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1.
Centella asiatica, as known as Pegagan was previously reported to have anti-hyperglycemic effects in animal diabetic model rats. However, its α-glucosidase activity in vitro assay not yet reported. Our goal in this study is to isolate and identify active compounds as α-glucosidase inhibitor and antioxidant from aqueous ethanol 70% (v/v) extract of C. asiatica. The extract was partitioned by n-hexane, EtOAc, and n-butanol sequentially. Among the fractions tested, EtOAc fraction was showed the highest antioxidant and α-glucosidase inhibitory activities with an IC50 values of 45.42 and 73.17 μg/mL, respectively. The antioxidant activity was conducted by determination of DPPH radical scavenging activity, whereas α-glucosidase inhibitory activity was determined against yeast α-glucosidase. Furthermore, isolation of the ethyl acetate extract yielded two active compounds, which were identified as kaempferol (1) and quercetin (2). Both of the compounds showed good yeast α-glucosidase inhibitory activity with IC50 values of 16.50 and 21.61 μg/mL, respectively. In addition those compounds also could scavenge DPPH radical activity with IC50 values of 9.64 and 11.97 μg/mL, respectively. Due to its ability in reducing α-glucosidase activity and scavenging free radical activity, the C. asiatica appears to be a potential as a good resource for future development of antioxidant and antidiabetic drug.  相似文献   

2.
In this work the physicochemical characteristics including fatty acids, tocopherols and sterols composition of Ecballium elaterium (L.) A. Rich seed oil was determined. Results showed that linoleic acid (48.64%) and punicic acid (22.38%) were the major polyunsaturated fatty acids. Among the phytosterols, β-sitosterol was the most abundant (396.25 mg/100 g), while the major tocopherol form was γ-tocopherol (44.23 mg/100 g). In addition, we evaluated for the first time the effect of E. elaterium seed oil on the growth of human colonic adenocarcinoma (HT29) and fibrosarcoma (HT1080) cell lines. The original finding was its potent antiproliferative effect on both tumour cell lines. This effect was dose-dependent, with half-maximal inhibition values of IC50 = 4.86 μg/ml and 4.16 μg/ml respectively. This pilot study opens the way for further investigation about the potential use of E. elaterium as an anticancer agent.  相似文献   

3.
Cobalt oxide nanoparticles were successfully biosynthesized by complete green process using aqueous leaf extracts of Sageretia thea as chelating agent. Diverse techniques were applied for characterization. Antibacterial (with and without UV illumination), antileishmanial, antioxidant and enzyme inhibition applications were assessed, while freshly isolated macrophages and red blood cells were used for biocompatibility studies. Good antibacterial nature and enhancement of bactericidal nature upon UV modulation is reported. Staphylococcus aureus and Escherichia coli are indicated as most susceptible bacterial strains. Significant cytotoxic potential is revealed with IC50 calculated as 12.82 µg/ml and 3.16 µg/ml against the axenic leishmanial promastigote and amastigote cultures respectively. Biogenic cobalt oxide nanoparticles indicated DPPH free radical scavenging potential, while moderate antioxidant capacity and reducing power was demonstrated. Bioinspired cobalt oxide also demonstrated alpha amylase and protein kinase inhibition at higher concentrations. Biogenic cobalt oxide was found as more cytotoxic to macrophages (IC50 = 58.55 µg/ml) then to RBC’s (IC50 >200 µg/ml). Our results indicate green synthesis as an alternative, effective and eco-friendly method for the biosynthesis of cobalt oxide nanoparticles with numerous biological applications.  相似文献   

