An emerging strategy for tracing the anti-erectile dysfunction components of raw and salt-processed semens of Astragali Complanati by combinatory liquid chromatography–mass spectrometry-based quantitative analysis,efficacy assessment on impotent rats,and partial least squares regression

Semens of Astragali Complanati own anti-erectile dysfunction effect; however, the components which contribute to the anti-erectile dysfunction effect remain unclear. This work raised a strategy that integrates liquid chromatography coupled mass spectrometry-based quantitative analysis, anti-erectile dysfunction assessment on impotent rats, and their relationship analysis for pinpointing anti-erectile dysfunction components from semens of Astragali Complanati. For simultaneous quantification of seven major components in raw and salt-processed semens of Astragali Complanati, an accurate and reliable liquid chromatography–mass spectrometry method was developed under multiple reaction monitoring mode. Of note, chloramphenicol was employed as the internal standard. The method showed good linearity and repeatability, where the recovery rates of each component ranged from 98.1 to 104.7%, and the precisions of intra- and interday were all within 3.4%. The method has been used for quantification of the seven major components in 10 batches of raw and salt-processed semens of Astragali Complanati. Then, the anti-erectile dysfunction effects of raw and salt-processed semens of Astragali Complanati were evaluated on impotent rats. Gray relationship analysis and partial least squares regression were combined for elucidating the relationship. As a result, complanatuside, astragalin, complanatoside B, and kaempferol were found to be responsible for anti-erectile dysfunction effect of Astragali Complanati.     

Surface domain potential difference-mediated efficient charge separation on a defective ZnIn2S4 microsphere photocatalyst

Low-efficiency charge separation in metal sulfides is a major obstacle to realizing high photocatalytic performance. Herein, we propose the concept of a similar surface domain potential difference between adjacent microdomains with and without surface S vacancies on ZnIn₂S₄ to mediate charge separation. Defective ZnIn₂S₄ microspheres (DZISNPs) are prepared through a solvothermal method combined with a low-temperature hydrogenation surface engineering strategy. The as-prepared DZISNPs with a narrowed bandgap of 2.38 eV possess a large specific surface area of 178.5 m² g^?1, a pore size of 6.89 nm, and a pore volume of 0.36 cm³ g^?1, which further improves the visible light absorption. The resultant DZISNPs exhibit excellent visible light activity (2.15 mmol h^?1 g^?1), which is ～two-fold higher than that of the original DZISNP. The experimental results and DFT calculations reveal that the enhanced property can be a result of the surface S vacancy-induced surface domain potential difference, promoting the spatial separation of electrons and holes. Furthermore, the long-term stability of the DZISNPs indicates that the formation of surface S vacancies can inhibit the photocorrosion of ZnIn₂S₄. This strategy provides new insights for fabricating highly efficient and stable sulfide photocatalysts.     

Evaluation on bioactivities of triterpenes from Bergenia emeiensis

Bergenia emeiensis is a traditional folk medicine in China. Most studies are focusing on the bioactivity of bergenin, neglecting other compounds. Therefore, in this present work, the antioxidant, antibacterial and anticancer abilities of triterpenes from B. emeiensis rhizomes (TBE) were comprehensively evaluated. The results showed that TBE could well scavenge DPPH with a lower EC50 of 0.29 mg/mL and could improve the cell viability of CHO cells against H₂O₂ induced cell death. Additionally, TBE also enhanced the resistance of C. elegans under thermal stress, exhibiting a strong antioxidant potential in vivo. Moreover, TBE showed a certain antibacterial ability on five kind strains such as Pseudomonas aeruginosa while TBE could not significantly inhibit the growth of plant pathogenic fungi. Furthermore, TBE possessed an excellent suppression ability on the proliferation of cancer cells especially Hela and Hep G2 cells with an IC50 of 41.79 μg/mL and 48.62 μg/mL at 48 h, respectively. After fractionally extracted with petroleum ether, ethyl acetate and ethanol, ethanol phase (EP) contained the most triterpenes, followed by ethyl acetate phase (EAP) and petroleum ether phase (PEP). Besides, EP and EAP exhibited a strong antioxidant capacity and also inhibited the proliferation of Hela and Hep G2 cells with the effect of pro-oxidation by inducing a high level of ROS and decreasing mitochondrial membrane potential, thus causing oxidative stress then inducing cell apoptosis. Therefore, these outcomes indicated the triterpenes from B. emeiensis possessed a strong antioxidant ability and an anticancer effect, thus making B. emeiensis become a promising potential alternative in pharmacological field.     

