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Storage energy is an effective means and key technology for overcoming the intermittency and instability of photovoltaic (PV) power. In the early stages of the PV and energy storage (ES) industries, economic efficiency is highly dependent on industrial policies. This study analyzes the key points of policies on technical support, management drive, and financial support. Focusing on the efficiency of PV power and the power load of users, including households and enterprises, in Shanghai City over 24 h in 2016, this study analyzes the costs, benefits, internal rates of return, and investment recovery periods of distributed PV (DPV) and ES systems in the current policy context. This study also discusses the influences of various policy variables, including the ES battery capacity, the peak-valley price ratio, feed-in tariffs for DPV, and the ratio of grid-connected surplus PV power, on economic efficiency. The results show that in China's current policy context, both household and enterprise users of PV power would gain some economic benefits if PV systems were fitted with aqueous sodium-ion batteries of an appropriate capacity. Finally, this study offers some additional government policy suggestions. [ABSTRACT FROM AUTHOR]

Bone marrow transplantation is regarded as the most effective immunotherapy for hematologic cancer, but it generally faces difficulties in matching. Aberrant expression of histone deacetylases (HDACs) is closely related to the occurrence and development of hematological cancer. Recent studies suggested that HDACs might play a critical role in initiating anti-cancer immune response or enhancing anti-cancer immunotherapy. Besides, combining HDAC inhibition and immunotherapy could prevent immunotherapy resistance in some degree and reach an extended treatment window. This review summarized the relationship between HDACs and immune and described the current understanding of HDACs in immunotherapy for hematologic cancer. HDACs may play a critical role in initiating anti-tumor immune response or enhancing anti-cancer immunotherapy. Combining HDACI and immunotherapy can prevent immunotherapy resistance in some degree and reach an extended treatment window. [Display omitted] •Targeting HDACs could initiate anti-tumor immune response in the hematologic cancer. •Targeting HDACs could enhance anti-tumor immunotherapy for hematologic cancer. •Combining HDACIs and immunotherapy could reach an extended treatment window. [ABSTRACT FROM AUTHOR]

Myocardial injury is a nonnegligible problem in cardiovascular diseases and cancer therapy. The functional feature of N-containing heterocycles in the cardiovascular field has attracted much attention in recent years. Herein, we discovered a lead compound 12a containing 1,3,4-oxadiazole by extensive screening of anticancer derivatives containing nitrogen-heterocycle, which exhibited potential protective activity against oxidative stress in cardiomyocytes. Follow-up structure-activity relationship (SAR) studies also highlighted the role of substitution sites and bisamide moiety in enhancing the protective activity against oxidative stress. Specifically, compound 12d exhibited low cytotoxicity under high concentration and potent myocardial protection against oxidative stress in H9c2 cells. Preliminary mechanistic studies showed compound 12d could decrease the expression of cardiac hypertrophy and oxidative stress-related proteins/genes and reduce mitochondria-mediated cell apoptosis, thereby enhancing the cell vitality of injured cardiomyocytes. In this study, 1,3,4-oxadiazole may represent a novel pharmacophore that possesses potential myocardial protection and provides more choices for future optimization of cardiovascular drugs, especially for the treatment of onco-cardiology. Compound 12d could decrease the expression of cardiac hypertrophy and oxidative stress-related proteins/genes and reduce mitochondria-mediated cell apoptosis, and thereby enhancing the cell vitality of injured cardiomyocytes. [Display omitted] • A series of novel 1,3,4-oxadiazole derivatives were designed and synthesized. • Representatively, 12d exhibited potent myocardial protection and low cytotoxicity. • 12d decreased the expression of hypertrophy and oxidative stress-related markers. • 12d could reduce mitochondria-mediated cell apoptosis. [ABSTRACT FROM AUTHOR]

