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1.
This study investigated the in vitro antioxidant, proapoptotic and anti-proliferative activity of phycocyanin extracted from Ulva lactuca (Chlorophyta) algae extract loaded on albumin nanoparticle (ULANP). The characterization of ULANP profile was done by using FTIR and its cytotoxicity was investigated by using MTT assay against HepG2 and MCF7 cell lines. The proapoptotic markers caspase 8 & 9 were measured. Analysis of ULANP by FTIR showed the characteristic band (2100 cm−1 ~3700 cm−1) that is indicated primarily by COO, CO and conjugated double bond. These bonds showed the spectral band at peaks of 2985 cm−1 and 2860 cm−1, 2986 cm−1 respectively. The antioxidant potential and radical scavenging property of ULANP was also appreciable as compared to the vitamin C and gallic acid. The antiproliferative assay carried out by WST-1 suggests that ULANP was effective against both HepG2 (93.17%) and MCF7 (91.3%). Caspase-8 and −9 were significantly elevated (p < 0.001) in both the cell lines of breast and liver cancer. It was concluded that ULANP induced anti-proliferative and pro-apoptotic activities on liver and breast cancer. It is promising as a novel antitumor activity for further investigation the mechanistic pathways mediated this action.  相似文献   

2.
Plants have natural products which use to possess antiproliferative potential against many cancers. In the present study, six isolated fractions (ethyl acetate, petroleum ether, chloroform, n-butanol, ethanol and aqueous) from Solanum nigrum were evaluated for their cytotoxic effect on different cell lines. Hepatic carcinoma cell line (HepG2), cervical cancer cell line (HeLa) and baby hamster kidney (BHK) used as normal non-cancerous cells were evaluated for cytotoxicity against isolated fractions. Cell viability assay was performed to evaluate the cytotoxicity of all fractions on different cell lines followed by the lactate dehydrogenase and vascular endothelial growth factor assays of most active fraction among all screened for cytotoxic analysis. HPLC analysis of most active fractions against cytotoxicity was performed to check the biological activity of compounds. Results displayed the potent cytotoxic activity of ethyl acetate fraction of S. nigrum against HepG2 cells with IC50 value of 7.89 μg/ml. Other fractions exhibited potent anticancer activity against HepG2 cells followed by HeLa cells. Fractions in our study showed no cytotoxicity in BHK cells. Cytotoxic activity observed in our current study exposed high antiproliferative potential and activity of ethyl acetate fraction against HepG2 cells. The results demonstrated that S. nigrum fractions exhibited anticancer activity against hepatic and cervical cancer cell lines with non-toxic effect in normal cells. These results reveal significant potential of S. nigrum for the therapeutic of cancers across the globe in future.  相似文献   

3.
This study assesses the antifungal efficacy of 14 essential oil (EO) components and some of their combinations as inhibitory to the growth of the aflatoxigenic fungus Aspergillus flavus LHPA9 isolated from biodeteriorating Asparagus racemosus herbal raw materials. The aim was to determine whether they could be recommended as plant-based preservatives for enhancement of the shelf life of herbal raw materials. Thymol, eugenol, menthol, and their combinations were highly efficacious as their minimum inhibitory concentration (MIC) for inhibition of fungal growth as well as aflatoxin B1 secretion was less than 1.0 μl ml−1. Geranyl acetate, linalool, β-asarone, 1, 8-cineol, and E-citral were moderately antifungal as their MIC ranged between 1.0 and 5.0 μl ml−1. During antioxidant activity 2, 2-diphenyl-1-picrylhydrazyl assay, thymol, eugenol, and β-caryophyllene showed strong radical scavenging activity, whereas β-asarone and p-cymene showed moderate activity. Some combinations of EO components showed synergism while others exhibited an additive or antagonism effect in their activity. The findings point to a recommendation that EO components are good alternatives to synthetic preservatives to prevent deterioration of stored herbal raw materials by fungal and aflatoxin contamination and free-radical oxidation.  相似文献   

