Chemical constituents of Salacia elliptica (Celastraceae)

The chemical investigation of Salacia elliptica allowed to the isolation of 20 constituents: two polyols, one xanthone, a mixture of long chain hydrocarbons, one carboxylic acid, one polymer, two steroidal compounds, one aromatic ester and eleven pentacyclic triterpenes. These triterpenes include 3β-stearyloxy-oleanane, 3β-stearyloxy-ursane, one seco-friedelane, and eight compounds of the friedelane serie. The chemical structure and the relative configuration of a new triterpene 1,3-dioxo-16α-hydroxyfriedelane (15) were established through ¹H and 13C NMR including 2D experiments (HMBC, HMQC, COSY and NOESY) and herein reported for the first time.

Constituintes químicos e atividade Leishmanicida de Gustavia elliptica (Lecythidaceae)

The phytochemical investigation of the stem bark and leaves of G. elliptica provided a mixture of the norisoprenoids blumenol B and 6-epiblumenol B along with the triterpenes friedelin, as the major constituent, friedelanol, ursa-9(11),12-dien-3-ol, a-amyrin, β-amyrin, morentenol, epifriedelanol, as well as the sesquiterpenes trans-caryophyllene, α-humulene, ethyl hydnocarpate and other fatty acid esters. The identification of the compounds was performed on basis of spectrometric methods such as GC-MS, IR, MS and 1D and 2D NMR. Stem bark extracts showed significant leishmanicidal activity against promastigote forms of Leishmania braziliensis, with the best results for the chloroform extract.

Tratamento de endometriomas ovarianos com implantes subcutâneos de ST-1435 (Elcometrina)

Objetivos: avaliar o efeito do progestínico ST 1435 (elcometrina) sobre a evolução de endometriomas ovarianos. Métodos: implantes subcutâneos contendo 50 mg da medicação foram administrados a 51 portadoras de endometriomas ovarianos, cujos volumes foram documentados por ultra-sonografia endovaginal antes e a cada intervalo de três meses após o início do tratamento. Um novo implante foi inserido ao fim de seis meses sempre que houvesse necessidade de continuação do tratamento. Resultados: na admissão, 74% das pacientes apresentavam dismenorréia, 57% dor pélvica crônica e 31% dispareunia. A intensidade da dor foi considerada incapacitante ou forte por 82% das pacientes. Um total de 924 meses de observação foi registrado durante os quatro anos de duração do estudo. O alívio da dor foi observado desde o primeiro mês de tratamento e, ao final do primeiro trimestre, nenhuma paciente referia dor incapacitante ou forte. O volume dos endometriomas foi reduzido em 86% das pacientes. Em 45% o volume normal do ovário foi restabelecido. Em 41% a redução de volume foi incompleta e em 14% das pacientes não houve redução do volume ovariano. Setenta e sete por cento das pacientes apresentaram amenorréia durante o tratamento. Os efeitos adversos mais comuns foram redução da libido (21%) e peso nos membros inferiores (14%). Um ano após a suspensão do tratamento, 33% das pacientes mantinham-se assintomáticas, ao passo que 28% tiveram recidivas com menos de três meses após a suspensão. Trinta e nove por cento optaram pela continuidade no uso do implante para prolongar a amenorréia. Conclusão: elcometrina é eficiente em provocar a regressão e reabsorção de endometriomas ovarianos sem apresentar alguns dos efeitos colaterais dos outros tratamentos.

Serum dosage of CPK-MB in dogs with ST deviation by chemiluminescence

Abstract: Although frequently in humans, hypoxic and ischemic heart diseases are poorly documented in dogs, with only few reports of acute myocardial infarction (AMI) in this species. Some electrocardiographic findings might suggest myocardium hypoxia/ischemia, like ST segment elevation or depression, but there are no studies showing whether deviations in ST segment are associated to myocardial injury and serum increase of creatine phosphokinase (CPK-MB). In order to investigate possible myocardial cells injury in poor perfusion conditions, 38 dogs were studied, 20 with normal electrocardiogram and 18 with ST segment elevation or depression, recorded in lead II, at a paper speed of 50 mm/sec and N sensibility (1mV=1cm). Serum measurement of creatine phosphokinase isoenzyme MB (CPK-MB) in normal dogs (group 1) determined control values (in ng/mL), which were compared to those obtained from dogs with deviation (group 2), which allowed confirmation or not of myocardial injury. CPK-MB mean values obtained from dogs in groups 1 and 2 were 0.540ng/ml (SD±0.890)ng/mL and 0.440ng/mL (SD±1.106), respectively. At a significance level of 5%, the relation of CPK-MB with age, mass and total creatine phosphokinase (CPK-T) was not significant in groups 1 and 2. CPK-MB showed no difference, at 5% level, between groups 1 and 2. In conclusion, it is possible to use the human chemiluminescent immunometric assay kit in canine species and that hypoxia/ischemia revealed by ST segment deviation does not mean significant myocardium injury.

