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1.
2.
A new series of asymmetric salicyl-, furanyl-, thienyl- and pyrrolyl-derived ONNO, NNNO, ONNS & NNNS donor antibacterial and antifungal Schiff-bases and their copper(II) and zinc(II) metal complexes have been synthesized and characterized. IR spectra indicated the ligands to act as quartdentate towards divalent metal ions via two azomethine-N, deprotonated-O of salicyl, furanyl-O, thienyl-S and/or pyrrolyl-N. The magnetic moments and electronic spectral data suggest octahedral geometry for Cu(II) and Zn(II) complexes. NMR spectral data of the ligands and their diamagnetic zinc(II) complexes well-define their proposed structures/geometries. Elemental analyses data of the ligands and metal complexes agree with their proposed structures/geometries. The synthesized ligands, along with their metal complexes were screened for their antibacterial activity against B. cereus, C. diphtheriae, E. coli, K. pneumoniae, P. mirabilis, P. aeruginosa, S. typhi, S. dysenteriae and S. aureus strains and for in-vitro antifungal activity against T. schoenleinii, C. glabrata, P. boydii, C. albicans, A. niger, M. canis and T. mentagrophytes. The results of these studies show the metal complexes to be more antibacterial/antifungal against one or more species as compared to the uncomplexed ligands. The brine shrimp bioassay was also carried out to study their in-vitro cytotoxic properties. Eight compounds, L4, (1), (7), (8), (11), (17), (19) and (23) displayed potent cytotoxic activity with LD50 = 1.445 × 10? 3, 1.021 × 10? 3, 7.478 × 10? 4, 8.566 × 10? 4, 1.028 × 10? 3, 9.943 × 10? 4, 8.730 × 10? 4 and 1.124 × 10? 3 M respectively, against Artemia salina.  相似文献   

3.
The Encyclia adenocarpos complex is restricted to the Pacific slopes of Megamexico, from Sonora, Mexico, to northern Nicaragua. It is characterized by pyriform to suborbicular pseudobulbs, (1-)2-3(4) thickly coriaceous, narrow leaves (> 15 times longer than wide), thin, verruculose inflorescences, and a verruculose ovary. The column is broad and wingless, fused to the labellum at its proximal 1/4. The flowers of the Encyclia adenocarpos complex feature what is here dubbed the Tupperware© labellum-column morphology, where the columnar ventral face is concave and fits tightly around the rim or upper margins of the callus, similar to the seal of this plasticware. All species grow on dry forests at low elevations from sea level to ca. 1500 m; most populations occurring below 500 m. The complex consists of six species, two of which are newly described herein: E. acapulcensis sp. nov., from southern Guerrero and E. enriquearcilae sp. nov., from western Oaxaca and neighboring Guerrero, Mexico. Encyclia rodolfoi is the correct name for populations of the Tehuantepec Isthmus whereas E. × nizandensis is here regarded as a natural hybrid between E. rodolfoi and E. parviflora; the evidence is presented and discussed. Encyclia schaeferi is treated as a morph of E. papillosa and included in its synonymy. A neotype is selected for Epidendrum adenocarpos and Epidendrum crispatum is rejected as a synonym thereof. All species are illustrated and discussed, and a key to the species is presented. Furthermore, the conservation status of each species is analyzed under the IUCN methodology. Other aspects of the biology of this complex are also discussed.  相似文献   

4.
The DNA-binding and photonuclease activity of newly synthesized tetra-azamacrocyclic ligand L (C32H32N8O4) and its complexes of type [MLCl2] and [ML]Cl2 (where M = Co(II), Fe(II) and Cu(II); L = N,N′-[3-(4-{5-[(2-amino-ethylamino)-methyl]-isoxazol-3yl}-phenyl)-isoxazol-5-yl methyl-ethane-1,2-diamine] are specified. An octahedral geometry has been proposed for Fe(II) and Co(II) complexes, while the Cu(II) complex has a square planar environment. The absorption spectral results indicate that the complexes bind with the base pairs of DNA, with an intrinsic binding constant Kb of Fe(II), Co(II), and Cu(II) complexes found to be 3.2 × 104 M?1, 5.3 × 104 M?1, and 4.2 × 104 M?1, respectively, in 5 mM Tris-HCl/50 mM NaCl buffer at pH 7.2. The large enhancement in the relative viscosity of DNA on binding to the complexes supports the proposed DNA binding modes. The viscosity and thermal denaturation studies sustain the effective intercalation with DNA. The DNA photocleavage studies demonstrated that compounds exhibit significant photonuclease activity by a concentration dependent on singlet oxygen mediated mechanism.  相似文献   

