Anti-plasmodial activity of Ailanthus excelsa

The anti-plasmodial activity of Ailanthus excelsa stem bark was investigated. The methanolic extract inhibited in vitro growth of chloroquine-sensitive (D10) and resistant strains (W2) of Plasmodium falciparum (IC50 4.6 and 2.8 microg/ml, respectively). The effect was retained in the chloroform fraction (3.1 and 2.1 microg/ml, respectively). The anti-plasmodial activity could be ascribed to the impairment of haemoglobin degradation through the inhibition of plasmepsin II activity (IC50 of 13.43+/-1.74 microg/ml) and of the haem detoxification to haemozoin.     

Antidiarrhoeal activity of Cyperus rotundus

The methanol extract of Cyperus rotundus rhizome, given orally at the doses of 250 and 500 mg/kg b.w., showed significant antidiarrhoeal activity in castor oil induced diarrhoea in mice. Among the fractions, tested at 250 mg/kg, the petroleum ether fraction (PEF) and residual methanol fraction (RMF) were found to retain the activity, the latter being more active as compared to the control. The ethyl acetate fraction (EAF) did not show any antidiarrhoeal activity.     

In vivo antidepressant activity of sesquiterpenes from the roots of Valeriana fauriei Briq

Antidepressant activity-guided fractionation of the MeOH extract of Valeriana fauriei Briq. roots resulted in the isolation of two new germacrane-type sesquiterpenes (1-2) in addition to seven known ones (3-9). Their structures were elucidated as 1β,10α-dihydroxyl-8α-acetoxyl-10β,11,11-trimethyl-4-formyl-bicyclogermacren-E-4(5)-ene (1), 1β-hydroxyl-8α-acetoxyl-11,11-dimethyl-4-formyl-bicyclogermacren-E-4(5),10(14)-diene (2), bicyclo[8,1,0]5β-hydroxyl-7β-1acetoxyl-5α,11,11'-trimethyl -E-1(10)-ene-4α,15-olide (3), 8α-acetoxyl-3α,4α,10-trihydroxyl-guaia-1(2)-ene-12,6α-olide (4), 2-Ethylhexyl-4-hydroxybenzoate (5), 11αH-gemacra-1(10)E,4Z-diene-3-one-12,6α-olide (6), β-Sitoterol (7), isovaleric acid (8), isoborneol acetate (9), using a combination of UV, IR, mass spectroscopy, 1D and 2D NMR spectroscopy. The antidepressant activity of compounds 1-4 was investigated by the FST on mice. Among them, compounds 3 and 4 showed the significant antidepressant activity (*, P<0.01).     

Cytotoxic sesquiterpenes and lignans from Saussurea deltoidea

Two new sesquiterpenes deltoiden A (1) and deltoiden B (2), and two new lignans deltoignan A (9) and deltoignan B (10), together with 14 known compounds, including six sesquiterpenes 3-8 and three lignans 11-13, were isolated from the whole plant of Saussurea deltoidea. Compounds 3-8 and 11-17 were isolated for the first time from this plant. Their structures were established by spectroscopic analysis, including 2D-NMR spectroscopic techniques. Cytotoxicities of compounds 1-13 were tested against three cancer cell lines A549, Hela and SMMC-7721. Results showed that 5, 6 and 7 exhibited cytotoxicity against SMMC-7721 with the IC(50) values of 6.49, 9.53, 1.23 μg/ml, 5 and 7 against A549 with the IC(50) values of 4.99 and 5.35 μg/ml, 5, 6, 7, 13 against Hela with the IC(50) values of 1.40, 4.75, 0.93 and 5.42 μg/ml, respectively. The structure-activity relationships of sesquiterpenes 1-8 were discussed on the base of cytotoxic results.     

New prenylflavans from Cyperus conglomeratus

In addition to luteolin and its 7-methyl ether, the CH2Cl2-MeOH (1:1) extract of Cyperus conglomeratus afforded two new prenylflavans identified as 7,3'-dihydroxy-5,5'-dimethoxy-8-prenylflavan and 5,7,3'-trihydroxy-5'-methoxy-8-prenylflavan. The structures were established by CIMS, 1H-NMR, 13C-NMR, H-H COSY, HMQC, HMBC and DEPT analysis.     

