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1.
Talanta ; 278: 126459, 2024 Oct 01.
Article in English | MEDLINE | ID: mdl-38941809

ABSTRACT

A novel "double chemical bonding" electrochemical peptide biosensor 2FcP-GA-GDY(Fe)@NMIL-B was developed for highly selective, ultrasensitive, and ultrastable identification of prostate-specific antigen (PSA). The C-Fe-O chemical bond linking Fe-Graphdiyne (Fe-GDY) with NH2-MIL88B(Fe) (NMIL88B) as the first chemical bonding of electrode carrier Fe-GDY@NH2-MIL88B(Fe) (GDY(Fe)@NMIL) significantly accelerates electron transport. With glutaraldehyde (GA) as a crosslinking agent, the Schiff-base -NC- formed by GDY(Fe)@NMIL nanocomposites links the two Fc molecules labeled peptides (2FcP) as the second chemical bonding, facilitating high-density attachment of peptides to the electrode carrier in a firm manner. When the PSA analyte is introduced to identify and cleave the specific peptide, the release of ferrocene from its head leads to a decrease in the electrical signal, enabling sensitive detection. The prepared sensing platform exhibits exceptional analytical performance for PSA with an extended linear response range from 10 fg mL-1 to 50 ng mL-1. Additionally, the detection limit has been significantly reduced to an ultra-low level of only 0.94 fg mL-1, surpassing those reported in most literature by several orders of magnitude. Moreover, the 2FcP-GA-GDY(Fe)@NMIL-B sensor has excellent selectivity and stability while also showcasing great potential for practical application of PSA detection in human serum using the standard addition method.


Subject(s)
Biosensing Techniques , Electrochemical Techniques , Limit of Detection , Peptides , Prostate-Specific Antigen , Prostate-Specific Antigen/blood , Prostate-Specific Antigen/analysis , Prostate-Specific Antigen/chemistry , Electrochemical Techniques/methods , Humans , Biosensing Techniques/methods , Peptides/chemistry , Electrodes , Nanocomposites/chemistry
2.
Eur J Pharmacol ; 946: 175620, 2023 May 05.
Article in English | MEDLINE | ID: mdl-36868291

ABSTRACT

Non-small cell lung cancer (NSCLC) is classified into many subclasses according to the specific kinase mutations. The most common mutation is epidermal growth factor receptor (EGFR) somatic mutation, which has promoted the development of several novel drugs (Tyrosine kinase inhibitors, TKIs). Although various TKIs are recommended as targeted therapy for NSCLC with EGFR mutations in NCCN guidelines, not all patients respond equally to the recommended TKIs, which lead to series of novel compound under development to satisfy actual clinical needs. Based on the structure of afatinib, a marketed drug recommended as the first-line therapy for patients with EGFR mutation, NEP010 was synthesized with structural modification. The antitumor efficacy of NEP010 on mouse tumor xenograft models with different EGFR mutations was determined. Results showed that with minor structural modifications on afatinib, the inhibitory effect of NEP010 on EGFR mutant tumors was significantly improved. Pharmacokinetics test was adopted, and compared with afatinib, the increased tissue exposure of NEP010 may be the potential factor responsible for the increased efficacy. Furthermore, tissue distribution test showed a high concentration of NEP010 in the lung which happens to be the target organ of NEP010 in clinical practice. In conclusion, data obtained suggested that NEP010 has an increased anti-tumor effect via improving pharmacokinetics, and may provide a potent therapeutic option for the patients with EGFR mutation of NSCLC in the future.


