Acaricidal efficacy and chemical study of hexane extracts of the leaves of Neoglaziovia variegata (Bromeliaceae) against the tick Rhipicephalus microplus.

The frequent use of acaricides against the tick Rhipicephalus microplus increases the risk of development of resistance. Recent studies have revealed that Neoglaziovia variegata, an indigenous plant species known in Brazil as 'caroá', has a deleterious effect against R. microplus. In the current study, extracts of N. variegata were studied for their possible acaricidal properties. A hexane extract of N. variegata leaves was fractionated in a chromatography column and the fractions were tested in adult tick immersion tests in triplicate using three concentrations (5, 10 and 25 mg/ml). All the fractions had harmful effects on the ticks. However, three fractions were more efficaceous. Phytochemical analysis indicated that stigmast-5-en-3-ol and stigmastanol were most abundant; they might be responsible for the acaricidal effects, making them potentially useful as alternative agents to control the tick R. microplus.

Antinociceptive and anti-inflammatory effects of Costus spicatus in experimental animals.

CONTEXT: Costus spicatus Swartz (Costaceae), commonly called "cana-do-brejo'" in Brazil's northeast, is a medicinal plant found in wet coastal forests. In folk medicine an infusion of the aerial parts is taken to treat inflammation and pain. OBJECTIVE: The methanol extract obtained from the leaves of Costus spicatus (MECs) was evaluated for antinociceptive and anti-inflammatory activities. METHODS: Analgesic and anti-inflammatory activities were studied by measuring nociception through acetic acid, formalin, and hot-plate tests, while inflammation was induced by carrageenan. All experiments were conducted with experimental animals. RESULTS AND DISCUSSION: Following oral administration, MECs (100, 200, and 400 mg/kg) significantly reduced the number of writhes (52.8, 43.1, and 55.3%, respectively) in the writhing test and the number of paw licks during phase 1 (61.9, 54.1, and 92.1%) and phase 2 (62.5, 82.9, and 98.1%, all doses) during the formalin test when compared to the control group animals. The reaction time during the hot-plate test was increased significantly and was dose-dependent, whereas pretreatment with naloxone rigorously reduced the analgesic potential of MECs, which suggested participation of the opioid system in the modulation of pain induced by MECs. Such results were unlikely to be provoked by motor abnormality, as MECs-treated mice did not exhibit any performance alteration during the Rota-rod test. The administration of 200 and 400 mg/ kg (i.p.) of MECs exhibited an anti-inflammatory effect during the carrageenan test, which was based on interference with inflammatory mediator synthesis. CONCLUSION: We conclude that MECs has antinociceptive and anti-inflammatory activities in rodents.

O Ácido (8)17,12E,14-labdatrieno-18-óico (labdano302), diterpeno tipo labdano isolado de Xylopia langsdorffiana St. Hil. & Tul. (Annonaceae) relaxa a traquéia isolada de cobaia / The (8)17,12E,14-labdatrien-18-oic acid (labdane302), labdane-type diterpene isolated from Xylopia langsdorffiana St. Hil. & Tul. (Annonaceae) relaxes the guinea-pig trachea

A espécie Xylopia langsdorffiana St. Hil.. & Tul. é popularmente conhecida como "pimenteira-da-terra" no Sudeste do Brasil. A partir do fracionamento do extrato etanólico, obtido das cascas do caule desta espécie, foi isolado um diterpeno tipo labdano, identificado como sendo o ácido 8(17),12E,14-labdatrieno-18-óico, e que neste trabalho é codificado como labdano302. O labdano302 relaxou o tônus basal dos anéis de traquéia isolada de cobaia com um valor de CE50 de 6,7 ± 0,5 x 10-8 M. O diterpeno labdano302 relaxou de maneira dependente de concentração os anéis pré-contraídos com carbacol (10-6 M), tanto na presença (CE50 = 1,4 ± 0,7 x 10-5 M) como na ausência de epitélio funcional (CE50 = 1,5 ± 0,3 x 10-5 M), bem como anéis pré-contraídos com 18 ou 60 mM de KCl, apresentando valores de CE50 de 2,3 ± 0,4 x 10(7) M e 1,8 ± 0,8 x 10-5 M, respectivamente. Este efeito relaxante, sobre as contrações induzidas por 18 mM de KCl, tanto foi significantemente mais potente quanto mais eficaz quando comparado ao efeito sobre as contrações induzidas por 60 mM de KCl. Assim, labdano302 mostra um efeito relaxante em traquéia isolada de cobaia, tanto em seu tônus basal como sob estímulo contrátil, aparentemente sem a participação dos fatores relaxantes derivados do epitélio, contudo com possível participação dos canais de K+.

Xylopia langsdorfiana St. Hil. & Tul. is popularly known as "pimenteira-da-terra" in Southeast of Brazil. The fractionation of the ethanol extract obtained from the stem-bark of this species yielded a labdane-type diterpene identified as 8(17),12E,14-labdatrien-18-oic acid, referred here as labdane302. In this study, we investigated the effect of labdane302 in guinea-pig trachea. labdane302 relaxed the basal tonus of trachea rings with EC50 value of 6.7 ± 0.5 x 10-8 M. The diterpene labdane302 relaxed the pre-contracted rings by carbachol 10-6 M both in the presence (EC50 = 1.4 ± 0.7 x 10-5 M) and absence of functional epithelium (EC50 = 1.5 ± 0.3 x 10-5 M), as well as pre-contracted by KCl 18 mM or 60 mM, presented EC50 values of 2.3 ± 0.4 x 10-7 M and 1.8 ± 0.8 x 10-5 M, respectively. This relaxant effect, upon contractions induced by KCl 18 mM, was more potent as well as more efficient than the one presented with KCl 60 mM pre-contracted rings. The labdane-type diterpene labdane302 shows the relaxant effect in isolated guinea-pig trachea, pre-contracted or upon basal tonus, apparently without participation of epithelium-derived relaxant factors, but apparently involving activation of K+ channels.

