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.     

Two new triterpenoids from the bark of Eucalyptus exserta and their molluscicidal and cytotoxic activities

Two new triterpenoids, 2α-hydroxyurs-12-en-28-oic acid-3β-trans- isoferulate (1) and 2α, 3α, 24-trihydroxyolean-18-en-28-oic acid (2), together with three known triterpenoids (3-5) were isolated from the methanol extract of the bark of Eucalyptus exserta. Their structures were determined by spectroscopic means. Compounds 1, 2, and 5 exhibited molluscicidal activity against Pomacea canaliculata. All isolated compounds showed significant cytotoxic activity against Spodoptera litura (SL) cells.     

Molluscicidal activity against Oncomelania hupensis of Ginkgo biloba

In search for molluscicidal active components, petroleum ether, ethyl acetate, ethanol, and water extracts from Ginkgo sarcotesta were evaluated against the snail Oncomelania hupensis. The bioassay-oriented showed that the activity concentrates in the petroleum ether extract (LD(50) 7.81 ppm). Ginkgolic acids, isolated from the petroleum ether extract, exhibited strong molluscicidal activity (LD(50) 1.49 ppm), gingkgolic acid C15:1 having the strongest molluscicidal activity.     

Anti-HBV activities of Streblus asper and constituents of its roots

The extracts from leaves, heartwood, barks and roots of the Streblus asper were investigated for anti-HBV activities, separately. The results suggested that the MeOH extracts of the heartwood, barks, and roots exhibited good anti-HBV activities. Further investigations displayed that ethyl acetate and n-butanol soluble parts of their MeOH extracts showed more significant anti-HBV activities. Moreover, a new lignan, together with 11 known compounds, was isolated from n-butanol-soluble part of MeOH extract of the roots of S. asper. The structures were elucidated by spectroscopic methods, including 1D NMR ((1)H NMR, (13)C NMR), 2D NMR (HMQC, HMBC) and HR-EI-MS experiments. Compounds 1-3 were evaluated for their anti-HBV activities. Honokiol showed significant anti-HBV activity with IC(50) values of 3.14μM and 4.74μM for HBsAg and HBeAg with no cytotoxicity respectively, while lamivudine (3TC, positive control) exhibited weak anti-HBV activity with IC(50) values of 11.81μM and 25.80μM for HBsAg and HBeAg respectively.     

Antibacterial carbazole alkaloids from Clausena harmandiana twigs

Three new carbazole alkaloids, harmandianamines A-C (1-3), together with fifteen known compounds (4-18) were isolated from the twigs of Clausena harmandiana. The structures were elucidated by spectroscopic methods, including UV, IR, NMR, and MS. The antibacterial activity against Escherichia coli TISTR 780, Salmonella typhimurium TISTR 292, Staphylococcus aureus TISTR 1466 and methicillin-resistant S. aureus (MRSA) SK1 of some isolated compounds was also evaluated. Compound 6 exhibited significant antibacterial activity against MRSA SK1 with an MIC value of 0.25 μg/mL which higher than that of standard drug, vancomycin (MIC value=1 μg/mL) whereas compounds 14 and 5 showed strong activity with MIC values of 4 and 8 μg/mL, respectively. Only compound 14 showed strong antibacterial activity against S. aureus TISTR 1466 with an MIC value of 4 μg/mL.     

Flavonoids with antiplasmodial and cytotoxic activities of Macaranga triloba

A new flavanone derivative, malaysianone A (1), four prenylated flavanones, 6-prenyl-3'-methoxyeriodictyol (2), nymphaeol B (3), nymphaeol C (4) and 6-farnesyl-3',4',5,7-tetrahydroxyflavanone (5), and two coumarins, 5,7-dihydroxycoumarin (6) and scopoletin (7), were isolated from the dichloromethane extract of the inflorescences of Macaranga triloba. The structures of these compounds were elucidated based on spectroscopic methods including nuclear magnetic resonance (NMR-1D and 2D), UV, IR and mass spectrometry. The cytotoxic activity of the compounds was tested against several cell lines, with 5 inhibiting very strongly the growth of HeLa and HL-60 cells (IC(50): 1.3 μg/ml and 3.3 μg/ml, respectively). Compound 5 also showed strong antiplasmodial activity (IC(50): 0.06 μM).     

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.     

