Preformulation studies for the development of a microemulsion formulation from Ambrosia peruviana All, with anti-inflammatory effect

Abstract Natural products are considered an important source of the therapeutic arsenal currently available. Among these alternatives are the seeds of Ambrosia peruviana (altamisa), whose extract has shown an anti-inflammatory effect. The main objective of this work was to perform a preformulation study of Ambrosia peruviana seeds ethanolic extract, where the main factors that affect the physical, chemical, and pharmacological stability of the extract were evaluated, as well as a compatibility study by differential scanning calorimetry (DSC) analysis against different excipients. A dry extract was obtained by rotary evaporation of the seeds macerated with 96% ethanol. The anti-inflammatory activity was determined by measuring its effect on NO production in RAW 264.7 macrophages, stimulated with LPS. The results showed that the dry extract maintained its stability over time when stored at a temperature of 4 and 25ºC, demonstrating its biological activity, the content of phenolic compounds, and its physicochemical parameters remain practically invariable. However, when exposed to high temperatures (60 ºC) it was affected. The thermal analysis revelated that the behavior of most of the selected excipients and the dry extract was maintained, which indicates that it did not present incompatibilities, therefore they can be candidates for formulating a microemulsion.

Composition, Antioxidant and Anti-inflammatory activities of Hexane and Methanol extracts of Acmella uliginosa from Terai region of Uttarakhand

Abstract Acmella uliginosa, an edible herb belonging to Asteraceae family, was collected from the Terai region of Uttarakhand, India. Methanol and hexane extracts of the whole plant were prepared using soxhlet apparatus. The GC-MS analysis of plant extracts identifies 22 and 35 major compounds of methanol and hexane extracts which comprises of 74.21% and 73.20% of the total composition of extracts, respectively. The major compound in hexane was 2, 4-heptadienal (7.99%) whereas trans, trans-9, 12-octadecadienoic acid propyl ester (16.96%) was major compound in methanol extract. The extracts were evaluated for antioxidant and anti-inflammatory properties. Methanol extract showed higher free radical scavenging and reducing power activities with IC50 value 153.82±1.69 µg/mL and RP50 value of 152.28±0.41 µg/mL, respectively. The metal chelating activity was higher in hexane extract as compared to methanol extract i.e., 62.08±0.25 µg/mL. The anti-inflammatory activity assessed by its ability to inhibit denaturation was higher in methanol having IB50 value 87.33±0.15 µg/mL. The total phenolic content (TPC), total flavonoid content (TFC) and ortho-dihydric phenol content (ODP) of methanol and hexane extracts were also evaluated. TPC, TFC and ODP was higher in methanol extract having value of 122.23±0.22, 35.01±0.29 and 8±0.86 mg/mL, respectively. Acmella uliginosa, might be considered as a natural source for antioxidant and anti-inflammatory properties

Chemical composition and biological activity of Baccharis erioclada DC. essential oil

Abstract The chemically complex essential oils of Baccharis species are associated with several biological activities, such as antimicrobial and antiulcerous properties. However, few studies have investigated Baccharis erioclada DC. Therefore, in this study, we aimed to characterize the essential oil of B. erioclada and evaluate its antioxidant, antimicrobial, and hemolytic potential. The essential oil was extracted by hydrodistillation using a Clevenger apparatus and analyzed via gas chromatography-mass spectrometry (GC-MS). Phosphomolybdenum complex formation, reducing antioxidant power, and thiobarbituric acid reactive substances (TBARS) methods were used to determine antioxidant potential. To evaluate the essential oil's antimicrobial activity, minimum inhibitory concentrations (MIC) in Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Candida albicans were calculated. Hemolytic activity was determined in sheep red blood cells. Thirty-one compounds were identified via GC-MS analysis, representing 81.60% of the total essential oil. These compounds included: turmerone (27.97%), fokienol (13.47%), ledol (9.78%), and santalol (5.35%). The class of compounds identified was the oxygenated sesquiterpenes (62.52%). Antioxidant activity was confirmed via phosphomolybdenum complex formation and TBARS methods. Moderate antimicrobial activity and low hemolysis rates were displayed at concentrations of 250 and 500 µg/mL

Analgesic, antipyretic, anti-inflammatory, and hepatoprotective activities of Pulicaria crispa (Forssk. ) Oliv. (Asteraceae)

