Separation of acteoside and linarin from Buddlejae Flos by high-speed countercurrent chromatography and their anti-inflammatory activities.

Buddleja officinalis Maxim., a deciduous, flowering shrub, is used as a traditional Chinese medicine; the bioactivity of B. officinalis is primarily due to flavonoids and phenylethanoid glycosides. In the study, acteoside and linarin were successfully isolated from B. officinalis by high-speed countercurrent chromatography with a two-phase solvent system composed of ethyl acetate: n-butanol: water (5:0.8:5, v/v/v). The purities of acteoside and linarin were determined to be 97.3 and 98.2%, respectively, using one-step high-speed countercurrent chromatography separation. The chemical structures of the two compounds were identified by electrospray ionization-mass spectrometry and nuclear magnetic resonance. After separation, the anti-inflammatory effects of the two compounds were evaluated using lipopolysaccharide-induced human umbilical vein endothelial cells. Acteoside and linarin inhibited the expression of nitric oxide, tumor necrosis factor α and interleukin 1ß, which demonstrated that acteoside and linarin possessed anti-inflammatory activity.

Phytochemical, anti-inflammatory and anti-trypanosomal properties of Anthocleista vogelii Planch (Loganiaceae) stem bark.

ETHNOPHARMACOLOGICAL RELEVANCE: Anthocleista vogelii Planch (Loganiaceae) is used in African Traditional Medicine for the treatment of pain and inflammatory disorders as well as sleeping sickness. AIM OF THE STUDY: To determine the in vivo anti-inflammatory and in vitro anti-trypanosomal activities of the extracts of A. vogelii stem bark and identify the phytochemical classes of the fractions responsible for the activities. MATERIALS AND METHODS: The in vivo anti-inflammatory activity of the extracts was evaluated using the egg albumin-induced rat paw oedema model while the in vitro anti-trypanosomal activity was assessed on Trypanosoma brucei brucei. The in vitro cytotoxicity was assessed on HeLa (human cervix adenocarcinoma) cell line. RESULTS: The methanolic extract of A. vogelii stem bark, with 11.2% yield, gave LD50 > 5000 mg/kg. The n-hexane fraction of the extract contains steroids, terpenes and fatty acids and yielded non-cytotoxic terpenoidal column fraction with anti-trypanosomal IC50 of 3.0 µg/mL. The ethylacetate fraction at 100 mg/kg dose significantly (p < 0.05) provoked 37.8, 62.5 and 69.7% inhibition of oedema induced by egg-albumin at the second, fourth and sixth hours respectively. CONCLUSION: The study demonstrated that the anti-inflammatory and anti-trypanosomal activities of A. vogelii are probably due to non-cytotoxic terpenoids and validated the traditional use of A. vogelii in the treatment of inflammation and sleeping sickness.

Neuroprotective Effects of the Anthocleista Schweinfurthii Gilg. (Loganiaceae) Stem Bark Extract in Postmenopause-Like Model of Ovariectomized Wistar Rats.

Background Estrogen deficiency in postmenopausal period causes severe neuroendocrine changes in brain which influences memory and other nervous functions. Anthocleista schweinfurthii is used traditionally to treat female infertility and menopause related symptoms. This study was performed to investigate the potential neuroprotective effects of aqueous extract of Anthocleista schweinfurthii on brain in a postmenopause-like model of ovariectomized Wistar rats. Methods Thirty animals were sham-operated or ovariectomized (Ovx) 84 days after surgery, six groups of five rats each were daily treated orally during 28 days with: distilled water for groups 1 (sham-operated) and 2 (Ovx), estradiol valerate (group 3) and the three doses of extracts {groups 4, 5 and 6 (Ovx)}. Biochemical and histological evaluations focused on brain. Results Compared to sham-operated control, ovariectomy decreased total protein levels in brain (p<0.01) which was increased by plant extract at the dose of 300 mg/kg (p<0.05), underlying its anabolic properties. Ovariectomy significantly decreased magnesium levels in brain (p<0.001). Anthocleista schweinfurthii increased significantly magnesium levels (p<0.01), showing its capacity to act on synaptic conduction. Ovariectomy induced oxidative stress by increasing malondialdehyde levels (p<0.05) and decreasing reduced glutathione levels (p<0.05) in brain. The plant extract exhibited antioxidative activity by reducing malondialdehyde levels and increasing glutathione levels in brain. Damage in brain structure which was caused by ovariectomy disappeared following the treatment. Conclusions Results suggest that Anthocleista schweinfurthii may have neuroprotective effects in Ovx Wistar rats by increasing total protein, magnesium levels and reducing oxidative stress in brain.

