, it significantly decreased PCSK9 protein level at cellular level, as well as in the liver and serum of mice in vivo. Furthermore, 9k markedly increased LDLR expression and LDL-C clearance via down-regulating PCSK9 protein. The mechanism of action of 9k is targeting HNF1α and/or Sp1 cluster modulation upstream of PCSK9, a different one from BBR. Therefore, 9k might have the potential to be a novel PCSK9 transcriptional inhibitor for the treatment of atherosclerosis, worthy for further investigation.

Berberine (BBR), a traditional Chinese medicine, has therapeutic effects on a variety of inflammation-related diseases, but its direct proteomic targets remain unknown. Using activity-based protein profiling, we first demonstrated that BBR directly targets the NEK7 protein via the hydrogen bond between the 2,3-methylenedioxy and 121-arginine (R121) residues. The fact that R121 is located precisely within the key domain involved in the NEK7-NLRP3 interaction allows BBR to specifically block the NEK7-NLRP3 interaction and successively inhibit IL-1β release, independent of the NF-κB and TLR4 signaling pathways. Moreover, BBR displays in vivo anti-inflammatory efficacy in a NEK7-dependent manner. Therefore, we consider NEK7 to be a key target of BBR in the treatment of NLRP3-related inflammatory diseases, and the development of novel NEK7-NLRP3 interaction inhibitors might be easily achieved using NEK7 as a target.

Vascular endothelial growth factor (VEGF) is a well-known angiogenic factor that plays a critical role in various physiological and pathological processes. VEGF also contributes to the process of embryo implantation by enhancing embryo development, improving endometrial receptivity, and facilitating the interactions between the developing embryo and the endometrium. There is a correlation between the alteration of VEGF expression and reproductive failure, including recurrent implantation failure (RIF) and recurrent miscarriage (RM). In order to clarify the role of VEGF in embryo implantation, we reviewed recent literature concerning the expression and function of VEGF in the reproductive system around the time of embryo implantation and we provide a summary of the findings reported so far. We also explored the effects and the possible underlying mechanisms of action of VEGF in embryo implantation.

Background: Dictamnine (Dic), a naturally occurring furoquinoline alkaloid isolated from the root bark of Dictamnus dasycarpus Turcz., is reported to display a wide range of potential pharmacological properties including anticancer activity against multiple cancer types. However, little is known about the direct target proteins and anticancer mechanisms of Dic.Methods: Anticancer effects of Dic and chemotherapy resistance of lung cancer were determined by CCK8, EdU and apoptosis assay. Boyden chamber migration and invasion, wound healing assay, plate colony formation and sphere formation assay were performed to explore the effects of Dic on metastasis and stemness of lung cancer cells. Protein docking analysis, cellular thermal shift assay (CETSA) and drug affinity responsive target stability (DARTS) were used for prediction and confirmation of the interaction between Dic and c-Met. qRT-PCR, Western blotting and immunohistochemistry (IHC) were used in mechanism investigation. Tumor xenograft model was used to evaluate the anti-tumor effects of Dic in vivo.Results: Dic was found to suppress the proliferation of lung cancer cells and attenuate the activation of the PI3K/AKT/mTOR and mitogen-activated protein kinase (MAPK) signaling pathways by directly inhibiting the phosphorylation and activation of the receptor tyrosine kinase c-Met. Moreover, Dic treatment significantly inhibited the colony formation, migration, invasion, stemness, adhesive ability, epithelial-mesenchymal transition and in vivo xenograft tumor growth of A549 lung cancer cells. Notably, the combination of Dic and gefitinib synergistically inhibited the cell proliferation, induced apoptosis, and suppressed the PI3K/Akt/mTOR and MAPK signaling pathways in PC9 gefitinib resistant cells.Conclusions: In conclusion, Dic was identified as a novel c-Met inhibitor and our results suggest the potential use of Dic as a new therapeutic agent in the treatment of lung cancer or other cancers with overactive c-Met pathway.

