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Bol. latinoam. Caribe plantas med. aromát ; 19(2): 188-206, mar. 2020. ilus, tab
Article in English | LILACS | ID: biblio-1104201


The present study aimed to screen the Rhazya stricta Decne root for its antihyperglycemic and antioxidants potential through invitro assays along with phytochemical and elemental analyses. The crude extract was prepared through maceration and fractionated using solvent-solvent extraction technique. The spectroscopic studies indicated the presence of various phytochemical classes in the extract and its fractions. The antioxidant assays showed notable results along with a good concentration of phenolic and flavonoid contents. Enzyme inhibition assays demonstrated glucose-lowering effects by inhibiting the enzyme activity which could reduce post-prandial blood glucose level. The Dipeptidyl peptidase-IV (DPP-IV) inhibition assay results showed the novel DPP-IV inhibition activity of the plant extract and all fractions showed noteworthy enzyme inhibition and antihyperglycemic activity. Conclusively, the Rhazya stricta root extract displayed its antioxidant and antihyperglycemic potential due to the presence of various classes of phytochemicals and micro-nutrients.

El presente estudio tuvo como objetivo examinar la raíz de Rhazya stricta Decne por su potencial antihiperglicémico y antioxidante a través de ensayos in vitro junto con análisis fitoquímicos y elementales. El extracto crudo se preparó por maceración y se fraccionó usando una técnica de extracción solvente-solvente. Los estudios espectroscópicos indicaron la presencia de varias clases fitoquímicas en el extracto y sus fracciones. Los ensayos antioxidantes mostraron resultados notables junto con una importante concentración de contenido fenólico y flavonoide. Los ensayos de inhibición enzimática demostraron efectos reductores de la glucosa al inhibir la actividad enzimática que podría reducir el nivel de glucosa posprandial en sangre. Los resultados del ensayo de inhibición de Dipeptidyl peptidase-IV (DPP-IV) mostraron la nueva actividad de inhibición de DPP-IV del extracto de la planta y todas las fracciones mostraron una notable inhibición enzimática y actividad antihiperglicémica. En conclusión, el extracto de raíz de Rhazya stricta Decne mostró su potencial antioxidante y antihiperglicémico debido a la presencia de varias clases de fitoquímicos y micronutrientes.

Plant Extracts/pharmacology , Apocynaceae/chemistry , Hypoglycemic Agents/pharmacology , Antioxidants/pharmacology , Phenols/analysis , Spectrophotometry, Ultraviolet , Flavonoids/analysis , Blood Glucose/drug effects , In Vitro Techniques , Plant Extracts/chemistry , Spectroscopy, Fourier Transform Infrared , Plant Roots/chemistry , Dipeptidyl-Peptidases and Tripeptidyl-Peptidases/antagonists & inhibitors , Phytochemicals , Hypoglycemic Agents/chemistry , Antioxidants/chemistry
Braz. j. med. biol. res ; 52(5): e7798, 2019. graf
Article in English | LILACS | ID: biblio-1001525


Himatanthus drasticus (Mart.) Plumel belongs to the Apocynaceae family and the latex from its trunk bark (Hd) is known as "janaguba milk". This latex is widely used in Northeast Brazil, mainly in the Cariri region, for its gastroprotective, anti-inflammatory, and antitumor properties. The objective of this study was to investigate a triterpene-rich fraction (FJNB) from H. drasticus latex on acute models of nociception and inflammation and to clarify its mechanisms of action. Wistar rats or Swiss mice were subjected to the carrageenan-induced paw edema test or the formalin test, respectively, after the acute oral treatment with FJNB. The inflamed paws from the carrageenan-induced paw edema and formalin tests were processed for histological and immunohistochemical assays, respectively. The results were analyzed by ANOVA and considered significant at P<0.05. FJNB (10 mg/kg) decreased the paw edema by 25% at the 3rd h after the carrageenan injection. Indomethacin, used as reference, inhibited the paw edema by 59% at the same time-point. In the formalin test, FJNB inhibited the 1st phase by 27, 49, and 52% and the 2nd phase by 37, 50, and 67%, at the doses of 1, 5, and 10 mg/kg, respectively. In addition, FJNB significantly inhibited the expressions of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and the inflammatory cytokine tumor necrosis factor (TNF)-alpha. The histone deacetylase (HDAC) expression and the transcription factor nuclear factor kappa (NF-kB) were also inhibited at the same doses. In conclusion, the FJNB inhibitory actions on iNOS, COX-2, TNF-α, HDAC, and NF-kB could be involved with the drug anti-inflammatory activity.

Animals , Male , Rabbits , Rats , Triterpenes/therapeutic use , Apocynaceae/chemistry , Edema/drug therapy , Analgesics/therapeutic use , Inflammation/drug therapy , Anti-Inflammatory Agents/therapeutic use , Triterpenes/isolation & purification , Immunohistochemistry , Biomarkers/blood , Rats, Wistar , Disease Models, Animal
Nutrire Rev. Soc. Bras. Aliment. Nutr ; 43: 1-7, Mar. 2018. tab, ilus, graf
Article in English | LILACS | ID: biblio-881664


