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1.

In this study, we look into the biogenic synthesis of (AgNPs) utilizing a simple and environmentally friendly method based on an aqueous extract of Moringa Oleifera (MO). The synthesized MOAgNPs were characterized using a UV–Visible spectrophotometry, X-ray diffraction (XRD), Fourier transform infrared (FT-IR) spectra and TEM image which confirmed the spherical shape of MOAgNPs with particle size range of 5–50 nm with an average particle size of 38.7 nm. Significantly, the prepared MOAgNPs showed high pesticidal activity towards Spodoptera littoralis. MOAgNPs also exhibited strong antibacterial activities against Gram-positive and Gram-negative bacteria. The prepared MOAgNPs were screened for their cytotoxic effect against (HCT-116), (HepG-2) and (MCF-7) carcinoma cell lines. Finally, the synthesized MOAgNPs have been used as a catalyst for the reduction of 2,4-Dinitrophenol using NaBH4 to 2,4-Diaminophenol. Taken together, the outstanding catalytic and biological activities of the synthesized MOAgNPs entitled them for applications as catalyst, pesticidal, antibacterial and anticancer agents in medical applications.

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2.
Akt acts as a pivotal regulator in the PI3K/Akt signaling pathway and represents a potential drug target for cancer therapy. To search for new inhibitors of Akt kinase, we performed a structure-based virtual screening using the DOCK 4.0 program and the X-ray crystal structure of human Akt kinase. From the virtual screening, 48 compounds were selected and subjected to the Akt kinase inhibition assay. Twenty-six of the test compounds showed more potent inhibitory effects on Akt kinase than the reference compound, H-89. These 26 compounds were further evaluated for their cytotoxicity against HCT-116 human colon cancer cells and HEK-293 normal human embryonic kidney cells. Twelve compounds were found to display more potent or comparable cytotoxic activity compared to compound H-89 against HCT-116 colon cancer cells. The best results were obtained with Compounds a46 and a48 having IC50 values (for HCT-116) of 11.1 and 9.5 µM, respectively, and selectivity indices (IC50 for HEK-293/IC50 for HCT-116) of 12.5 and 16.1, respectively. Through structure-based virtual screening and biological evaluations, we have successfully identified several new Akt inhibitors that displayed cytotoxic activity against HCT-116 human colon cancer cells. Especially, Compounds a46 and a48 may serve as useful lead compounds for further development of new anticancer agents.  相似文献   

3.
Background: Granulin is a secreted, glycosylated peptide—originated by cleavage from a precursor protein—which is involved in cell growth, tumor invasion and angiogenesis. However, the specific prognostic impact of granulin in human colorectal cancer has only been studied to a limited extent. Thus, we wanted to assess the expression of granulin in colorectal cancer patients to evaluate its potential as a prognostic biomarker. Methods: Expressional differences of granulin in colorectal carcinoma tissue (n = 94) and corresponding healthy colon mucosa were assessed using qRT-PCR. Immunohistochemistry was performed in colorectal cancer specimens (n = 97), corresponding healthy mucosa (n = 47) and colorectal adenomas (n = 19). Subsequently, the results were correlated with histopathological and clinical patients’ data. HCT-116 cells were transfected with siRNA for invasion and migration assays. Results: Immunohistochemistry and qRT-PCR revealed tumoral over expression of granulin in colorectal cancer specimens compared to corresponding healthy colon mucosa and adenomas. Tumoral overexpression of granulin was associated with a significantly impaired overall survival. Moreover, downregulation of granulin by siRNA significantly diminished the invasive capacities of HCT-116 cells in vitro. Conclusion: Expression of granulin differs in colorectal cancer tissue, adenomas and healthy colon mucosa. Furthermore, granulin features invasive and migrative capabilities and overexpression of granulin correlates with a dismal prognosis. This reveals its potential as a prognostic biomarker and granulin could be a worthwhile molecular target for individualized anticancer therapy.  相似文献   

