Antiinflammatory and ulcerogenic activities of Salvia triloba extracts

In continuation of our research on Salvia triloba, acute and chronic antiinflammatory and ulcerogenic activities of chloroform, ethanol, butanol and water extracts were detected at 25 mg/kg p.o. The chloroform extract showed the highest antiinflammatory activity in both acute and chronic models, while the ulcerogenic effects of all tested extracts were found to be less than that of acetyl salicylic acid.     

Sesquiterpene lactones from Centaurea musimomum. Antiplasmodial and cytotoxic activities

The chloroform extract of the aerial parts of Centaurea musimomum exhibited significant activity against Plasmodium falciparum. The phytochemical study of this extract gave seven native and four acetylated sesquiterpene lactones.     

Flavonoids from Acalypha indica

Four known kaempferol glycosides, mauritianin, clitorin, nicotiflorin and biorobin, have been isolated from the flowers and leaves of Acalypha indica. Some formerly published NMR data were corrected.     

Antimicrobial and cytotoxic activities of Achyranthes ferruginea

Chloroform extract (CE) of Achyranthes ferruginea and N-trans-feruloyl-4-methyldopamine (1) showed remarkable antimicrobial activities against a wide range of bacteria and fungi. Both crude extract (CE) and compound 1 showed significant cytotoxicity of LC(50) at 16.21 microg/ml and 11.70 microg/ml, respectively.     

Flavonoids with DNA strand-scission activity from Rhus javanica var. roxburghiana

The flavonoids isolated from the stems of Rhus javanica var. roxburghiana, taxifolin (1), fisetin (2), fustin (3), 3,7,4'-trihydroxyflavanone (4) and 3,7,4'-trihydroxyflavone (5) caused breakage of supercoiled plasmid pBR322 DNA in the presence of Cu(II). Cu(I) was shown to be an essential intermediate by using the Cu(I)-specific sequestering reagent neocuproine. The Cu(II)-mediated DNA scissions induced by 1, 2, 3 and 5 were inhibited by the addition of catalase and exhibited DNA strand break by the addition of KI and superoxide dimutase (SOD), while in the Cu(II)-mediated DNA scissions induced by 4 was inhibited by the addition of KI, SOD, and catalase. It is concluded that 1, 2, 3, and 5 can induce H(2)O(2) and superoxide anion, while 4 can induce OH() and H(2)O(2) and subsequent oxidative damage of DNA in the presence of Cu(II).     

New bibenzyl glycosides from leaves of Camellia oleifera Abel. with cytotoxic activities

Studies on the chemical constituents of leaves of Camellia oleifera Abel. led to the isolation of 3 new bibenzyl glycosides. Their structures have been elucidated as 1-(3′,5′-dihydroxy)phenyl-2-(4″-O-β-D-glucopyranosyl)phenylethane (1), 1-(3′,5′-dimethoxy)phenyl-2-(4″-O-β-D-glucopyranosyl)phenylethane (2) and 1-(3′,5′-dimethoxy)phenyl-2-[4″-O-β-D-glucopyranosyl(6→1)-O-α-L-rhamnopyranosyl]phenylethane (3) through spectral studies including HR-ESI-MS, ¹H NMR, ¹³C NMR and 2D NMR experiments. All the above 3 bibenzyl glycosides showed cytotoxic activities to Hela and hep2 cell lines.     

Novel indole C-glycosides from Isatis indigotica and their potential cytotoxic activity

Two novel indole C-glycosides, which were the first reported alkaloids C-glycosides from Isatis indigotica, together with five known alkaloids were isolated. The novel alkaloids were elucidated to be indole-3-acetonitrile-4-methoxy-2-C-β-D-glucopyranoside (1) and N-methoxy-indole-3-acetonitrile-2-C-β-D-glucopyranoside (2) on the basis of spectroscopic analysis. 1 exhibited significant cytotoxic activities against human myeloid leukemia HL-60 and human liver cancer HepG2 cells with the IC₅₀ of 1.3 ± 0.1 and 2.1 ± 0.3 μM, respectively. 2 showed potential cytotoxic activities against HL-60 and human myeloid leukemia Mata cells with the IC₅₀ of 5.1 ± 0.4 and 12.1 ± 0.8 μM, respectively.     