BACKGROUND: Carissa bispinosa, Ficus sycomorus, and Grewia bicolar are edible fruit plants that grow in the wild. The plants produce yellow-, red-, and purple-colored fruits and thus can be good sources of flavonoids for fighting oxidative reactions in humans, food, and the pharmaceutical industry. The present study aimed at isolating flavonoids from C.bispinosa, F. sycomorus, and G. bicolar fruits and determining their antioxidant activity using the 2, 2-diphenyl-1-picrylhydrazyl (DPPH) and 2, 2-azino-bis 3-ethylbenz-thiaz-oline-6-sulfonic acid (ABTS) model radical assays. METHODS: Analytical and preparative thin-layer chromatography was used to isolate flavonoids from the fruits using methanol/chloroform/hexane (7:2:1,v/v/v) as a mobile phase system. The ABTS and DPPH radical scavenging methods were used to test for the antioxidant activity of the samples, using quercetin and catechin as reference standards. RESULTS:Thin-layer chromatographic profiling revealed two different types of flavonoids from each plant.C. bispinosa yielded two flavonoid bands, Rfvalues 0.11 and 0.38;G. bicolaryielded two flavonoid bands,Rfvalues 0.63 and 0.81; andF.sycomorus also yielded two types of flavonoids, Rfvalues 0.094 and 0.81. All the extracted flavonoids exhibited significant antioxidant activity of over 80% at a concentration of 200 mg/L. The order of radical scavenging activity for the 200-mg/Lsamples is G. bicolar Rf(0.81) >C. bispinosa Rf(0.113) >F. sycomorus Rf(0.094) >F. sycomorus Rf(0.047) >C. bispinosa Rf(0.38) >G. bicolar Rf(0.63).G. bicolar(Rf= 0.81) exhibited antioxidant activitythat was superior to that of catechin. CONCLUSION:The present study results show that C. bispinosa,F. sycomorus,and G. bicolar contain different flavonoid types with significant antioxidant activity of over 80% at a concentration of 200 mg/L. Therefore, the fruits can be used as a source of natural antioxidants which can be used as nutraceuticals to promote health, as preservatives to delay peroxidation of foods, and as flavoring for packed foods.

Antioxidants/therapeutic use , Apocynaceae/chemistry , Ficus/chemistry , Flavonoids/analysis , Grewia/chemistry
Arq. bras. med. vet. zootec. (Online) ; 69(3): 513-522, jun. 2017. ilus, tab, graf
Article in English | LILACS, VETINDEX | ID: biblio-846834


This study aimed to evaluate Himatanthus drasticus latex in a mice wound healing experimental model. Animals were divided into four groups (n=7) according to the treatments: GI - saline 0.9% (control), GII - mineral oil (vehicle), GIII - H. drasticus commercial latex (HdCL) and GIV - H. drasticus mixed isolated fraction (MIF, 1 mg/mL). The treatments were applied topically once daily, 50 µL for 14 consecutive days. Macroscopic lesions were evaluated, considering parameters such as swelling, redness, granulation tissue and reepithelialization. VEGF+, CD68+ expressions and mast cells (Toluidin blue stain) were evaluated. HdCL induced higher contraction and exuberant granulation tissue (P > 0.05). HdCL showed a mild inflammatory process while MIF induced intense infiltrate inflammatory predominantly by lymphocytes, vascular congestion, bleeding and did not presented full reepithelialization. Reorganization of collagen fibers (red picrosirius stain) was observed. CD68+ expression and mast cells were presented as moderate, intense and mild in GI, GIII and GIV, respectively. Neovascularization occurred in all groups, while VEGF+ expression was intense in MIF in relation to HdCL. We concluded that HdCL presents wound healing potential, through modulation of mast cells, CD68+ and VEGF+ expressions that can be associated to triterpenes presence according MIF isolated from HdCL.(AU)

Objetivou-se avaliar o látex de Himatanthus drasticus em feridas induzidas experimentalmente em camundongos. Os animais foram divididos em quatro grupos (n=7): GI - salina 0,9% (controle), GII - óleo mineral (veículo), GIII - látex comercial de H. drasticus (HdCL) e GIV - fração isolada mista de H. drasticus (MIF, 1mg/mL). Os tratamentos foram aplicados topicamente uma vez ao dia (50µL), durante 14 dias consecutivos. Lesões macroscópicas, as expressões de VEGF+, CD68+ e a participação dos mastócitos (coloração azul de toluidina) foram avaliadas. HdCL induziu maior contração e tecido de granulação exuberante (P >0,05). HdCL induziu leve processo inflamatório enquanto MIF promoveu intenso infiltrado inflamatório predominantemente linfocítico, congestão vascular, hemorragia e reepitelização parcial. Observou-se reorganização das fibras colágenas (coloração picrosírius). A expressão de CD68+ e os mastócitos apresentaram-se moderados, intensos e leves em GI, GIII e GIV, respectivamente. A neovascularização foi observada em todos os grupos, enquanto a expressão de VEGF+ foi mais intensa em MIF em relação a HdCL. Conclui-se que HdCL apresenta potencial de cicatrização por meio da modulação dos mastócitos e das expressões de CD68+ e VEGF+, o que pode estar associado à presença de triterpenos de acordo com MIF isolada de HdCL.(AU)

Animals , Mice , Angiogenesis Inducing Agents/analysis , Apocynaceae/chemistry , Glycoproteins , Mast Cells , Vascular Endothelial Growth Factor A/analysis , Wound Healing/drug effects , Latex/chemistry
Braz. j. biol ; 76(1): 245-249, Feb. 2016. tab, graf
Article in English | LILACS | ID: lil-774493


Abstract The latex obtained from Hancornia speciosa Gomes (Mangabeira tree) is widely used in traditional medicine to treat a variety of diseases, including diarrhea, ulcer, gastritis, tuberculosis, acne and warts. In this study, the cytotoxicity and genotoxicity effects of H. speciosa latex on the root meristem cells of Allium cepa were examined. Onion bulbs were exposed to different concentrations of latex and then submitted to microscopic analysis using Giemsa stain. Water was used as a negative control and sodium azide as a positive control. The results showed that, under the testing conditions, the mitotic index (MI) of the onion roots submitted to latex treatment did not differ significantly from the negative control, which suggests that the latex is not cytotoxic. Low incidence of chromosome aberrations in the cells treated with H. speciosa latex was also observed, indicating that the latex does not have genotoxic effect either. The MI and the chromosome aberration frequency responded to the latex concentration, requiring more studies to evaluate the dosage effect on genotoxicity. The results indicate that in tested concentrations H. speciosa latex is probably not harmful to human health and may be potentially used in medicine.

