A New Calcium(II)-Based Substitute for Enrofloxacin with Improved Medicinal Potential.

Enrofloxacin (EFX) reacting with Ca(II) afforded a new complex, [Ca(EFX)2(H2O)4] (EFX-Ca), which was structurally characterized both in solid and solution chemistry. E. coli and S. typhi were tested to be the most sensitive strains for EFX-Ca. The LD50 value of EFX-Ca in mice was 7736 mg/kg, implying the coordination of EFX to Ca(II) effectively reduced its acute toxicity. EFX-Ca also decreased the plasma-binding rate and enhanced the drug distribution in rats along with longer elimination half-life. EFX-Ca also showed similar low in vivo acute toxicity and higher anti-inflammation induced by H2O2 or CuSO4 in zebrafish, with reactive oxygen species (ROS)-related elimination. The therapeutic effects of EFX-Ca on two types (AA and 817) of E. coli-infected broilers were also better than those of EFX, with cure rates of 78% and 88%, respectively. EFX-Ca showed promise as a bio-safe metal-based veterinary drug with good efficacy and lower toxicity.

Interpretation of genotype-environment-sowing date/plant density interaction in sorghum [Sorghum bicolor (L.) Moench] in early mature regions of China.

Sorghum [Sorghum bicolor (L.) Moench] is an important crop for food security in semiarid and arid regions due to its high tolerance to abiotic and biotic stresses and its good performance in marginal lands with relatively low fertility. To deeply understand the interrelationship among sorghum genotype, environment, sowing dates, and densities in the spring sowing early maturing (SSEM) areas of China, and to provide a basis for specifying scientific and reasonable cultural practices, a two-year field experiment was conducted with six popular varieties at six locations. Combined ANOVA showed that the yield difference between years was significant (P<0.05); the yield differences among locations, varieties, sowing dates, and densities were all highly significant (P<0.01). The variety effect was mainly influenced by location, year, sowing dates and their interactions. The sowing effect was mainly influenced by the location, year, variety and their interactions The plant density effect was significantly influenced by location and location-year interaction. Of the contributions of various test factors to yield variance, the location was the largest one (38.18%), followed by variety (12.31%), sowing date (1.53%), density (0.54%), and year (0.09%), with all these single factors accounting for 52.65%. The total contribution of all two-factor interactions accounted for 14.24%, among which the greatest contributor was location-hybrid interaction (8.07%). The total contribution of all three-factor interactions accounted for 14.58%, of which year-location-hybrid interaction was the largest contributor (9.02%). Sowing dates significantly affected model of sorghum growth and development, especially during the late period. The key climatic factors affecting yield were different among the six locations. Weather factors during the grain filling stages contributed much more than those during the early stage to grain yield. Mid-maturing varieties are recommended other than early maturing varieties for the SSEM areas even when late sowing occurs. Sowing as early as possible is recommended for areas with very short frost-free period (Harbin, Tongliao, and Datong). Proper delayed sowing is recommended for areas with a relative long frost-free period (Gongzhuling, Baicheng and Zhangjiakou). This research will provide a conducive reference for sorghum production in similar areas.

Study on Evaporation Characteristics of Water in Annular Liquid Pool at Low Pressures.

In order to investigate the energy transfer mechanism and the nonequilibrium effect during water evaporation in its own pure vapor at low pressures, a series of precise measurements are conducted to obtain the temperature profile near the liquid-vapor interface and the evaporation rates in an annular pool in a closed chamber. The results show that the interface temperature of the vapor side is higher than that of the liquid side when water evaporates in its own pure vapor at low pressures (ranging from 394 to 1467 Pa), the temperature discontinuity across the interface exists in all experimental conditions. The magnitude of the temperature discontinuity is strongly affected by the vapor pressure. A uniform temperature layer with a thickness of about 2 mm is found below the evaporating interface because of the coupling effect of evaporation cooling and thermocapillary convection. The energy required for evaporation is mainly transferred by thermocapillary convection in the uniform temperature layer. Furthermore, the numerical simulation results confirm that the evaporation flux near the cylinders is much larger than that at the middle region, which implies that most of the latent heat required for evaporation is transferred to the interface near the cylinders.

