Design and Synthesis of Disodium Phosphate Derivatives of Norcantharidin

Aim To design and synthesize norcantharidin disodium phosphate derivatives. Methotis Diels-Alder reaction between furan and maleic anhydride afforded dehydronorcantharidin, and subsequent hydrogenation, phosphorylation, and basification gave compounds 1 and 2, separately. Resuits The structures of compounds were confirmed by IR, NMR and FAB-MS. The aqueous solubility of 1 and 2 were improved, compared with the parent compounds, and their activities were more potent than norcantharidin 4 against MGCS03 cell lines. Conclusion The phosphorylation of norcantharidin analogues is an effective way to increase the activity and solubility.

Inhibiting Effect of Lobenzarit Disodium on the Inter-leukin-1 Activity in Normal and in Adjuvant ArthritisKats and on the H_2O_2 Release from Rat Peritoneal Macro-phages

The effects of Lobenzarit disodium (CCA) upon the activity of interleukin-1(IL-1) of peritoneal macrophages(PMΦ)in normal and in adjuvant arthritis AA) rats and on the release of hydrogen peroxide(H_2O_2)of rat peritoneal macrophages were studied. CCA 10～200 μg/ml could inhibit IL-1activity in normal rat in vitro;CCA 10 and 50 mg/kg could depress the level of increased IL-1 in AA rats in vivo;CCA 5～100μg/ml could inhibit the release of H_2O_2 from rat PMΦin vitro.The results suggest that these effects could be one of the mechanisms of anti-inflammatory action of CCA.

Transcriptome analysis of the effect of pyrroloquinoline quinone disodium（PQQ·Na2） on reproductive performance in sows during gestation and lactation

Background: Pyrroloquinoline quinone(PQQ), which is a water soluble, thermo-stable triglyceride-quinone, is widely distributed in nature and characterized as a mammalian vitamin-like redox cofactor. The objective of this study was to investigate the effects of pyrroloquinoline quinone disodium(PQQ·Na2) on reproductive performance in sows.Results: Dietary supplementation with PQQ·Na2 significantly increased the total number of piglets born, the number of piglets born alive and the born alive litter weight. It also increased the antioxidant status in the placenta, plasma and milk. The concentration of NO was significantly increased in the plasma and placenta. RNA-seq analysis showed that462 unigenes were differentially expressed between the control(Con) treatment and PQQ treatment groups.Among these unigenes, 199 were upregulated, while 263 unigenes were downregulated. The assigned functions of the unigenes covered a broad range of GO categories. Reproduction(27, 7.03%) and the reproduction process(27, 7.03%) were assigned to the biological process category. By matching DEGs to the KEGG database, we identified 29 pathways.Conclusions: In conclusion, dietary supplementation with PQQ·Na2 in gestating and lactating sows had positive effects on their reproductive performance.

Depressing behaviors and mechanism of disodium bis(carboxymethyl) trithiocarbonate on separation of chalcopyrite and molybdenite

This work focuses on the organic depressant,disodium bis(carboxymethyl)trithiocarbonate(DBT),as a selectivedepressant in copper?molybdenum sulfide flotation separation.Micro-flotation,Zeta potential,FTIR and XPS measurements werecarried out to investigate the selective depression mechanism of DBT on chalcopyrite.Zeta potential and FTIR measurementsrevealed that DBT had higher affinity for chalcopyrite than molybdenite and the XPS results of chalcopyrite before and aftertreatment with DBT further proved that DBT adsorbed on chalcopyrite surface.The investigation indicates that the mechanism ofDBT adsorbing on chalcopyrite is mainly physical adsorption.Locked circuit experiments were carried out and the results showedthat DBT could be considered as a cleaner option in commercial Cu?Mo flotation separation circuits.

