bluuebunny/crossref_metadata_2025 huggingface dataset:
Antimalarial Drugs Enhance the Cytotoxicity of 5-Aminolevulinic Acid-Based Photodynamic Therapy against the Mammary Tumor Cells of Mice In Vitro
Authors: Osaki Tomohiro , Takahashi Kiwamu , Ishizuka Masahiro , Tanaka Tohru , Okamoto Yoshiharu
Published: October 2019

Artemisinin and its derivatives, including artesunate (ART) and artemether (ARM), exert anticancer effects in the micromolar range in drug and radiation-resistant cell lines. Artemisinin has been reported to sensitize cervical cancer cells to radiotherapy. In the present study, we determined whether ART and ARM could enhance the cytotoxicity of 5-aminolevulinic acid (5-ALA)-based photodynamic therapy (PDT) against the mammary tumor cells of mice. The corrected PpIX fluorescence intensities in the control, 5-ALA, 5-ALA + ART, and 5-ALA + ARM groups were 3.385 ± 3.730, 165.7 ± 33.45, 139.0 ± 52.77, and 165.4 ± 51.10 a.u., respectively. At light doses of 3 and 5 J/cm2, the viability of 5-ALA-PDT-treated cells significantly decreased with ART (p < 0.01 and p < 0.01) and ARM treatment (p < 0.01 and p < 0.01). Besides, the number of annexin V-FITC and ethidium homodimer III-positive cells was greater in the 5-ALA-PDT with ARM group than that in the other groups. N-acetylcysteine could not significantly inhibit the percentages of apoptotic cells or inviable cells induced by 5-ALA-PDT with ARM. These reactive oxygen species-independent mechanisms might enhance cytotoxicity in 5-ALA-PDT with ARM-treated tumor cells, suggesting that the use of 5-ALA-PDT with ARM could be a new strategy to enhance PDT cytotoxicity against tumor cells. However, as these results are only based on in vitro studies, further in vivo investigations are required.
Simultaneous Quantitative Analysis of Six Isothiazolinones in Water-Based Adhesive Used for Food Contact Materials by High-Performance Liquid Chromatography–Tandem Mass Spectrometry (HPLC–MS/MS)
Authors: Zhong Huaining , Li Zicheng , Chen Sheng , Zeng Ying , Zheng Jianguo , Zeng You , Li Dan
Published: October 2019

In this study, a target analytical approach using high-performance liquid chromatography–tandem mass spectrometry (HPLC–MS/MS) was developed to simultaneously determine six isothiazolinones containing 2-Methylisothiazol-3(2H)-one (MI), 5-Chloro-2-methyl-4-isothiazolin-3-one (CMI), 1,2-benzisothiazolin-3-one (BIT), 2-Octyl-3(2H)-isothiazolinone (OIT), Dichlorooctylisothiazolinone (DCOIT), and 2-methyl-1,2-benzisothiazolin-3-one (MBIT) in water-based adhesive used for food contact materials. The main factors affecting extraction efficiency such as extraction method, extraction time, extraction solvent, and solid–liquid ratio have been evaluated by using real adhesive samples. Multiple-reaction monitoring (MRM) was used for the qualitative and quantitative analyses of targeted isothiazolinones. This method was demonstrated as an effective and reliable technique for detecting multiple isothiazolinones with satisfactory recoveries (81.5~107.3%), and the limits of detection (LOD) and quantification (LOQ) were obtained at a low level. This method was validated and applied to the determination of six isothiazolinones in commercial water-based adhesives. The present results revealed that these adhesives contained a combination of isothiazolinones (BIT, MI, CMI, and MBIT) with the concentration ranging from 2.27 to 123.5 mg/kg. To our knowledge, it is the first time it has been reported that MBIT was detected in water-based adhesives used for food contact materials, which requires a further investigation for its migration to food and the risk to human health.
A Comparative Characterization of Physicochemical and Antioxidants Properties of Processed Heterotrigona itama Honey from Different Origins and Classification by Chemometrics Analysis
Authors: Shamsudin Sharina , Selamat Jinap , Sanny Maimunah , A.R. Shamsul Bahari , Jambari Nuzul Noorahya , Khatib Alfi
Published: October 2019

Stingless bee honey produced by Heterotrigona itama from different botanical origins was characterised and discriminated. Three types of stingless bee honey collected from acacia, gelam, and starfruit nectars were analyzed and compared with Apis mellifera honey. The results showed that stingless bee honey samples from the three different botanical origins were significantly different in terms of their moisture content, pH, free acidity, total soluble solids, colour characteristics, sugar content, amino acid content and antioxidant properties. Stingless bee honey was significantly different from Apis mellifera honey in terms of physicochemical and antioxidant properties. The amino acid content was further used in the chemometrics analysis to evaluate the role of amino acid in discriminating honey according to botanical origin. Partial least squares-discriminant analysis (PLS-DA) revealed that the stingless bee honey was completely distinguishable from Apis mellifera honey. Notably, a clear distinction between the stingless bee honey types was also observed. The specific amino acids involved in the distinction of honey were cysteine for acacia and gelam, phenylalanine and 3-hydroxyproline for starfruit, and proline for Apis mellifera honey. The results showed that all honey samples were successfully classified based on amino acid content.
Antiproliferative Aspect of Benzimidazole Derivatives’ Activity and Their Impact on NF-κB Expression
Authors: Błaszczak-Świątkiewicz Katarzyna
Published: October 2019