Three new coordination polymers, [Zn(H 2 biim)(pzdc)] n ( 1 ), [Cd(H 2 biim)(pzdc)] n ( 2 ) and [Cd(H 2 biim) 0.5 (ip-OH)] n ( 3 ) (H 2 biim = 2,2′-biimidazolate, H 2 pzdc = 2,3-pyrazinedicarboxylic acid, H 2 ip-OH = 5-hydroxylisophthalic acid), have been hydrothermally synthesized and characterized by elemental analysis, infrared spectra and X-ray single-crystal diffraction. Complexes 1 and 2 are isostructural and display two-dimensional (2D) undulated layers with 3-connected (4.8 2 ) topologies, which are further extended into three-dimensional (3D) supramolecular structures through hydrogen-bonding and C–H⋯π interactions. Complex 3 is a relatively rare 3D compound, featuring a binodal (4,5)-connected (4 4 .6 2 )(4 4 .6 6 ) topology. A comparison of all the complexes demonstrates that the structural characteristics of the dicarboxylate ligands play a great role in the modulation of the coordination structures. Moreover, their luminescent properties and thermal stabilities were also investigated. [ABSTRACT FROM AUTHOR]

Six new coordination polymers, [CdCl 2 (bbim)] n ( 1 ), [ZnCl 2 (bbbm)] n ( 2 ), [ZnCl(HCOO)(bbbm)] n ( 3 ), [Cd(PhCOO) 2 (bbim)] n ( 4 ), [Cd(PhCOO) 2 (bbbm)] n ( 5 ), and {[Zn(ip-OH)(bbim)]·DMF} n ( 6 ) [bbim = 1,1′-(1,4-butanediyl)bis(2-methylbenzimidazole), bbbm = 1,1′-(1,4-butanediyl)bis(benzimidazole), H 2 ip-OH = 5-hydroxylisophthalic acid], have been prepared and characterized by elemental analysis, infrared spectra and X-ray single-crystal diffraction. Complexes 1 – 5 have one-dimensional (1D) chain structures. Complexes 1 , 3 and 4 possess similar 1D meso-helical chain structures, which are extended into 2D or 3D supramolecular network through intermolecular hydrogen-bonding, C–H⋯ π and π ⋯ π interactions. Complexes 2 and 5 exhibit similar 1D infinite helical chains. The 1D chains further form a three-dimensional (3D) supramolecular structure through intermolecular hydrogen-bonding and π ⋯ π interactions in 2 , but form a 2D supramolecular layer via C–H⋯ π interactions in 5 . Complex 6 possesses a 2D 4 4 -sql network. Furthermore, luminescent properties and thermal stabilities of 1 – 6 were also investigated. [ABSTRACT FROM AUTHOR]

This study was to analyze the pyrrolizidine alkaloids (PAs) in Eupatorium fortunei herbs and its derived finished products with a view to evaluating their effects on the proliferation and oligodendrogenesis of neural progenitor cells (NPCs). Using a LC-MS/MS method with 32 PAs reference standards, 8 PAs including intermedine, intermedine N-oxide, lycopsamine, lycopsamine N-oxide, retronecine, seneciphylline and senkirkine and 7-acetylintermedine N-oxide were identified with intermedine N-oxide and lycopsamine N-oxide being most abundant. The total PA amounts were found to vary from 0.18 to 61.81 μg/g in 30 batches of herbs and from 0.86 to 36.96 μg/g in 4 commercial finished products, respectively. Risk assessments indicated that the short-term intake seemed unlikely lead to acute toxic effects but the chronic use warranted cautions. Using NPCs derived from mouse induced pluripotent stem cells as an in vitro testing model, intermedine, intermedine N-oxide and lycopsamine N-oxide appeared to decrease cell viability at 30 μM whereas intermedine N-oxide inhibited oligodendrogenesis of NPCs at 10 μM. The present results suggested that the PAs in the majority of E. fortunei herbs and the derived products not only resulted in their exposure far exceeding the acceptable intake limit (i. e. 1.0 μg PA per day for adults) in herbal medicinal products recommended by the European Medicines Agency but also induced neurotoxicity to NPCs in vitro. • Eight PAs in Eupatorium fortunei herbs and finished products were identified. • Intermedine and lycopsamine N-oxides were the major PAs in Eupatorium fortunei. • The PA intakes from E. fortunei far exceeded the acceptable daily intake limit proposed by the EMA. • Intermedine and lycopsamine N-oxides were cytotoxic to neural progenitor cells. • Intermedine N-oxide impaired the oligodendrogenesis of neural progenitor cells. [ABSTRACT FROM AUTHOR]

