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1.
Polybrominated diphenyl ethers (PBDEs) are known as effective flame retardants and have vast industrial application in products like plastics, building materials and textiles. They are found to be structurally similar to thyroid hormones that are responsible for regulating metabolism in the body. Structural similarity with the hormones poses a threat to human health because, once in the system, PBDEs have the potential to affect thyroid hormone transport and metabolism. This study was aimed at designing quantitative structure–activity relationship (QSAR) models for predicting toxic endpoints, namely cell viability and apoptosis, elicited by PBDEs in mammalian cells. Cell viability was evaluated quantitatively using a general cytotoxicity bioassay using Janus Green dye and apoptosis was evaluated using a caspase assay. This study has thus modelled the overall cytotoxic influence of PBDEs at an early and a late endpoint by the Genetic Function Approximation method. This research was a twofold process including running in vitro bioassays to collect data on the toxic endpoints and modeling the evaluated endpoints using QSARs. Cell viability and apoptosis responses for Hep G2 cells exposed to PBDEs were successfully modelled with an r2 of 0.97 and 0.94, respectively.  相似文献   

2.
The effect of extensin-like cotton proteins (ELP) on animal cell gene (KML cell culture) was studied. Cells perish (50%) at protein dose 100 g/mL (cytotoxic effect). DNA fragmentation is not observed. Cell death from ELP is hypothesized to occur via necrosis resulting from destruction of intracellular biochemical processes  相似文献   

3.
Nemorosone is a polycyclic polyisoprenylated benzophenone (PPBs) with strong cytotoxic activity. It is the major constituent of Clusia rosea floral resin and brown Cuban propolis. Other PPBs found in Cuban propolis are oxidized and cyclized derivatives of nemorosone. The instability of PPBs carrying an enolizable 1,3-diketone system has been suggested, and the elucidation of this aspect is very fundamental for the evaluation of their biologic activity. Electrospray ionization multistage tandem mass spectrometry (ESI-MS n ) was employed to shed light on the origin of these derivatives of nemorosone and to define the stability of this natural product. For this purpose, we initially performed MS n experiments on seven related PPBs to obtain useful information for structural characterization of this class of compounds and to identify the degradation products of nemorosone. The proposed fragmentation pathways, supported by exact mass measurements, allowed the nature of side chains on the bicyclo core and the type and position of their modifications to be established. In a second part, the degradation profile of nemorosone under different conditions was investigated to assess the possible effects of isolation procedures, climatic, and storage conditions on its stability. Our results reveal that nemorosone undergoes rapid degradation in n-hexane and chloroform solutions. The degradation products, identified by HPLC-ESI/MS n and NMR, are identical to derivatives of nemorosone previously isolated from propolis and plants. Thus, these PPBs are artefacts formed predominantly during the extraction and purification procedures.  相似文献   

4.
Herpes simplex type 2 (HSV-2) infection causes a significant life-long disease. Long-term side effects of antiviral drugs can lead to the emergence of drug resistance. Thus, propolis, a natural product derived from beehives, has been proposed to prevent or treat HSV-2 infections. Unfortunately, therapeutic applications of propolis are still limited due its poor solubility. To overcome this, a nanoparticle-based drug delivery system was employed. An ethanolic extract of propolis (EEP) was encapsulated in nanoparticles composed of poly(lactic-co-glycolic acid) and chitosan using a modified oil-in-water single emulsion by using the solvent evaporation method. The produced nanoparticles (EEP-NPs) had a spherical shape with a size of ~450 nm and presented satisfactory physicochemical properties, including positively charged surface (38.05 ± 7.65 mV), high entrapment efficiency (79.89 ± 13.92%), and sustained release profile. Moreover, EEP-NPs were less cytotoxic on Vero cells and exhibited anti-HSV-2 activity. EEP-NPs had a direct effect on the inactivation of viral particles, and also disrupted the virion entry and release from the host cells. A significant decrease in the expression levels of the HSV-2 replication-related genes (ICP4, ICP27, and gB) was also observed. Our study suggests that EEP-NPs provide a strong anti-HSV-2 activity and serve as a promising platform for the treatment of HSV-2 infections.  相似文献   

