Comparative absorption kinetics of seven active ingredients of Eucommia ulmoides extracts by intestinal in situ circulatory perfusion in normal and spontaneous hypertensive rats

Eucommia ulmoides Oliv. (E. ulmoides) is a valuable and nourishing medicinal herb in China that has been used in the treatment of hypertension. Given the fact that most traditional Chinese medicine is mainly used to treat disease, investigating the pharmacokinetics of traditional Chinese medicines in the pathological state is more useful than that in the normal state. However, the differences in the absorption kinetics of active ingredients of E. ulmoides extract between pathological and physiological conditions have not been reported. Therefore, in this study, the rat intestinal in situ circulatory perfusion model was used to investigate the differences in absorption kinetics of seven active ingredients of E. ulmoides extract in normal and spontaneously hypertensive rats, namely, genipinic acid, protocatechuic acid, neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, (+)-pinoresinol di-O-β-D -glucopyranoside and (+)-pinoresinol 4′-O-β-D -glucopyranoside. Our results indicate that the pathological state of spontaneous hypertension may change the absorption of active components of E. ulmoides extracts, and these findings may provide a reference for improving the rational use of E. ulmoides in the clinic.     

Anti-neuraminidase activity of chemical constituents of Balanophora involucrata

Balanophora involucrata J. D. Hooker has been known to possess potential anti-inflammatory and antibacterial activities; however, its antiviral activity has not been evaluated so far. In order to find new neuraminidase inhibitors (NAIs), the neuraminidase (NA) inhibition activity of different B. involucrata extracts was evaluated. In this study, an in vitro NA inhibition assay was performed to identify which extract of B. involucrata exhibits (maximal) inhibitory activity against NA. Ultra high performance liquid chromatography/quadrupole time-of-flight–tandem mass spectroscopy (MS/MS) and molecular docking techniques were used to identify the specific compounds responsible for the anti-influenza activity of the extract, and to explore the potential natural NAIs. The ethyl acetate extract of B. involucrata exhibited significant inhibitory activity against NA with 50% inhibitory concentration (IC₅₀) value of 159.5 μg/mL. Twenty compounds were identified according to the MS/MS spectra; among them two compounds (quercitrin and phloridzin) showed obvious inhibitory activity against NA, with IC₅₀ of 311.76 and 347.32 μmol/L, respectively. This study suggested that B. involucrata can be a potential natural source of NAIs and may be useful in the fight against ferocious influenza viruses.     

Metabolic Profiling of Amino Acids by Liquid Chromatography–Tandem Mass Spectrometry (LC–MS) to Characterize the Significance of Glutamine in Triple-Negative Breast Cancer (TNBC)

Triple-negative breast cancer (TNBC) is considered to be aggressive based on its low overall survival and disease-free rates. Currently, there is no molecular-targeted therapy. The identification of a suitable biomarker is still a research focus for TNBC at the present time. Amino acid metabolism fulfills multiple important physiological roles in humans. Their metabolic abnormalities have been reported in numerous cancer studies and amino acid pathways may also be chemotherapeutic targets. This study reports the profiling analysis of amino acids in TNBC and non-TNBC cell lines for detecting biomarkers based on the strategy of N-phosphorylation labeling with liquid chromatography–tandem mass spectrometry (LC–MS). Glutamine (Gln) was found to be significantly down-regulated in TNBC cells because it was largely absorbed and consumed in the TNBC cell lines. These results indicate faster proliferation of TNBC and higher consumption of glutamine to meet the material and energy demand, suggesting its potential role in TNBC progression. Hence, glutamine may be regarded as a biomarker and Gln-targeted approaches may become a new therapeutic strategies for TNBC.     

Recent Progress on Nickel-Based Oxide/(Oxy)Hydroxide Electrocatalysts for the Oxygen Evolution Reaction

Developing clean and sustainable energies as alternatives to fossil fuels is in strong demand within modern society. The oxygen evolution reaction (OER) is the efficiency-limiting process in plenty of key renewable energy systems, such as electrochemical water splitting and rechargeable metal–air batteries. In this regard, ongoing efforts have been devoted to seeking high-performance electrocatalysts for enhanced energy conversion efficiency. Apart from traditional precious-metal-based catalysts, nickel-based compounds are the most promising earth-abundant OER catalysts, attracting ever-increasing interest due to high activity and stability. In this review, the recent progress on nickel-based oxide and (oxy)hydroxide composites for water oxidation catalysis in terms of materials design/synthesis and electrochemical performance is summarized. Some underlying mechanisms to profoundly understand the catalytic active sites are also highlighted. In addition, the future research trends and perspectives on the development of Ni-based OER electrocatalysts are discussed.     

