Effects of Gundelia tournefortii L. on biochemical parameters, antioxidant activities and DNA damage in a rat model of experimental obesity / Efeitos de Gundelia tournefortii L. em parâmetros bioquímicos, atividades antioxidantes e danos ao DNA em um modelo de obesidade experimental de rato

The present study was designed to investigate the effects of Gundelia tournefortii L. plant extract on different tissues in terms of DNA damage, biochemical and antioxidant parameter values in rats with high-calorie diets. With this aim, Wistar albino male rats were divided into 4 groups containing 6 rats each and the study was completed over 12 weeks duration. At the end of the implementation process over the 12 weeks, rats were sacrificed and blood and tissue samples were obtained. Analyses were performed on blood and tissue samples. According to results for DNA damage (8-OHdG), in brain tissue the OG2 group was significantly reduced compared to the NC group. For MDA results in liver tissue, OG1 and OG2 groups were determined to increase by a significant degree compared to the control group, while the OG2 group was also increased significantly compared to the obese group. In terms of the other parameters, comparison between the groups linked to consumption of a high calorie diet (HCD) and administration of Gundelia tournefortii L. in terms of antioxidant activities and serum samples obtained statistically significant results. Gundelia tournefortii L. plant extracts had effects that may be counted as positive on antioxidant parameter activity and were especially identified to improve DNA damage and MDA levels in brain tissues. Additionally, consumption of Gundelia tournefortii L. plant extract in the diet may have antiobesity effects; thus, it should be evaluated for use as an effective weight-loss method and as a new therapeutic agent targeting obesity.

O presente estudo foi desenhado para investigar os efeitos do extrato da planta Gundelia tournefortii L. em diferentes tecidos em termos de danos ao DNA, valores de parâmetros bioquímicos e antioxidantes em ratos com dietas hipercalóricas. Com esse objetivo, ratos Wistar albinos machos foram divididos em 4 grupos contendo 6 ratos cada e o estudo foi concluído ao longo de 12 semanas de duração. No final desse processo de implementação, os ratos foram sacrificados e amostras de sangue e tecido foram obtidas. As análises foram realizadas em amostras de sangue e tecido. De acordo com os resultados para danos ao DNA (8-OHdG), no tecido cerebral o grupo OG2 foi significativamente reduzido em comparação com o grupo NC. Para os resultados de MDA no tecido hepático, os grupos OG1 e OG2 aumentaram significativamente em comparação ao grupo controle, enquanto o grupo OG2 também aumentou significativamente em comparação ao grupo obeso. Quanto aos demais parâmetros, a comparação entre os grupos ligados ao consumo de dieta hipercalórica (DC) e à administração de Gundelia tournefortii L. em termos de atividades antioxidantes e amostras de soro obteve resultados estatisticamente significativos. Os extratos de plantas de Gundelia tournefortii L. tiveram efeitos que podem ser considerados positivos na atividade dos parâmetros antioxidantes e foram especialmente identificados para melhorar os danos ao DNA e os níveis de MDA nos tecidos cerebrais. Além disso, o consumo de extrato vegetal de Gundelia tournefortii L. na dieta pode ter efeitos antiobesidade; portanto, deve ser avaliado para uso como um método eficaz de perda de peso e como um novo agente terapêutico voltado para a obesidade.

Efecto citotóxico de diterpenos derivados del ácido ent-kaureno aislados de Coespeletia moritziana (Sch. Bip. ex Wedd.) Cuatrec / Cytotoxic effect of ent-kaurene acid-derived diterpenes isolated from Coespeletia moritziana (Sch. Bip. Ex Wedd.) Cuatrec

The objective of the work was to study the cytotoxic effect of ent-kaurene acid derivatives obtained from Coespeletia moritziana (Sch. Bip. Ex Wedd.) Cuatrec., After analysis by GC/MS, IR and NMR. Isolating: kaurenic acid (I), grandifloric acid (II), 15-α-hydroxy kaurenic acid (III), 15 α-acetoxy-kaur 16-en-19-oic acid (IV), Kaurenol (V); and by hemisynthesis: 15,16-epoxy-17-acetoxy-kauran 19-oic acid (VI), 15-oxo-ent-kaur-16-en-19-oic acid (VIII), ester 2,3,4,6 -15-oxo-kaur-16-en-19-oic acid acetyl α-D-pyranosyl tetra-tetra (VII). Cytotoxicity was tested in human cancer cell lines: uterus (HeLa), lung (A-549), breast (MCF-7), African green monkey kidney non-tumor line (Vero) and human peripheral blood mononuclear cells (CMPS). Compound (I) was active against HeLa, A-549 and Vero. Compounds (II and VIII) showed moderate and good (IC50 ≤ 9 µM) cytotoxicity, respectively, against the five cell lines. Compound (V) showed moderate activity against A-549 and compound (VII), slight cytotoxicity against HeLa and A-549. Results that show the cytotoxic specificity of the isolated kaurenes and derivatives of Coespeletia moritzianaand their therapeutic potential.

El objetivo del trabajo fue estudiar el efecto citotóxico de derivados del ácido ent-kaureno obtenidos de Coespeletia moritziana (Sch. Bip. ex Wedd.) Cuatrec., previo análisis mediante GC/MS, IR y RMN. Aislandose: ácido kaurénico(I), ácido grandiflorénico (II), ácido 15-α-hidroxi kaurénico(III), ácido 15 α-acetoxi-kaur 16-en-19-oico (IV), Kaurenol (V); y por hemisíntesis: ácido 15,16-epoxi-17-acetoxi-kauran 19-oico (VI), ácido15-oxo-ent-kaur-16-en-19-oico (VIII), éster 2,3,4,6-tetra acetil α-D-piranosilo del ácido 15-oxo-kaur-16-en-19-oico (VII). La citotóxicidad fue ensayada en líneas celulares cancerosas humanas: útero (HeLa), pulmón(A-549), mama (MCF-7), línea no tumoral de riñón de mono verde africano (Vero) y células mononucleares humanas de sangre periférica (CMPS). El compuesto (I) resultó activo frente a HeLa, A-549 y Vero. Los compuestos (II y VIII), mostraron moderada y buena (IC50≤9µM) citotoxicidad respectivamente, frente a las cinco líneas celulares. El compuesto (V) presentó moderada actividad frente a A-549 y el (VII), leve citotoxicidad frente a HeLa y A-549. Resultados que evidencian la especificidad citotóxica de los kaurenos aislados y derivados de Coespeletia moritzianay su potencial terapéutico.

