Antitrypanosomal activity of some medicinal plants from Nigerian ethnomedicine

Human African trypanosomiasis is a neglected tropical disease with complex clinical presentation, diagnosis, and difficult treatment. The available drugs for the treatment of trypanosomiasis are old, expensive, and less effective, associated with severe adverse reactions and face the problem of drug resistance. This situation underlines the urgent need for the development of new, effective, cheap, and safe drugs for the treatment of trypanosomiasis. The search for new antitrypanosomal agents in this study is based on ethnomedicine. In vitro antitrypanosomal activity of 36 plant extracts from 10 plant species from Nigerian ethnomedicine was evaluated against bloodstream forms of Trypanosoma brucei rhodesiense STIB 900. Cytotoxic activity was determined against mammalian L6 cells. Alamar blue assay was used to measure the endpoint of both antitrypanosomal and toxicity assays. The ethyl acetate extract of leaves of Ocimum gratissimum Linn. (Labiatae) showed the highest antitrypanosomal activity (IC₅₀ of 2.08 ± 0.01 μg/ml) and a high selective index of 29. Furthermore, the hexane, ethyl acetate, or methanol extracts of Trema orientalis (L.) Blume (Ulmaceae), Pericopsis laxiflora (Benth. ex Baker) Meeuwen, Jatropha curcas Linn. (Euphorbiaceae), Terminalia catappa Linn. (Combretaceae), and Vitex doniana Sweet (Verbenaceae) displayed remarkable antitrypanosomal activity (IC₅₀ 2.1–17.2 μg/ml) with high selectivity indices (20–80) for trypanosomes. The antitrypanosomal activity of T. catappa and T. orientalis against T. brucei rhodesiense (STIB 900) is being reported for the first time in Nigerian ethnomedicine, and these plants could be a potential source of antitrypanosomal agents.     

New Antitrypanosomal Tetranotriterpenoids from Azadirachta Indica

Organic extracts of the leaves of Azadirachta indica A. Juss. yielded ten antitrypanosomal terpenoids. Three of these (1 – 3), are novel and are derivatives of nimbolide and nimbin. They were extracted from chloroform fraction of methanol extract. These compounds were found to exhibit strong antitrypanosomal activities against Trypanosoma brucei rhodesiense with MIC values ranging of 6.9, 15.6 and 7.8 µg/ml respectively and were more active than Cymerlarsan ( a standard drug), which had an MIC value of 187.5 µg/ml when tested against T. b. rhodesiense The structures were elucidated by spectroscopic methods including; NMR, MS, UV and IR.     

In vivo antitrypanosomal effects of some ethnomedicinal plants from Nupeland of north central Nigeria

Four medicinal plants Acacia nilotica, Bombax buonopozense, Terminalia avicennioides and Zanthoxylum zanthoxyloides traditionally used for treatment of sleeping sickness in Nupeland were investigated for in vivo antitrypanosomal activity. Methanol extracts of different parts of each plant (stem barks and fruits) were obtained and evaluated for their in vivo antitrypanosomal activities against Trypanosoma brucei brucei. Phytochemical screening of the methanol extracts of each plant were performed by standard procedures. Methanol extracts of A. nilotica (stem bark), B. buonopozense (stem bark), T. avicennioides (round fruit) and Z. zanthoxyloides (stem bark) were effective on trypanosomes. The extracts of A. nilotica and B. buonopozense exhibited antitrypanosomal effects at 200 and 300 mg/kg body weight respectively. Doses were able to clear the parasites from circulation within 6 and 7 days of treatment respectively with prolonging survival period of up to 30 days. While the extracts of T. avicennioides and Z. zanthoxyloides showed trypanostatic effects and could not clear the parasites completely. The methanol extracts of these plants contain metabolites that are associated with antitrypanosomal effects; therefore, these medicinal plants may be sources of new compounds that may be active against T. b. brucei. This study has also justified the claim that some medicinal plants of Nupeland possess antitrypanosomal activity and could be useful in the management of trypanosomiasis.     

