Ayurvedic preparation of Zingiber officinale Roscoe: effects on cardiac and on smooth muscle parameters

The rhizome of the Zingiber officinale Roscoe, a biennial herb growing in South Asia, is commonly known as ginger. Ginger is used in clinical disorders, such as constipation, dyspepsia, diarrhoea, nausea and vomiting and its use is also recommended by the traditional medicine for cardiopathy, high blood pressure, palpitations and as a vasodilator to improve the circulation. The decoction of ginger rhizome is widely used in Ayurvedic medicine. In this papery by high-performance liquid chromatography, we have seen that its main phytomarkers were 6-gingerol, 8-gingerol and 6-shogaol and we report the effects of the decoction of ginger rhizome on cardiovascular parameters and on vascular and intestinal smooth muscle. In our experimental models, the decoction of ginger shows weak negative inotropic and chronotropic intrinsic activities but a significant intrinsic activity on smooth muscle with a potency on ileum is greater than on aorta: EC₅₀ = 0.66 mg/mL versus EC₅₀ = 1.45 mg/mL.     

Effects of flour or flaxseed oil upon testis mass in rats subjected to early weaning

Study evaluates testis mass in rats subjected to early weaning and subsequently nourished with diet containing flour or flaxseed oil. Pups were weaned for separation from mothers at 14 days (early weaning, EW) and 21 days (control, C). After 21 days, the control group (C60) was nourished with control diet. EW was divided as: control (EWC60), flaxseed flour (EWFF60) and flaxseed oil (EWFO60) group diets for the next 60 days. At 21st and 60th day, body mass, serum cholesterol and triglycerides and testis mass were evaluated. At 21 day, EW group showed lower (p < 0.05) body mass, serum cholesterol and testis mass. At 60 days, EWC60 and EWFO60 groups showed lower (p < 0.05) body mass (vs. C60 and EWFF60). EWFF60 group showed lower (p < 0.05) serum cholesterol (vs. EWC60 and EWFO60) and higher (p < 0.05) testis mass (vs. C60, EWC60 and EWFO60). Flaxseed flour (vs. oil) was associated with higher testis mass following early weaning.     

Polyphenolic characterisation of plant mixture (Lisosan® Reduction) and its hypocholesterolaemic effect in high fat diet-fed mice

Lisosan® Reduction is a plant mixture produced from powder of fermented Triticum aestivum (Lisosan® G), Desmodium adscendens, Malus domestica, Picrorhiza kurroa and Hordeum vulgare. The aim of this study was to characterise the phenolic profile of Lisosan® Reduction and to evaluate the effects of aqueous extract on mice fed a high fat diet (HFD). Syringic acid, trans sinapic acid and neochlorogenic acid were identified by HPLC-DAD to be the dominant polyphenols of Lisosan® Reduction, followed by vitexin, trans p-coumeric acid and trans ferulic acid. Mice treated with aqueous extract of Lisosan® Reduction (60 mg/kg b.w.) showed a significant decrease of serum cholesterol, glucose and triglycerides level and a significant increase of CYP7A1 gene expression, compared to HFD group.     

Development and Validation of a RP-HPLC–PDA Method for Determination of Curcuminoids in Microemulsions

A sensitive, specific and rapid high-performance liquid chromatography method was developed in an effort to quantify extremely low curcuminoid levels for the future transdermal experiments where the curcuminoids are incorporated with excipients such as microemulsion, liposomes, and micelles. The chromatographic separation was performed using a Symmetry^® C₁₈, 250 × 4.6 mm, 5-μm column, with a mobile phase composed of 5 mM acetonitrile:phosphoric acid (45:55, v/v) at a flow rate of 1.0 mL min⁻¹, it was sensitive with a low limit of quantitation for curcuminoids (0.626 ng mL⁻¹ for curcumin) and good linearity (r ² ≥ 0.999) over the range 1–100 ng mL⁻¹. All the validation data, such as accuracy and precision, were within the required limits from the ICH guideline. The assay method was successfully applied during forced degradation of curcuminoid solutions. The method retained its accuracy and precision when the standard addition technique was applied.

