Antimycobacterial,antibacterial and antifungal activities of Terminalia superba (Combretaceae)

The methanol extract from the stem bark of Terminalia superba (TSB), fractions (TSB1–7) and two compounds isolated following bio-assay guided fractionation namely 3,4′-di-O-methylellagic acid 3′-O-β-d-xylopyranoside (1) and 4′-O-galloy-3,3′-di-O-methylellagic acid 4-O-β-d-xylopyranoside (2) were evaluated for their antimycobacterial, antibacterial and antifungal activities. The broth microdilution, the microplate Alamar Blue assay (MABA) and the agar disc diffusion methods were used for the investigations. The results of the antimycobacterial assays showed that the crude extract, fractions TSB5–7 and compound 1 were able to prevent the growth of all the studied mycobacteria. The lowest minimal inhibitory concentration (MIC) value of 39.06 µg/ml for this extract was recorded on both M. smegmatis and M. tuberculosis MTCS2. The corresponding values were 19.53 µg/ml and 4.88 µg/ml for fractions and compounds respectively. The MIC determination results on other organisms indicated values ranging from 19.53 to 78.12 µg/ml for TSB and compound 2 on 90.9% of the tested organisms, meanwhile compound 1 as well as fractions TSB 6 and 7 exhibited detectable MIC values on all studied microorganisms. The overall results provide promising baseline information for the potential use of the crude extract from T. superba, fractions 6–7 and the tested compounds in the treatment of tuberculosis, bacterial and fungal infections.     

Antimycobacterial activity of ellagitannin and ellagic acid derivate rich crude extracts and fractions of five selected species of Terminalia used for treatment of infectious diseases in African traditional medicine

Ten crude extracts and their solvent partition fractions from five species of Terminalia collected in Tanzania were assessed for antimycobacterial effects using Mycobacterium smegmatis ATCC 14468 as a model organism. We report here, for the first time, on antimycobacterial effects of root and stem bark extracts of Terminalia sambesiaca and Terminalia kaiserana as well as of fruit extracts of Terminalia stenostachya and leaf extracts of Terminalia spinosa. T. sambesiaca gave the best effects of all the investigated species in terms of the sizes of the inhibitory zones of root and stem bark extracts. A crude methanol root extract of T. sambesiaca gave lower MIC values (1250 μg/ml) than its aqueous and butanol soluble fractions (MIC 2500 μg/ml). Our preliminary HPLC–DAD data indicates that methanol and aqueous extracts of T. sambesiaca roots are rich in ellagitannins and ellagic acid glycosides. Particularly, one polar ellagitannin at t_R 10.3–10.9 min dominates the extracts quantitatively and thus may be responsible for their good antimycobacterial effects. In contrast to the more polar fractions, a chloroform soluble fraction of the roots of T. sambesiaca was devoid of antimycobacterial activity. Also crude methanol and aqueous extracts of the stem bark of T. sambesiaca gave promising antimycobacterial effects (MIC 1250 μg/ml). All fractions of T. kaiserana roots, except from the aqueous insoluble gave good antimycobacterial effects (MIC 1250 μg/ml) and the aqueous extract showed the best effects of the fractions in terms of the size of inhibition zones. These results justify the uses of hot water decoctions of the roots of T. kaiserana for treatment of cough, one of the symptoms of TB. According to HPLC–DAD data methanol extracts of T. kaiserana roots and their aqueous fractions are rich in polar ellagitannins and ellagic acid glycosides. Quantitatively, the ellagitannins dominate these extracts and therefore the good antimycobacterial activity of the methanol and aqueous extracts is assumed to be due to these compounds. Sephadex LH-20 CC fractions of a methanol extract of the roots of T. kaiserana inhibited the growth of M. smegmatis, giving MIC values of 1000 μg/ml. Ellagic acid glycosides in these fractions must be responsible for their good antimycobacterial effects since they are present in high concentrations. Good antimycobacterial effects were also obtained with a root extract of Terminalia sericea, and especially the butanol soluble fraction was a good inhibitor of the growth of M. smegmatis (MIC 1562 μg/ml). Our preliminary HPLC–DAD results show that the roots of T. sericea are rich in ellagitannins, ellagic acid glycosides and at least one stilbene compound. Extracts of the fruits of T. stenostachya gave good antimycobacterial effects, butanol extracts being the most active. Also the leaves of T. stenostachya, and especially the butanol soluble extracts, give good antimycobacterial effects. Our HPLC–DAD data indicate that T. stenostachya leaves contain large quantities of gallic acid, ellagitannins and ellagic acid glycosides. Our results indicate that many of the investigated species of Terminalia might contain leads for development of anti-TB drugs. Standardized extracts of T. sambesiaca, T. kaiserana and T. sericea roots could be used as easily available and cheap medicines for treatment of TB in remote regions of East and South Africa.     