4.
Many gallate esters have been applied as food additives due to their good biological properties. Herein, nine novel gallate ester derivatives were synthesized by a Friedel-Crafts alkylation reaction and characterized by melting point (m.p.), infrared (IR) spectroscopy, nuclear magnetic resonance (1H- and 13C-NMR) spectra, and high-resolution mass spectrometry (HR-ESI-MS). Their antioxidant and antibacterial activities were measured using a series of classical assays. Studies found that the products showed favorable antioxidant and antibacterial activities. Their 1,1-diphenyl-2-picrylhydrazyl free radical (DPPH) scavenging effect IC50 values were less than 5.00 μg mL−1 and their reducing power was not less than that of vitamin C (Vc). Furthermore, the antibacterial results showed that the minimum inhibitory concentration (MIC) values of the products were not greater than 8.00 μg mL−1, and their antibacterial rates were over 95 % at 300 μg mL−1. The above data add valuable and novel information that gallate ester derivatives can be considered potential food additives to address food safety issues because of their high biological activity and health benefits.  相似文献   

5.
In the current study the potential use of aqueous and methanolic extracts of Ephedra alata aerial parts as biological control agent against pathogenic bacteria and especially Staphylococcus aureus methicillin resistant isolated from auricular infections was evaluated. Chemical tests and spectrophotometric methods were used for screening and quantification of phytochemicals. The assessment of the antioxidant activity was accomplished by DPPH and ABTS radicals scavenging assays. Extracts were evaluated for their antibacterial efficacy by diffusion and microdilution methods. Biofilm inhibition was tested using XTT assay and the cytotoxicity of extracts was carried out on Vero cell line. The GC-FID analysis revealed that E. alata was rich in unsatured fatty acids. In addition, the aqueous extract had the highest flavonoid and protein contents (30.82 mg QE /g dry extract and 98.92 mg BSAE/g dry extract respectively). However, the methanolic extract had the highest phenolic, sugars and tannins. The antioxidant activity demonstrated that the aqueous extract exhibited the strong potency (IC50 ranged between 0.001 and 0.002 mg/mL).Both extracts displayed antimicrobial activity on Gram negative and positive strains. They were effective against S. aureus isolated from auricular infections. The tested extracts were able to inhibit biofilm formation with concentration-dependent manner.Moreover, no cytotoxic effect on Vero cells line was demonstrated for the extracts. Overall, our findings highlight the potential use of E. alata extract as a novel source of bioactive molecules with antioxidant, antibacterial and antiobiofilm effects for the control of infectious disease especially those associated to S. aureus methicillin resistant.  相似文献   

6.
Edaravone (3-methyl-1-phenyl-2-pyrazoline-5-one) is a neuroprotective drug that has been used for brain ischemia injury treatment. Because its activity is speculated to be due to free radical scavenging activity, we carried out a quantitative determination of edaravone’s free radical scavenging activity against multiple free radical species. Electron spin resonance (ESR) spin trapping-based multiple free-radical scavenging (MULTIS) method was employed, where target free radicals were hydroxyl radical, superoxide anion, alkoxyl radical, alkylperoxyl radical, methyl radical, and singlet oxygen. Edaravone showed relatively high scavenging abilities against hydroxyl radical (scavenging rate constant k = 2.98 × 1011 M−1 s−1), singlet oxygen (k = 2.75 × 107 M−1 s−1), and methyl radical (k = 3.00 × 107 M−1 s−1). Overall, edaravone’s scavenging activity against multiple free radical species is as robust as other known potent antioxidant such as uric acid, glutathione, and trolox. A radar chart illustration of the MULTIS activity relative to uric acid, glutathione, and trolox indicates that edaravone has a high and balanced antioxidant activity with low specificity.  相似文献   