Resumo O látex obtido de Hancornia speciosa é amplamente utilizado na medicina popular para tratar uma variedade de doenças, tais como: diarreia, úlcera, gastrite, tuberculose, acne e verrugas. Nesse estudo, foram avaliados os efeitos citotóxicos e genotóxicos do látex de H. speciosa sobre as células meristemáticas das raízes de Allium cepa. Os bulbos das cebolas foram expostos a diferentes concentrações de látex e depois submetidos à analise microscópica usando o corante Giemsa. A água foi usada como controle negativo e a ázida sódica como controle positivo. Os resultados mostraram que o índice mitótico (IM) das raízes de cebola submetidas ao tratamento com látex, nas condições testadas, não diferiram significativamente do controle negativo, e sugerem que o látex não é citotóxico. Também foi observada uma baixa incidência de aberrações cromossômicas nas células tratadas com látex de H. speciosa, o que sugere que o látex também não possui efeito genotóxico. O IM e a frequência de aberrações cromossômicas foram dependentes da concentração de látex. Outros estudos devem ser realizados para avaliar o efeito da dose na genotoxidade. Os resultados indicam que o látex de mangabeira, nas concentrações testadas, provavelmente não é danoso para saúde humana e pode ter potencial para ser usado na medicina.

Apocynaceae/chemistry , DNA Damage , Latex/toxicity , Onions/drug effects , Chromosome Aberrations/drug effects , Mitotic Index , Mutagenicity Tests , Meristem/drug effects , Onions/genetics , Plant Roots/drug effects
Biol. Res ; 47: 1-8, 2014. ilus, graf, tab
Article in English | LILACS | ID: biblio-950728


BACKGROUND: Despite Cryptostegia grandiflora Roxb. ex R. Br. (Apocynaceae) leaves are widely used in folk Caribbean Colombian medicine for their anti-inflammatory effects, there are no studies that support this traditional use. Therefore, this work aimed to evaluate the effect of the total extract and primary fractions obtained from Cryptostegia grandiflora leaves, using in vivo and in vitromodels of inflammation, and further get new insights on the mechanisms involved in this activity. RESULTS: Ethanolic extract of Cryptostegia grandiflora leaves, and its corresponding ether and dichloromethane fractions, significantly reduced inflammation and myeloperoxidase activity (MPO) in ear tissue of mice treated with 12-O-tetradecanoyl-phorbol-13-acetate (TPA). Histological analysis revealed a reduction of edema and leukocyte infiltration. Complementarily, we demonstrated that extract and fractions reduced nitric oxide (NO•) and prostaglandin E2 (PGE2) production in LPS-stimulated RAW 264.7 macrophages, as well as scavenging activity on DPPH and ABTS radicals. CONCLUSIONS: Our results demonstrated for the first time the anti-inflammatory activity of Cryptostegia grandiflora leaves, supporting its traditional use. This activity was related to inhibition of MPO activity, and PGE2 and NO• production. These mechanisms and its antioxidant activity could contribute, at least in part, to the anti-inflammatory effect showed by this plant.

Animals , Female , Mice , Plant Extracts/therapeutic use , Apocynaceae/chemistry , Edema/drug therapy , Macrophages/drug effects , Anti-Inflammatory Agents/pharmacology , Oxytocics/analysis , Dinoprostone/analysis , Peroxidase/antagonists & inhibitors , Plant Leaves/chemistry , Cytotoxins/pharmacology , Cell Line, Tumor/drug effects , Inflammation/drug therapy , Mice, Inbred ICR , Nitric Oxide/analysis
Pakistan Journal of Pharmaceutical Sciences. 2014; 27 (3): 417-424
in English | IMEMR | ID: emr-142153


Allamanda species [Apocynaceae] are popular ornamentals. Additionally, A. cathartica possesses medicinal properties whereas all other species have not been reported. This research aims to analyze genetics and chemical contents of Allamanda species existing in Thailand. The explored species are A. blanchetii, A. cathartica, A. neriifolia, A. schottii, and A. violacea. The dendrogram constructed from 16 inter-simple sequence repeat markers clearly distinguished species with genetic similarity values of 0.92-0.93 for species level and 0.50-0.76 for genus level. Diverse chemicals content in hexane extracts from A. blanchetii, A. neriifolia, A. schottii, and A. violacea were detected by gas chromatography-mass spectrometry. A high amount of squalene was found in A. blanchetii [55.81%] and A. violacea [51.09%]. This content may function as a chemo preventative substance to protect people from cancer. Alpha-Tocopherol, a form of vitamin E, was one of the predominant components found in A. violacea [26.325%], A. schottii [15.41%], and A. neriifolia [9.16%]. One more substance, 9,12,15-octadecatrien-1-ol, was found to be relatively high in A. schottii [17.31%] and A. neriifolia [15.51%]. Other minor and unknown compounds were also detected. The discovery of these chemicals provides an alternative and supplement for improving human well-being and pharmaceutical industries with natural resources, especially in light of the population increase.

Apocynaceae/chemistry , Gas Chromatography-Mass Spectrometry , Microsatellite Repeats
Rev. biol. trop ; 61(4): 1891-1900, oct.-dic. 2013. ilus, tab
Article in English | LILACS | ID: lil-703935


The joint interpretation of phenology and nutritional metabolism provides important data on plant tissues reactivity and the period of gall induction. A population of Aspidosperma macrocarpon Apocynaceae with leaf galls induced by a Pseudophacopteron sp. Psylloidea was studied in Goiás state, Brazil. Assuming the morphological similarity between host leaves and intralaminar galls, a gradient from non-galled leaves towards galls should be generated, establishing a morpho-physiological continuum. The phenology, infestation of galls, and the carbohydrate and nitrogen contents were monthly evaluated in 10-20 individuals, from September 2009 to September 2010. Our objective was to analyze the nutritional status and the establishment of a physiological continuum between the galls and the non-galled leaves of A. macrocarpon. The period of leaf flushing coincided with the highest levels of nitrogen allocated to the new leaves, and to the lowest levels of carbohydrates. The nutrients were previously consumed by the growing leaves, by the time of gall induction. The levels of carbohydrates were higher in galls than in non-galled leaves in time-based analyses, which indicateed their potential sink functionality. The leaves were infested in October, galls developed along the year, and gall senescence took place from March to September, together with host leaves. This first senescent leaves caused insect mortality. The higher availability of nutrients at the moment of gall induction was demonstrated and seems to be important not only for the establishment of the galling insect but also for the responsiveness of the host plant tissues.