Botany, Phytochemistry, Pharmacology and Toxicity of Strychnos nux-vomica L.: A Review.

Strychnos nux-vomica L. belongs to the genus Strychnos of the family Loganiaceae and grows in Sri Lanka, India and Australia. The traditional medicinal component is its seed, called Nux vomica. This study provides a relevant and comprehensive review of S. nux-vomica L., including its botany, ethnopharmacology, phytochemistry, pharmacology and toxicology, thus providing a foundation for future studies. Up to the present day, over 84 compounds, including alkaloids, iridoid glycosides, flavonoid glycosides, triterpenoids, steroids and organic acids, among others, have been isolated and identified from S. nux-vomica. These compounds possess an array of biological activities, including effects on the nervous system, analgesic and anti-inflammatory actions, antitumor effects, inhibition of the growth of pathogenic microorganisms and regulation of immune function. Furthermore, toxicity and detoxification methods are preliminarily discussed toward the end of this review. In further research on S. nux-vomica, bioactivity-guided isolation strategies should be emphasized. Its antitumor effects should be investigated further and in vivo animal experiments should be performed alongside in vitro testing. The pharmacological activity and toxicology of strychnine [Formula: see text]-oxide and brucine [Formula: see text]-oxide should be studied to explore the detoxification mechanism associated with processing more deeply.

Monoterpenoid indole alkaloids from Gardneria multiflora.

Six new monoterpenoid indole alkaloids, 19(E)-9-demethoxy-16-dehydroxylchitosenine-17-O- ß-d-glucopyranoside (1), 19(E)-9,10-didemethoxy-16-dehydroxylchitosenine-17-O-ß-d-gluco-pyranoside (2), 19(E)-9,10-didemethoxy-16-dehydroxyl-11-methoxychitosenine (3), 19(E)-9,10-didemethoxy-16-dehydroxyl-11-methoxychitosenine-17-O-ß-d-glucopyranoside (4), 19(Z)-18-carboxylgardneramine (5), and 19(E)-18-demethoxygardneramine-N (4)-oxide (6), along with four known alkaloids, were isolated from Gardneria multiflora, and their structures were elucidated by spectroscopic analysis. Compounds 1, 2 and 4 are the first example of Gardneria alkaloids whose glucose units were attached to C-17. None of the compounds were cytotoxic to any of five human cancer cell lines.

In vitro anthelmintic effects of Spigelia anthelmia protein fractions against Haemonchus contortus.

Gastrointestinal nematodes are a significant concern for animal health and well-being, and anthelmintic treatment is mainly performed through the use of chemical products. However, bioactive compounds produced by plants have shown promise for development as novel anthelmintics. The aim of this study is to assess the anthelmintic activity of protein fractions from Spigelia anthelmia on the gastrointestinal nematode Haemonchus contortus. Plant parts were separated into leaves, stems and roots, washed with distilled water, freeze-dried and ground into a fine powder. Protein extraction was performed with sodium phosphate buffer (75 mM, pH 7.0). The extract was fractionated using ammonium sulfate (0-90%) and extensively dialyzed. The resulting fractions were named LPF (leaf protein fraction), SPF (stem protein fraction) and RPF (root protein fraction), and the protein contents and activities of the fractions were analyzed. H. contortus egg hatching (EHA), larval exsheathment inhibition (LEIA) and larval migration inhibition (LMIA) assays were performed. Proteomic analysis was conducted, and high-performance liquid chromatography (HPLC) chromatographic profiles of the fractions were established to identify proteins and possible secondary metabolites. S. anthelmia fractions inhibited H. contortus egg hatching, with LPF having the most potent effects (EC50 0.17 mg mL-1). During LEIA, SPF presented greater efficiency than the other fractions (EC50 0.25 mg mL-1). According to LMIA, the fractions from roots, stems and leaves also reduced the number of larvae, with EC50 values of 0.11, 0.14 and 0.21 mg mL-1, respectively. Protein analysis indicated the presence of plant defense proteins in the S. anthelmia fractions, including protease, protease inhibitor, chitinase and others. Conversely, secondary metabolites were absent in the S. anthemia fractions. These results suggest that S. anthelmia proteins are promising for the control of the gastrointestinal nematode H. contortus.

