Pharmacokinetics, metabolism, excretion and safety of iruplinalkib (WX-0593), a novel ALK inhibitor, in healthy subjects: a phase I human radiolabeled mass balance study.

BACKGROUND: Iruplinalkib is a novel anaplastic lymphoma kinase (ALK) inhibitor for the treatment of ALK-positive crizotinib-resistant NSCLC. RESEARCH DESIGN AND METHODS: A single oral dose of 120 mg/3.7 MBq [14C]iruplinalkib was administered to healthy subjects. Blood, urine and fecal samples were collected and analyzed for iruplinalkib and its metabolites. The safety of iruplinalkib was also assessed. RESULTS: Iruplinalkib was absorbed quickly and eliminated slowly from plasma, with a Tmax of 1.5 h and t1/2 of 28.6 h. About 88.85% of iruplinalkib was excreted at 312 h, including 20.23% in urine and 68.63% in feces. Seventeen metabolites of iruplinalkib were identified, and M3b (demethylation), M7 (cysteine conjugation), M11 (oxidative dehydrogenation and cysteine conjugation of M3b) and M12 (oxidative dehydrogenation and cysteine conjugation) were considered the prominent metabolites in humans. Iruplinalkib-related compounds were found to be covalently bound to proteins, accounting for 7.70% in plasma and 17.96% in feces, which suggested chemically reactive metabolites were formed. There were no serious adverse events observed in the study. CONCLUSIONS: Iruplinalkib was widely metabolized and excreted mainly through feces in humans. Unchanged iruplinalkib, cysteine conjugates and covalent protein binding products were the main drug-related compounds in circulation. Iruplinalkib was well tolerated at the study dose. TRIAL REGISTRATION: The trial is registered at ClinicalTrials.gov (Identifier: Anonymized).

In vitro and in vivo pharmacokinetics, disposition, and drug-drug interaction potential of tinengotinib (TT-00420), a promising investigational drug for treatment of cholangiocarcinoma and other solid tumors.

Early-stage clinical evaluation of tinengotinib (TT-00420) demonstrated encouraging preliminary efficacies in multiple types of refractory cancers, including fibroblast growth factor receptors (FGFR) inhibitors relapsed cholangiocarcinoma (CCA), castrate-resistant prostate cancer (CRPC), and HR+/HER2- breast cancer and triple negative breast cancer (TNBC). To further evaluate drug-like properties of the drug candidate, it is imperative to understand its metabolism and pharmacokinetic properties. This manuscript presented the investigation results of in vitro permeability, plasma protein binding, metabolic stability, metabolite identification, and drug-drug interaction of tinengotinib. Preclinical ADME (absorption, distribution, excretion, and metabolism) studies in rats and dogs was also conducted using a radioactive labeled tinengotinib, [14C]tinengotinib. Tinengotinib was found to have high permeability and high plasma protein binding and equally distributed between blood and plasma. There were no unique metabolites in human liver microsomes and tinengotinib showed moderate hepatic clearance. Tinengotinib is neither a potential inhibitor nor an inducer of P450 enzymes at clinically relevant concentrations, and unlikely to cause drug-drug interactions when used in combination with other drugs mediated by a key transporter, either as victim or perpetrator. Taken together, tinengotinib demonstrated a minimal risk of clinically relevant drug-drug interactions. Tinengotinib showed good oral bioavailability and dose-dependent exposures in both rat and dog after oral administration. The total radioactivity was largely distributed in the gastrointestinal system and liver, and tinengotinib could not easily pass through the blood-brain barrier. The major drug-related component in rat and dog plasma was unchanged drug (>89 %) with primary route of elimination via feces (>93 % of the dose) and minor via renal excretion (<4 % of the dose). Tinengotinib metabolism is mediated largely by CYP3A4, with minor contributions from CYP2D6 and CYP2C8. Major metabolic pathways include oxidation, oxidative cleavage of the morpholine ring, glucuronide and glutathione conjugations. The overall preclinical pharmacokinetics profile supported the selection and development of tinengotinib as a clinical candidate.

Optimized border irrigation delays winter wheat flag leaf senescence and promotes grain filling.

