Angelo R. Antoniolli

Anti-inflammatory, analgesic activity and acute toxicity of Sida cordifolia L. (Malva-branca).

Sida cordifolia L. (Malvaceae) is used in folk medicine for the treatment of inflammation of the oral mucosa, blenorrhea, asthmatic bronchitis and nasal congestion. The anti-inflammatory, analgesic effects and acute toxicity of an aqueous extract of S. cordifolia were evaluated in animal models. The extract was prepared using leaves collected before the flowering period. The aqueous extract (AE) showed a significant inhibition of carrageenin-induced rat paw edema at a dose of 400 mg/kg administered orally, but did not block the edema induced by arachidonic acid. The AE also increased the latency period for mice in the hot plate test, and inhibited the number of writhes produced by acetic acid at the oral dose of 400 mg/kg. The aqueous extract of S. cordifolia showed low acute toxicity in mice.

Bioassay‐guided Evaluation of Antioxidant and Antinociceptive Activities of Carvacrol

We examined the antioxidant properties in vitro and the antinociceptive effect of carvacrol (CARV) in several models of pain in mice. CARV presented a strong antioxidant potential according to the TRAP/TAR evaluation; it also presented scavenger activity against nitric oxide and prevented lipid peroxidation in vitro. In mice, when evaluated against acetic acid-induced abdominal writhing, CARV (25, 50 and 100 mg/kg, i.p.) reduced (p < 0.001) the number of writhing compared to the control group, without opioid participation. In the formalin test, CARV also significantly inhibited both the early (neurogenic pain) and the late (inflammatory pain) phases of formalin-induced licking, with inhibition percentage values of 56.8% (100 mg/kg) for the neurogenic phase and 41.2% (25 mg/kg), 73.8% (50 mg/kg) and 99.7% (100 mg/kg) for the inflammatory phase. CARV also produced a significant inhibition of the pain caused by capsaicin (63.1, 67.1 and 95.8%, p < 0.001) and glutamate (46.4, 61.4 and 97.9%, p < 0.01). When assessed in a thermal model of pain, CARV (100 mg/kg, i.p.) caused a significant increase (p < 0.05) in the latency response on the hot-plate test. Such results were unlikely to be provoked by motor abnormality. Together, these results indicate that the properties of CARV should be more thoroughly examined in order to achieve newer tools for management and/or treatment of painful conditions, including those related to pro-oxidant states.

In vitro antioxidant potential of medicinal plant extracts and their activities against oral bacteria based on Brazilian folk medicine

BACKGROUND AND OBJECTIVES This study aims to determine antibacterial activities of Cocos nucifera (husk fiber), Ziziphus joazeiro (inner bark), Caesalpinia pyramidalis (leaves), aqueous extracts and Aristolochia cymbifera (rhizomes) alcoholic extract against Prevotella intermedia, Porphyromonas gingivalis, Fusobacterium nucleatum, Streptococcus mutans and Lactobacillus casei. The antioxidant activity and acute toxicity of these extracts were also evaluated. MATERIAL AND METHODS The plant extracts antibacterial activity was evaluated in vitro and the minimal inhibitory concentration (MIC) was determined by the broth micro-dilution assay. The bacterial killing kinetic was also evaluated for all extracts. In addition, the antibacterial effect of the extracts was tested in vitro on artificial oral biofilms. The acute toxicity of each extract was determined in according to Lorke [Lorke D. A new approach to practical acute toxicity testing. Arch Toxicol 1983;54:275-87] and the antioxidant activity was evaluated by DPPH photometric assay [Mensor LL, Menezes FS, Leitão GG, Reis AS, Santos TC, Coube CS, et al. Screening of Brazilian plants extract for antioxidant activity by the use of DPPH free radical method. Phytother Res 2001;15:127-30]. RESULTS MIC and the bactericidal concentrations were identical, for each evaluated extract. However, microbes of artificial biofilms were less sensitive to the extracts than the planktonic strains. A. cymbifera extract induced the highest bactericidal effect against all tested bacteria, followed by C. nucifera, Z. joazeiro and C. pyramidalis extracts, respectively. All extracts showed good antioxidant potential, being C. nucifera and C. pyramidalis aqueous extracts the most active ones. CONCLUSION In conclusion, all oral bacteria tested (planktonic or in artificial biofilms) were more susceptible to, and rapidly killed in presence of A. cymbifera, C. pyramidalis and C. nucifera than Z. joazeiro extracts, respectively. Thus, these extracts may be of great interest for future studies about treatment of oral diseases, considering their potent antioxidant activity and low toxicity.

Evaluation of the analgesic and anti-inflammatory effects of the essential oil of Lippia gracilis leaves.

