Antinociceptive and anti-inflammatory effects of isolated fractions from Apium graveolens seeds in mice

The antinociceptive and anti-inflammatory effects of the aqueous and hexane extracts obtained from Apium graveolens L. (Apiaceae) seeds were evaluated. Formalin and xylene-induced ear edema tests were used in mice. The fractions were administered intraperitoneally at doses of 100-500?mg/kg body weight (BW). Both extracts with the xylene-induced ear edema test showed significant anti-inflammatory activity at all doses as compared with control. Only the hexane fraction reduced the nociception produced by formalin solution in the first phase (0-5?min) at 300, 400, and 500?mg/kg BW, and in the second phase (20-30?min) at 500?mg/kg BW. It is concluded that the hexane fraction has major contribution to the overall antinociceptive activity. Both fractions showed remarkable anti-inflammatory effect which supported the traditional use of Apium graveolens in diseases associated with inflammation.     

Antioxidant effects of flavonoid from Croatian Cystus incanus L. rich bee pollen

Oxidant/antioxidant status, estrogenic/anti-estrogenic activity and gene expression profile were studied in mice fed with Cystus incanus L. (Cistaceae) reach bee pollen from location in Central Croatia’s Dalmatia coast and offshore islands. Seven phenolic compounds (out of 13 tested) in bee pollen sample were detected by high performance liquid chromatography (HPLC) analysis. Phenolics detected in C. incanus L. bee pollen belong to flavonol (pinocembrin), flavanols (quercetin, kaempferol, galangin, and isorhamnetin), flavones (chrysin) and phenylpropanoids (caffeic acid). Bee pollen as a food supplement (100 mg/kg bw mixed with commercial food pellets) compared to control (commercial food pellets) modulated antioxidant enzymes (AOE) in the mice liver, brain and lysate of erythrocytes and reduced hepatic lipid peroxidation (LPO). Bee pollen induced 25% of anti-estrogenic properties while no estrogenic activity was found. Differential gene expression profile analyses after bee pollen enriched diet identify underexpressed gene Hspa9a, Tnfsf6 (liver) and down-regulated gene expression of Casp 1 and Cc121c (brain) which are important in the apoptosis pathway and chemotaxis. These results indicate that used bee pollen possess a noticable source of compounds with health protective potential and antioxidant activity.     

Antioxidant and hepatoprotective activities of phenolic rich fraction of Seabuckthorn (Hippophae rhamnoides L.) leaves

Present study was aimed to investigate antioxidant and hepatoprotective activities of phenolic rich fraction (PRF) of Seabuckthorn leaves on CCl₄ induced oxidative stress in Sprague Dawley rats. Total phenolic content was found to be 319.33 mg gallic acid equivalent (GAE)/g PRF and some of its phenolic constituents, such as gallic acid, myricetin, quercetin, kaempferol and isorhamnetin were found to be in the range of 1.935-196.89 mg/g of PRF as determined by reverse-phase high-performance liquid chromatography (RP-HPLC).Oral administration of PRF at dose of 25-75 mg/kg body weight significantly protected from CCl₄ induced elevation in aspartate aminotransferase (AST), alanine aminotransferase (ALT), γ-glutamyl transpeptidase (GGT) and bilirubin in serum, elevation in hepatic lipid peroxidation, hydroperoxides, protein carbonyls, depletion of hepatic reduced glutathione (GSH) and decrease in the activities of hepatic antioxidant enzymes; superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPX), glutathione reductase (GR) and glutathione-S-transferase (GST). The PRF also protected against histopathological changes produced by CCl₄ such as hepatocytic necrosis, fatty changes, vacuolation, etc. The data obtained in the present study suggests that PRF has potent antioxidant activity, prevent oxidative damage to major biomolecules and afford significant protection against CCl₄ induced oxidative damage in the liver.     