Benzimidazoles belong to a new class of bioreductive agents with cytotoxic activity towards solid tumor cells, especially in their first stage of growth, which is characterized by low oxygen concentration. Bioreductive agents represent a class of prodrugs that target hypoxic tumor cells. Their bioactivity depends on the reactivity of their functional chemical groups. Their efficacy requires metabolic reduction and subsequent generation of toxic prodrugs. Chemoresistance of tumor cells is a major problem for successful antitumor therapy for many types of tumors, especially for breast cancer. The present study was performed to assess the effect of the antiproliferation activity of the tested benzimidazoles by way of NF-κB expression inhibition. The activity of the tested compounds on T47D and MCF7 cells was examined by WST, western blot, NF-κB transactivation assay, and apoptotic cell population analysis. Compound 3 was highly cytotoxically active against T47D cells, especially in hypoxic conditions. Its IC50 of 0.31 ± 0.06 nM, although weaker than tirapazamine, was significantly higher than the other tested compounds (2.4–3.0 fold). The increased bax protein expression upon exposure to the tested compounds indicated intercellular apoptotic pathway activity, with tumor cell death by way of apoptosis. Increased bax protein synthesis and apoptotic cell dominance upon treatment, especially with N-oxide derivatives (92% apoptotic cells among T47D cell populations during treatment with compound 3), were correlated with each other. Additionally, both increased bax protein and decreased NF-κB protein expression supported antiproliferative activity via NF-κB–DNA binding inhibition associated with the tested compounds. Compound 3 appeared to be the strongest inhibitor of NF-κB expression in hypoxic conditions (the potency against NF-κB expression was about 75% of that of tirapazamine). The present studies involving this class of heterocyclic small molecules proved their potential usefulness in anticancer therapy as compounds be able to limit tumor cell proliferation and reverse drug resistance by NF-κB repression.
Fabrication of Spherical Titania Inverse Opal Structures Using Electro-Hydrodynamic Atomization
Authors: Lim Jong-Min , Jeong Sehee
Published: October 2019

Spherical PS/HEMA opal structure and spherical titania inverse opal structure were fabricated by self-assembly of colloidal nanoparticles in uniform aerosol droplets generated with electro-hydrodynamic atomization method. When a solution of PS/HEMA nanoparticles with uniform size distribution was used, PS/HEMA nanoparticles self-assembled into a face-centered cubic (FCC) structure by capillary force with the evaporation of the solvent in aerosol droplet, resulting in a spherical opal structure. When PS/HEMA nanoparticles and anatase titania nanoparticles were dispersed simultaneously into the solution, titania nanoparticles with relatively smaller size were assembled at the interstitial site of PS/HEMA nanoparticles packed in the FCC structure, resulting in a spherical opal composite structure. Spherical titania inverse opal structure was fabricated after removing PS/HEMA nanoparticles from the spherical opal composite structure by calcination.
Anti-Inflammatory Effects of Formononetin 7-O-phosphate, a Novel Biorenovation Product, on LPS-Stimulated RAW 264.7 Macrophage Cells
Authors: Kim Min-Seon , Park Jin-Soo , Chung You Chul , Jang Sungchan , Hyun Chang-Gu , Kim Seung-Young
Published: October 2019

Biorenovation is a microbial enzyme-catalyzed structural modification of organic compounds with the potential benefits of reduced toxicity and improved biological properties relative to their precursor compounds. In this study, we synthesized a novel compound verified as formononetin 7-O-phosphate (FMP) from formononetin (FM) using microbial biotransformation. We further compared the anti-inflammatory properties of FMP to FM in lipopolysaccharide (LPS)-treated RAW264.7 macrophage cells. We observed that cell viabilities and inhibitory effects on LPS-induced nitric oxide (NO) production were greater in FMP-treated RAW 264.7 cells than in their FM-treated counterparts. In addition, FMP treatment suppressed the production of proinflammatory cytokines such as prostaglandin-E2 (PGE2), interleukin-6 (IL-6), and interleukin-1β (IL-1β) in a dose-dependent manner and concomitantly decreased the mRNA expression of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2). We also found that FMP exerted its anti-inflammatory effects through the downregulation of the extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK), and nuclear factor kappa B (NF-κB) signaling pathways. In conclusion, we generated a novel anti-inflammatory compound using biorenovation and demonstrated its efficacy in cell-based in vitro assays.
Chemical Constituents of Stems and Leaves of Tagetespatula L. and Its Fingerprint
Authors: Wang Yu-Meng , Ran Xiao-Ku , Riaz Muhammad , Yu Miao , Cai Qian , Dou De-Qiang , Metwaly Ahmed M. , Kang Ting-Guo , Cai De-Cheng
Published: October 2019

Tagetespatula L. is a widely cultivated herbal medicinal plant in China and other countries. In this study, two new 2, 3-dihydrobenzofuran glucosides (1, 2) and fourteen known metabolites (3–16) were isolated from the stems and leaves of T. patula (SLT). The chemical structures of the isolated compounds were characterized comprehensively based on one- and two-dimensional NMR spectroscopy and high resolution mass spectrometry. Absolute configurations of compounds 1 and 2 were determined by ECD calculations. Compounds 1 and 2 exhibited moderate in vitro inhibitory activities against human gastric cancer cell lines (AGS) with IC50 values of 41.20 μmol/L and 30.43 μmol/L, respectively. The fingerprint profiles of stems and leaves of T. patula with three color types of flowers (Janie Yellow Bright, Jinmen Orange, Shouyao Red and Yellow color) were established by high-performance liquid chromatography (HPLC). Ten different batches of stems and leaves were examined as follow: Shouyao Red and Yellow color (1, 2, 3), Janie Yellow Bright (4, 5, 6, 7) and Jinmen Orange (8, 9, 10). Twenty-two common peaks were identified with similarity values ranging from 0.910 to 0.977. Meanwhile, the average peak area of SLT in the three types of flowers was different and it was the highest in Janie Yellow Bright.
Bicyclo [6.3.0] Undecane Sesquiterpenoids: Structures, Biological Activities, and Syntheses
Authors: Qin Guo-Fei , Liang Hong-Bao , Liu Wen-Xiu , Zhu Feng , Li Ping-Lin , Li Guo-Qiang , Yao Jing-Chun
Published: October 2019