5.
The alkaline hydrolysis reaction rates of 1,n‐bis(4‐cyanopyridinium)alkane derivatives Cnbis(CP)2+ with n = 3, 6, and 8 were studied and compared to the reaction rate of the N‐methyl‐4‐cyanopyridinium (MCP+). C6bis(CP)2+ and C8bis(CP)2+ obeyed the first‐order kinetic law. However for C3bis(CP)2+ data fitted to a consecutive two‐step model reaction, the observed rate constants (kobs) of C8bis(CP)2+ and C6bis(CP)2+ are approximately 50% and 100%, respectively, higher than those for MCP+, an effect mainly assigned to the higher charge density of these two derivatives. For C3bis(CP)2+, the kobs of the second (slow) step is almost twofold the value observed for C6bis(CP)2+, whereas the first (fast) step is approximately six times higher. As for MCP, the hydrolysis of Cnbis(CP)2+ generates pyridone (Po) and carbamidopyridinium (A+) units. For C3bis(CP)2+, however at pHs above 11.5, one additional product is formed. From the existence of the new product and the kinetic evidence, a “sandwiched‐type” complex with the OH? inserted between the rings is proposed. This structural effect in the C3bis(CP)2+ due to the conformational effect justifies the (i) two kinetic steps, (ii) high rate constants, (iii) high Po/A+ ratios, (iv) observed temperature and salt effects, and (v) the formation of the new product.  相似文献   

6.
One new monoterpene glucoside and five dihydroflavonols were isolated for the first time from the aerial parts of Pulicaria jaubertii and identified as p-menthane-2-O-β-D-glucopyranoside [1], dihydroquercetin (taxifolin) [2], 7,3′-di-O-methyltaxifolin [3], 3′-O-methyltaxifolin [4], 7-O-methyltaxifolin (padmatin) [5] and 7-O-methyl-dihydrokampferol (7-O-methylaromadenderin) [6]. The structures of these compounds were unambiguously assigned on the basis of NMR spectroscopic data (1H, 13C, DEPT, HSQC, HMBC) and MS analysis. 2D-NMR methods required revision of assignments of H-6 and H-8 for dihydroflavonol compounds. Possible cytotoxic activity as well as blood pressure (BP) lowering activity were tested. The alcoholic extract showed cytotoxic activity against prostate carcinoma (PC-3), breast carcinoma (MCF-7) and hepatocellular carcinoma (HepG-2) human cell lines with IC50 19.1, 20.0 and 24.1 μg, respectively. The higher dose levels of the alcoholic extract significantly reduced normal BP of rats in a dose-dependent manner.  相似文献   

7.
To investigate the effect of the spacers of S-/O-bridged dipyridylamides on the structures of Co(II)/Zn(II) complexes, [Co(L1)(chda)]·1.5H2O (CP1), [Co(L2)(chda)] (CP2), [Zn(L1)(hip)]·DMA·2H2O (CP3), and [Zn(L2)(hip)]·2.8H2O (CP4) [L1 = N,N′-bis(pyridine-3-yl)thiophene-2,5-dicarboxamide, H2chda = trans-1,4-cyclohexanedicarboxylic acid, L2 = N,N′-bis(pyridine-3-yl)-4,4′-oxybis(benzoic) dicarboxamide, H2hip = 5-hydroxyisophthalic acid, DMA = N,N-dimethylacetamide], have been solvothermally synthesized. X-ray single-crystal diffraction shows that CP1 is a 2-D 3,5-connected network based on Co-L1 linear chains and (Co-chda)2 double chains. CP2 features a 1-D structure derived from 1-D wave-like (Co-chda)2 double chains decorated by terminal L2 ligands. CP3 and CP4 show wave-like (4,4) networks constructed by 1-D Zn-L1 zigzag and Zn-hip zigzag (for CP3)/linear (for CP4) chains. The effect of the spacers of S-/O-bridged dipyridylamides on the structures of the title complexes was discussed. Electrochemical behaviors of CP1CP2 and solid-state luminescent properties of CP3CP4 were studied. The luminescence investigations show that CP3 and CP4 are recycled fluorescent probes for environmentally relevant Fe3+ ions. The photocatalytic properties for the degradation of methylene blue (MB) under ultraviolet light irradiation of CP3CP4 and the recyclable materials after fluorescent sensing Fe3+ ions (named CP3@Fe3+ and CP4@Fe3+) have also been investigated.  相似文献   

