Biological screening of extracts from leaf and stem bark of Croton floribundus Spreng. (Euphorbiaceae) / Triagem biológica de extratos das folhas e caules de Croton floribundus Spreng. (Euphorbiaceae)

Abstract This work describes the preliminary evaluation of cytotoxic, antimicrobial, molluscicidal, antioxidant and anticholinesterase activities from leaf (LECF) and stem bark alcoholic extracts (BECF) of the species Croton floribundus Spreng. (Euphorbiaceae), popularly known as capixingui or tapixingui. BECF presented significant toxicity (LC50 = 89.6 μg/ml) in the Artemia salina Leach, 1819 (Crustacea: Branchiopoda) bioassay, whereas LECF did not show activity (LC50 > 1000 μg/ml). From DPPH method, the values of IC50 for the LECF and BECF were 61.2 μg/ml and 62.2 μg/ml, respectively, showing that C. floribundus has an expressive antioxidant activity. Antimicrobial susceptibility was evaluated by microdilution technique and only BECF was active against Staphylococcus aureus (MIC = 39.6 μg/ml). The extracts did not present molluscicidal activity against snail Biomphalaria glabrata Say, 1818 (Gastropoda: Planorbidae). Both extracts revealed the presence of several components with an inhibiting capacity of acetylcholinesterase enzyme on the bioautographic assay. C. floribundus showed to be a promising species considering that it exhibited good biological activity in the most assays performed.

Resumo Este trabalho descreve a avaliação preliminar das atividades citotóxica, antimicrobiana, moluscicida, antioxidante e anticolinesterásica de extratos alcoólicos das folhas (LECF) e das cascas do caule (BECF) da espécie Croton floribundus Spreng. (Euphorbiaceae), popularmente conhecida como capixingui ou tapixingui. No bioensaio com Artemia salina Leach, 1819 (Crustacea: Branchiopoda), BECF apresentou toxicidade significante (LC50 = 89,6 µg/ml), enquanto que LECF não apresentou atividade (LC50 > 1000 µg/ml). A partir do método de DPPH, os valores de IC50 para o LECF e BECF foram 61,2 µg/ml e 62,2 µg/ml, respectivamente, evidenciando que C. floribundus tem uma atividade antioxidante expressiva. A susceptibilidade antimicrobiana foi avaliada pela técnica de microdiluição e apenas BECF foi ativo contra Staphylococcus aureus (MIC = 39,6 mg/ml). Os extratos não apresentaram atividade moluscicida contra o caramujo Biomphalaria glabrata Say, 1818 (Gastropoda: Planorbidae). Ambos os extratos revelaram a presença de componentes com capacidade inibidora da enzima acetilcolinesterase no ensaio bioautográfico. C. floribundus mostrou ser uma espécie promissora considerando que exibiu boa atividade biológica na maioria dos ensaios testados.

Bioactive sesquiterpene lactone from Artemisia santolina / Lactona sesquiterpénica bioactiva de Artemisia santolina

Most species of genus Artemisia L. (Compositae) are medicinal herbswith several uses in the folk medicine worldwide. In the present study, methanol extract of Artemisia santolina has been subjected for isolation of its metabolites along with evaluation of cytotoxic activity against Artemia salina larvae. The structures of the compounds determined by 1H-and 13C-NMR, HMQC, HMBC, 1H-1H COSY and Mass spectral analysis. Two sesquiterpenes, 1,5-dihydroxy- 4(15)eudesman-12,6-olid (artemin) (1), 2-hidroxy-2,6,10-trimethyl-7,10- oxide-3,11-dodecadien-5-one (2) and one flavonoid, 5,7,4'-trihydroxy-6,3'-dimethoxyflavone (jaceosidin) (3) have been successfully characterized. Cytotoxicity of the sesquiterpene lactone (1), was assessed on Artemia salina larvae and resulted in IC50 value of 6.44 µg/mL, which was more potent compared to the positive standard berberine hydrochloride (IC50 = 26 µg/mL). In this study, the separation and identification of two sesquiterpenes and one flavone from the aerial parts of A. santolina is described. Among them the compound artemin (1) showed a toxicity effect against A. salina nauplii.

La mayoría de las especies del género Artemisia L. (Compositae) son hierbas medicinales con varios usos en la medicina popular en todo el mundo. En el presente estudio, el extracto metanólico de Artemisia santolina ha sido sometido al aislamiento de sus metabolitos junto con la evaluación de la actividad citotóxica contra las larvas de Artemia salina. Las estructuras de los compuestos se determinaron mediante RMN 1H y 13C, HMQC, HMBC, 1H-1H COZY y análisis espectral de masas. Dos sesquiterpenos, 1,5-dihidroxi-4 (15) eudesman- 12,6-olid (artemin) (1), 2-hidroxi-2,6,10-trimetil-7,10-óxido-3,11-dodecadien-5-ona (2) y un flavonoide, 5,7,4'-trihidroxi-6,3'- dimetoxiflavona (jaceosidina) (3). Se evaluó la citotoxicidad de la lactona sesquiterpénica (1) en larvas de Artemia salina y resultó en un valor de CI50 de 6,44 µg/ml, que era más potente en comparación con el clorhidrato de berberina estándar positivo (CI50 = 26 µg/ml). En este estudio se describe la separación e identificación de dos sesquiterpenos y una flavona de las partes aéreas de A. santolina. Entre ellos, el compuesto artemin (1) mostró un efecto de toxicidad contra los nauplios de A. salina.

