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1.
Pharmaceutics ; 15(10)2023 Sep 28.
Article in English | MEDLINE | ID: mdl-37896161

ABSTRACT

Valencene and nootkatone are aromatic sesquiterpenes with known biological activities, such as antimicrobial, antioxidant, anti-inflammatory, and antitumor. Given the evidence that encapsulation into nanosystems, such as liposomes, could improve the properties of several compounds, the present study aimed to evaluate the activity of these sesquiterpenes in their isolated state or in liposomal formulations against strains of Staphylococcus aureus carrying efflux pumps. The broth microdilution method evaluated the antibiotic-enhancing activity associated with antibiotics and ethidium bromide (EtBr). The minimum inhibitory concentration was assessed in strains of S. aureus 1199B, IS-58, and RN4220, which carry the efflux proteins NorA, Tet(K), and MsrA. In tests with strain 1199B, valencene reduced the MIC of norfloxacin and EtBr by 50%, while the liposomal formulation of this compound did not show a significant effect. Regarding the strain IS-58, valencene, and its nanoformulation reduced norfloxacin MIC by 60.3% and 50%, respectively. In the non-liposomal form, the sesquiterpene reduced the MIC of EtBr by 90%. Against the RN4220 strain, valencene reduced the MIC of the antibiotic and EtBr by 99% and 93.7%, respectively. Nootkatone and its nanoformulation showed significant activity against the 1199B strain, reducing the EtBr MIC by 21.9%. Against the IS-58 strain, isolated nootkatone reduced the EtBr MIC by 20%. The results indicate that valencene and nootkatone potentiate the action of antibiotics and efflux inhibitors in strains carrying NorA, Tet(K), and MsrA proteins, which suggests that these sesquiterpenes act as efflux pump inhibitors in S. aureus. Therefore, further studies are needed to assess the impact of incorporation into liposomes on the activity of these compounds in vivo.

2.
Molecules ; 28(15)2023 Jul 26.
Article in English | MEDLINE | ID: mdl-37570622

ABSTRACT

The use of medicinal plants to treat inflammatory conditions and painful processes has attracted the attention of scientists and health professionals due to the evidence that natural products can promote significant therapeutic benefits associated with fewer adverse effects compared to conventional anti-inflammatory drugs. The genus Plectranthus is composed of various plants with pharmacological potential, which are used to treat various diseases in traditional communities worldwide. The present study systematically reviewed Plectranthus species with anti-inflammatory and analgesic potential. To this end, a systematic review was conducted following the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) protocol. The search was conducted on the following databases: PubMed, ScienceDirect, SciVerse Scopus, and Web of Science. Different combinations of search terms were used to ensure more excellent article coverage. After the selection, a total of 45 articles were included in this review. This study identified twelve Plectranthus species indicated for the treatment of different inflammatory conditions, such as wounds, fever, bronchitis, abscess, asthma, hepatitis, labyrinthitis, tonsillitis, and uterine inflammation. The indications for pain conditions included headache, sore throat, heartburn, menstrual cramp, colic, toothache, stomachache, migraine, chest pain, abdominal pain, local pain, labor pain, and recurring pain. Among the listed species, ten plants were found to be used according to traditional knowledge, although only four of them have been experimentally studied. When assessing the methodological quality of preclinical in vivo assays, most items presented a risk of bias. The SR results revealed the existence of different Plectranthus species used to treat inflammation and pain. The results of this systematic review indicate that Plectranthus species have the potential to be used in the treatment of diseases with an inflammatory component, as well as in the management of pain. However, given the risk of biases, the experimental analysis of these species through preclinical testing is crucial for their safe and effective use.


Subject(s)
Phytotherapy , Plectranthus , Female , Pregnancy , Humans , Ethnopharmacology , Abdominal Pain , Analgesics/pharmacology , Analgesics/therapeutic use , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Inflammation , Phytochemicals
3.
Plants (Basel) ; 12(12)2023 Jun 19.
Article in English | MEDLINE | ID: mdl-37376002