Sesquiterpenoids constitute a marvelously varied group of natural products that feature a vast array of molecular architectures. Among them, the unusual bicyclo [6.3.0] undecane sesquiterpenoids are one of the most representative. To date, only approximately 42 naturally occurring compounds with this unique scaffold, which can be classified into seven different groups, have been reported. As the first-found member of each type, dactylol, asteriscanolide, dumortenol, toxicodenane C, and capillosanane S are characteristic of the four methyl groups on the five-eight-membered ring system. Only 11-hydroxyjasionone and sinuketal decorate the core with an isopropyl group. These natural products exhibit a wide range of bioactivities, including antifouling, anti-inflammatory, immune suppression, cytotoxic, antimutagenic, antiplasmodial, and antiviral activities. It was noted that some total syntheses of precapnellane-sesquiterpenoids (dactylol, poitediol, precapnelladiene), asteriscanolide, and 11-hydroxyjasionone have been achieved, because their cyclooctanoid core represents an important target for the development of synthetic strategies to prepare eight-membered ring-containing compounds. This review focuses on these natural sesquiterpenoids and their biological activities and synthesis, and aims to provide a foundation for further research of these interesting compounds.
Appraisal of Comparative Therapeutic Potential of Undoped and Nitrogen-Doped Titanium Dioxide Nanoparticles
Authors: Ahmad Muhammad Arslan , Yuesuo Yang , Ao Qiang , Adeel Muhammad , Hui Zhang Yan , Javed Rabia
Published: October 2019

Nitrogen-doped and undoped titanium dioxide nanoparticles were successfully fabricated by simple chemical method and characterized using x-ray diffraction (XRD), scanning electron microscopy (SEM), energy dispersive x-ray (EDX), and transmission electron microscopy (TEM) techniques. The reduction in crystalline size of TiO2 nanoparticles (from 20–25 nm to 10–15 nm) was observed by TEM after doping with N. Antibacterial, antifungal, antioxidant, antidiabetic, protein kinase inhibition and cytotoxic properties were assessed in vitro to compare the therapeutic potential of both kinds of TiO2 nanoparticles. All biological activities depicted significant enhancement as a result of addition of N as doping agent to TiO2 nanoparticles. Klebsiella pneumoniae has been illuminated to be the most susceptible bacterial strain out of various Gram-positive and Gram-negative isolates of bacteria used in this study. Good fungicidal activity has been revealed against Aspergillus flavus. 38.2% of antidiabetic activity and 80% of cytotoxicity has been elucidated by N-doped TiO2 nanoparticles towards alpha-amylase enzyme and Artemia salina (brine shrimps), respectively. Moreover, notable protein kinase inhibition against Streptomyces and antioxidant effect including reducing power and % inhibition of DPPH has been demonstrated. This investigation unveils the more effective nature of N-doped TiO2 nanoparticles in comparison to undoped TiO2 nanoparticles indicated by various biological tests. Hence, N-doped TiO2 nanoparticles have more potential to be employed in biomedicine for the cure of numerous infections.
Synthesis and Antiplasmodial Activity of 1,2,3-Triazole-Naphthoquinone Conjugates
Authors: Oramas-Royo Sandra , López-Rojas Priscila , Amesty Ángel , Gutiérrez David , Flores Ninoska , Martín-Rodríguez Patricia , Fernández-Pérez Leandro , Estévez-Braun Ana
Published: October 2019

A series of 34 1,2,3-triazole-naphthoquinone conjugates were synthesized via copper-catalyzed cycloaddition (CuAAC). They were evaluated for their in vitro antimalarial activity against chloroquine-sensitive strains of Plasmodium falciparum and against three different tumor cell lines (SKBr-3, MCF-7, HEL). The most active antimalarial compounds showed a low antiproliferative activity. Simplified analogues were also obtained and some structure–activity relationships were outlined. The best activity was obtained by compounds 3s and 3j, having IC50 of 0.8 and 1.2 μM, respectively. Molecular dockings were also carried on Plasmodium falciparum enzyme dihydroorotate dehydrogenase (PfDHODH) in order to rationalize the results.
Biocide Potentiation Using Cinnamic Phytochemicals and Derivatives
Authors: Malheiro Joana F. , Maillard Jean-Yves , Borges Fernanda , Simões Manuel
Published: October 2019

Surface disinfection is of utmost importance in the prevention of bacterial infections. This study aims to assess the ability of ten phytochemicals and related derivatives as potentiators of two commonly used biocides—cetyltrimethylammonium bromide (CTAB) and lactic acid (LA). LA in combination with cinnamic, hydrocinnamic, α-methylcinnamic, and α-fluorocinnamic acids had a factional inhibitory concentration index (FICI) ≤ 1 for Escherichia coli and Staphylococcus aureus. Several phytochemicals/derivatives in combination with biocides improved the biocidal efficacy against early sessile bacteria. The most effective combination was LA with allyl cinnamate (2.98 ± 0.76 log CFU·cm−2 reduction) against E. coli. The combination with CTAB was successful for most phytochemicals/derivatives with a maximum bactericidal efficacy against sessile E. coli when combined with allyl cinnamate (2.20 ± 0.07 log CFU·cm−2 reduction) and for S. aureus when combined with α-methylcinnamic acid (1.68 ± 0.30 log CFU·cm−2 reduction). This study highlights the potential of phytochemicals and their derivatives to be used in biocide formulations.
Effects of the Essential Oil from Pistacia lentiscus Var. chia on the Lateral Line System and the Gene Expression Profile of Zebrafish (Danio rerio)
Authors: Serifi Iliana , Tzima Eleni , Bardouki Haido , Lampri Evangeli , Papamarcaki Thomais
Published: October 2019

