Essential Oil of Cestrum diurnum L.: GC/MS Analysis, in Vitro and in Silico Anti-HCoV-229E Effects and Inhibitory Activity against LPS-Induced Inflammation.

Cestrum diurnum L. (Solanaceae) is a fragrant ornamental tree cultivated in different parts around the world. In this study, the essential oil (EO) of the aerial parts was extracted by hydrodistillation (HD), steam distillation (SD) and microwave-assisted hydro-distillation (MAHD). GC/MS analysis of the three EOs revealed that phytol represents the major component in SD-EO and MAHD-EO (40.84 and 40.04 %, respectively); while in HD-EO it only represented 15.36 %. The SD-EO showed a strong antiviral activity against HCoV-229E with IC50 of 10.93 µg/mL, whereas, MAHD-EO and HD-EO showed a moderate activity with IC50 values of 119.9 and 148.2 µg/mL, respectively. The molecular docking of EO major components: phytol, octadecyl acetate and tricosane showed a strong binding to coronavirus 3-CL (pro). Moreover, the three EOs (50 µg/mL) decreased the levels of NO, IL-6 and TNF-α and suppressed IL-6 and TNF-α gene expression in LPS-induced inflammation model in RAW264.7 macrophage cell lines.

GC/MS profiling of essential oils from Bontia daphnoides L., chemometric discrimination, isolation of dehydroepingaione and evaluation of antiviral activity.

Bontia daphnoides L. has been utilized in traditional medicine for treatment of herpes, cough and colds. The aim of this study was to analyze the volatile constituents of this plant by GC/MS (Gas Chromatography coupled to Mass Spectrometry) and to assess their antiviral activity. A total of 64 compounds were identified where dehydroepingaione represented 83.60, 72.36, 58.78 and 34.18% in the leaves, stems, flowers and fruits, respectively. Principal component and hierarchical cluster analysis revealed the discrimination of the organs as the leaves and stems were distributed in the same cluster in contrast to the flowers and fruits. Furthermore, the antiviral activity was assessed where the oils of leaves and stems exhibited potent antiviral activity displaying IC50 of 11.98, 12.62 µg/ml against HSV-1 and 13.34, 14.50 µg/ml against CoxB4, respectively. Dehydroepingaione was isolated from the n-hexane fraction of the leaves and showed activity against HSV-1 and CoxB with IC50 of 24.46 and 25.32 µg/ml, respectively. Molecular modelling studies illustrated that the major compounds showed good affinity towards HSV type-1 thymidine kinase. Therefore, it can be concluded that the oils from B. daphnoides have promising antiviral activity that may be attributed to the major oxygenated sesquiterpenes.

Cyclodepsipeptides: Isolation from Endophytic Fungi of Sarcophyton ehrenbergi and Verification of Their Larvicidal Activity via In-Vitro and In-Silico Studies.

Culex pipiens mosquitoes are vectors to many viruses and can transmit diseases such as filariasis and avian malaria. The present study evaluated the larvicidal activity of marine-derived endophytic fungi Aspergillus nomius and Aspergillus flavus from the soft coral Sarcophyton ehrenbergi along with two known cyclodepsipeptide compounds, scopularide A (1) and B (2), isolated from A. flavus extract, against third-instar larvae of C. pipiens, using distilled water as a negative control and toosenedanin as a positive control. The structures of the isolated compounds were confirmed by various spectroscopic analyses. The lethal concentrations (LC50 and LC90) were calculated by probit analysis. Scopularide A was the most potent after 96 h treatment, with LC50 and LC90 values of 58.96 and 994.31 ppm, respectively, and with 82.66% mortality at a concentration of 300 ppm. To unravel the biochemical mechanism of the tested extracts and compounds, their effects against protease, chitinase, phenoloxidases and lipase enzymes from the whole-body tissue of C. pipiens were evaluated after 72 h treatment at LC50 dose. Superior activity was observed for A. flavus extract against all tested enzymes. A molecular docking study was conducted for scopularide A and B on the four tested enzymes, to further verify the observed activity. Results revealed good binding affinities for both compounds as compared to the docked ligands, mainly via a number of hydrogen bonds. This was the first study to report the isolation of endophytic fungi A. flavus and A. nomius from the marine soft coral S. ehrenbergi. The endophytic fungal extract of A. flavus was found to be a promising source for a natural larvicidal agent against C. pipiens populations.