c-Met hyperactivity has been observed in numerous neoplasms. Several researchers have shown that the abnormal activation of c-Met is mainly caused by transcriptional activation. However, the molecular mechanism behind this transcriptional regulation is poorly understood. Here, we suggest that Smad3 negatively regulates the expression and activation of c-Met via a transcriptional mechanism. We explore the molecular mechanisms that underlie Smad3-induced c-Met transcription inhibition. We found in contrast to the high expression of c-Met, Smad3 showed low protein and mRNA levels. Smad3 and c-Met expressions were inconsistent between lung cancer tissues and cell lines. We also found that Smad3 overexpression suppresses whereas Smad3 knockdown significantly promotes Epithelial-Mesenchymal Transition and production of the angiogenic factors VEGF, CTGF and COX-2 through the ERK1/2 pathway. In addition, Smad3 overexpression decreases whereas Smad3 knockdown significantly increases protein and mRNA levels of invasion-related β-catenin and FAK through the PI3K/Akt pathway. Furthermore, using the chromatin immunoprecipitation analysis method, we demonstrate that a transcriptional regulatory complex consisting of HDAC1, Smad3 and mSin3A binds to the promoter of the c-Met gene. By either silencing endogenous mSin3A expression with siRNA or by pretreating cells with a specific HDAC1 inhibitor (MS-275), Smad3-induced transcriptional suppression of c-Met could be effectively attenuated. These results demonstrate that Smad3-induced inhibition of c-Met transcription depends on of a functional transcriptional regulatory complex that includes Smad3, mSin3A and HDAC1 at the c-Met promoter. Collectively, our findings reveal a new regulatory mechanism of c-Met signaling, and suggest a potential molecular target for the development of anticancer drugs.

Intracerebral hemorrhage (ICH) is a devastating subtype of stroke with high morbidity and mortality. However, there is no effective therapy method to improve its clinical outcomes to date. Here we report an injectable gelatin hydrogel that is capable of suppressing inflammation and enhancing functional recovery in a mouse model of ICH. Thiolated gelatin was synthesized by EDC chemistry and then the hydrogel was formed through Michael addition reaction between the thiolated gelatin and polyethylene glycol diacrylate. The hydrogel was characterized by scanning electron microscopy, porosity, rheology, and cytotoxicity before evaluating in a mouse model of ICH. The in vivo study showed that the hydrogel injection into the ICH lesion reduced the neuron loss, attenuated the neurological deficit post-operation, and decreased the activation of the microglia/macrophages and astrocytes. More importantly, the pro-inflammatory M1 microglia/macrophages polarization was suppressed while the anti-inflammatory M2 phenotype was promoted after the hydrogel injection. Besides, the hydrogel injection reduced the release of inflammatory cytokines (IL-1β and TNF-α). Moreover, integrin β1 was confirmed up-regulated around the lesion that is positively correlated with the M2 microglia/macrophages. The related mechanism was proposed and discussed. Taken together, the injectable gelatin hydrogel suppressed the inflammation which might contribute to enhance the functional recovery of the ICH mouse, making it a promising application in brain injury of CNS diseases.

Nanoparticle fusion with cell membranes is an interesting phenomenon that may have crucial implications for their biomedical applications. Here, we proposed a biomimetic and controlled route to fusion of hydrophobic quantum dots (QDs) with the cell membranes of living cells, while preserving their sensing and optical properties and thus their capability of membrane imaging and single-nanoparticle tracking. Red blood cell (RBC) membrane lipids were extracted to phase transfer hydrophobic QDs and the resulting RBC-encapsulated QDs (RBC-QDs) can be well fused within cell membranes as membrane markers. The fusion was validated through single-nanoparticle imaging and different movement behaviours were reliably discriminated. RBC-QDs possessed some novel features, such as controllable selective membrane staining, no invasion, and high photobleaching resistance, which allowed for long-term imaging, and single-nanoparticle tracking. This approach provides a versatile platform for controlled hydrophobic QD-based fluorescence investigation of living cell membranes.

Taking palmatine (PMT) as the lead, 20 new PMT derivatives were synthesized and examined for their antibacterial activities against six tested metronidazole (MTZ)-resistant Helicobacter pylori (H. pylori) strains. The structure&ndash, activity relationship (SAR) indicated that the introduction of a suitable secondary amine substituent at the 9-position might be beneficial for potency. Among them, compound 1c exhibited the most potent activities against MTZ-resistant strains, with minimum inhibitory concentration (MIC) values of 4&ndash, 16 &mu, g/mL, better than that of the lead. It also exhibited a good safety profile with a half-lethal dose (LD50) of over 1000 mg/kg. Meanwhile, 1c might exert its antimicrobial activity through targeting H. pylori urease. These results suggested that PMT derivatives might be a new family of anti-H. pylori components.

