Chemical characterisation and hepatoprotective potential of Cosmos sulphureus Cav. and Cosmos bipinnatus Cav.

This study was conducted to validate the hepatoprotective activity of Cosmos sulphureus and Cosmos bipinnatus. Aqua-methanolic extracts of both plants were evaluated for the presence of various phyto-constituents through HPLC. Different doses of both plant extracts were administered to rats for nine days. Standard control was silymarin 100 mg/kg. Paracetamol 1 gm/kg was administered 3 h post treatment on 9th day for induction of hepatotoxicity. Blood was collected for the evaluation of liver biochemical markers and livers were removed for histopathological evaluation 24 h post-paracetamol treatment. HPLC analysis revealed the presence of quercetin, gallic acid, caffeic acid and chlorogenic acid in both plant extracts. The extracts of both plants decreased the level of alanine aminotransaminase and total bilirubin significantly (p < 0.05), dose dependently and protected hepatocytes from paracetamol-induced hepatotoxicity. It can be concluded that both plants may possess hepatoprotective activity possibly due to the presence of quercetin and phenolic compounds.     

Effects of aqueous extracts of Acacia albida stem bark on Wistar albino rats infected with Trypanosoma evansi

The effect of aqueous extract of Acacia albida stem bark was investigated in Wistar albino rats infected with Trypanosoma evansi. The extract showed highest reduction in parasitemia at the dose of 600 mg/kg body weight (bw). A dose of 300 mg/kg bw improved packed cell volume the most by 14.35%. The group treated with 150 and 600 mg/kg bw of the extract showed significant decrease (P < 0.05) in alanine transaminase and aspartate transaminase levels which were lower than those of the group treated with diminazene aceturate. The group treated with 150 mg/kg bw of the extract showed the least urea, albumin and protein level and lowest relative organ weight. There was a significant difference (P < 0.05) in the levels of catalase and Thiobarbituric acid reactive substances in liver and kidney of the animals in the infected-untreated group and the extracts-treated groups. The results of this study show that the extracts of A. albida have antitrypanosomal activity against T. evansi infection.     

Evaluation of the Antioxidant and Hepatoprotective Effect of Phyllanthus fraternus Against a Chemotherapeutic Drug Cyclophosphamide

In the present study, hepatoprotective and antioxidant properties of aqueous extract of Phyllanthus fraternus (AEPF 200, 300, and 400 mg/kg body weight (bw), orally) were investigated against cyclophosphamide (CPA 200 mg/kg, bw, intraperitoneally administered) induced liver damage in mice. Histopathological studies of CPA administration cause liver injury, featuring substantial increase in serum glutamic oxaloacetic transaminase, serum glutamate pyruvate transaminase, lactate dehydrogenase, alkaline phosphatase, acid phosphatase, and total bilirubin. Moreover, CPA intoxication also causes strong oxidative stress, which is evident from significant increase in lipid peroxide level. These changes were coupled with a decline in superoxide dismutase and catalase as well as albumin, cholesterol level, red blood cell (RBC), and white blood cell (WBC) count. AEPF-treated mice displayed a significant inhibition of lipid peroxidation and augmentation of endogenous antioxidants. The study emphasizes the hepatoprotective effect of AEPF against CPA-induced oxidative liver injury, which may serve as a promising medicinal herb in complementary chemotherapeutic modalities.     

A new triterpene and protective effect of Periploca somaliensis Browicz fruits against CCl4-induced injury on human hepatoma cell line (Huh7)

The potential hepatoprotective effect of the methanolic extract of Periploca somaliensis Browicz fruits, its different fractions (n-hexane, chloroform and n-butanol) and the major isolated compound ursolic acid was evaluated using the human hepatoma cell line (Huh7) based on the changes in the activity of aspartate aminotransferase, alanine transaminase, glutathione and superoxide dismutase. Each sample was tested at three different concentrations (1000, 100 and 10 μg/mL). All tested samples exhibited a potent concentration-independent cytoprotective effect relative to silymarin as a reference standard. Chromatographic fractionation of the chloroform-soluble fraction of the methanol extract of P. somaliensis Browicz fruits afforded two known triterpenes, namely ursolic acid, and 11α,12α-epoxy-3β-hydroxy-olean-13β,28-olide, and a newly discovered one, namely 3β-hydroxy-urs-11-en-13β,28-olide. The structures of the isolated compounds were elucidated by the analysis of 1D and 2D NMR spectral data.     