Cytotoxic effect of hydroalcoholic extract of Cota tinctoria (L) J. Gay on AGS and Hep-G2 cancer cell lines / Efecto citotóxico del extracto hidroalcohólico de Cota tinctoria (L) J. Gay sobre líneas celulares de cáncer AGS y Hep-G2

Cota tinctoria is a medicinal plant which has been used for management of cancer in folk medicine of various regions. The aim of present study is to investigate cytotoxic activity of different concentrations of hydroalcoholic extract of C. tinctoria flowers on gastric (AGS) and liver (Hep-G2) cancer cell lines as well as Human Natural GUM fibroblast (HUGU) cells. Cell mortality rates were examined after 24, 48 and 72 h incubations using the MTT assay. IC50of extract on AGS cells after 24, 48 and 72h was 1.46, 1.29 and 1.14 µg/mL respectively. The extract demonstrated IC50 of 5.15, 3.92 and 2.89 µg/mL on Hep-G2 cells after 24, 48 and 72 h respectively. No cytotoxic effect was detected on HUGU (Human Natural GUM fibroblast) cells. C. tinctoria seems to have a promising potential to be considered as a source for anticancer drug discovery. However, more experimental and clinical studies are required.

Cota tinctoria es una planta medicinal que se ha utilizado para el tratamiento del cáncer en la medicina popular de varias regiones. El objetivo del presente estudio es investigar la actividad citotóxica de diferentes concentraciones de extracto hidroalcohólico de flores de C. tinctoria en líneas celulares de cáncer gástrico (AGS) e hígado (Hep-G2), así como en células de fibroblasto GUM humano natural (HUGU). Se examinaron las tasas de mortalidad celular después de incubaciones de 24, 48 y 72 h utilizando el ensayo MTT. La CI50 del extracto en células AGS después de 24, 48 y 72 h fue de 1,46; 1,29 y 1,14 µg respectivamente. El extracto demostró una CI50 de 5,15, 3,92 y 2,89 µg/mL en células Hep-G2 después de 24, 48 y 72 h, respectivamente. No se detectó ningún efecto citotóxico en las células HUGU (fibroblasto GUM humano natural). C. tinctoria parece tener un potencial prometedor para ser considerada como una fuente de descubrimiento de fármacos contra el cáncer. Sin embargo, se requieren más estudios experimentales y clínicos.

In vitro and in vivo antioxidant potentials of the methanolic crude extract from Inula glomerata Oliv. & Hiern (Asteraceae) and Salacia kraussii (Harv) Harv (Celastraceae) / Potenciales antioxidantes in vitro e in vivo del extracto crudo metanólico de Inula glomerata Oliv. & Hiern. (Asteraceae) y Salacia kraussii (Harv) Harv (Celastraceae)

Reactive oxygen species are implicated in multiple pathological conditions including erectile dysfunction. This study evaluated the in vitro and in vivo antioxidant potential of the methanolic extracts of Inula glomerata and Salacia kraussii. The plant materials were pulverized and extracted with methanol. The phytochemical analysis, ability of the crude extracts to scavenge free radicals (ABTS, DPPH, NO.) in vitroas well as the total phenolic and flavonoid contents was investigated. In vivo, antioxidant potentials of the crude extracts (50/250 mg/kg body weight) were determined in an erectile dysfunction rat model. The phytochemical analysis revealed that both plants contain flavonoids, tannins, terpenoids, and alkaloids. The crude extracts at varying degree of efficiency, scavenged ABTS and DPPH radicals. The crude extracts at low concentrations (50 mg/kg b.w) significantly (p<0.05) diminished the level of malondialdehyde, augmented catalase activities and elevated glutathione levels. However, SOD activities were significantly boosted in a dose-dependent manner by the crude extracts. Therefore, I. glomerataand S. kraussiipossess antioxidant properties, hence, can serve as a therapeutic modality in the treatment of oxidative stress-induced erectile dysfunction.

Las especies reactivas de oxígeno están implicadas en múltiples condiciones patológicas, incluyendo la disfunción eréctil. Este estudio evaluó el potencial antioxidante in vitro e in vivo de extractos metanólicos de Inula glomeratay Salacia kraussii. Los materiales vegetales fueron pulverizados y extraídos con metanol. A estos extractos crudos se les llevó a cabo el análisis fitoquímico junto con el contenido total de fenólicos y flavonoides, así como se les investigó la capacidad in vitro para atrapar radicales (ABTS, DPPH, NO.). Los potenciales antioxidantes in vivo de los extractos crudos (50/250 mg/kg de peso corporal) se determinaron en un modelo en ratas con disfunción eréctil. El análisis fitoquímico reveló que ambas plantas contuvieron flavonoides, taninos, terpenoides y alcaloides. Los extractos crudos con un grado variable de eficiencia, atraparon a los radicales ABTS y DPPH. Los extractos crudos a bajas concentraciones (50 mg/kg p.c) significativamente (p<0.05) disminuyeron el nivel de malondialdehído, aumentaron las actividades de catalasa y elevaron los niveles de glutatión. Sin embargo, las actividades de SOD por los extractos crudos fueron significativamente dosis-dependientes. Así, los extractos de I. glomeratay S. kraussii mostraron propiedades antioxidantes, y por lo tanto, podrían servir como una alternativa terapéutica en el tratamiento de disfunción eréctil inducida por estrés oxidativo.