Antibacterial activity of plant extracts from Brazilian southeast region

A screening was conducted with 26 plants collected in the Brazilian southeast region, to identify plant extracts with antibacterial properties against Aeromonas hydrophila, Bacillus subtilis, Pseudomonas aeruginosa and Staphylococcus aureus. Initially, the agar diffusion method was employed. Then, those extracts presenting activity were submitted to a broth microdilution assay to determine the minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC). It was observed that 13 of the tested extracts showed antibacterial activity. The best results were obtained with those from Lantana lilacina and Phyllanthus tenellus.     

Antitrypsin activity of extracts from Ecballium elaterium seeds.

The antitrypsin activity of extracts obtained from two different seed types of Ecballium elaterium, was tested in vitro. The presence of trypsin inhibitors in three chromatographed samples for each extract, showed a strong and specific antitrypsin activity.     

Anti-androgenic effect of sesquiterpenes isolated from the rhizomes of Curcuma aeruginosa Roxb

Six sesquiterpenes: germacrone (1), zederone (2), dehydrocurdione (3), curcumenol (4), zedoarondiol (5) and isocurcumenol (6) were isolated from rhizomes of Curcuma aeruginosa Roxb. (Zingiberaceae). They inhibited 5α-reductase which converts testosterone to dihydrotestosterone (DHT). Germacrone (1) was the most potent (IC(50)=0.42±0.05 mg/mL). Compound 1 was anti-androgenic in LNCaP cells when proliferation was testosterone-induced. The growth of flank gland of male Syrian hamsters is dependent on circulating androgen and when maintained with testosterone, 1 (3, 30, 100μg) inhibited growth but was ineffective against DHT. The similar activity profile was observed on the 5α-reductase inhibitor, finasteride (100 μg) treatment group. The androgen receptor binding assay showed that 1 did not bind to the androgen receptor. In conclusion, 1 showed anti-androgenic effect on in vitro and in vivo assays. One of the possible mechanisms was inhibition 5α-reductase activity. Thus, 1 is a potential lead compound for treatment of androgen-dependent disorders.     

Antidiabetic activity of hydro-ethanolic extract of Cyperus rotundus in alloxan induced diabetes in rats

In light of the traditional claim of Cyperus rotundus in the treatment of diabetes, investigations were carried out to evaluate its effect on alloxan induced hyperglycemia in rats. Oral daily administration of 500 mg/kg of the extract (once a day for seven consecutive days) significantly lowered the blood glucose levels. This antihyperglycemic activity can be attributed to its antioxidant activity as it showed the strong DPPH radical scavenging action in vitro.     

Screening of Costus speciosus extracts for antioxidant activity

Different parts of Costus speciosus were investigated for their polyphenol content and antioxidant activity.     

Larvicidal activity of saponin containing extracts and fractions of fruit mesocarp of Balanites aegyptiaca

Chloroform, ethyl acetate, butanol and methanol extracts of fruit mesocarp of Balanites aegyptiaca and five fractions from the methanol extract were tested against the Aedes aegypti mosquito larvae. All extracts showed larvicidal effects however the highest larval mortality was found in methanol extract. One fraction obtained from the silica gel column chromatography of the latter was found most effective for larval mortality. This fraction also interfered with adult emergence. A concentration of 0.0014% (w/v) of this active fraction showed inhibition of the 50% of the test larval population from emerging adults (EC(50)). The analysis of total saponin content of these tested extracts and fractions revealed a strong correlation between saponin content and larval mortality.     

Antiinflammatory activity of Sambucus ebulus hexane extracts

Hexane extracts of aerial parts (flowered browes), leaves and roots of Sambucus ebulus were investigated for their antiinflammatory activity in rats. Aerial parts and roots extracts produced statistically significant and dose dependent inhibition of edema induced by carrageenan at all doses when compared to the control groups. On the contrary, hexane extract of leaves did not show any activity up to 600 mg/kg i.p. The highest activity was showed in the aerial parts and roots that at 600 mg/kg i.p. inhibited inflammation by ca. 80% (78% for diclofenac at 100 mg /kg i.p.). No extracts exhibit toxicity when injected up to 2 g/ kg intraperitoneally in mice.     