La interpretación conjunta de la fenología y el metabolismo nutricional proporciona datos importantes sobre la reacción de tejidos vegetales y el período de inducción de agallas. En el estado de Goiás, Brasil se estudió una población de Aspidosperma macrocarpon Apocynaceae con agallas foliares inducidas por un Pseudophacopteron sp. Psylloidea. Suponiendo que la similitud morfológica entre las hojas del hospedero y las agallas intralaminares genera un gradiente de hojas sin agallas hacia hojas con agallas, se establece un continuo morfo-fisiológico. La fenología, la infestación de las agallas y el contenido de carbohidratos y nitrógeno se evaluaron mensualmente en 10-20 individuos, de septiembre 2009 a septiembre 2010. El objetivo fue analizar el estado nutricional y el establecimiento de un continuo fisiológico entre las hojas que producen agallas y las hojas sin agallas de A. macrocarpon. El período de emergencia de hojas coincidió con los niveles más altos de nitrógeno en las hojas nuevas, y los niveles más bajos de carbohidratos.Los nutrientes se consumieron previamente por las hojas en crecimiento, en el momento de inducción de las agallas. Los niveles de carbohidratos fueron más altos en las hojas con agallas que en aquellas sin agallas, en análisis basados en tiempo, lo que indica su ciclo de funcionalidad potencial. Las hojas hospederas se infestaron en octubre, el desarrollo y la senescencia de las agallas se llevó a cabo entre marzo y septiembre, en las hojas hospederas. Estas primeras hojas senescentes causaron mortalidad de insectos. Hay mayor disponibilidad de nutrientes en el momento de la inducción de las agallas y parece ser importante no sólo para el establecimiento del insecto que produce agallas, sino también para la capacidad de respuesta de los tejidos de la planta hospedera.

Animals , Apocynaceae/parasitology , Hemiptera/physiology , Host-Parasite Interactions/physiology , Plant Tumors/parasitology , Apocynaceae/chemistry
Article in English | IMSEAR | ID: sea-163305


Aim: This study was designed to determine the antitumor and antioxidant properties of crude methanol extract from the leaves of Plumeria acuminata (Apocynaceae) (MEPA) against Ehrlich Ascites Carcinoma (EAC) bearing Swiss albino mice. Study Design: Study design is methodology, mentioned below. Place and Duration of Study: Division of Pharmacology, Department of Pharmaceutical Technology, Jadavpur University, Jadavpur, Kolkata, India between 2006 and 2007. Methodology: The extract was administered at the doses of 100, 250 and 500 mg/kg per day for 14 days, after 24 hr of tumor inoculation. After the administration of the last dose followed by 18 hr fasting, mice were then sacrificed for observation of antitumor activity. The effect of MEPA on the growth of transplantable murine tumor, life span of EAC bearing host, viable and non-viable cell count, packed cell volume, hematological profile and biochemical parameters such as lipid peroxidation (LPO), reduced glutathione content (GSH), superoxide dismutase (SOD) and catalase (CAT) activities were estimated. Results: MEPA caused significant (P<0.01) decrease in tumor volume, packed cell volume and viable count; and it prolonged the life span of EAC-tumor bearing mice. Hematological studies reveal that the Hb content and RBC count were decreased in EAC treated mice, whereas the restoration to near normal levels was observed in extract treated animals. MEPA significantly (P<0.05) decreased the levels of LPO and significantly increased the levels of GSH, SOD and CAT. Moreover the MEPA was found to be devoid of conspicuous short-term toxicity in the mice when administered daily for 14 days at the doses of 100, 250 and 500 mg/kg Conclusion: The results suggested that the methanol extract of Plumeria acuminata leaves exhibited antitumor effect by modulating lipid peroxidation and augmenting antioxidant defense system in EAC bearing Swiss albino mice.

Animals , Antioxidants/pharmacology , Antineoplastic Agents/pharmacology , Apocynaceae/blood , Apocynaceae/chemistry , Apocynaceae/pharmacology , Blood/analysis , Blood/chemistry , Blood/drug effects , Carcinoma, Ehrlich Tumor , Mice , Neoplasms, Experimental/drug therapy , Plant Extracts/administration & dosage , Plant Extracts/pharmacology
Article in English | IMSEAR | ID: sea-136329


Background & objectives: The severe toxicity, exorbitant cost and emerging resistance of Leishmania species against most of the currently used drugs underscores the urgent need for the alternative drugs. The present study evaluates in vitro anti-leishmanial activity of Plumeria bicolor and its isolated compounds. Methods: The in vitro anti-parasitic activity of chloroform extract of Plumeria bicolor, plumericin and isoplumericin were tested alongwith appropriate controls against promastigote and amastigote forms of Leishmania donovani using 96 well microtiter plate. The concentration used for assessing the anti-leishmanial activity of extract of Plumeria bicolor and both isolated compounds were 100 μg/ml and 15 μM, respectively. The viability of the cells was assessed by MTT assay. The cytotoxicity of these compounds was performed against J774G8 murine macrophage cells lines at the concentration of 30 μM. Results: The Plumeria bicolor extract showed activity with the IC50 of 21±2.2 and 14±1.6 μg/ml against promastigote and amastigote forms of L. donovani, respectively. Plumericin consistently showed high activity with the IC50 of 3.17±0.12 and 1.41±0.03 μM whereas isoplumericin showed the IC50 of 7.2±0.08 μM and 4.1±0.02 μM against promastigote and amastigote forms, respectively. Cytotoxic effect of the chloroform extract of P. bicolor, plumericin and isoplumericin was evaluated in murine macrophage (J774G8) model with CC50 value of 75±5.3 μg/ml, 20.6±0.5 and 24±0.7 μM, respectively. Interpretation & conclusions: Our results indicated that plumericin showed more potent activity than isoplumericin and might be a promising anti-leishmanial agent against L. donovani.

