Anticholinesterase,antioxidant, analgesic and anti-inflammatory activity assessment of Xeranthemum annuum L. and isolation of two cyanogenic compounds

Context: Xeranthemum annuum L. (Asteraceae) (XA) is an ornamental and medicinal species with limited bioactivity and phytochemical data.

Objective: Identification of anticholinesterase, antioxidant, anti-inflammatory and analgesic effects of the flower and root–stem (R-S) extracts of XA.

Materials and methods: Anticholinesterase (at 100?μg mL^?1) and antioxidant (at 1000?μg mL^?1) effects of various extracts were evaluated via microtiter assays, while anti-inflammatory and analgesic effects of the R-S extracts were tested using carrageenan-induced hind paw oedema (100 and 200?mg kg^?1) and p-benzoquinone (PBQ) writhing models (200?mg kg^?1) in male Swiss albino mice. The R-S ethanol extract of XA was subjected to isolation studies using conventional chromatographic methods.

Results: Most of the extracts showed inhibition over 85% against butyrylcholinesterase and no inhibition towards acetylcholinesterase. The flower chloroform and the R-S ethyl acetate extracts were most effective (97.85?±?0.94% and 96.89?±?1.09%, respectively). The R-S ethanol extract displayed a remarkable scavenging activity against DPPH (77.33?±?1.99%) and in FRAP assay, while the hexane extract of the R-S parts possessed the highest metal-chelating capacity (72.79?±?0.33%). The chloroform extract of the R-S caused a significant analgesic effect (24.4%) in PBQ writhing model. No anti-inflammatory effect was observed. Isolation of zierin and zierin xyloside, which were inactive in anticholinesterase assays, was achieved from the R-S ethanol extract.

Discussion and conclusion: This is the first report of anticholinesterase, antioxidant, analgesic and anti-inflammatory activities and isolation of zierin and zierin xyloside from XA. Therefore, XA seems to contain antioxidant and BChE-inhibiting compounds.     

Biological activities of ethyl acetate extract of different parts of Hyssopus angustifolius

Context: Hyssopus angustifolius M. Bieb. (Lamiaceae) is one of the most important medicinal plants in Iranian traditional medicine for the treatment of lung inflammation, laryngitis and cough relief. Much attention has been paid to this medicinal plant because of its traditional uses.

Objective: The present study examined the antioxidant and antihemolytic activities of ethyl acetate extract of stems, leaf and flowers of Hyssopus angustifolius.

Materials and methods: Antioxidant activity of extracts was evaluated by employing six different models, i.e., DPPH, nitric oxide and hydrogen peroxide scavenging, metal chelating and reducing power activities and hemoglobin-induced linoleic acid system. Also, antihemolytic activity was evaluated against hydrogen peroxide-induced hemolysis.

Results: Flowers extract showed the better activity than leaf and stems extracts in DPPH radical scavenging activity (IC₅₀ was 275.4?±?7.6 μg mL^?1). Leaf, stems and flowers extracts showed good nitric oxide scavenging activity (IC₅₀ were 376.6?±?11.4 µg mL^?1 for flowers, 297.6?±?9.6 μg mL^?1 µg mL^?1 for leaves and 837.8?±?19.2 µg mL^?1 for stems). The leaf extract exhibited better hydrogen peroxide scavenging and Fe²⁺ chelating activity than stems and flowers extracts. In hemoglobin-induced linoleic acid system, all of the extracts exhibited very good activity. Also, extracts show weak reducing power activity. The ethyl acetate extract of leaf showed better antihemolytic activity than the flower and stems (IC₅₀ was 94.0?±?2.4 μg mL^?1).

Discussion and conclusion: These findings give a scientific basis to the traditional usage of Hyssopus angustifolius, also showing its potential as rich sources of natural antioxidant compounds.     

Antioxidant,anticholinesterase and antibacterial activities of Stachys guyoniana and Mentha aquatica

Context: Stachys guyoniana Noë ex. Batt. and Mentha aquatica L. are two Algerian Lamiaceae used in folk medicine.

Objective: To investigate their antioxidant, anticholinesterase and antibacterial activities.

Material and methods: n-Butanol (BESG), ethyl acetate (EESG) and chloroform (CESG) extracts of S. guyoniana and methanol (MEMA) and chloroform (CEMA) aerial part extracts of M. aquatica and methanol (MERMA) and acetone (AERMA) roots extracts of M. aquatica were evaluated for their antioxidant activity by the β-carotene-linoleic acid, DPPH^? and ABTS^?+?scavenging, CUPRAC and metal chelating assays. The anticholinesterase activity was tested against AChE and BChE. The antibacterial activity was assessed by MICs determination against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Salmonella heidelberg, Klebsiella pneumoniae, Enterobacter aerogenes and Morganella morganii strains.

