Enzyme Inhibition and Antioxidant Activities of Asparagus officinalis L. and Analysis of Its Phytochemical Content by LC/MS/MS

In the study, water, ethanol, methanol, dichloromethane, and acetone extracts of Asparagus officinalis L. were obtained by maceration. DPPH⋅, ABTS⋅⁺, FRAP, and CUPRAC methods determined the antioxidant capacities of all extracts. Moreover, the in vitro effects of extracts on acetylcholinesterase (AChE), butyrylcholinesterase (BChE), carbonic anhydrase (CA)-I, CA-II and α-Glycosidase were investigated. At a 10 μg/ml concentration, the extract with the highest Fe³⁺ reduction capacity was ethanol (AE), and the extract with the highest Cu²⁺ reduction capacity was acetone (AA). AE for AChE (IC₅₀=21.19 μg/ml) and α-Glycosidase (IC₅₀: 70.00 μg/ml), methanol (AM) for BChE (IC₅₀=17.33 μg/ml), CA−I and II (IC₅₀=79.65 and 36.09 μg/ml, respectively) showed the most potent inhibition effect. The content analysis of acetone extract was performed with LC/MS-MS, the first three phytochemicals found most were p-Coumaric acid, rutin, and 4-hydroxybenzoic acid (284.29±3.97, 135.39±8.19, and 102.06±5.51 μg analyte/g extract, respectively).     

Antioxidant activities of cultured <Emphasis Type="Italic">Armillariella mellea</Emphasis>

This study aimed to evaluate the antioxidant activities of a cultured medicinal fungus—Armillariella mellea (Vahl. ex Fr.) Karst. (AM). Three antioxidant assay systems, namely cytochrome c, xanthine oxidase inhibition, and FeCl₂-ascorbic acid stimulated lipid peroxidation in rat tissue homogenate tests, were used. Total flavonoid and phenol contents of AM extracts were also analyzed. Results showed that both aqueous (AM-H₂O) and ethanolic (AM-EtOH) extracts of solid state cultured AM showed antioxidant activities in a concentration-dependent manner. At concentrations 1–100 μg/ml, the free radical scavenging activity was 73.7–92.1% for AM-H₂O, and 60.0–90.8% for AM-EtOH. These extracts also showed an inhibitory effect on xanthine oxidase activity, but with a lesser potency (IC₅₀ is 9.17 μg/ml for AM-H₂O and 7.48 μg/ml for AM-EtOH). In general, AM-H₂O showed a stronger antilipid peroxidation activity on different rat’s tissues than AM-EtOH. However, both AM extracts displayed a weak inhibitory effect on lipid peroxidation in plasma. Interestingly, the antilipid peroxidation activity of AM-H₂O (IC₅₀–6.66 μg/ml) in brain homogenate was as good as IC₅₀–5.42 μg/ml. AM-H₂O (80.0 mg/g) possessed a significantly higher concentration of total flavonoids than AM-EtOH (30.0 mg/g), whereas no difference was noted in the total phenol content between these two extracts. These results conclude that AM extracts possess potent free radical scavenging and antilipid peroxidation activities, especially the AM-H₂O in the brain homogenate. Published in Russian in Prikladnaya Biokhimiya i Mikrobiologiya, 2007, Vol. 43, No. 4, pp. 495–500. The text was submitted by the authors in English.     

Antimicrobial activity and mechanism of action of Nu-3, a protonated modified nucleotide

