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PubMed2003

Anti-inflammatory activity of Elsholtzia splendens.

Elsholtzia splendens Nakai has been used in North-East Asia as an ingredient of folk medicines for treating cough, headache and inflammation. The present investigation was carried out to establish its in vivo anti-inflammatory activity using several animal models of inflammation and pain. The 75% ethanol extract of the aerial part of E. splendens significantly inhibited mouse croton oil-induced, as well as arachidonic acid-induced, ear edema by oral administration (44.6% inhibition of croton oil-induced edema at 400 mg/kg). This plant material also showed significant inhibitory activity against the mouse ear edema induced by multiple treatment of phorbol ester for 3 days, which is an animal model of subchronic inflammation. In addition, E. splendens exhibited significant analgesic activity against mouse acetic acid-induced writhing (50% inhibition at 400 mg/kg), while indomethacin (5 mg/kg) demonstrated 95% inhibition. E. splendens (5-100 microg/mL) significantly inhibited PGE2 production by pre-induced cyclooxygenase-2 of lipopolysaccharide-treated RAW 264.7 cells, suggesting that cyclooxygenase-2 inhibition might be one of the cellular mechanisms of anti-inflammation.

Animals↗

PubMed2006

Clematis vitalba L. aerial part exhibits potent anti-inflammatory, antinociceptive and antipyretic effects.

Extracts obtained from the dried aerial parts of Clematis species are used as folk remedy worldwide for the treatment of various inflammatory ailments such as rheumatism and to reduce fever. In order to test the effectiveness of extracts, fractions and subfractions from dried Clematis vitalba L. (Ranunculaceae) aerial parts were studied on mice. Extracts are shown to have a potent effect on carrageenan-induced hind paw edema and acetic acid-induced increased vascular permeability models. Through bioassay-guided fractionation procedures a new C-glycosylflavon, 4'-O-coumaroyl-isovitexine (vitalboside) was isolated as the main active ingredient of the aerial parts. Vitalboside showed a potent and dose-dependent (in 75 and 150 mg/kg does, per os) in vivo anti-inflammatory activity against acute (carrageenan-, serotonin- and PGE(2)-induced hind paw edema model, castor oil-induced diarrhea), subacute (subcutaneous air-pouch) and chronic (Freund's complete adjuvant-induced arthritis) models of inflammation. The same compound was also isolated as the main antinociceptive principle which was assessed by using the models based on the inhibition of p-benzoquinone-induced writhings, as well as antipyretic activity against Freund's complete adjuvant-induced increased body temperature. Acute and subchronic toxicity studies were also performed.

Analgesics, Non-Narcotic↗

PubMed2004

Study of the hypoglycaemic activity of Fraxinus excelsior and Silybum marianum in an animal model of type 1 diabetes mellitus.

The hypoglycaemic effect of the aqueous extracts of Fraxinus excelsior (FE) seed and Silybum marianum (SM) aerial part was investigated in normal and streptozotocin (STZ) diabetic rats. After a single dose or 15 daily doses, oral administration of the aqueous extracts (20 mg/kg) produced a significant decrease of blood glucose levels in both normal and STZ diabetic rats (P < 0.001). From the first week, the body weight was increased in normal rats (P < 0.05) and decreased in STZ rats (P < 0.01) after FE administration. In addition, no changes were observed in basal plasma insulin concentrations after both FE and SM treatments in either normal and STZ diabetic rats indicating that these plants exert their pharmacological activity without affecting insulin secretion. We conclude that the aqueous extracts of FE and SM exhibit potent hypoglycaemic and anti-hyperglycaemic activities in normal and STZ rats, respectively, without affecting basal plasma insulin concentrations.

Administration, Oral↗

PubMed2004

Inhibitors of the LPS-induced NF-kappaB activation from Artemisia sylvatica.

Three guaianolide sesquiterpene lactones, 3alpha,4alpha-epoxyrupicolins C-E, together with six known sesquiterpenes, artemisolide, 3-methoxytanapartholide, deacetyllaurenobiolide, moxartenolide as well as arteminolides B and D were isolated by bioassay-guided fractionation from the methanol extract of the aerial parts of Artemisia sylvatica using the NF-kappaB mediated reporter gene assay. All isolated compounds displayed inhibitory activity on the LPS-induced NF-kappaB activation, NO production, and TNF-alpha production with IC50 values of 0.49-7.17, 1.46-6.16, and 3.19-27.76 microM, respectively, in RAW264.7 cells. It was also established that arteminolide B suppressed the expression of NF-kappaB target genes such as iNOS and COX-2. This is the first report of NF-kappaB inhibitory activities of these compounds and supports the pharmacological use of Artemisia sylvatica, which has been employed as an herbal medicine for the treatment of inflammation.