Assessment of Antioxidant and Cytotoxic Activities and Identification of Phenolic Compounds of Centaurea solstitialis and Urospermum picroides from Turkey

HIGHLIGHTS The phenolic composition, antioxidant activity and cytotoxic potential of the extracts of C. solstitialis and U. picroides were investigated. Caffeic acid was found as the most abundant phenolic compound in the extracts. Both species showed promising antioxidant activity towards different assays. The highest cytotoxic potential was observed in the extract of C. solstitialis.

Abstract It is known that some genera of the Asteraceae family are commonly used in Turkish folk medicine. Several studies have investigated the biological effects of different extracts of Centaurea and Urospermum species, but studies involving the phenolic composition of C. solstitialis and U. picroides extracts are very limited. This study aimed to investigate the phenolic composition and antioxidant activity of C. solstitialis and U. picroides and evaluate their possible cytotoxic effect. RP-HPLC analysis was used to elucidate the phenolic profiles of the ethanolic extracts of flowering parts of C. solstitialis and U. picroides.The both ethanolic extracts were assessed for their antioxidant properties using DPPH, FRAP, phosphomolybdenum and metal chelating assays. Furthermore, the effect of the extracts on cell viability was evaluated against MCF-7 and PC-3 cancer cells and HEK293 cell line using the MTT assay. The most abundant phenolic compound in both extracts was determined to be caffeic acid, and the amount of this compound was 24078.03 and 14329.59 µg g-1 in the extracts of C. solstitialis and U. picroides, respectively. The antioxidant activity of the extracts was found similar. Compared with U. picroides extract, C. solstitialis extract had higher potential on the inhibition of cell viability. The IC50 value of C. solstitialis on MCF cells was found as 58.53 µg mL-1. These data suggest that the extracts of C. solstitialis and U. picroides may be considered as novel and alternative natural antioxidant and anticancer sources.

Germacranolide sesquiterpenes from Carpesium cernuum and their anti-leukemia activity / 中国天然药物

In this study, three new germacranolide sesquiterpenes (1-3), together with six related known analogues (4-9) were isolated from the whole plant of Carpesium cernuum. Their structures were established by a combination of extensive NMR spectroscopic analysis, HR-ESIMS data, and ECD calculations. The anti-leukemia activities of all compounds towards three cell lines (HEL, KG-1a, and K562) were evaluated in vitro. Compounds 1-3 exhibited moderate cytotoxicity with IC

In vitro cytotoxic and genotoxic effects of Cissus verticillata and Sphagneticola trilobata used for treatment of Diabetes Mellitus in Brazilian folk medicine

Cissus verticillata and Sphagneticola trilobata have been used in Brazilian folk medicine for Diabetes Mellitus treatment, although their pharmacological and toxicological profile has not been clearly established. Thus, the aim of this study was to evaluate the preclinical toxicity of the aqueous extracts of C. verticillata and S. trilobata. The main groups of secondary metabolites were investigated, and the species differed by the presence of coumarins in C. verticillata and by tannins in S. trilobata extracts. The highest contents of phenolic compounds and flavonoids were quantified in C. verticillata infusion with 2.594 ± 0.04 mg equivalents of gallic acid g-1 of extract and 1.301 ± 0.015 mg equivalents of catechin g-1 of extract, respectively. While the extract of S. trilobata showed minimum values of these compounds, with 0.002 ± 0.001 mg equivalents of gallic acid g-1 extract and 0.005 ± 0.0004 mg equivalents of catechin g-1 of extract, respectively. These differences implied the results of in vitro antioxidant activity evaluated using ferric reducing antioxidant power (FRAP), in which the sample of C. verticillata at 5 mg mL-1 showed a value of 122 µM ferrous sulfate equivalents (FSE), while S. trilobata showed 0.93 µM FSE at the same concentration. With respect to cytotoxic assay with murine fibroblast cell line (3T3) only S. trilobata exhibited cytotoxic effects measured by MTT and Sulforhodamine B assays, evidenced by the cell viability value of approximately 16%, in both tests after 24 and 72 hours of exposure of the cells to 5 mg mL-1 of the extract. Comparatively, at 5 mg mL-1 the C. verticillata extract showed cell viability of 142% and 95%, respectively, after 24 hours of cell exposure. On the other hand, both species showed genotoxic profiles evidenced by chromosomal aberrations by Allium cepa bioassay, observed by the higher percentage values of chromosome bridges, chromosome loss, and disturbed anaphase for all concentrations of both extracts than those of the negative control. The results support the characterization of the toxicological profile for both species and create an alert regarding the use of S. trilobata, which should be avoided.

Avaliação morfo-histológica e morfo-histométrica de feridas cutâneas tratadas com Sphagneticola trilobata (L) Pruski em ratos / [Morphohistological and morphohistometric evaluation of skin wounds treated with Sphagneticola trilobata (L) Pruski in rats]

