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1.
This work aimed to investigate, for the first time, the chemical composition, antioxidant, antiparasitic, cytotoxicity, and antimicrobial activities of the aromatic plant Limonium oleifolium Mill. essential oil (EO) and organic extracts. L. oleifolium aerial parts essential oil was analyzed by GC-FID and GC-MS, and 46 constituents representing 98.25±1.12 % of the oil were identified. γ-Muurolene (10.81±0.07 %), cis-caryophyllene (7.71±0.06 %), o-cymene (7.07±0.01 %) and α-copaene (5.02±0.05 %) were the essential oil main compounds. The antioxidant activity of L. oleifolium EO and organic extracts (MeOH, CHCl3, AcOEt, BuOH) was explored using 2,2-diphenyl-1-picrylhydrazyl (DPPH), ABTS, β-carotene/linoleic acid, cupric reducing antioxidant capacity (CUPRAC), and ferric reducing power assays. The results showed that L. oleifolium EO exhibit antioxidant capacity (IC50=17.40±1.32 μg/mL for DPPH assay, IC50=29.82±1.08 μg/mL for β-carotene assay, IC50=25.23±1.01 μg/mL for ABTS assay, IC50=9.11±0.08 μg/mL for CUPRAC assay and IC50=19.41±2.06 mg/mL for reducing power assay). Additionally, the EO showed significant activity against trophozoite form of Acanthamoeba castellanii (IC50=7.48±0.41 μg/mL) and promastigote form of Leishmania amazonensis (IC50=19.36±1.06 μg/mL) and low cytotoxicity on murine macrophages (LC50 90.23±1.09 μg/mL), as well as good antimicrobial activity against Staphylococcus aureus, Escherichia coli, Klebsiella oxytoca, and Pseudomonas aeruginosa. These results suggest that L. oleifolium essential oil is a valuable source of bioactive compounds presenting antioxidant, antiparasitic, and antimicrobial activities. Furthermore, it is considered nontoxic.  相似文献   

2.
The aim of the present study was to examine the antioxidant activity of three Veronica species (Plantaginaceae). The antioxidant potential of various extracts obtained from aerial flowering parts was evaluated by DPPH-free (1,1-diphenyl-2-picrylhydrazyl-free) radical scavenging activity and ferric-reducing antioxidant power assays. Considerable antioxidant activity was observed in the plant samples (FRAP values ranged from 0.97 to 4.85 mmol Fe2+/g, and DPPH IC50 values from 12.58 to 66.34 μg/ml); however, these levels were lower than the activity of the control compound butylated hydroxytoluene (BHT) (FRAP: 10.58 mmol Fe2+/g; DPPH IC50: 9.57 μg/ml). Also, the in vivo antioxidant effects were evaluated in several hepatic antioxidant systems in rats (activities of glutathione peroxidase, glutathione reductase, peroxidase, catalase, xanthine oxidase, glutathione content and level of thiobarbituric acid reactive substances) after treatment with different Veronica extracts, or in combination with carbon tetrachloride (CCl4). Pretreatment with 100 mg/kg b.w. of Veronica extracts inhibited CCl4-induced liver injury by decreasing TBA-RS level, increasing GSH content, and bringing the activities of CAT and Px to control levels. The present study suggests that the extracts analyzed could protect the liver cells from CCl4-induced liver damage by their antioxidative effect on hepatocytes.  相似文献   

3.
Cynoglossum creticum Mill (Boraginaceae) is used traditionally as a remedy to manage several human ailments. In this context, the present study aimed to perform multiple pharmacological investigations on the hydroalcoholic extracts prepared from Cynoglossum roots and aerial parts (leaves and flowers). We evaluated the antioxidant and enzyme inhibitory (against cholinesterases, α-glucosidase, α-amylase, lipase and tyrosinase) activity of the extracts. The protective effect(s) of the extracts on cardiomyocyte C2C12 and intestinal HCT116 cell lines challenged with hydrogen peroxide (H2O2) was studied. We found that the aerial parts harbored the highest amount of phenolic compounds. Generally, aerial parts showed significant antioxidant and enzyme inhibitory effects. Leaves exhibited the best lipase inhibitory activity (173.15 mgOE/g extract), followed by flowers and roots. The root and aerial extracts were equally able to blunt intracellular H2O2 induced reactive oxygen species production from both C2C12 and HCT116 cell lines. Both cells lines could be treated with scalar concentrations of root and flower extracts in the range 50–300?μg/mL without interferences on cell viability. In conclusion, the present study showed protective effects exerted by Cynoglossum extracts, which could serve as a foundation for the development of pharmaceuticals and nutraceuticals derived from Cynoglossum.  相似文献   