While deferoxamine (DFO) has long been used as an FDA-approved iron chelator, its proangiogenesis ability attracts increasing number of research interests. To address its drawbacks such as short plasma half-life and toxicity, polymeric conjugated strategy has been proposed and shown superiority. Owing to intravenous injection and application in blood-related conditions, however, the blood interactions and antioxidation of the DFO-conjugates and the mechanisms underlying these outcomes remain to be elucidated. In this regard, incubating with three different molecular-weight (MW) alginate-DFO conjugates (ADs) red blood cells (RBCs), coagulation system, complement and platelet were investigated. To prove the antioxidant activity of ADs, we used hemoglobin oxidation model in vitro. ADs did not cause RBCs hemolysis while reversible aggregation and normal deformability ability were observed. However, the coagulation time, particularly APTT and TT, were significantly prolonged in a dose-dependent manner, and fibrinogen was dramatically decreased, suggesting ADs could dominantly inhibit the intrinsic pathways in the process of coagulation. The dose-dependent anticoagulation might be related with the functional groups along the alginate chains. The complements, C3a and C5a, were activated by ADs in a dose-dependent manner through alternative pathway. For platelet, ADs slightly suppressed the activation and aggregation at low concentration. Based on above results, the cross-talking among coagulation, complement and platelet induced by ADs was proposed. The antioxidation of ADs through iron chelation was proved and the antioxidant activity was shown in a MW-dependent manner.

Maternal metabolism dysregulation during pregnancy predisposes offspring to major diseases, including hypertension, in later life, but the mechanism involved remains to be fully elucidated. A high-fat-diet (HFD) pregnant rat model was used to investigate whether excessive intrauterine lipid exposure was associated with elevated blood pressure in offspring and increased levels of leptin, an important biomarker and mediator of vascular dysfunction and hypertension. We found that gestational hyperlipidemia predisposed offspring to blood pressure elevation and sustained increases in leptin levels with no difference in body weight in the rat model. Increased leptin expression and leptin promoter hypomethylation were found in adipose tissues of HFD-exposed offspring. The treatment of mesenchymal stem cells with free fatty acids during adipogenic differentiation resulted in increased leptin expression, accompanied by leptin promoter hypomethylation. In addition, we also followed up 121 children to evaluate the association between maternal triglyceride levels and offspring blood pressure. Consistent with the animal study results, we observed elevated serum leptin levels and blood pressure in the offspring born to women with gestational hypertriglyceridemia. Our findings provide new insights that maternal hyperlipidemia is associated with elevated blood pressure in offspring and is associated with increases in leptin levels through epigenetic memory.

The cannabinoid receptor 1 (CB1) is mainly expressed in the nervous system and regulates learning, memory processes, pain and energy metabolism. However, there is no way to directly measure its activation. In this study, we constructed a CB1 intramolecular fluorescence resonance energy transfer (FRET) sensor, which could measure CB1 activation by monitoring structural changes between the third intracellular loop and the C-terminal tail. CB1 agonists induced a time- and concentration-dependent increase in the FRET signal, corresponding to a reduction in the distance between the third intracellular loop and the C-terminal tail. This, in turn, mobilized intracellular Ca2+, inhibited cAMP accumulation, and increased phosphorylation of the ERK1/2 MAP kinases. The activation kinetics detected using this method were consistent with those from previous reports. Moreover, the increased FRET signal was markedly inhibited by the CB1 antagonist rimonabant, which also reduced phosphorylation of the ERK1/2 MAP kinases. We mutated a single cysteine residue in the sensor (at position 257 or 264) to alanine. Both mutation reduced the agonist-induced increase in FRET signal and structural changes in the CB1 receptor, which attenuated phosphorylation of the ERK1/2 MAP kinases. In summary, our sensor directly assesses the kinetics of CB1 activation in real-time and can be used to monitor CB1 structure and function.

Activation of the histamine-3 receptor (H3R) is involved in memory processes and cognitive action, while blocking H3R activation can slow the progression of neurological disorders, such as Alzheimer's disease, schizophrenia and narcolepsy. To date, however, no direct way to examine the activation of H3R has been utilized. Here, we describe a novel biosensor that can visualize the activation of H3R through an intramolecular fluorescence resonance energy transfer (FRET) signal. To achieve this, we constructed an intramolecular H3R FRET sensor with cyan fluorescent protein (CFP) attached at the C terminus and yellow fluorescent protein (YFP) inserted into the third intracellular loop. The sensor was found to internalize normally on agonist treatment. We measured FRET signals between the donor CFP and the acceptor YFP in living cells in real time, the results of which indicated that H3R agonist treatment (imetit or histamine) increases the FRET signal in a time- and concentration-dependent manner with Kon and Koff values consistent with published data and which maybe correlated with decreasing cAMP levels and the promotion of ERK1/2 phosphorylation. The FRET signal was inhibited by H3R antagonists, and the introduction of mutations at F419A, F423A, L426A and L427A, once again, the promotion of ERK1/2 phosphorylation, was diminished. Thus, we have built a H3R biosensor which can visualize the activation of receptor through real-time structure changes and which can obtain pharmacological kinetic data at the same time. The FRET signals may allow the sensor to become a useful tool for screening compounds and optimizing useful ligands.