Animals↗

PubMedDate not supplied

Oxygenated bisabolane fucosides from Carthamus lanatus L.

The aerial parts of Carthamus lanatus (Asteraceae) afforded four new oxygenated bisabolane fucosides, 10-hydroperoxy-bisabola-2,11-diene 7-O-beta-D-fucopyranoside, 11-hydro-peroxy-bisabola-2,9-diene 7-O-beta-D-fucopyranoside, 10-hydroxy-bisabola-2,11-diene 7-O-beta-D-fucopyranoside and 11-hydroxy-bisabola-2,9-diene 7-O-beta-D-fucopyranoside together with the known compounds a-bisabolol beta-D-fucopyranoside, asperuloside, sitosterol 3-O-beta-D-glucoside and stigmasterol 3-O-beta-D-glucoside. Asperuloside appears to be the second representative of the iridoid monoterpene group found in the plant family Asteraceae, which until recently was considered to lack iridoids. The main constituent a-bisabolol fucoside exhibited noticeable antibacterial and cytotoxic activities.

Anti-Infective Agents↗

PubMed2005

Digoniodiol, deoxygoniopypyrone A, and goniofupyrone A: three new styryllactones from Goniothalamus amuyon.

Three new styrylpyrone analogues, digoniodiol (2), deoxygoniopypyrone A (3), and goniofupyrone A (4), along with ten known styryllactones, were isolated from the aerial parts of Goniothalamus amuyon. Among these compounds, 2 is the first example of a bis-styrylpyrone. Compound 4 represents a new skeleton for styryllactones. All structures were established on the basis of spectroscopic data. The stereochemistry of 2 and 4 was determined by X-ray crystallographic analysis. The absolute configuration of 3 and 4 was further confirmed by Mosher ester derivatives. All styryllactones were subjected to cytotoxicity assays. Among them, goniothalamin, goniothalamin epoxide, and 8-chlorogoniodiol showed significant cytotoxicity against the HepG2 cancer cell line with IC50 in the range of 0.19 - 0.64 microg/mL, and moderate activity toward Hep3B, MDA-MB-231, and MCF-7 cancer cell lines.

Annonaceae↗

PubMed2005

C-glycosylflavones from the aerial parts of Eleusine indica inhibit LPS-induced mouse lung inflammation.

The infusion of aerial parts (EI) of Eleusine indica Gaertn (Poaceae) is used in Brazil against airway inflammatory processes like influenza and pneumonia. Pre-treatment with 400 mg/kg of crude extract inhibited 98% of lung neutrophil recruitment in mice exposed to aerosols of lipopolysaccharide (LPS) from Gram-negative bacteria, in a dose-dependent manner. At 400 microg/kg, schaftoside (6-C-beta-glucopyranosyl-8-C-alpha-arabinopyranosylapigenin) and vitexin (8-C-beta-glucopyranosylapigenin), isolated from EI, inhibited 62% and 80% of lung neutrophil influx, respectively. These results may justify the popular use of E. indica against airway inflammatory processes.

Animals↗

PubMed2005

Antitubercular sterols from Thalia multiflora Horkel ex Koernicke.

Bioassay guided isolation of an antitubercular extract of the aerial parts of Thalia multiflora led to the isolation of nine stigmast-5-ene and stigmasta-5,22-dien steroids, four isorhamnetin and quercetin flavonoid glycosides, two ceramides, an indole alkaloid and two simple phenolic compounds. Stigmast-5-en-3beta-ol-7-one (2), stigmast-4-ene-6beta-ol-3-one (3), stigmast-5,22-dien-3beta-ol-7-one (7) and stigmast-4,22-dien-6beta-ol-3-one (8) were found to be the most active compounds with MIC values of 1.98 +/- 0.02, 4.2 +/- 0.17, 1.0 +/- 0.06 and 2.2 +/- 0.3 microg/mL, respectively. Compounds 2, 3, 7 and 8 were not cytotoxic to Vero cells at 102 microg/mL. This investigation constitutes the first report of a chemical study of a species of the genus Thalia.