Electroacupuncture improves neuropathic pain Adenosine, adenosine 5'-triphosphate disodium and their receptors perhaps change simultaneously

Applying a stimulating current to acupoints through acupuncture needles–known as electroacupuncture–has the potential to produce analgesic effects in human subjects and experimental animals. When acupuncture was applied in a rat model, adenosine 5-triphosphate disodium in the extracellular space was broken down into adenosine, which in turn inhibited pain transmission by means of an adenosine A1 receptor-dependent process. Direct injection of an adenosine A1 receptor agonist enhanced the analgesic effect of acupuncture. The analgesic effect of acupuncture appears to be mediated by activation of A1 receptors located on ascending nerves. In neuropathic pain, there is upregulation of P2X purinoceptor 3 （P2X3） receptor expression in dorsal root ganglion neurons. Conversely, the onset of mechanical hyperalgesia was diminished and established hyperalgesia was significantly reversed when P2X3 receptor expression was downregulated. The pathways upon which electroacupuncture appear to act are interwoven with pain pathways, and electroacupuncture stimuli converge with impulses originating from painful areas. Electroacupuncture may act via purinergic A1 and P2X3 receptors simultaneously to induce an analgesic effect on neuropathic pain.

A Simple and Sensitive Liquid Chromatographic Technique for the Determination of Cefotetan Disodium in Human Plasma and Its Application in a Pharmacokinetic Study

A simple and sensitive liquid chromatographic method was developed for quantification of cefotetan disodium (CTT),a semi-synthetic cephamycin antibiotic,in human plasma.CTT and the internal standard chloramphenicol were extracted from plasma by a simple one-step protein precipitation with 35% (v/v) perchloric acid.Separation was carried out on a reverse-phase C18 column with a mobile phase of acetonitile-water containing 0.5% (v/v) phosphoric acids (20:80,v/v) at a flow rate of 1.0 mL/min.The column effluent was monitored by UV detection at 300 nm.The column temperature was maintained at 40°C.This method demonstrated good linearity in the range of 0.525-300.0 μg/mL,with correlation coefficients greater than 0.99.The limit of quantification (LOQ) was 0.525 μg/mL in human plasma.Intra-and inter-day precisions were less than 6.63% in terms of relative standard deviation (RSD).The accuracy,when expressed by the bias,ranged from 0.57% to 4.04%.The mean extraction recovery of CTT was higher than 40.94%.The method was found to be precise,accurate,and specific for CTT quantitative analysis,and was successfully applied for a pharmacokinetic study of CTT after a single intravenous dose of 1.0 g of CTT in healthy Chinese subjects.

Effect of dietary supplementation of pyrroloquinoline quinone disodium on growth performance, meat quality and antioxidative ability of broilers

This study was conducted to investigate the effect of dietary supplementation with pyrroloquinoline quinone(PQQ) in the form of PQQ disodium(PQQ·Na2) on the growth performance, carcass traits, meat quality and antioxidative ability of broilers. A total of 720 one-d-old Arbor Acres male broilers were randomly allocated to 1 of 6 treatments with 8 replicates of 15 birds per replicate in a completely randomized design. Birds were fed a PQQ·Na2-unsupplemented corn-soybean meal basal diet(control) or the basal diet supplemented with 0.1, 0.2, 0.3, 0.4 or 0.5 mg PQQ·Na2 kg-1 for 42 d. Compared with the control chicks, the chicks fed the diets supplemented with PQQ·Na2 had lower(P<0.05) feed:gain(F/G) during the grower phase and drip losses of breast muscles on day 42. As supplemental PQQ·Na2 level increased, plasma total antioxidant capacity(T-AOC) on d 42, liver T-AOC on d 21 and heart T-AOC on d 21 and 42 increased linearly(P<0.05), but malondialdehyde concentrations in plasma, liver and heart on d 21 or 42 decreased linearly(P<0.001) or quadratically(P<0.005). The results from the present study indicate that dietary supplemental PQQ·Na2 can improve antioxidant ability and meat quality of broilers, and in general, it is implied that the optimal supplemental PQQ·Na2 level is 0.1 mg kg-1 of diet for broilers from 1 to 42 d of age.