Bioactivities of black cumin essential oil and its main terpenes from Tunisia

Ex vivo antioxidant, anti-inflammatory, anticancer and antibacterial activities of the essential oil from Tunisian Nigella sativa seeds and its main terpenes (p-cymene, γ-terpinene, thymoquinone, β-pinene, carvacrol, terpinen-4-ol and longifolene) were determined. The essential oil exhibited strong ex vivo antioxidant activity, inhibiting DCFH oxidation with an IC₅₀ of 1.0 µg/ml, and high anti-inflammatory activity, inhibiting NO radical excretion with an IC₅₀ value of 6.3 µg/ml. Thymoquinone was found to be the most active to decrease DCFH oxidation and NO excretion. The oil was found to significantly inhibit the growth of A-549 and DLD-1 cancer cell lines (IC₅₀ values of 43.0 and 46.0 µg/ml, respectively) and to exert antibacterial activity against Staphylococcus aureus and Escherichia coli with IC₅₀ values of 12.0 and 62.0 µg/ml. The anticancer and antibacterial activities could be mainly due to the action of thymoquinone and longifolene.     

Design, synthesis and antimycobacterial activities of 1-methyl-2-alkenyl-4(1H)-quinolones

A series of 23 new 1-methyl-2-alkenyl-4(1H)quinolones have been synthesized and evaluated in vitro for their antimycobacterial activities against fast growing species of mycobacteria, such as Mycobacterium fortuitum, M. smegmatis and M. phlei. The compounds displayed good to excellent inhibition of the growth of the mycobacterial test strains with improved antimycobacterial activity compared to the hit compound, evocarpine. The most active compounds, which possessed chain length of 11-13 carbons at position-2 displayed potent inhibitory effects with an MIC value of 1.0 mg/L. In a human diploid embryonic lung cell line, MRC-5 cytotoxicity assay, the alkaloids showed weak to moderate cytotoxic activity. Biological evaluation of these evocarpine analogues on the less pathogenic fast growing strains of mycobacteria showed an interesting antimycobacterial profile and provided significant insight into the structure-activity relationships.     

Antimalarial compounds from Schefflera umbellifera

The organic extract of the leaves of Schefflera umbellifera exhibited good antimalarial activity when tested against the chloroquine-susceptible strain (D10). Bioassay-guided fractionation of the dichloromethane fraction of the dichloromethane/methanol extract yielded an active compound, betulin, which exhibited good antiplasmodial activity with an IC₅₀ value of 3.2 µg/ml. The reference compound, chloroquine gave an IC₅₀ value of 27.2 ng/ml. Two other compounds were also isolated from the dichloromethane extract namely, 7-hydroxy-6-methoxycoumarin and ent-kaur-16-en-19-oic acid. These two compounds did not exhibit any significant antiplasmodial activity.     

Antifungal, acetylcholinesterase inhibition, antioxidant and phytochemical properties of three Barleria species