Results: In the β-carotene test, the CESG (IC₅₀: 2.3?±?1.27?μg/mL) exhibited the highest activity. The BESG was the best scavenger of DPPH^? (IC₅₀: 2.91?±?0.14?μg/mL). In the ABTS test, AERMA was the most active (IC₅₀: 4.21?±?0.28?μg/mL). However, with the CUPRAC, the BESG exhibited the best activity (A_0.50: 0.15?±?0.05?μg/mL) and was active in metal chelating assay with 48% inhibition at 100?μg/mL. The BESG was the best AChE inhibitor (IC₅₀: 5.78?±?0.01?μg/mL) however, the AERMA showed the highest BChE inhibitory activity (IC₅₀: 19.23?±?1.42?μg/mL). The tested extracts exhibited a good antibacterial activity.

Conclusion: This study demonstrated good antioxidant, anticholinesterase and antibacterial potential of S. guyoniana and M. aquatica, which fits in well with their use in folk medicine.     

Antioxidant and anti-cholinesterase activity of Sargassum wightii

Abstract

Context. Sargassum has been used in traditional Chinese medicine since the eighth century AD to treat goiter. Sargassum wightii Greville (Sargassaceae) is a major source of alginic acid used widely in food and drug industries.

Objective: To evaluate the anti-Alzheimer potential of S. wightii through evaluation of antioxidant and cholinesterase inhibitory activities.

Materials and methods: Successive extraction was done using solvents of varying polarity. Solvent extracts (100–500?µg/mL) were employed for all the antioxidant assays. Free radical scavenging activity was evaluated by 2,2-diphenyl-1-picrylhydrazyl, OH?, H₂O₂ radical scavenging assay. The reducing power of the seaweed was evaluated by ferric reducing antioxidant power and reducing power assay. Cholinesterase (ChE) inhibitory activity was evaluated and the Km, Vmax and Ki were calculated. Further, compound characterization was done by GC-MS analysis.

Results: The non-polar extracts were found to possess significant antioxidant activity. At 100?μg/mL, petroleum ether, hexane, benzene and dichloromethane extracts showed significant ChE inhibitory activity with IC₅₀ values of 19.33?±?0.56, 46.81?±?1.62, 27.24?±?0.90, 50.56?±?0.90?µg/mL, respectively, for AChE, and 17.91?±?0.65, 32.75?±?1.00, 12.98?±?0.31, 36.16?±?0.64?µg/mL, respectively, for BuChE. GC-MS reveals that 1,2-benzenedicarboxylic acid, diisooctyl ester is the major compound present in dichloromethane extract of S. wightii. The mode of inhibition exhibited by dichloromethane extract against the cholinesterases was found to be competitive type.

Discussion and conclusion: The presence of high amount of terpenoids could be the possible reason for its potential antioxidant and ChE inhibitory activity.     

Phytochemical analysis,antiproliferative and antioxidant activities of Chrozophora tinctoria: a natural dye plant

Context: Chrozophora tinctoria (L.) A. Juss. (Euphorbiaceae) is known as ‘dyer’s-croton’ and used to obtain dye substances. Recently, natural antioxidants and colorants have been of interest because of their safety and therapeutic effects.

Objective: This study investigates the antiproliferative and antioxidant activities of the various extracts and fractions from C. tinctoria and analyzes their phytochemical contents.

Materials and methods: The aerial parts of C. tinctoria were extracted with water, ethyl acetate, n-butanol, and methanol/chloroform. Phenolic compounds and other constituents of the extracts were analyzed by HPLC/TOF-MS. The ethyl acetate extract (EA) was fractionated by flash chromatography. The extracts, fractions, and major phenolic compounds were investigated for their antiproliferative activities on human cervical adenocarcinoma (HeLa) cell line at the concentrations of 5–100?μg/mL by using BrdU ELISA assay during 24?h of incubation. DPPH radical scavenging activities (5–150?μg/mL) and total phenolic contents of the samples were also evaluated.

Results: 4-Hydroxybenzoic acid (268.20?mg/kg), apigenin-7-glucoside (133.34?mg/kg), and gallic acid (68.92?mg/kg) were the major components of EA. CT/E-F6 (IC₅₀?=?64.59?±?0.01?μg/mL) exhibited the highest antiproliferative activity. CT/E-F2 (IC₅₀=?14.0?±?0.0?μg/mL) and some fractions displayed higher radical scavenging activity compared to synthetic antioxidant BHT (IC_50?=_?23.1?±?0.0?μg/mL). Among the main phenolics, gallic acid exhibited the highest antiproliferative and radical scavenging abilities (IC_50?<_?5?μg/mL).

