Actividad antiproliferativa de Aldama arenaria (Baker) E. E. Schill. & Panero / Antiproliferative activity from Aldama arenaria (Baker) E. E. Schill. & Panero

El extracto de cloroformo (CE) y las fracciones obtenidas de las raíces de Aldama arenaria se evaluaron para determinar su actividad antiproliferativa in vitro contra 10 líneas celulares tumorales humanas [leucemia (K-562), mama (MCF-7), ovario que expresa un fenotipo resistente a múltiples fármacos (NCI/ADR-RES), melanoma (UACC-62), pulmón (NCI-H460), próstata (PC-3), colon (HT29), ovario (OVCAR-3), glioma (U251) y riñón (786-0)]. CE presentó actividad antiproliferativa débil a moderada (log GI50 medio 1.07), mientras que las fracciones 3 y 4, enriquecidas con diterpenos de tipo pimarane [ent-pimara-8 (14), ácido 15-dien-19-oico y ent-8(14),15-pimaradien-3ß-ol], presentaron actividad moderada a potente para la mayoría de las líneas celulares, con un log GI50 medio de 0.62 y 0.59, respectivamente. Los resultados mostraron una acción antiproliferativa in vitro prometedora de las muestras obtenidas de A. arenaria, con los mejores resultados para NCI/ADR-RES, HT29 y OVCAR-3, y valores de TGI que van desde 5.95 a 28.71 µg.mL-1, demostrando que los compuestos de esta clase pueden ser prototipos potenciales para el descubrimiento de nuevos agentes terapéuticos.

Chloroform extract (CE) and fractions obtained from Aldama arenaria roots were evaluated for their in vitro antiproliferative activity against 10 human tumor cell lines [leukemia (K-562), breast (MCF-7), ovary expressing a multidrug-resistant phenotype (NCI/ADR-RES), melanoma (UACC-62), lung (NCI-H460), prostate (PC-3), colon (HT29), ovary (OVCAR-3), glioma (U251), and kidney (786-0)]. CE presented weak to moderate antiproliferative activity (mean log GI50 1.07), whereas fractions 3 and 4, enriched with pimarane-type diterpenes [ent-pimara-8(14),15-dien-19-oic acid and ent-8(14),15-pimaradien-3ß-ol], presented moderate to potent activity for most cell lines, with mean log GI50 of 0.62 and 0.59, respectively. The results showed promising in vitro antiproliferative action of the samples obtained from A. arenaria, with the best results for NCI/ADR-RES, HT29, and OVCAR-3, and TGI values ranging from 5.95 to 28.71 µg.mL-1, demonstrating that compounds of this class may be potential prototypes for the discovery of new therapeutic agents.

Coronarin D Induces Apoptotic Cell Death and Cell Cycle Arrest in Human Glioblastoma Cell Line.

Glioblastoma (GBM) is the most frequent and highest-grade brain tumor in adults. The prognosis is still poor despite the use of combined therapy involving maximal surgical resection, radiotherapy, and chemotherapy. The development of more efficient drugs without noticeable side effects is urgent. Coronarin D is a diterpene obtained from the rhizome extract of Hedychium coronarium, classified as a labdane with several biological activities, principally anticancer potential. The aim of the present study was to determine the anti-cancer properties of Coronarin D in the glioblastoma cell line and further elucidate the underlying molecular mechanisms. Coronarin D potently suppressed cell viability in glioblastoma U-251 cell line, and also induced G1 arrest by reducing p21 protein and histone H2AX phosphorylation, leading to DNA damage and apoptosis. Further studies showed that Coronarin D increased the production of reactive oxygen species, lead to mitochondrial membrane potential depolarization, and subsequently activated caspases and ERK phosphorylation, major mechanisms involved in apoptosis. To our knowledge, this is the first analysis referring to this compound on the glioma cell line. These findings highlight the antiproliferative activity of Coronarin D against glioblastoma cell line U-251 and provide a basis for further investigation on its antineoplastic activity on brain cancer.

