Publications by authors named "Yong-Qiang Liu"

68 Publications

Phytochemical library screen reveals betulinic acid as a novel Skp2-SCF E3 ligase inhibitor in non-small cell lung cancer.

Cancer Sci 2021 Jun 3. Epub 2021 Jun 3.

Institute of Clinical Pharmacology, Science and Technology Innovation Center, Guangzhou University of Chinese Medicine, Guangzhou, 510405, China.

Skp2 is overexpressed in multiple cancers and plays a critical role in tumor development through ubiquitin/proteasome-dependent degradation of its substrate proteins. Drugs targeting Skp2 have exhibited promising anticancer activity. Here, we identified a plant-derived Skp2 inhibitor, betulinic acid (BA), via high-throughput structure-based virtual screening of a phytochemical library. BA significantly inhibited the proliferation and migration of non-small cell lung cancer (NSCLC) through targeting Skp2-SCF E3 ligase both in vitro and in vivo. Mechanistically, BA binding to Skp2, especially forming H-bond with residue Lys145, decreases its stability by disrupting Skp1-Skp2 interactions, thereby inhibiting the Skp2-SCF E3 ligase and promoting the accumulation of its substrates, that is, E-cadherin and p27. In both subcutaneous and orthotopic xenografts, BA significantly inhibited the proliferation and metastasis of NSCLC through targeting Skp2-SCF E3 ligase and upregulating p27 and E-cadherin protein levels. Taken together, BA can be considered a valuable therapeutic candidate to inhibit metastasis of NSCLC.
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http://dx.doi.org/10.1111/cas.15005DOI Listing
June 2021

Identification of pseudolaric acid B as a novel Hedgehog pathway inhibitor in medulloblastoma.

Biochem Pharmacol 2021 May 6;190:114593. Epub 2021 May 6.

Institute of Clinical Pharmacology, Science and Technology Innovation Center, Guangzhou University of Chinese Medicine, Guangzhou 510405, China; Research Center of Chinese Herbal Resources Science and Engineering, School of Pharmaceutical Sciences; Key Laboratory of Chinese Medicinal Resource from Lingnan, Ministry of Education, Guangzhou University of Chinese Medicine, Guangzhou 510006, China. Electronic address:

Aberrant activation of the Hedgehog (Hh) pathway is implicated in the pathogenesis and development of multiple cancers, especially Hh-driven medulloblastoma (MB). Smoothened (SMO) is a promising therapeutic target of the Hh pathway in clinical cancer treatment. However, SMO mutations frequently occur, which leads to drug resistance and tumor relapse. Novel inhibitors that target both the wild-type and mutant SMO are in high demand. In this study, we identified a novel Hh pathway inhibitor, pseudolaric acid B (PAB), which significantly inhibited the expression of Gli1 and its transcriptional target genes, such as cyclin D1 and N-myc, thus inhibiting the proliferation of DAOY and Ptch1 primary MB cells. Mechanistically, PAB can potentially bind to the extracellular entrance of the heptahelical transmembrane domain (TMD) of SMO, based on molecular docking and the BODIPY-cyclopamine binding assay. Further, PAB also efficiently blocked ciliogenesis, demonstrating the inhibitory effects of PAB on the Hh pathway at multiple levels. Thus, PAB may overcome drug-resistance induced by SMO mutations, which frequently occurs in clinical setting. PAB markedly suppressed tumor growth in the subcutaneous allografts of Ptch1 MB cells. Together, our results identified PAB as a potent Hh pathway inhibitor to treat Hh-dependent MB, especially cases resistant to SMO antagonists.
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http://dx.doi.org/10.1016/j.bcp.2021.114593DOI Listing
May 2021

Numerical analysis for the vertical bearing capacity of composite pile foundation system in liquefiable soil under sine wave vibration.

PLoS One 2021 17;16(3):e0248502. Epub 2021 Mar 17.

School of Construction Engineering, Shandong University of Technology, Zibo, Shandong, China.

Composite pile foundation has been widely used in ground engineering. This composite pile foundation system has complex pile-soil interactions under seismic loading. The calculation of vertical bearing capacity of composite pile foundation is still an unsolved problem if the soil around piles is partially or completely liquefied under seismic loading. We have completed indoor shaking table model tests to measure the vertical bearing capacity in a liquefiable soil foundation under seismic loading. This paper will use a numerical approach to analyze the change of this vertical bearing capacity under seismic loading. Firstly, the Goodman contact element is improved to include the Rayleigh damping. Such an improvement can well describe the reflection and absorption of seismic waves at the interface of soil and piles. Secondly, the Biot's dynamic consolidation theory incorporated an elastoplastic model is applied to simulate the soil deformation and the generation and accumulation of pore water pressure under seismic loading. Thirdly, after verification with our indoor shaking table test data, this approach is used to investigate the effects of pile spacing on liquefaction resistance of the composite pile foundation in liquefiable soil. The time histories of pore water pressure ratio (PPR') are calculated for the liquefiable soil and the vertical bearing capacity in partially liquefied soil is calculated and compared with our indoor shaking table test data at the 3D, 3.5D, 4D, 5D and 6D cases (D is the pile diameter). It is found that the pile spacing has some influence on the extent of soil liquefaction between piles. The vertical bearing capacity varies with liquefaction extent of inter-pile soil. The optimization of pile spacing varies with liquefaction extent. These results may provide some reference for the design of composite pile foundation under seismic loading.
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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0248502PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7968676PMC
March 2021

Adsorption properties of β-cyclodextrin modified hydrogel for methylene blue.

Carbohydr Res 2021 Mar 27;501:108276. Epub 2021 Feb 27.

College of Chemistry and Chemical Engineering, Southwest Petroleum University, Chengdu, 610500, China.

With the development of dye and printing, production wastewater has become one of the most primary pollution sources of water and soil pollution. Most of the dyes are toxic substances, which have the "three-way" effect of carcinogenic, teratogenic and mutagenic. Therefore, it is a very difficult but significant issue to deal with the dye in the wastewater. Here, we report a study on low-cost, high-capacity hydrogels that remove water-soluble dyes. The hydrogel is prepared by crosslinking the β-cyclodextrin and functional monomer: acrylamido and 2-acrylamide-2-methylpropane sulfonic acid by aqueous solution polymerization, meanwhile, alkaline hydrolysis is also an important step for adsorption performance. After alkaline hydrolysis, the amide and sulfonic groups in the hydrogel were converted into carboxylate and sulfonate, which was beneficial to the adsorption of cationic dyes. This polymer could remove 96.58% methylene blue (400 mg/L) and only requires 0.02 wt%. Its maximum adsorption capacity for methylene blue could reach 2638.22 mg/g under equilibrium condition. It is the most powerful adsorbent used to treat dye wastewater, according to the report. It also provides some references for hydrogel treatment of dye wastewater.
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http://dx.doi.org/10.1016/j.carres.2021.108276DOI Listing
March 2021

Decolourization of azo, anthraquinone and triphenylmethane dyes using aerobic granules: Acclimatization and long-term stability.