O objetivo deste trabalho foi avaliar macro e microscopicamente a atividade cicatrizante da Sphagneticola trilobata em feridas cutâneas induzidas em ratos, a partir da aplicação de creme contendo extrato hidroalcoólico bruto de folhas da planta. A análise fitoquímica apresentou terpenos e flavonoides como compostos majoritários. Sessenta ratos foram divididos em três grupos experimentais (n=20): grupo tratado (GT), grupo controle (GC) e grupo controle absoluto (GCA). Quatro feridas excisionais de 0,8cm de diâmetro foram realizadas no dorso dos animais, tratadas diariamente e avaliadas nos tempos três, sete, 14 e 21 dias de pós-operatório (PO) quanto à contração e à avaliação macroscópica, morfo-histológica e morfo-histométrica. Macroscopicamente, não houve diferença estatística na contração das feridas entre os grupos testados. Na avaliação morfológica e na morfométrica, o GT apresentou menor concentração de células inflamatórias, maior e melhor preenchimento do tecido de granulação pelas fibras colágenas e melhor vascularização das feridas. Não houve diferença entre o GC e o GCA. Conclui-se que o creme à base do extrato hidroalcoólico bruto das folhas de Sphagneticola trilobata contribui positivamente para o processo de cicatrização das feridas em pele de ratos.(AU)

The objective of this work was to macro and microscopically evaluate the healing activity of Sphagneticola trilobata in rat-induced skin wounds by applying cream containing crude hydroalcoholic extract from plant leaves. The phytochemical analysis showed terpenes and flavonoids as major compounds. Sixty rats were divided into three experimental groups (n=20): treated group (GT), control group (CG) and absolute control group (GCA). Four 0.8cm diameter excision wounds were performed on the back of the animals, treated daily and evaluated at the three, seven, 14 and 21 postoperative days (PO) for contraction, macroscopic, morphologic and morphologic evaluation. The TG presented smaller scar area at 21 postoperative days (P<0.05). In the morphological and morphometric evaluation, the WG presented lower inflammation, greater and better filling of granulation tissue by collagen fibers and better wound vascularization. There was no difference between GC and GCA. It was concluded that the cream based on the crude hydroalcoholic extract of Sphagneticola trilobata leaves contribute positively to the healing process of the skin wounds of rats.(AU)

Phenolic profile and antioxidant, acetylcholinesterase, and tyrosinase inhibitor activities of Jurinea tzar-ferdinandii Davidov, an endemic plant of the Balkans / Perfil fenólico y actividad antioxidante, acetilcolinesterasa e inhibidora de tirosinasa de Jurinea tzar-ferdinandii Davidov, planta endémica de los Balcanes

The methanol extract of the Balkan endemic species Jurinea tzar-ferdinandii Davidov demonstrated weak antioxidant activity against DPPH• and ABTS+• and low inhibitory potential against acetylcholinesterase (8.3% Inh.) and tyrosinase (IC50 = 208 ± 8 µg/mL) enzymes. Phytochemical investigation of the extract led to isolation and identification of apigenin, luteolin, apigenin-7-O-glucoside, apigenin-4'-O-glucoside, apigenin-7-O-gentiobioside, luteolin-4'-O-glucoside, rutin, narcissin, chlorogenic and 1,5-dicaffeoylquinic acid. With exception of apigenin and rutin, all isolated compounds are reported for the first time in the representatives of genus Jurinea. The distribution of flavonoids was discussed from chemotaxonomic point of view.

El extracto de metanol de la especie endémica de los Balcanes Jurinea tzar-ferdinandii Davidov demostró una actividad antioxidante débil contra DPPH• y ABTS+• y un bajo potencial inhibidor contra las enzimas acetilcolinesterasa (8.3% Inh.) tirosinasa (IC50 = 208 ± 8 µg/mL). La investigación fitoquímica del extracto condujo al aislamiento e identificación de apigenina, luteolina, apigenina-7-Oglucósido, apigenina-4'-O-glucósido, apigenina-7-O-gentiobiósido, luteolina-4'-O-glucósido, rutina, narcissin, clorogénico y ácido 1,5- dicafeoilquinico. Con excepción de la apigenina y la rutina, todos los compuestos aislados se informan por primera vez en el género Jurinea. La distribución de flavonoides se discute desde el punto de vista quimiotaxonómico.

Phytochemistry and Biological Activities of Werneria and Xenophyllum species / Fitoquímica y actividades biológicas de especies de Werneria y Xenophyllum

Plants of the genera Werneria (Asteraceae) and Xenophyllum (genus extracted from Werneria) are used in traditional medicine of Latin America for the treatment of mountain sickness, hypertension and gastrointestinal disorders. Only a small number of species of these genera have been studied, leading to the isolation of compounds belonging to the classes of benzofurans, chromenes, acetophenones, coumarates, diterpenes and pyrrolizidine alkaloids. Some of the plant extracts and/or compounds have shown antimicrobial, anti-HIV, hypotensive and photoprotective activities.

Las plantas de los géneros Werneria (Asteraceae) y Xenophyllum (género extraido de Werneria) son usadas en la medicina tradicional de América Latina para el tratamiento del mal de montaña, hipertensión y desórdenes gastrointestinales. Solo un pequeño número de especies de estos géneros ha sido investigado, lográndose aislar compuestos que pertenecen a las clases de benzofuranos, cromenos, acetofenonas, cumaratos, diterpenos y alcaloides pirrolizidínicos. Algunos de los extractos y/o compuestos de dichas plantas han mostrado actividades antimicrobianas, anti-HIV, hipotensoras y fotoprotectoras.

Morphoanatomical and phytochemical studies for the quality control of Neurolaena lobata (L.) R.Br. ex Cass. (Asteraceae) / Estudios morfoanatomicos y fitoquimicos para el control de calidad de Neurolaena lobata (L.) R.Br. ex Cass. (Asteraceae)

Neurolaena lobata (L.) R.Br. ex Cass. (Asteraceae)Is a popular folk remedy for in Central America. The plant is of commercial value in Guatemala but so far there is not any monograph to guide regional laboratories on ensuring identity and chemical tests for this species. As identity test we here run macro and micro morphoanatomical studies of the characters of the vegetative organs. We also developed standard chemical tests for quality by both TLC and HPLC for infusions and tinctures of varying alcoholic strength. Their radical scavenging activities in DPPH and NO were also measured. Macro and micro morphoanatomical characters of the vegetative organs present a set of characteristics to facilitate the identification of dry powdered samples of this species. We developed optimal conditions for the TLC and HPLC phytochemical fingerprints of the 4 most common pharmacopoeial liquid herbal preparations from this herbal drug, namely infusion, 70%, 45% and 20% hydroalcoholic tinctures. Our work provides the Latin-American industry with a set of analyses to establish the identity and chemistry of N. lobata samples for quality control purposes.

