Subject(s)
Nanoparticles , Propolis , Propolis/pharmacology , Leukocytes, Mononuclear , Gene Expression , CytokinesABSTRACT
The skin is essential to the integrity of the organism. The disruption of this organ promotes a wound, and the organism starts the healing to reconstruct the skin. Copaifera langsdorffii is a tree used in folk medicine to treat skin affections, with antioxidant and anti-inflammatory properties. In our study, the oleoresin of the plant was associated with nanostructured lipid carriers, aiming to evaluate the healing potential of this formulation and compare the treatment with reference drugs used in wound healing. Male Wistar rats were used to perform the excision wound model, with the macroscopic analysis of wound retraction. Skin samples were used in histological, immunohistochemical, and biochemical analyses. The results showed the wound retraction in the oleoresin-treated group, mediated by α-smooth muscle actin (α-SMA). Biochemical assays revealed the anti-inflammatory mechanism of the oleoresin-treated group, increasing interleukin-10 (IL-10) concentration and decreasing pro-inflammatory cytokines. Histopathological and immunohistochemical results showed the improvement of re-epithelialization and tissue remodeling in the Copaifera langsdorffii group, with an increase in laminin-γ2, a decrease in desmoglein-3 and an increase in collagen remodeling. These findings indicate the wound healing potential of nanostructured lipid carriers associated with Copaifera langsdorffii oleoresin in skin wounds, which can be helpful as a future alternative treatment for skin wounds.
Subject(s)
Fabaceae , Re-Epithelialization , Rats , Animals , Rats, Wistar , Skin/pathology , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Fabaceae/chemistry , LipidsABSTRACT
The Copaifera oleoresins are widely used in folk medicine to treat various diseases. The goal of this study was to develop a validated reverse-phase high-performance liquid chromatography method with photodiode array detection (RP-HPLC-PDA) to quantify eight terpenes: ent-hardwickiic acid, ent-copalic acid, ent-7α-acetoxy hardwickiic acid, ent-16-hydroxy-3,13-clerodadiene-15,18-dioic acid, ent-5,13-labdadiene-15-oic acid, junenol, ent-kaurenoic acid, and 13E-ent-labda-7,13-dien-15-oic acid in the oleoresins of Copaifera pubiflora L. (OCP), Copaifera trapezifolia L. (OCT) and Copaifera langsdorffii L. (OCL). The linearity of the method was confirmed in the range of 20.00-500 µg.mL-1 (r2 > 0.999). The limit of quantification was between 1,05 and 16.89 µg.mL-1. Precision and accuracy ranges were found to be %RSD <0.2 and 96% to 110%, respectively. Based on the obtained results, the developed analytical method is rapid, precise, accurate, and sensitive for quantifying these terpenes in Copaifera's oleoresins.
ABSTRACT
Staphylococcus pseudintermedius is the leading cause of canine pyoderma. Honeybee products are common to treat this and other types of infections. High average annual population loss of bees has been observed. This study evaluated antibacterial and antibiofilm profile of Green Propolis and Baccharis dracunculifolia against S. pseudintermedius and the chemical similarities among both. Ethanolic extracts were produced and chemically characterized. The isolates were subjected to treatment with the extracts in both planktonic and sessile forms. Green propolis minimum inhibitory concentration (MIC) was 0.156 mg / mL, and minimum bactericidal concentration (MBC) was 0.312mg / mL. Baccharis dracunculifolia extract MIC and MBC was 0.312mg / mL and 2.5 mg / mL, respectivelly. Both extracts reduced SD55 formation of biofilm at minimum inhibitory concentration and at 1/8 minimum inhibitory concentration. The results observed in relation to ED99, were similar for both extracts. Besides that, similar chemical indicators between both extracts, including the presence of Artepellin C, suggest that the Baccharis dracunculifolia extract could be an alternative to the Green Propolis extract in the treatment of staph infections.