Isolation, structural identification and cytotoxic activity of hexanic extract, cyperenoic acid, and jatrophone terpenes from Jatropha ribifolia roots

The cytotoxicity of a hexanic fraction produced from the ethanolic crude extract, obtained from Jatropha ribifolia (Pohl) Baill, Euphorbiaceae, roots was evaluated against ten human cancer cell lines (MCF-7, NCI-ADR/RES, OVCAR-3, PC-3, HT-29, NCI-H460,786-O, UACC-62, K-562, U251) compared with doxorrubicine as positive control. Compounds jatrophone and cyperenoic acid were isolated from the hexanic extract and characterized by spectroscopic techniques (NMR of ¹H, 13C and IR). The in vitro antiproliferative activity of jatrophone showed selectivity in a concentration dependent way with Total Inhibition growth of: glioma 0.57 µg mL-1 (U251), breast cancer 9.2 µg mL-1 (MCF-7), adriamycin-resistant ovarian cancer 0.96 µg mL-1 (NCI-ADR/RES), kidney 4.2 µg mL-1 (786-0), prostate cancer 8.4 µg mL-1 (PC-3), colon cancer 16.1 µg mL-1 (HT29) and leukemia 0.21 µg mL-1 (K-562).

Anti-oxidative and anti-ulcerogenic activity of Ipomoea imperati

Ipomoea imperati (Vahl) Griseb., Convolvulaceae, is used in traditional medicine for the treatment of inflammation, swelling and wounds, as well as to treat pains and stomach problems. This work evaluates the anti-oxidative activity by ESR (Electron Spin Resonance spectroscopy) and the preventive and curative actions of I. imperati in gastric ulcer animal model. Ipomoea imperati (200 mg/kg, p.o.) prevented the formation of gastric lesions in 78 percent (p<0.05) when compared with the negative control tween 80. Lanzoprazole, prevented in 85 percent the gastric lesions formation induced by ethanol (p<0.05). Therefore, the oral administration of I. imperati one hour before the ulcerogenic agent prevented the ulcer formation, conserving the citoprotection characteristics of the gastric mucosa and assuring the integrity of gastric glands and gastric fossets. The healing activity of I. imperati (200 mg/kg, p.o.) evaluated in chronic ulcer experiments induced by the acetic acid, was 72 percent (p<0.05). The positive control, ranitidine, healed 78 percent of the gastric lesions (p<0.05). The histological analysis confirmed the recovery of the mucosal layer and the muscle mucosal layer harmed by the acetic acid. Experiments in vitro with DPPH (2.2-diphenyl-1-picrylhydrazyl) of anti-oxidative activity demonstrated that I. imperati presents an IC50 of 0.73±0.01 mg/mL.

Antinociceptive activity of Ipomoea imperati (Vahl) Griseb., Convolvulaceae / Atividade antinociceptiva de Ipomoea imperati (Vahl) Griseb., Convolvulaceae

Ipomoea imperati (Vahl) Griseb., Convolvulaceae, is used in folk medicine for the treatment of inflammation, swelling and wounds, as well as to treat pains after childbirth and for stomach problems. Administration of ethanol extract, lipid and aqueous fraction of I. imperati(300, 100 and 200 mg/kg) significantly inhibited the abdominal constriction in mice induced by acetic acid; increased the sleeping time evoked by pentobarbital sodium and showed a significant activity by inhibiting formalin-induced paw edema in mice. The same dose of I. imperatialso raised the pain of mice in the hot-plate test and increased the latency at all observation times. The pre-treatment of the animals with naloxone (5 mg/kg, i.p.) suggested the participation of the opioid system in the antinociceptive effect of Ipomoea imperati.

A espécie vegetal Ipomoea imperati (Vahl) Griseb., Convolvulaceae, é usada popularmente para tratar inflamação, inchaço e feridas, bem como para tratar dor após o parto e dor estomacal. A administração do extrato etanólico e das frações lipídica e aquosa de I. imperati(300, 100 e 200 mg/kg) inibiu significativamente as contrações abdominais em camundongo induzidas por ácido acético, aumentou o tempo de sono evocado por pentobarbital sódico e mostrou significativa atividade inibitória sobre o edema de pata de camundongo induzido por formalina. As mesmas doses de I. imperati(300, 100 e 200 mg/kg) também elevou a latência de todos os tempos observados no teste da placa quente. O pré-tratamento de animais com naloxona (5 mg/kg, i.p) sugere a participação do sistema opioide no efeito anti-nociceptivo de Ipomoea imperati.