4.
The essential‐oil and fatty‐acid composition of the aerial parts of Ficaria kochii (Ledeb .) Iranshahr & Rech .f. native to Iran, and the antioxidant activity of various extracts of this plant were examined. The study by GC‐FID and GC/MS analysis of the essential oil resulted in the identification of 61 compounds, representing 86.01% of the total oil composition. Phytol (10.49%), farnesol (7.72%), methyl linoleate (5.57%), and α‐farnesene (4.96%) were the main components. The fatty‐acid composition of the aerial parts of F. kochii was also analyzed by GC/MS. The major components were palmitic acid (25.9%), linolenic acid (25.3%), and linoleic acid (17.5%). Polyunsaturated fatty acids (PUFAs) were found in higher amounts than saturated fatty acids. The possible antioxidant activity of various extracts (prepared by using solvents with different polarity) of the F. kochii aerial parts was evaluated by screening for their 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) radical‐scavenging activity, FeIII‐reducing power, total antioxidant activity, and inhibitory activity in the linoleic acid‐peroxidation system. H2O proved to be the most efficient solvent for the extraction of antioxidants, as the H2O extract contained the highest amount of phenolic compounds (2.78±0.23 GAE/g dry matter) and also exhibited the strongest antioxidant capacity in all the assays used. The results of the present investigation demonstrated that the aerial parts of F. kochii can be used as natural and safe nutrition supplement in place of synthetic ones.  相似文献   

5.
The antioxidant properties of methanol extracts of Lady’s Bedstraw (Galium verum L., Rubiaceae) herb from two different localities in Serbia were evaluated. Antioxidant activity was assessed in four different model systems. Free radical scavenging capacity (RSC) was examined by measuring the scavenging activity of extracts on 2,2-diphenyl-1-pycrylhydrazil (DPPH) and hydroxyl radical (OH), as well as on hydrogen peroxide. In addition, the protective effects of lipid peroxidation (LP) in corn oil were evaluated by the TBA-assay using the Fe2+/ascorbate system of induction. The amount of dried extract, the content of total phenolics, flavonoids and chlorophylls was also determined. Extracts from both locations expressed very strong scavenger activity, reducing the DPPH (IC50=3.10 μg/mland 8.04 μg/ml) and OH radical formation (IC50=0.05 μg/ml and 0.54 μg/ml) and neutralising H2O2 (IC50=4.98 μg/ml and 3.80 μg/ml), in a dose dependant manner. Also, examined extracts showed notable inhibition of LP (IC50=11.69 μg/ml and 19.47 μg/ml). The observed differences in antioxidant activity could be partially explained by the levels of phenolics (2.44–4.65 mg and 4.57–5.16 mg gallic acid equivalents/g dry extract), flavonoids (6.38–10.70 μg and 15.56–17.96 μg quercetin equivalents/g dry extract) and chlorophylls in the investigated Lady’s Bedstraw extracts.  相似文献   

