3-Phenyl-2-(piperidin-1-yl)-3,5,6,8-tetra­hydro-4H-thio­pyrano[3′,4′:2,3]thieno[5,4-d]pyrimidin-4-one

In the title compound, C20H21N3OS2, the piperidinyl ring has a distorted chair conformation. Weak inter­molecular C—H⋯O hydrogen bonds link the mol­ecules into centrosymmetric dimers. The crystal packing exhibits short inter­molecular S⋯S distances of 3.590 (2) Å

Comparison of endostatin(endostar)and avastin's inhibition effect on mice choroidal neovascularization

AIM:To observe the inhibition effect of endostatin(endostar)on mice choroidal neovascularization model(CNV)and compare with the Avastin.<p>METHODS: Using 532nm laser photocoagulation to establish a mouse model of CNV. We observed the formation of CNV by histopathological examination after 2wk later. Forty successful models of mice were randomly divided into control group(group 1, 10 rats), normal saline group(group 2, 10 rats), endostatin group(group 3, 10 rats)and avastin group(group 4, 10 rats). The drugs were injected into the mice' vitreous after photocoagulation 2wk later. Then 1wk later, we took the mice eyeballs to perform the HE and immunohistochemical staining to observe. The statistical analysis of ANOVA was done by SPSS 16.0 and the LSD-<i>t</i> test was used for multiple samples, taking <i>P</i><0.05 as the test standards.<p>RESULTS: Two weeks later, HE histopathological examination was done, light microscope showed large amount of new vessels' formation, the positive rate for CNV was 72.8%. The blank control group compared with the normal saline group <i>P</i>>0.05, had no inhibitory effect on CNV; endostatin treated group compared with control group, <i>P</i><0.05, had a certain inhibitory effect; avastin group compared with the control group, <i>P</i><0.05, had an inhibitory effect on CNV; the LSD-<i>t</i> was performed on Avastin group and endostatin group, <i>P</i><0.05, which were statistically significant. We thought that the two drugs have different inhibitory effect on mice' CNV, because <i>(-overx)</i>_Avastin=26.90,<i>(-overx)</i>_endostatin=29.13,<i>(-overx)</i>_Avastin<<i>(-overx)</i>_endostatin, we can infer that endostar had lower inhibitory effect on mice CNV than Avastin.<p>CONCLUSION: Laser-induced CNV animal models of colored mice C57BL/6J is of short time and high rate establishment and it is an ideal model for CNV study. Endostar has certain inhibitory effect on CNV, and it is likely to become one of the important drugs for CNV-related diseases in the future

Population Genetic Structure of Monimopetalum chinense (Celastraceae), an Endangered Endemic Species of Eastern China

• Background and Aims Monimopetalum chinense (Celastraceae) standing for the monotypic genus is endemic to eastern China. Its conservation status is vulnerable as most populations are small and isolated. Monimopetalum chinense is capable of reproducing both sexually and asexually. The aim of this study was to understand the genetic structure of M. chinense and to suggest conservation strategies. • Methods One hundred and ninety individuals from ten populations sampled from the entire distribution area of M. chinense were investigated by using inter-simple sequence repeats (ISSR). • Key Results A total of 110 different ISSR bands were generated using ten primers. Low levels of genetic variation were revealed both at the species level (Isp = 0·183) and at the population level (Ipop = 0·083). High clonal diversity (D = 0·997) was found, and strong genetic differentiation among populations was detected (49·06 %). • Conclusions Small population size, possible inbreeding, limited gene flow due to short distances of seed dispersal, fragmentation of the once continuous range and subsequent genetic drift, may have contributed to shaping the population genetic structure of the specie

Four new jacaranone analogs from the fruits of a Beibu Gulf mangrove Avicennia marina

Four new jacaranone analogs, marinoids F–I (1–4), were isolated from the fruits of a Beibu Gulf mangrove Avicennia marina. The structures were elucidated based on analysis of spectroscopic data. Marinoids F and G are shown to be diastereoisomers of chlorocornoside, a new halogen containing marine secondary metabolite. The antioxidant activity of the isolates was evaluated using a cellular antioxidant assay, and 4 showed good antioxidant activity (EC50 = 26 μM)

Ethyl 2-amino-6-benzyl-4,5,6,7-tetra­hydro­thieno[2,3-c]pyridine-3-carboxyl­ate

In the title compound, C17H20N2O2S, the tetra­hydro­pyridine ring adopts an envelope conformation with the N atom at the flap position; the phenyl ring makes a dihedral angle of 81.06 (10)° with the thio­phene ring. The amino group links with the carbonyl O atom via intra­molecular N—H⋯O hydrogen bonding, forming a six-membered ring. In the crystal, inter­molecular N—H⋯O hydrogen bonds link the mol­ecules into infinite chains running along the b axis

2,3:6,7-Bis(methyl­enedi­oxy)­phenanthrene

In the title mol­ecule, C16H10O4, all the non-H atoms are coplanar. The crystal structure is stabilized by weak inter­molecular C—H⋯O contacts and π–π stacking inter­actions (the inter­planar distance is 3.43 Å)

Loss of FKBP5 Affects Neuron Synaptic Plasticity: An Electrophysiology Insight

FKBP5 (FKBP51) is a glucocorticoid receptor (GR) binding protein, which acts as a co-chaperone of heat shock protein 90 (HSP90) and negatively regulates GR. Its association with mental disorders has been identified, but its function in disease development is largely unknown. Long-term potentiation (LTP) is a functional measurement of neuronal connection and communication, and is considered one of the major cellular mechanisms that underlies learning and memory, and is disrupted in many mental diseases. In this study, a reduction in LTP in Fkbp5 knockout (KO) mice was observed when compared to WT mice, which correlated with changes to the glutamatergic and GABAergic signaling pathways. The frequency of mEPSCs was decreased in KO hippocampus, indicating a decrease in excitatory synaptic activity. While no differences were found in levels of glutamate between KO and WT, a reduction was observed in the expression of excitatory glutamate receptors (NMDAR1, NMDAR2B and AMPAR), which initiate and maintain LTP. The expression of the inhibitory neurotransmitter GABA was found to be enhanced in Fkbp5 KO hippocampus. Further investigation suggested that increased expression of GAD65, but not GAD67, accounted for this increase. Additionally, a functional GABAergic alteration was observed in the form of increased mIPSC frequency in the KO hippocampus, indicating an increase in presynaptic GABA release. Our findings uncover a novel role for Fkbp5 in neuronal synaptic plasticity and highlight the value of Fkbp5 KO as a model for studying its role in neurological function and disease development