This study was aimed at evaluating the antifungal, acetylcholinesterase inhibition and antioxidant activities of petroleum ether, dichloromethane, ethanol and methanol extracts from different parts of Barleria prionitis, Barleria greenii and Barleria albostellata. Their phytochemical properties and the possibility of plant-part substitution as a conservation strategy against destructive harvesting (use of aerial parts and roots) of these species for medicinal purposes were also investigated. Microtitre plate assays were used in determining their antifungal (against Candida albicans) and acetylcholinesterase inhibition activities. All the extracts demonstrated both fungistatic and fungicidal activities with the minimum inhibitory concentration ranging from 0.78 to 9.38 mg/ml and minimum fungicidal concentration ranging from 1.17 to 12.50 mg/ml. The higher inhibitory activity of B. greenii leaf extracts in most cases compared to similar extracts of the stems and roots suggest the potential of B. greenii leaves in plant-part substitution. At the lowest extract concentration (0.156 mg/ml), the leaf extract of B. greenii demonstrated a significantly higher acetylcholinesterase (AChE) inhibition than its stem and root extracts. In B. albostellata, the AChE inhibitory activity demonstrated by the stem was significantly greater than that recorded in its leaf extract. These findings suggest that the idea of plant part substitution may be species and/or biological activity dependent. In the DPPH radical scavenging assay, different parts of Barleria species showed free radical scavenging activity with EC₅₀ values ranging from 6.65 to 12.56 μg/ml. The ability of the extracts from different plant parts to reduce ferric ion/ferricyanide complex to the ferrous form and decrease carotenoid bleaching rate suggests the presence of antioxidant compounds capable of donating electrons and hydrogen atoms in their reaction mechanisms. Flavonoids, iridoids and tannins were detected in the different parts of these Barleria species. These phytochemicals might be responsible for the observed biological activities. The isolation of specific bioactive compounds through bioassay-guided fractionation and their characterization as well as studies evaluating their safety may be necessary in the exploration of these species for potential new therapeutic drugs or drug leads.     

The ethnobotany,leaf anatomy,essential oil variation and biological activity of Pteronia incana (Asteraceae)

The only available ethnobotanical information on Pteronia incana has been recorded by the Montagu Museum in the Western Cape Province of South Africa. It was reported that the plant is used to treat influenza, fever, kidney ailments and backache. In common with other species of Pteronia, the plant contains an essential oil reminiscent of pine turpentine oil with β-pinene, limonene, 1,8-cineole, myrcene, spathulenol, p-cymene and methyleugenol as main compounds present in all or most of the samples, with smaller amounts of α-pinene, sabinene, γ-terpinene, terpinen-4-ol, biclogermacrene, globulol and α-bisabolol in some of the distillates. We investigated the oil composition of 11 individual plants collected at three geographically distant localities but found limited variation, both within and between populations. Leaf sections of P. incana showed that it is anatomically similar to P. divaricata in the presence of a secretory duct associated with the main vascular bundle (and often other bundles as well), in addition to glandular and non-glandular trichomes on both leaf surfaces. One yeast (Cryptococcus neoformans), two Gram-negative bacteria (Moraxella catarrhalis and Klebsiella pneumoniae) and one Gram-positive bacterium (Mycobacterium smegmatis) were selected for antimicrobial activity studies using the minimum inhibitory concentration (MIC) microtitre plate method. The results showed that methanol:dichloromethane (MeOH:CH₂Cl₂) extracts were active against M. smegmatis (lowest MIC values of 0.5–0.8 mg/ml) and C. neoformans (lowest MIC values of 0.5–2.0 mg/ml). The essential oil was most active against C. neoformans (lowest MIC value of 0.3 mg/ml). These results provide a scientific rationale for the use of P. incana in Cape herbal medicine.     

In vitro anti-influenza virus activity of a cardiotonic glycoside from Adenium obesum (Forssk.)

Methanolic extracts of six Saudi plants were screened for their in vitro antiviral activity using influenza virus A/PR/8/34 (H1N1) and MDCK cells in an MTT assay. The results indicated that the extracts of Adeniumobesum and Tephorosianubica possessed antiviral activity (99.3 and 93.3% inhibition at the concentration of 10 μg/ml, respectively). Based on these results A. obesum was selected for further study by applying bioactivity-guided fractionation to isolate its antiviral principle. The antiviral principle was isolated from the chloroform fraction through solvent fractionation, combined open liquid chromatography and HPLC. The isolated active compound A was identified as oleandrigenin-β-d-glucosyl (1 → 4)-β-d-digitalose, on the basis of its spectral analysis (MS, 1D and 2D NMR). The isolated glycoside showed reduction of virus titre by 69.3% inhibition at concentration of 1 μg/ml (IC₅₀ = 0.86 μg/ml).     