Mastic essential oil exhibits anti-bacterial, anti-inflammatory, and anti-oxidant properties. With the growing interest of the use of mastic oil in the food and pharmaceutical industry, systematic in vivo studies are needed to address controlled usage and safety issues. In the present work we evaluated the safety of mastic oil using as a model the zebrafish lateral line system. In addition, we studied the gene expression profile of zebrafish fed with mastic oil-supplemented diet using microarray analysis. Our results showed that the hair cells of lateral line neuromasts are functional upon exposure of zebrafish larvae up to 20 ppm of mastic essential oil, while treatment with higher concentrations, 100 and 200 ppm, resulted in increased larvae mortality. Dietary supplementation of zebrafish with mastic essential oil led to differential expression of interferon response-related genes as well as the immune responsive gene 1 (irg1) that links cellular metabolism with immune defense. Notably, mucin 5.2, a constituent of the mucus hydrogel that protects the host against invading pathogens, was up-regulated. Our in vivo work provides information concerning the safety of mastic essential oil use and suggests dietary effects on gene expression related with the physical and immunochemical properties of the gastrointestinal system.
Screening of the Hepatotoxic Components in Fructus Gardeniae and Their Effects on Rat Liver BRL-3A Cells
Authors: Li Chunnan , Lan Meng , Lv Jingwei , Zhang Ye , Gao Xiaochen , Gao Xu , Dong Lihua , Luo Guangming , Zhang Hui , Sun Jiaming
Published: October 2019

Fructus Gardeniae (FG) is a common Chinese medicine and food. However, the toxicity of FG has drawn increasing concern, especially its hepatotoxicity. The purpose of this study was to screen the hepatotoxic components of FG and evaluate their effects on rat liver BRL-3A cells. The chemical composition of FG was determined by HPLC-ESI-MS. CCK-8 assay was used to evaluate the cytotoxicity of ten chemical components from FG, and then the toxic components with significant inhibitory activity were selected for further study. The results showed that geniposide, genipin, genipin-1-gentiobioside, gardenoside, and shanzhiside all suppress cells viability. Apoptosis assays further indicated that geniposide and its metabolite genipin are the main hepatotoxic components of FG. Pretreatment of cells with geniposide or genipin increased the levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), and alkaline phosphatase (ALP). The activities of superoxide dismutase (SOD) and glutathione (GSH) were decreased, while the malondialdehyde (MDA) level was increased. The cell contents of tumor necrosis factor (TNF-α), interleukin-6 (IL-6), and nitric oxide (NO) were also increased. Molecular docking simulations were used to investigate the mechanism of FG-induced hepatotoxicity, revealing that geniposide and genipin bind strongly to the pro-inflammatory factor TNFR1 receptor of the NF-κB and MAPK signaling pathways. The obtained results strongly indicate that the hepatotoxicity of FG is caused by iridoids compounds. Genipin had the most significant hepatotoxic effect. These toxic substances destroy the cell antioxidant defense system, increasing inflammatory injury to the liver cells and leading to apoptosis and even necrosis. Thus, this study lays a foundation for toxicology research into FG and its rational application.
Investigation of Site-Specific Differences in Glycan Microheterogeneity by N-Glycopeptide Mapping of VEGFR-IgG Fusion Protein
Authors: Hahm Young Hye , Lee Ju Yeon , Ahn Yeong Hee
Published: October 2019

A biosimilar fusion protein VEGFR-IgG consisting of vascular endothelial growth factor receptors 1 and 2 (VEGFR-1, VEGFR-2) and the Fc portion of human IgG1 was prepared for this study. The prepared fusion protein was expected to possess a total of five N-linked glycosylation sites: two sites in the VEGFR-1 region, two sites in the VEGFR-2 region, and one site in the human IgG Fc region. For site-specific glycan analysis, the fusion protein was hydrolyzed with trypsin, and the resulting tryptic digests were analyzed by liquid chromatography–electrospray ionization tandem mass spectrometry (LC-ESI MS/MS). The expected N-linked glycosylation sites were successfully identified and site-specific glycopeptide mapping was completed by Integrated GlycoProteome Analyzer (I-GPA) for the resulting raw tandem mass data. Finally, it was clearly confirmed that N-linked glycans for each glycosylation site showed significantly different patterns in microheterogeneity, which may indicate certain functions for each glycosylation site in the protein. Based on the mapping results, the unique features in glycan microheterogeneity for the five glycosylation sites of VEGFR-IgG fusion protein were compared site-specifically and further discussed to understand the functional meaning of each glycosylation pattern.
Identification and Quantification of β-Sitosterol β-d-Glucoside of an Ethanolic Extract Obtained by Microwave-Assisted Extraction from Agave angustifolia Haw
Authors: López-Salazar Herminia , Camacho-Díaz Brenda Hildeliza , Ávila-Reyes Sandra Victoria , Pérez-García Ma Dolores , González- Cortazar Manases , Arenas Ocampo Martha L. , Jiménez-Aparicio Antonio R.
Published: October 2019