Subject(s)
Anti-Infective Agents , Baccharis , Propolis , Animals , Anti-Bacterial Agents/pharmacology , Anti-Infective Agents/pharmacology , Baccharis/chemistry , Biofilms , Dogs , Microbial Sensitivity Tests , Plant Extracts/chemistry , Plant Leaves/chemistry , Propolis/chemistry , Propolis/pharmacology , StaphylococcusABSTRACT
Propolis is a bee product that has been used in medicine since ancient times. Although its anti-inflammatory, antioxidant, antimicrobial, antitumor, and immunomodulatory activities have been investigated, its anti-parasitic properties remain poorly explored, especially regarding helminths. This review surveys the results obtained with propolis around the world against human parasites. Regarding protozoa, studies carried out with the protozoa Trypanosoma spp. and Leishmania spp. have demonstrated promising results inâ vitro and inâ vivo. However, there are fewer studies for Plasmodium spp., the etiological agent of malaria and less so for helminths, particularly for Fasciola spp. and Schistosoma spp. Despite the favorable inâ vitro results with propolis, helminth assays need to be further investigated. However, propolis has shown itself to be an excellent natural product for parasitology, thus opening new paths and approaches in its activity against protozoa and helminths.
Subject(s)
Antiparasitic Agents/pharmacology , Phenols/pharmacology , Plant Extracts/pharmacology , Propolis/chemistry , Animals , Antiparasitic Agents/chemistry , Antiparasitic Agents/isolation & purification , Brazil , Helminths/drug effects , Leishmania/drug effects , Molecular Structure , Parasitic Sensitivity Tests , Phenols/chemistry , Phenols/isolation & purification , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plasmodium/drug effects , Trypanosoma/drug effectsABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: Green propolis is produced by Apis mellifera honeybees using Baccharis dracunculifolia D.C. (Asteraceae) as substrate. This Southern Brazilian native plant and green propolis have been used in traditional medicine to treat gastric diseases, inflammation and liver disorders. AIM OF THE STUDY: Investigate the effects of baccharin (Bac) or p-coumaric acid (pCA) isolated from B. dracunculifolia D.C. (Asteraceae) over the inflammation induced by lipopolysaccharide (LPS) in vivo. MATERIALS AND METHODS: Inflammation was induced by LPS injection into air-pouches in mice, which were subsequently treated with Bac or pCA. Lavage fluid was collected from air pouches for the quantification of cellular influx via microscopy, and quantification of inflammatory mediators via colorimetric methods, ELISA and liquid chromatography-tandem mass spectrometry (LC-MS/MS). RESULTS: LPS-induced inflammation increased cellular influx and increased the levels of parameters related to vascular permeability and edema formation, such as nitric oxide (NO) and protein extravasation. Moreover, LPS increased the levels of cytokines and eicosanoids in the air-pouches. Importantly, both Bac and pCA suppressed the infiltration of neutrophils, production of NO and protein extravasation. Notably, the compounds promote differential regulation of cytokine and eicosanoid production. CONCLUSIONS: Our results suggest that Bac from green propolis directly affects inflammation by inhibiting the production of cytokines and eicosanoids, while pCA may exert direct, but also indirect effects on inflammation by stimulating the production of regulatory effectors such as interkeukin-10 in vivo.
Subject(s)
Baccharis/chemistry , Coumaric Acids/pharmacology , Propolis/metabolism , Trichothecenes/pharmacology , Animals , Anti-Inflammatory Agents/isolation & purification , Anti-Inflammatory Agents/pharmacology , Bees , Brazil , Coumaric Acids/isolation & purification , Cytokines/metabolism , Eicosanoids/metabolism , Female , Inflammation/drug therapy , Lipopolysaccharides , Male , Mice , Mice, Inbred BALB C , Plant Extracts/chemistry , Trichothecenes/isolation & purificationABSTRACT
Propolis is one of the most widely used products in traditional medicine. One of the most prominent types of Brazilian propolis is the red one, whose primary botanical source is Dalbergia ecastaphyllum (L.) Taub. Despite the potential of Brazilian red propolis for developing new products with pharmacological activity, few studies guarantee safety in its use. The objective of this study was the evaluation of the possible toxic effects of Brazilian red propolis and D. ecastaphyllum, as well as the cytotoxicity assessment of the main compounds of red propolis on tumoral cell lines. Hydroalcoholic extracts of the Brazilian red propolis (BRPE) and D. ecastaphyllum stems (DSE) and leaves (DLE) were prepared and chromatographed for isolation of the major compounds. RP-HPLC-DAD was used to quantify the major compounds in the obtained extracts. The XTT assay was used to evaluate the cytotoxic activity of the extracts in the human fibroblast cell line (GM07492A). The results revealed IC50 values of 102.7, 143.4, and 253.1 µg/mL for BRPE, DSE, and DLE, respectively. The extracts were also evaluated for their genotoxic potential in the micronucleus assay in Chinese hamster lung fibroblasts cells (V79), showing the absence of genotoxicity. The BRPE was investigated for its potential in vivo toxicity in the zebrafish model. Concentrations of 0.8-6.3 mg/L were safe for the animals, with a LC50 of 9.37 mg/L. Of the 11 compounds isolated from BRPE, medicarpin showed a selective cytotoxic effect against the HeLa cell line. These are the initial steps to determine the toxicological potential of Brazilian red propolis.