ABSTRACT

Antimicrobial resistance has become a growing public health concern in recent decades, demanding a search for new effective treatments. Therefore, this study aimed to elucidate the phytochemical composition and evaluate the antibacterial activity of the essential oil obtained from the fruits of Piper tuberculatum Jacq. (EOPT) against strains carrying different mechanisms of antibiotic resistance. Phytochemical analysis was performed using gas chromatography-mass spectrometry (GC/MS). The antibacterial activity of EOPT and its ability to inhibit antibiotic resistance was evaluated through the broth microdilution method. The GC-MS analysis identified 99.59% of the constituents, with ß-pinene (31.51%), α-pinene (28.38%), and ß-cis-ocimene (20.22%) being identified as major constituents. The minimum inhibitory concentration (MIC) of EOPT was determined to assess its antibacterial activity against multidrug-resistant strains of Staphylococcus aureus (IS-58, 1199B, K2068, and K4100). The compound showed a MIC of ≥ 1024 µg/mL, suggesting a lack of intrinsic antibacterial activity. However, when the EOPT was associated with antibiotics and EtBr, a significant decrease in antibiotic resistance was observed, indicating the modulation of efflux pump activity. This evidence was corroborated with the observation of increased fluorescent light emission by the bacterial strains, indicating the involvement of the NorA and MepA efflux pumps. Additionally, the significant potentiation of ampicillin activity against the S. aureus strain K4414 suggests the ß-lactamase inhibitory activity of EOPT. These results suggest that the essential oil from P. tuberculatum fruits has antibiotic-enhancing properties, with a mechanism involving the inhibition of efflux pumps and ß-lactamase in MDR S. aureus strains. These findings provide new perspectives on the potential use of EOPT against antibiotic resistance and highlight the importance of Piper species as sources of bioactive compounds with promising therapeutic activities against MDR bacteria. Nevertheless, further preclinical (in vivo) studies remain necessary to confirm these in vitro-observed results.

4.
Plants (Basel) ; 12(8)2023 Apr 17.
Article in English | MEDLINE | ID: mdl-37111898

ABSTRACT

Species belonging to the genus Lippia are used worldwide as foods, beverages, and seasonings. Studies have demonstrated that these species have antioxidant, sedative, analgesic, anti-inflammatory, and antipyretic activities. This work aimed to evaluate the antibacterial activity and anxiolytic effect by different pathways of essential oils and ethanolic extracts of three species of Lippia (Lippia alba, Lippia sidoides, and Lippia gracilis). The ethanolic extracts were characterized by HPLC-DAD-ESI-MSn and their phenolics were quantified. The antibacterial activity was evaluated by determining the minimal inhibitory concentration and modulation of antibiotic activity, and toxic and anxiolytic effects were evaluated in the zebrafish model. The extracts showed compositions with a low ratio and shared compounds. L. alba and L. gracilis showed higher amounts of phenols and flavonoids, respectively. All extracts and essential oils presented antibacterial activity, especially those obtained from L. sidoides. On the other hand, L. alba extract presented the most significant antibiotic-enhancing effect. The samples were not toxic after 96 h of exposure, but showed an anxiolytic effect through modulation of the GABAA receptor, while L. alba extract acted via modulation of the 5-HT receptor. This new pharmacological evidence opens horizons for therapeutic approaches targeting anxiolytic and antibacterial therapies and food conservation using these species and their constituents.

5.
J Cereb Blood Flow Metab ; 42(12): 2175-2187, 2022 12.
Article in English | MEDLINE | ID: mdl-35891578

ABSTRACT

Post-traumatic stress disorder (PTSD) is an anxiety disorder with manifestations somatic resulting from reliving the trauma. The therapy for the treatment of PTSD has limitations, between reduced efficacy and "PTSD pharmacotherapeutic crisis". Scientific evidence has shown that the use of ketamine has benefits for the treatment of depressive disorders and other symptoms present in PTSD compared to other conventional therapies. Therefore, this study aims to analyze the available evidence on the effect of ketamine in the treatment of post-traumatic stress. The systematic review and the meta-analysis were conducted following PRISMA guidelines and RevManager software, using randomized controlled trials and eligible studies of quality criteria for data extraction and analysis. The sample design evaluated included the last ten years, whose search resulted in 594 articles. After applying the exclusion criteria, 35 articles were selected, of which 14 articles were part of the sample, however, only six articles were selected the meta-analysis. The results showed that the ketamine is a promising drug in the management of PTSD with effect more evident performed after 24 h evaluated by MADRS scale. However, the main limitations of the present review demonstrate that more high-quality studies are needed to investigate the influence of therapy, safety, and efficacy.


