Evaluation of anti-inflammatory, diuretic and oral glucose tolerance activities of phenolic compound-rich fractions of Hammada articulata in Albino Wistar rats.

Hammada articulata is a plant widely used by the locals of the Algerian Sahara for multiple medicinal purposes. However, little was known about its chemical composition and the mechanisms of its bioactivity. For this purpose, the derived extracts [chloroform (CHCl3), ethyl acetate (EtOAc) and n-butanol (n-BuOH)] of the 80% ethanol extract of its aerial parts, were evaluated for their anti-inflammatory, diuretic, and anti-hyperglycemic activities in vivo. A preliminary phytochemical screening of H. articulata extracts showed the presence of a variety of secondary metabolites. RP-HPLC/DAD was used to analyze some fractions obtained by fractionation of the three derived extracts, by column chromatography and chosen because of the abundance and simplicity of their chemical composition. The fractions obtained from EtOAc and n-BuOH extracts showed a particular richness in phenolic compounds mainly naringenin, quercetin, kaempferol, myricetin, and rutin, which were known for their many interesting biological activities. The three derived extracts from H. articulata were assessed for their anti-inflammatory activity in the carrageenan-induced edema model in rats and their diuretic activity using hydrochlorothiazide (HCTZ) as a diuretic reference. All extracts showed considerable anti-inflammatory activity; the highest was registered in the group treated with the n-BuOH extract. However, for the diuretic activity, only the chloroform extract was active, with a diuretic spectrum similar to that of the standard diuretic HCTZ. The anti-hyperglycemic effect was carried out on the three derived extracts administered orally at a dose of 200 mg/kg, using the glucose tolerance test after gavage with the extracts. The EtOAc and n-BuOH extracts showed significant anti-hyperglycemic activity, improving oral glucose tolerance in normal rats.

The preventive effects of Centaurea maroccana Ball. extract against oxidative stress induced by cisplatin in mice brains: in vitro and in vivo studies.

Since antiquity, Centaurea species have been used in folk medicine to treat several diseases owing to their potential biological activities that distinguish this genus such as antioxidant, anticancer, and anti-inflammatory effect. The current study aimed to investigate the possible neuroprotective effects of the n-butanol extract of Centaurea maroccana (BECM) against cisplatin (CP) induced neurotoxicity in mice. BECM's potential neuroprotective properties were studied in vitro and in vivo models. Male Swiss albino mice were orally received BECM (200 mg/kg) for 10 days before a single intraperitoneal injection of cisplatin (8 mg/kg). Vitamin E (100 mg/kg) was given daily by gavage as a positive control. In vitro results revealed that BECM inhibited lipid peroxidation (LPO) levels and acetylcholinesterase (AChE) activity. In vivo findings showed that BECM pretreatment was able to regulate lactate dehydrogenase (LDH) levels and to improve CP-induced cholinergic dysfunction by inhibiting AChE activity in mice brains. Moreover, BECM attenuated CP-provoked oxidative stress by suppressing LPO levels, increasing total antioxidant capacity (TAC) and enhancing the activities of antioxidant enzymes (catalase (CAT), superoxide dismutase (SOD), reduced glutathione (GSH), glutathione peroxidase (GPx) and glutathione S-transferase (GST)) in both brain cytosolic and mitochondrial fractions. The histological analysis exhibited neurotoprotective effect of BECM by protecting the cerebral cortex and reducing the histomorphological alterations resulted by cisplatin. Interestingly, our extract achieved neuroprotection comparable to vitamin E in most evaluated parameters. It appears that protective potency of BECM against CP-induced neurotoxicity could be related to its richness in polyphenols confirmed by liquid-chromatography tandem mass spectrometry analysis (LC-MS/MS).

Neuroinflammation and Behavioral Deficit in Rotenone-Induced Neurotoxicity in Rats and the Possible Effects of Butanolic Extract of Centaurea africana.

