Bioactivity guided isolation of antipsychotic constituents from the leaves of Rauwolfia tetraphylla L

This study was undertaken to ascertain the antipsychotic properties of Rauwolfia tetraphylla L. leaves and to isolate and characterize the antipsychotic constituents. Among the MeOH extract and some alkaloidal fractions at different pHs, the alkaloidal CHCl(3) fraction at pH-9 (2C) showed the highest antipsychotic activity against dopaminergic (DA-D(2)) and serotonergic (5-HT(2A)) receptors in-vitro and amphetamine induced hyperactive mouse model in-vivo. The activity guided isolation of CHCl(3) fraction (2C) afforded six indole alkaloids: 10-methoxytetrahydroalstonine (1), isoreserpiline (2), an isomeric mixture of 11-demethoxyreserpiline (3) and 10-demethoxyreserpiline (4), α-yohimbine (5) and reserpiline (6). Given orally, alkaloids 3-6 showed significant antipsychotic activity in a dose dependent manner. None of the extract, alkaloidal fractions or alkaloids showed any extra pyramidal symptoms at the tested doses. It was also observed that MeOH extract was behaving similar to other clinically used novel atypical antipsychotics in having 5-HT(2A) occupancy greater than the DA-D(2) receptor at the tested doses. Further toxicity and safety evaluation studies of MeOH extracts of R. tetraphylla leaves at different doses (10, 100, 300 and 2000 mg/kg) on female Swiss albino mice showed that MeOH extract is non toxic. The isolated alkaloids, 3-6 could serve as a promising lead structure for drug development of treating psychotic conditions in human.     

The antiplasmodial activity of spermine alkaloids isolated from Albizia gummifera

In the present study the methanolic extract of Albizia gummifera was fractionated into various fractions. These fractions were tested against choroquine sensitive (NF54) and resistant (ENT30) strains of Plasmodium falciparum. All other fractions apart from the alkaloidal fraction showed low activity with IC 50 above 3 microg/ml. The alkaloidal fraction exhibited strong activity against NF54 and ENT30 with IC 50 of 0.16+/-0.05 and 0.99+/-0.06 microg/ml, respectively. Five known spermine alkaloids were isolated from the alkaloidal fraction. These alkaloids exhibited activities against NF54 and ENT30 with IC 50 ranging from 0.09+/-0.02 to 0.91+/-0.10 microg/ml. Four of the alkaloids were further evaluated for in vivo activity against rodent malaria parasite Plasmodium berghei. The alkaloids showed percentage chemosuppression of parasitaemia in mice ranging from 43 to 72%. The use of the extracts A. gummifera for treatment of malaria in traditional medicine seems to have a scientific basis.     

Antimicrobial activity of Leucas aspera flowers

The methanol extract of Leucas aspera flowers, its fractions, the alkaloidal residue and the expressed flower juice, tested for antimicrobial activity, showed good antibacterial activity for methanol extract and methanol fraction with maximum activity for the alkaloidal residue.     

In vitro antifungal activities of longan (Dimocarpus longan Lour.) seed extract

Longan, Dimocarpus longan Lour., contains polyphenolic compounds which exhibit several pharmacological properties. This study aims to evaluate antifungal activities of longan fruit extract in comparison to its active compounds. The results showed that longan seed exhibited antifungal activity against the opportunistic yeasts (Candida species and Cryptococcus neoformans). In contrast, longan pulp and whole fruit did not demonstrate any inhibitory effects. Ellagic acid showed the most potent antifungal activity followed by corilagin and gallic acid, respectively. Ellagic acid inhibited Candida parapsilosis and C. neoformans more effectively than Candida krusei and also some Candida albicans clinical strains. Baidam cultivar possessed higher antifungal activity (MIC=500-4000 μg/ml) as it contained higher contents of ellagic acid and gallic acid than Edor (MIC=1000-8000 μg/ml). For antibacterial activity, only corilagin and gallic acid possessed weak to moderate inhibitory effects against Staphylococcus aureus and Streptococcus mutans, respectively. Longan seed was then applied in the oral care products. Longan effervescent granule (5% extract) significantly reduced adhesion of C. albicans to acrylic strips. Mouthwash containing 0.5% extract exhibited good antifungal activity compared to a commercial product. These findings indicated that longan seed extract and its polyphenolic compounds can be used as an antifungal agent in oral care products for the treatment of opportunistic yeast infection.     

