Synthesis and evaluation of toxicity and antimicrobial activity of rifampicin associated with iron oxide nanoparticles

Rifampicin has broad-spectrum antimicrobial activity, but it can cause nephrotoxic and hepatotoxic damage because high doses are required. Nanosystems emerge as a perspective to improve the transport systems of this drug. In this work, iron oxide nanoparticles were synthesised, functionalized with lauric acid, and rifampicin was incorporated into the nanosystem. The samples were characterized by spectroscopic techniques: electronics in the visible ultraviolet region (UV-vis), vibrational absorption in the infrared region (IR), X-ray diffractometry (XRD), and dynamic light scattering (DSL). The toxicity of the nanocompounds and the antimicrobial activity against Staphylococcus aureus ATCC 25923 were studied by the Artemia salina lethality and disc diffusion techniques, respectively. As a result, IR analysis showed characteristic vibrations of laurate and rifampicin on the surface of the nanosystem. The presence of magnetic iron oxide was confirmed by XRD and the mean diameter of the crystallites was 8.37 nm. The hydrodynamic diameter of rifampicin associated with the nanosystem was 402 nm and that of the nanosystem without rifampicin was 57 nm. The compounds did not show toxicity to Artemia salina and the in vitro antimicrobial activity against Staphylococcus aureus was slightly decreased when rifampicin was associated with the nanosystem. In general terms, the results showed that iron oxide nanoparticles showed no toxicity and reduced the toxicity of rifampicin by 41.54% when carried compared to free rifampicin. Therefore, magnetic iron oxide nanoparticles may have the potential to act as a platform for associated drugs.

Mercury chloride toxicity attenuation of the Brine Shrimp Artemia Salinaafter treatment with Mercurius corrosivusas isotherapic

Isotherapics preparedfromtoxic substances have been described as attenuation factors for heavy metal intoxicationin aquatic animals. Herein, Artemia salinaand mercury chloride were usedas a model to identify treatment-related bioresilience. The aim was to describe the effects of Mercurius corrosivus(MC) in different potencies on Artemia salinacyst hatching and on mercury bioavailability. Artemia salinacysts were exposed to 5.0 µg/mL of mercury chloride during the hatching phase. MC6cH, 30cH, and 200cHwere prepared and poured into artificial seawater. Different controls were used (nonchallenged cysts and challenged cysts treated with water, succussed water, and Ethilicum 1cH). Four series of nine experiments were performed for4 weeks to evaluate the percentage of cyst hatchingconsidering all moon phases. Soluble total mercury (THg) levels and precipitated mercury content were also evaluated. Solvatochromic dyes were used to check for eventual physicochemical markers of MCbiological activity. Two-way analysis of variance (ANOVA) with mixed modelswas used for evaluating the effect of different treatments andthe simultaneous influence of the moon phases on the cystshatching rate, at both observation times (24 and 48 hours).When necessary, outliers were removed, using the Tukeycriterion.Thelevel of significance αwas set at 5%. Significant delay (p<0.0001) in cyst hatching was observed after treatment with MC30cH, compared with the controls. An increase inTHg concentration in seawater (p<0.0018) and of chlorine/oxygen ratio (p<0.0001) in suspended micro-aggregateswas also seen, with possiblerelation with mercury bioavailability. Specific interaction of MC30cH with the solvatochromic dye ET33 (p<0.0017) was found. The other observed potencies of Mercurius corrosivus6 and 200 cH were not significant in relation to the observed groups.The results werepostulated as being protective effects of MC30cH on Artemia salina, by improving its bioresilience.

Toxicity evaluation of the ethanolic Jambu bol [Syzygium malaccense (L.) Merr. and Perry] leaves extract and mechanisms underlying its antibacterial action

Aims@#Many plants and their derivatives are widely used in food manufacturing because of their biological activities. They play a significant role as food additives to control microbial growth and the occurrence of oxidation reactions. Syzygium malaccense L. is a well-known plant with biological activities such as antimicrobial and antioxidant activities. Thus, the aims of this study were to evaluate the toxicity of the ethanolic leaves extract of S. malaccense and to study its antibacterial mode of action.@*Methodology and results@#The toxicity assessment of S. malaccense leaves extract was determined using the brine-shrimp larvae model. The action mechanisms against bacterial membrane were determined by studying the intracellular material leakage by means of nucleic acid (DNA and RNA) release, crystal violet dye uptake and cellular protein leakage. The present findings proved the extract's safety as indicated by a high dose of 7.402 mg/mL for lethal concentration (LC50) against brine-shrimp larvae. On the other hand, the ethanolic extract caused a severe membrane permeability towards all the tested bacteria as indicated by the increased intracellular material leakage in a concentration-dependent manner.@*Conclusion, significance and impact of study@#The current study provides valuable information regarding the safety and antibacterial action mechanism of S. malaccense ethanolic leaves extract, thus paving the way for its utilization as a natural preservative in a wide range of food products.

