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Thermally-induced shape memory polymer composites (SMPCs) have the capability to self-deploy when stimulated by a specific temperature. As a basic component of deployable truss structure, SMPCs thin-wall circular tubes will undergo complex non-linear deformation and changing thermal boundary conditions during application. This article aims to research the mechanical behavior of thermally-induced SMPCs thin-wall circular tubes in a non-uniform thermal field. Thermal properties of SMPCs including thermal conductivities and coefficients of thermal expansion are tested as fundamental temperature-dependent parameters. A 500 mm-long SMPCs thin-wall tube is conducted in the flattening-folding-cooling-reheating experiments through a specially manufactured loading apparatus. Combining phase transition theory and Fourier heat conduction, a coupling algorithm is proposed to describe the thermo-mechanical behavior of SMPCs, which is implemented by the user subroutines VUMAT by commercial finite element analysis packages ABAQUS. By comparing the results from the simulation of the non-uniform thermal field, the simulation of the uniform thermal field and experiments, the coupling algorithm is verified, and the effect on SMPCs from the non-uniform thermal field is given. [ABSTRACT FROM AUTHOR]

(+)- and (-)-Tedanine [(+)-1 and (-)-1], a pair of new enantiomeric indolone alkaloids, along with nine compounds (2–10) were isolated from the marine sponge Tedania sp. The structures of (+)-1 and (-)-1 including absolute configurations were determined by spectroscopic analysis and quantum chemical calculation. Compounds (+)-1 and (-)-1 were the first examples of indolone alkaloids isolated from this genus. In addition, the cytotoxic and antibacterial activities of these compounds were also evaluated. [ABSTRACT FROM AUTHOR]

Two new alkaloids, spongimides A (1) and B (2), along with five known ones (3–7), were isolated from the marine sponge Spongia sp. The structures of 1 and 2 were determined by the spectroscopic methods (UV, IR, MS, and NMR) and X-ray diffraction analysis. Compounds 1, 3, and 4 were the first examples of 2,4-imidazolidinediones isolated from this genus. In addition, the cytotoxic and antibacterial activities of compounds 1 and 2 were also evaluated. [ABSTRACT FROM AUTHOR]

A new chlorobenzoate derivative, solieriate (1), together with six known compounds (2–7), were isolated from the red alga Solieria sp. The structures of 1–7 were determined by comprehensive spectroscopic methods and X-ray diffraction analysis. Compound 1 is the first example of halogenated derivative isolated from this genus. In addition, 1 exhibited moderate antibacterial activity on A. baumannii with MIC value of 64 μg/ml. [ABSTRACT FROM AUTHOR]

Cerebellopontine angle (CPA) oligodendrogliomas are very rare, and only three preoperative cases have been confirmed. Secondary CPA oligodendrogliomas after radiation therapy are exceptionally rare, and no other cases have been reported. We present a case of a 25-year-old male with CPA oligodendroglioma who experienced hearing loss in right ear with walking instability for more than 2 months. The patient underwent craniotomy in our hospital because of grade II astrocytoma of the right temporal lobe 10 years ago. Postoperative radiotherapy lasted for 30 days, and six rounds of chemotherapy were performed. Magnetic resonance imaging (MRI) of the head revealed a cystic lesion located in the right CPA. The patient underwent surgery without obvious complications, and the tumor was subtotally removed. Histopathological examination revealed a diagnosis of oligodendroglioma, World Health Organization (WHO) grade II. The patient was discharged on the tenth postoperative day with a good recovery. Two weeks after discharge, chemotherapy with temozolomide and radiotherapy were performed. The patient remained well at 8 months follow-up. To the best of our knowledge, no other cases of secondary CPA oligodendroglioma after cranial irradiation have been reported in the literature. Compared with general oligodendroglioma, the tumor has no typical calcification and is more aggressive. The cranial nerves in the CPA area are closely adhered, and the blood supply is abnormally rich. It is difficult to completely remove the tumor. Postoperative radiotherapy and chemotherapy should be carried out as soon as possible. [ABSTRACT FROM AUTHOR]

Two new halogenated metabolites, laurenhalogens A (1) and B (2), along with four known ones (3–6), were isolated from the red alga Laurencia sp. The structures of 1 and 2 were determined by the means of UV, IR, MS, NMR and X-ray diffraction analysis. In addition, the antibacterial activities of 1–6 were also evaluated. [ABSTRACT FROM AUTHOR]