Molluscicidal activity of Solanum species of the Northeast of Brazil on Biomphalaria glabrata

Seven species of Solanum were screened for their molluscicidal properties against Biomphalaria glabrata, the intermediated host of Schistosoma mansoni, Solanum agrarium, S. jabrense, S. melissarum, S. megalonyx, S. paludosum, S. paraibanum and S. stipulaceum. Four extracts showed molluscicidal activity with LC(50) from 22 to 56 microg/ml.     

Antifeedant activity of Momordica dioica fruit pulp extracts on Spodoptera litura

The hexane extract and ethyl acetate soluble fraction of methanolic extract of the fruit pulp of Momordica dioica exhibited moderate and concentration dependent antifeedant activity against Spodoptera litura.     

Antithrombotic phenolic compounds from Glycyrrhiza uralensis

A new coumestan, named glycyrurol, and nine phenolic compounds were isolated from the ethyl acetate extract of the roots and rhizomes of Glycyrrhiza uralensis. Their structures were elucidated based on spectroscopic analysis and literature data, and anticoagulative assay found significant antithrombotic activity of compounds 4, 8 and 10.     

Three new antibacterial active diarylheptanoids from Alpinia officinarum

Three new diarylheptanoids, together with ten known ones, were isolated from the ethanol extract from the rhizomes of Alpinia officinarum Hance. The structural identification of these compounds was mainly achieved by spectroscopic methods. The new compounds were elucidated as 7-(4″, 5″-dihydroxy-3″-methoxyphenyl)-1-phenyl -4-heptene-3-one (1), 1, 7-diphenyl-5-heptene-3-one (2) and 4-phenethyl-1, 7-diphenyl -1-heptene-3, 5-dione (3), respectively. All of the compounds showed antibacterial activity against Helicobactor pylori. Especially, the three new compounds showed strong antibacterial activity against Hp-Sydney strain 1 with the MIC values of 9–12 μg/mL, and against Hp-F44 with the MIC values of 25–30 μg/mL.     

Five new furostanol saponins from the rhizomes of Tupistra chinensis

Five new furostanol saponins (1-5), together with three known compounds (6-8) were obtained from the n-butanol soluble fraction of ethanol extract from Tupistra chinensis. Their structures were determined on the basis of chemical methods and spectral data. The isolated compounds were tested in vitro for their cytotoxic activities against the A549, HepG 2 and Caski cancer cell lines. Among them, compounds 6, 7, and 8 showed cytotoxicity against A549 cancer cell lines with IC(50) values of 6.6, 6.7 and 29.1 μM, respectively.     

Molluscicidal activity of some Moroccan medicinal plants

Among 14 plants of Moroccan folk medicine tested for molluscicidal activity, ethyl acetate extract from Origanum compactum and hexane extracts from both Chenopodium ambrosioides and Ruta chalepensis were the most active (LC(90)=2.00, 2.23 and 2.23 mg l(-1), respectively) against the schistosomiasis-transmitting snail Bulinus truncatus.     

Ent-trachyloban-19-oic acid isolated from Iostephane heterophylla as a promising antibacterial agent against Streptococcus mutans biofilms

From the roots of Iostephane heterophylla, six known compounds, namely, ent-trachyloban-19-oic acid (1), the mixture of ent-kaur-16-en-19-oic acid (2) and ent-beyer-15-en-19-oic acid (3), xanthorrhizol (4), 16α-hydroxy-ent-kaurane (5) and 16α-hydroxy-ent-kaur-11-en-19-oic acid (6) were isolated using a bioassay-guided fractionation method. The known compounds (1-6) were identified by comparison of their spectroscopic data with reported values in the literature. In an attempt to increase the resultant antimicrobial activity of 1 and 4, a series of reactions was performed on ent-trachyloban-19-oic acid (1) and xanthorrhizol (4), to obtain derivatives 1a, 1b, and 4a-4d. All the isolated compounds (1-6) and the derivatives 1a, 1b, and 4a-4d were evaluated for their antimicrobial activity against two oral pathogens, Streptococcus mutans and Porphyromonas gingivalis associated with caries and periodontal disease, respectively. Compounds 1, 1b, 2+3, 4 and 4d inhibited the growth of S. mutans with concentrations ranging from 4.1 μg/mL to 70.5 μg/mL. No significant activity was found on P. gingivalis except for 4 with an MIC of 6.8 μg/mL. The ability of 1, 1b, 2+3, 4 and 4d to inhibit biofilm formation by S. mutans was evaluated. It was found that 1, 1b, 4 and 4d interfered with the establishment of S. mutans biofilms, inhibiting their development at 32.5, 125.0, 14.1 and 24.4 μg/mL, respectively.     

