Genista cephalantha Spach. protects against acetaminophen-induced liver failure via preserving the glutathione redox system, reducing inflammatory response, and inhibiting hepatocyte death in rats.

Objectives: The current study was conducted to assess the protective mechanisms of n-BuOH fraction from the aerial part of Genista cephontala (BEGC) on APAP-induced liver injury compared to necrostatine-1 (Nec-1). Materials and Methods: A model of APAP-induced hepatotoxicity was created in male rats by injecting a single dose; 1000 mg/kg APAP, the protective effect was performed with (200 mg/kg; 10 days) BEGC compared to Nec-1, (1.8 mg/kg). Results: BEGC or NeC-1 pretreatment significantly abolished impaired effects in APAP-rats, by decreasing the generation of TBARS and ROS in mitochondrial and cytosolic fractions and maintaining liver function activities. A marked response was observed in the levels of both GSH and GSH-system enzymes in liver homogenates and mitochondrial fractions to BEGC. BEGC/ Nec-1 successfully regulated the inflammatory mediators (IL-ß, TNF-α, HMGB1, and acHMGB1) and MPO levels. During APAP treatment, no caspase-3 or -8 activity was detected, and the level of fk18; M30 was higher than the levels of cck18; M65. Moreover, RIPK3 and MLKL levels were increased in the APAP group. These results suggested that necroptosis predominates during the APAP liver injury model. Interestingly, these necroptotic factors were significantly down-regulated by BEGC treatment. Both biochemical and histopathological findings were consistent with each other. Conclusion: From all these findings, the hepatoprotective effect of BEGC could be due to the abundance of polyphenols identified by LC-MS/MS analysis, as well as the synergistic interactions of all contents.

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).

Chemical constituents and HRESI-MS analysis of an Algerian endemic plant - Verbascum atlanticum batt. - extracts and their antioxidant activity.

This is the first report on the phytochemistry and antioxidant activity of ethyl acetate and n- butanol extracts from an Algerian endemic plant Verbascum atlanticum Batt. (Scrophulariaceae). Both extracts were subjected to a phytochemical study by semi-preparative HPLC, which led to the isolation and identification of nine compounds: methyl linolenate (1), methyl linoleate (2), Phytol-1(3), Martynoside (4), Isomartynoside (5), Cis-martynoside (6), Ilwensisaponin C (7), Ilwensisaponin B (8), Ilwensisaponin A (9). In addition, the fractions from both extracts were analysed by LC-UV-MS and HRESI-MS. This later revealed the presence of eight other metabolites by using a comparison with known microbial metabolites data. Finally, both extracts were estimated for their phenolic and flavonoid contents as well as the evaluation of their antioxidant activity using five different assays DPPH, CUPRAC, reducing power, ß-carotene bleaching and superoxide DMSO alkaline. The results showed that the ethyl acetate extract had the most antioxidant effect.

Chemical constituents, cytotoxic, antifungal and antimicrobial properties of Centaurea diluta Ait. subsp. algeriensis (Coss. & Dur.) Maire

Objective To investigate the chemical composition of a moderately polar extract (CHCl

Chemical constituents, cytotoxic, antifungal and antimicrobial properties of Centaurea diluta Ait. subsp. algeriensis (Coss. & Dur.) Maire

OBJECTIVE@#To investigate the chemical composition of a moderately polar extract (CHCl3 soluble part of the MeOH-H2O extract) obtained from the aerial parts (leaves and flowers) of Centaurea diluta Ait. subsp. algeriensis (Coss. & Dur.) Maire, a species endemic to Algeria and Morocco on which no reports are available to date. To evaluate in vitro the cytotoxic, antifungal and antimicrobial activities of this extract and the cytotoxic and antimicrobial activities of its isolated secondary metabolites.@*METHODS@#The cytotoxic effects of the extract were investigated on 3 human cancer cell lines i.e. the A549 non-small-cell lung carcinoma (NSCLC), the MCF7 breast adenocarcinoma and the U373 glioblastoma using a MTT colorimetric assay. Biological data allowed to guide the fractionation of the extract by separation and purification on silica gel 60 (CC and TLC). The isolated compounds which were characterized by spectral analysis, mainly HR-ESIMS, HR-EIMS, UV and NMR experiments ((1)H, (13)C, COSY, ROESY, HSQC and HMBC) and comparison of their spectroscopic data with those reported in the literature, were evaluated for cytotoxic activities on six cancer cell lines (A549, MCF7, U373, Hs683 human glioma, PC3 human prostate and B16-F10 murine melanoma). The direct and indirect antibacterial and antifungal activities were determined using microdilution methods for the raw extract and TLC-bioautography and microdilution methods against standard and clinical strains for the isolated compounds.@*RESULTS@#The raw extract reduced cell viability with IC50s of 27, 25 and 21 μg/mL on A549, MCF7 and U373, respectively. Five secondary metabolites: two phenolic compounds (vanillin 1, paridol 3), a lignan [(-)-arctigenin 2] and two flavonoid aglycones (eupatilin 4 and jaceosidin 5), were then isolated from this extract. Moderate cytotoxic effects were observed for (-)-arctigenin 2 (IC50s: 28 and 33 μM on Hs683 and B16-F10, respectively), eupatilin 4 (IC50s: 33 and 47 μM on B16-F10 and PC3, respectively) and jaceosidin 5 (IC50s: 32 and 40 μM on PC3 and B16-F10, respectively).@*CONCLUSIONS@#All the isolated compounds were described for the first time from this species. Although inactive against 7 tested microorganisms (fungi, bacteria and yeast, human or plant pathogens), the raw extract was able to potentiate the effect of beta-lactam antibiotics on methicillin-resistant Staphylococcus aureus (MRSA), reducing the minimal inhibitory concentrations (MICs) by a factor of 2-32-fold. No synergy was found between the extract and streptomycin. From the five isolated compounds only jaseosidin 5 showed a moderate antimicrobial activity.