Neurolaena lobata (L.) R.Br. ex cass. (Asteraceae) es un remedio popular popular en América Central. La planta tiene un valor comercial en Guatemala, pero hasta el momento no existe una monografía que guíe a los laboratorios regionales para garantizar la identidad y las pruebas químicas para esta especie. Como prueba de identidad proponemos estudios macro y micro morfoanatómicos de los caracteres de los órganos vegetativos. También desarrollamos pruebas químicas de calidad mediante CCF y CLAR para infusiones y tinturas de grado alcohólico variable. También se midieron sus actividades de captación de radicales en DPPH y NO. Los caracteres macro y micro morfoanatómicos de los órganos vegetativos presentan un conjunto de características para facilitar la identificación de muestras de polvo seco de esta especie. Desarrollamos condiciones óptimas para las huellas dactilares fitoquímicas de CCF y CLAR de las 4 preparaciones herbales líquidas farmacopéicas más comunes de esta droga herbal, a saber, infusión, 70%, 45% y 20% tinturas hidroalcohólicas. Nuestro trabajo proporciona a la industria latinoamericana un conjunto de análisis base para establecer la identidad y la química de las muestras de N. lobata con fines de control de calidad.

Effectiveness of aqueous and hydroalcoholic extracts of Acanthospermum australe (Loefl) Kuntze against diarrhea-inducing bacteria / Eficácia de extratos aquosos e hidroalcoólicos de Acanthospermum australe (Loefl) Kuntze contra bactérias indutoras de diarreia

Abstract Leaves and roots of Acanthospermum australe (Asteraceae) have been used in Brazilian folk medicine for the treatment of various ailments including diarrhea, skin diseases, blennorrhagia, dyspepsia, parasitic worms and malaria. The aim of study was to characterize the chemical profiles of the aqueous and hydroalcoholic extracts of leaves and roots of A. australe, and to evaluate their antimicrobial activities against diarrhea-inducing bacteria (Enterococcus faecalis, Shigella dysenteriae and Yersinia enterocolitica), as well as their cytotoxic properties. Aqueous leaf extracts were obtained by infusion, while aqueous root extracts were obtained by decoction. The hydroalcoholic leaf and root extracts were prepared by maceration in 90% ethanol for 3 days. Antimicrobial activity was assessed using standard techniques and cytotoxicity was evaluated using Chinese hamster ovary cells CHO-K1. Chemical analysis revealed the presence of tannins, flavonoids, saponins and phenolic compounds in the extracts. Although root extracts were not effective against E. faecalis, leaf extracts at concentrations of 20 mg/mL exhibited bactericidal activities against this microorganism. The hydroalcoholic root extract was unique in presenting a bactericidal effect against S. dysenteriae. None of the extracts showed bacteriostatic or bactericidal activities against Y. enterocolitica. The results presented herein demonstrate that the Gram-positive E. faecalis and the Gram-negative S. dysenteriae were susceptible to A. australe extracts, although bacteriostatic/bactericidal activities were only observed at concentrations considered too high for clinical application. Our results support the ethnopharmacological use of A. australe in the treatment of gastrointestinal disorders, particularly diarrhea caused by infectious bacteria, although further studies are required to determine the anti-diarrhea effects and the toxicities of the extracts in vivo.

Resumo Folhas e raízes de Acanthospermum australe (Asteraceae) têm sido usadas na medicina popular brasileira para o tratamento de várias doenças, incluindo diarreia, doenças de pele, blenorragia, dispepsia, vermes parasitas e malária. O objetivo deste estudo foi caracterizar os perfis químicos dos extratos aquosos e hidroalcoólicos das raízes e folhas de A. australe, e avaliar as suas atividades antimicrobianas contra as bactérias indutoras de diarreia (Enterococcus faecalis, Shigella dysenteriae e Yersinia enterocolitica), bem como sua citotoxicidade. Os extratos aquosos de folhas foram obtidos por infusão, enquanto que os extratos aquosos de raízes foram obtidos por decocção. Os extratos hidroalcoólicos de folhas e raízes foram preparados por maceração em etanol a 90% durante 3 dias. A atividade antimicrobiana foi avaliada utilizando técnicas padrão e a citotoxicidade foi avaliada utilizando células de ovário de hamster chinês CHO-K1. A análise química revelou a presença de taninos, flavonóides, saponinas e compostos fenólicos nos extratos. Apesar de extratos de raiz não foram eficazes contra E. faecalis, extratos de folhas em concentrações de 20 mg/mL apresentaram atividades bactericidas contra este microrganismo. O extrato hidroalcoólico de raiz foi o único a apresentar um efeito bactericida contra S. dysenteriae. Nenhum dos extratos apresentaram atividades bacteriostáticas ou bactericidas contra Y. enterocolitica. Os resultados apresentados demonstram que a bactéria Gram-positiva E. faecalis e a Gram-negativa S. dysenteriae foram suscetíveis aos extratos de A. australe, embora as atividades bacteriostáticos/bactericidas tenham sido apenas observados em concentrações consideradas elevadas para aplicação clínica. Os nossos resultados apoiam a utilização de etnofarmacológica de A. australe no tratamento de perturbações gastrointestinais, especialmente diarreia causadas por bactérias infecciosas, embora sejam necessários mais estudos para determinar os efeitos anti-diarreia e as toxicidades dos extratos in vivo.

