ABSTRACT
The anti-inflammatory and analgesic effects of the ethanolic extract (SLEE) and fruticulin A from the leaves of Salvia lachnostachys were evaluated in mice, using experimental models of inflammation (paw oedema and pleurisy induced by carrageenan injection) and hyperalgesia (electronic Von Frey). Oral administration of SLEE (30, 100, and 300 mg/kg) and fruticulin A (0.3 and 3.0 mg/kg) decreased the total leucocytes number in pleural lavage, protein extravasation, and paw oedema. SLEE (100 mg/kg) and fruticulin A (3 mg/kg) also exhibited antihyperalgesic activity in carrageenan induced mechanical hyperalgesia. In addition, fruticulin A (3 mg/kg) prevented mechanical hyperalgesia, inhibiting TNF but not L-DOPA-induced mechanical hyperalgesia. In conclusion, SLEE and fruticulin A display anti-inflammatory and analgesic properties. Therefore, fruticulin A is at least partially responsible for the activity observed in the ethanolic extract of Salvia lachnostachys.
ABSTRACT
Salvia lachnostachys Benth., Lamiaceae, is a endemic species from southern Brazil. The essential oil of its leaves and flowers is mainly constituted by aliphatic compounds, such as dodecanoic acid, with sesquiterpenes as minor constituents. This work evaluated the morphology, anatomy, microchemistry, and phytochemistry of S. lachnostachys to provide advanced knowledge of Brazilian plants with medicinal potential. Light and scanning electron microscopy techniques were used in the anatomical and microchemical studies. Compounds were isolated by chromatographic techniques, identified by analysis of their NMR spectra and compared with published data. S. lachnostachys can be distinguished from other related species mainly by its petiolate leaves, terminal inflorescence, persistent bracts, and villous-glandular corolla. The stem and leaves of S. lachnostachys display anatomical characteristics common to the family Lamiaceae. However, this species can be distinguished from other family members by the morphology and the presence of eglandular and glandular trichomes, as well as the organization of the vascular bundles of the petiole. The phytochemical results revealed that S. lacnostachys produces oleanolic and ursolic acids in addition to the diterpene fruticuline A, which is a rare compound, previously found only in Salvia fruticulosa Benth. and S. corrugata Vahl. Ursolic and oleanolic acids are bioactive triterpenes that exhibit antiatherosclerotic, anticancer, antihypertensive, antinflammatory, antileukemic, antimutagenic, antioxidant, antiproliferative, and antiviral activities, and fruticuline A has antibacterial activity.
Subject(s)
Plants, Medicinal/anatomy & histology , Plants, Medicinal/chemistry , Salvia/anatomy & histology , Salvia/chemistry , Brazil , Chromatography , Magnetic Resonance Spectroscopy , Microscopy , Plant Leaves/anatomy & histology , Plant Leaves/chemistry , Plant Stems/anatomy & histology , Plant Stems/chemistry , Triterpenes/analysis , Triterpenes/isolation & purification , Triterpenes/pharmacologyABSTRACT
The gastrointestinal activity of hydroalcoholic extract (HE) of Salvia officinalis was evaluated in a model of ethanol-induced gastric lesion. HE showed excellent activity, with ID(50) 84.0 (54.8-128.9) mg/kg. The acetic acid-induced ulcer and the total acidity of the gastric secretion were also reduced by HE, and, in vitro experiments, the H(+),K(+)-ATPase activity was inhibited. Carnosol was identified as a possible active constituent for the gastroprotective effect of HE.