Chemosphere 2021 Jan 12;263:128312. Epub 2020 Sep 12.

Faculty of Engineering and Physical Sciences, University of Southampton, Southampton, SO17 1BJ, United Kingdom.

The long-term stability of aerobic granules is critical for decolourization of different dyes in textile wastewater. Here, we investigated dye decolourization and the stability of acetate-cultivated granules after exposure to dyes. Results show that granules can maintain excellent structure stability with the presence of azo and triphenylmethane dyes during a 200-day operation period, achieving biomass concentrations as high as 8-12 g L and 90% and 100% decolourization efficiency, respectively. Aerobic granules, however, partially disintegrated after exposure to anthraquinone, resulting in dye decolourization efficiency ranging from 50 to 80% and a biomass concentration as low as around 0.5 g L due to biomass wash-out. The study indicates that long-term granule stability is much dependent on the dye classes. The enrichment of specific species in granules for dye decolourization has not been affected by the granule structure. The specific dye decolourization rate and dye to microorganism ratio for anthraquinone were 5-6.5 and 13.5-16.4 times, respectively, higher than those for azo and triphenylmethane dyes, but the total reactor performance for anthraquinone decolourization is much poorer than azo and triphenylmethane dyes due to low biomass retention in the reactor. The results suggest the importance of stability of aerobic granules for biomass retention to achieve better treatment performance of dye-containing wastewater. For the first time, the long-term stability and decolourization performance of aerobic granules for treating anthraquinone and triphenylmethane dyes are reported here and compared with azo dye, which can be used to guide the treatment of real textile wastewater containing azo, anthraquinone and triphenylmethane dyes by aerobic granules.
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http://dx.doi.org/10.1016/j.chemosphere.2020.128312DOI Listing
January 2021

Comparison of life cycle toxicity assessment methods for municipal wastewater treatment with the inclusion of direct emissions of metals, PPCPs and EDCs.

Sci Total Environ 2021 Feb 20;756:143849. Epub 2020 Nov 20.

Faculty of Engineering and Physical Sciences, University of Southampton, Southampton SO17 1BJ, United Kingdom. Electronic address:

The occurrence of various micropollutants such as pharmaceuticals personal care products, endocrine disrupting chemicals (PPCPs/EDCs) and metals in municipal wastewater, and their poor removal efficiencies can lead to toxicity impact on humans, and freshwater and terrestrial ecosystems. Life cycle assessment is an efficient and effective tool to evaluate the environmental impact of wastewater treatment plants, but guidelines for toxicity assessment are lacking due to the complexity. This study aims to evaluate both life cycle inventory by including metals and PEC, and life cycle toxicity assessment (LCIA) methods namely CML-IA, Recipe, USEtox, EDIP 2003 and IMPACT 2002+ in midpoint category with a large centralised wastewater treatment plant in Malaysia as a case study. The removal efficiencies of metals and PPCPs/EDCs in the wastewater ranged from 9% to 99% and no clear patterns were found about occurrence and removal efficiencies of metals and PPCPs/EDCs in developing and developed countries. The inclusion of metals and PPCPs/EDCs in effluent resulted in 76% increase in freshwater ecotoxicity potential (FEP) and 88% increase in terrestrial ecotoxicity potential (TEP) while only 4% increase in human toxicity potential (HTP). The results indicate the importance of including direct emissions such as metals and PPCPs/EDCs even in low-strength municipal wastewater for environmental toxicity assessment. The comparison of five LCIA methods suggests that HTP assessment is more challenging due to inconsistency between five LCIA methods while CML-IA, Recipe, and IMPACT 2002+ achieved consistent human toxicity and ecotoxicity assessment results in the WWTP. The results highlight the importance of sampling and inclusion of metals and PPCPs/EDCs data especially prioritised micropollutants for life cycle toxicity assessment and recommends LCIA methods for ecotoxicity assessment of WWTPs in the current scientific development situation on toxicity studies, which can provide guidance to researchers for life cycle toxicity assessment of wastewater treatment.
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http://dx.doi.org/10.1016/j.scitotenv.2020.143849DOI Listing
February 2021

Pharmacokinetics, mass balance, and metabolism of [C]vicagrel, a novel irreversible P2Y inhibitor in humans.

Acta Pharmacol Sin 2020 Nov 26. Epub 2020 Nov 26.

State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201210, China.

Vicagrel, a novel irreversible P2Y receptor inhibitor, is undergoing phase III trials for the treatment of acute coronary syndromes in China. In this study, we evaluated the pharmacokinetics, mass balance, and metabolism of vicagrel in six healthy male Chinese subjects after a single oral dose of 20 mg [C]vicagrel (120 µCi). Vicagrel absorption was fast (T = 0.625 h), and the mean t of vicagrel-related components was ~38.0 h in both plasma and blood. The blood-to-plasma radioactivity AUC ratio was 0.55, suggesting preferential distribution of drug-related material in plasma. At 168 h after oral administration, the mean cumulative excreted radioactivity was 96.71% of the dose, including 68.03% in urine and 28.67% in feces. A total of 22 metabolites were identified, and the parent vicagrel was not detected in plasma, urine, or feces. The most important metabolic spot of vicagrel was on the thiophene ring. In plasma pretreated with the derivatization reagent, M9-2, which is a methylated metabolite after thiophene ring opening, was the predominant drug-related component, accounting for 39.43% of the radioactivity in pooled AUC plasma. M4, a mono-oxidation metabolite upon ring-opening, was the most abundant metabolite in urine, accounting for 16.25% of the dose, followed by M3-1, accounting for 12.59% of the dose. By comparison, M21 was the major metabolite in feces, accounting for 6.81% of the dose. Overall, renal elimination plays a crucial role in vicagrel disposition, and the thiophene ring is the predominant metabolic site.
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http://dx.doi.org/10.1038/s41401-020-00547-7DOI Listing
November 2020

Protection against chemotherapy- and radiotherapy-induced side effects: A review based on the mechanisms and therapeutic opportunities of phytochemicals.

Phytomedicine 2021 Jan 31;80:153402. Epub 2020 Oct 31.

School of Pharmaceutical Sciences, Shenzhen University Health Science Center, Shenzhen 518060, China. Electronic address:

Background: Although great achievements have been made in the field of cancer therapy, chemotherapy and radiotherapy remain the mainstay cancer therapeutic modalities. However, they are associated with various side effects, including cardiocytotoxicity, nephrotoxicity, myelosuppression, neurotoxicity, hepatotoxicity, gastrointestinal toxicity, mucositis, and alopecia, which severely affect the quality of life of cancer patients. Plants harbor a great chemical diversity and flexible biological properties that are well-compatible with their use as adjuvant therapy in reducing the side effects of cancer therapy.

Purpose: This review aimed to comprehensively summarize the molecular mechanisms by which phytochemicals ameliorate the side effects of cancer therapies and their potential clinical applications.

