Anti-ophidian activity of Bredemeyera floribunda Willd. (Polygalaceae) root extract on the local effects induced by Bothrops jararacussu venom

Bredemeyera floribunda roots are popularly used to treat snakebites in the semiarid region of Northeast Brazil, and previous studies indicate the anti-ophidian actions of triterpenoid saponins found in its roots. To assess B. floribunda root extract (BFRE) activity against the effects of Bothrops jararacussu venom (BjuV), antiphospholipasic, antiproteolytic, antihemorrhagic, antinecrotic, and anti-edematogenic activities were investigated in mice. Phytochemical analysis revealed the presence of saponins, flavonoids, and sugars, with rutin and saccharose being the major constituents of BFRE. Acute toxicity was determined and BFRE was nontoxic to mice. Phospholipase A2 and proteolytic activities induced by BjuV were inhibited in vitro by BFRE at all concentrations tested herein. BFRE (150 mg/kg) inhibited paw edema induced by BjuV (50 µg/animal), reducing total edema calculated by area under the curve, but carrageenan-induced paw edema was unchanged. Hemorrhagic and necrotizing actions of BjuV (50 µg/animal) were considerably decreased by BFRE treatment. Thus, BFRE blocked the toxic actions of B. jararacussu venom despite having no anti-inflammatory activity, which points to a direct inhibition of venom's toxins, as demonstrated in the in vitro assays. The larger amounts of rutin found in BFRE may play a role in this inhibition, since 3′,4′-OH flavonoids are known inhibitors of phospholipases A2.

Anti-ophidian activity of Bredemeyera floribunda Willd. (Polygalaceae) root extract on the local effects induced by Bothrops jararacussu venom.

Bredemeyera floribunda roots are popularly used to treat snakebites in the semiarid region of Northeast Brazil, and previous studies indicate the anti-ophidian actions of triterpenoid saponins found in its roots. To assess B. floribunda root extract (BFRE) activity against the effects of Bothrops jararacussu venom (BjuV), antiphospholipasic, antiproteolytic, antihemorrhagic, antinecrotic, and anti-edematogenic activities were investigated in mice. Phytochemical analysis revealed the presence of saponins, flavonoids, and sugars, with rutin and saccharose being the major constituents of BFRE. Acute toxicity was determined and BFRE was nontoxic to mice. Phospholipase A2 and proteolytic activities induced by BjuV were inhibited in vitro by BFRE at all concentrations tested herein. BFRE (150 mg/kg) inhibited paw edema induced by BjuV (50 µg/animal), reducing total edema calculated by area under the curve, but carrageenan-induced paw edema was unchanged. Hemorrhagic and necrotizing actions of BjuV (50 µg/animal) were considerably decreased by BFRE treatment. Thus, BFRE blocked the toxic actions of B. jararacussu venom despite having no anti-inflammatory activity, which points to a direct inhibition of venom's toxins, as demonstrated in the in vitro assays. The larger amounts of rutin found in BFRE may play a role in this inhibition, since 3',4'-OH flavonoids are known inhibitors of phospholipases A2.

Asemeia ovata (Polygalaceae): Quantitative determination and evaluation in silico of identified substances by HPLC-DAD.

BACKGROUND: In Brazil, the Asemeia genus has 19 species (12 endemic) and 2 varieties (both endemic) and some of them are found in semi-arid Bahia. OBJECTIVE: The objective of this study was to quantitatively determine identified substances by HPLC-DAD in Asemeia ovata extracts and to predict their biological activities in silico. METHOD: The quantification method by HPLC-DAD has been validated according to the guidelines of the International Conference of Harmonization. The prediction in silico activities was made by Target Fishing methods (TF), followed by docking by the program DOCK 6.7 and assessment of interaction profiles for Protein-Ligand Interaction Profiler server. RESULTS: It was possible to identify and quantify using HPLC-DAD substances: rutin, luteolin-7-O-glucoside, caffeic acid, p-coumaric acid and trans-ferulic acid. The ChemProt 2.0 server was selected for TF method, which has shown potential activity of compounds on molecular targets such as Carbonic anhydrase 12, epidermal growth factor receptor and sodium-glucose cotransporter 2. CONCLUSION: This work provides new results for the species both from a biological and chemical point of view, and has interesting potential to be discovered with the prospect of further studies.