Essential oils from the leaves and flowers of Leucophyllum frutescens (Scrophulariaceae): phytochemical analysis and inhibitory effects against elastase and collagenase in vitro.

Leucophyllum frutescens (Scrophulariaceae) is a medicinal plant of Mexican traditional medicine. The aim of this study was to analyse the volatile components from the leaves and flowers by GC/MS and to assess their anti-aging activity for the first time. A total of 30 compounds were identified where 1-octen-3-ol (73.56%) and D-limonene (11.12%) represented the major ingredients in the leaves, while n-heneicosane (32.30%) and dehydroepingaione (15.15%) were the major components in the flowers. In vitro anti-aging activity was measured via assessing collagenase and elastase inhibition. Essential oils from the leaves and flowers showed potential collagenase inhibitory activity with IC50 of 55.7 and 47.4 µg/mL. However, the oils from the leaves and flowers showed moderate anti-elastase activity with IC50 of 60.8 and 97.7 µg/mL. Therefore, the oil of Leucophyllum frutescens could afford a promising natural anti-aging drug.

Phytochemical discrimination of Pinus species based on GC-MS and ATR-IR analyses and their impact on Helicobacter pylori.

INTRODUCTION: The leaves and cones of Pinus plants as well as their essential oils have been used in traditional medicine for the treatment of several ailments. OBJECTIVES: Phytochemical discrimination of Pinus species and investigation of their anti-Helicobacter pylori activity in vitro and in silico. MATERIALS AND METHODS: Gas chromatography-mass spectrometry (GC-MS) and attenuated total reflectance infrared (ATR-IR) metabolic profiling of the essential oils of Pinus species. Principal component analysis (PCA) and hierarchal cluster analysis (HCA) were applied for discrimination and segregation of Pinus species. RESULTS: GC-MS revealed the presence of 76 constituents, where monoterpenes represented the major class with the dominance of α-pinene (72%) followed by ß-pinene (16%) for P. canariensis. ß-Pinene was the dominant component in P. pinea (24%) followed by terpinolene (11%). α-Pinene (17%) and caryophyllene (12%) were the major components in P. halepensis, while, 3-carene (33%) and α-pinene (17%) represented the major constituents of P. roxburghii oil. By applying PCA and HCA on GC-MS and ATR-IR data analysis, ATR-IR displayed much better discrimination for Pinus species. The pine oils showed promising inhibitory effects on Helicobacter pylori. Furthermore, in silico molecular modelling was carried out where the calculated free binding energies of phytochemicals identified ranged from -33.71 to -19.67 kcal/mol for urease and -41.18 to -16.57 kcal/mol for shikimate kinase. This suggests favourable binding of pine essential oil components to both enzymes, thus explaining their potential inhibitory activity on H. pylori. CONCLUSION: GC-MS and ATR-IR based metabolic analyses could discriminate between Pinus species. Pine essential oils can be used as promising therapeutic drugs to protect against H. pylori infection.

Vicia plants-A comprehensive review on chemical composition and phytopharmacology.

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.

Achillea spp.: A comprehensive review on its ethnobotany, phytochemistry, phytopharmacology and industrial applications.

