Antifungal activity of essential oils isolated from Egyptian plants against wood decay fungi

The essential oils of eighteen Egyptian plants were extracted by hydrodistillation and their chemical compositions were analyzed by GC-MS. The antifungal activity of the isolated oils was evaluated against two wood decay fungi Hexagonia apiaria and Ganoderma lucidum in vitro. The essential oil of Artemisia monosperma showed the highest inhibitory effect against H. apiaria (EC₅₀ = 31 mg L^?1) and G. lucidum (EC₅₀ = 53 mg L^?1). The results of in vitro tests indicated that the essential oils of Cupressus sempervirens, Citrus limon, Thuja occidentalis, Schinus molle, A. monosperma and Pelargonium graveolens were the most potent inhibitors against both fungi. These six oils caused significant reduction of wood mass loss of Scots pine sapwood after 6 weeks of fungal exposure. The oil of C. limon revealed the highest reduction of wood mass loss caused by H. apiaria, while A. monosperma oil displayed the highest reduction of wood loss caused by G. lucidum. These results support the potential use of essential oils for wood protection against decay fungi.     

Securidacaxanthone A, a heptaoxygenated xanthone from Securidaca longepedunculata

From the root bark of Securidaca longepedunculata, a heptaoxygenated xanthone (1) has been isolated as well as two known xanthones (2) and (3) and two salicylic acid derivatives (4) and (5). The structure of 1 has been elucidated from 1H and 13C-NMR spectral data.     

Antifungal compounds from turmeric and nutmeg with activity against plant pathogens

The antifungal activity of twenty-two common spices was evaluated against plant pathogens using direct-bioautography coupled Colletotrichum bioassays. Turmeric, nutmeg, ginger, clove, oregano, cinnamon, anise, fennel, basil, black cumin, and black pepper showed antifungal activity against the plant pathogens Colletotrichum acutatum, Colletotrichum fragariae, and Colletotrichum gloeosporioides. Among the active extracts, turmeric and nutmeg were the most active and were chosen for further investigation. The bioassay-guided fractionation led to the isolation of three compounds from turmeric (1–3) and three compounds from nutmeg (4–6). Their chemical structures were elucidated by spectroscopic analysis including HR-MS, 1D, and 2D NMR as curcumin (1), demethoxycurcumin (2) and bisdemethoxy-curcumin (3), erythro-(7R,8R)-Δ^8′-4,7-dihydroxy-3,3′,5′-trimethoxy-8-O-4′-neolignan (4), erythro-(7R,8R)-Δ8′-7-acetoxy-3,4,3′,5′-tetra-methoxy-8-O-4′-neolignan (5), and 5-hydroxy-eugenol (6). The isolated compounds were subsequently evaluated using a 96-well microbioassay against plant pathogens. At 30 μM, compounds 2 and 3 possessed the most antifungal activity against Phomopsis obscurans and Phomopsis viticola, respectively.     

Antidiarrheal activity of dehydroleucodine isolated from Artemisia douglasiana

Dehydroleucodine (DhL), a sesquiterpene lactone obtained from Artemisia douglasiana, was screened for antidiarrheal effects. DhL inhibited castor oil-induced diarrhea in mice by judged by a decrease in the number of wet faeces in the DhL-treatment groups. DhL significantly reduced intestinal transit in mice. Yohimbine and phentolamine counteracted the inhibitory effect of DhL. It is suggested that alpha(2)-adrenergic receptors mediate the effect of DhL in intestinal motility. DhL reduced also intraluminal accumulation of fluid. Thus, the antidiarrheal activity of DhL is possibly related, at least in part, to its inhibitory action against gastrointestinal motility and the inhibition of enteropooling property.     

Flavonoids with prolyl oligopeptidase inhibitory activity isolated from Scutellaria racemosa Pers

Prolyl oligopeptidase (POP) is a serine protease highly expressed in the brain that hydrolyses peptide bonds at the carboxyl terminal of prolyl residues. There is evidence that this enzyme participates in several functions of the central nervous system. Scutellaria racemosa Pers demonstrated significant and selective POP inhibition. Fractionation of the hydroalcoholic extract resulted in the isolation of four main constituents identified for the first time from S. racemosa Pers, the triterpenoid lupeol (1) and the flavonoids oroxylin A (5,7-dihydroxy-6-methoxyflavone, 2), hispidulin (4′,5,7-trihydroxy-6-methoxyflavone, 3), and oroxyloside (oroxylin A 7-O-glucuronide, 4). Inhibitory assays indicated that 3 and 4 at a concentration of 100 μM inhibit 43 and 34% of total POP activity, respectively.     