Abstract Some plants of the genus Pulicaria have been used in traditional medicines for treating back pain and inflammation. They possess various bioactivities such as antipyretic, analgesic, and hepatoprotective. This study aimed to investigate the potential analgesic, antipyretic, anti- inflammatory, and hepatoprotective activities of Pulicaria crispa (P. crispa) extract (PCE). Analgesic activity was evaluated using the hot plate and acetic acid-induced writhing tests. Antipyretic and anti-inflammatory activities were evaluated using rectal temperature and carrageenan-induced hind paw edema methods, respectively. CCl4-intoxication was used for hepatoprotective activity. Also, liver histopathology was assessed. PCE, at 500 mg/kg, exhibited significant analgesic, antipyretic, and anti-inflammatory effects. The increased serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), gamma-glutamyl transferase (GGT), and bilirubin of CCl4-exposed rats reflects their liver injury. PCE significantly decreased the elevated liver markers. The hepatoprotective effect of PCE was confirmed, as it successfully reversed the altered levels of total protein, malondialdehyde (MDA), and non-protein sulfhydryls (NP-SH) in the liver tissues of CCl4-exposed rats. Histopathological studies confirmed the hepatoprotective nature of PCE. Pretreatment of rats with PCE reduced the severity of CCl4-induced liver damage. These findings concluded that PCE possesses analgesic, antipyretic, anti-inflammatory, and hepatoprotective activities.

Antioxidant, antimicrobial and phytotoxic activities of Rhaponticum acaule DC essential oil

The in-vitro antioxidant activity of Rhaponticum acaule essential oil (RaEO) was evaluated using ß-carotene/linoleic acid bleaching, chelating activity, and lipid peroxidation inhibition (TBARS) assays. The antimicrobial activity of RaEO was assessed by disc diffusion and microdilution methods against 8 bacteria and 4 yeast. Finally, the allelopathic activity of RaEO on the seed germination and the shoot and root elongation of lettuce (Lactuca sativa L.) seedlings were investigated. According to our results, the RaEO exhibited significant antioxidant activity, similar to those of standards (BHT and ascorbic acid) with IC50 values of 0.042 and 0.045 mg/mL obtained by ß-carotene bleaching and TBARS assays, respectively. On the other hand, despite its interesting ferrous chelating activity, RaEO possesses moderate IC50 value (0.35 mg/mL) as compared with that of EDTA (0.015 mg/mL). RaEO exhibited a strong antimicrobial activity against all the tested microorganisms, with IZ, MIC and MBC values being in the range of 7.67 ± 0.58 to 13.33 ± 0.58 mm, 1.25 to 5.00 and 5.00 to 10.00 mg/mL, respectively. The results reveled also that RaEO inhibited the shoot and root growth of Lactuca sativa L. seedlings. Our data suggested that the RaEO had pharmaceutical benefits and could be used as a potential natural herbicide resource

Extract of Solidago chilensis Meyen inflorescences: cytotoxicity and inhibitory activity on nitric oxide synthesis in activated macrophage cell line J774A. 1

Solidago chilensis Meyen (= Solidago microglossa) popularly known as "Brazilian arnica" is used to treat of inflammatory disorders. S. chilensis is constant in the Therapeutic Memento of the Rio de Janeiro city and belongs to the medicinal species of Brazilian National List of Medicinal Plants of Interest of the Unified National Health System (SUS). There are no studies in the literature showing the direct activity of this plant species on immune system cells. The present study evaluated the chemical composition as well as the cytotoxic and pharmacological activity of the ether-ethanol extract from S. chilensis inflorescences (SCIE) in murine macrophage cell line J774A.1. The results showed that higher concentrations (50 to 200 µg/mL) of SCIE had significant cytotoxicity on J774A.1 cells, however, lower concentrations (from 10 to 0.1 µg/mL) did not produce significant cytotoxic effects and exhibited an inhibitory effect on nitric oxide production in LPS-stimulated J774A.1 cell line. The chemical analysis by HPLC-UV-PDA indicated that the SCIE contains flavonoid derived from quercetin and kaempferol; and diterpenes, probably labdanes. These findings complement data in the literature regarding the activity of this plant species on an important cell from the immune system involved in the innate and acquired immune response, the macrophages.

Stability of hydroalcoholic extracts of two species of guaco; Mikania glomerata SPRENG. and Mikania laevigata SCHULTZ. (Asteraceae), by UHPLC-MS

It is important to study the stability of plant extracts used as active ingredients in phytotherapic medicine, as degradation of the active principles directly affects the efficacy and safety of these products. Therefore, a stability study of the hydroalcoholic extract of the species: Mikania glomerata and Mikania laevigata was conducted in order to determine the speed of degradation and shelf life of these extracts, which are incorporated in cough syrup in Brazil. Leaves of both species were dried in an oven or by lyophilization (freeze-dried). Hydroalcoholic extracts underwent both accelerated stability study of six months and long-term stability study for 12 months. Samples were stored at different temperatures and every three months were analysed by ultra-high performance liquid chromatography-mass spectrometry (UHPLC-MS) to monitor their chemical profile, quantifying coumarin and chlorogenic acid. For all conditions of the study, a reduction of the content of the chemical marker of this species, coumarin, greater than 5% was observed, so a shelf life of two years cannot be assigned to the hydroalcoholic extracts of these species as observed in commercial extracts.