A new amide, baeriamide (1), along with nine known diketopiperazines (2-10), was isolated from the marine sponge Haliclona baeri. Their structures were identified by the means of UV, IR, MS and NMR. The absolute configuration of 1 was established by Marfey's method and comparing the specific optical rotation with the known compound HCO-Val-Gly methyl ester. Compound 1 was derived from dehydration of formylated L-valine with γ-amino-butanoic acid methyl ester. Compounds 2-10 were isolated from the genus of Haliclona for the first time. The absolute confirmation of 7 was confirmed first by the means of single-crystal X-ray diffraction. The cytotoxic, antibacterial, antiviral and antifouling activities of these compounds were also tested. However, none of them exhibited significant bioactivities. [ABSTRACT FROM AUTHOR]

Extensive application of anti-HER2 targeted therapy improves significantly the HER2-positive advanced breast cancer (BC) prognosis, however, it is still difficult to treat brain metastasis. In current study, we explored effective approaches via combining pyrotinib to treat brain metastasis in patients with HER2-positive advanced BC based upon clinical data. Current study included 61 HER2-positive BC patients with brain metastases (BM) who were treated by pyrotinib-based regimens. The systemic regimens included pyrotinib combined with capecitabine, pyrotinib combined with nab-paclitaxel, and pyrotinib combined with vinorelbine. Patients' progression-free survival (PFS), overall survival (OS), clinical benefit rate (CBR) and objective response rate (ORR), as well as drug-related adverse events (AEs) in regard of each combination regimen were analyzed. Pyrotinib-based systemic therapy resulted in 8.6 months median PFS (mPFS) and 18.0 months median OS (mOS) among the BM patients. Regarding different regimens, the combination of pyrotinib with nab-paclitaxel was superior to the combination with capecitabine and vinorelbine with respect to PFS and OS. The central nervous system (CNS) ORR did not showcase significant difference among 3 regimens, however, nab-paclitaxel combined regimen obtained the best peripheral ORR (84.6%) (p ≤.05). Pyrotinib-based combination therapy is safe for HER2-positive brain metastasis treatment. Compared with vinorelbine or capecitabine, pyrotinib combined with nab-paclitaxel is more effective with less toxicity, which is the preferable regimen for HER2-positive brain metastasis. Present investigation investigated effective methods through combining pyrotinib to treat brain metastasis with HER2-positive advanced brain cancer. The outcomes verified that pyrotinib-based combination therapy was safe and efficient to treat HER2-positive brain metastasis. Therefore, it is effective to treat brain metastasis applying anti-HER2 targeted therapies although pyrotinib showcases efficiency regarding its treatments for the metastasis. [ABSTRACT FROM AUTHOR]

The resistance of HIV-1 protease (PR) mutations seriously affects the efficiency of current drugs in the clinical treatment of AIDS. Therefore, it is important to understand the resistance mechanism of mutated residues for the development of PR inhibitors. In this work, the mechanism of G48M mutant PR to inhibitors Saquinavir and Atazanavir was studied by using molecular dynamics simulation combined with free energy prediction. The analysis results showed that, compared with the WT PR, the distance of the flap tip from the protease catalytic binding site and the dihedral angles in the flap regions in the mutant type complexes was changed. These changes resulted in a significant reduction in the occupancy of most of the hydrogen bonds in the mutant complex and the interaction energy of key residues with the inhibitor, which is the main reason for the resistance of the mutation to these inhibitors. This study can provide important guidance for the design of effective inhibitors against HIV-1 PR. [ABSTRACT FROM AUTHOR]

A significant decrease in red blood cell (RBC) survival has been observed in patients with renal failure, which is supposed to contribute to renal anemia. The aim of this observational study was to determine RBC survival in hemodialysis (HD) patients treated with roxadustat or recombinant human erythropoietin (rhuEPO) compared with healthy persons. RBC lifespan was measured by Levitt's CO breath test with newly developed automatic instrument ELS Tester. A total of 102 patients receiving long-term HD from two independent dialysis centers enrolled in the study, of whom 62 were treated with rhuEPO and 40 were on roxadustat therapy. A total of 25 healthy participants were recruited to match HD participants according to age and sex. Median RBC survival times in rhuEPO, roxadustat, and control groups were 65.0 (25th–75th percentile, 49.5–77.3), 75.5 (25th–75th percentile, 57.3–99.3), and 108.0 (25th–75th percentile, 89.0–141.5) d, respectively. Patients treated with roxadustat had significantly longer RBC survival time than patients treated with rhuEPO (p <.05). In multivariate analysis of factors affecting RBC lifespan in the whole HD patients, anemia treatment drugs (rhuEPO/roxadustat) and levels of hemoglobin were the significantly independent factors. RBC survival was not found to correlate with either weekly rhuEPO dosage (r = –0.087, p =.500) or weekly roxadustat dosage (r = −0.267, p =.110) in our cohort. HD patients treated with roxadustat had significantly longer RBC survival time than patients treated with rhuEPO, large prospective studies with long-term follow-up are warranted to verify the results in future. Abbreviations RBC: red blood cell; HD: hemodialysis; rhu EPO: recombinant human erythropoietin; ESRD: end-stage renal disease; EPO: erythropoietin; ROS: reactive oxygen species; CKD: chronic kideny disease; ESAs: erythropoiesis-stimulating agents; HIF-PHD: hypoxia-inducible factor prolyl hydroxylase; CO: carbon monoxide; Hb: hemoglobin [ABSTRACT FROM AUTHOR]