4.
Abstract

The objective of this present work is to optimize and prepare silver nanoparticles(AgNPs) in Dioctyl sodium sulfosuccinate (AOT) microemulsion (ME) for oral use and to investigate its antibacterial and anticancer activity in vitro and in vivo. In vitro drug release study confirmed that faster release of drug at the tumor cells compared to the blood circulation. It also showed a potential antibacterial activity against pathogenic bacteria. The optimized AgNPs loaded ME confirmed significant cytotoxicity against MCF-7 cancer cell line with IC50 16.72?±?0.014?μg/mL and significant reduction in solid Ehrlich tumor growth in compared to the control, placebo and pure drug.  相似文献   

5.
The aim of this study is to synthesize phenethyl-conjugated chitosan oligosaccharide (COS) (abbreviated as ChitoPEITC) conjugates and then fabricate chlorin E6 (Ce6)-incorporated nanophotosensitizers for photodynamic therapy (PDT) of HCT-116 colon carcinoma cells. PEITC was conjugated with the amine group of COS. Ce6-incorporated nanophotosensitizers using ChitoPEITC (ChitoPEITC nanophotosensitizers) were fabricated by dialysis method. 1H nuclear magnetic resonance (NMR) spectra showed that specific peaks of COS and PEITC were observed at ChitoPEITC conjugates. Transmission electron microscope (TEM) confirmed that ChitoPEITC nanophotosensitizers have spherical shapes with small hydrodynamic diameters less than 200 nm. The higher PEITC contents in the ChitoPEITC copolymer resulted in a slower release rate of Ce6 from nanophotosensitizers. Furthermore, the higher Ce6 contents resulted in a slower release rate of Ce6. In cell culture study, ChitoPEITC nanophotosensitizers showed low toxicity against normal CCD986Sk human skin fibroblast cells and HCT-116 human colon carcinoma cells in the absence of light irradiation. ChitoPEITC nanophotosensitizers showed a significantly higher Ce6 uptake ratio than that of free Ce6. Under light irradiation, cellular reactive oxygen species (ROS) production of nanophotosensitizers was significantly higher than that of free Ce6. Especially, PEITC and/or ChitoPEITC themselves contributed to the production of cellular ROS regardless of light irradiation. ChitoPEITC nanophotosensitizers showed significantly higher PDT efficacy against HCT-116 cells than that of free Ce6. These results indicate that ChitoPEITC nanophotosensitizers have superior potential in Ce6 uptake, ROS production and PDT efficacy. In the HCT-116 cell-bearing mice tumor-xenograft model, ChitoPEITC nanophotosensitizers efficiently inhibited growth of tumor volume rather than free Ce6. In the animal imaging study, ChitoPEITC nanophotosensitizers were concentrated in the tumor tissue, i.e., fluorescence intensity in the tumor tissue was stronger than that of other tissues. We suggest that ChitoPEITC nanophotosensitizers are a promising candidate for the treatment of human colon cancer cells.  相似文献   

6.
《Ceramics International》2023,49(20):32568-32576
In recent years, extensive assessments were performed on metal oxide nanoparticles (MONs) for numerous biomedical implementations. This study aimed to describe a facile, environment-friendly and, green route for the synthesis of Zinc Oxide nanoparticles (ZnO-NPs) by exerting Lepidium sativum L. seed extract as a capping agent and to evaluate their anticancer activities on important human colorectal cancer cell lines, SW480, HT-29 and Caco-2. Characterization of the green chemistry synthesized ZnO-NPs were carried out using UV–visible (UV–Vis) spectroscopy, X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy, Field emission scanning electron microscope (FE-SEM) and, energy-dispersive X-ray (EDX) spectroscopy. UV–Visible spectra confirmed the biosynthesis of ZnO-NPs and showed a broad absorption peak at 325–450 nm. Microscopic results revealed the formation of the spherical and hexagonal shaped NPs having average size 36.96 and 44.50 nm. In addition, the XRD data demonstrated the crystalline structure of our green ZnO-NPs. In biological experiments, the outcomes of MTT assay indicated the significant cytotoxic effect of ZnO-NPs against SW480, HT-29 and Caco-2 cancer cells through a dosage reliant mechanism. Moreover, the real-time PCR data revealed the potent capability of ZnO-NPs in inducing apoptosis throughout colon cancer cells through the down-regulation of Bcl-2 gene expression and up-regulation of Bax and p53 genes. Overall, these results suggested the applicability of green fabricated ZnO-NPs from the extract of Lepidium sativum L. as a novel and hopeful therapeutic agent for colorectal cancer treatment.  相似文献   

