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Introduction: Pomegranate (Punica granatum L.) peels are rich in various bioactive compounds. Characterization of these compounds is crucial for the utilization of peel waste in industrial processing., Objective: The study aimed (1) to establish and compare the metabolic profiles of the peel of seven pomegranate cultivars and (2) to identify bioactive compounds contributing to the larvicidal activity against the third instar larvae of Culex pipiens., Materials and Methods: UPLC-ESI-MS/MS was utilized to analyze peel methanol extracts of different pomegranate cultivars. The larvicidal activity was determined by calculating the larval mortality among the third instar larvae of C. pipiens. Multivariate data analysis was conducted to identify the metabolites that exhibited a larvicidal effect., Results: A total of 24 metabolites, including hydrolyzable tannins, flavonoids, and alkaloids, were tentatively identified in both negative and positive ionization modes. The extract of cultivar 'Black' exhibited the most potent larvicidal effect with LC 50 values of 185.15, 156.84, and 138.12 ppm/mL after 24, 48, and 72 h of treatment, respectively. By applying chemometric techniques, the larvicidal activity could be directly correlated to the bioactive compounds punicalagin, quercetin-O-rhamnoside, quercetin-O-pentoside, and galloyl-HHDP-glucose., Conclusion: The present study implemented UPLC-ESI-MS/MS and chemometric techniques as potential tools for metabolomics analysis and differentiation between peels of different pomegranate cultivars. In addition, cultivar 'Black' extract could be a promising natural insecticide against mosquitoes since it is rich in bioactive compounds with larvicidal activity., (© 2023 John Wiley & Sons, Ltd.)

The plants belonging to the genus Vicia are of great interest as a source of many bioactive compounds and micronutrients. A snapshot of their cultivation, habitat, main components, from which essential oils can be obtained, is given. The traditional medicinal uses of Vicia plants are also reported, as well as the wide spectrum of the main biological activities attributed to Vicia plants is discussed regarding potential health beneficial properties, in particular anti-Parkinson, anticholinesterase, antidepressant, anticonvulsant, antimicrobial, cytotoxic, antioxidant, antiinflammatory and antinociceptive, antidiabetic, antihemolytic, anticoagulant, estrogenic, diuretic, antihypoxic activities., (© 2020 John Wiley & Sons Ltd.)

Ethnopharmacological Relevance: Members of the genus Erythrina have been traditionally used in the treatment of various ailments such as inflammation and gastrointestinal disorders. Erythrina speciosa (Fabaceae) is a spiny, deciduous shrub or small tree native to Southern America in Brazil. It is cultivated in Africa and Asia. The traditional usage of E. speciosa indicated its antibacterial, analgesic, and anti-inflammatory activities., Aim of the Study: Evaluation of the phytochemical constituents, gastroprotective effects and possible mechanism of action of the ethyl acetate fraction obtained from the methanol extract of E. speciosa leaves (ESLE)., Materials and Methods: Chemical characterization of ESLE was done using high performance liquid chromatography coupled to mass spectrometry (HPLC-MS). The gastroprotective activity of ESLE was evaluated using ethanol-induced gastric-ulcer model in rats. Rats were pre-treated with ESLE 25, 50 and 100 mg/kg 1 h before the administration of absolute ethanol. Histological analysis, mucin content, and total acidity were evaluated. The possible mechanism of action of ESLE was studied through the examination of oxidative stress and inflammatory markers, PGE2, and NF-κB, iNOS, COX-2, and HSP-70 immunoexpression. In vitro, anti-Helicobacter pylori activity of ESLE was also studied using micro-well dilution method., Results: Fourteen compounds were tentatively identified including alkaloids, flavonoids, and saponins. ESLE exerted a powerful gastroprotective effect. The pre-treatment with ESLE at different doses resulted in a significant reduction in gastric lesions and significant elevation in the mucin production. These effects could be partially mediated by the potent anti-inflammatory activity of ESLE as evidenced by the significant reduction in the immunoexpression of NF-κB, COX-2, iNOS and the reduction in the pro-inflammatory marker, TNF-α. ESLE counteracted the ethanol-induced oxidative stress by increasing the levels of depleted GSH and catalase as well as significantly attenuating the ethanol-induced lipid peroxidation tissue levels. In addition, ESLE exhibited in vitro antibacterial activity against H. pylori., Conclusions: The chemical constituents of ESLE strongly support its potent gastroprotective effect suggesting its future potential application in the management of gastric ulcer by eliminating its symptoms and causes including H. pylori., (Copyright © 2019 Elsevier B.V. All rights reserved.)