8.
Activated protein C (APC) is a cytoprotective anticoagulant that can promote cutaneous healing. We examined the effect of APC on viability and differentiation of the osteoblastic line, MG63, in the presence and absence of bisphosphonates (BPs). Osteoblasts were cultured and treated for 24 or 48 h with Alendronate (Aln), Zoledronate (Zol) or Pamidronate (Pam) at concentrations ranging from 10−4 to 10−6 ℳ. Cell differentiation was measured using type 1 collagen production, Alizarin red staining and alkaline phosphatase activity, whereas cell viability was assessed using MTT and crystal violet assays. All three BPs induced MG63 cell death in a dose- and time-dependent manner. Pam- and Zol-related cell death was prevented by APC treatment; however, cell death induced by Aln was accelerated by APC. APC induced MG63 cell differentiation that was enhanced by Aln, but inhibited by Pam or Zol. Endothelial protein C receptor (EPCR) was expressed by MG63 cells and mediated the protective effect of APC on Zol-induced viability. In summary, we have demonstrated that (1) APC favorably regulates MG63 viability and differentiation toward bone growth, (2) APC differentially regulates the effects of specific BPs and (3) at least part of the effects of APC is mediated through EPCR. These findings highlight the potential importance of the PC pathway in bone physiology and provide strong evidence that APC may influence bone cells and has potential to be a therapeutic drug for bone regeneration, depending on concurrent BP treatment.  相似文献   

9.
Gingival fibroblasts have critical roles in oral wound healing. Photobiomodulation (PBM) has been shown to promote mucosal healing and is now recommended for managing oncotherapy-associated oral mucositis. This study examined the effects of the emission mode of a 940 nm diode laser on the viability and migration of human gingival fibroblasts. Cells were cultured in a routine growth media and treated with PBM (average power 0.1 W cm−2, average fluence 3 J cm−2, every 12 h for six sessions) in one continuous wave and two pulsing settings with 20% and 50% duty cycles. Cell viability was assessed using MTT, and digital imaging quantified cell migration. After 48 and 72 h, all treatment groups had significantly higher viability (n = 6, P < 0.05) compared with the control. The highest viability was seen in the pulsed (20% duty cycle) group at the 72-h time point. PBM improved fibroblast migration in all PBM-treated groups, but differences were not statistically significant (n = 2, P > 0.05). PBM treatments can promote cell viability in both continuous and pulsed modes. Further studies are needed to elucidate the optimal setting for PBM-evoked responses for its rationalized use in promoting specific phases of oral wound healing.  相似文献   

10.
Three lanthanide‐based two‐dimensional (2D) coordination polymers (CPs), [Ln(L)(H2O)2]n, {H3L=(HO)2P(O)CH2CO2H; Ln=Dy3+ (CP 1 ), Er3+ (CP 2 )} and [{Gd2(L)2(H2O)3}.H2O]n, (CP 3 ) were hydrothermally synthesized using phosphonoacetic acid as a linker. Structural features revealed that the dinuclear Ln3+ nodes were present in the 2D sheet of CP 1 and CP 2 while in the case of CP 3 , nodes were further connected to each other forming a chain‐type arrangement throughout the network. The magnetic studies show field‐induced slow magnetic relaxation property in CP 1 and CP 2 with Ueff values of 72 K (relaxation time, τ0=3.05×10?7 s) and 38.42 K (relaxation time, τ0=4.60×10?8 s) respectively. Ab‐initio calculations suggest that the g tensor of Kramers doublet of the lanthanide ion (Dy3+ and Er3+) is strongly axial in nature which reflects in the slow magnetic relaxation behavior of both CPs. CP 3 exhibits a significant magnetocaloric effect with ?ΔSm=49.29 J kg?1 K?1, one of the highest value among the reported 2D CPs. Moreover, impedance analysis of all the CPs show high proton conductivity with values of 1.13×10?6 S cm?1, 2.73×10?3 S cm?1 and 2, 6.27×10?6 S cm?1 for CPs 1 – 3 , respectively, at high temperature (>75 °C) and maximum 95 % relative humidity (RH).  相似文献   