BACKGROUND: Many studies have used rotenone (ROT) to create an experimental animal model of Parkinson's disease (PD) because of its ability to induce similar behavioral and motor deficits. PD is the most common age-related motoric neurodegenerative disorder. Neuroinflammation and apoptosis play an important role in the pathogenesis of this disease. OBJECTIVE: This study investigated the effect of butanolic (n-BuOH) extract of Centaurea africana (200 mg/kg, 16 days) on a ROT-induced neurotoxicity model in male Wistar albino rats. METHODS: Estimation of Tumor Necrosis Factor (TNF-α) and Nitric Oxide (NO) levels along with the myeloperoxidase (MPO) activity in brains was carried out in order to evaluate neuro-inflammation. Oxidative stress, Caspase 3 activity (apoptosis), and behavioral alterations were also evaluated. RESULTS: In behavior assessment, using Ludolph Movement Analysis Scale, all ROT treated animals showed a decreased locomotor activity. The mitochondrial dysfunction induced by ROT was expressed by a decreased activity of complex I of the mitochondrial respiratory chain and increased lipid peroxidation and caspase 3. Co-treatment with the n-BuOH extract significantly restored the activity of complex I (65.41 %) compared to treatment with ROT alone. The n-BuOH extract also reduced the neuroinflammation in rat brains by reducing MPO activity (75.12 %), NO levels (77.43 %), and TNF-α (71.48 %) compared to the group treated with ROT. CONCLUSION: The obtained results indicated that C. africana n-BuOH extract exhibited a protective effect in rats.

First report on phytochemical investigation, antioxidant and antidiabetic activities of Helianthemum getulum.

A new flavonoid, 5,7,2',4',5'-pentahydroxyflavone 3-O-ß-D-galactopyranoside (12) and twelve known derivatives: an aryltetralin-lignan (3), seven flavonoids (4-5, 7-10, 13) and four phenolic acids (1-2, 6, 11) have been isolated from the aerial parts of Helianthemum getulum Pomel. (Cistaceae family) an endemic species to the septentrional Sahara that is being studied for the first time. Structure elucidation of the isolated compounds was established by means of spectroscopic methods especially NMR and Mass Spectrometry. In vitro antioxidant (DPPH, ABTS, GOR and CUPRAC assays) and antidiabetic (micro-dilution method) activities of the crude extract, fractions and isolated compounds were performed. The new flavonol (12) and Compounds (2, 3, 7, 9) were found to be the most active, some of them exhibiting better activity than the antioxidant standards. Compounds 7, 9 and 3 showed higher α-glucosidase inhibitory activity compared to standard acarbose (IC50= 2.70 ± 0.03 µM, 3.09 ± 0.03 µM, 37.28 ± 1.20 µM and 275.43 ± 1.59 µM, respectively).

Bio-guided isolation of leishmanicidal and trypanocidal constituents from Pituranthos battandieri aerial parts.

Protozoan pathogens that cause neglected tropical diseases are a major public health concern in tropical and developing countries. In the course of our ongoing search for new lead compounds as potential antiprotozoal agents, this study aims to perform a bio-guided fractionation of Pituranthos battandieri, using an in vitro assay against Leishmania amazonensis and Trypanosoma cruzi. Two known polyacetylenes, (-)-panaxydiol (1) and (-)-falcarindiol (2) were identified from the ethanolic extract of the aerial parts of P. battandieri as the main bioactive constituents. Compounds 1 and 2 showed similar potency (IC50 values of 5.76 and 5.68 µM, respectively) against L. amazonensis to miltefosine (IC50 value of 6.48 µM), the reference drug, and low toxicity on macrophage cell lines J774. Moreover, compound 1 exhibited moderate activity (IC50 23.24 µM) against T. cruzi. In addition, three known furanocoumarins, 8-geranyloxypsoralen (3), 8-geranyloxy-5-methoxypsoralen (4), and phellopterin (5) were isolated. Their structures were elucidated by NMR and MS analysis. Compounds 1 and 2 are described for the first time in the Pituranthos genus, and this is the first report on their antiprotozoal activity. These results highlight this type of polyacetylenes as an interesting scaffold for the development of novel antiparasitic drugs.