β-sitosterol β-d-glucoside (BSSG) was extracted from “piña” of the Agave angustifolia Haw plant by microwave-assisted extraction (MAE) with a KOH solution such as a catalyst and a conventional maceration method to determine the best technique in terms of yield, extraction time, and recovery. The quantification and characterization of BSSG were done by high-performance thin layer chromatography (HPTLC), Fourier-transform infrared spectroscopy (FT-IR), and high-performance liquid chromatography−electrospray ionization−mass spectrometry (HPLC-ESI-MS). With an extraction time of 5 s by MAE, a higher amount of BSSG (124.76 mg of β-sitosterol β-d-glucoside/g dry weight of the extract) than those for MAE extraction times of 10 and 15 s (106.19 and 103.97 mg/g dry weight respectively) was shown. The quantification of BSSG in the extract obtained by 48 h of conventional maceration was about 4–5 times less (26.67 mg/g dry weight of the extract) than the yields reached by the MAE treatments. MAE achieved the highest amount of BSSG, in the shortest extraction time while preserving the integrity of the compound’s structure.
Structural Identification and Conversion Analysis of Malonyl Isoflavonoid Glycosides in Astragali Radix by HPLC Coupled with ESI-Q TOF/MS
Authors: Zheng Yunfeng , Duan Weiping , Sun Jie , Zhao Chenguang , Cheng Qizhen , Li Cunyu , Peng Guoping
Published: October 2019

In this study, four malonyl isoflavonoid glycosides (MIGs), a type of isoflavonoid with poor structural stability, were efficiently isolated and purified from Astragali Radix by a medium pressure ODS C18 column chromatography. The structures of the four compounds were determined on the basis of NMR and literature analysis. Their major diagnostic fragment ions and fragmentation pathways were proposed in ESI/Q-TOF/MS positive mode. Using a target precursor ions scan, a total of 26 isoflavonoid compounds, including eleven malonyl isoflavonoid glycosides coupled with eight related isoflavonoid glycosides and seven aglycones were characterized from the methanolic extract of Astragali Radix. To clarify the relationship of MIGs and the ratio of transformation in Astragali Radix under different extraction conditions, two MIGs (calycosin-7-O-glycoside-6″-O-malonate and formononetin-7-O-glycoside-6″-O-malonate) coupled with related glycosides (calycosin-7-O-glycoside and formononetin-7-O-glycoside) and aglycones (calycosin and formononetin) were detected by a comprehensive HPLC-UV method. Results showed that MIGs could convert into related glycosides under elevated temperature conditions, which was further confirmed by the conversion experiment of MIGs reference compounds. Moreover, the total contents of MIGs and related glycosides displayed no obvious change during the long-duration extraction. These findings indicated that the quality of Astragali Radix could be evaluated efficiently and accurately by using the total content of MIGs and related glycosides as the quality index.
Asatone and Isoasatone A Against Spodoptera litura Fab. by Acting on Cytochrome P450 Monoxygenases and Glutathione Transferases
Authors: Ling Ruimei , Yang Renyue , Li Ping , Zhang Xiongfei , Shen Tunkai , Li Xiaowen , Yang Quan , Sun Lirong , Yan Jian
Published: October 2019

Asatone and isoasatone A from Asarum ichangense Cheng were determined to be defensive compounds to some insects in a previous investigation. However, the anti-insect activity mechanisms to caterpillar are still unclear. The compounds asatone and isoasatone A from A. ichangense were induced by Spodoptera litura. The anti-insect activity of asatone and isoasatone A to S. litura was further tested by weight growth rate of the insect through a diet experiment. Isoasatone A showed a more significant inhibitory effect on S. litura than asatone on the second day. The concentration of asatone was higher than isoasatone A in the second instar larvae of S. litura after 12 h on the feeding test diet. Both compounds caused mid-gut structural deformation and tissue decay as determined by mid-gut histopathology of S. litura. Furthermore, some detoxification enzyme activity were measured by relative expression levels of genes using a qPCR detecting system. Asatone inhibited the gene expression of the cytochrome P450 monooxygenases (P450s) CYP6AB14. Isoasatone A inhibited the relative expression levels of CYP321B1, CYP321A7, CYP6B47, CYP6AB14, and CYP9A39. Asatone increased the relative gene expression of the glutathione transferases (GSTs) SIGSTe1 and SIGSTo1, in contrast, isoasatone A decreased the relative gene expression of SIGSTe1 by about 33 fold. Neither compound showed an effect on acetylcholinesterase SIAce1 and SIAce2. The mechanism of anti-insect activity by both compounds could be explained by the inhibition of enzymes P450s and GSTs. The results provide new insights into the function of unique secondary metabolites asatone and isoasatone A in genus Asarum, and a new understanding of why A. ichangense is largely free of insect pests.
Structure Water-Solubility Relationship in α-Helix-Rich Films Cast from Aqueous and 1,1,1,3,3,3-Hexafluoro-2-Propanol Solutions of S. c. ricini Silk Fibroin
Authors: Moseti Kelvin O. , Yoshioka Taiyo , Kameda Tsunenori , Nakazawa Yasumoto
Published: October 2019

Silk fibroin (SF) produced by the domesticated wild silkworm, Samia cynthia ricini (S. c. ricini) is attracting increasing interest owing to its unique mechanical properties, biocompatibility, and abundance in nature. However, its utilization is limited, largely due to lack of appropriate processing strategies. Various strategies have been assessed to regenerate cocoon SF, as well as the use of aqueous liquid fibroin (LFaq) prepared by dissolution of silk dope obtained from the silk glands of mature silkworm larvae in water. However, films cast from these fibroin solutions in water or organic solvents are often water-soluble and require post-treatment to render them water-stable. Here, we present a strategy for fabrication of water-stable films from S. c. ricini silk gland fibroin (SGF) without post-treatment. Aqueous ethanol induced gelation of fibroin in the posterior silk glands (PSG), enabling its separation from the rest of the silk gland. When dissolved in 1,1,1,3,3,3-hexafluoro-2-propanol (HFIP), the SGF-gel gave a solution from which a transparent, flexible, and water-insoluble film (SGFHFIP) was cast. Detailed structural characterization of the SGFHFIP as-cast film was carried out and compared to a conventional, water-soluble film cast from LFaq. FTIR and 13C solid-state NMR analyses revealed both cast films to be α-helix-rich. However, gelation of SGF induced by the 40%-EtOH-treatment resulted in an imperfect β-sheet structure. As a result, the SGF-gel was soluble in HFIP, but some β-sheet structural memory remains, and the SGFHFIP as-cast film obtained has some β-sheet content which renders it water-resistant. These results reveal a structure water-solubility relationship in S. c. ricini SF films that may offer useful insights towards tunable fabrication of novel biomaterials. A plausible model of the mechanism that leads to the difference in water resistance of the two kinds of α-helix-rich films is proposed.
Protective Effect and Mechanism of Boswellic Acid and Myrrha Sesquiterpenes with Different Proportions of Compatibility on Neuroinflammation by LPS-Induced BV2 Cells Combined with Network Pharmacology
Authors: MIAO Xiao-dong , ZHENG Li-jie , ZHAO Zi-zhang , SU Shu-lan , ZHU Yue , GUO Jian-ming , SHANG Er-xin , QIAN Da-wei , DUAN Jin-ao
Published: October 2019