The in vitro cytotoxic activity in Vero cells and the antiviral activity of Erythrina speciosa methanol extract, fractions, and isolated vitexin were studied. The results revealed that E. speciosa leaves ethyl acetate soluble fraction of the methanol extract (ESLE) was the most active against herpes simplex virus type 1 (HSV-1). Bioactivity-guided fractionation was performed on ESLE to isolate the bioactive compounds responsible for this activity. One sub-fraction from ESLE (ESLE IV) showed the highest activity against HSV-1 and Hepatitis A HAV-H10 viruses. Vitexin isolated from ESLE VI exhibited a significant antiviral activity (EC 50 =35±2.7 and 18±3.3 μg/mL against HAV-H10 and HSV-1 virus, respectively), which was notably greater than the activity of the extract and the fractions. Molecular docking studies were carried out to explore the molecular interactions of vitexin with different macromolecular targets. Analysis of the in silico data together with the in vitro studies validated the antiviral activity associated with vitexin. These outcomes indicated that vitexin is a potential candidate to be utilized commendably in lead optimization for the development of antiviral agents., (© 2019 Wiley-VHCA AG, Zurich, Switzerland.)

Gastric ulcer is a major health problem. Current treatment options of gastric ulcer, including antagonists of histamine H 2 receptor and inhibitors of the proton pump, do not cure gastric ulcers, but only provide temporary relief of symptoms and can be associated with severe side effects. The lack of effective and safe medications for this global health problem urges for the discovery of novel classes of compounds with potent activity and an acceptable safety profile. Ethanol-induced ulceration in rats was used to evaluate the gastroprotective activity of casuarinin, an ellagitannin isolated from Melaleuca leucadendra . Casuarinin (25, 50, and 100 mg/kg) reduced the ulcer area by 45, 78, and 99%, respectively, compared with the ulcer group. Casuarinin (100 mg/kg) increased mucin content by 1.8-fold and reduced acidity by 42%. At the same dose, it also increased the levels of reduced glutathione by 194%, catalase by 586%, and prostaglandin E2 to its normal level. In contrast, it attenuated the ethanol-increased levels of malondialdehyde by 56%, TNF- α by 58%, and caspase-3 by 87%. Histological findings demonstrated that casuarinin exhibited a protective effect against tissue alterations in response to the ethanol-induced ulcer. Casuarinin suppressed the immunoexpression of nuclear factor-kappa B, cyclooxygenase-2, and inducible nitric oxide synthase to their normal values. It also induced the expression of heat shock protein-70, reaching up to 4.9-fold in comparison with the ulcer group. The potent gastroprotective effect of casuarinin was thus attributed to its anti-inflammatory, antioxidant, and antiapoptotic effects. Our results suggest the potential application of casuarinin as an antiulcer agent from natural sources., Competing Interests: The authors declare that they have no conflict of interest., (Georg Thieme Verlag KG Stuttgart · New York.)