[Expression of androgen receptor in breast carcinoma and its relationship with estrogen receptor, progesterone receptor and HER2 status].

OBJECTIVE: to investigate the expression of androgen receptor (AR) in breast carcinoma and its relationship with estrogen receptor (ER), progesterone receptor (PR) and HER2 status, and to discuss its potential as treatment target. METHODS: immunohistochemical method was used to detect AR, ER, PR and HER2 expression in 175 cases of invasive ductal carcinoma of breast, which were divided into four groups: luminal A, luminal B, HER2(-) overexpression and triple negative group. RESULTS: eighty-eight cases (50.3%) were AR positive in 175 cases, the expression of AR was positively correlated with ER, PR and HER2 status. All the cases were grouped as follows: 53 cases (30.3%) were luminal A, 33 cases (18.9%) were luminal B, 23 cases (13.1%) were HER2(-) overexpression and 66 cases (37.7%) were triple negative, the AR expression rate was 56.6% (30/53), 75.8% (25/33), 47.8% (11/23), 33.3% (22/66), respectively. There was significant difference among the four groups' AR expression rates. With respect to the clinico-pathological features, AR positive cases were younger in luminal A and had lower mitosis rate in triple negative subgroups than the negative cases (χ(2) = 4.567, P = 0.033; χ(2) = 5.140, P = 0.023, respectively). CONCLUSION: AR has a high positive rate in breast carcinoma, and may be an ideal therapeutic target for breast carcinoma, especially for the triple negative subtype.

Structural characterization and pharmacological assessment in vitro/in vivo of a new copper(II)-based derivative of enrofloxacin.

Enrofloxacin (EFX) was selected as the medicinal ligand to afford a new copper(ii)-based complex, EFX-Cu, which was structurally characterized by spectroscopic analyses including X-ray single crystal diffraction. It was also stable and could retain the coordination state in aqueous solution. The in vitro antibacterial activity of EFX-Cu against a panel of pathogenic bacteria was about the same as that of EFX, except that it was twice as active against E. coli. The in vivo test on mice gave a LD50 value of 8148 mg kg-1 for EFX-Cu, which was much lower than those for EFX (LD50, 5312 mg kg-1) and its clinically used sodium salt, EFX-Na (LD50, 1421 mg kg-1). In addition, no obvious lesions in the organs of the dead mice were found by histopathological examination. Pharmacokinetic studies on rats suggested similar pharmacokinetics between EFX-Cu and EFX. On the other hand, EFX-Cu showed higher acute toxicity than EFX-Na in zebrafish, which was inconsistent with that in mice. The ROS-related inflammation and anti-inflammatory assay of EFX-Cu, respectively, in normal cells and zebrafish could be ascribed to its ROS-related redox property. Unfortunately, the final in vivo therapeutic assay in the E. coli-infected mouse model indicated that the therapeutic effect of EFX-Cu, mainly in terms of mortality in mice, was found to be lower than that of EFX-Na at the same dosage (800 mg kg-1, continuous gavage), although the contradictory factors between toxicity and antibacterial activity could not be excluded in this trial.

A new calcium(II) complex of marbofloxacin showing much lower acute toxicity with retained antibacterial activity.

Marbofloxacin (MB) is a newly developed veterinary drug with broad-spectrum antibacterial activity. In this study, a new calcium(II)-based complex of marbofloxacin, MB-Ca, was synthesized and structurally characterized by IR, ESI-MS, UV-Vis and single crystal X-ray diffraction analysis. The characterization of this complex in solution state indicated that the coordinated MB-Ca was partly retained, along with the monomeric and dimeric forms of MB. It also showed satisfactory water solubility (1.89 mg/mL), comparing with MB (2.82 mg/mL) at 35 °C. The in vitro antibacterial activity of MB-Ca was also screened towards a series of typical pathogenic bacteria, and determined by the methods of turbidimetry and disc diffusion. The results indicated it showed comparable antibacterial activity to MB. However, it exhibited higher inhibitive ability in vitro on DNA gyrase than MB alone. Furthermore, MB-Ca showed significantly lower acute toxicity (LD50, 3186 mg/kg) than MB (LD50, 1294 mg/kg) in mice, based on the in vivo acute toxicity test. The histopathological examination on the major organs of the mice by the oral administration of MB-Ca did not show obvious organic lesions, which is similar to those treated by MB. The research results suggest that MB-Ca could be further developed into a new promising metal-based veterinary drug and a better substitute of MB, showing unabated antibacterial activity along with lower toxicity.