Plasmodium falciparum: In vitro interaction of quassin and neo-quassin with artesunate, a hemisuccinate derivative of artemisinin

Quassia amara L. (Family Simaroubaceae) is known to have several medicinal properties including the activity against malaria. An HPLC method was employed for purification of the biologically active quassinoids; quassin (Q) and neo-quassin (NQ), further characterized by MALDI-TOF analyses. Purified Q, NQ and the crude bark extract (S1) along with artesunate (AS) were studied for their in vitro anti-plasmodial activity. The in vivo toxicity studies at intraperitoneal doses with higher concentrations of the crude bark extract (S1) in Balb/C mice ruled out the apprehension of toxicity. Interaction studies between the test compounds among themselves (Q + NQ) and individually with artesunate (AS + Q, AS + NQ), were carried out in vitro at four ratios (1:5, 1:2, 2:1 and 5:1) on chloroquine sensitive (MRC-pf-20) and resistant (MRC-pf-303) strains of Plasmodium falciparum. The crude bark extracts of Q. amara exhibited higher P. falciparum inhibitory activity (IC₅₀ = 0.0025 μg/ml) as compared to that of the isolated compounds, quassin (IC₅₀ = 0.06 μg/ml, 0.15 μM), neo-quassin (IC₅₀ = 0.04 μg/ml, 0.1 μM) and also to the positive control, artesunate (IC₅₀ = 0.02 μg/ml, 0.05 μM). The in vitro drug interaction study revealed the compounds, quassin and neo-quassin to be additive to each other. At lower ratios, artesunate was found to be a potential combination partner with both the compounds. It was interesting to note that none of the combinations exhibited antagonistic interactions. This phenomenon offers the opportunity for further exploration of novel therapeutic concentrations and combinations.     

Temperature and salinity tolerance of Mesopodopsis africana O. Tattersall in the freshwater-deprived St. Lucia Estuary, South Africa

Mesopodopsis africana is a key species in the St. Lucia Estuary, Africa's largest estuarine lake. This system is currently undergoing an unprecedented crisis due to freshwater deprivation. A reversed salinity gradient has persisted with hypersaline conditions (> 300) occurring in the upper regions of the estuarine lake. In the context of climate change, rising temperatures will not only push the thermal tolerance limits of estuarine organisms, but increased evaporation from this lake's large surface area will lead to further salinity increases. The present study aims to determine the temperature and salinity tolerance of M. africana, both through in situ studies and the use of laboratory experiments. Results indicate that M. africana is a broad euryhaline species. Mysids were recorded at salinity levels ranging from 2.55 to 64.5 in situ. While experiments revealed a narrower salinity tolerance, acclimation resulted in a significant increase in the tolerance range of this species. It is probable, however, that slower acclimation times may increase survival rates even further, particularly in the higher salinity treatments. M. africana was especially tolerant of the lower salinity levels. In the 20 °C acclimation experiment, LS₅₀ at 1 and 2.5 was only reached after 8 and > 168 h, respectively. Survival at 10 and 40 °C was negligible at all salinity levels. This concurs with field results which documented mysids at temperatures ranging from 16.2 to 30.9 °C. Salinity and temperature increases associated with global climate change may, therefore, have significant implications for these mysid populations, with cascading effects on the higher trophic levels which they support.     

Copper accumulation and oxidative stress in the sea anemone, Aiptasia pallida, after waterborne copper exposure

Copper is a common marine pollutant yet its effects on symbiotic cnidarians are largely understudied. To further understand the impact of elevated copper concentrations on marine symbiotic organisms, toxicity tests were conducted using the model sea anemone, Aiptasia pallida, with and without its zooxanthellae symbiont. Symbiotic and aposymbiotic A. pallida were exposed to sublethal copper concentrations (0, 5, 15, and 50 µg/L) for 7 d and copper accumulation, behavior, and the activity of the oxidative stress enzymes, superoxide dismutase (SOD), and catalase (CAT) were measured. Additionally, acute 96-h toxicity tests were conducted to determine LC₅₀ values of the organisms after copper exposure. Both symbiotic and aposymbiotic A. pallida rapidly accumulated copper in a time and dose dependent manner. However, higher copper concentrations accumulated in the aposymbiotic as compared to the symbiotic A. pallida. In response to the highest two copper exposures (15 and 50 µg/L) symbiotic A. pallida upregulated CAT activity to combat the damaging effects of hydrogen peroxide. Contrary to these results, SOD activity significantly decreased during the highest copper exposure, when compared to controls. CAT activity was not detected and SOD was substantially (> 10 fold) reduced in aposymbiotic A. pallida, suggesting that the zooxanthellae are associated with the oxidative stress response. Copper exposure as low as 5 µg/L caused tentacle retraction and increased mucus production in both symbiotic and aposymbiotic anemones. The LC₅₀ values for symbiotic and aposymbiotic A. pallida exposed to copper for 96 h were 148 µg/L (95% confidence interval = 126.4, 173.8) and 206 µg/L (95% confidence interval = 175.2, 242.2), respectively. Understanding the varying responses of symbiotic and aposymbiotic A. pallida to copper stress may advance our comprehension of the functional roles of zooxanthellae and host. Although the mechanism of copper toxicity has not been fully elucidated, it is clear that A. pallida accumulate copper and are sensitive, as effects were detected at environmentally relevant copper concentrations. Likewise, A. pallida may be useful in biomonitoring copper polluted environments.     