Frankincense and myrrha (FM), commonly used as a classical herbal pair, have a wide range of clinical applications and definite anti-inflammatory activity. However, anti-neuroinflammation effects and mechanisms are not clear. In this study, we adopted a lipopolysaccharide (LPS)-induced microglial (BV2) cell model and a network pharmacology method to reveal the anti-neuroinflammatory effects and mechanisms of boswellic acid (BA) and myrrha sesquiterpenes (MS) with different proportions of compatibility. The data showed that the different ratios of BA and MS had different degrees of inhibition of interleukin-1β (IL-1β), IL-6, and inducible nitric oxide synthase (iNOS) mRNA expression, down-regulated the phosphor-nuclear factor kappa B/nuclear factor kappa B (p-NF-ҡB)/(NF-ҡB), phosphorylated protein kinase b/protein kinase b (p-AKT/AKT), and Toll-like receptor 4 (TLR4) protein expression levels, and increased phospho-PI3 kinase (p-PI3K) protein expression levels. When the ratios of BA and MS were 10:1, 5:1, and 20:1, better effective efficacy was exhibited. According to the correlation analysis between the effect index and bioactive substances, it was suggested that 2-methoxy-5-acetoxy -fruranogermacr-1(10)-en-6-one (Compound 1), 3α-acetyloxylanosta-8,24-dien-21-oic acid (Compound 2), 11-keto-boswellic acid (Compound 3), and 3-acetyl-11-keto-β -boswellic acid (Compound 4) made important contributions to the treatment of neuroinflammation. Furthermore, based on the network pharmacological analysis, it was found that these four active compounds acted on 31 targets related to neuroinflammation and were involved in 32 signaling pathways which mainly related to the immune system, cardiovascular system, and nervous system, suggesting that BA and MS could be used to treat neuroinflammation.
Supramolecular Carotenoid Complexes of Enhanced Solubility and Stability—The Way of Bioavailability Improvement
Authors: Focsan A. Ligia , Polyakov Nikolay E. , Kispert Lowell D.
Published: October 2019

Carotenoids are natural dyes and antioxidants widely used in food processing and in therapeutic formulations. However, their practical application is restricted by their high sensitivity to external factors such as heat, light, oxygen, metal ions and processing conditions, as well as by extremely low water solubility. Various approaches have been developed to overcome these problems. In particular, it was demonstrated that application of supramolecular complexes of “host-guest” type with water-soluble nanoparticles allows minimizing the abovementioned disadvantages. From this point of view, nanoencapsulation of carotenoids is an effective strategy to improve their stability during storage and food processing. Also, nanoencapsulation enhances bioavailability of carotenoids via modulating their release kinetics from the delivery system, influencing the solubility and absorption. In the present paper, we present the state of the art of carotenoid nanoencapsulation and summarize the data obtained during last five years on preparation, analysis and reactivity of carotenoids encapsulated into various nanoparticles. The possible mechanisms of carotenoids bioavailability enhancement by multifunctional delivery systems are also discussed.
A Potential Anti-Tumor Herb Bred in a Tropical Fruit: Insight into the Chemical Components and Pharmacological Effects of Momordicae Semen
Authors: Xu Xiao-Rong , Luo Chuan-Hong , Cao Bo , Xu Run-Chun , Wang Fang , Wei Xi-Chuan , Zhang Ting , Han Li , Zhang Ding-Kun
Published: October 2019

Gac fruit (Momordica cochinchinensis Spreng) is a popular tropical fruit in southeast Asia. What is amazing is that its seeds (Momordicae Semen) and arils are traditional herbs with anti-tumor activity, and have protected human health for more than 1000 years. In recent years, its anti-tumor activity has received extensive attention and research. This manuscript summarized the chemical composition of saponins, fatty acids, volatile constituents, proteins, peptides, and other components from Momordicae Semen (MSE). The effect and mechanism of MSE and its extract on breast cancer, gastric cancer, lung cancer, esophagus cancer, melanomas, and human cervical epithelial carcinoma were discussed. In addition, its antioxidant, anti-inflammatory, and other pharmacological effects were also analyzed. We hope that this review will provide new ideas for the treatment of cancer and other diseases, and become a reference for the further research into complementary and alternative medicine.
The Early Years of 2,2′-Bipyridine—A Ligand in Its Own Lifetime
Authors: Constable Edwin C. , Housecroft Catherine E.
Published: October 2019

The first fifty years of the chemistry of 2,2′-bipyridine are reviewed from its first discovery in 1888 to the outbreak of the second global conflict in 1939. The coordination chemistry and analytical applications are described and placed in the context of the increasingly sophisticated methods of characterization which became available to the chemist in this time period. Many of the “simple” complexes of 2,2′-bipyridine reported in the early literature have been subsequently shown to have more complex structures.
Extraction and Purification of Capsaicin from Capsicum Oleoresin Using a Combination of Tunable Aqueous Polymer-Phase Impregnated Resin (TAPPIR) Extraction and Chromatography Technology
Authors: Lu Yanmin , Cui Bo
Published: October 2019