5.
Abstract

Temporal changes of algicidal and growth-inhibiting bacteria on the fish-killing raphidophyte flagellate, Chattonella antiqua, at an eelgrass (Zostera marina) bed in southern Ariake Sea, Japan in 2011 was investigated. The maximum value (5.1?×?107 CFU g?1 wet leaf) of algicidal bacteria (AB) was detected from a biofilm formed on Z. marina on August 1 when AB in the adjacent seawater had also peaked (1.2?×?104 CFU mL?1). Two causative bacteria isolated from the biofilm and seawater on August 1 were both identified to be of the genus Alteromonas (γ-proteobacteria). AB and growth-inhibiting bacteria (GIB) were present from the beginning of sampling (May 20) to August 26, fluctuating between 8.6?×?102 and 1.2?×?104, 1.2?×?103 and 9.3?×?103 CFU mL?1, respectively. The highest phytoplankton density observed was 6423 cells mL?1 on September 29 and was comprised of centric diatoms such as Chaetoceros, Skeletonema, and Thalassiosira and coincided with the absence of AB and GIB where the decline of Z. marina was also observed. These findings provide a new ecological insight on AB and GIB associated with Z. marina beds, indicating eelgrass beds have the important role as the nursery of those bacteria that can be utilized as mitigation measures of harmful algal blooms (HABs) in the future.  相似文献   

6.
Abstract

The chemistry of Co(II) complexes showing efficient light induced DNA cleavage activity, binding propensity to calf thymus DNA and antibacterial PDT is summarized in this article. Complexes of formulation [Co(mqt)(B)2]ClO4 1–3 where mqt is 4-methylquinoline-2-thiol and B is N,N-donor heterocyclic base, viz. 1,10-phenanthroline (phen 1), dipyrido[3,2-d:2′,3′-f]quinoxaline (dpq 2) and dipyrido[3,2-a:2′,3′-c]phenazine (dppz 3) have been prepared and characterized. The DNA-binding behaviors of these three complexes were explored by absorption spectra, viscosity measurements and thermal denaturation studies. The DNA binding constants for complexes 1, 2 and 3 were determined to be 1.6?×?103?M?1, 1.1?×?104?M?1 and 6.4?×?104?M?1 respectively. The experimental results suggest that these complexes interact with DNA through groove binding mode. The complexes show significant photocleavage of supercoiled (SC) DNA proceeds via a type-II process forming singlet oxygen as the reactive species. Antimicrobial photodynamic therapy was studied using photodynamic antimicrobial chemotherapy (PACT) assay against E. coli and all complexes exhibited significant reduction in bacterial growth on photoirradiation.  相似文献   

7.
ABSTRACT

Background: Hurricanes have a strong influence on the ecological dynamics and structure of tropical forests. Orchid populations are especially vulnerable to these perturbations due to their canopy exposure and lack of underground storage organs and seed banks.

Aims: We evaluated the effects of Hurricane Ivan on the population of the endemic epiphytic orchid Encyclia bocourtii to propose a management strategy.

Methods: Using a pre- and post-hurricane dataset (2003–2013), we assessed the population asymptotic and transient dynamics. We also identified the individual size-stages that maximise population inertia and E. bocourtii’s spatial arrangement relative to phorophytes and other epiphytes.

Results: Hurricane Ivan severely affected the survival and growth of individuals of E. bocourtii, and caused an immediate decline of the population growth rate from λ = 1.05 to λ = 0.32, which was buffered by a population reactivity of ρ1 = 1.42. Our stochastic model predicted an annual population decrease of 14%. We found an aggregated spatial pattern between E. bocourtii and its host trees, and a random pattern relative to other epiphytes.