Antitubercular Agents↗

PubMed2006

Intestinal antiinflammatory activity of a lyophilized infusion of Turnera ulmifolia in TNBS rat colitis.

Turnera ulmifolia is a plant popularly known in Brazil and South America as chanana. Some species of Turnera are widely used in folk medicine for different types of inflammatory diseases. In this study, the preventive intestinal antiinflammatory activity of a lyophilized infusion obtained from the aerial parts of T. ulmifolia was tested in the trinitrobenzenesulphonic acid (TNBS) model of rat colitis. The results obtained revealed that pretreatment to colitic rats with the extract, at 250 and 500 mg/kg, significantly attenuated the colonic damage induced by TNBS. This beneficial effect was associated with an improvement in the colonic oxidative status, since the infusion prevented the glutathione depletion that occurred as a consequence of the colonic inflammation. On the other hand, this antioxidant activity was confirmed in in vitro studies. In conclusion, the preventive effect exerted by the lyophilized infusion of T. ulmifolia in the TNBS model of rat colitis is probably related to its antioxidant properties, due to its flavonoids content.

Administration, Oral↗

PubMed2003

Phytotoxic compounds from Flourensia cernua.

Bioassay-directed fractionation of a CH(2)Cl(2)-MeOH (1:1) extract of the aerial parts of Flourensia cernua led to the isolation of three phytotoxic compounds, namely, dehydroflourensic acid (1), flourensadiol (2) and methyl orsellinate (3). Dehydroflourensic acid is a new natural product whose structure was established by spectral means. In addition, the known flavonoid ermanin and seven hitherto unknown gamma-lactones were obtained, these being tetracosan-4-olide, pentacosan-4-olide, hexacosan-4-olide, heptacosan-4-olide, octacosan-4-olide, nonacosan-4-olide, and triacontan-4-olide. Compounds 1-3 caused significant inhibition of radicle growth of Amaranthus hypochondriacus and Echinochloa crus-galli, interacted with bovine-brain calmodulin and inhibited the activation of the calmodulin-dependent enzyme cAMP phosphodiesterase.

3',5'-Cyclic-AMP Phosphodiesterases↗

PubMed2004

Lipoxygenase inhibition by anadanthoflavone, a new flavonoid from the aerial parts of Anadenanthera colubrina.

Chemical investigation of the aerial parts of Anadenanthera colubrina led to the isolation of a new flavonoid named anadanthoflavone ( 1), along with 11 known compounds: alnusenol, lupenone, lupeol, betulinic acid, alpha-amyrin, beta-amyrin, beta-sitosterol, stigmasterol, apigenin, 4-hydroxybenzoic acid and cinnamic acid. The isolated compounds were evaluated for their inhibitory activity on human platelet 12-lipoxygenase (12-hLO), human reticulocyte 15-lipoxygenase (15-hLO) and soybean lipoxygenase-1 (15-sLO). Compound 1 was found to be active against 12-hLO and 15-hLO with IC50 values of 13 +/- 3 microM and 17 +/- 3 microM, respectively. Apigenin selectively inhibited the activity of 15-hLO (IC50 : 4.0 +/- 1 microM), while lupenone, lupeol and alpha-amyrin were found active against 15-sLO (IC50 : 22 +/- 3 microM, 35 +/- 9 microM and 15 +/- 3 microM, respectively).

Fabaceae↗

PubMed2006

Echinacea extracts modulate the pattern of chemokine and cytokine secretion in rhinovirus-infected and uninfected epithelial cells.

Extracts of Echinacea purpurea are among the most widely used herbal medicines throughout Europe and North America for the prevention or treatment of common cold, coughs, bronchitis and other upper respiratory infections. Popular preparations include expressed juice from the aerial parts of the plant (which contain polysaccharides) and alcoholic tinctures from roots (containing caffeic acid derivatives and alkylamides). Since immune modulation has been reported for similar extracts, cytokine antibody arrays were used to investigate the changes in the pro-inflammatory cytokines and chemokines released from a cultured line of human bronchial epithelial cells exposed to Rhinovirus 14 and two different chemically characterized Echinacea extracts. Virus infection stimulated the release of at least 31 cytokine-related molecules, including several important chemokines known to attract inflammatory cells. Most of these effects were reversed by simultaneous exposure to either of the two Echinacea extracts, although the patterns of response were different for the two extracts. These results could explain the antiinflammatory properties of Echinacea extracts. Furthermore, a number of these cytokines were stimulated by the same Echinacea preparations in uninfected cells. These observations therefore provide support for the alleged beneficial uses of Echinacea extracts.