Capsaicin, which mainly comes from pepper, exhibits anticancer, antioxidant, and anti-obesity properties. This work aims to construct a comprehensive technology for the extraction and purification of capsaicin from capsicum oleoresin. The tunable aqueous polymer phase impregnated HZ816 resins were selected in extraction step. In the extraction process, 3 g of impregnated HZ816 macroporous resin was employed per system. The results showed that a higher molecular weight of Polyethylene glycol (PEG) and 1-ethyl-3-methyl imidazolium acetate ([Emim] [OAc]) are more beneficial to the improvement of the yield of capsaicin. Screening experiment using fractional factorial designs indicated that the amount of sample loading, pH, and concentration of [Emim] [OAc] and PEG 6000 significantly affect the yield of capsaicin. Mathematical models of capsaicin yield in tunable aqueous polymer-phase impregnated resins were established and optimum condition was obtained using response surface methodology. The optimum impregnated phase was the polymer phase of an aqueous two-phase system which contained 18.5% (w/w) PEG6000, 15% (w/w) sodium citrate, and 10% (w/w) [Emim] [OAc] at pH 6.5. Under the optimal conditions, the yield of capsaicin reached 95.82% when the extraction system contains 0.25 g capsicum oleoresin. Ultimately, capsaicinoids extract was purified by reverse-phase resin (SKP-10-4300) chromatographic column. The capsaicin recovery and purity achieved 85% and 92%, respectively.
Silver Quantum Dot Decorated 2D-SnO2 Nanoflakes for Photocatalytic Degradation of the Water Pollutant Rhodamine B
Authors: Siva Kumar Nadavala , Asif Mohammad , Ranjeth Kumar Reddy T. , Shanmugam Gnanendra , Ajbar Abdelhamid
Published: October 2019

Decoration of 2D semiconductor structures with heterogeneous metal quantum dots has attracted considerable attention due to advanced optical, electrical, and catalytic properties that result from the large surface-to-volume ratio associated with these structures. Herein, we report on silver quantum dot decorated 2D SnO2 nanoflakes for the photocatalytic abatement of water effluents, the synthesis of which was achieved through a straightforward and mild hydrothermal procedure. The photocatalysts were systematically investigated using UV–Vis, XRD, electron microscopy (SEM, HR-TEM), EDX, XPS and FTIR. The photocatalytic activity of the nanostructures was evaluated for the abatement of water pollutant rhodamine B (RhB), under light irradiation. The mild hydrothermal synthesis (100 °C) proved highly efficient for the production of large scale Ag quantum dot (QD)/SnO2 nanoflakes for a novel photocatalytic application. The decoration of SnO2 with Ag QDs significantly enhances the synergetic charge transfer, which diminishes the photo-induced electron-hole reunion. Moreover, the plasmonic effect from Ag QDs and 2D-SnO2 structures acts as an electron tank to collect the photo-induced electrons, generating a Schottky barrier between the SnO2 structures and quantum dots. Overall, this resulted in a facile and efficient degradation of RhB, with a rate double that of pristine SnO2.
Cultivar-Dependent Anticancer and Antibacterial Properties of Silver Nanoparticles Synthesized Using Leaves of Different Olea Europaea Trees
Authors: De Matteis Valeria , Rizzello Loris , Ingrosso Chiara , Liatsi-Douvitsa Eva , De Giorgi Maria Luisa , De Matteis Giovanni , Rinaldi Rosaria
Published: October 2019

The green synthesis of nanoparticles (NPs) is currently under worldwide investigation as an eco-friendly alternative to traditional routes (NPs): the absence of toxic solvents and catalysts make it suitable in the design of promising nanomaterials for nanomedicine applications. In this work, we used the extracts collected from leaves of two cultivars (Leccino and Carolea) belonging to the species Olea Europaea, to synthesize silver NPs (AgNPs) in different pH conditions and low temperature. NPs underwent full morphological characterization with the aim to define a suitable protocol to obtain a monodispersed population of AgNPs. Afterwards, to validate the reproducibility of the mentioned synthetic procedure, we moved on to another Mediterranean plant, the Laurus Nobilis. Interestingly, the NPs obtained using the two olive cultivars produced NPs with different shape and size, strictly depending on the cultivar selected and pH. Furthermore, the potential ability to inhibit the growth of two woman cancer cells (breast adenocarcinoma cells, MCF-7 and human cervical epithelioid carcinoma, HeLa) were assessed for these AgNPs, as well as their capability to mitigate the bacteria concentration in samples of contaminated well water. Our results showed that toxicity was stronger when MCF-7 and Hela cells were exposed to AgNPs derived from Carolea obtained at pH 7 presenting irregular shape; on the other hand, greater antibacterial effect was revealed using AgNPs obtained at pH 8 (smaller and monodispersed) on well water, enriched with bacteria and coliforms.
Controlling the Growth Locations of Ag Nanoparticles at Nanoscale by Shifting LSPR Hotspots
Authors: Zhu Qi , Zhang Xiaolong , Wang Yaxin , Zhu Aonan , Gao Renxian , Zhao Xiaoyu , Zhang Yongjun , Chen Lei
Published: October 2019