Hypoglycemic and hypolipidemic effects of flavonoid rich extract from Eugenia jambolana seeds on streptozotocin induced diabetic rats

The hypoglycemic and hypolipidemic effects of flavonoid rich extract obtained from seeds of Eugenia jambolana (EJ) was analyzed in streptozotocin induced diabetic rats. Hypoglycemic activity was assessed by reduction in fasting blood glucose (FBG) and peak blood glucose level within 60 min of glucose tolerance test (GTT) in mild and severe diabetic (MD and SD respectively) rats. Different biochemical parameters like glycogen biosynthesis, glucose homeostatic enzyme (glucose-6-phosphatase, hexokinase) activities demonstrated significant (p<0.05) improvement as compared to diabetic counter parts. Further, the flavonoids also stimulated 16% increase in insulin release in vitro from pancreatic islets. The hypolipidemic action after this extract supplementation was confirmed by significant (p<0.05) decrease in the levels of LDL (27% MD, 29% SD), triglycerides (about 35% MD, 37% SD) and increase in HDL (21% MD, 34% SD) over untreated diabetic rats. The above mentioned action of this plant extract was found to be through dual up regulation of both the peroxisome proliferators-activated receptors (PPARalpha and PPARgamma) up to about 3-4 folds (over control) and their capacity to differentiate 3T3-L1 preadipocytes. The present data suggests that the flavonoid rich extract from EJ plant has both hypoglycemic and hypolipidemic effects which can help the cure and management of diabetes.     

Potential analgesic,anti-inflammatory and antioxidant activities of hydroalcoholic extract of Areca catechu L. nut

The hydroalcoholic extract of Areca catechu L. (ANE) nut was screened for its analgesic, anti-inflammatory and in vitro antioxidant potential. Three doses of ANE (250, 500 and 1000 mg/kg orally) were tested for analgesic and anti-inflammatory activities. Evaluation of analgesic activity of ANE was performed using hot plate and formalin test in mice. ANE showed maximum increase in hot plate reaction time (56.27%, p < 0.01), while reduced the duration of licking/biting behaviors in first (39.45%, p < 0.05) and second (92.71%, p < 0.01) phases of the formalin test indicating significant analgesic activity. ANE reduced the paw edema considerably (86.79% inhibition after 24 h, p < 0.01) in dose-dependent manner compared to carrageenan-induced rat. In addition, in vitro antioxidant activity of ANE was investigated by total phenolic content (TPC) and hydrogen peroxide assay. The IC₅₀ observed in hydrogen peroxide assay was 83.14 μg/ml and TPC 120.56 ± 21.09 mg QE/g. Altogether, these results suggest that the hydroalcoholic extract of Areca catechu could be considered as a potential analgesic, anti-inflammatory and antioxidant agent.     

In vitro antioxidant and in vivo anti-inflammatory potential of crude polysaccharide from Turbinaria ornata (Marine Brown Alga)

Water-soluble crude polysaccharide from a brown alga Turbinaria ornata (TCP) was screened for its antioxidant and anti-inflammatory potential. The major functional groups of polysaccharide were analyzed by Fourier Transmission-Infra Red (FT-IR). In vitro free radical quenching and total antioxidant activity of TCP was investigated by 1, 1-diphenyl-2-picryl hydrazyl (DPPH), nitric oxide (NO) scavenging, lipid peroxidation (LPO) inhibition and ABTS radical assay. Evaluation of anti-inflammatory activity of TCP was performed using carrageenan-induced paw edema in rats and vascular permeability test in mice. Phytochemical analysis of TCP showed the presence of carbohydrates, proteins and polyphenols further, the FT-IR analysis of TCP showed the presence of functional groups of sugar moiety, uronic acids and sulfate groups. TCP showed maximum LPO, NO and DPPH inhibition of 78.04%, 38.82% and 80.21% at a concentration of 1000, 125 and 500 μg/ml respectively. Oral administration of TCP (2.5, 5, 10, 20 mg/kg) reduced the paw edema considerably (p < 0.05) in a dose dependent manner compared to carrageenan induced rats. Similarly, oral administration of TCP (3, 10, 30 mg/kg) evoked a significant (p < 0.05) dose dependent inhibitory effect on vascular permeability in mice. Altogether, these results suggest that the crude polysaccharide of T.ornata could be considered as a potential antioxidant and anti-inflammatory agent.     