Toxicity of clove essential oil and its ester eugenyl acetate against Artemia salina / Toxicidade do óleo essencial de cravo e seu éster acetato de eugenila contra Artemia salina

Abstract The production of compounds via enzymatic esterification has great scientific and technological interest due to the several inconveniences related to acid catalysis, mainly by these systems do not fit to the concept of “green chemistry”. Besides, natural products as clove oil present compounds with excellent biological potential. Bioactives compounds are often toxic at high doses. The evaluation of lethality in a less complex animal organism can be used to a monitoring simple and rapid, helping the identification of compounds with potential insecticide activity against larvae of insect vector of diseases. In this sense, the toxicity against Artemia salina of clove essential oil and its derivative eugenyl acetate obtained by enzymatic esterification using Novozym 435 as biocatalyst was evaluated. The conversion of eugenyl acetate synthesis was 95.6%. The results about the evaluation of toxicity against the microcrustacean Artemia salina demonstrated that both oil (LC50= 0.5993 µg.mL–1) and ester (LC50= 0.1178 µg.mL–1) presented high toxic potential, being the eugenyl acetate almost 5 times more toxic than clove essential oil. The results reported here shows the potential of employing clove oil and eugenyl acetate in insecticide formulations.

Resumo A produção de compostos via esterificação enzimática possui grande interesse científico e tecnológico devido às inúmeras inconveniências relacionadas com a catálise ácida, principalmente por estes sitemas não se adequarem ao atual termo “tecnologias limpas”. Além disso, produtos naturais como o óleo de cravo, apresentam compostos com excelentes potenciais biológicos. Compostos bioativos são quase sempre tóxicos em altas doses. A avaliação da letalidade em um organismo animal menos complexo pode ser usada para um monitoramento simples e rápido, servindo também para a identificação de compostos com potencial atividade inseticida contra larvas de insetos vetores de doenças. Neste sentido, foi determinada a toxicidade frente a Artemia salina do óleo essencial de cravo e do seu derivado acetato de eugenila obtido por esterificação enzimática com lipase Novozym 435. A conversão da reação de síntese de acetato de eugenila foi de 95,6%. Os resultados referentes à avaliação da toxicidade frente ao microcrustáceo Artemia salina demonstraram que tanto o óleo (LC50= 0,5993 µg.mL–1) quanto o éster (LC50= 0,1178 µg.mL–1) apresentam elevado potencial toxicológico, sendo que o éster apresenta aproximadamente 5 vezes mais toxicidade em relação ao óleo. Estes resultados demonstram o potencial emprego do óleo de cravo e de acetato de eugenila em formulações de inseticidas.

Concentraciones de alcaloides, glucósidos cianogénicos, polifenoles y saponinas en plantas medicinales seleccionadas en Ecuador y su relación con la toxicidad aguda contra Artemia salina / Concentrations of alkaloids, cyanogenic glycosides, polyphenols and saponins in selected medicinal plants from Ecuador and their relationship with acute toxicity against Artemia salina