Animals , Antiparasitic Agents/pharmacology , Apocynaceae/chemistry , Cell Line , Humans , Indenes/pharmacology , Inhibitory Concentration 50 , Iridoids/pharmacology , Leishmania/drug effects , Leishmania/parasitology , Leishmania donovani/drug effects , Leishmania donovani/pathogenicity , Macrophages/cytology , Mice , Plant Extracts/pharmacology
Bol. latinoam. Caribe plantas med. aromát ; 10(4): 363-368, jul. 2011. tab, graf
Article in English | LILACS | ID: lil-654648


The crude methanolic extract of the bark of Sarcolobus globosus (Family-apocynaceae) and its different organic soluble Kupchan fractions were screened for total phenol content (TPC), cytotoxic, membrane stabilizing and thrombolytic activities. The polyphenol content was determined colorimetrically using Folin-Ciocalteu method and expressed in gallic acid equivalent. The chloroform soluble Kupchan fraction (CSF) exhibited higher level of Total Polyphenol Contents (TPC, 54.21 gm of GAE/100 gm of dried extract). In the brine shrimp lethality bioassay, the crude methanolic extract (MEBP) exhibited significant cytotoxicity. The membrane stabilizing activity was assessed by using erythrocyte in hypotonic solution and was compared with acetyl salicylic acid. The hexane soluble Kupchan fraction (HSF) produced 52.73 percent inhibition of hemolysis of RBC as compared to 65.38 percent revealed by acetyl salicylic acid (0.10 mg/mL). In thrombolytic study screening, the crude methanolic extract demonstrated significant thrombolytic activity in human blood specimen.

El extracto crudo metanólico de la corteza de Sarcolobus globosus (Familia-apocynaceae) y sus diferentes fracciones solubles Kupchan fueron identificadas para contenido total de fenoles (CTF), actividades citotóxicas, estabilizantes de membrana y trombolíticas. El contenido de polifenoles fue determinado colorimétricamente usando el método Folin-Ciocalteu y expresados en equivalentes a ácido gálico. La fracción Kupchan soluble en cloroformo (FSC) exhibió los mayores niveles de Contenido Total de Polifenoles (CFT, 54,21 gm of GAE/100gm de extracto seco). En el bioensayo de letalidad (Artemia salina), el extracto metanólico crudo (EMC) exhibió una siginificativa citotoxicidad. La actividad estabilizadora de membrana fue estimada usando eritrocitos en un medio hipotónico y fue comparado con el ácido acetil salicílico. La fracción Kupchan soluble en hexano (FSH) produjo un 52,73 por ciento de inhibición de la hemólisis de los glóbulos rojos comparado con un 65,38 por ciento revelado por el ácido acetil salicílico (0,1 mg/mL). En las determinaciones trombolíticas, el extracto metanólico crudo demostró una significativa actividad trombolítica en una muestra de sangre humana.

Apocynaceae/chemistry , Plant Extracts/pharmacology , Plant Extracts/chemistry , Phenols/analysis , Fibrinolytic Agents/pharmacology , Apocynaceae/chemistry , Cell Membrane , Polyphenols/analysis
Article in English | IMSEAR | ID: sea-135607


Background & objective: Hedranthera barteri (HB) is used in folk medicine as a vermifuge, laxative and an anti-inflammatory agent. The aim of this study was to evaluate the anti-ulcer and antioxidant properties of the dichloromethane fraction of HB root (DMHBR). Methods: Anti-ulcerogenic activity was assessed in cold-restraint (CRU), aspirin (ASP), alcohol (AL), pyloric ligation (PL) induced gastric ulcer models in rats and histamine-induced duodenal ulcer (HST) in guinea pigs. The effect of DMHBR (100 mg/kg) on gastric juice for free and total acidity, peptic activity and mucin secretion, using the pylorus ligated model, were evaluated. The H+, K+-ATPase activity was assayed in gastric microsomes, spectrophotometrically. The in vitro anti-oxidant assays were explored through DPPH, nitric oxide, hydroxyl radical, superoxide anion scavenging assays. Results: DMHBR reduced the incidence of ulcers in CRU (63.3%), PL (58.5%), ASP (52.7%), HST (75.0%) and AL (53.87%). Also, reductions were observed in the free acidity (49.4%), total acidity (45.8%) and peptic activity (32.9%) with increase in the mucin secretion by 81.6 per cent. DMHBR (60-100 μg/ml) inhibited the H+,K+-ATPase activity with IC50 of 89.64 μg/ml compared with omeprazole (10-50 μg/ml ) with IC50 of 32.26 μg/ml. DMHBR showed antioxidant activity with IC50 values of DPPH (397.69 μg/ml), nitric oxide (475.88 μg/ml), hydroxyl radical (244.22 μg/ml) and superoxide anion radical (285.20 μg/ml). Interpretation & conclusion: DMHBR showed anti-ulcer activity against experimentally-induced peptic ulcer models and exhibited both cytoprotective and anti-secretory property. It exhibited a proton pump inhibition activity and its anti-ulcer properties may be partly ascribed to its antioxidant activities.