A pair of new enantiomeric furoquinoline alkaloids, (±)-zanthonitidine A (1), together with nine known ones (2–10) were isolated from the radix of Zanthoxylum nitidum. Their chemical structures were elucidated based on the extensive spectroscopic analysis. The racemic mixture of 1 was separated by chiral column chromatography, and the absolute configurations of (+)-1 and (−)-1 were determined by the comparison of experimental and calculated electronic circular dichroism spectra. Antibacterial activities of compounds 1–9 were evaluated, and compounds (+)-1, (−)-1, 3, 7 and 8 showed antibacterial activities against Bacillus subtilis, Enterococcus faecalis or Staphylococcus aureus. Graphical Abstract Electronic supplementary material The online version of this article (10.1007/s13659-018-0169-7) contains supplementary material, which is available to authorized users.

Thermal energy storage (TES) composites were fabricated by employing diatomite stabilized paraffin as phase change material (PCM) and wood flour/high-density polyethylene (WF/HDPE) as matrix. TES capacity of the small pores inside diatomite was investigated. The morphology, pore diameter and structure of diatomite and form-stable phase change material (FSPCM) were measured by scanning electron microscopy (SEM), mercury intrusion porosimetry and X-ray diffractometer (XRD). The prepared TES composites were characterized by differential scanning calorimetry (DSC) and infrared thermography. Physical and mechanical strength were also tested. The results showed that: (1) diatomite has abundant pores and these isolated small pores below 10 μm result in excellent TES capacity; (2) the FSPCM presented outstanding stability without any chemical reactions, and the liquid leakage was completely solved by using WF/HDPE as the secondary encapsulation material; (3) the TES composites possess considerable energy storage capacity and temperature-regulating ability; (4) the satisfying TES performance and acceptable mechanical strength indicated that the TES composites could be used as building material for energy conversation.

Verapamil is reported to prevent scar formation. However, whether verapamil is involved in the ureteral stricture scar and the underlying mechanism need further investigation. Fibroblasts were isolated from ureteral scar tissues. TGF-β1 stimulation was used to induce fibrosis of fibroblasts. Inhibition of CaMK II was achieved by shRNA transfection. CCK-8 was performed to evaluate cell viability. qRT-PCR was applied to determine the level of mRNA while western blotting was used to determine the level of proteins. Immunofluorescence was used to detect the level of vimentin, collagen I and collagen III. Primary fibroblasts was successfully isolated from ureteral scar tissues. TGF-β1 stimulation was capable to induce collagen production and fibrosis in primary fibroblasts while inhibition of CaMK II attenuate collagen production. Overexpression of wild type CaMK II lead to further increase of collagen production upon TGF-β1 stimulation while the mutated CaMK II did not exert this promotion. Treatment of verapamil inhibits TGF-β1 induced collagen production via inhibiting CaMK II. In present study, we revealed a vital role of Verapamil and CaMK II in the formation of ureteral scar. Verapamil inhibited TGF-β1 induced collagen fiber formation by regulating CaMK II. Our finding might provide new insight into mechanism of prevention and treatment of ureteral scar.

Interface modification to minimize charge recombination and trapping for efficient charge transport is crucial for the performance of perovskite solar cells (PSCs). Herein, functionalized p-type blue carbon dots (B-CDs) are ventured as an interface passivation layer to enhance the efficiency and long-term stability of all-inorganic CsPbI2 Br PSCs. It is found that first the blue carbon dots with abundant NH, CN, CO, and CO functional groups effectively passivate defects by reacting with I- and Pb2+ ions in the perovskite through hydrogen and coordinative bonds. Second, the p-type B-CDs modifiers form a P-N junction with the n-type perovskite to provide efficient pathways for hole transfer and electron blocking. Third, the B-CDs increase the hydrophobicity of the perovskite film to improve the stability of CsPbI2 Br PSCs. With the above advantages, the CsPbI2 Br PSC with B-CDs modification shows an efficiency as high as 16.76%, one of the highest for its type. In addition, the modification renders significant improvement of air and light stability, with 95.33% of the initial PCE retained after storage in the ambient environment for 1000 h. This work demonstrates the great potential of B-CDs application in perovskite-based optoelectronic devices.