ResumenEntre los principales compuestos químicos sintetizados por las plantas, pero considerados no esenciales para su metabolismo básico, están los alcaloides, los polifenoles, los glucósidos cianogénicos y las saponinas que tienen diversas funciones en las plantas y reconocidas propiedades medicinales y farmacológicas. En esta investigación se determinaron las concentraciones de los mencionados metabolitos secundarios en los extractos de las hojas de las plantas medicinales Taraxacum officinale, Parthenium hysterophorus, Artemisia absinthium, Cnidoscolus aconitifolius y Piper carpunya y se relacionaron con la toxicidad aguda contra Artemia salina. En cada bioensayo con A. salina se usaron los extractos alcohólicos de las hojas de las plantas seleccionadas a diferentes concentraciones, calculándose la proporción de organismos muertos y los CL50. Las concentraciones de alcaloides, fenoles totales, taninos, glucósidos cianogénicos y saponinas fueron determinadas mediante métodos espectrofotométricos. Este es el primer reporte de cuantificación de metabolitos secundarios en las plantas analizadas provenientes de Ecuador. T. officinale presentó las mayores concentraciones de fenoles (22.30 ± 0.23 mg/g) y taninos (11.70 ± 0.10 mg/g), C aconitifolius de glucósidos cianogénicos (5.02 ± 0.37 µg/g) y P. hysterophorus de saponinas (6.12 ± 0.02 mg/g). Las plantas evaluadas presentaron actividades hemolíticas dependiendo de las concentraciones de saponinas. Los valores de taninos determinados estuvieron entre 0.20 ± 0.01 y 11.70 ± 0.10 mg/g, por lo que no son adversos para su consumo. Aunque los valores de glucósidos cianogénicos son permisibles, es necesario monitorear la presencia de estos compuestos químicos en las plantas para minimizar problemas de salud. Los CL50 obtenidos oscilaron entre los valores 3.37 µg/mL, extremadamente letal o tóxica, para P. carpunya y 274.34 µg/mL, altamente tóxica, para T. officinale. De los análisis de correlaciones realizados a los resultados, se observó que los alcaloides favorecen de manera significativa (p<0.001) a la toxicidad aguda contra A. salina, mientras que a mayor contenido de polifenoles dicha toxicidad disminuye significativamente (p<0.001) el nivel de toxicidad de las plantas. Del análisis de componentes principales, se demuestra que las saponinas están en sinergia con los polifenoles para disminuir la toxicidad, pero tienen un efecto antagónico con los alcaloides y los glucósidos cianogénicos, lo cual evidencia que estos metabolitos secundarios presentan variabilidades en los mecanismos de acción contra A. salina, como compuestos citotóxicos. Estos resultados demuestran que las saponinas y los polifenoles pueden ser letales para A. salina a bajas concentraciones, evidenciando que este bioensayo permite evaluar extractos vegetales que contengan bajas concentraciones de compuestos con altas polaridades. La correspondencia significativamente positiva entre citoxicidad y concentración de los alcaloides, confirmada con el bioensayo de Artemia salina, puede ser útil para hallar fuentes promisorias de compuestos antitumorales y para evaluar los límites tolerables que no afecten otras células benignas. El contenido de metabolitos secundarios hallados en las plantas analizadas les atribuye un gran valor farmacológico.

Abstract:Alkaloids, polyphenols, cyanogenic glycosides and saponins are among the main chemical compounds synthesized by plants but not considered essential for their basic metabolism. These compounds have different functions in plants, and have been recognized with medicinal and pharmacological properties. In this research, concentrations of the mentioned secondary metabolites were determined in the medicinal plants Artemisia absinthium, Cnidoscolus aconitifolius, Parthenium hysterophorus, Piper carpunya and Taraxacum officinale, from Ecuador, and related with cytotoxic effects against Artemia salina. Alcoholic and aqueous extracts from leaves of these selected plants were prepared at different concentrations. To assess cytotoxicity of these extracts, different bioassays with A. salina were undertaken, and the mortality rates and LC50 were obtained. Besides, concentrations of alkaloids, cyanogenic glycosides, phenols, tannins and saponins were determined by spectrophotometric methods; this constituted the first report of quantification of secondary metabolites in the selected plants from Ecuador. T. officinale had the highest concentration of total phenols (22.30 ± 0.23 mg/g) and tannins (11.70 ± 0.10 mg/g), C. aconitifolius of cyanogenic glycosides (5.02 ± 0.37 µg/g) and P. hysterophorus of saponins (6.12 ± 0.02 mg/g). Tannins values obtained were not adverse to their consumption. Alcoholic and aqueous extracts of selected plants had hemolytic activity depending on the concentration of saponins. Although the values of cyanogenic glycosides were permissible, it was necessary to monitor the presence of this metabolite in plants to minimize health problems. LC50 values ranged from extremely toxic (3.37 µg/mL) to highly toxic (274.34 μg/mL), in P. carpunya and T. officinale, respectively. From correlation analysis, it was observed that increase values of alkaloids concentrations had highly significant (p<0.001) acute toxicity against A. salina, while at a higher polyphenol concentration the level of plants cytotoxicity decreased significantly (p<0.001). The results of principal component analysis showed that saponins apparently were in synergy with polyphenols to decrease cytotoxicity, but antagonize with alkaloids and cyanogenic glycosides, indicating that these secondary metabolites present variability in the mechanisms of action against A. salina, as cytotoxic compounds. These results also demonstrate that polyphenols and saponins can be lethal at low concentrations, demonstrating the potential of brine shrimp bioassay as a model to evaluate plant extracts containing low concentrations of chemical compounds with high polarities. The significant positive correlation between cytotoxicity and concentration of alkaloids confirmed by the bioassay of brine shrimp can be useful to identify promising sources of antitumor compounds, and to evaluate tolerable limits not affecting other benign cells. Contents of secondary metabolites found in the selected plants confer them great pharmacologic values. Rev. Biol. Trop. 64 (3): 1171-1184. Epub 2016 September 01.