Subject(s)
Dalbergia/chemistry , Plant Extracts/pharmacology , Propolis/pharmacology , Animals , Brazil , Cells, Cultured , Dose-Response Relationship, Drug , Humans , Molecular Structure , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Propolis/chemistry , Propolis/isolation & purification , ZebrafishABSTRACT
Cernumidine (CER) is a guanidinic alkaloid isolated from Solanum cernuum leaves. In this work, we investigated the cytotoxicity, chemosensitizing effect of cernumidine to cisplatin (cDDP) and the possible mechanism of action of the combination on bladder cancer cells. Cernumidine showed cytotoxicity and could sensitize bladder cancer cells to cisplatin. The combination of CER+cDDP inhibited cell migration on T24 cells. CER+cDDP down-regulated MMP-2/9 and p-ERK1/2, while it increased EGFR activity corroborating the observed cell migration inhibition. Down-regulation of Bcl-2 and up-regulation pro-apoptotic Bax and further depletion of the mitochondrial membrane potential (ΔΨm) indicates that mitochondria play a central role in the combination treatment inducing the mitochondrial signaling pathway of apoptosis in T24 cells. Our data showed that the alkaloid cernumidine is worthy of further studies as a chemosensitizing agent to be used in complementary chemotherapy.
Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Caffeic Acids/pharmacology , Guanidines/pharmacology , Solanum/chemistry , Urinary Bladder Neoplasms/drug therapy , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Apoptosis/drug effects , Caffeic Acids/chemistry , Caffeic Acids/isolation & purification , Cell Movement/drug effects , Cell Proliferation/drug effects , Drug Screening Assays, Antitumor , Guanidines/chemistry , Guanidines/isolation & purification , Humans , Membrane Potential, Mitochondrial/drug effects , Microscopy, Fluorescence , Mitochondria/drug effects , Mitochondria/metabolism , Plant Leaves/chemistry , Tumor Cells, Cultured , Urinary Bladder Neoplasms/metabolism , Urinary Bladder Neoplasms/pathologyABSTRACT
OBJECTIVE: This study proposed to use the nanotechnology to deliver glycoalkaloidic extract (AE) to bladder cancer cells, evaluating their activity in 2D and 3D models and the biological mechanism of cell death. METHODS: NPs were prepared by nanoprecipitation method using polylactic acid (PLA) and characterized considering their size, charge, particle concentration and stability. The cytotoxicity was evaluated in 2D and 3D model, and the apoptosis and cell cycle were investigated using flow cytometry. KEY FINDINGS: NPs loading AE (NP-AE) had diameter around 125 ± 6 nm (PdI <0.1) and negative charge. The encapsulation efficiency of SM and SS was higher than 85% for both compounds. The obtained formulation showed a significant in-vitro cytotoxic effect against RT4 cells in a dose-dependent manner with IC50 two fold lower than the free AE. The cytotoxic effect of NP-AE was mediated by apoptosis and cell cycle arrested in the S phase. RT4 cells cultured under 3D conditions exhibited a higher resistance to the treatments (IC50 ~ three fold higher than in 2D cell culture). CONCLUSION: The NP-AE might be a promising nanocarrier to load and deliver glycoalkaloids against bladder cancer.