Cell Line, Transformed↗

PubMed2006

Hepatoprotective effect of extracts from Pergularia daemia Forsk.

Pergularia daemia (Asclepiadaceae) is a perennial herb growing widely along the road sides of India. It has been used in folk medicine for the treatment of liver disorders. The aim of this work is to study the hepatoprotective effect of crude ethanolic and aqueous extracts from the aerial parts of Pergularia daemia. The aqueous and ethanolic extracts obtained from aerial parts of Pergularia daemia were evaluated for hepatoprotective activity in rats by inducing liver damage by carbon tetrachloride. The ethanolic extract at an oral dose of 200 mg/kg exhibited a significant (P<0.05) protective effect by lowering serum levels of glutamic oxaloacetic transaminase, glutamic pyruvic transaminase, alkaline phosphatase, total bilirubin and total cholesterol and increasing the levels of total protein and albumin levels as compared to silymarin used as a positive control. These biochemical observations were supplemented by histopathological examination of liver sections. The activity may be a result of the presence of flavonoid compounds. Furthermore, the acute toxicity of the extracts showed no signs of toxicity up to a dose level of 2000 mg/kg. Thus it could be concluded that ethanolic extract of Pergularia daemia possesses significant hepatoprotective properties.

Administration, Oral↗

PubMed2006

Bactericidal activity of organic extracts from Flourensia cernua DC against strains of Mycobacterium tuberculosis.

BACKGROUND: Tuberculosis is a chronic disease caused mainly by Mycobacterium tuberculosis. The emergence of antibiotic-resistant strains of this species underscores the need for novel effective drugs against resistant mycobacteria as first-line antituberculosis medications. METHODS: Crude aqueous (obtained by decoction, in accordance with the traditional mode of preparation), methanol, acetone, and hexane extracts from aerial parts of Artemisia ludoviciana Nutt., Chenopodium ambrosioides L., Marrubium vulgare L., Mentha spicata L., and Flourensia cernua DC were assessed for their ability to either inhibit the growth of or kill M. tuberculosis strains H37Rv and CIBIN:UMF:15:99, the former being sensitive to, and the latter resistant to, streptomycin, isoniazide, rifampin, ethambutol, and pyrazinamide. These five plant species are used in Mexico to treat respiratory disorders. RESULTS: Flourensia cernua was the uniquely active plant among those evaluated. Its hexane and acetone extracts not only inhibited the growth of but killed M. tuberculosis. The hexane extract showed a minimal inhibitory concentration (MIC) of 50 and 25 microg/mL against sensitive and resistant strains, respectively; the acetone extract was active against only CIBIN:UMF:15:99 (MIC = 100 microg/mL). CONCLUSIONS: The hexane extract from F. cernua leaves could be an important source of bactericidal compounds against multidrug-resistant M. tuberculosis.

Acetone↗

PubMed2006

[Studies on flavonoids of Andrographis paniculata].

OBJECTIVE: To study the flavonoids of the aerial parts of Andrographis paniculata. METHOD: Twelve flavonoids from the 85% EtOH extract were isolated by the silica gel column, Sephadex LH-20 column, ODS column chromatography and HPLC, and their structures were identified by the spectal analyses and chemical evidences. RESULT: The 12 compounds were obtained and identified as 7-O-methylwogonin (1), 7-O-methyldihydrowogonin (2), 5-hydroxy-7, 8, 2', 5'-tetramethoxy-flavone (3), skullcapflavone-2'-methoxylether (4), 5-hydroxy-7, 8, 2', 3'-tetramethoxyflavone (5), 5, 4'-dihydroxy-7, 8, 2', 3'-tetramethoxyflavone (6), dihydroskullcapflavone (7), 5, 7, 8-trimethoxydihydroflavone (8), 5, 2'-dihydroxy-7, 8-dimethoxyflvone (9), andrographidine C (10), 5, 7, 4'-trihydroxyflavone (11), 5, 7, 3', 4'-tetrahydroxyflavone (12). CONCLUSION: Compound 6 is a new naturally occurring product isolated from A. paniculata, and compound 8, 11 and 12 are obtained for the first time from the Andrographis species.

