Formulation development and evaluation of gastroretentive floating beads with Brucea javanica oil using ionotropic gelation technology / 中国天然药物

In the present study, a gastric retention floating system for Brucea javanica oil, composed of alginate and carrageenan, was prepared using ionotropic gelation. Parameters for floatability, drug load, encapsulation efficiency, bead morphology, in vitro release, and in vivo gastric retention were evaluated. The optimized formulation via Box-Behnken design consisted of 1.7% alginate (W/V), 1.02% carrageenan (W/V), 1.4% CaCO (W/V), and a gelling bath of pH 0.8. The alginate-carrageenan-Brucea javanica oil beads had a porous structure and exhibited up to 24 h of in vitro floatability with a load capacity of 45%-55% and an encapsulation efficiency of 70%-80%. A 6-h sustained release was observed in vitro. The beads had a prolonged gastric retention (> 60% at 6 h) in fasted rats, compared to non-floating beads (15% at 6 h), as measured by gamma scintigraphy with single-photon emission tomography/computed tomography (SPET/CT). In conclusion, the alginate-carrageenan-Brucea javanica oil system showed enhanced oil encapsulation efficiency, excellent floating and gastric retention abilities, and a favorable release behavior.

Formulation development and evaluation of gastroretentive floating beads with Brucea javanica oil using ionotropic gelation technology / 中国天然药物

In the present study, a gastric retention floating system for Brucea javanica oil, composed of alginate and carrageenan, was prepared using ionotropic gelation. Parameters for floatability, drug load, encapsulation efficiency, bead morphology, in vitro release, and in vivo gastric retention were evaluated. The optimized formulation via Box-Behnken design consisted of 1.7% alginate (W/V), 1.02% carrageenan (W/V), 1.4% CaCO (W/V), and a gelling bath of pH 0.8. The alginate-carrageenan-Brucea javanica oil beads had a porous structure and exhibited up to 24 h of in vitro floatability with a load capacity of 45%-55% and an encapsulation efficiency of 70%-80%. A 6-h sustained release was observed in vitro. The beads had a prolonged gastric retention (> 60% at 6 h) in fasted rats, compared to non-floating beads (15% at 6 h), as measured by gamma scintigraphy with single-photon emission tomography/computed tomography (SPET/CT). In conclusion, the alginate-carrageenan-Brucea javanica oil system showed enhanced oil encapsulation efficiency, excellent floating and gastric retention abilities, and a favorable release behavior.

Lignans from barks of Ailanthus altissima / 中国中药杂志

Eleven lignans were isolated from the ethanol extract of the barks of Ailanthus altissima through various column chromatography methods including silica gel, Sephadex LH-20, ODS and HPLC. By physical, chemical and comprehensive spectroscopic methods, their structures were identified as (+)-neoolivil(1), prunustosanan AI (2), (7S,8R)-guaiacyl-glycerol-β-O-4'-neolignan (3), (7R,8S)-guaiacyl-glycerol-β-O-4'-neolignan (4), (7S,8R)-1-(4-hydroxy-3-methoxyphenyl)-2-[4-(3-hydroxypropyl)-2,6-dimethoxyphenoxy]-1,3-propanediol(5), pinnatifidanin B V (6), pinnatifidanin B VI (7), (7R,7'R,7″S,8S,8'S,8″S)-4',4″-dihydroxy-3,3',3″,5-tetramethoxy-7,9':7',9-diepoxy-4,8″-oxy-8,8'-sesquineolignan-7″,9″-diol (8), hedyotol D (9), 5-(2-propenyl)-7-methoxy-2-(3,4-methylenediovxyphenyl)benzofuran (10), and (7R,8S,7'E)-guaiacyl-glycerol-β-O-4'-sinapyl ether(11).All of these compounds were isolated from this plant for the first time.

Research Progress in Chemical Constituents and Biological Activities of Simaroubaceae Plants / 中国药师

The chemical constituents and their biological activities of simaroubaceae plants were reviewed in the paper. The chemical constituents of simaroubaceae plants are alkaloids and terpenoids, and the biological activities are anti-tumor, insecticidal, antihypertensive, anti-inflammatory, antibacterial and anti-malaria and so on. The review alms to provide references for the comprehen-sive development and utilization of simaroubaceae plants.