Preliminary antinociceptive, antioxidant and cytotoxic activities of Leucas aspera root

The ethanolic extract of Leucas aspera root was subjected to acetic acid induced writhing inhibition, 1,1-diphenyl-2-picryl hydrazyl (DPPH) free radical scavenging assay and brine shrimp lethality bioassay for screening of antinociceptive, antioxidant and cytotoxic activity, respectively. The extract produced significant writhing inhibition in acetic acid induced writhing in mice at the doses of 250 and 500 mg/kg. The extract showed a significant free radical scavenging activity with an IC(50) of 8 microg/ml. The extract showed significant lethality to brine shrimp with an LC(50) value.     

New neo-clerodane diterpenoids from Scutellaria barbata with cytotoxic activities

Two new neo-clerodane diterpenoids have been isolated from the whole plant of Scutellaria barbata D. Don, and their structures were established by detailed spectral analyses as scutehenanine H (1) and 6-(2,3-epoxy-2-isopropyl-n-propoxyl)barbatin C (2). In vitro, the isolated two new compounds showed significant cytotoxic activities against three human cancer lines, and gave IC₅₀ values in the range OF 2.0-4.2 μΜ.     

New cytotoxic quinolone alkaloids from fruits of Evodia rutaecarpa

Three new quinolone alkaloids, 1-methyl-2-[7-hydroxy-(E)-9-tridecenyl]-4(1H)-quinolone (1), 1-methyl-2-[(Z)-4-nonenyl]-4(1H)-quinolone (2), 1-methyl-2-[(1E,5Z)-1,5-undecadienyl]-4(1H)-quinolone (3) and one new natural product, 1-methyl-2-[(E)-1-undecenyl]-4(1H)-quinolone (4), were isolated from the dried and nearly ripe fruits of Evodia rutaecarpa (Juss.) Benth., along with thirteen known compounds (5-17). In addition, one new artificial product, 1-methyl-2-[7-carbonyl-(E)-9-tridecenyl]-4(1H)-quinolone (1A) was also obtained. The structures of these compounds were determined by spectroscopic analyses. The cytotoxic activities of all of the compounds against the human cancer cell lines HL-60, N-87, H-460, and Hep G(2) cells were evaluated by MTT assay. The results showed that these alkaloids inhibited cell proliferation with IC(50) values between 14μM and 22μM.     

In vitro antileishmanial, antiplasmodial and cytotoxic activities of phenolics and triterpenoids from Baccharis dracunculifolia D. C. (Asteraceae)

Baccharis dracunculifolia (Asteraceae), the most important plant source of the Brazilian green propolis (GPE), displayed in vitro activity against Leishmania donovani, with an IC₅₀ value of 45 µg/mL, while GPE presented an IC₅₀ value of 49 µg/mL. Among the isolated compounds of B. dracunculifolia, ursolic acid, and hautriwaic acid lactone showed IC₅₀ values of 3.7 µg/mL and 7.0 µg/mL, respectively. Uvaol, acacetin, and ermanin displayed moderate antileishmanial activity. Regarding the antiplasmodial assay against Plasmodium falciparum, BdE and GPE gave similar IC₅₀ values (about 20 µg/mL), while Hautriwaic acid lactone led to an IC₅₀ value of 0.8 µg/mL (D6 clone).     

Antiplasmodial activity and cytotoxicity of Albertisia delagoensis

Leaves and rhizome methanol extracts of Albertisia delagoensis tested positive against Plasmodium falciparum, with a very low cytotoxic activity in leaves against the Graham cell line.     

A new dilactone from the seeds of Gaultheria yunnanensis

Gaultheriadiolide (1), a new compound, together with the known dauosterol (2), ginkgetin (3), myricetin (4), 6-ethyl-5-hydroxy-2,7-dimethoxy-1,4-naphthoquinone (5), ursolic acid (6), methyl salicylate 2-O-β-d-xylosyl(1→6)β-d-glucopyranoside (7), and methyl salicylate 2-O-β-d-glucopyranoside (8) were isolated from Gaultheria yunnanensis. The structure was elucidated on the basic of spectral analysis, especially 1D and 2D NMR. Primary bioassays showed that compound 1 had medium cytotoxic activity against HEp-2 and HepG2 Cells, with IC₅₀ of 23.337 μM and 29.4497 μM, respectively.     

Anthelmintic activities of three medicinal plants from Nigeria

Aqueous extracts of the leaf, stem bark and root bark from Canna bidentata, Spondias mombin and Commiphora africana were examined for anthelmintic activity against earthworm. All the extracts demonstrated a concentration-dependent activity at tested concentrations of 10-80 mg/ml. Higher activities were observed at the higher concentrations, 40-80 mg/ml for all the plant extracts. C. bidentata with a paralysis time of 3-5 min and death time of 5-18 min at these concentrations for the stem bark, and S. mombin which exhibited comparatively higher efficacy (34-44 min paralysis time and 105 min death time for the leaf) at lower concentrations of 10-20 mg/ml were adjudged the outstanding anthelmintics of plant origin accordingly.     

