We showed that S. obtusifolium presents a potent anti-inflammatory activity, due to the presence of the N-methyl-(2S,4R)-trans-4-hydroxy-l-proline(NMP) in the plant extract. This action is related to the inhibition by NMP of TNF-alpha and inflammatory enzymes.
Piper tuberculatum, popularly known in Brazil as "jaborandi falso" and "pimenta darta", is widely used in folk medicine for the treatment of several diseases. In this study, the in vivo hollow fiber assay was used to investigate the antitumour efficacy of the crude extract and piplartine obtained from P. tuberculatum roots. Human glioblastoma (SF-295) and colon carcinoma (HCT-8) cell lines were used. In vitro cytotoxicity was assayed by the MTT assay. In the hollow fiber assay, nude mice implanted with tumour cells in hollow fibers were treated for four consecutive days via the intraperitoneal route, and tumour cell populations were assessed by the MTT assay. Both the crude extract and piplartine displayed cytotoxicity. In the hollow fiber assay, tumour growth inhibition rates were 24.6-54.8 % for the crude extract and 33.7-62.2 % for piplartine. No signal of toxicity was noticed. In conclusion, the crude extract and piplartine obtained from P. tuberculatum roots displayed in vitro and in vivo anticancer efficacy.
BackgroundThis study evaluated the in vitro activity of essential oil extracted from the leaves of Myracrodruon urundeuva.MethodsThe oil was obtained by hydro-distillation and characterized by Gas Chromatography coupled to Mass Spectrometry (GC-MS) and Gas Chromatography with Flame Ionization Detector (GC-FID). The antibacterial activity was evaluated by the broth microdilution technique and the MIF was determined by using growth indicator CTT (2,3,5-triphenyl-tetrazolium) and CBM in BHI agar. The oil’s cytotoxicity was evaluated in HeLa, HEK-293, and Vero E6 cells using MTT, 3- (4,5-dimethylthiazol-2-yl) -2,5-diphenyl tetrazolium.ResultsThe oil showed chemical markers, including α-pinene (87.85%), trans-caryophyllene (1.57%), limonene (1.49%) and β -pinene (1.42%), and activity against all strains: Staphylococcus aureus (MIC = MBC = 0.22 mg/mL), Staphylococcus epidermidis (MIC = 0.11 mg/mL and MBC = 0.22 mg/mL), Escherichia coli (MIC = 0.88 mg/mL and MBC = 1.75 mg/mL), Pseudomonas aeruginosa (MIC = MBC = 7 mg/mL) and Salmonella Enteritidis (MIC = MBC = 0.44 mg/mL). In vitro cytotoxicity tests showed that the oil is not toxic and has slight antitumor activity.ConclusionsWe conclude that the M. urundeuva oil results are promising, with prospects of being pharmacologically viable.
Piplartine {5,6-dihydro-1-[(2E)-1-oxo-3-(3,4,5-trimethoxyphenyl)-2-propen-1-yl]-2(1H)-pyridinone} is an alkamide present in Piper species that exhibits promising anticancer properties. It was previously shown that piplartine is mutagenic in yeast and cultured mammalian cells. This study was performed to increase the knowledge on the mutagenic potential of piplartine using the Salmonella/microsome assay, V79 cell micronucleus and chromosome aberration assays, and mouse bone-marrow micronucleus tests. Piplartine was isolated from the roots of Piper tuberculatum. This extracted compound was unable to induce a mutagenic response in any Salmonella typhimurium strain either in the presence or absence of metabolic activation. Piplartine showed mutagenic effects in V79 cells, as there was an increased frequency of aberrant cells and micronuclei formation. In addition, piplartine administered at 50mg/kg did not induce micronucleus formation in vivo, but a dose of 100mg/kg induced an increase in the levels of micronucleus polychromatic erythrocytes (MNPCEs). Overall, these results provide further support that piplartine induces in vivo and in vitro mutagenicity in eukaryotic models.
