[Screening of small molecule inhibitors of IL-15Rα using molecular docking and surface plasmon resonance technology].

The study aims to explore the active molecules of traditional Chinese medicine that specifically bind to interleukin-15 receptor α (IL-15Rα) using molecular docking and surface plasmon resonance (SPR) technology. AutoDock molecular docking software was used to perform simulated docking of more than 3 000 compounds from 48 traditional Chinese medicines at IL-15Rα and screen the specific binding compounds. Then Biocore T200 biomolecular interaction analysis system of SPR was used to confirm the binding specificity of the selected target compounds. Finally, the biological effects of the target compounds on IL-15Rα were verified by cell biological experiments. The results showed that neoprzewaquinone A (Neo) possessed the highest specific binding affinity among the active molecules from traditional Chinese medicine, and the dissociation constant (KD) value was (0.62 ± 0.20) µmol/L. The results of cell experiment showed that Neo significantly inhibited the proliferation of Mo7e cells induced by IL-15, and the IC50 was 1.075 µmol/L, approximately 1/120 of the IC50 of Cefazolin (IL-15 specific antagonist). These results suggest that Neo is a specific inhibitor of IL-15Rα and may be a potential active drug for the treatment of diseases related to the dysfunction of the IL-15Rα signaling.

Effects of instantaneous changes in temperature, light, and salinity on the dynamics of dissolved organic carbon release by Sargassum thunbergii.

Although macroalgae are regarded as the emerging fourth category of "blue carbon", few studies are available on the dynamics of dissolved organic carbon (DOC) release. Sargassum thunbergii is a typical intertidal macroalgae; and tidal action usually triggers instantaneous changes in temperature, light and salinity. Therefore, we investigated the mechanism of short-term changes in temperature, light and salinity on DOC release by S. thunbergii. As well as these factors coupled with desiccation, the combined effect of DOC release was revealed. The results showed the DOC release rate of S. thunbergii was from 0.028 to 0.037 mg C g -1(FW) h-1 under different photosynthetically active radiation (PAR, 0-1500 µmol photons m-2 s-1). The DOC release rate of S. thunbergii was from 0.008 to 0.208 mg C g -1(FW) h-1 under different salinity (5-40). The DOC release rate of S. thunbergii was from 0.031 to 0.034 mg C g -1(FW) h-1 under different temperature (10-30 °C). Either the increase in intracellular organic matter concentration due to increased photosynthesis (change in PAR and temperature, active), cell dehydration due to dry-out process (passive) or the decrease in extracellular salt concentration (passive) would lead to an increase in the difference in osmotic pressure and promote DOC release.

The use of biochemical indexes in hair for clinical studies of psychiatric diseases: What can we learn about mental disease from hair?

Analysis of hair samples provides unique advantages, including non-invasive sampling, sample stability, and the possibility of additional optimization of high sensitivity detection methods. Hair sample analysis is often used in psychiatric disease research to evaluate previous periods of stress encountered by patients. Glucocorticoid analysis is the most frequently tested indicator of stress. Furthermore, the hypothalamus-pituitary-gonad axis and endocannabinoid system also are involved in the occurrence and development of mental disorders. The endocannabinoid and sex hormone levels in patients experiencing mental illness are considerably different from levels observed in healthy individuals. Nevertheless, due to the different methods used to assess the degree of disease and the range of analytical methods involved in clinical research, the trends in changes for these biomarkers are not uniform. The correlations between changes in biomarker concentrations and illness severity also are not clear. The observed alterations suggest these biochemical substances in hair have potential as biomarkers for diagnosis or predictive treatment. However, the variable results obtained thus far could hamper further development of hair samples for clinical assessment in psychiatric disorders. This article summarizes the published reports documenting the changes in the content of relevant substances in hair in individuals experiencing mental illness and the degree of correlation. In the discussion section, we proposed several issues that should be considered in future studies of hair samples obtained from patients with mental disorders to promote the use of hair sample assessment as an aid in diagnosis or predictive treatment.