7.
《Phytomedicine》2004,11(5):461-466
A total of 27 methanol extracts obtained from different plant parts of 10 species of rain forest trees belonging to four genera of the Flacourtiaceae and originating from Australia were investigated. In vitro cytotoxicity was measured by an ATP Lite-M assay method against the mouse P388 lymphocytic leukemia cell line. The total antioxidant activity has been assessed based on scavenging activity of stable ABTS free radicals. The minimum inhibition concentration (MIC) was determined by the dilution method performed in 96 well plates against four different microbes. The leaf extract of Casearia sp. (RB 3051), mature stem extract of Casearia grayi and stem extract of Scolopia braunii were found to have most antioxidant activity (IC50=2.9 μg/ml), cytotoxic activity (LC50=0.89 μg/ml) and antimicrobial activity against all four different microbes, respectively. The results obtained suggested that among the four genera studied Casearia is the most promising in respect of finding significant antioxidant, cytotoxic and also antimicrobial activity.  相似文献   

8.
Plants have always been the prime focus in medicine industries due to their enormous ethnobotanical uses and multitude of biological and therapeutic properties. In the current study, preliminary phytochemical composition, Total phenolic content (TPC), and total flavonoid content (TFC) with the antioxidant and antibacterial activity of hydroalcoholic extract and n-hexane, chloroform and n-butanol fractions of five selected medicinal plants [Tephrosia purpurea (L.) Pers., Lavandula stoechas L., Aesculus indica (Wall. ex Cambess.) Hook, Iris ensata Thunb., and Kalanchoe pinnata (Lam.) Pers.] from Pakistan, have been evaluated. TPC and TFC were determined by Folin-Ciocalteu’s and AlCl3 methods respectively. The antioxidant activity was performed by DPPH, ABTS, FRAP, and CUPRAC while the antibacterial potential of these plants was determined by agar well diffusion assay. K. pinnata (Lam.) Pers. exhibited the highest TPC (695 ± 13.2 mg.GA.Eq.g-1DE ± SD) in n-butanol fraction and the highest TFC in its chloroform faction (615 ± 6.31 mg Q.Eq.g−1 DE ± SD). The n-butanol fraction and hydroalcoholic extract of I. ensata Thunb. exhibited strong antioxidant potential by DPPH and CUPRAC assays respectively, whereas K. pinnata (Lam.) Pers. n-butanol fraction exhibited the strongest reducing potential. The hydroalcoholic extract of all tested plants exhibited significant antibacterial activity against tested bacterial strains with ZI (12–18 mm). Conclusively, K. pinnata (Lam.) Pers. (Family: Crassulaceae) and I. ensataThunb. (Family: Iridaceae) exhibited the highest antioxidant and antibacterial potential. They can be explored for the isolation of phytoconstituents responsible for this potential and serve as a lead for the production of new natural antioxidants and antibacterial agents that can be used to cure various diseases.  相似文献   

9.
This study aimed to investigate the antiproliferative and antioxidant properties of crude venom from the nematocyst of Jellyfish Acromitus flagellates on human lung cancer (A549) and liver cancer (HepG2) cell lines. The prepared crude venom was subjected to analyses of the biochemical constituents, protein profiles, antioxidant and anticancer activities by standard methods. The extracted venom was pale-yellow in color and viscous/sticky. The biochemical composition such as, protein (1.547 mg/ml), lipid (0.039 mg/ml) and carbohydrate (0.028 mg/ml) was estimated. Protein profiles were determined by SDS PAGE, the result revealed that the molecular weight range from 205 ? 3.5 kDa. The free radical scavenging activity was analyzed by the reducing potential (56.36%), DPPH (72.47%), hydroxyl (68.50%), superoxide anion (65.75%), and nitric oxide (33.04%). The cell viability was observed by using different concentrations (20 to 100 µg/ml) of crude venom on A549 and HepG2 cancer cell lines and the IC50 values were recorded in (60 μg/ml and 40 μg/ml) respectively, while it had none cytotoxic effects on Vero cell line up to the concentration of 90 μg/ml. These results suggest that crude venom from nematocyst of A. flagellatus possesses anti-cancer activity and able to develop novel drugs on marine-derived compounds.  相似文献   

