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1.
The essential oil from different parts of Datura metel L. were extracted using hydrodistillation and GC–MS was used to analyse the essential oil. The main components of flowers were ketone (23.61%) and ethyl palmitate (15.84%). The main components of leaves were ketone (18.84%) and phytol (18.71%). Ketone (39.45%) and phytol (31.32%) were the major components of petioles. Palmitic acid (30.60%) and ethyl linoleate (21.56%) were the major components of seeds. The major ingredient of roots was palmitic acid (52.61%). The main ingredients of the stems were palmitic acid (38.38%) and ethyl linoleate (17.38%). All the different parts of essential oil were screened for cytotoxicity. The roots and stems showed the inhibitory effects against HepG-2 with IC50 levels of 613.88 and 341.12 mg/L. The leaves and roots showed the inhibitory effects against HeLa with IC50 levels of 267.76 and 348.35 mg/L. All the six parts have inhibitory effects against SGC-7901 cell lines.  相似文献   

2.
The fruit body of Lasiosphaera fenzlii was found to show cytotoxicity on cancer cells during a preliminary screening. Repeated column chromatography of the fungal methanol extract resulted in the isolation of six compounds identified as 5α,8α-epidioxy-ergosta-6,22-dien-3β-ol (1), 5α,8α-epidioxy-ergosta-6,9(11),22-trien-3β-ol (2), 5α-ergosta-7,22-dien-3β-ol (3), 5α-ergosta-7,22-dien-3-one (4), ergosta-7,22-dien-3β,5α,6β-triol (5) and 6-dihydroxy-2,3-dihydro-1H-isoindol-1-one (6). The two peroxide compounds, 1 and 2, showed cytotoxic activity and compound 1 was selectively cytotoxic to cancer cells. Furthermore, compound 1 synergised the cytotoxicity of paclitaxel on Hela cells by increasing intracellular accumulation of paclitaxel in cancer cells but not in normal cells.  相似文献   

3.
The exploitation of various plant materials for the biosynthesis of nanoparticles is considered a green technology because it does not involve any harmful chemicals. The aim of the experiment was chemical characterization and evaluation of cytotoxicity, antioxidant, antibacterial, antifungal, and cutaneous wound healing activities of gold nanoparticles using aqueous extract of Gundelia tournefortii L. leaves (AuNPs@GT). These nanoparticles were characterized by fourier transformed infrared spectroscopy (FT‐IR), field emission scanning electron microscopy (FE‐SEM), energy dispersive X‐ray spectroscopy (EDS), and UV–visible spectroscopy. DPPH free radical scavenging test was done to assess the antioxidant properties, which indicated similar antioxidant potentials for AuNPs@GT and butylated hydroxytoluene. Agar diffusion tests were applied to determine the antibacterial and antifungal characteristics. Minimum Inhibitory Concentration (MIC), Minimum Bactericidal Concentration (MBC), and Minimum Fungicidal Concentration (MFC) were specified by macro‐broth dilution assay. AuNPs@GT indicated higher antibacterial and antifungal effects than all standard antibiotics (p ≤ 0.01). Also, AuNPs@GT inhibited the growth of all bacteria and fungi and removed them at 2‐4 mg/mL concentrations (p ≤ 0.01). In vivo experiment, after creating the cutaneous wound, the rats were randomly divided into six groups: untreated control, treatment with Eucerin basal ointment, treatment with 3% tetracycline ointment, treatment with 0.2% HAuCl4 ointment, treatment with 0.2% G. tournefortii ointment, and treatment with 0.2% AuNPs@GT ointment. These groups were treated for 10 days. For histopathological and biochemical analysis of the healing trend, a 3 × 3 cm section was prepared from all dermal thicknesses at day 10. Use of AuNPs@GT ointment in the treatment groups substantially reduced (p ≤ 0.01) the wound area, total cells, neutrophil, and lymphocyte and remarkably raised (p ≤ 0.01) the wound contracture, hydroxyl proline, hexosamine, hexuronic acid, fibrocyte, fibroblast, and fibrocytes/fibroblast rate compared to other groups. The synthesized AuNPs@GT had great cell viability dose‐dependently (Investigating the effect of the plant on HUVEC cell line) and revealed this method was nontoxic. The results showed that the leave aqueous extract of G. tournefortii is very good bioreductant in the synthesis of gold nanoparticles for treatment of bacterial, fungal, and skin diseases.  相似文献   