Transformation of microstructure and phase of disodium guanosine 5′-monophosphate: Thermodynamic perspectives

Microstructure and phase transformation of disodium guanosine 5′-monophosphate(5′-GMPNa_2) are extremely important for controlling the process and understanding the mechanism of crystallization. In this work, the thermodynamic properties of polymorphous 5′-GMPNa_2 especially the solubility were studied, the solubility results show that 5′-GMPNa_2 is more soluble in ethanol–water(E–W) than in isopropanol–water(I–W). The amorphous form of 5′-GMPNa_2 is more soluble than the crystalline form at the same mole fraction and temperature. Meanwhile, the crystalline forms and morphologies of the residual solids were characterized by PXRD and SEM. The results indicate that solid forms of 5′-GMPNa_2 transformed spontaneously from amorphous to crystalline when the ethanol proportion is ≥20%. In addition, increasing the pH facilitates the dissolution of 5′-GMPNa_2 and helps to maintain the crystalline form. The associated Gibbs free energy values were calculated to verify the trend of transformation from amorphous to crystalline 5′-GMPNa_2. These results should help to guide the industrial crystallization process and to obtain the crystalline form of 5′-GMPNa_2.

Synthesis, Crystal Structure and Magnetic Property of Disodium Biscarbonato cobaltate(Ⅱ) Tetrahydrate, Na_2Co(CO_3)_2·4H_2O

The title compound, Na 2Co(CO 3) 2·4H 2O, was synthesized by dropwise addition of 1.0 mL of 1 mol/L Co(CH 3COO) 2 to 50 mL of aqueous solution containing 7.0 g(66.0 mmol) of Na 2CO 3 and 2.5 g(29.8 mmol) of NaHCO 3 under stirring. A rose colored rhombohedral crystal grew by the slow evaporation of the solution of the title compoud at room temperature. The crystal structure was established on the basis of the single crystal X ray diffraction data. Na 2Co(CO 3) 2·4H 2O crystallizes in the monoclinic space group C2/c with a =0.856 6(1) nm, b =0.714 6(1) nm, c = 1 438 7(2) nm, β =97.59(1)° , V =0.873 0(2) nm 3 , D x=2.260 g/cm 3, F (000)=596, M r=296 99, μ (Mo K α)=21.06 cm -1 , Z =4 and the final R(F) =0.032 and wR(F 2) =0.068 on the basis of 947 reflections ( F 2 ≥ 2σ(F 0 2)). The crystal consists of H 2O molecules, Na + ions and 2D 2 ∞[Co(CO 3) 2] 2- layers extending parallel to (001). H 2O molecules and Na + cations are located between the 2D layers. Each Co atom is tetrahedrally coordinated by four O atoms from four CO 2- 3 groups with d (Co\_O)=0.206 5(2) nm, 0.207 6(2) nm and the angle of O\_Co\_O is in the range of 97.7(1)°—128.5(1)°. The CO 2- 3 group bridging two Co atoms via two O atoms deviates from D 3h symmetry with d (C\_O)=0.127 2(3)\_0.129 9(3) nm and the angle of O\_C\_O is in the range of 119.5(2)°\_123.4(2)°. Each Na atom, with two close Na neighbours at 0.338 4(2) nm and 0 346 7(2) nm, respectively, is octahedrally coordinated by six O atoms from four H 2O molecules and two carbonate groups belonging to two layers with d (Na\_O)=0.232 7(2)\_0.241 1(2) nm. Of two crystallographically different H 2O molecules, one forms hydrogen bonds to two CO 3 2- groups of one 2D layer, and the other to those from two different 2D layers. Na 2Co(CO 3) 2·4H 2O is antiferromagnetic below 16 K, and between 30\_300 K its magnetic behaviour obeys Curie Weiss law χ m(cm 3·mol -1 )=2.625/( T -12.1) with μ eff =4.5 B.M. at 298 K.