Spasmolytic action of the methanol extract and isojuripidine from Solanum asterophorum Mart. (Solanaceae) leaves in guinea-pig ileum.

Solanum asterophorum Mart. (Solanaceae) is a shrub popularly known as "jurubeba-defogo" in the northeast of Brazil. In the present work, the methanol extract (SA-MeOH, 3750 microg/mL) and isojuripidine (10(-7) - 3 x 10(-4) M), a steroidal alkaloid obtained from S. asterophorum Mart. leaves, inhibited phasic contractions induced by both 1 microM histamine [IC50 = (225.8 +/- 47.4), g/mL and (3.5 +/- 0.8) x 10(-5) M] or 1 microm acetylcholine [IC50 = (112.5 +/- 20.6) microg/mL and (2.3 +/- 0.4) x 10(-5) M] in guinea-pig ileum, respectively. The extract and isojuripidine also relaxed the ileum (SA-MeOH, 1-750 microg/mL, and isojuripidine, 10(-9) - 3 x 10(-4) M) pre-contracted with 1 M histamine [EC50 = (101.1 +/- 17.4) microg/mL and (1.2 +/- 0.3) x 10(-6) M] or 1 microM acetylcholine [EC50 = (136.8 +/- 21.1) microg/mL and (1.9 +/- 0.4) x 10(-6) M] or 40 mm KCl [EC50 = (149.4 +/- 19.5) microg/mL and (1.8 +/- 0.7) x 10(-6) M], respectively, in an equipotent and concentration-dependent manner. This effect is probably due to inhibition of calcium influx through voltage-operated calcium (Ca(v)) channels. To confirm this hypothesis, we evaluated their effect on cumulative CaCl2 curves in depolarizing medium nominally without Ca2+. SA-MeOH (27, 243, 500, and 750 microg/mL) and isojuripidine (3 x 10(-8), 10(-6), 3 x 10(-5), and 3 x 10(-4) M) inhibited the contractions induced by CaCl2, in a concentration-dependent manner. The concentration-response curves to CaCl2, in the presence of SA-MeOH and isojuripidine, were shifted downward in relation to a control curve in a non-parallel manner resulting in reduction of the maximum effect [E(max) = (71.2 +/- 9.2); (57.4 +/- 9.2); (43.8 +/- 3.4); (41.5 +/- 2.4) and (90.6 +/- 4.8); (74.7 +/- 8.7); (66.4 +/- 3.9); (31.3 +/- 4.1)%, respectively]. SA-MeOH and isojuripidine present spasmolytic action in guinea-pig ileum due to a partially blockade of calcium influx through Ca(v) channels.

The use of topical anesthesia in diagnostic hysteroscopy and endometrial biopsy.

OBJECTIVE: To show that intrauterine anesthesia is a reliable method for reducing pain associated with endocavitary procedures. DESIGN: A prospective, randomized, double-blind study. SETTING: The Department of Obstetrics and Gynecology, Tor Vergata University of Rome, Rome, Italy. PATIENTS: Forty-five patients undergoing diagnostic hysteroscopy (n = 27) or hysteroscopy and endometrial biopsy (n = 18). INTERVENTIONS: Five milliliters of 2% mepivacaine or saline solution were injected transcervically into the uterine cavity before performing the procedures. MAIN OUTCOME MEASURES: Evaluation of pain reduction on a visual analogue scale. RESULTS: Pain expectation and pain reported were reduced during and after the procedures. CONCLUSION: Topical anesthesia effectively reduces pain during hysteroscopy and endometrial biopsy.

The use of topical anesthesia in diagnostic hysteroscopy and endometrial biopsy.

STUDY OBJECTIVE: To determine whether the pain and discomfort of routine hysteroscopy with endometrial biopsy to diagnose infertility and endometrial pathology can be minimized by topical application of mepivacaine. DESIGN: Prospective, randomized, double-blind study. SETTING: The Department of Obstetrics and Gynecology at a teaching hospital in Rome, Italy. PATIENTS: Eighteen women undergoing diagnostic hysteroscopy. INTERVENTIONS: Hysteroscopy and endometrial biopsy were performed after transcervical injection of 5 ml 2% mepivacaine or 5 ml saline solution into the uterine cavity. MEASUREMENTS AND MAIN RESULTS: Difficulty introducing the hysteroscope was rated by the operator on a scale of 1 to 3. An observer scored visible signs of each woman's distress using a three-point scale. The patients reported their pain 15, 30, 60, 120 minutes after the procedure on a visual analog scale. Mepivacaine was more effective than placebo according to all measurements. CONCLUSIONS: Topical mepivacaine reduced the pain experienced during and after hysteroscopy and endometrial biopsy.