4.
Passion fruit (Passiflora leschenaultii DC), an endemic species to peninsular India, is traditionally used to treat various ailments such as dysentery, urinary stone disease and wounds. The present study aimed to investigate the antioxidant, analgesic, anti-inflammatory, antipyretic activities and chemical composition of leaf extracts of P. leschenaultii. Bioactive secondary metabolites such as total phenolics, tannins and flavonoids were quantified. Antioxidant activities were determined by DPPH, ABTS+, FRAP, metal chelating and phosphomolybdenum assays. Hot plate, acetic acid and formalin induced pain models were used to evaluate the analgesic activity. In order to study the acute and chronic anti-inflammatory activities, carrageenan and cotton pellet induced models were used in rats. Brewer’s yeast induced pyrexia method was applied for the antipyretic test. Functional compounds from the plant were identified and quantified through HPLC–DAD–MS analysis. The obtained results revealed that the acetone extract of leaves exhibited higher phenolic (440.24 mg GAE/g extract) and flavonoid (253.33 mg RE/g extract) contents and scavenged the DPPH (IC50 29.14 μg/mL), ABTS+ (10509.69 μM TEAC/g extract) effectively. On investigating the analgesic, anti-inflammatory and antipyretic activities, the acetone extracts of leaves, at a dose of 400 mg/kg (p.o.) reduced significantly (p < 0.001) the pain, inflammation and fever responses in vivo. Bioactive compounds such as hyperin, chlorogenic acid, rutin and caffeic acids were identified in the leaves of P. leschenaultii employing HPLC–DAD–MS analysis. These findings illustrate the excellent potential of this species as valuable source of natural phytochemicals with pharmacological properties.  相似文献   

5.
A novel ubiquinone derivative, pseudoalteromone A (1), possessing a 9C nor-monoterpenoid moiety was produced from a marine bacterium Pseudoalteromonas sp. CGH2XX. This bacterium is originally isolated from a cultured-type octocoral Lobophytum crassum. The structure of ubiquinone 1 was established by spectroscopic methods. Pseudoalteromone A (1) exhibited significant cytotoxicity toward the MOLT-4 (human acute lymphoblastic leukemia, IC50 = 3.764 μg/mL) cells and displayed a significant inhibitory effect (inhibition rate 45.1%) on the release of elastase by human neutrophils at a concentration of 10 μg/mL.  相似文献   

6.
Catharoseumine (1), a new monoterpenoid indole alkaloid possessing a unique peroxy bridge moiety, was isolated from the whole plants of Catharanthus roseus. Its structure was elucidated on the basis of NMR, IR, UV, and high-resolution mass spectrometric data, and its absolute configuration was determined by ECD and chemical methods. Catharoseumine (1) exhibited cytotoxicity against HL-60 cell line with IC50 value of 6.28 μM and potential inhibition against Plasmodium falciparum falcipain-2 (IC50 = 4.06 μM). A plausible biogenetic pathway of 1 was also proposed.  相似文献   

7.
Green and ecofriendly route for biosynthesis of lead oxide nanoparticles has been successfully demonstrated using aqueous leaf extracts of Sageretia thea (Osbeck.). Biosynthesized PbO (∼27 nm) nanoparticles were extensively characterized using XRD, FTIR, Raman, EDS etc. Morphology was studied through HR-TEM/SEM. As synthesized nanoparticles were investigated for their iv-vitro biological properties. Antibacterial activities revealed enhancement upon modulation by UV in a concentration dependent manner. Pseudomonas aeruginosa was found to be the most resistant strain (MIC = 250 µg/mL and MICuv = 31.25 µg/ml). MTT cytotoxicity on leishmania promastigotes and amastigotes revealed significant inhibition as indicated by their IC50 values of 14.7 µg/mL and 11.95 µg/m respectively. Cytotoxicity was also confirmed using brine shrimp lethality (IC50 = 27.7 µg/mL). Bio-compatibility evaluation indicated cytotoxicity to freshly isolated human macrophages (IC50 = 57.1 µg/mL). Insignificant alpha-amylase inhibition and moderate protein kinase inhibition was revealed. Antioxidant activities indicated free radical scavenging activity (58 ± 2.45) at 200 µg/mL. Moderate total reducing power and total antioxidant activity was also indicated. Overall, we conclude lead oxide as a potential candidate for biological applications, however further studies are recommended on their in vitro and in vivo cytotoxicity.  相似文献   