Two new pyrrolidine alkaloids, acanthophoraines B (1) and C (2), together with five known ones (3–7) were isolated from the red alga Acanthophora spicifera. Their structures were elucidated by extensive spectroscopic methods and single-crystal X-ray diffraction analysis. The absolute configuration of 2 was established by ECD calculation. The antibacterial activities of 1–7 were also evaluated. [ABSTRACT FROM AUTHOR]

A new polyketide, solieritide A (1), along with six known ones (2–7), had been isolated from the red alga Solieria sp. The structures of these compounds were elucidated by spectroscopic analysis. The absolute configuration of 1 was determined by the method of X-ray diffraction. Compound 1 was a rare polyketide bearing benzopyrone ring fused with γ-butyrolactone. Compounds 2–7 were isolated from the red algae of genus Solieria for the first time. The antibacterial activities of 1–7 were also discussed. [ABSTRACT FROM AUTHOR]

Intradural extramedullary (IDEM) ependymomas are very rare, and IDEM ependymomas with craniospinal disseminated metastasis are exceptionally rare; only 2 preoperative cases have been confirmed, and postoperative cases have not been reported. We present a case of a 21-year-old female with an IDEM ependymoma of the craniocervical junction who experienced head and neck pain for more than 1 month. Magnetic resonance imaging (MRI) of the cervical spine revealed a large IDEM cystic lesion located in the medulla oblongata and the upper cervical spinal cord. The patient underwent surgery without complications, and the tumor was completely removed. Histopathological examination revealed a diagnosis of aplastic ependymoma, World Health Organization (WHO) grade III. The patient failed to follow-up with radiotherapy for one month after discharge. Nearly three months after surgery, craniospinal disseminated metastasis was found in the patient; subsequently, chemoradiotherapy was administered to prolong the survival time of the patient. Unfortunately, the patient underwent radiotherapy and chemotherapy for only 7 days; then, the patient gave up treatment and died 5 months later. To the best of our knowledge, no other cases of craniocervical junction anaplastic ependymomas with craniospinal disseminated metastasis have been reported in the literature. Total resection does not completely prevent recurrence and metastasis, and MRI of the entire neuraxis and timely postoperative craniospinal radiotherapy are necessary for the treatment of this disease. [ABSTRACT FROM AUTHOR]

(+)- and (−)-Spongiterpene [(+)-1 and (−)-1], a pair of new valerenane sesquiterpene enantiomers, along with four known compounds (2-5) were isolated from the marine sponge Spongia sp. The structures of (+)-1 and (−)-1 including absolute configurations were determined by spectroscopic analysis, quantum chemical calculation and X-ray diffraction. Compounds (+)-1 and (−)-1 were the first examples of valerenane sesquiterpenes isolated from the marine sponges. The cytotoxic activities of (+)-1 and (−)-1 were also evaluated. [ABSTRACT FROM AUTHOR]

High-dose vitamin C is an essential adjunctive drug for sepsis treatment. This study aimed to determine if high-dose vitamin C could lead to erroneous point-of-care glucose testing results. This retrospective, single-center, observational case series involved septic patients treated with high-dose vitamin C. We monitored their paired point-of-care glucose and laboratory glucose levels for statistical analysis. The glucose oxidase-peroxidase colorimetric method and hexokinase spectrophotometric method were applied for point-of-care glucose and laboratory glucose monitoring, respectively. Parkes Consensus Error Grid Analysis was used to assess the clinical influence of paired blood glucose values. Subgroup analyses were conducted to explore the effect of different vitamin C dosages and various renal function levels on point-of-care glucose readings. During a 3-year period, 82 eligible septic patients who accepted at least three days of high-dose vitamin C treatment were included in this study. Compliance with ISO15197:2013 criteria was met in 30 (36.59%) paired values, a proportion considerably lower than the minimum criteria for accuracy. Subgroup analysis showed that worse renal function or higher vitamin C dosage could lead to greater bias in point-of-care glucose readings; however, these inaccuracies rarely represented a clinical risk. High-dose intravenous ascorbate acid infusion may interfere with point-of-care glucose testing results. Thus, laboratory glucose measurements are recommended for more accurate results. Nonetheless, the inaccuracies magnitude of point-of-care glucose readings does not represent a significant clinical risk when physicians alter clinical action based on these results. [ABSTRACT FROM AUTHOR]