Methods: We obtained information from PubMed, Science Direct, Web of Science, and Google scholar, and introduced the molecular mechanisms by which chemotherapeutic drugs and irradiation induce toxic side effects. Accordingly, we summarized the underlying mechanisms of representative phytochemicals in reducing these side effects.

Results: Representative phytochemicals exhibit a great potential in reducing the side effects of chemotherapy and radiotherapy due to their broad range of biological activities, including antioxidation, antimutagenesis, anti-inflammation, myeloprotection, and immunomodulation. However, since a majority of the phytochemicals have only been subjected to preclinical studies, clinical trials are imperative to comprehensively evaluate their therapeutic values.

Conclusion: This review highlights that phytochemicals have interesting properties in relieving the side effects of chemotherapy and radiotherapy. Future studies are required to explore the clinical benefits of these phytochemicals for exploitation in chemotherapy and radiotherapy.
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http://dx.doi.org/10.1016/j.phymed.2020.153402DOI Listing
January 2021

High numerical aperture microwave metalens.

Opt Lett 2020 Nov;45(22):6262-6265

The numerical aperture (NA) of a lens determines its focusing resolution capability and the maximum light collection or emission angle. In this Letter, an ultrathin high NA metalens operating in the microwave band is designed and demonstrated both numerically and experimentally. The proposed element is constructed by a multi-layer complementary split ring resonator, which can cover full 2 phase shift simultaneously with high transmission magnitude by varying its radius gradually. The numerical and experimental results reveal that the designed ultrathin (thickness is only ∼0.23) metalens can focus normal incident microwave efficiently to a spot of full width at half-maximum (FWHM) as small as ∼0.54 with a corresponding high NA exceeding 0.9. Besides, the high NA metalens also possesses a relatively large focusing efficiency with a peak 48% within considered broad frequency range from 7.5 to 10 GHz. The performances of the presented metalens can be comparable or even superior to nowadays high-quality optical metalenses and represent an important step to develop a high-performance metalens in low spectrum. Besides, it can greatly facilitate the development of some novel miniaturized devices like a high-gain low profile scanning antenna, an ultra-compact retroreflector, and cloaks.
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http://dx.doi.org/10.1364/OL.412040DOI Listing
November 2020

Upgrading a large and centralised municipal wastewater treatment plant with sequencing batch reactor technology for integrated nutrient removal and phosphorus recovery: Environmental and economic life cycle performance.

Sci Total Environ 2020 Dec 5;749:141465. Epub 2020 Aug 5.

Faculty of Engineering and Physical Sciences, University of Southampton, Southampton SO17 1BJ, United Kingdom.

Although nutrient removal and recovery from municipal wastewater are desirable to protect phosphorus resource and water-bodies from eutrophication, it is unclear how much environmental and economic benefits and burdens it might cause. This study evaluated the environmental and economic life cycle performance of three different upgraded Processes A, B and C with commercially available technologies for nutrient removal and phosphorus recovery based on an existing Malaysian wastewater treatment plant with a sequencing batch reactor technology and diluted municipal wastewater. It is found that the integration of nutrient removal, phosphorus recovery and electricity generation in all upgraded processes reduced eutrophication potential by 62-76%, and global warming potential by 7-22%, which, however, were gained at the cost of increases in human toxicity, acidification, abiotic depletion (fossil fuel) and freshwater ecotoxicity potentials by an average of 23%. New technologies for nutrient removal and phosphorus recovery are thus needed to achieve holistic rather than some environmental benefits at the expense of others. In addition, the study on two different functional units (FU), i.e. per m treated wastewater and per kg struvite recovered, shows that FU affected environmental assessment results, but the upgraded Process C had the least overall environmental burden with either of FUs, suggesting the necessity to use different functional units when comparing and selecting different technologies with two functions such as wastewater treatment and struvite production to confirm the best process configuration. The total life cycle costs of Processes A, B and C were 10.7%, 29.8% and 28.1%, respectively, higher than the existing process due to increased capital and operating costs. Therefore, a trade-off between environmental benefits and cost has to be balanced for technology selection or new integrated technologies have to be developed to achieve environmentally sustainable wastewater treatment economically.
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http://dx.doi.org/10.1016/j.scitotenv.2020.141465DOI Listing
December 2020

Effect of Fabrication Parameters on the Performance of 0.5 wt.% Graphene Nanoplates-Reinforced Aluminum Composites.

Materials (Basel) 2020 Aug 7;13(16). Epub 2020 Aug 7.

National Engineering Laboratory for Coalmine Backfilling Mining, Shandong University of Science and Technology, Tai'an 271019, China.

Aluminum composites reinforced by graphene nanoplates(GNP) with a mass fraction of 0.5% (0.5 wt.% GNP/Al) were fabricated using cold pressing and hot pressing. An orthogonal test was used to optimize the fabrication parameters. Ball milling time, ball milling speed, and ultrasonic time have the largest influence on the uniformity of the graphene in the composites. Afterwards, the microstructure, interfacial properties, and fracture morphology of the composites obtained with different parameters were further analyzed. The results show that ball milling time and ball milling speed have obvious influences on the mechanical properties of the composite. In this paper, when the ball milling speed is 300 r/min and the ball milling time is 6 h, the dispersion uniformity of graphene in the 0.5 wt.% GNP/Al composite is the best, the agglomeration is the lowest, and the mechanical properties of the composites are the best, among which the tensile strength is 156.8 MPa, 56.6% higher than that of pure aluminum fabricated by the same process (100.1 MPa), and the elongation is 19.9%, 39.8% lower than that of pure aluminum (33.1%).
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http://dx.doi.org/10.3390/ma13163483DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7475921PMC
August 2020

Odorant Binding Proteins and Chemosensory Proteins in Episyrphus balteatus (Diptera: Syrphidae): Molecular Cloning, Expression Profiling, and Gene Evolution.

J Insect Sci 2020 Jul;20(4)

State Key Laboratory for Biology of Plant Diseases and Insect Pests, Institute of Plant Protection, Chinese Academy of Agricultural Sciences, Beijing, China.

Aphidophagous syrphids (Diptera: Syrphidae) are important insects in agroecosystems for pollination and biological control. Insect chemoreception is essential for these processes and for insect survival and reproduction; however, molecular determinants is not well understood for these beneficial insects. Here, we used recent transcriptome data for the common hoverfly, Episyrphus balteatus, to characterize key molecular components of chemoreception: odorant-binding proteins (OBPs) and chemosensory proteins (CSPs). Six EbalCSPs and 44 EbalOBPs were cloned from this species, and sequence analysis showed that most share the characteristic hallmarks of their protein family, including a signal peptide and conserved cysteine signature. Some regular patterns and key conserved motifs of OBPs and CSPs in Diptera were identified using the online tool MEME. Motifs were also compared among the three OBP subgroups. Quantitative real-time PCR (qRT-PCR) showed that most of these chemosensory genes were expressed in chemosensory organs, suggesting these genes have chemoreceptive functions. An overall comparison of the Ka/Ks values of orthologous genes in E. balteatus and another predatory hoverfly species to analyze the evolution of these olfactory genes showed that OBPs and CSPs are under strong purifying selection. Overall, our results provide a molecular basis for further exploring the chemosensory mechanisms of E. balteatus, and consequently, may help us to understand the tritrophic interactions among plants, herbivorous insects, and natural enemies.
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http://dx.doi.org/10.1093/jisesa/ieaa065DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7414794PMC
July 2020

Assessing environmental impacts of large centralized wastewater treatment plants with combined or separate sewer systems in dry/wet seasons by using LCA.