Subject(s)
Cognitive Behavioral Therapy , Ketamine , Stress Disorders, Post-Traumatic , Humans , Stress Disorders, Post-Traumatic/drug therapy , Stress Disorders, Post-Traumatic/diagnosis , Psychotherapy/methods , Ketamine/therapeutic use , Cognitive Behavioral Therapy/methods
6.
Chem Biol Interact ; 359: 109890, 2022 May 25.
Article in English | MEDLINE | ID: mdl-35318036

ABSTRACT

Eugenol (EUG) is a phenylpropanoid widely used in the food and cosmetic industries. It is commonly referred to in the literature by its biological activities such as antioxidant, anti-inflammatory, antimicrobial, and relaxing in organs of laboratory animals, especially in rodent vessels. However, its vasorelaxant potential in human tissue, has not been investigated. Thus, this study characterizes the vasodilatory effect of EUG in the human umbilical artery (HUA). HUAs were isolated, cleaned, sectioned (3-4 mm) and placed in an organ bath (10 mL Krebs Henseleit, 37 °C; and carbogenic mixture). EUG (100-1400 µM), obtained total relaxation of electromechanical contractions induced by KCl (60 mM), and pharmacomechanical contractions (30-1200 µM), induced by serotonin (10 µM) and by histamine (10 µM), showing statistically significant concentrations: 600 µM, 400 µM and 200 µM, and EC50 values: 759.8 ± 6.5 µM, 229.9 ± 7.9 and 279.0 ± 3.4 µM, respectively. EUG (1200 and 1400 µM) prevented the contraction promoted by BaCl2 (0.1-30 mM), similar to the effects of nifedipine (10 µM), sugesting the involvement of EUG in blocking VOCCs. In the presence of tetraethylammonium (10 µM), EUG (30-1200 µM) did not produce a total relaxation (88.6%), suggesting that an alternative pathway where potassium channels, may partially mediate EUG effect. In the presence of 4-aminopyridine (1 mM), glibenclamide (10 µM), and tetraethylammonium (1 mM), EUG relaxed HUAs 100%, although the pharmacological potency was statistically altered, demonstrating the participation of K+ channels (Kv, KATP, BKCa). Our data indicates that EUG has a vasorelaxant effect on HUAs, had a greater pharmacological potency in the serotoninergic pathway, showing effective participation of VOCCs and a partial modulation of K+ channels. These data suggest new possibilities for the use of EUG in human vascular dysfunctions, such as preeclampsia. More studies are necessary to confirm the safety and effectivity in future treatments.


Subject(s)
Eugenol , Vasodilator Agents , Animals , Arteries , Eugenol/pharmacology , Humans , Tetraethylammonium/pharmacology , Umbilical Cord , Vasodilation , Vasodilator Agents/pharmacology
9.
Biology (Basel) ; 9(6)2020 May 30.
Article in English | MEDLINE | ID: mdl-32486128

ABSTRACT

Croton rhamnifolioides is used in popular medicine for the treatment of inflammatory diseases. The objective of this study was to characterize and evaluate the anti-inflammatory effect of C. rhamnifolioides essential oil complexed in ß-cyclodextrin (COEFC). The physicochemical characterization of the complexes was performed using different physical methods. The anti-inflammatory activity was evaluated in vivo by ear edema, paw edema, cotton pellet-induced granuloma, and vascular permeability by Evans blue extravasation. The mechanism of action was validated by molecular docking of the major constituent into the cyclooxygenase-2 (COX-2 enzyme). All doses of the COEFC reduced acute paw edema induced by carrageenan and dextran, as well as vascular permeability. Our results suggest the lowest effective dose of all samples inhibited the response induced by histamine or arachidonic acid as well as the granuloma formation. The complexation process showed that the pharmacological effects were maintained, however, showing similar results using much lower doses. The results demonstrated an involvement of the inhibition of pathways dependent on eicosanoids and histamine. Complexation of ß-cyclodextrin/Essential oil (ß-CD/EO) may present an important tool in the study of new compounds for the development of anti-inflammatory drugs.