Análise farmacobotânica de folha e caule de Tanacetum vulgare (L. ) / Pharmacobotanical analysis of leaf and stem of Tanacetum vulgare (L. )

RESUMO Tanacetum vulgare L., conhecida popularmente como catinga-de-mulata, é utilizada na medicina tradicional como vermífugo, digestivo e emenagogo. Objetivou-se analisar a morfoanatomia de folhas e caules dessa espécie medicinal com vistas ao controle da qualidade. Foram utilizadas técnicas usuais de microscopia de luz e eletrônica de varredura. As folhas são compostas, pinatissectas e anfiestomáticas. Tricomas tectores flageliformes simples e glandulares capitados são observados. A nervura central tem formato biconvexo, o pecíolo é côncavo-convexo, a ráque é plano-convexa e o caule é arredondado. Feixes vasculares colaterais, calotas de fibras perivasculares e colênquima lamelar estão presentes na folha e no caule. Os caracteres morfoanatômicos evidenciados contribuem na identificação do táxon e fornecem subsídios farmacobotânicos para o controle da qualidade de drogas vegetais e fitoterápicos.

ABSTRACT Tanacetum vulgare L., popularly known as tansy, is used in traditional medicine as a vermifuge, digestive and emmenagogue. This study aimed to analyze the morphoanatomical leaves and stems of this medicinal plant in order to control the quality. Usual techniques of light and scanning electron microscopy were used. The leaves are composed, pinatissect and amphistomatic. Simple and flagelliform non- glandular trichomes and capitate glandular trichomes are observed. The midrib has biconvex shape, the petiole is concavo-convex, the rachis is plano-convex, and the stem is rounded. Collateral vascular bundles, perivascular fiber caps and laminar collenchyma are encountered in the leaves and stems. Evidenced the morphological and anatomical features contribute to the identification of the taxon and provide pharmacobotanical data for the quality control of herbal drugs.

Pérdida de pubescencia foliar y sus efectos fisiológicos en Espeletia paipana(Asterales, Asteraceae), en el departamento de Boyacá-Colombia / Loss of leaf pubescence and its physiological effects on Espeletia paipana (Asterales, Asteraceae), in the Boyacá-Colombia department

Espeletia paipanaes una roseta caulescente gigante en peligro de extinción, endémica del departamento de Boyacá. Con el fin de establecer si una enfermedad en la planta, atribuida a la acción patogénica de microorganismos endófitos y caracterizada por la pérdida de pubescencia foliar (PPF), puede ser causante de la acelerada mortandad poblacional, se evaluó el desempeño fisiológico de la especie con y sin PPF. La incidencia (% de hojas afectadas por cada uno de los 27 individuos de la población actual) y severidad (% de área foliar afectada en 135 hojas) de la PPF fueron monitoreadas durante un periodo de nueve meses, en tres zonas topográficas a diferentes altitudes. Parámetros fisiológicos como conductancia estomática (Gs) y temperatura foliar (Tfol) e índice de contenido de clorofila (ICC) fueron medidos en hojas sanas y enfermas durante cuatro días consecutivos, tanto en la época seca como en la época húmeda. El estudio fue complementado con aislamientos y pruebas de patogenici-dad para identificar el agente causal de la PPF. En general, aunque la incidencia de la enfermedad en E. paipanafue constante a lo largo del tiempo, la severidad avanzó superando el 60 % del área foliar. El aumento de la severidad en el haz fue atribuido al efecto foto-oxidativo de las altas radiaciones entre las 11:00 y14:00 h. La reducción del área foliar funcional a causa de la PPF, llevó a una baja Gs con serias implicaciones en la fijación de carbono, y por tanto limitando el crecimiento y la renovación de biomasa. El efecto estacional en la Tfol varió de acuerdo con la zona topográfica, mientras que el ICC no presentó un patrón definido con relación a la PPF; sus valores bajos podrían estar relacionados con la producción de otros pigmentos. Finalmente, aunque no es posible asegurar que Botrytissp. es el causante de la pérdida de pubescencia foliar, se postula como el agente causal más probable debido a su alta representatividad en los aislamientos y su potencial de infección durante las pruebas de patogenicidad. En general, la reducción de biomasa foliar sana y disminución del rendimiento fisiológico sugieren que la PPF afecta negativamente la sobrevivencia de E. paipana,lo que significa que el uso de biocontroladores podría ser una estrategia para el rescate poblacional.