Subject(s)
Carcinoma, Non-Small-Cell Lung , Lung Neoplasms , Humans , Animals , Mice , Afatinib/pharmacology , Afatinib/therapeutic use , Carcinoma, Non-Small-Cell Lung/pathology , Lung Neoplasms/pathology , Protein Kinase Inhibitors/adverse effects , ErbB Receptors/genetics , Mutation
3.
Int J Biol Macromol ; 236: 123936, 2023 May 01.
Article in English | MEDLINE | ID: mdl-36894064

ABSTRACT

Recently, ionic conductive hydrogels have attracted extensive attention in the field of flexible pressure sensors due to their mechanical flexibility and high conductivity. However, the trade-off between the high electrical and mechanical properties of ionic conductive hydrogels and the loss of mechanical and electrical properties of traditional high water content hydrogels at low temperature are still the main hurdles in this area. Herein, a rigid Ca-rich silkworm excrement cellulose (SECCa) extracted from silkworm breeding waste was prepared. SEC-Ca was combined with the flexible hydroxypropyl methylcellulose (HPMC) molecules through hydrogen bonding and double ionic bonds of Zn2+ and Ca2+ to obtain the physical network SEC@HPMC-(Zn2+/Ca2+). Then, the covalently cross-linked network of polyacrylamide (PAAM) and the physical network were cross-linked by hydrogen bonding to obtain the physical-chemical double cross-linked hydrogel (SEC@HPMC-(Zn2+/Ca2+)/PAAM). The hydrogel showed excellent compression properties (95 %, 4.08 MPa), high ionic conductivity (4.63 S/m at 25 °C) and excellent frost resistance (possessing ionic conductivity of 1.20 S/m at -70 °C). Notably, the hydrogel can monitor pressure changes in a wide temperature range (-60-25 °C) with high sensitivity, stability and durability. This newly fabricated hydrogel-based pressure sensors can be deemed of great prospects for large-scale application of pressure detection at ultra-low temperatures.


Subject(s)
Bombyx , Cellulose , Animals , Hydrogels , Electric Conductivity , Hypromellose Derivatives , Ions
4.
Int J Mol Sci ; 24(2)2023 Jan 06.
Article in English | MEDLINE | ID: mdl-36674685

ABSTRACT

Osthole (OST) is a simple coumarin derivative with pharmacological effects in many types of cancer cells. However, its role and its mechanism of action in breast cancer 4T1 cells remain unclear. In this study, we explored the effects and potential mechanisms of action of OST in 4T1 cells. The MTT, PI, and Annexin V-FITC/PI methods were used to evaluate the effects of OST-treated and untreated 4T1 cells on viability, cell cycle, and apoptosis, respectively. UPLC-Q-TOF/MS combined with multivariate data analysis was used to screen potential biomarkers relevant to the therapeutic mechanisms of OST. Additionally, mTOR, SREBP1, and FASN protein levels were detected using western blotting in OST-treated and untreated 4T1 cells. OST inhibited 4T1 cell proliferation, blocked the cells from remaining in S-phase, and induced apoptosis. In 4T1 cells, OST mainly affected the phospholipid biosynthesis, methyl histidine metabolism, pyrimidine metabolism, and ß-oxidation of very long chain fatty acid pathways, suggesting that metabolic changes related to lipid metabolism-mediated signaling systems were the most influential pathways, possibly via inhibition of mTOR/SREBP1/FASN signaling. Our findings reveal biomarkers with potential therapeutic effects in breast cancer and provide insight into the therapeutic and metabolic mechanisms of OST in 4T1 cells.


Subject(s)
Breast Neoplasms , Humans , Female , Breast Neoplasms/drug therapy , Coumarins/pharmacology , TOR Serine-Threonine Kinases , Metabolomics , Biomarkers
5.
Front Pharmacol ; 13: 1046402, 2022.
Article in English | MEDLINE | ID: mdl-36506558