Subject(s)
Alkaloids/chemistry , Alkaloids/pharmacology , Nanoparticles/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Urinary Bladder Neoplasms/drug therapy , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Apoptosis/drug effects , Cell Cycle Checkpoints/drug effects , Cell Line, Tumor , Drug Carriers/chemistry , Humans , Nanotechnology/methods , Particle Size , Polyesters/chemistry , S Phase/drug effects , Urinary Bladder/drug effectsABSTRACT
INTRODUCTION: Galloylquinic acid derivatives and flavonoids are the main phenolic metabolites found in Copaifera langsdorffii leaves (Leguminosae, Detarioideae), a medicinal plant with potential therapeutic application in the treatment of kidney stones. The factors that affect metabolite production in this plant species are not well understood but may include environmental and genetic factors. OBJECTIVE: To quantify the variation in metabolite production over a 12-month period for 10 groups of C. langsdorffii cultivated under the same environmental conditions. METHODS: Copaifera langsdorffii seeds were collected from 10 different regions in southeast, Brazil and grown in the same field. HPLC-UV was used to quantify nine galloylquinic acid derivatives and two flavonoids in leaf samples from mature trees. Climate data for humidity, radiation, precipitation and temperature were provided by the National Institute of Meteorology, Brazil. Multivariate analyses were performed to correlate chemical and environmental variables. RESULTS: The overall effect of environmental factors on the production of phenolic metabolites was uniform among C. langsdorffii groups. Chemical variation between groups was present, but small, and probably due to differences in their genetics and physiology. Seasonal changes influenced the production of the major phenolic metabolites, with increases in temperature and radiation levels favouring metabolite production. CONCLUSION: When C. langsdorffii trees are cultivated in the same environment, the production of the major secondary metabolites found in their leaves is very similar quantitatively, varying based on geographic location of original population and seasonal changes. This favours the standardisation of plant raw material for the production of a phytomedicine.
Subject(s)
Fabaceae/metabolism , Phenols/analysis , Plant Leaves/metabolism , Chromatography, High Pressure Liquid/methods , Geography , Phenols/metabolism , Phenols/standards , Reference Standards , Seasons , Spectrophotometry, Ultraviolet/methodsABSTRACT
Six dibenzylbutyrolactonic lignans ((-)-hinokinin (1), (-)-cubebin (2), (-)-yatein (3), (-)-5-methoxyyatein (4), dihydrocubebin (5) and dihydroclusin (6)) were isolated from Piper cubeba seed extract and evaluated against Schistosoma mansoni. All lignans, except 5, were able to separate the adult worm pairs and reduce the egg numbers during 24 h of incubation. Lignans 1, 3 and 4 (containing a lactone ring) were the most efficient concerning antiparasitary activity. Comparing structures 3 and 4, the presence of the methoxy group at position 5 appears to be important for this activity. Considering 1 and 3, it is possible to see that the substitution pattern change (methylenedioxy or methoxy groups) in positions 3' and 4' alter the biological response, with 1 being the second most active compound. Computational calculations suggest that the activity of compound 4 can be correlated with the largest lipophilicity value.