Animals , Anti-Ulcer Agents/pharmacology , Antioxidants/pharmacology , Apocynaceae/chemistry , Gastric Juice/drug effects , H(+)-K(+)-Exchanging ATPase/antagonists & inhibitors , Methylene Chloride , Microsomes/metabolism , Phytotherapy/methods , Plant Extracts/pharmacology , Plant Roots/chemistry , Rats , Rats, Sprague-Dawley , Stomach Ulcer/drug therapy
Braz. j. pharm. sci ; 46(3): 515-523, July-Sept. 2010. ilus
Article in English | LILACS | ID: lil-564918


Macrosiphonia velame (Apocynaceae), popularly known as "velame-branco", is mainly used for treating inflammatory conditions. The antiinflammatory, antinociceptive and antipyretic effects of the hydroethanolic extract of the xylopodium from M. velame (HEMv) were evaluated using several animal models. HEMv showed low acute oral toxicity with LD50 of 4.176 ± 218.5 mg/kg in mice. In tests of carrageenan and dextran-induced paw edema and carrageenan-induced pleurisy in rats, and croton oil-induced cutaneous dermatitis in mice, HEMv presented systemic and topical antiinflammatory activities. In experiments of nociception induced by acetic acid, formalin and capsaicin in mice, the HEMv evidenced an antinociceptive effect, being active against both inflammatory and neurogenic pain. Additionally, the HEMv prevented brewer's yeast-induced pyrexia in rats. It is likely that the pharmacologic mechanism of HEMv may involve the inhibition of different mediators of the inflammatory response, such as histamine, serotonin, prostaglandins and leukotrienes. A preliminary phytochemical study was also undertaken on HEMv, which revealed the presence of flavonoids, phenolic compounds, pentacyclic triterpenoids, saponins, coumarins, catechins, tannins, and alkaloids. Taken together, these results suggest that M. velame extract has antiinflammatory, antinociceptive and antipyretic properties and further validate the traditional use of this plant in inflammatory conditions.

Macrosiphonia velame (Apocynaceae), conhecida popularmente como velame-branco, é utilizada no tratamento de inflamações. Avaliou-se nesse estudo, os efeitos antiinflamatório, antinociceptivo e antipirético do extrato hidroetanólico do xilopódio de M. velame (HEMv) em modelos animais. O HEMv apresentou baixa toxicidade aguda oral, com DL50= 4.176 ± 218,5 mg/kg nos camundongos. Nos testes de edema de pata por carragenina e dextrana e pleurisia por carragenina em ratos e dermatite cutânea por óleo de croton em camundongos, o HEMv apresentou atividade antiinflamatória sistêmica e tópica. Nos experimentos de nocicepção induzida por ácido acético, formalina e capsaicina em camundongos, o HEMv inibiu a resposta nociceptiva nos três modelos, mostrando-se ativo tanto na dor de origem inflamatória como neurogênica. Adicionalmente, o HEMv bloqueou a hipertermia induzida por levedura de cerveja nos ratos. É provável que os efeitos farmacológicos observados para o HEMv decorram da inibição de mediadores da resposta inflamatória produzidos pelas vias da COX e/ou LOX bem como da inibição da liberação de histamina e serotonina. A análise fitoquímica do HEMv revelou a presença de flavonóides, compostos fenólicos, triterpenóides pentacíclicos, saponinas, cumarinas, catequinas, taninos catéquicos e alcalóides. Estes resultados validam sob o ponto de vista pré-clínico, o uso popular de M. velame em processos inflamatórios.

Animals , Male , Adult , Rats , Anti-Inflammatory Agents , Analgesics, Non-Narcotic/analysis , Analgesics/analysis , Apocynaceae/chemistry , Plant Extracts/pharmacology , Analysis of Variance , Pharmacognosy/statistics & numerical data , Skin Tests , Statistical Analysis
Braz. j. pharm. sci ; 46(3): 555-561, July-Sept. 2010. ilus
Article in English | LILACS | ID: lil-564923


Rauvolfia sellowii Müll. Arg. (Apocynaceae), a Brazilian native tree rich in indole alkaloids, is known as "pau-pra-tudo" and popularly used as hypocholesterolemic, hypoglycemic and antihypertensive. The aim of this work was to study the anatomy of the young stems and stem barks of this medicinal plant, in order to contribute to the identification of the species as a drug. The plant material was fixed and prepared according to standard microtechniques. The young stems have remaining epidermis, but a suberified peridermis is evident. The phellogen is located in the cortical region, forming suber externally. Underneath the phellogen, lies the phelloderm and collenchymatic region. In the cortex, there are numerous laticifers and some fibers. There is an incomplete sclerenchymatic sheath, consisting of several groups of fibers and stone cells. The stem has internal phloem ordered as isolated groups side by side. Numerous laticifers, calcium oxalate crystals, idioblasts and amyloplasts are found in the cortex, phloem, xylem and pith. The stem bark has many layers of suber and cortical parenchyma, a sheath composed of fibers and stone cells totally lignified, and external phloem. These anatomical characteristic, taken together, can be used as quality control parameters for this species.

Rauvolfia sellowii Müll. Arg. (Apocynaceae), uma árvore nativa brasileira rica em alcaloides indólicos, é conhecida como "pau-pra-tudo" e utilizada popularmente como hipocolesterolêmica, hipoglicêmica e anti-hipertensiva. O presente trabalho teve como objetivo caracterizar anatomicamente o caule jovem e a casca caulinar dessa planta medicinal, a fim de contribuir para a identificação e autenticidade da droga. O material vegetal foi fixado e submetido às microtécnicas usuais. O caule jovem possui epiderme remanescente, porém uma periderme suberificada é observada. O felogênio instala-se na região cortical, formando súber externamente. Subjacentes ao felogênio são observadas a feloderme e uma região colenquimática. No córtex, há numerosos laticíferos e algumas fibras. Há uma bainha esclerenquimática incompleta, constituída de vários grupos de fibras e células pétreas. O caule mostra floema interno organizado em grupos isolados lado a lado. Numerosos laticíferos, cristais de oxalato de cálcio, idioblastos e amiloplastos são encontrados no córtex, no floema, no xilema e na medula. A casca do caule possui várias camadas de súber e parênquima cortical, uma bainha composta de fibras e células pétreas totalmente lignificadas, e floema externo. Estes caracteres anatômicos, quando analisados em conjunto, podem ser utilizados como parâmetros para controle de qualidade desta espécie.