[Effect of minimally invasive anterior lateral approach for total hip arthroplasty on serum type I collagen propeptide, tartrate-resistant acid phosphatase 5b and hip joint function in patients with femoral neck fracture].

OBJECTIVE: To analyze the level of serum N-terminal propeptide of type I precollagen (PINP) and tartrate resistant acid phosphatase 5b(TRACP-5b) in patients with femoral neck fracture(FNF) after minimally invasive anterior lateral approach with total hip arthroplasty and the effects of hip function. METHODS: From September 2016 to May 2017, 98 cases of femoral neck fracture were divided into control group and observation group, 49 cases in each group. There were 49 patients in control group, including 30 males and 19 females, ranging in age from 63 to 72 years old, who underwent minimally invasive anterolateral total hip arthroplasty. There were 49 patients in observation group, including 29 males and 20 females, ranging in age from 62 to 73 years old, who underwent minimally invasive anterolateral total hip arthroplasty. The perioperative conditions(operation time, bleeding volume, incision length, hospitalization time), bone metabolism indexes including PINP, TRACP-5b, fibroblast growth factor(FGF), bone gla-protein(BGP), propetide carboxy-terminal procollagen (PICP), bone-specific alkaline phosphatase(BAP), and pain mediators such as prostaglandin E2 (PGE2) and 5-hydroxytrytamine (5-HT) levels were compared between the two groups. The hip joint function and complications were evaluated. RESULTS: The operation time of the observation group was longer than that of the control group(P<0.05); there was no significant difference in bleeding volume, incision length and hospitalization time between two groups(P>0.05). PINP, fibroblast growth factor, BGP, PICP and BAP in observation group were higher than those in control group 1 month after operation, and TRACP-5b was lower than those in control group(P<0.05); PGE2 and 5-HT in observation group 1 month after operation were lower than those before operation, and lower than those in control group(P<0.05). The excellent and good rate of hip function in observation group was higher than that in control group (P<0.05), and the incidence of complications was not significantly different from that in the control group (P>0.05). CONCLUSIONS: Minimally invasive anterolateral approach total hip arthroplasty is safe and reliable, and can improve hip function, improve bone metabolism, promote fracture healing, alleviate pain in patients with femoral neck fracture, which is worthy of promotion.

Three hierarchical porous magnesium borate microspheres: a serial preparation strategy, growth mechanism and excellent adsorption behavior for Congo red.

The 3D hierarchical porous 7MgO·2B2O3·7H2O (MBH) microspheres were prepared by a phase transformation of chloropinnoite firstly, and anhydrous α-3MgO·B2O3 (MBA) microspheres were obtained by thermal conversion of 7MgO·2B2O3·7H2O, and then ß-3MgO·B2O3 (MBB) microspheres were obtained by phase conversion of α-3MgO·B2O3. All samples were characterized by XRD, FT-IR, TG and SEM. The microsphere nanostructures with a hierarchical porous structure were assembled by nanosheets with a thickness of 20-30 nm, and the growth mechanisms were also proposed. By using N2 adsorption-desorption, the specific surface areas were measured as 103.62 m2 g-1 for MBH and 46.10 m2 g-1 for MBA. They exhibited excellent selective adsorption performance for Congo red (CR) with maximum adsorption capacities of 202.84 and 170.07 mg g-1 respectively, and the corresponding adsorption mechanisms were also investigated. The adsorption processes were well fitted with the pseudo-second-order rate equation and Langmuir adsorption model. In addition, the corresponding adsorption thermodynamic parameters were also calculated. It is necessary to highlight that the hierarchical porous microspheres could be considered as promising candidates for removal of CR dye pollutants.

Optimal timing of staged percutaneous coronary intervention in ST-segment elevation myocardial infarction patients with multivessel disease.