11.
A simple and effective extraction method based on matrix solid-phase dispersion (MSPD) was developed to determine bifenthrin, buprofezin, tetradifon, and vinclozolin in propolis using gas chromatography–mass spectrometry in selected ion monitoring mode (GC–MS, SIM). Different method conditions were evaluated, for example type of solid phase (C18, alumina, silica, and Florisil), the amount of solid phase and eluent (n-hexane, dichloromethane, dichloromethane–n-hexane (8:2 and 1:1, v/v) and dichloromethane–ethyl acetate (9:1, 8:2 and 7:3, v/v)). The best results were obtained using 0.5 g propolis, 1.0 g silica as dispersant sorbent, 1.0 g Florisil as clean-up sorbent, and dichloromethane–ethyl acetate (9:1, v/v) as eluting solvent. The method was validated by analysis of propolis samples fortified at different concentration levels (0.25 to 1.0 mg kg−1). Average recoveries (four replicates) ranged from 67% to 175% with relative standard deviation between 5.6% and 12.1%. Detection and quantification limits ranged from 0.05 to 0.10 mg kg−1 and 0.15 to 0.25 mg kg−1 propolis, respectively.  相似文献   

12.
A new dinuclear coordination compound of palladium(II), [Pd2(terpy)2(μ‐tas‐N1,N4)]SO4?11H2O ( 1 ), was synthesized by tethering a doubly deprotonated 1,2,4‐triazole‐3‐sulfonate (tas) linker generated in situ via oxidation of 1,2,4‐triazole‐3‐thione (tat) under the synthetic conditions. X‐ray diffraction analysis reveals that tat molecules adopt the thione form in the solid state, and are combined in infinite chains by symmetrically related classical intermolecular hydrogen bonds N1─H1???S1, N3─H3???N2 to give rise to R22(7) pattern in one‐dimensional chains along the b‐axis propagating along the a‐axis. Further short contacts through lone pairs of N2???S1 on the rings between the adjacent chains along the a‐axis lead to a two‐dimensional network structure. Compound 1 was characterized using infrared, 1H NMR and UV–visible spectroscopies, electrospray ionization mass spectrometry and X‐ray crystallography. The crystal structure determination of 1 reveals that the Pd(II) ions are coordinated with four nitrogen atoms: three from terpy and one from tas acting as an end‐to‐end (μ‐1,4) bridging ligand. The Pd(II) ions in 1 adopt a distorted square planar geometry. The anti‐growth effect of 1 was tested on colorectal cancer (HCT‐15), non‐small‐cell lung cancer (A549), prostate cancer (PC‐3) and cervical cancer (HeLa) cell lines using sulforhodamine B viability assay. The cytotoxic effect was further confirmed using adenosine triphosphate viability assay. Compound 1 shows a promising cytotoxic activity in the diverse cancer cell models in vitro (p <0.0001).  相似文献   

13.
Three CdII coordination polymers (CPs) were synthesized with a tripodal ligand N,N‘,N‘ ‘‐tris(4‐pyridinylmethyl)‐1,3,5‐benzenetricarboxamide in combination with three different substituted isophthalic acids with general formulas {[Cd2( L )(NIP)2(H2O)2].4H2O}n, (CP‐ 1 ), {[Cd2( L )(AIP)2(H2O)2].4H2O}n, (CP‐ 2 ) and {[Cd( L )(BIP) (H2O)].4H2O}n, (CP‐ 3 ). The substituent groups on the co‐ligand had profound effect on the network topologies of the corresponding CPs as well as their properties. Out of the three, CP‐ 1 and 2 were found to form 3D networks whereas CP‐ 3 was a 1D linear chain with uncoordinated pyridyl sites. Due to its structural features CP‐ 3 was found to show interesting properties. The 1D CP containing uncoordinated pyridyl site exhibited an excellent ability for doping with CoII which in turn acts as an efficient water oxidation electrocatalyst with required overpotential of 380 mV for an anodic current density of 1 mA cm?2. The CP also exhibited luminescence‐based detection of nitroaromatics (LOD: 0.003 mm ) without any significant interference in presence of other organic compounds.  相似文献   