ABSTRACT

Plant-derived alkaloids are a kind of very important natural organic compounds. Nitidine chloride is one of the main active ingredients in Zanthoxylum nitidum (Roxb.) DC. which is a frequently-used Chinese herbal medicine. Z. nitidum has many kinds of efficacy, such as activating blood circulation and removing stasis, promoting qi circulation and relieving pain, and detoxication and detumescence. In China, Z. nitidum is usually used for the treatment of gastrointestinal diseases, toothache, and traumatic injury. At present, there are numerous studies of nitidine chloride with regard to its pharmacology, pharmacokinetics, toxicology, etc. However, a systematic, cutting-edge review of nitidine-related studies is extremely lacking. The present paper aimed at comprehensively summarizing the information on the extraction, separation and purification, pharmacology, pharmacokinetics, toxicology and formulation of nitidine chloride. The knowledge included in the present study were searched from the following academic databases involving Web of Science, PubMed, Google scholar, Elsevier, CNKI and Wanfang Data, till July 2022. In terms of nitidine chloride extraction, enzymatic method and ultrasonic method are recommended. Resin adsorption and chromatography were usually used for the separation and purification of nitidine chloride. Nitidine chloride possesses diversified therapeutical effects, such as anti-tumor, anti-inflammation, anti-colitis, anti-malaria, anti-osteoporosis, anti-rheumatoid and so on. According to pharmacokinetics, the intestinal absorption of nitidine chloride is passive diffusion, and it is rarely excreted with urine and feces in the form of prototype drug. Nitidine chloride has a moderate binding to plasma protein, which is independent of the drug concentration. As to toxicology, nitidine chloride showed certain toxicity on liver, kidney and heart. Certain new formulations, such as nanoparticle, microsphere and nano-micelle, could increase the therapeutic effect and decrease the toxicity of nitidine chloride. Despite limitations such as poor solubility, low bioavailability and certain toxicity, nitidine chloride is still a promising natural alkaloid for drug candidates. Extensive and intensive exploration on nitidine chloride is essential to promote the usage of nitidine-based drugs in the clinic practice.

6.
J Immunol Res ; 2022: 5882136, 2022.
Article in English | MEDLINE | ID: mdl-36313178

ABSTRACT

Targeting dendritic cells (DCs) metabolism-related pathways and in-situ activation of DCs have become a new trend in DC-based immunotherapy. Studies have shown that Lycium barbarum polysaccharide can promote DCs function. This study is aimed at exploring the mechanism of LBP affecting DCs function from the perspective of metabolomics. MTT method was used to detect the activity of DC2.4 cells. ELISA kit method was used to detect the contents of IL-6, IL-12, and TNF-α in the supernatant of cells. Ultra-performance liquid chromatography-quadrupole-time-of-flight mass spectrometry (UPLC-Q-TOF/MS) was used to detect general changes in DC2.4 cell metabolism. And then multidistance covariates and bioinformatics, partial least squares-discriminant analysis (PLS-DA) were used to analyze differential metabolites. Finally, metabolic pathway analysis was performed by MetaboAnalyst v5.0. The results showed that LBP had no significant inhibitory effect on the activity of DC2.4 cells at the experimental dose of 50-200 µg/ml. LBP (100 µg/ml) could significantly stimulate DC2.4 cells to secrete IL-6, TNF-α, and IL-12. Moreover, 20 differential metabolites could be identified, including betaine, hypoxanthine, L-carnitine, 5'-methylthioadenosine, orotic acid, sphingomyelin, and L-glutamine. These metabolites were involved 28 metabolic pathways and the top 5 metabolic pathways were aspartate metabolism, pyrimidine metabolism, phenylacetate metabolism, methionine metabolism, and fatty acid metabolism. These results suggest that the effect of LBP on DCs function is related to the regulation of cell metabolism.


Subject(s)
Lycium , Lycium/chemistry , Tumor Necrosis Factor-alpha , Interleukin-6 , Polysaccharides/pharmacology , Dendritic Cells , Interleukin-12
7.
Dalton Trans ; 49(32): 11129-11141, 2020 Aug 18.
Article in English | MEDLINE | ID: mdl-32743621

ABSTRACT

A pair of homologues, [Zn(Hssa)(1,4-bib)·H2O]n (1) and [Zn3(ssa)2(1,4-bib)3·4H2O]n (2), were successfully assembled using the same metals and ligands [H3ssa = 5-sulfosalicylic acid; 1,4-bib = 1,4-bis(1H-imidazol-1-yl)benzene] under solvothermal conditions. Polymer 1 is a two-dimensional (2D) sql network and polymer 2 is a three-dimensional (3D) framework. Polymer 2 can be simplified into two topology types: bct and tfc. The two polymers show significant differences in the fluorescence sensing of metal ions and proton conductivity. Their applications in detecting metal ions and proton conductivity were explored. Polymer 1 shows high sensitivity and selectivity for Fe3+, while polymer 2 can detect Hg2+ ions. The limit of detection was 1.66 µM with Fe3+ for 1 and 0.23 µM with Hg2+ for 2 in water. In addition, both 1 and 2 exhibit high water stability and proton conductivity. At 60 °C and 95% relative humidity, their conductivities were 3.45 × 10-5 and 6.26 × 10-6 S cm-1, respectively. A detailed analysis of the Hirshfeld surface and fingerprints was carried out for 1 and 2 to compare the interactions between the molecules, which is essential for analysing the relationship between their structures and material properties.

