Pharmacokinetics and Pharmacodynamics of a Depolymerized Glycosaminoglycan from Holothuria fuscopunctata,a Novel Anticoagulant Candidate,in Rats by Bioanalytical Methods

dHG-5 (Mw 5.3 kD) is a depolymerized glycosaminoglycan from sea cucumber Holothuria fuscopunctata. As a selective inhibitor of intrinsic Xase (iXase), preclinical study showed it was a promising anticoagulant candidate without obvious bleeding risk. In this work, two bioanalytical methods based on the anti-iXase and activated partial thromboplastin time (APTT) prolongation activities were established and validated to determine dHG-5 concentrations in plasma and urine samples. After single subcutaneous administration of dHG-5 at 5, 9, and 16.2 mg/kg to rats, the time to peak concentration (T_max) was at about 1 h, and the peak concentration (C_max) was 2.70, 6.50, and 10.11 μg/mL, respectively. The plasma elimination half-life(T_1/2β) was also about 1 h and dHG-5 could be almost completely absorbed after s.c. administration. Additionally, the pharmacodynamics of dHG-5 was positively correlated with its pharmacokinetics, as determined by rat plasma APTT and anti-iXase method, respectively. dHG-5 was mainly excreted by urine as the unchanged parent drug and about 60% was excreted within 48 h. The results suggested that dHG-5 could be almost completely absorbed after subcutaneous injection and the pharmacokinetics of dHG-5 are predictable. Studying pharmacokinetics of dHG-5 could provide valuable information for future clinical studies.     

EPS364, a Novel Deep-Sea Bacterial Exopolysaccharide,Inhibits Liver Cancer Cell Growth and Adhesion

The prognosis of liver cancer was inferior among tumors. New medicine treatments are urgently needed. In this study, a novel exopolysaccharide EPS364 was purified from Vibrio alginolyticus 364, which was isolated from a deep-sea cold seep of the South China Sea. Further research showed that EPS364 consisted of mannose, glucosamine, gluconic acid, galactosamine and arabinose with a molar ratio of 5:9:3.4:0.5:0.8. The relative molecular weight of EPS364 was 14.8 kDa. Our results further revealed that EPS364 was a β-linked and phosphorylated polysaccharide. Notably, EPS364 exhibited a significant antitumor activity, with inducing apoptosis, dissipation of the mitochondrial membrane potential (MMP) and generation of reactive oxygen species (ROS) in Huh7.5 liver cancer cells. Proteomic and quantitative real-time PCR analyses indicated that EPS364 inhibited cancer cell growth and adhesion via targeting the FGF19-FGFR4 signaling pathway. These findings suggest that EPS364 is a promising antitumor agent for pharmacotherapy.     

土壤调理粉剂处理下茶园土壤重金属污染特征及潜在风险评价

本文以贵州安顺不同土壤调理粉剂处理下“瀑布毛峰”茶园土壤为供试样品,通过样品测试与理化分析,对CK处理(0 kg/hm²)、A处理(600 kg/hm²)、B处理(750 kg/hm²)和C处理(900 kg/hm²)下茶园土壤重金属含量特征及污染水平进行探讨。结果表明：不同土壤调理粉剂处理下,研究区域土壤重金属Cr、Hg、Pb、Cu、Zn、Ni、As和Cd的变异程度各异,且土壤中这8种重金属含量也各不相同,其中pH、Cr、Pb和Ni含量在C处理中最高,As、Hg和Cd含量在A处理中最高,Cu和Zn含量在B处理中最高;对各重金属元素进行相关性分析可知,Ni与Pb之间存在极显著相关性,表明两者之间的同源性极高,其余元素之间相关性特征不明显;由综合污染指数（P_综）得出A处理为轻度污染,CK处理、B处理和C处理均为中度污染,不同处理土壤中Cr均在国家Ⅱ级标准(GB15618—2008)规定范围内,样点达标率为100%,在所选定的污染评价因子中,Cu的贡献率最高,为土壤主要影响因子,其次是Cd和Ni;研究区土壤重金属单项潜在生态风险指数($E_{r}^{i}$)中Hg属于强生态风险,其余7种重金属处于轻微潜在生态风险等级;综合潜在生态风险指数(RI)平均值为196.79,总体处于中等潜在生态风险水平,Hg对RI的贡献率最大,是最主要的生态风险元素。     

苗期调控对晚播小麦产量及氮素利用的影响

针对冬小麦因播期推迟造成产量损失的问题,以2个不同分蘖能力的冬小麦品种中麦8号和航麦501为供试材料,研究苗期覆膜和补施氮肥对晚播小麦产量及氮素利用的影响。试验设置3个播期：10月5日适期播种（S0,对照）、10月15日适当晚播（S1）和10月25日过晚播（S2）。结果表明：随着播期推迟,小麦产量逐渐降低。晚播条件下,苗期覆膜和补施氮肥可调控冬小麦产量构成因素、农艺性状、茎蘖生长、成穗率以及氮素的吸收利用。综合而言,晚播条件下,覆膜和补施氮肥有利于提高小麦穗长、总小穗数及冬前群体数量;同时,覆膜可显著提高2个品种晚播条件下的分蘖成穗率和过晚播条件下的植株氮素积累量（PNA）及氮肥偏生产力（PFP）,增幅分别为46.4%~89.1%、12.7%~26.5%和19.5%~20.1%;补施氮肥在过晚播条件下有利于成穗率的提高,增幅为18.5%~34.7%。2种调控措施均有利于增加晚播小麦产量,增幅达1.4%~19.5%。但不同分蘖力的小麦对2种调控措施的响应存在差异。综合考虑产量及氮素利用等各方面因素,在晚播条件下,相比于补施氮肥,苗期覆膜更有利于提高晚播小麦产量,弥补晚播造成的产量损失,但在实际操作和节约生产成本方面,前者优于后者。     