Espeletia paipanais an endangered giant caulescent rosette endemic to Boyacá department. In order to establish whether a plant disease, characterized by the loss of leaf pubescence (PPF) and attributed to the pathogenic action of endophytic microorganisms, is the cause of the increasing mortality of population, the physiological performance of the species was evaluated with and without PPF. The incidence (% leaves affected in each of the 27 individuals in the current population) and severity (% leaf area affected on 135 leaves) of the PPF were monitored over a period of nine months, in three topographic zones of different heights. During four consecutive days in both dry and wet season, physiological parameters as chlorophyll content index (ICC), stomatal conductance (Gs) and leaf temperature (Tfol) were measured in healthy and affected leaves. The study was complemented with isolations and pathogenicity tests to identify the causal agent of the PPF. Overall, although the disease incidence in E. paipanawas constant over time, the severity progressed surpassing 60 % of the leaf area. The increasing of severity in the upper side of leaves was attributed to the photo-oxidative effect of high radiation between 11:00 h and 14:00 h of the day. The reduction of functional leaf area because of the PPF, led to low Gs with serious implications for carbon fixation and thus limiting growth and biomass renewal. The effect of season in Tfol varied according to the topographic zone, while the ICC did not present a defined pattern with respect to the PPF; its low values could be associated with the production of other pigments. Finally, although it is not possible to ensure that Botrytissp. is the causative of the loss of leaf pubescence, it is postulated as the most probably causal agent due to its high representativeness in the isolates and its infectious potential during the pathogenicity tests. In general, the reduction of healthy leaf biomass and decrease of physiological performance suggest that PPF affect negatively the survival of E. paipana,which means that the use of biological controllers could be a strategy to mitigate its effect on the population.

Antibacterial and anti-inflammatory activities of an extract, fractions, and compounds isolated from Gochnatia pulchra aerial parts

This paper reports on the in vitro antibacterial and in vivo anti-inflammatory properties of a hydroethanolic extract of the aerial parts of Gochnatia pulchra (HEGP). It also describes the antibacterial activity of HEGP fractions and of the isolated compounds genkwanin, scutellarin, apigenin, and 3,5-O-dicaffeoylquinic acid, as evaluated by a broth microdilution method. While HEGP and its fractions did not provide promising results, the isolated compounds exhibited pronounced antibacterial activity. The most sensitive microorganism was Streptococcus pyogenes, with minimum inhibitory concentration (MIC) values of 100, 50 and 25 µg/mL for genkwanin and the flavonoids apigenin and scutellarin, respectively. Genkwanin produced an MIC value of 25 µg/mL against Enterococcus faecalis. A paw edema model in rats and a pleurisy inflammation model in mice aided investigation of the anti-inflammatory effects of HEGP. This study also evaluated the ability of HEGP to modulate carrageenan-induced interleukin-1 beta (IL-1β), tumor necrosis factor alpha (TNF-α), and monocyte chemoattractant protein-1 (MCP-1) production. Orally administered HEGP (250 and 500 mg/kg) inhibited carrageenan-induced paw edema. Regarding carrageenan-induced pleurisy, HEGP at 50, 100, and 250 mg/kg diminished leukocyte migration by 71.43%, 69.24%, and 73.34% (P<0.05), respectively. HEGP suppressed IL-1β and MCP-1 production by 55% and 50% at 50 mg/kg (P<0.05) and 60% and 25% at 100 mg/kg (P<0.05), respectively. HEGP abated TNF-α production by macrophages by 6.6%, 33.3%, and 53.3% at 100, 250, and 500 mg/kg (P<0.05), respectively. HEGP probably exerts anti-inflammatory effects by inhibiting production of the pro-inflammatory cytokines TNF-α, IL-1β, and MCP-1.

Micropropagation of Pluchea sagittalis (Lam. ) Cabrera / Micropropagação do quitoco (Pluchea sagittalis (Lam. ) Cabrera)

ABSTRACT: The objective of this study was to develop an in vitro protocol for the micropropagation of Pluchea sagittalis (Lam.) Cabrera. Plants were regenerated in vitro from stem segments. The procedure employed includes: 1) surface sterilization of shoots by immersion in 70% ethanol for 10 s followed by 1.0% NaOCl for 10 min, and subsequent immersion in 0.05% HgCl2 for 3 min and two washes with sterile distilled water; 2) induction of root and shoot by culture on hormone-free Murashige and Skoog medium (MS); 3) acclimatization of 60 day-old-plantlets in soil under ex vitro conditions. Minimum contamination was observed for apical shoot explants (10%). However, independently of the explant position in the stem, all explants regenerated new shoots. Various successive cultivations from stem explants every 60 days during more than 1 year have been shown to be a suitable method to propagate P. sagittalis in vitro. Low salt concentration (25% of the normal concentration) in the medium promoted greater growth of plantlets because the plants had a higher number of roots and longer roots in such an environment. Our protocol for the micropropagation of P. sagittalis can be accomplished as a two-step procedure within a short period of time (two months) before transplanting.