Antimicrobial activity of the Maniltoa schefferi extracts

All fractions of Maniltoa schefferi exhibited a broad spectrum of antibacterial activity. Good activity was demonstrated by the petrol and dichloromethane fractions of seed pods, seeds with coat and by methanol fractions of stem heartwood, root bark, root heartwood and stem bark whose butanol fraction was equally good. None of the fractions showed any antifungal activity.     

Three new sesquiterpenes from Tithonia diversifolia and their anti-hyperglycemic activity

Three new germacrane sesquiterpenes (1), (2), (3), along with eleven known sesquiterpenes, namely, tirotundin-3-O-methyl ether (4), deacetylvguiestin (5), 1β-hydroxydiversifolin-3-O-methyl ether (6), tagitinin C (7), 1β-hydroxytirotundin-3-O-methyl ether (8), 1β-hydroxytirotundin-1,3-O-dimethyl ether (9), tagitinin F-3-O-methyl ether (10), tagitinin F (11), tagitinin A (12), 3β-acetoxy-4α-hydroxyeduesm-11(13)-en-12-oic acid (13) and ilicic acid (14) were isolated from the aerial parts of Tithonia diversifolia. Their structures were established by spectroscopic analysis, while the relative configuration of compound 1 was confirmed by X-ray diffraction analysis. In addition, compounds 1–14 were evaluated in vitro for their anti-hyperglycemic activity by glucose uptake in 3T3-L1 adipocytes. It was found that 10 μg/mL 1, 3, 6 and 8 could significantly increase glucose uptake without significant toxic effects.     

Free radical scavenging activity of different extracts and some constituents from the leaves of Ligustrum vulgare and L. delavayanum

The free radical scavenging activity of the water infusions, different organic solvent extracts and some constituents from Ligustrum vulgare and Ligustrum delavayanum leaves was assessed with the aid of DPPH radical. Among the samples screened, water infusions had the strongest free radical scavenging capacity. From the tested compounds scavenging active flavonoid aglycones are present in the most active chloroform fractions from both leaves samples.     

Repellence and toxicity of Schinus molle extracts on Blattella germanica

The biological activities of ethanol and petroleum ether extracts from leaves and fruits of Schinus molle against adults of Blattella germanica were examined by repellence test and topical application. All extracts produced significant repellent effect and mortality.     

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.     

Screening of antioxidant activity of three Euphorbia species from Turkey

Euphorbia acanthothamnos, E. macroclada and E. rigida were investigated for their antioxidant activity. The antioxidant potential of extracts of E. acanthothamnos, E. macroclada and E. rigida was evaluated using different complementary antioxidant tests.     

Antibacterial and allelopathic activity of methanolic extract from Iris pseudopumila rhizomes

The methanolic extract of rhizomes of Iris pseudopumila was tested for its antibacterial and allelopathic activity. The extract was shown to have antibacterial effects. The allelopathic effect was tested against Raphanus sativus seed germination. The extract caused a decrease in the percentage of seed germination and root and epicotyl growth.     

Diarylheptanoids from the rhizomes of Alpinia officinarum and their anticancer activity

Two new diarylheptanoids (1, 2), together with two known analogs (3, 4), were isolated from the rhizomes of Alpinia officinarum. The new compounds were elucidated to be (5S)-5-hydroxy-7-(3, 4-dihydroxyphenyl)-1-phenyl-3-heptanone (1) and (5R)-5-hydroxy-7-(3-methoxy-4, 5-dihydroxyphenyl)-1-phenyl-3-heptanone (2) based on their spectral analysis. Compound 4 showed moderate cytotoxicity against human tumor cell lines, HepG2, MCF-7 and SF-268, while no significant effect were found for compounds 1-3.