Evidence for the involvement of the GABA-ergic pathway in the anticonvulsant activity of the roots bark aqueous extract of Anthocleista djalonensis A. Chev. (Loganiaceae).

BACKGROUND: The root bark of Anthocleista djalonensis A. Chev. (Loganiaceae) is widely used in traditional medicine in Northern Cameroon to treat epilepsy and related conditions, such as migraine, insomnia, dementia, anxiety, and mood disorders. METHODS: To investigate the anticonvulsant effects and the possible mechanisms of this plant, an aqueous extract of Anthocleista djalonensis (AEAD) was evaluated by using animal models of bicuculline-, picrotoxin-, pilocarpine-, and pentylenetetrazole-induced convulsions. Their effects on brain γ-aminobutyric acid (GABA) concentration and GABA-T activity were also determined. RESULTS: This extract significantly protected mice against bicuculline-induced motor seizures. It provided 80% protection against picrotoxin-induced tonic-clonic seizures, and strongly antagonized convulsions induced by pilocarpine. AEAD also protected 100% of mice against pentylenetetrazole-induced seizures. Flumazenil, a central benzodiazepine receptor antagonist and FG7142, a partial inverse agonist in the benzodiazepine site of the GABAA receptor complex, were found to have an inhibitory effect on the anticonvulsant action of AEAD in pentylenetetrazole test. Finally, the brain GABA concentration was significantly increased and GABA-T activity was inhibited by AEAD. CONCLUSIONS: The effects of Anthocleista djalonensis suggested the presence of anticonvulsant properties that might involve an action on benzodiazepine and/or GABA sites in the GABAA receptor complex or by modulating GABA concentration in the central nervous system (CNS).

A systems pharmacology approach to investigate the mechanisms of action of Semen Strychni and Tripterygium wilfordii Hook F for treatment of rheumatoid arthritis.

ETHNOPHARMACOLOGY RELEVANCE: The angiogenesis control at the initiation of rheumatoid arthritis (RA) that mainly blocks the inflammatory cascades expects to attenuate the action of angiogenic mediators, synovial angiogenesis, and to partially reverse the erosive bone damage. Two typical Chinese herbs, Semen Strychni and Tripterygium wilfordii Hook F (TwHF) have been used as a remedy to treat RA since ancient time. However, their functioning mechanisms are still unknown. Thus it is necessary to exploit their underlying mechanism for the treatment of RA. METHODS: This study was undertaken to analyze their underlying mechanism based on a systems biology platform. Firstly, active components of the two herbs were screened out from TcmSP database based on their OB and DL values. Then their potential targets were predicted by using Random Forest, Support Vector Machine, and validated via docking process. Finally, a network of compound-target was constructed. RESULTS: In this work, 27 and 33 active compounds were screened out from Semen Strychni and TwHF, targeting 28 and 32 potential proteins, respectively. The results show that the two herbs modulate the angiogenesis mediators through both direct and indirect pathways, and 21 common targets shared by Semen Strychni and TwHF bear major responsibility for treating RA. CONCLUSIONS: The underlying mechanism of Semen Strychni and TwHF in treatment of RA is through multiple targets interaction by their blocking of the angiogenesis mediator cascades. This may provide us a better understanding of the function of the two herbs for the treatment of RA, as well as a clue to unveil their possible treatment effects of other systemic diseases, and in this way, hopefully the screening models may facilitate the discovery of novel combined drugs.

Some Strychnos spinosa (Loganiaceae) leaf extracts and fractions have good antimicrobial activities and low cytotoxicities.