Conclusion: In this study, we have determined the biologically active fractions and their high effects may be attributed to the presence of gallic acid.     

Chemical composition,antioxidant and antibacterial activities of two Spondias species from Northeastern Brazil

Context: The leaves of Spondias tuberosa Arr. Cam. (Anacardiaceae) and Spondias mombin L. have been traditionally used for medicinal purposes. Some studies reveal their antibacterial, antimicrobial, and antiviral properties.

Objective: Determine the chemical composition, antioxidant, and antimicrobial activities of Spondias species to justify its ethnopharmacological use.

Materials and methods: Spondias species extracts were prepared with methanol:water 80:20 and analyzed by silica gel column chromatography and reversed phase liquid chromatography (HPLC). The antioxidant activity was evaluated by scavenging the radicals 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) and 2,2-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS?+) and measuring antimicrobial activity (agar well diffusion method, minimum inhibitory concentration and minimum bactericidal concentrations).

Results: The HPLC analysis of Spondias extracts demonstrated the occurrence of high yield of flavonoids. Found in S. mombin were quercetin (2.36?±?0.01?mg/g) and ellagic acid (41.56?±?0.01?mg/g) and in S. tuberosa species rutin (53.38?±?1.71?mg/g), quercetin (24.46?±?0.87?mg/g), and ellagic acid (169.76?±?0.17?mg/g). The antibacterial activity of the extracts against the various bacteria strains varied from 8.8 to 20.1?mm. MIC values from 62.5 to 125 µg/mL were satisfactory when compared with other plant products. Medium DPPH scavenging activity IC₅₀ for Spondias extracts varied from 0.042 to 0.558?mg/mL and for ABTS from 0.089 to 0.465?mg/mL. DPPH scavenging activity for constituent ellagic acid IC₅₀?=?0.042?mg/mL and for quercetin IC₅₀?=?0.081?mg/mL.

Discussion and conclusion: The chemical study of Spondias leaf extracts showed the occurrence of quercetin, rutin and ellagic acid, substances with relevant antioxidant and antimicrobial activities.     

Bioactive compounds from endemic plants of Southwest Portugal: Inhibition of acetylcholinesterase and radical scavenging activities

Context: Natural products are reported to have substantial neuroprotective activity due to their radical scavenging capacity, and also acetylcholinesterase (AChE) inhibitory capacity, both activities important in neurodegeneration.

Objective: The undesirable side effects of compounds in pharmacological use make it important to identify natural neuroprotective molecules. This work assesses the potential of five endemic Portuguese plants as sources of neuroprotective compounds.

Materials and methods: Antioxidant capacity for peroxyl radical was determined by Oxygen Radical Absorbance Capacity method and for hydroxyl by Electron Paramagnetic Resonance, as well as AChE inhibitory capacity of the plant hydroethanolic extracts. The molecules responsible for these valuable properties were also tentatively identified by HPLC.

Results and discussion: Armeria rouyana and Thymus capitellatus presented some of the highest phenolic contents (76.60?±?7.19 and 12.82?±?0.24?mg GAE g^?1 dw, respectively) and antioxidant capacities (592?±?116 and 449?±?57 μmol TE g^?1 dw, respectively). The flavonoids were identified as the phytomolecules related to the antioxidant capacity of these plant extracts; in the case of A. rouyana, l-ascorbic acid also made an important contribution (3.27?±?0.26?mg g^?1 dw). Plant extracts clearly demonstrated effective AChE inhibitory activity (480?±?98 and 490?±?46 μg mL^?1, respectively), that could be associated to polyphenols.

Conclusions: The extracts of A. rouyana and T. capitellatus and their active components, especially polyphenols, demonstrate interesting neuroprotective potential. They, therefore, deserve further study as their phytomolecules are promising sources of either natural neuroprotective products and/or novel lead compounds.     

Antioxidant,anticholinesterase and tyrosinase inhibition activities,and fatty acids of Crocus mathewii – A forgotten endemic angiosperm of Turkey

Context We report the first ever chemical/biochemical study on Crocus mathewii Kerndorff (Iridaceae) – a Turkish endemic angiosperm. This plant has never been explored for its phytochemistry and bioactivities.

Objective This study explores C. mathewii corm and aerial parts for the chemical and biological properties of hexane, ethyl acetate, methanol and water fractions of the extracts.