8.
J Colloid Interface Sci ; 564: 276-285, 2020 Mar 22.
Article in English | MEDLINE | ID: mdl-31918195

ABSTRACT

Rational design of a stable, highly active non-precious metal-based electrocatalysts for oxygen reduction reaction (ORR) is vitally important for industrial application of fuel cells technology. As a potential alternative of Pt/C catalyst, two-dimensional (2D) porous carbon materials are widely investigated due to the highly accessible surface area and active sites, wherein carbon films doped with a plurality of metals and non-metal elements are rarely reported due to an uncontrollable synthesis process. Here, a bi-metallic (NiCo alloy nanoparticles) and nonmetallic (N) co-doped porous carbon film (Ni-Co-N@CF) is fabricated by a simple controllable and scalable strategy comprising the synthesis of NiCo alloy nanoparticles, modification of organic molecules, and high-temperature carbonization process. The optimized Ni-Co-N@CF catalyst shows an excellent ORR electrocatalytic activity with a larger electrochemically active surface area (2.31 m2 g-1), a higher half-wave potential (0.86 V) and a lower diffusion limited current density (-4.43 mA cm-2) than all the prepared control catalysts. Moreover, the designated catalyst also exhibits high durability and superior methanol tolerance in alkaline media, significantly better than the commercial Pt/C (20 wt%). The superior ORR performance is attributed to the synergetic interactions of ternary doping of Ni/Co/N in the 2D film skeleton, which not only greatly enhances conductivity but also provides more Co-N active sites.

9.
Article in English | MEDLINE | ID: mdl-29849721

ABSTRACT

BACKGROUND: Jinshuibao capsules (JSB) have been widely used to treat early diabetic nephropathy (DN), but the specific effects are still inconsistent. A meta-analysis of randomized controlled trials (RCTs) was conducted to evaluate the clinical efficacy of JSB for early DN. METHODS: Four international databases and four Chinese databases were searched from publication dates to March 1, 2018. The RCTs reporting the results of JSB's specific effects were included, and comparisons were between JSB combined with Angiotensin Receptor Blockers (ARBs) as experimental intervention and ARBs as the control. Included studies' quality was evaluated and the extracted data were analyzed with RevMan 5.3 software. RESULTS: Twenty-six RCTs including 2198 early DN participants were adopted in the meta-analysis. The results showed that, compared with the ARBs alone, JSB could remarkably improve the ORR (OR = 3.84; 95% CI: 2.37~6.24; P < 0.00001) and decrease 24 h UTP (MD = -93.32; 95% CI: -128.60 ~-58.04; P < 0.00001), UAER (MD = -24.02; 95% CI: -30.93 ~-17.11; P < 0.00001), BUN (MD = -0.26; 95%: -0.44 ~-0.08; P = 0.005), Scr (MD = -9.07; 95% CI: -14.26 ~-3.88; P = 0.0006), ACR (MD = -17.55; 95% CI: -22.81 ~-12.29; P < 0.00001), Cys-C (MD = -0.60; 95% CI: -0.88 ~-0.32; P < 0.00001), SBP (MD = -3.08; 95% CI: -4.65 ~-1.52; P = 0.0001), DBP (MD = -2.09; 95% CI: -4.00 ~-0.19; P = 0.03), and TG (MD = -0.36; 95% CI: -0.50 ~-0.21; P < 0.00001). However, it showed no significant differences in TC (MD = -0.32; 95% CI: -0.69~0.04; P = 0.08), FBG (MD = 0.04; 95% CI: -0.39~0.47; P = 0.87), HbA1c (MD = -0.26; 95% CI: -0.59~0.06; P = 0.11), and ß2-MG (MD = -15.61; 95% CI: -32.95~1.73; P = 0.08). CONCLUSIONS: This study indicates that JSB is an effective accessory therapeutic medicine for patients with early DN. It contributes to decreasing blood pressure and the content of triglyceride and improving the renal function of early DN patients. However, there is still a need to further verify the auxiliary therapeutic effect of JSB with more strictly designed RCTs with large sample and multiple centers in the future.

