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Ethnopharmacological relevance Ficus deltoidea Jack (FD) is widely consumed in traditional medicine as a treatment for various diseases in Malaysia. Each part of the plant such as its leave, stem, fruit and root are used traditionally to treat different types of diseases. Vitexin and isovitexin are bioactive compounds abundantly found in the leaves of FD that possessed many pharmacological properties including neuroprotection. Nonetheless, its effects on key events in neuroinflammation are unknown. Aim of the study: To determine the inhibitory properties of FD aqueous extract on pro-inflammatory mediators involved in lipopolysaccharide (LPS)-induced microglial cells. Methods Vitexin and isovitexin in the extract were quantified via high performance liquid chromatography (HPLC). The extract was evaluated for its cytotoxicity activity via 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Pre-treatment with the extract on LPS-induced microglial cells was done to determine its antioxidant and anti-neuroinflammatory properties by measuring the level of reactive oxygen species (ROS), nitric oxide (NO), tumour necrosis factor alpha (TNF-α), interleukin-1β (IL-1β) and interleukin-6 (IL-6) via 2′-7′-dichlorofluorescin diacetate (DCFDA) assay, Griess assay and Western blot respectively. Results The extract at all tested concentrations (0.1 μg/mL, 1 μg/mL, 10 μg/mL, 100 μg/mL) were not cytotoxic as the percentage viability of microglial cells were all above ~80%. At the highest concentration (100 μg/mL), the extract significantly reduced the formation of ROS, NO, TNF-α, IL-1β and IL-6 in microglial cells induced by LPS. Conclusion The extract showed neuroprotective effects by attenuating the levels of pro-inflammatory and cytotoxic factors in LPS-induced microglial cells, possibly by mediating the nuclear factor-kappa B (NF-κB) signalling pathway.

Ethnopharmacological relevance Tsantan Sumtang (TS), a traditional Tibetan medicine, has been used in the clinic for the treatment of myocardial ischemia (MI) for ages, however, the bioactive ingredients that are responsible for improving MI remain unknown. Aim of the study This study investigated the chemical components of TS and their medicinal efficacies at cell levels, in order to expound the bioactive ingredients in TS. Materials and methods First, a response-surface methodology was employed to determine the optimum ethanol reflux extraction process of polyphenols in TS (PTS) due to their close correlation with MI improvement. Second, a serum pharmacochemistry technique was used to analyze the compounds of PTS absorbed into the blood of rats. Third, hypoxia-, H2O2-, and adriamycin (ADM)-induced H9c2 cell injury models were used to investigate the cardioprotective effects of these compounds in vitro. Fourth, protective effects of isovitexin, quercitrin, and isoeugenol on mitochondrial function were further tested. Results The optimum extraction conditions for obtaining PTS were an ethanol concentration of 78.22%, an extraction time of 67.4 min, and a material–liquid ratio of 1:72.60 mL/g. Serum pharmacochemistry analysis detected 21 compounds, of which 11 compounds were always present in the blood within 5 hours. Cytotoxicity and the protective effect of 11 compounds in hypoxia-, H2O2-, and ADM-induced H9c2 cell injury models shown that isovitexin, quercitrin, and isoeugenol had almost no cytotoxicity, and they could elevate the survival rate in injured H9c2 cells. Furthermore, isovitexin, quercitrin, and isoeugenol could decrease mitochondrial reactive oxygen species (ROS) releasion, inhibite mitochondrial permeability transition pore (mPTP) opening, ameliorate the change of mitochondrial membrane potential (MMP) to exert mitochondrial protection effect. Conclusion Isovitexin, quercitrin, and isoeugenol exhibited cardioprotective effect at cell levles, these three compounds might be the bioactive ingredients in TS. These findings elucidate the pharmacodynamic substances and mechanisms of TS, guiding its clinical use.