10.
Ultrasonic circulating extraction technology was applied for the polysaccharide extraction from Asparagus officinalis. The crude polysaccharides were deproteinized by Sevag method and three main polysaccharide fractions, AOP-4, AOP-6 and AOP-8 were obtained by fractional precipitation with gradient concentrations of ethanol (40%, 60% and 80%). The in vitro antitumor and antioxidant activities of the polysaccharide fractions were evaluated by MTT assay and free radical-scavenging assay, respectively. Deproteinized AOPs showed higher antioxidant and antitumor activities than crude AOP. AOP-4 with molecular weight 5.75 × 104 Da showed significant function of scavenging hydroxyl radical. Three AOP fractions had significant antitumor activity against HeLa and BEL-7404 cells in a dose dependent manner. Furthermore, the inhibit activity of AOP-4 against HeLa cells was higher than those of other AOPs and the inhibition rate reached 83.96% at the concentration of 10 mg/mL. These results indicated that the AOP might be useful for developing natural safe antitumor drugs or health food.  相似文献   

11.
The extraction and characterization of the essential oils (EO) from Satureja montana L., Myristica fragrans H. and Cymbopogon flexuosus and the determination of their antibacterial and antioxidant activities were achieved. The EO were identified by gas chromatography/mass spectrometry and quantified by gas chromatography using a flame ionization detector. The antibacterial potential against Escherichia coli and Staphylococcus aureus was evaluated by cell susceptibility assays and by scanning electron microscopy. The antioxidant activity was evaluated by the 2,2-diphenyl-1-picrylhydrazyl assay, by β-carotene bleaching and by determining the reducing power. Borneol (36·18%), γ-terpineol (12·66%) and carvacrol (11·07%) were the principal components in the EO from S. montana, and sabinene (49·23%) and α-pinene (13·81%) were found in the EO from M. fragrans. Geranial (59·66%) and neral (38·98%) isomers were the only major components in the EO from C. flexuosus. The EO from S. montana was effective against E. coli, with minimum inhibitory and bactericidal concentrations (MIC and MBC) of 6·25 µl ml−1, whereas bactericidal potential against both was observed for the EO from M. fragrans; MIC = 6·25 µl ml−1 for S. aureus and MBC = 12·5 µl ml−1 for E. coli. A significant protective role on lipid substrates in the β-carotene bleaching assay was seen for the EO from S. montana and M. fragrans. Overall, such EO can be promising agents against pathogenic bacteria and for protecting biomolecules during oxidative stress.  相似文献   

12.
A novel water-soluble polysaccharide pMTPS-3, obtained from Melia toosendan Sieb. Et Zucc fruit by hot-water extraction and ethanol precipitation, was fractionated by DEAE-52 cellulose anion-exchange and Sephadex G-100 gel filtration chromatography. Its primary structural features and molecular weight were characterized by Fourier infrared spectrometry (FTIR), gel permeation chromatography (GPC) and gas chromatography (GC). And the antioxidant activities of pMTPS-3 in vitro were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay, superoxide radical scavenging assay and hydroxyl radical scavenging assay. The results suggested that pMTPS-3 was a heteropolysaccharide, composed of arabinose, glucose, mannose, and galactose in the molar ratio of 17.3:28.3:41.6:12.6 with molecular weight 26 100 Da. The purified pMTPS-3 was revealed to have notable scavenging activity against DPPH radical in a concentration-dependent manner and present a moderate inhibition of superoxide radicals with an IC50 (5.6 mg/ml), and potent inhibiting power for hydroxyl radical compared with crude polysaccharide. Further, it exhibited strong inhibition effect in vitro on the growth of human gastric cancer BGC-823 cells. It is strongly evidenced that pMTPS-3 purified from the crude polysaccharides of Melia toosendan Sieb. Et Zucc could be explored as a potential antioxidant and therapeutics.  相似文献   