Anti-acne activity of tannin-related compounds isolated from Terminalia laxiflora

In our investigation to find out new anti-acne agent, we focused on Terminalia laxiflora Engl & Diels (Combretaceae) methanolic wood extract, which has been selected during previous screening experiments for anti-acne agents, which included 29 species of Sudanese medicinal plants. Based on the biologically guided fractionation using an antibacterial assay against Propionibacterium acnes, a lipase inhibitory assay and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity assay; five tannin-related compounds were isolated, such as ellagic acid, flavogallonic acid dilactone, terchebulin and gallic acid. Terchebulin showed good antibacterial activity; minimum inhibitory concentration (MIC) = 125 μg/ml and minimum bactericidal concentration (MBC) = 250 μg/ml. Gallic acid exhibited lipase inhibitory activity with IC₅₀ value of 149.3 μM, which showed strong inhibition compared with terchebulin, IC₅₀ 260.7 μM. However, all compounds exhibited better or equal DPPH radical scavenging activity to (+)-catechin as positive control. Ellagic acid and terchebulin showed the best DPPH radical scavenging activities, IC₅₀ 4.86 and 4.90 μM, respectively. This study demonstrated that terchebulin has potentiality as an anti-acne agent.     

Immunomodulatory activity of cucurbitacin E isolated from Ecballium elaterium

The immunomodulatory effect of cucurbitacin E, extracted from Ecballium elaterium, was tested on peripheral human lymphocytes. These lymphocytes were co-cultured with cancer cells and an interesting lymphocyte-mediated cytotoxicity was observed.     

Antitumor activity of three benzopyrans isolated from Hypericum polyanthemum

In the present study we have investigated the in vitro antitumor effects of three benzopyrans, 6-isobutyryl-5,7-dimethoxy-2,2-dimethylbenzopyran (1), 7-hydroxy-6-isobutyryl-5-methoxy-2,2-dimethylbenzopyran (2) and 5-hydroxy-6-isobutyryl-7-methoxy-2,2-dimethylbenzopyran (3) isolated from Hypericum polyanthemum. The three compounds tested demonstrated potent growth inhibitory activity at 40 microg/ml (<25% control growth) in the NCI-H460, HT-29 and U-373MG human cell lines. Determination of cell cycle distribution demonstrated that the antiproliferative effect of the three benzopyrans could be associated to alterations in the cell cycle phase distribution. Treatment with the IC50 of the three compounds induced an arrested in S phase. Only in cells treated with compound 3 did the percentage of sub-G1 population increase up to 9%, suggesting that this compound induced more cell death than the others. Consistent with sub-G1 analysis, appreciable oligonucleosomal DNA fragmentation was only observed in the NCI-H460 cell line treated with compound 3. From these results it can be suggested that despite no differences among the cytotoxicity of the three compounds, it was observed that the mechanism of their antiproliferative effects appears to be different.     

Cytotoxic activity of five compounds isolated from Colombian plants

Cytotoxic effect of five known compounds, khellin, berberine, lupeol, scopolin, rapanone, obtained from Colombian plants, were determined against human tumor cell lines as an indicator of the potential anticancer activity of these compounds. Berberine and rapanone presented interesting cytotoxicity.     

Antifungal activity of sterols and triterpenes isolated from Ganoderma annulare

Three sterols, 5alpha-ergost-7-en-3beta-ol, 5alpha-ergosta-7,22-dien-3beta-ol and 5,8-epidioxy-5alpha,8alpha-ergosta-6,22-dien-3beta-ol and five triterpenes, applanoxidic acids A, C, F, G and H, have been isolated from Ganoderma annulare. The applanoxidic acids A, C and F were found to inhibit the growth of the fungi Microsporum cannis and Trichophyton mentagrophytes at concentrations of 500 to 1000 microg/ml.     

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.     

Xanthone derivatives from the fermentation products of an endophytic fungus Phomopsis sp.