10.
Inorg Chem ; 54(18): 9046-59, 2015 Sep 21.
Article in English | MEDLINE | ID: mdl-26331268

ABSTRACT

A series of uranyl-organic frameworks (UOFs), {[(UO2)2(H2TTHA)(H2O)]·4,4'-bipy·2H2O}n (1), {[(UO2)3(TTHA)(H2O)3]}n (2), and {[(UO2)5(TTHA) (HTTHA)(H2O)3]·H3O}n (3), have been obtained by the hydrothermal reaction of uranyl acetate with a flexible hexapodal ligand (1,3,5-triazine-2,4,6-triamine hexaacetic acid, H6TTHA). These compounds exhibited three distinct 3D self-assembly architectures as a function of pH by single-crystal structural analysis, although the used ligand was the same in each reaction. Surprisingly, all of the coordination modes of the H6TTHA ligand in this work are first discovered. Furthermore, the photoluminescent results showed that these compounds displayed high-sensitivity luminescent sensing functions for nitrobenzene. Additionally, the surface photovoltage spectroscopy and electric-field-induced surface photovoltage spectroscopy showed that compounds 1-3 could behave as p-type semiconductors.


Subject(s)
Acetates/chemistry , Coordination Complexes/chemistry , Luminescence , Semiconductors , Triazines/chemistry , Uranium/chemistry , Hydrogen-Ion Concentration , Ligands , Molecular Conformation , Nitrobenzenes/analysis
11.
Dalton Trans ; 44(25): 11562-71, 2015 Jul 07.
Article in English | MEDLINE | ID: mdl-26038888

ABSTRACT

Four uranyl complexes [(UO2)(pht)H2O]·H2O (pht = phthalic acid) (1), (UO2)2(Hipa)4(H2O)2 (Hipa = isophthalic acid) (2), (UO2)(tpa)(DMF)2 (tpa = terephthalic acid) (3) and (UO2)(box)2 (box = benzoic acid) (4) were synthesized by the reaction of UO2(CH3COO)2·2H2O as the metal source and phthalic acid, isophthalic acid, terephthalic acid or benzoic acid as the ligand. They were characterized by elemental analyses, IR, UV-Vis, XRD, single crystal X-ray diffraction analysis and thermal gravimetric analysis. The structural analysis reveals that complex 1 exhibits a one-dimensional chain structure constructed by the building unit [(UO2)2(pht)4(H2O)2] and further extends the chain into a 2D supramolecular architecture by hydrogen bonding interactions. Complex 2 is a discrete [(UO2)2(Hipa)4(H2O)2] structure, and by the hydrogen bonding interaction, forms a 3D supramolecular structure. In complexes 3 and 4, adjacent uranyl polyhedra form a 1D chain through bridging terephthalic acid and benzoic acid, respectively. In order to extend their functional properties, their photoluminescence, surface photovoltage and dye adsorption properties have been studied.

