Development of novel liver X receptor modulators based on a 1,2,4-triazole scaffold

Liver?X?Receptor (LXR) agonists have been reported as a potential treatment for atherosclerosis, Alzheimer’s disease and hepatitis C virus (HCV) infection. We have designed and synthesized a series of potent compounds based on a 1,2,4-triazole scaffold as novel LXR modulators. In cell-based cotransfection assays these compounds generally functioned as LXR agonists and we observed compounds with selectivity towards LXRα (7-fold) and LXRβ (7-fold) in terms of potency. Assessment of the effects of selected compounds on LXR target gene expression in HepG2 cells revealed that compounds 6a-b and 8a-b behaved as inverse agonists on FASN expression even though they were agonists in the LXRα and LXRβ cotransfection assays. Interestingly, these compounds had no effect on the expression of SREBP-1c confirming a unique LXR modulator pharmacology. Molecular docking studies and evaluation of ADME properties in-silico show that active compounds possess favorable binding modes and ADME profiles. Thus, these compounds may be useful for in vivo characterization of LXR modulators with unique profiles and determination of their potential clinical utility.     

Karyotype Comparison of Populus SectTacamahaca

The paper identified and compared the karyotypes of 10 species(varieties) of Populus sectTacamhaca.The results were as follows:Ppseudo simonii Kitag.2n=38=27m+6sm(1SAT)+4st(2SAT)+1t(1SAT);Ptrichocarpa Torr.2n=38=2M+18m(1SAT)+8sm+10st(1SAT);Pcathayana Rehd.var.Beijing 2n=38=1M+24m+6sm+7st(2SAT);Pבpopularis’ 2n=38=3M+27m+2sm(1SAT)+4st(2SAT)+2t(1SAT);Pcathayana Rehd.var.Wutai 2n=38=5M+22m+4sm+5st+2t(2SAT);Pcathayana Rehd.var.Gansulinxiaman 2n=38=2M+28m+1sm+7st(1SAT);Pcathayana Rehd.var.Qinghai 2n=38=1M+27m+3sm+6st(3SAT)+1t(1SAT);Pcathayana×Zhongqing 10 2n=38=1M+26m+4sm+5st(2SAT)+2t(2SAT);Pcathayana×Zhongqing 48 2n=38=16m+10sm(1SAT)+10st(2SAT)+2t(1SAT).The results showed definite karyotype differences among the species of Tacamhaca.The karyotypes of most species(varieties) are made of m and sm and a few with st and t chromosomes.The karyotypes of Tacamhaca were all of 2B type of Stebbins.This study provided important basic data for taxon of Populus.     

胡杨(Populus euphratica Oliv)的耐盐性

文章对胡杨耐盐性的研究进展进行了介绍。     

Identification of assembly precursors to photosystems emitting fluorescence at 683 nm and 687 nm by cryogenic fluorescence microspectroscopy

Photosystem I (PSI) and photosystem II (PSII) play key roles in photoinduced electron-transfer reaction in oxygenic photosynthesis. Assemblies of these PSs can be initiated by illumination of the etiolated seedlings (greening). The study aimed to identify specific fluorescence spectral components relevant to PSI and PSII assembly intermediates emerging in greening seedlings of Zea mays, a typical C4 plant. The different PSII contents between the bundle sheath (BS) and mesophyll (M) cells were utilized to spectrally isolate the precursors to PSI and PSII. The greening Zea mays leaf thin sections were observed with the cryogenic microscope combined with a spectrometer. With the aid of the singular-value decomposition analysis, we could identify four independent fluorescent species, SAS677, SAS685, SAS683, and SAS687, named after their fluorescence peak wavelengths. SAS677 and SAS685 are the dominant components after the 30-minute greening, and the distributions of these components showed no clear differences between M and BS cells, indicating immature cell differentiation in this developing stage. On the other hand, the 1-hour greening resulted in reduced distributions of SAS683 in BS cells leading us to assign this species to PSII precursors. The 2-hour greening induced the enrichment of SAS687 in BS cells suggesting its PSI relevance. Similarity in the peak wavelengths of SAS683 and the reported reaction center of PSII implied their connection. SAS687 showed an intense sub-band at around 740 nm, which can be assigned to the emission from the red chlorophylls specific to the mature PSI.     