Conclusion: Our findings suggest that E. bocourtii is not safe from local extinction. We propose the propagation and reintroduction of reproductive specimens, the relocation of surviving individuals, and the establishment of new plantations of phorophytes.  相似文献   

8.
A series of antibacterial and antifungal sulfonamide (sulfanilamide, sulfaguanidine, sulfamethaxozole, 4-aminoethylbenzenesulfonamide and 4-amino-6-trifluoromethyl-benzene-1,3-disulfonamide) derived chromones, previously reported as inhibitors of carbonic anhydrase, have been screened for in-vitro antibacterial activity against four Gram-negative (Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi and Shigella flexeneri) and two Gram-positive (Bacillus subtilis and Staphylococcus aureus) bacterial strains, and for in-vitro antifungal activity against Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani, Candida glaberata. All compounds (1)–(5) showed significant antibacterial activity against all four Gram-negative species and both Gram-positive species. However, three of them, (1), (4) and (5), were found to be comparatively much more active compared to (2) and (3). Of these, (5) was found to be the most active one. For antifungal activity, generally compounds (1) and (2) showed significant activity against more than three strains whereas (3)–(5) also showed significant activity against varied fungal strains. In the brine shrimp bioassay for in-vitro cytotoxic properties, only two compounds, (4) and (5) displayed potent cytotoxic activity, LD50 = 2.732 × 10? 4 M) and LD50 = 2.290 × 10? 4 M) respectively, against Artemia salina.  相似文献   

9.
The interaction between thiamine hydrochloride (TA) and bovine serum albumin (BSA) was investigated by fluorescence, FTIR, UV–vis spectroscopic and cyclic voltammetric techniques under optimised physiological condition. The fluorescence intensity of BSA is gradually decreased upon addition of TA due to the formation of a BSA–TA complex. The binding parameters were evaluated and their behaviour at different temperatures was analysed. The quenching constants (Ksv) obtained were 2.6 × 104, 2.2 × 104 and 2.0 × 104 L mol?1 at 288, 298 and 308 K, respectively. The binding mechanism was static-type quenching. The values of ΔH° and ΔS° were found to be 26.87 kJ mol?1 and 21.3 J K?1 mol?1, and indicated that electrostatic interaction was the principal intermolecular force. The changes in the secondary structure of BSA upon interaction with TA were confirmed by synchronous and 3-D spectral results. Site probe studies reveal that TA is located in site I of BSA. The effects of some common metal ions on binding of BSA–TA complex were also investigated.  相似文献   

10.
Abstract

This study was carried out to determine the lethality of the entomopathogenic fungus, Lecanicillium longisporum on eggs, young and old nymphs of the greenhouse whitefly, Trialeurodes vaporariorum. Mortality percentage was significantly differed based on stage of T. vaporariorum and conidial concentrations of L. longisporum. Average of the infection level to insect was very low particularly in egg with only 9.81%, even with higher conidial concentrations (1×107 conidia mL-1). Whereas, it was higher in 1st and 2nd instar (46.56%) and 3rd and 4th instars (37.21%). Three parameters were assessed with T. vaporariorum eggs, namely; egg infection, egg hatchability and crawlers emergence. Egg mortality percentages averaged 3.56, 7.14, 9.64, 16.42 and 20.35% with fungal concentrations of 1×103, 1×104, 1×105, 1×106 and 1×107 conidia mL-1, respectively. Daily infection percentages were varied depend upon the conidia concentration where the highest infection rate of eggs was occurred with 1×107. Egg hatch was very high and the mortality among the emerged crawlers was neglectable compared with the control. Efficiency of L. longisporum on whitefly nymphs also was varied based on the insect instar and fungal concentration. Mortality percentages were obviously higher in young nymphs (1st and 2nd instars) than in older ones (3rd and 4th instars). The results indicated that nymphs were highly susceptible to fungal treatment compared with eggs.  相似文献   