     

Biological activity and LC-MS profiling of ethyl acetate extracts from Nitraria sibirica (Pall.) fruits

Nitraria sibirica is a traditional Uighur medicine. This study was undertaken to investigate the bioactivity of N. sibirica fruit extract and to evaluate their chemical compositions. The ethyl acetate extract from N. sibirica fruits exhibited the potential antioxidant activity (SC₅₀ = 30.17 ± 0.06 μg/mL) and protein tyrosine phosphatase 1B inhibitory activity (IC₅₀ = 7.15 ± 0.03 μg/mL) in vitro. In order to investigate the active constituents in this extract, a LC-QTOF-MS/MS method was developed and established. A total of 28 compounds including seven cinnamic acids, nine benzoic acids and 12 flavonoids were identified or partially characterised according to the accurate mass and the characteristic fragment ions at low and high collision energy. Most of them were reported for the first time in this plant. Phytochemical profiles of the active extract will help the development and utilisation of N. sibirica in food and medicine.     

A new ultra-high pressure liquid chromatography method for the determination of antioxidant flavonol aglycones in six Lysimachia species

UPLC-DAD method was developed and validated for the quantitative determination of free flavonol aglycones (kaempferol, quercetin and myricetin) after acidic hydrolysis in six Lysimachia species. Quantitative analyses showed that the amounts of various flavonol aglycones were significantly different in Lysimachia vulgaris, Lysimachia nummularia, Lysimachia punctata, Lysimachia christinae, Lysimachia ciliata and Lysimachia clethroides. The L. clethroides sample was found to be the richest in kaempferol (25.77 ± 1.29 μg/mg extract) and quercetin (97.67 ± 4.61 μg/mg extract), while the L. nummularia sample contained the highest amount of myricetin (20.79 ± 1.00 μg/mg extract). The antioxidant capacity of hydrolysed extracts was evaluated using in vitro DPPH^? (2,2-diphenyl-1-picrylhydrazyl) and ABTS^?+ [2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulphonic acid)] decolourisation tests. The observed radical scavenging capacities of the extracts showed a relationship with the measured flavonol aglycone content and composition. The acidic treatment resulted in an increased free radical scavenging activity compared to the untreated methanol extract.     

Structure determination and quantification of a new flavone glycoside with anti-acetylcholinesterase activity from the herbs of Elsholtzia ciliata

Three acacetin triglycosides (compounds 1, 2 and 3) were isolated from the herbs of Elsholtzia ciliata (Labiatae). The structure were identified as 7-O-β-D-glucopyranosyl-(1 → 2)[α-L-rhamnopyranosyl-(1 → 6)]-β-D-glucopyranoside (compound 1), 7-O-(6-O-acetyl)-β-D-glucopyranosyl-(1 → 2)[α-L-rhamnopyranosyl-(1 → 6)]-β-D-glucopyranoside (compound 2) and 7-O-(6-O-acetyl)-β-D-glucopyranosyl-(1 → 2)[(4-O-acetyl)-α-L-rhamnopyranosyl-(1 → 6)]-β-D-glucopyranoside (compound 3) of acacetin. The structures of these compounds were determined on the basis of 2D-NMR spectroscopic data. Compound 3 has not been isolated from a natural source. In addition, the three compounds were quantitatively analysed by HPLC. Acetylcholinesterase (AChE) inhibition activity was assayed to find anti-Alzheimer’s activity, since this enzyme increases the concentration of acetylcholine (ACh), a neurotransmitter, responsible for brain’s memory. Acacetin, the aglycone of the three compounds, exhibited a potent anti-cholinesterase activity (IC₅₀, 50.33 ± 0.87), though its glycosides (1, 2 and 3) were less active. HPLC analysis demonstrated that the three compounds were contained in the MeOH extract in the order of compounds 2 (12.63 mg/g extract) > 3 (3.10 mg/g) > 1 (2.92 mg/g).     

