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Two neolignan glycosides including a new one (1), along with seven iridoid glycosides (3 − 9) and nine flavonoid glycosides (10 − 18), were isolated from the leaves of Vaccinium bracteatum. Their structures were established mainly on the basis of 1D/2D NMR and ESIMS analyses, as well as comparison to known compounds in the literature. The structure of 1 with absolute stereochemistry was also confirmed by chemical degradation and ECD calculation. Selective compounds showed antiradical activity against ABTS and/or DPPH. Moreover, several isolates also suppressed the production of ROS in RAW264.7 cells and exerted neuroprotective effect toward PC12 cells. [ABSTRACT FROM AUTHOR]

In our chemical investigation into Penicillium sp. UJNMF0740 derived from mangrove sediment, fourteen indole diterpene analogs, including four new ones, are purified by multiple chromatographic separation methods, with their structures being elucidated by the analyses of NMR, HR-ESIMS, and ECD data. The antibacterial and neuroprotective effects of these isolates were examined, and only compounds 6 and 9 exhibited weak antibacterial activity, while compounds 5, 8, and 10 showed protective effects against the injury of PC12 cells induced by 6-hydroxydopamine (6-OHDA). Additionally, compound 5 could suppress the apoptosis and production of reactive oxygen species (ROS) in 6-OHDA-stimulated PC12 cells as well as trigger the phosphorylation of PI3K and Akt. Taken together, our work enriches the structural diversity of indole diterpenes and hints that compounds of this skeleton can repress the 6-OHDA-induced apoptosis of PC12 cells via regulating the PI3K/Akt signaling pathway, which provides evidence for the future utilization of this fascinating class of molecules as potential neuroprotective agents. [ABSTRACT FROM AUTHOR]

Insects and their gut bacteria can degrade insecticides separately, which is helpful for insecticide resistance development. However, there is little knowledge about insect and gut bacteria cooperation or their respective roles in an insecticide degradation complex. In this study, we investigated the activities of three enzymes related to pesticide degradation in a leaf beetle, Ambrostoma quadriimpressum Motschulsky. The activities of glutathione S-transferase (GST), carboxylesterase (CarE), and catalase (CAT) were up-regulated in the holo-gut (including lumen) after 5 days of exposure to beta-cypermethrin. The roles of the beetle gut and its bacteria were partitioned via transcriptome sequencing and 16S rDNA sequencing. The results showed that the elevated activities of CarE were attributed to the beetle gut, whereas GST and CAT were attributed to its bacteria. Pathway enrichment analysis based on a reference database hybridized with the BioCyc and KEGG databases showed that the gluconeogenesis pathway plays an important role in the gut of the beetle to counter the insecticide. The guts may be injured by the insecticide, and the epithelial cells regenerated via the Hippo signaling pathway activated by glutamate. The results from PICRUSt 2 and LEfSe showed a possible community pathway degrading the insecticide in the gut, i.e., beta-cypermethrin was degraded into intermediates (e.g., protocatechuate and catechol) and subsequently degraded by gut bacteria via the ortho- or meta-cleavage pathway. [ABSTRACT FROM AUTHOR]

The complete mitogenome sequence of Eothenomys eleusis Thomas 1911 was determined using PCR. A circular double-stranded structure makes up the mitochondrial genome of E. eleusis. The complete length of the mitochondrial genome is 16,419 bp. The mitochondrial genome of E. eleusis included 13 protein-coding genes, 1 control region, 22 tRNA genes, 2 rRNA genes and 1 origin of L strand replication. The total base composition of E. eleusis mitochondrial genome was A (32.6%), T (26.3%), G (13.6%) and C (27.5%). We found significant A-T skew in base composition, especially in control regions and protein-coding genes. E. eleusis was supported by bootstrap values of 100%. This study verifies the evolutionary status of E. eleusis in Myodini tribe of Cricetidae at the molecular level. The mitochondrial genome would be a significant supplement for the E. eleusis genetic background. [ABSTRACT FROM AUTHOR]

The health benefits of Vaccinium bracteatum are well recorded in ancient Chinese medical books and were also demonstrated by modern researches. However, the relationship between its beneficial functions and specific chemical constituents has not been fully characterized. This study investigated the bioactive small-molecule constituents in the leaves of V. bracteatum, which afforded 32 compounds including ten new ones (1–9) and ten pairs of enantiomers (9–18). Their structures with absolute configurations were elucidated by spectroscopic methods, especially nuclear magnetic resonance (NMR) and electronic circular dichroism (ECD) analyses, with 1–4 bearing a novel revolving-door shaped scaffold. While half-compounds exhibited decent antioxidant activity by scavenging 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals, all except 19 and 20 exerted significant capturing activity against diammonium 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonate) (ABTS) radicals. In addition, the new iridoids 1, 5, 6, and 7 exerted apparent neuroprotective activity toward PC12 cells, with 1 being comparable to the positive control, and selective compounds also displayed anti-diabetic and anti-inflammatory properties by inhibiting α-glucosidase and NO production, respectively. The current work revealed that the bioactive small-molecule constituents could be closely related to the functional food property of the title species. [ABSTRACT FROM AUTHOR]

