Croton stipulaceus Kunth, a native Mexican medicinal plant with antioxidant and anti-inflammatory activities / Croton stipulaceus Kunth, planta medicinal mexicana con actividad antioxidante y antiinflamatoria

Leaves of Croton stipulaceuswere extracted (EHex, ECHCl3and EEtOH extracts) to assesstheir antioxidant potential, anti-inflammatory activity in murine models and acute toxicity. EEtOH showed the highest effect in DPPH (37.80% inhibition), FRAP (1065.00 ± 55.30 µmolFe2+) and total polyphenols (231.24 ± 9.05 meq AG/gM). EHex was the most active, ~ 50% inhibition of TPA-induced ear edema; while EEtOH (dose of 2 mg/ear) showed the highest inhibition in the chronic model (97% inhibition), and inhibited MPO activity (48%). In carrageenan-induced edema, ECHCl3(dose 500 mg/kg) was the most active. None of the extracts showed acute toxicity (LD50) at 2 g/kg (p.o.). This work is the first report that supports the traditional use of C. stipulaceusas an anti-inflammatory.

De las hojas de Croton stipulaceusse obtuvieron diferentes extractos (EHex, ECHCl3y EEtOH) evaluando el potencial antioxidante y la actividad antiinflamatoria en modelos murinos y la toxicidad aguda. El EEtOH mostró mayor efecto en DPPH (37.80% inhibición), FRAP (1065.00 ± 55.30 µmolFe2+) y polifenolestotales (231.24 ± 9.05 meq AG/gM). El EHex fue el más activo, cercano al 50% de inhibición del edema auricular inducido con TPA; mientras que el EEtOH (dosis de 2 mg/oreja) mostró la mayor inhibición en el modelo crónico (97% inhibición), e inhibió la actividad de la MPO (48%). En el edema inducido con carragenina, el ECHCl3(dosis 500 mg/kg) fue el más activo. Ninguno de los extractos mostró una toxicidad aguda (DL50) mayor a 2 g/kg (p.o). Este trabajo es el primer reporte que sustenta el uso tradicional de C. stipulaceuscomo antiinflamatorio.

Phytochemical characterization, antioxidant potential and antibacterial activity of the Croton argyrophylloides Muell. Arg. (Euphorbiaceae) / Caracterização fitoquímica, potencial antioxidante e atividade antibacteriana do Croton argyrophylloides Muell. Arg. (Euphorbiaceae)

Abstract Croton argyrophylloides Muell. Arg., from the Euphorbiaceae family, popularly known as marmeleiro prateado or sacatinga, is a plant from the Caatinga biome commonly found in Brazil's northeastern region. The present study aimed to evaluate the antioxidant activity of the species. The phytochemical study was performed through qualitative analysis of chemical constituents and quantitative determination of the total phenol content through the Folin-Ciocalteu test. The qualitative and quantitative antioxidant tests were performed using the DPPH method (2.2 diphenyl-1-picryl hydrazil) and ferric reducing antioxidant power (FRAP). The minimum inhibitory concentration (MIC) was determined by microdilution in 96-well plates. The ethanolic extract of the leaves of C. argyrophylloides manifested antioxidant action in the quantitative DPPH test with a significant bioactivity of 84.70 AAO% in 500 µg/mL, with an EC50 of 236.79. The content of total phenolic compounds was 946.06 mg of gallic acid equivalents/g of sample, and total flavonoids was 58.11 mg of quercetin equivalents/g of sample, the result obtained for FRAP was 15294.44 µM Trolox/g of sample and ABTS was 718 μM Trolox of sample. The prospecting of the chemical constituents of the leaves of C. argyrophylloides revealed the presence of the main compounds that manifests the antioxidant activity and it was proven by the DPPH method that there is antioxidant activity in the analyzed sample, in addition to demonstrating a significant content of phenolic compounds and total flavonoid content in the species, which corroborates the antioxidant activity of the plant sample. The leaf extracts presented growth inhibition halos of 10 and 12 mm upon Staphylococcus aureus ATCC 25923.

Resumo Croton argyrophylloides Muell. Arg., pertencente à família Euphorbiaceae, conhecida popularmente como marmeleiro prateado e sacatinga, é um vegetal do bioma caatinga comumente encontrado no Nordeste do Brasil. O presente trabalho teve como objetivo avaliar a atividade antioxidante da espécie. O estudo fitoquímico foi realizado por meio de análise qualitativa dos constituintes químicos e determinação quantitativa do teor de fenóis totais pelo teste de Folin-Ciocalteu. Os testes antioxidantes qualitativos e quantitativos foram realizados pelo método do DPPH (2,2 difenil-1- picril-hidrazila) e redução do ferro (FRAP). A concentração inibitória mínima (CIM) foi determinada por microdiluição em placas de 96 poços. O extrato etanólico das folhas de C. argyrophylloides apresentou ação antioxidante no teste DPPH quantitativo com uma significativa bioatividade de 84.70 AAO% em 500 µg/mL, apresentando um CE50 de 236.79. O teor de compostos fenólicos totais, foi de 946,06 mg equivalentes de ácido gálico/g de amostra, e de flavonoides totais de 58,11 mg equivalentes de quercetina/g da amostra, o valor encontrado para FRAP foi de 15294,44 µM Trolox/g da amostra e de ABTS foi 718 μM Trolox da amostra. A prospecção dos constituintes químicos das folhas de C. argyrophylloides revelou a presença dos principais compostos que caracterizam a atividade antioxidante e foi possível comprovar pelo método de DPPH que há atividade antioxidante na amostra analisada, além de demonstrar um resultado significativo de teor de compostos fenólicos e teor de flavonoides totais na espécie e o que corrobora com a atividade antioxidante da amostra vegetal. Os extratos das folhas apresentaram halos de inibição de crescimento de 10 e 12mm frente a Staphylococcus aureus ATCC 25923.