Polyphenolic content and bioactivities of Crataegus oxyacantha L. (Rosaceae).

Solid-Liquid Extraction (SLE) using solvent of different polarities (CHCl3, EtOAc, and n-BuOH) has been applied to leaves and fruits from (Crataegus oxyacantha L.), a deciduous shrub with an expected rich phytochemical profile. The total polyphenols content and the radical scavenging activity of each extract were evaluated. These extracts were analyzed by HPLC-DAD and rutin, quercetin-3-glucoside, caftaric and caffeic acid had been positively identified. The phytochemical study of the ethyl acetate extract of C. oxyacantha, led to the isolation and structural elucidation of quercetin (1); quercetin-3-O-ß-glucoside (2); epicatechin (3); naringenin (4), reported for the first time from this species except caffeic acid and epicatechin. These compounds were identified by 1D and 2D NMR combined analysis as well as by MS and UV.The antimicrobial activity of these extracts has also been tested, showing strong antibacterial activity-solvent dependent-against Gram positive bacteria. Additionally, bactericidal power was demonstrated in fruit extracts.

Antioxidant, Anti-Inflammatory and Cytotoxic Properties of Centaurea africana Lamk var. [Bonnet] M].

BACKGROUND: In Algerian traditional medicine, Centaurea species are well known in traditherapy. Centaurea africana has been used in folk medicine for the treatment of several inflammatory disorders. OBJECTIVE: This study aims to examine the antioxidant, anti-inflammatory and anti-proliferative potential of both n-Butanol (BECA) and ethyl acetate (EAECA) extracts of Centaurea africana. METHODS: The phytochemical analysis of both BECA and EAECA were explored and the antioxidant activities were investigated by measuring the DPPH° scavenging effect, the reducing power and the inhibition of lipid peroxidation (LPO) induced by by Fe2+/ ascorbic acid system. The antiinflammatory properties were determined by measuring the NO° scavenging effect and by using carrageenan-induced rat paw oedema. The antiproliferative activity was studied on HT29 (human colorectal adenocarcinoma), OV2008 (human ovarian cancer) and C6 (Rattus norvegicus brain glioma) cell lines using the Sulforhodamine B assay. RESULTS: The total polyphenol contents (TPC) of EAECA and BECA are recorded at 125.24±10.14 and 53.03±2.50 mgGAE/g extract, respectively. Both extracts revealed the antioxidant activity in a concentration-dependent manner; this effect is more pronounced with EAECA. The BECA exhibited a higher anti-inflammatory activity. This anti-inflammatory activity was reflected in a reduction of swelling of carrageenan-evoked edemas (48.45 %), inhibition of nitric oxide (84.7 %), effective decrease in myeloperoxidase activity (58.82 %) and malondialdehyde level (65.58 %). The cytotoxic effect of BECA was found to be more pronounced against C6 cell lines (IC50 value: 131.93 µg/mL) while the cytotoxic activity of EAECA was more effective against HT29 and OV2008 cell lines. CONCLUSION: The obtained results indicated that EAECA exhibited a high antioxidant activity, while BECA has significant anti-inflammatory activity. Both extracts showed cytotoxic effects against cancer cell lines at certain concentrations in a cell-specific manner.

New sesquiterpenes from Asteriscus graveolens.