12.
Soft Matter ; 11(26): 5301-12, 2015 Jul 14.
Article in English | MEDLINE | ID: mdl-26053236

ABSTRACT

In an effort to construct smart artificial glutathione peroxidase (GPx) featuring high catalytic activity in an efficient preparation process, an artificial microgel GPx (PPAM-ADA-Te) has been prepared using a supramolecular host-guest self-assembly technique. Herein, 6,6'-telluro-bis(6-deoxy-ß-cyclodextrin) (CD-Te-CD) was selected as a tellurium-containing host molecule, which also served as the crosslinker for the scaffold of the supramolecular microgel. And an adamantane-containing block copolymer (PPAM-ADA) was designed and synthesized as a guest building block copolymer. Subsequently, PPAM-ADA-Te was constructed through the self-assembly of CD-Te-CD and PPAM-ADA. The formation of this self-assembled construct was confirmed by dynamic light scattering, NMR, SEM and TEM. Notably, PPAM-ADA-Te not only exhibits a significant temperature responsive catalytic activity, but also features the characteristic saturation kinetics behaviour similar to that of a natural enzyme catalyst. We demonstrate in this paper that both the hydrophobic microenvironment and the crosslinker in this supramolecular microgel network played significant roles in enhancing and altering the temperature responsive catalytic behaviour. The successful construction of PPAM-ADA-Te not only provides a novel method for the preparation of microgel artificial GPx with high catalytic activity but also provides properties suitable for the future development of intelligent antioxidant drugs.


Subject(s)
Biomimetic Materials/chemistry , Glutathione Peroxidase/metabolism , Adamantane/chemistry , Catalysis , Drug Design , Gels , Kinetics , Models, Molecular , Molecular Conformation , Polymers/chemistry , Tellurium/chemistry , beta-Cyclodextrins/chemistry
13.
Chembiochem ; 16(4): 670-6, 2015 Mar 02.
Article in English | MEDLINE | ID: mdl-25683962

ABSTRACT

A supramolecular artificial glutathione peroxidase (PNIPAM-CD-g-Te) was prepared based on a supramolecular graft copolymer. PNIPAM-CD-g-Te was constructed by supramolecular host-guest self-assembly. Significantly, PNIPAM-CD-g-Te displayed noticeable temperature-dependent catalytic activity and typical saturation kinetics behavior. It was also proved that the change in the self-assembled structure of PNIPAM-CD-g-Te during the temperature-dependent process played a significant role in the temperature-dependent catalytic behavior. The construction of PNIPAM-CD-g-Te based on supramolecular graft copolymer endows artificial GPx with temperature-dependent catalytic ability, enriched catalytic centers, and homogeneously distributed catalytic centers. This work bodes well for the development of other biologically related host-guest supramolecular biomaterials.


Subject(s)
Acrylic Resins/chemistry , Biomimetic Materials/chemistry , Cyclodextrins/chemistry , Glutathione Peroxidase/chemistry , Tellurium/chemistry , Catalysis , Kinetics , Temperature
14.
Zhongguo Zhong Yao Za Zhi ; 40(22): 4491-6, 2015 Nov.
Article in Chinese | MEDLINE | ID: mdl-27097429

ABSTRACT

The purpose of this study was to evaluate the effect and safety of Jinlong capsule combined with chemotherapy or radio-therapy for non-small cell lung cancer (NSCLS) using Meta-analysis. PubMed, Embase, CNKI and Wanfang databases were all searched without language restriction, and searching time was from January 1990 to July 2015. All eligible published studies were included in this study for quality assessment and data extraction. All the data were analyzed using Revman 5.3. A total of ten studies including 736 subjects (370 in Jinlong capsule plus chemoradiotherapy and 366 in chemoradiotherapy only) were finally included in this Meta-analysis. The result of Meta analysis showed that compared with pure chemoradiotherapy group, Jinlong capsule combined with chemoradiotherapy for NSCLC could improve the patients' curative effect (OR = 1.77, 95% CI: 1.29-2.43, P < 0.05), clinical benefit rate (OR = 1.89, 95% CI: 1.22-2.91, P < 0.05), life quality improvement rate (OR = 2. 56, 95% CI: 1.61-4.05, P < 0.05), and decrease leucopenia incidence rate (OR = 0.35, 95% CI: 0. 22-0.56, P < 0.05) and gastrointestinal reaction rate (OR = 0.67, 95% CI: 0.40-1.11, P < 0.05). The pooled results showed that Jinlong capsule combined with chemoradiotherapy for NSCLC could improve the curative effect and life quality, and decrease the adverse reaction of patients.