8.
In the present investigation, few 3-(substitutedphenyl)-1-[2-(1-hydroxy-ethyl)]-1H-benzimidazol-1-yl)prop-2-en-1-ones are EGFR antagonist are designed, by molecular docking analysis. The synthesized compounds were tested for their in vitro anticancer activity by propidium iodide fluorescent assay and Trypan blue viability assay against colorectal cancer cell lines (HCT116) and non-small cell lung cancer cell lines (H460). Human Epithelial Kidney cell lines (HEK) are used as normal cell lines for studying effect of drug on non-cancerous cells within human body. Evaluation of cytotoxic studies of synthesized compounds CHL(1–8) reveal that compound CHL1 [IC50 = 7.31 and 10.16 μM against HCT116 and H460 cell lines respectively, by PI assay] and CHL8 [IC50 = 12.52 and 6.83 against HCT116 and H460 μM cell lines respectively] possess promising cytotoxic activity.  相似文献   

9.
The complex tris(ethylenediamine)cobalt(III)chloride oxalate trihydrate [Co(en)3]Cl(C2O4)·3H2O crystallizes in the monoclinic space group C2/c with the following unit cell parameters a = 19.9318 (13), b = 9.3344 (4), c = 19.0881 (13) Å β = 96.846(3)°, Z = 8. The crystal structure was solved by direct methods and refined by full matrix least squares procedures to a final R value of 0.0314 for 4330 observed reflections. The reported cobalt complex is six co-ordinated through amine nitrogen with distorted octahedral geometry. There are uncoordinated chloride and oxalate ions along with the water molecules. In-vitro antimicrobial activity was studied against various test organisms and found to be good. From in-vitro cytotoxic activity of the synthesized complex, the IC50 value was found to be 55.85 μg/ml.  相似文献   

10.
Three Echeveria species from Sinaloa, Mexico (Echeveria craigiana, Echeveria kimnachii and Echeveria subrigida) were analyzed for their content of antioxidant compounds (β-carotene, ascorbic acid, α-tocopherol, total phenolics and flavonoids) and the in vitro antioxidant (DPPH, ABTS, ORAC and β-carotene bleaching [β-CBM]), α-glucosidase inhibitory and antibacterial activities. The studied Echeveria species showed high α-tocopherol content (2.9–9.0 mg/100 g f.w.) and total phenolics as Gallic Acid Equivalents (GAE) (152.2–400.5 mg GAE/100 g f.w.). Antioxidant activities of the three Echeveria methanol extracts (ME) were higher than those of other well-known plants with this property; the activities of E. craigiana (ABTS, 65.91 μmol ET/g f.w.) and E. subrigida (β-CBM, 79.3%) were remarkable. The Echeveria ME showed stronger α-glucosidase inhibition (IC50 25.21–50.57 μg/mL) than acarbose (IC50 3.59 mg/mL) as well as high antibacterial activity (Minimal Inhibitory Concentrations, MICs  1 mg/mL), mainly against Gram positive bacteria. The results showed the three Echeveria species had components/biological activities with high potential for food/pharmacological uses and could be exploited by sustainable management schemes.  相似文献   

11.
There is an urgent need for novel therapeutics possessing new modes of action to treat tuberculosis (TB) infections. In this study we report on the synthesis and biological evaluation of a series of pyrido[2,3,4-kl]acridin-6-one alkaloids related to the anti-TB (MIC 0.35 μM) but cytotoxic (IC50 <0.14 μM) marine natural product ascididemin (1). The most interesting compounds identified were 21 and 24, which were found to inhibit the growth of Mycobacterium tuberculosis (Mtb) H37Rv with MIC 2.0 μM, but with negligible cytotoxicity towards Vero and P388 cells (IC50>25 μM). Another analogue (10) was evaluated against a range of singly-drug-resistant strains of Mtb and was found to exhibit no cross-resistance. These results suggest that the pyrido[2,3,4-kl]acridin-6-one skeleton may provide a useful scaffold for future studies directed towards possible anti-TB drugs.  相似文献   