13.
A detailed phytochemical study of the aerial parts of Bupleurum marginatum Wall. ex DC revealed a novel aryltetraline lactone lignan identified as 9-(benzo[d][1,3]dioxol-5-yl)-6,7,8-trimethoxy-3a,4,9,9a-tetrahydronaphtho[2,3-c]furan-1(3H)-one (marginatoxin) along with nine known compounds and characterization of five other compounds either by GLC/MS or LC/MS techniques. Chemical structures of the isolated compounds were unambiguously elucidated by both 1D, 2D NMR and mass spectrometry techniques.The in vitro cytotoxic activity of both methanol and dichloromethane extracts as well as the isolated compounds was assessed in two human cancer cell lines HepG2 and HeLa using the MTT assay. The new aryltetraline lactone lignan exhibited a potent cytotoxic activity with IC50 values of 12.14 and 16.90 μM after 24 h treatment for HepG2 and HeLa cells, respectively.  相似文献   

14.
IntroductionThe use of chemical products to neutralize microorganisms has always been a subject of discussion and research for alternative solutions, indeed, the use of essential oils has been a promising natural methodology.MethodsIn our study we used the essential oils from different parts of Thapsia transtagana (Apiaceae), obtained by hydrodistillation, were identified and using Gas chromatography–mass spectrometry (GC–MS) and Gas Chromatography-Flame Ionization Detection (GC/FID) methods and evaluated against several bacteria of Gram- and Gram + bacteria. Disk diffusion, Minimum Inhibitory Concentration (MIC) and Minimum Microbicidal Concentration (MMC) methods have been used. Free radical-scavenging activity and insecticidal activity of Thapsia transtagana essential oils were also identified.ResultsMajority products from different parts of Thapsia transtagana essential oil identified by GC–MS and GC/FID methods are 2,6-Dimethylnaphthalene, Pinane and Hexahydrofarnesyl acetone. The highest activity was found against Staphylococcus aureus using inflorescence essential oil with minimal inhibitory concentration value for 0,56 μg/μL. Insecticidal activity was also the subject of this study, roots and inflorescence essential oils demonstrated to have a remarkable potent against Acanthoscelides obtectus and Sitophilus oryzae using contact assessment, inhalation assessment and ingestion assessment tests. Insecticidal activity assay results showed a significant enhancement of mortality in both test insect pest on increasing the dose and exposure period. In the other hand, the different essential oils of Thapsia transtagana were evaluated for their radical scavenging activities by means of the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) assay. The strongest scavenging activity was observed in inflorescences essential oil fraction scavenged radicals effectively at 100% using 500 mgL-1 concentration.ConclusionIts essential oils were proved to have strong antimicrobial, insecticidal and antioxidant activities that allows it to be used by the pharmaceutical and cosmetic industries as natural preservative.  相似文献   

15.
The freshwater alga Spirogyra porticalis (Muell.) Cleve, a filamentous charophyte, collected from the Indian trans-Himalayan cold desert, was identified on the basis of morpho-anatomical characters. Extracts of this alga were made using solvents of varying polarity viz. n-hexane, acetonitrile, methanol and water. The antioxidant capacities and phenolic profile of the extracts were estimated. The methanol extract showing highest antioxidant capacity and rich phenolic attributes was further investigated and phytochemical profiling was conducted by gas chromatography-mass spectrometry (GC/MS) hyphenated technique. The cytotoxic activity of methanol extract was evaluated on human hepatocellular carcinoma HepG2 and colon carcinoma RKO cell lines. The anti-hypoxic effect of methanol extract of the alga was tested on in vivo animal system to confirm its potential to ameliorate oxidative stress. The antioxidant assays viz. ferric reducing antioxidant power (FRAP), 2,2''-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS), 1,1-diphenyl-2-picrylhydrazyl (DPPH) and nitric oxide (NO) radical scavenging capacities, β-carotene-linoleic acid bleaching property and lipid peroxidation exhibited analogous results, wherein the algal extracts showed significantly high antioxidant potential. The extracts were also found to possess high content of total proanthocyanidin, flavonoid and polyphenol. GC/MS analysis revealed the presence of thirteen chemotypes in the methanol extract representing different phytochemical groups like fatty acid esters, sterols, unsaturated alcohols, alkynes etc. with substantial phyto-pharmaceutical importance. The methanol extract was observed to possess anticancer activity as revealed from studies on HepG2 and RKO cell lines. In the present study, S. porticalis methanol extract also provided protection from hypoxia-induced oxidative stress and accelerated the onset of adaptative changes in rats during exposure to hypobaric hypoxia. The bioactive phytochemicals present in this trans-Himalayan alga are of enormous interest and can be utilized sustainably for discovery of novel drugs against oxidative stress.  相似文献   