A new pyrrolidine alkaloid, acanthophoraine A (1), along with six known alkaloids (2–7), had been isolated from the red alga Acanthophora spicifera. The structures of these compounds were identified by spectroscopic analyses. The absolute configuration of 1 was established by ECD calculation. Compound 1 represents the first example of N-isobutyl pyrrolidone with an urea arm. The antimicrobial activity of 1 was also evaluated. [ABSTRACT FROM AUTHOR]

Objective: Three differently designed multilayer films of TiCu/TiCuN multilayer (M1, M2, and M3) were deposited on 316L stainless steel surface using the axial magnetic field-enhanced arc ion plating (AMFE-ARP) method. The aim of this study was to investigate both cytocompatibility and antibacterial activity of the multilayer films. Methods: The antibacterial rate, attached bacteria and developed biofilms were studied from quantitative antibacterial test and bacterial morphological examination. The in vitro biocompatibilities of the films were systematically investigated by means of methods of CCK8 cell proliferation assay, phalloidin cytoskeleton staining and Annexin-V/PI flow cytometry. Results: The multilayer film of M2 revealed a better cytocompatibility and antibacterial activity than the others. The M2 film is suggested to be much application potential as antibacterial films on the biomedical implants. [ABSTRACT FROM AUTHOR]

A new thiodiketopiperzaine, tedanizaine A (1), together with six known ones, were isolated from the marine sponge Tedania sp. Their structures were determined by spectroscopic analyses. The absolute configuration of 1 was established by ECD calculation. Compound 1 was the second example of thiodiketopiperazine bearing a thiazolidine unit. Cytotoxic activities of 1 were also evaluated. [ABSTRACT FROM AUTHOR]

A novel valerenane sesquiterpenoid sinulaspirolactam A (1), together with five known compounds, was isolated from the soft coral Sinularia sp. Their structures were determined by spectroscopic analyses. The absolute configuration of 1 was established by ECD calculation. Compound 1 was the first example of valerenane sesquiterpenoid bearing an aza-spiro[4.5] ring moiety, the plausible biogenetic pathway of which was proposed. Cytotoxic activities of these compounds were also evaluated. [ABSTRACT FROM AUTHOR]

Pulmonary adenoid cystic carcinoma is a rare and indolent lung malignancy, characterized by a protracted but unpredictable growth behavior. Currently, the treatment of PACC relies on surgery and local radiotherapy. However, treatment options for advanced PACC patients are limited. A larger number of studies demonstrated that advanced PACC patients obtained limited benefit from chemotherapy. Moreover, only a few case reports revealed PACC patients were candidates for target therapy. Therefore, there is an urgent need to develop novel therapies. Due to its rareness, its mutational landscape remains largely elusive. In this study, we performed capture-based ultra-deep sequencing on multiregional surgical specimens obtained from 8 PACC patients using a panel consisting of 295 cancer-related genes. Our data revealed distinctive mutational spectrum of PACC, which differed from non-small cell lung cancer and adenoid cystic carcinomas originated from other anatomical sites. PACC, lacking mutations in a majority of non-small cell lung cancer driver genes, has frequent mutations in genes participating in chromatin remodeling and NOTCH signaling pathway. We also elucidated spatial intra-tumoral heterogeneity, which varied among cases. Most mutations in chromatin remodelers were subclonal. Collectively, our findings elucidated molecular signature associated with PACC and highlighted the potential for epigenetic therapy in this disease. [ABSTRACT FROM AUTHOR]