Material and methods Plant material (20 g) was extracted by methanol (250?mL?×?5, 3 days each) and fractioned into hexane, ethyl acetate, methanol and water. All fractions were subjected to β-carotene–linoleic acid, DPPH^·, ABTS^·+, CUPRAC, metal chelating and tyrosinase inhibition activities. Hexane fractions were submitted to GC–MS analysis.

Results Ethyl acetate fractions showed excellent IC₅₀ values in DPPH^· (aerial 36.21?±?0.76 and corm 33.87?±?0.02?mg/L) and ABTS^·+ (aerial 33.01?±?0.79 and bulb 27.87?±?0.33?mg/L); higher than the IC₅₀ of the standard α-tocopherol (DPPH 116.25?±?1.97; ABTS 52.64?±?0.37?mg/L), higher than BHA in DPPH (57.31?±?0.25?mg/L), but slightly lower in ABTS (19.86?±?2.73?mg/L). Methanol extract of aerial parts also showed higher activity than α-tocopherol in DPPH (85.56?±?11.51?mg/L) but slightly less (72.90?±?3.66?mg/L) than both the standards in ABTS. Linoleic (aerial 53.9%, corm 43.9%) and palmitic (aerial 22.2%, corm 18%) were found as the major fatty acids.

Discussion and conclusion Some fractions of C. mathewii showed higher antioxidant activities than the standards. There is a need to explore more about this plant.     

In vitro anti-aging activities of Terminalia chebula gall extract

Context: The Thai Lanna region has its own folklores and wisdoms in various fields such as traditional medicines. The galls of Terminalia chebula Retz. (Combretaceae) frequently appear in many Thai Lanna medicinal plant recipes for promoting longevity.

Objectives: To investigate the in vitro anti-aging activities of the extracts from 15 plants including T. chebula gall selected from the Thai medicinal plant recipes that have been traditionally used for longevity.

Materials and methods: The plant extracts were prepared by four extraction methods including hot (HW) and cold (CW) aqueous processes and hot (HM) and cold (CM) methanol processes. These extracts were tested for antioxidative and tyrosinase inhibition activity as well as the proliferative and MMP-2 inhibition activity on early aging human skin fibroblasts in order to evaluate their in vitro anti-aging activity.

Results: At 0.1?mg/mL, the CW extract of T. chebula gall exhibited the highest DPPH radical scavenging activity with scavenging of 84.64%?±?2.22%, whereas ascorbic acid, α-tocopherol and butylated hydroxyl toluene gave 96.50%?±?0.1%, 35.74%?±?0.2% and 27.43%?±?0.1%, respectively. The CW extract of T. chebula gall indicated the highest stimulation index (SI) on normal human fibroblast proliferation of 1.441 which was more active than ascorbic acid (SI 1.21). This extract has also demonstrated MMP-2 inhibition on fibroblasts determined by zymography 1.37 times more potent than ascorbic acid.

Discussion and conclusion: This study has confirmed the traditional use of T. chebula gall in many Thai medicinal plant recipes for longevity which will be beneficial for further development of anti-aging products.     

Phytochemical screening and evaluation of in vitro antioxidant and antimicrobial activities of the indigenous medicinal plant Albizia odoratissima

Context: Albizia odoratissima (L. f.) Benth has been used in Indian folk medicine to treat numerous inflammatory pathologies, such as leprosy, ulcers, burns and asthma.

Objective: To evaluate the antioxidant and antimicrobial properties of A. odoratissima.

Materials and methods: Dried leaves of A. odoratissima were extracted in organic solvents (hexane, chloroform, ethyl acetate, and methanol). The total phenolic content (TPC) and total flavonoid content (TFC) were determined using the Folin-Ciocalteu and aluminum chloride colorimetric methods, respectively. The antioxidant activity was examined using 2,2-diphenyl-1-picrylhydrazyl (DPPH), hydrogen peroxide (H₂O₂), 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS), and ferric reducing antioxidant power (FRAP) assays. The antibacterial activity was examined using minimum inhibitory concentration (MIC) and the minimum bacterial concentration (MBC), determined by broth microdilution method against Gram-negative bacteria (Klebsiella pneumoniae, Escherichia coli, Pseudomonas aeruginosa, and Proteus vulgaris) and Gram-positive bacterium (Staphylococcus aureus).

Results: The TPC ranged from 4.40?±?1.06 to 1166.66?±?31.85?mg GAE/g of dry weight (DW), and the TFC ranged from 48.35?±?3.62 to 109.74?±?1.84?mg QE/g of DW. The IC₅₀ values of the ethyl acetate extract for DPPH, ABTS, and H₂O₂ were 10.96?±?0.40, 4.35?±?0.07, and 163.82?±?1.52?μg/mL, respectively. Both methanol and ethyl acetate extracts demonstrated effective antibacterial activity with MICs and MBCs values ranging 136–546?μg/mL and 273–1093?μg/mL, respectively, against the tested pathogenic species.