Insulators' Identification and Missing Defect Detection in Aerial Images Based on Cascaded YOLO Models.

Insulators identification and their missing defect detection are of paramount importance for the intelligent inspection of high-voltage transmission lines. As the backgrounds are complex, some insulators may be occluded, and the missing defect of the insulator is so small that it is not easily detected from aerial images with different backgrounds. To address the above issues, in this study, a cascaded You Only Look Once (YOLO) models are mainly explored to perform insulators and their defect detection in aerial images. Firstly, the datasets used for insulators location and missing defect detection are created. Secondly, a new model is proposed to locate the position of insulators, which is improved in the feature extraction network and multisacle prediction network based on previous YOLOv3-dense model. An improved YOLOv4-tiny model is used to conduct missing defect detection on the detected insulators. And then, the proposed YOLO models are trained and tested on the built datasets, respectively. Finally, the final models are cascaded for insulators identification and their missing defect detection. The average precision of missing defect detection can reach 98.4%, which is 5.2% higher than that of faster RCNN and 10.2% higher than that of SSD. The running time of the cascaded YOLO models for missing defect detection can reach 106 frames per second. Extensive experiments demonstrate that the proposed deep learning models achieve good performance in insulator identification and its missing defect detection from the inspection of high-voltage transmission lines.

Ultrasound guided microwave ablation of thyroid nodular goiter and cystadenoma: A single center, large cohort study.

ABSTRACT: Thyroid nodules are one of the most common entities that affect the thyroid gland. Traditionally, their treatment was surgery. Currently, ablation combination with percutaneous procedure became a good option.To analyze safety, efficacy, and describe our experience in microwave-ablation using ultrasound-guidance for benign thyroid nodules.A total of 304 patients with 1180 thyroid nodules (thyroid cystadenoma and nodular goiter) were studied retrospectively. Two hundred sixty-seven patients who underwent microwave-ablation successfully in our hospital were enrolled in this study. The baseline, follow-up nodule volume, thyroid function tests, thyroid antibodies, and posttherapy complications were analyzed. The informed written consent was obtained from patients or guardians. The study was approved by the ethics committee of our hospital.The average age was 50.1 ±â€Š11.7 (21-83 years), 214 were women (80.1%) and 53 (19.9%) were men. The average number of nodules per patient was 4.02 ±â€Š1.8 (1-8), 9.86%, 6.13%, and 84% located in the right thyroid lobe, left lobe, and bilateral, respectively. The average size of the nodules was 5.28 cm2 ±â€Š3.63 (0.09-23.45 cm2). The average ablation time was 11 minutes ±â€Š5.36 (3-20 minutes). The hospitalization period was 24 hours ±â€Š10.16 (7-48 hours). Eighteen complications were reported. Postablation volume reduction rate was 54.74% and 93.3% at 3 and 12 months follow-up respectively (P < .05). The thyroid function tests, pre and postablation showed no significant changes (P > .05).Ultrasound-guided microwave-ablation of thyroid nodules is safe and effective. More clinical trials are needed to define the true use of microwave-ablation.

Higher Serum C-Reactive Protein Levels in Catatonic Patients: A Comparison to Non-catatonic Patients and Healthy Controls.