Subject(s)
Carcinoma, Non-Small-Cell Lung/drug therapy , Carcinoma, Non-Small-Cell Lung/radiotherapy , Drugs, Chinese Herbal/administration & dosage , Lung Neoplasms/drug therapy , Lung Neoplasms/radiotherapy , Antineoplastic Combined Chemotherapy Protocols/administration & dosage , Capsules/administration & dosage , Chemoradiotherapy , Combined Modality Therapy , Humans
15.
Mol Med Rep ; 10(3): 1355-62, 2014 Sep.
Article in English | MEDLINE | ID: mdl-24939038

ABSTRACT

Glycyrrhiza uralensis (G. uralensis) is a common medicinal plant that has mainly been used to modulate the pharmaceutical activity of herbal medicines. Although G. uralensis has been shown to affect the expression and activity of the key metabolic enzyme cytochrome P450 (CYP450), the detailed mechanism of this process has yet to be elucidated. The present study aimed to elucidate the effects of bioactive components of G. uralensis on different isoforms of CYP450 and determine the ability of these components to modulate drug properties. In the present study, mRNA levels of CYP1A2, CYP2D6, CYP2E1, and CYP3A4 were investigated by quantitative polymerase chain reaction (qPCR) in HepG2 cells following treatment with the major bioactive compounds of G. uralensis. The activity of CYP450 enzymes was investigated in human liver microsomes using the cocktail probe drug method, and the metabolites of specific probes were detected by UPLC­MS/MS. The effects of G. uralensis on CYP450 were assessed using bioinformatics network analysis. Several compounds from G. uralensis had various effects on the expression and activity of multiple CYP450 isoforms. The majority of the compounds analysed the inhibited expression of CYP2D6 and CYP3A4. Several CYP isoforms were differentially modulated depending on the specific compound and dose tested. In conclusion, the present study suggested that G. uralensis influenced the expression and activity of CYP450 enzymes. Therefore, caution should be taken when G. uralensis is co­administered with drugs that are known to be metabolized by CYP450. This study contributed to the knowledge of the mechanisms by which this medicinal plant, commonly known as licorice, modulates drug efficacy.


Subject(s)
Cytochrome P-450 Enzyme System/metabolism , Glycyrrhiza uralensis/chemistry , Plant Preparations/pharmacology , Plants, Medicinal/chemistry , Cell Survival/drug effects , Cytochrome P-450 CYP1A2/genetics , Cytochrome P-450 CYP1A2/metabolism , Cytochrome P-450 CYP2D6/genetics , Cytochrome P-450 CYP2D6/metabolism , Cytochrome P-450 CYP2E1/genetics , Cytochrome P-450 CYP2E1/metabolism , Cytochrome P-450 CYP3A/genetics , Cytochrome P-450 CYP3A/metabolism , Cytochrome P-450 Enzyme System/genetics , Hep G2 Cells , Humans , Microsomes, Liver/drug effects , Microsomes, Liver/enzymology , RNA, Messenger/genetics , RNA, Messenger/metabolism , Tandem Mass Spectrometry
16.
Acta Crystallogr Sect E Struct Rep Online ; 68(Pt 6): o1726, 2012 Jun 01.
Article in English | MEDLINE | ID: mdl-22719514

ABSTRACT

The title Schiff base compound, C(14)H(12)N(4)O(3), displays an E conformation with respect to the C=N double bond [1.268 (3) Å]. The dihedral angle between the benzene rings is 3.2 (5)°, consistent with an essentially planar mol-ecule. In the crystal, N-H⋯O and N-H⋯N hydrogen bonds, as well as C-H⋯O inter-actions, link the mol-ecules into layers that stack along the c axis.

17.
Acta Crystallogr Sect E Struct Rep Online ; 68(Pt 5): o1546-7, 2012 May 01.
Article in English | MEDLINE | ID: mdl-22590408

ABSTRACT

The title compound, C(14)H(12)ClN(3)O(2), displays an E conformation with respect to the C=N double bond. The dihedral angle between the benzene rings is 41.3 (5)°. The mol-ecular structure is stabilized by an intra-molecular O-H⋯N hydrogen bond. In the crystal, N-H⋯O and weak N-H⋯Cl hydrogen bonds link the mol-ecules into a three-dimensional architecture. In addition, there are weak C-H⋯π stacking inter-actions.