16.
《Phytomedicine》2014,21(4):497-505
The study investigates the antioxidant, hepatoprotective and antiproliferative effects of novel icetexane diterpenoids (ice 14) isolated from hexane extract of stem bark of Premna tomentosa. A549, HT-29, MCF-7, MDA-MB-231, A431 cells were used to assess the antiproliferative activity by MTT assay. Cell death induced by apoptosis was determined by morphological assessment studies using acridine orange/ethidium bromide staining (dual staining), mitochondrial potential measurement by JC-1 staining, and cell cycle analysis by propidium iodide staining method by Muse cell analyser. Anti oxidant activity was investigated by in vitro assays such as DPPH, nitric oxide and superoxide scavenging activities. Hepatoprotective activity was determined in vitro with HepG2 cells and in vivo by tBHP induced hepatic damage mice model. Based on the in vitro cytotoxic assays and morphological assessment studies using fluorescence microscopic study (acridine orange and ethidium bromide double staining) and mitochondrial potential measurements, it was found that ice 2 and 3 possess good antiproliferative effect via mitochondrial mediated apoptosis in human lung and breast cancer cells. Results of in vitro antioxidant studies demonstrated that ice-4 has showed good antioxidant activity. The restoration of serum levels of SGOT, SGPT and ALKP, liver GSH status and reduction or inhibition of lipid peroxidation in liver of tBHP intoxicated mice after administration of ice-4 at dose of 250 mg/kg indicated its potential use for hepatoprotective activity.  相似文献   

17.
A substantial interest has been manifested in utilizing oil/metal oxide hybrid bionanocomposite, especially organic/ inorganic to design different biomedical applications. The present study reports the synthesis, characterization, antibacterial and anticancer properties of biogenic silver nanoparticles (AgNPs) and L.satiVum oil/PEG/Ag-MgO bionanocomposite. The fabricated AgNPs and L.sativum oil/PEG/Ag-MgO bionanocomposite were characterized by employing different spectroscopic (UV, FTIR, XRD) and microscopic (TEM, SEM) techniques. The particle size analysis showed that the mean size of 16.32 nm for AgNPS and 13.45 nm L.satiVum oil/PEG/Ag-MgO, indicating the excellent dispersion of Ag-MgO nanoparticles in the PEG– L.satiVum oil matrix. The antimicrobial activity of AgNPs and polymeric bionanocomposite was investigated against two pathogenic bacteria. The highest antibacterial effect was observed for bionanocomposite towards Gram-positive Staphylococcus aureus (27 mm) and Gram-negative Escherichia coli (25 mm) at 40 µg/well. The bionanocomposite completely vanished the bacterial growth (100%) at 80 µgmL−1 concentrations. Moreover, the AgNPs and polymeric bionanocomposite was evaluated for anticancer activity against human cervical cancer cells (HeLa cells) at different doses (50, 250, 500, and 1000 µgmL−1). The results showed polymeric bionanocomposite was stronger in inducing the HeLa cancer cell death than AgNPs. Overall, the fabricated L.satiVum oil/PEG/Ag-MgO bionanocomposite serve as a potential antimicrobial and anticancer agent and could be used in the development of novel drugs and health care products in near future.  相似文献   