Phytochemical characterization, antioxidant potential and antibacterial activity of the Croton argyrophylloides Muell. Arg. (Euphorbiaceae) / Caracterização fitoquímica, potencial antioxidante e atividade antibacteriana do Croton argyrophylloides Muell. Arg. (Euphorbiaceae)

Croton argyrophylloides Muell. Arg., from the Euphorbiaceae family, popularly known as marmeleiro prateado or sacatinga, is a plant from the Caatinga biome commonly found in Brazil's northeastern region. The present study aimed to evaluate the antioxidant activity of the species. The phytochemical study was performed through qualitative analysis of chemical constituents and quantitative determination of the total phenol content through the Folin-Ciocalteu test. The qualitative and quantitative antioxidant tests were performed using the DPPH method (2.2 diphenyl-1-picryl hydrazil) and ferric reducing antioxidant power (FRAP). The minimum inhibitory concentration (MIC) was determined by microdilution in 96-well plates. The ethanolic extract of the leaves of C. argyrophylloides manifested antioxidant action in the quantitative DPPH test with a significant bioactivity of 84.70 AAO% in 500 µg/mL, with an EC50 of 236.79. The content of total phenolic compounds was 946.06 mg of gallic acid equivalents/g of sample, and total flavonoids was 58.11 mg of quercetin equivalents/g of sample, the result obtained for FRAP was 15294.44 µM Trolox/g of sample and ABTS was 718 µM Trolox of sample. The prospecting of the chemical constituents of the leaves of C. argyrophylloides revealed the presence of the main compounds that manifests the antioxidant activity and it was proven by the DPPH method that there is antioxidant activity in the analyzed sample, in addition to demonstrating a significant content of phenolic compounds and total flavonoid content in the species, which corroborates the antioxidant activity of the plant sample. The leaf extracts presented growth inhibition halos of 10 and 12 mm upon Staphylococcus aureus ATCC 25923.

Croton argyrophylloides Muell. Arg., pertencente à família Euphorbiaceae, conhecida popularmente como marmeleiro prateado e sacatinga, é um vegetal do bioma caatinga comumente encontrado no Nordeste do Brasil. O presente trabalho teve como objetivo avaliar a atividade antioxidante da espécie. O estudo fitoquímico foi realizado por meio de análise qualitativa dos constituintes químicos e determinação quantitativa do teor de fenóis totais pelo teste de Folin-Ciocalteu. Os testes antioxidantes qualitativos e quantitativos foram realizados pelo método do DPPH (2,2 difenil-1- picril-hidrazila) e redução do ferro (FRAP). A concentração inibitória mínima (CIM) foi determinada por microdiluição em placas de 96 poços. O extrato etanólico das folhas de C. argyrophylloides apresentou ação antioxidante no teste DPPH quantitativo com uma significativa bioatividade de 84.70 AAO% em 500 µg/mL, apresentando um CE50 de 236.79. O teor de compostos fenólicos totais, foi de 946,06 mg equivalentes de ácido gálico/g de amostra, e de flavonoides totais de 58,11 mg equivalentes de quercetina/g da amostra, o valor encontrado para FRAP foi de 15294,44 µM Trolox/g da amostra e de ABTS foi 718 µM Trolox da amostra. A prospecção dos constituintes químicos das folhas de C. argyrophylloides revelou a presença dos principais compostos que caracterizam a atividade antioxidante e foi possível comprovar pelo método de DPPH que há atividade antioxidante na amostra analisada, além de demonstrar um resultado significativo de teor de compostos fenólicos e teor de flavonoides totais na espécie e o que corrobora com a atividade antioxidante da amostra vegetal. Os extratos das folhas apresentaram halos de inibição de crescimento de 10 e 12mm frente a Staphylococcus aureus ATCC 25923.

Chemical characterization, cytotoxicity, antimicrobial and antioxidant potential of Justicia pectoralis Jacq and Croton jacobinensis Baill extracts

Abstract In this research, aqueous and ethanolic extracts from Justicia pectoralis Jacq and Croton Jacobinensis Baill were characterized. The UPLC-QTOF-MSE analysis was performed on the extracts identified, predominantly, flavonoids, tannins and acids. The extracts did not indicate toxicity in human epithelial cells. C. jacobinensis presented a concentration of phenolics 60.5% higher than J. pectoralis in all scenarios evaluated and, for both samples, the hydroalcoholic extract at 70% exhibited the best efficiency in the extraction (14501.3 and 32521.5 mg GAE 100 g-1 for J. pectoralis and C. jacobinensis, respectively). The antioxidant activity presented a positive correlation with the concentration of phenolics, being 1.186,1 and 1.507,9 µM of Trolox for J. pectoralis and C. jacobinensis at 70% of ethanol; however, it was not verified statistical difference between the ethanolic solutions (p < 0.05). The antimicrobial activity of J. pectoralis extracts was highlighted once was the most effective against gram-positive bacteria. The results suggest that both J. pectoralis and C. jacobinensis extracts present the potential to be applied as natural additives due to their antioxidant and antimicrobial activity and safety. Thus, it is suggesting the development of studies that could investigate the interaction of these plant extracts with food matrices is required