AIM OF THE STUDY The aim of the present study is to investigate the antinociceptive, anti-inflammatory, and antioxidant activities of essential oil (EO) of Lippia gracilis Schauer (Verbenaceae) leaves to support the medicinal uses claimed by folklore practitioners in the caatinga region (semi-arid) of Northeastern Brazil. MATERIALS AND METHODS The chemical composition and antinociceptive and anti-inflammatory activities of the EO of Lippia gracilis leaves (50-200 mg/kg) were investigated. Antinociceptive activity of the EO was evaluated by writhing test. Anti-inflammatory activity of the EO was evaluated using paw oedema and peritonitis methods. RESULTS Oral treatment with the EO of Lippia gracilis leaves elicited inhibitory activity on acetic acid effect at 50, 100, and 200 mg/kg (30.33+/-2.36, 25.20+/-1.48, and 21.00+/-1.54 abdominal writhes, respectively, P<0.05), as compared with the control group (36.73+/-1.92 writhes). The compound acetylsalicylic acid (ASA, 300 mg/kg) inhibited the acetic acid-induced writhing (12.67+/-0.50 abdominal writhes, P<0.001). Carrageenan-induced oedema formation was reduced with the EO of Lippia gracilis leaves at 200 mg/kg (0.72+/-0.06 mL h, P<0.001) and by the reference compound ASA (300 mg/kg, 0.85+/-0.04 mL h, P<0.001), as compared with the control group (1.76+/-0.06 mL h). Leukocyte migration into the peritoneal cavity induced by carrageenan was reduced with the EO of Lippia gracilis leaves at 50, 100, and 200 mg/kg (13.81+/-0.61, 11.77+/-0.91, and 10.30+/-0.60 leukocytes x 10(6)/mL, respectively, P<0.01), and by the compound dexamethasone (2 mg/kg, 5.34+/-0.33 leukocytes x 10(6)/mL, P<0.001), as compared with the control group (16.71+/-0.54 leukocytes x 10(6)/mL). The analyses of the essential oil allowed the identification of Lippia gracilis as a thymol-p-cymene chemotype (32.68% and 17.82%, respectively). CONCLUSIONS The EO of Lippia gracilis leaves shows antinociceptive and anti-inflammatory activities.

Hypotensive and Vasorelaxant Effects of Citronellol, a Monoterpene Alcohol, in Rats

Citronellol is an essential oil constituent from the medicinal plants Cymbopogon citratus, Cymbopogon winterianus and Lippia alba which are thought to possess antihypertensive properties. Citronellol-induced cardiovascular effects were evaluated in this study. In rats, citronellol (1-20 mg/kg, i.v.) induced hypotension, which was not affected by pre-treatment with atropine, hexamethonium, N(omega)-nitro-L-arginine methyl ester hydrochloride or indomethacin, and tachycardia, which was only attenuated by pre-treatment with atropine and hexamethonium. These responses were less than those obtained for nifedipine, a reference drug. In intact rings of rat mesenteric artery pre-contracted with 10 microM phenylephrine, citronellol induced relaxations (pD(2) = 0.71 +/- 0.11; E(max) = 102 +/- 5%; n = 6) that were not affected by endothelium removal, after tetraethylamonium in rings without endothelium pre-contracted with KCl 80 mM. Citronellol strongly antagonized (maximal inhibition = 97 +/- 4%; n = 6) the contractions induced by CaCl(2) (10(-6) to 3 x 10(-3 )M) and did not induce additional effects on the maximal response of nifedipine (10 microM). Finally, citronellol inhibited the contractions induced by 10 microM phenylephrine or 20 mM caffeine. The present results suggest that citronellol lowers blood pressure by a direct effect on the vascular smooth muscle leading to vasodilation.

Antinociceptive and anti-inflammatory activities of Bowdichia virgilioides (sucupira).

ETHNOPHARMACOLOGICAL RELEVANCE Bowdichia virgilioides Kunth (Leguminosae Papilonoideae) is a plant with anti-inflammatory activity used in folk medicine. The importance of this plant promoted its inclusion in Brazilian Pharmacopoeia. AIM OF THE STUDY In order to evaluate the actions of this plant, studies were performed on antinociceptive and anti-inflammatory activities. MATERIALS AND METHODS The aqueous extracts (AE) of Bowdichia virgilioides inner bark and leaves were used at 100, 200, and 400mg/kg. Antinociceptive activity of plant extract was evaluated by writhing, hot-plate and formalin tests. Anti-inflammatory activity was evaluated using paw oedema and peritonitis methods. RESULTS Oral treatment with the AE of inner bark or leaves elicited inhibitory activity (P<0.01) on acetic acid effect at 200 and 400mg/kg, and reduced the formalin effect at the second-phase (200 and 400mg/kg, P<0.01), however it did not elicit any inhibitory effect on hot-plate test. The indomethacin inhibited the acetic acid-induced writhing and the formalin effect at the second-phase (P<0.001), and the morphine reduced the both phases of formalin test (P<0.001). Carrageenan-induced oedema formation and neutrophil migration into the peritoneal cavity were reduced with the AE of inner bark or leaves at 100, 200, and 400mg/kg (P<0.05), and by the reference compounds aspirin (P<0.001) and dexamethasone (P<0.001), respectively. CONCLUSIONS The AE of Bowdichia virgilioides shows antinociceptive and anti-inflammatory activities, supporting the folkloric usage of the plant to treat various inflammatory diseases.