6.
Gundelia species are known as “Kenger-kereng dikeni” in Anatolia, and their aerial parts are consumed as food. Also, roots and seeds (disseminules) of the Gundelia species are used to prepare gum and coffee. The chemical contents of ethanol and hexane extracts of disseminules of 17 Gundelia species, 13 of them are endemic, were studied using LC/MS/MS and GC/MS. Additionally, their antioxidant potential and enzyme inhibitory capacity against acetyl- and butyryl-cholinesterase, urease, and tyrosinase were determined. The unsaturated fatty acid ratios of Gundelia species were higher than their saturated fatty acid ratio. The highest sum of oleic and linoleic acid was detected in G. tournefortii var. tenuisecta (70.42 %). β-Sitosterol, α-amyrin, 3-acetyllupeol were identified in 17 Gundelia species by GC/MS, while chlorogenic acid and luteolin by LC/MS/MS as major compounds. The ethanol and hexane extracts of G. siirtica, G. rosea, and G. mesopotamica indicated good cholinesterase inhibitory activity. Among all species, ethanol extract of G. colemerikensis exhibited the best activity in ABTS (IC50: 32.30±0.98 μg/mL), DPPH (IC50: 59.91±0.89 μg/mL), and CUPRAC (A0.5: 57.41±1.03 μg/mL) assays. Ethanol extract of G. colemerikensis also displayed the highest inhibitory activity against butyrylcholinesterase (51.14±0.25 % at 200 μg/mL), urease (51.71±1.75 % at 200 μg/mL), and tyrosinase (39.50±0.85 % at 200 μg/mL) enzymes. According to the chemometric analysis of fatty acids, four groups were observed. Therefore, it is suggested that G. colemerikensis can be used in the pharmaceutical, food, and cosmetic industries due to its antioxidant and enzyme inhibition properties.  相似文献   

7.
Abstract

Cardiospermum halicacabum is widely used in traditional medicine. Previous studies have focused on the aerial parts, while the seeds have been poorly investigated. This work aimed to analyse the chemical composition of extracts from aerial parts and seeds obtained using Naviglio and Soxhlet (PN, PS, and SN, SS, respectively), the inhibitory properties against tyrosinase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) and the antioxidant effects. PN total extract showed significant anti-tyrosinase activity (IC50 value of 10.8?µg/mL). After partitioning with n-hexane, an HPLC method for analysing chemical constituents was established. Apigenin, luteolin, and apigenin-7-O-glucoside are the predominant constituents. SN n-hexane fraction was the most active inhibitor of BChE (IC50 of 57.9?µg/mL). Gas chromatography-mass spectrometry analysis revealed fatty acids, including eicosanoic acid, methyl 11-eicosenoate and oleic acid, as the major constituents. These findings suggest the potentiality of both seeds and aerial parts of C. halicacabum in the treatment of neurological disorders.  相似文献   

8.
The present study was aimed at determining total phenolic and flavonoid contents and studying the antioxidant activity of ginger (Zingiber officinale Rosc.) rhizome and callus, 6-gingerol and 6-shogaol and callus treated with elicitors. Petroleum ether (PE) and chloroform: methanol (1:1, v/v) (CM) extracts were prepared by maceration. Highest total phenolic content was obtained from the CM extract (60.34?±?0.43?mg gallic acid/g) of rhizome while callus showed lower content detected in the CM extract (33.6?±?0.07?mg gallic acid/g). Flavonoids were only detected in rhizome (CM extract 40.25?±?0.21?mg quercetin/g). Both rhizome extracts exhibited good antioxidant activity with higher activity recorded in PE extract (IC50 value 8.29?±?1.73?μg/mL). Callus extracts revealed lower antioxidant activity (IC50 value 1265.49?±?59.9?μg/mL obtained from CM extract). 6-gingerol and 6-shogaol displayed high antioxidant activity in both assays with IC50 4.85?+?0.58DPPH and 5.35?±?0.33ABTS μg/mL for the former and IC50 7.61?±?0.81DPPH and IC50 7.05?±?0.23ABTS μg/mL for the latter. Treatment of callus with elicitors showed significant (p?<?0.05) effects in enhancing phenolic content and related antioxidant activity. The highest significant increase in phenolic content (37% and 34%) and antioxidant activity in DPPH assay (34% and 30%) was observed in callus treated with 100?mg/L yeast extract and 50?mg/L salicylic acid respectively. Therefore, studying the effect of the elicitation of ginger cultured tissues in phenolic accumulation would be of immense importance for pharmacological, cosmetic and agronomic industries.  相似文献   