Low cytotoxicity, and antiproliferative activity on cancer cells, of the plant Senna alata (Fabaceae) / Baja citotoxicidad, y actividad antiproliferativa sobre las células cancerosas, de la planta Senna alata (Fabaceae)

Introduction: The leaves of Senna alata from the Fabaceae family have been used in folk medicine for the cure of skin disease. In this study, we tested the extract and fractions on brine shrimp lethality test and antiproliferative activity on cancer and normal cell lines. Objective: In this study, we assessed the cytotoxicity of S. alata using brine shrimp test and two cell lines. Methods: The 80 % ethanolic leaf extract and its fractions were examined for possible cytotoxic effect using sulforhodamine B (SRB) cytotoxicity assay towards breast cancer (MCF-7), normal (MCF10A) cell lines, and brine shrimp lethality test (BSLT). Results: The brine shrimp lethality bioassay exhibits no cytotoxicity even at high concentration (5 000 µg/mL). The LC50 for dichloromethane, chloroform, butanol, and aqueous were > 1 000 µg/mL (non-toxic). The IC50 for in vitro SRB cytotoxicity against MCF-7 for n-hexane was 0.013 µg/mL, which was considered highly toxic, while dichloromethane and chloroform recorded at 47.11 and 57.61 µg/mL, respectively after 72 hours exposure time although there was no cytotoxicity found on the normal cell line. Conclusion: This study shows that S. alata crude ethanolic leaf extract and its fractions potentially contain significant bioactive compounds that are safe from adverse effects, which proves the therapeutic application of S. alata in traditional remedy.

Introducción: Las hojas de Senna alata de la familia Fabaceae se han utilizado en la medicina popular para la cura de enfermedades de la piel. En este estudio, probamos el extracto de la planta en líneas celulares normales y cancerosas. Objetivo: Evaluamos la citotoxicidad de S. alata usando una prueba del camarón Artemia y la actividad antiproliferativa. Métodos: El extracto de hoja etanólico al 80 % y sus fracciones se examinaron en busca de un posible efecto citotóxico utilizando un ensayo de citotoxicidad de sulforrodamina B (SRB) frente a líneas celulares de cáncer de mama (MCF-7), normales (MCF10A) y prueba de letalidad del camarón Artemia (BSLT). Resultados: El bioensayo de letalidad del camarón Artemia no presenta citotoxicidad incluso en alta concentración (5 000 µg/mL). La CL50 para diclorometano, cloroformo, butanol y acuoso fue > 1000 µg/mL (no tóxico). La CI50 para la citotoxicidad in vitro de SRB contra MCF-7 para n-hexano fue de 0.013 µg/mL, que se consideró altamente tóxica, mientras que el diclorometano y el cloroformo registraron 47.11 y 57.61 µg/mL, respectivamente, después de 72 horas de tiempo de exposición, aunque no hubo citotoxicidad encontrada en la línea celular normal. Conclusión: Este estudio muestra que el extracto de hoja etanólico crudo de S. alata y sus fracciones contienen potencialmente compuestos bioactivos significativos que están a salvo de efectos adversos, lo que demuestra la aplicación terapéutica de S. alata como remedio tradicional.

Identification and Production of Beauvericin by Fusarium subglutinansand F. sacchari from Sugarcane

Abstract Fusarium is producing several important mycotoxins including beauvericin (BEA). Two species of Fusarium viz. F. subglutinans and F. sacchari cause the Pokkahboeng disease of sugarcane. The studies on the occurrence and toxicity of BEA are scarce. Therefore, this study aimed to identify the isolates of Fusarium and detect their ability to produce BEA. The toxicity of BEA was also tested on brine shrimp Artemia salina. Many isolates of Fusarium were isolated from the infected plants of sugarcane in Malaysia. We identified the species of Fusarium according to their morphological characteristics. The capability of Fusarium isolates for producing the BEA was estimated by using a thin layer chromatography. The toxicity bioassay of BEA was conducted on the brine shrimp larvae. The results were identified on F. subglutinans and F. sacchari in 55 isolates of Fusarium. All isolates demonstrated the ability to produce BEA. Interestingly, BEA exhibited variation in toxicity between low toxic to very higher toxicity 100%. F. subglutinans and F. sacchari were able to produce BEA and possibly BEA may be causing toxicity in the host tissue and may be acting as a potential pathogenicity factor. Therefore, we consider BEA as an interesting factor in determining the virulence of fusarium isolate.

