A valepotriate-enriched fraction from Valeriana glechomifolia Meyer inhibits leukocytes migration and nociception in formalin test in rodents

Abstract Previous pre-clinical studies demonstrated that a valepotriates enriched fraction from Valeriana glechomifolia F.G. Mey., Caprifoliaceae, was effective against lipopolysaccharide from Escherichia coli (LPS)-induced sickness behavior as well as significantly decreased the cortical expression of pro inflammatory cytokines interleukin-1β and tumor necrosis factor-α. Other studies revealed anti-inflammatory properties of V. wallichii and V. amurensis. These findings open up new perspectives for Valeriana genus pharmacology, once it has been commonly associated to sedative and anxiolytic properties. The aim of this study was to investigate the antichemotactic, antinociptive and anti-inflammatory activities of a valepotriate-enriched fraction obtained from aerial and subterranean parts of V. glechomifolia submitted to supercritical CO2 extraction. The biological activities were assessed by means of formalin test in CF1 mice and Wistar rat's leukocytes migration assay (modified Boyden chamber method). Valepotriate-enriched fraction (1, 10 and 30 mg/kg, p.o.) inhibited the nociceptive behavior in the late phase of the formalin test in a dose dependent manner. The effect of the valepotriate-enriched fraction highest dose was comparable with that of diclofenac 50 mg/kg (p.o.). Valepotriate-enriched fraction (0.1-1 µg/ml) inhibited the leukocyte migration induced by lipopolysaccharide from Escherichia coli in a concentration dependent manner. This antichemotatic effect was comparable with that of indomethacin (0.1-1 µg/ml) and better than diclofenac (1 µg/ml) effect. This study demonstrated for the first time that a valepotriate-enriched fraction obtained from V. glechomifolia display a peripheral anti-inflammatory like activity.

Effects of hydroalcoholic extract of Celtis iguanaea on markers of cardiovascular diseases and glucose metabolism in cholesterol-fed rats

ABSTRACT Celtis iguanaea (Jacq.) Sarg., Cannabaceae, is popularly used in the treatment of diabetes mellitus. However, chemical and pharmacological investigations are lacking. In this study, we investigated the effects of the hydroalcoholic extract from C. iguanaea on markers of cardiovascular diseases and the glucose metabolism in cholesterol-fed rats. Therefore, hypercholesterolemic rats (1% cholesterol) were orally treated with C. iguanaea extract (C-150, CI-300, or CI-600 mg/kg) or simvastatin (4 mg/kg) (n = 6) once a day (30 days) with a hypercholesterolemic diet. A control group (C) was given saline. C. iguanaea extract showed significant decreases in serum levels of total cholesterol, LDL-cholesterol, HMG-CoA-reductase, interleukin-1 and 6, TNF-α and IFN-γ when compared to group C (p < 0.001). Hypoglycemic effects were observed along with a decrease of the activity of sucrase (CI-600), maltase (CI-150, CI-300), and an increase in muscle glycogen levels (CI-300). Antioxidant effects were observed in plasma by the decrease of TBARS and increase of nonprotein thiols levels (CI-600). The histopathological analysis showed a significant decrease in the liver fat area for C. iguanaea extract compared to group C (p < 0.001). Our results suggest that the biological effects of C. iguanaea extract could be related to the flavonoids that possibly exert antioxidant, enzymatic inhibitory, and insulin-mimetic effects.

Uliginosin B, a natural phloroglucinol derivative with antidepressant-like activity, increases Na+,K+-ATPase activity in mice cerebral cortex

ABSTRACT Uliginosin B, a phloroglucinol isolated from Hypericum polyanthemum Klotzsch ex Reichardt, Hypericaceae, has antidepressant-like effect in the forced swimming test in rodents and inhibits monoamines neuronal reuptake without binding to their neuronal carriers. Studies showed the involvement of Na+,K+-ATPase brain activity in depressive disorders, as well as the dependence of neuronal monoamine transport from Na+ gradient generated by Na+,K+-ATPase. This study aimed at evaluating the effect of uliginosin B on Na+,K+-ATPase activity in mice cerebral cortex and hippocampus (1 and 3 h after the last administration) as well as the influence of veratrine, a Na+ channel opener, on the antidepressant-like effect of uliginosin B. Mice were treated (p.o.) with uliginosin B single (10 mg/kg) or repeated doses (10 mg/kg/day, 3 days). Acute administration reduced the immobility in the forced swimming test and tail suspension test and increased Na+,K+-ATPase activity in cerebral cortex 1 h after treating, whereas the repeated treatment induced the antidepressant-like effect and increased the Na+,K+-ATPase activity at both times evaluated. None treatment affected the hippocampus enzyme activity. Veratrine pretreatment prevented uliginosin B antidepressant-like effect in the forced swimming test, suggesting the involvement of Na+ balance regulation on this effect. Altogether, these data indicate that uliginosin B reduces the monoamine uptake by altering Na+ gradient.

Survey of plants popularly used for pain relief in Rio Grande do Sul, southern Brazil

Ethnobotanical data can be an important tool in the search for new drugs. The Brazilian Health Surveillance Agency accepts the registration of herbal medicines based on ethnopharmacological and ethnobotanical studies. With the purpose of increasing the knowledge of potentially useful plants for the treatment of painful conditions, we analyzed the ethnobotanical studies carried out in Rio Grande do Sul state (RS-Southern Brazil); we had access to nineteen studies.To our knowledge, this is the first compilation of ethnobotanical studies that focus on pain relief carried out in RS. The species native to RS cited in at least nine (about 50%) of these studies were selected. The search retrieved 28 native species cited as used to alleviate painful conditions, which are distributed in eighteen botanical families, being Asteraceae the most mentioned. The species more frequently cited for pain relief were Achyrocline satureioides, Baccharis articulata, Baccharis crispa, Lepidium didymum, Eugenia uniflora and Maytenus ilicifolia. The only species not reported in any pre-clinical study associated with pain relief was B. articulata. Among the six species cited, no studies on clinical efficacy were found. In conclusion, the folk use of native plants with therapeutic purposes is widespread in RS State (Brazil), being pain relief an important property.