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Pharmacological activities of some Argyranthemum species growing in the Canary Islands.

Methanolic extracts of eight subspecies of genus Argyranthemum were evaluated against brine shrimps, human cancer cell lines, malarial parasites and microorganisms under in vitro conditions. In the shrimp assay, samples of A. adauctum ssp. adauctum, A. adauctum ssp. erythrocarpon and A. frutetescens ssp. succulentum were active with ED50 values in the range of around 300 to 360 microg/ml. In the Caco-2, HepG2 and MCF-7 cell lines, the samples A. adauctum ssp. jacobaeifolium and A. adauctum ssp. palmensis were active with LC50 values ranging between 80-90 microg/ml. The secondary assay results of antimalarial activity of samples, A. adauctum ssp. adauctum, A. adauctum ssp. dugourii, A. adauctum ssp. erythrocarpon and A. adauctum ssp. jacobaeifolium have IC50 values <50 microg/ml. The samples demonstrated broad specific antimicrobial activity against five different microorganisms.

Animals↗

The hepatoprotective action of ten herbal extracts in CCl4 intoxicated liver.

The effect of ten phytotherapeutic products on CCl(4) intoxicated liver in albino male Wistar rats was investigated. Biochemical parameters, including serum transaminase activity (GPT and GOT), histoenzymological measurements (lactate dehydrogenase, LDH; succinate dehydrogenase, SDH, cytochromoxidase, CyOx; Mg(2+)-dependent adenosine triphosphatase, ATP-ase) and histochemical (Sudan black) and histological examinations (haematoxylin-eosin staining) of the liver were investigated. Some positive effects such as the reduction of hepatocytolysis and steatosis, and a return to normal values of the activity of some enzymes in the following plants: Chrysanthemum balsamita, Echinacea pallida, Calendula officinalis and Corylus avelana were obtained.

Animals↗

Phytochemical, pharmacological and toxicological aspects of Hibiscus sabdariffa L.: a review.

This article reviews the reported phytochemical, pharmacological and toxicological properties of Hibiscus sabdariffa L. (English: roselle, red sorrel; Arabic: karkade), the calyces of which are used in many parts of the world to make cold and hot drinks. Nutritionally, these contain ascorbic acid (vitamin C). In folk medicine, the calyx extracts are used for the treatment of several complaints, including high blood pressure, liver diseases and fever. The pharmacological actions of the calyx extracts include strong in vitro and in vivo antioxidant activity. In rats and rabbits, the extract showed antihypercholesterolaemic, antinociceptive and antipyretic, but not antiinflammatory activities. In rat and man a strong antihypertensive action has been demonstrated. The effects of the calyx extracts on smooth muscles in vitro are variable, but they mostly inhibit the tone of the isolated muscles. In healthy men, consumption of H. sabdariffa has resulted in significant decreases in the urinary concentrations of creatinine, uric acid, citrate, tartrate, calcium, sodium, potassium and phosphate, but not oxalate. Oil extracted from the plant's seeds has been shown to have an inhibitory effect on some bacteria and fungi in vitro. The plant extracts are characterized by a very low degree of toxicity. The LD50 of H. sabdariffa calyx extract in rats was found to be above 5000 mg/kg. A single report has suggested that excessive doses for relatively long periods could have a deleterious effect on the testes of rats. In view of its reported nutritional and pharmacological properties and relative safety, H. sabdariffa and compounds isolated from it (for example, anthocyanins and Hibiscus protocatechuic acid) could be a source of therapeutically useful products.

Animals↗

Cytotoxic constituents of the twigs of Simarouba glauca collected from a plot in Southern Florida.

Activity-guided fractionation of a chloroform-soluble extract of Simarouba glauca twigs collected from a plot in southern Florida, and monitored with a human epidermoid (KB) tumor cell line, afforded six canthin-6-one type alkaloid derivatives, canthin-6-one (1), 2-methoxycanthin-6-one (2), 9-methoxycanthin-6-one (3), 2-hydroxycanthin-6-one (4), 4,5-dimethoxycanthin-6-one (5) and 4,5-dihydroxycanthin-6-one (6), a limonoid, melianodiol (7), an acyclic squalene-type triterpenoid, 14-deacetyleurylene (8), two coumarins, scopoletin (9) and fraxidin (10), and two triglycerides, triolein (11) and trilinolein (12). Among these isolates, compounds 1-4, 7 and 8 exhibited cytotoxic activity against several human cancer cell lines. 14-Deacetyleurylene (8) was selectively active against the Lu1 human lung cancer cell line, but was inactive in an in vivo hollow fiber assay using this same cell type.