Letalidad de citocalasina B y otros compuestos aislados del hongo Aspergillus spp. (Trichocomaceae) endófito de Bauhinia guianensis (Fabaceae) / Lethality of cytochalasin B and other compounds isolated from fungus Aspergillus sp. (Trichocomaceae) endophyte of Bauhinia guianensis (Fabaceae)

Los hongos endofíticos son hongos que colonizan los tejidos internos de las plantas; varios compuestos biológicamente activos se han aislado a partir de estos hongos. Existen pocos estudios de compuestos aislados de hongos endófitos de plantas amazónicas. Por lo tanto, este estudio tuvo como objetivo el aislamiento y la identificación estructural de ergosterol (1), peróxido de ergosterol (2), mevalonolactona (3), citocalasina B (4) y citocalasina H (5) a partir de Aspergillus spp. EJC 04, un hongo endofítico de Bauhinia guianensis. La citocalasina B (4) y el derivado diacetato de citocalasina B (4a) mostraron una alta letalidad en el ensayo de Artemia salina. Esta es la primera aparición de citocalasinas en hongos endófitos amazónica de B. guianensis

Endophytic fungi are fungi that colonize internal tissues of plants; several biologically active compounds have been isolated from these fungi. There are few studies of compounds isolated from endophytic fungi of Amazon plants. Thus, this study aimed the isolation and structural identification of ergosterol (1), ergosterol peroxide (2), mevalonolactone (3), cytochalasin B (4) and cytochalasin H (5) from Aspergillus sp. EJC 04, an endophytic fungus from Bauhinia guianensis. The cytochalasin B (4) and the diacetate derivative of cytochalasin B (4a) showed high lethality in the brine shrimp assay. This is the first occurrence of cytochalasins in Amazonian endophytic fungi from B. guianensis

Antitumor compounds from Streptomyces sp. KML-2, isolated from Khewra salt mines, Pakistan

BACKGROUND: Actinomycetes are gram positive bacteria with high G + C content in their DNA and are capable of producing variety of secondary metabolites. Many of these metabolites possess different biological activities and have the potential to be developed as therapeutic agents. The aim of the present study was to screen actinomycetes inhabiting halophilic environment such as Khewra salt mines present in Pakistan for cytotoxic and antitumor compounds. RESULTS: An actiomycetes strain designated as Streptomyces sp. KML-2 was isolated from a saline soil of Khewra salt mines, Pakistan. The strain Streptomyces sp. KML-2 showed 84 % cytotoxic activity against larvae of Artemiasalina. In the screening phase, the strain exhibited significant antitumor activity with IC50 values of 12, 48 and 56 µg/ml against Hela, MDBK and Vero cell lines, respectively. After that extract from 20 l fermentation was used to purify secondary metabolites by several chromatographic techniques. Structure elucidation of isolated compounds revealed that it is highly stable producer of Chromomycin SA (1) and 1-(1H-indol-3-yl)-propane-1,2,3-triol (2). Both of the isolated compounds showed significant antitumor activity against Hela and MCF-7 cancer cell lines (IC50 values 8.9 and 7.8 µg/ml against Hela; 12.6 and 0.97 µg/ml against MCF-7, respectively). The 16S rRNA gene sequence (1437 bp) of the strain confirm its identity (99 %) with Streptomyces griseus. CONCLUSIONS: From this research work we were successful in isolating two potent antitumor compounds, Chromomycin SA and 1-(1H-indol-3-yl)-propane-1,2,3-triol from Streptomyces KML-2 strain, isolated from Khewra salt mine. As such this is the second report which confirms that S. griseus can produce Chromomycin SA without introducing any mutagenesis in its biosynthesizing gene cluster and isolated indole derivative is being reported first time from any member of actinomycetes group with having novel antitumor activity against Hela and MCF-7 cells Nucleotide sequences: Nucleotide sequence data reported are available in the GenBank database under the accession number: GenBank KJ009562.

Estimation of antioxidant, antimicrobial activity and brine shrimp toxicity of plants collected from Oymyakon region of the Republic of Sakha (Yakutia), Russia

BACKGROUND: Several plants are reported to be produced various biological active compounds. Lichens from the extreme environments such as high altitude, high UV, drought and cold are believed to be synthesized unique types of secondary metabolites than the other one. Several human pathogenic bacteria and fungi have been muted into drug resistant strains. Various synthetic antioxidant compounds have posed carcinogenic effects. This phenomenon needs further research for new effective drugs of natural origin. This manuscript aimed to screen new source of biological active compounds from plants of subarctic origin. RESULTS: A total of 114 plant species, including 80 species of higher plants, 19 species of lichens and 15 species of mosses, were collected from Oymyakon region of the Republic of Sakha (Yakutia), Russia (63˚20′N, 141˚42′E - 63˚15′N, 142˚27′E). Antimicrobial, DPPH free radical scavenging and brine shrimp (Artemia salina) toxicity of all crude extract were evaluated. The obtained result was analyzed and compared with commercial standards. A total of 28 species of higher plants showed very strong antioxidant activity (DPPH IC50, 0.45-5.0 µg/mL), 13 species showed strong activity (DPPH IC50, 5-10 µg/mL), 22 species showed moderate antioxidant activity (DPPH IC50,10-20 µg/mL) and 17 species showed weak antioxidant activity (DPPH IC50 more than 20 µg/mL). Similarly, 3 species of lichen showed strong antioxidant activity, one species showed moderate and 15 species showed weak DPPH reducing activity. In addition, 4 species of mosses showed moderate antioxidant activity and 11 species showed weak antioxidant activity. Similarly, extracts of 51 species of higher plants showed antimicrobial (AM) activity against Staphylococcus aureus and 2 species showed AM activity against Candida albicans. Similarly, 11 species of lichen showed AM activity against S. aureus and 3 species showed AM activity against Escherichia coli. One species of moss showed AM activity against S. aureus. And finally, one species of higher plant Rheum compactum and one species of lichen Flavocetraria cucullata showed the toxicity against Brine shrimp larvae in 100 µg/mL of concentration. CONCLUSION: The experimental results showed that subarctic plant species could be potential sources of various biologically active natural compounds.