For centuries, plants have been used in traditional medicines and there has been recent interest in the chemopreventive properties of compounds derived from plants. In the present study, we investigated the antibutyrylcholinestrasic (anti-BuChE) and antioxidant (against some free radicals) activities of extracts from Rhus pentaphyllum. Aqueous extracts were prepared from powdered R. pentaphyllum roots, leaves and seeds and characterized for the presence of tannins, flavonoids and coumarins. Seeds aqueous extract contained the highest quantities of both flavonoids and tannins (21.12% and 17.45% respectively). In the same way, seeds extracts displayed remarkable inhibition against BuChE over 95%, at 100 μg/ml and with IC₅₀ 0.74 μg/ml. In addition, compared to leaves and roots extracts, seeds aqueous extract revealed relatively strong antiradical activity towards the ABTS ^.+ (IC₅₀ = 0.25 μg/ml) and DPPH (IC₅₀ = 2.71 μg/ml) free radicals and decreased significantly the reactive oxygen species such O₂ ^.- (IC₅₀ = 2.9 μg/ml) formation evaluated by the non-enzymatic generating O₂ ^.- system (Nitroblue tetrazolium/riboflavine). These data suggest that the anti-BuChE activities mechanism of these extracts occurs through a free radical scavenging capacities. The present study indicates that extracts of Rhus pentaphyllum leaves, seeds and roots are a significant source of compounds, such as tannins, flavonoids and coumarins, with anti-BuChE and antioxidant activities, and thus may be useful for chemoprevention.     

Barks of Three Wild Pyrus Taxa: Phenolic Constituents,Antioxidant Activity,and in Vitro and in Silico Investigations of α-Amylase and α-Glucosidase Inhibition

Dry MeOH extracts of the twig barks of Pyrus communis subsp. pyraster, P. spinosa and their hybrid P.×jordanovii nothosubsp. velenovskyi, collected in wild in Serbia, were analyzed. By LC/MS, the contents of arbutin (99.9–131.0 mg/g), chlorogenic acid (2.2–6.3 mg/g), catechin (1.0–5.3 mg/g) and total dimeric and trimeric procyanidins (42.2–61.3 mg/g), including procyanidin B2 (8.9–17.2 mg/g), were determined. Colorimetrically, high contents of total phenolics (436.2–533.4 mg GAE/g) and tannins (339.4–425.7 mg GAE/g), as well as strong total antioxidant activities (FRAP values 4.5–5.9 mmol Fe²⁺/g), and DPPH (SC₅₀=6.6–7.1 μg/ml) and hydroxyl radical (SC₅₀=447.1–727.7 μg/ml) scavenging abilities were revealed. In vitro, all extracts exhibited notable inhibition of α-amylase (IC₅₀=310.8–617.7 μg/ml) and particularly strong inhibition of α-glucosidase (IC₅₀=2.1–3.7 μg/ml). Molecular docking predicted that among identified compounds procyanidin B2 is the best inhibitor of these carbohydrate-digesting enzymes. Obtained results showed that the barks of investigated Pyrus hybrid and its parent taxa have similar composition and bioactivity.     

LC-ESI-MS/MS Chemical Characterization,Antioxidant and Antidiabetic Properties of Propolis Extracted with Organic Solvents from Eastern Anatolia Region

Geographic conditions (altitude, climate, and local flora) lead to significant differences in the chemical composition of propolis. Therefore, more research is needed for propolis in different geographical regions. So, the aim of this study was to evaluate the phenolic profile, total phenolic content, antioxidant, and antidiabetic properties of Pülümür propolis from Turkey. Methanol (MeOH), chloroform (CHCl₃), and hexane extracts of propolis were analyzed. LC-ESI-MS/MS analysis of the extracts showed that the most abundant phenolic compound is caffeic acid in the MeOH extract (2943.12±11.12 μg phenolics/g extract), while on the other hand, CHCl₃ extract had the highest total phenolic content (125.75±1.02 mg GAE/g extract). Antioxidant activity was measured using ABTS and DPPH assays, whereas CHCl₃ extract (IC₅₀=6.35±0.11 and 28.84±0.10 μg/mL, respectively) and MeOH extracts (IC₅₀=5.04±0.07 and 28.80±0.09 μg/mL, respectively) showed relatively high antioxidant activity. The MeOH extract showed better antidiabetic activity than the standard compound, acarbose (IC₅₀=0.544 and 0.805 mg/mL, respectively).     