Anti-acetylcholinesterase activity and antioxidant properties of extracts and fractions of Carpolobia lutea.

CONTEXT: There is an unmet need to discover new treatments for Alzheimer's disease. This study determined the anti-acetylcholinesterase (AChE) activity, DPPH free radical scavenging and antioxidant properties of Carpolobia lutea G. Don (Polygalaceae). OBJECTIVE: The objective of this study is to quantify C. lutea anti-AChE, DPPH free radical scavenging, and antioxidant activities and cell cytotoxicity. MATERIALS AND METHODS: Plant stem, leaves and roots were subjected to sequential solvent extractions, and screened for anti-AChE activity across a concentration range of 0.02-200 µg/mL. Plant DPPH radical scavenging activity, reducing power, and total phenolic and flavonoid contents were determined, and cytotoxicity evaluated using human hepatocytes. RESULTS: Carpolobia lutea exhibited concentration-dependent anti-AChE activity. The most potent inhibitory activity for the stem was the crude ethanol extract and hexane stem fraction oil (IC50 = 140 µg/mL); for the leaves, the chloroform leaf fraction (IC50 = 60 µg/mL); and for roots, the methanol, ethyl acetate and aqueous root fractions (IC50 = 0.3-3 µg/mL). Dose-dependent free radical scavenging activity and reducing power were observed with increasing stem, leaf or root concentration. Total phenolic contents were the highest in the stem: ∼632 mg gallic acid equivalents/g for a hexane stem fraction oil. Total flavonoid content was the highest in the leaves: ∼297 mg quercetin equivalents/g for a chloroform leaf fraction. At 1 µg/mL, only the crude ethanol extract oil was significantly cytotoxic to hepatocytes. DISCUSSION AND CONCLUSIONS: Carpolobia lutea possesses anti-AChE activity and beneficial antioxidant capacity indicative of its potential development as a treatment of Alzheimer's and other diseases characterized by a cholinergic deficit.

Carpolobia lutea G. Don (Polygalaceae) Inhibits Inflammation and Oxidative Stress in an Acetic Acid Induced Model of Rat Colitis.

Carpolobia lutea G. Don (CL) is used in folk medicine for the treatment of inflammatory disorders. Effort in this study is to evaluate the beneficial effect of the aqueous-methanol extract of leaf of CL in a rat model of acetic acid induced colitis. Male Wistar rats were distributed into 6 groups of 7 rats each; non colitic, untreated colitic and colitic rats treated with graded doses of CL (100-800 mg/kg). Rats were pre-treated for 2 days before colitis induction and thereafter for 7 days post colitic induction. 24 h after the last treatment, animals were sacrificed and colonic inflammation was evaluated both macroscopically and biochemically. Macroscopic damage score, weight/length ratio, myeloperoxidase (MPO) activity and tumor necrotic factor alpha (TNF-α) levels, were significantly higher in untreated colitic rats in comparison with non colitic rats (P<0.05). Treatment with CL significantly reduced the macroscopic damage scores, neutrophil infiltration (MPO activity) and TNF-α level (P<0.05). In addition, C. lutea significantly prevented depletion of colonic GSH and (SOD) levels (P<0.05). It appears that the beneficial effect of methanol extract of C. lutea leaf observed in this study is dose dependent and is related to its antioxidant and anti-inflammatory activity.

Antidiarrheal mechanism and ionic profile of Carpolobia lutea ethanolic stem-bark extract in rats.

BACKGROUND: The stem-bark extract of Carpolobia lutea (Polygalaceae), used in ethno-medicine as anti-diarrhea was pharmacologically evaluated. This was the first report of assessment of the ethanolic stem extract (ESE), of C. lutea as anti-diarrhoeal agent in rats. The anti-diarrhoeal effects, acute toxicity and ionic profile are investigated and reported. MATERIALS AND METHODS: The acute toxicity was established using Lock's method. The anti-diarrhoeal effects were demonstrated using castor oil-induced diarrheal and fluid accumulation and its effect on normal intestinal transit. The mechanism elucidated using yohimbine, isosorbide dinitrate, and diphenoxylate. The elemental and ionic profile of ESE was established using inductively coupled argon-plasma emission spectrometer and potentiometric titration respectively. The finger print of ESE was revealed by Jasco (Tokyo, Japan), HPLC and active compounds by phytochemical screening using standard procedure. RESULTS: The LD50 obtained is 866.025 mg/kg (i.p). The doses of 43.3, 86.6, and 173.2 mg/kg of ESE showed inhibition of castor oil-induced diarrheal (p<0.05 -0.001). The most abundant cations in the extract are potassium and phosphorus (1.00 ±0.01 and 0.80 ± 0.030 mg/g respectively); while the most abundant anions are phosphate and sulphate (33.50±7.09 and 7.19±3.29 mg/g respectively). The HPLC fingerprint of ESE revealed UV spectra of biomolecules. Phytochemical screening revealed presence of saponins, polyphenols and glycosides. CONCLUSION: These investigations indicate presence of bioactive and elemental substances which could play major role in diarrheal management. This investigation justifies the use of stem-bark of C. lutea in illicit gin (akpatashi), among the Effiks in Nigeria as antidiarrheal.