Background: Our aim was to establish the reference interval (RI) for serum CYFRA 21-1 in healthy Chinese Han ethnic adults, since there has been no report about it.Methods: After screening, 9954 healthy Chinese Han adults (age range 18-95 years) were recruited, including 6639 (66.7%) males and 3315 (33.3%) females. Electrochemiluminescence immunoassay was used to measure serum CYFRA21-1. The RI was defined by nonparametric 95% percentile interval.Results: The distribution for serum CYFRA21-1 level was non-Gaussian. The RI for healthy Chinese Han adults calculated by nonparametric method was 0-4.47 ng/ml in this study, higher than that recommended by Roche Diagnostics GmbH (≤3.3 ng/ml). The reference values were higher in males than females before 50 years of age, although the difference was hardly seen after 50 years of age. The reference value increased with age in both males and females. Of slight difference, the increase of male reference value was obvious at 60-69 and more than 80 years of age, while that of female obvious at 50-69 and more than 80 years of age.Conclusions: We establish the RI for serum CYFRA21-1 in healthy Chinese Han population, which is higher than that recommended by Roche Diagnostics GmbH. Furthermore, our study suggests that it is necessary to establish the age- and sex-specific RIs for serum CYFRA21-1. [ABSTRACT FROM AUTHOR]

This work is focused on the development of a convenient and efficient approach for the synthesis of furoquinolinones and furopyridinones through palladium-catalyzed cyclization reactions between styrenes and 4-hydroxyquinolinones/4-hydroxypyridinones under air conditions. Studies conducted to evaluate the antitumoral potential of the resulted compounds revealed that some of the obtained furoquinolinones exhibited in vitro antiproliferative activity on human-derived stomach cancer cell lines. [ABSTRACT FROM AUTHOR]

We have developed a new method to simultaneously determine five marker compounds in Menthae Herba via HPLC/PDA – including hesperidin (1), rosmarinic acid (2), diosmin (3), didymin (4) and buddleoside (5). The newly developed method was successfully used to analyse for two species (Mentha arvensis L. and Mentha haplocalyx Briq.) of Menthae Herba, and the satisfactory results were obtained from the validation of developed method. The pattern analysis could greatly discriminate between M. arvensis L. and M. haplocalyx Briq. In conclusion, the proposed HPLC/PDA method is suitable for quality evaluation of Menthae Herba. [ABSTRACT FROM AUTHOR]

Eupatorium adenophorum can induce liver toxicity in animals. For the safe utilisation of the weed, the hepatotoxic components need to be discovered. In this study, in vitro hepatotoxicity of different extracts from E. adenophorum were determined on human hepatocyte cell line L02 and hepatocellular carcinoma cell line HepG2. The results showed that water extracts of E. adenophorum exhibited no hepatotoxicity in vitro while high concentrations of the organic solvent extracts had obvious hepatotoxicity. Sesquiterpenes may contribute to the toxicity based on the comparison of composition analysis. Three cadinene sesquiterpenes were purified and identified as 9-oxo-10,11-dehydroageraphorone, 10Hα-9-oxo-ageraphorone and 10Hβ-9-oxo-ageraphorone. In vitro hepatotoxic effects of these components were investigated, the IC50 of the three compounds were 122.53, 87.52, and 108.80 μM in L02 cells and 151.92, 104.48, and 138.08 μM in HepG2 cells by Cell Counting Kit-8 (CCK-8) assay. The three components were confirmed to be, at least partial, hepatotoxic components. [ABSTRACT FROM AUTHOR]

Macamides are bioactive and marker compounds of maca (Lepidium meyenii). Thirty-five commercial maca products were surveyed for macamide composition and content by HPLC-UV/MS. Significant variations of macamide content were found in these products (69-2738 μg/g). Analysis of the macamide biosynthetic pathway suggests that: (a) glucosinolate catabolism, (b) lipid hydrolysis, and (c) amide formation are key steps controlling macamide accumulation in the tissues during the postharvest drying process. Therefore, we further investigated the effects of sample forms, drying temperatures, and storage times on macamide accumulation. Our results show that (1) powdered maca provided the largest macamide accumulation followed by sliced hypocotyls, while whole roots displayed a significantly reduced amide-generating potential; (2) the ideal temperature for macamide formation is about 30°C; (3) macamide content increases continuously along with storage time; (4) exposure to air results in the percentage of unsaturated macamides decreasing. These findings provide useful insights which can be applied in the industrial manufacture of maca products with higher content of bioactive amides. [ABSTRACT FROM AUTHOR]

A new α-pyrone, nocapyrone S (1), together with five known compounds (2-6), were isolated from the deep-sea actinomyceteNocardiopsis dassonvilleisubsp.dassonvilleiDSM 43111(T). Their structures were determined by spectroscopic analyses. The absolute configuration of1was established by quantum approaches. Cytotoxic activity of1was evaluated against K562, MCF-7, SGC7901, A375, Hela, and HepG2 cell lines. [ABSTRACT FROM PUBLISHER]