14.
tert ‐Butyl‐1′‐methoxycarbonyl‐1‐ferrocenecarbamate ( 1 ) was Boc‐deprotected to give free amine which underwent oxalyl chloride‐mediated dimerization. The structure of the so‐obtained oxalamide‐bridged ferrocene 2 was elucidated using infrared and NMR (1H, 13C, COSY, NOESY, HSQC, HMBC) spectroscopies, crystal structure analysis, and electrospray ionization and high‐resolution mass spectrometry. The preliminary conformational analysis in solution suggested the intramolecular engagement of oxalamide protons, while single‐crystal analysis revealed an intermolecular hydrogen‐bonding pattern. Also, the effect of oxalamide‐bridged ferrocene 2 on cell viability of three human cell lines (HEK293T, HeLa and HepG2) was tested. In vitro screening revealed proliferative as well as cytotoxic effects of the tested compound in the applied concentration range (1–350 μM) on HEK293T and HepG2 cells. Stimulatory effect on cell growth was the most pronounced for normal HEK293T cells, while the highest cytotoxic effect was observed towards HeLa tumour cells and it was dose‐dependent. The observed dual biological activity of 2 implies its potential application in drug development.  相似文献   

15.
In an attempt to achieve promising cytotoxic agents, a series of new (Z)‐3‐benzyl‐5‐((1‐phenyl‐3‐(3‐((1‐substituted phenyl‐1H‐1,2,3‐triazol‐4‐yl)methoxy)phenyl)‐1H‐pyrazol‐4‐yl)methylene)thiazolidine‐2,4‐diones 10 a‐n were designed, synthesized, and characterized by 1H NMR, 13C NMR, IR, and ESI‐MS techniques. These compounds synthesized from appropriate reaction procedures with better yields. All the novel synthesized compounds 10a‐n were evaluated for their cytotoxic activity against the MCF‐7 cell line (Human breast cancer cell line) at different concentrations of 0.625, 1.25, 2.5, 5, and 10 μM, respectively. The cytotoxic evaluation assay is presented in terms of IC50 values and percentage cell viability reduction compared against standard drug cisplatin. Among all novel synthesized compounds 10a‐n , some of the representative analogues particularly 10g and 10e exhibit remarkable cytotoxic activity with IC50 values 0.454 and 0.586 μM, comparable to that of the standard drug cisplatin, and some analogues 10d , 10f , 10k, and 10m also have shown significant activity.  相似文献   

16.
In this study, vic‐dioxime ligand, (1E,2E)‐2‐(hydroxyimino)‐N′‐[(1E)‐2‐oxo‐2‐phenylethylidene]ethanehydroximohydrazide (LH2), and its Cu (II) and Ni (II) transition metal complexes were synthesized and characterized using analytical and spectroscopic techniques. Furthermore, in vitro cytotoxic and apoptotic effects of this vic‐dioxime ligand and its Cu (II) and Ni (II) complexes on Caco‐2 heterogeneous human epithelial colorectal adenocarcinoma cells were evaluated. The effect of the vic‐dioxime ligand and its Ni (II) and Cu (II) complexes in combination with Campto on the cells was also investigated. The cytotoxicity test was carried using the MTT assay, and the apoptotic effect was tested by DNA diffusion assay. Campto was used as a standard anti‐cancer drug, Caco‐2 cancer cells treated with dimethylsulfoxide acted as solvent control, and human peripheral lymphocytes were used as control. The ligand and its complexes exhibit concentration‐dependent cytotoxic and apoptotic behavior. The ligand induces the weakest cytotoxic and apoptotic effects on both Caco‐2 cancer cells and lymphocytes. The Ni (II) complex of ligand induces high cytotoxic and apoptotic effects on both Caco‐2 cancer cells and lymphocytes. The Cu (II) complex of ligand has high cytotoxic and apoptotic effects on Caco‐2, but weak cytotoxic and apoptotic effects on lymphocytes. The cytotoxic and apoptotic effects of the ligand and its Ni (II) and Cu (II) complexes were found to be concentration dependent, i.e. the higher the concentration is the more cytotoxic it will be. The present findings suggest that Cu (II) complex has the potential to act as a promising anti‐cancer compound against Caco‐2 colon cancer cells.  相似文献   