Xanthones from the roots of Moutabea guianensis Aubl.

The phytochemical investigation of Moutabea guianensis roots led to the isolation of five polyoxygenated xanthones, including two new ones named moutabeone B (1,8-dihydroxy-4,5,6,7-tetramethoxyxanthone) and moutabeone C (1-hydroxy-4,5,6,7,8-pentamethoxyxanthone), along with the three known xanthones, 1,8-dihydroxy-4,6-dimethoxyxanthone, 1,8-dihydroxy-4,5,6-trimethoxyxanthone and augustin A (1,8-dihydroxy-4,6,7-trimethoxyxanthone). Structural characterization of all compounds was established on the basis of spectroscopic methods, mainly 1D and 2D nuclear magnetic resonance (NMR) and comparison with literature data. The antioxidant activity of compounds was tested through a thin layer chromatography (TLC) bioautography assay using 1,1-diphenyl-2-picryl-hydrazyl radical (DPPH·) as detection reagent. All tested compounds were more active (DL < 0.13-0.03 µg) than Trolox (DL < 0.15 µg), used as reference standard.

Two new diphenylmethyl-substituted xanthones from Seicuridaca longepedunculata.

Two new diphenylmethyl-substituted xanthones, named muchimangins K (1) and L (2), have been isolated from the roots of Securidaca longepedunculata (Polygalaceae) collected in the Democratic Republic of Congo. Their structures were established by analyses of the spectral data, including 2D NMR spectra, to be 1 ,3,6,8-tetrahydroxy-2.5-dimethoxy-4-[ -(2,4,5-trimethoxyphenyl)-1-phenylmethyl]xanthone (1) and 1,3,6-trihydroxy-4,7-dimethoxy-2-[1-(2,4,5-trimethoxyphenyl)- 1-phenylmethyl]xanthone (2).

A new xanthone from Moutabea guianensis Aubl.

The ethyl acetate extract of the roots of Moutabea guianensis gave 1,6-dihydroxy-4,7,8-trimethoxy-9H-xanthen-9-one (1), a new xanthone. The isolation was accomplished by column chromatography on silica gel and the structural elucidation of this compound was established by spectroscopic analyses including 1D and 2D NMR and HRESIMS.

Protective effect of Basella alba and Carpolobia alba extracts against maneb-induced male infertility.

CONTEXT: Male infertility is one of the leading causes of social frustration and marginalization, mainly in the developing world. It is attributed to many factors including exposure to agropesticides such as manganese ethylenebis (dithiocarbamate) (maneb), which is one of the most frequently used fungicides in Cameroon. Previous reports support efficiency of some medicinal plants commonly used in Cameroonian folk medicine for the treatment of this disorder. OBJECTIVE: The present study was aimed at assessing the protective effect of extracts from selected plant species, namely Basella alba L. (Basellaceae) (MEBa) and Carpolobia alba G. Don (Polygalaceae) (AECa), in alleviating the maneb-induced impairment of male reproductive function in Wistar albino rats. MATERIALS AND METHODS: The rats were treated with vehicle, plant extract (MEBa or AECa), maneb and maneb plus plant extract, respectively, and their fertility was assessed. Animals were thereafter sacrificed and organs (liver, kidneys and reproductive organs) were dissected out and weighed. Serum androgens together with alanine aminotransferase, liver glutathione and thiobarbituric acid reactive species (TBARS) were also measured. RESULTS AND DISCUSSION: From this study, both plant extracts stimulated testosterone and improved fertility. Administration of MEBa plus maneb prevented fertility reduction by maneb and minimized the inhibitory effect of maneb on testosterone levels. AECa also improved fertility of the maneb-exposed rats, though without restoring testosterone levels, and other investigated parameters remained unaffected by different treatments. CONCLUSION: These findings emphasized the beneficial effects of B. alba and C. alba extracts on male fertility, and suggest their protective effect against maneb-induced toxicity in male reproductive function.