Ethnopharmacological relevance Numerous Alphonsea species including Alphonsea elliptica (mempisang) leaves and fruits are indigenously used in inflammatory conditions such as postpartum swelling and rheumatism in southeast Asian countries. In our previous in-vitro findings, A. elliptica methanol extract exhibited platelet-activating factor inhibition, suggesting the presence of phyto-constituents with anti-inflammatory potential. Aim of the study However, so far there is no literature available on the anti-inflammatory activity of this species. Henceforth, based on the above background and our previous laboratory findings, we hypothesize that phytoconstituents of A. elliptica could possess anti-inflammatory potential against inflammatory mediators including prostaglandin-E2 (PGE2), cyclooxegenase-2 (COX-2) and cytokines (IL-1β and IL-6). Materials and methods Vacuum and column chromatography techniques were employed for the isolation of phytoconstituents. The structure elucidation was carried out using HRESI-MS, 1H and 13C-NMR analysis and compared with the published literature. For cytotoxicity analysis, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay was performed on peripheral blood mononuclear cells. In-vitro anti-inflammatory activities were evaluated against the levels of PGE2, COX-2, IL-1β and IL-6 in lipopolysaccharide (LPS)-induced human plasma using enzyme-linked immunosorbent assay and radioimmunoassay. Results Unprecedentedly, chromatographic purification of methanolic leaves extract afforded five flavones namely vitexin, isovitexin, orientin, isoorientin, schaftoside with three flavanols; kaempferol, myricetin and rutin from A elliptica. In cell viability analysis, isolates did not present cytotoxicity up to 50 μM. In anti-inflammatory evaluation, orientin and isoorientin exhibited strong (≥70%), while isovitexin and vitexin produced strong to moderate (50–69%) PGE2, COX-2, IL-1β and IL-6 inhibition at 25 and 50 μM. Isoorientin, orientin, isovitexin, and vitexin showed significant (p Conclusion Conclusively, isolated phytoconstituents are reported for the first time from the A. elliptica. Moreover, isovitexin, vitexin orientin and isoorientin abrogated LPS-induced inflammatory responses in human plasma at non-cytotoxic concentrations.

Ethnopharmacological relevance Combretum aculeatum Vent was traditionally used in Sudan, Eretria and Ethiopia as anti-inflammatory in case of skin inflammation, catarrh, wounds, scorpion stings and snake bites. Nevertheless, there is no scientific information regarding this activity. Aim of study The present study aimed to evaluate the phytochemical constituents and the scientific basis for the traditional use of Combretum aculeatum Vent through studying its anti-inflammatory properties for the first time to illustrate the putative mechanisms behind this bioactivity. Materials and methods the ethanolic extract was partitioned by petroleum ether, methylene chloride, ethyl acetate, and n-butanol saturated with water. The petroleum ether fraction was saponified and the saponifiable and unsaponifiable fractions were analyzed on GC/MS. The different fractions were subjected to phytochemical investigation to isolate pure compounds. In-vivo anti-inflammatory activity of the ethanolic extract was evaluated using carrageenan induced rat paws edema method at doses of 200, 400 and 600 mg/kg and proved based on histopathological and biochemical parameters. Results Five known compounds were isolated for the first time from the aerial parts of Combretum aculeatum Vent: quercetin, vitexin, isorhamnetin 3-O-β-glucoside, isovitexin and rutin, in addition to two previously isolated ones: β-sitosterol and its glucoside. The ethanolic extract evidenced in-vivo anti-inflammatory activity by oral intake of 400 mg/kg of the ethanolic extract significantly (P ≥ 0.05) decreased the paw edema (only 32±1.9% increase in paw weight after 4 h) compared to indomethacin (28.6±2.5%). Moreover, it significantly suppressed the serum malondialdehyde (MDA) and nitric oxide (NO) and increased the GSH to be 11.76±0.85, 5.13±0.62 μmol/mL and 5.66±0.28 μM/mL, respectively. It diminished the serum cytokines TNF-α, IL-6 and IL-1β levels to be 39.1±1.2, 32.6±1.1 and 37.5±1.2 pg/mL, respectively. Results are accompanied by histopathological examination. Conclusion Overall, the results herein presented significant anti-inflammatory properties traditionally ascribed to Combretum aculeatum Vent. Moreover, the biochemical mechanisms associated to this action were highlighted, introducing new prospects for the development of effective anti-inflammatory herbal medicinal products.