Biological activity in extracts of ascidians (Tunicata, Ascidiacea) from the northeastern Brazilian coast

Ascidians are marine animals with a great ability to synthesize bioactive substances. This study examined the cytotoxic potential of 10 ascidians found in the coastal waters of Northeast Brazil. Samples of the species Eudistoma vannamei Millar, 1977, Eudistoma sp., Didemnum ligulum Monniot F., 1983, Didemnum psammatodes (Sluiter, 1895), Didemnum sp., Polysyncraton sp., Trididemnum sp., Cystodytes dellechiajei (Della Valle, 1877), Euherdmania sp., and an unidentified species belonging to the Holozoidae family were extracted in methanol 5:1 (v/w). The extracts were tested for cytotoxicity using the brine shrimp lethality assay, sea urchin egg development assay, hemolysis assay, and MTT assay using tumor cell lines. The extract of E. vannamei showed the highest toxicity in brine shrimp (LD₅₀=34.7 μg/ml) and in all tumor cell lines tested, with an IC₅₀ of <2 μg/ml for CEM, 11.2 μg/ml for HL-60, 23.8 μg/ml for B16, and 14.3 μg/ml for HCT-8. In sea urchin eggs, it inhibited the cell cycle progression mainly at the blastula stage (IC₅₀=74.8 μg/ml). The extract of Euherdmania sp. also exhibited some toxicity in these assays, but at a lower potency than that of E. vannamei. The extracts of D. psammatodes and Polysyncraton sp. showed a strong inhibition of the sea urchin egg cell cycle during both phases examined, first cleavage and blastula, with a possible action on the cell microfilament apparatus. The extract of D. ligulum showed selective toxicity toward HCT-8 cells (IC₅₀=35.3 μg/ml). The extract from the Holozoidae was the only one that possessed a hemolytic effect, with an IC₅₀ of 175.2 μg/ml. Further studies are necessary for a better characterization of the active principles of these extracts and a possible elucidation of the mechanisms of action.     

Evaluation of the bioactivities of extracts of endophytes isolated from Taiwanese herbal plants

The endophytic extracts from 19 endophytes, isolated from 13 species of Taiwanese plants, were evaluated for biological activity, including cytotoxicity, anti-platelet aggregation, and anti-inflammatory activity. The extracts of 12 endophytes exhibited inhibitory effects on collagen-induced platelet aggregation with IC₅₀ values of 19.85–87.64 μg/ml. Four strains, Rahnella aquatilis, Pantoea agglomerans, Rhodotorula sp., and Penicillium paxilli, also showed inhibitory effects on thrombin-induced platelet aggregation with IC₅₀ values of 42.80–61.54 μg/ml. Additionally 12 extracts of endophytes exhibited cytotoxicities with IC₅₀ values of 0.12–19.83 μg/ml. However, eight extracts revealed inhibitory effects on superoxide anion generation induced by fMLP (N-formyl-l-methionyl-l-leucyl-l-phenylalanine) in human neutrophils. The extract of Rahnella aquatilis showed anti-platelet aggregation activity, and bioassay-directed fractionation led to the isolation of six compounds, including one isoalloxazine: lumichrome (1); two isoflavones: genistein (2) and daidzein (3); two cyclic peptides: cyclo-Pro-Val (4) and cyclo-Pro-Phe (5); and one benzenoid: methyl 2,4,5-trimethoxybenzoate (6). These results indicated that endophytes from Taiwanese herbal plants could be useful sources for research and development of bioactive lead compounds from nature.     