Valeriana wallichii root extracts and fractions with activity against Leishmania spp

Leishmanial diseases, posing a public health problem worldwide, are caused by Leishmania parasites with a dimorphic life cycle alternating between the promastigote and amastigote forms. Promastigotes transmitted by the vector are transformed into amastigotes residing in the host tissue macrophages. Presently, new antiparasitic agents are needed against Leishmania donovani and Leishmania major, the respective organisms causing visceral and cutaneous leishmaniasis, since the available treatments are unsatisfactory due to toxicity, high cost, and emerging drug resistance. Over the years, traditional medicinal flora throughout the world enriched the modern pharmacopeia. Hence, roots of 'Indian Valerian' (Valeriana wallichii DC) were studied for its antileishmanial activity for the first time. The methanol and chloroform extracts showed activity against L. donovani promastigotes and both promastigotes and amastigotes of L. major. The most active fraction, F3, obtained from the chloroform extract, showed IC(50) at ～ 3-7 μg/ml against both the promastigotes and 0.3 μg/ml against L. major amastigotes. On investigation of the mechanism of cytotoxicity in L. donovani promastigotes, the 'hall-mark' events of morphological degeneration, DNA fragmentation, externalization of phosphatidyl serine, and mitochondrial membrane depolarization indicated that F3 could induce apoptotic death in leishmanial cells. Therefore, the present study revealed a novel and unconventional property of V. wallichii root as a prospective source of effective antileishmanial agents.     

In vitro antiplasmodial, antileishmanial and antitrypanosomal activities of selected medicinal plants used in the traditional Arabian Peninsular region

ABSTRACT: BACKGROUND: Worldwide particularly in developing countries, a large proportion of the population is at risk for tropical parasitic diseases. Several medicinal plants are still used traditionally against protozoal infections in Yemen and Saudi Arabia. Thus the present study investigated the in vitro antiprotozoal activity of twenty-five plants collected from the Arabian Peninsula. METHODS: Plant materials were extracted with methanol and screened in vitro against erythrocytic schizonts of Plasmodium falciparum, intracellular amastigotes of Leishmania infantum and Trypanosoma cruzi and free trypomastigotes of T. brucei. Cytotoxic activity was determined against MRC-5 cells to assess selectivity. The criterion for activity was an IC50 < 10 ug/ml (<5 ug/ml for T. brucei) and selectivity index of >4. RESULTS: Antiplasmodial activity was found in the extracts of Chrozophora oblongifolia, Ficus ingens, Lavandula dentata and Plectranthus barbatus. Amastigotes of T. cruzi were affected by Grewia erythraea, L. dentata, Tagetes minuta and Vernonia leopoldii. Activity against T. brucei was obtained in G. erythraea, L. dentata, P. barbatus and T. minuta. No relevant activity was found against L. infantum. High levels of cytotoxicity (MRC-5 IC50 < 10 ug/ml) and hence non-specific activities were noted in Cupressus empervirens, Kanahia lanifloraand Kniphofia sumarae. CONCLUSION: The results endorse that medicinal plants can be promising sources of natural products with antiprotozoal activity potential. The results support to some extent the traditional uses of some plants for the treatment of parasitic protozoal diseases.     

In vitro anti-plasmodial activity of some traditionally used medicinal plants against Plasmodium falciparum

The anti-plasmodial activity of different solvent extracts of Adhatoda vasica (root), Caesalpinia pulcherrima (leaf), Carica papaya (pulp), Erythroxylum monogynum (leaf), Lantana camara (whole plant), Ocimum sanctum (root) and Phyllanthus niruri (whole plant) were studied against Plasmodium falciparum. Of the 35 extracts tested, seven extracts showed good anti-plasmodial activity. Methanol extract of C. pulcherrima showed the lowest IC50 value (10.96 μg/mL) followed by methanol extract of A. vasica (IC(50)=11.1 μg/mL), chloroform extract of O. sanctum (IC(50)=11.47 μg/mL), methanol extract of E. monogynum (IC(50)=12.23 μg/mL), acetone extract of C. pulcherrima (IC(50)=12.49 μg/mL), methanol extract of O. sanctum and acetone extract of A. vasica (IC(50)=14.04 μg/mL). The results of the present study justify the use of these medicinal plants in traditional practice, and also, a further study on the isolation of anti-plasmodial molecules from their active crude extracts is in progress.     

