Vasorelaxant effects of ellagitannins isolated from Cuphea carthagenensis.

Cuphea carthagenensis (Jacq.) J. F. Macbr. is a popular plant in Brazilian folk medicine owing to its hypotensive and central nervous system depressant effects. This study aimed to validate the hypotensive effect of the plant's aqueous extract (AE) in rats and examine the vascular actions of three hydrolyzable tannins, oenothein B, woodfordin C, and eucalbanin B, isolated from AE. Systolic blood pressure in unanesthetized rats was determined using the non-invasive tail-cuff method. Oral treatment of normotensive rats with 0.5 and 1.0 g/kg/day AE induced a dose-related hypotensive effect after 1 week. In rat aortic rings pre-contracted with noradrenaline, all ellagitannins (20 - 180 µM) induced a concentration-related vasorelaxation. This effect was blocked by either removing the endothelium or pre-incubating with NG-nitro-l-arginine methyl ester (10 µM), an inhibitor of nitric oxide (NO) synthase. In KCl-depolarized rat portal vein preparations, the investigated compounds did not affect significantly the maximal contractile responses and pD2 values of the concentration-response curves to CaCl2. Our results demonstrated the hypotensive effect of C. carthagenensis AE in unanesthetized rats. All isolated ellagitannins induced vasorelaxation in vitro via activating NO synthesis/NO release from endothelial cells, without altering the Ca2+ influx in vascular smooth muscle preparations. Considering the low oral bioavailability of ellagitannins, the determined in vitro actions of these compounds are unlikely to account for the hypotensive effect of AE in vivo. It remains to be determined the role of the bioactive ellagitannin-derived metabolites in the hypotensive effect observed after oral treatment of unanesthetized rats with the plant extract.

Bauhinia Protease Inhibitors Attenuate Gastric Ulcer by Blocking Neutrophil Enzymes.

Proteases play a pivotal role in many signaling pathways; inhibitors of well-established proteases have shown a substantial therapeutic success. This study aimed to examine the in vivo effects of 3 protease inhibitors isolated from Bauhinia species: i) Bauhinia mollis elastase inhibitor, which blocks human neutrophil elastase (Kiapp 2.8 nM) and cathepsin G (Kiapp 1.0 nM) activities; ii) Bauhinia mollis trypsin inhibitor, a trypsin inhibitor (Kiapp 5.0 nM); and iii) Bauhinia bauhinioides cruzipain inhibitor, which inhibits elastase (Kiapp 2.6 nM), cathepsin G (Kiapp 160.0 nM), and the cysteine proteases cathepsin L (Kiapp 0.2 nM). Bauhinia bauhinioides cruzipain inhibitor, Bauhinia mollis elastase inhibitor, and Bauhinia mollis trypsin inhibitor were isolated using acetone and ammonium sulfate fractionations, DEAE-Sephadex, trypsin-Sepharose, and Resource-Q chromatographies. Mice and rats were treated intraperitoneally with 1 dose of inhibitor; gastric mucosal lesions were induced by cold-restraint stress. Oral pretreatment of mice with Bauhinia mollis elastase inhibitor or Bauhinia mollis trypsin inhibitor (1 - 10 mg/kg) did not show anti-ulcer effect, while Bauhinia bauhinioides cruzipain inhibitor (0.1 - 1.0 mg/kg) produced a similar reduction of the index of mucosal damage at all effective doses (30 to 33% < control). In rats at doses lower than those used in mice, Bauhinia mollis elastase inhibitor and Bauhinia bauhinioides cruzipain inhibitor reduced the index of mucosal damage by 66% and 54% of controls, respectively. The results indicate a protective effect against gastric mucosal lesions associated with elastase inhibition but not inhibition of trypsin activities. Moreover, the lack of Bauhinia mollis elastase inhibitor efficacy observed in mice may possibly be related to the reported structural differences of elastase in mice and rats.

Altered release and uptake of gamma-aminobutyric acid in the cerebellum of dystrophin-deficient mice.

