Identification of urine metabolites of TFAP,a cyclooxygenase-1 inhibitor

Only a few COX-1-selective inhibitors are currently available, and the research on COX-1 selective inhibitors is not fully developed. The authors have produced several COX-1 selective inhibitors including N-(5-amino-2-pyridinyl)-4-trifluoromethylbenzamide: TFAP (3). Although 3 shows potent analgesic effect without gastric damage, the urine after administration of 3 becomes red–purple. Since the colored-urine should be avoided for clinical use, in this research we examined the cause of the colored-urine. UV–vis spectra and LC–MS/MS analyses of urine samples and metabolite candidates of 3 were performed to afford information that the main reason of the colored urine is a diaminopyridine (4), produced by metabolization of 3. This information is useful to design new COX-1 selective inhibitors without colored urine based on the chemical structure of 3.     

Structure-based virtual screening of novel tubulin inhibitors and their characterization as anti-mitotic agents

Microtubule cytoskeletons are involved in many essential functions throughout the life cycle of cells, including transport of materials into cells, cell movement, and proper progression of cell division. Small compounds that can bind at the colchicine site of tubulin have drawn great attention because these agents can suppress or inhibit microtubule dynamics and tubulin polymerization. To find novel tubulin polymerization inhibitors as anti-mitotic agents, we performed a virtual screening study of the colchicine binding site on tubulin. Novel tubulin inhibitors were identified and characterized by their inhibitory activities on tubulin polymerization in vitro. The structural basis for the interaction of novel inhibitors with tubulin was investigated by molecular modeling, and we have proposed binding models for these hit compounds with tubulin. The proposed docking models were very similar to the binding pattern of colchicine or podophyllotoxin with tubulin. These new hit compound derivatives exerted growth inhibitory effects on the HL60 cell lines tested and exhibited strong cell cycle arrest at G2/M phase. Furthermore, these compounds induced apoptosis after cell cycle arrest. In this study, we show that the validated derivatives of compound 11 could serve as potent lead compounds for designing novel anti-cancer agents that target microtubules.     

Improved genome assembly provides new insights into genome evolution in a desert poplar (Populus euphratica)

Populus euphratica is well adapted to extreme desert environments and is an important model species for elucidating the mechanisms of abiotic stress resistance in trees. The current assembly of P. euphratica genome is highly fragmented with many gaps and errors, thereby impeding downstream applications. Here, we report an improved chromosome‐level reference genome of P. euphratica (v2.0) using single‐molecule sequencing and chromosome conformation capture (Hi‐C) technologies. Relative to the previous reference genome, our assembly represents a nearly 60‐fold improvement in contiguity, with a scaffold N50 size of 28.59 Mb. Using this genome, we have found that extensive expansion of Gypsy elements in P. euphratica led to its rapid increase in genome size compared to any other Salicaceae species studied to date, and potentially contributed to adaptive divergence driven by insertions near genes involved in stress tolerance. We also detected a wide range of unique structural rearrangements in P. euphratica, including 2,549 translocations, 454 inversions, 121 tandem and 14 segmental duplications. Several key genes likely to be involved in tolerance to abiotic stress were identified within these regions. This high‐quality genome represents a valuable resource for poplar breeding and genetic improvement in the future, as well as comparative genomic analysis with other Salicaceae species.     

Length-weight relationships of four fish species from the Hei River in northwest China

Length-weight relationships (LWRs) were assessed from four fish species in Hei River in northwest China. All specimens were collected using (fishing1 km along the river and 3 meters along the river bank) and netting (gill nets, nets: 30 × 1.2 m; mesh size: 3 × 3 cm) and shrimp cages (nets: 20.0 × 0.5 × 0.4m; mesh size: 0.5 cm) seasonally from April 2019 to October 2020. The gill nets and shrimp cages were soaked in water in the afternoon and pulled in around 10 a.m. the next day after an overnight stay. These specimens were measured for total length (L, 0.1 cm) and body weight (W, 0.1 g) while the specimens were fresh. The parameters for the LWRs were estimated with the basic statistical analyses. The study provided the new maximum total length for Gymnocypris chilianensis (21.0 cm) and Triplophysa tenuis (17.0 cm).     