Environ Sci Pollut Res Int 2020 May 20;27(13):15674-15690. Epub 2020 Feb 20.

Faculty of Engineering and Physical Sciences, University of Southampton, Southampton, SO17 1BJ, UK.

Rainfall can affect influent flow rate and compositions of wastewater, and thus further affect wastewater treatment performance and the effluent quality. This study aims to study the influence of rainfall on the environmental impacts of centralized wastewater treatment plants. The correlations between rainfall, and influent flow rate and compositions of wastewater in wet and dry seasons with two sewer systems, i.e. combined and separate sewer systems, were primarily established. Environmental impacts were assessed with life cycle assessment (LCA) to understand the temporal environmental burdens in wet and dry seasons. Functional units as per m treated wastewater (FU1) and as per kg PO-eq. removed (FU2), respectively, were used to evaluate impacts of wastewater treatment to the environment. Strong correlation between rainfall and the influent flow rate was found in the wastewater treatment plants with either a combined sewer system (with Pearson correlation coefficient r at 0.66) or a separate sewer system (with r at 0.84), where r represents the strength of the association between two variables. The rainfall effect is more obvious on the eutrophication potential and global warming potential than on other environmental indicators while sewer system, i.e. combined or separate, seems not important in the two cases studied. Both wastewater treatment plants (WWTPs) show a lower environmental burden in the wet season than in the dry season partially due to the dilution of wastewater by using FU1. The WWTP receiving high strength wastewater, however, demonstrates higher environmental impacts in the wet season by using FU2 than FU1, due to the less efficient treatment caused by heavy rainfall. Meanwhile, it is found that environmental impacts from the WWTP receiving low strength wastewater have no difference when using either FU1 or FU2. The results indicate that the environmental burdens particularly eutrophication and global warming caused by WWTPs are dependent on the correlations of rainfall intensity with wastewater quantity and quality instead of combined or separate sewer system. This could be used to guide a stricter control of eutrophication in a more sensitive season in more vulnerable receiving waters.
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http://dx.doi.org/10.1007/s11356-020-08038-2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7190677PMC
May 2020

A novel surgical technique for spontaneous intracerebral hematoma evacuation.

Neurosurg Rev 2021 Apr 20;44(2):925-934. Epub 2020 Feb 20.

Departments of Neurosurgery, The Third Affiliated Hospital of Southern Medical University, Guangzhou, 510000, Guangdong, China.

Stereotactic removal of intracerebral hematoma is a routine procedure for treating hypertensive intracerebral hemorrhage, but the complex sequence of operations limits its adoption. We explored the application of a novel surgical technique for the removal of spontaneous intracerebral hematomas. The surgical technique based on computed tomography (CT) images was used in hematoma projection and surgical planning. Markers placed on the scalp based on an Android smartphone app allowed the installation of a stereotactic head frame to facilitate the selection of the best trajectory to the hematoma center for removing the hematoma. Forty-two patients with spontaneous intracerebral hemorrhage were included in the study, including 33 cases of supratentorial hemorrhage, 5 cases of cerebellum hemorrhage, and 4 cases of brain stem hemorrhage. The surgical technique combined with the stereotactic head frame helped the tip of the drainage tube achieve the desired position. The median surgical time was 45 (range 25-75) min. The actual head frame operating time was 10 (range 5-15) min. Target alignment performed by the surgical technique was accurate to ≤ 10.0 mm in all 42 cases. No patient experienced postoperative rebleeding. In 33 cases of supratentorial intracerebral hemorrhage, an average evacuation rate of 77.5% was achieved at postoperative 3.1 ± 1.4 days, and 29 (87.9%) cases had a residual hematoma of < 15 ml. The novel surgical technique helped to quickly and effortlessly localize hematomas and achieve satisfactory hematoma removal. Clinical application of the stereotactic head frame was feasible for intracerebral hemorrhage in various locations.
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http://dx.doi.org/10.1007/s10143-020-01252-zDOI Listing
April 2021

Centipeda minima extract exerts antineuroinflammatory effects via the inhibition of NF-κB signaling pathway.

Phytomedicine 2020 Feb 30;67:153164. Epub 2019 Dec 30.

Science and Technology Innovation Center, Guangzhou University of Chinese Medicine, Guangzhou 510405, China; Institute of Clinical Pharmacology, Guangzhou University of Chinese Medicine, Guangzhou 510405, China. Electronic address:

Background: Centipeda minima (L.) A.Br. (C. minima) has been used in traditional Chinese herbal medicine to treat nasal allergy, diarrhea, asthma and malaria for centuries. Recent pharmacological studies have demonstrated that the ethanol extract of C. minima (ECM) and several active components possess anti-bacterial, anti-arthritis and anti-inflammatory properties. However, the effects of ECM on neuroinflammation and the underlying mechanisms have never been reported.

Purpose: The study aimed to examine the potential inhibitory effects of ECM on neuroinflammation and illustrate the underlying mechanisms.

Methods: High performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) was performed to qualify the major components of ECM; BV2 and primary microglial cells were used to examine the anti-inflammatory activity of ECM in vitro. To evaluate the anti-inflammatory effects of ECM in vivo, the mice were orally administrated with ECM (100, 200 mg•kg•d) for 2 days before cotreatment with LPS (2 mg•kg•d, ip) for an additional 3 days. The mice were sacrificed the day after the last treatment and the hippocampus was dissected for further experiments. The expression of inflammatory proteins and the activation of microglia were respectively detected by real-time PCR, ELISA, Western blotting and immunofluorescence.

Results: HPLC-MS/MS analysis confirmed and quantified seven chemicals in ECM. In BV2 and primary microglial cells, ECM inhibited the LPS-induced production of tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β), thus protecting HT22 neuronal cells from inflammatory damage. Furthermore, ECM inhibited the LPS-induced activation of NF-κB signaling pathway and subsequently attenuated the induction of inducible nitric oxide synthase (iNOS), cyclooxygenase 2 (COX2), NADPH oxidase 2 (NOX2) and NADPH oxidase 4 (NOX4), leading to the decreased production of nitrite oxide, prostaglandin E (PGE) and reactive oxygen species (ROS). In an LPS-induced neuroinflammatory mouse model, ECM was found to exert anti-inflammatory activity by decreasing the production of proinflammatory mediators, inhibiting the phosphorylation of NF-κB, and reducing the expression of COX2, iNOS, NOX2 and NOX4 in the hippocampal tissue. Moreover, LPS-induced microglial activation was markedly attenuated in the hippocampus, while ECM at a high dose possesses a stronger anti-inflammatory activity than the positive drug dexamethansone (DEX).