7.
Block copolymers composed of poly(3-hydroxyoctanoate) (PHO) and methoxy poly(ethylene glycol) (PEG) were synthesized to prepare paclitaxel-incorporated nanoparticle for antitumor drug delivery. In a 1H-NMR study, chemical structures of PHO/PEG block copolymers were confirmed and their molecular weight (M.W.) was analyzed with gel permeation chromatography (GPC). Paclitaxel as a model anticancer drug was incorporated into the nanoparticles of PHO/PEG block copolymer. They have spherical shapes and their particle sizes were less than 100 nm. In a 1H-NMR study in D2O, specific peaks of PEG solely appeared while peaks of PHO disappeared, indicating that nanoparticles have core-shell structures. The higher M.W. of PEG decreased loading efficiency and particle size. The higher drug feeding increased drug contents and average size of nanoparticles. In the drug release study, the higher M.W. of PEG block induced the acceleration of drug release rate. The increase in drug contents induced the slow release rate of drug. In an antitumor activity study in vitro, paclitaxel nanoparticles have practically similar anti-proliferation activity against HCT116 human colon carcinoma cells. In an in vivo animal study using HCT116 colon carcinoma cell-bearing mice, paclitaxel nanoparticles have enhanced antitumor activity compared to paclitaxel itself. Therefore, paclitaxel-incorporated nanoparticles of PHO/PEG block copolymer are a promising vehicle for antitumor drug delivery.  相似文献   

8.
以冬凌草甲素为原料,丁二酸为连接臂在其C-14位引入氨基磷酸酯及含氮化合物,设计并合成了6个未见文献报道的目标化合物。所有衍生物均经过氢谱、碳谱以及高分辨质谱进行结构确认,并采用噻唑蓝比色法(MTT)对目标化合物进行人结肠癌HCT-116、人肝癌BEL-7402、人乳腺癌MCF-7细胞系抗癌活性筛选。结果表明,绝大多数化合物表现出较强的抗增殖作用,其中(1S,4aR,5S,6S,6aR,9S,11aS,11bS,14R)-1,5,6-三羟基-4,4-二甲基-8-亚甲基-7-氧代十二氢-1H-6,11b-(环氧甲酰基)-6a,9-甲基环庚[a]萘-14-基4-(((二乙氧基磷酰基)(苯基)甲基)氨基)-4-氧代丁酸酯表现出最强的抗增殖作用,尤其对人乳腺癌MCF-7细胞系的抗增殖活性最好,其IC50值仅为2.73μmol/L,活性提高约4.61倍,具有进一步开发的价值。  相似文献   

9.
Plant-derived natural polyphenols exhibit anticancer activity without showing any noticeable toxicities to normal cells. The aim of this study was to investigate the role of p53 on the anticancer effect of polyphenols isolated from Korean Artemisia annua L. (pKAL) in HCT116 human colorectal cancer cells. We confirmed that pKAL induced reactive oxygen species (ROS) production, propidium iodide (PI) uptake, nuclear structure change, and acidic vesicles in a p53-independent manner in p53-null HCT116 cells through fluorescence microscopy analysis of DCF/PI-, DAPI-, and AO-stained cells. The pKAL-induced anticancer effects were found to be significantly higher in p53-wild HCT116 cells than in p53-null by hematoxylin staining, CCK-8 assay, Western blot, and flow cytometric analysis of annexin V/PI-stained cells. In addition, expression of ectopic p53 in p53-null cells was upregulated by pKAL in both the nucleus and cytoplasm, increasing pKAL-induced cell death. Moreover, Western bot analysis revealed that pKAL-induced cell death was associated with upregulation of p53-dependent targets such as p21, Bax and DR5 and cleavage of PARP1 and lamin A/C in p53-wild HCT116 cells, but not in p53-null. Taken together, these results indicate that p53 plays an important role in enhancing the anticancer effects of pKAL by upregulating p53 downstream targets and inducing intracellular cell death processes.  相似文献   