Conclusions: The leaves of A. odoratissima showed potent free radical scavenging property and antimicrobial activity.     

In vitro antioxidant and anti-cholinesterase activities of Rhizophora mucronata

Context: Rhizophora mucronata Lam. (Rhizophoraceae), commonly known as Asiatic mangrove, has been used traditionally among Asian countries as folk medicine.

Objective: This study investigates the cholinesterase inhibitory potential and antioxidant activities of R. mucronata.

Materials and method: Rhizophora mucronata leaves were successively extracted using solvents of varying polarity and a dosage of 100–500?µg/ml were used for each assay. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities were assessed according to the method of Ellman. In vitro antioxidant activity was assessed using free radical scavenging, reducing power, and metal-chelating activity (duration – 3 months). Total phenolic and flavonoid content were quantified spectrophotometrically. Compound characterization was done using column chromatography, NMR, FTIR, and LC-MS analysis.

Results: Methanolic leaf extract (500?µg/ml) exhibited the highest inhibitory activity against AChE (92.73?±?0.54%) and BuChE (98.98?±?0.17%), with an IC₅₀ value of 59.31?±?0.35 and 51.72?±?0.33?µg/ml, respectively. Among the different solvent extracts, methanolic extract exhibited the highest antioxidant activity with an IC₅₀ value of 47.39?±?0.43, 401.45?±?18.52, 80.23?±?0.70, and 316.47?±?3.56?µg/ml for DPPH, hydroxyl, nitric oxide radical, and hydrogen peroxide, respectively. Total polyphenolic and flavonoid contents in methanolic extract were observed to be 598.13?±?1.85?µg of gallic acid equivalent and 48.85?±?0.70?μg of rutin equivalent/mg of extract. Compound characterization illustrated (+)-catechin as the bioactive compound responsible for cholinesterase inhibitory and antioxidant activities.

Conclusion: The presence of rich source of flavonoids, in particular catechin, might be responsible for its cholinesterase inhibitory and antioxidant activities.     

Phytochemical analysis and antioxidant activity of Lycium barbarum (Goji) cultivated in Greece

Context: The fruit of Lycium barbarum L. (Solanaceae), known as goji berry, has been exploited for a long time in traditional Chinese medicine. In recent decades, it has received much attention as one of the trendiest functional foods with a wide array of pharmacological activities in Western diets.

Objective: In this study the phenolic profile and potential antioxidant capacity of Lycium barbarum cultivated in Crete (Greece) were investigated.

Materials and methods: The berries were defatted with hexane and then extracted with dichloromethane and methanol using a Soxhlet apparatus. Furthermore, the methanol extract was fractionated with ethyl acetate and butanol. All fractions/extracts were tested for their antioxidant activity (DPPH, FRAP, chemiluminescence). Folin–Ciocalteu and LC-DAD-MS analyses were utilized for the identification of the phenolic compounds.

Results: The total phenolic content ranged from 14.13?±?0.40 (water fraction) to 109.72?±?4.09 (ethyl acetate fraction) mg gallic acid equivalent/g dry extract. Ethyl acetate extract exhibited the highest scavenging activities determined as EC₅₀ (4.73?±?0.20?mg/mL) and IC₅₀ (0.47?±?0.001?mg/mL) using DPPH and chemiluminescence assays. Seventeen phenolic compounds, including cinnamoylquinic acids and derivatives, hydrocinnamic acids and flavonoid derivatives, were tentatively identified. To the best of our knowledge, quercetin 3-O-hexose coumaric ester and quercetin 3-O-hexose-O-hexose-O-rhamnose are reported for the first time in goji berry fruits.

Discussion and conclusion: The results of this study suggest that consumption of goji berry fruits could serve as a potential source of natural antioxidant compounds and that goji berry phenolic extracts could be exploited for nutritional pharmaceutical purposes.     

Effect of macronutrient deficiency on withanolides content in the roots of Withania somnifera and its correlationship with molybdenum content

Abstract

Context: The content of withanolides in the roots of Withania somnifera (L.) Dunal (Solanaceae) is important for therapeutic application. Earlier studies have shown that the deficiency of macro- and micronutrients affects the growth of W. somnifera. Therefore, we examined the effect of these deficiencies on the withanolides content of the roots.

Objective: To examine the effect of molybdenum accretion in nitrogen-, phosphorus-, calcium- and potassium-deficient soils on the accumulation of withanolides in the roots of W. somnifera. Different withanolides have different therapeutic applications hence major bioactive withanolides assume importance.