Study on chemical composition,anti-inflammatory and anti-microbial activities of extracts from Chinese pear fruit (Pyrus bretschneideri Rehd.)

Pyrus bretschneideri Rehd. belongs to the genus Pyrus, a member of Rosaceae family. It is a routine edible fruit, and also used as a folk medicine to treat cough, eliminate constipation, and relieve alcoholism. In order to clarify the active compounds of P. bretschneideri, the phytochemical study were performed. Five compounds were isolated and identified as 2β,19α-dihydroxy ursolic acid, quercitrin, dibutyl phthalate, diisobutyl phthalate and α-amyrin. Additionally, we investigate the anti-inflammatory and anti-microbial effects of the fractions of P. bretschneideri partitioned with petroleum ether, ethyl acetate and n-butanol, respectively. In the carrageenan-induced rat paw edema test, the EtOAc fraction showed the strongest inhibition of edema formation 0.5–5 h after edema induction, followed by n-butanol. EtOAc also displayed potent anti-inflammatory activity against xylene-induced ear edema (22.03% and 43.69%, respectively) and acetic acid-induced extravasation of Evan’s blue dye (39.58% and 49.92%, respectively) at the dose of 200 and 400 mg/kg. While, the anti-microbial results showed that ethyl acetate and n-butanol fractions exhibited strong activity against the bacteria strains. Moreover, 2β,19α-dihydroxy ursolic acid, α-amyrin and quercitrin could significantly inhibit the ear edema induced by xylene at the dose of 20 mg/kg, and exhibited moderate anti-microbial activities against the bacteria strains.     

Liquid chromatography/tandem mass spectrometry study of anti-inflammatory activity of Plantain (Plantago L.) species

To evaluate anti-inflammatory activity of selected Plantago species (P. lanceolata L. and P. major L.) an optimized in vitro test for determination of cyclooxygenase-1 (COX-1) and 12-lipoxygenase (12-LOX) inhibition potency was undertaken. By using intact cell system (platelets) as a source of COX-1 and 12-LOX enzymes and highly sensitive and specific LC–MS/MS technique for detection of main arachidonic acid metabolites formed by COX-1 and 12-LOX, this test provides efficient method for evaluation of anti-inflammatory potential of plant extracts and isolated compounds. Our results validated the well-known COX-1 inhibitory activity of P. lanceolata and P. major methanol extracts (concentration required for 50% inhibition (IC₅₀) was 2.00 and 0.65 mg/ml, respectively). Furthermore, 12-LOX inhibitory activity of examined extracts was reported for the first time (IC₅₀ = 0.75 and 1.73 mg/ml for P. lanceolata and P. major, respectively). Although renowned inhibitors, such as acetylsalicylic acid and quercetin showed higher activity, this study verifies P. lanceolata and P. major as considerable anti-inflammatory agents.     

Protective effects of proanthocyanidins of grape (Vitis vinifera L.) seeds on DNA damage induced by Doxorubicin in somatic cells of Drosophila melanogaster

Proanthocyanidins (PAs), also known as condensed tannins, are naturally occurring oligomers and polymers of flavan-3-ol monomer units widely found in the leaves, flowers, fruits, seeds, nuts and barks of many plants. Grape seed proanthocyanidins (GSPs) have been used as nutritional supplements, as antioxidants, in preventing atherosclerosis and cardiovascular diseases, and for dislipidemy treatment. The anthracycline antibiotic adriamycin (Doxorubicin, DXR) is a cancer chemotherapeutic agent that interferes with the topoisomerase II enzyme and generates free radicals. In the present study, GSPs (1.680, 3.375, or 6.750 mg/mL) alone were examined for genotoxicity, and combined with DXR (0.125 mg/mL) for antigenotoxicity, using the standard (ST) and high bioactivation (HB) versions of the wing somatic mutation and recombination test in Drosophila melanogaster. The results observed in both crosses were rather similar. GSPs themselves did not show genotoxicity at the doses used. GSPs suppressed the DNA damage induced by DXR in a dose-dependent manner. Comparison of the frequencies of wing spots in the marker-heterozygous (MH) flies and balancer-heterozygous (BH) flies from both crosses, indicated that induced recombination was the major response for the treatments with DXR alone. The co-treatments demonstrated that GSPs have some anti-mutagenic activity; however, anti-recombinagenic activity was the major response.     