10.
In this study, silver nanoparticles were synthesized using the Crataegus douglasii fruit extract as a reducing agent. The reaction process was monitored by UV–vis spectroscopy. Further characterization was carried out using scanning electron microscopy (SEM). To optimize the biosynthesis of silver nanoparticles, the effect of process variables such as extract concentrations, mixing ratio of the reactants, time and pH were also investigated. The SEM images showed silver nanoparticles with 29.28 nm size and nearly spherical shape at 24 h interaction time. The antibacterial activity of the synthesized silver nanoparticles was confirmed against Staphylococcus aureus and Escherichia coli.  相似文献   

11.
Ruthenium compounds have been shown to be promising alternatives to platinum(II) drugs. However, their clinical success depends on achieving mechanisms of action that overcome Pt-resistance mechanisms. Electron-deficient organoruthenium complexes are an understudied class of compounds that exhibit unusual reactivity in solution and might offer novel anticancer mechanisms of action. Here, we evaluate the in vitro and in vivo anticancer properties of the electron-deficient organoruthenium complex [(p-cymene)Ru(maleonitriledithiolate)]. This compound is found to be highly cytotoxic: 5 to 60 times more potent than cisplatin towards ovarian (A2780 and A2780cisR), colon (HCT116 p53+/+ and HCT116 p53−/−), and non-small cell lung H460 cancer cell lines. It shows no cross-resistance and is equally cytotoxic to both A2780 and A2780cisR cell lines. Furthermore, unlike cisplatin, the remarkable in vitro antiproliferative activity of this compound appears to be p53-independent. In vivo evaluation in the hollow-fibre assay across a panel of cancer cell types and subcutaneous H460 non-small cell lung cancer xenograft model hints at the activity of the complex. Although the impressive in vitro data are not fully corroborated by the in vivo follow-up, this work is the first preclinical study of electron-deficient half-sandwich complexes and highlights their promise as anticancer drug candidates.  相似文献   

12.
The goal of the present study was to investigate the toxicity of biologically prepared small size of silver nanoparticles in human lung epithelial adenocarcinoma cells A549. Herein, we describe a facile method for the synthesis of silver nanoparticles by treating the supernatant from a culture of Escherichia coli with silver nitrate. The formation of silver nanoparticles was characterized using various analytical techniques. The results from UV-visible (UV-vis) spectroscopy and X-ray diffraction analysis show a characteristic strong resonance centered at 420 nm and a single crystalline nature, respectively. Fourier transform infrared spectroscopy confirmed the possible bio-molecules responsible for the reduction of silver from silver nitrate into nanoparticles. The particle size analyzer and transmission electron microscopy results suggest that silver nanoparticles are spherical in shape with an average diameter of 15 nm. The results derived from in vitro studies showed a concentration-dependent decrease in cell viability when A549 cells were exposed to silver nanoparticles. This decrease in cell viability corresponded to increased leakage of lactate dehydrogenase (LDH), increased intracellular reactive oxygen species generation (ROS), and decreased mitochondrial transmembrane potential (MTP). Furthermore, uptake and intracellular localization of silver nanoparticles were observed and were accompanied by accumulation of autophagosomes and autolysosomes in A549 cells. The results indicate that silver nanoparticles play a significant role in apoptosis. Interestingly, biologically synthesized silver nanoparticles showed more potent cytotoxicity at the concentrations tested compared to that shown by chemically synthesized silver nanoparticles. Therefore, our results demonstrated that human lung epithelial A549 cells could provide a valuable model to assess the cytotoxicity of silver nanoparticles.  相似文献   

13.
N–heterocyclic carbene (NHC) complexes of palladium(II) are generally active as catalysts toward various coupling reactions, while their pharmacological efficiencies are seldom explored. A new series of palladium(II) complexes of both, functionalized and non–functionalized NHCs that were active against the human colon cancer (HCT116) cells are reported. Complexes were prepared by the technique of transmetallation using palladium source and in situ prepared silver(I)–NHC complexes in acetonitrile, and all complexes are characterized using spectroscopic and analytical tools. Additionally, the structure of palladium complex 9 was elucidated using single crystal X–ray diffraction method. In vitro anticancer studies revealed that the palladium complexes, 9 and 10, having xylyl–spacers significantly inhibited the HCT116 cell growth, exhibiting IC50 values in low micromolar range in MTT assay.  相似文献   