Antibacterial and antioxidant activities of four kaempferol methyl ethers isolated from Dodonaea viscosa Jacq. var. angustifolia leaf extracts

Fractionation of dichloromethane and acetone fractions obtained by serial extraction from the leaf powder of Dodonaea viscosa Jacq. var. angustifolia (Sapindaceae) resulted in the isolation of four kaempferol methyl ethers. The compounds were identified by spectral data (¹H NMR, ¹³C NMR and MS) as: 3, 5, 7-trihydroxy-4'-methoxyflavone (1); 5, 7, 4'-trihydroxy-3, 6-dimethoxyflavone (2); 5, 7-dihydroxy-3, 6, 4'-trimethoxyflavone (santin) (3); and 5-hydroxy -3, 7, 4'-trimethoxyflavone (4) together with 3,4',5,7-tetrahydroxy flavone (kaempferol) (5). Antioxidant potential of the compounds was evaluated using a DPPH spectrophotometric assay, while antibacterial activity was determined using a serial dilution microplate technique. The isolates demonstrated varying degrees of antioxidant and antibacterial activities. Of all the compounds investigated, compounds 1 and 5 demonstrated some antioxidant activity (EC₅₀ = 75.49 ± 1.76 µM and 35.06 ± 0.85 respectively) but lower than l-ascorbic acid (EC₅₀ = 13.55 ± 0.28 µM) used as a standard antioxidant agent. The minimum inhibitory concentration (MIC) of isolated compounds against Staphylococcus aureus, Enterococcus faecalis, Escherichia coli and Pseudomonas aeruginosa varied from 16 µg/ml to more than 250 µg/ml. Some structure activity relationships could be established for these compounds.     

Cardiodepressive effect elicited by the essential oil of Alpinia speciosa is related to L-type Ca current blockade

This study was undertaken to elucidate the effect of the essential oil from Alpinia speciosa (EOAs) on cardiac contractility and the underlying mechanisms. The essential oil was obtained from Alpinia speciosa leaves and flowers and the oil was analyzed by GC-MS method. Chemical analysis revealed the presence of at least 18 components. Terpinen-4-ol and 1,8-cineole corresponded to 38% and 18% of the crude oil, respectively. The experiments were conducted on spontaneously-beating right atria and on electrically stimulated left atria isolated from adult rats. The effect of EOAs on the isometric contractions and cardiac frequency in vitro was examined. EOAs decreased rat left atrial force of contraction with an EC₅₀ of 292.2 ± 75.7 μg/ml. Nifedipine, a well known L-type Ca²⁺ blocker, inhibited in a concentration-dependent manner left atrial force of contraction with an EC₅₀ of 12.1 ± 3.5 μg/ml. Sinus rhythm was diminished by EOAs with an EC₅₀ of 595.4 ± 56.2 μg/ml. Whole-cell L-type Ca²⁺ currents were recorded by using the patch-clamp technique. EOAs at 25 μg/ml decreased I_Ca,L by 32.6 ± 9.2% and at 250 μg/ml it decreased by 89.3 ± 7.4%. Thus, inhibition of L-type Ca²⁺ channels is involved in the cardiodepressive effect elicited by the essential oil of Alpinia speciosa in rat heart.     