Three new xanthones, 1,5-dihydroxy-3-hydroxyethyl-6-methoxycarbonylxanthone (1), 1-hydroxy-5- methoxy-3-hydroxyethyl-6-methoxycarbonylxanthone (2), and 1-hydroxy-3-hydroxyethyl- 8-ethoxycarbonylxanthone (3), along with seven known xanthones (4–10) were isolated from the fermentation products of an endophytic fungus Phomopsis sp.. Their structures were elucidated by spectroscopic methods including extensive 1D- and 2D-NMR techniques. Compounds 1–10 were also tested for their cytotoxicity against five human tumor cell lines (NB4, A549, SHSY5Y, PC3, and MCF7) by MTT method using paclitaxel as positive control. Compounds 1 and 3 showed cytotoxicity against A549 cell lines with IC50 values of 3.6 and 2.5 μM, respectively. In addition, 1 was cytotoxic to MCF7 cells with IC50 value of 2.7 μM.     

Biflavanones with anti-proliferative activity against eight human solid tumor cell lines from Stellera chamaejasme

Six 3,3″-biflavanones, including a new compound isochamaejasmenin C (1), were isolated from EtOH extracts of the roots of Stellera chamaejasme L. Their structures were elucidated on the basis of spectroscopic methods, including HR-ESI-MS and 2D NMR techniques. The absolute configurations on 2, 3, 3″, and 2″ of compounds 1, 3, and 6, which represent three geometry types of these compounds, were determined by TDDFT quantum chemical calculations of their ECD spectra. All compounds were evaluated for their cytotoxicities against eight human solid tumor cell lines and compounds 2, 4, and 6 showed strong anti-proliferative effects against all these cell lines with IC₅₀ values ranging from 1.08 to 15.97 μM, which were in the same range as the positive control paclitaxel.     

Antibacterial activity of xanthorrhizol from Curcuma xanthorrhiza against oral pathogens

The antibacterial activity of xanthorrhizol, isolated from the methanol extract of Curcuma xanthorrhiza roots, was evaluated against oral microorganisms in comparison with chlorhexidine.     

Inhibitory activity of homoisoflavonoids from Caesalpinia sappan against Beauveria bassiana

Four homoisoflavonoids, 4-O-methylsappanol (1), protosappanin A (2), brazilin (3) and caeasalpin J (4), isolated from Caesalpinia sappan, were tested for inhibitory activity against Beauveria bassiana. Compound 1 showed activity against this fungus.     

Antimicrobial activity of aqueous extracts and of berberine isolated from Berberis heterophylla

The antimicrobial activity of Berberis heterophylla leaves, stems and root aqueous extracts was studied in vitro on Gram-positive and Gram-negative bacteria and fungi. The in vitro antifungal activity of berberine isolated from the same source against different Candida species was also investigated.     

Anti-inflammatory activity of patchouli alcohol isolated from Pogostemonis Herba in animal models

Pogostemonis Herba has long been used in traditional Chinese medicine for the treatment of inflammatory disorders. Patchouli alcohol (PA), a tricyclic sesquiterpene isolated from Pogostemonis Herba, is known to possess a variety of pharmacological activities. The present study aimed to investigate the in vivo anti-inflammatory effect of PA using two common inflammatory animal models i.e., xylene-induced ear edema in mice and carrageenan-induced paw edema in rats. The degree of edema in both inflammatory animals, as well as the protein and mRNA expression of some inflammatory mediators including tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), prostaglandin E₂ (PGE₂) and nitric oxide (NO) in the hind paw of carrageenan-treated rats were measured. Results showed that PA (10–40 mg/kg) significantly inhibited the ear edema induced by xylene in mice and the paw edema induced by carrageenan in rats. In addition, treatment with PA (10–40 mg/kg) also dose-dependently decreased the production of TNF-α, IL-1β, PGE₂ and NO in the hind paw of carrageenan-treated rats. Furthermore, PA treatment also suppressed the mRNA expression of TNF-α, IL-1β, inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in the hind paw of carrageenan-treated rats. These results suggest that PA possesses potent anti-inflammatory activity, which may be mediated, at least in part, by down-regulating the mRNA expression of a panel of inflammatory mediators including TNF-α, IL-1β, iNOS and COX-2.     

(+)-Totarol from Chamaecyparis nootkatensis and activity against Mycobacterium tuberculosis.

The isolation of (+)-totarol as active compound against Mycobacterium tuberculosis is reported from Chamaecyparis nootkatensis outerbark.     

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.