• SME-1 improved in vitro release, cellular uptake, and transport. • SME-1 decreased the production of phase II metabolite, CSA-G. • Inhibitory SME-1resulted in significantly higher oral bioavailability. • Enhanced oral bioavailability attributed to the inhibition of glucuronidation. Cajaninstilbene acid (CSA) exerts wide pharmacological activities, such as anti-inflammation, hypoglycaemic activity, analgesic effect and cognition improvement. However, it underwent severe phase II metabolism mediated by UDP-glucuronosyltransferase (UGT) in the gastrointestinal (GI) tract after oral administration, affecting its oral bioavailability. In the present study, we utilize UGT inhibitory excipient containing self-microemulsion (SME) delivery system to reduce the production of glucuronide metabolites and increase its oral bioavailability. The present results showed that although similar properties in physiochemical, cytotoxicity, cellular uptake, absorption and transport across rat everted gut sacs between SME-1 (inhibitory excipient containing SME) and SME-2 (control SME, without inhibitory excipient), an improved absolute bioavailability of 57.3 % was conferred by SME-1, significantly higher than the value of 35.4 % by SME-2 and 34.0 % by free CSA. Noticeably, the significantly lower AUC value of CSA glucuronide was determined in rats treated with SME-1 than those either treated with SME-2 or free CSA. Thus, the ability of SME-1 to enhance oral bioavailability of CSA is mainly attributed to the inhibition of phase II metabolism in the GI tract. [ABSTRACT FROM AUTHOR]

Oxidized low density lipoprotein (oxLDL)-induced endothelial oxidative damage promotes the development of atherosclerosis. Caveolae play an essential role in maintaining the survival and function of vascular endothelial cell (VEC). It is reported that the long coiled-coil protein NECC2 is localized in caveolae and is associated with neural cell differentiation and adipocyte formation, but its role in VECs needs to be clarified. Our results showed NECC2 expression increased in the endothelium of plaque-loaded aortas and oxLDL-treated HUVECs. Down-regulation of NECC2 by NECC2 siRNA or compound YF-307 significantly inhibited oxLDL-induced VEC apoptosis and the adhesion factors expression. Remarkably, inhibition of NECC2 expression in the endothelium of apoE−/− mice by adeno-associated virus (AAV)-carrying NECC2 shRNA or compound YF-307 alleviated endothelium injury and restricted atherosclerosis development. The immunoprecipitation results confirmed that NECC2 interacted with Tyk2 and caveolin-1(Cav-1) in VECs, and NECC2 further promoted the phosphorylation of Cav-1 at Tyr14 b y activating Tyk2 phosphorylation. On the other hand, inhibiting NECC2 levels suppressed oxLDL-induced phosphorylation of Cav-1, uptake of oxLDL by VECs, accumulation of intracellular reactive oxygen species and activation of NF-κB. Our findings suggest that NECC2 may contribute to oxLDL-induced VEC injury and atherosclerosis via modulating Cav-1 phosphorylation through Tyk2. This work provides a new concept and drug target for treating atherosclerosis. [Display omitted] • Endothelial NECC2 promotes the development of atherosclerosis. • NECC2 contributes to oxLDL-induced endothelial oxidative damage. • NECC2-induced Cav-1 phosphorylation via Tyk2 promotes oxLDL accumulation in VECs. • Compound YF-307 inhibits endothelial oxidative damage and atherosclerosis. [ABSTRACT FROM AUTHOR]