Feeding and growth kinetics of the planktotrophic larvae of the spionid polychaete Polydora ciliata (Johnston)

We studied the effect of food concentration on the feeding and growth rates of different larval developmental stages of the spionid polychaete Polydora ciliata. We estimated larval feeding rates as a function of food abundance by incubation experiments with two different preys, presented separately, the cryptophyte Rhodomonas salina (ESD = 9.7 µm) and the diatom T.weissflogii (ESD = 12.9 µm). Additionally, we determined larval growth rates and gross growth efficiencies (GGE) as a function of R. salina concentration.P.ciliata larvae exhibited a type II functional response. Clearance rates decreased continuously with increasing food concentration, and ingestion rates increased up to a food saturation concentration above which ingestion remained fairly constant. The food concentration at which feeding became saturated varied depending on the food type, from ca. 2 µg C mL^− 1 when feeding on T. weissflogii to ca. 5 µg C mL^− 1 when feeding on R. salina. The maximum carbon specific ingestion rates were very similar for both prey types and decreased with increasing larval size/age, from 0.67 d^− 1 for early larvae to 0.45 d^− 1 for late stage larvae. Growth rates as a function of food concentration (R. salina) followed a saturation curve; the maximum specific growth rate decreased slightly during larval development from 0.22 to 0.17 d^− 1. Maximum growth rates were reached at food concentrations ranging from 2.5 to 1.4 µg C mL^− 1 depending on larval size. The GGE, estimated as the slope of the regression equations relating specific growth rates versus specific ingestion rates, were 0.29 and 0.16 for early and intermediate larvae, respectively. The GGE, calculated specifically for each food level, decreased as the food concentration increased, from 0.53 to 0.33 for early larvae and from 0.27 to 0.20 for intermediate larval stages.From an ecological perspective, we suggest that there is a trade-off between larval feeding/growth kinetics and larval dispersal. Natural selection may favor that some meroplanktonic larvae, such as P.ciliata, present low filtration efficiency and low growth rates despite inhabiting environments with high food availability. This larval performance allows a planktonic development sufficiently long to ensure efficient larval dispersion.     

Thermogenic characteristics and evaporative water loss in the tree shrew (Tupaia belangeri)

Thermogenic characteristics and evaporative water loss were measured at different temperatures in Tupaia belangeri. The thermal neutral zone (TNZ) of T. belangeri was 30–35 °C. Mean body temperature was 39.76±0.27 °C and mean body mass was 100.86±9.09 g. Basal metabolic rate (BMR) was 1.38±0.03 ml O₂/g h. Average minimum thermal conductance (C_m) was 0.13±0.01 ml O₂/g h °C. Evaporative water loss in T. belangeri increased when the temperature rose; the maximal evaporative water loss was 3.88±0.41 mg H₂O/g h at 37.5 °C. The results may reflect features of small mammals in the sub-tropical plateau region: T. belangeri had high basal metabolic rate and high total thermal conductance, compared with the predicted values based on their body mass whilst their body temperatures are relatively high; T. belangeri has high levels of evaporative water loss and poor water-retention capacity. Evaporative water loss plays an important role in temperature regulation.     

Using a starch-rich mutant of Arabidopsis thaliana as feedstock for fermentative hydrogen production

A mutant plant (Arabidopsis thaliana), sex1-1 (starch excess 1-1), accumulating high starch content in leaves was created to serve as better biomass feedstock for a H₂-producing strain Clostridium butyricum CGS2, which efficiently utilizes starch for H₂ production but cannot assimilate cellulosic materials. The starch content of the mutant plant increased to 10.67 mg/fresh weight, which is four times higher than that of wild type plant. Using sex1-1 mutant plant as feedstock, C. butyricum CGS2 could produce 490.4 ml/l of H₂ with a H₂ production rate of 32.9 ml/h/l. The H₂ production performance appeared to increase with the increase in the concentration of mutant plant from 2.5 to 10 g/l. The highest H₂ to plant biomass yield was nearly 49 ml/g for the mutant plant. This study successfully demonstrated the feasibility of using a starch-rich mutant plant for more effective bioH₂ production with C. butyricum CGS2.     