9.
Mimosa pudica L. (MP) is well-known plant in traditional medicinal system, especially in India. Unfortunately, leaves of MP are less explored. To determine the food and nutritional value of the neglected part of Mimosa pudica L. (MP), that is MP leaves, phytochemicals and metal ions of MP were quantified by newly developed HPLC and ICPOES-based methods. The content of phytochemicals observed using HPLC analysis for chlorogenic acid, catechin, and epicatechin was 141.823 (±8.171), 666.621 (±11.432), and 293.175 (±12.743) μg/g, respectively. Using GC/MS/MS analysis, fatty acid like oleic acid were identified. In ICP-OES analysis, a significant content of Na, K, Ca, Cu, Fe, Mg, Mn, and Zn was observed. The observed TPC and TFC for MP leaf extracts was 44.327 (±1.041) mg GAE/ g of wt. and 214.217 (±4.372) mg QCE/ g of wt., respectively. The DPPH assay depicted a strong antioxidant activity of MP leaf extracts with IC50 values of 0.796 (±0.081) mg/mL and a TEAC value of 0.0356 (±0.0003). A significant antacid activity (666 mg MP+400 mg CaCO3 >400 mg CaCO3 ≫666 mg Gelusil) of MP leaves was noticed. The methanolic extract of MP leaves demonstrated anti-microbial activity against Staphylococcus aureus (15±2mm), Pseudomonas aeruginosa (12±2mm) and Escherichia coli (10±2mm). In silico studies confirmed the in vitro results obtained for antioxidant, antiacid, and anti-microbial activities. In addition, in silico studies revealed the anti-cancerous and anti-inflammatory potential of the MP leaves. In summary, this study demonstrated the medicinal significance of MP leaves and the conversion of agro-waste or the under-utilized part of MP into pharmaceutical potent materials. Consequently, the present study highlighted that MP leaves alone have medicinal importance with good nutritional utility and possess large promise in the pharma industry along with improving bio-valorization and the environment.  相似文献   

10.
Geographic conditions (altitude, climate, and local flora) lead to significant differences in the chemical composition of propolis. Therefore, more research is needed for propolis in different geographical regions. So, the aim of this study was to evaluate the phenolic profile, total phenolic content, antioxidant, and antidiabetic properties of Pülümür propolis from Turkey. Methanol (MeOH), chloroform (CHCl3), and hexane extracts of propolis were analyzed. LC-ESI-MS/MS analysis of the extracts showed that the most abundant phenolic compound is caffeic acid in the MeOH extract (2943.12±11.12 μg phenolics/g extract), while on the other hand, CHCl3 extract had the highest total phenolic content (125.75±1.02 mg GAE/g extract). Antioxidant activity was measured using ABTS and DPPH assays, whereas CHCl3 extract (IC50=6.35±0.11 and 28.84±0.10 μg/mL, respectively) and MeOH extracts (IC50=5.04±0.07 and 28.80±0.09 μg/mL, respectively) showed relatively high antioxidant activity. The MeOH extract showed better antidiabetic activity than the standard compound, acarbose (IC50=0.544 and 0.805 mg/mL, respectively).  相似文献   

11.
This study was designed to define and compare the antioxidant and cytotoxic properties of polar extracts obtained from basal leaves (It-BL), cauline leaves (It-CL) and flowers (It-F) of Isatis tinctoria L. growing wild around Acireale (Sicily, Italy). The phenolic profile was characterized by HPLC-PDA-ESI-MS analysis and the correlation between phenolic content and the observed biological effects was established. Further, LC/MS analysis showed that the extracts contain glucosinolates at very low concentrations. The antioxidant activity of the extracts was tested in vitro; It-F was the most effective in the DPPH test (IC50 = 0.437 ± 0.003 mg/mL), whilst It-CL showed the best reducing power (1.546 ± 0.006 ASE/mL) and ferrous ions chelating activity (IC50 = 0.564 ± 0.011 mg/mL). The extracts exhibited anti-proliferative effects against three different human thyroid carcinoma cell lines, and It-BL displayed the strongest activity; particularly, it markedly inhibited the growth of CAL-62 cells, causing nearly 85% reduction of viability at the highest tested dose. No cytotoxicity against Artemia salina was observed. The results of our investigations indicate that the polar extracts obtained from I. tinctoria are a potential source of antioxidant and anticancer compounds, which could be suitable for nutraceutical and therapeutic applications.  相似文献   