RESUMO: O Objetivo deste estudo foi desenvolver um protocolo para a micropropagação in vitro da Pluchea sagittalis (Lam.) Cabrera. Plantas foram regeneradas in vitro a partir de segmentos de ramo. O procedimento empregado incluiu: 1) esterilização da superfície de ramos pela imersão em etanol 70% por 10 s seguida pela de NaOCl 1.0% por 10 min e, subsequentemente, em HgCl2 0.05% por 3 min e duas lavagens em água destilada e esterilizada; 2) indução de raízes e parte aérea pelo cultivo em meio Murashige & Skoog (MS) isento de hormônio; 3) aclimatização de plantas com 60 dias de idade em solo sob condições ex vitro. Contaminação mínima foi observada em explantes caulinares do ápice (10%). Entretanto, independentemente da posição do segmento no caule, todos explantes regeneraram novos ramos. Vários cultivos sucessivos a cada 60 dias durante mais de um ano tem mostrado ser um método adequado para a propagação in vitro de P. sagittalis. A baixa concentração de sais no meio (25% da concentração normal) promoveu maior crescimento das plântulas devido às mesmas apresentarem maior número e comprimento de raízes. O protocolo para a micropropagação da P. sagittalis pode ser executado em procedimento de duas etapas dentro de um período de tempo curto (dois meses) antes do transplantio.

Atividade antioxidante e toxicidade preliminar do extrato e frações obtidas das folhas e cascas do caule de Dasyphyllum tomentosum (Spreng. ) Cabrera / Antioxidant activity and preliminary toxicity of the extracts and fractions obtained from the leaves and stem bark of Dasyphyllum tomentosum (Spreng. ) Cabrera

Dasyphyllum tomentosum (Spreng.) Cabrera, açucará ou espinho-de-agulha, pertence à família Asteraceae, a qual compreende muitas espécies com propriedades terapêuticas. O objetivo deste trabalho foi avaliar extratos e frações de folhas e de cascas do caule de D. tomentosum, com relação as atividade antioxidante, citotóxica e hemolítica em testes in vitro. Todas as amostras apresentaram atividade antioxidante pelo método de inibição de DPPH, com destaque para a fração acetato de etila obtida das folhas cuja atividade foi comparável à dos padrões ácido ascórbico e rutina. Com relação à redução do complexo fosfomolibdênio, observou-se que esta mesma fração foi semelhante somente a rutina enquanto a fração obtida das cascas do caule apresentou resultado superior. Não foi observada atividade citotóxica e hemolítica frente aos modelos utilizados com os extratos e frações. Os resultados obtidos demonstram o potencial antioxidante da espécie sem apresentar toxicidade.

Dasyphyllum tomentosum (Spreng.) Cabrera, which belongs to the Asteraceae family, is well known for having many species with therapeutic properties. The aim of this study was to evaluate the extracts and fractions from the leaves and stem bark of D. tomentosum with respect to the antioxidant, cytotoxic and hemolytic activity in in vitro tests. All samples showed antioxidant activity by the DPPH inhibition method, especially the ethyl acetate fraction obtained from the leaves, whose activity was comparable to that of standard ascorbic acid and rutin. Regarding the reduction of the phosphomolybdenum complex, we noted that this same fraction was only similar to rutin and the fraction obtained from the stem bark showed superior results. There was no cytotoxicity and hemolytic activity compared to the models used in the extracts and fractions. The results demonstrate the antioxidant potential of the species without showing toxicity.

In Vitro Antitumor Activity of Sesquiterpene Lactones from Lychnophora trichocarpha / Atividade antitumoral in vitro de lactonas sesquiterpenicas de Lychnophora

The sesquiterpene lactones lychnopholide and eremantholide C were isolated from Lychnophora trichocarpha Spreng. (Asteraceae), which is a plant species native to the Brazilian Savannah or Cerrado and popularly known as arnica. Sesquiterpene lactones are known to present a variety of biological activities including antitumor activity. The present paper reports on the evaluation of the in vitro antitumor activity of lychnopholide and eremantholide C, in the National Cancer Institute, USA (NCI, USA), against a panel of 52 human tumor cell lines of major human tumors derived from nine cancer types. Lychnopholide disclosed significant activity against 30 cell lines of seven cancer types with IC100 (total growth concentration inhibition) values between 0.41 µM and 2.82 µM. Eremantholide C showed significant activity against 30 cell lines of eight cancer types with IC100 values between 21.40 µM and 53.70 µM. Lychnopholide showed values of lethal concentration 50% (LC50) for 30 human tumor cell lines between 0.72 and 10.00 µM, whereas eremantholide C presented values of LC50 for 21 human tumor cell lines between 52.50 and 91.20 µM. Lychnopholide showed an interesting profile of antitumor activity. The α-methylene-γ-lactone present in the structure of lychnopholide, besides two α,β- unsaturated carbonyl groups, might be responsible for the better activity and higher cytotoxicity of this compound in relation to eremantholide C.