Catatonia is a psychomotor syndrome defined by a constellation of predominantly motor symptoms. The aim of the present study was to determine whether recently admitted psychiatric patients with catatonia exhibited higher serum C-reactive protein (hs-CRP) levels compared to non-catatonic psychiatric patients and healthy controls (HCs). Recently admitted psychiatric patients were screened and evaluated for the catatonia syndrome using the Bush-Francis Catatonia Rating Scale and the Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition (DSM-5). The study sample was formed by 150 individuals (39 male and 111 female), including 51 catatonic patients, 55 non-catatonic patients, and 44 HCs. Serum hs-CRP levels were processed with the enzyme-linked immunosorbent assay. Serum levels of creatine kinase (CK), adrenocorticotropic hormone (ACTH), immunoglobulin G (IgG), complement component 3 (C3), and complement component 4 (C4) were also determined. There was a significantly higher percentage of patients with high inflammatory levels (hs-CRP > 3000ng/ml) in the catatonic (43.1%) than in the non-catatonic (14.5%) or HCs group (9.1%) (χ 2 =18.9, P < .001). Logistic regression showed that catatonic patients had significantly higher hs-CRP levels compared to non-catatonic patients even after controlling for other clinical and laboratory variables (OR = 3.52, P = .015, 95% CI 1.28-9.79). Multiple linear regression analysis revealed that log-transformed hs-CRP was independently predicted by body mass index and log-transformed C4, ACTH, and Cortisol in catatonic patients. Findings of the present study suggest that catatonia is specifically linked to a higher level of systemic inflammation, not merely attributable to the overall psychopathology, or alterations in the stress level and complement system.

1,1'-Binaphthyl Consisting of Two Donor-π-Acceptor Subunits: A General Skeleton for Temperature-Dependent Dual Fluorescence.

Temperature-dependent dual fluorescence with the anti-Kasha's rule is of great interest, but is a very challenging property to achieve in small organic molecules. The highly sensitive temperature-dependent dual fluorescence of 2,2'-bis(dimethylamino)-6,6'-bis(dimesitylboryl)-1,1'-binaphthyl (BNMe2 -BNaph), which essentially consists of two donor-π-acceptor (D-π-A) subunits, inspired the exploration of the importance of its structural features and the general utility of this molecular design. The reference compound MBNMe2 -BNaph, which lacks one electron-accepting Mes2 B, is found to show less sensitive temperature-dependent dual fluorescence, suggesting that the structure of BNMe2 -Bnaph, consisting of two symmetrical D-π-A subunits, is very important for achieving highly sensitive temperature-dependent dual fluorescence. In addition, it is found that another two 1,1'-binaphthyls, CHONMe2 -BNaph and CNNMe2 -BNaph, which also consist of two D-π-A subunits with Mes2 B groups replaced by CHO and CN, respectively, also show temperature-dependent dual fluorescence, with the fluorescence changing in a similar manner to BNMe2 -BNaph, indicating the general utility of the current molecular design for temperature-dependent dual fluorescence. Furthermore, the temperature-dependent dual fluorescence behaviors, such as the relative intensities of the two emission bands, the separation of the two emissions bands, and the sensitivity of the fluorescence intensity ratio to temperature, are greatly influence by the electron acceptors.

2,2'-Diamino-6,6'-diboryl-1,1'-binaphthyl: A Versatile Building Block for Temperature-Dependent Dual Fluorescence and Switchable Circularly Polarized Luminescence.

Temperature-dependent dual fluorescence and switchable circularly polarized luminescence (CPL) are two highly pursued but challenging properties for small organic molecules (SOMs). We herein disclose a triarylborane π-system based on a 2,2'-diamino-6,6'-diboryl-1,1'-binaphthyl scaffold that can serve as a versatile building block for achieving these two properties by simply choosing different amino groups. BNMe2 -BNaph with less bulky dimethylamino groups displays temperature-dependent dual fluorescence, and can thus be used as a highly sensitive ratiometric fluorescence thermometer. On the other hand, BNPh2 -BNaph with bulky diphenylamino groups exhibits intense fluorescence in both solution and in the solid state. A change of solvent from nonpolar cyclohexane to highly polar MeCN not only shifts the CPL position to much longer wavelength but also inverts the CPL sign. In addition, the complexation of BNPh2 -BNaph with fluoride greatly enhances the CPL intensity.

Shuxuetong injection protects cerebral microvascular endothelial cells against oxygen-glucose deprivation reperfusion.