Plant Traditional Culture of Populus euphratica and Populus pruinosa of Uyghurs Folk ——A Case Study in Xinjiang Lopnur

The study on traditional knowledge and experience of using plants by Uyghurs folk people has a potential application in socio economic development and resource protection. Populus euphratica Oliv and Ppruinosa Schrenk are major plants in Taklimakan desert ecosystem of Xinjiang. This study aims to ascertain the Lopnur Uyghurs traditional knowledge on two Populus species and their cultural system related to these species. We investigated the key informants for interviews on using Populus plants. The Populus plants were used for various purposes. The white alkali crystals are using for the treatment of bloating, sore throat, stomach ulcers, duodenal ulcers and indigestion and also in soda, while black crystal is used for the treatment of back pain, leg pain, swelling and relieve pain. Alkali crystals are even used as shampoo after a simple processing and also as a laundry detergent. Populus plants water is applied as a treatment of neurasthenia. It is also used for anti aging, reducing blood pressure, high cholesterol and heart morbidity. Plants foliages are used as veterinary medicine such as bloating and rot of muscular and stomach of livestock. In addition, Lopnur people used the plants to build the Desert Ecological Park and controlling desertification. This article ascertained the two Populus speceis and Lopnur Uyghurs cultural system. Present study will improve the conservation of Lopnur Uyghurs folk indigenous/ traditional knowledge on Populus plants and to promote the sustainable development in the socio economic diversity.     

Fast scanning calorimetry of lysozyme unfolding at scanning rates from 5 K/min to 500,000 K/min

Background

Protein denaturation is often studied using differential scanning calorimetry (DSC). However, conventional instruments are limited in the temperature scanning rate available. Fast scanning calorimetry (FSC) provides an ability to study processes at much higher rates while using extremely small sample masses [ng]. This makes it a very interesting technique for protein investigation.

In vitro induction of tetraploid and resulting trait variation in Populus alba × Populus glandulosa clone 84 K

Plant Cell, Tissue and Organ Culture (PCTOC) - As a model plant, poplar 84 K (Populus alba?×?P. glandulosa) plays a key role in fundamental research in forest molecular...     

Permanent seed implant brachytherapy in low-risk prostate cancer: Preoperative planning with 145 Gy versus real-time intraoperative planning with 160 Gy

Aim

The present retrospective study was to compare toxicity and survival outcomes in a group of low-risk PCa patients treated with either the preoperative planning technique (145?Gy) or the real-time IoP technique (160?Gy).

毛白杨(Populus tomentosa)茎的解剖构造

一.前言杨属(Populus)是世界上分布很广的树木,目前已知约有40种,而我国有二十余种之多,分布于华北、东北、西南、华东、华中、以及新疆阿尔泰山一带,由于它适应性强,生长快,繁殖易,已被广泛地利用。杨树木材是纤维工业如人造丝的重要原料;在造纸工业方     

胡杨(Populus euphratica Oliv.)根繁殖特征

以新疆塔里木河中游河岸北部河漫滩的胡杨幼林带为对象,从克隆生态学的角度,采用挖掘法、高压冲洗法及断根胁迫实验,研究了胡杨在资源异质环境中的风险分担、资源觅食与保持功能以及根源性克隆生长形态特征。结果表明:胡杨的地下根分枝类型为单轴型,同一生长方向2水平根的夹角平均约为180°,水平根与垂直根的夹角为90°～100°,水平根和垂直根的空间构型近似T形;基株的胚根周长>分株的次根周长;水平根呈侧圆台形,胡杨的2水平根之间存在着养分的传递。     

杨属(Populus L.)种质资源遗传学评价研究进展

杨属(Populus L.)种质资源极其丰富, 为了有效保存、合理利用杨属种质资源, 国内外开展了大量的种质资源遗传学评价研究。该文在介绍杨树系统分类的基础上, 概述了白杨派、青杨派和黑杨派等在生物学特性、抗性(耐盐、抗旱、抗冻及抗病虫)、适应性及DNA遗传多态性等方面的遗传学评价研究进展, 重点讨论了杨树种质资源评价研究中存在的问题和不足, 并对其研究前景进行了展望。     

Plant regeneration from cell suspension-derived protoplasts of Populus × beijingensis

A protocol for plant regeneration from cell suspension-derived protoplasts of Populus × beijingensis is described. Protoplasts were isolated from cell suspension cultures 6 d after subculture and further cultured in liquid NH₄NO₃-free Murashige and Skoog (MS) medium supplemented with 0.6 M glucose, 9.05 μM 2,4-dichlorophenoxyacetic acid, and 0.89 μM 6-benzyladenine at a density of 2?×?10⁵ protoplasts per milliliter. The initial plating efficiency and final plating efficiency recorded after 10 and 30 d reached 33.7 and 1.07%, respectively. The proliferated calli transferred to regeneration medium supplemented with 2.22 μM 6-benzyladenine and 0.54 μM α-naphthaleneacetic acid gave the highest rate of shoot formation (44.4%). All protoplast-derived shoots were able to form roots on half-strength MS medium supplemented with 2.46 μM indole-3-butyric acid.     