Antiprotozoan activity of Brazilian marine cnidarian extracts and of a modified steroid from the octocoral <Emphasis Type="Italic">Carijoa riisei</Emphasis>

In the present investigation, we have evaluated the antileishmanial and antitrypanosomal activity of methanolic crude extracts obtained from eight species of cnidarians and of a modified steroid isolated from the octocoral Carijoa riisei. The antileishmanial activity of cnidarians crude extracts showed 50% inhibitory concentration (IC₅₀) values in the concentration range between 2.8 and 93.3 μg/mL. Trypomastigotes of Trypanosoma cruzi were less susceptible to the crude extracts, with IC₅₀ values in the concentration range between 40.9 and 117.9 μg/mL. The steroid (18-acetoxipregna-1,4,20-trien-3-one) displayed a strong antileishmanial activity, with an IC₅₀ value of 5.5 μg/mL against promastigotes and 16.88 μg/mL against intracellular amastigotes. The steroid also displayed mammalian cytotoxicity (IC₅₀ of 10.6 μg/mL), but no hemolytic activity was observed at the highest concentration of 12.5 μg/mL. The antileishmanial effect of the steroid in macrophages suggested other mechanism than macrophage activation, as no upregulation of nitric oxide was observed. The antitrypanosomal activity of the steroid resulted in an IC₅₀ value of 50.5 μg/mL. These results indicate the potential of cnidarian natural compounds as antileishmanial drug candidates.     

In vitro activity of extracts and isolated polyphenols from West African medicinal plants against Plasmodium falciparum

The aim of the study was to screen 11 selected traditional medicinal plants from West Africa for their in vitro antiplasmodial activity in order to determine the activity of single and of combination of plant extracts and to examine the activity of isolated pure compounds. Ethanolic and aqueous extracts of the 11 selected plants and pure compounds from Phyllanthus muellerianus and Anogeissus leiocarpus were tested in vitro against Plasmodium falciparum 3D7. Proliferation inhibitory effects were monitored after 48 h. Among the plants and pure compounds investigated in this study, geraniin from P. muellerianus, ellagic, gentisic, and gallic acids from A. leiocarpus, and extracts from A. leiocarpus, P. muellerianus and combination of A. leiocarpus with P. muellerianus affected the proliferation of P. falciparum most potently. Significant inhibitory activity was observed in combination of A. leiocarpus with P. muellerianus (IC(50)?=?10.8 μg/ml), in combination of A. leiocarpus with Khaya senegalensis (IC(50)?=?12.5 μg/ml), ellagic acid (IC(50)?=?2.88 μM), and geraniin (IC(50)?=?11.74 μM). In general growth inhibition was concentration-dependent revealing IC(50) values ranging between 10.8 and -40.1 μg/ml and 2.88 and 11.74 μM for plant extracts and pure substances respectively. Comparison with literature sources of in vivo and in vitro toxicity data revealed that thresholds are up to two times higher than the determined IC(50) values. Thus, the present study suggests that geraniin from P. muellerianus; ellagic acid, gallic acid, and gentisic acid from A. leiocarpus; and combination of extracts from A. leiocarpus with either P. muellerianus or K. senegalensis could be a potential option for malaria treatment.     