Subject(s)
Anthelmintics/pharmacology , Lignans/pharmacology , Piper/chemistry , Plant Extracts/pharmacology , Schistosoma mansoni/drug effects , Animals , Carbon-13 Magnetic Resonance Spectroscopy , Density Functional Theory , Female , Lignans/chemistry , Lipids/chemistry , Male , Mice, Inbred BALB C , Models, Theoretical , Molecular Docking Simulation , Molecular Structure , Parasite Egg Count , Plant Extracts/chemistry , Proton Magnetic Resonance Spectroscopy , Schistosoma mansoni/chemistry , Static Electricity , Tubulin/chemistryABSTRACT
Copaifera (Leguminoseae) species produce a commercially interesting oleoresin that displays several biological activities, including antimicrobial and anti-inflammatory properties. Labdane-type diterpenes are the main chemical constituents of these oleoresins, and copalic acid is the only compound that has been detected in all Copaifera oleoresins. In this study, we investigate some aspects of the gas-phase fragmentation reactions involved in the formation of the product ions from the deprotonated compounds (-)-ent-copalic acid (1), (-)-ent-3ß-hydroxy-copalic acid (2), (-)-ent-3ß-acetoxy-copalic acid (3), and (-)-ent-agathic acid (4) by electrospray ionization tandem mass spectrometry (ESI-MS/MS) and multiple stage mass spectrometry (MSn ). Our results reveal that the product ion with m/z 99 is common to all the analyzed compounds, whereas the product ion with m/z 217 is diagnostic for compounds 2 and 3. Moreover, only compound 4 undergoes CO2 (44 u) and acetic acid (60 u) elimination from the precursor ion. Thermochemical data obtained by computational chemistry at the B3LYP/6-31G(d) level of theory support the proposed ion structures. These data helped us to identify these compounds in a crude commercial Copaifera langsdorffii oleoresin by selective multiple reaction monitoring (MRM). Finally, a precursor ion scan (PIS) strategy aided screening of labdane-type acid diterpenes other than 1 to 4 in the same Copaifera oleoresin sample and led us to propose the structures of 8,17-dihydro-ent-agathic acid (5) and 3-keto-ent-copalic acid (6), which have not been previously reported in Copaifera oleoresins.
Subject(s)
Diterpenes/analysis , Spectrometry, Mass, Electrospray Ionization/methods , Tandem Mass Spectrometry/methods , Anti-Bacterial Agents/analysis , Balsams/analysis , Chromatography, High Pressure Liquid , Fabaceae/chemistry , Models, Molecular , Molecular Structure , Plant Extracts/chemistryABSTRACT
ETHOPHARMACOLOGICAL RELEVANCE: The propolis is extensively used in folk medicine in natura or to prepare pharmaceutical formulations since ancient time to improve health or prevent diseases, among them gastrointestinal disorders. Aiming to contribute in the scientific validation about the popular use of Brazilian Green propolis (BGP) against gastritis and gastric ulcer, this work evaluated the antiulcer potential of isolated compounds from BGP, three prenylated p-coumaric acid derivatives and two flavonoids, respectively named: 3,5 diprenyl-4-hydroxycinnamic acid (artepillin C) (1), 3-prenyl-4-dihydroxycinnamoiloxy cinnamic acid (baccharin) (2), 3-prenyl-4-hydroxycinnamic acid (drupanin) (3), aromadendrin-4'-O-methyl-ether (4) and kaempferide (5). MATERIAL AND METHODS: The compounds were characterized by nuclear magnetic resonance and mass spectrometry. Their gastroprotective effects were evaluated against ethanol/HCl- and indomethacin-induced ulcer in mice. Further, histological, histochemical, oxidative and inflammatory parameters were analyzed at ulcerated tissue. Acid antisecretory activities also were also assessed. RESULTS: Compound 2 did not reduce the ethanol/HCl- induced ulcer at 30â¯mg/kg (p.o), whereas the minimum oral gastroprotective doses of 1, 3, 4 and 5 were 0.3, 0.3, 3 and 3â¯mg/kg, respectively. Besides, these compounds prevented ethanol/HCl-induced ulcer by intraperitoneal route, as well as indomethacin-induced ulcer by oral route. The gastroprotection was accompanied by normalization of superoxide dismutase, catalase and glutathione-S-transferase activities and reduction in myeloperoxidase activity. Moreover, the compounds 4 and 5 increased the gastric mucin content and 1 reduced TNF amount. Furthermore, 1, 3, 4 and 5 decreased volume, pH, total acidity and pepsin activity of the gastric juice from rats. CONCLUSIONS: Together, our findings showed a diversified mode of action elicited by 1, 3, 4 and 5 on the gastroprotection and contribute to explain the anti-ulcer activity reported for BGP.