BACKGROUND: Studies have shown that staged percutaneous coronary intervention (PCI) for non-culprit lesions is beneficial for prognosis of ST-segment elevation myocardial infarction (STEMI) patients with multivessel disease. However, the optimal timing of staged revascularization is still controversial. This study aimed to find the optimal timing of staged revascularization. METHODS: A total of 428 STEMI patients with multivessel disease who underwent primary PCI and staged PCI were included. According to the time interval between primary and staged PCI, patients were divided into three groups (≤ 1 week, 1-2 weeks, and 2-12 weeks after primary PCI). The primary endpoint was major adverse cardiovascular events (MACE), a composite of all-cause death, non-fatal re-infarction, repeat revascularization, and stroke. Cox regression model was used to assess the association between staged PCI timing and risk of MACE. RESULTS: During the follow-up, 119 participants had MACEs. There was statistical difference in MACE incidence among the three groups (≤ 1 week: 23.0%; 1-2 weeks: 33.0%; 2-12 weeks: 40.0%; P = 0.001). In the multivariable adjustment model, the timing interval of staged PCI ≤ 1 week and 1-2 weeks were both significantly associated with a lower risk of MACE [hazard ratio (HR): 0.40, 95% confidence intervals (CI): 0.24-0.65; HR: 0.54, 95% CI: 0.31-0.93, respectively], mainly attributed to a lower risk of repeat revascularization (HR: 0.41, 95% CI: 0.24-0.70; HR: 0.36, 95% CI: 0.18-0.7), compared with a strategy of 2-12 weeks later of primary PCI. CONCLUSIONS: The optimal timing of staged PCI for non-culprit vessels should be within two weeks after primary PCI for STEMI patients.

Histochemical studies on intestinal metaplasia adjacent to gastric cardia adenocarcinoma in subjects at high-incidence area in Henan, north China.

AIM: To characterize the histochemical type and pattern of intestinal metaplasia (IM) adjacent to gastric cardia adenocarcinoma (GCA) and distal gastric cancer (GC) in Linzhou, Henan Province, China. METHODS: Alcian-blue-periodic acid Schiff and high iron diamine-Alcian blue histochemical methods were performed on 142 cases of IM, including 49 cases of GCA and 93 cases of GC. All the patients were from Linzhou, Henan Province, China, the highest incidence area for both GCA and squamous cell carcinoma. Radio- or chemotherapy was not applied to these patients before surgery. RESULTS: The detection rate of IM in tissues adjacent to GCA tissues was 44.9%, which was significantly lower than that in GC tissues (80.64%, P<0.01). The rates of both incomplete small intestinal and colonic IM types identified by histochemistry in GCA tissues (31.82% and 63.64%, respectively) were significantly higher than those in GC (5.33% and 21.33%, respectively, P<0.01). CONCLUSION: IM in GCA and GC should be considered as a separate entity. Further research is needed to evaluate whether neoplastic progression of IM is related to its mucin profile in GCA.

[Influence of moxibustion of baihui (GV 20) on hemodynamics of common carotid artery in healthy subjects].

OBJECTIVE: To observe the effect of moxibustion of Baihui (GV 20) on the hemodynamics of internal carotid artery in health subjects so as to study its underlying mechanism of moxibustion in the treatment cerebrovascular disorders. METHODS: Thirty healthy male volunteer students between 20 and 22 years in age were enrolled into this study. Qm (mean blood flow), Vm) (mean velocity of blood flow), Vmax (maximal velocity of blood flow), Vmin (minimal velocity of blood flow), Wv (pulse wave velocity), Zcv (characteristic impedance), Rv (peripheral resistance), DR (dynamic resistance), CP (critical pressure) and DP (difference of pressure) of the right and left common carotid arteries were measured before and after moxibustion of GV20 (5-10 min each time, once daily, 5 times altogether) by using CBA CV-300 Cerebrovascular Hemodynamics Detector. RESULTS: Following moxibustion of GV20, Qm, Vm and Vmin of both right and left common carotid arteries increased significantly (P < 0.01); while Rv and DR of the brain artery lowed evidently (P < 0.05); The rest indexes had no significant changes (P > 0.05). CONCLUSION: Moxibustion of Baihui (GV 20) can significantly raise the velocity of blood flow of the common carotid artery and low the resistance of blood vessels.