12.
Ruellia prostrata Poir. has been used historically as an anti-cancer, wound healing agent and to treat gonorrhea. We aimed to determine the phytochemicals present in ethyl acetate extract of R. prostrata Poir. (EAERP). We sought to determine the antioxidant, anti-inflammatory, and antibacterial activities in vitro, and toxicity properties in vivo. We also analyzed the Prediction of Activity Spectra for Substances (PASS), physicochemical, ADMET, and drug-likeness properties of phytochemicals in EAERP. To determine phytoconstituents, preliminary phytochemical screening and GC–MS were performed, while FT-IR was used to identify functional groups. The antioxidant activity was evaluated using a DPPH scavenging assay, whereas BSA denaturation and RBC hemolysis inhibition were used to assess anti-inflammatory activity. An agar-well-diffusion assay was performed to estimate the antibacterial activity. Brine shrimp lethality bioassay and oral delivery of EAERP of single-dose were performed to determine cytotoxicity and acute toxicity, respectively. The phytochemical screening revealed the presence of phenols, triterpenoids, saponins, steroids, amino acids, and fat and fixed oils. FT-IR analysis of EAERP showed the presence of many functional groups: alcohols/phenols, carboxylic acids, aldehydes, alkanes, esters, amines, amides, aromatic hydrocarbons, sulfoxides, and alkyl halides. GC–MS revealed the presence of 39 phytoconstituents including steroids, consistent with compounds and functional groups found in preliminary screening and FT-IR. EAERP showed dose-dependent antioxidant activity with an IC50 value of 21.402 µg/mL and anti-inflammatory activity with an IC50 value of 20.564 µg/mL in RBC hemolysis inhibition and 21.115 µg/mL in BSA denaturation assays. EAERP also exhibited dose-related antibacterial activity. EAERP exerted cytotoxicity with an LC50 value of 17.619 μg/mL and acute toxicity with an LD50 value of 4095.328 mg/kg without any adverse effects. The PASS server also predicted that the phytoconstituents of EAERP have antioxidant, anti-inflammatory, and antibacterial activities with probable activity (Pa) ranging from 0.310 to 0.717. Analysis of physicochemical, ADMET, and drug-likeness properties revealed the drug-able efficacy and safety of most compounds. The findings of this study indicated that R. prostrata Poir. contains phytoconstituents with potent antioxidant, anti-inflammatory, and antibacterial activities. Taken together, our measurements suggest that R. prostrata Poir. is a prime candidate for further exploration as a potential therapeutic agent.  相似文献   

13.
The effect of gamma irradiation on the content of total phenolic compounds, especially quercetin (Q), in onion (Allium cepa L.) skin was investigated. Onion skin extracts contained two predominant flavonoid compounds, Q and quercetin-4′-glucoside (Q4′G). After 10 kGy gamma irradiation, the yield of Q in the extracts increased significantly from 36.8 to 153.9 μg/ml of the extract, and the Q4′G content decreased slightly from 165.0 to 134.1 μg/ml. In addition, the total phenolic compound content also increased after irradiation at 10 kGy, from 228.0 μg/g of fresh weight to 346.6 μg/g; negligible changes (237.1–256.7 μg/g) occurred at doses of up to 5 kGy. As we expected, radical-scavenging activity was enhanced remarkably (by 88.8%) in the 10 kGy irradiated sample. A dose-dependent increase in the peak intensity of the electron paramagnetic resonance (EPR) spectra was observed in all irradiated samples, with a maximum increase at 10 kGy. The intensity relative to that of the control was 0.15, and it increased to 1.10 in 10 kGy irradiated samples. The optimum gamma irradiation dose, which is sufficient to break the chemical or physical bonds and release soluble phenols of low molecular weight in onion skin, is about 10 kGy.  相似文献   