Dystrophin deficiency caused by mutations of the related gene leads to muscle wasting in Duchenne muscular dystrophy (DMD). Some patients with DMD also present with intellectual disability and various degrees of neurological disorders, which have been related to a decreased number of postsynaptic gamma-aminobutyric acid type A receptors (GABAARs) in the hippocampus (HPC) and cerebellum (CBL). The aim of this study was to examine the relevance of dystrophin in the presynaptic GABAergic function in brain regions in which this protein is normally abundant. [3H]-GABA release, induced by nicotinic receptor (nAChR) activation or K+ depolarization, and [3H]-GABA uptake were determined using synaptosomes extracted from the cortex (CTX), HPC, and CBL of littermate control and mdx mice. Superfusion of the synaptosomes with nicotine or high K+ solutions led to a concentration-dependent and Ca2+-dependent [3H]-GABA release in control and mdx synaptosomes. [3H]-GABA release induced by 10 µM nicotine in mdx CBL synaptosomes was 47% less than that in control mice. K+-induced [3H]-GABA release did not differ between control and mdx synaptosomes. α7-containing and ß2-containing nAChRs were involved in nicotine-induced [3H]-GABA release in control and mdx synaptosomes. Kinetic analysis of [3H]-GABA uptake in mdx CBL synaptosomes showed a reduced (50%) half-maximal uptake time (t1/2) and increased (44%) rate of [3H]-GABA uptake (Vmax) compared to controls. The apparent transporter affinity (Km) for GABA was not altered. Our findings show that dystrophin deficiency in mdx mice is associated with significant changes in the release and uptake of GABA in the CBL. These presynaptic alterations may be related to the reported decrease in postsynaptic GABAAR in the same brain region. The results indicate possible dysfunction of GABAergic synapses associated with dystrophin deficiency in the CBL, which may contribute to the cognitive and neurobehavioral disorders in mdx mice and patients with DMD.

Effects of the butanol-containing fraction from leaves of Calea prunifolia H.B.K. on blood pressure and smooth muscle responses of Wistar rats / Efecto de la fracción butanólica de las hojas de Calea prunifolia H.B.K. sobre la presión arterial y la relajación muscular en ratas wistar

The butanol-containing fraction from leaves of Calea prunifolia H.B.K. was obtained in order to examine cardiovascular effects on two distinct rat preparations. The responses elicited in isolated aorta and isolated vas deferens, were examined, as were the changes in blood pressure in anesthetized and conscious Wistar rats. In addition, the effects on angiotensin-converting enzyme activity in plasma and the effects on cytosolic calcium in cardiomyocytes and uterine cells were measured. Results show that the butanol-containing fraction from C. prunifolia (0.1-100 µg/mL) relaxes phenylephrine-induced contractions in isolated aorta (CI50: 58 µg/mL), decreases the contractile response induced by noradrenaline in vas deferens, and shows a competitive antagonism profile (pA2: 4.48, m: 1024). The butanol-containing fraction from C. prunifolia also decreases blood pressure in anesthetized rats in a dose-dependent manner (1-100 mg/kg, i.v.), yet is devoid of hypotensive effects in normotensive, conscious rats. In addition, C. prunifolia does not modify the hypertensive effects induced by the nitric oxide synthase inhibitor L-NAME, and it also does not affect the angiotensin-converting enzyme plasma activity nor the cytosolic calcium in cardiomyocytes and uterine cells. According to these results, C. prunifolia relaxes smooth muscle and vascular tone, favoring the decrease in blood pressure in rats via mechanisms related to alpha adrenergic inhibition.