Tannins from barks of Pinus caribaea protect Escherichia coli cells against DNA damage induced by gamma-rays

This work was aimed to evaluate genotoxicity and antigenotoxicity activity against gamma-rays of a tannin fraction obtained from barks of Pinus caribaea, as well as to elucidate the antigenotoxic mechanisms involved in radioprotection by using different approaches as pre-, co- and post-irradiation cell treatments with plant extract. The tannin fraction was not genotoxic to Escherichia coli cells in experiments using different exposure times. This extract was antigenotoxic against gamma-rays when the cells were pre- or co-treated with this extracts, but not during post-irradiation treatments, suggesting a possibly antigenotoxic action through free radical scavenging mechanisms. The results are discussed in relation to the chemopreventive and therapeutic potential of the studied plant species.     

Antiulcer activity of Mikania cordata

The alkaloidal fraction obtained from an ethanolic extract of the leaves of Mikania cordata exhibited significant in vivo antiulcer activity in diclofenac sodium-induced gastric erosions in Long Evans rats.     

Antimicrobial activity of Diospyros anisandra

Leaves, root and stem bark of Diospyros anisandra were screened against two strains of Mycobacterium tuberculosis, one resistant and one susceptible to antibiotics, using the microplate Alamar blue assay test. The lypophylic fractions of the root and bark showed significant inhibitory activity against both strains, with the hexane fraction of the bark showing the strongest activity (MIC 6.25 microg/ml) against the resistant strain and a significant antimicrobial activity against Staphylococcus aureus, Bacillus subtilis, Candida albicans, Aspergillus niger, and Colletotrichum gloeosporioides. The bioassay-guided purification of the bioactive hexane fraction resulted in the isolation and identification of the naphthoquinone plumbagin as one of the metabolites responsible for the biological activity.     

Molluscicidal activity of Aglaia duperreana and the constituents of its twigs and leaves

The methanol (MeOH) extract of the twigs and leaves of Aglaia duperreana was investigated for its molluscicidal activity against Pomacea canaliculata. The extract was found to exhibit significant molluscicidal activity. The ethyl acetate soluble fraction of the extract showed the most potent molluscicidal activity among different solvent fractions. The bioactivity-guided chemical investigation of the ethyl acetate soluble fraction led to a new triterpenoid along with 15 known compounds. Their structures were elucidated by spectroscopic methods, including one- and two-dimensional nuclear magnetic resonance techniques as well as mass spectroscopic analysis. The molluscicidal activities of compounds 2-16 against P. canaliculata were also investigated. Naringenin trimethyl ether showed significant molluscicidal activity with a median lethal concentration (LC(50)) of 3.9 μg/mL, which was indicated higher potency than the positive control, tea saponin (LC(50)=4.5 μg/mL).     

Evaluation of antioxidant effect of extracts of Symphyopappus casarettoi

The ethanolic extract of Symphyopappus casarettoi syn. Eupatorium casarettoi was partionated in hexanic, chloroformic and methanolic fractions. Extract and fractions were tested for their antioxidant activity in vitro and ex vivo assays. The methanolic fraction showed a higher antioxidant potential compared to the others fractions, which was correlated with its total phenol content. In addition, the ethanolic extract and the methanolic fraction attenuated ex vivo iron-induced cell death, quantified by lactate dehydrogenase leakage, and effectively protected against lipid damage induced by iron. These findings suggest that the ethanolic extract of S. casarettoi inflorescence and its methanolic fraction have in vitro and ex vivo antioxidant properties.     

Antibacterial effect of Dryopteris crassirhizoma against methicillin-resistant Staphylococcus aureus

Methanol extract and its fractions (hexane, EtOAc, n-BuOH, and H2O) of Dryopteris crassirhizoma were investigated for antibacterial activity against methicillin-resistant Staphylococcus aureus. The hexane fraction showed a good antibacterial activity against all tested strains.     

In vitro antifungal activities of Allium cepa, Allium sativum and ketoconazole against some pathogenic yeasts and dermatophytes

By using an agar dilution assay, the antifungal activity of aqueous extracts prepared from Allium cepa (onion; AOE) and Allium sativum (garlic; AGE) were evaluated against Malassezia furfur (25 strains), Candida albicans (18 strains), other Candida sp. (12 strains) as well as 35 strains of various dermatophyte species and compared with the activity of a known antifungal drug, ketoconazole (KTZ). All the AOE, AGE and KTZ were found to be able to inhibit growth of all fungi tested in a dose-dependent manner with maximum of 100% at defined concentrations. The results indicate that onion and garlic might be promising in treatment of fungal-associated diseases from important pathogenic genera Candida, Malassezia and the dermatophytes.     

Inhibition of clotrimazole-resistant Candida albicans by some endemic Sideritis species from Turkey

The anticandidal activity of the methanol extracts of seven endemic Sideritis species were evaluated at 30 mg/ml concentration against clotrimazole-resistant Candida albicans.     