Shuxuetong injection composed of leech (Hirudo nipponica Whitman) and earthworm (Pheretima aspergillum) has been used for the clinical treatment of acute stroke for many years in China. However, the precise neuroprotective mechanism of Shuxuetong injection remains poorly understood. Here, cerebral microvascular endothelial cells (bEnd.3) were incubated in glucose-free Dulbecco's modified Eagle's medium containing 95% N2/5% CO2 for 6 hours, followed by high-glucose medium containing 95% O2 and 5% CO2 for 18 hours to establish an oxygen-glucose deprivation/reperfusion model. This in vitro cell model was administered Shuxuetong injection at 1/32, 1/64, and 1/128 concentrations (diluted 32-, 64-, and 128-times). Cell Counting Kit-8 assay was used to evaluate cell viability. A fluorescence method was used to measure lactate dehydrogenase, and a fluorescence microplate reader used to detect intracellular reactive oxygen species. A fluorescent probe was also used to measure mitochondrial superoxide production. A cell resistance meter was used to measure transepithelial resistance and examine integrity of monolayer cells. The fluorescein isothiocyanate-dextran test was performed to examine blood-brain barrier permeability. Real-time reverse transcription polymerase chain reaction was performed to analyze mRNA expression levels of tumor necrosis factor alpha, interleukin-1ß, interleukin-6, and inducible nitric oxide synthase. Western blot assay was performed to analyze expression of caspase-3, intercellular adhesion molecule 1, vascular cell adhesion molecule 1, occludin, vascular endothelial growth factor, cleaved caspase-3, B-cell lymphoma 2, phosphorylated extracellular signal-regulated protein kinase, extracellular signal-regulated protein kinase, nuclear factor-κB p65, I kappa B alpha, phosphorylated I kappa B alpha, I kappa B kinase, phosphorylated I kappa B kinase, claudin-5, and zonula occludens-1. Our results show that Shuxuetong injection increases bEnd.3 cell viability and B-cell lymphoma 2 expression, reduces cleaved caspase-3 expression, inhibits production of reactive oxygen species and mitochondrial superoxide, suppresses expression of tumor necrosis factor alpha, interleukin-1ß, interleukin-6, inducible nitric oxide synthase mRNA, intercellular adhesion molecule-1, and vascular cell adhesion molecule-1, markedly increases transepithelial resistance, decreases blood-brain barrier permeability, upregulates claudin-5, occludin, and zonula occludens-1 expression, reduces nuclear factor-κB p65 and vascular endothelial growth factor expression, and reduces I kappa B alpha, extracellular signal-regulated protein kinase 1/2, and I kappa B kinase phosphorylation levels. Overall, these findings suggest that Shuxuetong injection has protective effects on brain microvascular endothelial cells after oxygen-glucose deprivation/reperfusion. Moreover, its protective effect is associated with reduction of mitochondrial superoxide production, inhibition of the inflammatory response, and inhibition of vascular endothelial growth factor, extracellular signal-regulated protein kinase 1/2, and the nuclear factor-κB p65 signaling pathway.

Impact of the 2,2'-Bithienyl Framework on the Charge-Transfer Emission of Triarylborane-Based o,o'-Substituted Biaryls.

Two new triarylborane-based o,o'-substituted 2,2'-bithienyls, BT-BNMe 2 and BT-BNBn 2 , which contain BMes2 and NMe2/NBn2 groups at the 3,3'-positions, have been synthesized. Similar to the o,o'-substituted biphenyl analogues, BP-BNMe 2 and BP-BNBn 2 , which contain BMes2 and NMe2/NBn2 groups at the 2,2'-positions, the steric effect of the amino group has significant influence on the conformation of the 2,2'-bithienyl skeleton. The boryl and amino groups are located at the same side of 2,2'-bithienyls axis with a short B···N distance (3.63 Å) for the NMe2-substituted BT-BNMe 2 . On the contrary, the two substituents are arranged on the two different sides of the 2,2'-bithienyls axis for BT-BNBn 2 , which is modified with bulky NBn2. Despite the remarkable differences in the steric structure, the two 2,2'-bithienyls display fluorescence at close wavelengths, which is in sharp contrast to the much red-shifted fluorescence of BP-BNMe 2 than BP-BNBn 2 . The theoretical calculations demonstrated that the two 2,2'-bithienyls have close highest occupied molecular orbital-lowest unoccupied molecular orbital gaps in the excited state, which firmly support the experimental results. Thus, the parent main chain framework can exhibit great impact on the charge-transfer emission of o,o'-substituted biaryls.