12.
The chemical composition, antioxidant, cytotoxic, anticholinesterase and anti‐tyrosinase activities of the hydrodistilled essential oil of the aerial parts of Beta vulgaris subsp. maritime (L.) Arcang . from Tunisia have been evaluated. The chemical composition of the oil (yield 0.037% [w/w]), determined by GC‐FID and GC/MS is reported for the first time. Twenty five components, accounting for 98.1% of the total oil have been identified. The oil was characterized by a high proportion of oxygenated sesquiterpenes (39.2%), followed by sesquiterpene hydrocarbons (30.3%) and one apocarotenoids (26.3%). The main compounds were γ‐irone (26.3%), α‐cadinol (12.1%), T‐cadinol (10.6%), bicyclogermacrene (10.4%) and δ‐cadinene (6.0%). The isolated oil was tested for its antioxidant activity using the DPPH·, ABTS, catalase, and paraoxonase assays and also for its cytotoxic, anticholinesterase, and anti‐tyrosinase activities. The essential oil exhibited high antioxidant activity (IC50 = 0.055 ± 0.006 mg/ml) and important result oncatalase (524.447 ± 2.58 Units/mg protein). Furthermore, it exerted a significant cytotoxic effect against A549 cell line, with IC50 = 42.44 ± 1.40 μg/ml. The results indicate that the essential oil of Bvulgaris subsp. maritima (L.) Arcang . aerial parts may be used in future as an alternative to synthetic antioxidant agents, with potential application in the food and pharmaceutical industries.  相似文献   

13.
Ceropegia thwaitesii Hook (Asclepiadaceae), an endemic plant species, due to habitat destruction and over exploitation has a very restricted distribution in the Western Ghats of Tamil Nadu, India. The present wrok aimed to determine the chemical composition, the total phenolic (TPC), flavonoid (TFC) and tannin content (TEC), and to assess the antioxidant properties of various extracts of in vivo plants (IVP) and in vitro regenerated plants (IRP) of C. thwaitesii. Some phenolic compounds like gallic acid, cathechol, vanillin and salicylic acid were identified and quantified by HPLC. All the extracts possessed relevant radical scavenging activity on DPPH, Superoxide radical scavenging activity, and Nitric oxide radicals as well as total antioxidant ability. DPPH assay of in vitro methanol stems extracts and ethanol leaves extracts revealed the best antioxidant properties with important IC50 values of 0.248?±?0.45?µg/mL and 0.397?±?0.67?µg/mL, respectively, whereas in vivo chloroform stems extracts showed a lower antioxidant activity (IC50 of 10.99?±?0.24?µg/mL). The IRP methanol extracts of stem and leaves had good inhibitory activity against all tested microorganisms in a dose-dependent manner. These results suggested that in vitro raised plants of C. thwaitesii are an excellent source of antioxidant compounds to be exploited on an industrial level as food additive.  相似文献   

14.
Allium species are widely consumed as food all over the world. The phenolic profile of ethanol extracts of aerial parts and roots of 12 Allium species, collected from five different Eastern Anatolia regions, were studied using LC-MS/MS. In vitro antioxidant, anticholinesterase, cytotoxic and antimicrobial activities were also tested. The multivariate analyses were performed using principal component and hierarchical cluster analyses. Seventeen of 27 standard compounds were detected in all Allium species. The major components were mainly identified as quinic acid, malic acid, vanillin, and p-coumaric acid. The aerial parts possessed better antioxidant activity than roots. Aerial parts of A. atroviolaceum, A. chrysantherum, A. kharputense, and A. shirnakiense exhibited high cytotoxic activity against DLD-1 colon cancer cell lines (IC50 12.5 μg/mL). A. shatakiense and A. vineale demonstrated good antimicrobial activity against S. aureus and E. coli (MIC 75 μg/mL). According to chemometric analysis, differences were detected between aerial parts and the roots. The aerial parts of A. atroviolaceum, A. chrysantherum, A. kharputense, and A. shirnakiense could be potent in the pharmaceutical industry while A. shatakiense and A. vineale in the food industry after further investigations.  相似文献   