BODIPY-based Fluorescent Probe for Fast Detection of Hydrogen Sulfide and Lysosome-targeting Applications in Living Cells

Hydrogen sulfide (H₂S) is recognized as an endogenous gaseous signaling agent in many biological activities. Lysosomes are the main metabolic site and play a pivotal role in cells. Herein, we designed and synthesized two new fluorescent probes BDP-DNBS and BDP-DNP with a BODIPY core to distinguish H₂S. The sensing mechanism is based on the inhibition-recovery of the photo-induced electron transfer (PET) process. Through comparing the responsive behaviors of the two probes toward H₂S, BDP-DNBS showed a fast response time (60 s), low limit of detection (LOD, 51 nM), high sensitivity and selectivity. Moreover, the reaction mechanism was demonstrated by mass spectrometry and fluorescence off-on mechanism was proved by density functional theory (DFT). Significantly, confocal fluorescence imaging indicated that BDP-DNBS was successfully used to visualize H₂S in lysosomes in living HeLa cells.     

磁共振扩散加权成像联合血清AFP对小肝癌临床诊断及疗效评估的价值

将194例小肝癌患者纳入小肝癌组,185例肝细胞结节患者纳入结节组,所有患者均行MRI扩散加权成像(DWI-MRI),评估患者在DWI-MRI上的形态学表现及ADC值,检测患者血清AFP水平,比较不同检测方法诊断小肝癌的准确度、灵敏度、特异度。结果显示,应用DWI-MRI联合血清AFP诊断小肝癌的特异度、灵敏度和准确度均显著高于单独应用DWI-MRI,或血清AFP(P<0.05)。表明DWI-MRI联合血清AFP对小肝癌的诊断价值显著,可为病情评估提供切实可行的参考。     

MRI参数对腰椎间盘突出症患者椎间盘退变程度的评估价值及与JOA、VAS评分相关性

选择腰椎间盘突出症(LDH)患者60例,分为轻度退变组、中度退变组、重度退变组。患者均行MRI检查,比较3组的MRI参数,包括髓核(NP)区、纤维环(AF)区T2值。检测比较发现,3组LDH患者NP区、AF区T2值间存在明显差异,且与腰椎功能评分(JOA)呈正相关,与腰部疼痛评分(VAS)呈负相关(P<0.05)。NP区、AF区T2值联合鉴别轻中度、中重度椎间盘退变程度的AUC大于各指标单一鉴别,具有较高评估效能。因此,MRI参数评估LDH患者椎间盘退变程度方面具有良好价值,可为临床明确患者病情提供重要参考。     

CT检查参数对腰椎管狭窄症的诊断价值及与疗效、腰椎功能改善的相关性分析

选取我院60例腰椎管狭窄症(LSS)患者作为研究组,同期健康者60例作为对照组,探究CT检查参数对LSS的诊断价值及与疗效、腰椎功能改善的相关性。结果显示,研究组椎管面积、硬膜囊面积、椎管矢径、椎管横径、侧隐窝矢径、侧隐窝角小于对照组(P<0.05);CT各参数联合诊断LSS的AUC值大于任一参数单独诊断;疗效优良患者术后3个月椎管面积、硬膜囊面积、椎管矢径、侧隐窝矢径、侧隐窝角大于治疗前及非优良患者(P<0.05);经偏相关性分析发现,CT检查参数与疗效显著相关(P<0.05)。说明LSS疗效、腰椎功能改善情况与椎管面积、硬膜囊面积、椎管矢径等关系密切,CT检查对指导临床完善手术方案有重要意义。     