New Continuous Air Pumping Technique to Improve Clinical Outcomes of Descemet-Stripping Automated Endothelial Keratoplasty in Asian Patients with Previous Ahmed Glaucoma Valve Implantation

Background

To evaluate the outcomes of Descemet-stripping automated endothelial keratoplasty (DSAEK) with the use of continuous air pumping technique in Asian eyes with previous Ahmed glaucoma valve implantation.

Methods

The DSAEK procedure was modified in that complete air retention of the anterior chamber was maintained for 10 min using continuous air pumping at 30 mm Hg. The primary outcome measurement was graft survival, and postoperative clinical features including, rate of graft detachment, endothelial cell count, intraocular pressure (IOP), surgical time and cup/disc ratio were also recorded.

Results

A total of 13 eyes of 13 patients which underwent modified DSAEK and 6 eyes of 6 patients which underwent conventional DSAEK were included. There was a significant difference in graft survival curves between two groups (P = 0.029); the 1-year graft survival rates were estimated as 100% and 66.7% for patients with modified DSAEK and those with traditional DSAEK, respectively. The rate of graft detachment were 0% and 33.3% for the modified DSAEK and conventional DSAEK groups, respectively (P = 0.088). The significantly lowered surgical time for air tamponade was noted in the modified DSAEK group compared to that in the conventional DSAEK group [median (IQR): 10.0 (10.0, 10.0) min vs. 24.5 (22.0, 27.0) min; P<0.001] Postoperatively, patients in the modified DSAEK group had significantly lower IOP as compared to the conventional DSAEK group [12.0 (11.0, 15.0) mm Hg vs. 16.0 (15.0, 18.0) mm Hg; P = 0.047]. Modified DSAEK patients had higher endothelial cell counts as compared to conventional DSAEK patients [2148.0 (1964.0, 2218.0) vs. 1529.0 (713.0, 2014.0)], but the difference did not reach statistical significance (P = 0.072).

Conclusions

New continuous air pumping technique in DSAEK can be performed safely and effectively in patients with prior GDDs placement who have corneal failure.     

Use of proteomics to understand seed development in rice

Rice is an important cereal crop and has become a model monocot for research into crop biology. Rice seeds currently feed more than half of the world's population and the demand for rice seeds is rapidly increasing because of the fast‐growing world population. However, the molecular mechanisms underlying rice seed development is incompletely understood. Genetic and molecular studies have developed our understanding of substantial proteins related to rice seed development. Recent advancements in proteomics have revolutionized the research on seed development at the single gene or protein level. Proteomic studies in rice seeds have provided the molecular explanation for cellular and metabolic events as well as environmental stress responses that occur during embryo and endosperm development. They have also led to the new identification of a large number of proteins associated with regulating seed development such as those involved in stress tolerance and RNA metabolism. In the future, proteomics, combined with genetic, cytological, and molecular tools, will help to elucidate the molecular pathways underlying seed development control and help in the development of valuable and potential strategies for improving yield, quality, and stress tolerance in rice and other cereals. Here, we reviewed recent progress in understanding the mechanisms of seed development in rice with the use of proteomics.     

2012年中国植物科学若干领域重要研究进展

2012年中国植物科学研究继续快速发展。中国科学家在植物科学多个领域中取得了大量的原创性、高水平研究成果, 包括植物基因组研究、植物天然免疫抗性及其应答环境的信号转导机制以及植物去甲基化作用和DNA双链断裂修复机制研究等, 受到国内外的高度评价。该文对2012年中国本土植物生命科学若干领域取得的重要研究进展进行概括性评述, 旨在全面追踪当前中国植物科学领域发展的最新前沿和热点事件, 并展现我国科学家所取得的杰出成就。