Se evaluó el efecto cardiovascular en ratas inducido por la fracción butanólica de las hojas de Calea prunifolia H.B.K., examinando el efecto generado en preparaciones de anillos aislados de aorta y conducto deferente, y los cambios de presión arterial en ratas wistar anestesiadas y despiertas. También se cuantificó el efecto sobre la enzima convertidora de angiotensina (ECA) en plasma y sobre el calcio citosólico en cardiomiocitos y uteromiocitos. Los resultados mostraron que la fracción butanólica de C. prunifolia (0,1-100 µg/mL) relajaba anillos de aorta contraídos con fenilefrina (CI50: 58 µg/mL) y disminuía la contracción del conducto deferente inducido por noradrenalina con un perfil de inhibición competitiva (pA2: 4.48, m: 1.024). La fracción butanólica de C. prunifolia disminuye la presión sanguínea en ratas anestesiadas en función de la dosis (1-100 mg/kg, i.v.), si bien estuvo desprovista de efectos hipotensores en ratas despiertas. C. prunifolia tampoco modificó el efecto hipertensor inducido por el inhibidor de óxido nítrico sintetasa L-NAME, ni los niveles de ECA, ni la concentración de calcio citosólico en cardio y uteromiocitos. De acuerdo con estos resultados, C. prunifolia relaja el músculo liso y disminuye el tono vascular favoreciendo la disminución de la presión arterial en ratas por medio de mecanismos vinculados con la inhibición alfa adrenérgica.

A comparative study of two clerodane diterpenes from Baccharis trimera (Less.) DC. on the influx and mobilization of intracellular calcium in rat cardiomyocytes.

Baccharis trimera (Less.) D.C. (Asteraceae) is a medicinal species native to South America and used in Brazilian folk medicine to treat gastrointestinal and liver diseases, kidney disorders and diabetes. The aqueous extract (AE) of the aerial parts of this species presented two mainly constituents: the ent-clerodane diterpene (Fig. 1) and the neo-clerodane diterpene (Fig. 2). The objective of this work was to study their activities on the blockade of Ca(2+)-induced contractions in KCL-depolarized rat portal vein preparations, and on the influx and mobilization of cytosolic calcium in rat cardiomyocytes by fluorescence measurements. The results showed that both the neo- and the ent-clerodane diterpenes reduced the maximal contractions induced by CaCl2, in KCl depolarized rat portal vein preparations, without modifying the EC50. The data on the concentration of cytosolic calcium ([Ca(2+)]c) showed that, while the neo-clerodane diterpene stimulates the mobilization of [Ca(2+)]c in rat cardiomyocytes, this effect was not observed with the ent-clerodane diterpene. On the other hand, the influx of calcium was not altered by the neo-clerodane diterpene, but was reduced in the presence of the ent-clerodane diterpene, indicating that this compound induces a blockade of the voltage-dependent calcium channels.

Quantitative changes of nicotinic receptors in the hippocampus of dystrophin-deficient mice.

Lack of dystrophin in Duchenne muscle dystrophy (DMD) and in the mutant mdx mouse results in progressive muscle degeneration, structural changes at the neuromuscular junction, and destabilization of the nicotinic acetylcholine receptors (nAChRs). One-third of DMD patients also present non-progressive cognitive impairments. Considering the role of the cholinergic system in cognitive functions, the number of nAChR binding sites and the mRNA levels of α4, ß2, and α7 subunits were determined in brain regions normally enriched in dystrophin (cortex, hippocampus and cerebellum) of mdx mice using specific ligands and reverse-transcription polymerase chain reaction assays, respectively. Membrane preparations of these brain regions were obtained from male control and mdx mice at 4 and 12 months of age. The number of [³H]-cytisine (α4ß2) and [¹²5I]-α-bungarotoxin ([¹²5I]-αBGT, α7) binding sites in the cortex and cerebellum was not altered with age or among age-matched control and mdx mice. A significant reduction in [³H]-cytisine (48%) and [¹²5I]-αBGT (37%) binding sites was detected in the hippocampus of mdx mice at 12 months of age. When compared with the age-matched control groups, the mdx mice did not have significantly altered [³H]-cytisine binding in the hippocampus, but [¹²5I]-αBGT binding in the same brain region was 52% higher at 4 months and 20% lower at 12 months. mRNA transcripts for the nAChR α4, ß2, and α7 subunits were not significantly altered in the same brain regions of all animal groups. These results suggest a potential alteration of the nicotinic cholinergic function in the hippocampus of dystrophin-deficient mice, which might contribute to the impairments in cognitive functions, such as learning and memory, that have been reported in the dystrophic murine model and DMD patients.