Andrographis↗

PubMed2006

Analgesic activity of the methanolic extract and total alkaloids of Glaucium paucilobum.

The species of Glaucium have been used in Iranian herbal medicine as laxative, hypnotic, narcotic, and antidiabetic agents and also in the treatment of dermatitis. The analgesic activity of the aerial parts of Glaucium Freyn (Papaveraceae), a native plant of Iran, were studied using formalin, hot plate, and writhing tests in rodents. The methanolic extract and total alkaloids of Glaucium paucilobum caused graded inhibition of both phases of formalin-induced pain. In the hot plate test, i.p. administration of G. paucilobum extract at the doses of 50-90 mg/kg and total alkaloids at the dose of 10-60 mg/kg significantly raised the pain threshold at an observation time of 30 min in comparison with control (p < 0.001). In the writhing test, the extract at the doses of 30-90 mg/kg and total alkaloids at the doses of 10-60 mg/kg produced a significant decrease in the number of writhings in comparison with the control group (p < 0.001). The methanolic extract and total alkaloids of G. paucilobum, at antinociceptive doses, did not affect the motor coordination of animals when assessed in the rotarod model. The results showed that analgesic activity of this plant may be related partly to the alkaloids.

Acetic Acid↗

PubMed2004

Antiinflammatory activity of Synurus deltoides.

Synurus deltoides Aiton, Nakai, is an edible plant that has been used as a folk medicine for treating inflammatory disorders. This investigation was carried out to establish the antiinflammatory activity of this plant material using a 75% ethanol extract from the aerial part of S. deltoides. Against the acute inflammatory animal model of mouse croton oil-induced ear oedema assay, the extract did not show significant inhibition at 100-800 mg/kg by oral administration. On the other hand, the extract showed considerable inhibition against the chronic inflammatory animal model of rat adjuvant-induced arthritis (25% inhibition at 100 mg/kg/day) while prednisolone exerted 40% inhibition at 10 mg/kg/day. In addition, S. deltoides possessed strong analgesic activity (IC50 = 50 mg/kg) in the acetic acid-induced writhing test. From the extract, ursolic acid and scopoletin were successfully isolated and their contents were found to be 0.31% and 0.37% (w/w), respectively, based on the dried extract by HPLC analysis. All the results obtained indicate that this plant material may be used beneficially as an antiinflammatory agent having analgesic action.

Acetic Acid↗

PubMed2005

Evaluation of some medicinal plant extracts for antidiarrhoeal activity.

The antidiarrhoeal effect of seven plant extracts namely: the aerial parts of Euphorbia paralias L. (EP), Bidens bipinnata L. (BB), Cynachum acutum L. (CyAc), Diplotaxis acris (Forssk.) Boiss (DA), Convolvulus fatmensis (CF) and Schouwia thebaica Webb (ST) and the leaves of Plantago major L. (PM), was evaluated on castor oil-induced diarrhoea, gastrointestinal movement in rats (charcoal meal) and on the motility of duodenum isolated from freshly slaughtered rabbits. A significant antidiarrhoeal effect of the tested plant extracts against castor oil-induced diarrhoea in rats was achieved by 200 and 400 mg/kg. The tested plant extracts decreased the gastrointestinal movement as indicated by the significantly (p<0.05 to 0.001) decreased distance travelled by the charcoal meal. The large dose of the tested plant extracts was slightly more effective than the small one. The antidiarrhoeal effect was confirmed by the reported dose dependent inhibition of the motility of duodenum isolated from freshly slaughtered rabbits. The EP and PM methanol extract produced a transient stimulation followed by inhibition in doses of less than 0.05 and 1.6 mg/kg, respectively. Higher concentrations caused rapid muscle relaxation. Tannins, flavonoids, unsaturated sterols/triterpenes, carbohydrates, lactones and proteins/amino acids were reported as major active constituents of the tested plants.

Administration, Oral↗