Therapeutic effects of rocket seeds (Eruca sativa L.) against testicular toxicity and oxidative stress caused by silver nanoparticles injection in rats

Silver nanoparticles (AgNPs), one of the most well‐known nanomaterials, are regularly utilized in everyday consumer products. The present study aimed to investigate the testicular toxicity and oxidative stress by AgNPs and the therapeutic role of the rocket seeds (Eruca sativa) in treatments. Forty male Wistar rats were divided into four equivalent groups (group 1, control; group 2, rocket seeds extract [RS]; group 3, AgNPs; group 4, AgNPs+RS). Our results showed that AgNPs induced a significant decrease in serum total testosterone, FSH (follicle‐animating hormone), prolactin and LH (luteinizing hormone), testicular glutathione (GSH), superoxide dismutase (SOD), and glutathione S‐transferase (GST). In contrast, a significant increase in testicular DNA, injury, testicular thiobarbituric acid, proliferating cell nuclear antigen, and tumor necrosis factor‐α (TNFα) expressions after treatments with AgNPs when contrasted with the control group. Treatments of AgNPs with rocket seeds extract (AgNPs+RS) improved testicular functions and structure. Rocket seeds extract might offer benefits against the toxic nature of AgNPs.     

Antinociceptive and anti-inflammatory effects of olive oil (Olea europeae L.) in mice

Context: Olive [Olea europaea L. (Oleaceae)] is a long-lived evergreen tree that is widespread in different parts of the world.

Objective: Olive oil has been reported to relieve pain; however, there is still insufficient data in the literature on the subject. Thus, it is considered worthwhile investigating the antinociceptive and anti-inflammatory effects of olive oil in adult male Balb/C mice.

Materials and methods: The antinociceptive effects were studied using formalin, hot plate and writhing tests. The acute anti-inflammatory effects of olive oil in mice were studied using xylene ear edema test. Olive oil (1, 5 and 10?ml/kg body wt.) was injected intraperitoneally. Intact animals served as controls.

Results: Our results showed that the olive oil only decreased the second phase of formalin-induced pain. In the hot plate test, olive oil did not raise the pain threshold over the 60?min duration of the test. Olive oil exhibited antinociceptive activity against writhing-induced pain by acetic acid. In the xylene ear edema test, olive oil showed significant anti-inflammatory activity in the mice.

Discussion and conclusion: The present data indicated that olive oil has antinociceptive and anti-inflammatory effects in mice but further investigation of these effects is required to elucidate the mechanism(s) involved in analgesic and anti-inflammatory effects of Olea europaea oil.     

Neuroprotective and anti-inflammatory effects of flavonoids isolated from Rhus verniciflua in neuronal HT22 and microglial BV2 cell lines

The neuroprotective and anti-inflammatory activities of the methanolic extract of Rhus verniciflua Stokes (Anacardiaceae) were investigated with mouse hippocampal and microglial cells. Bioactivity-guided isolation yielded 10 flavonoids including fustin (1), fisetin (2), sulfuretin (3), butein (4), butin (5), eriodictyol (6), morin hydrate (7), quercetin (8), kaempferol (9) and isoliquiritigenin (10). Among the isolated flavonoids, compounds 2–5 significantly protected the murine hippocampal HT22 cells against glutamate-induced neurotoxicity and attenuated reactive oxygen species (ROS) generations. In addition, these flavonoids significantly maintained antioxidative defense systems preserving the activities of superoxide dismutase (SOD), glutathione reductase (GR), glutathione peroxidase (GSH-Px) and the content of glutathione (GSH) decreased by glutamate insult. These compounds also showed significant inhibitory effects on LPS-induced nitric oxide (NO) production in BV2 cells. Especially, compound 4 dose-dependently suppressed the expression of both inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). These results suggest that these flavonoids possess therapeutic potentials as a multipotent agent against neurodegenerative diseases related to oxidative stress and pathological inflammatory responses.     