17.
UV radiations are principal causes of skin cancer and aging. Suntan creams were developed to protect epidermis and derma layers against photodegradation and photooxidation. The addition of antioxidant plant extracts (i.e. essential oil) to sunscreens is habitually performed, to increase their UV protective effects and to contrast pro‐radical and cytotoxic compounds present in these solutions. According to these observations, in the present work, the alteration of chemical composition and bioactive properties of Lavandula angustifolia Miller essential oil, exposed to UV light, was investigated. UV induced a significant deterioration of lavender oil biochemical profile. Moreover, the antioxidant activity of this solution, in in vitro tests and directly on B16‐F10 melanoma cells, greatly decreased after UV treatment. Our results also showed that essential oil was shielded from UV stress by propolis addition. Even after UV treatment, bee glue highly protected lavender oil secondary metabolites from degradation and also preserved their antiradical properties, both in in vitro antioxidant assays and in cell oxidative damage evaluations. This research proposed propolis as highly efficient UV protective and antiradical additive for sunscreens, cosmetics and alimentary or pharmaceutical products containing plant extracts.  相似文献   

18.
Extraordinary electronic and photonic features render black phosphorus (BP) an important material for the development of novel electronics and optoelectronics. Despite recent progress in the preparation of thinly layered BP flakes, scalable synthesis of large‐size, pristine BP flakes remains a major challenge. An electrochemical delamination strategy is demonstrated that involves intercalation of diverse cations in non‐aqueous electrolytes, thereby peeling off bulk BP crystals into defect‐free flakes comprising only a few layers. The interplay between tetra‐n‐butylammonium cations and bisulfate anions promotes a high exfoliation yield up to 78 % and large BP flakes up to 20.6 μm. Bottom‐gate and bottom‐contact field‐effect transistors, comprising single BP flakes only a few layers thick, exhibit a high hole mobility of 252±18 cm2 V?1 s?1 and a remarkable on/off ratio of (1.2±0.15)×105 at 143 K under vacuum. This efficient and scalable delamination method holds great promise for development of BP‐based composites and optoelectronic devices.  相似文献   

19.
The tertiary chlorine (Clt) content of vinyl chloride/2‐chloropropene copolymers [P(VC‐co‐2CP)] was determined by NMR spectroscopy. Copolymers containing 6.8–47.0 Clt's per P(VC‐co‐2CP) chain were used to initiate the cationic grafting of α‐methylstyrene, norbornadiene, indene, and norbornene with Et2AlCl under various conditions. Grafting was demonstrated by selective solvent extraction, and the effect of the experimental conditions on the grafting efficiency was examined. Select rheological and thermal characteristics of P(VC‐co‐2CP) grafts, including the glass‐transition temperature, heat deflection temperature, and discoloration upon heating, were studied. P(VC‐co‐2CP) carrying 7–11 poly(α‐methylstyrene) or polynorbornadiene branches per chain raised the glass‐transition temperature to, or above, that of a blend control. P(VC‐co‐2CP)s fitted with polyindene or polynorbornene branches were less effective in raising the mechanical properties. © 2002 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 40: 3644–3651, 2002  相似文献   

20.
Pancreatic cancer is one of the most malignant cancers with high mortality. Therefore, it is of great urgency to develop new agents that could improve the prognosis of Pancreatic cancer patients. Chinese propolis (CP), a flavonoid-rich beehive product, has been reported to have an anticancer effect. In this study, we applied CP to the human Pancreatic cancer cell line Panc-1 to verify its impact on tumor development. CP induced apoptosis in Panc-1 cells from 12.5 µg/mL in a time- and dose-dependent manner with an IC50 value of approximately 50 µg/mL. Apoptosis rate induced by CP was examined by Annexing FITC/PI assay. We found that 48 h treatment with 50 µg/mL CP resulted in 34.25 ± 3.81% apoptotic cells, as compared to 9.13 ± 1.76% in the control group. We further discovered that the Panc-1 cells tended to be arrested at G2/M phase after CP treatment, which is considered to contribute to the anti-proliferation effect of CP. Furthermore, our results demonstrated that CP suppressed Panc-1 cell migration by regulating epithelial–mesenchymal transition (EMT). Interestingly, the Hippo pathway was activated in Panc-1 cells after CP treatment, serving as a mechanism for the anti-pancreatic cancer effect of CP. These findings provide a possibility of beehive products as an alternative treatment for pancreatic cancer.  相似文献   

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