Subject(s)
Anti-Ulcer Agents/therapeutic use , Propolis/chemistry , Stomach Ulcer/drug therapy , Animals , Cinnamates/therapeutic use , Ethanol , Flavonoids/therapeutic use , Hydrochloric Acid , Indomethacin , Kaempferols/therapeutic use , Male , Mice , Phenylpropionates/therapeutic use , Propolis/therapeutic use , Stomach Ulcer/chemically inducedABSTRACT
OBJECTIVES: To examine whether the hydroalcoholic extract from Baccharis dracunculifolia leaves (BdE) modulates the human neutrophil oxidative metabolism, degranulation, phagocytosis and microbial killing capacity. METHODS: In-vitro assays based on chemiluminescence, spectrophotometry, flow cytometry and polarimetry were used, as well as docking calculations. KEY FINDINGS: At concentrations that effectively suppressed the neutrophil oxidative metabolism elicited by soluble and particulate stimuli (<10 µg/ml), without clear signs of cytotoxicity, BdE (1) inhibited NADPH oxidase and myeloperoxidase activity; (2) scavenged H2 O2 and HOCl; (3) weakly inhibited phagocytosis; and (4) did not affect neutrophil degranulation and microbial killing capacity, the expression levels of TLR2, TLR4, FcγRIIa, FcγRIIIb and CR3 and the activity of elastase and lysozyme. Caffeic acid, one of the major B. dracunculifolia secondary metabolites, did not inhibit phagocytosis but interfered in the myeloperoxidase-H2 O2 -HOCl system by scavenging H2 O2 and HOCl, and interacting with the catalytic residues His-95, Arg-239 and Gln-91. CONCLUSIONS: BdE selectively modulates the effector functions of human neutrophils, inhibits the activity of key enzymes and scavenges physiological oxidant species. Caffeic acid contributes to lower the levels of oxidant species. Our findings help to unravel the mechanisms by which these natural products exert immunomodulatory action towards neutrophils.
Subject(s)
Baccharis/chemistry , Immunologic Factors/pharmacology , Neutrophils/drug effects , Plant Extracts/pharmacology , Adult , Caffeic Acids/isolation & purification , Caffeic Acids/pharmacology , Flow Cytometry , Free Radical Scavengers/isolation & purification , Free Radical Scavengers/pharmacology , Humans , Immunologic Factors/isolation & purification , Luminescence , Neutrophils/metabolism , Phagocytosis/drug effects , Plant Leaves , SpectrophotometryABSTRACT
Copaiba oleoresins are used in alternative medicine as anti-inflammatory, antitumoral, and antimicrobial treatments. (-)-Copalic acid (CA) is the major diterpene found in exudates from Copaifera species. We have examined the genotoxicity and the chemopreventive potential of Copaifera multijuga oleoresin (CM) and CA. Genotoxicity assessment was examined with the peripheral blood micronucleus test and the comet assay (male Swiss mouse hepatocytes). In the chemoprevention study, we evaluated the effects of CM and CA on the formation of 1,2-dimethylhydrazine (DMH)-induced aberrant crypt foci (ACF) in male Wistar rat colon. Neither agent caused a significant increase in micronucleus frequency relative to controls, but the highest CM dose tested (400mg/kg b.w.) caused DNA damage in the comet assay. Both agents significantly reduced the frequency of DMH-induced ACF. Both CM and CA suppressed ACF formation and may have a protective effect against colon carcinogenesis.