Five tigliane (1−5) and one ingenane (6) diterpenoids were isolated from the ethanol extract of Euphorbia tirucalli. The structures of these compounds were identified based on analysis of their spectroscopic data. Among them, compound 12-O-(2E,4E,6E,8E-tetradecatetraenoyl)-13-O-isobutyroyl-4β-deoxyphorbol (1) was a new tigliane. The Rho123 effluxion assay showed that tiglianes with a trans-fused 5/7 ring system such as compounds 1, 2, and 4 had potent inhibitory activity against P-glycoprotein in HepG2/ADR cells. [ABSTRACT FROM AUTHOR]

One new clerodane-type furanoditerpenoid tinosinoid A (1) and nine new nor-clerodane analogs tinosinoids B–J (2−10) have been isolated from the stems of Tinospora sinensis. The structures of the new compounds with absolute configurations have been elucidated by spectroscopic means, including MS, NMR and ECD techniques, as well as chemical correlation. Compound 1 is a rare sulfur-containing clerodane diterpenoid incorporating a 2-mercaptoethanol unit via a thioether bond, while compounds 4/5 and 9 represent two pairs of unusual equilibrium regioisomers through an interesting intramolecular transesterification. Our bioassays established that 1 and 8 displayed moderate antiproliferative effects against two human tumor cell lines, and 9 and 10 showed significant α-glucosidase inhibitory activities. A kinetics study revealed that compound 10 was a noncompetitive α-glucosidase inhibitor, and its possible binding mode to the enzyme was further probed by molecular docking experiments. [ABSTRACT FROM AUTHOR]

Peritoneal metastases from invasive lobular carcinoma (ILC) of breast are uncommon and usually related to poor prognosis due to difficulty of detection in clinical practice and drug resistance. Therefore, recognizing the entities of peritoneal metastases of ILC and the potential mechanism of drug resistance is of great significance for early detection and providing accurate management. We herein report a case of a 60-year-old female who presented with nausea and vomiting as the first manifestation after treated with abemaciclib (a CDK4/6 inhibitor) plus fulvestrant for 23 months due to bone metastasis of ILC. Exploratory laparotomy found multiple nodules in the peritoneum and omentum, and immunohistochemistry confirmed that the peritoneal metastatic lesions were consistent with ILC. Palliative therapy was initiated, but the patient died two months later due to disease progression with malignant ascites. Whole exome sequencing (WES) was used to detect the tumor samples and showed the peritoneal metastatic lesions had acquired ESR1 and PI3KCA mutations, potentially explaining the mechanism of endocrine therapy resistance. We argue that early diagnosis of peritoneal metastasis from breast cancer is crucial for prompt and adequate treatment and WES might be an effective supplementary technique for detection of potential gene mutations and providing accurate treatment for metastatic breast cancer patients. [ABSTRACT FROM AUTHOR]

Ten thiophene derivatives (1–10), including two previously undescribed ones (1 and 2), have been obtained and structurally characterized from the aerial parts of a traditional Chinese herb Eclipta prostrata. Six of them with one chiral center were identified to be scalemic mixtures, and the pure enantiomers of two isolates (1 and 3) were successfully separated via chemical derivatization and chiral HPLC, with the absolute configurations being established by analysis of optical rotations. All the thiophenes were subjected to a series of assays and compounds 9 and 10 exhibited mild antibacterial activity against Staphylococcus aureus. [ABSTRACT FROM AUTHOR]

The complete mitogenome sequence of Micromys erythrotis was determined using long PCR. The genome was 16,238 bp in length and contained 13 protein-coding genes, 2 ribosomal RNA genes, 22 transfer RNA genes, 1 origin of L strand replication and 1 control region. The overall base composition of the heavy strand is A (33.7%), C (24.8%), T (29.1%) and G (12.4%). The base compositions present clearly the A–T skew, which is most obviously in the control region and protein-coding genes. Mitochondrial genome analyses based on MP, ML, NJ and Bayesian analyses yielded identical phylogenetic trees. This study verifies the evolutionary status of Micromys erythrotis in Muridae at the molecular level. The mitochondrial genome would be a significant supplement for the Micromys erythrotis genetic background. [ABSTRACT FROM AUTHOR]