Phytochemical Screening,Antioxidant Assay and Cytotoxic Profile for Different Extracts of Chrysopogon zizanioides Roots

The Chrysopogon zizanioides plant possesses multiple traditional uses, especially in therapeutics, but only a few articles have reported its biological activity. Hence, the present study was planned to explore the phytochemical constituents, cytotoxic potential, radical scavenging activity, and GC/MS (Gas chromatography & Mass spectrometry) analysis of the vetiver root extracts. The roots extracted with different solvents exhibited more significant phytochemical constituents in polar solvents in comparison to non-polar ones, favoring the extraction of a greater number of components in highly polar solvents. All the extracts were tested for their cytotoxicity using SRB (Sulforhodamine B) assay. They confirmed ethanolic extract as a potent extract with GI₅₀ 56±0.5 μg/ml in oral cancer (SCC-29B) along with no cytotoxicity in healthy cells (Vero cells), making it a safer therapeutic option in comparison to standard Adriamycin. This extract was also analyzed for its antioxidant potential by DPPH (1,1-Diphenyl-2-picrylhydrazyl) assay with IC₅₀ value 10.73 μg/ml, which was quite comparable to Ascorbic acid having IC₅₀ value 4.61 μg/ml. The quantitative analysis of ethanolic extract exhibited 107 compounds amongst which Khusenic acid, Ascorbic acid, Junipen, gamma-Himachalene, alpha-Guaiene were the majorly occurring compounds that can be explored further for their cytotoxic activity.     

Biological activities of the essential oils and methanol extract of tow cultivated mint species (<Emphasis Type="Italic">Mentha longifolia</Emphasis> and <Emphasis Type="Italic">Mentha pulegium</Emphasis>) used in the Tunisian folkloric medicine

The composition of the essential oils and methanolic extracts of two cultivated mint species (M. longifolia and M. pulegium), as well as the in vitro antimicrobial and antioxidant activities of the essential oil and methanol extract of Mentha longifolia and Mentha pulegium were compared. GC-MS analysis of the essential oil identified 41 compounds constituting 96.66 and 96.13% of the total oil from M. longifolia and M. pulegium, respectively. The later oils were rich on pulegone (47.15 and 61.11%, respectively). Moreover, 1,8 cineole (11.54%), menthone (10.7%), α-pinene (3.57%), α-terpineol (3.17%) and d-cadinene (3.53%) were only present in M. longifolia oil, while isomenthone (17.02%), and piperitone (2.63%), were characteristic of M. pulegium oil. Shoot extract of the two species showed significantly different contents in total polyphenols (89.1 and 37.41 mg GAE/g DW), flavonoids (63.93 and 33.83 mg CE/g DW) and tannins (1.47 and 3.07 mg CE/g DW), respectively in M. longifolia and M. pulegium. The essential oils showed strong antimicrobial activity against all 16 microorganisms tested, whereas the methanol extracts were inactive. Moreover, the essential oils showed higher antioxidant activity than the methanolic extracts against the DPPH and superoxide radical scavenging. In fact, antioxidant activities of the oils were the same for both M. longifolia and M. pulegium against DPPH (IC₅₀ = 9 and 10 μg/ml, respectively) and 2-fold and 4-fold higher than shoot extracts (IC₅₀ = 20 and 48 μg/ml, respectively). Moreover, both oils showed the same antioxidative abilities as compared to the positive control (butylated hydroxytoluene). In the same way, the capacity to inhibit superoxide anion was very significant for the two oils (0.1 μg/ml for M. longifolia and 0.11 μg/ml for M. pulegium).     

Isolation and characterization of dihydromonacolin-MV from <Emphasis Type="Italic">Monascus purpureus</Emphasis> for antioxidant properties

The methanolic extract of Monascus purpureus cultivated by solid-state fermentation on rice showed strong 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity and better yield as compared to other polarity based extracted fractions. It was selected for further purification of the antioxidant. The activity-guided repeated fractionation of methanolic extract on a silica gel column chromatography yielded a compound that exhibited strong antioxidant activity. Based on the spectroscopic analysis by UV, IR, ¹H NMR, ¹³C NMR, 2D-HSQCT NMR, and MS, the antioxidant isolated was elucidated as a derivative of dihydromonacolin-K, where the ester group is 2-methyl propionate, designated as dihydromonacolin-MV. The DPPH radical was significantly scavenged by the dihydromonacolin-MV (IC₅₀ 20±1 μg ml⁻¹). The dihydromonacolin-MV showed strong inhibition of lipid peroxidation in a liposome model with an IC₅₀ value of 5.71±0.38 μg ml⁻¹ and superoxide radical scavenging activity with an IC₅₀ value of 163.97±2.68 μg ml⁻¹.     

