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1.
Present research was planned to assess the in vitro and in vivo anti-arthritic potential of Caralluma tuberculata N. E. Brown. methanolic (CTME) and aqueous (CTAQ) extracts. Chemical characterization was done by high-performance liquid chromatography and gas chromatography–mass spectrometry analysis. The Complete Freund’s Adjuvant (CFA) was injected in left hind paw of rat at day 1 and dosing at 150, 300 and 600 mg/kg was started on the 8th day via oral gavage in all groups except normal and disease control rats (which were given distilled water), whereas methotrexate (intraperitoneal; 1 mg/kg/mL) was administered to standard control. The CTME and CTAQ exerted significant (p < 0.01–0.0001) in vitro anti-arthritic action. Both extracts notably reduced paw edema, and restored weight loss, immune organs weight, arthritic score, RBCs, ESR, platelet count, rheumatoid factor (RF), C-reactive protein, and WBCs in treated rats. The plant extracts showed significant (p < 0.05–0.0001) downregulation of tumor necrosis factor-α, Interleukin-6, -1β, NF-κB, and cyclooxygenase-2, while notably upregulated IL-4, IL-10, I-κBα in contrast to disease control rats. The plant extracts noticeably (p < 0.001–0.0001) restored the superoxide dismutase and catalase activities and MDA levels in treated rats. Both extracts exhibited significant anti-arthritic potential. The promising potential was exhibited by both extracts probably due to phenolic, and flavonoids compounds.  相似文献   

2.
In this paper we report the antimicrobial, antiradical and urease inhibitory potential along with photochemical investigation of the crude extracts of Cyphostemma digitatum Lam. Phytochemical screening of both the crude (hot/cold) alcoholic and aqueous extracts of C. digitatum showed the presence of alkaloids, flavonoids, saponins, coumarins, steroids, terpenoids and tannins. The crude methanolic extract (hot/cold) exhibited good antioxidant activity, while the aqueous extract was a weak antioxidant. The crude methanolic extract was found to be more active against Bacillus subtilis, while both the extracts showed moderate antifungal potential, the methanolic crude extract showed good urease inhibitory activity compared with the aqueous crude extract.  相似文献   

3.
The chemical composition of the hydroethanolic extracts (60% v/v) from the aerial parts of Thymus marschallianus Willd (TM) and Thymus seravschanicus Klokov (TS) from Southern Kazakhstan flora was analyzed together with their hexane fractions. Determination of antibacterial, antifungal and antioxidant activities of both extracts was also performed. RP-HPLC/PDA and HPLC/ESI-QTOF-MS showed that there were some differences between the composition of both extracts. The most characteristic components of TM were rosmarinic acid, protocatechuic acid, luteolin 7-O-glucoside, and apigenin 7-O-glucuronide, while protocatechuic acid, luteolin 7-O-glucoside, luteolin 7-O-glucuronide, and eriodictyol predominated in TS. The content of polyplenols was higher in TS than in TM. The GC-MS analysis of the volatile fraction of both examined extracts revealed the presence of thymol and carvacrol. Additionally, sesquiterpenoids, fatty acids, and their ethyl esters were found in TM, and fatty acid methyl esters in TS. The antioxidant activity of both extracts was similar. The antibacterial activity of TS extract was somewhat higher than TM, while antifungal activity was the same. TS extract was the most active against Helicobacter pylori ATCC 43504 with MIC (minimal inhibitory concentration) = 0.625 mg/mL, exerting a bactericidal effect. The obtained data provide novel information about the phytochemistry of both thyme species and suggest new potential application of TS as a source of bioactive compounds, especially with anti-H. pylori activity.  相似文献   

4.
The present study was designed to evaluate polarity-dependent extraction efficiency and pharmacological profiling of Polygonum glabrum Willd. Crude extracts of leaves, roots, stems, and seeds, prepared from solvents of varying polarities, were subjected to phytochemical, antioxidant, antibacterial, antifungal, antidiabetic, and cytotoxicity assays. Maximum extraction yield (20.0% w/w) was observed in the case of an acetone:methanol (AC:M) root extract. Distilled water:methanol (W:M) leaves extract showed maximum phenolic contents. Maximum flavonoid content and free radical scavenging potential were found in methanolic (M) seed extract. HPLC-DAD quantification displayed the manifestation of substantial quantities of quercetin, rutin, gallic acid, quercetin, catechin, and kaempferol in various extracts. The highest ascorbic acid equivalent total antioxidant capacity and reducing power potential was found in distilled water roots and W:M leaf extracts, respectively. Chloroform (C) seeds extract produced a maximum zone of inhibition against Salmonella typhimurium. Promising protein kinase inhibition and antifungal activity against Mucor sp. were demonstrated by C leaf extract. AC:M leaves extract exhibited significant cytotoxic capability against brine shrimp larvae and α-amylase inhibition. Present results suggest that the nature of pharmacological responses depends upon the polarity of extraction solvents and parts of the plant used. P. glabrum can be considered as a potential candidate for the isolation of bioactive compounds with profound therapeutic importance.  相似文献   