Materials and methods: Methanol extracts of the roots were subjected to HPTLC and individual withanolides were identified by comparing their R_f values with those of the authentic samples. Molybdenum was quantified by atomic absorption spectroscopy. Free radical scavenging activity was monitored by the 1,1-diphenyl-2-picryl-hydrazyl (DPPH) assay.

Results: Molybdenum content in roots of nitrogen-, phosphorus-, calcium-, potassium-deficient, and control plants were 7.02?±?2.1, 13.1?±?1.6, 17.1?±?0.9, 33.5?±?3.3, and 33.9?±?1.6?ppm, respectively. Levels of withaferine A increased with the increase in the Mo content in roots from 7.79?±?2.2?mg/g to 12.57?±?3.4?mg/g. Antioxidant activity of nitrogen-deficient plants was the lowest (24.7?±?2.2%) compared to other groups.

Discussion and conclusion: It was observed that nitrogen metabolism-dependent molybdenum uptake influences the withanolides accumulation in the roots.     

Antioxidant and anticholinesterase activities of five wild mushroom species with total bioactive contents

Abstract

Context: Recently, mushrooms are interesting natural products to be investigated due to exhibiting various bioactivities.

Objective: This study determines the antioxidant and anticholinesterase activities of various extracts of five wild mushroom species. In addition, the total bioactive contents, namely, ascorbic acid, β-carotene, and lycopene along with phenolic and flavonoid contents were also determined spectrophotometrically.

Materials and methods: Antioxidant activity was tested by using five complementary tests; namely, β-carotene-linoleic acid, DPPH^? scavenging, ABTS^?+ scavenging, cupric-reducing antioxidant capacity (CUPRAC), and metal chelating assays. The in vitro anticholinesterase activity was tested against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes using the Ellman method. The spectrophotometric methods were used to determine the total phenolic, flavonoid, ascorbic acid, β-carotene, and lycopene contents.

Results: The current study has shown that ethyl acetate extracts of Ganoderma lucidum (Curtis) P. Karst (IC₅₀: 1.55?±?0.05?µg/mL) and Funalia trogii (Berk.) Bondartsev & Singer (IC₅₀: 4.31?±?0.18?µg/mL) exhibited good lipid peroxidation inhibitory activity. The DPPH, ABTS, and CUPRAC assays supported this activity. The ethyl acetate and methanol extracts of Funalia trogii and Ganoderma lucidum indicated good anticholinesterase activity. Ganoderma lucidum had rich phenolic and flavonoid contents, indicating 98.67?±?0.32?mg PEs/g extract and 160.38?±?1.25?mg QEs/g extract, respectively.

Discussion and conclusion: The results demonstrate that some of the mushroom species tested herein could be used in food and pharmaceutical industries as natural antioxidants.     

Chemical profile and biological activities of Veronica thymoides subsp. pseudocinerea

Abstract

Context: In Turkey, Veronica species (Plantaginaceae) have been used as a diuretic and for wound healing in traditional medicine.

Objective: To examine the fatty acid and essential oil profiles, the antioxidant, anticholinesterase, antimicrobial, and DNA damage effects of Veronica thymoides P.H. Davis subsp. pseudocinerea M.A. Fischer as a potential source of natural active compounds.

Materials and methods: GC/MS was used to analyze essential oil and fatty acid obtained from whole plant. The antioxidant activity was evaluated by the β-carotene-linoleic acid test system, DPPH-free and ABTS cation radicals scavenging, and cupric reducing antioxidant capacity assays. The anticholinesterase and antimicrobial activities were determined by Ellman and broth macrodillution methods, respectively. The effect of the methanol extract on DNA cleavage was investigated.

Results: Hexatriacontene (21.0%) was found to be the main constituent in essential oil, and linoleic acid (25.2%) and palmitic acid (20.6%) in fatty acid. Methanol extract demonstrated the best IC₅₀ values in lipid peroxidation (49.81?±?0.31?µg/ml) and DPPH-free radical scavenging activity (15.32?±?0.17?µg/ml). Methanol and water extracts possessed strong ABTS cation radical scavenging activity with IC₅₀ values 9.15?±?0.28 and 8.90?±?0.14?µg/ml, respectively. The acetone extract exhibited moderate butyrylcholinesterase inhibitory activity. The highest antimicrobial activity was determined in methanol extract against Escherichia coli with 31.25?µg/ml MIC value. Inhibition of methanol extract on plasmid DNA cleavage by OH radicals was found to be 93.32% at 500?µg/ml.

Conclusion: The methanol extract having strong antioxidant and DNA damage effects could be investigated phytochemically to find natural active compounds.     