Identificación y determinación estructural de un sesquiterpeno de las hojas de Tessaria integrifolia Ruiz & Pav. y evaluación de su actividad leishmanicida / Identification and structural determination of a sesquiterpene of Tessaria integrifolia Ruiz & Pav. leaves and evaluation of its leishmanicidal activity

RESUMEN Objetivos. Identificar y determinar la estructura del fitoconstituyente de hojas de Tessaria integrifolia Ruiz & Pav con efecto leishmanicida. Materiales y métodos. Se preparó un extracto fluido de hojas de Tessaria integrifolia Ruiz & Pav. que fue concentrado a extracto blando y se utilizó para evaluar la actividad leishmanicida en Mesocricetus auratus con leishmaniasis experimental, administrando vía intramuscular la dosis de 250 mg/kg del extracto blando por 15 días. El extracto fue fraccionado en columna cromatográfica de 45 cm, con un diámetro de 2,5 cm que contiene silicagel G-60, de 70-230 mesh (Sigma-Aldrich®), las nueve fracciones obtenidas fueron evaluadas sobre macrófagos infectados con Leishmania sp para determinar la fracción activa y aislar el compuesto activo, mediante separación, purificación y cristalización, siendo analizado por resonancia magnética nuclear (RMN) de 1H, 13C, y cromatografía líquida acoplada a espectroscopía de masas (LC/MS). Resultados. El extracto fluido de las hojas de Tessaria integrifolia Ruiz & Pav. presenta actividad leishmanicida en Mesocricetus auratus y la fracción F8 es activa sobre macrófagos infectados a dosis de 14 µg/mL. Se elucidó en esa fracción un sesquiterpeno tipo eudesmano ((4aS, 5R,6R,8aR)-6-hidroxi-5,8a-dimetil-3-(1-metiletiliden) octahidronaftalen-2(1H)-ona), según análisis de RMN 1H, 13C, y LC/MS. Conclusiones. El extracto fluido de hojas de Tessaria integrifolia Ruiz & Pav. presenta actividad leishmanicida sobre Mesocricetus auratus. La fracción F8 presenta actividad leishmanicida sobre macrófagos infectados a dosis de 14 µg/mL. Se elucidó en la fracción activa un sesquiterpeno tipo eudesmano según los análisis de RMN 1H, 13C, y LC/MS.

ABSTRACT Objective. To identify and determine the phytoconstituent structure of Tessaria integrifolia Ruiz & Pav. leaves with leishmanicidal activity. Materials and Methods. Fluid extract of leaves was prepared, concentrated to soft extract, and used to evaluate leishmanicidal activity in Mesocricetus auratus with experimental leishmaniasis, at the dose of 250 mg/kg of soft extract by intramuscular route for 15 days. Extract was fractionated in 45 cm column chromatography with a 2.5 cm diameter, containing G-60 silica gel, and 70-230 mesh (Sigma-Aldrich®). Nine fractions were obtained and assessed on macrophages infected with Leishmania sp to determine the active fraction and isolate the active compound, by separation, purification, and crystallization, analyzed by nuclear magnetic resonance (NMR) of 1H, 13C, and liquid chromatography coupled to mass spectroscopy (LC/ MS). Results. Fluid extract from the leaves of T. integrifolia presents leishmanicidal activity in M. auratus. Fraction F8 is active on infected macrophages at a dose of 14 μg/mL. An eudesman type sesquiterpene ((4aS, 5R, 6R, 8aR) -6-hydroxy-5, 8a-dimethyl-3- (1-methylethylidene) octahydronaphthalen-2 (1H) -one) was identified, by RMN 1 H, 13C, and LC / MS analysis. Conclusions. Fluid extract of leaves of Tessaria integrifolia Ruiz & Pav. presents leishmanicidal activity on Mesocricetus auratus with experimental leishmaniasis. Fraction F8 presents leishmanicidal activity on infected macrophages at a dose of 14 μg/mL. An eudesman type sesquiterpene was identified, according to 1 H, 13C, and LC / MS NMR analysis.

Repellent activity of essential oils extracted from five Artemisia species against Tribolium castaneum (Coleoptera: Tenebrionidae) / Actividad repelente de aceites esenciales extraídos de cinco especies de Artemisia contra Tribolium castaneum (Coleoptera: Tenebrionidae)

Artemisia genus (family Asteraceae) has been widely used as medicines and cosmetic. The chemical compositions of essential oils extracted from five Artemisia species (A. anethoides, A. giraldii, A. roxburghiana, A. rubripes and A. sacrorum) were analyzed and the repellent activities of five essential oils were investigated by testing percent repellency (PR) in petri dish against Tribolium castaneum. By GC-MS analysis, the common components of the five essential oils were eucalyptol (11.09%-50.05%), camphor (6.28%-33.10%), terpinen- 4-ol (2.46%-12.41%), ß-caryophyllene (0.63%-10.68%) and germacrene D (2.28%-10.01%). 3,3,6-trimethyl-1,4-heptadien-6-ol (11.72%), 2-isopropyl-5-methyl-3-cyclohexen-1-one (24.80%) and ß-farnesene (12.23%) were the characteristic compounds in essential oils of A. sacrorum, A. anethoides and A. rubripes respectively. The essential oils of five plants showed repellent activity against T. castaneum. The PR of others four essential oils were comparable with DEET expect for A. sacrorum. The results indicated that the essential oils of A. anethoides, A. giraldii, A. roxburghiana and A. rubripes had the potential to be developed as repellent for control of T. castaneum.