Figures of merit in the quantification of ibuprofen enantiomers by chiral HPLC.

The determination of ibuprofen (IBU) enantiomers by chiral high-performance liquid chromatographic is described. The methodology is based on chiral recognition of ibuprofen by a chiral column based on cellulose tris(4-methylbenzoate) coated on silica gel (Chiralcel OJ-H). The mobile phase is n-hexane-2-propanol-trifluoroacetic acid (98:2:0.1, v/v/v). The flow rate was 1.0 mL/min, and UV detection was 254 nm. The samples of ibuprofen were prepared in n-hexane in the concentration range 50-100% of (S)-IBU 1 x 10(-3) mol/L. Calibration and validation method were performed with six and nine samples, respectively. Goodness-of-fit measures represented by correlation coefficient, y-intercept, and slope of the regression line were 0.9836, 21373, 2162, respectively. Average of the relative error of the proposed method was 3.0%, 0.9% (S)-IBU selectivity, and 2162% (S)-IBU-1 sensitivity. The minimum concentration difference between two samples that could be determined in the linear dynamic range was 0.4% (S)-IBU. Limits of detection and quantification were 8.1 and 27.0% (S)-IBU, respectively. These results indicate that the proposed method can be employed for determination of the enantiomeric composition of IBU.

13C and 1H NMR signal assignments of some new synthetic dehydroabietic acid derivatives.

The (1)H and (13)C NMR signal assignments of a series of new synthetic derivatives of dehydroabietic acid are presented.

Basal encephalocele associated with morning glory syndrome: case report.

The basal encephaloceles refer to rare entities and they correspond to herniation of brain tissue through defects of skull along the cribiform plate or the sphenoid bone. A rare morning glory syndrome, with characteristic retinal defect has been reported in association with basal encephaloceles. Hypophysis hormonal deficiencies may occur. We accounted for a pituitary dwarfism with delayed diagnosed transsphenoidal encephalocele associated with morning glory syndrome, showing the alterations found in retinography, computed tomography and magnetic resonance imaging.

Basal encephalocele associated with morning glory syndrome: case report

The basal encephaloceles refer to rare entities and they correspond to herniation of brain tissue through defects of skull along the cribiform plate or the sphenoid bone. A rare morning glory syndrome, with characteristic retinal defect has been reported in association with basal encephaloceles. Hypophysis hormonal deficiencies may occur. We accounted for a pituitary dwarfism with delayed diagnosed transsphenoidal encephalocele associated with morning glory syndrome, showing the alterations found in retinography, computed tomography and magnetic resonance imaging.

As encefaloceles basais são entidades raras e correspondem a herniações do tecido cerebral através de um defeito do crânio, ao longo da lâmina crivosa etmoidal ou do osso esfenoidal. A rara síndrome morning glory, com alterações de fundo de olho características pode apresentar-se associada à encefalocele basal. Deficiências hormonais hipofisárias podem ocorrer. Relatamos caso de nanismo hipofisário com encefalocele transesfenoidal de diagnóstico tardio associada à síndrome de morning glory, mostrando as alterações na retinografia, tomografia computadorizada e ressonância magnética.

A program for organizing field research data and bibliography on medicinal plants

In the formulation of working hypotheses based on ethnopharmacological information and publications, a rapid access to data is necessary. We present a microcomputer program especially designed for the organization of field data on traditional uses of medicinal plants (data bank 1) and related bibliographic reference (data bank 2). It was developed in Clipper language and turned into an independent executable through compilation, has many help screens (on-line), allows up to 100,000 entries in each data bank, changing and deletion of data, back-up copies, indexed and not indexed searches, and several possibilities of printing or listing data on the screen. Practical routines for the use of the program are presented, handling the existing 300 field work records and 1,000 references.