5.
Ipomoea carnea Jacq. is an important folklore medicinal plant, assessed for its underexplored biological potential. Antioxidant, cytotoxic, antiproliferative and polyphenolic profile of whole plant was evaluated using various techniques. Maximum extract recovery (29% w/w), phenolic [13.54 ± 0.27 μg GAE/mg dry weight (DW)] and flavonoid (2.11 ± 0.10 μg QE /mg DW) content were recorded in methanol-distilled water (1:1) flower extract. HPLC-DAD analysis quantified substantial amount of six different polyphenols ranging from 0.081 to 37.95 μg/mg extract. Maximum total antioxidant and reducing potential were documented in methanol-distilled water and acetone-distilled water flower extracts (42.62 ± 0.47 and 24.38 ± 0.39 μg AAE/mg DW) respectively. Ethanol-chloroform root extract manifested highest free radical scavenging (IC50 of 61.22 μg/mL) while 94.64% of the extracts showed cytotoxicity against brine shrimps. Ethanol leaf extract exhibited remarkable activity against THP-1 cell line (IC50 = 8 ± 0.05 μg/mL) and protein kinases (31 mm phenotype bald zone).  相似文献   

6.
Ziziphora species (Lamiaceae) have been used in traditional medicine as sedatives, antiseptics, carminatives, or expectorants. Despite their common applications in phytotherapy, there is still lack of evidence about the composition of their extracts and its impact on biological properties of the plants. The aim of this study was to evaluate the content of Ziziphora bungeana, a less studied species growing in Kazakhstan, using HPLC-ESI-QTOF-MS/MS instrumentation and to determine its antimicrobial, antioxidant, and cytotoxic activity together with inhibitory properties against tyrosinase and toxicity in erythrocyte lysis assay. Extracts from Z. bungeana were found to be sources of flavonoids, phenolic acids, organic acids, and terpenes that determined their antiradical activity. The minimum inhibitory concentrations of extracts were lower for Gram-positive bacteria (1.25–10 mg/mL) than for Gram-negative bacteria and fungi (5–20 mg/mL). The EC50 value calculated for antiradical activity ranged between 15.00 ± 1.06 µg/mL and 13.21 ± 3.24 µg/mL for ABTS and DPPH assays, respectively. Z. bungeana extracts were found to decrease the activity of tyrosinase by 50% (at 200 µg/mL) similarly to kojic acid and were slightly cytotoxic for human melanoma A375 cell line (at 200 µg/mL) with no effect on HaCaT keratinocytes. In the end, Z. bungeana did not reveal toxic effects in hemolytic assay as compared to the positive control Triton X-100. The performed tests show potential application of the plant in the treatment of infectious diseases, disorders caused by free radicals, and skin problems.  相似文献   

7.
Acacia ehrenbergiana (Hayne), also known as Salam, is a highly drought resistant shrub distributed in North and East Africa, and the Arabian Peninsula. The plant is gathered for its gum and fiber, and is an important legume species for indigenous populations. In this study, the phytochemical analysis, antibacterial, and antioxidant properties of various alcoholic and aqueous extracts of Acacia ehrenbergiana grown in Qatar were investigated. The qualitative phytochemical screening of this species exhibited the presence of glycosides, tannins, flavonoids, terpenoids, saponins, phenol, and anthraquinones in various extracts. The agar diffusion method was performed to check the antibacterial activity. The acetone and ethanol extracts showed 85% antibacterial activity of the control against Gram-negative E. coli, while the acetone extract had 65% activity against the Bacillus Gram-positive species. The highest activity against Staphylococcus aureus was 65% for the butanol extract. The antioxidant capacities were evaluated by the DPPH method. Various extracts exhibited antioxidant activities similar to or higher than standard antioxidants, with the highest percent inhibition of 95% for the acetone and ethanol extracts. The acetone extracts were further purified by reverse phase combiflash chromatography followed by HPLC. Three of the pure compounds isolated were subjected to MS, FTIR, and NMR spectral analysis and were found to be stigmasterol, spinasterol, and theogallin. In conclusion, the observed antibacterial and antioxidant activities as well as the presence of secondary metabolites with potential medicinal activities makes Acacia ehrenbergiana a potent valuable endemic medicinal plant.  相似文献   

8.
The present study aims to evaluate phytochemical and pharmacological potentials of Dysphania ambrosioides (L.) Mosyakin & Clemants previously known as Chenopodium ambrosioides L. Extraction was carried out using 14 solvents with wide range of polarity to find out the best solvent system for each bioactivity. Total phenolic and flavonoids contents were measured colorimetrically and polyphenolics were quantified via HPLC-DAD analysis. The samples were screened for inhibitory potentials against free radicals, leishmania, cancer cell lines, protein kinase, α-Amylase enzymes and microbial strains. Among all solvents, maximum percentage of extract was recovered from methanol-water fraction of leaves. HPLC analysis exhibited the presence of rutin, myricetin and quercetin. In DPPH assay, methanolic leaf extract exhibited IC50 value of 130.7 ± 0.57 μg/mL. Considerable α-amylase inhibitory, cytotoxic, leishmanicidal and antimicrobial potentials were exhibited by plant samples. D. ambrosioides revealed significant antioxidant, cytotoxic, antimicrobial and anti-diabetic potentials and thus warrant further detailed studies to find novel drugs.  相似文献   