New cardenolides from the stem bark of Trewia nudiflora

Phytochemical investigation of the stem bark of Trewia nudiflora led to the isolation of two new cardenolides, trewianin (1) and trewioside (2), along with scopoletin (3) and indole-3-carboxylic acid (4). Structures were established by 1D- and 2D NMR spectroscopy, HR-MS analysis, and by comparison with literature data.     

Antinociceptive and antiplasmodial activities of cassane furanoditerpenes from Caesalpinia volkensii H. root bark

The chloroform and ethyl acetate extract (100 mg/kg) of Caesalpinia volkensii H. exhibited significant (P ≤ 0.05) antinociceptive activities using hot plate and writhing tests in mice while the later showed antiplasmodial activity (IC₅₀ 0.23 ± 0.07 and 4.39 ± 2.49 μg/ml) against chloroquine sensitive (D6) and chloroquine-resistant (W2), respectively. Two new furanoditerpenes [rel. 1β,5α-dihydroxyvoucapane (1) and rel. 1β,6β-dihydroxyvoucapane; 19β-methyl ester (2)] together with seven known compounds [voucapane (3), voucapan-5-ol (4), deoxycaesaldekarin C (5), caesaldekarin C (6), 5-hydroxyvinhaticoic acid (7), triacontanyl-(E)-ferulate (8), triacontanyl-(E)-caffaete (9) and 30′-hydroxytriacontanyl-(E)-ferulate (10)] were isolated from the two extracts. The administration of 3, 4, 5 and 6 (100 mg/kg i.p) caused a significant (P ≤ 0.05) reduction in the number of writhing episodes induced by acetic acid and (P ≤ 0.01) increased pain latency threshold in hot-plate test compared to control. However, the pure compounds indicated relatively (P ≤ 0.05) low antiplasmodial activity. The phytochemical constituents from the root bark of C. volkensii had better analgesic properties than antimalarial properties, justifying the use of the plant root bark as a remedy for pain.     

New sphingolipids from the root of Isatis indigotica and their cytotoxic activity

Two new sphingolipids were isolated from the 95% EtOH extract of traditional Chinese medicinal plant Isatis indigotica. Their structures were elucidated as (2S,3R)-3-hydroxymethyl-N-(2'-hydroxynonacosanoyl)-trideca-9E-sphingenine(1) and 1-O-beta-D-glucopyranosyl-(2S,3R)-3-hydroxymethyl-N-(2'-hydroxynonacosanoyl)-trideca-9E-sphingenine(2) on the basis of spectroscopic data. Their cytotoxic effects were evaluated by using MTT method.     

Cerebrosides with antiproliferative activity from Euphorbia peplis L.

Two new cerebrosides have been isolated from the whole plants of Euphorbia peplis L. The structures were established by FT-IR spectroscopy, FAB MS, EI-MS, ESI-MS, 1D and 2D NMR spectroscopy.     

Investigation of in vitro anthelmintic activities of Pycnanthus angolensis and Sphenocentrum jollyanum

Extracts from Pycnanthus angolensis stem bark, and fruits and seeds of Sphenocentrum jollyanum, when tested in vitro, showed potent anthelmintic activity on the earthworm, Eudrilus eugeniae. Methanolic extract of P. angolensis was more active than its chloroform extract (P<0.001), while fruit ethanolic extract of S. jollyanum was also more potent than the seed extract. When compared with other worms, S. jollyanum fruit extract showed the greatest activity on wireworms when tested at 80 mg/ml.     

A new cytotoxic 1-azaanthraquinone from the stems of Goniothalamus laoticus

A new 1-azaanthraquinone, named laoticuzanone A (1), and a synthetically known 3-methyl-1H-1-azaanthracene-2,9,10-trione (2), together with four known compounds, Griffithazanone A (3), methyl sinapate (4), methyl p-coumarate (5), and p-hydroxyphenylethyl p-coumarate (6) were isolated from the stems of Goniothalamus laoticus. Their structures were established on the basis of spectroscopic data as well as comparisons with the previous literature data. Compound 1 showed the highest cytotoxicity against KB and HeLa cells with IC₅₀ values of 0.68 and 0.50 μg/ml, respectively.