Apoplexia hipofisária em macro-prolactinomas durante tratamento com bromocriptina oral e injetável: relato de 2 casos / Pituitary apoplexy in macro-prolactinomas during treatment with oral and injected bromocriptine: report of 2 cases

Apoplexia hipofisária é caracterizada clinicamente por cefaiéia súbita, frequentemente acompanhada por vômitos e sinais de irritaçao meníngea, além de alteraçoes de campo visual e oftalmoplegia. Descrevemos 2 casos de pacientes com macroprolactinomas que, durante o tratamento com bromocriptina oral ou injetável, desenvolveram apoplexia. O primeiro caso foi tratado clinicamente e o segundo através de cirurgia transesfenoidal. Ambos apresentaram melhora clínica e tomográfica. A apoplexia hipofisária é uma entidade pouco frequente em macroprolactinomas tratados com bromocriptina. Esta última, apesar de ter sido utilizada nos 2 casos relatados, nao poderia ser responsabilizada como fator causal.

Macroprolactinoma resistente ao CV 205-502 / Macroprolactinoma resistent for the CV 205-502

Prolactinomas resistentes a agonistas dopaminérgicos sao raros. Descrevemos o caso de um paciente de 19 anos, masculino, portador de macroprolactinoma invasivo, nao responsivo tanto à bromocriptina (BCP) oral e injetável, como ao CV 205-502 (Sandoz, Suiça). O CV 205-502 é um novo agonista dopaminérgico D2 seletivo, nao derivado da ergotamina, 35 a 100 vezes mais potente que a BCP. O paciente foi encaminhado após craniotomia onde houve ressecçao parcial do tumor. A prolactina (PRL) pré-operatória era 1O.OOO ng/ml, e a tomografia mostrava adenoma hipofisário grau IV. Foi tratado com BCP oral (até 60 mg/dia) e depois com BCP injetável, permanecendo porém com níveis bastante elevados de PRL. Também nao houve reduçao do tumor. A seguir iniciou CV 205-502 (até O,300 mg/dia), com uma queda máxima dos níveis de PRL de 57 por cento (7.950 ng/ml). Contudo, as ressonâncias magnéticas pré e pós 53 dias da medicaçao mostraram um aumento do tumor. O paciente foi posteriormente submetido a duas cirurgias e encaminhado à radioterapia (RT). Catorze meses após a RT houve uma queda de 82 por cento nos níveis de PRL (de 11.900 para 2.199 ng/ml), e considerável reduçao tumoral. Em conclusao, além da ausência de normalizaçao da PRL, nosso paciente apresentou crescimento do tumor em vigência de agonistas dopaminérgicos, o que é extremamente raro.

Neurilemoma oftálmico / Ocular neurilemmoma

Apresenta-se um caso de neurilemoma orbitário benigno, solitário, operado sem recidiva ou malignizaçäo durante a evoluçäo. Discute-se aspecto clínico e os achados neuroftalmológicos e neurocirúrgicos, assim como o quadro anátomo-patológico desta entidade nosológica

Síndrome da "Morning Glory": quadro clínico sugerindo sua patogenia / Morning glory syndrome: clinical picture suggesting its pathogeny

A provável patogenia da Síndrome da "Morning Glory" é sugerida como sendo decorrente de um defeito no fechamento da fissura embrionária, que secundariamente induziria às alteraçöes principalmente mesodérmicas que danificariam as fibras nervosas. Os autores apresentam cinco casos associados à perda da acuidade visual e ao déficit pupilar aferente e enfatizam a importância da embriogênese e do quadro clínico, no conhecimento dessa anomalia

Utilizaçäo do teste de tempo cíclico pupilar em pacientes da neurooftalmologia / Use of the pupil cycle time test in neurophtalmologic patients

A determinaçäo quantitativa e objetiva da funçäo visual da porçäo anterior é possível com o teste do tempo cíclico pupilar. Para a sua medida é necessário apenas um simples cronômetro e uma lâmpada de fenda com características físicas definidas. Este trabalho apresenta o resultado desse método após a avaliaçäo de algumas doenças neuroftalmológicas näo relatadas na literatura e sugere uma ampla aplicaçäo clínica