Controlling chemical reactions by plasma is expected to be a new method for improving the structural properties of substrates. An Au nanojar array was prepared when Au was deposited onto a 2D polystyrene (PS) array. The site-selective chemical growth of Ag nanoparticle rings was realized around the Au nanojar necks by a local surface plasmon resonance (LSPR)-assisted chemical reaction. The catalytic hotspots in the nanostructure array could be controlled by both etching the nanojars and Au or TiO2 sputtering onto the nanojars, which were confirmed by the growth sites of the Ag nanoparticle in the LSPR-assisted chemical reaction. The structure of the nanojars and the electric field distributions of the growing nanoparticles were simulated and analyzed using Finite-Difference Time-Domain. FDTD simulations showed that the changes in the nanojar shape led to the changed hotspot distributions. At the same time, tracking the hotspot shifts in the process of structural change was also achieved by the observation of Ag growth. Nanoarray structure prepared by LSPR-assisted chemical reaction is one of the hot fields in current research and is also of great significance for the application of Surface-Enhanced Raman Scattering.
Influence of Teaching Style on Physical Education Adolescents’ Motivation and Health-Related Lifestyle
Authors: Trigueros Rubén , Mínguez Luis A. , González-Bernal Jerónimo J. , Jahouh Maha , Soto-Camara Raul , Aguilar-Parra José M.
Published: October 2019

According to various WHO reports in 2018, a large number of adolescents worldwide are either overweight or obese. This situation is the result of not following a healthy and balanced diet, combined with a lack of practice of physical activity. In this sense, Physical Education classes could help to solve the problem. The present study seeks to analyze the relationship between the role of the teacher in relation to the structural dimensions of the PE teaching environment and the basic psychological needs and self-motivation of adolescents as determinants of their behaviors related to eating habits and the practice of physical activity. A total of 1127 secondary school adolescents between the ages of 13 and 18 participated in this study. Questionnaires were used: Perceived Autonomy Support Scale, Psychologically Controlling Teaching Scale, Basic Psychological Needs in Physical Education, Frustration of Psychological Needs in PE context, Physical Activity Class Satisfaction Questionnaire, Perceived Locus of Causality Revised, and WHO’s Global school-based student health survey. A structural equations model was elaborated to explain the causal relationships between the variables. The results showed that autonomy support positively predicted the three structural dimensions of PE classes, while, in contrast, they were negatively predicted by psychological control. The three structural dimensions positively predicted the satisfaction of psychological needs and negatively predicted the thwarting of psychological needs. Self-determined motivation was positively predicted by the satisfaction of psychological needs and negatively predicted by the thwarting of psychological needs. Finally, self-determined motivation positively predicted healthy eating habits and the practice of physical activity and negatively predicted unhealthy eating habits. Certainly, the results obtained in this study support the postulates of the self-determination theory, demonstrating the predictability of PE class context towards the adoption of healthy lifestyle habits, such as a proper diet and the regular practice of physical activity.
Single Nucleotide Polymorphisms in PEMT and MTHFR Genes are Associated with Omega 3 and 6 Fatty Acid Levels in the Red Blood Cells of Children with Obesity
Authors: Serafim Vlad , Chirita-Emandi Adela , Andreescu Nicoleta , Tiugan Diana-Andreea , Tutac Paul , Paul Corina , Velea Iulian , Mihailescu Alexandra , Șerban Costela Lăcrimioara , Zimbru Cristian G. , Puiu Maria , Niculescu Mihai Dinu
Published: October 2019

Polyunsaturated fatty acids (PUFAs) play important roles in health and disease. PUFA levels are influenced by nutrition and genetic factors. The relationship between PUFA composition in red blood cells (RBCs) and genetic variations involved in PUFA metabolism has not been investigated in children with obesity. This study evaluated the association between several genetic variations and PUFA levels in RBCs in children with obesity. One hundred ninety-six children with obesity (101 females, 95 males) were evaluated using anthropometric measurements, dietary intakes, plasma and RBC PUFA quantification, blood biochemistry, and 55 single nucleotide polymorphisms within 14 genes. phosphatidylethanolamine N-methyltransferase (PEMT) rs1109859 and methylenetetrahydrofolate reductase gene (MTHFR) rs4846052 genotypes were associated with PUFA levels in RBCs. PUFA intake did not influence the RBC eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) levels. Higher RBC DHA and EPA levels were observed for PEMT rs1109859 GG and GA genotypes versus the AA genotype. Higher levels of RBC DHA, EPA, arachidonic acid (ARA), and linoleic acid (LA) and were observed for MTHFR rs4846052 TT genotype versus TC and CC genotypes. Genetic variations in PEMT rs1109859 and MTHFR rs4846052 were associated with different PUFA levels in RBC membranes and are estimators for PUFA species in RBCs. Further research is needed to establish whether these genotype-specific alterations are specific to overweight children.
Racial/Ethnic Disparities in Dietary Intake of U.S. Children Participating in WIC
Authors: Zimmer Meghan C. , Rubio Veronica , Kintziger Kristina W. , Barroso Cristina
Published: October 2019

Recent studies have assessed diet quality of low-income U.S. children participating in the Special Supplemental Nutrition Program for Women, Infants, and Children (WIC), but differences by race/ethnicity remain unknown. We assessed racial/ethnic disparities in nutrient intake from dietary sources (not supplements) among children participating in WIC, with a focus on priority nutrients and food groups for future WIC food package revisions, as described in a recent report by the National Academies of Sciences, Engineering, and Medicine (NASEM). We used data from the 2011–2014 National Health and Nutrition Examination Surveys (NHANES) and multivariable linear regression analysis to evaluate relationships between race/ethnicity and nutrient/food group intake of children participating in WIC. All data were analyzed using SAS 9.4 survey procedures, accounting for the complex survey design of the NHANES. Compared to non-Hispanic White children, Hispanic children had diets with better nutrient distribution and lower dietary energy density, while non-Hispanic Black children had diets with poorer nutrient intake. Hispanic children had higher potassium and fiber intake, and consumed more legumes, while non-Hispanic Black children had lower calcium and vitamin D intake, higher sodium intake, and lower total dairy intake, compared to non-Hispanic White children. These findings can inform WIC nutrition education messages and future food package revisions.