As lactonas sesquiterpênicas licnofolida e eremantolida C foram isoladas de Lychnophora trichocarpha Spreng. (Asteraceae), espécie vegetal nativa do cerrado brasileiro e popularmente conhecida por arnica brasileira. As lactonas sesquiterpênicas são conhecidas por apresentarem variadas atividades biológicas, incluindo atividade antitumoral. O presente artigo relata a avaliação da atividade antitumoral in vitro de licnofolida e eremantolida C frente a um painel de 52 linhagens de células tumorais, provenientes de tumores humanos referentes a nove principais tipos de câncer. Os testes foram conduzidos no National Cancer Institute, USA (NCI, USA). Licnofolida apresentou atividade significativa frente a 30 linhagens de células tumorais referentes a sete tipos de câncer, com valores de CI100 (concentração que inibe 100% do crescimento celular) entre 0,41 µM e 2,82 µM. Eremantolida C mostrou atividade significativa frente a 30 linhagens de células tumorais referentes a oito tipos de câncer, com valores de CI100 entre 21,40 µM e 53,70 µM. Licnofolida apresentou valores de concentração letal 50% (CL50) para 30 linhagens de células tumorais humanas entre 0,72 e 10,00 µM, enquanto eremantolida C mostrou valores de CL50 para 21 linhagens entre 52,50 e 91,20 µM. Licnofolida apresentou um interessante perfil de atividade antitumoral. A presença na estrutura química da licnofolida de uma α-metileno-γ-lactona, além de dois grupos ésteres α,β-insaturados, podem ser responsáveis pela melhor atividade e maior citotoxicidade desta substância em relação à eremantolida C.

Estudo das propriedades físico-químicas e avaliação da toxicidade aguda do extrato etanólico das folhas de Mikania glomerata Sprengel / Study of the physicochemical properties and acute toxicity evaluation of the ethanolic extract of the leaves of Mikania glomerata Sprengel

A Mikania glomerata é uma planta pertencente à família Asteraceae que é bastante utilizada na medicina popular devido às suas ações broncodilatadora, antiasmática, expectorante e antitussígena. O objetivo do presente estudo foi determinar as propriedades físico-químicas do pó obtido a partir das folhas de M. glomerata, bem como, avaliar a toxicidade em camundongos após tratamento agudo com doses repetidas do extrato etanólico padronizado preparado a partir das folhas dessa espécie. Durante o estudo das propriedades físico-químicas do pó obtido a partir das folhas de M. glomerata foram feitas as determinações da densidade bruta e de compactação, do teor de cinzas totais, do teor de umidade, e da granulometria. De acordo com os resultados obtidos podemos sugerir que o pó pode ser usado na formulação de uma forma farmacêutica sólida. Na segunda parte do estudo foi determinada a Dose Letal 50% (DL50), bem como, realizada a análise morfológica macroscópica e avaliados a toxicidade aguda com doses repetidas e os parâmetros bioquímicos e hematológicos de camundongos. De acordo com os dados obtidos na segunda parte deste estudo podemos sugerir que o extrato etanólico pode ser usado de forma segura em humanos, uma vez que apresentou valor de DL50 de aproximadamente 3000 mg Kg-1), bem como, não produziu nenhuma alteração morfológica nos principais órgãos, e nem provocou alterações nos parâmetros bioquímicos e hematológicos de camundongos.

The Mikania glomerata is a plant belonging to the Asteraceae that is widely used in folk medicine because of its bronchodilator, antiasthmatic, expectorant and antitussive actions. The aim of this study was to determine the physicochemical properties of the powder obtained from the leaves of M. glomerata, and to evaluate its toxicity in mice after acute treatment with repeated doses of standardized ethanol extract prepared from the leaves of this plant species. We determined the bulk and packing density, the total ash content, the moisture content and the particle size. The results suggest that the powder can be used in the formulating of a solid pharmaceutical form. In the second part of this study, we determined the 50% lethal dose (LD50), performed the gross morphological analysis and evaluated the acute toxicity from the use of repeated doses and the biochemical and hematologic parameters in mice. The data obtained in this part suggest that the ethanol extract can be used safely in humans, since it has a LD50 value of approximately 3000 mg kg -1 and produced no morphological changes in the major organs, or caused alterations in the biochemical and hematological parameters in mice.