In this work, a novel phase change energy storage wood (PCESW) was fabricated by impregnating solid-solid phase change materials (SSPCM) into delignified wood. The SSPCM was prepared by using polyethylene glycol (PEG) 1500 as the thermal energy storage ingredient, hexamethylene diisocyanate (HDI) as the cross-linking agent and castor oil (CO) as the skeleton material. The chemical composition and structure of SSPCM and PCESW were confirmed by fourier transform infrared spectroscopy (FTIR); the crystalline structure of PEG and SSPCM were tested by x-ray diffraction (XRD); the microstructure of PCESW was observed by scanning electron microscopy (SEM); thermal properties and durability of SSPCM and PCESW were investigated by differential scanning calorimetry (DSC) and thermogravimetric analysis (TG). The results showed that: (1) the porosity of wood was improved obviously after delignification and SSPCM mainly distributed in wood vessels; (2) PCESW-15 exhibited superior temperature-regulating performance and thermal stability; (3) PCESW-15 presented outstanding shape stability and no liquid leakage occurred during the phase transition. The great thermal performance of PCESWs suggested that it can be used as energy-saving building materials for indoor temperature regulating.

Background Docosahexaenoic acid-derived protectin D1 (PD1) was identified critical in the resolution of inflammation in vivo, where it modulates the innate immune response and stimulates resolution. Acute pancreatitis (AP) is characterized by local pancreatic inflammation with mild forms whereas systemic inflammation with severe forms. Herein we investigate the impact of PD1 in murine models of pancreatitis. Methods Three independent AP models, which induced in male mice via intraperitoneal injection of caerulein, L-arginine or pancreatic duct ligation, were used to confirm the protective effect of PD1. Infiltrationsof neutrophils and macrophages in pancreas were detected by flow cytometry and immunohistochemistry. In vitro and in vivo neutrophil extracellular traps formation was detected by immunofluorescence staining. Expression of peptidylarginine deiminase 4 (PAD4) in activated neutrophils was evaluated by western blotting. Results Systemic treatment with PD1 reduced serum activities of amylase and lipase, blunted the concentrations of tumor necrosis factor-α and interleukin-6 in serum and protected against pancreas histologic damage in three AP models. PD1 also prolonged the survival in the pancreatic duct ligation model. Moreover, pancreatic infiltrationofneutrophils and neutrophil CitH3 expression were reduced after PD1 administration. In vitro studies revealed PD1 decreased supernatant cell-free DNA and CitH3 levels and downregulated PAD4 expression in mouse bone-marrow derived neutrophils. However, in the caerulein mice pretreated with GSK484 hydrochloride, an inhibitor of PAD4, PD1 treatment showed no more protective effect. Conclusions PD1 ameliorates AP by decreasing early infiltration of neutrophils into the pancreas and neutrophil extracellular traps formation through PAD4. These results supply the foundation to consider PD1 as a therapy for AP.

Wood plastic composites can absorb water in exterior applications due to the hygroscopicity of wood flour (WF). The cycle of adsorption and desorption process causes damage to the interfacial bonding between WF and polymer matrix, which benefits the fungal attack. In this study, WF was, respectively, immersed with silane, wax emulsion, and their compound systems for modification at different concentrations (1, 2, and 4%, respectively). Then, the modified WF was mixed with polypropylene (PP) to produce WF/PP composites at mass ratio of 6:4. The water absorption and mold susceptibility of the composites against Aspergillus niger were investigated. The results showed that silane can improve the interfacial adhesion between WF and PP. The water uptake of WF/PP composites treated with 4% silane decreased by 6% compared with the control, and the average mold growth rating decreased from level 4 (mold covering of 75–100%) to level 1 (mold covering of 0–25%). The strong hydrophobicity of wax had a negative effect on the interfacial adhesion of the composites. Thus, composites modified with wax and silane-wax compounds showed higher water uptake than the control. However, the mold resistance of composites was improved in these groups. POLYM. COMPOS., 2017. © 2017 Society of Plastics Engineers

Thermal energy storage composites were fabricated using paraffin as phase change material (PCM) and wood flour/high-density polyethylene (WF/HDPE) as the composite matrix. Expanded graphite (EG) was added to modify the thermal conductivity. The prepared paraffin/WF/HDPE composites were examined by scanning electron microscopy (SEM), X-ray diffractometer (XRD), differential scanning calorimetry (DSC), thermogravimetry (TG), infrared thermography, and laserflash thermal analysis. Physical and mechanical properties of the composites were also investigated. The results showed that: (1) the composite was the integration of paraffin, EG, WF, and HDPE with no new diffraction peaks were found in the XRD pattern; (2) thermal tests indicated that the paraffin/WF/HDPE composites had satisfying temperature conditioning ability, and the thermal conductivity of the composites was improved with the addition of EG; (3) incorporation of paraffin and EG into composites benefited their impact strength, but negatively affected the flexural properties; and (4) mechanical properties of the composites can be acceptable as building materials where mechanical strength are less important. POLYM. COMPOS., 2017. © 2017 Society of Plastics Engineers