Effect of ethanolic extract of Carpolobia lutea G. Don (polygalaceae) root on learning and memory in CD1 mice.

Carpolobia lutea, commonly called cattle stick or poor man's candle, is used by traditional herbalists in eastern Nigeria to treat 'madness'. It has a reported analgesic and anti-nociceptive effect. The effect of its ethanolic root extract on learning and memory was investigated. Thirty mice were divided into three groups of ten each. One group of mice served as the control and was given normal saline (p.o.) while the other two groups were given acute low dose (1500mg/kg, p.o.) and high dose (2500mg/kg, p.o.) (LD50 3338.83mg/kg). The effect of the extract on cognitive memory was investigated using the Novel Object recognition task (NORT) while the effect on visuospatial learning and memory was studied using the Morris Water maze (MWM). The results obtained in the NORT show that the index of habituation was significantly lower following acute treatment with a low dose of C. lutea extract compared to control. However, the index of habituation did not differ following treatment with a high dose of C. lutea compared to control but it was higher compared to the low dose. Following treatment with a low dose of the extract, the index of discrimination was significantly higher compared to control. The index of discrimination in the high dose treatment group did not differ from control, but it was lower compared to the low dose treatment. This indicated that there was improved cognitive memory only in the low dose treatment group. In the MWM there was no significant difference in swim latency during Acquisition and Reversal training. There also was no significant difference in quadrant duration during probe trial. The swim latency during the visible platform test showed that all mice used had good visual acuity. Therefore, the ethanolic extract of C. lutea root enhanced cognitive memory. However it did not affect visuospatial learning and memory.

Contraceptive, estrogenic and anti-estrogenic potentials of methanolic root extract of Carpolobia lutea in rodents.

Several plants are used in herbal medicine for family planning. Carpolobia lutea is a medicinal plant in South Eastern Nigeria used for family planning. The study was designed to investigate the contraceptive, estrogenic and antiestrogenic potentials of the methanolic root extract of Carpolobia lutea in both rats and mice. The contraceptive effect of extract (7 - 21mg/kg) administered by intraperitoneal route for four days in divided doses was tested in mice and rats. Sexually-active males were introduced on day 5 at the ratio of 3F:1M and kept with these females till the end of the experiment. Investigations on the estrogenic and antiestrogenic property of the extract (7-21mg/kg) were done in immature rats that had undergone surgical removal of both ovaries. The effects of the extract (vaginal opening, vaginal cornification, uterine wet weight) were compared with 17-beta-estradiol (0.1µg/rat/day) as standard drug. Twenty-four hours later, the animals were sacrificed following the last dose and the weights of uterus, kidney, liver and small intestine were recorded. The extract prevented conception in both mice and rats for two gestational periods. Significant changes (p<0.05-0.001) were observed in the length and weight of pups relative to control. There were no abnormalities observed in the pups over thirty days. In ovariectomized immature young rats, the extract showed estrogenic effect (vaginal opening, vaginal cornification and increased uterine wet weight) in low doses while in high doses, it showed anti-estrogenic effect. These findings agree with the traditional use of Carpolobia lutea in the control of fertility. The contraceptive property of the extract may be associated with the direct effects of its chemical constituents.

Antidiarrheal mechanism of Carpolobia lutea leaf fractions in rats.