Expression of annexin A5 in serum and tumor tissue of patients with colon cancer and its clinical significance.

AIM: To investigate the expression of annexin A5 in serum and tumor tissue of patients with colon cancer and to analyze its clinical significance. METHODS: Ninety-three patients with colon cancer treated at our hospital between February 2013 and March 2016 were included in an observation group, and 40 healthy individuals were included in a control group. Enzyme-linked immunosorbent assay was performed to determine the serum level of annexin A5, while immunohistochemistry was performed to determine the expression of annexin A5 in cancer tissues. RESULTS: The serum level of annexin A5 was 0.184 ± 0.043 ng/mL in the observation group, which was significantly higher than that in the control group (P < 0.05). Annexin A5 expression was detected in 79.31% of the patients with lymph node metastasis, which was significantly higher than that in patients without lymph node metastasis (P < 0.05). Moreover, annexin A5 expression was detected in 86.96% of the patients with stage III to IV disease, which was significantly higher than that in patients with stage I to II disease (P < 0.05). The serum level of annexin A5 was 0.215 ± 0.044 ng/mL in patients whose tumors were positive for annexin A5 expression, which was significantly higher than that in patients whose tumors were negative for annexin A5 expression (P < 0.05). The serum level of annexin A5 was correlated with annexin A5 expression in colon cancer tissues (r = 0.312, P < 0.05). When a cutoff value of > 0.148 ng/mL for serum level of annexin A5 was used in the diagnosis of colon cancer, the sensitivity was 83.90%, and the specificity was 57.50%. CONCLUSION: For patients with colon cancer, annexin A5 expression in cancer tissues is related to lymph node metastasis and tumor grade. Serum level of annexin A5 is related to annexin A5 expression in cancer tissues and is of diagnostic relevance.

Molecular cloning, characterization and expression analysis of (B-cell lymphoma-2) Bcl-2 in the orange-spotted grouper (Epinephelus coioides).

Bcl-2 is a pro-survival member of Bcl-2 like superfamily, playing an important role in regulating the apoptotic process. In this study, the full-length Bcl-2 (EcBcl-2) was obtained, consisting of a 5'UTR of 290 bp, an ORF of 699 bp and a 3'UTR of 920 bp. EcBcl-2 gene encoded a polypeptide of 232 amino acids with an estimated molecular mass of 26.12 KDa and a predicted isoelectric point (pI) of 6.93. The deduced amino acid sequence analysis showed that EcBcl-2 consisted of the conserved residues and characteristic domains known to the critical functionality for Bcl-2. qRT-PCR analysis revealed that EcBcl-2 transcript was expressed in all the examined tissues, while the strongest expression level was observed in liver, followed by the expression in blood, gill, kidney, spleen, heart, intestine and muscle. The groupers challenged with V. alginolyticus showed a significant increase of EcBcl-2 mRNA in immune tissues. In addition, western blotting analysis confirmed that the up-regulation of EcBcl-2 protein expression was detected in liver. Subcellular localization analysis revealed that EcBcl-2 was localized in both nucleus and cytoplasm. Overexpression of EcBcl-2 can inhibit the LPS-induced apoptosis and activate the transcription activity of NF-κB and AP-1, while the deletion of BH1, BH2, BH3 or BH4 domain from EcBcl-2 can impede the signaling transduction. These results indicate that EcBcl-2 may play a regulatory role in the apoptotic process.

Assessment of Crohn's disease activity by Doppler sonography.