Natural compounds endowed with cholinergic or anticholinergic activity. Enhancement of acetylcholine release by a quaternary derivative of L-hyoscyamine.

New compounds that target nicotinic receptors (nAChRs) have been sought to correct disorders affecting cholinergic transmission in central and peripheral synapses. A quaternary derivate of l-hyoscyamine, phenthonium (Phen), was shown by our group to enhance the spontaneous acetylcholine (ACh) release without altering the nerve-induced transmitter release at the neuromuscular junction. The effect was unrelated to membrane depolarization, and was not induced by an increase of calcium influx into the nerve terminal. Phen also presented a competitive antimuscarinic activity and blocked noncompetitively the neuromuscular transmission. In this work we re-examined the mechanisms underlying the facilitatory actions of Phen on [(3)H]-ACh release in isolated ganglia of the guinea pig ileal myenteric plexus. Exposure of the preparations to Phen (10-50 microM) increased the release of [(3)H]-ACh by 81 to 68% over the basal. The effect was not affected by the ganglionic nAChR antagonist hexamethonium (1 nM) at a concentration that inhibited the increase of [(3)H]-ACh release induced by the nicotinic agonist dimethylphenylpiperazinium (DMPP, 30 microM). Association of Phen (10 microM) with DMPP potentiated the facilitatory effect of Phen. [(3)H]-ACh release was not altered by the muscarinic antagonists atropine (1 nM) or pirenzepine (1 microM). However, both antagonists inhibited the release of [(3)H]-ACh induced by either the muscarinic M1 agonist McN-343 (10 microM) or Phen (20 microM). The facilitatory effect of Phen was not altered by CdCl(2) (50 mM), but it was potentiated in the presence of tetraethylammonium (40 mM). The results indicate that the facilitatory action of Phen appears to be mediated by an increase of the inwardly rectifying potassium channels conductance probably related to the compound antimuscarinic activity.

In vivo inhibition of gastric acid secretion by the aqueous extract of Scoparia dulcis L. in rodents.

The freeze-dried aqueous extract (AE) from the aerial parts of Scoparia dulcis was tested for its effects on experimental gastric hypersecretion and ulcer in rodents. Administration of AE to animals with 4h pylorus ligature potently reduced the gastric secretion with ED(50)s of 195 mg/kg (rats) and 306 mg/kg (mice). The AE also inhibited the histamine- or bethanechol-stimulated gastric secretion in pylorus-ligated mice with similar potency suggesting inhibition of the proton pump. Bio-guided purification of the AE yielded a flavonoid-rich fraction (BuF), with a specific activity 4-8 times higher than the AE in the pylorus ligature model. BuF also inhibited the hydrolysis of ATP by H(+),K(+)-ATPase with an IC(50) of 500 microg/ml, indicating that the inhibition of gastric acid secretion of Scoparia dulcis is related to the inhibition of the proton pump. Furthermore, the AE inhibited the establishment of acute gastric lesions induced in rats by indomethacin (ED(50)=313 mg/kg, p.o.) and ethanol (ED(50)=490 mg/kg, p.o.). No influence of the AE on gastrointestinal transit allowed discarding a possible CNS or a cholinergic interaction in the inhibition of gastric secretion by the AE. Collectively, the present data pharmacologically validates the popular use of Scoparia dulcis in gastric disturbances.