Development of an LC‐MS/MS method for determining the pharmacokinetics of clonidine following oral administration of Zhenju antihypertensive compound

Zhenju antihypertensive compound (ZJAHC) is a combined Chinese–Western medicine formula including clonidine (CLO), hydrochlorothiazide (HCT), rutin, Chrysanthemum indicum extract and pearl powder. Compared with CLO preparations, ZJAHC shows improved activities and decreased adverse effects. It is believed that the side effects of CLO are caused by its high peak plasma concentration. Hence, study of the influence of ZJAHC on the pharmacokinetic behaviors of clonidine seems essential. In present study, the plasma concentrations of CLO were determined with a liquid chromatography–tandem mass spectrometry (LC‐MS/MS) method. The MS/MS transitions monitored for clonidine and internal standard were 230.2 → 213.1 and 152.2 → 110.2, respectively. The analyte was quantified in a single run within 3 min. The pharmacokinetic study showed that the area under the plasma concentration–time curve of CLO in ZJAHC (60 µg/kg CLO) was similar to that of CLO‐HCT‐high (120 µg/kg CLO) but the peak concentration was much lower than that in CLO‐HCT‐high. ZJAHC could enhance the bioavailability without greatly increasing peak concentration of clonidine. This comprehensive effect of enhancing the bioavailability and avoiding the high peak plasma concentration for CLO might mainly result from the co‐contribution of Western medicine and traditional Chinese medicine (TCM), while the effect of TCM was stronger than that of Western medicine. Copyright © 2014 John Wiley & Sons, Ltd.     

The Berry–Esseen bounds of the weighted estimator in a nonparametric regression model

Consider the following nonparametric model: \(Y_{ni}=g(x_{ni})+ \varepsilon _{ni},1\le i\le n,\) where \(x_{ni}\in {\mathbb {A}}\) are the nonrandom design points and \({\mathbb {A}}\) is a compact set of \({\mathbb {R}}^{m}\) for some \(m\ge 1\), \(g(\cdot )\) is a real valued function defined on \({\mathbb {A}}\), and \(\varepsilon _{n1},\ldots ,\varepsilon _{nn}\) are \(\rho ^{-}\)-mixing random errors with zero mean and finite variance. We obtain the Berry–Esseen bounds of the weighted estimator of \(g(\cdot )\). The rate can achieve nearly \(O(n^{-1/4})\) when the moment condition is appropriate. Moreover, we carry out some simulations to verify the validity of our results.

     

Unlocking the Drug Potential of the Bryostatin Family: Recent Advances in Product Synthesis and Biomedical Applications

Bryostatins are a class of naturally occurring macrocyclic lactones with a unique fast developing portfolio of clinical applications, including treatment of AIDS, Alzheimer's disease, and cancer. This comprehensive account summarizes the recent progress (2014–present) in the development of bryostatins, including their total synthesis and biomedical applications. An emphasis is placed on the discussion of bryostatin 1 , the most-studied analogue to date. This review highlights the synthetic and biological challenges of bryostatins and provides an outlook on their future development.     

Fast Liquid Phase Epitaxial Growth for Perovskite Single Crystals

Semiconductors grown by the solution-processed method have shown low-cost,facile fabrication process and comparable performance.However,there are many reasons why it is difficult to achieve high quality films.For example,lattice constant mismatch is one of the problems when photovoltaic devices made of organ metallic perovskites.In this work,MAPbBr^{MA=CH3NH3^+}perovskites single crystals grown on the surface of MAPbBr2.5 CI0.5 perovskites single crystals via liquid epitaxial growth method is demonstrated.It is found that when the lattice constants of the two perovskite single crystals are matched,another crystal can be grown on the surface of one crystal by epitaxial growth.The whole epitaxy growth process does not require high heating temperature and long heating time.X-ray diffraction method is used to prove the lattice plane of the substrate and the epitaxial grown layer.A scanning electron microscope is used to measure the thickness of the epitaxial layer.Compared with perovskite-based photodetectors without epitaxial growth layer,perovskite-based photodetectors with epitaxial growth layer have lower dark current density and higher optical responsibility.     

Water-induced formation of an alkali-ion dimer in cryptomelane nanorods

Tunneled metal oxides such as α-Mn₈O₁₆ (hollandite) have proven to be compelling candidates for charge-storage materials in high-density batteries. In particular, the tunnels can support one-dimensional chains of K⁺ ions (which act as structure-stabilizing dopants) and H₂O molecules, as these chains are favored by strong H-bonds and electrostatic interactions. In this work, we examine the role of water molecules in enhancing the stability of K⁺-doped α-Mn₈O₁₆ (cryptomelane). The combined experimental and theoretical analyses show that for high enough concentrations of water and tunnel-ions, H₂O displaces K⁺ ions from their natural binding sites. This displacement becomes energetically favorable due to the formation of K²⁺ dimers, thereby modifying the stoichiometric charge of the system. These findings have potentially significant technological implications for the consideration of cryptomelane as a Li⁺/Na⁺ battery electrode. Our work establishes the functional role of water in altering the energetics and structural properties of cryptomelane, an observation that has frequently been overlooked in previous studies.

Water displaces potassium ions and initiates the formation of a homonuclear dimer ion (K²⁺) in the tunnels of hollandite.