电感耦合等离子发射光谱法测定水质中的金元素

应用电感耦合等离子体发射光谱法测定了废水中的金元素,探讨了金测定的谱线选择、离子干扰等问题,实验结果表明:在最佳仪器条件和测定条件下,该方法的检出限为0.008 mg/L,方法精密度的方法标准偏差(RSD)在4.28%~1.44%之间,回收率为96%~104%。该方法操作简便,快捷。     

Molecular Characterization of the Von Willebrand Factor Type D Domain of Vitellogenin from Takifugu flavidus

The von Willebrand factor type D (VWD) domain in vitellogenin has recently been found to bind tetrodotoxin. The way in which this protein domain associates with tetrodotoxin and participates in transporting tetrodotoxin in vivo remains unclear. A cDNA fragment of the vitellogenin gene containing the VWD domain from pufferfish (Takifugu flavidus) (TfVWD) was cloned. Using in silico structural and docking analyses of the predicted protein, we determined that key amino acids (namely, Val¹¹⁵, ASP¹¹⁶, Val¹¹⁷, and Lys¹²²) in TfVWD mediate its binding to tetrodotoxin, which was supported by in vitro surface plasmon resonance analysis. Moreover, incubating recombinant rTfVWD together with tetrodotoxin attenuated its toxicity in vivo, further supporting protein–toxin binding and indicating associated toxicity-neutralizing effects. Finally, the expression profiling of TfVWD across different tissues and developmental stages indicated that its distribution patterns mirrored those of tetrodotoxin, suggesting that TfVWD may be involved in tetrodotoxin transport in pufferfish. For the first time, this study reveals the amino acids that mediate the binding of TfVWD to tetrodotoxin and provides a basis for further exploration of the molecular mechanisms underlying the enrichment and transfer of tetrodotoxin in pufferfish.     

基于农用STM32的电动机转速监测系统设计

农业作业环境复杂,实时监控农用电动机转速对判断电动机运行状况具有重要意义。笔者设计了一种电动机转速监测系统,该系统主要由光电开关传感器、触发圆盘、OLED、STM32单片机组成,通过单片机的定时器中断和外部中断功能,可实现对电动机转速的实时监控,通过IIC通信技术,可实现转速数据的可视化。该系统抗干扰能力强、精度高、实用性强,适用于恶劣的农业作业环境,同时为其他转速监测方案提供了设计依据。     

Responses of carbon metabolism and antioxidant system of summer maize to waterlogging at different stages

A field experiment was performed to explore responses of carbon metabolism, antioxidant system and endogenous hormone content of summer maize hybrids DengHai605 (DH605) and ZhengDan958 (ZD958) to waterlogging at the third leaf stage (V3), the sixth leaf stage (V6) and the 10th day after the tasselling stage (10VT). Results showed that waterlogging significantly decreased the contents of zeatin riboside (ZR), indole‐3‐acetic acid (IAA) and gibberellic acid (GA), compared to those of CK. However, leaf abscisic acid (ABA) content was significantly increased by waterlogging at different stages, with the most significant increase was found in the treatment of waterlogging at V3 (V3‐W), with an increase of 30% and 29% for DH605 and ZD958, respectively. Waterlogging significantly decreased antioxidative enzyme activities, accelerating leaf senescence, resulted in the disorder of leaf gas exchange parameters and chlorophyll fluorescence parameters. In addition, waterlogging decreased key enzyme activities of carbon metabolism (ribulose bisphosphate carboxylase and phosphoenolpyruvate carboxylase), with the most significant reduction in V3‐W, with a decrease of 46% and 49% for DH605, and 53% and 55% for ZD958, respectively. Visibly, waterlogging disturbed carbon metabolism, affected plant endogenous hormone content, accelerated leaf senescence and eventually resulted in a significant reduction in photosynthetic characteristic and grain yield. V3 was most susceptible to waterlogging, followed by V6 and 10VT.     

Bamboo NiR gene is associated with regeneration capacity

It was reported that the activity of NiR (nitrite reductase) enzyme encoded by the NiR gene was correlated with the regeneration ability in rice. To testify the function of NiR gene in bamboo, seven bamboo species whose calli had different differentiation rate were chosen to analyse their NiR enzyme activity. The results showed that bamboo NiR enzymatic activity had a certain correlation with the regeneration capacity. A NiR gene named DhNiR from Dendrocalamus hamiltonii with high regeneration capacity was cloned. Sequence analysis revealed that the ORF of DhNiR was 1779bp encoding 592 amino acids. Overexpression of DhNiR in rice reduced the time of shoot differentiation and increased the transformation rate, suggesting that DhNiR might play an important role in the regeneration ability of bamboo, and can be applied in regeneration and gene transformation of bamboo and other plant species.