Graphical abstract Abstract The pulmonary fate of inhaled poorly water-soluble drugs is not entirely clear. In this study, the main objective was to investigate the in vivo inhalation biopharmaceutics in the aspects of dissolution, mucociliary clearance, absorption and tissue binding using intratracheally administered budesonide and ciclesonide suspensions as model drugs. In doing so, this study first developed a method to differentiate between dissolved and undissolved ciclesonide in the lungs for evaluating in vivo dissolution. Following deposited in rat airways, the drug particles underwent rapid dissolution and mucociliary clearance, leading to the complete removal of drugs from the airways within 2 h and a limited absorption time less than 2 h. Upon dissolution, budesonide and ciclesonide were taken up and retained in the lung tissues for up to 12 h and 24 h, respectively. The in vivo dissolution profiles in the airways exhibited the sameness as the in vitro counterparts in a 0.5% sodium dodecyl sulfate solution as indicated by the similarity factor f2. The efficacy results in a lipopolysaccharide induced lung injury model showed that the duration of local anti-inflammatory was dependent on the drug levels in the lung tissues, but not on the in vitro/in vivo dissolution and plasma pharmacokinetics. The present results demonstrated that ciclesonide suspension has the potential to achieve once-daily dosing for nebulization therapy and the in vitro dissolution profile has limited usefulness in predicting in vitro–in vivo correlation. [ABSTRACT FROM AUTHOR]

The role of polysaccharides in quality control of ginseng is underestimated. Large-scale comparison on the polysaccharides of Panax ginseng (PG), P. quinquefolius (PQ), P. notoginseng (PN), Red ginseng (RG), P. japonicus (ZJS), and P. japonicus var. major (ZZS), was performed by both chemical and biological approaches. Holistic fingerprinting at polysaccharide and the hydrolyzed oligosaccharide and monosaccharide levels utilized various chromatography methods, while OGD and OGD/R models on H9c2 cells were introduced to evaluate the protective effects on cell viability and mitochondrial function. Polysaccharides from six ginseng species exhibited remarkable content difference (RG > PG/ZZS/ZJS/PQ > PN), but weak differentiations in molecular weight distribution and oligosaccharide profiles, while Glc and GalA were richer for monosaccharide compositions of PG and RG polysaccharides, respectively. RG polysaccharides (25/50/100 μg/mL) showed significant cardiomyocyte protection by regulating mitochondrial functions. These new evidences may provide support for the supplementary role of polysaccharides in quality control of ginseng. [Display omitted] • A large-scale comparison study on six ginseng polysaccharides was performed. • Polysaccharides fingerprinting and cardiomyocyte protection were investigated. • Six ginseng polysaccharides showed differentiations in contents and compositions. • Red ginseng polysaccharides could protect against OGD and OGD/R-induced • injury. • Polysaccharides exhibit potentials in quality control of ginseng aside from saponins. [ABSTRACT FROM AUTHOR]

Twenty-five novel pregnenolone/2-cyanoacryloyl conjugates ( 6 – 30 ) were designed and prepared, with the aim of developing novel anticancer drugs with dual NF-κB inhibitory and anti-proliferative activities. Compounds 22 and 27 – 30 showed inhibition against TNF-α-induced NF-κB activation in luciferase assay, which was confirmed by Western blotting. Among them, compound 30 showed potent NF-κB inhibitory activity (IC 50 = 2.5 μM) and anti-proliferative against MCF-7, A549, H157, and HL-60 cell lines (IC 50 = 6.5–36.2 μM). The present study indicated that pregnenolone/2-cyanoacryloyl conjugate I can server as a novel scaffold for developing NF-κB inhibitors and anti-proliferative agents in cancer chemotherapy. [ABSTRACT FROM AUTHOR]

Abstract: An efficient and rapid procedure for ring opening reaction of various epoxides with phenol and thiophenol derivatives was developed. The procedure can be obtained at room temperature under solvent-free condition in presence of (C4H12N2)2[BiCl6]Cl·H2O (1 mol %). This catalyst can be reused several times without significant loss of activity. [Copyright &y& Elsevier]

Abstract: An efficient and rapid procedure for ring opening of various epoxides with aromatic, aliphatic and heterocyclic amines is developed at room temperature under solvent-free conditions in the presence of (C4H12N2)2[BiCl6]Cl·H2O (1mol%). This catalyst can be reused several times without losing of its activity. [Copyright &y& Elsevier]