Asteriscus graveolens (Forsk) Less. is a Saharan medicinal plant of Asteraceae family. A new acyclic sesquiterpene [7,12-dihydroxy-6,7-dihydro-5,(6) E-dehydronerolidol (3)] and sesquiterpene germacranolide lactone derivatives [9ß-hydroxy-11ß,13-dihydroparthenolide-9-O-ß-D-glucopyranoside (7) and 9α-hydroxy-11ß,13-dihydroparthenolide-9-O-ß-D-glucopyranoside (8)] along with eight known compounds were isolated from polar extracts of aerial parts. Their structures were established by the analysis of 1 D- 2 D-NMR and high-resolution mass spectrometry data. A. graveolens extracts and compounds showed a significant (P < 0.05) and concentration dependent inhibitory effect on the growth of Human Colon Carcinoma (HCT116) and Human Colorectal Adenocarcinoma (DLD1) cells with IC50 in a concentration range from 89.4 to 296.0 µg/mL for extracts and from 32.6 to 728.1 µg/mL for compounds. No cytotoxic effects was evidenced in normal Primary Human Dermal Fibroblast (HDFa) up to 0.050 mg/mL for extracts and 1.0 mg/mL for pure compounds.

Limonium duriusculum (de Girard) Kuntze Exhibits Anti-inflammatory Effect Via NF-κ B Pathway Modulation

HIGHLIGHTS L. duriusculum n-BuOH extract reduces inflammatory responses both in vitro and in vivo. L. duriusculum n-BuOH extract inhibits NF-κB-dependent transcriptional responses. L. duriusculum n-BuOH extract decreases the expression of TNF-α and IL-6 genes.

Abstract Limonium duriusculum is used in folk medicine to treat inflammatory disorders and has gained attention due to its richness in apigenin. The present investigation was performed to evaluate and confirm its anti-inflammatory properties, in cell lines and animal models. The potential anti-inflammatory properties of n-butanol (n-BuOH) extract of L. duriusculum (BEL) and isolated apigenins were examined on NF-κB transcriptional activity in TNFα- or LPS-stimulated cells, and on in vivo acute inflammatory models (carrageenan induced paw edema and peritonitis). BEL treatment was able to inhibit the activity of an NF-κB reporter gene in HCT116 cells both in the absence and in the presence of exogenous TNFα, used as NF-κB pathway inducer. This anti-inflammatory effect was even more potent compared to Apigenin (APG1) and was confirmed using monocyte-derived THP-1 cells treated with LPS to stimulate NF-κB-dependent transcription of IL-6 and TNFα mRNAs. Apigenin7-O-β-(6''-methylglucuronide) (APG2) was instead inactive both in HCT116 and THP-1 cells. BEL (oral, 200 mg/kg) led to paw swelling inhibition, vascular permeability and peritoneal leukocyte and PN migration diminution. Apigenins (intraperitoneal, APG1, APG2: 20 mg/kg) also evoked a significant anti-edema effect, early vascular permeability and leukocyte influx reduction. Collectively, this study demonstrates for the first time the effectiveness of L. duriusculum to inhibit NF-κB-dependent transcriptional responses in HCT116 and THP-1 cells. In vivo studies also established that L. duriusculum possesses a potential anti-inflammatory effect, confirm its traditional, empirical use, that could be attributed to its richness in apigenin.

Chemical Constituents, Antioxidant, Anticholinesterase and Antiproliferative Effects of Algerian Pistacia atlantica Desf. Extracts.