Border irrigation is still the main irrigation method in the Huang-Huai-Hai Plain of China (HPC), and the suitable irrigation border length for water saving and high yield under traditional irrigation is still unclear. Therefore, a 2-year traditional border irrigation experiment (2017-2019) was conducted on the HPC. Four border lengths were tested: 20 m (L20), 30 m (L30), 40 m (L40), and 50 m (L50). These treatments were given supplementary irrigation at jointing and anthesis. An exclusively rainfed condition formed the control treatment. Compared with other treatments, the activities of superoxide dismutase antioxidant and sucrose phosphate synthetase, and the contents of sucrose and soluble proteins after anthesis were higher in the L40 and L50 treatments, while the content of malondialdehyde content was lower. Therefore, the L40 treatment effectively delayed the decrease in the soil plant analysis development (SPAD) value and chlorophyll fluorescence characteristics, promoted grain filling, and achieved the highest thousand-grain weight. Compared with the L40 treatment, the grain yields of the L20 and L30 treatment were significantly reduced, while the water productivity of the L50 treatment was significantly reduced. These findings suggest that 40 m was the optimal border length for both high yield and water saving in this experiment. This study provides a simple and low-cost water-saving irrigation method for winter wheat in the HPC under traditional irrigation, which can help alleviate the pressure of agricultural water use.

Effects of planting density on photosynthetic characteristics of flag leaf and senescence of leaf and root under wide-width sowing condition.

To determine the optimal planting density under wide-width sowing condition, we investigated the effects of different planting densities on photosynthetic characteristics of flag leaves, senescence characteristics of flag lea-ves and roots, grain yield, and water use efficiency under four planting density levels, 90×104 plants·hm-2 (D1), 180×104 plants·hm-2 (D2), 270×104 plants·hm-2 (D3) and 360×104 plants·hm-2 (D4), in field condition set in Yanzhou, Shandong during the growing season of 2018-2019 and 2019-2020. The results showed that compared with D1 and D4 treatments, D2 treatment significantly improved photosynthetic characteristics of wheat flag leaves during grain filling, increased the activity of superoxide dismutase (SOD) and soluble protein content, reduced the malondialdehyde (MDA) content, and delayed the senescence of flag leaves and roots. Compared with other treatments, D2 treatment significantly increased root length, root surface area and root volume in 0-40 cm soil layer. Compared with D1, D3 and D4 treatments, the grain yield of D2 treatment was increased by 11.8%, 2.5%, 6.4% in 2018-2019 and 22.7%, 5.7%, 17.1% in 2019-2020, respectively. In addition, water use efficiency was increased by 9.2%, 8.8%, 14.2% in 2018-2019 and 21.1%, 6.2%, 21.5% in 2019-2020, respectively. The planting density at 180×104 plants·hm-2 improved photosynthetic characteristics of flag leaves and root morphology during filling stage, delayed plant senescence, increased grain number per spike and grain weight. Consequently, the highest grain yield and water use efficiency were obtained under D2 treatment, which was the optimal treatment under the experimental wide-width sowing condition.

Optimized border irrigation improved soil water content, increased winter wheat grain yield and water productivity.

Border irrigation is still the main irrigation method in the Huang-Huai-Hai Plain of China (HPC), we aimed to find a suitable border length to reduce the quantity of irrigation water through a traditional border irrigation system to alleviate groundwater depletion. A 2-year experiment (2017-2019) was conducted with four border lengths: 20 m (L20), 30 m (L30), 40 m (L40) and 50 m (L50); supplementary irrigation was implemented during jointing and anthesis. The results showed that compared with the L20 and L30 treatments, the L40 treatment did not significantly increase the total water consumption. Compared with the L50 treatment, the L40 treatment significantly reduced the water consumption of ineffective tillers from jointing to anthesis. There was no significant difference in flag leaf net photosynthetic rate (Pn) between L40 treatment and L50 treatment at 14-28 days after anthesis, which was 12.36% and 21.31% higher than L30 and L20 treatments respectively, and significantly increased dry matter accumulation after anthesis. Grain yield were the higher in the L40 and L50 treatments, while the water productivity (WP) was highest in the L40 treatment, which was 3.98%, 4.54% and 7.94% higher than L50, L30, and L20 treatments, respectively. Hence, the irrigation field treatments with a border length of 40 m were considered the most efficient, which provides a theoretical basis for optimizing the traditional irrigation border length in HPC.