OBJECTIVES: To investigate the diagnostic accuracy of ultrasound for evaluation of inflammatory activity in patients with Crohn's disease (CD). Methods: Fifty-six patients with histologically proven CD (39 with active, 17 with inactive disease) and 30 healthy volunteers as a control group were enrolled in the study at WeiFang People's Hospital, Weifang Province, China from October 2012 to December 2014. Bowel wall thickness, and vascularity pattern were measured by Doppler ultrasound. Results: There was a significant difference in flow volume of the superior mesenteric artery (585 ± 235 ml/min) in the patients with active disease, compared with those with inactive disease (401 ± 238 ml/min) and the control group (390 ± 189 ml/min, p less than 0.001). Wall thickness was 5.1 ± 1.5 mm in the active CD group, 3.3 ± 1.6 mm in the inactive disease group (p less than 0.001) and  less than 3 mm in the control group. Resistance index in the thickened bowel wall showed some differences: 0.68 ± 0.05 in the active disease group, 0.78 ± 0.08 in the inactive disease group, and 0.85 ± 0.07 in the control group (p less than 0.05). Conclusion: Doppler ultrasound is a useful diagnostic tool in detecting CD and assessing inflammatory activity.

The effects of Chinese medicines on cAMP/PKA signaling in central nervous system dysfunction.

Neuropathological injury in the mammalian adult central nervous system (CNS) may cause axon disruption, neuronal death and lasting neurological deficits. Failure of axon regeneration is one of the major challenges for CNS functional recovery. Recently, the cAMP/PKA signaling pathway has been proven to be a critical regulator for neuronal regeneration, neuroplasticity, learning and memory. Also, previous studies have shown the effects of Chinese medicines on the prevention and treatment of CNS dysfunction mediated in part by cAMP/PKA signaling. In this review, the authors discuss current knowledge of the role of cAMP/PKA signaling pathway in neuronal regeneration and provide an overview of the Chinese medicines that may enable CNS functional recovery via this signaling pathway.

A triarylborane-based biphenyl exhibiting abrupt fluorescence enhancement at a specific high temperature.

A triarylborane-based biphenyl, 4,4'-dibromo-2-dimesitylboryl-2'-(N,N-dimethylamino)biphenyl (Br2-BN-BPh), exhibits very unique temperature-dependent fluorescence behavior. Although Br2-BN-BPh is weakly emissive at room temperature, its fluorescence increases abruptly at a specific high temperature (68 °C in MOE, 88 °C in toluene). In addition, the fluorescence still remains very strong even after cooling to room temperature, providing the possibility of the fluorescence detection of a specific high temperature.

Charge-Transfer Emitting Triarylborane π-Electron Systems.

Triarylboranes have attracted significantly increasing research interest as a remarkable class of photoelectronic π-electron materials. Because of the presence of vacant p orbital on the B center, the boryl group is a very unique electron acceptor that exhibits not only electron-accepting ability through p-π* conjugation but also high Lewis acidity to coordinate with Lewis bases and steric bulk arising from the aryl substituent on the B center to get enough kinetic stability. Thus, the incorporation of a trivalent B element into π-conjugated systems is an efficient strategy to tune the electronic and stereo structures and thus the photoelectronic properties of π-electron systems. When an electron-donating group, such as amino, is present, triarylboranes would likely display intramolecular charge-transfer transitions. These kinds of molecules are often highly emissive. In addition, the geometry of the molecules has a great impact on the emission properties. In this Forum Article, we herein describe our recent progress on the charge-transfer emitting triarylborane π-electron systems with novel geometries, which include the lateral boryl-substituted π-system with amino groups at the terminal positions, the o,o'-substituted biaryl π-system with boryl and amino groups at the o,o'-positions, a triarylborane-based BODIPY system, and a B,N/S-bridged ladder-type π-system. We mainly put the emphasis on the molecular design concept, structure-property relationships, intriguing emission properties and great applications of the corresponding triarylborane π-systems.

The Role of Group II Metabotropic Glutamate Receptors in the Striatum in Electroacupuncture Treatment of Parkinsonian Rats.