Anthelmintic activity of medicinal plants used in C?te d’Ivoire for treating parasitic diseases

Natural products play an important role in the discovery and development of new pharmaceuticals. In the present study, we assessed the anthelmintic properties of medicinal plants used in Cote d'Ivoire. Ethanolic extracts from 50 medicinal plants were tested in vitro against trematodes (Echinostoma caproni, Schistosoma mansoni) and nematodes (Ancylostoma ceylanicum, Heligmosomoides bakeri, Trichuris muris). Active extracts were evaluated for their cytotoxicity and followed up in vivo in mice harbouring adult S. mansoni, E. caproni and T. muris at single oral doses of 400 or 800 mg/kg. All extracts tested were active against at least one helminths species. Ten of the 65 extracts tested (15.4%) in vitro revealed activity against all helminths tested. Of 65 extracts tested in vitro at a concentration of 2 mg/ml, all caused death of schistosomula and 34.4% and 39.1% were lethal against adult S. mansoni and E. caproni 72 h post-incubation, respectively. The highest activity against A. ceylanicum in vitro was observed with Sclerocarya birrea at 2 mg/ml, which resulted in death of adult worms and inhibition of activity of third-stage larvae (L3). Of the extracts, 41.5% completely inhibited movement of H. bakeri L3 at minimal lethal concentration (MLC) values of 20-200 μg/ml 48 h post-incubation, and 15.4% paralysed adult H. bakeri at 200 μg/ml 72 h after incubation. Of the extracts, 19% resulted in death of adult T. muris at MLC values of 10-100 μg/ml. In vivo, none of the extracts tested revealed activity against E. caproni. Olax subscorpioidea achieved total and female worm burden reductions of 60% and 84%, respectively in S. mansoni-infected mice. Combretum mucronatum was the most active extracts in vivo against T. muris with a worm burden reduction of 85.3%. In conclusion, several of the medicinal plants used in C?te d'Ivoire are active against different helminths, hence might play a role in the treatment of helminthiases. Further studies are necessary to isolate the active components from these extracts.     

Predominant induction of kinetochore-containing micronuclei by extracts of diesel exhaust particulates in cultured human lymphocytes

The aneuploidy-inducing activity of extracts of diesel exhaust particulates from light duty (LD) and heavy duty (HD) engines was investigated in cultured peripheral blood lymphocytes of 8 healthy donors using the cytokinesis-block micronucleus test with the kinetochore labelling modification. A majority of the subjects tested showed a significant kinetochore-positive micronucleus induction after treatment with the highest dose (150 μg/ml) of LD extract, although some subjects also showed induction of kinetochore-negative micronuclei. Only one subject had significantly increased numbers of kinetochore-positive micronuclei at a dose of 400 μg/ml of HD extract. These results suggest that diesel extract, at least LD extract, possesses the ability to induce whole chromosome loss (aneuploidy) preferentially, although there are also chromosome breaks. © 1994 Wiley-Liss, Inc.     

Computerized tongue image segmentation via the double geo-vector flow

Background

Bupleurum marginatum Wall. ex DC (Apiaceae) is a perennial herb widely used in traditional Chinese and Kampo medicine for the treatment of various infectious diseases. The biological activities of B. marginatum have not been fully investigated. This study aims to investigate the antitrypanosomal, antimicrobial and antiviral activities of methanol (ME) and dichloromethane (DCM) extracts of B. marginatum aerial parts and the ability of both extracts to inhibit the growth of different cancer cell lines.

Methods

Phytochemical characterization of the extracts was performed by LC-MS profiling. The antitrypanosomal activity was evaluated using the resazurin method. The antimicrobial activity was assessed using agar diffusion and microdilution methods, and the minimum inhibitory concentration (MIC) values were determined. The antiviral activity was determined for 6.25, 12.5, and 50 μg/mL doses using a plaque reduction assay. Cytotoxicity was investigated in eight cancer cell lines (Caco-2, CCL-81, CCRF-CEM, COS-7, HL-60, MIA PaCa-2, MCF-7, and PANC-1) using the MTT assay and the caspase 3/7 activity was determined over the range of 62.5–1000 μg/mL.