Toxicity and phytochemistry of eight species used in the traditional medicine of sul-mato-grossense, Brazil / Toxicidade e fitoquímica de oito espécies usadas na medicina tradicional sul-mato-grossense, Brasil

Abstract The Brazilian Cerrado has several botanical species for medicinal purposes used by traditional communities and many of these plants are not included in the list of Medicinal Plants Research Program of Central Medicines. The purpose of this study was the phytochemical screening and toxicology bioassay front of Brine shrimp L. of ethanolic extracts of eight species of plants used in folk medicine of Campo Grande, Mato Grosso do Sul, Brazil. The ethanolic extracts were submitted to phytochemical screening, determination of phenolic compounds and flavonoids. Toxicological assays were carried front of Brine shrimp according to standard methodology. The analysis TLC and HPLC-DAD confirmed the predominance of phenolic compounds and derivatives, specifically for the quercetin. The most toxic was the C. affinis DC. with death at all concentrations, the A. humile A. St. Hil. showed no mortality and the other species showed intermediate toxicity. The extracts of the investigated species are rich in phenolic compounds and derivatives, specifically quercetin, and feature toxicity between moderate to high, a fact that requires attention, since much of the traditional communities rely on herbal drugs in its raw form with preventive and curative purpose, meeting the basic health care.

Resumo O Cerrado brasileiro possui diversas espécies botânicas com fins medicinais utilizadas por comunidades tradicionais e muitas dessas plantas não estão incluídas na lista do Programa de Pesquisa de Plantas Medicinais da Central de Medicamentos. O objetivo deste estudo foi a triagem fitoquímica e o bioensaio toxicológico frente ao Brine shrimp L. de extratos etanólicos de oito espécies de plantas utilizadas na medicina popular de Campo Grande, Mato Grosso do Sul. Os extratos etanólicos foram submetidos à triagem fitoquímica, determinação de compostos fenólicos e flavonoides. Os ensaios toxicológicos foram realizados frente ao Brine shrimp de acordo com a metodologia padrão. A análise de cromatografia de camada delgada e HPLC-DAD confirmou a predominância de compostos fenólicos e derivados, especificamente para a quercetina. O mais tóxico foi o C. affinis DC. com a morte em todas as concentrações, o A. humile A. St. Hil. não apresentou mortalidade e as demais espécies apresentaram toxicidade intermediária. Os extratos das espécies investigadas são ricos em compostos fenólicos e derivados, especificamente a quercetina e apresentam toxicidade entre moderada a alta, fato que requer atenção, pois grande parte das comunidades tradicionais conta com fitoterápicos em sua forma bruta com preventivo e finalidade curativa, atendendo aos cuidados básicos de saúde.

In silico and in vitro cytotoxicity profile of hydroalcoholic extract/ fraction(s) of Pachygone ovata

Medicinal plants have been used in the past for the treatment of diseases and continue to be an important reservoirfor the development of new drugs. With the increasing burden of cancer globally, there is a need to find neweranticancer agents. The process of identification and evaluation of cytotoxic molecules from plants can be achievedconveniently by using simple yet reliable screening models and combining with in silico techniques. Pachygone ovata,least explored plant from Menispermaceae family, is known to be rich in alkaloids. This study aimed to identify thecytotoxic constituents from Pachygone ovata through bioactivity-guided fractionation using Brine shrimp lethalitybioassay as a screening model. The active fraction in this assay was evaluated for its in vitro cytotoxic activity onhuman tumor cell lines. Some reported alkaloids were studied for their binding affinities with topoisomerase II bymolecular docking. The study revealed the cytotoxic constituents from P. ovata. The study also revealed alkaloids withhigher binding affinity with topoisomerase II, and the scope for further use leads to the development of new drugs.

Xylaroisopimaranin A, a New Isopimarane Derivative from an Endophytic Fungus Xylaralyce sp

Five secondary metabolites, including a new isopimarane derivative xylaroisopimaranin A (1), were isolated from the endophytic fungus Xylaralyce sp. (HM-1), and their structures were elucidated by 1D, 2D NMR, MS and CD spectra. Their bioactivities were performed to antibacterial, Hep G2 cells cytotoxicity and brine shrimp inhibition. The biological evaluation results showed that the xylaroisopimaranin A (1), xylabisboein B (2), griseofulvin (3) , 5-methylmellein (4) and mellein-5-carboxlic acid (5) displayed no significant Hep G2 cells cytotoxicity and antibacterial acitivity, but they inhibited the brine shrimp with IC₅₀ from 0.5 to 25 µmol/mL.