Subject(s)
Anticarcinogenic Agents/pharmacology , DNA Damage , Diterpenes/pharmacology , Fabaceae/chemistry , Micronuclei, Chromosome-Defective/chemically induced , Plant Extracts/pharmacology , Aberrant Crypt Foci/prevention & control , Animals , Anticarcinogenic Agents/isolation & purification , Anticarcinogenic Agents/toxicity , Colonic Neoplasms/prevention & control , Comet Assay , Diterpenes/isolation & purification , Diterpenes/toxicity , Dose-Response Relationship, Drug , Hepatocytes/drug effects , Hepatocytes/pathology , Male , Mice , Plant Extracts/isolation & purification , Plant Extracts/toxicity , Rats, WistarABSTRACT
This article reports on the in vitro activity of the hydroalcoholic extract of Pfaffia glomerata roots, its hydrolyzed fractions, and pfaffic acid against Trypanosoma cruzi. The hydroalcoholic extract obtained from dried, milled P. glomerata roots was submitted to acid hydrolysis followed by partition with CHCl3 . The concentrated CHCl3 fraction was suspended in MeOH/H2 O and partitioned with hexane (F1), CHCl3 (F2), and AcOEt (F3), in this sequence. The trypanocidal activity of the hydrolyzed extract and its fractions was evaluated in vitro. The hydroalcoholic extract displayed low activity, but fraction F1 was active against trypomastigotes of the Y strain of T. cruzi, with IC50 = 47.89 µg/ml. The steroids campesterol (7.7%), stigmasterol (18.7%), ß-sitosterol (16.8%), Δ7 -stigmastenol (4.6%), and Δ7 -spinasterol (7.5%) were the major constituents of F1, along with fatty acid esters (7.6%) and eight aliphatic hydrocarbons (30.1%). Fractions F2 and F3 exhibited moderate activity, and pfaffic acid, one of the main chemical constituents of these fractions, displayed IC50 = 44.78 µm (21.06 µg/ml). On the other hand, the hydroalcoholic extract of P. glomerata roots, which is rich in pfaffosides, was inactive. Therefore, the main aglycone of pfaffosides, pfaffic acid, is much more active against trypomastigotes of the Y strain of T. cruzi than its corresponding glycosides and should be further investigated.
Subject(s)
Amaranthaceae/chemistry , Plant Extracts/pharmacology , Triterpenes/pharmacology , Trypanocidal Agents/pharmacology , Trypanosoma cruzi/drug effects , Chemical Fractionation , Hydrolysis , Plant Extracts/isolation & purification , Plant Roots/chemistry , Triterpenes/isolation & purification , Trypanocidal Agents/isolation & purificationABSTRACT
Solanum cernuum Vell is a Brazilian shrub or small tree, restricted to Southeast states of the country. The leaves are commercialized as "panacéia" and indicated for the treatment of urinary disorders, gonorrhea, scabies, skin diseases and as desobstruent, diuretic and antiarrhythmic. The hydroalcholic extract is active in the treatment of gastric ulcer. The aim of this study was to evaluate the genotoxic and antigenotoxic potential of S. cernuum hydroalcoholic extract (SC) in Swiss mice by micronucleus and comet assays. The animals were treated by gavage with the doses of 500, 1000 and 2000mg/kg body weight (b.w.). For antigenotoxicity assessment, the doses of 15, 30, 60, 120 and 240mg/kg b.w SC were administered simultaneously with the mutagen methyl methanesulfonate (MMS, 40mg/kg b.w., i.p.). The results showed that the SC was not genotoxic in both micronucleus and comet assays. On the other hand, the treatment with the lowest dose of SC (15mg/kg b.w.) plus MMS showed a statistically significant reduction in the frequency of micronuclei compared to treatment only with MMS. For the comet assay, significant reduction in extensions of DNA damage was observed in all treatments with SC combined with MMS in comparison with only MMS. The antigenotoxic activity observed for the SC may be due to the antioxidant potential of the compounds present in the extract such as guanidine alkaloids and flavonoids.
Subject(s)
Chromosomes, Mammalian/metabolism , DNA Damage/genetics , Genome , Methyl Methanesulfonate/toxicity , Plant Extracts/pharmacology , Protective Agents/pharmacology , Solanum/chemistry , Animals , Chromatography, High Pressure Liquid , Hepatocytes/drug effects , Hepatocytes/pathology , Male , Mice , Plant Leaves/chemistryABSTRACT
The oral cavity, which harbors more than 750 bacterial species, is one of the most diverse sites of the human body. Some of these bacteria have been associated with oral diseases, such as dental caries and endodontic infections. We report on the antimicrobial and cytotoxic activities of Copaifera oblongifolia oleoresin against bacteria that cause caries and endodontic infections. The aim of this study is to determine the minimum (MIC) and the bactericidal (MBC) inhibitory concentrations as well as the biofilm inhibition ability (through determination of MBIC50) of the C. oblongifolia oleoresin. This study also investigated the bactericidal kinetics (time-kill curves) and the synergistic effect of the C. oblongifolia oleoresin. Additionally, this study evaluated the cytotoxic activity of the oleoresin toward V79 cells by means of the colony-forming assay. The C. oblongifolia oleoresin gave promising MIC and MBC values, which ranged from 25 to 200 µg/mL. Analysis of the MBIC50values of the oleoresin revealed it displayed biofilm inhibitory activity against all the assayed bacteria. Analysis of the bactericidal kinetics showed different behaviors of the oleoresin against the tested bacteria at the different time intervals and concentrations assayed in this study. An additive effect of the oleoresin with chlorhexidine dihydrochloride occurred only for S. mitis and A. actinomycetemcomitans. The C. oblongifolia oleoresin showed cytotoxic activity at concentrations ≥ 625 µg/mL.