CONTEXT: Carpolobia lutea G. Don (Polygalaceae) leaf is reputable as an antidiarrheal agent among the Efik and Ibibio tribe of Akwa Ibom State, Nigeria. The crude extract is reported to show antidiarrheal and antiulcer effects in rodents. OBJECTIVE: The isolation and characterization of drug molecules from the leaf fraction with antidiarrheal bioactivity and determination of mechanism of action are reported. MATERIAL AND METHODS: Gradient extraction by maceration yielding n-hexane, chloroform, ethyl acetate, and ethanol fractions (770 mg/kg) were used to establish the fractions suitable for drug discovery. The antidiarrheal effect of the leaf fractions of Carpolobia lutea was evaluated using castor oil-induced diarrhea, castor oil-induced intestinal transit, and enteropooling. RESULTS: Results indicate that all fractions produced a significant (p < 0.01-0.001) decrease in castor oil-induced diarrhea in rats. This effect was not antagonized by isosorbide dinitrate (150 mg/kg, p.o), diphenoxylate (5 × 10⁻³ mg/kg p.o) and yohimbine (1 mg/kg, s.c.) except for the chloroform fraction. The ethyl acetate fraction produced 100% inhibition of intestinal transit, an effect greater than pure drug. Phytochemical analysis of the ethyl acetate fraction yielded polyphenolic compounds. CONCLUSION: The leaf fractions contain two types of antidiarrheal agents, one mediating its effect through α1-presynaptic adrenoceptor while the other does not. Polyphenols isolated may in part lend credence for observed antidiarrheal activity.

Anti-nociceptive effects of Carpolobia lutea G. Don (Polygalaceae) leaf fractions in animal models.

Leaves from Carpolobia lutea (Polygalaceae) were screened to establish the antiulcer ethnomedicinal claim and to quantitatively isolate, elucidate the active compounds by semi-preparative HPLC. The anti-nociceptive effects of Carpolobia lutea (CL) G. Don (Polygalaceae) organic leaf extracts were tested in experimental models in mice. The anti-nociceptive mechanism was determined using tail-flick test, acetic acid-induced abdominal constrictions, formalin-induced hind paw licking and the hot plate test. The fractions (ethanol, ethyl acetate, chloroform, n-hexane) and crude ethyl acetate extract of CL (770 mg/kg, i.p.) produced significant inhibitions of both phases of the formalin-induced pain in mice, a reduction in acetic acid-induced writhing as well as and an elevation of the pain threshold in the hot plate test in mice. The inhibitions were greater to those produced by indomethacin (5 mg/kg, i.p.). Ethyl acetate fraction revealed cinnamic and coumaric acids derivatives, which are described for the first time in literature. These cinnamalglucosides polyphenols characterised from CL may in part account for the pharmacological activities. These findings confirm its ethnomedical use in anti-inflammatory pain and in pains from gastric ulcer-associated symptoms.

In vivo antimalarial activities of ethanolic crude extracts and fractions of leaf and root of Carpolobia lutea.

Carpolobia lutea (leaves and root) is used traditionally as malarial remedy by the Ibibios of Niger Delta of Nigeria and Benin. This study was aimed to investigate the antiplasmodial potentials of the crude leaf and root extracts of this plant as well as their fractions in vivo in Plasmodium berghei berghei-infected mice to give scientific proof to the ethnobotanical claims and correlate with the reported in vivo activity. The ethanolic extracts of Carpolobia lutea leaf (245-735 mg/kg/day) and root (7-21 mg/kg/day) were screened for blood plasmocidal activity against chloroquine-sensitive Plasmodium berghei in mice. The antimalarial activity in 4-day and curative tests was evaluated. Carpolobia lutea leaf extract (245-735 mg/kg/day) and fractions exhibited significant (p<0.05-0.01) antiplasmodial activity both in 4-day early infection test and in established infection with a considerable mean survival time which was incomparable to that the standard drug, chloroquine (5 mg/kg/day). The root extract (7-21 mg/kg/day) and fractions also demonstrated a promising blood schizontocidal activity in early and established infections. These plant extracts and fractions possess considerable antiplasmodial activities which justify their use in ethnomedicine and can be exploited in the control of malaria.

Isolation and structural characterization of glycosides from an anti-angiogenic extract of Monnina obtusifolia H.B.K.