Phytochemical and toxicological investigations of crude methanolic extracts, subsequent fractions and crude saponins of Isodon rugosus

BACKGROUND: Isodon rugosus is used traditionally in the management of hypertension, rheumatism, tooth-ache and pyrexia. Present study was arranged to investigate I. rugosus for phytoconstituents, phytotoxic and cytotoxic activities to explore its toxicological, pharmacological potentials and to rationalize its ethnomedicinal uses. Briefly, qualitative phytochemical analysis of the plant extracts were carried out for the existence of alkaloids, flavonoids, saponins, oils, glycosides, anthraquinones, terpenoids, sterols and tannins. Plant crude methanolic extract (Ir.Cr), its subsequent fractions; n-hexane (Ir.Hex), chloroform (Ir.Chf), ethyl acetate (Ir.EtAc), aqueous (Ir.Aq) and saponins (Ir.Sp) in different concentrations were tested for phytotoxic and cytotoxic activities using radish seeds and brine shrimps (Artemia salina) respectively. The phytotoxic activity was determined by percent root length inhibition (RLI) and percent seeds germination inhibition (SGI) while the cytotoxicity was obtained with percent lethality of the brine shrimps. RESULTS: Ir.Cr was tested positive for the presence of alkaloids, glycosides, flavonoids, oils, terpenoids, saponins, tannins and anthraquinones. Among different fractions Ir.Sp, Ir.Chf, Ir.EtAc, and Ir.Cr were most effective causing 93.55, 89.32, 81.32 and 58.68% inhibition of seeds in phytotoxicity assay, with IC50 values of 0.1, 0.1, 0.1 and 52 µg/ml respectively. Similarly, among all the tested samples, Ir.Sp exhibited the highest phytotoxic effect causing 91.33% root length inhibition with IC50 of 0.1 µg/ml. Ir.Sp and Ir.Chf were most effective against brine shrimps showing 92.23 and 76.67% lethality with LC50 values of 10 and 12 µg/ml respectively. CONCLUSIONS: It may be inferred from the current investigations that I. rugosus contains different secondary metabolites and is a potential source for the isolation of natural anticancer and herbicidal drug molecules. Different fractions exhibited phytotoxic and cytotoxic activities, thus providing pharmacological basis for ethnomedicinal uses of this plant.

In vivo antipyretic, antiemetic, in vitro membrane stabilization, antimicrobial, and cytotoxic activities of different extracts from Spilanthes paniculata leaves

BACKGROUND: The study was conducted to evaluate the in vitro antimicrobial activity, cytotoxic, and membrane stabilization activities, and in vivo antiemetic and antipyretic potentials of ethanolic extract, n-hexane and ethyl acetate soluble fractions of Spilanthes paniculata leaves for the first time widely used in the traditional treatments in Bangladesh. RESULTS: In antipyretic activity assay, a significant reduction (P < 0.05) was observed in the temperature in the mice tested. At dose 400 mg/kg-body weight, the n-hexane soluble fraction showed the effect (36.7 ± 0.63°C ) as like as the standard (dose 150 mg/kg-body weight) after 5 h of administration. Extracts showed significant (P < 0.001) potential when tested for the antiemetic activity compared to the standard, metoclopramide. At dose 50 mg/kg-body weight, the standard showed 67.23% inhibition, whereas n-hexane and ethyl acetate soluble fractions showed 37.53% and 24.93% inhibition of emesis respectively at dose 400 mg/kg-body weight. In antimicrobial activity assay, the n-hexane soluble fraction (400 µg/disc) showed salient activity against the tested organisms. It exerts highest activity against Salmonella typhi (16.9 mm zone of inhibition); besides, crude, and ethyl acetate extracts showed resistance to Bacillus cereus and Bacillus subtilis, and Vibrio cholera respectively. All the extracts were tested for lysis of the erythrocytes. At the concentration of 1mg/ml, ethanol extract, and n-hexane and ethyl acetate soluble fractions significantly inhibited hypotonic solution induced lysis of the human red blood cell (HRBC) (27.406 ± 3.57, 46.034 ± 3.251, and 30.72 ± 5.679% respectively); where standard drug acetylsalicylic acid (concentration 0.1 mg/ml) showed 77.276 ± 0.321% inhibition. In case of heat induced HRBC hemolysis, the plant extracts also showed significant activity (34.21 ± 4.72, 21.81 ± 3.08, and 27.62 ± 8.79% inhibition respectively). In the brine shrimp lethality bioassay, the n-hexane fraction showed potent (LC50 value 48.978 µg/ml) activity, whereas ethyl acetate fraction showed mild (LC50 value 216.77 µg/ml) cytotoxic activity. CONCLUSIONS: Our results showed that the n-hexane extract has better effects than the other in all trials. In the context, it can be said that the leaves of S. paniculata possess remarkable pharmacological effects, and justify its folkloric use as antimicrobial, antipyretic, anti-inflammatory, and antiemetic agent. Therefore, further research may be suggested to find possible mode of action of the plant part.