15.
Extracts of Malus hupehensis (Pamp.) Rehder, containing flavonoids with good antioxidant and antiliver injury properties, possess various biological activities. The aim of this study was to explore the antioxidant activity of these extracts in vitro and in vivo. The antioxidant activity of the extracts was studied using scavenging 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radicals, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals, and superoxide free radicals and by inhibiting mushroom tyrosinase activity in vitro. An in vivo antioxidant experiment was performed using a rat-aging model. Aging was induced in rats with D-galactose through treating them at doses of extracts about 150, 300, and 600 mg·kg−1·day−1. The Malus hupehensis extracts showed high antioxidant activity; the IC50 values of DPPH radicals, ABTS radicals, superoxide radicals, and mushroom tyrosinase inhibition were 19.00 μg/mL, 303.94 μg/mL, and 3.71 mg/mL, and 1.16 mg/mL, respectively. Our experiments showed that the extracts significantly increased the activity of antioxidant enzymes in the serum and tissue homogenate in vivo, and that the effects were positively correlated with the dose, compared with the activity observed in controls. Histopathological observation also confirmed that the extracts had protective effects after oxidative injury in rat tissues. In conclusion, the extracts of M. hupehensis showed effective antioxidant activity both in vitro and in vivo.  相似文献   

16.
From the aerial parts of Salsola oppositofolia, S. soda and S. tragus an alkaloid extract was obtained and tested to evaluate antioxidant and anti-cholinesterase activities. The in vitro study of the antioxidant activity by the DPPH method revealed a significant activity of Salsola alkaloid extracts with IC50 values ranging from 16.30 μg/mL for S. oppositifolia to 26.17 μg/mL for S. tragus. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities were evaluated. S. tragus alkaloid extract exerted the highest inhibitory activity against AChE (IC50 of 30.2 μg/mL) and BChE (IC50 of 26.5 μg/mL). Interestingly, S. soda and S. oppositifolia exhibited a selective inhibitory activity against BChE with IC50 values of 34.3 μg/mL and 32.7 μg/mL, respectively. Tetrahydroisoquinoline alkaloids were identified and quantified by GC/MS analysis.  相似文献   

17.
Abstract

The antioxidant potential of crude extracts and fractions from leaves of Ouratea parviflora, a Brazilian medicinal plant used for the treatment of inflammatory diseases, was investigated in vitro through the scavenging of radicals 2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH), hydroxyl radical (HO?), superoxide anion (O2??), and lipid peroxidation in rat liver homogenate. The crude extract (CEOP) and hydro-alcoholic fraction (OP4) showed strong inhibitory activity toward lipid peroxidation induced by tert-butyl peroxide (IC50 = 2.3 ± 0.2 and 1.9 ± 0.1 μg/ml, respectively). The same products exhibited a strong concentration-dependent inhibition of deoxyribose oxidation (14.9 ± 0.2 and 0.2 ± 0.1 μg/ml, respectively), and also showed a considerable antioxidant activity against O2??(87.3 ± 0.1 and 73.1 ± 0.4 μg/ml, respectively) and DPPH radicals (55.4 ± 0.3 and 38.3 ± 0.4 μg/ml, respectively). The protective effects of CEOP and OP4 were also studied in mouse liver. CCl4 significantly increased (by 90%) levels of lipid hydroperoxides, carbonyl protein content (64%), DNA damage index (133%), aspartate aminotransferase (261%), alanine aminotransferase (212%), catalase activity (23%), and also caused a decrease of 60% in GSH content. The results showed that CEOP and OP4 exerted cytoprotective effects against oxidative injury caused by CCl4 in rat liver, probably related to the antioxidant activity showed by the in vitro free radical scavenging property.  相似文献   