Grain-filling characteristics and yield formation of wheat in two different soil fertility fields in the Huang-Huai-Hai Plain.

Clarifying factors that underpinning the variation in wheat yield components between high and middle soil fertility fields is critical to increase grain production and narrow yield gap for smallholder farming systems in the Huang-Huai-Hai Plain (3HP), which characterized by a large variation in soil fertility. Two-year field experiments were conducted to investigate wheat tillering, leaf photosynthesis, and grain filling characteristics in different soil fertility fields: high soil fertility field (HF) and middle soil fertility field (MF). Results showed that the spike formation rate in HF was 12.7%-13.0% higher than that in MF, leading to an 18.0%-19.8% increase in spike number. In addition, HF improved canopy light interception and leaf photosynthesis characteristics after anthesis and delayed leaf senescence, contributing to the increase in both the active grain filling period and grain filling rate. This resulted in a higher 1,000 grain weight in HF, which was 8.2%-8.3% higher than that in MF. Compared to MF, HF obtained higher yields at 9,840 kg ha-1 in 2017/18 and 11,462 kg ha-1 in 2018/19, respectively. In summary, higher spike number and 1,000-grain weight, which were mediated by spike-formation rate, maximization of light interception and improved leaf photosynthesis. These results would have important implications for narrowing yield gap between MF and HF in the 3HP.

Impacts of Fertilization Optimization on Soil Nitrogen Cycling and Wheat Nitrogen Utilization Under Water-Saving Irrigation.

Scholars have proposed the practice of split nitrogen fertilizer application (SNFA), which has proven to be an effective approach for enhancing nitrogen use efficiency. However, the combined effects of SNFA on wheat plant nitrogen use efficiency, ammonia (NH3) emission flux, as well as the rates of nitrification and denitrification in different ecosystems remain unclear. Meanwhile, few studies have sought to understand the effects of the split nitrogen fertilizer method under water-saving irrigation technology conditions on nitrogen loss. The current study assessed soil NH3 volatilization, nitrification, and denitrification intensities, as well as the abundance of nitrogen cycle-related functional genes following application of different treatments. Specifically, we applied a nitrogen rate of 240 kg⋅ha-1, and the following fertilizer ratios of the percent base to that of topdressing under water-saving irrigation: N1 (basal/dressing, 100/0%), N2 (basal/dressing, 70/30%), N3 (basal/dressing, 50/50%), N4 (basal/dressing, 30/70%), and N5 (basal/dressing, 0/100%). N3 treatment significantly reduced NH3 volatilization, nitrification, and denitrification intensities, primarily owing to the reduced reaction substrate concentration (NO3 - and NH4 +) and abundance of functional genes involved in the nitrogen cycle (amoA-AOB, nirK, and nirS) within the wheat-land soil. 15N tracer studies further demonstrated that N3 treatments significantly increased the grain nitrogen accumulation by 9.50-28.27% compared with that under other treatments. This increase was primarily due to an increase in the amount of nitrogen absorbed by wheat from soil and fertilizers, which was caused by an enhancement in total nitrogen uptake (7.2-21.81%). Overall, N3 treatment (basal/dressing, 50/50%) was found to effectively reduce nitrogen loss through NH3 volatilization, nitrification and denitrification while improving nitrogen uptake by wheat. Thus, its application will serve to further maximize the yield and provide a fertilization practice that will facilitate cleaner wheat production in the North China Plain.

The metabolism and excretion of the dipeptidyl peptidase 4 inhibitor [14C] cetagliptin in healthy volunteers.