Two new polyketides, aspergchromones A (1) and B (2), together with five known compounds, secalonic acid D (3), noreugenin (4), (3S)-5-hydroxymellein (5), (4S)-6-hydroxyisosclerone (6), and (-)-regiolone (7), were isolated from the ethyl acetate extract of marine sponge-derived fungusAspergillussp. SCSIO XWS03F03. Their structures were elucidated by means of spectroscopic techniques (1D and 2D NMR, MS, UV, and IR). The absolute configurations of the new compounds were established by ECD calculations. Compound3showed moderate antimicrobial activity. [ABSTRACT FROM PUBLISHER]

An efficient method for simultaneous detoxification and preparative separation of chlorogenic acid fromEupatorium adenophorumwas developed. The entire procedure consisted of two separation steps. The first step was enrichment of chlorogenic acid from the crude extract by NKA-II macroporous resin. The purity of chlorogenic acid increased from 5.3% to 20.9% with a recovery of 88.7%. Subsequently, polyamide resin was used to achieve a higher purity. After the polyamide resin treatment, the main toxin 9-oxo-10,11-dehydroageraphorone was removed and the purity of chlorogenic acid reached 86.5% with a recovery of 84.8%. It provided a new way for the utilization ofE. adenophorum. [ABSTRACT FROM AUTHOR]

Context: Despite phytochemical studies ofAgrimonia pilosaLedeb. (Rosaceae), the antidiabetic effects of this plant are unknown. Objective: This study characterizes the isolated compounds from the aerial parts ofA. pilosaand evaluates their PTP1B and α-glucosidase inhibitory properties. Materials and methods: Ethanol extract ofA. pilosawas found to inhibit 64% PTP1B activity at 30 μg/mL. The ethanol extract was partitioned with methylene chloride, ethyl acetate,n-butanol, and water fractions. Among these, the ethyl acetate fraction displayed the most potent PTP1B activity. The ethyl acetate extract was separated by chromatographic methods to obtain flavonoids and triterpenoids (1–11); which were evaluated for their inhibitory effects on PTP1B activity withp-nitrophenyl phosphate (p-NPP) as a substrate, and also α-glucosidase enzyme. Results: Compounds1–11were identified as apigenin-7-O-β-d-glucuronide-6″-methyl ester, triliroside, quercetin-7-O-β-d-glycoside, quercetin-3-O-β-d-glycoside, kaempferol, kaempferol-3-O-α-l-rhamnoside, β-sitosterol, ursolic acid, tormentic acid, methyl 2-hydroxyl tricosanoate, and palmitic acid. Compounds8,9, and11displayed inhibitory effects on PTP1B activity with IC50values of 3.47 ± 0.02, 0.50 ± 0.06, and 0.10 ± 0.03 μM, respectively. Compounds3,4,6, and9exhibited inhibition of the α-glucosidase activity with IC50values of 11.2 ± 0.2, 29.6 ± 0.9, 28.5 ± 0.1, and 23.8 ± 0.4 μM, respectively. Discussion and conclusion: As major ingredients ofA. pilosa, compounds1,6,8, and9showed the greatest inhibitory potency on PTP1B activity. Compounds3,6,8, and9also showed potent inhibitory effects on α-glucosidase enzyme. This result suggested the potential of these compounds for developing antidiabetic agents. [ABSTRACT FROM AUTHOR]

A new taraxastane-type triterpenoid glycoside, clematiunicinoside I (1), together with four known ones (2–5), was isolated from the roots ofClematis uncinata. The structure of the new compound was elucidated on the basis of spectroscopic analyses and acid hydrolysis. The cytotoxic activities of all the compounds against caski cervical cancer (Caski) cells were evaluated. This is the first report of the presence of taraxastane-type triterpenoid glycoside in the genusClematis. [ABSTRACT FROM PUBLISHER]

This study was conducted to evaluate the adjuvant potential of sulfated Radix Cyathulae officinalis Kuan polysaccharides (sRCPS) and their effects on specific cellular and humoral immune responses to hepatitis B subunit vaccine in mice. Our data demonstrated that sRCPS significantly promoted the rHBsAg-specific IgG, IgG1, IgG2a, and IgG2b antibody titers, the activities of natural killer cells (NK) and cytotoxic T lymphocytes (CTL), T cells proliferation, and phagocytic capacity of peritoneal macrophages. Furthermore, sRCPS increased the levels of IL-4, IL-2, and IFN-γ in CD4+T cells and the level of IFN-γ in CD8+T cells. In addition, sRCPS enhanced the expression of CD40+, CD80+, CD86+, MHC I and MHC II in dendritic cells (DCs) and upregulated the mRNA levels of MHC I, MHC II. sRCPS downregulated the frequency of CD4+CD25+Foxp3+ Treg cells. sRCPS increased both cellular and humoral immune responses by upregulating DC maturation, and suppressing the frequency of Treg cells. [ABSTRACT FROM AUTHOR]