Wound healing involves the interaction of blood cells, proteins, proteases, growth factors, and extracellular matrix components. Inflammation is one of the first events occurring during this process. Previously, we showed that the N-Methyl-(2S,4R)-trans-4-Hydroxy-L-Proline (NMP) from Sideroxylon obtusifolium leaves (a Brazilian medicinal species) presents an anti-inflammatory action. Considering inflammation as an important event in the wound healing process, the objectives were to investigate the topical effects of the NMP gel on a mice wound-induced model. Male Swiss mice were divided into 4 groups: Sham (surgical procedure only), Control (gel-base treated), and 3% or 10% NMP gel-treated groups. Measurements of wound areas and microscopic analyses (HE [hematoxylin-eosin] and PSR [picrosirius red] stainings) were carried out, at the 7th and 12th, days after the wound induction. Furthermore, immunohistochemical assays for iNOS (inducible nitric oxide synthase) and COX-2 (cyclooxygenase-2) and biochemical measurements for TBARS (thiobarbituric acid reactive substances), GSH (glutathione), and myeloperoxidase (MPO) were also performed, at the second day after the wound induction. The work showed that NMP decreases the wound areas, after topical application, relatively to the Sham and Control groups. In addition, microscopic alterations were reduced and collagen deposition was increased, at the 7th and 12th days, in the 10% NMP group. While iNOS and COX-2 immunostainings and GSH contents increased, in relation to the Sham and Control groups, TBARS and MPO decreased. Altogether, the results showed NMP to improve the wound healing process, by upregulating iNOS and COX-2 activities, reducing lipid peroxidation and MPO activity, and increasing GSH contents. In addition, NMP certainly contributes to the increased collagen deposition. These data may stimulate translational studies dealing with the possible use of NMP from Sideroxylon obtusifolium or from other sources for the management of wound healing.
Myracrodruon urundeuva (Anacardiaceae) is the scientific designation of "aroeira-do-sertão", a tree well dispersed at the northeastern Brazil. The medicinal use of this plant is widespread throughout the rural population and the inner trunk bark decoction is used to treat cutaneous affections, urinary and respiratory diseases, and gynecological problems. "Aroeira-do-sertão" has been included in the list of native species under extinction threat. In order to find a sustainable source of the plant, seedlings have been cultivated. The purpose of this work was to investigate the chemical composition of the decoction from leaves of cultivated plants (aqueous extract from Myracrodruon urundeuva (AEMU)) and its anti-inflammatory activity on human neutrophils. The addition of AEMU on cells suspension inhibited significantly its activation/degranulation induced by phorbol myristate acetate. AEMU since at 50 µg mL-1 showed better pattern of inhibitions when related to indomethacin, nonselective cyclooxygenase inhibitor used as reference anti-inflammatory. The decoction fractionation was performed by high-speed counter-current chromatography (HSCCC) and semi-preparative highperformance liquid chromatography (HPLC) using a phenyl column as the stationary phase, allowing the isolation of 24 compounds. These results showed how the AEMU is rich in bioactive metabolites, which probably contribute for the anti-inflammatory effects of this plant extract, modulating the degranulation of human neutrophils, one of the pro-inflammatory mechanism of these cells.
Myracrodruon urundeuva Allemão, Anacardiaceae, is popularly known as "aroeira-do-sertão". It is a common species in the state of Ceará and widely used for its anti-inflammatory, anti-ulcer, astringent, anti-allergic, and antidiarrheal activities and also in the treatment of skin wounds. The aim of this study was to evaluate the healing effect of the cream prepared with the decoction from the stem bark of a 7-year-old cultivated M. urundeuva in rats submitted to excisional wounds. Male Wistar rats were divided into three groups: sham group, which did not received a treatment; 10% "aroeira" cream group, which received application of the plant cream; and control group, which received application of the base cream. The animals had their skin fragments (8 mm in diameter) removed, and each group was observed at 2, 7, and 12 days after surgery. The macroscopic analysis was performed with a digital paquimeter. The fragments of newly formed tissue were removed from the skin for slides processing and hematoxylin-eosin (HE) and picrosirius red staining techniques, in order to verify the effect of the 10% "aroeira" cream in different stages of the healing process. Macroscopic analyses demonstrated a decrease in the area of the 10% "aroeira" cream treated wounds, compared with controls. In addition, the histological study evidenced an improvement in the inflammatory aspects (infiltrate, edema, hemorrhage), in this treated group, as well as the presence of a new epithelium and a greater intensity in collagen deposition. Thus, a favorable effect was observed regarding the use of 10% "aroeira" cream in the cicatricial process of cutaneous wounds in rats, modulating the inflammatory response of healing and accelerating tissue repair of experimental excisional skin wounds.
Myracrodruon urundeuva Fr. Allem. (Anacardiaceae) is the scientific designation of "aroeira-do-sertão", a tree well dispersed through the "Caatinga", the characteristic northeastern Brazil flora. Its trunk bark decoction is used to treat cutaneous affections, urinary and respiratory diseases and as a postpartum aseptic bath. This work reports the analyses of the essential oils from leaves of 62 specimens of "aroeira-do-sertão". Analyses by 1 H nuclear magnetic resonance (NMR) and gas chromatography coupled to mass spectrometry (GC-MS) of all oil samples permitted the characterization of all major components and, in consequence, the characterization of six different chemotypes of M. urundeuva, represented by the chemomarkers: myrcene, α-pinene, limonene, Δ 3 -carene, (Z) and (E)-β-ocimene.
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