The metabolism and excretion of cetagliptin were investigated in healthy male subjects after a single oral dose of 100mg/50µCi [14C] cetagliptin.The mean concentration-time profile of cetagliptin was similar to that of total radioactivity in plasma after oral administration of [14C] cetagliptin in healthy male subjects. Cetagliptin was rapidly absorbed after oral administration. Unchanged cetagliptin was the most abundant radioactive component in all matrices investigated. Approximately 53.13% of plasma AUC of total radioactivity was accounted for by cetagliptin. Each metabolite plasma AUC was not higher than 2.93% of plasma AUC of total radioactivity. By 336 h after administration, 91.68% of the administered radioactivity was excreted, and the cumulative excretion in the urine and faeces was 72.88% and 18.81%, respectively. The primary route of excretion of radioactivity was via the kidneys.Four metabolites were detected at trace levels, and it involved hydroxylated (M436-1 and M436-3), N- sulphate (M500), and N-carbamoyl glucuronic acid conjugates (M640B) of cetagliptin. These metabolites were detected also in plasma, urine, and faeces at low levels, except that metabolite M640B was not detected in faeces. All metabolites were observed with <10% of parent compound systemic exposure after oral administration.

Optimized nitrogen fertilizer application strategies under supplementary irrigation improved winter wheat (Triticum aestivum L.) yield and grain protein yield.

BACKGROUND: Exploring suitable split nitrogen management is essential for winter wheat production in the Huang-Huai-Hai Plain of China (HPC) under water-saving irrigation conditions, which can increase grain and protein yields by improving nitrogen translocation, metabolic enzyme activity and grain nitrogen accumulation. METHODS: Therefore, a 2-year field experiment was conducted to investigate these effects in HPC. Nitrogen fertilizer was applied at a constant total rate (240 kg/ha), split between the sowing and at winter wheat jointing growth stage in varying ratios, N1 (0% basal and 100% dressing fertilizer), N2 (30% basal and 70% dressing fertilizer), N3 (50% basal and 50% dressing fertilizer), N4 (70% basal and 30% dressing fertilizer), and N5 (100% basal and 0% dressing fertilizer). RESULTS: We found that the N3 treatment significantly increased nitrogen accumulation post-anthesis and nitrogen translocation to grains. In addition, this treatment significantly increased flag leaf free amino acid levels, and nitrate reductase and glutamine synthetase activities, as well as the accumulation rate, active accumulation period, and accumulation of 1000-grain nitrogen. These factors all contributed to high grain nitrogen accumulation. Finally, grain yield increase due to N3 ranging from 5.3% to 15.4% and protein yield from 13.7% to 31.6%. The grain and protein yields were significantly and positively correlated with nitrogen transport parameters, nitrogen metabolic enzyme activity levels, grain nitrogen filling parameters. CONCLUSIONS: Therefore, the use of split nitrogen fertilizer application at a ratio of 50%:50% basal-topdressing is recommended for supporting high grain protein levels and strong nitrogen translocation, in pursuit of high-quality grain yield.

Differences in Water Consumption of Wheat Varieties Are Affected by Root Morphology Characteristics and Post-anthesis Root Senescence.

Selecting high-yielding wheat varieties for cultivation can effectively increase water use efficiency (WUE) in the Huang-Huai-Hai Plain, where is threatened by increasing water shortages. To further identify the difference in water use and its relationship with root morphology and senescence characteristics, wheat varieties with different yield potentials-Yannong 1212 (YN), Jimai 22 (JM), and Liangxing 99 (LX)-were studied in a high-yielding wheat field. The water consumption percentage (CP) in YN decreased from planting to anthesis; however, crop evapotranspiration and CP increased from anthesis to maturity compared with JM and LX. In YN, a higher soil water consumption from anthesis to maturity in the 0-100 cm soil layer was partly attributed to the greater root weight density in the 20-60 cm soil layer. In topsoil (0-40 cm), root length density, root surface area density, and root diameter at 20 days after anthesis, root superoxide dismutase activity, and root triphenyl tetrazolium chloride reduction activity during mid grain filling stage were higher in YN than in JM and LX. YN had the highest grain yields of 9,840 and 11,462 kg ha-1 and increased grain yield and WUE by 12.0 and 8.4%, respectively, as compared with JM, and by 30.3 and 21.3%, respectively, as compared with LX. Ensuring more soil water extraction post-anthesis by increasing roots in the 20-60 cm soil profile, improving root morphology traits, and alleviating root senescence in the topsoil during mid-grain filling stage will assist in selecting wheat varieties with high yield and WUE.