Toxicity of the feathers of Yellow Grosbeak, Pheucticus chrysopeplus (Passeriformes: Cardinalidae), a chemically defended neotropical bird / Toxicidad de las plumas del Picogrueso amarillo, Pheucticus chrysopeplus (Passeriformes: Cardinalidae), un ave neotropical con defensa química

Abstract Chemical defense is a widespread mechanism on many animals and plants. However, just a few cases are known for avian species. In this study we evaluate the toxicity of Pheucticus chrysopeplus feather extract via lethality test with brine shrimp (Artemia salina) as an in vivo model. Mortality of A. salina was evaluated after 24 hour exposure to artificial seawater, methanol, and the methanolic feather extract. Kruskal-Wallis test showed a significant difference in mortality between treatments (X2 = 65.25, P < 0.0001, n = 50). With this we describe P. chrysopeplus as the first known toxic avian species of Guatemala and Central America, raising awareness about its conservation and the identification of the toxic substance present in its feathers. We also highlight the possible mimicry mechanism taking part between P. chrysopeplus and two sympatric oriole species (Icterus pectoralis and I. pustulatus).(AU)

Resumen La defensa química es un mecanismo que se encuentra presente en varios animales y plantas. Sin embargo, pocos casos son conocidos para especies de aves. En este estudio evaluamos la toxicidad de extractos de plumas de Pheucticus chrysopeplus con un ensayo de letalidad utilizando artemia (Artemia salina) como modelo in vivo. La mortalidad de A. salina se evaluó luego de ser expuesta por 24 horas a agua marina artificial, metanol y extracto metanólico de plumas de P. chrysopeplus. La prueba de Kruskal-Wallis mostró que existe una diferencia significativa entre los porcentajes de mortalidad de los tratamientos evaluados (X2 = 65.25, P < 0.0001, n = 50). Con esto, describimos a P. chrysopeplus como la primera especie de ave tóxica reportada para Guatemala y Centroamérica, resaltando la importancia de su conservación, así como la identificación de la sustancia tóxica presente en sus plumas. También destacamos el posible mecanismo de mimetismo que podría estar ocurriendo entre P. Chrysopeplus y dos especies simpátricas de orioles (Icterus pectoralis e I. pustulatus).(AU)

Antibacterial activity and toxicity of Duckweed, Lemna minor L. (Arales: Lemnaceae) from Malaysia

Aims@#New therapeutics are needed to ease the prevailing waterborne disease, and one of the alternatives is by exploring the natural compounds with antimicrobial properties. Duckweed, Lemna sp. is recorded as a medicinal herb that known to have antifungal and antibacterial activities towards several fungi and bacteria. Suitability of duckweed (Lemna minor) as an antibacterial resource against selected waterborne bacteria were evaluated in terms of its antibacterial activity and toxicity.@*Methodology and results@# Antibacterial activity of the duckweed methanolic extract was tested against 11 selected waterborne bacteria using disc diffusion, minimum inhibition concentration (MIC) and minimum bactericidal concentration (MBC) assay. Brine shrimp lethality assay was used to determine the toxicity of this extract. The lethal concentrations of plant extract resulting in 50% mortality of the brine shrimp (LC50) were then determined.@*Conclusion, significance and impact of study@#Results showed that duckweed extract exhibited bacteriostatic and bactericidal against the selected bacteria activity at the concentration of MIC = 1.8-2.0 mg/mL and MBC ≥ 2.0 mg/mL. This study shows that methanolic extract of L. minor may contain bioactive compounds against bacteria and potential therapeutic effect. The crude extract is slightly toxic and may not safe to be used in high concentration but is valuable in further study as a potential antitumor agent.