4.
Dynamic changes in reactive oxygen species (ROS) of Taxus cuspidata cells immobilized on polyurethane foam were investigated and the relation between ROS content and taxol production was discussed. Immobilization shortened the lag period of cell growth and moderately increased H2O2 and O2 −• contents inside the microenvironment within the first 15 d. After 20 d, excessive production of H2O2 and O2 −• was observed accompanied by marked increases in membrane lipid peroxidation and cell membrane permeability. The taxol content of immobilized cells was fourfold that of suspended cells at d 35. The addition of exogenous H2O2 barely affected malondialdehyde content and cell membrane permeability but led to an obvious accumulation of taxol. It is inferred that the intracellular and extracellular H2O2 inside the microenvironment might be one factor promoting taxol biosynthesis under the immobilization stress.  相似文献   

5.
Cedronella canariensis is a lemon-scented species of the family Lamiaceae endemic to the Canary Islands where it is used in the traditional medicine to prepare infusions or inhalations for anti-catarrhal, tonic, diuretic, hypoglycaemiant, hypotensive, anti-inflammatory and decongestant of the respiratory tract. In this work we investigated for the first time the antioxidant activity of the essential oil and its inhibitory effects on tumour cells (A375, MDA-MB-231, HCT 116) proliferation by DPPH, ABTS, FRAP and MTT assays, respectively. The oil, analysed by GC-ionisation flame detector and GC–MS, was characterised by pinocarvone (58.0%) and β-pinene (10.8%) as the major constituents, being typical of the chemotype ‘canariensis’. Noteworthy was the cytotoxic activity of the oil against the tumour cells examined, with IC50 values of 4.3, 7.3 and 11.4 μg/mL on A375, MDA-MB-231 and HCT 116 tumour cells, respectively, as well as the scavenging activity against the ABTS radical (IC50 of 10.5 μg/mL).  相似文献   

6.
Five 2‐aroyl‐5‐bromobenzo[b]furan‐3‐ol compounds (two of which are new) and four new 2‐aroyl‐5‐iodobenzo[b]furan‐3‐ol compounds were synthesized starting from salicylic acid. The compounds were characterized by mass spectrometry and 1H NMR and 13C NMR spectroscopy. Single‐crystal X‐ray diffraction studies of four compounds, namely, (5‐bromo‐3‐hydroxybenzofuran‐2‐yl)(4‐fluorophenyl)methanone, C15H8BrFO3, (5‐bromo‐3‐hydroxybenzofuran‐2‐yl)(4‐chlorophenyl)methanone, C15H8BrClO3, (5‐bromo‐3‐hydroxybenzofuran‐2‐yl)(4‐bromophenyl)methanone, C15H8Br2O3, and (4‐bromophenyl)(3‐hydroxy‐5‐iodobenzofuran‐2‐yl)methanone, C15H8BrIO3, were also carried out. The compounds were tested for their in vitro cytotoxicity on the four human cancer cell lines KB, Hep‐G2, Lu‐1 and MCF7. Six compounds show good inhibiting abilities on Hep‐G2 cells, with IC50 values of 1.39–8.03 µM.  相似文献   

7.
Binuclear diphenyltin(IV) dithiocabamate macrocyclic complexes [(Ph2SnIV)2‐μ2‐bis{(κ2S,S‐S2CN(R)CH2CONHC6H4)2O}] (R = iPr ( 1 ), sBu ( 2 ), nBu ( 3 ), Cy ( 4 ), 2‐furfuryl ( 5 ) or benzyl ( 6 )) were synthesized through a self‐assembly process involving novel diamino precursors 4,4′‐bis(2‐(alkylamino)acetamido)diphenyl ethers ( L1 , L2 , L3 , L4 , L5 , L6 ), CS2 and Ph2SnCl2. These were characterized using microanalysis and relevant spectroscopic methods. The geometry of all compounds was optimized using the density functional theory method. In vitro cytotoxic activity was evaluated against HEP 3B (hepatoma) and IMR 32 (neuroblastoma) using the MTT assay. Notably, complexes 1 , 2 , 3 , 4 , 5 , 6 were found to be extremely active against both cell lines and cytotoxicity data confirmed their 16‐fold better potency compared to cisplatin, a well‐known antineoplastic drug. Flow cytometric analysis of annexin V–propidium iodide‐stained cells demonstrated the ability of L5 , 4 and 6 to induce apoptosis in HEP 3B and IMR 32 cells, required for major therapeutic implication in cancer therapy. The extraordinary potency of binuclear complex 4 can be correlated with higher LUMO energy together with the greatest value of residual charge on the Sn(IV) centre among the compounds under investigation. Copyright © 2015 John Wiley & Sons, Ltd.  相似文献   