Mass balance, pharmacokinetics and pharmacodynamics of intravenous HSK3486, a novel anaesthetic, administered to healthy subjects.

AIMS: This trial (NCT03751956) investigated the mass balance, pharmacokinetics and pharmacodynamics of HSK3486, a novel anaesthetic, in healthy subjects. METHODS: A single dose of 0.4 mg/kg [14 C]HSK3486 was administered to six healthy subjects. Blood, urine and faecal samples were collected, analysed for radioactivity, unchanged HSK3486 and profiled for metabolites. The Modified Observer's Assessment of Alertness/Sedation (MOAA/S) scale and vital signs were closely monitored during the study. RESULTS: The mean recovery of total radioactivity in excreta was 87.3% in 240 h, including 84.6% in urine and 2.65% in faeces. The exposure (AUC0-t ) of total radioactivity was much higher than that of unchanged HSK3486 in plasma, indicating there were circulating metabolites in plasma. The glucuronide conjugate of HSK3486 (M4) was found as the only major circulating metabolite in plasma (79.3%), while unchanged HSK3486 accounted for only 3.97% of the total radiation exposure. M4 also resulted in a longer estimated elimination half-life (t1/2 ) of total radioactivity than that of unchanged HSK3486 in plasma. Fortunately, the metabolite was detected to be not specific to red blood cells and was suggested to be nonhypnotic and nontoxic. All the subjects were quickly anaesthetized (2 min) after drug administration and woke up smoothly after a short time (5.5-14.1 min) with few residual effects. The only adverse event in the study was mild (grade 1) and consisted of hypotension. CONCLUSION: HSK3486 is a promising anaesthetic candidate with rapid onset of action and clear absorption, distribution, metabolism, excretion (ADME) processes. HSK3486 showed favourable pharmacokinetic characteristics, pharmacodynamic responses and safety at the study dose.

Optimized split nitrogen fertilizer increase photosynthesis, grain yield, nitrogen use efficiency and water use efficiency under water-saving irrigation.

This study aims to investigate optimization of the basal-top-dressing nitrogen ratio for improving winter wheat grain yield, nitrogen use efficiency, water use efficiency and physiological parameters under supplemental irrigation. A water-saving irrigation (SI) regime was established and sufficient irrigation (UI) was used as a control condition. The split-nitrogen regimes used were based on a identical total nitrogen application rate of 240 kg ha-1 but were split in four different proportions between sowing and the jointing stage; i.e. 10:0 (N1), 7:3 (N2), 5:5 (N3) and 3:7 (N4). Compared with the N1, N2 and N4 treatments, N3 treatment increased grain yield, nitrogen and water use efficiencies by 5.27-17.75%, 5.68-18.78% and 5.65-31.02%, respectively, in both years. The yield advantage obtained with the optimized split-nitrogen fertilizer application may be attributable to greater flag leaf photosynthetic capacity and grain-filling capacity. Furthermore, the N3 treatment maintained the highest nitrogen and water use efficiencies. Moreover, we observed that water use efficiency of SI compared with UI increased by 9.75% in 2016 and 10.79% in 2017, respectively. It can be concluded that SI along with a 5:5 basal-top-dressing nitrogen ratio should be considered as an optimal fertigation strategy for both high grain yield and efficiency in winter wheat.

Nitrogen supply modulates nitrogen remobilization and nitrogen use of wheat under supplemental irrigation in the North China Plain.