Background and aims: Male breast cancer is an uncommon disease. The benefit of adjuvant chemotherapy in the treatment of male breast cancer patients has not been determined. The aim of this study was to explore the value of adjuvant chemotherapy in men with stage I–III breast cancer, and we hypothesized that some male patients may safely skip adjuvant chemotherapy. Methods: Male breast cancer patients between 2010 and 2015 from the Surveillance Epidemiology and End Results database were included. Univariate and multivariate Cox analyses were used to analyse the factors associated with survival. The propensity score matching method was adopted to balance baseline characteristics. Kaplan–Meier curves were used to evaluate the impacts of adjuvant chemotherapy on survival. The primary endpoint was survival. Results: We enrolled 514 patients for this study, including 257 patients treated with chemotherapy and 257 patients without. There was a significant difference in overall survival (OS) but not in breast cancer-specific survival (BCSS) between the two groups (p < 0.001 for OS and p = 0.128 for BCSS, respectively). Compared with the non-chemotherapy group, the chemotherapy group had a higher 4-year OS rate (97.5% versus 95.2%, p < 0.001), while 4-year BCSS was similar (98% versus 98.8%, p = 0.128). The chemotherapy group had longer OS than the non-chemotherapy group among HR+, HER2–, tumour size >2 cm, lymph node-positive male breast cancer patients (p < 0.05). Regardless of tumour size, there were no differences in OS or BCSS between the chemotherapy and non-chemotherapy cohorts for lymph node-negative patients (OS: p > 0.05, BCSS: p > 0.05). Adjuvant chemotherapy showed no significant effects on both OS and BCSS in patients with stage I (OS: p = 0.100, BCSS: p = 0.858) and stage IIA breast cancer (OS: p > 0.05, BCSS: p > 0.05). Conclusion: For stage I and stage IIA patients, adjuvant chemotherapy could not improve OS and BCSS. Therefore, adjuvant chemotherapy might be skipped for stage I and stage IIA male breast cancer patients. [ABSTRACT FROM AUTHOR]

A magnetic and thermal design of high-temperature superconducting (HTS) quadrupole magnet for newly developed superconducting proton cyclotron was presented in this research. With superconducting technology, the design can reduce the magnet size and remove the heat loads more efficiently. Calculations are conducted with finite element method (FEM) to study the quadrupole magnet's magnetic and thermal properties. For the magnet cold-mass and cryostat system, the heat load is mainly generated by conduction and radiation. Multilayer thermal insulation and G10 supports are used to restrict them. The magnetic field distribution in the HTS coils is calculated to consider the critical current degradation of the YBCO tapes. The effects on the field gradient quality in relation to the pole tip profile and end chamfer are analyzed. The sixth multipole component in the integral field can be improved with end chamfer. Finally, a 20 T/m HTS quadrupole magnet with integral field uniformity less than 0.05% out to 75% of the inscribed radius is proposed. [ABSTRACT FROM AUTHOR]

The complete mitogenome sequence of Ochotona hyperborea was determined using long PCR. The genome was 17,063 bp in length and contained 13 protein-coding genes, two ribosomal RNA genes, 22 transfer RNA genes, one origin of L strand replication, and one control region. The overall base composition of the heavy strand is A (31.1%), C (28.7%), T (26.3%), and G (13.9%). The base compositions present clearly the A–T skew, which is most obvious in the control region and protein-coding genes. Mitochondrial genome analyses based on MP, ML, NJ, and Bayesian analyses yielded identical phylogenetic trees. This study verifies the evolutionary status of Ochotona hyperborea in Ochotonidae at the molecular level. The mitochondrial genome would be a significant supplement for the Ochotona hyperborea genetic background. The eight Ochotona species formed a monophyletic group with the high bootstrap value (100%) in all examinations. [ABSTRACT FROM AUTHOR]

Five selaginellin derivatives (1 and 3-6) including a new one, selaginellin T (1), and a new triarylbenzophenone analog, selagibenzophenone A (2), were isolated from the whole plants of Selaginella pulvinata. Their structures were determined by 1D- and 2D-NMR and HR-ESI-MS data. Selagibenzophenone A (2) is the first example of naturally occurring triarylbenzophenone. The results of the phosphodiesterase-4 (PDE4) inhibitory screening assays showed that compounds 1−6 exhibited potent activities with the IC50 values in the range of 1.04−9.35 μM. [ABSTRACT FROM AUTHOR]

