ABSTRACT
CONTEXT: Despite several pharmacological applications of Rosmarinus officinalis L. (Lamiaceae), studies on its analgesic and anti-inflammatory properties have been scarce. OBJECTIVE: The aim of this work was to use in vivo models to evaluate the analgesic and anti-inflammatory activities of the aqueous extracts obtained from leaves (AEL) and stems (AES) of Rosmarinus officinalis, as well as its isolated compound--rosmarinic acid (RA). We also prepared and assessed the acetyl ester derivative of RA. MATERIALS AND METHODS: The analgesic activity was evaluated using abdominal constriction and formalin tests. For the evaluation of the anti-inflammatory effects, carrageenin-induced paw edema in rats were used. The extracts were used at doses of 100, 200 and 400 mg kg⻹ compounds were tested at 10, 20 and 40 mg kg⻹. RESULTS: Orally administered AEL, AES and RA were not significantly active at any of the doses tested during the abdominal constriction test; the acetyl ester derivative of RA displayed significant analgesic activity. In the carrageenin-induced paw edema assay, the acetyl derivative of RA at all the tested doses produced significant anti-inflammatory effects and reduced the number of paw licks in the second phase of the formalin test. DISCUSSION AND CONCLUSION: The results suggest that the analgesic effects of the acetyl derivative of RA operate via a peripheral-mediated mechanism. The acetyl ester derivative of RA is potentially applicable as a new lead compound for the management of pain and inflammation.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Cinnamates/therapeutic use , Depsides/therapeutic use , Disease Models, Animal , Neuralgia/prevention & control , Neurogenic Inflammation/prevention & control , Plant Extracts/therapeutic use , Rosmarinus/chemistry , Acetylation , Administration, Oral , Animals , Anti-Inflammatory Agents, Non-Steroidal/isolation & purification , Behavior, Animal/drug effects , Brazil , Cinnamates/administration & dosage , Cinnamates/chemistry , Cinnamates/isolation & purification , Depsides/administration & dosage , Depsides/chemistry , Depsides/isolation & purification , Dose-Response Relationship, Drug , Ethnopharmacology , Male , Medicine, Traditional , Mice , Plant Extracts/administration & dosage , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plant Leaves/chemistry , Plant Stems/chemistry , Rats , Rats, Wistar , Rosmarinic AcidABSTRACT
The essential oil of Rosmarinus officinalis L. (rosemary) was obtained by hydro-distillation and analysed by gas chromatography-mass spectrometry. Sixty-two constituents were identified, representing 98.06% of the total oil content. Oxygenated monoterpenes were the predominant components. The rosemary oil was characterized as having prominent (> 5%) contents of camphor (18.9%), verbenone (11.3%), a-pinene (9.6%), beta-myrcene (8.6%), 1,8-cineole (8.0%), and beta-caryophyllene (5.1%). The antimicrobial activity of the oil as well as of its major constituents was tested against the following microorganisms: Streptococcus mutans, Streptococcus mitis, Streptococcus sanguinis, Streptococcus salivarius, Streptococcus sobrinus, and Enterococcus faecalis, which are potentially responsible for the formation of dental caries in humans. The microdilution method was used for determination of the minimum inhibitory concentration (MIC) during evaluation of the antibacterial activity. The essential oil displayed low activity against the selected microorganisms. In the present study, the pure major compounds were more active than the essential oil. Among all the microorganisms tested, the pathogen S. mitis was the most susceptible and E. faecalis was the most resistant to the evaluated samples. This is the first report on antimicrobial activity of the major components of rosemary oil against oral pathogens.
Subject(s)
Anti-Bacterial Agents/pharmacology , Oils, Volatile/pharmacology , Rosmarinus , Acyclic Monoterpenes , Anti-Bacterial Agents/isolation & purification , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Bicyclic Monoterpenes , Camphor/isolation & purification , Camphor/pharmacology , Chlorhexidine/isolation & purification , Chlorhexidine/pharmacology , Enterococcus faecalis/drug effects , Gas Chromatography-Mass Spectrometry , Microbial Sensitivity Tests , Monoterpenes/isolation & purification , Monoterpenes/pharmacology , Plant Oils/isolation & purification , Plant Oils/pharmacology , Polycyclic Sesquiterpenes , Sesquiterpenes/pharmacology , Streptococcus/drug effects , Streptococcus mitis/drug effects , Streptococcus mutans/drug effects , Streptococcus sobrinus/drug effects , Terpenes/isolation & purification , Terpenes/pharmacologyABSTRACT
The in vitro inhibitory activity of crude EtOH/H2O extracts from the leaves and stems of Rosmarinus officinalis L. was evaluated against the following microorganisms responsible for initiating dental caries: Streptococcus mutans, S. salivarius, S. sobrinus, S. mitis, S. sanguinis, and Enterococcus faecalis. Minimum inhibitory concentrations (MIC) were determined with the broth microdilution method. The bioassay-guided fractionation of the leaf extract, which displayed the higher antibacterial activity than the stem extract, led to the identification of carnosic acid (2) and carnosol (3) as the major compounds in the fraction displaying the highest activity, as identified by HPLC analysis. Rosmarinic acid (1), detected in another fraction, did not display any activity against the selected microorganisms. HPLC Analysis revealed the presence of low amounts of ursolic acid (4) and oleanolic acid (5) in the obtained fractions. The results suggest that the antimicrobial activity of the extract from the leaves of R. officinalis may be ascribed mainly to the action of 2 and 3.