Polyphenolic Content and Physiological Activities of Chinese Hawthorn Extracts

Hawthorn polyphenol (HP) was prepared by ethyl acetate treatment of the ethanol extract (HE) of Chinese hawthorn fruit. The concentrations of 15 polyphenols in the HP, HE, extraction residue (HJ), and a hawthorn leaf extract (HF) were determined by HPLC. For HP, the total content of the 15 polyphenols was 21.4%, comprised of 19.7% of procyanidins, 1.21% of chlorogenic acid, and 0.48% of flavonoids, compared to 2.55% for the HE. The yields of procyanidin monomer, dimer, trimer, tetramer, and pentamer were 50.5%, 30.3%, 23.0%, 14.6%, and 12.5% respectively, and the mean degree of polymerization was reduced to 1.39 (HP) from 1.65 (HE). Seven different physiological actions of the four extracts were investigated. The HP showed strong O₂ ^? and ^?OH scavenging capacities (IC₅₀ values of 6.3 μg/ml and 1.1 μg/ml respectively), as well as selective prolyl endopeptidase inhibition (IC₅₀ of 60 μg/ml). The active constituents appeared to be procyanidins.     

<Emphasis Type="Italic">In vivo</Emphasis> and <Emphasis Type="Italic">in vitro</Emphasis> antioxidant effects of three Veronica species

The aim of the present study was to examine the antioxidant activity of three Veronica species (Plantaginaceae). The antioxidant potential of various extracts obtained from aerial flowering parts was evaluated by DPPH-free (1,1-diphenyl-2-picrylhydrazyl-free) radical scavenging activity and ferric-reducing antioxidant power assays. Considerable antioxidant activity was observed in the plant samples (FRAP values ranged from 0.97 to 4.85 mmol Fe²⁺/g, and DPPH IC₅₀ values from 12.58 to 66.34 μg/ml); however, these levels were lower than the activity of the control compound butylated hydroxytoluene (BHT) (FRAP: 10.58 mmol Fe²⁺/g; DPPH IC₅₀: 9.57 μg/ml). Also, the in vivo antioxidant effects were evaluated in several hepatic antioxidant systems in rats (activities of glutathione peroxidase, glutathione reductase, peroxidase, catalase, xanthine oxidase, glutathione content and level of thiobarbituric acid reactive substances) after treatment with different Veronica extracts, or in combination with carbon tetrachloride (CCl₄). Pretreatment with 100 mg/kg b.w. of Veronica extracts inhibited CCl₄-induced liver injury by decreasing TBA-RS level, increasing GSH content, and bringing the activities of CAT and Px to control levels. The present study suggests that the extracts analyzed could protect the liver cells from CCl₄-induced liver damage by their antioxidative effect on hepatocytes.     

Interaction of benzo[c]phenanthridine and protoberberine alkaloids with animal and yeast cells