Chemical constituents of essential oil of endemic Rhanterium suaveolens Desf. growing in Algerian Sahara with antibiofilm,antioxidant and anticholinesterase activities

Twenty compounds were detected in the essential oil of Rhanterium suaveolens representing 98.01% of the total oil content. Perillaldehyde (45.79%), caryophyllene oxide (24.82%) and β-cadinol (5.61%) were identified as the main constituents. In β-carotene–linoleic acid assay, both the oil and the methanol extract exhibited good lipid peroxidation inhibition activity, with IC₅₀ values of 17.97 ± 5.40 and 11.55 ± 3.39 μg/mL, respectively. In DPPH and CUPRAC assays, however, the methanol extract exhibited a good antioxidant activity. The highest antibiofilm activity has been found 50.30% against Staphylococcus epidermidis (MU 30) at 20 μg/mL for essential oil and 58.34% against Micrococcus luteus (NRRL B-4375) at 25 mg/mL concentration for methanol extract. The in vitro anticholinesterase activity of methanol extract showed a moderate acetylcholinesterase inhibitory (IC₅₀ = 168.76 ± 0.62 μg/mL) and good butyrylcholinesterase inhibitory (IC₅₀ = 54.79 ± 1.89 μg/mL) activities. The essential oil was inactive against both enzymes.     

Quick supramolecular solvent-based microextraction for quantification of low curcuminoid content in food

There is a need to monitor the consumption of curcuminoids, an EU-permitted natural colour in food, to ensure that acceptable daily intakes are not exceeded, especially by young children. This paper describes a sensitive method able to quantify low contents of curcumin (CUR), demethoxycurcumin (DMC) and bis-demethoxycurcumin (BDMC) in foodstuffs. The method was based on a single-step extraction by use of a supramolecular solvent (SUPRAS) made up of reverse aggregates of decanoic acid, and direct analysis of the extract by use of liquid chromatography–photodiode array (PDA) detection. The extraction involved the stirring of 200 mg foodstuff with 600 μL SUPRAS for 15 min. No cleanup or concentration of the extracts was required. Curcuminoid solubilisation occurred via dispersion and hydrogen bonding. The method was used for the determination of curcuminoids in different types of foodstuff (snack, gelatine, yoghurt, mayonnaise, butter, candy and fish products) that encompassed a wide range of protein, fat, carbohydrate, sugar and water contents (0.85–11.04, 0–81.11, 0.06–75, 0.06–79.48, and 10.08–85.10 g, respectively, in each 100 g of food). Method quantification limits for the foodstuffs analysed were in the ranges 2.9–7.7, 2.8–11.2 and 3.3–9.0 μg kg^?1 for CUR, DMC and BDMC, respectively. The concentrations of curcuminoids detected in the foodstuffs and the recoveries obtained from fortified samples were in the ranges ND–284, ND–201 and ND–61.3 μg kg^?1, and 82–106, 89–106 and 90–102 %, for CUR, DMC and BDMC, respectively. The relative standard deviations were in the range 2–7 %. This method enabled quick and simple microextraction of curcuminoids with minimal solvent consumption, while delivering accurate and precise data.

In vitro antimicrobial activity of extracts and compounds isolated from Cladonia uncialis

Heptane (Hep), diethyl ether (Et₂O), acetone (Me₂CO) and methanolic (MeOH) extracts, as well as ( ? )-usnic acid and squamatic acid, were obtained from thallus of Cladonia uncialis (Cladoniaceae). The antimicrobial activities of these extracts, ( ? )-usnic acid and squamatic acid, were tested against reference strains: Staphylococcus aureus, Escherichia coli and Candida albicans. In addition, Me₂CO extract was analysed against 10 strains of Methicillin-resistant S. aureus (MRSA) isolated from patients. All extracts exerted antibacterial activity against the reference strain S. aureus, comparably to chloramphenicol [minimum inhibitory concentration (MIC) = 5.0 μg/mL]. The Me₂CO extract exhibited the strongest activity against S. aureus (MIC = 0.5 μg/mL), higher than ( ? )-usnic acid, whereas squamatic acid proved inactive. The Me₂CO extract showed potent antimicrobial activity against MRSA (MIC 2.5–7.5 μg/mL). Also no activity of C. uncialis extracts against E. coli and C. albicans was observed.     