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

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

Preventive effect of Ligularia fischeri on inhibition of nitric oxide in lipopolysaccharide-stimulated RAW 264. 7 macrophages depending on cooking method

BACKGROUND: Ligularia fischeri (common name Gomchwi) is known for its pharmaceutical properties and used in the treatment of jaundice, scarlet-fever, rheumatoidal arthritis, and hepatic diseases; however, little is known about its anti-inflammatory effect. In this study the influence of blanching and pan-frying on the anti-inflammatory activity of Ligularia fischeri (LF) was evaluated. RESULTS: Fresh LF and cooked LF showed no significant effect on the viability of macrophages after 24 h incubation. Fresh LF was found to be the most potent inhibitor of nitric oxide (NO) production at 100 µg/ml, while pan-fried LF showed little inhibitory effect on lipoloysaccharide (LPS) stimulated murine machrophage RAW264.7 cells. In contrast with its effect on NO production, pan-fried LF showed significant attenuation of the expression of inducible nitiric oxide synthase (iNOS) compared with fresh LF. In the cooking method of LF, PGE2 production was not affected in the LPS-induced RAW 264.7 cells. In LPS-induced RAW 264.7 cells, pretreatment by fresh and cooked LF increased COX2 mRNA expression. The 3-O-caffeoylquinic acid content of blanching and pan-frying LF increased by 4.92 and 9.7 fold with blanching and pan-frying respectively in comparison with uncooked LF. CONCLUSIONS: Regardless of the cooking method, Ligularia fischeri exhibited potent inhibition of NO production through expression of iNOS in LPS-induced RAW264.7 cells.

Reubicación de plantas de Espeletia grandiflora (Asteraceae) como estrategia para el enriquecimiento de áreas de páramo alteradas (PNN Chingaza, Colombia)

Relocation of Espeletia grandiflora (Asteraceae) plants as a strategy for enrichment of disturbed paramo areas (PNN Chingaza, Colombia). Ecological restoration of the Andean paramos faces several ecological barriers mainly at the phase of dispersal and establishment of native species. With the aim to contribute to the enrichment of degraded areas, different strategies have to be developed to overcome those barriers. In this work we studied the response of individuals of Espeletia grandiflora (Asteraceae) to the relocation as a strategy for ecological restoration programs. We also evaluated the effect of size of relocated individuals on their survival and development. The work was carried out in an experimental plot at 3 424m altitude in the sector Lagunas de Siecha of Chingaza National Park, Colombia. We relocated 200 plants that belonged to three different size classes: 5, 10 and 15cm of initial height. The following variables were registered: survival, plant height, number of living leaves and stem diameter of each individual. We also evaluated the differences between individuals in survival and development. In terms of survival the most efficient size classes corresponded to 15cm high; the survival was 85% after two years. The relative growth rates for height and stem diameter decreases with the increase in size, but the absolute increase in height did not show significant differences between the three sizes tested. Since the stem diameter was found the strongest survival predictor after two years of relocation activities, we suggest its use as a criterion for selection of relocation individuals. The relocation of individuals of E. grandiflora had a positive side effect, carrying other species that may contribute to the enrichment and restoration of degraded areas. Among these, we found species of the genus Hypericum, as well as Arcytophyllum nitidum and Calamagrostis effusa, which should be evaluated in terms of survival and development for the subsequent implementation of the relocation strategy. In this study we verified the successful relocation of individuals of E. grandiflora as a strategy for enrichment of paramos, and provided values of survival and growth, which should be useful for planning and predicting with greater certainty the success of restoration programs in the paramo.

El trasplante o reubicación de individuos ha sido ampliamente usado para la adición de especies en procesos de restauración. En este trabajo se estudió la respuesta de individuos de Espeletia grandiflora a la reubicación como estrategia de restauración ecológica; así mismo, se evaluó el efecto del tamaño de los individuos reubicados sobre la supervivencia y desarrollo. Se reubicaron individuos de tres diferentes tamaños, 5, 10 y 15cm de altura. Se registraron las variables supervivencia, altura de la planta, número de hojas vivas y diámetro del tallo de cada uno de los individuos, se evaluaron las posibles diferencias en cuanto a supervivencia y desarrollo. La categoría de tamaño más eficaz corresponde a la de 15cm de altura, que presentó una supervivencia del 85% luego de dos años. Se sugiere el uso del diámetro del tallo como criterio de selección de los individuos a reubicar, ya que es la variable que mejor predice la supervivencia dos años luego de la reubicación. Las tasas de crecimiento relativo en altura y diámetro del tallo disminuyen conforme aumenta el tamaño de los individuos; sin embargo, el incremento absoluto en altura no presenta diferencias entre los tres tamaños evaluados. A partir de los resultados se verifica el éxito de la reubicación de plantas de E. grandiflora como estrategia de enriquecimiento en pastizales de páramos alterados.

Phytochemical Profile and Qualification of Biological Activity of an Isolated Fraction of Bellis perennis

This study describes the isolation and identification of apigenin-7-O-ghicopyranoside, a flavonoid isolated from the flowers of Bellis perennis L., Asteraceae, an species with a broad spectrum of biological activities. The in vitro antioxidant activity and the inhibition of the enzyme acetylcholinesterase were evaluated. The flavonoid showed strong in vitro antioxidant potential, because of the capacity of removal of hydroxyl radicals and nitric oxide, and also prevented the formation of thiobarbituric acid-reactive substances. These parameters were inhibited at the highest concentration of ApG at rates of 77.7%, 72% and 73.4%, respectively, in addition to inhibiting acetylcholinesterase, suggesting potential use in the treatment of neurodegenerative diseases.