BACKGROUND: Pistacia atlantica Desf. (Anacardiaceae) has various applications for dietetic and medicinal purposes. OBJECTIVE: The aim of the present study was to evaluate antioxidant, antiproliferative and anticholinesterase activities of different extracts from leaf and stem of Pistacia atlantica Desf. METHODS: The antioxidant activity was performed by four methods: DPPH, ABTS, CUPRAC and reducing power assays. Anti-cholinesterase activity was performed against acetylcholinesterase (AChE) and Butyrylcholinesterase (BuChE) enzymes. Antiproliferative assays were investigated against HeLa cell lines using xCELLigence RTCA instrument. The secondary metabolites composition was established by HPLC-TOF/MS analysis. RESULTS: In DPPH, reducing power and in ABTS .+ scavenging activity, all the extracts showed strong inhibitory activity compared to synthetic antioxidants such as butylated hydroxytoluene (BHT) and butylated hydroxyanisole (BHA), in which the activities were almost equal to the two standards. The results were less significant in CUPRAC assay. The ethyl acetate (EtOAc) extracts exhibited the best antioxidant activity in all tests. Moreover, P. atlantica extracts inhibited AChE and BChE activities in a dose-dependent manner. The strongest AChE and BuChE inhibition activities were obtained for EtOAc extract of the stem (IC50 values 15.14±0.74 and 24.01±0.21 µg/mL, respectively) compared to galantamine (IC50 values 6.27±1.15 and 34.75±1.99 µg/mL, respectively). P. atlantica extracts also showed significant antiproleferative activity against HeLa cell lines, the best antiproleferative activity was obtained for the methanol and EtOAc extracts. The observed biological activities can be attributed to the presence of phenolic compounds and flavonoids in the extracts. The HPLC-TOF/MS analysis identified the presence of 22 phytochemicals. Gallic acid and rutin were the main compounds detected. Cichoric, gentisic, vanillic, protocatechuic and rosmarinic acids as well as catechin and quercetin were also present. CONCLUSION: This study demonstrated good antioxidant, anticholinesterase and antiproliferative activities of P. atlantica extracts, which opens up new possibilities for pharmaceutical and food industries.

Characterization of ethyl acetate and n-butanol extracts of Cymbopogon schoenanthus and Helianthemum lippii and their effect on the smooth muscle of the rat distal colon.

ETHNOPHARMACOLOGY RELEVANCE: Cymbopogon schoenanthus (C. schoenanthus) and Helianthemum lippii (H. lippii) are Saharan species found in the South West of Algeria, in the region of Bechar. Both plants are used in traditional medicine to treat gastrointestinal disorders. OBJECTIVE: The aim of our study was to characterize the composition of the ethyl acetate (EtOAc) and n-Butanol (n-BuOH) extracts of C. schoenanthus and H. lippii, and to elucidate and compare their effect on the reactivity of the rat distal colon. MAIN METHODS: The plants were macerated in a hydroalcoholic solution. After concentration, the aqueous solutions of the residues were submitted to liquid-liquid extractions to obtain EtOAc and n-BuOH extracts. The phenolic and flavonoid content of the extracts was determined by high performance liquid chromatography coupled with mass spectrometry with a time of flight analyzer (HPLC-TOF/MS). The effect of the extracts was tested on the rat distal colon, namely on the basal tone and on KCl- and Ach-induced precontracted preparations. RESULTS: HPLC-TOF/MS identified 32 phenols and flavonoids in the extracts. The four extracts relaxed the rat distal colon, the effect being noticed on the basal tone and on the KCl- and Ach-induced precontractions. The EtOAc and the n-BuOH extracts of H. lippii decreased the basal tone of the rat distal colon more markedly than the correspondent extracts of C. schoenanthus. Moreover, the n-BuOH extract of C. schoenanthus decreased the basal tone more markedly than the EtOAc extract of this plant but there was no difference between extracts of H. lippii. The EtOAc extracts of both C. schoenanthus and H. lippii totally reverted both the KCl- and the Ach-induced precontraction of the rat distal colon. However, the n-BuOH extracts of the two plants reverted the Ach-precontracted colon but not the colon that has been precontracted with KCl. CONCLUSION: Extracts of H. lippii contain a higher level of phenols compared to the extracts of C. schoenanthus. All extracts of C. schoenanthus and H. lippii caused marked relaxation of the isolated rat distal colon, either when applied directly or when tested over KCl- and Ach-induced precontraction. These results give support to the use of C. shoenanthus and H. lippii in traditional medicine, namely for gastrointestinal diseases.

Chemical constituents, in vitro antioxidant and antimicrobial properties of ethyl acetate extract obtained from Cytisus triflorus l'Her.