Antioxidant, antimicrobial, toxicity and analgesic properties of ethanol extract of Solena amplexicaulis root

BACKGROUND: This study was subjected to investigate different pharmacological properties of ethanol extract ofSolena amplexicaulis root. RESULTS: The extract contains flavonoid, alkaloid, saponin and steroid compounds. The extract exhibited excellent antioxidant activity in DPPH radical scavenging activity. The extract also showed potent activity in brine shrimp lethality bioassay. The LC50 value was found to 44.677 µg/ml. The extract showed better anti-bacterial activity against gram-negative bacteria. In antifungal assay, the maximum 79.31% of anti-mycotic activity was observed against Aspergillus ochraceus while minimum 44.2% against Rhizopus oryzae. MIC value ranged between 1500 - 3000 µg/ml. The extract was found moderately toxic with a 24-hr LD50 value of 81.47 mg/kg in Swiss albino mice. The degree of inhibition by the ethanolic extract of the root was found less than that of standard analgesic drug diclofenac sodium. The extract also showed moderate anti-inflammatory and antinociceptive activity and anti-diabetic property. Reducing power of the extract was comparable with standard ascorbic acid. Moderate in vitro thrombolytic activity, lipid peroxidation inhibition property, metal chelating ability and stress-protective activity was also observed. CONCLUSION: Ethanol extract of Solena amplexicaulis root can be valuable for treatment of different diseases.

Extraction of saponins and toxicological profile of Teucrium stocksianum boiss extracts collected from District Swat, Pakistan

BACKGROUND: The current era is facing challenges in the management of neoplasia and weeds control. The currently available anti-cancer and herbicidal drugs are associated with some serious side effects. Therefore numerous researchers are trying to discover and develop plant based alternative particularly for the rational management of cancer and weed control. Teucrium stocksianum possess antioxidant and analgesic activities. The current study was designed to evaluate crude saponins (CS), methanolic extract and sub-fractions of T. stocksianum for cytotoxic and phytotoxic potentials. CS, methanolic extract and sub-fractions were extracted from powdered plant material using different solvents. Cytotoxic potential of the extracts at a dose of 10, 100 and 1000 µg/ml were evaluated against Brine shrimp's nauplii. Phytotoxic assay also performed at the same concentration against Lemna minor. Etoposide and Paraquat were used as positive controls in cytotoxic and phytotoxic assays respectively. RESULTS: The percent yield of crude saponins was (5%). CS demonstrated tremendous brine shrimp lethality showing < 10 µg/ml LC50. The n-hexane (HF) and chloroform fractions (CF) demonstrated excellent cytotoxicity with 80 and 55 µg/ml LC50 respectively. Whereas the methanolic extract (TSME), ethyl acetate (EAF) and aqueous fractions (AF) revealed moderate cytotoxicity showing 620, 860 and 1000 µg/ml LC50 values respectively. In phytotoxic assay profound inhibition was displayed by HF (96.67%) and TSME (95.56%, 30 µg/ml LC50) against the growth of Lemna minor at 1000 µg/ml respectively. Both CF and EAF demonstrated profound phytoxicity (93.33%) respectively at highest concentration (1000 µg/ml), while AF and CS demonstrated weak phytotoxicity with 1350 and 710 µg/ml LC50 values respectively. CONCLUSION: Cytotoxicity and phytotoxicity assays indicated that the crude saponins, n-hexane and chloroform fractions of T. stocksianum could play a vital role in the treatment of neoplasia and as potential natural herbicides. Therefore these sub-fractions are recommended for further investigation with the aim to isolate novel anti-cancer and herbicidal compounds.

Evaluation of larvicidal activity and brine shrimp toxicity of rhizome extracts of Zingiber zerumbet (L.) Smith

Introduction In this study, we used dichloromethane (DCM) and methanol (MeOH) extracts of the Zingiber zerumbet rhizome to evaluate brine shrimp lethality and larvicidal activity on Aedes aegypti and Anopheles nuneztovari mosquitoes. Methods Bioassays were performed by exposing third-instar larvae of each mosquito species to the DCM or MeOH extracts. Results Probit analysis with DCM and MeOH extracts demonstrated efficient larvicidal activity against A. aegypti and A. nuneztovari larvae. Conclusions The DCM and MeOH extracts showed higher activity against A. nuneztovari larvae than against A. aegypti larvae, suggesting that the extracts have species-specific activity. .