Antioxidant,cytoprotective and antibacterial effects of Sea buckthorn (Hippophae rhamnoides L.) leaves

The present study was carried out to investigate the antioxidant, cytoprotective and antibacterial effects of aqueous and hydroalcoholic extracts of Hippophae rhamnoides L. (Sea buckthorn) (SBT) leaves by using various invitro systems and analysis of marker compounds by reverse phase-high performance liquid chromatography (RP-HPLC). The chemical composition of the leaf extracts was quantified by colorimetric reaction in terms of total phenol and flavonoids contents. Further, some of its bioactive phenolic constituents, such as quercetin-3-O-galactoside, quercetin-3-O-glucoside, kaempferol and isorhamnetin were also quantified in both SBT leaf extracts by RP-HPLC. The SBT leaf extracts exhibited potent antioxidant activity determined by 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS), 2,2-diphenyl-1-picryl-hydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) assays. Further, both extracts were observed to have cytoprotective activity against hydrogen peroxide and hypoxanthine-xanthine oxidase induced damage to BHK-21 cell line. The SBT leaf extracts showed growth inhibiting effect against Bacillus cereus, Pseudomonas aeruginosa, Staphylococcus aureus and Enterococcus faecalis. These observations suggest that aqueous and hydroalcoholic extracts of Sea buckthorn leaves have marked antioxidant, cytoprotective and antibacterial activities.     

Free radical scavenging activity from leaves of Acacia nilotica (L.) Wild. ex Delile,an Indian medicinal tree

The present study compares the two extraction methods and evaluates the free radical scavenging activity of Acacia nilotica. Results indicated that the sequential extraction method was effective in concentrating the active principles in the ethanol extract as compared to the maceration method in DPPH assay. Based on the results, free radical scavenging property of the extracts obtained from sequential extraction method was analyzed in different assays to find out the possible antioxidant mechanism. Our results indicate that ethanol extract rich in phenolic and flavonoid contents had potent antioxidant activity and were significant in comparison with all the positive controls used in this study. The possible antioxidant mechanism of the ethanol extract can be due to its hydrogen or electron donating and direct free radical scavenging properties. Hence, the ethanol extract represents a source of potential antioxidants that could be used in pharmaceutical and food preparations.     

黄皮叶提取物镇咳祛痰、平喘作用及有效部位研究

【摘要】目的 研究黄皮叶不同溶剂萃取物的镇咳、祛痰、平喘作用。方法 （1）将60只小鼠随机分为正常组、枸橼酸喷托维林组、石油醚萃取物组、二氯甲烷萃取物组、乙酸乙酯萃取物组及水提物组,给予相应药物灌胃7 d,用浓氨水引咳,观察小鼠咳嗽潜伏期及2 min内咳嗽次数。（2）将另60只小鼠随机分为正常组、氯化铵组、石油醚萃取物组、二氯甲烷萃取物组、乙酸乙酯萃取物组及水提物组,灌胃相应药物7 d后采用腹腔注射5%酚红溶液,观察小鼠气管酚红排泌量。（3）70小鼠随机分为正常组、模型组、地塞米松组、石油醚萃取物组、二氯甲烷萃取物组、乙酸乙酯萃取物组及水提物组,于第1、7、14 天腹腔注射卵蛋白致敏液;第18～22 天给予相应药物灌胃,并用卵蛋白溶液雾化激发,观察哮喘小鼠支气管肺泡灌洗液（BALF）中白细胞总数及细胞分类计数。结果 （1）与正常组比较,石油醚萃取物、二氯甲烷萃取物能延长小鼠咳嗽潜伏期并减少2 min内咳嗽次数,差异有统计学意义（P ＜0.01）。（2）与正常组比较,二氯甲烷萃取物、乙酸乙酯萃取物及水提物能增加小鼠气管酚红排泌量,差异有统计学意义（P ＜ 0.01）。（3）与模型组比较,石油醚萃取物能减少哮喘小鼠BALF液中白细胞总数、嗜酸性粒细胞比例及中性粒细胞比例,差异有统计学意义（P ＜0.01）。结论 黄皮叶萃取物具有明显的镇咳、祛痰及平喘作用。     