El género Artemisia (familia Asteraceae) ha sido ampliamente utilizado como medicamentos y cosméticos. Se analizaron las composiciones químicas de los aceites esenciales extraídos de cinco especies de Artemisia (A. anethoides, A. giraldii, A. roxburghiana, A. rubripes y A. sacrorum) y se investigaron las actividades repelentes de cinco aceites esenciales mediante la prueba de repelencia porcentual (PR) en placa de petri contra Tribolium castaneum. Por análisis GC-MS, los componentes comunes de los cinco aceites esenciales fueron eucaliptol (11,09% -50,05%), alcanfor (6,28% -33,10%), terpinen-4-ol (2,46% -12,41%), ß-cariofileno 0,63% -10,68%) y germacrén D (2,28% -10,01%). 3,3,6-trimetil-1,4-heptadien-6-ol (11,72%), 2-isopropil-5-metil-3-ciclohexen-1-ona (24,80%) y ß-farneseno (12,23%). Los compuestos característicos en los aceites esenciales de A. sacrorum, A. anethoides y A. rubripes respectivamente. Los aceites esenciales de cinco plantas mostraron actividad repelente contra T. castaneum. El PR de otros cuatro aceites esenciales eran comparables con DEET esperado para A. sacrorum. Los resultados indicaron que los aceites esenciales de A. anethoides, A. giraldii, A. roxburghiana y A. rubripes tienen el potencial de ser desarrollados como repelentes para el control de T. castaneum.

Evaluation of cytotoxic and antitumoral properties of Tessaria absinthioides (Hook & Arn) DC, "pájaro bobo", aqueous extract

Higher plants have provided various natural derived drugs used currently in western medicine. Tessaria absinthioides (Hook. & Arn.) DC, Asteraceae, is a native plant from South-America with reported ethnopharmacological and culinary uses. Despite recent scientific reports about plants properties, there is not a well conducted research about its anticancer and potential toxic effects. The current work demonstrates the plant aqueous extract composition; the in vitro induced cytotoxicity, and explores, in vivo, its oral toxicity and antitumoral effects. Composition of aqueous extract was determined by phytochemical reactions. Cytotoxicity was tested in tumoral (Hela, Gli-37, HCT-116 and MCF-7) and non-tumoral (HBL-100) cells, using MTT assay. Oral toxicity and the antitumor activity against colorectal carcinoma were studied in rodents. The chemical analysis revealed the presence of flavonoids, carbohydrates, sterols, terpenes and tannins. Cytotoxicity towards tumoral cells was observed (CV50: 3.0 to 14.8 μg/ml); while in non-tumoral cells, extracts evidenced a selective reduced toxicity (CV50: 29.5 μg/ml). Oral administration of the extract does not induce acute nor dose-repeated toxicity at doses up to 2000 mg/kg and 1000 mg/kg/day, respectively. The antitumoral effect was confirmed by a significant increase in a median survival from 24 weeks (non-treated) to 30 weeks (T. absinthioides treated). The present data indicate that T. absinthioides extract exhibits cytotoxicity against cancer cell lines, with no-toxic effects and significant antitumoral effects in colorectal cancer when is orally administrated. In conclusion, T. absinthioides possesses selective cytotoxicity and antitumoral activities, making its plant derivatives products promising for cancer research and treatment.

Las plantas superiores han provisto numerosos derivados naturales usados actualmente por la medicina occidental. Tessaria absinthioides (Hook & Arn) DC, Asteraceae, es una planta autóctona de Sudamérica con informes de uso etnofarmacológico y culinario. A pesar de los reportes científicos sobre las propiedades de esta planta, no existen estudios que caractericen sus efectos antitumorales ni sus efectos tóxicos. En el presente trabajo se describe la composición del extracto acuoso de T. absinthioides, sus propiedades citotóxicas in vitro, y explora in vivo la toxicidad oral y su capacidad de afectar la progresión de tumores. La composición se determinó mediante reacciones fitoquímicas. La citotoxicidad se estudió en líneas celulares tumorales (Gli-37, HeLa, HCT-116 y MCF-7) y no tumorales (HBL-100), utilizando el ensayo de MTT. La toxicidad oral de los extractos y su capacidad antitumoral sobre carcinoma colorrectal se analizaron en roedores. El análisis del extracto acuoso evidenció flavonoides, carbohidratos, esteroles, terpenos y taninos. La citotoxicidad sobre células tumorales resultó similar a la observada para el 5-fluoracilo (CV50: 3.0 a 14.8 μg/ml); mientras que, en células no tumorales, el efecto estuvo selectivamente reducido (CV50: 29.5 μg/ml). La administración oral del extracto no indujo toxicidad aguda ni a dosis repetidas (dosis hasta 2000 mg/kg y 1000 mg/kg/día, respectivamente). Los efectos antitumorales se confirmaron mediante un significativo aumento de la supervivencia en el grupo tratado con T. absinthioides. En conclusión, de acuerdo a los resultados obtenidos, T. absinthioides y sus derivados naturales representan un campo prometedor de estudio para la investigación en el tratamiento del cáncer.

Descripción de Tessaria dodeneifolia (Hook. & Arn.) Cabrera, (Asteraceae), "la planta dulce" como endulzante natural / Description of Tessaria dodeneifolia (Hook. & Arn.) Cabrera, (Asteraceae), the sweet plant

Los conocimientos etnobotánicos constituyen aportes importantes en la vida del hombre y han permitido la aplicación del uso tradicional de las plantas medicinales, aromáticas, alimenticias. Así, en la comunidad de Ybabiyu, Distrito de Guazucua del Departamento de Ñeembucú, Paraguay, se reporta la utilización de las hojas de una especie vegetal conocida con el nombre de "hierba dulce" ("ka ́a he ́ê") (hierba dulce) como endulzante en sustitución del azúcar. El estudio fue cualitativo, observacional y descriptivo. El ámbito geográfico fue la Región del Ñeembucú, en la localidad conocida como Ybabiyu, distrito de Guazucua. La especie fue colectada en su hábitat natural, procedente de una propiedad privada de la zona. Fue identificada como Tessaria dodoneifolia (Hook. & Arn.) Cabrera (Asteraceae). Este uso, para esta especie, es reportado por primera vez para el Paraguay. A, además se describe las características y los aspectos ecológicos de la especie denominada "ka ́a he ́hierba dulceê" (Tessaria dodoneifolia) utilizada como endulzante de alimentos líquido, en la Región de Ñeembucú, Paraguay. Esta especie tiene amplia distribución y usos variados en países de América del Sur.