Long-term Efficacy and Safety of Pamidronate Disodium in Treatment of Bone Metastases in Breast Cancer

Objective： To evaluate the long-term efficacy and safety of pamidronate disodium in patients with bone lesions secondary to advanced breast carcinoma. Methods： A retrospective chart review was conducted of 62 patients receiving intravenous pamidronate disodium for metastatic breast cancer. The proportion of patients experiencing at least one skeletal related event （SRE） after 12 months of therapy was determined. Results： The proportion of patients who had an SRE was 29.00% （18 individuals） and the median time to first event was greater than 350 days. Radiotherapy（ll individuals）and pathologic fracture（6 individuals）were the most frequent type of SRE, while cord compression（1 individuals） and hypercalcaemia（0 individuals） were rare. A total of 37 individuals had transient hypocalcaemia without any clinical symptom. No significant creatinine abnormalities were encountered. There were no clinically relevant changes of calcium ,phosphate and creatinine before and after therapy. Conclusion： Long-term treatment with pamidronate disodium significantly reduces and delays skeletal morbidity from osteolytic metastases . Prolonged therapy was well tolerated. This study suggests that the rate of clinically relevant SREs is substantially lower than the event rate observed in phase llI clinical trials.

FDA批准Alimta(pemetrexed disodium)与顺铂联用治疗恶性胸膜间皮瘤(一种罕见的癌症)

FDA批准Alimta(pemetrexed disodium)与顺铂联用治疗恶性胸膜间皮瘤(一种罕见的癌症)Alimta早先已被FDA指定为治疗此罕见病用药,它也是得到FDA批准的第一种治疗此症的药物。

培美曲唑 Pemetrexed disodium

商品名：Alimta 化学式：C20H19N5Na2O6·7H2O 化学名：Glutamicacid，N-[4-[2-amino-4，7-dihydm-4-8oxo-1H-pyrmlo[2，3-d]pyrimidin-5-y1]ethyl]benzoy]-，disodiumsalt，heptahydrate LAS：150399-23-8化学结构：别名：LY231514，MTA 相对分子质量：597．46 类别：抗肿瘤药 开发单位：礼莱公司(Lilly)上市国家：美国 作用机制：胸苷酸合酶(Thymidylate synthase)／二氢叶酸还原酶双重抑制剂，抗代谢类抗癌药。

Efficacy of Danshen Injection Combined with Phosphocreatine Disodium in Treating Frequent Premature Contractions during Pregnancy and Its Effects on Maternal and Infant Outcomes

[Objectives]To explore the efficacy of Danshen Injection combined with phosphocreatine disodium in treating frequent premature contractions during pregnancy and its effect on maternal and infant outcomes.[Methods]A total of 200 pregnant women with normal pregnancy and frequent premature contractions who were treated in the outpatient department of internal medicine in Women and Children's Hospital of Hubei Province and Xinzhou District People's Hospital of Wuhan Central Hospital during September 2015 and October 2018 were selected and randomly divided into the control group and observation group,100 cases for each group.The observation group was treated with Danshen Injection combined with phosphocreatine disodium,and the control group was treated with phosphocreatine disodium alone.The course of treatment in both groups was one week.During the treatment,the changes of heart rate,heart rhythm,electrocardiogram and 24-h dynamic electrocardiogram(DCG)of both groups were observed.[Results]After treatment,the clinical efficacy of the observation group was better than that of the control group,and the difference was statistically significant(P<0.01).There were no adverse drug reactions in both groups.However,in the control group,non-sustained ventricular tachycardia(NSVT)was found in 24-h dynamic electrocardiogram(DCG)of 2 pregnant women with premature ventricular contraction.The pregnancy process was smooth,with full-term natural delivery and no fetal malformation.There was no significant difference in gestational age and neonatal weight between the two groups(P>0.05).However,there was a statistically significant difference in Apgar score between the two groups(P<0.05).During the 6-month postpartum follow-up,the mother and child were unharmed,and examination of repeated electrocardiograms showed that the conditions were normal.[Conclusions]Danshen Injection combined with phosphocreatine disodium has better efficacy in the treatment of frequent premature contractions during pregnancy and the maternal and infant outcomes than the treatment with phosphocreatine disodium alone,and it has good safety and can prevent premature contractions from progressing to tachyarrhythmias.