14.
Development of new strategies of drug delivery is essential for effective treatment of cancer. In the present work, nanobiocomposite of fungal asparaginase was produced by immobilizing with silver nanoparticles. Asparaginase bound silver nanoparticle has shown higher enzyme activity than crude asparaginase. The primary and secondary amine/amide functional groups were found responsible for binding of asparaginase to silver nanoparticles. The silver nanobiocomposite of asparaginase was found to have smooth surface and crystalline in nature. The size of the nanobiocomposites ranged from 60 to 80 nm. The cytotoxicity of silver nanobiocomposite of asparaginase was found to be higher than free asparaginase on ovarian cancer cell line. The silver nanobiocomposite of asparaginase showed better cytotoxicity against ovarian cancer cell line A2780 than lung cancer cell line A549. Thus the synthesized silver nanobiocomposite of asparaginase can be used as an effective anticancer agent against lung cancer.  相似文献   

15.
Sun Y  Gou S  Liu F  Yin R  Fang L 《ChemMedChem》2012,7(4):642-649
A series of platinum(II) complexes with N-monocyclopentyl/cyclohexyl derivatives of 1R,2R-diaminocyclohexane as carrier ligands and dicarboxylate anions as leaving groups were synthesized and characterized. All complexes were characterized by elemental analysis, IR, (1)H NMR, and (13)C NMR spectroscopy, as well as ESIMS. The in vitro antiproliferative activities were tested by MTT assay against four human cancer cell lines; breast carcinoma (MCF-7) and colon cancer (HCT-116) cells were particularly sensitive, especially to complexes 1f (IC(50) =9.81 and 1.49 μM) and 2f (IC(50) =4.59 and 0.36 μM). Flow cytometry indicated that representative compounds exert cytotoxicity toward MCF-7 and HCT-116 cells through induction of apoptosis and blockage of cell-cycle progression in the S phase, similar to cisplatin. The interaction between the platinum(II) complexes and pET22b plasmid DNA was observed by agarose gel electrophoresis, revealing that complex 2f has the capacity to distort plasmid DNA in a manner distinct from that of oxaliplatin.  相似文献   

16.
The development of eco-friendly and nontoxic processes for the synthesis of nanoparticles is one of the most important discussed issues in nanotechnology science. This study reports the green synthesis of silver nanoparticles (AgNPs) using aqueous extract of leaf, stem, and root of Avicennia marina, the native and dominant mangrove plant in southern Iran. Among the different plant parts, the extract of leaves yielded the maximum synthesis of AgNPs. Synthesized AgNPs were investigated using UV–visible spectrophotometry, transmission electron microscopy (TEM), field emission scanning electron microscopy (FESEM), X-ray diffraction (XRD), energy-dispersive spectroscopy (EDS), and Fourier transform infrared (FTIR) spectroscopy. Absorption spectrum in 420?nm confirmed the synthesis of AgNPs. TEM images revealed that the synthesized AgNPs had the same spherical morphology with a size range between 0 and 75?nm. The distribution size histogram indicated that the most frequent particles were in the range of 10–15?nm and the mean size of nanoparticles was 17.30?nm. The results of SEM image showed nanoparticles with a size range between 15 and 43?nm. XRD pattern indicated the crystalline nature of synthesized nanoparticles. EDS results confirmed the presence of elements like silver, carbon, chlorine, nitrogen, and oxygen in the nanoparticles produced from leaf extract. Silver had the maximum percentage of formation, 51.6%. FTIR indicated the presence of different functional groups such as amines, alcohol, alkanes, phenol, alkyl halides, and aromatic loops in the synthesis process. Green biosynthesis of AgNPs using aqueous extract of native A. marina appears rapid, reliable, nontoxic, and eco-friendly.  相似文献   