10.
Molecules ; 25(11)2020 Jun 09.
Article in English | MEDLINE | ID: mdl-32527034

ABSTRACT

Carveol is a monoterpene present in the structure of many plant products. It has a variety of biological activities: antioxidant, anticancer and vasorelaxation. However, studies investigating the effect of monoterpenoids on human vessels have not yet been described. Thus, the present study aimed to characterize the effect of (-)-carveol on human umbilical arteries (HUAs). HUA ring preparations were isolated and subjected to isometric tension recordings of umbilical artery smooth muscle contractions. (-)-Carveol exhibited a significant vasorelaxant effect on KCl and 5-HT-induced contractions, obtaining EC50 values of 344.25 ± 8.4 and 175.82 ± 4.05 µM, respectively. The participation of calcium channels in the relaxation produced by (-)-carveol was analyzed using vessels pre-incubated with (-)-carveol (2000 µM) in a calcium-free medium, where the induction of contractions was abolished. The vasorelaxant effect of (-)-carveol on HUAs was reduced by tetraethylammonium (TEA), which increased the (-)-carveol EC50 to 484.87 ± 6.55 µM. The present study revealed that (-)-carveol possesses a vasorelaxant activity in HUAs, which was dependent on the opening of calcium and potassium channels. These results pave the way for further studies involving the use of monoterpenoids for the vasodilatation of HUAs. These molecules have the potential to treat diseases such as pre-eclampsia, which is characterized by resistance in umbilical arteries.


Subject(s)
Calcium Channels/physiology , Cyclohexane Monoterpenes/pharmacology , Endothelium, Vascular/drug effects , Potassium Channels/physiology , Umbilical Arteries/drug effects , Vasodilation/drug effects , Vasodilator Agents/pharmacology , Calcium Channels/drug effects , Endothelium, Vascular/metabolism , Female , Humans , Potassium Channels/drug effects , Umbilical Arteries/metabolism
11.
Infect Genet Evol ; 84: 104370, 2020 10.
Article in English | MEDLINE | ID: mdl-32445918

ABSTRACT

Isolated substances and those organically synthesized have stood out over the years for their therapeutic properties, including their antibacterial activity. These compounds may be an alternative to the production of new antibiotics or may have the ability to potentiate the action of preexisting ones. In this context, the objective of this study was to evaluate the in vitro antibacterial and efflux pump inhibitory activity of hydroxyamines derived from lapachol and norlachol, more specifically the compounds 2-(2-Hydroxyethylamino)-3-(3-methyl-2-butenyl)-1,4 dihydro-1,4-naphthalenedione, 2-(2-Hydroxyethylamino)-3-(2-methyl-propenyl)[1,4]naphthoquinone and 2-(3-Hydroxypropylamino)-3-(3-methyl-2-butenyl)-[1,4]naphthoquinone, against Staphylococcus aureus strains carrying the NorA efflux pump mechanism. The substances were synthesized from 2-hydroxy-quinones, lapachol and nor-lapachol, obtaining the corresponding 2-methoxylated derivatives via dimethyl sulfate alkylation in a basic medium, which then reacted chemoselectively with 2-ethanolamine and 3-propanolamine to form the corresponding amino alcohols. All three molecules underwent a virtual structure-based analysis (docking). The antibacterial activity of the substances was measured by determining their Minimum Inhibitory Concentration (MIC) and a microdilution assay was performed to verify efflux pump inhibition using the substances at a sub-inhibitory concentration. The results were subjected to statistical analysis using an analysis of variance (ANOVA) followed by Bonferroni's post hoc test. The substances obtained MIC values ≥1024 µg/mL, however, a significant reduction of their MICs was observed when the substances were associated with norfloxacin and ethidium bromide, with this effect being attributed to efflux pump inhibition. Following a virtual analysis based on its structure (docking), information regarding the affinity of new ligands for the ABC efflux pump were observed, thus contributing to the understanding of their mechanism of molecular interactions and the discovery of functional ligands associated with a reduction in bacterial resistance.


Subject(s)
Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Bacterial Proteins/antagonists & inhibitors , Multidrug Resistance-Associated Proteins/antagonists & inhibitors , Staphylococcus aureus/drug effects , Anti-Bacterial Agents/chemical synthesis , Bacterial Proteins/chemistry , Bacterial Proteins/genetics , Computer Simulation , Drug Evaluation, Preclinical , Microbial Sensitivity Tests , Molecular Docking Simulation , Multidrug Resistance-Associated Proteins/chemistry , Multidrug Resistance-Associated Proteins/genetics , Naphthoquinones/chemistry , Norfloxacin/chemistry , Norfloxacin/pharmacology , Staphylococcus aureus/genetics
12.
Food Chem ; 325: 126923, 2020 May 01.
Article in English | MEDLINE | ID: mdl-32387952