Calcium handling in a testosterone responsive skeletal muscle of the MDX mouse

Muscle necrosis in Duchenne muscle dystrophy (DMD) and in the mdx mouse has been related to abnormal calcium homeostasis associated with the lack of dystrophin. We have previously shown that the testosterone-dependent levator ani (LA) muscle of the mdx mouse develops a mild muscle wasting and fiber degeneration compared to the less hormone sensitive diaphragm (DIA) muscle, suggesting a protective effect of androgens. This study assessed the calcium handling mechanisms and cytosolic calcium concentration ([Ca2+]i) in LA muscles of mdx mice at critical stages of muscle disease. Muscle contractures induced by caffeine and 4-chloro-m-cresol (4-CmC), two activators of ryanodine channels, were recorded in LA and DIA muscles of prepubertal (1 month-old), adult (4 month-old) and aged (18 month-old) wild-type (wt) and mdx mice. [Ca2+]i was estimated with the fura-2 fluorescent dye in enzymatically dissociated LA muscle fibers of the same wt and mdx groups. Tetanus tension (TT) in the LA increased proportionately to the muscle weight (4 to 5-fold), but specific TT (TT/mg) did not differ among age-matched wt and mdx groups. Muscle contractures induced by caffeine (3-100 mM) or 4-CmC (0.1-5.0 mM) in the LA were greater in prepubertal than in adult and aged mice, but they did not differ among age-matched wt and mdx groups. The resting [Ca2+]i in mdx LA muscle fibers was not significantly affected at any age. Comparatively, dystrophic DIA presented reduced muscle strength in adult (40%) and aged (45%) mice, whereas the muscle responses to caffeine increased with age (63 to 82%), indicating changes in the Ca2+ handling mechanisms. The results indicated that muscle strength and calcium homeostasis in dystrophic LA muscle fibers were not significantly altered, confirming previous evidence of androgens’ beneficial effects on hormone-sensitive skeletal muscles.

Assessing the therapeutic use of Lafoensia pacari St. Hil. extract (mangava-brava) in the eradication of Helicobacter pylori: double-blind randomized clinical trial.

BACKGROUND: The eradication of Helicobacter pylori is easily achieved by combining antisecretory agents and antibiotics; however, the cost of these associations is very high for the population of Third World countries, where the prevalence of the infection is even higher and leads to markedly reduced treatment effectiveness. We tested a plant (Lafoensia pacari) that is used in the central region of Brazil. According to previous studies, this plant has high concentrations of ellagic acid, which presents gastric antisecretory and antibacterial actions. MATERIAL AND METHODS: One hundred dyspeptic, urease-positive patients were randomized to receive 500 mg of methanolic extract of L. pacari (n = 55) or placebo (n = 45), for 14 days, in a double-blind clinical trial. The main variables assessed were the eradication of H. pylori 8 weeks after the intervention and complete symptom relief at the end of the treatment. RESULTS: The examinations (urease and histology) showed persistence of H. pylori in 100% of participants. Complete symptom relief was experienced by 42.5% of patients (95% CI: 29.4-55.8) in the intervention group and by 21% (95% CI: 8.8-33.1) in the control group, p = .020. The side-effects were minimal and similar in both groups. CONCLUSIONS: The extract of L. pacari as a single agent was not effective to eradicate H. pylori. However, it was well tolerated and many participants reported relief of symptoms. Future studies may test the agent using larger doses and longer periods, in monotherapy or in combination with antibiotics.

Mild dystrophic damage in the androgen-sensitive levator ani muscle of the mdx mouse.

The time course of muscular dystrophy on the androgen-sensitive levator ani muscle was compared to that of the diaphragm of dystrophic (mdx) mice aged 1-20 months. Muscle growth, isometric contractile properties and caffeine-induced contractures were determined to assess the hormone myotrophic effect, muscle strength and sarcoplasmic reticulum function, respectively, of both control and dystrophic muscles. Histological analysis of mdx muscles showed variable fiber size, centronucleated cells, infiltration of connective tissue, and necrosis which was less severe in the levator ani than in the diaphragm muscle. Tetanic tension per unit weight in the mdx levator ani was reduced (29%) after aging, while the contraction time remained unchanged. The tetanic tension of the mdx diaphragm muscle decreased with age from 3 to 20 months (20-64%), and the relaxation time was prolonged after aging (22%). Gonadectomy of young adult mdx mice caused atrophy of the levator ani muscle, accelerated muscle wasting, reduced the tetanic force (31%), but it did not affect the contraction time and caffeine responses. The results showed that testosterone does not prevent the progress of muscle disease in the mdx levator ani, but androgen withdrawal accelerates muscle wasting suggesting a normonal beneficial effect.