Antineoplastic Agents, Phytogenic↗

Comparison of the antiinflammatory effects of Drosera rotundifolia and Drosera madagascariensis in the HET-CAM assay.

The antiinflammatory effects of ethanol and aqueous extracts from Drosera rotundifolia and from Drosera madagascariensis were compared in vivo in the HET-CAM assay. Both extracts from D. rotundifolia and the ethanol extract from D. madagascariensis showed remarkable efficacy at doses of 500 microg/pellet. The inhibition of the inflammation by the extracts was stronger than that by 50 microg hydrocortisone/pellet. In contrast, there was only a very weak effect observed at a dose of 500 microg/pellet of the water extract from D. madagascariensis. The chemical analyses of the extracts showed that the effect cannot be attributed to naphthoquinones, but might be due to flavonoids. Ellagic acid obviously plays an important role in the antiangiogenic effect of the Drosera extracts.

Allantois↗

Evaluation of antipyretic activity of Calotropis gigantea (Asclepiadaceae) in experimental animals.

The roots of Calotropis gigantea have been used in leprosy, eczema, syphilis, elephantiasis, ulceration and cough in the Indian system of traditional medicine. The present communication evaluated its antipyretic activity by using yeast-induced and TAB (Typhoid) vaccine-induced pyrexia in rats and rabbits. In both yeast-induced and TAB vaccine-induced fever, the fever was significantly reduced and the body temperature was normalized by administration of 200 and 400 mg/kg dose intraperitoneally. Based on the results of the present study it can be concluded that the extract of C. gigantea has potential antipyretic activity against both yeast-induced and TAB vaccine-induced fever, indicating the possibility of developing C. gigantea as a cheaper and potent antipyretic agent.

Analgesics, Non-Narcotic↗

Stimulation of lymphocyte proliferation and inhibition of nitric oxide production by aqueous Urtica dioica extract.

The immunomodulatory and antiinflammatory activities of aqueous Urtica dioica extract were investigated for their effect on the mitogenic response of murine splenocytes and nitric oxide production by murine peritoneal macrophages in vitro. It was found that this extract stimulated the proliferation of T-lymphocytes and suppressed NO production in lipopolysaccharide-stimulated macrophages without affecting cell viability.

Animals↗

Structure-activity relationship for antiinflammatory effect of luteolin and its derived glycosides.

Luteolin and its derived glycosides such as a cynaroside, cesioside, isoorientin and stereolensin have been isolated and identified from different kinds of plant species. A (13)C NMR spectroscopic analysis of stereolensin has been done for the first time. These structurally related flavonoids were examined in vitro for their abilities to inhibit enzymes for the synthesis of thromboxane B(2) and leukotriene B(4) as well as hydrogen peroxide scavenging activity. Luteolin exhibited a high inhibitory activity against both thromboxane and leukotriene synthesis. In particular, a remarkable inhibitory effect was observed against leukotriene enzyme activity. The glycosides, cynaroside and cesioside, possessed a moderate inhibition activity against both enzyme synthesis pathways, while isoorientin and stereolensin exhibited selectively good activity against thromboxane synthesis. All the flavonoids showed excellent scavenging activity for the hydrogen peroxide at all the concentrations tested. The results demonstrated that the reactivities of luteolin and its related glycosides against arachidonic acid synthesis and hydrogen peroxide scavenging are dependent on their molecular structures. The presence of ortho-dihydroxy groups at the B ring and OH substitution pattern at C-5 position of the A ring could significantly contribute to the antiinflammatory and antioxidant activities of flavonoids.

Animals↗

Phytochemical investigation and antioxidant activity of Duranta repens.

The ethylacetate fraction of the methanol extract of Duranta repens L. (Verbenaceae) showed radicalscavenging activity in the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay. Three compounds were isolated from this fraction, i.e. the phenylethanoid glycoside acteoside, the iridoid lamiide and the saponin pseudo-ginsenoside-RT1. Acteoside showed an IC50 of 3.05 +/- 0.09 microg/mL in the DPPH assay, while lamiide and pseudo-ginsenoside-RT1 were not active.