Chemical composition and phytotoxicity of essential oils of Croton doctoris S. Moore (Euphorbiaceae) / Composição química e fitotoxicidade dos óleos essenciais de Croton doctoris S. Moore (Euphorbiaceae)

Essential oils from the stems and leaves of Croton doctoris were analyzed by gas chromatography and mass spectrometry, resulting in 22 identified compounds. The effects of these essential oils on the germination, root and shoot growth, total chlorophyll content, potential root respiration, peroxidase activity, catalase, superoxide dismutase, and mitotic index in lettuce and onion were determined. Antioxidant, antimicrobial, and cytotoxic activity were also investigated. The results revealed that the stem oil consisted of 15 compounds, of which caryophyllene oxide (24.5%) and E-caryophyllene (13.3%) were the major constituents. The leaf oil contained E-caryophyllene (39.6%) and α-humulene (13.2%) as major compounds. The oils inhibited the germination and growth of lettuce and onion seedlings and reduced chlorophyll content, root respiration, and cell division. They also caused oxidative stress, indicated by the increased activity of the evaluated antioxidant enzymes. These abnormal physiological processes contributed to the inhibition of plant growth. The most pronounced phytotoxic effects were observed in the stem oil. The cytotoxicity tests indicated that leaf oil was more active than stem oil, resulting from the presence of biologically active sesquiterpenes that inhibit the growth of cancer cells.

Os óleos essenciais do caule e da folha de Croton doctoris foram analisados por cromatografia gasosa (GC) e espectrometria de massa (GC-MS) resultando em 22 compostos identificados. Os efeitos dos óleos essenciais na germinação, crescimento de raízes e parte aérea, teor total de clorofila, respiração radicular, atividade de peroxidase, catalase e superóxido de dimetase e índice mitótico foram determinados em alface e cebola. Atividade antioxidante, antimicrobiana e citotóxica também foram investigadas. Os resultados revelaram que o óleo do caule é constituído por 15 compostos, dos quais os principais são o óxido de cariofileno (24,5%) e E-cariofileno (13,3%). O óleo foliar apresentou E-cariofileno (39,6%) seguido de α-humuleno (13,2%) como compostos majoritários. Os óleos inibiram a germinação e o crescimento das plântulas de alface e cebola e reduziram o conteúdo de clorofila, a respiração radicular e a divisão celular. Eles também causaram estresse oxidativo, indicado pelo aumento da atividade das enzimas antioxidantes avaliadas. Esses processos fisiológicos anormais contribuem para a inibição do crescimento das plantas. Os efeitos fitotóxicos mais pronunciados foram observados no óleo do caule. Nos testes de citotoxicidade observou-se que o óleo das folhas foi mais ativo, resultante da presença de sesquiterpenos biologicamente ativos que atuam inibindo o crescimento das células cancerígenas.

Chemical composition and phytotoxicity of essential oils of Croton doctoris S. Moore (Euphorbiaceae) / Composição química e fitotoxicidade dos óleos essenciais de Croton doctoris S. Moore (Euphorbiaceae)

Essential oils from the stems and leaves of Croton doctoris were analyzed by gas chromatography and mass spectrometry, resulting in 22 identified compounds. The effects of these essential oils on the germination, root and shoot growth, total chlorophyll content, potential root respiration, peroxidase activity, catalase, superoxide dismutase, and mitotic index in lettuce and onion were determined. Antioxidant, antimicrobial, and cytotoxic activity were also investigated. The results revealed that the stem oil consisted of 15 compounds, of which caryophyllene oxide (24.5%) and E-caryophyllene (13.3%) were the major constituents. The leaf oil contained E-caryophyllene (39.6%) and α-humulene (13.2%) as major compounds. The oils inhibited the germination and growth of lettuce and onion seedlings and reduced chlorophyll content, root respiration, and cell division. They also caused oxidative stress, indicated by the increased activity of the evaluated antioxidant enzymes. These abnormal physiological processes contributed to the inhibition of plant growth. The most pronounced phytotoxic effects were observed in the stem oil. The cytotoxicity tests indicated that leaf oil was more active than stem oil, resulting from the presence of biologically active sesquiterpenes that inhibit the growth of cancer cells.

Os óleos essenciais do caule e da folha de Croton doctoris foram analisados por cromatografia gasosa (GC) e espectrometria de massa (GC-MS) resultando em 22 compostos identificados. Os efeitos dos óleos essenciais na germinação, crescimento de raízes e parte aérea, teor total de clorofila, respiração radicular, atividade de peroxidase, catalase e superóxido de dimetase e índice mitótico foram determinados em alface e cebola. Atividade antioxidante, antimicrobiana e citotóxica também foram investigadas. Os resultados revelaram que o óleo do caule é constituído por 15 compostos, dos quais os principais são o óxido de cariofileno (24,5%) e E-cariofileno (13,3%). O óleo foliar apresentou E-cariofileno (39,6%) seguido de α-humuleno (13,2%) como compostos majoritários. Os óleos inibiram a germinação e o crescimento das plântulas de alface e cebola e reduziram o conteúdo de clorofila, a respiração radicular e a divisão celular. Eles também causaram estresse oxidativo, indicado pelo aumento da atividade das enzimas antioxidantes avaliadas. Esses processos fisiológicos anormais contribuem para a inibição do crescimento das plantas. Os efeitos fitotóxicos mais pronunciados foram observados no óleo do caule. Nos testes de citotoxicidade observou-se que o óleo das folhas foi mais ativo, resultante da presença de sesquiterpenos biologicamente ativos que atuam inibindo o crescimento das células cancerígenas.