We compared the effects of four quaternary benzo[c]phenanthridine alkaloids – chelerythrine, chelilutine, sanguinarine, and sanguilutine – and two quaternary protoberberine alkaloids – berberine and coptisine – on the human cell line HeLa (cervix carcinoma cells) and the yeastsSaccharomyces cerevisiae andSchizosaccharomyces japonicus var. versatilis. The ability of alkaloids to display primary fluorescence, allowed us to record their dynamics and localization in cells. Cytotoxic, anti-microtubular, and anti-actin effects in living cells were studied. In the yeasts, neither microtubules nor cell growth was seriously affected even at the alkaloid concentration of 100 μg/ml. The HeLa cells, however, responded to the toxic effect of alkaloids at concentrations ranging from 1 to 50 μg/ml. IC₅₀ values for individual alkaloids were: sanguinarine IC₅₀ = 0.8 μg/ml, sanguilutine IC₅₀ = 8.3 μg/ml, chelerythrine IC₅₀ = 6.2 μg/ml, chelilutine IC₅₀ = 5.2 μg/ml, coptisine IC₅₀ = 2.6 μg/ml and berberine IC₅₀ >10.0 μg/ml. In living cells, sanguinarine produced a decrease in microtubule numbers, particularly at the cell periphery, at a concentration of 0.1 μg/ml. The other alkaloids showed a similar effect but at higher concentrations (5–50 μg/ml). The strongest effects of sanguinarine were explained as a consequence of its easy penetration through the cell membrane owing to nonpolar pseudobase formation and to a high degree of molecular planarity. This revised version was published online in July 2006 with corrections to the Cover Date.     

Anti-Inflammatory,Antioxidant and Enzyme Inhibition Activities in Correlation with Mycochemical Profile of Selected Indigenous Ganoderma spp. from Balkan Region (Serbia)

The aim of this research work was to study the bioactivity potentials (antioxidant, anti-inflammatory, and enzyme inhibitory) of ethanol (EtOH), water (H₂O) and chloroform (CHCl₃) extracts of G. applanatum, G. lucidum, G. pfeifferi and G. resinaceum as well as their mycochemical profile: the total content of phenolics (TP) and sugars (TS) and LC/MS/MS detection of phenolics. LC/MS/MS profile showed that p-hydroxybenzoic and protocatechuic acids were mostly found. The highest ABTS and DPPH activities were detected in polar G. applanatum extracts (159.84±0.59 mg TE/g d.w., IC₅₀=0.85±0.30 μg/mL, respectively), while G. resinaceum CHCl₃ extract was the most potent in NO assay (IC₅₀=41.21±0.18−81.89±0.81 μg/mL). The highest TP and TS were generally determined in G. applanatum EtOH extracts. Enzyme inhibitory effects were determined in H₂O extracts. Generally, CHCl₃ extracts showed the most powerful anti-inflammatory potential. These results suggest that analyzed species are a promising source of bioactive compounds and may be considered as candidates for new food supplements or drug formulations.     

A Comprehensive Search of the Primary and Secondary Metabolites and Radical Scavenging Potential of Trillium govanianum Wall. ex D. Don

Trillium govanianum rhizomes are traditionally consumed as a raw powder and decoction for the treatment of health complications. Hence, the present study aimed to investigate whether aqueous and alcoholic extracts of T. govanianum rhizomes under hot and cold extraction conditions have similar or dissimilar chemical, nutrient, and antioxidant profiles. The total phenolics, flavonoids, carbohydrates, proteins, fats, and energy values were estimated in all the conditionally prepared samples. The total phenolics (21.23±1.4 mg GAE/g extract), flavonoids (70.57±3.24 mg RE/g extract) were found higher in hot ethanolic extract (TGHEt), while cold water extract (TGGC) showed higher nutrients including amino acids (10.545±0.219 mg/g) and nucleosides (1.803±0.018 mg/g). The nutrient energy value (2.60 and 2.49 Kcal/g extract) was higher in cold and hot ethanolic extracts. Further, TGHEt scavenged the DPPH^. (IC₅₀; 870±22 μg/mL) and ABTS^.+ (IC₅₀; 80±1.49 μg/mL) effectively and proved its highest antioxidant activity compared to other samples. In LC/MS/MS-based metabolite profiling, twenty-six metabolites (fatty acids, steroidal saponins, triterpene saponins, ecdysteroid hormones) were confirmed with mass fragmentation and literature, while one hundred nine metabolites were identified using the METLIN database. The principal component analysis showed clustering of hot condition extracts while cold extracts were differentially located in quadrants. The heatmaps exhibited the associations and differences between metabolite composition, solvents, and extraction conditions. The identified metabolites speculatively predicted the biosynthesis pathway of T. govanianum. Findings also illustrated that T. govanianum is a source of bioactive nutritional components and saponins. The current metabolite profiling of T. govanianum will help in its agricultural and biotechnological interventions for higher quality produce.     