Antimicrobial activity of Bryum argenteum

The antimicrobial activity of Bryum argenteum ethanol extracts was evaluated by microdilution method against four bacterial (Escherichia coli, Bacillus subtilis, Micrococcus luteus and Staphilococcus aureus) and four fungal species (Aspergillus niger, Penicillium ochrochloron, Candida albicans and Trichophyton mentagrophyes). All the investigated ethanol extracts have been proved to be active against all bacteria and fungi tested.     

Antibacterial activities of some mosses including Hylocomium splendens from South Western British Columbia

The antibacterial activity of methanol extracts of ten moss species and fractions prepared from 80% methanol extract of Hylocomium splendens were evaluated by disk diffusion method. Nine moss species showed antibacterial activity against Gram (+) bacteria, in particular H. splendens and its ethyl acetate fractions showed stronger activity. Enhancement of antibacterial activity against Staphylococci by UV-A light irradiation was demonstrated in the extracts of Bartramia pomiformis, Ceratodon purpureus and Neckera douglasii.     

Molluscicidal activity against Bulinus truncatus of Croton campestris

The bark of Croton campestris provided three furano-clerodane named, respectively, velamone, velamolone acetate and velamolone. Fractions containing these diterpenoids were investigated for their molluscicidal activity against Bulinus truncatus, one of the aquatic snail vectors of schistosomiasis. A dichloromethanic extract of root barks, rich in furano-clerodane and molluscicidal at 20ppm was promising as natural molluscicide. Enriched fraction with velamone gave 80% mortality from 25ppm, while its LD(100) was at 50ppm. The LD(80) was ca. at 45ppm, while LD(100) was at 60ppm for the enriched fraction containing velamolone acetate. The velamolone-enriched fraction was less efficient and gave a mortality of 90% at 90ppm. The pure compounds, velamone and velamolone acetate were active at 100% at 3 and 6ppm, respectively. Velamolone showed a molluscicidal activity at 20ppm.     

Inhibitory effect of a bioactivity-guided fraction from Rheum undulatum on the acid production of Streptococcus mutans biofilms at sub-MIC levels

Rheum undulatum root has been used traditionally in Korea for the treatment of dental diseases. The purpose of this study was to separate a fraction from R. undulatum showing anti-acid production activity against Streptococcus mutans biofilms and identify the main components in that fraction. Methanol extract of R. undulatum root and its fractions were prepared. To select a fraction exhibiting anti-acid production activity, suspension glycolytic pH-drop assay was performed. Among the fractions tested, dichloromethane fraction exhibited the strongest activity in a dose-dependent manner. To examine the effect of the selected fraction on the anti-acid production of S. mutans biofilms, 74 h old S. mutans biofilms were used. The selected fraction reduced the initial rate of acid production of S. mutans biofilms at sub-minimum inhibitory concentration (MIC) levels. HPLC qualitative analysis of the selected fraction indicated that the presence of anthraquinone derivatives, such as aloe-emodin, emodin, chrysophanol and physcion, as main components.     

Antifungal activity of Agapanthus africanus extractives

The ethanolic extract of the rhizomes of Agapanthus africanus showed antifungal activity. In bioassay guided fractionation, n-butanol fraction exhibited significant activity against human pathogens. A saponin, (25R)-spirost-7-en-2alpha,3beta,5alpha-triol-3-O-[alpha-L-rhamnopyranosyl(1-->2)-[beta-D-galactopyranosyl (1-->3)] beta-D-glucopyranoside (1), responsible for the antifungal activity and having MIC value of 15.6 microg/ml against Trychophyton mentagrophytes and Sporothrix schenekii, was isolated and identified as active constituent of the plant.     

Antifungal activity of fruit pulp extract from Psidium sartorianum

The methanol extract of the fruit pulp of Psidium sartorianum was evaluated against seven Candida spp. and nine other fungal strains that are human pathogens. The extract showed a significant activity against seven Trichophyton species. Candida species were insensitive.     

Antimicrobial activity of coupled hydroxyanthracenones isolated from plants of the genus Karwinskia

The in vitro activity of some isolated hydroxyanthracenones belonging to the genus Karwinskia against four bacteria, six filamentous fungi and four yeast are reported. These hydroxyanthracenones were found to possess antimicrobial activity, particularly against Streptococcus pyogenes, Candida albicans, C. boidinii, C. glabrata and Cryptococcus neoformans; minimal inhibitory concentrations range between 16 and 2 microg/ml.     

Antimicrobial activity of crude methanolic extract of Satureja khuzistanica

The methanolic extract of the aerial parts of Satureja khuzistanica was investigated for its antimicrobial activity. The maximum antibacterial and antifungal activities were observed against Staphylococcus aureus and Candida albicans.