Toxicity and phytochemistry of eight species used in the traditional medicine of sul-mato-grossense, Brazil

Abstract The Brazilian Cerrado has several botanical species for medicinal purposes used by traditional communities and many of these plants are not included in the list of Medicinal Plants Research Program of Central Medicines. The purpose of this study was the phytochemical screening and toxicology bioassay front of Brine shrimp L. of ethanolic extracts of eight species of plants used in folk medicine of Campo Grande, Mato Grosso do Sul, Brazil. The ethanolic extracts were submitted to phytochemical screening, determination of phenolic compounds and flavonoids. Toxicological assays were carried front of Brine shrimp according to standard methodology. The analysis TLC and HPLC-DAD confirmed the predominance of phenolic compounds and derivatives, specifically for the quercetin. The most toxic was the C. affinis DC. with death at all concentrations, the A. humile A. St. Hil. showed no mortality and the other species showed intermediate toxicity. The extracts of the investigated species are rich in phenolic compounds and derivatives, specifically quercetin, and feature toxicity between moderate to high, a fact that requires attention, since much of the traditional communities rely on herbal drugs in its raw form with preventive and curative purpose, meeting the basic health care.

Resumo O Cerrado brasileiro possui diversas espécies botânicas com fins medicinais utilizadas por comunidades tradicionais e muitas dessas plantas não estão incluídas na lista do Programa de Pesquisa de Plantas Medicinais da Central de Medicamentos. O objetivo deste estudo foi a triagem fitoquímica e o bioensaio toxicológico frente ao Brine shrimp L. de extratos etanólicos de oito espécies de plantas utilizadas na medicina popular de Campo Grande, Mato Grosso do Sul. Os extratos etanólicos foram submetidos à triagem fitoquímica, determinação de compostos fenólicos e flavonoides. Os ensaios toxicológicos foram realizados frente ao Brine shrimp de acordo com a metodologia padrão. A análise de cromatografia de camada delgada e HPLC-DAD confirmou a predominância de compostos fenólicos e derivados, especificamente para a quercetina. O mais tóxico foi o C. affinis DC. com a morte em todas as concentrações, o A. humile A. St. Hil. não apresentou mortalidade e as demais espécies apresentaram toxicidade intermediária. Os extratos das espécies investigadas são ricos em compostos fenólicos e derivados, especificamente a quercetina e apresentam toxicidade entre moderada a alta, fato que requer atenção, pois grande parte das comunidades tradicionais conta com fitoterápicos em sua forma bruta com preventivo e finalidade curativa, atendendo aos cuidados básicos de saúde.

Environmental biotoxicity screening of some pyrrole and 1,4-dihydropyridine heterocyclic derivatives.

Synthesis of pyrrole 1-3 and 1,4-dihydropyridine derivatives 4-6 were prepared from condensation method and synthesized compounds were screened for environmental biotoxicity such as Brine shrimp cytotoxicity, Ichthyotoxic, Larvicidal and Nematicidial activities. Among the compounds 3 and 6 shows that highly toxic (LD50: 8.72 and 12.30 μg/mL) against Brain shrimp cytotoxic screening and compound 3 and 6 was highly toxicity ( LD50 : 5.01 and 7.75 μg/mL) against Antifeedant screening (ichthyotoxic profile). The compounds 3 and 6 was highly active (LD50: 12.88 μg/mL, and 14.79 μg/mL) against Larvicidal activity and compound 3 and 6 was highly active (LD50 : 8.20 μg/mL, and 7.43 μg/mL) against Nematicidal activity.

Evaluation of cytotoxic and antioxidant activity of different fractions of methanolic extract of Baccaurea ramiflora (Lour.) fruits.

Chloroform and petroleum ether soluble fractions of the crude methanolic extract of the fruits of Baccaurea ramiflora (Lour.) have been investigated for the evaluation of cytotoxic and antioxidant activity. Brine shrimp lethality bioassay was used to evaluate the cytotoxic activity and free radical scavenging activity method was used to evaluate antioxidant activity. In brine shrimp lethality bioassay, the chloroform soluble fraction showed greater cytotoxic activity (LC50 value 74.2 μg/ml) than petroleum ether soluble fraction (LC50 value 129 μg/ml) compared to the standard drug vincristine sulfate (LC50 value 0.54 μg/ml). In free radical scavenging activity method (DPPH assay method), the chloroform soluble fraction showed greater antioxidant activity (IC50 value 49.78 μg/ml) than petroleum ether soluble fraction (IC50 value 75.31 μg/ml) compared to the standard antioxidant butylated hydroxytoluene (IC50 value 24.51μg/ml). This study reveals that Baccaurea ramiflora fruit possesses cytotoxic and antioxidant activity hence can be a potential source for the isolation of active principle(s) for different therapies.

Phytochemical Analysis, Toxicity and Cytotoxicity Evaluation of Dendropthoe Pentandra Leaves Extracts.