Effects of Desloratadine Citrate Disodium combined with Budesonide suspension on serum IgE, EOS and inflammatory factors in patients with CRS after endoscopic sinus surgery

Objective: To observe the clinical application of Desloratadine Citrate Disodium combined with Budesonide suspension in patients with chronic rhinosinusitis CRS after endoscopic sinus surgery, and analyze the change of serum immunoglobulin E (IgE), eosinophils (EOS) and inflammatory factors level in patients. Method: A total of 90 cases of patients with CRS were randomly divided into control group (n=45) and observation group (n=45) according to the lottery method. Both groups were treated with endoscopic sinus surgery. On the basis of this, control group was given Budesonide suspension and observation group was treated with Desloratadine Citrate Disodium combined with Budesonide suspension. The change of serum IgE, EOS and inflammatory factors were measured before and after operation in all subjects. Results: There was no significant difference in IgE and EOS levels between control group and observation group before treatment. After treatment, the levels of serum IgE and EOS in the two groups were significantly lower than those before treatment. Moreover, after treatment, observation group was lower than control group, and the difference was significant. There was no significant difference in inflammatory factors level between control group and observation group before treatment. After treatment, the levels of serum IL-6, IL-8, TNF-α and hs-CRP were significantly lower than those before treatment. After treatment, observation group was lower than the control group in the same period, the difference was significant. Conclusion:Combined Desloratadine Citrate Disodium treatment for CRS patients on the basis of endoscopic sinus surgery and Budesonide Nasal Spray treatment, it can more effectively reduce serum IgE and EOS levels, decrease the inflammatory response. Therefore it was a potential effective treatment for patients with CRS.

In situ tracking of the lithiation and sodiation process of disodium terephthalate as anodes for rechargeable batteries by Raman spectroscopy

Organic compounds represent an appealing group of electrode materials for rechargeable batteries due to their merits of biomass,sustainability,environmental friendliness,and processability.Disodium terephthalate(Na_(2)C_(8)H_(4)O_(4),Na_(2)TP),an organic salt with a theoretical capacity of 255 mAh·g^(-1),is electroactive towards both lithium and sodium.However,its electrochemical energy storage(EES)process has not been directly observed via in situ characterization techniques and the underlying mechanisms are still under debate.Herein,in situ Raman spectroscopy was employed to track the de/lithiation and de/sodiation processes of Na2TP.The appearance and then disappearance of the–COOLi Raman band at 1625 cm^(-1) during the de/lithiation,and the increase and then decrease of the–COONa Raman band at 1615 cm^(-1) during the de/sodiation processes of Na2TP elucidate the one-step with the 2Li+or 2Na+transfer mechanism.We also found that the inferior cycling stability of Na2TP as an anode for sodium-ion batteries(SIBs)than lithium-ion batteries(LIBs)could be due to the larger ion radium of Na+than Li+,which results in larger steric resistance and polarization during EES.The Na2TP,therefore,shows greater changes in spectra during de/sodiation than de/lithiation.We expect that our findings could provide a reference for the rational design of organic compounds for EES.