Ethno-pharmacological relevance Artemisia judaica L is an aromatic medicinal plant growing widely in Saint Katherine, Sinai, Egypt, and used in traditional medicine as a herbal remedy for antibacterial, anthelmintic, antidiabetic, analgesic and anti-inflammatory activities. Additionally, other Arabic regions commonly used it in their folk medicines for the treatment of fungal infections, atherosclerosis, cancer, diabetes, arthritis, and inflammatory-related diseases. Aim of the study Based on the traditional medicinal uses of A. judaica, the present study was designed to validate some of the traditional uses as the analgesic, anti-inflammatory, antipyretic, hepatoprotective, antidiabetic, and antioxidant activities of 80% aqueous methanol extract (AME) of A. judaica aerial parts as well as isolation and identification of its flavonoid content. Materials and methods AME of A. judaica aerial parts was fractionated using column chromatography and the structures of the isolated compounds were established using different spectroscopic data. Analgesic activity was evaluated using acetic acid-induced writhing in mice; antipyretic activity was assessed using yeast suspension-induced hyperthermia in rats; anti-inflammatory activity was evaluated using carrageenan-induced paw edema; the hepatoprotective effect was studied by measuring liver enzymes in carbon tetrachloride(CCl4)-induced hepatotoxicity rats while antidiabetic activity was estimated in alloxan hyperglycemia. Results Eight flavone compounds namely luteolin 4′ methyl ether 7-O-β-D-4C1-glucopyranoside (1), 8-methoxyapigenin 7-O-β-D-4C1-galactopyranoside (2), isovitexin (3), 8-methoxyluteolin 7-O-β-D-4C1-glucopyranoside (4), diosmetin (5), cirsimaritin (6), luteolin (7), and apigenin (8) were identified from AME of A. judaica. The AME was found to be non-toxic to mice up to 5 g/kg b.w. Moreover, it exhibits significant analgesic antipyretic, anti-inflammatory, antidiabetic, hepatoprotective, and antioxidant activities in a dose-dependent manner. Conclusion The AME was nontoxic; it exhibits significant analgesic, antipyretic, anti-inflammatory, antidiabetic, hepatoprotective, and antioxidant activities. Moreover, the isolated flavone was identified from AME for the first time.

Ethnopharmacological relevance The leaves of Ficus deltoidea are used as a traditional medicine by diabetes patients in Malaysia. Aim of the study The objective of the study is to identify and evaluate bioactive constituents with in vivo α-glucosidase inhibition. Materials and Methods The partitioned extracts, subfractions and pure bioactive constituents were subjected to α-glucosidase inhibition assay. The identified bioactive constituents were administered orally to sucrose loaded normoglycemic mice and induced diabetic rats. The postprandial blood glucose levels were monitored at 30 min interval. Acute toxicity was evaluated in both normoglycemic mice and induced diabetic rats. Results Bioactivity guided fractionation led to the isolation of both vitexin (1) and isovitexin (2). Oral administration of 1 mg/kg of either vitexin (1) or isovitexin (2) significantly (p

Aim of the study To compare the anxiolytic activities and flavonoid compositions of the two populations of the species Passiflora edulis, Passiflora edulis ‘edulis’ with purple fruit and Passiflora edulis ‘flavicarpa’ with yellow fruit. Materials and methods Four samples for each population of Passiflora edulis were collected from different districts of China. Swiss albino mice were used as experimental animals in elevated plus-maze (EPM) test to assay the anxiolytic effects of ethanol extracts of the samples. The conventional parameters and ethological items of the behavior of the mice were recorded and analyzed. Flavonoid compositions of the samples were analyzed by RP-HPLC monitored with diode array detection and the chromatograms were compared. Results The ethanol extracts of the samples of Passiflora edulis ‘flavicarpa’ displayed anxiolytic activity at 400 mg/kg, while those of Passiflora edulis ‘edulis’ exhibited sedative effect at 400 mg/kg. The chromatograms of the samples belonging to similar population of Passiflora edulis were identical, but those belonging to different population were distinct from each other. The series of peaks between 16 and 24 min in the chromatograms of Passiflora edulis ‘flavicarpa’ did not appear in those of Passiflora edulis ‘edulis’, either did the peaks between 54 and 90 min in chromatograms of Passiflora edulis ‘edulis’ not appear in those of Passiflora edulis ‘flavicarpa’. The six major flavonoid compounds isolated from the leaves of Passiflora edulis ‘flavicarpa’, lucenin-2, vicenin-2, isoorientin, isovitexin, luteolin-6-C-chinovoside, and luteolin-6-C-fucoside, had not been detected in Passiflora edulis ‘edulis’. Conclusions Passiflora edulis ‘flavicarpa’ is extremely different from Passiflora edulis ‘edulis’ and they should be distinguished when pharmacological studies are performed on them. The aerial part of Passiflora edulis ‘flavicarpa’ is possible to be utilized as the resource of Passionflower Extract.