Simaroubaceae family: botany, chemical composition and biological activities

The Simaroubaceae family includes 32 genera and more than 170 species of trees and brushes of pantropical distribution. The main distribution hot spots are located at tropical areas of America, extending to Africa, Madagascar and regions of Australia bathed by the Pacific. This family is characterized by the presence of quassinoids, secondary metabolites responsible of a wide spectrum of biological activities such as antitumor, antimalarial, antiviral, insecticide, feeding deterrent, amebicide, antiparasitic and herbicidal. Although the chemical and pharmacological potential of Simaroubaceae family as well as its participation in official compendia; such as British, German, French and Brazilian pharmacopoeias, and patent registration, many of its species have not been studied yet. In order to direct further investigation to approach detailed botanical, chemical and pharmacological aspects of the Simaroubaceae, the present work reviews the information regarding the main genera of the family up to 2013.

Intoxicação experimental por Simarouba versicolor (Simaroubaceae) em ovinos e indução de resistência ao consumo da planta / Experimental poisoning by Simarouba versicolor (Simaroubaceae) in sheep and induced resistance to consumption of the plant

Simarouba versicolor é uma árvore semidecídua pertencente à família Simaroubaceae. Um surto de intoxicação por S. versicolor em bovinos por brotos da planta presente no pasto em Mato Grosso do Sul e sua reprodução experimental foram descritos. Esse estudo teve por objetivos verificar experimentalmente se os ovinos podem ser utilizados como modelo clínico-patológico no estudo da intoxicação por Simarouba versicolor St. Hil. (fam. Simaroubaceae), determinar se há indução de resistência pela ingestão de pequenas e repetidas doses e, se a planta mantém sua toxicidade quando dessecada. Foram realizados dois experimentos, sendo o primeiro com folhas verdes ou folhas dessecadas e trituradas de S. versicolor em doses únicas de 5g/kg, 5g/kg e 3g/kg a três ovinos (Ovino 1, 2 e 3 respectivamente). O experimento 2, foi realizado com diferentes doses diárias de folhas dessecadas e trituradas de S. versicolor em quatro ovinos que receberam 1,5g/kg, 0,75g/kg, 0,6g/kg e 0,3g/kg e, com um ovino que recebeu 3g/kg como controle positivo (Ovino 4). A administração foi suspensa quando os ovinos apresentaram sinais clínicos da intoxicação. Após doze dias de recuperação, os animais sobreviventes foram desafiados com a mesma dose diária da planta ingerida anteriormente para avaliar o desenvolvimento de resistência. Os sinais clínicos observados nos dois experimentos caracterizaram-se por anorexia, mucosas oculares congestas, polidipsia, sialorreia, fezes pastosas que evoluíram para diarreia líquida fétida esverdeada, decúbito lateral e morte para os Ovinos 1 a 7. As principais lesões histológicas observadas foram necrose do tecido linfoide (linfonodos, baço, placas de Peyer) e enterite necrosante. Com os resultados obtidos, pode-se concluir que os ovinos podem ser utilizados como modelo experimental clínico-patológico na intoxicação por S. versicolor. Com o método utilizado, não houve resistência ao consumo diário de folhas da planta pelos ovinos e, as folhas mantiveram sua toxicidade quando dessecadas.(AU)

Simarouba versicolor St. Hil. is a semideciduous tree belonging to the Simaroubaceae family. An outbreak of poisoning in cattle by shoots of S. versicolor present in the pasture in Mato Grosso do Sul and experimental reproduction of the poisoning was described. This study aimed to verify experimentally whether sheep could be used as a clinical-pathological model in the study of the poisoning caused by S. versicolor, to determine if there develops resistance induced by ingestion of small and repeated doses of the leaves, and if the plant keeps its toxicity when dried. Two experiments were conducted: Experiment 1 with green leaves or dried and powdered leave of S. versicolor, given in single doses of 5g/kg, 5g/kg and 3g/kg to three sheep (Sheep 1, 2 and 3 respectively). Experiment 2 was made with different daily doses of dried and powdered leaves of S. versicolor; to four sheep was given 1.5g/kg, 0.75g/kg, 0.6g/kg and 0.3g/kg, and the positive control (Sheep 4) received 3g/kg. The administration was suspended when the animals showed clinical signs of poisoning. After twelve days of recovery, the surviving sheep were challenged with the same daily dose given previously, to assess the development of resistance. Clinical signs observed in both experiments were characterized by anorexia, congested ocular mucosa, polydipsia, drooling, loose stools which evolved into fetid greenish watery diarrhea, lateral decumbency and death of Sheep 1 to 7. The main histological lesions observed were necrosis of lymphoid tissue (lymph nodes, spleen, Peyer's patches) and necrotizing enteritis. With the results it can be concluded that sheep can be used as experimental model for the clinic-pathological aspects of poisoning by S. versicolor. The method used has not shown resistance to the daily consumption of the plant by the sheep, and the leaves kept their toxicity when dried.(AU)