A straightforward multiparametric quality control protocol for proton magnetic resonance spectroscopy: Validation and comparison of various 1.5 T and 3 T clinical scanner systems

PurposeThe aim of this study was to propose and validate across various clinical scanner systems a straightforward multiparametric quality assurance procedure for proton magnetic resonance spectroscopy (MRS).MethodsEighteen clinical 1.5 T and 3 T scanner systems for MRS, from 16 centres and 3 different manufacturers, were enrolled in the study. A standard spherical water phantom was employed by all centres. The acquisition protocol included 3 sets of single (isotropic) voxel (size 20 mm) PRESS acquisitions with unsuppressed water signal and acquisition voxel position at isocenter as well as off-center, repeated 4/5 times within approximately 2 months. Water peak linewidth (LW) and area under the water peak (AP) were estimated.ResultsLW values [mean (standard deviation)] were 1.4 (1.0) Hz and 0.8 (0.3) Hz for 3 T and 1.5 T scanners, respectively. The mean (standard deviation) (across all scanners) coefficient of variation of LW and AP for different spatial positions of acquisition voxel were 43% (20%) and 11% (11%), respectively. The mean (standard deviation) phantom T₂ values were 1145 (50) ms and 1010 (95) ms for 1.5 T and 3 T scanners, respectively. The mean (standard deviation) (across all scanners) coefficients of variation for repeated measurements of LW, AP and T₂ were 25% (20%), 10% (14%) and 5% (2%), respectively.ConclusionsWe proposed a straightforward multiparametric and not time consuming quality control protocol for MRS, which can be included in routine and periodic quality assurance procedures. The protocol has been validated and proven to be feasible in a multicentre comparison study of a fairly large number of clinical 1.5 T and 3 T scanner systems.     

Fluorine-18 (18F)-labeled retinoid x receptor (RXR) partial agonist whose tissue transferability is affected by other RXR ligands

Bexarotene (1), a retinoid X receptor (RXR) agonist approved for the treatment of cutaneous T cell lymphoma (CTCL), was reported to migrate into baboon brain based on findings obtained by positron emission tomography (PET) with a ¹¹C-labeled tracer. However, co-administration of non-radioactive 1 had no effect on the distribution of [¹¹C]1, probably due to non-specific binding of 1 as a result of its high lipophilicity. Here, we report a fluorine-18 (¹⁸F)-labeled PET tracer [¹⁸F]6 derived from RXR partial agonist CBt-PMN (2), which has lower lipophilicity and weaker RXR-binding ability than [¹¹C]1. The concomitant administration of 1 or 2 with [¹⁸F]6 with resulted in decreased accumulation of [¹⁸F]6 in liver, together with increased brain uptake and increased accumulation in kidney and muscle, as visualized by PET. A plausible explanation of these findings is the inhibition of [¹⁸F]6 uptake into the liver by concomitantly administered 1 or 2, leading to an increase in blood concentration of [¹⁸F]6 followed by increased accumulation in other tissues.     

Phylogenetic Relationship ofPopulusSections by ITS Sequence Analysis

ITS sequences of 15 representative species of five sections in the genus Populus L. were determined. By using direct sequencing of PCR product, it was found that the fragments of internal transcribed spacers (ITS) are about 594 bp in length. The length of ITS-1 and ITS-2 is about 220 bp and 210 bp, respectively, while that of 5.8s is 164 bp. Its G+C content is about 69.0%. The number of phylogenetically informative loci is higher in ITS-2 than in ITS-1. Transversion and transition are two main factors that drive the ITS evolution, and more insertions and deletions occurred in ITS-2. Taking Salix matsudana Koidz. and Salix suchowensis Cheng as outgroups, phylogenetic analysis of ITS sequences using PAUP 4.0 software indicated that Populus is monophyletic group and can be divided into two main clades. One is the section Leuce , and the other is the remaining sections.