8.
以天然不饱和脂肪酸共轭亚油酸(CLA)为绿色单体, 通过简单的分子自组装和可控自交联反应制备聚共轭亚油酸(PCLA)聚集体. 透射电子显微镜(TEM)结果显示, PCLA聚集体的形貌呈现独特网状结构, 其联结单元为来自于CLA胶束的膨大颗粒. 采用氯金酸在极性聚合物表面原位还原, 2 d后在网状PCLA基底上制备得到以CLA胶束为核(20 nm)的网状纳米金结构, 而且网状PCLA的原位还原作用与模板作用相结合是获得PCLA基网状纳米金的充分必要条件. 与普通球形胶态金纳米颗粒[(5±1) nm]相比, PCLA基网状纳米金对苯硫酚具有更好的表面增强拉曼散射(SERS)效应, 对对硝基苯酚具有更好的催化还原效果.  相似文献   

9.
A novel activated carbon spheres (ACS)@SnO2@NiO hierarchical hybrid architecture was first synthesized and applied for enhancing the flame retardancy of epoxy (EP) resin via a cooperative effect. Herein, using activated carbon microspheres as the template, SnO2 and NiO nanospheres were successively anchored to it by a sedimentation‐calcination strategy. The well‐designed ACS@SnO2@NiO significantly enhanced the flame retardancy for consistency of EP composites, as demonstrated by thermogravimetric and cone calorimeter experiments. For instance, the incorporation of 2 wt% ACS@SnO2@NiO decreased by 15.5% maximum in the total smoke production, accompanying the higher graphitized char layer. In addition, the synergetic mechanism of flame retardancy between ACS@SnO2@NiO and aluminum hypophosphite (AHP) was investigated. The obtained sample satisfied the UL‐94 V‐0 rating with a 5.0 wt% addition of AHP and ACS@SnO2@NiO (the ratio of the mass fraction of AHP to ACS@SnO2@NiO is 4.5:0.5). Notably, the incorporation of AHP and ACS@SnO2@NiO resulted in a significant decrease in the fire hazard properties of EP resin; for instance, 4.5AHP‐0.5ACS@SnO2@NiO/EP resulted in a maximum decrease of 32.4% in the total smoke production as compared with that of pure EP resin. It should be noted that the improved flame‐retardant performance for the EP composites is primarily attributed to the synergistic effect of ACS@SnO2@NiO and AHP in promoting the formation of residual char in the condensed phase.  相似文献   

10.
Conjugated linoleic acid (CLA) was covalently bonded onto the surface of a polysulfone (PSF) membrane via esterification. The surface was characterized with contact angle measurement and FT‐IR spectrometery. The capability of bonded CLA on the suppression of oxidative stress was evaluated. The level of reactive oxygen species (ROS) was measured by the chemiluminescence (CL) method to evaluate the oxidative stress. Furthermore, the removal of bacterial endotoxin (lipopolysaccharide, LPS) by CLA‐bonding PSF was measured with enzyme‐linked immunosorbent assay (ELISA). The reduction in the platelet adhesion on the PSF surface was evaluated using a SF‐3000 automated hematology analyzer. The result indicates that CLA‐bonding PSF can reduce the adhesion of platelets by 73%. The concentration of LPS can be reduced by CLA‐bonding PSF 1.6 times more than unmodified PSF membrane. In addition, the level of ROS against CLA‐bonding PSF membrane was 23% of that against unmodified PSF membrane. Therefore CLA‐bonding PSF membrane could offer protection for patients against oxidative stress and could also inhibit LPS for clinical applications. Copyright © 2007 John Wiley & Sons, Ltd.  相似文献   