Conclusion: These findings demonstrate that ECM exerts antineuroinflammatory effects via attenuating the activation of NF-κB signaling pathway and inhibiting the production of proinflammatory mediators both in vitro and in vivo. C. minima might become a novel phytomedicine to treat neuroinflammatory diseases.
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http://dx.doi.org/10.1016/j.phymed.2019.153164DOI Listing
February 2020

6-O-angeloylplenolin exerts neuroprotection against lipopolysaccharide-induced neuroinflammation in vitro and in vivo.

Acta Pharmacol Sin 2020 Jan 18;41(1):10-21. Epub 2019 Jun 18.

Institute of Clinical Pharmacology, Guangzhou University of Chinese Medicine, Guangzhou, 510405, China.

Neuroinflammation is one of the critical events in neurodegenerative diseases, whereas microglia play an important role in the pathogenesis of neuroinflammation. In this study, we investigated the effects of a natural sesquiterpene lactone, 6-O-angeloylplenolin (6-OAP), isolated from the traditional Chinese medicine Centipeda minima (L.) A.Br., on neuroinflammation and the underlying mechanisms. We showed that treatment with lipopolysaccharide (LPS) caused activation of BV2 and primary microglial cells and development of neuroinflammation in vitro, evidenced by increased production of inflammatory cytokines TNF-α and IL-1β, the phosphorylation and nuclear translocation of NF-κB, and the transcriptional upregulation of COX-2 and iNOS, leading to increased production of proinflammatory factors NO and PGE. Moreover, LPS treatment induced oxidative stress through increasing the expression levels of NOX2 and NOX4. Pretreatment with 6-OAP (0.5-4 μM) dose-dependently attenuated LPS-induced NF-κB activation and oxidative stress, thus suppressed neuroinflammation in the cells. In a mouse model of LPS-induced neuroinflammation, 6-OAP (5-20 mg·kg·d, ip, for 7 days before LPS injection) dose-dependently inhibited the production of inflammatory cytokines, the activation of the NF-κB signaling pathway, and the expression of inflammatory enzymes in brain tissues. 6-OAP pretreatment significantly ameliorated the activation of microglia and astrocytes in the brains. 6-OAP at a high dose caused a much stronger antineuroinflammatory effect than dexamethansone (DEX). Furthermore, we demonstrated that 6-OAP pretreatment could inhibit LPS-induced neurite and synaptic loss in vitro and in vivo. In conclusion, our results demonstrate that 6-OAP exerts antineuroinflammatory effects and can be considered a novel drug candidate for the treatment of neuroinflammatory diseases.
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http://dx.doi.org/10.1038/s41401-019-0261-5DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7470812PMC
January 2020

Ethanol Extract of Exerts Antioxidant and Neuroprotective Effects via Activation of the Nrf2 Signaling Pathway.

Oxid Med Cell Longev 2019 3;2019:9421037. Epub 2019 Apr 3.

Institute of Clinical Pharmacology, Guangzhou University of Chinese Medicine, Guangzhou 510405, China.

Oxidative stress is implicated in the pathogenesis of neurodegeneration and other aging-related diseases. Previous studies have found that the whole herb of has remarkable antioxidant activities. However, there have been no reports on the neuroprotective effects of , and the underlying mechanism of its antioxidant properties is unclear. Here, we examined the underlying mechanism of the antioxidant activities of the ethanol extract of (ECM) both and in and found that ECM treatment attenuated glutamate and tert-butyl hydroperoxide (tBHP)-induced neuronal death, reactive oxygen species (ROS) production, and mitochondria dysfunction. tBHP-induced phosphorylation of p38 mitogen-activated protein kinase (p38 MAPK) and c-Jun N-terminal kinases (JNK) was reduced by ECM, and ECM sustained phosphorylation level of extracellular signal regulated kinase (ERK) in SH-SY5Y and PC12 cells. Moreover, ECM induced the activation of nuclear factor erythroid 2-related factor 2 (Nrf2) and the upregulation of phase II detoxification enzymes, including heme oxygenase-1 (HO-1), superoxide dismutase-2 (SOD2), and NAD(P)H quinone oxidoreductase-1 (NQO-1) in both two cell types. In a D-galactose (D-gal) and aluminum muriate (AlCl)-induced neurodegenerative mouse model, administration of ECM improved the learning and memory of mice in the Morris water maze test and ameliorated the effects of neurodegenerative disorders. ECM sustained the expression level of postsynaptic density 95 (PSD95) and synaptophysin (SYN), activated the Nrf2 signaling pathway, and restored the levels of cellular antioxidants in the hippocampus of mice. In addition, four sesquiterpenoids were isolated from to identify the bioactive components responsible for the antioxidant activity of ; 6--angeloylplenolin and arnicolide D were found to be the active compounds responsible for the activation of the Nrf2 signaling pathway and inhibition of ROS production. Our study examined the mechanism of and its active components in the amelioration of oxidative stress, which holds the promise for the treatment of neurodegenerative disease.
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http://dx.doi.org/10.1155/2019/9421037DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6470452PMC
January 2020

Efficacy of levetiracetam compared with phenytoin in prevention of seizures in brain injured patients: A meta-analysis.

Medicine (Baltimore) 2018 Nov;97(48):e13247

Department of Neurosurgery, the Second Hospital of Hebei Medical University.

Background: Early and/or late onset in patients with brain injury (BI) is associated with a poorer prognosis, and phenytoin (PHT) is standard of care to prevent seizures. Levetiracetam (LEV), an alternative antiepileptic drug, is associated with less cognitive disruption. The purpose of this study was to evaluate the safety and efficacy of LEV in the prevention of brain traumatic seizures with the standard drug PHT.

Methods: Search the publications on comparison the safety and efficacy of LEV against the standard agent PHT in prevention of traumatic seizures in BI to January 2018. After rigorous reviewing on quality, the data were extracted from eligible trials. All trials analyzed the summary hazard ratios of the endpoints of interest.

Results: LEV was found not more effective than PHT in terms of overall seizure (odds ratio [OR] = 0.73; 95% confidence interval [CI] = 0.51-1.05; P = .09), and late seizure (OR = 0.64; 95% CI = 0.34-1.19; P = .16) occurrence. However, there is significant difference in terms of early seizure (OR = 0.63; 95% CI = 0.40-0.99; P = .04). Moreover, there were no significant differences in terms of mortality (OR = 0.67; 95% CI = 0.43-1.05; P = .08), or side effects (OR = 1.31; 95% CI = 0.80-2.15; P = .29) between groups.