Caracterização morfológica dos frutos, das sementes e do desenvolvimento das plântulas de Jatropha elliptica Müll. Arg. (Euphorbiaceae)

O objetivo deste trabalho foi descrever a morfologia do fruto, da semente e do desenvolvimento de plântulas de Jatropha elliptica Müll. Arg. Os frutos foram coletados em setembro e outubro de 2003, na Fazenda Experimental da Universidade Federal de Mato Grosso, no Município de Santo Antônio de Leverger. Para a descrição da morfologia dos frutos e das sementes foram utilizados 50 frutos e 50 sementes. Para a caracterização das etapas da germinação foram utilizadas quatro repetições de 20 sementes, colocadas sobre papel mata-borrão, umedecidas com ácido giberélico (400 ppm), em caixas de plástico transparente, mantidas em câmara para germinação, a 30 ºC e fotoperíodo de oito horas, durante 40 dias. O fruto de J. elliptica é seco, tricoca, endocarpo lenhoso e de deiscência explosiva. A semente é ovalada, endospérmica, de envoltório liso e marmoreado, com carúncula presa na parte ventral; o hilo é visível na base e a rafe é bem marcada longitudinalmente. A germinação é epígea e fanerocotiledonar. O tempo médio de germinação é de 13 a 25 dias. Foi possível descrever e ilustrar, de forma distinta, a morfologia do fruto, da semente e da plântula de J. elliptica, que se apresentou bastante homogênea e confiável para a identificação.

Effect of the acupoints ST-36 (Zusanli) and SP-6 (Sanyinjiao) on intestinal myoelectric activity of Wistar rats

Despite its ancient use as a therapeutic tool to treat several ailments, acupuncture still faces the challenge of scrutiny by Western science both in terms of its efficacy and in terms of the characterization of its effects and mechanisms of actions underlying these effects. We investigated under well-controlled and carefully characterized conditions the influence of electrical stimulation of acupuncture points ST-36 (Zusanli) and SP-6 (Sanyinjiao) on the myoelectric activity of the small intestine of 38 adult male Wistar rats. Electrical recordings obtained by means of four electrodes chronically implanted in the small intestine were used to assess the effects of acupuncture (electroacupuncture stimulation set at 2 Hz, intermittent stimulation, 1 V, for 30 min). Immobilization of the animals was associated with a consistent decrease (-8 ± 7%) in the myoelectric activity of the small intestine as measured by means of the root mean square. Conversely, acupuncture was able to significantly increase (overshoot) this activity compared to baseline (+44 ± 7%). In contrast, immobilized animals subjected to sham acupuncture had only modest (nonsignificant) increases in myoelectric activity (+9 ± 6%). Using carefully controlled conditions we confirmed previous noncontrolled studies on the ability of acupuncture to alter intestinal motility. The characterization of the topographic and temporal profiles of the effects observed here represents a basis for future dissection of the physiological and pharmacological systems underlying these effects.

The starch from Solanum lycocarpum St. Hill. fruit is not a hypoglycemic agent

We have investigated the hypoglycemic effect induced by the starch obtained from the unripe fruits of Solanum lycocarpum (Solanaceae). Per os administration of the starch (1000 or 2000 mg/kg, twice daily for 7 days, N = 6) did not change glycemia levels of nondiabetic female Swiss mice weighing 25-30 g. In streptozotocin-induced diabetic mice, similar treatment with the starch did not change the elevated glycemia 3 h after the last dose (diabetic treated with saline = 288 ± 17/309 ± 18; starch 1000 mg/kg = 295 ± 33; starch 2000 mg/kg = 258 ± 37; N = 5). In animals fasted for 15 h, per os administration of glucose (600 mg/kg) significantly increased glycemia 1 h later. Previous (-30 min) treatment of the animals with the starch (1000 or 2000 mg/kg; N = 5) did not change the increase of glycemia. Per os administration of the starch (1000 or 2000 mg kg-1 day-1, twice daily for 7 days) did not induce body weight gain or loss. The chemical analysis of the starch indicated the presence of glycoalkaloids, a finding that represents a reason for concern since many of these substances are generally toxic. In interviews with 56 diabetic patients, 29 medicinal plants were reported as useful in their treatment of diabetes and S. lycocarpum was the sixth most frequently mentioned. All patients interviewed reported that they also used insulin or oral hypoglycemic drugs. The results of the present study do not provide evidence for a hypoglycemic effect associated with the polysaccharide fraction of S. lycocarpum in either normal or hyperglycemic mice. These data demonstrate the need for adequate pharmacological investigation of the natural products widely used in folk medicine.

Noninvasive assessment of endothelial function and ST segment changes during exercise testing in coronary artery disease

Endothelial function (EF) plays an important role in the onset and clinical course of atherosclerosis, although its relationship with the presence and extent of coronary artery disease (CAD) has not been well defined. We evaluated EF and the ST segment response to an exercise test in patients with a broad spectrum of CAD defined by coronary angiography. Sixty-two patients submitted to diagnostic catheterization for the evaluation of chest pain or ischemia in a provocative test were divided into three groups according to the presence and severity of atherosclerotic lesions (AL): group 1: normal coronaries (N = 19); group 2: CAD with AL <70% (N = 17); group 3: CAD with AL ≥70% (N = 26). EF was evaluated by the percentage of flow-mediated dilatation (%FMD) in the brachial artery during reactive hyperemia induced by occlusion of the forearm with a pneumatic cuff for 5 min. Fifty-four patients were subjected to an exercise test. Gender and age were not significantly correlated with %FMD. EF was markedly reduced in both groups with CAD (76.5 and 73.1% vs 31.6% in group 1) and a higher frequency of ischemic alterations in the ST segment (70.8%) was observed in the group with obstructive CAD with AL ≥70% during the exercise test. Endothelial dysfunction was observed in patients with CAD, irrespective of the severity of injury. A significantly higher frequency of ischemic alterations in the ST segment was observed in the group with obstructive CAD. EF and exercise ECG differed among the three groups and may provide complementary information for the assessment of CAD.