Parámetros micrográficos para la identificación de hojas, corteza y leño de Picrasma crenata (Vell.) Engl. (Simaroubaceae) / Micrographic parameters for the identification of leaves, bark and wood of Picrasma crenata (Vell.) Engl. (Simaroubaceae)

Picrasma crenata (Vell.) Engler (Simaroubaceae) es un árbol de bajo porte conocido popularmente como "palo amargo" o "quina brava", que habita en el noreste de la Argentina, principalmente en la provincia de Misiones. En la medicina tradicional el leño se emplea en forma de infusión, como antimalárico, antipalúdico, antisifilítico y tónico; se lo utiliza también como insecticida en la elaboración de tinturas alcohólicas como sustituto de Quassia amara, para el tratamiento de la pediculosis. El objetivo de este trabajo fue realizar un estudio morfoanatómico de la corteza, el leño y las hojas de P. crenata con el fin de obtener caracteres de valor diagnóstico que permitan una correcta identificación de la especie. Se efectuaron cortes transversales y longitudinales de material fresco que fue incluido en parafina de los tres órganos de la planta, y se colorearon con Safranina-Fast Green y Violeta de Cresilo. Los resultados mostraron que: la corteza se halla constituida por 5-7 peridermis de disposición imbrincada, el floema se halla interrumpido por numerosos radios muy sinuosos y torsionados; el leño, de color blanco amarillento, tiene crecimiento semianular a anular con porosidad difusa no uniforme; las hojas son compuestas, sus folíolos oval elípticos, alternos, presentan mesófilo dorsiventral, estomas anomocíticos solo en la epidermis inferior, tricomas simples y una cavidad esquizolisígena en el parénquima central del nervio medio. (AU)

Actividad antioxidante, análisis fitoquímico y micrografía analítica de hojas de Castela tweedii (Simaroubaceae) / Antioxidant activity, phytochemical analisys and micrographic characterization of Castela tweedii (Simaroubaceae) leaves

Castela tweedii is a small tree belonging to Simaroubaceae family. Infusions of its leaves are used in folk medicine to treat gastrointestinal disorders and diarrhea. In this work, we evaluated the antioxidant activity of ethanol and dicloromethane leaves extracts against DPPH radical (2,2-difenilpicrilhidrazil) in order to justify, at least in part, its popular use. Ethanol extract showed scavenging activity, with an IC50=0.1288 mg/mL. Responsible compounds for these activity were tannins, flavonoids and phenylcarboxilic acids, among them we identified rutine and chlorogenic acid. Microscopic and histochemical analysis of leaves was carry out to developed useful characterizations that will allow a future identification and authentication of raw material: such as, the presence of mucilaginous hypodermis, leaf of dorsiventral structure, 1 to 2 rows of empalisade parenchyma with tannin deposits, anomocytic stomata in low epidermis and simple, unicellular trichomes in both epidermis.

Castela tweedii es un árbol de bajo porte perteneciente a la Familia Simaroubaceae, las infusiones de sus hojas son utilizadas en la medicina popular Argentina para el tratamiento de desordenes gastrointestinales y diarreas. Con el objetivo de fundamentar el uso popular de esta especie se evaluó la actividad antioxidante de los extractos etanólicos y diclorometánicos de forma cuantitativa y cualitativa frente al radical 2,2-difenilpicrilhidrazilo (DPPH); el extracto etanólico demostró actividad obteniéndose una CI50= 0,1288 mg/mL. El análisis fitoquímico mostró que los compuestos responsables de esta actividad fueron taninos, flavonoides y ácidos fenilcarboxílicos, entre ellos se identificó rutina y ácido clorogénico. Además se realizó el estudio morfoanatómico e histoquímico de las hojas que aportó datos de valor diagnostico para el control de calidad de la droga vegetal: presencia de una hipodermis mucilaginosa, estructura dorsiventral con una a dos hileras de parénquima en empalizada conteniendo taninos, estomas anomocíticos solo en la epidermis abaxial y tricomas simples unicelulares en ambas epidermis.