Conclusion: The meta-analysis showed that LEV prevention of seizures was associated with early seizure rates that were lower than the PHT-prolonged course of treatment. There is no statistically significant difference in the efficacy and safety profile of PHT and LEV in cases of traumatic BI.
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http://dx.doi.org/10.1097/MD.0000000000013247DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6283080PMC
November 2018

Corrigendum to "Dexmedetomidine relieves formaldehyde-induced pain in rats through both α2 adrenoceptor and imidazoline receptor" [Biomed. Pharmacother. 90 (2017) 914-920].

Biomed Pharmacother 2017 12 16;96:1569. Epub 2017 Nov 16.

Department of Anesthesiology, First Hospital of Lanzhou University, Lanzhou Gansu 730000, PR China.

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http://dx.doi.org/10.1016/j.biopha.2017.08.080DOI Listing
December 2017

Dexmedetomidine relieves formaldehyde-induced pain in rats through both α2 adrenoceptor and imidazoline receptor.

Biomed Pharmacother 2017 Jun 22;90:914-920. Epub 2017 Apr 22.

Department of Anesthesiology, First Hospital of Lanzhou University, Lanzhou Gansu 730000, PR China.

Dexmedetomidine (DEX) is a highly selective α2 adrenergic receptor agonist. In this study, we investigated the analgesic effect and the underlying mechanisms of DEX on inflammatory visceral pain in rats. Twenty-five male Sprague Dawley (SD) rats were randomly divided into 5 groups, including control, sham, low dose DEX, medium dose DEX and high dose DEX group. Pain was induced with 10% formalin and scored every 15min till 2 h-post the induction. Hematoxylin-eosin (HE) staining was used to evaluate the toxicity of DEX on spinal cord neurons. Acetycholine (Ach) and noradrenaline (NA) levels were determined by using ELISA method. The expressions of natural nitric oxide synthase (nNOS), protein kinase γ (PKCγ) and protease-activated receptor 2 (PAR2) were determined by using western blot. DEX treatment relieved formaldehyde-induced pain in rats in a dose-dependent manner. Furthermore, DEX showed little neuro-toxicity on the spinal cord neurons, even at the highest dosage used in our study. Ach level was significantly increased in Sham group compared with control group. DEX treatment decreased NA levels and increased Ach levels in the incubation medium of spinal cord sections. Western blot analysis showed that the expression of nNOS, PKCγ and PAR2 was significantly decreased in DEX group compared with Sham group, whereas these effects of DEX on nNOS, PKCγ and PAR2 were blocked by both yohimbine and idazoxan, indicating that the analgesic effect of DEX is mediated by both α2 adrenergic receptor and imidazoline receptor. Yohimbine and idazoxan treatment significantly enhanced pain scores compared to DEX group, and which antagonizes the effects DEX. In conclusion, our study demonstrated that DEX could inhibit formaldehyde-induced pain by inhibiting nNOS, PKCγ and PAR2 expression through α2 adrenergic receptor and imidazoline receptor.
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http://dx.doi.org/10.1016/j.biopha.2017.04.047DOI Listing
June 2017

Indirect ultraviolet detection of alkaline earth metal ions using an imidazolium ionic liquid as an ultraviolet absorption reagent in ion chromatography.

J Sep Sci 2017 Apr 21;40(8):1660-1666. Epub 2017 Mar 21.

College of Chemistry and Chemical Engineering, Harbin Normal University, Harbin, China.

A convenient and versatile method was developed for the separation and detection of alkaline earth metal ions by ion chromatography with indirect UV detection. The chromatographic separation of Mg , Ca , and Sr was performed on a carboxylic acid base cation exchange column using imidazolium ionic liquid/acid as the mobile phase, in which the imidazolium ionic liquid acted as an UV-absorption reagent. The effects of imidazolium ionic liquids, detection wavelength, acids in the mobile phase, and column temperature on the retention of Mg , Ca , and Sr were investigated. The main factors influencing the separation and detection were the background UV absorption reagent and the concentration of hydrogen ion in ion chromatography with indirect UV detection. The successful separation and detection of Mg , Ca , and Sr within 14 min were achieved using the selected chromatographic conditions, and the detection limits (S/N = 3) were 0.06, 0.12, and 0.23 mg/L, respectively. A new separation and detection method of alkaline earth metal ions by ion chromatography with indirect UV detection was developed, and the application range of ionic liquids was expanded.
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http://dx.doi.org/10.1002/jssc.201601297DOI Listing
April 2017

Proteomic identification of the oncoprotein STAT3 as a target of a novel Skp1 inhibitor.

Oncotarget 2017 Jan;8(2):2681-2693

Division of Molecular Carcinogenesis and Targeted Therapy for Cancer, State Key Laboratory of Membrane Biology, Institute of Zoology, Chinese Academy of Sciences, Beijing 100101, China.

The S phase kinase-associated protein 1 (Skp1), an adaptor protein of the Skp1-Cul1-F-box protein complex, binds the ubiquitin E3 ligase Skp2 and is critical to its biological functions. Targeting of Skp1 by a small compound 6-O-angeloylplenolin (6-OAP) results in dissociation and degradation of Skp2 and mitotic arrest of lung cancer cells. Here, by using a proteome microarray containing 16,368 proteins and a biotinylated 6-OAP, we identified 99 proteins that could bind 6-OAP, with Skp1 and STAT3 sitting at the central position of the 6-OAP interactome. 6-OAP formed hydrogen bonds with Ser611/Ser613/Arg609 at the SH2 domain of STAT3 and inhibited the constitutive and interleukin-6-induced phosphorylated STAT3 (pSTAT3), leading to inhibitory effects on lung cancer cells and suppression of Skp2 transcription. STAT3 was overexpressed in tumor samples compared to counterpart normal lung tissues and was inversely associated with prognosis of the patients. 6-OAP inhibited tumor growth in SCID mice intravenously injected with lung cancer cells, and downregulated both STAT3 and Skp2 in tumor samples. Given that 6-OAP is a Skp1 inhibitor, our data suggest that this compound may target Skp1 and STAT3 to suppress Skp2, augmenting its anti-lung cancer activity.
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http://dx.doi.org/10.18632/oncotarget.13153DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5356833PMC
January 2017

Proteomic identification of the oncoprotein STAT3 as a target of a novel Skp1 inhibitor.

Oncotarget 2017 Jan;8(2):2681-2693

Division of Molecular Carcinogenesis and Targeted Therapy for Cancer, State Key Laboratory of Membrane Biology, Institute of Zoology, Chinese Academy of Sciences, Beijing 100101, China.