14.
Acridine and its derivatives, well known as DNA intercalates lead to cell cycle arrest and apoptosis. 9-Aminoacridine derivatives were synthesized, characterized and evaluated against lung cancer (A-549) cell line and cervical cancer (HeLa) cell line by MTT assay. Compound 9 exhibited potent anticancer activity with CTC50 (13.75 & 18.75 μg/ml) for cervical cancer cell (HeLa) line and lung cancer cell (A-549) line respectively. In vitro short term cytotoxicity evaluation of compound 9 was carried out by Dalton’s Lymphoma Ascites (DLA) with percentage growth inhibition CTC50 (337.5 μg/ml). Compound 7 also exhibited good anticancer activity with CTC50 (31.25 & 36.25 μg/ml) for cervical cancer cell (HeLa) line and lung cancer cell (A-549) line respectively. Further in vivo study of newly synthesized 9-aminoacridine derivative can give a ray of light in the field of anticancer drugs.  相似文献   

15.
A series of diazenyl schiff bases have been synthesized by reaction of salicylaldehyde containing azo dyes with various substituted aniline derivatives in the presence of acetic acid as catalyst. The structures of diazenyl derivatives were determined by FTIR, UV–vis, 1H NMR, 13C NMR, CHN analysis, fluorimetric and mass spectroscopic studies. The synthesized derivatives were screened for their in vitro antimicrobial activity against various Gram-positive (S. aureus, B. subtilis, B. cereus), Gram-negative (S. typhi, S. enterica, E. coli, P. aeruginosa) bacterial and fungal (C. albicans, A. niger and A. fumigatus) strains, using cefadroxil (antibacterial) and fluconazole (antifungal) as standard drugs. The diazenyl schiff bases were also screened for their cytotoxicity against human colorectal carcinoma cell line (HCT-116) using 5-fluorouracil as standard drug by Sulforhodamine-B Stain (SRB) assay. The schiff bases exhibited significant activity toward both Gram-positive, Gram-negative bacterial and fungal strains. Most of the synthesized derivatives showed high activity against S. enterica. 4-((2,5-Dichlorophenyl)diazenyl)-2-((3-bromophenylimino)methyl)phenol (SBN-40) was found to be very active against S. aureus, B. cereus and E. coli, with MIC = 0.69 (µM/ml × 102). The compound 4-((2-bromophenyl)diazenyl)-2-((4-nitrophenylimino)methyl)phenol (SBN-13) possessed comparable activity (IC50 = 7.5 µg/ml) to the standard drug 5-fluorouracil (IC50 = 3.0 µg/ml) against human colorectal carcinoma cell line (HCT-116).  相似文献   

16.
The effects of ethanolic extracts of Mulberry Leaves (Morus alba L.) on nitric oxide (NO) serum level in rat and diameter of blood vessels in rabbit ear were investigated. NO level of ethanolic extract of mulberry leaves at dose of 100 mg/kg bw rats gave significant difference compared to negative control (P<0,05) at minute 30 after extract administration (4,51 ± 4,31 μM). Ethanolic extract of mulberry leaves at dose of 200 mg/kg bw had no significant difference in NO serum level. However, ethanolic extract of mulberry leaves at dose of 400 mg/kg bw rats increased NO serum level significantly compared to negative control (P<0,05) at minute 0, 10, 30, 60, and 90 after extract administration. The maximum serum level of NO of 400 mg/kg bw mulberry extract was 4,62 ± 3,05 μM, and it is the highest among other groups. Therefore this dose was choosen for vasodilatation assay in rabbit. Observation on blood vessels diameter in rabbit ears showed that ethanolic extract of mulberry leaves were able to dilatate the big vessels and small vessels of rabbit ears significantly compared to negative control (P<0,05) at minute 60 after extract administration. In conclusion, ethanolic extract of mulberry leaves at dose of 400 mg/kg bw rats or 202.67 mg/kg bw rabbits has a vasodilator effect, probably due to an increase of NO serum level.  相似文献   