Sigma-1 Receptor Agonist TS-157 Improves Motor Functional Recovery by Promoting Neurite Outgrowth and pERK in Rats with Focal Cerebral Ischemia

Sigma-1 (σ-1) receptor agonists are considered as potential treatment for stroke. TS-157 is an alkoxyisoxazole-based σ-1 receptor agonist previously discovered in our group. The present study describes TS-157 profile in a battery of tests for cerebral ischemia. Initial evaluation demonstrated the compound’s safety profile and blood–brain barrier permeability, as well as its ability to induce neurite outgrowth in vitro. The neurite outgrowth was shown to be mediated via σ-1 receptor agonism and involves upregulation of ERK phosphorylation (pERK). In particular, TS-157 also significantly accelerated the recovery of motor function in rats with transient middle cerebral artery occlusion (tMCAO). Overall, the results herein support the notion that σ-1 receptor agonists are potential therapeutics for stroke and further animal efficacy studies are warranted.     

A Novel Solid Nanocrystals Self-Stabilized Pickering Emulsion Prepared by Spray-Drying with Hydroxypropyl-β-cyclodextrin as Carriers

A drug nanocrystals self-stabilized Pickering emulsion (NSSPE) with a unique composition and microstructure has been proven to significantly increase the bioavailability of poorly soluble drugs. This study aimed to develop a new solid NSSPE of puerarin preserving the original microstructure of NSSPE by spray-drying. A series of water-soluble solid carriers were compared and then Box-Behnken design was used to optimize the parameters of spray-drying. The drug release and stability of the optimized solid NSSPE in vitro were also investigated. The results showed that hydroxypropyl-β-cyclodextrin (HP-β-CD), rather than solid carriers commonly used in solidification of traditional Pickering emulsions, was suitable for the solid NSSPE to retain the original appearance and size of emulsion droplets after reconstitution. The amount of HP-β-CD had more influences on the solid NSSPE than the feed rate and the inlet air temperature. Fluorescence microscopy, confocal laser scanning microscopy and scanning electron microscopy showed that the reconstituted emulsion of the solid NSSPE prepared with HP-β-CD had the same core-shell structure with a core of oil and a shell of puerarin nanocrystals as the liquid NSSPE. The particle size of puerarin nanocrystal sand interfacial adsorption rate also did not change significantly. The cumulative amount of released puerarin from the solid NSSPE had no significant difference compared with the liquid NSSPE, which were both significantly higher than that of puerarin crude material. The solid NSSPE was stable for 3 months under the accelerated condition of 75% relative humidity and 40 °C. Thus, it is possible todevelop the solid NSSPE preserving the unique microstructure and the superior properties in vitro of the liquid NSSPE for poorly soluble drugs.     

The Total Solubility of the Co-Solubilized PAHs with Similar Structures Indicated by NMR Chemical Shift

The synergism/inhibition level, solubilization sites and the total solubility (S_t) of co-solubilization systems of phenanthrene, anthracene and pyrene in Tween 80 and sodium dodecyl sulfate (SDS) are studied by ¹H-NMR, 2D nuclear overhauser effect spectroscopy (NOESY) and rotating frame overhauser effect spectroscopy (ROESY). In Tween 80, inhibition for phenanthrene, anthracene and pyrene is observed in most binary and ternary systems. However, in SDS, synergism is predominant. After analysis, we find that the different synergism or inhibition situation between Tween 80 and SDS is related to the different types of surfactants used and the resulting different co-solubilization mechanisms. In addition, we also find that three polycyclic aromatic hydrocarbons (PAHs) have similar solubilization sites in both Tween 80 and SDS, which are almost unchanged in co-solubilization systems. Due to the similar solubilization sites, the chemical shift changes of surfactant and PAH protons follow the same pattern in all solubilization systems, and the order of chemical shift changes is consistent with the order of changes in the St of PAHs. In this case, it is feasible to evaluate S_t of PAHs by chemical shift. In both Tween 80 and SDS solutions, the ternary solubilization system has relatively high S_t rankings. Therefore, in practical applications, a good overall solubilization effect can be expected.