Apocynaceae/anatomy & histology , Apocynaceae/chemistry , Plant Stems/chemistry , Plant Leaves/chemistry , Biological Phenomena , Pharmacognosy , Plants, Medicinal/chemistry
Braz. j. pharm. sci ; 46(2): 245-250, Apr.-June 2010. ilus, tab
Article in English | LILACS | ID: lil-564891


In this study, the radical scavenging capacity of Guiera senegalensis, Ipomoea asarifolia and Anisopus mannii were compared. The ascorbic acid equivalent of the stem bark (2.1 mM), leaves (2.05 mM) and root barks (1.89 mM) of Guiera senegalesis are much higher than any part of Ipomoea asarifolia or Anisopus manii. The stem bark, leaves and root bark of Guiera Senegalensis had IC50 of 15.4, 20.0 and 17.0 µL respectively, while corresponding parts of Ipomoea asarifolia showed IC50 of 50, 42 and 65 µL, respectively. These results suggest that Guiera senegalensis and Ipomoea asarifolia possess significant antioxidant capacities to warrant further detailed studies on the role of this property in their therapeutic effects.

Comparou-se a capacidade de sequestrar radicais livres de Guiera senegalensis, Ipomoea asarifolia e Anisopus mannii. O equivalente em ácido ascórbico da casca do caule (2,1 mM), folhas (2,05 mM) e da casca da raiz (1,89 mM) de Guiera senegalesis foi muito mais alto do que qualquer parte da Ipomoea asarifolia e da Anisopus manii. A casca do caule, as folhas e a casca da raiz de Guiera senegalensis apresentaram IC50 de 15,4, 20,0 and 17,0 µLl, respectivamente, enquanto as partes correspondentes de Ipomoea asarifolia apresentaram IC50 de 50, 42 e 65 µL respectivamente. Esses resultados sugerem que Guiera senegalensis e Ipomoea asarifolia possuem capacidade oxidante significativa que demanda estudos posteriores detalhados acerca do papel dessa propriedade em seus efeitos terapêuticos.

Apocynaceae/chemistry , Combretaceae/chemistry , Ipomoea/chemistry , Physiology, Comparative , Antioxidants/analysis , Plant Extracts/analysis
Mem. Inst. Oswaldo Cruz ; 104(6): 805-812, Sept. 2009. ilus, graf, tab
Article in English | LILACS | ID: lil-529568


It has been shown previously that the laticifer fluid of Calotropis procera (Ait.) R.Br. is highly toxic to the egg hatching and larval development of Aedes aegypti L. In the present study, the larvicidal potential of other laticifer fluids obtained from Cryptostegia grandiflora R.Br., Plumeria rubra L. and Euphorbia tirucalli L. was evaluated. We attempted to correlate larvicidal activity with the presence of endogenous proteolytic activity in the protein fraction of the fluids. After collection, the fluids were processed by centrifugation and dialysis to obtain the soluble laticifer protein (LP) fractions and eliminate water insoluble and low molecular mass molecules. LP did not visibly affect egg hatching at the doses assayed. LP from Cr. grandiflora exhibited the highest larval toxicity, while P. rubra was almost inactive. E. tirucalli was slightly active, but its activity could not be correlated to proteins since no protein was detected in the fluid. The larvicidal effects of LP from C. procera and Cr. grandiflora showed a significant relationship with the proteolytic activity of cysteine proteinases, which are present in both materials. A purified cysteine proteinase (papain) from the latex of Carica papaya (obtained from Sigma) was similarly effective, whereas trypsin and chymotrypsin (both serine proteinases) were ineffective. The results provide evidence for the involvement of cysteine proteinase activity in the larvicidal action of some laticifer fluids. C. procera is an invasive species found in areas infested with Ae. aegypti and thus could prove useful for combating mosquito proliferation. This is the first report to present evidence for the use of proteolytic enzymes as chemical agents to destroy Ae. aegypti larvae.

Animals , Aedes/drug effects , Apocynaceae/chemistry , Apocynaceae/chemistry , Cysteine Proteases/pharmacology , Euphorbia/chemistry , Insect Proteins/drug effects , Latex/pharmacology , Aedes/growth & development , Cysteine Proteases/isolation & purification , Insect Proteins/physiology , Larva/drug effects , Larva/growth & development , Latex/chemistry , Latex/isolation & purification
Mem. Inst. Oswaldo Cruz ; 104(4): 659-661, July 2009. tab
Article in English | LILACS | ID: lil-523737


Himatanthus articulatus (Vahl) Woodson is a tree found in the northern Amazon savannahs (common name: sucuba) that is used in local Amerindian medicine. Leaf, bark and branch wood methanol extracts, sequentially obtained hexane, ethyl acetate and methanol extracts and latex were evaluated for antifungal and antibacterial activities against American Type Culture Collection (ATCC) and local clinical strains using the disc diffusion method. Methanol extracts and latex inhibited Candida albicans, leaf methanol extracts inhibited Staphylococcus aureus and Bacillus subtilis and bark methanol extracts inhibited B. subtilis. Active extracts inhibited the ATCC and clinical strains. Polar antifungal and antibacterial principles in latex and extracts are thought to be responsible for the inhibition.

Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Apocynaceae/chemistry , Candida albicans/drug effects , Escherichia coli/drug effects , Gram-Positive Endospore-Forming Rods/drug effects , Anti-Bacterial Agents/isolation & purification , Antifungal Agents/isolation & purification , Bacillus subtilis/drug effects , Disk Diffusion Antimicrobial Tests , Plant Extracts/pharmacology , Staphylococcus aureus/drug effects
Mem. Inst. Oswaldo Cruz ; 102(3): 359-366, June 2007. tab, graf
Article in English | LILACS | ID: lil-452514


In the present study, a quassinoid, neosergeolide, isolated from the roots and stems of Picrolemma sprucei (Simaroubaceae), the indole alkaloids ellipticine and aspidocarpine, isolated from the bark of Aspidosperma vargasii and A. desmanthum (Apocynaceae), respectively, and 4-nerolidylcatechol, isolated from the roots of Pothomorphe peltata (Piperaceae), all presented significant in vitro inhibition (more active than quinine and chloroquine) of the multi-drug resistant K1 strain of Plasmodium falciparum. Neosergeolide presented activity in the nanomolar range. This is the first report on the antimalarial activity of these known, natural compounds. This is also the first report on the isolation of aspidocarpine from A. desmanthum. These compounds are good candidates for pre-clinical tests as novel lead structures with the aim of finding new antimalarial prototypes and lend support to the traditional use of the plants from which these compounds are derived.

Animals , Antimalarials/pharmacology , Apocynaceae/chemistry , Plasmodium falciparum/drug effects , Simaroubaceae/chemistry , Antimalarials/isolation & purification , Brazil , Parasitic Sensitivity Tests , Plant Extracts/pharmacology
Indian J Exp Biol ; 2007 May; 45(5): 419-24
Article in English | IMSEAR | ID: sea-56707


The effect of chloroform soluble fraction (F-A) of twigs of Sarcostemma brevistigma on contractions induced by KCl, histamine, and acetylcholine in the isolated guinea pig ileum and taenia coli smooth muscles has been evaluated. F-A (19.5 microg/ml) significantly inhibited the contraction induced by 40 mM KCl to the extent of 87.6% in the isolated guinea pig ileum. In the isolated guinea pig ileum, F-A (64.3 and 59.2 microg/ml) significantly inhibited the contractions induced by acetylcholine and histamine to the extent of 85 and 83% respectively. In the isolated guinea pig taenia coli, F-A (65.2 microg/ml) significantly inhibited the contraction induced by 40 mM KCl to the extent of 96.0%. The inhibitory effect of F-A (40 microg/ml) on the isolated guinea pig taenia coli was reduced by Bay K 8644 (10(-6) M) to the extent of 61.6 from 73.6%. These results suggest that the F-A may exhibit smooth muscle relaxant activity by blocking the Ca2+ channels.

Acetylcholine/pharmacology , Animals , Apocynaceae/chemistry , Dose-Response Relationship, Drug , Guinea Pigs , Histamine/pharmacology , Ileum/drug effects , Male , Muscle Contraction/drug effects , Muscle, Smooth/drug effects , Parasympatholytics/pharmacology , Plant Extracts/chemistry , Potassium Chloride/pharmacology , Verapamil/pharmacology
West Indian med. j ; 55(4): 219-223, Sept. 2006.
Article in English | LILACS | ID: lil-472126


The antifungal properties of aqueous and ethanol extracts of Funtumia elastica and Mallotus oppositifolius were carried out using the disc diffusion agar assay. The crude extracts exhibited definite significant antifungal activity on most of the fungi. The zone of inhibition varied for the fungi, which were: Aspergillus flavus, Candida albicans, Microsporium audouinii, Penicillium sp, Trichophyton mentagrophytes, Trichoderma sp and Trichosporon cutaneum with respect to the type of plant extract. The aqueous extracts of Mallotus oppositifolius had the highest zone of inhibition of 24.75 +/- 0.86 mm on Penicillium sp. The fulcin antibiotic had zone of inhibition of 11.94 +/- 0.43 mm on Microsporium audouinii, being its highest inhibition on any of the fungi tested. Preliminary phytochemical studies of F elastica and M oppositifolius extracts revealed that they contain anthocyanins, butacyanin, flavonoids, steroids and tannins. Phytobutanin was absent in the extracts. Heavy metal analysis of plant materials showed absence of cadmium, zinc, lead, chromium and nickel, while the presence of copper iron and manganese was less than 0.95.

Las propiedades antifúngicas de los extractos acuosos y etanólicos de Funtumia elastica y Mallotus oppositifolius fueron probadas mediante ensayo de difusión con discos en agar. Los extractos crudos mostraron poseer una actividad antifúngica definitivamente significativa sobre la mayoría de los hongos. La zona de inhibición varió en correspondencia con los hongos, a saber, Aspergillus flavus, Candida albicans, Microsporium audouinii, Penicillium sp, Trichophyton mentagrophytes, Trichoderma sp y Trichosporon cutaneum, con respecto al tipo de extracto de planta. Los extractos acuosos de Mallotus oppositifolius presentaron la zona de inhibición más alta, a saber, 24.75 ± 0.86 mm, al aplicarse sobre Penicillium sp. El antibiótico fulcin presentó una zona de inhibición de 11.94 ± 0.43 mm al aplicarse sobre Microsporium audouinii, resultando ser ésta la inhibición más alta en relación con todos los hongos sometidos a prueba. Los estudios fitoquímicos de los extractos de F elastica y M oppositifolius revelaron contenidos de antocianinas, butacianinas, flavonoides, esteroides, y taninas. La fitobutanina estuvo ausente en todos los extractos. El análisis de metales pesados en las muestras de plantas mostró ausencia de cadmio, zinc, plomo, cromo y níquel, en tanto que la presencia de cobre, hierro y manganeso estuvo por debajo de 0.95%.

Humans , Alkaloids/chemistry , Alkaloids/pharmacology , Antifungal Agents/pharmacology , Plant Extracts/chemistry , Mycoses , Phytotherapy , Plants, Medicinal/chemistry , Apocynaceae/chemistry , Mallotus Plant/chemistry , Nigeria , Pilot Projects