Results

Phytochemical analyses resulted in the characterization of 15 components, mainly flavonoids and lignans. The DCM extract showed significant antitrypanosomal activity (IC₅₀: 36.21 μg/mL) and moderate activity against Streptococcus pyogenes (MIC value: 0.25 mg/mL). At a dose of 12.5 μg/mL, the DCM extract inhibited 73.6% of the plaque production by hepatitis A virus. CCRF-CEM cells were the most sensitive to both extracts (IC₅₀: 12.5–22.7 μg/mL). The cytotoxicity was mediated by induction of apoptosis (19-fold increase in the cellular caspase 3/7 level after treatment with the DCM extract at 1 mg/mL).

Conclusions

ME and DCM extract of B. marginatum showed anti-infective and antiproliferative effects.

     

Screening of antileishmanial activity from marine sponge extracts collected off the Tunisian coast

The present study reports on the in vitro antileishmanial activity of two Ircinidae (Dictyoceratida, Demospongiae, Porifera) Ircinia spinosula and Sarcotragus sp. Sampled from the east coast of Tunisia. The ethyl acetate, dichloromethane, and aqueous extracts were tested against Leishmania major promastigotes. The anti-proliferative activity was checked using different extracts concentration during 72 h. We found that the IC50 (sub-inhibitory concentration) values ranged from 1.39 to 264.67 μg/ml. The most active extract was that from sarcotragus sp dichloromethane extract. Microscopic observations showed that the extracts promoted cellular alterations and induce enlargement of the nucleus and modification of the parasite shape. These promising results in relation with in vitro antileishmanial activity open the way for complementary investigation in order to purify and identify active molecules.     

An ethanolic extract of leaves of <Emphasis Type="Italic">Piper betle</Emphasis> (Paan) Linn mediates its antileishmanial activity via apoptosis

An unprecedented increase in the incidence of unresponsiveness to antimonial compounds has highlighted the urgent need to develop new antileishmanial agents. The leaves of Piper betle (locally known as Paan) have long been in use in the Indian indigenous system of medicine for its antimicrobial properties but its antileishmanial potential has not been studied. Accordingly, an ethanolic extract of leaves of Piper betle (PB) was tested for its antileishmanial activity that was evidenced in both promastigotes and amastigotes, with IC₅₀ values of 9.8 and 5.45 μg/ml, respectively; importantly, it was accompanied by a safety index of >12-fold. This leishmanicidal activity of PB was mediated via apoptosis as evidenced by morphological changes, loss of mitochondrial membrane potential, in situ labeling of DNA fragments by terminal deoxyribonucleotidyltransferase-mediated deoxyuridine triphosphate nick end labeling, and cell-cycle arrest at the sub-G₀/G₁ phase. Taken together, the data indicate that PB has promising antileishmanial activity that is mediated via programmed cell death and, accordingly, merits consideration and further investigation as a therapeutic option for the treatment of leishmaniasis.     

Mangrove plants as a source of lead compounds for the development of new antiplasmodial drugs from South East coast of India

Malaria is the world's leading killer among the infectious diseases. The treatment of malaria is mystified by the challenges of widespread resistance of the malaria parasites to cheap and affordable antimalarial drugs. The present study was made in an attempt to identify the in vitro antiplasmodial activity against mangrove plant parts. (Avicennia marina, Acanthus ilicifolius, Bruguiera cylindrica, Excoecaria agallocha, Rhizophora apiculata, and Rhizophora mucronata mangrove plant extracts exhibited in vitro antiplasmodial activity against Plasmodium falciparum). Of the selected mangrove plant parts, the bark extract of A. marina exhibited minimum concentration of inhibitory activities IC(50) 49.63 μg.ml(-1). The leaf extract of A. marina, the hypocotyl extract of B. cylindrica, the leaf extract of E. agallocha, the flower extract of R. mucronata, and the hypocotyl extract of R. apiculata showed IC(50) values between 50 and 100 μg.ml(-1). Statistical analysis reveals that significant antiplasmodial activity (P<0.05) was observed between the concentrations and time of exposure. The chemical injury to erythrocytes was also carried out, and it shows that there were no morphological changes in erythrocytes by the ethanolic extract of mangrove plants after 48 h of incubation. The in vitro antiplasmodial activity might be due to the presence of alkaloids, carboxylic acids, coumarins, saponins, flavonoids, xanthoproteins, tannins, phenols, sugars, resins, steroids, and proteins in the ethanolic extracts of mangrove plants. It is concluded from the present study that the ethanolic extracts of mangrove plant parts of A. marina possess lead compounds for the development of antiplasmodial drugs.     