Kinetic study of complicated anti-solvent and cooling crystallization of disodium 5′-ribonucleotide

Disodium 5′-ribonucleotide,which is composed of disodium 5′-inosine(IMP)and disodium 5′-guanosine(GMP),is an important food additive.The lack of kinetic studies of it causes a lack of clarity in understanding the complicated multi-solute crystallization of IMP+GMP in ethanol-water.In this work,process analytical technology tools were used to obtain the thermodynamics and kinetic data from the experiments,the kinetic parameters of anti-solvent and cooling crystallization were investigated.The crystal form of IMP+GMP mixed crystal was determined,which was consistent with the IMP whether crystallized from pure water or ethanol-water.The effects of different anti-solvent addition rates and cooling rates on the metastable zone widths were studied,and the opposite effect on metastable zone width was found.The modified exponential empirical function was developed to correlate nucleation and growth kinetic equations under different conditions.The kinetic data were well fitted with adjusted correlation coefficient(adj-R^(2)>0.7),which is sufficient to provide a valid reference for process design and control.

类风湿性关节炎治疗药Fostamatinib disodium

脾酪氨酸激酶（spleen tyrosine kinase,SYK）为一种非受体型酪氨酸蛋白激酶,具有广泛的生物活性,其在免疫细胞的成熟和激活中发挥着重要作用,

镉污染土壤淋洗修复技术研究

采用振荡淋洗法处理Cd污染土壤。考察了不同淋洗剂对污染土壤中Cd的去除效果,以及淋洗剂浓度、淋洗剂pH、淋洗剂体积与土壤质量比(液土比)等条件对淋洗效果的影响。采用Tessier分步提取法对淋洗前后的Cd形态分布进行分析,并对淋洗废液的再生利用情况进行了研究。实验结果表明:乙二胺四乙酸二钠(EDTANa_(2))是高效的Cd污染土壤淋洗剂,当EDTA-Na_(2)浓度为0.03 mol/L、淋洗剂pH为3、液土比为4:1时,Cd去除率可达73.27%;土壤中Cd的主要去除形态为可交换态;采用新型二硫代羧酸功能化树枝状聚合物(DPETACSSNa)对淋洗废液进行再生,再生后淋洗液的Cd去除性能基本不变。

甲磺酸奥希替尼联合常规培美曲塞二钠加卡铂化疗方法治疗晚期非小细胞肺癌的临床效果分析

目的探讨甲磺酸奥希替尼联合常规培美曲塞二钠加卡铂化疗方法治疗晚期非小细胞肺癌(NSCLC)的临床效果。方法选取2018年10月至2023年1月首都医科大学宣武医院收治的105例晚期NSCLC患者为研究对象。依照随机数字表法分为对照组(52例)和观察组(53例)。对照组给予培美曲塞二钠加卡铂化疗,观察组在对照组基础上给予甲磺酸奥希替尼治疗,3周为1个疗程,2组均连续治疗2个疗程。治疗后进行疾病控制率评价,比较2组治疗前后的Karnofsky功能状态(KPS)评分、CD_(3)^(+)、CD_(4)^(+)水平、CD_(4)^(+)/CD_(8)^(+)比值及细胞角蛋白19片段(CYFRA21-1)、癌胚抗原、胸苷激酶1水平及治疗期间不良反应发生率。结果观察组疾病控制率高于对照组[83.0%(44/53)比65.4%(34/52)],差异有统计学意义(P<0.05)。治疗后观察组KPS评分高于对照组[(76±6)分比(64±6)分];观察组CD_(3)^(+)、CD_(4)^(+)水平及CD_(4)^(+)/CD_(8)^(+)比值高于治疗前且高于对照组;2组CYFRA21-1、癌胚抗原、胸苷激酶1水平均低于治疗前且观察组低于对照组,差异均有统计学意义(均P<0.05)。治疗期间,观察组与对照组不良反应发生率差异无统计学意义[13.2%(7/53)比9.6%(5/52)](P>0.05)。结论甲磺酸奥希替尼联合常规培美曲塞二钠加卡铂化疗方法治疗晚期NSCLC的临床效果较好,有助于患者生活质量和免疫功能的提高,且具有较好的安全性。