Subject(s)
Abietanes/therapeutic use , Anti-Ulcer Agents/therapeutic use , Gastric Mucosa/drug effects , Phytotherapy , Plant Extracts/therapeutic use , Salvia officinalis/chemistry , Stomach Ulcer/drug therapy , Abietanes/isolation & purification , Abietanes/pharmacology , Acetic Acid , Animals , Anti-Ulcer Agents/isolation & purification , Anti-Ulcer Agents/pharmacology , Ethanol , Female , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Leaves , Proton Pump Inhibitors , Rats , Rats, Wistar , Stomach Ulcer/chemically inducedABSTRACT
The present study assessed the possible antinociceptive action of the hydroalcoholic extract, fractions and pure compounds obtained from the aerial parts of Baccharis illinita DC (Asteraceae) in behavioural models of chemical nociception in mice. The hydroalcoholic extract and fractions (hexane and aqueous but not EtOAc fraction) obtained from B. illinita (30-1000 mg/kg orally) produced a dose-related inhibition of the acetic acid-induced nociceptive response. However, the hexane fraction was more potent than the hydroalcoholic extract and the aqueous fraction. The hexane fraction derivatives baurenol, alpha-spinasterol and oleanolic acid (0.00001-10 mg/kg intraperitoneally) also caused potent inhibition of acetic acid-induced pain. The hexane fraction (300-1000 mg/kg orally) produced inhibition of both phases of formalin-induced pain. Moreover, the hexane fraction (30-600 mg/kg orally) also caused a dose-dependent inhibition of glutamate-induced pain. Nevertheless, the hexane fraction only at the dose of 300 mg/kg orally, produced partial inhibition of the paw oedema caused by carrageenan. Furthermore, the hexane fraction (300 mg/kg orally) caused inhibition of the nociceptive response induced by intrathecal injection of N-methyl-d-aspartic acid, alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid, tumour necrosis factor-alpha and interleukin-1beta. In contrast, the hexane fraction did not affect the biting response induced by the metabotropic or ionotropic glutamatergic receptor agonist (+/-)-1-aminocyclopentane-trans-1,3-dicarboxylic acid and kainate, respectively. In addition, the antinociception caused by the hexane fraction (300 mg/kg orally) in the acetic acid test was not affected by intraperitoneal treatment of mice with naloxone (a non-selective opioid receptor antagonist). The precise mechanism responsible for the antinociceptive effect of the hexane fraction remains unclear, but appears to be partly associated with an inhibition of glutamatergic transmission and an inhibition of pathways dependent on pro-inflammatory cytokines. Finally, baurenol, alpha-spinasterol and oleanolic acid have an important role in the antinociceptive effects of the hexane fraction. Moreover, the antinociceptive action demonstrated in the present study supports the ethnomedical uses of this plant.
Subject(s)
Analgesics/pharmacology , Baccharis/chemistry , Pain/drug therapy , Plant Extracts/pharmacology , Analgesics/administration & dosage , Analgesics/isolation & purification , Animals , Cytokines/drug effects , Cytokines/metabolism , Disease Models, Animal , Dose-Response Relationship, Drug , Female , Mice , Oleanolic Acid/administration & dosage , Oleanolic Acid/isolation & purification , Oleanolic Acid/pharmacology , Pain Measurement , Plant Components, Aerial , Plant Extracts/administration & dosage , Receptors, Glutamate , Solvents/chemistry , Stigmasterol/administration & dosage , Stigmasterol/analogs & derivatives , Stigmasterol/isolation & purification , Stigmasterol/pharmacology , Triterpenes/administration & dosage , Triterpenes/isolation & purification , Triterpenes/pharmacologyABSTRACT
Tabebuia avellanedae is commonly used for the treatment of peptic ulcers. We carried out this study with the ethanolic extract of bark from Tabebuia avellanedae (EET) (30-1000 mg/kg) to determine its gastroprotective activity and to clarify the pathways involved in this effect. Acute gastric ulceration in rats was produced by oral administration of ethanol and ibuprofen. After ethanol administration, the gastric wall mucus was examined. Chronic gastric ulceration was produced by injection of acetic acid in rat gastric subserosa. Anti-secretory studies were undertaken using Shay rat pylorus ligature technique and measurement of enzymatic activity of H+, K+-ATPase in vitro. Administration of EET p.o. or i.p. significantly inhibited gastric mucosa damage induced by ethanol and ibuprofen. The anti-ulcer effect was further confirmed by enhanced gastric mucus production. In pylorus ligature rats, EET significantly reduced the basal gastric acid secretion and total acidity; moreover, it inhibited the increase in total acidity induced by histamine. In addition, EET reduced the activity of H+, K+, ATPase. The results obtained in the present pharmacological assay indicate that this plant has a protective action against gastric lesions, involving the maintenance of protective factors, such as mucus and prostaglandin, besides the reduction of gastric total acidity.