In vitro antiplasmodial activity of some medicinal plants of Burkina Faso

Malaria remains a major public health problem due to the emergence and spread of Plasmodium falciparum drug resistance. There is an urgent need to investigate new sources of antimalarial drugs which are more effective against Plasmodium falciparum. One of the potential sources of antimalarial drugs is traditional medicinal plants. In this work, we studied the in vitro antiplasmodial activity of chloromethylenic, methanolic, and MeOH/H₂O (1/1) crude extracts and decoction obtained from eight medicinal plants collected in Burkina Faso and of total alkaloids for five plants. Extracts were evaluated in vitro for efficacy against Plasmodium falciparum strain K1, which is resistant to chloroquine, pyrimethamine and proguanil using the fluorescence-based SYBR Green I assay. The antiproliferative activity on human-derived hepatoma cell line HepG2 and Chinese hamster ovary (CHO) cells was evaluated using the 3-[4,5-dimethylthyazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) test in order to determine the selectivity index. Among the plant extracts tested for in vitro antiplasmodial activity, 16 were considered to be inactive (with IC₅₀?>?10 μg/ml), six showed a moderate activity (5?<?IC₅₀?≤?10 μg/ml), and six were found to have a good in vitro activity with IC₅₀ value?≤?5 μg/ml. The highest antiplasmodial activity was found for extracts from: the alkaloid leaf extract and the chloromethylenic extracts of Combretum fragrans (IC₅₀?=?3 μg/ml, IC₅₀?=?5 μg/ml), the total alkaloids and the chloromethylenic leaf extracts of Combretum collinum (IC₅₀?=?4 μg/ml), the MeOH/H₂O leaf extract of Terminalia avicennioides (IC₅₀?=?3.5 μg/ml), and the alkaloid leaf extract of Pavetta crassipes (IC₅₀?=?5 μg/ml). Three other extracts showed moderate antiplasmodial activity (5?<?IC₅₀?≤?10 μg/ml): Terminalia avicennioides and Combretum fragrans methanolic extracts and Acacia kirkii alkaloid leaf extract (IC₅₀?=?6.5, 9 and 10 μg/ml respectively). The Terminalia avicennioides crude MeOH/H₂O (80:20 v/v) extract of the leaves was submitted to a successive liquid/liquid extraction with ethylacetate and n-butanol respectively. The extracts were investigated for in vitro antiplasmodial activity and antioxidant properties using DPPH^●, ABTS⁺ and FRAP methods. The ethylacetate extract showed the best antiplasmodial activity (7 μg/ml) and the active constituent was isolated as ellagic acid by bioguided fractionation with an IC₅₀?=?0.2 μM on Plasmodium falciparum and SI?=?152. Besides, Terminalia avicennioides leaf extract and ellagic acid showed a good antioxidant activity. Our finding confirms the importance of investigating the antimalarial activity of plant species used in traditional medicine. Overall, two plants belonging to the Combretaceae family, Combretum fragrans and Combretum collinum appeared to be the best candidates and will be further investigated for their antiplasmodial properties, in order to isolate the molecules responsible for the antiplasmodial activity.     