Application of organic nitrogen (N) has been proposed as a method to reduce potential environmental pollution due to N loss without sacrificing grain yield. The mechanism responsible for organic N regulation of maize (Zea maysL.) N metabolism is nonetheless largely unknown. In this study, we compared the expression of genes related to N assimilation and remobilization during the grain filling stage in maize plants grown under field conditions. We applied five different N treatments, which consisted of N supplied in organic and/or inorganic forms at the following rates: 0/45, 0/120, 0/240, 120/120, and 240/0 kg ha−1organic/inorganic N. Yield was found to increase with increasing N input, but no significant difference was found in grain yield among 0/240, 240/0 and 120/120 treatments. Organic N application tended to decrease N accumulation and to increase N utilization efficiency. Genes related to N assimilation activity in leaves, such asZmNR1andZmFd-GOGAT1, were unaffected by different N forms. In contrast, genes related to N remobilization activity in leaves, such asZmGS1.1andZmGDH1, were up-regulated, especially in old leaves, by the pure organic N supply treatment (240/0). These data suggest that application of pure organic N likely induces a N-deficiency response in maize plants, with a consequent increase in physiological N utilization efficiency due to up-regulation of key genes involved in N remobilization processes. [ABSTRACT FROM PUBLISHER]

Phytochemical investigation on the fruits of Flueggea suffruticosa resulted in the isolation of three new Securinega alkaloids, secu'amamine H (1), 15β-methoxy-14,15-dihydrosecurinine (3), and securinol E (7), as well as eight known ones (2, 4–6, and 8–11). Their structures were elucidated by means of spectroscopic techniques (1D and 2D NMR, MS, UV, and IR). The absolute configurations of the new compounds were established by single-crystal X-ray diffraction and CD analyses. [ABSTRACT FROM AUTHOR]

Five new stilbene glycosides (1–5), together with six known ones, were isolated from the roots of Polygonum multiflorum. Their structures were elucidated on the basis of spectroscopic analysis and chemical evidence. [ABSTRACT FROM AUTHOR]

In this study, the underwater behaviour of sediment thermals (i.e. sediment clouds in the self-preserving phase), formed by releasing dry sediments instantaneously from various heights above water, was investigated experimentally. Measurements show that as the air release height increases, the initial acceleration phase of the sediment cloud in water is shortened, while the growth rate during its self-preserving phase remains constant. Therefore, the effect of air release height can be accounted for by utilizing a new concept of simultaneous virtual distance and time origins, which are found to be related to an impact densimetric Froude number (defined as the ratio between the impact velocity of the sediment cluster at the water surface and the characteristic velocity of the sediment thermal generated by buoyancy excess). Based on the measurement results, a semi-empirical model is utilized to predict the growth and penetration behaviours of the sediment thermal. Predictions by the model with the virtual origins correction match well with the experimental data. [ABSTRACT FROM PUBLISHER]

Two new euglobals, R1 (1) and R2 (2), together with eight known euglobals (3–10) were isolated from the leaves of Eucalyptus robusta. Their structures were established by means of spectroscopic analysis and single-crystal X-ray diffraction. Euglobal R1 (1) represents a new skeleton of formyl-isovaleryl phloroglucinol-coupled β-phellandrene. [ABSTRACT FROM PUBLISHER]

Aminopeptidase N (APN), recognized by Asn-Gly-Arg (NGR) peptides, is expressed in the pericytes associated with the BBB, and the main objective of this study is to confirm the hypothesis that NGR-modified DSPE--PEG micelles containing paclitaxel (NGR-M-PTX) can bind to and kill brain tumor angiogenic blood vessels and penetrate into the brain tumor interstitial space, resulting in direct cell death. NGR-M-PTX is prepared by a thin-film hydration method. The in vitro targeting characteristics of NGR-modified micelles on BMEC (murine brain microvascular endothelial cells) were investigated. The effect of NGR-M-PTX on BMEC proliferation and the cytotoxicity of NGR-M-PTX in C6 glioma cells were also tested. The antitumor activity NGR-M-PTX was evaluated in C6 glioma tumor--bearing rats in vivo. The particle size of NGR-M-PTX was approximately 54.2 nm. The drug encapsulation efficiency of NGR-M-PTX was 82.11 ±± 2.82%. The cellular coumarin-6 level of NGR-M-coumarin-6 in the BMEC was about 2.2-fold higher than that of M-coumarin-6. BMEC proliferation was significantly inhibited by NGR-M-PTX. NGR-M-PTX had a much lower IC50 value than M-PTX and free drug. The growth of C6 glioma tumor was markedly inhibited by NGR-M-PTX compared with Taxol. In conclusion, our results show that antiangiogenic therapy using NGR-M-PTX exhibits potent in vivo antitumor activity in a C6 glioma--bearing animal model. [ABSTRACT FROM AUTHOR]