The gastroprotective effect of Ocimum basilicum L. (Basil) hexane extract (OBHE) in aspirin-induced gastric ulcers in mice and its ameliorative effect on behavioral alterations were determined. Pretreatment with OBHE (100 or 200 mg kg-1) or misoprostol (50 μg kg-1) alleviated the aspirin-induced oxidative stress by significantly decreasing (p < 0.001) gastric ulcer index scores (57, 76 and 79%), gastric TBARS (by 49, 51 and 52%), NO (21, 28 and 29%), H2O2 (24, 42 and 45%), and the serum pro-inflammatory mediator TNF-α (21, 53 and 53%) and IL-6 (29, 30 and 31%), as well as by markedly increasing gastric GSH (41, 61 and 70%), GSH-Px (21, 32 and 34%), GST (33, 63 and 70%), GR (90, 99 and 112%), CAT (167, 211 and 267%) and serum PGE-2 levels (22, 135 and 200%) and IL-4 (64, 81 and 104%), respectively, compared with the aspirin-treated group. Meanwhile, OBHE and misoprostol induced a significant decrease (p < 0.001) in the freezing time (53, 56 and 64%), and the grooming time (by 25, 43 and 44%), respectively, compared to the aspirin treated group. This study provides evidence that OBHE confers anxiolytic, antioxidant and anti-inflammatory prophylactic effects on aspirin-induced gastric ulcers. GC/MS was used for the characterization of OBHE components. Based on the findings of this study, basil may be used as a nutritional supplement or therapeutic drug to protect against aspirin-induced gastric ulcers, a common problem resulting from the use of aspirin.

Context In a previous study, the total extract of Melaleuca styphelioides Sm. (Myrtaceae) showed a significant hepatoprotective effect in a CCl4-induced toxicity model in mice. However, the active components responsible for the activity of the extract were not identified. Objective To determine the in vitro hepatoprotective activity of the isolated pure compounds from M. styphelioides leaves using the CCl4-challenged HepG2 cell model. Materials and methods The hepatoprotective activity of the compounds (at concentrations of 100, 50 and 25 μm), the total extract and silymarin (Sil) (100, 50 and 25 μg/ml) was determined by measuring the activities of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) after pretreatment with the tested samples for one hour. Glutathione (GSH) and superoxide dismutase activity (SOD) were estimated to determine the mechanisms of the hepatoprotective activity. Results Some compounds showed marked hepatoprotection, including tellimagrandin I, which produced 42, 36 and 31% decrease in ALT and 47, 43 and 37% decrease in AST, at the tested concentrations, respectively, pedunculagin (32, 32 and 30% decrease for ALT and 48, 48 and 45% for AST), tellimagrandin II (38, 32 and 26% decrease for ALT and 45, 40 and 34% for AST) and pentagalloyl glucose (30, 28 and 26% decrease for ALT and 45, 38 and 36% for AST). Tellimagrandin I and II showed the highest increase in GSH (113, 105 and 81% and 110, 103 and 79%, respectively), which was comparable to Sil. Pedunculagin produced the highest increase in SOD (497, 350 and 258%). Conclusion This study highlights promising natural hepatoprotective candidates derived from M. styphelioides.

Context: Terminalia is used in folk medicine for the treatment of various diseases., Objective: The objective of this study is to investigate the hepatonephro protective activity of a polyphenol-rich fraction (TMEF) obtained from Terminalia muelleri Benth. (Combretaceae) against CCl4-induced toxicity in mice., Materials and Methods: TMEF was administered (100, 200, and 400 mg/kg/d) for 5 d. CCl4 was administered at the end of the experiment. Hepatic and renal biomarkers were measured in the serum. Glutathione (GSH), superoxide dismutase (SOD), and malondialdehyde (MDA) were estimated in the liver and kidney tissues. The active constituents of TMEF were identified by HPLC-PDA-ESI/MS/MS., Results: TMEF is rich in ellagitannins, galloyl esters, phenolic acids, and flavone-C-glucosides. TMEF pretreatment significantly (p < 0.001) inhibited the CCl4-induced increase in ALT (17, 43, and 53%), AST (20, 46, and 58%), ALP (20, 48, and 56%), LDH (21, 47, and 58%), hepatic MDA (23, 49, and 54%), renal MDA (22, 35, and 52%), creatinine (48, 66, and 91%), uric acid (16, 34, and 59%), urea (22, 39, and 59%), and cholesterol (20, 27, and 46%). Furthermore, TMEF administration significantly (p < 0.001) increased hepatic GSH (15, 51, and 79%), renal GSH (23, 45, and 73%), hepatic SOD (9, 52, and 95%), renal SOD (39, 66, and 85%) and protein levels (17, 24, and 29%) at the tested doses of TMEF, respectively. Pretreatment with TMEF preserved the hepatic architecture and protected from ballooning degeneration, liver necrosis, renal inflammation, and degeneration of the kidney tubules., Conclusion: TMEF has a marked hepato-nephro protective effect.