In vitro antioxidant and anticancer activity of young Zingiber officinale against human breast carcinoma cell lines

Background

Saponins isolated from plant sources have a number of traditional and industrial applications. Saponins have pharmacological effects like anti-inflammatory, molluscicidal, antimicrobial, antispasmodic, antidiabetic, anticancer, anticonvulsant, anthelmintic, antitussive and cytotoxic activities. The current work describes the anthelmintic and cytotoxic activities of crude saponins of Achillea Wilhelmsii and Teucrium Stocksianum as these plants are rich with saponins.

Methods

Brine shrimp cytotoxic activity of crude saponins was determined by Meyer et al. (1982) at test concentrations of 1000 μg/ml, 100 μg/ml, 10 μg/ml, 7.5 μg/ml, 5.0 μg/ml, 2.5 μg/ml and 1.25 μg/ml. Percentage mortality of test concentrations was determined. Similarly, in vitro anthelmintic activity was determined against roundworms, tapeworms and earthworms. Albendazole and piperazine citrate at concentration 10 mg/ml were used as standard anthelmintic drugs.

Results

Crude saponins of Achillea wilhelmsii (CSA) and Teucrium stocksianum (CST) had, respectively, cytotoxic activity with LC₅₀ values 2.3 ± 0.16 and 5.23 ± 0. 34 μg/ml. For in vitro anthelmintic activity, time for paralysis and death of parasites (parasiticidal activity) was noted. At concentration 40 mg/ml, crude saponins of Achillea wilhelmsii are 1.96 and 2.12 times more potent than albendazole against Pheretima posthuma and Raillietina spiralis, respectively. Similarly, at concentration 40 mg/ml, crude saponins of Teucrium stocksianum (CST) has 1.89, 1.96 and 1.37 times more parasiticidal activity than albendazole against Pheretima posthuma, Raillietina spiralis and Ascardia galli, respectively.

Conclusion

Crude saponins of Achillea wilhelmsii and Teucrium stocksianum have cytotoxic and anthelmintic activity. The crude saponins may be excellent sources of cytotoxic and anthelmintic constituents that warrant its isolation and purification for new drug development.     

Antileishmanial potential of a marine sponge, <Emphasis Type="Italic">Haliclona exigua</Emphasis> (Kirkpatrick) against experimental visceral leishmaniasis

In this study, we are reporting antileishmanial activity of a marine sponge Haliclona exigua, belonging to phylum Porifera. The crude methanol extract and its three fractions were tested both in vitro and in vivo. The crude extract exerted almost complete inhibition of promastigotes at 50 μg/ml and 76.4 ± 6.5% inhibition of intracellular amastigotes at 100 μg/ml concentration with IC₅₀ values of 18.6 μg/ml and 47.2 μg/ml, respectively. When administered to Leishmania donovani infected hamsters at a dose of 500 mg/kg × 5, p.o., it resulted in 72.2 ± 10.4% inhibition of intracellular amastigotes. At a lower dose (250 mg/kg), it exhibited 43.9 ± 5.1% inhibition. Among the fractions, highest antileishmanial activity both in vitro (>90%) and in vivo (60.9 ± 18.3%) was observed in n-butanol (soluble) fraction with IC₅₀ values of 8.2 μg/ml and 31.2 μg/ml against promastigotes and intracellular amastigotes, respectively. Hexane fraction also showed comparatively good activity against both the stages of parasites in vitro but was moderately active in leishmania-infected hamsters. Chloroform fraction resulted in 45 ± 10.2% inhibition in vivo at a dose of 500 mg/kg × 5, p.o., whereas it was inactive in vitro. n-Butanol (insoluble) fraction was inactive both in vitro and in vivo. Araguspongin C, an alkaloid isolated from n-butanol (soluble) fraction exhibited moderate inhibition of promastigotes and intracellular amastigotes at 100 μg/ml but showed weak antileishmanial action in vivo. Our findings indicate that this marine sponge has the potential to provide new lead toward development of an effective antileishmanial agent and, hence, calls for more exhaustive studies for exploiting the vast world of marine resources to combat the scourge of several parasitic diseases.     