Aim of the study Dianthus versicolor (Caryophyllaceae) and Lilium pumilum (Liliaceae) are two medicinal plants used in traditional Mongolian medicine to treat hepatic and gastrointestinal disorders. In this study aqueous (AE) and methanolic (ME) extracts of Dianthus versicolor and Lilium pumilum were investigated for their influence on the bile flow. The aqueous extracts of both plants were tested in absence and presence of 10 μM taurocholic acid at three different concentrations (100, 250, and 500 mg/L). The aqueous extract of Dianthus versicolor was further purified in order to locate the active principles. Two resulting fractions, one enriched in flavonoids and the other in sugars, were investigated for their influence on the bile flow in absence of taurocholic acid at 10, 20, and 40 mg/L. The aqueous extracts of both plants were analysed qualitatively by LC-MSn and quantitatively by UV-spectrophotometry. Materials and methods The bile flow experiments were performed in the isolated perfused rat liver. The compounds were identified by LC-DAD-MSn and TLC using references. The UV-spectrophotometric analysis was based on the monograph “Passiflorae herba” of the European Pharmacopoeia, and the total flavonoid contents were calculated and expressed as vitexin. Results AE and ME of both plants increased the bile flow dose-dependently (between 9% and 30%), and no hepatotoxic effect was seen even during longer perfusions. Stimulation of bile secretion was comparable in the presence and in the absence of taurocholic acid. The flavonoid fraction of Dianthus versicolor increased the bile flow by 18% (p

Ethnopharmacological relevance The leaves of Piper carpunya Ruiz & Pav. (syn Piper lenticellosum C.D.C.) (Piperaceae), are widely used in folk medicine in tropical and subtropical countries of South America as an anti-inflammatory, anti-ulcer, anti-diarrheal and anti-parasitical remedy as well as an ailment for skin irritations. Aims of the study To study the anti-inflammatory, anti-secretory and anti-Helicobacter pylori activities of different fractions isolated from an ethanolic extract of the leaves of Piper carpunya, in order to provide evidence for the use of this plant as an anti-ulcer remedy. Moreover, to isolate the main compounds of the extract and relate their biological activity to the experimental results obtained with the fractions. Materials and methods Sixteen fractions were obtained from the ethanolic extract (F I–XVI) and 16 pure compounds were isolated and identified from these fractions. We studied the effects of the fractions (0.1–400 μg/mL) on the release of myeloperoxidase (MPO) enzyme from rat peritoneal leukocytes, on rabbit gastric microsomal H+, K+-ATPase activity and anti-Helicobacter pylori anti-microbial activity using the microdilution method (MM). The main compounds contained in the fractions were isolated and identified by 1H- and 13C NMR spectra analysis and comparison with the literature data. Results Eight fractions showed inhibition of MPO enzyme (F I–IV, X, XII, XIV and XV). The highest inhibition was observed with F XIV (50 μg/mL, 60.9%, p

Taiuiá or tayuya (Cayaponia tayuya, Cucurbitaceae) is a climbing, lignified plant with a large swollen root that has traditionally been used as an anti-inflammatory and anti-rheumatic agent in the folk medicine of Brazil, Peru, and Colombia.We have assayed the pharmacological properties of a flavonoid fraction obtained from the butanol extract of Cayaponia tayuya roots using two models of topical mouse ear oedema, paying special attention to its influence on the induction on pro-inflammatory enzymes and peptidic mediators.The in vivo experiments involved both the acute oedema induced by a single application of TPA and the subchronic inflammation brought on by repeated applications of TPA. The effects on the induction of pro-inflammatory enzymes and peptidic mediators in RAW 264.7 macrophages were analyzed with the aid of Western blot analysis.The extract was identified as a mixture of flavonoids in which vicenin-2, spinosin, isovitexin, and a mixture of swertisin and isoswertisin were found. In acute TPA-induced oedema in mouse ears, the flavonoid-enriched fraction (at a dose of 0.5mg/ear) inhibited the oedema by 66% (4.2+/-0.6 mg vs. 12.3+/-1.4 mg, P0.01) while in the subchronic model, the inhibition reached 37% at a dose of 0.5mg/ear x 7 applications (7.5+/-0.6 mg vs. 11.9+/-1.3mg, P0.05). When assayed in vitro, the flavonoid showed no toxicity at 33.45 microg/mL on RAW 264.7 macrophages. Although the nitric oxide production in these cells was moderately reduced (42%) at 33.45 microg/mL, the flavonoid-enriched fraction had no effect on TNF-alpha production. In addition, at 22.30 microg/mL, the test sample inhibited both iNOS and COX-2 expression by 98% and 49%, respectively.These results indicate that the anti-inflammatory activity of flavonoids from tayuya roots most likely stems from their inhibition of the induction of the enzymes COX-2 and iNOS.

