Polyphenolic profiling of Ipomoea carnea Jacq. by HPLC-DAD and its implications in oxidative stress and cancer

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).     

α-Glucosidase inhibitory activity of marine sponges collected in Mauritius waters

This report describes the use of α-glucosidase to evaluate the anti-diabetic potential of extracts from marine sponges collected in the Mauritius waters. Initial screening at 1.0 mg/mL of 141 extracts obtained from 47 sponge species revealed 10 extracts with inhibitory activity greater than 85%. Seven of the 10 extracts were further tested at 0.1 and 0.01 mg/mL and only the methanol extract of two sponges namely Acanthostylotella sp. (ASSM) and Echinodictyum pykei (EPM) showed inhibition activity greater than 60% at 0.1 mg/mL with an IC₅₀ value of 0.16 ± 0.02 and 0.04 ± 0.01 mg/mL, respectively, while being inactive at 0.01 mg/mL.     

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).     

Assessment on in vitro medicinal properties and chemical composition analysis of Solanum virginianum dried fruits

The study was aimed to screen the presence of phytoconstituents and determine distinct in vitro medicinal traits of aqueous and ethanolic extracts of Solanum virginianum dried fruits. Aqueous and ethanolic extract showed total phenolic content of 207.5 ± 0.16 and 268.4 ± 0.42 GAE/mg, respectively. Likewise, total flavonoid content of 50.12 ± 0.39 and 192.88 ± 0.27 QE/mg was estimated for the aqueous and ethanolic extract, respectively. In vitro antibacterial, antioxidant, α-amylase inhibition, anti-inflammatory, and anticancer attributes of extracts were assessed using standard protocols. The antibacterial traits of both the extracts were assessed against certain pathogenic bacteria which exhibited maximum zone of inhibition of 22.3 ± 0.6 mm against Staphylococcus aureus. Antioxidant tests showed not only significant scavenging of DPPH, superoxide, hydroxyl, and ABTS^●+ radicals but also estimated ferric reducing power and phosphomolybdenum reduction activities of extracts in a concentration dependent manner. The aqueous extract (54.12 ± 0.44–86.80 ± 0.27%) depicted higher rate of α-amylase inhibition than ethanolic extract (23.07 ± 0.47–81.61 ± 0.43%) at distinct concentrations. Similarly, the aqueous extract protected the haemolysis (46.19 ± 0.14–66.21 ± 0.17%) effectively as compared to the ethanolic extract (12.67 ± 0.19–38.03 ± 0.41%). The aqueous and ethanolic extract showed cytotoxicity against HepG2 cell lines in the range of 32.23 ± 0.34–54.82 ± 0.26% and 49.25 ± 0.38–73.2 ± 0.3%, respectively. Additionally, the GC–MS analysis confirmed the availability of total 15 predominant bioactive constituents in both extracts. Findings of this context indicated pronounced applications of S. virginianum fruits as future therapeutic.     

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.     

HPLC profiling of phenolics and flavonoids of Adonidia merrillii fruits and their antioxidant and cytotoxic properties

In this study the antioxidant and cytotoxicity activity of the Adonidia merrillii fruits were investigated using different solvent polarities (methanol, ethyl acetate and water). The results showed that the total phenolic and flavonoid contents of the methanolic extract was higher compare with other extract with respective values of 17.80 ± 0.45 mg gallic acid equivalents/g dry weight (DW) and 5.43 ± 0.33 mg rutin equivalents/g DW. Beside that The RP-HPLC analyses indicated the presence of gallic acid, pyrogallol, caffeic acid, vanillic acid, syringic acid, naringin and rutin. In the DPPH, NO2 and ABTS scavenging assays, the methanolic extract exhibited higher antioxidant activity as compared to the ethyl acetate and water extracts. The extracts exhibited moderate to weak cytotoxic activity in the assays using human hepatocytes (Chang liver cells) and NIH/3T3 (fibroblasts cell) cell lines. The findings showed the Adonidia merrillii fruit extracts to possess considerable antioxidant and cytotoxicity properties. The fruit, therefore, is a potential candidate for further work to discover antioxidant and cytotoxic drugs from natural sources.     

A new acylated flavonol from the aerial parts of Asteriscus maritimus (L.) Less (Asteraceae)

Phytochemical investigation of the flowering aerial parts of Asteriscus maritimus (L.) Less (Asteraceae) led to the isolation of a new compound: patuletin 7-O-β-D-[(2″′S) 6″(3″′-hydroxy-2″′-methyl-propanoyl)] glucopyranoside, together with five known metabolites; β-sitosterol 2, chlorogenic acid 3, P-hydroxy -methylbenzoate 4, luteolin 5 and protocatechuic acid 6. The structures of the isolated compounds were determined by comprehensive analyses of its 1D and 2D NMR, HRMS and compared with previously known analogues. The ethanolic extract of the flowering aerial parts of A. maritimus was found to be safe (LD₅₀ = 4.6 mg/kg) and possess significant antioxidant and anti-inflammatory activities and this was in accordance with its high phenolic content (107.36 ± 0.051 mg GAE/g extract).     