A novel series of 1,3-bis(2-dihydrothiazolyl)thiaalkoxy-p-tert-butylcalix[4]arenes generated by the reaction between 4,5-dihydrothiazole-2-thiol and the different dibromide calix[4]aryl groups have been synthesized and structurally characterized by IR, 1H NMR, 13C NMR, and MS. From their analytical data, it was found that compounds 8, 9, and 10 had cone conformations, whereas compound 11 existed as a mixture conformation. To verify the structure of the synthetic compounds, a single-crystal X-ray structure of compound 8 was obtained. [ABSTRACT FROM AUTHOR]

Reaction of thianthrene cation radical tetrafluoroborate and hexafluorophosphate with an excess of 1,4-hexadiene, 1,5-hexadiene, 1,7-octadiene, 1,8-nonadiene and 1,9-decadiene gave, in each case, a mixture of bis- and monoadduct from addition to one of the diene’s double bonds. Addition to both double bonds did not occur. The monoadduct of each diene and the bisadduct (7a) of 1,5-hexadiene were isolated. All monoadducts and 7a were characterized with 1 H and 13 C NMR spectroscopy. By reaction on activated alumina adducts were converted into ( E )- and ( Z )-(5-thianthreniumyl)dienes, all of which were characterized with 1 H and 13 C NMR spectroscopy. The monoadduct (6a) of 1,4-hexadiene and the bisadduct 7a were characterized with X-ray crystallography. [ABSTRACT FROM AUTHOR]

Reaction of thianthrene cation radical tetrafluoroborate with 1,5-hexadiene, 1,7-octadiene, 1,8-nonadiene and 1,9-decadiene in the molar ratio 4:1 caused addition to occur to one and both of each diene’s double bonds. A mixture of four adducts was thus obtained, namely a bisadduct (12a–d), a monoadduct (13a–d), a di(bis)adduct (14a–d) and a di(mono)adduct (15a–d). The di(mono)adducts (15b–d) were isolated and characterized with 1 H and 13 C NMR spectroscopy. Under the same condition of excess of cation radical, addition occurred to only one double bond of 1,4-cyclohexadiene and 1,5-cyclooctadiene. Addition to both double bonds was not observed. The bisadduct (16) of 1,4-cyclohexadiene was characterized with 1 H and 13 C NMR spectroscopy and X-ray crystallography. On activated alumina, 15b–d underwent fast opening of dicationic rings to form mixtures of ( E , E ) – (17b–d) and ( E , Z )-di(5-thianthreniumyl)diene (18b–d) in which the ( E , E )-isomer was dominant and was characterized with 1 H and 13 C NMR spectroscopy. [ABSTRACT FROM AUTHOR]

Polarization-dependent infrared spectra of an antiferroelectric liquid crystal in the phase were measured at 60°C, for investigation of the relative orientation of the terminal alkyl chain and mesogen. The polarization angle-dependent infrared spectra obtained were analysed by two-dimensional (2D) correlation spectroscopy. The orientation of the mesogen segment and the alkyl chains in the phase is similar to that in the SmC* phase. Four new CH 3 and CH 2 stretching modes were observed from the 2D correlation spectra. From these we can clearly separate the vibrational mode for two hydrocarbon chains and conclude that the orientations of the two chains are different. The C=O group adjacent to the chiral segment is also separated by 2D correlation spectra into two bands, which may arise from either the C=O group hydrogen-bonded with the phenyl ring, or from another rotational conformation of the molecule. [ABSTRACT FROM AUTHOR]

AbstractA new steroid, 2a-oxa-2-oxo-5β-hydroxy-3,4-dinor-24-methylcholesta-22E-ene (1), together with 10 known ones (2–11), was isolated from the marine sponge Cliona sp. The structures of these compounds were determined by the spectroscopic methods (UV, IR, MS, and NMR) and X-ray diffraction analysis. Compound 1 was the third example of 3,4-dinorsteroid with a hemiketal at C-5 that was isolated from the natural source. In addition, the antibacterial activities of these compounds were also evaluated. However, none of them exhibited significant inhibition effects. [ABSTRACT FROM AUTHOR]