Chemical constituents of Anacolosa pervilleana and their antiviral activities

In an effort to identify novel inhibitors of Chikungunya (CHIKV) and Dengue (DENV) virus replication, a systematic study with 820 ethyl acetate extracts of Madagascan plants was performed in a virus-cell-based assay for CHIKV and a DENV NS5 RNA-dependant RNA polymerase (RdRp) assay. The extract obtained from the leaves of Anacolosa pervilleana was selected for its significant activity in both assays. One new (E)-tridec-2-en-4-ynedioic acid named anacolosine (1), together with three known acetylenic acids, the octadeca-9,11,13-triynoic acid (2), (13E)-octadec-13-en-9,11-diynoic acid (3), (13E)-octadec-13-en-11-ynoic acid (4), two terpenoids, lupenone (5) and β-amyrone (6), and one cyanogenic glycoside, (S)-sambunigrin (7) were isolated. Their structures were elucidated by comprehensive analyses of NMR spectroscopy and mass spectrometry data. The inhibitory potency of these compounds was evaluated on CHIKV, DENV RdRp and West-Nile polymerase virus (WNV RdRp). Both terpenoids showed a moderate activity against CHIKV (EC(50) 77 and 86 μM, respectively) and the acetylenic acids produced IC(50) values around 3 μM in the DENV RdRp assay.     

A new epicatechin gallate and calpain inhibitory activity from Orostachys japonicus

Calpains are calcium-dependent proteases that cleave a variety of intracellular substrates. The overactivation of mu-calpain is associated with a wide range of disease conditions. To search for calpain inhibitors from natural products, the phytochemical constituents of the ethyl acetate fraction of the whole plant of Orostachys japonicus (Crassulaceae) were studied. The various chromatographic separation of this fraction led to the isolation of a new tannin, (-)-epicatechin 5-gallate (1) along with 9 known compounds. Their structures were elucidated by spectroscopic and chemical analyses. Among them, (-)-epicatechin 5-gallate (1) and kaempferol (9) exhibited moderate inhibitory activity against mu-calpain with IC(50) values of 18.0+/-2.9 and 15.4+/-2.0 microg/ml, respectively.     

Molluscicidal and radical scavenging activity of quinones from the root bark of Caryopteris x clandonensis

In the search for new molluscicidal natural products, the activity of the chloroform extract of the root barks of Caryopteris x clandonensis was tested. The LC(100) was <5 ppm. The fractionation and purification of the extract afforded 15-deoxyfuerstione, fuerstione and alpha-caryopterone as the main compounds. These compounds were tested against the snail Bulinus truncatus, an intermediate host snail of a schistosomiasis parasite and showed strong molluscicidal activity with LC(100)<4 ppm. In addition, they were found to have potent radical scavenging properties on superoxide radical.     

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.     

美洲大蠊乙酸乙酯提取物的分离和抑菌活性分析

采用活性追踪法和柱层析法,以金黄色葡萄球菌、大肠杆菌等5种细菌为供试菌种,对美洲大蠊乙酸乙酯提取物进行分离和抑菌试验.研究发现:美洲大蠊乙酸乙酯提取物对供试的革兰氏阳性菌具有一定的抑制作用,其中,对枯草芽孢杆菌的抑菌活性最好;经硅胶柱层析初分离后,从乙酸乙酯提取物获得了9个具有抑菌活性的组分,其中,组分Fr7对5种供试菌均显示了较好的抑菌活性;组分Fr7及其相邻组分Fr8经硅胶和凝胶柱层析进一步分离纯化后,得到了7个具有抑菌活性的不饱和脂肪酸类化合物,均对藤黄微球菌表现出最好的抑菌活性.结果表明:美洲大蠊乙酸乙酯提取物的抑菌活性物质为不饱和脂肪酸类化合物,对供试的革兰氏阳性菌的抑菌活性较强.     

Antioxidant activity of Erica arborea

The antioxidant properties of the methanol extract of leaves and flowers of Erica arborea and the ethyl acetate, butanol and water soluble fractions were investigated. The ethyl acetate extract was found to be the richest for phenolic and flavonoid content which showed the highest antioxidant activity.