The S phase kinase-associated protein 1 (Skp1), an adaptor protein of the Skp1-Cul1-F-box protein complex, binds the ubiquitin E3 ligase Skp2 and is critical to its biological functions. Targeting of Skp1 by a small compound 6-O-angeloylplenolin (6-OAP) results in dissociation and degradation of Skp2 and mitotic arrest of lung cancer cells. Here, by using a proteome microarray containing 16,368 proteins and a biotinylated 6-OAP, we identified 99 proteins that could bind 6-OAP, with Skp1 and STAT3 sitting at the central position of the 6-OAP interactome. 6-OAP formed hydrogen bonds with Ser611/Ser613/Arg609 at the SH2 domain of STAT3 and inhibited the constitutive and interleukin-6-induced phosphorylated STAT3 (pSTAT3), leading to inhibitory effects on lung cancer cells and suppression of Skp2 transcription. STAT3 was overexpressed in tumor samples compared to counterpart normal lung tissues and was inversely associated with prognosis of the patients. 6-OAP inhibited tumor growth in SCID mice intravenously injected with lung cancer cells, and downregulated both STAT3 and Skp2 in tumor samples. Given that 6-OAP is a Skp1 inhibitor, our data suggest that this compound may target Skp1 and STAT3 to suppress Skp2, augmenting its anti-lung cancer activity.
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http://dx.doi.org/10.18632/oncotarget.13153DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5356833PMC
January 2017

Synchronous vitellogenin expression and sexual maturation during migration are negatively correlated with juvenile hormone levels in Mythimna separata.

Sci Rep 2016 09 15;6:33309. Epub 2016 Sep 15.

State Key Laboratory for Biology of Plant Diseases and Insect Pests, Institute of Plant Protection, Chinese Academy of Agricultural Sciences, Beijing 100193, China.

Annual migration of pests between different seasonal habitats can lead to serious crop damage. Reproductive immaturity is generally associated with the migratory process (oogenesis-flight syndrome), but the mechanism of reproductive development during migration varies unpredictably. Here, the vitellogenin gene (MsVg) and three key regulatory enzyme genes (MsJhamt, MsJheh and MsJhe) related to juvenile hormone (JH) synthesis and degradation were identified and characterized in Mythimna separata. The relative expression of MsVg varied significantly in response to seasonal changes and was significantly correlated with stages of ovarian development. The relatively low levels of JH titer did not differ significantly in male moths but slightly increased in female adults during the migratory season, which was consistent with changes in mRNA levels for MsJhamt, MsJheh and MsJhe. JH titer was negatively associated with relative seasonal levels of vitellogenin mRNA transcripts and with ovarian development in migrating M. separata. The synchrony of MsVg expression with sexual maturation highlighted the potential of MsVg transcript levels to serve as an index to monitor the adult reproductive status. In addition, the level of JH and sexual maturity were correlated with the extent of JH in regulating the MsVg expression and reproduction during seasonal northern and southern migration.
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http://dx.doi.org/10.1038/srep33309DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5024112PMC
September 2016

[Estimating Surface Broadband Emissivity of the Taklimakan Desert with FTIR and MODIS Data].

Guang Pu Xue Yu Guang Pu Fen Xi 2016 Aug;36(8):2414-9

Surface broadband emissivity in the thermal infrared region is an important parameteras for the studies of the surface energy balance. This paper analyzed and offered an equation to estimate the surface broadband emissivity for the spectral domains 8~14 μm against the MODIS data, and then, the distribution characteristic of surface emissivity for Taklimakan Desert was obtained with this equation. Firstly, along two highways crossing the Taklimakan Desert, twenty sample sites were selected and their spectral of broadband emissivity were observed with Fourier Transform Infrared spectrometer (FTIR). Secondly, using the Moderate Resolution Imaging Spectrometer (MODIS) land surface temperature and emissivity product MOD11A1 and MOD11C1, derived emissivities in three thermal infrared channels 29 (8.4~8.7 μm), 31 (10.78~11.28 μm) and 32 (11.77~12.27 μm) and MODIS surface reflectance products MOD09A1, derived reflectance in near-infrared channel 7 (2.105~2.155 μm), developing an empirical regression equation to convert these spectral emissivities and reflectance to a broadband emissivity. The FTIR data were used to determine the coefficients of the regression equation, another part of FTIR data were used to investigate the accuracy of equation. It was found that the equation consist of MODIS channels 29, 31 and 32 has more accuracy; furthermore, the accuracy is improved when channel 7 data was added in the regression equation. The root mean square error (RMSE) and Bias were 0.004 5 and 0.000 1, respectively. Comparing to other six equations originated from literatures, which also estimate the surface broadband emissivity from narrowband emissivities. The RMSE and Bias of our equation are lower one order and two orders of magnitude than other six equations, respectively. Lastly, our equation is applied in the Taklimakan Desert area to build a distribution image of emissivity based on MODIS data. It demonstrates that the emissivity of Taklimakan Desert is in the range of 0.880~0.910 over the central regions, the averaged value is 0.906; The emissivity is in the range of 0.910~0.940 where the areas covered by spare vegetation; The emissivity is in range of 0.950~0.980 where the regions near to the oasis.
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August 2016

Ion chromatography with the indirect ultraviolet detection of alkali metal ions and ammonium using imidazolium ionic liquid as ultraviolet absorption reagent and eluent.

J Sep Sci 2016 Aug 1;39(16):3156-62. Epub 2016 Aug 1.

College of Chemistry and Chemical Engineering, Harbin Normal University, Harbin, China.

Indirect ultraviolet detection was conducted in ultraviolet-absorption-agent-added mobile phase to complete the detection of the absence of ultraviolet absorption functional group in analytes. Compared with precolumn derivatization or postcolumn derivatization, this method can be widely used, has the advantages of simple operation and good linear relationship. Chromatographic separation of Li(+) , Na(+) , K(+) , and NH4 (+) was performed on a carboxylic acid base cation exchange column using imidazolium ionic liquid/acid/organic solvent as the mobile phase, in which imidazolium ionic liquids acted as ultraviolet absorption reagent and eluting agent. The retention behaviors of four kinds of cations are discussed, and the mechanism of separation and detection are described. The main factors influencing the separation and detection were the background ultraviolet absorption reagent and the concentration of hydrogen ion in the ion chromatography-indirect ultraviolet detection. The successful separation and detection of Li(+) , Na(+) , K(+) , and NH4 (+) within 13 min was achieved using the selected chromatographic conditions, and the detection limits (S/N = 3) were 0.02, 0.11, 0.30, and 0.06 mg/L, respectively. A new separation and analysis method of alkali metal ions and ammonium by ion chromatography with indirect ultraviolet detection method was developed, and the application range of ionic liquid was expanded.
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http://dx.doi.org/10.1002/jssc.201600585DOI Listing
August 2016

Skp1: Implications in cancer and SCF-oriented anti-cancer drug discovery.

Pharmacol Res 2016 09 26;111:34-42. Epub 2016 May 26.