11.
Abstract

Myeloperoxidase is very susceptible to reducing radicals because the reduction potential of the ferric/ferrous redox couple is much higher compared with other peroxidases. Semiquinone radicals are known to reduce heme proteins. Therefore, the kinetics and spectra of the reactions of p-hydroquinone, 2,3-dimethylhydroquinone and 2,3,5-trimethylhydroquinone with compounds I and II were investi-gated using both sequential-mixing stopped-flow techniques and conventional spectrophotometric measurements. At pH 7 and 15°C the rate constants for compound I reacting with p-hydroquinone, 2,3-dimethylhydroquinone and 2,3,5-trimethylhydroquinone were determined to be 5.6±0.4×107 M-1s-1, 1.3±0.1×106 M-1s-1 and 3.1±0.3×106 M-1s-1, respectively. The corresponding reaction rates for compound II reduction were calculated to be 4.5±0.3×106 M-1s-1, 1.9±0.1×105 M-1s-1 and 4.5±0.2×104 M-1s-1, respectively. Semiquinone radicals, produced by compounds I and II in the classical peroxidation cycle, promote compound III (oxymyeloperoxidase) formation. We could monitor formation of ferrous myeloperoxidase as well as its direct transition to compound III by addition of molecular oxygen. Formation of ferrous myeloperoxidase is shown to depend strongly on the reduction potential of the corresponding redox couple benzoquinone/semiquinone. With 2,3-dimethylhydroquinone and 2,3,5-trimethylhydroquinone as substrate, myeloperoxidase is extremely quickly trapped as compound III. These MPO-typical features could have potential in designing specific drugs which inhibit the production of hypochlorous acid and consequently attenuate inflammatory tissue damage.  相似文献   

12.
A real-time polymerase chain reaction approach was used in this study to determine the population of major ruminal bacterial species (Fibrobacter succinogenes, Ruminococcus albus, and Ruminococcus flavefaciens) in digesta and rumen fluid of swamp buffalo (Bubalus bubalis). Four rumen-fistulated, male swamp buffalo were randomly assigned according to a 4 × 4 Latin square design to evaluate the effect of the urea-treated rice straw (roughage source)-to-concentrate ratio on cellulolytic bacterial distribution. Animals were fed roughage-to-concentrate (R:C) ratios of 100:0, 75:25, 50:50, and 25:75, respectively. At the end of each period, rumen fluid and digesta were collected at 0 h and 4 h post-morning-feeding. It was found that feeding urea-treated rice straw solely increased these three cellulolytic bacteria numbers up to 2.65 × 109 and 3.54 × 109 copies per milliliter for F. succinogenes, 5.10 × 107 and 7.40 × 107 copies per millilter for R. Flavefaciens, and 4.00 × 106 and 6.00 × 106 copies per milliliter for R. albus in rumen fluid and digesta, respectively. The distribution of the three cellulolytic bacteria species in digesta were highest at 3.21 × 109, 4.55 × 107, and 4.56 × 106 copies per milliliter for F. succinogenes, R. flavefaciens, and R. albus, respectively. Moreover, at 4 h post-morning-feeding, the populations of the three cellulolytic bacteria were higher than found at 0 h post-morning-feeding. It is most notable that F. succinogenes were the highest in population in the rumen of swamp buffalo and cellulolytic bacteria mostly adhered to feed digesta in the rumen.  相似文献   

13.
A series of 15 previously reported N4-substituted isatin-3-thiosemicarbazones 3a-o has been screened for cytotoxic, antibacterial, antifungal and urease inhibitory activities. Compounds 3b, 3e and 3n proved to be active in cytotoxicity assay; 3e exhibited a high degree of cytotoxic activity (LD50 = 1.10 × 10? 5 M). Compound 3h exhibited significant antibacterial activity against B. subtilis, whereas compounds 3a, 3k and 3l displayed significant antifungal activity against one or more fungal strains i.e. T. longifusus, A. flavus and M. canis. In human urease enzyme inhibition assay, compounds 3g, 3k and 3m proved to be the most potent inhibitors, exhibiting relatively pronounced inhibition of the enzyme. These compounds, being non-toxic, could be potential candidates for orally effective therapeutic agents to treat certain clinical conditions induced by bacterial ureases like H. pylori urease. This study presents the first example of inhibition of urease by isatin-thiosemicarbazones and as such provides a solid basis for further research on such compounds to develop more potent inhibitors.  相似文献   