Kininogenase activity of Thalassophryne nattereri fish venom.

Accidents caused by the venomous fish Thalassophryne nattereri are characterized by edema, intense pain and necrosis at the site of the sting. This study assessed the nociceptive and edematogenic activities of T. nattereri venom after injection into the mouse hindpaw and determination of the paw licking duration and weight. Subplantar injections of the venom (0.1-6 microg) induced a dose-related increase of the paw licking time and paw swelling with maximal values at 3 microg (209.5 +/- 57.5 s and 135.0 +/- 6.8 mg, respectively). Pretreatment of mice with either indomethacin (10 mg/kg, i.p.), a cyclooxygenase inhibitor, dexamethasone (1 mg/kg, s.c.), a steroid anti-inflammatory agent, cyproheptadine (1 mg/kg, i.p.), antagonist of serotonin receptors or L-NAME (100 mg/kg, s.c.), inhibitor of nitric oxide syntase, did not affect the venom-induced nociceptive and edematogenic responses. Injection of the opioid analgesic fentanyl (0.1 mg/kg, s.c.) reduced the paw licking time induced by 1 microg venom by 84% of control, without affecting the paw swelling. Both nociceptive and edematogenic responses were reduced after treatment with a specific tissue kallikrein inhibitor (TKI, 100 mg/kg, i.p.) by 78% and 24% from control values, respectively. Administration of a specific plasma kallikrein inhibitor (PKSI(527,) 100 mg/kg, s.c.) did not affect the venom-induced nociceptive response, but it decreased the paw edema by 15% from control. After injection of the angiotensin-converting enzyme inhibitor captopril (100 mg/kg, i.p.) the venom-induced nociceptive end edematogenic responses were increased by two-fold. The role of kallikreins possibly present in the venom was further assessed by hydrolysis of human kininogen and kininogen-derived synthetic peptides, showing the release of kallidin (Lys-bradykinin). The hydrolysis was inhibited by metal chelating agents but not by serino-, aspartyl- or cysteino-proteinase inhibitors. The data suggest that a protease with tissue-kallikrein-like activity plays a major role in nociception and edema induced by T. nattereri venom and this should be considered to achieve efficient treatments for human accidents with this venom.

Antinociceptive and antiinflammatory activities of the aqueous extract and isolated Cuphea carthagenensis (Jacq.) J. F. Macbr.

The aqueous extract (AE) and isolated fraction (ppt-3) of Cuphea carthagenensis (Jacq.) J. F. Macbr (sete-sangrias) were tested using models of nociception and inflammation in mice. Oral administration (p.o.) of the AE (10 to 100 mg/kg) and fraction ppt-3 (0.1 to 10 mg/kg) reduced the acetic acid-induced writhing in mice by 40 to 50 percent and by 46 to 70 percent of control, respectively. At the same doses AE and ppt-3 did not affect the tail flick response. Fraction ppt-3 also reduced the carrageenininduced paw edema, but at a dose 1000 times higher than that inducing antinociception. The results indicated the presence in the plant of antinociceptive constituents devoid of antiinflammatory activity, with actions apparently mediated by non-opioid mechanisms.

Actividad antioxidante y ácidos fenólicos del alga marina Bryothamnion triquetrum (S G Gmelim) Howe / Antioxidant activity related to phenolic acids in the aqueous extract of the marine seaweed Bryothamnin triquetrum (S G Gmelim) Howe

El estrés oxidativo esta asociado con diferentes patologías de altas incidencias en el hombre, entonces la busqueda de antioxidantes naturales reviste una extraordinaria importancia. El objetivo del presente trabajo fue demostrar la actividad antioxidante del alga marina Bryothamnion triquetrum y los posibles compuestos que pudieran explicar esta actividad. El extracto acuoso de esta alga contiene 8.08 mg de polifenoles totales/g de extracto liofilizado y una concentración inhibitoria media ('CI IND.50') de la lipoperoxidación espontanea de 23.3µg. Se realizo un fraccionamiento con extracciones liquido-liquido, TLC'GAMA' columna de Amberlite XAD-2, monitoreado por TLC'GAMA' actividad antioxidante...