Synthesis and cytotoxic activity of some derivatives of alkyl piperidine

Synthesis of novel phenacyl derivatives of alkyl piperidine as cytotoxic agents via simple and single step reaction procedure is going to be reported here. Twelve new compounds were successfully synthesized in moderate yield and in solid form. Their synthesis was confirmed by TLC, melting point, CHN analysis and through different spectral studies such as UV, IR, Mass and proton NMR. The advantages of this synthetic route are simple operation, mild reaction conditions and good yields. These newly synthesized derivatives were extensively explored for their cytotoxicity by brine shrimp lethality assay

Bioactivity evaluation against Artemia salina Leach of medicinal plants used in Brazilian Northeastern folk medicine / Avaliação da bioatividade frente à Artemia salina Leach de plantas medicinais utilizadas na medicina popular na Região Nordeste do Brasil

The brine shrimp (Artemia salina Leach) lethality bioassay offers an advantage in standardization and quality control of botanical products. This test is well correlated with antitumor activity (cytotoxicity) and can be used to monitor the activity of bioactive natural products. This paper reports the bioactivity of ethanol extracts from seven medicinal plants from the Northeast of Brazil (Acmella uliginosa, Ageratum conyzoides, Eugenia uniflora, Plectranthus neochilus, Moringa oleifera, Justicia pectoralis and Equisetum sp.) against Artemia salina. Biological activity was evaluated for extracts at 1, 10, 100, and 1000 µg/mL in triplicate, and the mean lethal concentration values (LC50) were obtained by probit analysis. The species Acmella uliginosa showed the highest bioactivity, and its flower extract was more active than its leaf extract.

O bioensaio em Artemia salina Leach oferece uma vantagem na padronização e no controle de qualidade de produtos botânicos. Esse teste é bem correlacionado com a atividade antitumoral (citotoxicidade) e pode ser usado para monitorar a atividade de produtos naturais bioativos. Este trabalho relata a bioatividade de extratos etanólicos de sete plantas medicinais (Acmella uliginosa, Ageratum conyzoides, Eugenia uniflora, Plectranthus neochilus, Moringa oleifera, Justicia pectoralis e Equisetum sp.) contra Artemia salina. A bioatividade foi avaliada em triplicata paraextratos nas concentrações de 1, 10, 100 e 1000 µg/mL, e os valores das concentrações letais para metade dos animais (CL50) foram obtidos por meio da análise de probitos. A espécie Acmella uliginosa apresentou a maior bioatividade frente à Artemia salina e o extrato etanólico de suas flores apresentou maior atividade do que o das folhas.

Anti-proliferation effect of Hevea brasiliensis latex B-serum on human breast epithelial cells

The rubber tree [Hevea brasiliensis] extracts are becoming increasingly visible in pharmaceutical and therapeutical research. The present study is aimed at examining the specific anti-proliferation property of H. brasiliensis latex B-serum sub-fractions against human breast cancer epithelial cell lines MCF-7 and MDA-MB231. The results showed that the latex whole B-serum and DBP sub-fraction exerted a specific anti-proliferation activity against cancer origin cells MDA-MB231 but had little effect on non-cancer-origin cells. On the other hand, the anti-proliferative activity was diminished in the pre-heated B-serum fractions. With the low toxicity that the B-serum demonstrated previously in Brine Shrimp Lethality Test [BSLT], the present results suggest the potential use of the B-serum subfractions in cancer treatment

Pharmacological and biological evaluation of extracts from Gratiola officinalis L. [Scrophulariaceae]

The crude extract of Gratiola officinalis and its n-hexane, chloroform, ethyl acetate, n-butanol and aqueous fractions were subjected to biological [Brine Shrimp Bioassay, Insecticidal and Phytotoxicity/Cytotoxic] and neuropharmacological [Head dip, Open field Forced swimming test, Sodium pentothal induced sleep] activities. Results obtained in this study indicated that at high concentration dose [1000microg/ml], all test samples showed 60-95% phytotoxicity. In crude extract, n-butanol and aqueous fractions produced more than 85% phytotoxicity. While low concentration [10microg/ml] dose showed 25-28% phytotoxicity in all test samples. The crude extract was devoid of any effect against the growth of Callosbruchus analis and Tribolium castaneum and caused 10 mortality of Rhyzopertha dominica. n-Hexane, chloroform, ethylacetate, n-butanol and aqueous fractions caused 50, 30, 40, 10 and 20% mortality respectively of C. analis where as chloroform, ethyl-acetate, aqueous and crude extract, n-hexane, ethyl-acetate fractions also caused low mortality [10%] of Tribolium castaneum and Rhyzopertha dominica respectively. In cytotoxic assay at 1000microg/ml concentration, n-butanol fraction produced 36.7% and the crude extract produced 13.3% mortality of brine shrimp, its aqueous fraction was inactive at all concentrations. The results of head dip, open field, mobility time and Pentothal Na induced sleep indicated that crude extract, n-butanol and ethylacetate fractions of G. officinalis had mild sedative effect. However aqueous fraction was found to produce a significant decrease in motor activities and potentiated the duration of sleep