Modulation of antibiotic activity by the hydroalcoholic extract from leaves of Caryocar coriaceum WITTM

The aim of this study was to identify the presence of tannins, phenols and flavonoids on the hydroalcoholic extract of Caryocar coriaceum leaves (HECCL) and to determine the antioxidant and antibacterial activity of this extract. The extract was tested alone (1024–1 μg/mL) or associated (MIC/8) with several antibiotics in order to identify any antibacterial activity against multiresistant bacterial strains (Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa). The existence of tannins, total phenols (901.31 mg/g) and flavonoids (89.68 mg/g) was confirmed in the HECCL. The presence of rutin and quercetin were confirmed by Thin-layer chromatography (TLC). Using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method, the antioxidant activity of the extract (9 μg/mL) was determined. Moreover, the Minimum Inhibitory Concentration (MIC) value found for HECCL was 1024 μg/mL and the association between HECCL (MIC/8) with benzylpenicillin significantly changed its minimum inhibitory concentration from 2500 to 625 μg/mL against E. coli.     

Antioxidant,antimicrobial and urease inhibiting activities of methanolic extracts from Cyphostemma digitatum stem and roots

Cyphostemma digitatum stem and roots extracts were investigated for antioxidant, antimicrobial, urease inhibition potential and phytochemical analysis. Phytochemical screening of the roots and stem extract revealed the presence of secondary metabolites including flavonoids, alkaloids, coumarins, saponins, terpenoids, tannins, carbohydrates/reducing sugars and phenolic compounds. The methanolic extracts of the roots displayed highest antioxidant activity (93.518%) against DPPH while the crude methanolic extract of the stem showed highest antioxidant activity (66.163%) at 100 μg/mL concentration. The methanolic extracts of both stem and roots were moderately active or even found to be less active against the selected bacterial and fungal strains (Tables S2 and S3). The roots extract (methanol) showed significant urease enzyme inhibition activity (IC₅₀ = 41.2 ± 0.66; 0.2 mg/mL) while the stem extract was found moderately active (IC₅₀ = 401.1 ± 0.58; 0.2 mg/mL) against thiourea (IC₅₀ = 21.011; 0.2 mg/mL).     

Benefits of Anthocyanin-Rich Black Rice Fraction and Wood Sterols to Control Plasma and Tissue Lipid Concentrations in Wistar Kyoto Rats Fed an Atherogenic Diet

Background: This study reports on the relative effects of administrating a cyanidin-3-O-glucoside-rich black rice fraction (BRF), a standardized wood sterol mixture (WS), and a combination of both to lower plasma and target tissue lipid concentrations in Wistar Kyoto (WKY) rats fed atherogenic diets. Methods: Male WKY (n = 40) rats were randomly divided into five groups, which included a nonatherogenic control diet and atherogenic diets that included a positive control and atherogenic diets supplemented with BRF or WS, respectively, and a combination of both BRF + WS. Plasma and target tissue liver, heart and aorta cholesterol, and triacylglycerides (TAG) content were also measured. Results: Rats fed atherogenic diets exhibited elevated hyperlipidemia compared to counterparts fed nonatherogenic diets (p < 0.001); this effect was mitigated by supplementing the atherogenic diets with BRF and WS, respectively (p < 0.05). Combining BRF with WS to enrich the supplement lowered cholesterol similar to the WS effect (p < 0.05) and lowered TAG characteristic to the BRF effect (p < 0.05). Conclusions: Rats fed diets containing BRF or WS effectively mitigate the hypercholesterolemia and elevated TAG induced by feeding an atherogenic diet. The benefit of adding BRF + WS together is relevant to the lipid parameter measured and is target tissue-specific.     