Evaluation of the protection and release rate of bougainvillea (Bougainvillea spectabilis) extracts encapsulated in alginate beads

There is a growing demand in the food industry for natural food products to replace synthetic ingredients. Motivated by this fact, the present work studied the extraction of coloring compounds from Bougainvillea spectabilis under aqueous and ethanolic conditions, and the encapsulation of the extract in alginate beads. Ethanolic extraction was more efficient as reflected by the higher values for total phenols (6.78?±?0.24?mg EAG/g), betacyanins (5.04?±?0.13?mg/g), betaxanthines (1.35?±?0.06?mg/g,) and inhibition capacity (81.31?±?4.23%). FTIR analysis suggested the presence of interactions between the extract and the alginate chains. The release kinetics of compounds in alginate beads was measured under aqueous and ethanolic conditions at 25.0?°C and at 70.0?°C. Color was also monitored, showing that the color parameters followed a kinetics pattern similar to the released extract. However, the release of betalains exhibited a mixed behavior, reflecting interactions between the different compounds of the bougainvillea extract and the alginate chains. The extracts released from the beads were characterized to determine the preservation of their properties during encapsulation, concluding that the encapsulation is efficient to protect and release the bioactive compounds from bougainvillea extracts.     

A new aromatic glycoside and its anti-proliferative activities from the leaves of Bergenia purpurascens

Chemical investigation of the ethanolic extracts of the dried leaves of Bergenia purpurascens led to the isolation and identification of a new aromatic glycoside, 1-O-β-D-glucopyranosyl-2-methoxy-3-hydroxyl-phenylethene (1), along with other 19 known compounds (2–20). The structure of compound 1 was determined by a detailed analysis using various analytical techniques, including 1D and 2D NMR. In vitro anti-proliferative activities of compound 1 on five human cancer cell lines were evaluated. The results showed that compound 1 possessed the most potent effects with the IC₅₀ values of 14.36 ± 1.04 μM against T24 cells. The further bioactivity analysis showed that compound 1 induced apoptosis of T24 cells, and altered anti- and pro-apoptotic proteins, leading to mitochondrial dysfunction and activation of caspase-3 for causing cell apoptosis. The present investigation illustrated compound 1 might be used as a potential antitumour chemotherapy candidate.     

Screening of bioconstituents and in vitro cytotoxicity of Clematis gouriana leaves

Clematis gouriana (Ranunculaceae), a perennial herb, is used by the local inhabitants of the western Himalayan region for its medicinal properties. Major bioconstituents of C. gouriana leaves using different solvent extracts were obtained and analysed. The results revealed promising contents of phenolics (from 18.19 ± 0.10 to 22.17 ± 0.10 mg g^? 1) as gallic acid and flavonoids (from 2.83 ± 0.01 to 6.52 ± 0.08 mg g^? 1) as quercetin equivalent in different extracts. Aqueous acetone extract showed higher antioxidant activity with IC₅₀ value of 129.11 and 25.35 μg mL^? 1 against DPPH and ABTS free radicals, respectively. Antioxidant yield ranged from 16.87 ± 0.27 to 24.48 ± 0.13 mg g^? 1 of Trolox equivalent in different extracts as measured by the FRAP assay. Furthermore, ethylacetate extract exhibited strong in vitro cytotoxicity against Chinese hamster ovary and glioma cell lines. Proximate composition (proteins, fats, ash and minerals) of C. gouriana leaves was also assessed. Results demonstrated the potential of C. gouriana bioconstituents as nutraceuticals.     

Anti-proliferation effects of ethanolic extracts from Sophora moorcroftiana seeds on human hepatocarcinoma HepG2 cell line

Previous studies have shown that the ethanolic extracts from Sophora moorcroftiana seeds (ee-Sms) have in vitro anticancer properties. The anti-proliferation effects of ee-Sms on HepG2 cells were assessed by MTT assay and cell cycle analysis. Total cell proteins were separated by two-dimensional electrophoresis (2-DE), and protein spots with more than two-fold difference were analysed by MALDI-TOF/TOF-MS. MTT assay showed that the anti-proliferation of ee-Sms demonstrates dose- and time dependently. HepG2 cells were treated with ee-Sms at 1.30 mg/mL for 48 h induced cell cycle arrest in S phase. The differentially-expressed proteins were involved in DNA repair, cell proliferation, cell metabolism and immunoreaction. This study sheds new insights into the molecular mechanisms underlying the anti-proliferation properties of ee-Sms in HepG2 cells.     