BACKGROUND: Strychnos spinosa Lam. is a deciduous tree used in traditional medicine to treat infectious diseases. This study is designed to determine the antimicrobial, antioxidant and cytotoxic activities of extracts and fractions from leaves of S. spinosa. METHODS: Extracts were obtained by maceration with acetone, methanol and dichloromethane/methanol (1/1) while fractions were prepared by liquid-liquid fractionation of the acetone extract. A broth serial microdilution method with tetrazolium violet as growth indicator was used to determine the minimum inhibitory concentration (MIC) against fungi, Gram-positive and Gram-negative bacteria. The antioxidant activity was determined using free-radical-scavenging assays, and the 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide reduction assay was used to determine cytotoxicity. RESULTS: Four extracts and five fractions had good to weak antimicrobial activity with MICs ranging from 0.04 to >1.25 mg/ml against both fungi and bacteria. The chloroform and ethyl acetate fractions had an MIC of 0.08 mg/ml against Aspergillus fumigatus. The n-butanol fraction had an MIC of 0.04 mg/ml against Cryptococcus neoformans. The hexane and chloroform fractions had an MIC of 0.08 mg/ml against Staphylococcus aureus. The antioxidant activities were much lower than that of the positive controls. Except for the alkaloid extract, all the extracts and fractions had free-radical-scavenging activity (IC50 ranging from 33.66 to 314.30 µg/ml). The cytotoxicity on Vero cells was reasonable to low with LC50 values ranging between 30.56 and 689.39 µg/ml. CONCLUSION: The acetone extract and the chloroform fraction had the highest antibacterial activity. By solvent-solvent fractionation it was possible to increase the activity against A. fumigatus and to decrease the cytotoxicity leading to a potentially useful product to protect animals against aspergillosis. Our results therefore support the use of S. spinosa leaves in traditional medicine to treat infectious diseases.

HPLC-DAD method for comprehensive quality control of Semen Strychni.

CONTEXT: Semen Strychni is the seed of Strychnos nux-vomica L. (Loganiaceae). Its quality control procedure remains an issue since previous reports only focused on Strychnos alkaloids. To the best of our knowledge, chlorogenic acid (a phenolic acid) and loganin (an iridoid glycoside) are selected for the first time as marker constituents of quality control for Semen Strychni because of their bioactive activity correlating with therapeutic effects. OBJECTIVE: This study aimed to develop a simple and comprehensive quantity control method for Semen Strychni. MATERIALS AND METHODS: The optimal ultrasonic extraction procedure was carried out for 45 min using 50% aqueous methanol with 1% formic acid. The satisfactory chromatographic separation was achieved on an Ultimate LP-C18 column with gradient elution using acetonitrile and water containing 30 mmol/L ammonium acetate and 1% formic acid. The high performance liquid chromatography method with diode array detector was validated for linearity, limit of detection and quantification (LOQ), precision, repeatability, accuracy and stability. RESULTS: All the calibration curves showed good linearity (r(2) ≥ 0.999). The LOQ values for chlorogenic acid, loganin, strychnine, brucine, strychnine N-oxide and brucine N-oxide were 0.54, 0.83, 0.48, 0.50, 0.52 and 0.54 µg/mL, respectively. The method was reproducible with good accuracy in the range 95.6-104.4% and relative standard deviation (RSD) values less than 4.55%. The method was then applied to determine the components of the seed coat, seed leaf, endosperm and whole seed of Semen Strychni. CONCLUSION: This newly established method is validated as a simple and practical tool for authentication and quality control of Semen Strychni.

Macrocyclic spermidine alkaloids from Androya decaryi L. Perrier.

Three new spermidine alkaloids and two known compounds were isolated from the leaves of Androya decaryi. Their structures were elucidated on the basis of their spectroscopic data (NMR and mass spectrometry), by X-Ray diffraction and by comparison with literature values. Evaluation of the in vitro antiplamosdial properties of the isolated compounds revealed they did not possess any significant activity.

Alpha-amylase inhibitory activity of two Anthocleista species and in vivo rat model anti-diabetic activities of Anthocleista djalonensis extracts and fractions.