Anti-proliferative and matrix metalloproteinase-2 inhibition of Longkong (Lansium domesticum) extracts on human mouth epidermal carcinoma

Abstract

Context: Longkong [Lansium domesticum Corr. (Meliaceae)] is a popular tropical plant producing economic edible fruits found mainly in Southeast Asia. However, limited information is available concerning anticancer activity of Longkong.

Objective: To investigate anticancer activities in human mouth epidermal carcinoma (KB) of Longkong extracts.

Materials and methods: Various parts of Longkong which was collected from Northern and Eastern of Thailand were extracted by the hot and cold processes using water, chloroform, and methanol. The extracts were tested for anti-oxidative activities and anti-proliferation as well as matrix metalloproteinase inhibition on KB cells.

Results: The hot water extract of seeds from Northern region (NSEWH), the cold water extract of old leaves from Northern region (NOLWC), and the hot chloroform extract of young leaves from Eastern region (EYLCH) showed the highest free radical scavenging, metal ion chelating, and lipid peroxidation inhibition with SC₅₀, MC₅₀ and IPC₅₀ values of 0.34?±?0.03, 0.47?±?1.60 and 0.86?±?0.31?mg/ml, respectively. The hot and cold chloroform extract of young fruits from Northern region (NYFCH and NYFCC) exhibited anti-proliferation effect against KB cells with IC₅₀ values of 603.45?±?55.35 and 765.06?±?46.19?mg/ml, respectively. NYFCC exhibited the highest pro- and active MMP-2 inhibition at 53.03?±?2.65 and 31.30?±?0.43%, more than all tested standard anticancer drugs except cisplatin.

Discussion and conclusion: The cold chloroform extract of young fruits from Northern region appeared to contain anticancer active compounds against KB cells because of its high anti-proliferation and MMP-2 inhibition activities.     

Antioxidant activity of phenolic extracts from different cultivars of Italian onion (Allium cepa) and relative human immune cell proliferative induction

Context: The total antioxidant activity (TAC) may vary considerably between onion cultivars. Immunological effects of onion phenolic compounds are still underestimated.

Objective: The objective of this study is to determine the total phenol content (TPC) and the relative TAC of three Allium cepa L. (Liliaceae) onion cultivars cultivated in Cannara (Italy): Rossa di Toscana, Borettana di Rovato, and Dorata di Parma, and to evaluate the phenol extracts ability to induce human immune cell proliferation.

Materials and methods: TPC was determined by the Folin–Ciocalteu method, TAC with FRAP, TEAC/ABTS, and DPPH methods. Peripheral blood mononuclear cells from healthy human donors were incubated for 24?h at 37?°C with 1?ng/mL of phenolic extract in PBS, immunostained, and then analyzed by 4-color flow cytometry for the phenotypic characterization of T helper cells (CD4+ cells), cytotoxic T lymphocytes (CD8+ cells), T regulatory cells (CD25high CD4+ cells), and natural killer cells/monocytes (CD16+ cells).

Results: Rossa di Toscana displayed the highest TPC (6.61?±?0.87?mg GA equivalents/g onion bulb DW) and the highest TAC with the experienced methods: FRAP, 9.19?±?2.54 μmol Trolox equivalents/g onion bulb DW; TEAC/ABTS, 21.31?±?0.41 μmol Trolox equivalents/g onion bulb DW; DPPH, 22.90?±?0.01 μmol Trolox equivalents/g onion bulb DW. Incubation with Rossa di Toscana extract determined an increase in the frequency of the antitumor/anti-infection NK CD16+ immune cells (23.0?±?0.4%).

Discussion and conclusions: Content of health-promoting phenols and the deriving antioxidant and immunostimulating activity vary considerably among the investigated cultivars. Rossa di Toscana can be considered as a potential functional food.     

In vitro anti-aging activities of extracts from leaves of Ma Kiang (Cleistocalyx nervosum var. paniala)

Abstract

Context: Cleistocalyx nervosum (DC.) Kosterm. var. paniala (Roxb.) J. Parn. & Chantaran. (Myrtaceae) or Ma Kiang contains high amounts of phenolic compounds. Antioxidant activity of its fruit and seed has been investigated. However, limited available information concerning the biological activities of its leaves has been reported.

Objective: To investigate the in vitro anti-aging potential of young and old leaves of Ma Kiang.

Materials and methods: Ma Kiang leaves were extracted using water, methanol, and chloroform as the solvents by cold (sonication) and hot (boiling) processes. The extracts were determined for total phenolic and flavonoid contents. The extracts (at 0.001–10?mg/ml) were tested for antioxidative and tyrosinase inhibition activities using a colorimetric method. The cytotoxicity of extracts (at 0.0001–1?mg/ml) was determined with human skin fibroblasts. Also, the extracts at 0.001, 0.01, and 0.1?mg/ml which showed no toxicity were tested for MMP-2 inhibition.