Free Radical Scavengers↗

Effects of two Prunella species on lymphocyte proliferation and nitric oxide production.

Water extracts of Prunella vulgaris and P. laciniata have been investigated for their immunomodulatory and antiinflammatory activities concerning their effect on the mitogenic response of murine splenocytes and nitric oxide production by murine peritoneal macrophages in vitro. It was found that both extracts stimulated the proliferation of T-lymphocytes and suppressed NO production in lipopolysaccharide-stimulated macrophages dose dependently without any cytotoxicity.

Animals↗

Composition and antimicrobial activity of Equisetum arvense L. essential oil.

The volatile constituents of the sterile stems of Equisetum arvense L. (Equisetaceae) were investigated for the first time using GC, GC/MS and (13)C-NMR. Twenty-five compounds were identified. Hexahydrofarnesyl acetone (18.34%), cis-geranyl acetone (13.74%), thymol (12.09%) and trans-phytol (10.06%) were the major constituents. A disk diffusion method was used for the evaluation of the antimicrobial activity of this oil against a panel of microorganisms (bacteria: Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa and Salmonella enteritidis; fungi: Aspergillus niger and Candida albicans). The 1:10 dilution of the essential oil of Equisetum arvense L. was shown to possess a broad spectrum of a very strong antimicrobial activity against all tested strains.

Anti-Infective Agents↗

Composition and antibacterial activity of Abies balsamea essential oil.

The antibacterial activity of the essential oil of Abies balsamea (balsam fir) was evaluated against Escherichia coli and Staphylococcus aureus. The essential oil of A. balsamea was found to be inactive against E. coli (>100 microg/mL) and active against S. aureus, with an MIC of 56 microg/mL. The oil composition was analysed by GC-MS and the antibacterial activity of each oil constituent was determined. The essential oil of A. balsamea is essentially constituted of monoterpenes (>96%) and some sesquiterpenes. beta-pinene (29.9%), delta-3-carene (19.6%) and alpha-pinene (14.6%) were the major components. beta-pinene and delta-3-carene were found inactive against both bacteria strains. However, three constituents of the essential oil were active against S. aureus: alpha-pinene, beta-caryophyllene (0.4%) and alpha-humulene (0.2%) with MIC values of 13.6 microg/mL, 5.1 microg/mL and 2.6 microg/mL, respectively.

Abies↗

Echinacea extracts modulate the production of multiple transcription factors in uninfected cells and rhinovirus-infected cells.

Extracts of Echinacea purpurea are widely used for the prevention and treatment of common colds, coughs, bronchitis and other upper respiratory infections, many of which are caused by rhinoviruses (RVs). Recent reports have indicated that rhinoviruses can stimulate the release of various pro-inflammatory cytokines and chemokines from cultured nasal and bronchial human epithelial cells, and several transcription factors (TFs) have been implicated in this process. The effects of Echinacea treatment and rhinovirus infection on the activation of a range of transcription factors were evaluated by means of a protein/DNA array analysis. The BEAS-2B cell line was used as the model, and nuclear extracts of uninfected cells and rhinovirus-14 infected cells were examined with and without treatment with one of two chemically different Echinacea extracts. It was found that both Echinacea extracts increased the nuclear content of more than 30 transcription factors, including the 12 pro-inflammatory factors examined, such as NFkB, AP-1, AP-2 and STATs 1-6. Virus infection resulted in a more dramatic increase in these same TFs. However, when RV-infected cells were treated with either of the two Echinacea extracts, TF levels were reduced to low levels, although the pattern of the reductions was different for the two extracts. These results indicate that rhinovirus infection of epithelial cells, and treatment with Echinacea extracts, led to profound effects on numerous transcription factors, which could explain the previously observed modulation of secreted cytokines and chemokines, as well as other signaling pathways. In addition, the results could help to explain the beneficial effects of Echinacea consumption.

Cell Line↗

Screening of some medicinal plants from cameroon for beta-lactamase inhibitory activity.