ETHNOPHARMACOLOGICAL RELEVANCE: Anthocleista djalonensis (A. Chev) and Anthocleista vogelii Planch are plants being used in West Africa traditionally to treat various diseases such as malaria, hernia, hypertension, stomach aches, hemorrhoids, syphilis, and diabetes. Diabetes causes about 5% of all deaths globally each year. Chemotherapeutic agents such as biguanides, sulfonylureas, and thiozolidinediones are available for the treatment of diabetes, however, they have undesirable side effects. The need for newer, more effective and less toxic drugs is imperative and the biodiversity of Nigeria has a high potential for drug discovery based on plants used in the ethnomedicine. AIM OF THE STUDY: To investigate the leaves, stem bark and roots of these plants for their probable alpha-amylase inhibitory activities and establish their anti-diabetic activities. The overall goal is do bioassay-guided fractionation and isolation of active anti-diabetic compounds. MATERIALS AND METHODS: Powdered samples (leaves, stem bark and roots) macerated with 80% aqueous methanol were evaluated in vitro using alpha-amylase inhibitory assay while in vivo investigations were carried out on hyperglycemic rats. Diabetes was induced in albino rats by an intraperitoneal injection of alloxan monohydrate (80mg/kg). Plant extracts (1g/kg) were given orally for 7 days, while blood glucose levels were monitored using a one touch glucometer. The crude methanol extracts found to be most active were further partitioned into hexane and ethyl acetate fractions which were also tested in vivo on the diabetic animals. RESULTS: The leaves and stem bark crude methanol extracts of Anthocleista djalonensis gave comparable α-amylase inhibition of 73.66% and 72.90%, respectively which were quite higher than the 38.93% and 22.90% of the same plant parts given by Anthocleista vogelii. The crude stem bark extract of Anthocleista djalonensis exhibited significant peak blood glucose reduction on day 6 (72.59%, p<0.05) which was higher than the leaves or roots which gave 45.73% and 47.46% (p<0.05), respectively The stem bark ethyl acetate fraction of Anthocleista djalonensis gave reduction in blood glucose level of 60.86% (p<0.05). CONCLUSION: From our results, the leaves, stem bark and whole root of both plants exhibited α-amylase inhibitory activities with Anthocleista djalonensis also showing good anti-diabetic activities in vivo indicating that they contain active principles for the management of diabetes. There is justification for the use of the plants traditionally to manage diabetes.

Monoterpenoid indole alkaloids from Gardneria ovata.

Eight new monoterpenoid indole alkaloids, gardfloramine-9-O-ß-D-glucopyranoside (1), 19(E)-18-demethoxygardfloramine-N(4)-oxide (2), gardfloramine-N(4)-oxide (3), 18-demethylgardfloramine (4), 19(E)-9,18-didemethoxygardneramine (5), 19(E)-11-methoxy-9,18-didemethoxygardneramine (6), 9-demethoxy-18-demethylgardneramine (7), and minfiensine-N(4)-oxide (8), along with six known alkaloids, were isolated from Gardneria ovata. The structures of the new alkaloids were established by means of spectroscopic methods. None of the compounds were cytotoxic to five human cancer cell lines.

Dormancy break in seeds of quina (Strychnos pseudoquina A. St.-Hil.) / Superação da dormência de sementes de quina (Strychnos pseudoquina A. St.-Hil.)

"Quina" (Strychnos pseudoquina A. St. Hil) is a medicinal plant species from the Brazilian Cerrado. As its seeds show dormancy, they were subjected to the treatments pre-cooling at 5ºC during 7 days, pre-heating at 40ºC during 7 days, pre-soaking in sulfuric acid PA during 5 and 15 min, pre-soaking in boiling water during 5 and 15 min, pre-soaking in 100 and 200 ppm gibberellic acid during 48 h, pre-soaking in distilled water during 24 and 48 h, and mechanical scarification to break dormancy. Counts were daily conducted from the 2nd day after the experiment implementation until the germination stabilization at the 65th day. The germination speed index (GSI) and the germination percentage were evaluated. Germination rates above 96 percent were reached in seeds pre-soaked in water during 48 h and substrate moistened with water or KNO3.