17.
HCOOH, CH3COOH, and CH3CH2OH were used as chemical modifiers in a solution-cathode glow discharge. Emission was measured directly from the discharge, without a gas–liquid separator or a secondary excitation source. Emission from Ag, Se, Pb, and Hg was strongly enhanced, and the detection limits (DL) for these elements were improved by up to an order of magnitude using a combination of HCOOH and HNO3 compared to using HNO3 alone. The DL was measured for Mg (1 μg/L), Fe (10 μg/L), Ni (6 μg/L), Cu (6 μg/L), Pb (1 μg/L), Ag (0.1 μg/L), Se (300 μg/L), and Hg (2 μg/L). Coefficients of determination (R2) were between 0.9986 and 0.9999. A voltage of 1 kV was used, which produced a current of approximately 70 mA.  相似文献   

18.
Previous study showed that kaffir lime leaf contains alkaloid, flavonoid, terpenoid, tannin and saponin. The objective of this study was to examine the cytotoxic effect of kaffir lime leaf extract on cervical cancer and neuroblastoma cell lines. The method used for this research to determine cell viability was an 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results showed that an ethyl acetate extract had an IC50 for HeLa cells, UKF-NB3, IMR-5 and SK-N-AS parental cells of 40.7 μg · mL–1, 28.4 μg · mL–1, 14.1 μg · mL–1, and 25.2 μg · mL–1 respectively. Furthermore, the IC50 of chloroform extracts for HeLa cells, UKF-NB3, IMR-5 and SK-N-AS parental were 17.6 μg · mL–1, 18.9 μg · mL–1, 6.4 μg · mL–1, and 9.4 μg · mL–1 respectively. These data showed that kaffir lime extract reduces the viability of cervical and neuroblastoma cell lines and may have potential as anti-cancer compounds.  相似文献   

19.
The possible toxicological effects and in vitro antioxidant activity of the ethanolic extracts of Crocus sativus and Propolis were investigated. Both extracts did not cause any mortalities or signs of toxicity in mice when administered orally at doses up to 5 g/kg b.wt. In the sub-chronic study; the tested extracts did not produce any significant change in liver and kidney functions of rats, following oral administration for 8 successive weeks at doses of 500 mg/kg b.wt. of each. Propolis showed remarkable in vitro antioxidant activity at concentrations of (40–100 mg/ml). In contrast, the ethanolic extract of C. sativus ethanolic extract showed weak antioxidant activity in concentrations of (1–10 mg/ml) while at concentrations of (20–100 mg/ml) failed to exhibit any antioxidant activity. It was concluded that: both extracts were non-toxic, as they did not cause any mortalities or signs of toxicity in mice when administered orally at doses up to 5 g/kg b.wt. Daily oral administration of C. sativus, Propolis ethanolic extracts alone or in combination for 8 successive weeks to rats was quiet safe and didn't cause any toxic changes in liver and kidney. Antioxidant study showed that Propolis ethanolic extract was a more potent antioxidant than C. sativus extract.  相似文献   

20.
《Comptes Rendus Chimie》2008,11(3):324-330
The chemical composition of essential oil isolated from the flowerheads of Chrysanthemum trifurcatum (Desf.) Batt. and Trab. var. macrocephalum (viv.) Beg. (Asteraceae) by hydrodistillation was analysed by GC and GC/MS. A total of 56 compounds representing 97.48% of the oil were identified: limonene (20.89%), γ-terpinene (19.13%), 1,8-cineole (10.64%), β-pinene (8.77%), α-pinene (5.32%), 2-hexenal (4.85%), 4-terpenyl acetate (3.42%), β-myrcene (2.31%), germacrene-B (2.01%), β-spathulenol (1.62%), longifolene (1.39%), α-cadinol (1.39%), α-thujene (1.23%) and β-bourbobene (1.06%) were found to be the major components. Essential oil of flowerheads of C. trifurcatum was tested for antibacterial activity against eight strains, using a microdilution method, and for cytotoxicity and antiviral activity against Herpes simplex virus type 1 using a neutral red incorporation method. The oil showed a great potential of antibacterial effect against Staphylococcus epidermidis and Bacillus subtilis, in the inhibition range of 64–66% and IC50 ranging from 62.5 to 125 μg/ml. On Vero cells, the CC50 of the oil was 735.9 μg/ml and it did not exhibit a significant antiviral activity.  相似文献   

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