Anticholinesterase activity of endemic plant extracts from Soqotra

A total of 30 chloroform and methanol extracts from the following endemic Soqotran plants Acridocarpus socotranus Olive, Boswellia socotranao Balf.fil, Boswellia elongata Balf. fil., Caralluma socotrana N. Br, Cephalocroton socotranus Balf.f, Croton socotranus Balf. fil.., Dendrosicycos socotrana Balf.f., Dorstenia gigas Schweinf. ex Balf. fil., Eureiandra balfourii Cogn. & Balf. fil., Kalanchoe farinaceae Balf.f, Limonium sokotranum (Vierh) Radcl. Sm), Oldenlandia pulvinata, Pulicaria diversifolia (Balf. and Pulicaria stephanocarpa Balf. were screened for their acetylcholinesterase inhibitory activity by using in vitro Ellman method at 50 and 200 μg/ml concentrations. Chloroform extracts of Croton socotranus, Boswellia socotrana, Dorstenia gigas, and Pulicaria stephanocarpa as well as methanol extracts of Eureiandra balfourii exhibited inhibitory activities higher than 50 % at concentration of 200 μg. At a concentrations of 50 μg, the chloroform extract of Croton socotranus exhibited an inhibition of 40.6 %.     

Toxicity of Brazilian plant seed extracts to two strains of Aedes aegypti (Diptera: Culicidae) and nontarget animals

Seed ethanolic extracts of 21 Brazilian plants were evaluated for ovicidal, larvicidal, and pupicidal activities against insecticide-susceptible (SS) and field-collected (FC) strains of Aedes aegypti (L.) (Diptera: Culicidae), as well as for their effects on nontarget organisms. Myracrodruon urundeuva Fr. Allemao extract was highly toxic to both mosquito strains. Schinopsis brasiliensis Engler extract showed low toxicity and was 38-68 times less toxic to Ae. aegypti larvae than was M. urundeuva extract. The pupicidal activity (LC50) of 14 plant seed extracts ranged between 9 and 433/g/ml, and toxicities were comparable to both mosquito strains. Piptadenia moniliformis Benth. and Luetzelburgia auriculata (Allemao) Ducke extracts showed the highest activities against pupae of FC and SS strains. None of the extracts showed 100% ovicidal activity. In addition, the active extracts did not show high acute toxicity to mice (LD50 > 1.5 g/kg), except that of Enterolobium contortisiliquum (Vell.) Morong. Most of the active extracts exhibited low toxicity against brine shrimp (Artemia sp.) nauplii. The extracts of M. urundeuva, P. moniliformis, and L. auriculata are promising sources of recognized classes of insecticidal compounds with good selectivity against immature stages of Ae. aegypti.     

Vernonia cinerea L. scavenges free radicals and regulates nitric oxide and proinflammatory cytokines profile in carrageenan induced paw edema model

In this study, we evaluated the anti-oxidant and anti-inflammatory activities of the medicinal plant, Vernonia cinerea L (Asteraceae) using in vitro as well as in vivo models. Methanolic extract of Vernonia cinerea was found to scavenge the hydroxyl radical generated by Fenton reaction (IC₅₀130 μg/ml), Superoxide generated by photo reduction of riboflavin (IC₅₀190 μg/ml) and inhibited lipid peroxidation significantly (IC₅₀130.5 μg/ml). The drug also scavenged nitric oxide (IC₅₀210 μg/ml). Intraperitoneal administration of Vernonia cinerea was found to inhibit the PMA induced Superoxide generation in mice peritoneal macrophages. The administration of Vernonia cinerea to mice significantly increased the levels of catalase, superoxide dismutase, glutathione, glutathione peroxidase and glutathione-S transferase in blood and liver, whereas lipid peroxidation activity was significantly decreased. It was also found that Vernonia cinerea extract significantly inhibited carrageenan induced inflammation, compared with control models. Down regulation of pro-inflammatory cytokine level and gene expression were also support the above result.