The genus Achillea genus houses more than 100 species, a number of them are popularly used in traditional medicine for spasmodic gastrointestinal, gynecological and hepatobiliary disorders, hemorrhages, pneumonia, rheumatic pain, inflammation, wounds healing etc. Members of the genus contain a wide variety of volatile and non-volatile secondary metabolites, including terpenes, polyphenols, flavonoids and others. Multiple studies have assessed the biological effects and other aspects of Achillea spp. In a number of preclinical studies, Achillea plants and their essential oils have demonstrated promising antibacterial properties against a number of human and plant pathogens. Besides, the plants have displayed strong antioxidative and potent anti-proliferative and anticancer properties in various cellular and animal models. Achillea plants have widely been used as food preservative in food industry. Clinical studies have indicated its potential against multiple sclerosis (MS), irritable bowel syndrome (IBS), ulcerative colitis, episiotomy wound, primary dysmenorrhea, oral mucositis etc. The present work focuses to provide a brief overview on folk knowledge, phytochemistry, biological activity and applications of Achillea plants. There is a close relationship between the traditional ethnobotanical usage and pharmacological and clinical data from different Achillea spp. The application of Achillea plants and their extracts seems to be a promising alternative for antimicrobial and antioxidant purposes in food, pharmaceutical and cosmetic industries.

Anti-inflammatory, hepatoprotective and antioxidant activity of ellagitannin isolated from Melaleuca styphelioides.

Ellagitannins have a marked antioxidant effect and can prevent liver injury induced by free radicals. An undescribed ellagitannin named styphelioidin was isolated from Melaleuca styphelioides Sm. The structure of styphelioidin was elucidated by using various spectroscopic methods. The hepatoprotective activity of styphelioidin (25, 50, and 100 µM) was tested using the CCl4-challenged HepG2 cell model by measuring alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels in HepG2 cells treated with styphelioidin for 1 h followed by 40 mM CCl4. Glutathione (GSH), superoxide dismutase activity (SOD) and lipid peroxidation (MDA) were evaluated to determine the mechanisms of the hepatoprotective activity. Styphelioidin significantly reduced the levels of ALT, AST, and MDA at all tested concentrations. Moreover, it conferred a marked increase in the GSH levels and the SOD activity compared to the CCl4-treated groups. Styphelioidin also exerted DPPH· radical-scavenging effects with an IC50 value of 3.67 µM. Results indicated the hepatoprotective therapeutic potential of styphelioidin comparable to silymarin. Moreover, anti-inflammatory activity was assessed and styphelioidin inhibited fMLF/CB-induced elastase release in human neutrophils with IC50 2.51 µM. Cell-free experiments with human neutrophil elastase indicated a direct enzymatic inhibitory effect of styphelioidin on the enzyme activity (IC50 2.58 µM). The potential of styphelioidin to interact with human neutrophil elastase binding sites was further confirmed by molecular docking of styphelioidin into human neutrophil elastase crystal structure using AutoDock 4.2. Styphelioidin represents a potent hepatoprotective and antioxidant agent with effects on ALT, AST, MDA, GSH, and SOD comparable to silymarin. The beneficial anti-elastase properties hold the potential for drug development against elastase-related inflammatory diseases. This study highlights a promising natural hepatoprotective and anti-inflammatory candidate derived from M. styphelioides.

Gastroprotective effects of Erythrina speciosa (Fabaceae) leaves cultivated in Egypt against ethanol-induced gastric ulcer in rats.

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.

Protective Role of Casuarinin from Melaleuca leucadendra against Ethanol-Induced Gastric Ulcer in Rats.

Gastric ulcer is a major health problem. Current treatment options of gastric ulcer, including antagonists of histamine H2 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.

Breaking Down the Barriers to a Natural Antiviral Agent: Antiviral Activity and Molecular Docking of Erythrina speciosa Extract, Fractions, and the Major Compound.

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 (EC50 =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.

Alkaloids of genus Erythrina: An updated review.