Phytochemical investigation of Cephalotaxus sinensis has led to the isolation of a new bisabolane sesquiterpenoid (1), a new abietane diterpenoid (2), and 13 known compounds (3–15). Their structures were elucidated by extensive spectroscopic analysis (MS, UV, IR, and NMR). [ABSTRACT FROM AUTHOR]

The nun moth, Lymantria monacha L., is one of the most important defoliators of Eurasian coniferous forests. Outbreaks during 2011-2015 in the natural/planted larch, and larch-birch mixed forests of the Greater Khingan Range in Inner Mongolia, China, caused tremendous timber losses from severe defoliation and tree mortality. A series of trapping experiments were conducted in these outbreak areas to evaluate the efficacy of a synthetic species-specific pheromone lure based on the female pheromone blend of European nun moth populations. Our results clearly show that the nun moth in Inner Mongolia is highly and specifically attracted to this synthetic pheromone, with few gypsy moths ( Lymantria dispar) captured. Flight activity monitoring of L. monacha male moths using pheromone-baited Unitraps at 2 locations during the summer of 2015 indicated that the flight period started in mid-July, peaking in early August at both locations. Based on male moth captures, there was a strong diurnal rhythm of flight activity throughout the entire scotophase, peaking between 22:00 and 24:00. Unitraps and wing traps had significantly and surprisingly higher catches than the gypsy moth traps. Unitraps fastened to tree trunks 2 m above ground caught significantly more male moths than those at the ground level or at 5 m height. Male L. monacha moths can be attracted to pheromone-baited traps in open areas 150-200 m distant from the infested forest edge. Our data should allow improvement on the performance of pheromone-baited traps for monitoring or mass-trapping to combat outbreaks of this pest in northeastern China. [ABSTRACT FROM AUTHOR]

Five new cassane diterpenoids, caesalmins I-M ( 1- 5), and 23 known analogs were isolated from the seeds of Caesalpinia minax. Their structures were elucidated by spectroscopic methods and comparison with reported data. The antioxidant properties of 1- 28 were determined by the method of oxygen radical absorbance capacity of fluorescein (ORAC-FL), and 14 compounds exhibited good antioxidant activities with ORAC-FL values of 2.24-4.89 Trolox equivalents. The structureactivity relationship of the active compounds was also discussed. [ABSTRACT FROM AUTHOR]

There has been little research conducted regarding autophagy in oral squamous cell carcinoma ( OSCC). Given the prevalence of oral cancers which are OSCC and the severe side effects of current treatments, there is a pressing need to develop effective alternative therapies. In this study, we have endeavored to explore the biological characteristics of oral squamous cell carcinoma cell line KB cells, in particular with regard to the role played by autophagy in their survival. Autophagy was activated by nutrient depletion via culturing cells in Earle's balanced salts ( EBSS) and was measured via indices relating to Beclin 1, microtubule-associated protein light chain 3 ( MAPLC3, LC3), p62, and Green fluorescent protein-light chain 3 plasmid transfection ( GFP- LC3). Cell death and apoptosis induced by nutrient depletion was measured using both MTT assay and flow cytometry ( FCM). Compared to initial levels at 0 h, Beclin 1 density in EBSS-treated cells was found to have increased at 6, 12, and 18 h in a time-dependent manner and was found to have subsequently declined at 24 and 48 h. p62 levels, LC3- II/ LC3-I ratio, and GFP- LC3 levels increased at 6, 12, 18, 24, and 48 h in a time-dependent manner. 3-methyladenine (3- MA) was found to inhibit autophagy and the expression of Beclin 1 and significantly enhanced nutrient depletion-induced apoptosis and death. We concluded that nutrient depletion enhances OSCC cell autophagy in time-course patterns and that the inhibition of autophagy augments apoptosis in OSCC cells. We also deduced that Beclin 1 takes part in the development and progression of autophagy, potentially playing an important role in the crosstalk between apoptosis and autophagy in OSCC cells. These findings suggest that nutrient depletion may be an effective way to explore autophagy and that autophagy inhibitors should be investigated as a potential novel agent for the adjuvant treatment of human OSCC. [ABSTRACT FROM AUTHOR]

ABSTRACT Two pairs of new neolignan enantiomers, (±)-torreyayunan A ( 1a/ 1b) and (±)-torreyayunan B ( 2a/ 2b), featuring a rare C-8 − C-9′ linked skeleton, were isolated from leaves and twigs of Torreya yunnanensis. Their absolute configuration involving two chiral centers was determined by combined spectral and Density Functional Theory (DFT) calculation. This is the first report of the absolute configuration of this group of neolignans. Chirality 26:825-828, 2014. © 2014 Wiley Periodicals, Inc. [ABSTRACT FROM AUTHOR]