Bioactive 3,8‐Epoxy Iridoids from Valeriana jatamansi

Twelve 3,8‐epoxy iridoids, including four new compounds, jatamanins R–U ( 1 – 4 ), and eight known compounds ( 5 – 12 ), were obtained from the roots and rhizomes of Valeriana jatamansi. The structures were elucidated from analysis of spectroscopic data. The absolute configurations of 1 – 4 were determined by comparison of experimental and literature ECD spectra. Moreover, the compounds were evaluated for cytotoxic effects against glioma stem cells, inhibition of NO production, activity against influenza A virus and reversal of multidrug resistance of HepG2/ADR cells. Compounds 9 and 12 showed significant cytotoxic potency against GSC‐18# (IC₅₀=1.351 and 4.439 μg ml^?1, respectively) and GSC‐3# (IC₅₀=10.88 and 6.348 μg ml^?1, respectively) glioma stem cells, while compound 12 was also slightly less potent against GSC‐12# (IC₅₀=13.45 μg ml^?1) glioma stem cell growth. In addition, compounds 9 and 12 displayed obvious inhibition of NO production (IC₅₀=4.6 and 15.8 μm , respectively).     

The in vitro anti-platelet,antioxidant and cellular immunity activity of <Emphasis Type="Italic">Phellinus gilvus</Emphasis> fractional extracts

The in vitro anti-platelet and antioxidant activities of various solvent extracts from Phellinus gilvus (PG), and the effects of hot water extract from PG (PGW) on murine cellular immunity were investigated. Chloroform extract (CE), methanol extract (ME) and butanol extract (BE) from PG could significantly inhibit platelet aggregation induced by thrombin. Ethyl acetate extract (EAE), BE, ME from PG had significant 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity compared with the control, and the EAE showed the highest effect with IC₅₀ values of 13.34 μg/ml, which is higher than that of ascorbic acid (40 μg/ml). In addition, EAE displayed the inhibition of xanthine oxidase (XO) activity with IC₅₀ value of 2.45 μg/ml. As to the cellular immunity activity, PGW could enhance both the lipopolysaccharide (LPS)-induced B lymphocyte proliferation and concanavalin A (Con A)-induced T lymphocyte proliferation in vitro. The phagocytosis of both peritoneal macrophages and RAW264.7 macrophage cells were also increased by the addition of PGW. Moreover, PGW was found to inhibit the nitric oxide (NO) production of RAW264.7 macrophages induced by LPS in a concentration-dependant manner.     

Antiplasmodial and cytotoxicity activities of some selected plants used by the Maasai community, Kenya

Malaria has continued to be a major global public health problem and a health concern in most of African countries. An estimated 350–500 million cases of malaria each year result in about one million deaths, mainly children under five. The rate of malaria infection is increasing rapidly partly due to drug resistance by the Plasmodium falciparum. The cost of the current drugs is prohibitive to the poor. There is therefore urgent need to identify new antimalarial agents that are effective, safe and affordable. In our continuous search for these new antimalarial compounds, extracts from five medicinal plants from the Maasai community in Kenya were tested against P. falciparum (D6; chloroquine sensitive and W2; chloroquine resistant strains). Of the tested total plant extracts, 5 crude extracts showed good antiplasmodial activity against D6 strain of P. falciparum with IC₅₀ values lower or equal to 14.3 μg/ml, 2 were moderately active with IC₅₀ values in between 26.6 and < 50 μg/ml. The petroleum ether extracts of the aerial parts and roots of Fuerstia africana demonstrated high antiplasmodial activity against the chloroquine sensitive antiplasmodial strain D6 (IC₅₀ 1.5 and 4.6 μg/ml, respectively with a selectivity index of 44 against vero cells). Manilkara discolor also exhibited promising antiplasmodial activity especially against D6 (IC₅₀ 11.5 and 26.6 μg/ml). In addition, ethyl acetate extract of the roots of Pentas lanceolata and the aerial parts of Sericocomopsis hildebrandtii demonstrated moderate antiplasmodial activity against D6 and W2 (IC₅₀ 14.3 and 16.51 μg/ml) respectively. F. africana therefore has high potential and can be pursued for the development of an antimalarial drug.     