A quina (Strychnos pseudoquina A. St.-Hil) é espécie medicinal do Cerrado Brasileiro. As sementes apresentam dormência e, por isso, foram submetidas aos tratamentos pré-resfriamento a 5ºC durante 7 dias, pré-aquecimento a 40ºC durante 7 dias, pré-embebição em ácido sulfúrico P.A. durante 5 e 15 minutos, pré-embebição em água fervente durante 5 e 15 minutos, pré-embebição em ácido giberélico a 100 e 200 ppm, durante 48 horas, pré-embebição em água destilada durante 24 e 48 horas e escarificação mecânica, visando à superação da dormência. Foram realizadas contagens diárias entre o 2º dia após a implantação do experimento até a estabilização da germinação, que ocorreu no 65º dia. Foram avaliados o índice de velocidade de germinação (IVG) e a porcentagem de germinação. Taxas de germinação acima de 96 por cento foram atingidas em sementes pré-embebidas em água durante 48 horas e substrato umedecido com água ou KNO3.

Loganiáceas: da toxicologia ao repertório / Loganiaceous: from toxicology to repertory

Com o grupo dos medicamentos homeopáticos derivados de Loganiáceas, este artigo discute as possíveis relações entre o conhecimento toxicológico e potenciais núcleos sintomáticos desses medicamentos, resultantes da experimentação patogenética homeopática. A perspectiva toxicológica aponta consistentemente para expressões sintomatológicas derivadas da ação dos alcalóides componentes de todas as plantas desta família, estricnina e, secundariamente, estricnina. A análise comparativa, com ajuda do repertório homeopático, permite identificar, não somente núcleos sintomáticos comuns a uma família ou grupo de medicamentos, mas também as diferenças específicas de cada um dos membros, contribuindo assim no diagnóstico de individualização mórbida, na base da prescrição homeopática.

By taking the group of homeopathic remedies derived from Loganiaceae, this article discusses the possible relations between toxicological knowledge and the potential symptomatic nuclei of these remedies, as resulting from homeopathic pathogenetic trials. The toxicological perspective consistently points out to symptomatic expressions derived from the action of the alkaloid components of all the plants belonging to this family, strychnine and secondarily brucine. The comparative analysis, with the help of the homeopathic repertory, allows to identify not only symptomatic nuclei common to a family or group of remedies, but also the specific differences that distinguish each of its members, contributing in this way to the diagnosis of individual disease, which lays at the ground of homeopathic prescription.

Loganiáceas: da toxicologia ao repertório / Loganiaceous: from toxicology to repertory

Com o grupo dos medicamentos homeopáticos derivados de Loganiáceas, este artigo discute as possíveis relações entre o conhecimento toxicológico e potenciais núcleos sintomáticos desses medicamentos, resultantes da experimentação patogenética homeopática. A perspectiva toxicológica aponta consistentemente para expressões sintomatológicas derivadas da ação dos alcalóides componentes de todas as plantas desta família, estricnina e, secundariamente, estricnina. A análise comparativa, com ajuda do repertório homeopático, permite identificar, não somente núcleos sintomáticos comuns a uma família ou grupo de medicamentos, mas também as diferenças específicas de cada um dos membros, contribuindo assim no diagnóstico de individualização mórbida, na base da prescrição homeopática.(AU)

By taking the group of homeopathic remedies derived from Loganiaceae, this article discusses the possible relations between toxicological knowledge and the potential symptomatic nuclei of these remedies, as resulting from homeopathic pathogenetic trials. The toxicological perspective consistently points out to symptomatic expressions derived from the action of the alkaloid components of all the plants belonging to this family, strychnine and secondarily brucine. The comparative analysis, with the help of the homeopathic repertory, allows to identify not only symptomatic nuclei common to a family or group of remedies, but also the specific differences that distinguish each of its members, contributing in this way to the diagnosis of individual disease, which lays at the ground of homeopathic prescription.(AU)

Anthelmintic activity of Spigelia anthelmia extract against gastrointestinal nematodes of sheep.