Previous studies have shown that increasing estradiol concentrations had a toxic effect on the embryo and were deleterious to embryo adhesion. In this study, we evaluated the physiological impact of estradiol concentrations on endometrial cells to reveal that serum estradiol levels probably targeted the endometrium in controlled ovarian hyperstimulation (COH) protocols. An attachment model of human choriocarcinoma (JAr) cell spheroids to receptive-phase endometrial epithelial cells and Ishikawa cells treated with different estradiol (10−9 M or 10−7 M) concentrations was developed. Differentially expressed protein profiling of the Ishikawa cells was performed by proteomic analysis. Estradiol at 10−7 M demonstrated a high attachment rate of JAr spheroids to the endometrial cell monolayers. Using iTRAQ coupled with LC–MS/MS, we identified 45 differentially expressed proteins containing 43 significantly upregulated and 2 downregulated proteins in Ishikawa cells treated with 10−7 M estradiol. Differential expression of C3, plasminogen and kininogen-1 by Western blot confirmed the proteomic results. C3, plasminogen and kininogen-1 localization in human receptive endometrial luminal epithelium highlighted the key proteins as possible targets for endometrial receptivity and interception. Ingenuity pathway analysis of differentially expressed proteins exhibited a variety of signaling pathways, including LXR/RXR activation pathway and acute-phase response signaling and upstream regulators (TNF, IL6, Hmgn3 and miR-140-3p) associated with endometrial receptivity. The observed estrogenic effect on differential proteome dynamics in Ishikawa cells indicates that the human endometrium is the probable target for serum estradiol levels in COH cycles. The findings are also important for future functional studies with the identified proteins that may influence embryo implantation.

Formaldehyde abuse for retaining squid freshness is detrimental to public health. The aim is to establish a rapid and quantitative detection method of formaldehyde in squid for screening massive samples. A linear relationship between formaldehyde concentration in squid and formaldehyde concentration in squid soaked water was observed using HPLC. Chemical profile variances of squids were rapidly analyzed by Tri-step infrared spectroscopy. Specifically, with increasing formaldehyde concentration, peak intensities of 2927cm-1 (vas(CH2)), 1081cm-1 (glycogen), 1631cm-1 (β-sheet proteins) decreased while 1655cm-1 (α-helix proteins) increased. Spectral curve-fitting results further disclosed that β-sheet proteins were transformed to α-helix and β-turn conformations. Furthermore, a quantitative prediction model based on IR spectra was established by PLS (R2, 0.9787; RMSEC, 5.51). The developed method was applicable for rapid (c.a. 5min) and quantitative analysis of formaldehyde in squids with LOD of 15mg/kg.

We have studied the plasmon-driven photoreaction of a dual thiol-anchored o-nitrobenzyl-based photouncaging ligand on silver nanoparticles. Previous results have shown that this compound strongly anchors to gold surfaces, and a 1 J/cm2 dose of UV light induces the intended photoreaction, uncaging an amine on the surface. This allows for photopatterning and the selective adhesion of gold nanospheres (AuNSs) to a surface via electrostatic attraction between the positively charged amines and negatively charged AuNSs. Here, we report that when the ligand is adsorbed on a silver nanospheroid film (AgNS), an additional photoreaction induced by green light inhibits AuNSs adhesion in the UV exposed film. Our findings suggest that this is a result of the neutralization of the amine group’s ability to become charged, as opposed to the removal of the ligand from the surface of the silver nanospheroids. We hypothesize that this neutralization may be due to a form of hot-hole-induced photocatalysis, resulting in an N═...

A novel liquid chromatography tandem mass spectrometry (LC–MS/MS) method was developed and validated for the determination of four water-soluble vitamins (B1, B2, B6 and B9) in human serum and applied to compare with the electrochemical (EC) method clinically used for routine vitamin determination in patients. Vitamin separation were achieved at 30 °C on a Venusil XBP-C18 column (150 × 4.6 mm, 3 μm, 100A), and eluted with the mobile phase of 5 mM ammonium acetate: methanol (40:60, v/v) at a flow rate of 0.5 mL min−1, and with a run time of 6 min. The established LC–MS/MS method linearity was in the ranges 1–200, 5–40, 1–80, 5–40 ng mL−1 for vitamin B1, B2, B6 and B9, respectively. LC–MS/MS method met the precision and accuracy criteria (RSD%