The present study investigates the phenolic composition, antioxidant and antimicrobial activities of an ethyl acetate extract from C. triflorus L'Her. The phytochemical study on the aerial parts of C. triflorus belonging to the Fabaceae family led to the isolation and structural elucidation of 5-Hydroxy-7-O-glucosylflavone (P1), 5-Hydroxy-7-O-galactosylflavone (P2), 5,7-Dihydroxy-flavone (P3), 5,7,3'-Trihydroxy,4'-methoxy-flavone (P4). These compounds were identified by 1D and 2D NMR combined analysis as well as by UV.Ethyl acetate extract of C. triflorus showed a significant and dose-dependent antioxidant activity in vitro, related to the presence of phenolics (180.33 ± 12.22 µg GAE/mg) and flavonoids (16.78 ± 1.54 µg QE/mg). The antimicrobial activity was evaluated in vitro against Staphylococcus aureus CECT 240 and Escherichia coli CECT 4099, by agar-diffusion method. The most active antibacterial activity was expressed by ethyl acetate extract of C. triflorus against Gram-positive bacteria S. aureus. The gathered results suggest that C. triflorus polyphenols and flavonoids are closely associated to its antioxidant and antimicrobial properties.

Anti-inflammatory and Antioxidant Effects of Lotus corniculatus on Paracetamol-induced Hepatitis in Rats.

BACKGROUND: Herbal medicines have been used in the treatment of liver diseases for a long time. The current study was elaborated to evaluate in vitro and in vivo antioxidant and anti-inflammatory effects of Lotus corniculatus (L. corniculatus) butanolic extract. METHODS: The in vitro antioxidant and anti-inflammatory properties of L. corniculatus were investigated by employing DPPH radical scavenging, H2O2 scavenging and BSA denaturation assays. In vivo antioxidant and anti-inflammatory effects of L. corniculatus were evaluated against paracetamol (APAP)-induced hepatitis in rats. L.corniculatus at doses of 100 and 200 mg/kg was administered orally once daily for seven days. Serum transaminases (AST and ALT) and lactate dehydrogenase (LDH), total bilirubin levels, liver malondialdehyde (MDA), reduced glutathione (GSH), glutathione S- transferase (GST) and superoxide dismutase (SOD) levels and inflammatory markers, such as serum Creactive protein (CRP), circulating and liver myeloperoxidase (MPO) levels were investigated. Further histopathological analysis of the liver sections was performed to support the effectiveness of L. corniculatus. RESULTS: L. corniculatus exhibited strong antioxidant and anti-inflammatory effects in vitro. In the in vivo study, our findings demonstrate that L. corniculatus (100 and 200 mg/kg) administration led to an amelioration of APAP effects on liver histology, liver functions parameters (AST, ALT, LDH, and total bilirubin levels) and liver oxidative stress markers (MDA, GSH, GST and SOD levels). Furthermore, serum CRP, circulating MPO and liver MPO levels were declined by both doses of L. corniculatus extract. The best benefits were observed with 200 mg/kg of L. corniculatus extract. CONCLUSION: Antioxidant and anti-inflammatory effects of L. corniculatus extract may be due to the presence of active components.

Chemical composition, in vitro antiparasitic, antimicrobial and antioxidant activities of Frankenia thymifolia Desf.

This study was performed on the derived fractions [chloroform (FT-C), ethyl acetate (FT-E) and n-butanol (FT-B)] of the 70% ethanol extract prepared from Frankenia thymifolia, endemic to North Africa. The fractions showed high total phenolic and flavonoid contents particularly FT-E. These results agreed with their antioxidant effects. Indeed, all the fractions were able to scavenge 1,1-diphenyl-2-picrylhydrazyl radical, with a better power of FT-E. These results were supported by the inhibition of ß-carotene oxidation assay. The fractions showed moderate activity against Acanthamoeba castellanii and Leishmania amazonensis with a better activity of FT-E against A. castellanii. Moreover, FT-B exhibited an interesting antimicrobial activity against all tested bacteria. The phytochemical investigation of the most active fractions (FT-E and FT-B) led to the isolation and structural determination of six compounds. The observed biological activities may be associated with the presence of quercetin and its derivatives found in the chemical composition of these fractions.