Excessive nitrogen (N) input and irrigation exacerbate N leaching in winter wheat production in the North China Plain (NCP). To explore the optimal N for better N remobilization and higher N utilization of wheat under water-saving irrigation will be conductive to less environmental contamination. A field experiment was conducted at 300 (N300), 240 (N240), 180 (N180), and 0 (N0) kg N ha-1 of N application under supplemental irrigation (SI) that brought the relative soil water content (RSWC) to 70% at jointing and 65% at anthesis. Compared with N0, N180 improved the free amino acid content in the flag leaf and grain after anthesis, dry matter and plant N accumulation at maturity, N translocation amount of vegetable organs and its contribution to grain from anthesis to maturity. Compared to N240 and N300, N180 increased the N translocation efficiency of vegetable organs, and reduced the soil NO3-N residue in the 60-180 cm soil layer, which contributing to no significant reduction in grain yield and grain protein yield, but higher grain N recovery efficiency (GREN), N recovery efficiency (REN), and N partial factor productivity (PFPN). Positive relationships were found between leaf N translocation efficiency and grain yield, grain protein yield, PFPN, GREN, and REN. Therefore, N180 is appropriate to obtain a steady grain yield over 7.5 t ha-1 for at least 2 years under SI based on RSWC in the NCP.

[Light energy utilization and distribution characteristics of flag leaf 13C assimilate in different spike-type wheat varieties and their responses to supplementary irrigation]. / ä¸åŒç©—åž‹å°éº¦å ‰èƒ½åˆ©ç”¨å’Œæ——å¶13CåŒåŒ–ç‰©åˆ†é ç‰¹æ€§åŠå¯¹è¡¥çŒæ°´å¹³çš„å“åº”.

To clarify the differences in light energy utilization and distribution characteristics of flag leaf 13C assimilate in different spike-type wheat varieties and their responses to supplementary irrigation, we set three water treatments in a field experiment, including no irrigation during growth duration of wheat (W0), water-saving irrigation (W1, irrigating at jointing and anthesis of wheat to keep the relative moisture of 0-40 cm soil to 65% and 70%), full irrigation (W2, irrigating at jointing and anthesis of wheat to keep the relative moisture of 0-40 cm soil to 85% and 90%) with the medium-spike wheat cultivars Jimai 22 and Qingnong 2, large-spike wheat cultivars Shannong 23 and Shannong 30 as test materials. The effects of different water treatments on canopy light energy utilization and 13C assimilate distribution characteristics of two spike-type wheat varieties were examined. The results showed that leaf area index, canopy light interception rate, and light energy utilization rate of the two varieties at 2, 11, 20 and 31 days after anthesis were significantly higher than W0 treatment, but there was no significant change in each index when the irrigation increased to W2 treatment. The distribution of flag leaf 13C assimilates of Jimai 22 and Shannong 23 of W1 in grain was 159.34 and 171.1 g·hm-2 higher than W0, respectively, and the distribution ratio was 6.5% and 6.5%, with no significant difference compared with W2. The grain yields of both varieties under W1 were significantly higher than that under W0, but with no significant difference with W2. Under water-saving irrigation, the medium-spike cultivars had higher canopy photosynthetically active radiation interception and utilization ability at 2 and 11 days after anthesis and large-spike cultivars at 20 and 31 days after anthesis. The distribution amount and ratio of 13C assimilates in the grain of medium-spike variety Jimai 22 flag leaf were 6.8% and 2.7% lower than that of the large-spike variety Shannong 23.

Strip rotary tillage with a two-year subsoiling interval enhances root growth and yield in wheat.

Excessive tillage and soil compaction threaten the sustainable farmlands in the Huang-Huai-Hai Plains of China. Our study explores tillage practices to improve soil and root ecology and promote productivity in the winter wheat fields. We tested the impact of plowing, rotary, strip rotary tillage and strip rotary tillage with a two-year subsoiling interval (SRS) on wheat yield and root quality. SRS decreased soil bulk density compared with other treatments, resulting in lower soil penetration resistance. Root morphology and weight density decreased with the increased soil depth and was higher in SRS. Moreover, SRS increased the indoleacetic acid and trans zeatin riboside levels corresponding to greater TTC reduction activities, the total and active absorption root area. SRS increased the superoxide dismutase and catalase activities and soluble protein concentration and decreased the malondialdehyde concentration. The first two factors extracted using 11 root attributes in various soil layers through principal component analysis were selected as the integrated indicators for the minimum data set, and their integrated score was calculated to quantify the root quality. Our study suggests that SRS could significantly improve root morphology and enhance the root activity in subsoil layers, thus, delaying root senescence and increasing winter wheat yield.

Radiation Interception, Chlorophyll Fluorescence and Senescence of Flag leaves in Winter Wheat under Supplemental Irrigation.