Hepatoprotective effect of chiisanoside against acetaminophen-induced acute liver injury in mice

This study was designed to investigate the hepatoprotective effect of chiisanoside (CSS) and its possible mechanisms on acetaminophen (APAP)-induced acute liver damage in mice. The serum activities of alanine transaminase (ALT), aspartate transaminase (AST), tumor necrosis factor alpha (TNF-α), interleukin-1 beta (IL-1β), interleukin-6 (IL-6), and the hepatic levels of superoxide dismutase (SOD), catalase (CAT), glutathione (GSH) and malondialdehyde (MDA) were determined using the commercially available assay kits. The hepatic mRNA levels were measured by RT-PCR. The hepatic protein expressions of nuclear factor-kappa B (NF-κB), MAPK and their phosphorylated isoforms were evaluated by western blot assays. The results indicated that CSS (240 mg/kg) exhibited the hepatoprotective effects by inhibiting oxidative stress and inflammation on APAP-induced acute liver injury. Furthermore, the anti-inflammatory activity of CSS is largely related to the regulation of the NF-κB and MAPKs signaling pathways. These findings suggested that CSS possessed hepatoprotective effect against APAP-induced hepatotoxicity in mice.     

Enhancement of the Protective Activity of Vanillic Acid against Tetrachloro-Carbon (CCl4) Hepatotoxicity in Male Rats by the Synthesis of Silver Nanoparticles (AgNPs)

In the current study, the hepatoprotective activity of vanillic acid, silymarin, and vanillic acid-loaded silver nanoparticles (AgNPs) against CCl₄-induced hepatotoxicity was tested in male rats for four weeks. Thirty male rats were divided into five groups (n = 6). The 1st group was a negative control, the 2nd group was a positive control, the 3rd group was treated with 100 mg/kg b.w. of vanillic acid, the 4th group was treated with 100 mg/kg b.w. of vanillic acid–AgNPs, and the 5th group was treated with 50 mg/kg b.w. of silymarin. The CCl₄-induced hepatic toxicity in the 2nd group was revealed by the liver function and all other biochemical tests. Liver enzymes, bilirubin, lipid peroxidation, lactate dehydrogenase, and interleukin-6 were elevated, whereas, total protein, antioxidant enzymes, and irisin were decreased compared to the negative control. The hepatic tissues were also injured as a result of the CCl₄-induced hepatotoxicity. Treating the hepatotoxic rats with vanillic acid moderately protected the rats of the 3rd group, whereas treatment with vanillic AgNPs and silymarin in G4 and G5, respectively, greatly protected the rats against the CCl₄ hepatotoxicity, approaching the normal biochemical levels and liver tissue appearance. The biochemical tests were confirmed by the histological investigations of liver tissue.     

Chemical composition,protoscolicidal effects and acute toxicity of Pistacia atlantica Desf. fruit extract

The present study was designed to evaluate the chemical composition and scolicidal effects of Pistacia atlantica Desf. extract against protoscoleces of hydatid cysts and its acute toxicity in mice model. Various concentrations of the methanolic extract (5–50 mg/mL) were used for 10–60 min. Viability of protoscoleces was confirmed using eosin exclusion test (0.1%). Acute toxicity was also determined in mice model. The main components were β-myrcene (41.4%), α-pinene (32.48%) and limonene (4.66%). Findings demonstrated that P. atlantica extract at the concentrations of 25 and 50 mg/mL after 20 and 10 min of exposure killed 100% protoscoleces. The LD₅₀ of the intraperitoneal injection of the P. atlantica methanolic extract was 2.43 g/kg and the maximum non-fatal dose was 1.66 g/kg. Obtained results showed the potential of P. atlantica extract as a natural source with no significant toxicity for the production of new scolicidal agent to use in hydatid cyst surgery.     