Urease inhibitory profile of extracts and chemical constituents of Pistacia atlantica ssp. cabulica Stocks

The current study was designed to evaluate the urease inhibitory profile of extract and fractions of Pistacia atlantica ssp. cabulica Stocks followed by bioactivity-guided isolated compounds. The crude extract was found significantly active with urease inhibitor (95.40% at 0.2 mg/mL) with IC₅₀ values of 32.0 ± 0.28 μg/mL. Upon fractionation, ethyl acetate fraction displayed 100% urease inhibition with IC₅₀ values of 19.9 ± 0.51 μg/mL at 0.2 mg/mL. However, n-hexane and chloroform fractions exhibited insignificant urease inhibition. Similarly, the isolated compound, transilitin (1) and dihydro luteolin (2) demonstrated marked urease attenuation with 95 and 98% respectively, at 0.15 mg/mL. Both the isolated compounds showed marked potency with IC₅₀ values of 8.54 ± 0.54 and 9.58 ± 2.22 μg/mL, respectively. In short, both the extract and fractions and isolated compounds showed marked urease inhibition and thus a useful natural source of urease inhibition.     

Identification and in vitro antioxidant activities of phenolic compounds isolated from Cynoglossum cheirifolium L.

In an extensive search for bioactive compounds from plant sources, the quantitative and qualitative characterisation of the compounds present in Cynoglossum cheirifolium extracts was studied. Total phenolic and flavonoid contents were determined by spectrophotometric techniques. In vitro antioxidant and radical scavenging profiling was determined through DPPH^? scavenging activity and Ferric reducing antioxidant power (FRAP). Our study showed that leaves produce more phenolic compounds, followed by flowering aerial part. The butanolic fraction obtained from leaves extract exhibited the highest total phenolics (78.65 ± 3.58 mg GAE/g DW) and flavonoids (22.15 ± 4.66 mg CE/g DW). In contrast, this fraction displayed the highest DPPH^? scavenging ability with IC₅₀ values of 0.06 ± 0.003 mg/mL. The RP-HPLC-PDA analysis of phenolic compounds from leaves of C. cheirifolium lets to identify: rosmarinic acid, ferulic acid, caffeic acid, p-coumaric acid, syringic acid, sinapic acid and rutin. The obtained results indicate that this plant represent a valuable source of natural antioxidants.     

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.     

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.     

Aedes aegypti larvicide from the ethanolic extract of Piper nigrum black peppercorns

Due to unavailability of a vaccine and a specific cure to dengue, the focus nowadays is to develop an effective vector control method against the female Aedes aegypti mosquito. This study aims to determine the larvicidal fractions from Piper nigrum ethanolic extracts (PnPcmE) and to elucidate the identity of the bioactive compounds that comprise these larvicidal fractions. Larvicidal assay was performed by subjecting 3rd to 4th A. aegypti instar larvae to PnPcmE of P. nigrum. The PnPcmE exhibited potential larvicidal activity having an LC₅₀ of 7.1246 ± 0.1304 ppm (mean ± Std error). Normal phase vacuum liquid chromatography of the PnPcmE was employed which resulted in five fractions, two of which showed larvicidal activity. The most active of the PnPcmE fractions is PnPcmE-1A, with an LC₅₀ and LC₉₀ of 1.7101 ± 0.0491 ppm and 3.7078 ppm, respectively. Subsequent purification of PnPcmE-1A allowed the identification of the larvicidal compound as oleic acid.     

Extracts of the unripe fruit of Ilex paraguariensis as a potential chemical control against the golden apple snail Pomacea canaliculata (Gastropoda,Ampullariidae)

Plant extracts can provide a viable alternative to controlling many crop pests. This study sought to assess the efficacy of vegetable extracts of the unripe fruits of Ilex paraguariensis (yerba maté) for chemical control of the channeled apple snail (Pomacea canaliculata) and of non-target species as the South American catfish (Rhamdia quelen) under laboratory conditions. In P. canaliculata, the LC₅₀ of the decoction extract was 31.39 mg.L^?1 and the LT₅₀ was over 26 h. The LC₅₀ of the butanol extract was 24.75 mg.L^?1 and the LT₅₀ was in the range of 28 to 32 h. In juvenile R. quelen, the LC₅₀ of the decoction was 17.98 mg.L^?1 and the LT₅₀ was in the range of 10–12 h. These extracts are particularly attractive considering the source of compounds and their effectiveness as molluscicides.     

Diuretic activity of ethanolic extract of Panicum repens L. roots and rhizomes

The diuretic activity of ethanolic extract of Panicum repens was investigated in rats. A single oral dose of 500 mg/kg of P. repens extract were given to rats, after 24 h, urine volume, its sodium and potassium concentrations were estimated. Treatment with P. repens extract caused a significant increase in tested parameters as compared to their corresponding controls, p < 0.05.