Antioxidant, Antibacterial activity and Brine shrimp toxicity test of some Mountainous Lichens from Nepal

A total of twenty four lichen species belonging to six families were collected from mountainous region of Nepal. The methanol extracts of each species were tested for antimicrobial and antioxidant activitiesin vitro. It was found that extracts of twenty one lichen species were active againstB. subtilis and seven species were active againstS. aureus. Similarly, in DPPH assay, three speciesPeltigera sp.,Cladonia sp., andCanoparmelia sp. showed comparable activity with commercial standard, BHA. In ABTS+ assay, extracts ofParmoterma sp.,Ramalina sp.,Peltigera sp. andCladonia sp. showed stronger activity than ascorbic acid. The observed data after comparison with previously published reports indicated that the high altitude lichens contain stronger antioxidant and antibacterial constituents. Similarly, the methanol extracts ofHeterodermia sp. andRamalina sp. showed comparable toxicity effect with commercial standard berberine chloride indicating a potent source of anticancer drugs.

antifungal, cytotoxic, antitermite and insecticidal activities of zizyphus jujube

Plants are very useful, self-generating machines, producing a variety of useful bioactive products. Keeping in view this idea, the crude methanolic extract and various fractions of Zizyphus jujuba were screened for antifungal, cytotoxic, antitermite and insecticidal activities. Low activity was shown by the crude methanolic extract [12%], n-hexane [9%], chloroform [20%] and ethyl acetate [14%] fraction against Penicillium notatum. Low activity was shown by the ft-hexane fraction against Aspergillus niger [10%] and Trichoderma harzianum [13%] and inactive against Aspergillus flavus, Fusarium oxysporum and Rhizopus stolonifer. The CHC1[3] fraction exhibited low activity of 10% against F. oxysporum while showing no activity against the rest of the test fungi. All the test samples were inactive against Rhizopus stolonifer. The crude methanolic extract was highly cytotoxic [73.33%] at the concentration of 1000 [microg/ml] while the rest of the test samples were low in toxicity at the same concentration. The crude methanolic extract of Zizyphus jujuba showed significant antitermite activity against Heterotermes indicola, among the test samples. Against Tribolium castaneum, Rhizopertha dominica and Callosbruchus analis the insecticidal activity was determined. All the test samples except rc-hexane showed low activity [20%] against T. castaneum. The w-hexane fraction showed low activity [20%] against R. dominica while the rest of the fractions were inactive against it. Low activity of 40% and 20% was shown by the chloroform and "-hexane fraction respectively against C. analis. The results of the present study revealed that the plant could be as potent source of cytotoxic drugs

Chronic toxicity bioassay with populations of the crustacean Artemia salina exposed to the organophosphate diazinon

A chronic toxicity bioassay was conducted with the microcrustacean Artemia salina as the testing organism for the toxic organophosphate diazinon in order to determine if the species is an appropriate indicator of pollution in aquatic environments. Tests of animal exposure to different concentrations of the toxicant were performed for 24, 48 and 72 hours after larvae hatching. Registered mortality data was used to obtain the lethal dose 50 (LD50) of the organophosphate for each exposure time, considering the immobilization of A. salina larvae as the mortality parameter. The lethal concentration (LD50) in the same exposure times was calculated by evaluating morphological changes on the three initial stages of larval development. Both doses were determined by using probit statistical analysis. Results indicate greater dose-response exactitude after 24 hours of exposure to the toxicant. High sensitivity of the organism to the toxicant was determined, thus indicating that A. salina is an appropriate ecotoxicological bioindicator of aquatic environments polluted with pesticides, with the special consideration that this species is a natural resident of saline water bodies, and thus could be used to control pollution in these environments as a result of the unrestrained usage of such toxic substances.

In vitro antiplasmodial activity and toxicity assessment of plant extracts used in traditional malaria therapy in the Lake Victoria Region

As part of our program screening the flora of the Lake Victoria Region, a total of 54 organic extracts from seven plant families (8 species) were individually tested for antiplasmodial activity against chloroquine-sensitive [Sierra Leone (D-6)] and chloroquine-resistant [Vietnam (W-2)] strains. Only 22 percent of these extracts exhibited very high in vitro antiplasmodial activity. Six methanol (MeOH) extracts and one chloroform extract showed in vitro antiplasmodial activity against the D-6 Plasmodium falciparum strain, while only three MeOH extracts were active against the W-2 strain. All of the ethyl acetate extracts proved to be inactive against both strains of P. falciparum. A brine shrimp cytotoxicity assay was used to predict the potential toxicity of the extracts. The cytotoxicity to antiplasmodial ratios for the MeOH extracts were found to be greater than 100, which could indicate that the extracts are of low toxicity.