Subject(s)
Anti-Bacterial Agents/pharmacology , Bacteria/drug effects , Biofilms/drug effects , Fabaceae/physiology , Plant Extracts/chemistry , Chlorhexidine/administration & dosage , Chlorhexidine/pharmacology , Dental Caries/microbiology , Dental Caries/prevention & control , Humans , Microbial Sensitivity Tests , Mouth Diseases/microbiology , Mouth Diseases/prevention & control , Mouthwashes/administration & dosage , Mouthwashes/pharmacologyABSTRACT
Despite reports on the pharmacological potential of Copaifera langsdorffii Desf. (Leguminosae-Caesalpinioideae) leaf extract, little is known about its chemical composition. In this work, a phytochemical study from the C. langsdorffii ethanol/H2O 7:3 (v/v) extract was undertaken. Separation was performed by high-speed counter-current (HSCCC) and Sephadex LH-20 column chromatographies, followed by preparative HPLC. The EtOAc- and H2O-soluble fractions of the extract furnished the flavonoids quercitrin (1) and afzelin (2) and 3-O-(3-O-methyl-galloyl)quinic acid (3), respectively. The H2O-soluble fraction furnished 3,4-di-O-(3-O-methyl-galloyl)quinic acid (4), 3,5-di-O-(galloyl)-4-O-(3-O-methyl-galloyl)quinic acid (5), and 3,5-di-O-(3-O-methyl-galloyl)-4-O-(galloyl)quinic acid (6). Their chemical structures were elucidated by NMR means.
Subject(s)
Fabaceae/chemistry , Flavonoids/chemistry , Plant Extracts/chemistry , Plant Leaves/chemistry , Quinic Acid/chemistry , Flavonoids/isolation & purification , Molecular Structure , Plant Extracts/isolation & purification , Quinic Acid/isolation & purificationABSTRACT
BACKGROUND: Oral mucositis is a common inflammatory complication among patients undergoing hematopoietic stem cell transplantation (HSCT). Among its therapeutic properties, Chamomilla recutita has anti-inflammatory effects. OBJECTIVE: The aim of this study was to identify the dosage of the liquid extract of C recutita in mouthwash that is needed to reduce the incidence and intensity of oral mucositis in adult patients undergoing allogenic HSCT. METHODS: In a randomized phase II clinical trial, 40 patients were randomized to receive routine care plus mouthwash containing a liquid extract of C recutita at 0.5%, 1%, or 2% (experimental groups) or standard care alone (control group). Daily evaluation was performed using the measurement scale for oral toxicity defined by the World Health Organization. Statistical analysis was performed, in which the incidence, intensity, and duration of oral mucositis were compared between each experimental group and the control group. RESULTS: The experimental group at the 1% dosage demonstrated reduced incidence, intensity, and duration of oral mucositis compared with the control group. The formulation was well tolerated by patients and was safe, as no moderate or severe adverse effects were identified. CONCLUSIONS: In this study, the use of mouthwash containing 1% C recutita extract can be associated with reduced incidence, intensity, and duration of mucositis in adults patients undergoing allogenic HSCT. IMPLICATIONS FOR PRACTICE: The results of this investigation will help nurses and other professionals in selecting the C recutita dosage used to manage oral mucositis in patients undergoing HSCT.