Plantas medicinais usadas nos distúrbios do trato gastrintestinal no povoado Colônia Treze, Lagarto, SE, Brasil

Models of socioeconomic development adopted by human societies reflect different ways of relating to Nature, which, given the present paradigm, have evolved towards great natural-resource loss. Within the sphere of this relationship, both the conservation and preservation of medicinal-plant biodiversity are fundamental because of the importance of medicinal plants as genetic potential for the development of new drugs, and as the primary access to health care for many communities. Using an ethnopharmacological approach in the study of medicinal plants, this work aimed to study the medicinal plants popularly used for gastro-intestinal tract ailments, at Colonia Treze village, in Lagarto/Sergipe, since this community is culturally attuned to the use of medicinal plants. Methodology consisted of field work within the community, adopting the ethnographic Rapid Assessment Procedure. The sample was composed of community leaders, plant users and practitioners of folk medicine. Based on their indications of medicinal-plant use, eight plants were selected and subject to pharmacological experimental tests. Plants tested by the Intestinal Transit Model did not provoke alterations in motility. However, those that underwent the Acute Gastric Lesion Induction Model proved to be effective in anti-ulcerogenic activity. Based on these results, strategies for local development at the community level are proposed, which will tie the conservation of medicinal flora to improvements in life quality.

Sida cordifolia Leaf Extract Reduces the Orofacial Nociceptive Response in Mice

In this study, we describe the antinociceptive activity of the ethanol extract (EE), chloroform (CF) and methanol (MF) fractions obtained from Sida cordifolia, popularly known in Brazil as “malva branca” or “malva branca sedosa”. Leaves of S. cordifolia were used to produce the crude ethanol extract and after CF and MF. Experiments were conducted on Swiss mice using the glutamate and formalin‐induced orofacial nociception. In the formalin test, all doses of EE, CF and MF significantly reduced the orofacial nociception in the first (p < 0.001) and second phase (p < 0.001), which was also naloxone‐sensitive. In the glutamate‐induced nociception test, only CF and MF significantly reduced the orofacial nociceptive behavior with inhibition percentage values of 48.1% (100 mg/kg, CF), 56.1% (200 mg/kg, CF), 66.4% (400 mg/kg, CF), 48.2 (200 mg/kg, MF) and 60.1 (400 mg/kg, MF). Furthermore, treatment of the animals with EE, CF and MF was not able to promote motor activity changes. These data demonstrate that S. cordifolia has a pronounced antinociceptive activity on orofacial nociception. However, pharmacological and chemical studies are necessary in order to characterize the responsible mechanisms for this antinociceptive action and also to identify other bioactive compounds present in S. cordifolia. Copyright

Antiinflammatory activity and acute toxicity (LD50) of the juice of Kalanchoe brasiliensis (comb.) leaves picked before and during blooming

Kalanchoe brasiliensis Comb. (Cassulaceae) extracts from leaves picked before and during plant blooming (extracts 1 and 2, respectively) were tested for their antiinflammatory effect on carrageenin‐induced rat paw oedema and for acute toxicity (LD50). Oral doses of 0.25, 0.5 and 1.0 g/kg of extract 1 significantly inhibited the paw oedema during the first 4 h after injection of 2% carrageenin, while oral doses of 0.5, 1.0 and 2.0 g/kg of extract 2 had no inhibitory activity on the paw oedema induced by carrageenin. The results indicate an antiinflammatory effect of extract 1 and a proinflammatory effect of extract 2. K. brasiliensis extracts 1 and 2 presented no acute toxicity on mice at the doses of 0.25 to 5 g/kg administered intraperitoneally. Copyright

Cardiovascular effects induced by Cymbopogon winterianus essential oil in rats: involvement of calcium channels and vagal pathway.

Objectives This study has investigated the cardiovascular effects of the Cymbopogon winterianus essential oil (EOCW) in rats. C. winterianus is a plant used in folk medicine for the treatment of hypertension.