11.
Square planar metallic and homonuclear bimetallic complexes of Pd(II) with 2‐thiouracil (HTU) and organophosphines have been synthesized and characterized by FT‐IR and multinuclear 1H, 13C, 31P NMR spectroscopy. The thiouracil ligand TU acts as bidentate, is bound through the thioxo moiety and the endo amino group and forms a bridge between a PdCl(R3P) and a PdCl(R3P)2 moiety [R3P = Ph3P (o‐tolyl)3P, ClPh2P] in the homonuclear bimetallic complexes. The square planar geometry around Pd(II) has been confirmed for these complexes by a single‐crystal X‐ray diffraction study of compound 1 , [Pd2(TU)(PPh3)3Cl2]. These compounds were also screened against human tumor cell lines and showed promising in vitro cytotoxicity. Copyright © 2007 John Wiley & Sons, Ltd.  相似文献   

12.
The determination of the absolute configuration of chiral molecules is an important aspect of molecular stereochemistry. Vibrational circular dichroism (VCD) is the extension of electronic CD into the infrared region where fundamental vibrational transitions occur. VCD has a number of advantages over all previous methods of absolute configuration assignment. The absolute configuration and predominant solution-state conformation in CDCl(3) of the chiral lactone, 5-formyl-cis,cis-1,3,5-trimethyl-3-hydroxymethylcyclohexane-1-carboxylic acid lactone, 1, obtained by the comparison of measured and calculated VCD spectra, are reported. It is found that (-)-1 corresponds to the absolute configuration (1S,3S,5R)-1.  相似文献   

13.
Synthesis, characterization, and in vitro toxicity evaluation of upconversion luminescence NaLuF4:Yb3+/Tm3+ nanoparticles (UCLNPs) are reported in the current study. Initially, the synthesized lanthanide trifluoroacetate (Ln(OOCCF3)3) precursor was used to fabricate NaLuF4 nanoparticles doped with Yb3+ and Tm3+ metal ions. The nanoparticles were coated with calcium carbonate (CaCO3) after removing the hydrophobic species on them to enhance their biocompatibility. The in vitro methylthiazolyldiphenyl-tetrazoliumbromide (MTT) test was used to evaluate the toxicity of synthesized NaLuF4:Yb3+/Tm3+ nanoparticles (NLF-5) on L929 mouse fibroblast cell lines. The transmission electron microscopy image showed that the particle size of NaLuF4:Yb3+/Tm3+ was 32 nm. The synthesized NLF-5 nanoparticles have both α-cubic and β-hexagonal crystalline structures that provided a superb near-infrared-to-near-infrared upconversion luminescence signal when excited at 980 nm. MTT test results show that the death of L929 fibroblast cells was observed only at concentrations above 250 μg/mL of NaLuF4:Yb3+/Tm3+ nanoparticles. In addition, with an increase in patrol time of 24, 48, and 72 hr, cell toxicity increased significantly, while the coated nanoparticles did not have any toxic effects. The synthesized nanoparticles could be used as a suitable material for medical applications due to their small particle size, high photoluminescence emission intensity, and low toxicity.  相似文献   