Relationship correlation of antioxidant and antiproliferative capacity of Cyperus rotundus products towards K562 erythroleukemia cells

A Total Oligomers Flavonoids (TOFs) and ethyl acetate extracts of Cyperus rotundus were analyzed, in vitro, for their antioxidant activity using several biochemical assays: the xanthine (X)/xanthine oxidase (XO), the lipid peroxidation induced by H₂O₂ in K562 human chronic myelogenous leukemia cells and the DNA damage in pKS plasmid DNA assay induced by H₂O₂/UV-photolysis and for their apoptotic effect. TOF and ethyl acetate extracts were found to be efficient in inhibiting xanthine oxidase with IC₅₀ values of 240 and 185 μg/ml and superoxide anion with IC₅₀ values of 150 and 215 μg/ml, respectively. Also, all the extracts tested were effective in reducing the production of thiobarbituric acid reactive substances (TBARS) and were able to protect against H₂O₂/UV-photolysis induced DNA damage. The highest activity, measured as equivalents of MDA concentration, was observed in the ethyl acetate extract (MDA = 2.04 nM). In addition, the data suggest that only TOF enriched extract exerts growth inhibition on K562 cells through apoptosis induction. Therefore, these extracts were subjected to further separation by chromatographic methods. Thus, three major compounds (catechin, afzelechin and galloyl quinic acid) were isolated from the TOF enriched extract and five major compounds (luteolin, ferulic acid, quercetin, 3-hydroxy, 4-methoxy-benzoic acid and 6,7-dimethoxycoumarin) from ethyl acetate extract. Their structures were determined by spectroscopic data analysis and comparison with the literature. In addition, we evaluate the biological activities of the catechin, ferulic acid and luteolin. This investigation has revealed that the luteolin was the most active in reducing the production of TBARS (MDA = 1.5 nM), inhibiting significantly the proliferation of K562 cells (IC₅₀ = 25 μg/ml) and protecting against H₂O₂/UV-photolysis induced DNA damage. In conclusion, the study reveals that the ability of C. rotundus to inhibit the enzyme xanthine oxidase (XO), the lipid peroxidation and to exert apoptotic effect, may explain possible mechanisms by which C. rotundus exhibits its health benefits.     

Antiplasmodial benzophenones from the trunk latex of Moronobea coccinea (Clusiaceae)

In an effort to find antimalarial drugs, a systematic in vitro evaluation on a chloroquine-resistant strain of Plasmodium falciparum (FcB1) was undertaken on sixty plant extracts collected in French Guiana. The methanol extract obtained from the latex of Moronobea coccinea exhibited a strong antiplasmodial activity (95% at 10 μg/ml). The phytochemical investigation of this extract led to the isolation of eleven polycyclic polyprenylated acylphloroglucinols (PPAPs), from which eight showed potent antiplasmodial activity with IC50 ranged from 3.3 μM to 37.2 μM.     

Synthesis, characterization, X-ray structure and in vitro antimycobacterial and antitumoral activities of Ru(II) phosphine/diimine complexes containing the "SpymMe2" ligand, SpymMe2=4,6-dimethyl-2-mercaptopyrimidine

The reaction of cis-[RuCl₂(dppb)(N-N)], dppb = 1,4-bis(diphenylphosphino)butane, complexes with the ligand HSpymMe₂, 4,6-dimethyl-2-mercaptopyrimidine, yielded the cationic complexes [Ru(SpymMe₂)(dppb)(N-N)]PF₆, N-N = bipy (1) and Me-bipy (2), bipy = 2,2′-bipyridine and Me-bipy = 4,4′-dimethyl-2,2′-bipyridine, which were characterized by spectroscopic and electrochemical techniques and X-ray crystallography and elemental analysis. Additionally, preliminary in vitro tests for antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27264 and antitumor activity against the MDA-MB-231 human breast tumor cell line were carried out on the new complexes and also on the precursors cis-[RuCl₂(dppb)(N-N)], N-N = bipy (3) and Me-bipy (4) and the free ligands dppb, bipy, Me-bipy and SpymMe₂. The minimal inhibitory concentration (MIC) of compounds needed to kill 90% of mycobacterial cells and the IC₅₀ values for the antitumor activity were determined. Compounds 1-4 exhibited good in vitro activity against M. tuberculosis, with MIC values ranging between 0.78 and 6.25 μg/mL, compared to the free ligands (MIC of 25 to >50 μg/mL) and the drugs used to treat tuberculosis. Complexes 1 and 2 also showed promising antitumor activity, with IC₅₀ values of 0.46 ± 0.02 and 0.43 ± 0.08 μM, respectively, against MDA-MB-231 breast tumor cells.