Ruta chalepensis L. (Rutaceae) leaf extract: chemical composition,antioxidant and hypoglicaemic activities

Ruta chalepensis L. (Rutaceae) leaf extract was investigated for its chemical profile and antioxidant and hypoglycaemic properties. The antioxidant effects were investigated by 2,2-diphenyl-1-picrylhydrazyl (DPPH), β-carotene bleaching, and metal chelating activity assays. The carbohydrate-hydrolysing enzymes inhibition assay was used to test the hypoglycaemic potential. R. chalepensis showed a high content of hesperidin and rutin with values of 591.9 and 266.7 mg/g dry extract, respectively. The extract exhibited a promising protection of lipid peroxidation (IC₅₀ value of 16.9 μg/mL) and inhibited both α-amylase and α-glucosidase enzymes in a concentration-dependent manner. The highest activity was found against α-amylase (IC₅₀ value of 69.0 μg/mL). The obtained results support the use of R. chalepensis leaves as healthy food ingredients.     

Chemical composition,in vitro antioxidant activity and α-glucosidase inhibitory effects of the essential oil and methanolic extract of Elsholtzia densa Benth.

Elsholtzia densa Benth. is a traditional aromatic herb used in the pharmaceutical and flavouring industries. To analyse and compare the chemical composition, the oils and nonvolatile compounds in E. densa and Mosla chinensis Maxim. were extracted via hydrodistillation, solvent extraction or ultrasound-assisted extraction. Seventy-three volatile compounds in the volatile oil (0.35 ± 0.06%) obtained by E. densa via hydrodistillation were investigated by gas chromatography–mass spectrometer and compared based on different parameters. Also, the antioxidant activity and α-glucosidase inhibitory effects of the five sub-fractions of the methanolic extract were studied and the ethyl acetate sub-fraction (EC₅₀ = 7.9 μg/mL) and petroleum ether sub-fraction (EC₅₀ = 0.0955 mg/mL) showed the strongest activity, respectively. This study has provided a scientific basis for scientific collection, effective development, use of E. densa Benth., and suggested that it can be used as a potential source of antioxidants in food and a potential candidate for the management of type 2 diabetes mellitus.     

Lycopus europaeus: phenolic fingerprint,antioxidant activity and antimicrobial effect on clinical Staphylococcus aureus strains

Lycopus europaeus L. leaves water extract (LEL) was subjected to phytochemical analysis, and evaluated for its antibacterial and antioxidant effects. Antibacterial activity testing was performed on Staphylococcus aureus clinical strains from catheter-related and skin infections by broth microdilution test. LEL showed bactericidal activity at concentrations from 2500 to 5000 μg/mL against all, including methicillin resistant and polyresistant nosocomial, strains. Antioxidant activity was examined using DPPH and ABTS (11.3 and 9.8 μg/mL, respectively) and by ferric reducing ability of the plasma method (891 μmol AAE/g dry extract). Phytochemical analysis of LEL was performed by LC-DAD-MS/MS. Ten phenolic compounds were identified; two minor compounds (glucopyranosyl rosmarinic acid and sagerinig acid) have not been described in Lycopus yet. The major compounds, considered to be responsible for biological activities detected in the study, were determined as rosmarinic acid (76 mg/g) and luteolin-7-O-glucuronide (23 mg/g). L. europaeus arises from our study as a promising source of antibacterial agent for topical usage.     

HPLC-ESI-MS/MS analysis of phenolics and in vitro antioxidant activity of Epilobium angustifolium L.