New sources of botanical acaricides from species of Croton with potential use in the integrated management of Tetranychus urticae / Nuevas fuentes de acaricidas botánicos de especies de Croton con uso potencial en el manejo integrado de Tetranychus urticae

Essential oils from the leaves and stems of Croton adenocalyx, C. grewioides, C. heliotropiifoliusand C. blanchetianus obtained through hydrodistillation were analyzed by GC-MS. We then investigated the lethal and sublethal effects of the Croton oils and 15 major constituents against Tetranychus urticae. ß-Caryophyllene was the major component in the leaf and stem oils from C. heliotropiifolius and C. adenocalyx. Spathulenol and (E)-anethole were the major constituents identified in the leaf and stem oils of C. blanchetianus and C. grewioides, respectively. The oil with the greatest lethal and sublethal effects was those from C. adenocalyx. Among the constituents ß-caryophyllene and spatulenol were the most toxic to the mite, where as eugenol and methyl eugenol were the most repellent. The toxicity and repellency of the Croton oils, particularly the oils from C. adenocalyx, demonstrate that these oils constitute a promising alternative to synthetic acaricides for use in the control of T. urticae.

Los aceites esenciales de las hojas y tallos de Croton adenocalyx, C. growioides, C. heliotropiifolius y C. blanchetianus obtenidos mediante hidrodestilación fueron analizados a través de GC-MS. Se investigaron los efectos letales y subletales de los aceites de Croton y 15 componentes principales contra Tetranychus urticae. El ß-cariofileno fue el componente principal en los aceites de hojas y tallos de C. heliotropiifolius y C. adenocalyx. El espatulenol y el (E)-anetol fueron los principales componentes identificados en los aceites de hojas y tallos de C. blanchetianus y C. growioides, respectivamente. El aceite con los mayores efectos letales y subletales fue el de C. adenocalyx. Entre los componentes, el ß-cariofileno y el espatulenol fueron los más tóxicos para el ácaro, mientras que el eugenol y el metil eugenol fueron los más repelentes. La toxicidad y la repelencia de los aceites de Croton, particularmente los aceites de C. adenocalyx, demuestran que estos aceites constituyen una alternativa prometedora respecto a los acaricidas sintéticos para uso en el control de T. urticae.

Vascular interactions of Croton schiedeanus major flavonoids in isolated aortic rings from Wistar rats / Interacciones vasculares de los principales flavonoides de Croton schiedeanus en anillos aislados de aorta de ratas Wistar

Background: Ayanin (3,7,4'-Tri-O-methylquercetin) and 3,7-Di-O-methylquercetin (DMQ) are the main active metabolites isolated by bioguided fractionation from Croton schiedeanus, species known popularly in Colombia as "almizclillo", which has been studied in experimental models in rats, exerting vasodilator and antihypertensive effects. Also, when the effect of these flavonoids was studied separately, important vasodilation was observed. Objective:To evaluate whether flavonoids from Croton schiedeanus have synergistic vasodilator properties when different combinations are used in isolated aorta rings. Methods: Cumulative concentrations of ayanin (10-8 M - 6x10-5 M or 0.01 µM - 60 µM) were assayed in the absence and presence of an increasing concentration of 3,7-Di-O-methylquercetin (DMQ) (10-8 ­ 3x10-5M or 0.01­30 µM) in isolated rings from Wistar rats, pre-contracted with phenylephrine. The concentration-response curve with the maximal effect was compared with that obtained by Croton schiedeanus whole ethanolic extract (10-6 ­ 3x10-4 g/mL). Also, this combination was assayed in the presence of the nitric oxide synthetase inhibitor L-NAME (10-4 M) and the guanylate cyclase inhibitor methylene blue (10-4 M) to assess the role of the NO/cGMP pathway in this interaction. Results: Ayanin and DMQ display a dual interaction in vascular relaxant response: agonism at higher concentration ranges (10-6 ­ 3x10-5 M or 1­30 µM) and antagonism at lower concentration ranges (10-8 ­ 3x10-7 M or 0.01­0.3 µM). The efficacy at the highest concentration was greater than that obtained by the whole extract (Emax: 98.4% vs. 33.9%). This response was decreased but not reverted in the presence of L-NAME and methylene blue. Thus, the vasodilator effect of this combination does not depend entirely on the NO/cGMP cyclic pathway. Conclusion: The combined use of appropriate concentrations of these flavonoids could represent an advantage over Croton schiedeanus whole extract for vasodilator purposes