Distribution of free amino acids,polyphenols and sugars of Ziziphus jujuba pulps harvested from plants grown in Tunisia

Ziziphus jujuba pulps are very much appreciated by the inhabitants and have been recently exported. This article reports on the chemical composition (amino acids, polyphenols and sugars) of the pulps of four Z. jujuba ecotypes (Choutrana, Mahdia, Mahres and Sfax). The major amino acids identified were proline, aspartic acid and glutamic acid. Among these, proline was the most abundant amino acid (17.4 mol). Considerable differences in total phenolic contents (15.85 mg/L) were found. Predominant phenols identified by using HPLC were rutin (1.09 mg/L) and chlorogenic acid (2.57 mg/100 g). Sugars isolated from Ziziphus pulps were found at a rate of 43.52%. Using HPLC method, three sugars from the pulp extract were identified: glucose, galactose and sucrose. The Mahdia ecotype was the richest in these sugars with 0.45, 136.51 and 113.28 mg/L, respectively.     

Phytochemical characterisation and bioprospection for antibacterial and antioxidant activities of Lippia alba Brown ex Britton & Wilson (Verbenaceae)

Ethanol extract and fractions obtained from fresh and dry aerial parts of Lippia alba were examined in order to determine their phytochemical composition, antioxidant capacity and antibacterial activities. The ethanol extracts and fractions exhibited an antioxidant effect by the DPPH assay, especially samples of fresh plant. HPLC analysis of the ethyl acetate fractions identified the presence of phenolic acids and flavonoids. The ethanol extract and fractions showed activity against reference and multidrug-resistant strains of Staphylococcus aureus and Enterococcus faecalis (MIC range 2000–250 μg/mL). The hexane and dichloromethane fractions of fresh plant showed better activity against reference strains of Escherichia coli (MIC of 250 and 125 μg/mL, respectively), but all extracts and fractions were less active against multidrug-resistant strains of all the Gram-negative species evaluated. The results showed that the extract and fractions of L alba aerial parts showed antibacterial activity, even against multidrug-resistant Gram-positive bacteria, and antioxidant effect (DPPH assay).     

Antioxidant Extract from Cleistocalyx nervosum var. paniala Pulp Ameliorates Acetaminophen-Induced Acute Hepatotoxicity in Rats

The indigenous purplish red fruit, Cleistocalyx nervosum var. paniala (CN), is grown in northern Thailand. The aqueous extract of CN pulp is known to exhibit antioxidant and anticarcinogenic properties. To search for an antioxidant fraction separated from CN, various hydroalcoholic extractions were performed. The acidified ethanolic extract of CN obtained from 0.5% (v/v) citric acid in 80% (v/v) ethanol yielded greater polyphenol content and DPPH radical scavenging activity when compared with other hydroethanolic extracts. Cyanidin-3-glucoside is a major anthocyanin present in the acidified ethanolic extract of CN (AECN). At a dose of 5000 mg/kg bw, an anthocyanin-rich extract was found to be safe when given to rats without any acute toxicity. To examine the hepatoprotective properties of AECN, an overdose of acetaminophen (APAP) was induced in a rat model, while silymarin was used as a standard reference. The administration of AECN at a dose of 300 mg/kg bw for 28 days improved hepatocyte architecture and modulated serum alanine aminotransferase levels in APAP-induced rats. Furthermore, it significantly decreased serum and hepatic malondialdehyde levels but increased hepatic glutathione content, as well as glutathione peroxidase and UDP-glucuronosyltransferase activities. In conclusion, AECN may effectively reduce oxidative stress induced acute hepatotoxicity in overdose APAP-treated rats through the suppression of oxidative stress and the enhancement of the antioxidant system in rat livers.     

Chemical constituents and protective effect of Ficus ingens (Miq.) Miq. on carbon tetrachloride-induced acute liver damage in male Wistar albino rats