Genus Erythrina (Fabaceae) comprises several species, which are widely distributed in tropical and subtropical regions of the world. The plants of this genus exhibited significant role in traditional medicine targeting different diseases. Alkaloids and flavonoids were reported as the chief bioactive constituents of this genus with a wide range of biological activities. About 143 alkaloids were isolated from Erythrina sp. Anticonvulsant, anxiolytic, curare-like activity, insecticidal and cytotoxic activities were reported for Erythrina sp. alkaloids. The present work is an overview of the isolated alkaloids from Erythrina sp. with their reported biological activities.[Figure: see text]Abbreviations: CHCl3: Chloroform; CNS: Central nervous system; DCM: Methylene chloride; DPPH: 2,2-Diphenyl-1-picrylhydrazyl; E.: Erythrina; ERα/ß: Estrogen receptors α/ß; EtOAc: Ethyl acetate; EtOH: Ethanol; Hep-G2: Human liver carcinoma cell lines; HIV: Human immunodeficiency virus; HL-60: Human promyelocytic leukemia cells; K-562: Human immortalized myelogenous leukemia cell line; LPS: Lipopolysaccharide; MeOH: Methanol; MOLT-4: Acute lymphoblastic leukemia cell line; nAChRs: nicotinic acetylcholine receptors; NO: Nitric oxide; NREM: non-rapid eye movement; Pet. ether: Petroleum ether; RBA: Receptor binder affinity; TRAIL: Tumor necrosis factor (TNF)-related apoptosis-inducing ligand.

Hepatoprotective activity of praecoxin A isolated from Melaleuca ericifolia against carbon tetrachloride-induced hepatotoxicity in mice. Impact on oxidative stress, inflammation, and apoptosis.

The hepatoprotective activity of praecoxin A, an ellagitannin from Melaleuca ericifolia, was determined against CCl4 -induced toxicity in mice. Praecoxin A was administered (25, 50, and 100 mg/kg) for 5 days followed by CCl4 . Praecoxin A markedly ameliorated the CCl4 -induced increase in AST (by 19, 52, and 56%), ALP (22, 45, and 48%), ALT (11, 47, and 54%), total bilirubin (14, 27, and 28%), and MDA (26, 44, and 51%) at the tested doses, respectively, as compared with CCl4 group. It was evident that praecoxin A significantly (p < 0.001) increased the antioxidant parameters GSH (45, 99, and 137%) and SOD (61, 129, and 159%). Histological findings revealed a marked amelioration of hepatocyte degeneration, necrosis, inflammatory cell infiltration, and hemorrhage in the groups treated with praecoxin A. COX-2 and caspase-3 hepatic expressions were significantly downregulated (p < 0.001) in praecoxin A-treated groups (up to 57, 83, and 93% for COX-2 and by 30, 82, and 99% for caspase-3). These findings suggest that praecoxin A exerts a beneficial effect against oxidative stress by reducing lipid peroxidation, enhancing the antioxidant defense status, and protecting against the histopathological changes induced by CCl4 . This study highlights a promising natural hepatoprotective candidate derived from M. ericifolia that might be an alternative to silymarin.

The protective role of Ocimum basilicum L. (Basil) against aspirin-induced gastric ulcer in mice: Impact on oxidative stress, inflammation, motor deficits and anxiety-like behavior.

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.

Genus Spondias: A Phytochemical and Pharmacological Review.

It is believed that many degenerative diseases are due to oxidative stress. In view of the limited drugs available for treating degenerative diseases, natural products represent a promising therapeutic strategy in the search for new and effective candidates for treating degenerative diseases. This review focuses on the genus Spondias which is widely used in traditional medicine for the treatment of many diseases. Spondias is a genus of flowering plants belonging to the cashew family (Anacardiaceae). This genus comprises 18 species distributed across tropical regions in the world. A variety of bioactive phytochemical constituents were isolated from different plants belonging to the genus Spondias. Diverse pharmacological activities were reported for the genus Spondias including cytotoxic, antioxidant, ulcer protective, hepatoprotective, anti-inflammatory, antiarthritic, and antidementia effects. These attributes indicate their potential to treat various degenerative diseases. The aim of this review is to draw attention to the unexplored potential of phytochemicals obtained from Spondias species, thereby contributing to the development of new therapeutic alternatives that may improve the health of people suffering from degenerative diseases and other health problems.

Antioxidant activity of phenolic compounds from extracts of Eucalyptus globulus and Melaleuca styphelioides and their protective role on D-glucose-induced hyperglycemic stress and oxalate stress in NRK-49Fcells.