Antecedentes: Ayanina (3,7,4'-Tri-O-metilquercetina) y 3,7-Di-O-metilquercetina (DMQ) son los principales metabolitos activos aislados mediante fraccionamiento bioguiado, a partir de Croton schiedeanus, especie conocida popularmente en Colombia como "almizclillo", la cual ha sido estudiada en modelos experimentales en ratas, ejerciendo efectos antihipertensivos y vasodilatadores. Además, al estudiar por separado el efecto de los flavonoides, se observó importante vasodilatación. Objetivo:Evaluar si los principales flavonoides de Croton schiedeanus tienen propiedades vasodilatadoras sinérgicas al utilizar diferentes combinaciones de ellos en anillos de aorta aislados. Metodología: Se analizaron concentraciones acumulativas de ayanina (10-8 M - 6x10-5 M o 0,01 µM - 60 µM) en ausencia y en presencia de concentraciones crecientes de DMQ (10-8 M - 3x10-5 M o 0,01 µM ­ 30 µM) en anillos aislados de ratas Wistar, pre-contraídos con fenilefrina. La curva concentración respuesta obtenida con el efecto máximo, fue comparada con la obtenida con el extracto etanólico de Croton schiedeanus (10-6 - 3x10-4 g/mL). Adicionalmente, esta combinación fue ensayada en presencia del inhibidor de óxido nítrico sintetasa L-NAME (10-4 M) y el inhibidor de guanilato ciclasa, azul de metileno (10-4 M) para evaluar el papel de la vía NO/GMPc en esta interacción. Resultados: Ayanina y DMQ muestran una interacción dual en la respuesta vascular relajante: agonismo en el rango más alto (10-6 M ­ 3x10-5 M o 1 µM ­ 30 µM), y antagonismo en el rango más bajo (10-8 M ­ 3x10-7 M o 0.01 µM ­ 0,3 µM). A altas concentraciones, la eficacia de los flavonoides fue mayor que las obtenidas por el extracto completo (Emáx: 98,4% vs 33,9%). Esta respuesta disminuyó, pero no se revirtió en presencia de L-NAME y azul de metileno. Por lo tanto, el efecto vasodilatador de esta combinación no depende enteramente de la vía NO/GMPc. Conclusión: El uso combinado de las concentraciones apropiadas de estos flavonoides podría representar una ventaja sobre el extracto de Croton schiedeanus, con propósitos vasodilatadores

Actividad sinérgica in vitro de los alcaloides Crotsparina y Esparsiflorina aislados de Croton bomplandianum frente a Pseudomonas aeruginosa / In vitro synergic activity of the alkaloids Crotsparine and Sparsiflorine, isolated from Croton bomplandianum, against Pseudomonas aeruginosa

Se evaluó la actividad sinérgica de los alcaloides crotsparina y esparsiflorina, aislados de Croton bomplandianum Baill. con los antibacterianos gentamicina y ciprofloxacina frente a Pseudomonas aeruginosa, microorganismo frecuentemente responsable de infecciones intrahospitalarias. Se empleó el método del "tablero de damas". Se encontraron combinaciones que presentaban efecto sinérgico, logrando la reducción de 87,5% de la CMI de gentamicina, mientras que para ciprofloxacina se logró una reducción del 25,0%. Esto abre interesantes perspectivas sobre el uso combinado de productos naturales puros y fármacos en uso clínico para el tratamiento de infecciones producidas por este microrganismo(AU)

Incompatibility mechanism of Crotonis Semen Pulveratum and Glycyrrhizae Radix et Rhizoma based on diuretic effect and intestinal flora structure / 中国中药杂志

Based on the toxic characteristics caused by the compatibility between "Zaoji Suiyuan" and Glycyrrhizae Radix et Rhizoma, which was found in the previous studies, the expanded study was carried out on the incompatibility mechanism between Crotonis Semen Pulveratum(CT) and Glycyrrhizae Radix et Rhizoma(GU) with the diuretic effect and intestinal flora as the characteristic indexes. The results showed that GU could slow down the rapid diuretic effect of CT, which suggested a tendency of decreasing the efficacy. Both the high and low dose of CT could significantly induce the intestinal injury and change the intestinal bacteria structure of mice. Low dose CT combined with GU could significantly increase the levels of Streptococcus and Rikenellaceae＿ukn. The relative abundance of Desulfovibrio and Streptococcaceae＿ukn were increased after the combined application of high dose CT and GU. It also suggested that there was a risk of inflammation in the liver and intestines when combined application of these two herbs. The results revealed that the combination of CT and GU has a tendency to reduce the clinical effect and increase the toxicity from the aspects of its traditional efficacy and its effect on intestinal microflora structure, which could provide the data for the clinical use of CT.

Evaluación de la actividad anticolagenasa del látex de Croton lechleri / Evaluation of the anti-collagenase activity of the latex of Croton lechleri latex

Objetivo. Determinar la capacidad inhibitoria del látex de Crotón lechleri (sangre de grado) frente a la enzima colagenasa, atenuando la formación de arrugas como consecuencia del efecto hidrolítico del colágeno por parte de la enzima. Materiales y métodos. Se ha utilizado el método in vitro de Thing para probar la actividad anticolagenasa, comparando la actividad del látex con el control positivo conformado por una solución epigalocatequina (EGCG) a concentraciones de 125, 250, 500 1000 ug/mL. Resultados. El porcentaje de inhibición de Látex de Croton lechleri a concentración de 0 ug/mL es 0; de 125 ug/mL es 5,67; de 250 ug/mL es 17,34, de 500 ug/mL es 33,41 y de 1000 ug/mL es 59,53. Conclusiones. El látex de Croton lechleri exhibió una actividad anticolagenasa significativa superando al control positivo, mostrando una IC50 de 908,02 y 1892,03 ug/mL respectivamente.