AIMS: Glutamatergic transmission may play a critical role in the pathogenesis of Parkinson's disease (PD). Electroacupuncture (EA) has been demonstrated to effectively alleviate PD symptoms. In this study, a potential glutamate-dependent mechanism underlying the therapeutic action of EA was investigated. METHODS: The effects of EA stimulation on motor behaviors, dopamine contents, glutamate release, and group II metabotropic glutamate receptor (mGluR2/3) expression in unilateral 6-hydroxydopamine (6-OHDA)-lesioned rats were examined. RESULTS: Unilateral 6-OHDA lesions of the nigrostriatal system caused a marked increase in glutamate content in the ipsilateral cortex and striatum. mGluR2/3 protein expression and mGluR3 mRNA expression were reduced in the striatum. Noticeably, prolonged EA stimulation at 100 Hz significantly reversed these changes in the striatal glutamate system. Behaviorally, EA improved the motor deficits induced by 6-OHDA lesions. Intrastriatal infusion of an mGluR2/3 antagonist APICA blocked the improving effect of EA. CONCLUSIONS: These data collectively demonstrate that the group II mGluR-mediated glutamatergic transmission in the striatum is sensitive to dopamine depletion and may serve as a substrate of EA for mediating the therapeutic effect of EA in a rat model of PD.

Molecular cloning and characterization of PTEN in the orange-spotted grouper (Epinephelus coioides).

PTEN is a key tumor suppressor gene that can play a regulatory role in the cellular proliferation, survival and apoptosis. In this study, the full-length PTEN (EcPTEN) was obtained, containing a 5'UTR of 745 bp, an ORF of 1269 bp and a 3'UTR of 106 bp. The EcPTEN gene encoded a polypeptide of 422 amino acids with an estimated molecular mass of 49.14 KDa and a predicted isoelectric point (pI) of 6.34. The deduced amino acid sequence analysis showed that EcPTEN comprised the conserved residues and the characteristic domains known to the critical functionality of PTEN. qRT-PCR analysis revealed that EcPTEN mRNA was broadly expressed in all the examined tissues, while the highest expression level was observed in liver, followed by the expression in blood, kidney, spleen, heart, gill, muscle and intestine. The groupers challenged with Vibrio alginolyticus showed a sharp increase of EcPTEN mRNA expression in immune tissues. In addition, western blotting analysis confirmed that the up-regulation of EcPTEN protein expression was steadily induced in liver. Subcellular localization analysis indicated that EcPTEN was localized in both nucleus and cytoplasm. Overexpression of EcPTEN can activate the apoptotic cascade and abrogate NF-kB, AP-1, Stat3 and Myc promoter activity in Hela cells. These results indicated that EcPTEN harboring highly-conserved domains with a close sequence similarity to those of PTP superfamily may disrupt the mammalian signalings and play a regulatory role in the apoptotic process.

Chirality Relay in 2,2'-Substituted 1,1'-Binaphthyl: Access to Propeller Chirality of the Tricoordinate Boron Center.

It is a challenging issue to achieve propeller chirality for triarylboranes owing to the low transition barrier between the P and M forms of the boron center. Herein, we report a new strategy to achieve propeller chirality of triarylboranes. It was found that the chirality relay from axially chiral 1,1'-binaphthyl to propeller chirality of the trivalent boron center can be realized when a Me2 N and a Mes2 B group (Mes=mesityl) are introduced at the 2,2'-positions of the 1,1'-binaphthyl skeleton (BN-BNaph) owing to the strong π-π interaction between the Me2 N-bonded naphthyl ring and the phenyl ring of one adjacent Mes group, which not only exerts great steric hindrance on the rotation of the two Mes groups but also gives unequal stability to the two configurations of the boron center for a given configuration of the binaphthyl moiety. The stereostructures of the boron center were fully characterized through 1 H NMR spectroscopy, X-ray crystal analyses, and theoretical calculations. Detailed comparisons with the analog BN-Ph-BNaph, in which the Mes2 B group is separated from 1,1'-binaphthyl by a para-phenylene spacer, confirmed the essential role of π-π interaction for the successful chirality relay in BN-BNaph.