Actividad anti-inflamatoria de Urera baccifera (Urticaceae) en ratas Sprague-Dawley / Anti-inflammatory activity of Urera baccifera (Urticacceae) in Sprague-Dawley rats

On a preliminary test, anti-inflammatory and analgesic dose-related activities on rats were observed for the aqueous fraction of Urera baccifera; this extract was biossay-guided fractionated and the final aqueous fraction was used according the ethnobotanical use. Carrageenan-induced edema (n=6), was used as an assay in the fractionating process. The anti-inflammatory and antinociceptive properties of the final aqueos fraction were studied using in vivo models. For the anti-inflammatory activity rat paw edema (n=6), pleurisy induced by carrageenan (n=6) and ear edema induced by topical croton oil (n=6) models were used, and tail-flick test (n=6), abdominal constrictions induced by acetic acid (n=6), and formalin test (n=6), were used for the antinociceptive activity. The test performed showed an inhibition effect on leukocyte migration, and a reduction on pleural exudate, as well as dose-dependant peripheral analgesic activity, at a range of 25-100 mg/kg i.p. The final aqueous fraction contains most of the anti-inflammatory activity of the plant U. baccifera. A possible mechanism of action is discussed and based on the results we conclude that this plant has a potencial for both anti-inflammatory and analgesic activity at the clinical level. Key words: Urera baccifera, anti-inflammatory agent, analgesic, antinociceptive, rat paw edema, Urticaceae

Efeitos do tratamento cronico de ratos com o extrato de Chamaecrista nictans Irwin and Barneby na eliminacao de calculos renais / Effects of chronic treatment of rats with Chamaecrista nictans Irwin and barneby on eliminition of renal calculli

Chamaecrista nictans subs. patellaria var. ramosa Irwin and Barneby (Cassia patellaria DC), tambem conhecida pelo nome popular de peninha, e uma erva daninha originaria do Brasil cujo cha e utilizado na medicina popular para eliminacao de calculos renais. O ensaio farmacologico foi feito a fim de testar o efeito do tratamento cronico com extrato fluido da planta, na urolitiase experimental em ratos atraves da inducao de calculo vesical. Os resultados indicam que o extrato fluido da peninha nao apresentou atividade antilitiasica no modelo experimental testado

Efeitos da ofloxacina no granuloma de corpo estranho induzido por fio de sutura (prolene), em ratos / Effects of ofloxacin in foreign body granuloma induced by surgical stitches (prolene)

Todo fio de sutura no organismo induz à formaçao de granuloma de corpo estranho, no qual os macrófagos predominam. Em cirurgia, a ofloxacina é freqüentemente ministrada em hospedeiro que recebeu sutura cirúrgica. Foi demonstrado in vitro que a ofloxacina inibe a topoisomerase II, que é a contraparte eucariótica da d-girase bacteriana (procariótica), a qual, por sua vez, é o alvo da atuaçao antiproliferativa da ofloxacina sobre as bactérias. Nesta pesquisa se investigou em ratos a influência da ofloxacina nos macrófagos de granuloma de corpo estranho por fios de sutura (Prolene). Os macrófagos foram contados no grupo 3 (tratado com 30 mg / Kg de ofloxacina) e no grupo 4 (90 mg / Kg), sendo comparados com o grupo 1 (nao tratado com drogas). O grupo 2 recebeu indometacina - reconhecidamente antiproliferativa para células inflamatórias - e evidenciou diminuiçao dos macrógafos. O grupo 4 (mas nao o grupo 3) teve número de macrófagos menor que o grupo 1. Concluiu-se que a ofloxacina em altas doses é antiproliferativa para macrófagos murinos in vivo.