The morphologies, sizes, compositions and volume fractions of dendritic phases in in situ Ti-based metallic glass matrix composites (MGMCs) containing beryllium (Be) with the nominal composition of Ti47Zr19Cu5V12Be17 (mole fraction, %) were investigated using XRD, SEM, EBSD, TEM, EDS and three-dimensional reconstruction method. Moreover, visualized at the nanoscale, Be distribution is confirmed to be only present in the matrix using scanning transmission electron microscopy–electron energy loss spectroscopy (STEM–EELS). Based on these findings, it has been obtained that the accurate chemical compositions are Ti28.3Zr19.7Cu8V6.4Be37.6 (mole fraction, %) for glass matrix and Ti62.4Zr18.4Cu2.6V16.6 (mole fraction, %) for the dendritic phases, and the volume fractions are 38.5% and 61.5%, respectively. It is believed that the results are of particular importance for the designing of Be-containing MGMCs.

Coronary artery involvement in Takayasu arteritis (TAK) leads to poor prognosis and high mortality. Tocilizumab (TCZ) has been used to effectively treat large vessel vasculitis. However, the efficacy of TCZ in resolving coronary artery involvement in TAK is unclear. The aim of this retrospective study was to evaluate the efficacy of TCZ in the treatment of coronary artery involvement in TAK. Clinical features and manifestations of coronary artery lesions in 11 TAK patients were evaluated before and after TCZ treatment, and the results were compared with those of 11 patients treated with traditional disease-modifying antirheumatic drugs (DMARDs). C-reactive protein (p = 0.006), erythrocyte sedimentation rate (ESR) (p = 0.011), and Kerr score (p = 0.007) were significantly decreased post-TCZ treatment for 6 months. The Indian Takayasu Clinical Activity Score (ITAS) 2010 (p = 0.019) and ITAS-A (p = 0.019) were significantly lower in patients treated with TCZ compared with those treated with traditional DMARDs. The glucocorticoid (GC) dose was tapered to 2.50 (0.00, 7.50) mg day−1 after TCZ treatment for 6 months, which was significantly lower than the GC dose after traditional DMARDs treatment [10.0 (5.00, 11.25) mg.day−1, (p = 0.033)]. After 6-month TCZ treatment, the total number of coronary artery lesions was reduced from 23 to 15 in 6 patients. Vascular wall thickening was remarkably improved in 2 lesions (in the ostia of the left main and right coronary arteries). TCZ may decrease the disease activity and improve coronary artery lesion in patients with TAK.

Environmentally persistent free radicals (EPFRs) are detected in the clay, mineral or humic part of the soil, especially in soil contaminated with phenolic compounds. To clarify the detailed information on the formation of EPFRs, we used the contaminated soil with catechol to mimic their formation process in laboratory scale and tested their biotoxicity with luminescent bacteria (Photobacterium phosphoreum, P. phosphoreum). Our results showed that the concentration of EPFRs reached the maximum at pyrolysis temperature of 300 °C, and EPFRs could significantly inhibit the luminescence of P. phosphoreum. Based on the detection of OH radicals in the aquatic system we used, we speculated that the generation of OH may be a crucial contributor to the toxicity of EPFRs. Our results aid to understand the detailed process on the formation of EPFRs in contaminated soil, as well as the basic biotoxicity data of EPFRs, which will be helpful and essential for their potential environmental risk assessments.

Objectives To reveal the role of circular RNA (circRNA) DOCK1 (circDOCK1) as a potential biomarker and therapeutic target and its competing endogenous RNA mechanism in bladder carcinoma (BC). Methods The next‐generation sequencing (NGS) technology was introduced to screen the circRNA expression profiles of BC using microarray. qPCR and Western blots assay were employed to measure the gene expression in different groups. Cell counting kit‐8, EdU and transwell assays were applied to detect the cell viability, proliferation and migration potential, respectively. Luciferase reporter assay was used to test the binds between hsa‐miR‐132‐3p/Sox5. Xenografted tumour growth of nude mice was performed to test the role of circDOCK1 in vivo. Results CircDOCK1 was upregulated in BC tissues and cell lines. Repression of circDOCK1 reduced cell viability, inhibited cell proliferation and curbed the cell migration potential of BC cell. CircDOCK1 played its role via regulation of circDOCK1/hsa‐miR‐132‐3p/Sox5 pathway in BC cells. Suppression circDOCK1 inhibited the tumour growth in vivo. Conclusion In this study, we revealed that circDOCK1 affected the progression of BC via modulation of circDOCK1/hsa‐miR‐132‐3p/Sox5 pathway both in vitro and in vivo and providing a potential biomarker and therapeutic targets for BC.