Water shortage threatens agricultural sustainability in China, effective water-saving technologies urgently need to be developed. In this study, five treatments were conducted: rainfed (W0), a local supplemental irrigation (SI) practice (W1), and three treatments in which soil water content was tested prior to SI, specifically at 0-20 (W2), 0-40 (W3) and 0-60 cm (W4) soil layers. Soil water consumption in W3 had no differ with W2 but was higher than W1 and W4. Crop evapotranspiration in W1, W3 and W4 treatments were higher than that in W2. W3 treatment had higher leaf area index than W1 and W4 at later grain filling stages. The mean photosynthetically active radiation capture ratio in W3, especially at 20, 40 and 60 cm plant heights, were significantly higher than those in W1, W2 and W4. The chlorophyll content index, actual photosynthetic activities, catalase and superoxide dismutase activities of flag leaves from W3 were the highest after the middle grain filling stages. W3 treatment obtained the highest grain yield (9169 kg ha-1) and water use efficiency (20.8 kg ha-1 mm-1) in the two seasons. These benefits likely accrued through created a suitable soil moisture environment in W3 treatment.

[Effects of supplemental irrigation by monitoring soil moisture on the'water-nitrogen utilization of wheat and soil NO3(-)-N leaching].

Field experiments were conducted during 2012-2014 wheat growing seasons. With no irrigation in the whole stage (WO) treatment as control, three supplemental irrigation treatments were designed based on average relative soil moisture contents at 0-140-cm layer, at jointing and anthesis stages (65% for treatment W1 ; 70% for treatment W2; 75% for treatment W3; respectively), to examine effects of supplemental irrigation on nitrogen accumulation and translocation, grain yield, water use efficiency, and soil nitrate nitrogen leaching in wheat field., Soil water consumption amount, the percentage of soil water consumption and water irrigation to total water consumption in W2 were higher, and soil water consumption of W2 in 100-140 cm soil layer was also higher. The nitrogen accumulation before anthesis and after anthesis were presented as W2, W3>W1>W0, the nitrogen accumulation in vegetative organs at maturity as W3>W2>Wl>W0, and the nitrogen translocation from vegetative organs to grain and the nitrogen accumulation in grain at maturity as W2> W3>W1>W0. At maturity, soil NO3(-)-N content in 0-60 cm soil layer was presented. as W0>W1>W2>W3, that in 80-140 cm soil layer was significantly higher in W3 than in the other treatments, and no significant difference was found in 140-200 cm soil layer among all treatments. W treatment obtained the highest grain yield, water use efficiency, nitrogen uptake efficiency and partial productivity of applied nitrogen. As far as grain yield, water use efficiency, nitrogen uptake efficiency and soil NO3(1)-N leaching were concerned, the W2 regime was the optimal irrigation treatment in this experiment.

[Effects of supplemental irrigation by measuring moisture content in different soil layers on water consumption characteristics, photosynthesis and grain yield of winter wheat].

Field experiments were conducted during 2012-2014 winter wheat growing seasons. Six irrigation treatments were designed: rainfed, W0; a local irrigation practice that irrigated at jointing and anthesis with 60 mm each time, W1; four irrigation treatments were designed with target relative soil moisture of 65% field capacity (FC) at jointing and 70% FC at anthesis in 0-20 (W2) 0-40 (W3), 0-60 (W4) , and 0-140 cm (W5) soil layers, respectively, to study the effects of supplemental irrigation by measuring moisture content in different soil layers on water consumption characteristics and photosynthesis and grain yield of winter wheat. The irrigation amounts at jointing in W1 and W4 were the highest, followed by W3 treatment, W2 and W5 were the lowest. The irrigation amounts at anthesis and total irrigation amounts were ranked as W5 > Wl, W4 > W3 > W2, the total water consumption in W3 was higher than that in W2, but had no difference with that in W1, W4 and W5 treatments, W3 had the higher soil water consumption than W1, W4 and W5 treatments, and the soil water consumption in 40-140 cm soil layers from jointing to anthesis and in 60-140 cm soil layers from anthesis to maturity in W3 were significantly higher than the other treatments. The photosynthetic rate, transpiration rate and water use efficiency of flag leaf at middle stage of grain filling from the W3 treatment were the highest, followed by the W1 and W4 treatments, and W0 treatment was the lowest. In the two growing seasons, the grain yield and water use efficiency in the W3 were 9077-9260 kg · hm(-2) and 20.7-20.9 kg · hm(-2) · mm(-1), respectively, which were higher than those from the other treatments, and the irrigation water productivity in the W3 was the highest. As far as high-yield and high-water use efficiency were concerned in this experiment, the most appropriate soil layer for measuring moisture content was 0-40 cm.