14.
The syntheses of nine new 5‐iodosalicylic acid‐based 1,3,4‐oxadiazoline derivatives starting from methyl salicylate are described. These compounds are 2‐[4‐acetyl‐5‐methyl‐5‐(3‐nitrophenyl)‐4,5‐dihydro‐1,3,4‐oxadiazol‐2‐yl]‐4‐iodophenyl acetate ( 6a ), 2‐[4‐acetyl‐5‐methyl‐5‐(4‐nitrophenyl)‐4,5‐dihydro‐1,3,4‐oxadiazol‐2‐yl]‐4‐iodophenyl acetate ( 6b ), 2‐(4‐acetyl‐5‐methyl‐5‐phenyl‐4,5‐dihydro‐1,3,4‐oxadiazol‐2‐yl)‐4‐iodophenyl acetate, C19H17IN2O4 ( 6c ), 2‐[4‐acetyl‐5‐(4‐fluorophenyl)‐5‐methyl‐4,5‐dihydro‐1,3,4‐oxadiazol‐2‐yl]‐4‐iodophenyl acetate, C19H16FIN2O4 ( 6d ), 2‐[4‐acetyl‐5‐(4‐chlorophenyl)‐5‐methyl‐4,5‐dihydro‐1,3,4‐oxadiazol‐2‐yl]‐4‐iodophenyl acetate, C19H16ClIN2O4 ( 6e ), 2‐[4‐acetyl‐5‐(3‐bromophenyl)‐5‐methyl‐4,5‐dihydro‐1,3,4‐oxadiazol‐2‐yl]‐4‐iodophenyl acetate ( 6f ), 2‐[4‐acetyl‐5‐(4‐bromophenyl)‐5‐methyl‐4,5‐dihydro‐1,3,4‐oxadiazol‐2‐yl]‐4‐iodophenyl acetate ( 6g ), 2‐[4‐acetyl‐5‐methyl‐5‐(4‐methylphenyl)‐4,5‐dihydro‐1,3,4‐oxadiazol‐2‐yl]‐4‐iodophenyl acetate ( 6h ) and 2‐[5‐(4‐acetamidophenyl)‐4‐acetyl‐5‐methyl‐4,5‐dihydro‐1,3,4‐oxadiazol‐2‐yl]‐4‐iodophenyl acetate ( 6i ). The compounds were characterized by mass, 1H NMR and 13C NMR spectroscopies. Single‐crystal X‐ray diffraction studies were also carried out for 6c , 6d and 6e . Compounds 6c and 6d are isomorphous, with the 1,3,4‐oxadiazoline ring having an envelope conformation, where the disubstituted C atom is the flap. The packing is determined by C—H…O, C—H…π and I…π interactions. For 6e , the 1,3,4‐oxadiazoline ring is almost planar. In the packing, Cl…π interactions are observed, while the I atom is not involved in short interactions. Compounds 6d , 6e , 6f and 6h show good inhibiting abilities on the human cancer cell lines KB and Hep‐G2, with IC50 values of 0.9–4.5 µM.  相似文献   

15.
The physicochemical properties, thereby the biological efficacy, of metal complexes are affected based on their structure and geometry that vary in the presence of coordinating and non‐coordinating solvents. To investigate this, in the present work, we synthesized three hitherto unreported β‐diketone‐based oxovanadium(IV) complexes, namely [VO(tfdmh)2] (tfdmh =1,1,1‐trifluro‐5,5‐dimethyl‐2,4‐hexanedione), [VO(dmh)2] (dmh = 2,2‐dimethyl‐3,5‐hexanedione) and [VO(dbm)2] (dbm = 1,3‐diphenylpropane‐1,3‐dione), and characterized them using electron paramagnetic resonance, UV–visible, Fourier transform infrared and electrospray ionization mass spectroscopies and single‐crystal X‐ray diffraction. The structural changes in the presence of dichloromethane, dimethylsulfoxide and dimethylformamide were analysed using spectroscopic techniques. Further, in vitro glucose uptake efficacy and cytotoxicity were assessed using C2C12 (rat skeletal muscle) and HeLa (human cervical cancer) cell lines, respectively.  相似文献   

16.
This study investigates cytotoxic and genotoxic activities of (+)-Usnic acid and (-)-usnic acid isolated from the lichen Ramalina farinacea and the lichen Cladonia foliacea, respectively. To determine the activities of these acids, we used the MTT assay on V79 (Chinese hamster lung fibroblast like) and A549 (human lung carcinoma epithelial like) cell lines and cytokinesis-blocked micronucleus (CBMN) assay in human lymphocytes in vitro. Our results suggest that both enantiomers of usnic acid are non-genotoxic shown by the absence of micronucleus induction in human lymphocytes and have significant cytotoxic and apoptotic effects to induce cell killing in cultured human lymphocytes, V79 and A549 cell lines. Even low doses of (+)-usnic acid showed high cytotoxic activity against cancerous cells. The MTT results and cell proliferation index (CPI) values based on the CBMN test results are found in good agreement.  相似文献   