18.
Int J Inj Contr Saf Promot ; 19(3): 267-71, 2012.
Article in English | MEDLINE | ID: mdl-22519302

ABSTRACT

The aim of this study was to investigate the knowledge-attitude-practice (KAP) and their related factors on injury prevention and safety promotion among children's parents in the city area, in order to provide scientific data for the development of Safe School in mainland China. A total of 3617 subjects were investigated in Jinan with the help of a self-administered questionnaire which included parental demographic characteristics and 40 questions related to KAP about injury prevention and safety promotion. Responses to each question included only one correct answer. A score of 1 was given if the participant answered correctly, otherwise the score was 0. Therefore, the total KAP score was 40 if all the 40 questions were answered correctly by one respondent. The total KAP scores were classified into two categories for which the cutoff value was the mean of the total KAP scores. The results showed that the KAP scores ranged from 13 to 39, with an average of 30.79 ± 3.54. Higher KAP scores were statistically associated with mothers (odds ratio [OR] = 1.79) and higher education level (OR = 1.34). It was concluded that parental KAP about injury prevention and safety promotion was unsatisfactory, and health education on KAP about injury prevention and safety promotion for parents, especially among fathers and parents with low education levels, should be strengthened further by Safe School programmes.


Subject(s)
Health Knowledge, Attitudes, Practice , Parents , Schools , Wounds and Injuries/prevention & control , Accident Prevention , Adult , Child , China , Cross-Sectional Studies , Female , Humans , Male , Middle Aged , Safety Management , Surveys and Questionnaires
19.
Guang Pu Xue Yu Guang Pu Fen Xi ; 30(9): 2443-6, 2010 Sep.
Article in Chinese | MEDLINE | ID: mdl-21105414

ABSTRACT

Six cobalt complexes, Co(Hz2O)6.H2btec(1); {[Co2(HCOO)6].CH3OH}n(2); {[Co(4,4'-bipy)2(H2O)4].suc.4H2O)}n(3); Co(NA)2(H2O)4(4); [Co(mal)(4,4'-bipy)H2O]n(5) and [Co(HCOO)4Co(H2O)4]n(6), were synthesized through hydrothermal method. UV-Vis absorption spectra and surface photovoltage spectra of the complexes were detected and the structures of the complexes were determined by single-crystal X-ray diffraction. There are positive responses in the range of 300-800 nm in the SPS. There are good corresponding relationships between response bands of SPS and absorption peaks of UV-Vis absorption spectra by the comparison. Comparing the SPS of six complexes, the valence, coordination mode and coordination micro-environment affect the position and the shape of the response bands.

20.
Zhongguo Zhong Yao Za Zhi ; 34(16): 2092-6, 2009 Aug.
Article in Chinese | MEDLINE | ID: mdl-19938554

ABSTRACT

OBJECTIVE: To study on pharmacologic actions on quail hyperlipidemia and atherosclerosis model. METHOD: To duplicate quail hyperlipidemia model by ectogenesis cholesterol and high fat forage, induce to atherosclerosis model, observe influence of sugarcane alkane alcohol to model animals' blood fat level, formation of atherosclerosis plaque, pathological changes of coronary vessels and vascular intimal. RESULT: TC, TG, LDL-C level in blood serum of quail hyperlipidemia markedly decreased after administered sugarcane alkane alcohol by dose of 30, 15, 7.5 mg x kg(-1), proliferation of aorta and brachiocephalic artery tunica intima foam cells was suppressed. CONCLUSION: Sugarcane alkane alcohol has satisfactory pharmacologic actions on hyperlipidemia and atherosclerosis animal model by regulating blood fat.


Subject(s)
Alkanes/therapeutic use , Atherosclerosis/drug therapy , Ethanol/therapeutic use , Hyperlipidemias/drug therapy , Quail , Saccharum/chemistry , Alkanes/chemistry , Animals , Cholesterol/blood , Disease Models, Animal , Ethanol/chemistry , Male , Plant Extracts/chemistry , Plant Extracts/therapeutic use , Random Allocation
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