The aerial parts of Epilobium plants are widely used as folk medicine and food around the world. The present study was aimed to investigate the antioxidant activities and active chemical constituents from Epilobium angustifolium L. The results revealed that the EtOAc extract, rich in phenolic compounds and flavonoids (16.81 ± 0.67 g GAE/100 g extract and 4.95 ± 0.21 g QE/100 g extract, respectively), possessed significantly antioxidant activities in reducing power, DPPH radical scavenging activity, ABTS radical scavenging activity and highly in inhibiting lipid peroxidation activity. Simultaneously, active fractions F to H from EtOAc extracts showing potent in vitro antioxidant activities also contained high content of total phenolic and flavonoid. Twenty-eight compounds were identified as phenolic compounds and flavonoids by LC-MS/MS. The results illustrate that the E. angustifolium L., which is rich in phenolics, could be used as a natural resource of antioxidant ingredient.     

Evaluation of hepatoprotective activity of aqueous extracts of leaves of Basella alba in albino rats

This study was done to evaluate possible hepatoprotective effects of aqueous leaf extracts of Basella alba in comparison with silymarin in paracetamol-induced hepatotoxicity in albino rats. Six groups of six albino rats each received orally for 6 weeks, vehicle, paracetamol (2 g/kg/day), paracetamol (2 g/kg/day) plus silymarin (50 mg/kg/day), paracetamol (2 g/kg/day) plus B. alba extract (60 mg/kg/day), paracetamol (2 g/kg/day) plus B. alba extract (80 mg/kg/day) and paracetamol (2 g/kg/day) plus B. alba extract (100 mg/kg/day). Hepatoprotective effect was evaluated by comparing serum bilirubin, serum glutamic oxaloacetic transaminase, serum glutamic pyruvic transaminase, proteins, alkaline phosphatase and liver histopathology. Results were represented as mean ± SEM. One-way ANOVA was done followed by post hoc Tukey's test with a highly significance level of P < 0.001. Aqueous leaf extracts of B. alba 100 mg/kg/day orally had significant hepatoprotective effect in paracetamol-induced hepatotoxicity in albino rats. The results were well comparable and even in some respects superior to standard drug silymarin.     

An insight into antimicrobial activity of the freshwater bryozoan Pectinatella magnifica

The antimicrobial activity of five crude extracts of the freshwater bryozoan Pectinatella magnifica (Leidy, 1851) was evaluated in vitro for the first time. P. magnifica acetone extract exhibited the highest antibacterial activity (minimum inhibitory concentrations (MIC) 0.004–0.350 mg/mL and MBC 0.007–0.500 mg/mL), while its methanol extract showed the most promising antifungal activity (MIC 0.03–0.12 mg/mL and MFC 0.06–0.25 mg/mL). Furthermore, at a concentration of 0.25 MIC, the methanol extract reduced biofilm formation of the bacterial strain Pseudomonas aeruginosa PAO1 in a considerable extent (59.14%). FTIR spectra of the most active extracts indicate the presence of carbonyl compounds, long-chain alcohols and/or sterols. According to the experimental data obtained, P. magnifica methanol extract may be considered as a good resource of novel natural products with potent antibiofilm activity against the bacterium well known for its resistance.     

Quantification of polyphenols and flavonoid content and evaluation of anti-inflammatory and antimicrobial activities of Stenocereus stellatus extracts

The hexanic, ethyl acetate and methanolic extracts from branches of Stenocereus stellatus were tested in both the 12-O-tetradecanoylphorbol-13-acetate (TPA) – induced ear oedema model and antimicrobial activity assay. The % of oedema inhibition, the Minimum Inhibitory Concentration (MIC), as well as the polyphenolic and flavonoid content were determined. Also, extracts were analysed by gas chromatography–mass spectrometry (GC–MS). In TPA model, the three extracts showed moderate oedema inhibition. In the antimicrobial activity assay, methanolic extract shows better MIC against all strains. The lowest MICs were for Candida albicans (31 μg/mL) and Rhizopus sp. (15 μg/mL). Also, 50.78 mg eq. of gallic acid/g extract of polyphenol and 115.12 mg eq. of catequine/g extract of flavonoids content were founded in ethyl acetate extract. In the chromatographic analysis, β-sitosterol, β-amyrine, betulin and some other molecules were identified. The results show that S. stellatus possess antimicrobial activities against some fungus species.