The hepatoprotective and nephroprotective activity of a polyphenol-rich fraction (BHPF) obtained from Bauhinia hookeri was investigated against CCl4-induced acute hepatorenal toxicity in mice. BHPF was administered (100, 200 and 400 mg/kg/day) for 5 days, then CCl4 was administered. BHPF pretreatment significantly (p < 0.001) inhibited the CCl4-induced increase in ALT, AST, ALP, LDH, total bilirubin, cholesterol, creatinine, uric acid, urea and malondialdehyde in a dose-dependent manner. In contrast, BHPF pretreatment markedly increased the contents of glutathione and superoxide dismutase in the liver and kidney tissues, indicating the strong in vivo antioxidant activity of BHPF. Pretreatment with BHPF preserved the hepatic architecture and conferred marked protection against necrosis and ballooning degeneration. Pretreatment with BHPF reduced the inflammatory cell aggregation and degenerative changes in the lining epithelium of the kidney tubules. It can be concluded that BHPF has a remarkable hepato- and nephroprotective activity by enhancing the antioxidant defense status, reducing lipid peroxidation and protecting against the histopathological changes induced by CCl4 in the liver and kidney tissues.

Context: Liver disease is a serious problem. Polyphenolic compounds have marked antioxidant effect and can prevent the liver damage caused by free radicals. In vitro studies have revealed the strong antioxidant activity of an ellagitannin-rich plant, namely, Melaleuca styphelioides Sm. (Myrtaceae)., Objective: In view of the limited therapeutic options available for the treatment of liver diseases, the hepatoprotective potential of the methanol extract of M. styphelioides leaves (MSE) was investigated against CCl4-induced liver injury in mice., Materials and Methods: MSE was administered (500 and 1000 mg/kg/d p.o.) along with CCl4 for 6 weeks. Alanine aminotransferase (ALT), aspartate aminotransferase (AST), and alkaline phosphatase (ALP) were determined in the serum. Glutathione (GSH), superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase (GR), glutathione transferase (GST), and malondialdehyde (MDA) were estimated in the liver homogenate. The bioactive components of MSE were identified by NMR, UV and HRESI-MS/MS data., Results: MSE treatment (500 and 1000 mg/kg/d) markedly inhibited the CCl4-induced increase in the levels of AST (31 and 38%), ALT (29 and 32%), ALP (13 and 19%), and MDA (22 and 37%) at the tested doses, respectively. MSE treatment markedly increased the levels of GSH (29 and 57%) and antioxidant enzymes compared with the CCl4-treated group. MSE was more effective than silymarin in restoring the liver architecture and reducing the fatty changes, central vein congestion, Kupffer cell hyperplasia, inflammatory infiltration, and necrosis induced by CCl4. The LD50 of MSE was more than 5000 mg/kg., Conclusion: MSE confers potent antioxidant and hepatoprotective effects against CCl4-induced toxicity.