Objective. Determine the inhibitory capacity of Croton lechleri latex (Dragon's Blood) against the collagenase enzyme, reducing wrinkle formation as a consequence of the hydrolytic effect of the collagen by the enzyme. Materials and methods. Thing's in vitro method has been used to test the anti-collagenase activity, compared the activity of the latex with the positive control formed by an epigallocatechin solution (EGCG) at concentrations of 125, 250, 500 1000 ug/mL. Results. The percentage of Croton lechleri latex inhibition at a concentration of 0 ug/mL is 0, 125 ug/mL is 5.67, 250 ug/mL is 17.34, 500 ug/mL is 33.41 and 1000 ug / mL is 59.53. Conclusion. It has been concluded that Croton lechleri latex has exhibited significant anti collagenase activity exceeding the positive control, showing an IC50 of 908.02 and 1892.03 ug/mL respectively.

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.

Atividade antibiofilme de substâncias de Croton urucurana em Staphylococcus aureus isolado de mastite bovina / Antibiofilm activity of Croton urucurana compounds against Staphylococcus aureus isolated from mastitis in dairy cattle

A mastite bovina é a enfermidade que causa maior impacto na produção leiteira, sendo o microrganismo Staphylococcus aureus o mais prevalente. Este gênero possui a capacidade de produzir biofilmes que é um importante mecanismo de resistência aos antibióticos. Considerando a capacidade terapêutica das plantas, a espécie Croton urucurana, nativa do Cerrado, foi alvo do presente estudo, que teve como objetivo avaliar a atividade antibiofilme in vitro do extrato vegetal e substâncias isoladas desta espécie, frente Staphylococcus aureus, isolados de leite de vacas com mastite, bem como dos antibióticos gentamicina e vancomicina. A atividade antibiofilme foi avaliada por meio do cristal violeta e da contagem de unidades formadoras de colônia. As imagens foram obtidas por microscopia eletrônica de varredura. O extrato bruto e frações de C. urucurana apresentaram atividade antibiofilme superior à gentamicina e semelhante à vancomicina, enquanto a substância isolada α-Costol foi significativamente mais ativa quando comparada aos demais tratamentos avaliados, reduzindo cerca de 6 ciclos logarítmicos da população bacteriana em biofilme. Conclui-se que os fitocomplexos e a substância α-Costol isolados de Croton urucurana são promissores no combate a um dos principais agentes etiológicos da mastite bovina.(AU)

Mastitis in dairy cattle is the disease that impacts dairy production the most; Staphylococcus aureus is the main causative agent of this condition. The genus Staphylococcus has the ability to produce biofilms, an important mechanism of antibiotic resistance. Bearing in mind that plants have therapeutic action, this study investigated the in vitro antibiofilm activity of the plant extract and compounds isolated from the species Croton urucurana, native to the Brazilian Cerrado, against Staphylococcus aureus isolated from the milk of cows with mastitis, as well as the antibiotic gentamycin and vancomicyn. The antibiofilm activity was evaluated by means of violet crystal and the counting of Colony Forming Units. The images were obtained by scanning electron microscopy. The C. urucurana crude extract and fraction displayed better antibiofilm effect than gentamycin; their antibiofilm action was similar to the action of vancomycin. Compared with all the assessed treatments, the isolated compound α-Costol was significantly more active it reduced six logarithmic cycles of the bacterial population composing the biofilm. The phytocomplexs and the α-Costol substance isolated from Croton urucurana are promising in the fight against one of the main etiological agents of bovine mastitis.(AU)

The Ethanol Extract of Croton Seed Inhibits the Oral Pathogen, Streptococcus mutans

It is noted that Streptococcus mutans (S. mutans) triggers dental caries establishment by two major factors: the synthesis of organic acids, which demineralize dental enamel, and the synthesis of glucans, which mediate the attachment of bacteria to the tooth surface. Therefore, it is noted that the development of a more effective, substantial and safe preventive agent that works against dental caries and periodontal disease is required at this time. For this reason, the present study was designed to investigate the effect of croton seed ethanol extracts on the growth, acid production, adhesion, and insoluble glucan synthesis of S. mutans. In this case, the ethanol extract of croton seed showed concentration dependent inhibitory activity against the growth, acid production and adhesion of S. mutans. Especially, it is important to note that it has produced significant inhibition at the concentration of 0.1 and 0.2 mg/ml as compared to the control group. Moreover, these results suggest that the application of croton seed extract may be considered to be a useful method for the prevention of dental caries.

Flavonols and sesquiterpenoids from outer bark and leaves of Croton polycarpus Benth. (Euphorbiaceae) / Flavonoles y sesquiterpenoides de la corteza y hojas de Croton polycarpus Benth. (Euphorbiaceae)

Some known flavonols from the outer bark polar fraction of the native species Croton polycarpus Benth. (Euphorbiaceae) were isolated and quercetin, quercitrin and rutin were identified as the most abundant constituents. From this sample, a clean TLC non polar sub- fraction (A-1) obtained by CC, afforded several isomeric compounds, which were characterized by GC-MS/EI and its results conduct to a group of eighteen sesquiterpenoids with a unique Rf value in TLC; among them, one sesquiterpene hydrocarbon with molecular weight (MW) of 200 g/mol (C15H20), two with MW 202 g/mol,(C15H22), thirteen with a MW of 204 g/mol (C15H24) and two sesquiterpenols with MW 220 g/mol (C15H24O) were determined. From its fresh leaves essential oil obtained by two methods, hydro-distillation and supercritical CO2 extraction, other terpenoids were identified, where the first one process was more efficient (1.5% DM yield) than the last one, and it was selected for a pilot study. This is the first report about chemical composition of the native species C. polycarpus, and the analysis of sesquiterpene isomerism is very important to recognize its structural diversity and similar chemical behavior.