Polyphenol Characterization,Antioxidant and Skin Whitening Properties of Alnus cordata Stem Bark

In this study, we investigated the phenolic composition of the crude extract (MeOH 80 %) of Alnus cordata (Loisel .) Duby stem bark (ACE) and its antioxidant and skin whitening properties. RP‐LC‐DAD analysis showed a high content of hydroxycinnamic acids (47.64 %), flavanones (26.74 %) and diarylheptanoids (17.69 %). Furthermore, ACE exhibited a dose‐dependent antioxidant and free‐radical scavenging activity, expressed as half‐maximal inhibitory concentration (IC₅₀): Oxygen radical absorbance capacity (ORAC, IC₅₀ 1.78 μg mL^?1)>Trolox equivalent antioxidant capacity (TEAC, IC₅₀ 3.47 μg mL^?1)>2,2‐Diphenyl‐1‐picrylhydrazyl (DPPH, IC₅₀ 5.83 μg mL^?1)>β‐carotene bleaching (IC₅₀ 11.58 μg mL^?1)>Ferric reducing antioxidant power (FRAP, IC₅₀ 17.28 μg mL^?1). Moreover, ACE was able to inhibit in vitro tyrosinase activity (IC₅₀ 77.44 μg mL^?1), l ‐DOPA auto‐oxidation (IC₅₀ 39.58 μg mL^?1) and in an in vivo model it exhibited bleaching effects on the pigmentation of zebrafish embryos (72 h post fertilization) without affecting their development and survival. In conclusion, results show that A. cordata stem bark may be considered a potential source of agents for the treatment of skin disorders due to its bleaching properties and favorable safety profiles, associated to a good antioxidant power.     

Endophytic fungi with anti-microbial,anti-cancer and anti-malarial activities isolated from Thai medicinal plants

A total of 81 Thai medicinal plant species collected from forests in four geographical regions of Thailand were examined for the presence of endophytic fungi with biological activity. Of 582 pure isolates obtained, 360 morphologically distinct fungi were selected for cultivation on malt Czapek broth and yeast extract sucrose broth, from which extracts were tested for biological activity. Extracts of 92 isolates could inhibit Mycobacterium tuberculosis (MIC 0.0625–200 μg ml⁻¹) when tested by the microplate Alamar blue assay, while extracts of six inhibited Plasmodium falciparum (IC₅₀ of 1.2–9.1 μg ml⁻¹) as determined by the [³H]hypoxanthine incorporation method. Strong anti-viral activity against Herpes simplex virus type 1 was observed in 40 isolates (IC₅₀ of 0.28–50 μg ml⁻¹). The sulphorhodamine B assay for activity against cancer cell lines revealed that 60 were active against human oral epidermoid carcinoma cells (EC₅₀ 0.42–20 μg ml⁻¹) and 48 against breast cancer cells (EC₅₀ 0.18–20 μg ml⁻¹). Bioactivity profile was affected by the type of culture medium. Given the high incidence of bioactive extracts and the fact that most of the isolated fungi could not be identified due to lack of spore formation, the results suggested that Thai medicinal plants can provide a wide variety of endophytes that might be a potential source of novel bioactive compounds. This revised version was published online in August 2006 with corrections to the Cover Date.