Abstract: A novel somatostatin (SS) DNA vaccine (pGM-CSF/SS), delivered orally by attenuated Salmonella typhimurium (CSO22), was used to immunize female mice at 5, 7, and 11 wk of age; the objective was to investigate the humoral immune response and effects of this vaccine on growth, reproduction and lactation. The pGM-CSF/SS induced SS-specific antibodies, which peaked (3.69 ± 0.89; mean ± S.D) 4 wk after the first booster immunization. Compared with a saline-treated control group, body weight gain of a pGM-CSF/SS immunized group increased 30.3% (23.88 vs. 18.32 g, P < 0.05) during the growth period (from 2 wk after primary immunization to 4 wk after the first booster immunization). Immunized mice had higher plasma estradiol concentrations (84.10 ± 2.16 vs. 81.45 ± 2.12 pg/ml, P < 0.05) and a shorter estrous cycle (4.06 ± 0.75 vs. 5.33 ± 0.49 d, P < 0.05), but serum progesterone concentrations were not significantly affected. Since offspring produced by immunized mice gained weight faster (P < 0.05) in the first 2 wk of life (4.27 ± 0.62 and 7.81 ± 1.30 g in Weeks 1 and 2, respectively vs. 3.70 ± 0.23 and 7.14 ± 0.48 g), we inferred that pGM-CSF/SS could have a direct or indirect role in regulating lactation in mice. In conclusion, GM-CSF and CSO22 served as adjuvant and attenuated live vector, respectively, with efficient oral delivery of an SS DNA vaccine which successfully induced a humoral immune response and enhanced rate of weight gain. Furthermore, the DNA vaccine pGM-CSF/SS affected plasma estradiol concentrations and the estrous cycle, and seemed to enhance lactation performance of female mice. [ABSTRACT FROM AUTHOR]

To discover novel anticancer agents with potent and low toxicity, we designed and synthesized a range of new thiosemicarbazone-indole analogues based on lead compound 4 we reported previously. Most compounds displayed moderate to high anticancer activities against five tested tumor cells (PC3, EC109, DU-145, MGC803, MCF-7). Specifically, the represented compound 16f possessed strong antiproliferative potency and high selectivity toward PC3 cells with the IC 50 value of 0.054 μM, compared with normal WPMY-1 cells with the IC 50 value of 19.470 μM. Preliminary mechanism research indicated that compound 16f could significantly suppress prostate cancer cells (PC3, DU-145) growth and colony formation in a dose-dependent manner. Besides, derivative 16f induced G1/S cycle arrest and apoptosis, which may be related to ROS accumulation due to the activation of MAPK signaling pathway. Furthermore, molecule 16f could effectively inhibit tumor growth through a xenograft model bearing PC3 cells and had no evident toxicity in vivo. Overall, based on the biological activity evaluation, analogue 16f can be viewed as a potential lead compound for further development of novel anti-prostate cancer drug. Image 1 • New thiosemicarbazone-indole derivatives were designed and synthesized based on previous work. • Most compounds were more sensitive to prostate cancer PC3 cells in comparison to other cancer cells. • 16f exhibited stronger activity and better safety profile than 3-AP, DPC and lead 4. • 16f induced G1/S cycle arrest and apoptosis in prostate cancer cells (PC3, DU-145) via ROS accumulation. [ABSTRACT FROM AUTHOR]

This study intended to investigate the in vivo pulmonary fate of intratracheally dosed nanosuspensions of fluticasone propionate (FP). Three FP suspensions, including a microsuspension and two nanosuspensions with different dissolution profiles, were prepared and they exhibited comparable aerodynamic performances after nebulization via a jet nebulizer. Following intratracheal administration to rats, the microsuspension underwent extensive mucociliary clearance, leading to a limited absorption time whereas the nanosuspensions decreased the mucociliary clearance and allowed dissolution rate-limiting and extended pulmonary absorption, resulting in prolonged pulmonary retention and long-acting anti-inflammatory efficacy in a lipopolysaccharide induced lung injury model. Delaying the FP dissolution of a nanosuspension by phospholipid coating increased AUC value in lung tissues to 1.72-fold of a conventional nanosuspension, but led to a decreased pharmacological efficacy. This study demonstrated that inhalable nanosuspensions were a feasible means for the sustained pulmonary delivery of FP and the local anti-inflammatory efficacy was highly dependent on the dissolution profiles. [ABSTRACT FROM AUTHOR]