Results: The cold methanol extract of the old leaves showed the highest total phenolic and flavonoid contents of 511.44?±?18.23?μg GAE/mg and 262.96?±?2.98?μg QE/mg, respectively. This extract also gave high free radical scavenging, lipid peroxidation inhibition, and tyrosinase inhibition activities with SC₅₀, IPC₅₀, and IC₅₀ values of 0.02?±?0.004, 0.23?±?0.13, and 0.02?±?0.006?mg/ml, respectively. The extract at 0.1?mg/ml exhibited the highest MMP-2 inhibition of 91.14?±?1.67%.

Discussion and conclusion: The anti-aging potential of the cold methanol extract from old leaves of Ma Kiang can be further developed as an anti-aging agent.     

Evaluation of the antidiarrheal and antioxidant properties of Justicia hypocrateriformis

Content: Justicia hypocrateriformis Vahl (Acanthaceae) is used as an herbal remedy for diarrhea in Cameroon folk medicine.

Objective: This study evaluates the antidiarrheal and antioxidant properties of the aqueous extract of J. hypocrateriformis (JH).

Materials and methods: Preliminary phytochemical screening and an acute toxicity testing of the extract were carried out. The antidiarrheal activity of JH extract (100, 250, and 500?mg/kg) was assessed at curative and preventive levels in castor oil-induced diarrhea in mice. The antioxidant activity was measured by ferric reducing antioxidant power (FRAP), total phenolic content, and radical scavenging activity.

Results: A high lethal dose (LD₅₀) of 14.35?g/kg obtained in acute toxicity implies the extract is not toxic. Phytochemical screening revealed the presence of phenols, tannins, flavonoids, saponins, anthraquinones, and anthocyanins. JH showed a significant protection against castor oil-induced diarrhea as evidenced by a decrease in the number of defecation and wet stool. JH (100–500?mg/kg, p.o.) produced a non-significant dose-dependent decrease in castor oil-induced intestinal transit in the preventive study. In the curative and in healthy mice study, the decrease was only significant at 500?mg/kg. JH possessed a radical scavenging activity with an IC₅₀ of 9.93?mg/ml compared to 4.90?mg/ml for catechin. JH FRAP of 2703.77?±?0?mg/g (catechin equiv) and phenolic concentration of 14?169.99?±?612.39?mg/g (catechin equiv) were also obtained.

Conclusion: Justicia hypocrateriformis extract possesses antidiarrheal activity supported by its antioxidant potential and phytochemical constituents.     

Comparative pharmacokinetics of chlorogenic acid in beagles after oral administrations of single compound,the extracts of Lonicera japanica,and the mixture of chlorogenic acid,baicalin, and Forsythia suspense

Context: Chlorogenic acid (ChA) is the major compound in Shuang-Huang-Lian (SHL), which is mainly composed of ChA, baicalin, and Forsythia suspense Thunb Vahl.

Objective: The effects of co-existing compounds in SHL and Lonicera japanica Thunb on the absorption of ChA was investigated.

Materials and methods: According to 3?×?3 Latin-square test, ChA alone, the extracts of Lonicera japanica, or the mixture of ChA, baicalin and Forsythia suspense (ChA effective doses is 60?mg/kg) was separately given to six beagles for seven days. The oral pharmacokinetic parameters of ChA in plasma, urine and faeces were quantified by HPLC/UV and analyzed.

Results: The pharmacokinetic parameters of ChA alone, the extracts of Lonicera japanica, and the mixture of ChA, baicalin, and Forsythia suspense were as followed: C_max (2.350?±?0.483, 1.655?±?0.576, 2.332?±?0.606?μg/mL), AUC_0-∞ (6.324?±?1.853, 4.216?±?1.886, 6.074?±?1.473?μg·h/mL), t_1/2 (0.911?±?0.187, 1.204?±?0.309, 1.094?±?0.193?h), and T_max (1.861?±?0.499, 1.000?±?0.459, 1.833?±?0.279?h). Accumulative fraction excretion of ChA in urine were 0.73?±?0.55, 1.25?±?1.23, 1.05?±?0.96%, while that in faeces were 0.68?±?0.94, 0.19?±?0.40, and 1.76?±?3.57%.

Discussion and conclusion: Co-existing compounds in SHL have no effect on the absorption of ChA, while the concomitant compounds in Lonicera japanica could decrease that of ChA. ChA in Beagles might have high biological transformation.