Dry Matter Production, Photosynthesis of Flag Leaves and Water Use in Winter Wheat Are Affected by Supplemental Irrigation in the Huang-Huai-Hai Plain of China.

Winter wheat is threatened by drought in the Huang-Huai-Hai Plain of China, thus, effective water-saving irrigation practices are urgently required to maintain its high winter wheat production. This study was conducted from 2012 to 2014 to determine how supplemental irrigation (SI) affected soil moisture, photosynthesis, and dry matter (DM) production of winter wheat by measuring the moisture in 0-20 cm (W2), 0-40 cm (W3), and 0-60 cm (W4) soil profiles. Rainfed (W0) and local SI practice (W1, irrigation with 60 mm each at jointing and anthesis) treatments were designed as controls. The irrigation amount for W3 was significantly lower than that for W1 and W4 but higher than that for W2. The soil relative water content (SRWC) in 0-40 cm soil profiles at jointing after SI for W3 was significantly lower than that for W1 and W4 but higher than that for W2. W3 exhibited lower SRWC in 100-140 and 60-140 cm soil profiles at anthesis after SI and at maturity, respectively, but higher root length density in 60-100 cm soil profiles than W1, W2 and W4. Compared with W1, W2 and W4, photosynthetic and transpiration rates and stomatal conductance of flag leaves for W3 were significantly greater during grain filling, particularly at the mid and later stages. The total DM at maturity, DM in grain and leaves, post-anthesis DM accumulation and its contribution to grain and grain filling duration were higher for W3. The 1000-grain weight, grain yield and water use efficiency for W3 were the highest. Therefore, treatment of increasing SRWC in the 0-40 cm soil profiles to 65% and 70% field capacities at jointing and anthesis (W3), respectively, created a suitable soil moisture environment for winter wheat production, which could be considered as a high yield and water-saving treatment in Huang-Huai-Hai Plain, China.

[Effects of supplemental irrigation based on soil moisture on photosynthetic characteristics and enzyme activity of flan leaf in wheat].

A field experiment was conducted to study the effects of supplemental irrigation based on soil moisture on the photosynthesis characteristics and enzyme activity of flag leaf using the wheat cultivar Jimai 20. Three irrigation treatments were designed with target soil moisture of 65% (W65), 70% (W70) and 75% (W75) both at jointing and anthesis stages. Zero-irrigation ( CK) was used as the control. The results showed that the net photosynthetic rate (Pn) of flag leaf in treatment W70 was dramatically higher than in other treatments from 14 to 21 days after anthesis, as well as sucrose content and sucrose phosphate synthase (SPS) activity. The dry matter mass per area of W70 was higher than that of W65 and CK, and was not significantly different from that of W75. The single stem mass of W70 was higher than that of the other treatments. The activities of superoxide dismutase (SOD) and catalase (CAT) and the soluble protein concentration in flag leaf of W70 were significantly higher than in other treatments from 14 to 28 days after anthesis. The malondialdehyde (MDA) content of W70 was lower than that of W65 and CK, and was not significantly different from that of W75 from 14 to 21 days after anthesis. Grain yields of W70 were 8941.4 and 9125.4 kg · hm⁻² in the 2012-2013 and 2013-2014 wheat growing seasons, showing no significant difference with those of W75, but obviously higher than those of W65 and CK. And the water use efficiency (WUE) of W70 was the highest. Considering grain yield and WUE, maintaining the relative soil water content at 70% by supplemental irrigation both at jointing and anthesis stages was the best treatment.