The spasmolytic effects of an acqueous extract of cedrón (AEC) were studied on rat isolated duodenums. This plant (Aloysia citriodora Palau, Verbenaceae) is widely used for gastrointestinal disorders and as eupeptic in South America. AEC non-competitively inhibited the dose–response curve (DRC) of Ach (IC50 of 1.34 ± 0.49 mg lyophilized/mL) and the DRC of Ca2+ in high-[K2−]o (IC50 of 2.64 ± 0.23 mg/mL). AEC potentiated the non-competitive inhibition of either 30 μmol/L W-7 (a calmodulin blocker) and 5–15 μmol/L papaverine on the Ca2+-DRC. Also, AEC relaxed the contracture produced by high-[K+]o (IC50 of 2.6 ± 0.2 mg/mL) until 81.0 ± 3.2% of the maximal effect of papaverine and 78.1 ± 5.0% of the quercetin, the most selective inhibitor of PDE. The AEC relaxation was non-competitively inhibited by 10–30 μmol/L methylene blue and competitively antagonized by 40 mmol/L TEA. The relaxation of 1 mg/mL AEC was inhibited by hypoxia, but not that of 2 mg/mL. Two flavonoids were identified by HPLC in the AEC: vitexin and isovitexin. Vitexin non-competitively inhibited the Ach-DRC ( of 5.7 ± 0.4) but significantly run leftward the DRC of Ca2+. Isovitexin did not significantly inhibit the DRC of Ach nor Ca2+. The results suggest that the spasmolytic effect of AEC could be mostly associated to the increase in cGMP (target shared with the PDE inhibitors) and the activation of K+-channels. At low concentrations, AEC also inhibits the aerobic metabolism. The flavonoid vitexin is partially responsible for the effect, since it non-competitively inhibits Ach but not the Ca2+ influx. Isovitexin was devoid of activity on duodenums. Fil: Ragone, María Inés. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas. Cátedra de Farmacología; Argentina Fil: Sella, Mariana. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas. Cátedra de Farmacología; Argentina Fil: Conforti, Paula Andrea. Provincia de Buenos Aires. Gobernación. Comisión de Investigaciones Científicas. Centro de Investigación y Desarrollo en Criotecnología de Alimentos. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Centro de Investigación y Desarrollo en Criotecnología de Alimentos. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Centro de Investigación y Desarrollo en Criotecnología de Alimentos; Argentina Fil: Volonté, María G.. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas. Cátedra de Control de Calidad de Medicamentos; Argentina Fil: Consolini, Alicia Elvira. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas. Cátedra de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina

Lyophilised hydroalcoholic and aqueous extracts of the aerial parts of Passiflora incarnata L. (Passifloraceae) (Passion-flower), as well as chemical constituents of the plant, indole alkaloids (harman, harmin, harmalin, harmol, and harmalol) maltol and flavonoids (orientin, isoorientin, vitexin and isovitexin) were assessed for behavioral effects in mice. The accordance with the traditional use of P. incarnata, psychotropic properties were confirmed by some behavioral tests in mice. The anxiolytic properties of hydroalcoholic extract were confirmed at 400 mg/kg by the increase of rears and steps climbed in the staircase test (non-familiar environmental test), and the increase in locomotion and time spent in light side in the light/dark box choice test (non-familiar environmental test). The sedative properties of aqueous extract were confirmed at 400 g/kg by decrease of rears and steps climbed in the staircase test and the decrease of rears and locomotion in the free exploratory test. Moreover, the aqueous extract induced sleep in mice after treatment with a sub-hypnotic dose of pentobarbital.