Peripheral neuropathy is the major dose-limiting side effect of paclitaxel (PTX), affecting both the quality of life and the survival of cancer patients. Nab-paclitaxel (nab-PTX) was developed to provide additional clinical benefits and overcome the safety drawbacks of solvent-based PTX. However, the prevalence of peripheral neuropathy induced by nab-PTX was reported higher than that induced by solvent-based PTX. Upon investigation, oxidative stress plays a major role in the toxicity of nab-PTX. In order to assess if the antioxidant alphalipoic acid (α-LA) could prevent the nab-PTX-induced peripheral neuropathy, Sprague-Dawley (SD) rats were treated with three doses of α-LA (15, 30, and 60 mg/kg in normal saline, i.p., q.d. (days 1-30)) and/or nab-PTX (7.4 mg/kg in normal saline, i.v., q.w. (days 8, 15, and 22)). Body weight and peripheral neuropathy were measured and assessed regularly during the study. The assessment of peripheral neuropathy was performed by the von Frey and acetone tests. A tumor xenograft model of pancreatic cancer was used to assess the impact of α-LA on the antitumor effect of nab-PTX. Results showed that α-LA significantly ameliorated the peripheral neuropathy induced by nab-PTX (p<0.05) without promoting tumor growth or reducing the chemotherapeutic effect of nab-PTX in a tumor xenograft model. Moreover, α-LA might significantly reverse the superoxide dismutase (SOD), glutathione (GSH), and malondialdehyde (MDA) levels altered by nab-PTX in the serum and the spinal cord of rats. Furthermore, α-LA could reverse the mRNA and protein expressions of Nrf2 (nuclear factor erythroid 2-related factor 2) and three Nrf2-responsive genes (HO-1, γ-GCLC, and NQO1) altered by nab-PTX in the dorsal root ganglion (DRG) of rats. In conclusion, our study suggests that α-LA could prevent oxidative stress and peripheral neuropathy in nab-PTX-treated rats through the Nrf2 signalling pathway without diminishing chemotherapeutic effect.

We quantitatively investigate lithographic patterning of a thiol-anchored self-assembled monolayer (SAM) of photocleavable o-nitrobenzyl ligands on gold through a multi-photon absorption process at 1.7 eV (730 nm wavelength). The photocleaving rate increases faster than the square of the incident light intensity, indicating a process more complex than simple two-photon absorption. We tentatively ascribe this observation to two-photon absorption that triggers the formation of a long-lived intermediate aci-nitro species whose decomposition yield is partially determined either by absorption of additional photons or by a local temperature that is elevated by the incident light. At the highest light intensities, thermal processes compete with photoactivation and lead to damage of the SAM. The threshold is high enough that this destructive process can largely be avoided, even while power densities are kept sufficiently large that complete photoactivation takes place on time scales of tens of seconds to a few minutes. This means that this type of ligand can be activated at visible and near infrared wavelengths where plasmonic resonances can easily be engineered in metal nanostructures, even though their single-photon reactivity at these wavelengths is negligible. This will allow selective functionalization of plasmon hotspots, which in addition to high resolution lithographic applications would be of benefit to applications such as Surface Enhanced Raman Spectroscopy and plasmonic photocatalysis as well as directed bottom-up nanoassembly. Published version

Chitosan oligosaccharide (COS) is known for its unique biological activities such as anti-tumor, anti-inflammatory, anti-oxidant, anti-bacterial activity, biological recognition, and immune enhancing effects, and thus continuous attracting many research interests in drug, food, cosmetics, biomaterials and tissue engineering fields. In comparison to its corresponding polymer, COS has much higher absorption profiles at the intestinal level, which results in permitting its quick access to the blood flow and potential contacting with blood components. However, the effects of COS on blood components remain unclear to date. Herein, two COS with different molecular weight (MW) were characterized by FTIR and 1H NMR, and then their effects on human blood components, including red blood cells (RBCs) (hemolysis, deformability, and aggregation), coagulation system [activated partial thromboplastin time (APTT), prothrombin time (PT), thrombin time (TT), and the concentration of fibrinogen (Fib)], complement (C3a and C5a activation), and platelet (activation and aggregation), were comprehensively studied. In the case of RBCs, COS exhibited a low risk of hemolysis in a dose and molecular weight dependent manner and the irreversible aggregation was observed in their high concentration. For coagulation system, COS has a mild anticoagulation activity through blocking the intrinsic coagulation pathway. In addition, COS showed no effect on complement activation in C3a and C5a and on platelet activation while inhibition of platelet aggregation was evident. Finally, the mechanism that effects of COS on blood components was discussed and proposed.