State Key Laboratory of Membrane Biology, Institute of Zoology, Chinese Academy of Sciences, Beijing 100101, PR China. Electronic address:

In the last decade, the ubiquitin proteasome system (UPS), in general, and E3 ubiquitin ligases, in particular, have emerged as valid drug targets for the development of novel anti-cancer therapeutics. Cullin RING Ligases (CRLs), which can be classified into eight groups (CRL1-8) and comprise approximately 200 members, represent the largest family of E3 ubiquitin ligases which facilitate the ubiquitination-derived proteasomal degradation of a myriad of functionally and structurally diverse substrates. S phase kinase-associated protein 1 (Skp1)-Cullin1-F-Box protein (SCF) complexes are the best characterized among CRLs, which play crucial roles in numerous cellular processes and physiological dysfunctions, such as in cancer biology. Currently, there is growing interest in developing SCF-targeting anti-cancer therapies for clinical application. Indeed, the research in this field has seen some progress in the form of cullin neddylation- and Skp2-inhibitors. However, it still remains an underdeveloped area and needs to design new strategies for developing improved form of therapy. In this review, we venture a novel strategy that rational pharmacological targeting of Skp1, a central regulator of SCF complexes, may provide a novel avenue for SCF-oriented anti-cancer therapy, expected: (i) to simultaneously address the critical roles that multiple SCF oncogenic complexes play in cancer biology, (ii) to selectively target cancer cells with minimal normal cell toxicity, and (iii) to offer multiple chemical series, via therapeutic interventions at the Skp1 binding interfaces in SCF complex, thereby maximizing chances of success for drug discovery. In addition, we also discuss the challenges that might be posed regarding rational pharmacological interventions against Skp1.
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http://dx.doi.org/10.1016/j.phrs.2016.05.027DOI Listing
September 2016

Lethal, sublethal and transgenerational effects of the novel chiral neonicotinoid pesticide cycloxaprid on demographic and behavioral traits of Aphis gossypii (Hemiptera: Aphididae).

Insect Sci 2017 Oct 13;24(5):743-752. Epub 2016 Jul 13.

French National Institute for Agricultural Research (INRA), Sophia-Antipolis, France.

Aphis gossypii Glover (Hemiptera: Aphididae) is a key pest in cotton crops, notably owing to its increasing resistance to commonly used pesticides. Such resistance prompts for the development of integrated pest management (IPM) programs that include novel pesticides being effective against the aphid. In the present study, we assessed lethal and sublethal effects of cycloxaprid, a novel chiral neonicotinoid pesticide developed in China, on A. gossypii. The lethal concentration at 50% (LC ) value of cycloxaprid on A. gossypii was estimated, using the dipping method, at 7.73 mg/L. The impact of a sublethal concentration (LC ) and a lethal concentration (LC ) of cycloxaprid on A. gossypii population growth and feeding behavior (using electrical penetration graph technique [EPG]), and its transgenerational effect were further assessed. Adult longevity and fecundity significantly decreased after exposure to LC or LC of cycloxaprid. Cycloxaprid with sublethal concentrations (especially LC ) had negative effects on phloem ingestion by A. gossypii. Additionally, the offspring of the adults exposed to LC of cycloxaprid had shorter nymphal development duration and adult longevity than the control, and those from LC and LC treatments had lower adult fecundity and net productive rate. We demonstrated that cycloxaprid is a pesticide showing both lethal and sublethal activities, and transgenerational effects on A. gossypii; it may be useful for implementation in IPM programs against this aphid pest.
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http://dx.doi.org/10.1111/1744-7917.12357DOI Listing
October 2017

[Determination of Bioactive Components in Paeonia lactiflora Roots Cultivated in Various Areas by UHPLC].

Zhong Yao Cai 2016 May;39(5):980-5

Objective: To assess the quality of Paeonia lactiflora roots by the multi-bioactive chemical markers.

Methods: Total of66 Paeonia lactiflora roots samples were collected from Sichuan,Zhejiang and Anhui. An UHPLC-DAD technique was employed to quantify the contents of paeoniflorin,hydroypaeoniflorin,abiflorin,pentagalloyglucose,benzoypaeoni-florin,paeonol,gallic and catechin in these samples. These chemical components in each sample were also calculated by Principal Component Analysis( PCA).

Results: The eight bioactive components were good separated in 30 min on the UHPLC chromatogram. The correlation coefficients between peak areas and concentration for these bioactive components were not less than 0. 9990( n = 6). And their recoveries were in the range of95. 94% ~ 100. 92%( n = 6). The contents of paeoniflorin in Paeonia lactiflora roots samples collected from Sichuan,Zhejiang and Anhui were 40. 54 mg / g( n = 23),33. 09 mg / g( n = 22) and 39. 47 mg / g( n = 21),respectively. The values of PCA were 0. 4435( n = 23)for the samples from Sichuan,0. 0122( n = 22) for the samples from Zhejiang and- 4. 9850( n = 21) for the samples from Anhui. The content of paeoniflorin in biennial,triennial,four-year,five-year and six-year old Paeonia lactiflora roots were 24. 76( n = 2),37. 17( n= 16),37. 83( n = 23),39. 71( n = 16) and 37. 45 mg / g( n = 7),respectively.

Conclusion: The developed method can accurately quantify the content of principal bioactive compounds in Paeonia lactiflora roots. The quality is various among Paeonia lactiflora roots cultivated in Sichuan, Zhejiang and Anhui on the basis of paeoniflorin content or the value of PCA,but the quality of Paeonia lactiflora roots cultivated in Sichuan is the best. Moreover, it is suggested Paeonia lactiflora roots should be harvested in third or fourth year based on the output and quality.
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May 2016

Diterpenoid constituents of Euphorbia macrorrhiza.

Phytochemistry 2016 Feb 17;122:246-253. Epub 2015 Dec 17.

The Key Laboratory of Plant Resources and Chemistry of Arid Zone, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, PR China; State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, PR China. Electronic address:

Ten diterpenoids, named macrorilone A-B, macroripremyrsinone A, macrorilathyrone A-B, macrorieuphorone A-B and macroricasbalone A-C, together with ten known diterpenoids, jatrophalone, sikkimenoids A-D, jatrophodione A, latilagascenes F, jolkinol B, 15β-O-benzoyl-5α-hydroxyisolathyrol and jatrophalactone were isolated from the whole plant of Euphorbia macrorrhiza C.A. Mey. These diterpenoids belong to six skeleton-types, including jatropholane, premyrsinane, lathyrane, euphoractin, casbene and rhamnofolane diterpenoids. Their structures were elucidated by extensive analysis of 1D, 2D NMR and HRESIMS spectroscopic data. The absolute configurations of macrorilone B, macroripremyrsinone A and macrorilathyrone A were established by comparing their experimental and calculated electronic circular dichroism (ECD) spectra. Several of the isolated compounds exhibited weak cytotoxicity against the KB and KBv200 cell lines with IC50 values ranging from 21.19 to 47.87μM. Some also showed multidrug resistance (MDR) reversal activity, among which macrorilathyrone B exhibited a remarkable inhibitory effect on P-gp-mediated drug exclusion.
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http://dx.doi.org/10.1016/j.phytochem.2015.12.003DOI Listing
February 2016