De la fracción polar de la corteza de la especie nativa Croton polycarpus, (Euphorbiaceae) se separaron algunos flavonoles y quercetina, quercitrina y rutina se identificaron como los constituyentes más abundantes. Desde una fracción apolar de esta muestra, se obtuvo por CC una fracción limpia en CCD (C-2), cuyo fraccionamiento por análisis por CGAR-EM/IE permitió determinar un grupo de 18 sesquiterpenoides mayoritarios los cuales presentan un valor único de Rf; entre estos se detectó un hidrocarburo de PM 200 (C15H20), dos derivados de PM 202 (C15H22), trece son hidrocarburos isómeros con PM 204 g/mol (C15H24) y dos terpenoles de PM 220 uma (C15H24O). De igual forma, de las hojas frescas se extrajo el aceite esencial, por dos métodos: hidrodestilación y extracción con CO2 supercrítico (SFE), y el primero de ellos fue el más eficiente (1,5% rendimiento en peso seco) por lo cual se seleccionó para el desarrollo de experimentos a escala de planta piloto. Este informe es la primera contribución al conocimiento de la composición química y la bioactividad de las hojas y corteza de la especie arbórea nativa Croton polycarpus (Euphorbiaceae) y el análisis de mezclas de sesquiterpenos isómericos es muy importante para reconocer la diversidad estructural y su similitud en polaridad y comportamiento químico.

Efecto de la administración crónica del látex liofilizado de Croton lechleri Muell. Arg. "sangre de drago" en Rattus norvegicus var. Albinus / Effect of chronic administration of latex lyophilised Croton lechleri Muell. Arg. "sangre de drago" in Rattus norvegicus var. Albinus

Objetivo: Determinar si la administración crónica (90 días) del látex liofilizado de Croton lechleri Muell. Arg. "Sangre de drago" modifica los parámetros hematológicos y bioquimicos en Rattus norvegicus var albinus. Materiales y métodos: Se utilizó ratas con un peso corporal (p.c.) entre 150 g a 170 g, distribuidos en Grupo A (control) y Grupos B y C (experimentales), de 20 especímenes cada uno (10 hembras y 10 machos) a las que se administró por vía oral NaCl 0.9% y una dosis diaria de 100 y 200 mg de látex liofilizado/Kg p.c. respectivamente, durante 90 días. Se tomaron muestras de sangre cada 15 días para determinar parámetros hematológicos (hematocrito, linfocitos, leucocitos y segmentados) y bioquímicos (glucosa, urea, creatinina, colesterol total y perfil hepático). Resultados: Todos los valores se encontraron dentro del rango normal. Se encontraron diferencias significativas al comparar los grupos de estudio en los resultados de glucosa (Control vs Grupo I: p<0.001 y Grupo II: p=0.003) y creatinina (Grupo II vs Grupo I: p=0.008 y control: p<0.001). Los valores de bilirrubina total y proteínas totales variaron significativamente durante el tiempo de estudio (p=0.001 y p<0.001, respectivamente). El resto de parámetros no presentaron variaciones significativas por grupos (p>0.05). Conclusión: El látex liofilizado de Croton lechleri Muell. Arg. no generó toxicidad en los parámetros hematológicos y bioquímicos estudiados en Rattus norvegicus var Albinus.

Efecto antinflamatorio in vitro de los extractos etanólicos de cuatro plantas medicinales peruanas / In vitro anti-inflammatory effect of four peruvian medicinal herbs ethanolic extracts

Objetivo: Determinar la actividad antinflamatoria in vitro de los extractos etanólicos de Croton lechleri, Chenopodium ambrosioides L., Peperomia congona Sodiro y Perezia coerulescens, mediante el método de estabilización de la membrana de glóbulos rojos. Materiales y métodos: Se emplearon muestras de sangre humana, donde se evaluaron cuatro diluciones seriadas, 200, 100, 50 y 10 µg/mL de los diferentes extractos, usando una solución isosalina (0,85%, pH 7,2) como medio de dilución, y como fármaco de referencia dexametasona (200 ug/mL). Se determinaron los porcentajes de hemólisis y protección de la membrana del glóbulo rojo. Resultados: Se encontraron diferencias significativas entre los promedios de porcentajes de protección y las concentraciones en el caso de Ch. ambrosioides L (p<0,001), P. coerulescens p<0,001) y C. lechleri (p<0,001). Se encontró correlación lineal entre los porcentajes de protección y la concentración en el caso de Ch. ambrosioides L (R2= 0,795; p<0,001), C. lechleri (R2= 0,631; p<0,001) y P. coerulescens (R2= 0,899; p<0,001). Los extractos de C. lechleri a 100 y 200 ug/mL; y el extracto de P. coerulescens a 200 ug/mL no presentaron diferencias significativas en sus porcentajes de protección en comparación al uso de dexametasona 200 ug/mL (p>0,05). Conclusión: Los extractos etanólicos de P. coerulescens, Ch. ambrosioides L y C. lechleri, presentan actividad antinflamatoria mediante la inhibición de la lisis de la membrana celular en glóbulos rojos. En el caso del extracto de C. lechleri a 100 y 200 ug/mL, así como el extracto de Ch. ambrosioides L a una concentración de 200 ug/mL, mostraron un desempeño similar al fármaco de referencia (dexametasona).