In vitro (larval development assay) and in vivo studies were conducted to determine possible direct anthelmintic effect of ethanolic and aqueous extracts of Spigelia anthelmia towards different ovine gastrointestinal nematodes. The effect of extracts on development and survival of infective larvae stage (L(3)) was assessed. Best-fit LC(50) values were computed by global model of non-linear regression curve fitting (95% confidence interval). Therapeutic efficacy of the ethanolic extracts administered orally at a dose rate of 125, 250, and 500 mg/kg, relative to a non-medicated control group of sheep harbouring naturally acquired infection of gastrointestinal nematodes, was evaluated in vivo.The presence of S. anthelmia extracts in the cultures decreased the survival of L(3) larvae. The LC(50) of aqueous extract (0.714 mg/ml) differ significantly from the LC(50) of the ethanolic extract (0.628 mg/ml) against the strongyles (p < 0.05, paired t-test). Faecal egg counts on day 12 after treatment showed that the extract is effective, relative to control (one-way analysis of variance [ANOVA], Dunnett's multiple comparison test) at 500 mg/kg against Strongyloides spp. (p < 0.01), 250 mg/kg against Oesophagostomum spp., Trichuris spp. (p < 0.05), and 125 mg/kg against Haemonchus spp. and Trichostrongylus spp. (p < 0.01). The effect of the doses is significant in all cases, the day after treatment is also extremely significant in most cases, whereas interaction between dose and day after treatment is significant (two-way ANOVA). S. anthelmia extract could, therefore, find application in the control of helminth in livestock, by the ethnoveterinary medicine approach.

Anthelmintic efficacy of extracts of Spigelia anthelmia Linn on experimental Nippostrongylus braziliensis in rats.

Spigelia anthelmia Linn is used as a herb and is a common annual weed of cultivation in open re-growths, on unused land in towns as well as on road sides. The plant can grow to approximately 30 cm in height. The aim of this study was to screen extracts of Spigelia anthelmia for their anthelmintic activity against an experimental Nippostrongylus braziliensis infection in rats. Acute oral toxicity occurred at a dose of 1,140 mg/kg, while anthelmintic trials against Nippostrongylus braziliensis in rats using the aqueous fraction showed a progressive decrease in worm count with increasing dose (10, 13, 16, 20 and 25 mg per kg body weight) (p < 0.05). At 25 mg per kg body weight, the worm count was significantly lower than that at 10 mg per kg body weight (p < 0.05).

Anthelmintic efficacy of extracts of Spigelia anthelmia Linn on experimental Nippostrongylus braziliensis in rats

Spigelia anthelmia Linn is used as a herb and is a common annual weed of cultivation in open re-growths, on unused land in towns as well as on road sides. The plant can grow to approximately 30 cm in height. The aim of this study was to screen extracts of Spigelia anthelmia for their anthelmintic activity against an experimental Nippostrongylus braziliensis infection in rats. Acute oral toxicity occurred at a dose of 1,140 mg/kg, while anthelmintic trials against Nippostrongylus braziliensis in rats using the aqueous fraction showed a progressive decrease in worm count with increasing dose (10, 13, 16, 20 and 25 mg per kg body weight) (p < 0.05). At 25 mg per kg body weight, the worm count was significantly lower than that at 10 mg per kg body weight (p < 0.05).

Neuromuscular effects and acute toxicity of an ethyl acetate extract of Spigelia anthelmia Linn.

An ethyl acetate extract of Spigelia anthelmia (EASa), with validated anthelmintic activity, was evaluated for its acute toxicity and general effects in albino Swiss mice and for neuromuscular relaxant activity in the frog sciatic-gastrocnemius and rectus abdominis preparation. The extract induced a dose-related myotonia and muscular paralysis of rapid onset at higher doses. The calculated LD50 after oral and intraperitoneal administration was 345.9 [241.4-484.7] mg/kg and 60.8 [47.4-80] mg/kg, respectively. In broilers, intramuscular injection of EASa-induced spastic paralysis qualitatively similar to that obtained after succinylcholine administration and contrasting to the flaccid paralysis induced by D-tubocurarine. The contraction elicited by direct stimulation of the gastrocnemius was blocked by EASa by 54.3+/-4.7% (IC50 = 21.4 [11.2-35.8] microg/ml) and the twitches evoked by stimulation of the sciatic nerve were blocked by 69.1+/-7.4% (IC50 = 17.9 [4.5-34.23] microg/ml). EASa also blocked acetylcholine-induced contractions in the frog rectus abdominis by 58.6+/-7.4% (IC50 = 7.4 [1.7-15.28] microg/ml) but did not decrease tonic contractions induced by a high-potassium Ringer solution. In summary, the ethyl acetate extract of Spigelia anthelmia induces tonic paralysis in vivo, and decreases amplitudes of twitches and increases tonus of skeletal muscle in vitro.