18.
Thymus vulgaris L. (thyme), Origanum majorana L. (marjoram), and Origanum vulgare L. (oregano) were used to determine whether light modification (plants grown under nets with 40% shaded index or in un-shaded open field) could improve the quantity and quality of essential oils (EOs) and antioxidant activity. The yield of EOs of thyme, marjoram, and oregano obtained after 120 min of hydrodistillation was 2.32, 1.51, and 0.27 mL/100 g of plant material, respectively. At the same time under shading conditions plants synthetized more EOs (2.57, 1.68, and 0.32 mL/100 g of plant material). GC/MS and GC/FID analyses were applied for essential oils determinations. The main components of the thyme essential oil are thymol (8.05–9.35%); γ-terpinene (3.49–4.04%); p-cymene (2.80–3.60%) and caryophyllene oxide (1.54–2.15%). Marjoram main components were terpinene 4-ol (7.44–7.63%), γ-terpinene (2.82–2.86%) and linalool (2.04–2.65%) while oregano essential oil consisted of the following components: caryophyllene oxide (3.1–1.93%); germacrene D (1.17–2.0%) and (E)-caryophyllene (1.48–1.1%). The essential oil from thyme grown under shading (EC50 value after 20 min of incubation) have shown the highest antioxidant activity – 0.85 mg mL−1 in comparison to marjoram and oregano (shaded plants EC50 19.97 mg mL−1 and 7.02 mg mL−1 and unshaded, control plants EC50 54.01 mg mL−1 and 7.45 mg mL−1, respectively). The medicinal plants are a good source of natural antioxidants with potential application in the food and pharmaceutical industries. For production practice, it can be recommended to grow medicinal plants in shading conditions to achieve optimal quality parameters.  相似文献   

19.
Biological activities of a series of palladium(II) complexes (M1–M9) bearing NN, NS, and NO chelating ligands are reported. The palladium complexes were tested for their cytotoxic properties against human cervical cancer (HeLa) cells and antibacterial activity against Gm+ve and Gm–ve bacteria. Among the palladium complexes studied (M1-M9), the complex M5, M8, and M9 were found to be more effective in inhibiting the proliferation of HeLa cells. Hence, these complexes were further investigated for their potential role in cellular damage and apoptosis. DCFDA staining, Rhodamine 123 staining and DNA cleavage assay revealed that complex M5, M8 and M9 induced apoptotic cell death in HeLa cells through ROS generation, DNA damage and mitochondrial depolarization. Computational and titration studies also indicated strong electrostatic interaction with DNA groove. Most of the complexes exhibited good antibacterial activity against both Gm+ve and Gm−ve bacteria. The antibacterial activity of the compounds could not be correlated with their anticancer activity indicating a differential mechanism at their effective concentrations. The detailed study on the antibacterial mechanism of the most potent complex M7 revealed that it exerted its antibacterial activity by inhibiting the function of FtsZ and perturbing the localization of the Z-ring at the mid cell.  相似文献   

20.
In the present study, an endosulfan degrading strain Paenibacillus sp. ISTP10 was isolated from activated sludge. Soil microcosms were set up with endosulfan (60 mg kg−1 of dry soil) to evaluate the degradation potency of the strain. Soil samples from the microcosms were collected at regular intervals and the organic compounds were extracted with hexane. GC–MS analysis of the soil extract showed the formation of metabolites of endosulfan such as endosulfan diol and endosulfan ether confirming that the strain degrades endosulfan via a hydrolytic pathway. Methyl tetrazolium (MTT) assay for cytotoxicity and alkaline comet assay for genotoxicity were carried out in human hepato-carcinoma cell line HepG2 to evaluate the toxic potential of endosulfan and its degraded metabolites. The bacterium reduced toxicity as determined by an increase in LC50 value by 75.86 fold and a reduction in Olive Tail Moment by 21 fold after 30 days of treatment. The by-products of degradation were found to be less toxic than the parent compound showing the biodegradation and detoxification potential of endosulfan by Paenibacillus sp. ISTP10.  相似文献   

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