Angiogenesis, the growth of new blood vessels from the pre-existing vasculature is of physiological and pathological importance. Substantial data over the last decade has implicated uncontrolled angiogenesis with various pathological states. Vascular endothelial growth factors (VEGFs) play a critical role in its regulation, and have become one of the most interesting anti-angiogenesis targets. We have investigated the anti-angiogenic potential of plant extracts in a preliminary ELISA screening. The n-BuOH extract obtained from the leaves of Monnina obtusifolia (Polygalaceae) demonstrated an inhibition of VEGF-A or Placental Growth Factor interaction with Flt-1 (VEGF receptor 1), with an inhibition over 50% in particular for VEGF-A/Flt-1 interaction at a concentration of 500 µg/mL. Successively fractionation of the bioactive n-BuOH extracts of M. obtusifolia aerial parts led to the isolation of six new compounds, 1-O-(4-hydroxy-2-methylene-butanoic acid)-6-O-ß-D-(4-hydroxy-2-methylene-butanoyl)-glucopyranose (1), 1-O-(isopentenyl)-6-O-ß-D-(4-hydroxy-2-methylene-butanoyl)-glucopyranose (2), 1-O-(4-hydroxy-2-methylene-butanoic acid)-6-O-ß-D-(isovaleroyl)-glucopyranose (3), 1-O-(3-methylbut-3enyl)-6-O-ß-D-(isovaleroyl)-glucopyranose (4), two new sucrose esters, 3,4-O-ß-D-di-feruloyl-fructofuranosyl-6-O-α-D-(p-coumaroyl)-glucopyranoside (5), and 3,4-O-ß-D-di-feruloyl-fructofuranosyl-6-O-α-D-(caffeoyl)-glucopyranoside (6), together with known flavonoids. Their structures were established on the basis of detailed spectral analysis. Since none of the isolated compounds showed a relevant inhibition of VEGFs, the biological activity observed for the butanolic extract might be due to the presence of a combination of compounds acting synergistically.

Evaluation of the sedative and anticonvulsant properties of three Cameroonian plants.

Millettia thonningii, Ocinum sanctum and Securitaca longepedunculaca are used in traditional medicine in Cameroon to treat epilepsy, insomnia and headaches. Animal models of epilepsy (maximal electroshock (MES), n-methyl-d-aspartate (NMDA), pentylenetetrazol (PTZ), isonicotinic hydrazide acid (INH), picrotoxine (PIC) and strychnine (STR)-induced convulsions or turning behavior were used to evaluate anticonvulsant activity while diazepam-induced sleep test was used to evaluate sedative activity of the plants. Four doses of extracts were used for each plant (100, 200, 500 and 1000 mg/kg). At a dose of 1000 mg/kg, Millettia thonningii protected 60 and 90% of mice against MES and PTZ-induced convulsions, respectively. At the same dose, Millettia thonningii also protected 80% of mice against NMDA-induced turning behavior. At a dose of 1000 mg/kg, Ocinum sanctum provided complete protection against MES, PIC and STR- induced convulsions and 83.3% of protection in PTZ test. Securitaca longepedunculata completely protected (100%) mice in PIC test at a dose of 200 mg/kg, in MES test at a dose of 500 mg/kg and in PTZ test at a dose of 1000 mg/kg. 66.7% of mice were protected against STR-induced convulsions. All the three plants showed also sedative properties for they increased significantly and in a dose dependent manner the total sleep time induced by diazepam. The total sleep time of the control groups was multiplied by a factor of 3 at least by each extract. The presence of sedative and anticonvulsant activity in the three plants could explain their use in traditional medicine in the treatment of epilepsy and insomnia in Cameroon.

Antiulcerogenic activity of extract, fractions, and some compounds obtained from Polygala cyparissias St. Hillaire & Moquin (Polygalaceae).

The present study evaluates the gastroprotective properties of acetone extract, chloroform, and methanol fractions, alpha-spinasterol (1); 1,3-dihydroxy-7-methoxyxanthone (2); and 1,7-dihydroxy-2,3-methylenedioxyxanthone (3) obtained from Polygala cyparissias (Polygalaceae). Gastroprotective assays were performed in mice using ethanol/HCl and nonsteroidal anti-inflammatory drug (NSAID)/bethanechol-induced ulcer models. Chloroformic fraction showed no interesting results. On the other hand, in the ethanol/HCl-induced ulcer model, the treatment using doses of 50, 125, and 250 mg/kg promoted ulcer inhibition of 45.19+/-12.93%, 62.99+/-3.49%, and 67.40+/-4.75% for acetone extract and 43.70+/-5.12%, 64.56+/-5.64%, and 74.49+/-6.13% for methanol fraction. In the model of NSAID/bethanechol-induced ulcer, the ulcer inhibitions in the same doses were 28.12+/-12.45%, 60.16+/-6.58%, and 77.86+/-7.18% for the acetone extract and 46.09+/-6.92%, 67.45+/-4.36%, and 75.00+/-2.92% for the methanol fraction. In view of the antiulcer potential of the acetone extract and its high yield and xanthone content, it was submitted to chromatographic procedures, giving compounds 1-3, which were also evaluated in the ethanol-induced ulcer model. The results showed that at a dose of 50 mg/kg, these compounds reduced the percentage of ulcer by around 71.26+/-9.40%, 81.10+/-5.75%, and 86.22+/-3.42%, for compounds 1, 2, and 3, respectively. The antiulcerogenic activity of P. cyparissias may be attributed, at least in part, to these compounds.