Evaluation of analgesic and anti-inflammatory potential of Hedyotis puberula (G. Don) R. Br. ex Arn. in experimental animal models

Hedyotis puberula (G. Don) R. Br. ex Arn. is used for the treatment of several ailments in the traditional system of medicine. In the present study, the methanol extract of the whole plant (200 and 400 mg/kg) exhibited significant analgesic and anti-inflammatory activities in a dose dependent manner. The analgesic effect, evaluated in mice in hot plate as well as acetic acid-induced writhings, were higher than the standard drugs pentazocine (30 mg/kg) and indomethacin (5 mg/kg), respectively. Further, the methanol extract at the dose of 400 mg/kg produced significant inhibition of carrageenan induced paw edema and reduced the weight of granuloma in cotton pellet-induced granuloma pouch model.     

Anti-visceral obesity and antioxidant effects of powdered sea buckthorn (Hippophae rhamnoides L.) leaf tea in diet-induced obese mice

The potential health benefits of tea have long been studied. This study examined the role of powdered sea buckthorn leaf tea (SLT) in high-fat diet-induced obese mice. The mice were fed two different doses of SLT (1% and 5%, wt/wt) for six weeks. SLT suppressed body weight gain in a dose-dependent manner and significantly reduced visceral fat, plasma levels of leptin, triglyceride and total cholesterol and ALT activity compared with the high-fat-fed control mice. SLT also decreased hepatic triglyceride and cholesterol concentrations and lipid accumulation, whereas elevated fecal lipid excretion. High-fat feeding resulted in simultaneously decreasing hepatic FAS and G6PD activities and increasing PAP, β-oxidation and CPT activities. However, SLT supplementation during high-fat feeding led to a significant decrease in PAP, β-oxidation and CPT activities with a simultaneous increase in G6PD activity. The hepatic CYP2E1 activity and hepatic and erythrocyte lipid peroxides were significantly lowered with SLT supplements. Hepatic and erythrocyte SOD and CAT activities were also increased with SLT supplements in a dose-dependent manner, whereas GSH-Px activity was increased in erythrocytes only. These results indicate that SLT has potential anti-visceral obesity and antioxidant effects mediated by the regulation of lipid and antioxidant metabolism in high-fat diet-induced obese mice.     

Phytochemical profile, antioxidant, anti-inflammatory and hypoglycemic potential of hydroalcoholic extracts from Citrus medica L. cv Diamante flowers, leaves and fruits at two maturity stages

Since the past decade consumption of certain foods has been reported to have a positive effect on health. The object of the study was to determine for the first time the chemical composition and the antioxidant, anti-inflammatory and hypoglycemic potential of Citrus medica L. cv Diamante flowers, leaves and fruits (endocarp and mesocarp) at two maturity stages. Flowers and leaves were characterized by the highest total phenols and flavonoids content. A declining trend was observed during maturity of fruits for both phenols and flavonoids. The antioxidant activity evaluated by the β-carotene bleaching test showed a strong activity for flowers and endocarp of mature fruits with IC₅₀ values of 2.8 μg/mL and 3.5 μg/mL, respectively, after 30 min of incubation. Interestingly, the mature fruits endocarp (IC₅₀ value of 426.0 μg/mL) could inhibit α-amylase with an IC₅₀ value 2-fold higher than immature fruits. None of the tested extracts affected the proliferation of human skin fibroblasts 142BR. The obtained results suggest a potential use of C. medica L. cv Diamante as new valuable Citrus species with functional properties for food or nutraceutical product on the basis of high content of phytochemicals.