Gram-scale isolation of isobrucein B and neosergeolide from Picrolemma sprucei Hook. f. / Isolamento de isobruceina B e neosergeolida de Picrolemma sprucei Hook. f. em escala-grama

Quassinoids neosergeolide and isobrucein B, obtained from Picrolemma sprucei, have proven in vitro antitumor, antimalarial, anthelminthic, cytotoxic, insecticide and leishmanicidal activities. There is interest in the in vivo pharmacological study of these natural compounds and their semi-synthetic derivatives, however, the quantities obtained in previous extraction processes have been shown to be a limiting factor for continuation of these studies. Herein, we describe a method for obtaining grams of these quassinoids whose purification relies only on recrystallization.

Os quassinóides neosergeolida e isobruceína B, obtidos de Picrolemma sprucei, possuem atividades antitumoral, antimalárica, anti-helmíntica, citotóxica, inseticida e anti-leishmania comprovadas em estudos in vitro. Há interesse no estudo farmacológico in vivo dessas substâncias naturais e de seus derivados semi-sintéticos, porém a quantidade obtida nos processos de extração tem se mostrado um fator limitante à continuação desses estudos. No presente trabalho, descrevemos um método para obtenção de gramas desses quassinóides cuja purificação depende apenas de cristalização fracionada.

Anatomia Foliar e Caulinar de Picrolemma sprucei Hook (Simaroubaceae)

Anatomical studies of the leaves and stems of Picrolemma sprucei revealed that the epidermes of the leaves are glabrous, with undulating cell walls and anomocytic stomata. The mesophyll is dorsiventral with a layer of cells in palisade and a spongy parenchyma. The vascular bundles are bicollateral and have a dark tannin containing idioblast. The stem possesses a developed cortical parenchyma with schlerenchymatous thick walled cells. These are either isolated or gathered in small groups. Internally the vascular region exhibits xylematic vessels some isolated and some in groups submerged in fibrous tissue. The stem possesses a paratracheal, vasicentric parenchyma with central pith. Histochemical tests (sudan III and ferric chloride) made on the central section of the midrib and on the petiole showed the presence, respectively, of tannin or oleoresin in some cells.

Os estudos anatômicos das folhas e caules de Picrolemma sprucei revelaram que as epidermes das folhas são glabras, apresentam células de paredes onduladas e estômatos anomocíticos. O mesofilo é dorsiventral com uma camada de células em paliçada e um parênquima lacunoso. Os feixes vasculares são bicolaterais e apresentam idioblastos escuros de conteúdo tânico. No caule evidencia-se um parênquima cortical desenvolvido, com células de natureza esclerenquimática, isoladas ou reunidas em pequenos grupos, de paredes espessas. Internamente observa-se a região vascular com vasos xilemáticos isolados ou em grupos imersos em tecido fibroso, sendo o parênquima do tipo paratraqueal, vasicêntrico. Na região central encontra-se uma medula desenvolvida. Testes histoquímicos (sudam III e cloreto férrico) realizados na nervura mediana do terço médio do limbo foliar e no pecíolo revelaram respectivamente, a presença de um conteúdo tânico e óleo-resinoso em algumas de suas células.

Cantinona de simaba polyphylla(cavalc.) thomas (simaroubaceae)

A canthin-2,6-dione (1) was isolated from the ethanol extract wood of Simaba polyphylla (Cavalc.) Thomas colleted near Manaus. Compound 1 was previously isolated from S. multiflora, S. guianensis and S. cedron, this is the first occurrence in S. polyphylla.

Uma cantin-2,6-diona (1) foi isolada do extrato etanólico da madeira de Simaba polyphylla (Cavale.) Thomas coletada próximo a Manaus. O composto 1 foi previamente isolado de S. multiflora, S. guianensis e S. cedron, sendo essa a primeira citação de ocorrência em S. polyphylla.