Ethnobotanical knowledge is important contributions in the life of man and allowed the application of traditional use of medicinal, aromatic, food plants. Thus, in the community of Ybabiyu, Guazucua District Department of Ñeembucú, the use of the leaves of a plant species known as "sweet plant" ("ka ́a he ́ê " (sweet plant) as a sweetener to replace sugar is reported . The study was qualitative, observational and descriptive. The geographical area was the region of Ñeembucú, in the locality known as Ybabiyu, Guazucua district. The species was collected in the wild, from a private property in the area. It was identified as Tessaria dodoneifolia (Hook. & Arn.) Cabrera (Asteraceae). This use is reported for the first time for Paraguay, plus features and ecological aspects of the species called "ka ́a he ́ê " (Tessaria dodoneifolia) used as a sweetener in liquid food, in the region of Ñeembucú, Paraguay. This species is widely distributed and has varied used in South America countries.

Inhibitory effect of the Pseudobrickellia brasiliensis (Spreng) R.M. King & H. Rob. aqueous extract on human lymphocyte proliferation and IFN-γ and TNF-α production in vitro

Pseudobrickellia brasiliensis (Asteraceae) is a plant commonly known as arnica-do-campo and belongs to the native flora of the Brazilian Cerrado. The alcoholic extract of the plant has been used as an anti-inflammatory agent in folk medicine, but the biological mechanism of action has not been elucidated. The present study evaluated the composition of P. brasiliensis aqueous extract and its effects on pro-inflammatory cytokine production and lymphocyte proliferation. The extracts were prepared by sequential maceration of P. brasiliensis leaves in ethanol, ethyl acetate, and water. Extract cytotoxicity was evaluated by trypan blue exclusion assay, and apoptosis and necrosis were measured by staining with annexin V-FITC and propidium iodide. The ethanolic (ETA) and acetate (ACE) extracts showed cytotoxic effects. The aqueous extract (AQU) was not cytotoxic. Peripheral blood mononuclear cells stimulated with phorbol myristate acetate and ionomycin and treated with AQU (100 μg/mL) showed reduced interferon (IFN)-γ and tumor necrosis factor (TNF)-α expression. AQU also inhibited lymphocyte proliferative response after nonspecific stimulation with phytohemagglutinin. The aqueous extract was analyzed by liquid chromatography coupled with photodiode array detection and mass spectrometry. Quinic acid and its derivatives 5-caffeoylquinic acid and 3,5-dicaffeoylquinic acid, as well as the flavonoids luteolin and luteolin dihexoside, were detected. All these compounds are known to exhibit anti-inflammatory activity. Taken together, these findings demonstrate that P. brasiliensis aqueous extract can inhibit the pro-inflammatory cytokine production and proliferative response of lymphocytes. These effects may be related to the presence of chemical substances with anti-inflammatory actions previously reported in scientific literature.

Tridax procumbens flavonoids: a prospective bioactive compound increased osteoblast differentiation and trabecular bone formation

BACKGROUND: The Tridax procumbens extracts (TPE) are known for their ethno-medicinal properties to increase osteogenic functioning in mesenchymal stem cells. Recently, we found that the T. procumbens flavonoids (TPF) significantly suppressed the RANKL-induced osteoclasts differentiation and bone resorption. The TPF also promoted osteoblasts differentiation and bone formation demonstrated by increasing bone formation markers in cultured mouse primary osteoblasts. However, the effects of the TPF on in vivo bone formation remain unclear. In this study, we investigated the effects of the TPF on in vivo bone formation, injected the TPF (20 mg/kg) twice a day in the low calcium diet mice and killed them after 21 day. Radiographic and histomorphometric analyses were performed on the dissected bones to determine the anabolic effects of the TPF. RESULTS: Bone mineral density and bone mineral content of the TPF-treated mice were significantly increased compared to the control mice. Bone formation-related indices like osteoblast number, osteoblast surface, bone volume, mineralizing surface, mineral apposition rate and bone formation rate were significantly increased in the TPF-treated mice compared to the control mice. CONCLUSION: Our findings point towards the stimulation of bone formation by TPF, suggested that the TPF could be a potential natural anabolic agent to treat patients with bone loss-associated diseases such as osteoporosis.

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.

Effects of budlein A on human neutrophils and lymphocytes

ABSTRACT Sesquiterpene lactones (SLs) are the active constituents of a variety of medicinal plants used in traditional medicine for the treatment of inflammatory diseases and other ailments. Objective In this study, we evaluated whether budlein A modulates the activation of innate and adaptive immune cells such as neutrophils and lymphocytes. Material and Methods Our research group has investigated several plant species and several compounds have been isolated, identified, and their medical potential evaluated. Budlein A is a SL isolated from the species Aldama buddlejiformis and A. robusta (Asteraceae) and shows anti-inflammatory and anti-nociceptive activities. Advances in understanding how plant-derived substances modulate the activation of innate and adaptive immune cells have led to the development of new therapies for human diseases. Results Budlein A inhibited MPO activity, IL-6, CXCL8, IL-10, and IL-12 production and induces neutrophil apoptosis. In contrast, budlein A inhibited lymphocyte proliferation and IL-2, IL-10, TGF-β, and IFN-γ production, but it did not lead to cell death. Conclusions Collectively, our results indicate that budlein A shows distinct immunomodulatory effects on immune cells.