14.
A new series of 12 N4-substituted isatin-3-thiosemicarbazones 2a-l has been synthesized, characterized and screened for in vitro cytotoxic, phytotoxic and urease inhibitory effects. All the compounds proved to be active in the brine shrimp bioassay; 2a, 2b, 2d, 2f and 2h-l exhibited a high degree of cytotoxic activity (LD50 = 1.10 × 10? 5 M–3.10 × 10? 5 M). In urease-inhibition assay, compounds 2a, 2b, 2e, 2f, 2h-j and 2l proved to be potent inhibitors displaying relatively much greater inhibition of the enzyme with IC50 values ranging from 20.6 μM to 50.6 μM. Amongst these, 2a and 2f were found to be the most potent ones exhibiting pronounced inhibition with IC50 value 20.6 μM. All the synthetic compounds showed weak to moderate (10–40%) phytotoxicity at the highest tested concentration (500 μg/mL) indicating their usefulness as inhibitors of soil ureases.  相似文献   

15.
Abstract

Saffron is the red dried stigmas of Crocus sativus L. flowers and used both as a spice and as a drug in traditional therapeutic. The biological activity of saffron in modern medicine is in development. Its numerous applications as an anti-oxidant and anti-cancer agent are due to its secondary metabolites and their derivatives (safranal, crocins, crocetin, dimethylcrocetin). The aim of this study was to examine the interaction of transfer RNA with safranal, crocetin, and dimethylcrocetin in aqueous solution at physiological conditions. Constant tRNA concentration (6.25 mM) and various drug/tRNA (phosphate) molar ratios of 1/48 to 1/8 were used. FT-IR and UV-Visible difference spectroscopic methods have been applied to determine the drug binding mode, the binding constants and the effects of drug complexation on the stability and conformation of tRNA duplex. External binding mode was observed for safranal crocetin and dimethylcrocetin, with overall binding constants Ksafranal = 6.8 (± 0.34) × 103 M?1, KCRT = 1.4 (± 0.31) × 104 M?1, and KDMCRT = 3.4 (± 0.30) × 104 M?1. Transfer RNA remains in the A-family structure, upon safranal, crocetin and dimethylcrocetin complexation.  相似文献   

16.
A new series of antibacterial and antifungal furanyl-derived sulfonamides and their cobalt (II), copper (II), nickel (II) and zinc (II) metal complexes have been synthesized, characterized and screened for their in-vitro antibacterial activity against four Gram-negative (Escherichia coli, Shigella flexneri, Pseudomonas aeruginosa and Salmonella typhi) and two Gram-positive (Bacillus subtilis and Staphylococcus aureus) bacterial strains and, for in-vitro antifungal activity against Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani and Candida glaberata. The results of these studies revealed that all compounds showed significant to moderate antibacterial activity. However, the zinc (II) complexes were found to be comparatively much more active as compared to the others. For antifungal activity generally, compounds (22) and (24) showed significant activity against Escherichia coli (a), (6) against Shigella flexeneri (b), (16) and (22) against Pseudomonas aeruginosa (c), (14) and (16) against Salmonella typhi (d), (9) against Staphylococcus aureus (e) and, (14) and (16) against Bacillus subtilis (f) fungal strains. The brine shrimp (Artemia salina) bioassay was also carried out to study their in-vitro cytotoxic properties. Only three compounds, (6), (10) and (23) displayed potent cytotoxic activity with LD50 = 1.8535 × 10? 4, 1.8173 × 10? 4 and 1.9291 × 10? 4 respectively.  相似文献   

17.
Summary The growth profile and hydrocarbonoclastic potential of microorganisms isolated from tarballs harvested from Ibeno beach in the Bight of Bonny were examined to determine their role in the degradation of the aquatic pollutants (tarballs). The results of the analysis revealed that the mean heterotrophic bacterial count ranged from 3 (±0.01) × 103 to 3.18 (±0.2) × 105 c.f.u./g. The mycological count ranged from 1 (±0.3) × 102 to 2 (±0.4) × 104 c.f.u./g while the mean count of biodegraders on tarball mineral salt medium (TMSM) ranged from 1 (±0.3) × 102 to 2 (±0.4) × 104 c.f.u./g. The ability of the microbial isolates to utilize the tarballs as their sole source of carbon and energy was examined and noticed to vary in growth profiles between the isolates. Chromobacterium violaceum, Cladosporium resinae, Bacillus submarinus, Micrococcus varians, Pseudomonas aeruginosa, Candida marina and Saccharomyces estuari were the most efficient utilizers and biodegraders while Corynebacterium glutamicum, Nocardia marina, and Cryptococcus albidus exhibited moderate growth in TMSM. Vibrio parahaemolyticus and Escherichia coli were opportunistic inhabitants, as they could neither grow nor degrade the balls in TMSM. The results imply that the efficient biodegraders like Chromobacterium violaceum could extensively degrade the balls with time.  相似文献   