Dendrophthoe pentandra known as mistletoe is a semi-parasitic plant with traditional claims for some medicinal properties. This research was done to determine phytochemical constituents of Dendropthoe petandra (DP) leaves extract, to evaluate toxicity of extracts by brine shrimp lethality test (BSLT) and to confirm cytotoxicity activity of DPME against various normal cell lines. The most potent extract was then evaluated by GC-MS. DP leaves that have been extracted with petroleum ether (DPPEE), methanol (DPME) and water (DPWE) were screened for phytochemical constituents. BSLT was carried out to determine the lethality concentration that kills 50% of tested population (LC50). The cytotoxicity was assessed by Methylene Blue Assay (MBA) that evaluates the inhibition concentration for cell growth by 50% (IC50). The normal cell lines used were MDCK, L929 and Vero. Phytochemical analysis revealed the presence of alkaloid, flavonoid, saponin, tannin and terpenoid in those extracts. Highest total phenolic content was found in DPME (471.63±2.02 mg GAE/g). BSLT have determined the lowest LC50 value is 2.74±1.23 ppm in DPME. No IC50 detected when MDCK, L929 and Vero cell line were treated with all extracts. Therefore, this can be concluded that DP extracts did not show any harmful effects towards MDCK, L929 and Vero cell lines although the DPME, DPPEE and DPWE are toxic towards brine shrimp. Hexadecanoic acid, methyl ester and 9,12,15-Octadecatrienoic acid, methyl ester are among compounds present in DPME. Further studies using mammalian cancer cell lines should be conducted on DP extracts to know if they posses anticancer potential.

Evaluation of cytotoxic and antioxidant activity of different fractions of methanolic extract of Baccaurea ramiflora (Lour.) fruits.

Chloroform and petroleum ether soluble fractions of the crude methanolic extract of the fruits of Baccaurea ramiflora (Lour.) have been investigated for the evaluation of cytotoxic and antioxidant activity. Brine shrimp lethality bioassay was used to evaluate the cytotoxic activity and free radical scavenging activity method was used to evaluate antioxidant activity. In brine shrimp lethality bioassay, the chloroform soluble fraction showed greater cytotoxic activity (LC50 value 74.2 μg/ml) than petroleum ether soluble fraction (LC50 value 129 μg/ml) compared to the standard drug vincristine sulfate (LC50 value 0.54 μg/ml). In free radical scavenging activity method (DPPH assay method), the chloroform soluble fraction showed greater antioxidant activity (IC50 value 49.78 μg/ml) than petroleum ether soluble fraction (IC50 value 75.31 μg/ml) compared to the standard antioxidant butylated hydroxytoluene (IC50 value 24.51μg/ml). This study reveals that Baccaurea ramiflora fruit possesses cytotoxic and antioxidant activity hence can be a potential source for the isolation of active principle(s) for different therapies.

Atividades biológicas de espécies amazônicas de Rubiaceae / Biological activities of Amazonian species of Rubiaceae

RESUMORubiaceae é uma família botânica com grande potencial químico e biológico Neste trabalho realizou-se a prospecção fitoquímica e avaliou-se as atividades citotóxica, antioxidante e antifúngica dos extratos diclorometânicos e metanólicos das folhas de Duroia saccifera, Ferdinandusa goudotiana, F. hirsuta, F. paraensis, Ferdinandusa sp., Palicourea corymbifera e P. guianensis. A avaliação da citotoxicidade foi realizada empregando-se o ensaio de toxicidade sobre Artemia salina. A atividade antifúngica foi determinada pelo método de difusão em ágar utilizando-se os fungos: Epidermophyton floccosum, Microsporum canis 32905, M. gipseum 29/00, Trichophyton mentagrophytes ATCC 9533/03, T. rubrum ATCC 28189, T. tonsurans 21/97, Cladosporium cladosporioides, C. sphaerospermum, FusariumU. 662/06, Scytalidium U. 661/06, Candida albicans ATCC 3632 e C. albicans U. 5/99. A atividade antioxidante foi determinada através dos ensaios de redução do radical livre 1,1-difenil-2-picrilhidrazila (DPPH) e de descoloração do cátion radical ácido-6-sulfônico-2,2-azinobis-3-etilbenzotiazolina (ABTS). Para o ensaio de toxicidade sobre A. salina observou-se maior toxicidade no extrato metanólico de F. goudotiana, que se mostrou tóxico até a concentração de 5 µg mL-1. A presença de princípios antifúngicos foi observada em F. hirsuta e F. paraensiscontra quatro dos fungos testados. Na avaliação da atividade antioxidante os extratos metanólicos mostraram maior atividade que os extratos diclorometânicos, sendo coincidente o resultado obtido através de ambos os métodos (redução do DPPH e descoloração do ABTS). Os resultados criam possibilidades para futuras investigações relacionadas à estrutura e atividade dos componentes de cada extrato ativo.