9.
Abstract

In this paper we report for the first time a method for the extraction of the protein fraction from Feijoa sellowiana Berg. fruit and its electrophoretic analysis. In addition we analyzed the protein fraction for its antioxidant activity and its effectiveness against different Gram-positive and Gram-negative bacteria both as American type culture collection (ATCC) standard and clinically isolated strains. Both antimicrobial and antioxidant activity resulted stronger respect to that previously obtained for the acetonic extract from the same fruit. Further, we study both activities also on the product of in vitro gastrointestinal digestion of F. sellowiana fruit proteins. The results showed that in vitro gastrointestinal digestion increased 10 fold the antioxidant activity, while the antimicrobial activity, tested only on ATCC strains, resulted from 2 to 4 fold increased. MTT assays showed the non-toxicity of these proteins both before and after digestion.  相似文献   

10.
Solid‐state NMR is a powerful tool for studying membrane proteins in a native‐like lipid environment. 3D magic angle spinning (MAS) NMR was employed to characterize the structure of E.coli diacylglycerol kinase (DAGK) reconstituted into its native E.coli lipid membranes. The secondary structure and topology of DAGK revealed by solid‐state NMR are different from those determined by solution‐state NMR and X‐ray crystallography. This study provides a good example for demonstrating the influence of membrane environments on the structure of membrane proteins.  相似文献   

11.
Adverse effects associated with synthetic drugs in diabetes therapy has prompted the search for novel natural lead compounds with little or no side effects. Effects of phenolic compounds from Carpobrotus edulis on carbohydrate-metabolizing enzymes through in vitro and in silico methods were assessed. Based on the half-maximal inhibitory concentrations (IC50), the phenolic extract of the plant had significant (p < 0.05) in vitro inhibitory effect on the specific activity of alpha-amylase (0.51 mg/mL), alpha-glucosidase (0.062 mg/mL) and aldose reductase (0.75 mg/mL), compared with the reference standards (0.55, 0.72 and 7.05 mg/mL, respectively). Molecular interactions established between the 11 phenolic compounds identifiable from the HPLC chromatogram of the extract and active site residues of the enzymes revealed higher binding affinity and more structural compactness with procyanidin (−69.834 ± 6.574 kcal/mol) and 1,3-dicaffeoxyl quinic acid (−42.630 ± 4.076 kcal/mol) as potential inhibitors of alpha-amylase and alpha-glucosidase, respectively, while isorhamnetin-3-O-rutinoside (−45.398 ± 4.568 kcal/mol) and luteolin-7-O-beta-d-glucoside (−45.102 ± 4.024 kcal/mol) for aldose reductase relative to respective reference standards. Put together, the findings are suggestive of the compounds as potential constituents of C. edulis phenolic extract responsible for the significant hypoglycemic effect in vitro; hence, they could be exploited in the development of novel therapeutic agents for type-2 diabetes and its retinopathy complication.  相似文献   

12.
The nature of E–E bonding in group 13 compounds X2E–EX2 (E = B, Al, Ga, In, Tl; X = H, F, Cl, Br, I) has been investigated by means of an energy decomposition analysis (EDA) at the BP86/TZ2P level of theory. The calculated equilibrium geometries of all molecules B2X4?Tl2X4 have a perpendicular (D2d) geometry. The largest energy barriers for rotation about the E‐E bond are predicted for the hydrogen species B2H4?Tl2H4. The EDA shows that the rotational barriers of B2X4?Tl2X4 may not be used for an estimate of the hyperconjugative strength in the D2d structures except for the tetrahydrides. The values for the planar (D2h) transition states reveals that π conjugation of the halogen lone‐pair electrons stabilizes the transition states. The bonding analysis shows that hyperconjugation in B2I4 is stronger than in B2H4 although the latter compound has a higher rotational barrier than the former. In B2F4, hyperconjugative stabilization of the perpendicular structure and conjugative stabilization of the planar structure nearly cancel each other yielding a nearly vanishing rotational barrier. The heavier analogues Al2X4?Tl2X4 have low rotational barriers and rather weak hyperconjugative interactions. The larger rotational barriers of the hydrogen systems Al2H4?Tl2H4 compared with the tetrahalogen compounds is explained with the cooperation of the relatively large hyperconjugation in the perpendicular form and the relatively weak conjugation in the planar transition structures. The EDA also indicates that the electrostatic (ΔEelstat) and molecular orbital (ΔEorb) components of the E–E bonding are similar in magnitude.Thecalculated B‐B bond dissociation energies of B2X4 (De = 93.0–108.4 kcal/mol) show that the bonds are rather strong. The heavier analogues Al2X4?Tl2X4 have weaker bonds (De = 16.6–61.7 kcal/mol). In general, the X2E‐EX2 bond dissociation energies follow the trend for atoms E: B ? Al > Ga > In > Tl and for atoms X: H > F > Cl > I.  相似文献   

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