Phytochemicals serve as potential therapeutic agents for the prevention and treatment of diseases. In this study, we elucidate the renoprotective activity of compounds isolated from Eucalyptus globulus and Melaleuca styphelioides extracts in glucose- and oxalate-challenged NRK-49F cell model. The antioxidant potential of isolated compounds was evaluated based on their effect on antioxidant enzyme activities and lipid peroxidation levels. The results demonstrated that exposure of NRK-49F cells to glucose and oxalate stress augmented cell damage and attenuated antioxidant enzyme activities. The phytochemicals 2,2,8-trimethyl-6-formyl-chrom-3-ene-7-O-ß-D-glucopyranoside, Cornusiin B and tellimagrandin I treatment restored antioxidant enzyme activity, significantly lowered lipid peroxidation levels and effectively protected cells from glucose and oxalate stress equivalent to the known antioxidant, N-acetyl cysteine. Pterocarinin A significantly reversed cellular damage owing to glucose stress. In conclusion, the compounds isolated from E. globulus and M. styphelioides showed potential cytoprotective and anti-oxidative property against glucose- and oxalate-induced oxidative stress in NRK-49F cells.

Anti-inflammatory and analgesic activities of cupressuflavone from Cupressus macrocarpa: Impact on pro-inflammatory mediators.

Hit, Lead & Candidate Discovery Inflammation is a complex biological process that is generally occurs in response to pathological triggers. Both neurodegenerative diseases and cancer have been linked to inflammation. The analgesic and anti-inflammatory effects of cupressuflavone (CUF) isolated from Cupressus macrocarpa were examined. The analgesic effects of CUF (40, 80 and 160 mg/kg po) were assessed in the acetic acid-induced writhing and hot plate models in mice with diclofenac sodium as the reference standard (100 mg/kg). CUF dose-dependently inhibited the writhing response in mice by 25, 48, and 62%, at the three CUF doses with 160 mg/kg being equivalent to the diclofenac control. CUF dose-dependently increased the hot plate model reaction time with a maximal effect after 120 min. In the carrageenan-induced paw edema model of inflammation, CUF demonstrated anti-inflammatory activity by inhibiting paw edema by 55, 60, and 64% at doses of 40, 80, and 160 mg/kg po, respectively. CUF also reduced the plasma pro-inflammatory mediators PGE2 (44, 54, and 58%), TNF-α (26, 37, and 53%), IL-1ß (19, 33, and 41%), and IL-6 (32, 44, and 55%) at the three doses tested with the highest dose having similar effects to diclofenac sodium (100 mg/kg). This finding from this study indicates that CUF has both analgesic and anti-inflammatory effects.

Anti-Inflammatory and Analgesic Activities of Terminalia Muelleri Benth. (Combretaceae).

Preclinical Research The anti-inflammatory and analgesic activities of a polyphenol-rich fraction (TMEF) obtained from Terminalia muelleri Benth. were measured. The analgesic activity of TMEF was tested using acetic acid-induced writhing and hot plate models in mice. The anti-inflammatory activity was assessed using carrageenan-induced paw edema model by measuring PGE2 , TNF-α, IL-1ß, and IL-6 plasma levels as well as the paw thickness. TMEF was tested at doses of 100, 200, and 400 mg/kg p.o. and diclofenac sodium was used as a standard (100 mg/kg) in all experiments. The group treated with 400 mg/kg of TMEF showed a greater inhibition in the number of writhes (by 63%) than the standard-treated group (61%). Pretreatment with TMEF increased the analgesic effect in hot plate test in a dose-dependent manner with a maximum effect after 120 min. TMEF pretreatment alos reduced the edema thickness by 48, 53, and 62% at the tested doses, respectively. TMEF administration inhibited the carrageenan-induced elevations in PGE2 (by 34, 43, and 47%), TNF-α (18, 28, and 41%), IL-1ß (14, 22, and 29%), and IL-6 (26, 31, and 46%). Four phenolic compounds were isolated from Terminalia muelleri for the first time. Drug Dev Res 78 : 146-154, 2017. © 2017 Wiley Periodicals, Inc.

Hepatoprotective and antioxidant effect of ellagitannins and galloyl esters isolated from Melaleuca styphelioides on carbon tetrachloride-induced hepatotoxicity in HepG2 cells.

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.