ABSTRACTRubiaceae is a plant family with great chemical and biological potential. In this work a phytochemical prospection was performed and it was assessed the cytotoxic, antioxidant and antifungal activities of dichloromethanic and methanolic extracts of the leaves of Duroia saccifera, Ferdinandusagoudotiana, F. hirsuta, F. paraensis, Ferdinandusa sp., Palicourea corymbifera and P. guianensis. The cytotoxicity evaluation was carried out using the test toxicity on Artemia salina. The antifungal activity was determined by agar diffusion method using fungi: Epidermophyton floccosum, Microsporum canis 32905, M. gipseum 29/00, Trichophyton mentagrophytes ATCC 9533/03, T.rubrum ATCC 28189, T. tonsurans 21/97 , Cladosporium cladosporioides, C. sphaerospermum, FusariumU. 662/06, Scytalidium U. 661/06, Candida albicans ATCC 3632 and C. albicans U. 5/99. The antioxidant activity was determined by testing the amount of free radical 1,1-diphenyl-2-picrylhydrazyl (DPPH) and the discoloration of the radical cation 6-sulfonic acid-2 ,2-azinobis-3-ethylbenzothiazoline (ABTS). For the toxicity test on A. salina greater toxicity in the methanol extract of F. goudotiana was observed, which proved to be toxic up to a concentration of 5 µg mL-1. The presence of antifungal principles was observed in the F. hirsuta and F. paraensis against four tested fungi. In the evaluation of the antioxidant activity, the methanol extracts showed greater activity than the dichloromethanic ones, being similar the obtained result through both methods (reduction of DDPH and ABTS decolorization) . The results create possibilities for future researches related to the structure and activity of the components of each active extract.

Cytotoxic, Thrombolytic and Membrane Stabilizing Activities of Swietenia mahagoni (L.) Jacq. Flower Extract.

Aims: To investigate cytotoxic, thrombolytic and membrane stabilizing activities of methanol extract and its different Kupchan partitionates of flowers of Swietenia mahagoni. Study Design: Evaluation of cytotoxic activity using brine shrimp nauplii, thrombolytic and membrane stabilizing activities on human RBCs. Place and Duration of Study: Phytochemical Research Laboratory, Department of Pharmacy, School of Health Science, State University of Bangladesh, from April to September, 2013. Methodology: The eggs of brine shrimp nauplii were hatched in artificial sea water for 24 hours. Cytotoxic activity was determined by measuring the percentage of their mortality after application of different partitionates to them. Human RBCs were obtained from 3 healthy volunteers. Thrombolytic activity was calculated by weighing the clot before and after addition of different partitionates while membrane stabilizing activity was evaluated in terms of inhibition of percentage of haemolysis of RBCs by measuring optical density in both hypotonic and heat induced conditions. Results: The highest cytotoxic activity was achieved with the crude methanol extract (LC50 = 0.10±0.01 mg/ml) among the partitionates while vincristine sulfate, the positive control, achieved an LC50 value of 0.40±0.02 mg/ml. While investigating thrombolytic activity, the petroleum ether soluble fraction achieved the highest clot lysis activity (34.30±0.78%) compared to the standard streptokinase (70.27±1.26%). While determining the membrane stabilizing activity, in hypotonic solution induced condition, the crude methanol extract inhibited 84.71±3.25% haemolysis of RBCs whereas in heat induced condition, the aqueous soluble fraction inhibited 86.30±4.98% haemolysis of human RBCs. Here, acetyl salicylic acid (0.01mg/ml) used as reference standard showed 71.91±2.29% and 45.45±4.87% inhibition of haemolysis of human RBCs in hypotonic solution and heat induced conditions, respectively. Conclusion: From our investigation, it can be suggested that, the flower extractives can further be studied extensively to find out their efficacy.

Assessment of cytotoxic activities of Phyllanthus amarus and Monstera deliciosa.