The aim of the present study was to investigate the chemical constituents and hepatoprotective effect of Ficus ingens (Miq.) Miq. (Moraceae) extract against carbon tetrachloride-induced acute liver damage in male Wistar albino rats. The ethanol extract of F. ingens, was subjected to phytochemical study. In addition, its acute and sub-chronic toxicities were assessed. Eight compounds were isolated from this plant and identified as β-sitosterol, β-sitosterol glucoside, chryasophanol, 7-hydroxy-2,5 dimethyl chromen-4-one, quercetin, Aloe emodin glucoside, rutin and Patuletin-3′-O-methyl-3-O-rutinoside. The structure elucidation was based on ¹H and ¹³C NMR, proton–proton correlation spectroscopy (¹H–¹H Cosy), distortionless enhancement by polarization transfer (DEPT), Heteronuclear Multiple-Quantum Correlation (HMQC), and heteronuclear multiple bond correlations spectrum (HMBC). Hepatotoxicity induced with CCl₄ was evidenced by elevation of liver marker enzymes (ALT, AST, ALP and LDH) and TB content in serum. In addition, antioxidant enzymes were drastically inhibited with significant reduction of GSH and increased LPO in liver homogenate of CCl₄-intoxicated rats. Pre-treatment with F. ingens (200 and 400 mg/kg) and silymarin (50 mg/kg) avoided the changes observed in CCl₄-intoxicated rats. In conclusion, the ethanol extract of F. ingens showed protective activity against liver injury, which might be developed into a new hepatoprotective agent.     

GC–MS characterisation and biological activity of essential oils from different vegetative organs of Plectranthus barbatus and Plectranthus caninus cultivated in north Italy

Essential oils (EOs) from the roots, stems and leaves of Plectranthus barbatus (A) and Plectranthuscaninus (B), cultivated in north Italy, were obtained by steam distillation and chemically characterised by gas chromatography–mass spectrometry. The highest yields were obtained from roots (268.15 and 673.60 mg/kg from A and B), followed by leaves (64.34 and 26.65 mg/kg) and stems (19.76 and 18.63 mg/kg). A total of 128 structures were identified in A and 121 in B. Fe⁺⁺ chelating and antiradical activities (DPPH and ABTS) were evaluated: root and stem EOs showed the strongest activities, while EOs from leaves did not show relevant activities. All EOs were tested for their in vitro antimicrobial activity, showing optimal growth-inhibition in antibiogram (?>35 mm) and MIC tests (32–64 μg/mL) against Candida albicans, while EOs from leaves of both species showed a good activity (25 < ? < 34 mm, MIC 64–128 μg/mL) against Escherichia coli.     

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).     

Acute and sub-acute toxicological evaluation of the alcoholic leaf and root extracts of Clerodendrum infortunatum L.

Leaf and root extracts of Clerodendrum infortunatum L. have been reported to show anthelmintic efficacy on a cestode parasite Raillietina tetragona. Its leaf showed no toxicity at 1000 mg/kg body weight but root toxicity study was not known. Therefore, our study is to test both leaf and root extracts at 2000 and 3000 mg/kg body weight concentration given orally for 15 days in four groups of Swiss albino mice, keeping another set as control (without plant extract). Weight and behaviour of mice were recorded daily. Feeding, movement pattern were normal in all treatments as that of control. Though body weight increase, there was no change in the relative organ weight. Biochemical and haematological studies revealed no significant change from control and no alteration in histopathological study of liver and kidney from that of control. The plant extracts thus shown to be safe for consumption.     

Antihyperglycemic,antihyperlipidemic and antioxidative evaluation of compounds from Senna sophera (L.) Roxb in streptozotocin-induced diabetic rats

Senna sophera (L.) Roxb (Common name: Kasunda, Baner) (Leguminosae) is used as traditional medicine in Africa and Asia. The compounds were isolated from methanolic extract of leaves of Senna sophera (MFCS). Compound A was identified as Hexahydroxy diphenic acid and Compound B as Kaempferol. MFCS administration to diabetic rats exhibited significant reduction in the blood sugar level and showed gain in body weight. After the treatment of 100 mg/kg of MFCS, the blood sugar level was reduced to 52.33 ± 2.83 mg/dl in comparison to the blood sugar level of vehicle control 76.66 ± 3.17 mg/dl, whereas treatment with 50 mg/kg of MFCS reduced the blood sugar level slightly (72.33 ± 2.42 mg/dl). The daily continuous administration of MFCS for a period of 21 days normalised the serum lipid levels confirming the effect of MFCS on diabetic hyperlipidemia. Treatment with MFCS also reversed the activities of antioxidants, which could be a result of decreased lipid peroxidation.     