On-line screening and identification of polyphenolic antioxidant compounds of Convolvulus trabutianus.

Convolvulus trabutianus Schweinf. & Muschl. is an endemic plant from northern Sahara used in folk medicine. Herein we report, the isolation, characterization and evaluation of the radical scavenging properties of twenty three compounds from different extracts of this species by on-line HPLC-ABTS•+ screening. These compounds include nine phenolic acids: 2, 6, 10-16, two phytosterols: 3-4, four coumarins: 5, 7-9, two quinic acids: 21 and 22 and six flavonoids: 1, 17-20 and 23 among which the most active were: 10, 16, 21 and 22. All the extracts showed a significant antioxidant activity on-line. These results were validated off-line by ORAC and TEAC assays. Four compounds: 1, 5, 18 and 19 were described for the first time from the Convolvulaceae family, whereas compounds 2, 6, 8, 10, 13 and 21 were new for the genus Convolvulus.

Antioxidant and Leishmanicidal Evaluation of Pulicaria Inuloides Root Extracts: A Bioguided Fractionation.

Leishmaniasis remains a major world health problem, and in particular, Algeria ranks second for the incidence of cutaneous leishmaniasis. Pulicaria inuloides is a well-known Arabian Peninsula medicinal plant. In the present study, the chloroform, ethyl acetate and n-butanol extracts from the roots of Pulicaria inuloides were analyzed for antioxidant activity and its correlation with the total phenolic and flavonoid contents. The highest antioxidant activity using a DPPH assay was showed by the ethyl acetate extract (IC50 4.08 µg/mL), which also had the highest total phenolic content (307.12 µgAGE). Furthermore, P. inuloides root extracts were evaluated against Leishmania amazonensis and Leishmania donovani. The results highlighted the chloroform extract as the most active one against both tested Leishmania strains. A bioguided fractionation of the chloroform extract led to the isolation of (8R:8S)-(75:25 er)-10-isobutyryloxy-8,9-epoxy-thymol isobutyrate as the main bioactive component, showing a potent leishmanicidal activity on L. amazonensis promatigote and amastigote stages (IC50 5.03 and 2.87 µM, respectively) and a good selectivity index on murine macrophages (CC50 19.37 µM). This study provides the first report of the antioxidant and leishmanicidal activities of P. inuloides root extracts and the results point to this species as a source of potential bioactive agents.

In vitro antioxidant, DNA-damaged protection and antiproliferative activities of ethyl acetate and n-butanol extracts of Centaurea sphaerocephalaL.

This study aimed to evaluate the in vitro antiproliferative and inhibition of oxidative DNA-damage activities of n-butanol (n-BuOH) extract of Centaurea sphaerocephala. The in vitro antioxidant activity of the ethyl acetate (EtOAc) and the n-BuOH extracts of this plant were also assayed. To investigate the antioxidant potential, extracts were tested for their capacity to scavenge 1,1-diphenyl-2-picrylhydrazyl (DPPH·) and to inhibit lipid peroxidation using the TBARs method. The contents of total phenolics and flavonoids were measured. Additionally, antiproliferative activity and DNA-damage inhibition of the n-BuOH extract was determined using XCELLigence RTCA instrument and photolyzing 46966 plasmid, respectively. The results exhibited that the scavenging abilities of the EtOAc extract were better than the n-BuOH extract with an IC50= 11.59 µg/mL and 16.67 µg/mL for both extracts, respectively. The phenolic and flavonoid contents were found higher in the n-BuOH and EtOAc extracts. Furthermore, our results showed that n-BuOH extract exhibited a remarkable inhibition of lipid peroxidation with an IC50 of 340.94±7.49 µg/mL and had an antiproliferative effect against Hela cells. Extracts of C. sphaerocephala showed antioxidant activity on scavenging DPPH·. In addition, the n-BuOH extract inhibited the lipid peroxidation and exhibited an antiproliferative effect against HeLa cells line (human cervix carcinoma).