17.
This study deals with the green synthesis of chromium oxide (Cr2O3) nanoparticles using a leaf extract of Abutilon indicum (L.) Sweet as a reducing and capping agent. Different characterization techniques were used to characterize the synthesized nanoparticles such as X-ray diffraction (XRD), Scanning electron microscope (SEM), Transmission electron microscope (TEM), Energy-dispersive X-ray (EDX), Fourier transform infrared (FTIR), X-ray photoelectron spectroscopy (XPS), and ultraviolet-visible (UV-VIS) spectroscopy. The X-ray diffraction technique confirmed the purity and crystallinity of the Cr2O3 nanoparticles. The average size of the nanoparticles ranged from 17 to 42 nm. The antibacterial activity of the green synthesized nanoparticles was evaluated against four different bacterial strains, E. coli, S. aureus, B. bronchiseptica, and B. subtilis using agar well diffusion and a live/dead staining assay. The anticancer activities were determined against Michigan Cancer Foundation-7 (MCF-7) cancer cells using MTT and a live/dead staining assay. Antioxidant activity was investigated in the linoleic acid system. Moreover, the cytobiocompatibility was analyzed against the Vero cell lines using MTT and a live/dead staining assay. The results demonstrated that the green synthesized Cr2O3 nanoparticles exhibited superior antibacterial activity in terms of zones of inhibition (ZOIs) against Gram-positive and Gram-negative bacteria compared to plant extracts and chemically synthesized Cr2O3 nanoparticles (commercial), but comparable to the standard drug (Leflox). The green synthesized Cr2O3 nanoparticles exhibited significant anticancer and antioxidant activities against MCF-7 cancerous cells and the linoleic acid system, respectively, compared to chemically synthesized Cr2O3 nanoparticles. Moreover, cytobiocompatibility analysis displayed that they presented excellent biocompatibility with Vero cell lines than that of chemically synthesized Cr2O3 nanoparticles. These results suggest that the green synthesized Cr2O3 nanoparticles’ enhanced biological activities might be attributed to a synergetic effect. Hence, green synthesized Cr2O3 nanoparticles could prove to be promising candidates for future biomedical applications.  相似文献   

18.
A new series of 2-amino-benzo[de]isoquinoline-1,3-diones was synthesized and fully characterized in our previous paper. Here, their cytotoxic effects have been evaluated in vitro in relation to colon HCT-116, hepatocellular Hep-G2 and breast MCF-7 cancer cell lines, using a crystal violet viability assay. The IC50-values of the target compounds are reported in µg/mL, using doxorubicin as a reference drug. The findings revealed that compounds 14, 15, 16, 21 and 22 had significant cytotoxic effects against HCT-116, MCF-7 and Hep-G2 cell lines. Their IC50 values ranged between 1.3 and 8.3 μg/mL in relation to doxorubicin (IC50 ≈ 0.45–0.89 μg/mL). Therefore, these compounds could be used as templates for furthering the development and design of more potent antitumor agents through structural modification.  相似文献   

19.

The present investigation showed the green synthesis of silver nanoparticles (AgNPs) using Ficus benghalensis (F. benghalensis) leaf extract. UV–Vis spectra of the biofabricated AgNPs displayed its maximum peak of absorption at 461 nm. High resolution-transmission electron microscopy images displayed the shape of AgNPs as spherical with an average diameter of 35 nm size. The analysis of X-ray diffraction confirmed the presence of crystalline AgNPs. The analysis of Fourier-transform infrared spectroscopy confirmed the existence of bioconstituents such as terpenoids, phenolics and flavonoids, which functions as bio-reducing agents. When compared with F. benghalensis extract, AgNPs displayed the considerably greater bioactivities. The exceptional antimicrobial functionalities of AgNPs against both the gram positive and gram negative bacteria makes them appropriate candidates for the production of antibiotics against the species that are resistant to traditional antibiotics. The assay of HDFa cell scratch confirmed that the AgNPs have greater ability of wound healing than the leaf extract of F. benghalensis. Altogether, the obtained results showed the application of synthesized AgNPs in the production of novel drugs that are used for wound healing in nursing care after rectal surgery.

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20.
Silver nanoparticles were obtained by chemical reduction of silver nitrate in water with sodium borohydride (NaBH4) in the presence of SDS (sodium dodecyl sulfate) as a stabilizer. The synthesized silver nanoparticles were characterized by UV-vis spectroscopy (UV-vis) and transmission electron microscopy (TEM). The formation of silver nanoparticles was confirmed from the appearance of surface plasmon absorption maxima at 400 nm by UV-vis. TEM showed the spherical nanoparticles with size in 10–20 nm. The antibacterial activity of silver nanoparticles was tested by using Gram-positive Staphylococcus aureus (S. aureus) and Gram-negative Escherichia coil (E. coli). The silver nanoparticles, whose bacterial activity was dependent on the aggregation degree between particles, exhibited bacterial activity against S. aureus and E. coli.  相似文献   

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