Avaliação de modelos matemáticos na descrição das curvas de secagem por convecção de Pectis brevipedunculata (Gardner) Sch. Bip. / Assessment of mathematical models for the description of Pectis brevipedunculata (Gardner) Sch. Bip. convective drying curves

O presente trabalho foi realizado com o objetivo de selecionar, dentre cinco modelos matemáticos, aquele que melhor descreve as curvas experimentais de secagem da parte aérea de P. brevipedunculata. Os testes foram realizados em protótipo de secador de leito fixo, em camada delgada, a 30, 40 e 50°C, com fluxo mássico de ar seco de 0,27 e 0,54 kg s-1 m-2. O grau de ajuste dos modelos foi avaliado por meio do coeficiente de determinação, da raiz do erro quadrático médio, do erro percentual absoluto médio, do chi-quadrado reduzido, pela análise de dispersão de resíduos, e considerando o princípio da parcimônia. O modelo exponencial simples de três parâmetros foi o que melhor representou as curvas experimentais de secagem podendo ser utilizado com segurança na simulação do processo em camada espessa. Embora o modelo de Lewis não tenha sido capaz de descrever as curvas de secagem com grau de acurácia satisfatório, observou-se que a relação funcional entre a constante de secagem k e a temperatura, pode ser representada pela equação de Arrhenius.

The aim of this study was to select, among five mathematical models, the one that best describes the experimental drying curves of the shoot of P. brevipedunculata. Tests were conducted in a thin-layer prototype laboratory drier, at 30, 40 and 50°C, employing a dry air mass flow rate of 0.274 and 0.542 kg s-1 m-2. The goodness of fit of the models was assessed based on correlation coefficient, root mean square error, mean absolute percentage error, reduced chi-squared, residual plot analysis, and taking into account the principle of parsimony. The model that best described the experimental drying curves was the simple-exponential, three-parameter model, which can be safely used to simulate the deep-bed process. Although the Lewis model was found not to produce accurate predictions of the drying curves, an Arrhenius-type equation represents the relationship between the drying constant k and the temperature.

Baccharis rufescens Spreng. var. tenuifolia (DC. ) Baker: contribuição ao estudo farmacognóstico / Baccharis rufescens Spreng. var. tenuifolia (DC. ) Baker: contribution to the pharmacognostic study

Baccharis rufescens Spreng. var. tenuifolia (DC.) Baker pertence à família Asteraceae e é usada na medicina tradicional como estomáquico e hepatoprotetor. Um estudo fitoquímico mostrou a presença de flavonoides e triterpenos, sendo que os extratos clorofórmico e metanólico de folhas apresentaram-se ativos no bioensaio de toxicidade sobre Artemia salina Leach. Além disso, extratos clorofórmicos evidenciaram a presença de peróxidos, sugerindo sua aplicação no tratamento da malária (Schenkel at al., 2002; Montanher et al., 2002; Moreira et al., 2003). Considerando a importância farmacológica de B. rufescens var. tenuifolia, o presente trabalho objetivou o estudo morfoanatômico e histoquímico do caule e da folha dessa espécie, a fim de fornecer subsídios farmacognósticos para o controle de qualidade. O material botânico foi submetido às técnicas usuais empregadas na microscopia de luz e microscopia eletrônica de varredura. Folha anfiestomática, presença de estômatos anomocíticos, tricomas glandulares capitados bisseriados, tricomas tectores flageliformes simples unisseriados, dutos secretores associados ao floema, calota de fibras perivasculares e cristais de oxalato de cálcio do tipo estiloide e prismático na região medular do caule foram as principais características observadas que auxiliam na identificação do táxon.

Baccharis rufescens Spreng. var. tenuifolia (DC.) Baker belongs to the Asteraceae family. It is used for liver and stomach problems in traditional medicine. Previous phytochemical data reported flavonoid and triterpene contents. Chloroform and methanol extracts of the leaves showed activity in the bioassay of brine shrimp. Chloroform extracts showed the presence of peroxides that can be used to treat malaria (Schenkel et al., 2002; Montanher et al., 2002; Moreira et al., 2003). Considering the pharmacological importance of B. rufescens var. tenuifolia, the purpose of this paper was to perform the anatomical analysis of aerial vegetative parts of Baccharis rufescens var. tenuifolia in order to provide pharmacognostic data for quality control. The plant material was studied by the usual methods of light and scanning electron microscopy. Amphistomatic leaves, anomocytic stomata, biseriate capitate glandular trichomes, uniseriate simple flagelliform non-glandular trichomes, secretory ducts associated to the phloem, perivascular fiber cap, calcium oxalate as prismatic and styloid crystals in the pith of the stem were reported as the mainly anatomical data for B. rufescens var. tenuifolia.Ouvir Ler foneticamente.