Context: Schistosomiasis is a parasitic disease that results in severe organ damage. Snail control is the best measure to control schistosomiasis. Plant-derived molluscicides have gained increasing attention for the control of schistosomiasis because they have low toxicity towards non-target organisms. Tannins are particularly suitable for snail control because they are less toxic than saponins to non-target organisms., Objective: To identify the most toxic components of two plants belonging to the family Myrtaceae, namely Eucalyptus globulus Labill. and Melaleuca styphelioides Sm against the different developmental stages of Schistosoma mansoni and its snail host., Materials and Methods: The 80% MeOH leaf extracts of the tested plants and their isolated compounds were screened for their molluscicidal activity (expressed as LC50 and LC90 after 24 h exposure) against the snail Biomphalaria alexandrina. The anti-schistosomal activity of the tested samples was determined at 20 ppm (after 1 or 2 h exposure) against the different developmental stages of S. mansoni, including the miracidia, cercariae and worms. Biochemical parameters were measured to determine the toxicity mechanisms of the treated snails. The structures of the isolated compounds were elucidated based on NMR, UV and HRESI-MS/MS data., Results: Potent molluscicidal activity was observed for the ellagitannin dimer eucalbanin B (12), with an LC50 value of 55 ppm. Treatment of the snails with the LC25 of eucalbanin B (30.8 ppm) resulted in a significant decrease in the protein level by 22.7% and 25.8% in the snail tissues and hemolymph, respectively. The decreased protein content was attributed to destruction of the snail tissue and impairment in protein synthesis under stress conditions of intoxication with eucalbanin B. Alterations in the activities of the transaminases and phosphatases in the treated snails indicated destruction and intoxication of the snail tissues. A significant increase in the levels of the transaminases alanine aminotransferase (ALT) (57.8%) and aspartate aminotransferase (AST) (113.2%) in the snail hemolymph and a significant decrease in their tissue levels to 7.4 and 48.6%, respectively, were attributed to their release from the damaged tissue into the hemolymph. Alkaline phosphatase (ALP) was significantly increased by 38.5 and 181.4% in the hemolymph and tissues, respectively. Acid phosphatase (ACP) was also significantly increased by 48.4 and 21.2% in the hemolymph and tissues, respectively. The 80% MeOH extract of E. globulus together with mallophenol B (3), 2,2,8-trimethyl-6-formyl-chrom-3-ene-7-O-β-d-glucopyranoside (5) and benzyl alcohol 7-O-(3',4',6'-tri-O-galloyl)-β-d-glucopyranoside (10) exhibited miracidicidal activity with almost 100% toxicity at 20 ppm for the three compounds and 80% toxicity for the extract. Moreover, E. globulus extract showed cercaricidal and schistosomicidal activity with 100 and 40% mortality, respectively., Conclusion: E. globulus is a potential source for biocidal compounds against S. mansoni and its snail host. This is the first study to test the biocidal activity of the isolated compounds.

The hepatoprotective and antioxidant activity of Bauhinia hookeri ethanol extract (BHE) against CCl4-induced liver injury was investigated in mice. BHE was administered (500 and 1000 mg/kg/day) along with CCl4 for 6 weeks. The hepatic marker enzymes: alanine aminotransferase (ALT), aspartate aminotransferase (AST), and alkaline phosphatase (ALP) were determined in the serum. The antioxidant parameters: glutathione (GSH), superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase (GR), glutathione transferase (GST), and malondialdehyde (MDA) were estimated in the liver homogenate. BHE treatment significantly inhibited the CCl4-induced increase in ALT (44 and 64%), AST (36 and 46%), ALP (28 and 42%), and MDA (39 and 51%) levels at the tested doses, respectively. Moreover, BHE treatment markedly increased the activity of antioxidant parameters GSH, GPx, GR, GST, and SOD. Histological observations confirmed the strong hepatoprotective activity. These results suggest that a dietary supplement of BHE could exert a beneficial effect against oxidative stress and various liver diseases by enhancing the antioxidant defense status, reducing lipid peroxidation, and protecting against the pathological changes of the liver. The hepatoprotective activity of BHE is mediated, at least in part, by the antioxidant effect of its constituents. The active constituents of BHE were identified by HPLC-PDA-ESI/MS/MS.