Report: In vitro antimicrobial activities of extracts of Carpolobia lutea root.

Several plants are used in folk medicine to treat infections. Carpolobia lutea, G.Don (Polygalaceae) is a medicinal plant commonly used by herbalists in Southern Nigeria against dental and genitourinary infections. The study was to evaluate the in vitro antimicrobial activities of n-hexane, chloroform, ethyl acetate and methanol extracts of Carpolobia lutea root. Four typed cultures of bacteria namely, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis and two clinical strains of fungi, namely Candida albicans and Tinea capitis were analyzed using agar well diffusion method. The extracts that showed antimicrobial activity were then tested to determine the Minimum Inhibitory Concentration for each bacterial or fungal sample.The ethyl acetate extract gave the widest zone of inhibition (21.0 mm) followed by chloroform when tested on E. coli. No inhibition was observed with E.Coli. None of the extracts showed any inhibitory effect against Pseudomonas aeruginosa and the fungal strains of Candida albicans and Tinea capitis. The most potent of these extracts was Chloroform extract with Minimum Inhibitory Concentration (MIC) of 25 mg/ml for bacteria. The phytochemical screening of the root of C. lutea revealed the presence of saponins, anthraquinones, flavonoids, cardiac glycosides, simple sugar and terpenes.

Anticonvulsant activity of Nylandtia spinosa L. Dumont (Polygalaceae) aqueous and methanol leaf extracts in mice.

Aqueous and methanol leaf extracts of Nylandtia spinosa L. Dumont (Polygalaceae) were evaluated for anticonvulsant activity against tonic seizures produced in mice by pentylenetetrazole (PTZ), bicuculline, picrotoxin, and N-methyl-DL-aspartic acid (NMDLA). Aqueous leaf extract of N. spinosa (50-400 mg/kg, i.p.) and methanol extract (50-400 mg/kg, i.p.) significantly attenuated PTZ (95 mg/kg, i.p.)-induced tonic seizures. Doses of 400 mg/kg (i.p.) and 100-400 mg/kg (i.p.) of aqueous extract of N. spinosa significantly delayed the onset of tonic seizures elicited by bicuculline (35 mg/kg, i.p.) and picrotoxin (12 mg/kg, i.p.), respectively. Methanol extract (200-400 mg/kg, i.p.) and (50-400 mg/kg, i.p.) significantly delayed the onset of tonic seizures induced by bicuculline (35 mg/kg, i.p.) and picrotoxin (12 mg/kg, i.p.), respectively, whereas 400 mg/kg (i.p.) significantly reduced the incidence of picrotoxin (12 mg/kg, i.p.)-induced seizures. Both aqueous and methanol leaf extracts of N. spinosa did not affect NMDLA (400 mg/kg, i.p.)-induced tonic seizures. Phenobarbitone (12.5 mg/kg, i.p.) and diazepam (0.5 mg/kg, i.p.) antagonized tonic seizures induced by PTZ (95 mg/kg, i.p.), bicuculline (35 mg/kg, i.p.), and picrotoxin (12 mg/kg, i.p.) but did not affect NMDLA (400 mg/kg, i.p.)-induced seizures. Phenytoin (30 mg/kg, i.p.) did not alter the tonic seizures produced by either PTZ (95 mg/kg, i.p.), bicuculline -2-(35 mg/kg, i.p.), or picrotoxin (12 mg/kg, i.p.). The results obtained indicate that both aqueous and methanol leaf extracts of N. spinosa possess anticonvulsant property, thus justifying the use of the plant by traditional medicine practitioners in the treatment of epilepsy. The relatively high LD(50) of greater than 3600 mg/kg (p.o.) and 1780 mg/kg (i.p.) obtained with the aqueous extract suggest that the plant is relatively safe in mice. The phytochemical analysis carried out showed the presence of tannins, saponins, reducing sugars, alkaloids, flavonoids, triterpene steroids, and cardiac glycosides in the plant material.