Crotonis Fructus Extract Inhibits 12-O-Tetradecanoylphorbol-13-Acetate-Induced Expression of Matrix Metalloproteinase-9 via the Activator Protein-1 Pathway in MCF-7 Cells / 한국유방암학회지

PURPOSE: Metastatic cancers spread from the primary site of origin to other parts of the body. Matrix metalloproteinase-9 (MMP-9) is essential in metastatic cancers owing to its major role in cancer cell invasion. Crotonis fructus (CF), the mature fruits of Croton tiglium L., have been used for the treatment of gastrointestinal disturbance in Asia. In this study, the effect of the ethanol extract of CF (CFE) on MMP-9 activity and the invasion of 12-O-tetradecanoylphorbol-13-acetate (TPA)-treated MCF-7 cells was examined. METHODS: The cell viability was evaluated using the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. The expression of MMP-9 was examined by Western blotting, zymography, and real-time polymerase chain reaction. An electrophoretic mobility gel shift assay was performed to detect activator protein-1 (AP-1) DNA binding activity and cell invasiveness was measured by an in vitro Matrigel invasion assay. RESULTS: CFE significantly suppressed MMP-9 expression and activation in a dose-dependent manner. Furthermore, CFE attenuated the TPA-induced activation of AP-1. CONCLUSION: The results indicated that the inhibitory effects of CFE against TPA-induced MMP-9 expression and MCF-7 cell invasion were dependent on the protein kinase C δ/p38/c-Jun N-terminal kinase/AP-1 pathway. Therefore, CFE could restrict breast cancer invasiveness owing to its ability to inhibit MMP-9 activity.

Chemical composition, antibacterial and modulatory action of the essential oil of Croton rhamnifolioides leaves Pax and Hoffman / Composição química, ação antibacteriana e moduladora do óleo essencial das folhas de Croton rhamnifolioides Pax and Hoffman

The species Croton rhamnifolioides is a shrub popularly known as "quebra faca", utilized in teas or infusions for the treatment of gastrointestinal disorders as ulcers, gastric discomfort, vomiting and hemorrhagic diarrhea. This work has as its main objective to evaluate the chemical composition of the essential oil of the Croton rhamnifolioides leaves (EOC), antibacterial activity and modulatory activity of antibiotic resistance, against bacterial strains of Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa and, and antifungal activity against Candida albicans, Candida krusei and Candida tropicalis. The chemical composition was determined through chromatography with a gas phase coupled with mass spectrometry (CG/MS), whereas antimicrobial activity and modulation were determined by microdilution assay. The chemical composition of the oil revealed 21 compounds, with the major compounds being spathulenol (22.46%) and 1,8-cineol (18.32%). The antimicrobial activity was not significant with MIC>1024 µg/mL, however, was observed a synergistic interference when essential oil associated with the antibiotics aminoglycoside and -lactam, and the antifungal polyene.

Croton rhamnifolioides is é um arbusto conhecido popularmente como "quebra-faca" e utilizado como chá ou infusão para o tratamento de problemas gastro-intestinais como úlceras, desconforto gástrico, vômitos e diarréias hemorrágicas. O objetivo deste trabalho foi avaliar a composição química do óleo essencial das folhas de Croton rhamnifolioides (OEC), atividade antibacteriana, moduladora da resistência bacteriana, contra linhagens bacterianas de Escherichia coli, Staphylococcus aureus e Pseudomonas aeruginosa e, atividade antifúngica contra Candida albicans, C. krusei e C. tropicalis. A composição química foi determinada através de Espectroscopia de Massas acoplada a Cromatografia Gasosa (EM/CG), enquanto as atividades antimicrobianas e moduladoras foram determinadas pelo método de microdiluição. A composição química do OEC revelou a presença de 21 compostos, sendo os principais o Espatulenol (22,46%) e 1,8-cineol (18,32%). A atividade antimicrobiana não foi considerada significativa apresentando MIC > 1024 µg/mL, contudo, foi observado um sinergismo quando o óleo essencial foi associado com aminoglicosídios, -lactâmicos e antifúngicos poliênicos.

Chemical composition and larvicidal activity against Aedes aegypti of essential oil from Croton jacobinenesis Baill / Composición química y actividad larvicida contra Aedes aegypti de los aceites esenciales de Croton jacobinenesis Baill

The chemical composition of essential oils from leaves, stalks and inflorescences of Croton jacobinensis obtained by hydrodistillation were analyzed by GC-MS. E-caryophyllene, 1,8-cineole, alpha-pinene, viridiflorene, 8-cadinene were the main components in essential oils from plant parts. Essential oils of leaves, stalks, and inflorescences were tested at different concentrations against instar III larvae of Aedes aegypti and showed LC50 of 79.3, 117.2, 65.8 ug/ml, respectively.

La composición química de los aceites esenciales de las hojas, los tallos y las inflorescencias de Croton jacobinensis obtenidos por hidrodestilación se analizaron mediante GC-MS. E-cariofileno, alfa-pineno, 1,8-cineol, viridifloreno, 8-cadineno fueron los principales componentes de los aceites esenciales de partes de la planta. Los aceites esenciales de las hojas, tallos e inflorescencias fueron probados en diferentes concentraciones en contra de instar III de las larvas de Aedes aegypti y mostraron LC50 de 79,3; 117,2; 65,8 ug/ml, respectively.