In efforts to find new bioactive beta-lactamase inhibitors, this study investigated 16 Cameroonian plants belonging to 10 families which were evaluated for anti-beta-lactamase activity. The investigation showed that extracts 2, 6, 3 and 5 of the 16 plants investigated presented interesting in vitro beta-lactamase inhibition (over 90%), respectively, of the beta-lactamases TEM-1, OXA-10, IMP-1 and P99. These extracts were from Mammea africana (all beta-lactamases), Garcinia lucida, G. kola (OXA-10, IMP-1 and P99), Bridelia micrantha (OXA-10, P99), Ochna afzelii (OXA-10, P99), Prunus africana (IMP-1) and Adenia lobata (TEM-1). After elimination of tannins (according to the European Pharmacopoeia) the extracts from B. micrantha, G. lucida and M. africana were tested further for their anti-beta-lactamase activity. The extracts from B. micrantha and G. lucida exhibited potent inhibitory activity, respectively, of beta-lactamase OXA-10 (IC(50) = 0.02 mg/mL) and P99 (IC(50) = 0.01 mg/mL). The anti-beta-lactamase activity of M. africana extract was weak. The isolation and the structural elucidation of the active constituents of G. lucida and B. micrantha will provide useful leads in the development of beta-lactamase inhibitors.

Anti-Bacterial Agents↗

Moringa oleifera: a food plant with multiple medicinal uses.

Moringa oleifera Lam (Moringaceae) is a highly valued plant, distributed in many countries of the tropics and subtropics. It has an impressive range of medicinal uses with high nutritional value. Different parts of this plant contain a profile of important minerals, and are a good source of protein, vitamins, beta-carotene, amino acids and various phenolics. The Moringa plant provides a rich and rare combination of zeatin, quercetin, beta-sitosterol, caffeoylquinic acid and kaempferol. In addition to its compelling water purifying powers and high nutritional value, M. oleifera is very important for its medicinal value. Various parts of this plant such as the leaves, roots, seed, bark, fruit, flowers and immature pods act as cardiac and circulatory stimulants, possess antitumor, antipyretic, antiepileptic, antiinflammatory, antiulcer, antispasmodic, diuretic, antihypertensive, cholesterol lowering, antioxidant, antidiabetic, hepatoprotective, antibacterial and antifungal activities, and are being employed for the treatment of different ailments in the indigenous system of medicine, particularly in South Asia. This review focuses on the detailed phytochemical composition, medicinal uses, along with pharmacological properties of different parts of this multipurpose tree.

Flowers↗

Phytol, SSADH inhibitory diterpenoid of Lactuca sativa.

The succinic semialdehyde dehydrogenase (SSADH) inhibitory component was isolated from the EtOAc fraction of Lactuca sativa through repeated column chromatography; then, it was identified as phytol, a diterpenoid, based on the interpretation of several spectral data. Incubation of SSADH with the phytol results in a time-dependent loss of enzymatic activity, suggesting that enzyme modification is irreversible. The inactivation followed pseudo-first-order kinetics with the second-rate order constant of 6.15 x 10(-2) mM(-1) min(-1). Complete protection from inactivation was afforded by the coenzyme NAD+, whereas substrate succinic semialdehyde failed to prevent the inactivation of the enzyme; therefore, it seems likely that phytol covalently binds at or near the active site of the enzyme. It is postulated that the phytol is able to elevate the neurotransmitter GABA levels in central nervous system through its inhibitory action on one of the GABA degradative enzymes, SSADH.

Aldehyde Oxidoreductases↗

Brine shrimp lethality of the compounds from Phryma leptostachya L.

Brine shrimp assay-guided fractionation and isolation of the EtOAc soluble fraction of Phryma leptostachya L. (Phrymacaceae) gave two active compounds, phrymarolin II (1) and ursolic acid (2), which were identified by physicochemical and spectroscopic methods. Compound 1 exhibited potent lethality with LD50 value of 0.0013 microg/ml, whereas 2 showed moderate lethality with LD50 value of 27.0 microg/ml against brine shrimp. The cytotoxic activities of 1 and 2 were also evaluated against one murine and five human cancer cell lines employing the sulforhodamin B (SRB) method. Compound 2 exhibited cytotoxic activity against L1210 and SK-MEL-2 cells with ED50 values of 3.70 and 9.27 mg/ml, respectively, whereas 1 was devoid of any cytotoxic activity against all cancer cells tested.

Animals↗