18.
Synthesis, characterization and biological studies of Schiff base-derived sulfonamides and their Co (II), Cu (II), Ni (II) and Zn (II) complexes have been reported and screened for in-vitro antibacterial activity against six Gram-negative; E. coli, K. pneumoniae, P. aeruginosa, P. mirabilis, S. typhi and S. dysenteriae and four Gram-positive; B. cereus, C. diphtheriae, S. aureus and S. pyogenes bacterial strains and for in-vitro antifungal activity against T. longifusus, C. albicans, A. flavus, M. canis, F. solani, and C. glaberata. All compounds showed moderate to significant antibacterial activity, however, the zinc (II) complexes were found to be more active. Some of the compounds also showed significant antifungal activity against various fungal strains. Only compounds (6) and (10) displayed potent cytotoxic activity with LD50 = 4.644 × 10? 4 and 4.106 × 10? 4 moles/mL respectively, against Artemia salina. The X-ray structure of 4-[(2-hydroxybenzylidene)amino]benzenesulfonamide is also reported.  相似文献   

19.
Summary The aim of this study was to investigate the microbiological quality and the indigenous lactic acid bacteria (Lactobacillus) of Civil cheese. In this study, for identification of lactic acid bacteria isolated from cheese samples, the Microbiology Identification System (MIS) was used. In the samples, average of total aerobic mesophilic bacteria, yeast and moulds, lactic acid bacteria and Staphylococcus aureus (Staph. aureus) were determined to be 3.0×108, 2.0×106, 1.4×107, 4.10×104 c.f.u./g, respectively. Coliform bacteria were lower than <10 c.f.u./g in 26.67 % of the samples. On the other hand, the coliform-positive samples showed an average of 4.2×104 c.f.u./g. Staph. aureus was not detected in 33.33% of Civil cheese samples. Seventy-two strains of Lactobacillus isolated from Civil cheese were identified. Growth at 5, 10 and 37 °C, 2.5% and 6.5% NaCl and gas (CO2) production from glucose of the isolated strains were also determined. Of the 72 isolates, 20 were identified as Lb. malefermentans, 18 as Lb. fermentum, 17 as Lb. parabuchneri, 10 as Lb. vaccinostercus, 2 as Lb. oris, 1 as Lb. bifermentans, 1 as Lb. delbruecki subsp. bulgaricus, 1 as Lb. cellobiosus, 1 as Lb. hilgardii, 1 as Lb. paracasei subsp. tolerans.  相似文献   

20.
THE CYTOLOGY AND PHYLOGENETICS OF THE DIPLOID SPECIES OF GOSSYPIUM   总被引:2,自引:0,他引:2  
Meiotic chromosome behavior of 11 inter-genomic hybrids of Gossypium (2n = 26) were investigated. Per cell univalent frequencies at meiotic metaphase I in these hybrids were: A genome × Cgenome—G. herbaceum × sturtianum, 10.53; G. herbaceum × australe, 18.05. A genome × E genome—G. smnalense × arboreum, 21.82. B genome × C genome—G. anomalum × sturtianum, 9.23; G. anomalum × australe, 13.11. B genome × D genome—G. anomalum × klotzschianum, 17.45; G. anomalum × raimondii, 18.83. C genome × D genome—G. robinsonii × davidsonii, 12.77; G. sturtianum (armourianum × thurberi), 8.63. C genome × E genome—G. somalense × australe, 23.78; G. somalense × bickii, 25.58. Trivalent and quadrivalent frequencies were relatively high for those hybrids involving a C genome species, indicating that a reciprocal translocation differentiates the C genome from the A, B, D, and E genomes. The results of this study and the data of similar studies cited from the literature on Gossypium cytogenetics are discussed relative to the phylogenetics and evolution of the major (genome) groups of Gossypium and their constituent taxa.  相似文献   

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