17.
The reaction of α,α′‐dimercapto‐o‐xylene (H2dmox) with different precursors such as SnMe2Cl2, [Ti(η5‐C5H5)2Cl2] and [Ti(η5‐C5H4Me)2Cl2] (1:1) in the presence of two equivalents of NEt3 yielded the complexes [SnMe2(dmox)] (1), [Ti(η5‐C5H5)2(dmox)] (2) and [Ti(η5‐C5H4Me)2(dmox)] (3), respectively. 1–3 have been characterized by spectroscopic methods; in addition, complex 3 has been determined by X‐ray diffraction studies. Furthermore, structural studies based on density functional theory calculations of 1 and 2 have been carried out. The cytotoxic activity of 1–3 was tested against the tumour cell lines human adenocarcinoma HeLa, human myelogenous leukaemia K562 and human malignant melanoma Fem‐x. The results of this study show a higher cytotoxicity of the tin(IV) complex (1) in comparison to their titanium(IV) counterparts (2 and 3) as well as an improvement in the cytotoxic activity of compounds 2 and 3 compared to their titanocene(IV) dichloride analogues [Ti(η5‐C5H5)2Cl2] and [Ti(η5‐C5H4Me)2Cl2]. In view of the relatively high cytotoxicity of compound 1, a detailed study on the effects of the in vitro treatment of cancer cell lines using this compound was carried out. Thus cell cycle experiments on all the studied cell lines treated with 1 show that this complex seems to cause disturbances in the G1 phase of HeLa, and in the G1 and G2/M phases of Fem‐x cell line, while almost no disturbances were observed in the cycle of K562 cells treated with 1. Finally, DNA laddering method showed that treatment of the HeLa and Fem‐x cell lines with IC90 doses of 1 resulted in the induction of apoptosis. Copyright © 2012 John Wiley & Sons, Ltd.  相似文献   

18.
《印度化学会志》2022,99(11):100719
The essential intention of the existing article is to illustrate the effect of wall properties on flow and thermal behavior, through a sinusoidal inclined wavy pipe. To succeed this phenomena we assume a sinusoidal pipe consist of wavy surface, whose walls traveling down to its borders and located at an inclined position, moreover titanium dioxide (TiO2), ferrosoferric oxide (Fe3O4) and nichrome (80% Ni and 20% Cr) are considered as nano-particles and unused engine oil is assumed as a base fluid. The arising mathematical equations for thermal and flow ratio with wall slip impact are solved by mathematica. Also, evaluate graphically the thermal and flow behavior of nanofluids for multi values of solid volume fractions (η), rigidity parameter (M1), stiffness parameter (M2), viscous damping parameter (M3), Grashof number (Gr), slip parameter (β) and heat generation parameter (H) also discuss the streamlines for different values of solid volume fraction.  相似文献   

19.
3-Carboxy-4-methyl-5-propyl-2-furanpropionic acid (furanpropionic acid), a metabolite commonly found in human blood and urine, is one of the major acidic components which accumulates in the blood of patients with renal failure. Polyunsaturated fatty acids such as eicosapentaenoic acid (C20:5 ω?3) and long chain furan fatty acids, both present in commonly available fish oil capsules, are regarded as possible precursors of furanpropionic acid. Because of its strong binding to albumin and its various interactions with other endogenous and exogenous components, it is of great importance to determine the concentration of furanpropionic acid in blood and urine regularly. Solid phase extraction has been used to concentrate furanpropionic acid from both blood and urine samples. After esterification with ethereal diazomethane, gas chromatographic separation was performed on a HP-1 column (dimethylpolysiloxane). Quantitation with an internal standard was performed by mass selective detection in SIM-mode, qualifier ions being used for identification and accuracy. Fish oil supplementation of the diet of 24 patients for four weeks led to 3-fold and 5 to 6-fold increases in the levels of furanpropionic acid in serum and urine, respectively.  相似文献   

20.
Four novel triarylbismuth(V) di(N‐salicylidene)amino carboxylates were synthesized. Their structures were confirmed by IR, 1H NMR, 13C NMR and elemental analysis. The crystal structure of (2‐HOC6H4CH?NCH2CO2)2BiPh3 was determined by X‐ray diffraction. The in vitro cytotoxicity of all compounds against three human cancer cells (HL‐60, BGC‐823 and MDA‐MB‐435) at 10 µM are reported. Copyright © 2005 John Wiley & Sons, Ltd.  相似文献   

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