18.
In this study, a series of fluorine‐containing chiral hydrazide‐hydrazone derivatives [III‐XII] from ?‐cysteine ethyl ester hydrochloride was synthesized as new antioxidant and anticholinesterase agents. The antioxidant activity of these derivatives was evaluated by ABTS and DPPH· scavenging and CUPRAC assays and the anticholinesterase activity by the Ellman method spectrophotometrically. The results of the antioxidant assay showed that compounds V , IX , and X exhibited higher activity than BHT and α‐tocopherol used as positive standards. Among the synthesized derivatives, compound IX (IC50: 2.3 ± 1.6 μM) exhibited higher acetylcholinesterase inhibitory activity than galantamine (IC50: 4.5 ± 0.8 μM). Compounds XI (IC50: 9.6 ± 1.0 μM), IX (IC50: 12.5 ± 1.6 μM), III (IC50: 16.0 ± 1.6 μM), X (IC50: 17.2 ± 1.8 μM), VI (IC50: 20.2 ± 0.8 μM), XII (IC50: 21.5 ± 1.0 μM), and VII (IC50: 24.6 ± 0.6 μM) displayed better butyrylcholinesterase inhibitory activity than galantamine (IC50: 46.03 ± 0.14 μM). ADME‐Tox analysis was used to probe the drug‐like properties of the compounds. Molecular docking studies were also applied to understand the interactions between compounds and targets. The docking calculations were supported by the experimental data. In particular, compound IX , having better activity than galantamine against acetylcholinesterase and butyrylcholinesterase enzymes, was visualized using molecular docking.  相似文献   

19.
The chemical composition, antimicrobial and antioxidant activity of Eryngium palmatum, an endemic plant species from the Balkan Peninsula, were investigated. The flavonoids apigenin (9.5±0.3 mg g?1) and apigenin 7-O-glucoside (2.4±0.1 mg g?1) were determined in a methanol extract of aerial parts using HPLC analysis. The methanol extract of roots contained catechin (5.0±0.1 mg g?1), epicatechin (2.9±0.1 mg g?1), chlorogenic acid (1.6±0.0 mg g?1), gallic acid (0.9±0.0 mg g?1) and rosmarinic acid (0.9±0.2 mg g?1). GC-FID and GCMS analysis of a chloroform extract of aerial parts showed that the main volatile constituents were falcarinol, linoleic acid, hexadecanoic acid and methyl linoleate (comprising 32.6%; 24.4%; 19.9; 13.2% of the volatile fraction, respectively), while octanoic acid, tetradecanol and dodecanol dominated in the chloroform extract of the roots (34.9%; 25.8%; 22.2% of the volatile fraction, respectively). Investigation of antimicrobial activity by broth microdilution showed that the methanol and chloroform extracts of aerial parts and roots exerted a significant effect (MIC 3.5–15.6 μg mL?1) against tested Gram-positive and Gram-negative bacteria. The methanol extracts of aerial parts or roots exerted moderate ferric reducing antioxidant power, DPPH radical scavenging activity and hydroxyl radical scavenging activity.  相似文献   

20.
Malaria has continued to be a major global public health problem and a health concern in most of African countries. An estimated 350–500 million cases of malaria each year result in about one million deaths, mainly children under five. The rate of malaria infection is increasing rapidly partly due to drug resistance by the Plasmodium falciparum. The cost of the current drugs is prohibitive to the poor. There is therefore urgent need to identify new antimalarial agents that are effective, safe and affordable. In our continuous search for these new antimalarial compounds, extracts from five medicinal plants from the Maasai community in Kenya were tested against P. falciparum (D6; chloroquine sensitive and W2; chloroquine resistant strains). Of the tested total plant extracts, 5 crude extracts showed good antiplasmodial activity against D6 strain of P. falciparum with IC50 values lower or equal to 14.3 μg/ml, 2 were moderately active with IC50 values in between 26.6 and < 50 μg/ml. The petroleum ether extracts of the aerial parts and roots of Fuerstia africana demonstrated high antiplasmodial activity against the chloroquine sensitive antiplasmodial strain D6 (IC50 1.5 and 4.6 μg/ml, respectively with a selectivity index of 44 against vero cells). Manilkara discolor also exhibited promising antiplasmodial activity especially against D6 (IC50 11.5 and 26.6 μg/ml). In addition, ethyl acetate extract of the roots of Pentas lanceolata and the aerial parts of Sericocomopsis hildebrandtii demonstrated moderate antiplasmodial activity against D6 and W2 (IC50 14.3 and 16.51 μg/ml) respectively. F. africana therefore has high potential and can be pursued for the development of an antimalarial drug.  相似文献   

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