Hepatoprotective effects of the n-butanol extract from Perralderia coronopifolia Coss. against PCP-induced toxicity in Wistar albino rats.

In the present study, in vivo antioxidant properties of the n-butanol extract obtained from aerial parts of Perralderia coronopifolia were investigated in term of its hepatoprotective effect of female Wistar albino rats (n, 36; average age, 48 ± 5 days; weighing 150 ± 18 g) against PCP (pentachlorphenol)-induced toxicity. PCP (20 mg/kg b.w.) and plant extract (50 mg/kg b.w.) were administered daily by gavages for 2 weeks. Vitamin E (100 mg/kg b.w.) was given intraperitoneally as a positive control. Lipid peroxidation (LPO) levels, reduced glutathione (GSH) levels, and glutathione peroxidase (GPx) activities were evaluated in liver homogenates. While, aspartate aminotransferase (AST), alanine aminotransferase (ALT), cholesterol, and triglyceride parameters were analyzed in serums. The liver fragments were observed using light microscopy. Experimental results exhibited that PCP-treated group has a significant increase in the liver lipid peroxidation (LPO) levels of animals while decreased in plant extract-treated group. In addition, PCP caused significant decreases in glutathione peroxidase (GPx) activities and reduced glutathione (GSH) levels. Moreover, PCP induced hepatotoxicity by increasing serum transaminase enzymes, cholesterol, and triglyceride levels. While, these levels were restored to control value in animals treated with plant extract. The regularized levels of LPO, GSH, cholesterol, triglyceride, transaminase enzymes, and GPx activities revealed the antioxidant properties of the extract plant as well as of the vitamin E. The histological study showed the hepatoprotective effect of our extracts against PCP-induced acute intoxication, protecting the hepatic architecture and decreasing the functional and structural alterations of the liver. The plant extract had high antioxidant potential and completely prevented the toxic effect of PCP on the above of liver and serum parameters.

Antioxidant and anti-inflammatory activity of phenolic extracts of Genista ferox (Fabaceae).

Phenolic extracts of aerial parts of Genista ferox have been characterized and evaluated for their pharmacological properties which are still not reported. The total phenol and flavonoid contents in the extracts were estimated spectrophotometrically via the Folin-Ciocalteu and aluminium chloride methods, respectively. Leaves and pods extracts showed the highest contents of total phenols and total flavonoids. The same extracts exhibited also the highest antioxidant capacity (IC50 of 105.37µg/mL and 113.98µg/mL, respectively) assessed by the in-vitro DPPH radical scavenging method. Leave and stem extracts were explored for their possible anti-inflammatory activity assayed by carrageenan-induced paw edema model. Both extracts (at 400mg/kg) showed edema inhibitory effect, which was found to be close to that of Dichlofenac reference. However, the leave extract produced the highest significant (p<0.001) anti-inflammatory activity when compared with the control. A preliminary characterisation of these phenolic extracts were carried out by high performance liquid chromatography (HPLC) coupled with diode-array detector (DAD), in order to determine the relevance of identified compounds in the pharmacological properties of the plant.

Amino acid-sesquiterpene lactone conjugates from the aerial parts of Centaurea pungens and evaluation of their antimicrobial activity.

Two new amino acid-sesquiterpene lactone conjugates, named centaureolide A (1) and centaureolide B (2) along with a germacrane derivative (3), five flavonoids (4-8) and one quinic acid derivative (9) have been isolated from the aerial parts of Centaurea pungens (Asteraceae). Their structures were established by a combination of one- and two-dimensional NMR techniques, and mass spectrometry. The never reported sesquiterpene lactones have been determined as germacrane derivatives (1 and 2) characterized by the unusual occurrence of a proline moiety. In order to validate the use of the extract of C. pungens in folk medicine, the antimicrobial activity of the isolated compounds against the Gram-positive strains Bacillus cereus, Staphylococcus aureus and Listeria innocua and the Gram-negative strains Pseudomonas aeruginosa and Pseudomonas fragi was evaluated.