Bioactive compounds content and their biological properties of acetone extract of Cuscuta reflexa Roxb. grown on various host plants

The present study is aimed to evaluate the total phenolic and flavonoid contents, and free phenolic compounds of acetone extract of Cuscuta reflexa grown on five different hosts: Coccinia grandis, Ficus racemosa, Samanea saman, Streblus asper and Zollingeria dongnaiensis, and to explore the antioxidant activities, α-glucosidase and tyrosinase inhibitory properties of the extracts. The highest level of total phenolic and flavonoid contents were observed in the extract of C. reflexa that was grown on S. asper (65.45 mg GAE/g extract) and C. grandis (97.83 mg QE/g extract), respectively. According to HPLC results, vanillic acid, rutin and quercetin were found in all extracts of C. reflexa grown on diversified hosts. The extract of C. reflexa grown on C. grandis possessed the greatest antioxidant activities (DPPH; 251.64 μg/mL, FRAP; 26.44 mg GAE/g extract), α-glucosidase inhibition accounted for 84.36 per cent and antityrosinase activity was at 18.29 mg KAE/g sample.     

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.     

In Vitro and In Vivo Protective Effects of Lentil (Lens culinaris) Extract against Oxidative Stress-Induced Hepatotoxicity

Excessive oxidative stress plays a role in hepatotoxicity and the pathogenesis of hepatic diseases. In our previous study, the phenolic extract of beluga lentil (BLE) showed the most potent in vitro antioxidant activity among extracts of four common varieties of lentils; thus, we hypothesized that BLE might protect liver cells against oxidative stress-induced cytotoxicity. BLE was evaluated for its protective effects against oxidative stress-induced hepatotoxicity in AML12 mouse hepatocytes and BALB/c mice. H₂O₂ treatment caused a marked decrease in cell viability; however, pretreatment with BLE (25–100 μg/mL) for 24 h significantly preserved the viability of H₂O₂-treated cells up to about 50% at 100 μg/mL. As expected, BLE dramatically reduced intracellular reactive oxygen species (ROS) levels in a dose-dependent manner in H₂O₂-treated cells. Further mechanistic studies demonstrated that BLE reduced cellular ROS levels, partly by increasing expression of antioxidant genes. Furthermore, pretreatment with BLE (400 mg/kg) for 2 weeks significantly reduced serum levels of alanine transaminase and triglyceride by about 49% and 40%, respectively, and increased the expression and activity of glutathione peroxidase in CCl₄-treated BALB/c mice. These results suggest that BLE protects liver cells against oxidative stress, partly by inducing cellular antioxidant system; thus, it represents a potential source of nutraceuticals with hepatoprotective effects.     

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.     

Morus alba Prevented the Cyclophosphamide Induced Somatic and Germinal Cell Damage in Male Rats by Ameliorating the Antioxidant Enzyme Levels

Cytogenetic analysis is essential to determine the effect of mutagens and antimutagens on genetic material. This study was done to evaluate the protective effect of root bark extract of Morus alba (M. alba) against cyclophosphamide induced somatic and germinal cell damage in male rats. The ethanolic extract of M. alba (0.25, 0.5 and 1 g/kg, 2 weeks) was evaluated against cyclophosphamide (75 mg/kg, single dose) induced nuclear damage. The sampling was done after 48 h of the clastogen treatment. The somatic and germinal nuclear damage was studied by bone marrow micronucleus and sperm analysis, respectively. Serum superoxide and catalase levels were estimated to determine the antioxidant status in each group. The results were analyzed statistically to find the significant variation. The administration of M. alba for 2 weeks suppressed dose-dependently the changes induced by cyclophosphamide. M. alba (0.5 g/kg) decreased the frequency of micronucleated erythrocyte, sperm shape abnormality and enhanced the sperm count, sperm motility and polychromatic-normochromatic erythrocytes ratio significantly (p < 0.05) in comparison with the cyclophosphamide treated group. The highest tested dose of M. alba (1 g/kg) produced more prominent suppression (p < 0.01) in the cyclophosphamide-induced somatic and germinal cell defects. The results also showed significant (p < 0.05) improvement in the serum antioxidant enzymes levels with M. alba when compared with the challenge group. The lower dose of M. alba extract (0.25 g/kg) prevented the CP-induced changes but was found to be statistically insignificant. Therefore, antimutagenic potential of the high dose of the extract of M. alba is possibly due to its antioxidant nature. The ability of the M. alba extract to prevent the nuclear damage could play an important role in overcoming several mutational defects that are associated with anticancer chemotherapy.