Medicinal plants constitute an important component of flora and are widely distributed in Bangladesh. The pharmacological evaluation of substances from plants is an established method for the identification of lead compounds which shows the way to the development of novel and safe medicinal agents. Based on the ethnopharmacological literature two widely used medicinal plants Phyllanthus amarus and Monstera deliciosa were chosen to investigate their cytotoxicity through brine shrimp lethality bioassay which is simple, reliable and convenient method for assessment of bioactivity of medicinal plants. The plants were collected from their natural habitat, dried under shade and extracted with ethyl acetate. In this study, ethyl acetate extract of Phyllanthus amarus exhibited potent cytotoxicity with LC50 values of 9.15μg/ml and 20.16μg/ml of leaves and the whole plant respectively. Monstera deliciosa exhibited cytotoxicity with LC50 values of 36.60μg/ml and 300.4 μg/ml of leaves and branches respectively. From the result, it can be predicted that extractives of Phyllanthus amarus possess cytotoxic principles and showed significantly more potency than in leaves rather than whole plant. In case of Monstera deliciosa the extractives of leaves exhibited very mild mortality while the extractives of branches did not show considerable cytotoxicity.

Antioxidant, Brine Shrimp Lethality and Antimicrobial Activities of Methanol and Ethyl-Acetate Extracts of Citrus macroptera Montr. Fruit Using In vitro Assay Models.

Aims: To study and evaluate In vitro antioxidant, brine shrimp lethality and antimicrobial activities of both methanol and ethyl-acetate extracts of Citrus macroptera Montr. Fruit (Family-Rutaceae). Study Design: In vitro antioxidant, brine shrimp lethality and antimicrobial activities. Place and Duration of Study: Department of Pharmacy, Jahangirnagar University, Savar, Dhaka-1342. The study was carried out from November 2013 to January 2014. Methodology: In vitro antioxidant activities of the extracts were studied using DPPH radical scavenging assay, NO scavenging assay, total phenol, total flavonoid content, total antioxidant capacity, total tannin content, lipid peroxidation by TBA, lipid peroxidation in human erythrocyte cell, reducing power capacity and cupric reducing capacity assays. Lethality bioassay was performed on Artemia salina Leach nauplii. Antimicrobial activity was investigated by disc diffusion technique. Results: Methanol extract showed better activity than ethyl acetate extract in DPPH, NO, lipid peroxidation by TBA, reducing power capacity assay, total phenol, total flavonoid and total antioxidant capacity assays while ethyl –acetate extract showed more potency than methanol extract in total tannin content, cupric reducing capacity and lipid peroxidation in human erythrocyte assays. In brine shrimp bioassay both extracts showed promising lethal activity but methanol extract was found to be more potent than ethyl acetate extract (χ2=39.874, P<0.0001). In disc diffusion technique among six bacterial species, ethyl acetate extract showed broad spectrum antimicrobial activity against two gram positive Bacillus sublitis and Staphylococcus aureus and one gram negative Escherichia coli. Conclusion: The results demonstrate that methanol and ethyl-acetate extracts of C. macroptera fruit can be used as potential antioxidant, cytotoxic and antimicrobial agents. That is why extensive researches are necessary to search for active principles responsible for these activities.

Comparative Phytochemical Screening and In vitro Evaluation of Biological Activities between Aqueous and Ethanolic Extract of Momordica charantia L. Fruits.

Aims: The study was conducted to compare the presence of different phytochemicals and biological activities like cytotoxicity, anthelmintic activity, antioxidant and free radical scavenging activities between aqueous and ethanolic extract of Momordica charantia L. Fruits. Methodology: The cytotoxic assay was undertaken using brine shrimp lethality test (BSLT) while the anthelmintic activity was carried out with the determination of time of paralysis and death of earthworm (Pheritima posthuma) at five different concentrations. Antioxidant and free radical scavenging activities were measured by 1,1-diphenyl-2-picrylhydrazyl (DPPH) method and determining the total phenolic contents. Results: Study revealed that several phytochemicals were found common for both of the extracts, though proteins and amino acids were only found in ethanolic extract. Both the extracts showed mild cytotoxic activity where the ethanolic extract showed better potency (LC50=24.245 μg/ml) than aqueous extract (LC50=24.515 μg/ml). In case of anthelmintic activity, ethanolic extract was also found significantly potent than aqueous extract at five different concentrations. IC50 values for the total antioxidant activity were 304.41±0.903 μg/ml and 479.05±1.393 μg/ml for ethanolic and aqueous extract, respectively. Ethanolic extract contained a significantly higher concentration of total phenols (71.08 ± 0.380 mg of GAE/g of extract) in comparison to aqueous extract (57.33±0.520 mg of GAE/g of extract). Conclusion: Therefore, in all aspects of the study, ethanolic extract was found more potent than aqueous extract. It can be concluded that M. charantia fruits are abundant of various phytochemicals and possess versatile biological activities.