ABSTRACT

This study aimed to investigate the myorelaxant action of the Dysphania ambrosioides essential oil (EODa) and its major constituent α-terpinene on tracheal smooth muscle isolated from rats. In tracheal smooth muscle ex vivo, in organ baths, isometric contractions recordings were done in order to evaluated the effect of EODa (1-1000 µg/mL) and α-terpinene (1-3000 µg/mL) on the following parameters: basal tone, contractions evoked by potassium (KCl 60 mM), acetylcholine (ACh 10 µM) or serotonin (5-HT 10 µM). The EODa and its major constituent α-terpinene, did not statistically alter basal tone; however, they induced myorelaxant effects on top of contractions induced by KCl, ACh and 5-HT. EODa and α-terpinene also inhibited the contractions induced by barium in presence of High [K+] (80 mM). The data suggest that the relaxation induced by these agents is caused by the inhibition of L-type VGCC, inhibiting the inward Ca2+ current through these channels, but does not exclude the possibility of participation of other mechanisms. Results from this study also suggest the EODa, due to their efficacy on relaxation of the respiratory tract, posses a therapeutic potential as a antispasmodic agent for respiratory tract.

13.
Antibiotics (Basel) ; 9(1)2020 Jan 14.
Article in English | MEDLINE | ID: mdl-31947642

ABSTRACT

Efflux pumps are proteins present in the plasma membrane of bacteria, which transport antibiotics and other compounds into the extracellular medium, conferring resistance. The discovery of natural efflux pump inhibitors is a promising alternative. α-Bisabolol is a sesquiterpene isolated from several plants such as Matricaria chamomilla L. and has important properties such as antibacterial and anti-inflammatory activity. Currently, the formation of inclusion complexes with ß-Cyclodextrin has been used for improving the physicochemical characteristics of the host molecule. This study evaluated the effect of α-Bisabolol, in isolation and in complexation with ß-Cyclodextrin, as TetK and NorA efflux pump inhibitors in Staphylococcus aureus strains. The minimum inhibitory concentration (MIC) was determined. Subsequently, inhibitory activity over the pumps was observed by an MIC reduction for the antibiotics, by using subinhibitory concentrations (MIC/8) in combination with tetracycline and norfloxacin. The MIC of the compounds was ≥1024 µg/mL. α-Bisabolol potentiated the action of tetracycline and reduced the MIC of norfloxacin to a clinically relevant concentration. The complexed substance showed synergism however, the effect of the isolated α-Bisabolol was superior to the complex. These results indicate α-Bisabolol is a potential substance to be used as an efflux pump inhibitor.

14.
Biomed Pharmacother ; 92: 554-561, 2017 Aug.
Article in English | MEDLINE | ID: mdl-28577494

ABSTRACT

The increase in microorganisms with resistance to medications has caused a strong preoccupation within the medical and scientific community. Animal toxins studies, such as parotoid glandular secretions from amphibians, possesses a great potential in the development of drugs, such as antimicrobials, as these possess bioactive compounds. It was evaluated Rhinella jimi (Stevaux, 2002) glandular secretions against standard and multi-resistant bacterial strains; the effect of secretions combined with drugs; and determined the toxicity using two biologic in vivo models, and a in vitro model with mice livers. Standard strains were used for the determination of the Minimum Inhibitory Concentration (MIC), while for the modulatory activity of antibiotics, the clinical isolates Escherichia coli 06, Pseudomonas aeruginosa 03 and Staphylococcus aureus 10 were used. Modulatory activity was evaluated by the broth microdilution method with aminoglycosides and ß-lactams as target antibiotics. The secretions in association with the antibiotics have a significant reduction in MIC, both the aminoglycosides and ß-lactams. The toxicity and cytotoxicity results were lower than the values used in the modulation. R. jimi glandular secretions demonstrated clinically relevant results regarding the modulation of the tested antimicrobials.


Subject(s)
Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/pharmacology , Biological Products/isolation & purification , Biological Products/pharmacology , Bufonidae , Parotid Gland/metabolism , Animals , Anti-Bacterial Agents/toxicity , Artemia , Biological Products/toxicity , Dose-Response Relationship, Drug , Drosophila melanogaster , Escherichia coli/drug effects , Female , Male , Mice , Microbial Sensitivity Tests/methods , Pseudomonas aeruginosa/drug effects , Staphylococcus aureus/drug effects
15.
Biomed Pharmacother ; 92: 1111-1118, 2017 Aug.
Article in English | MEDLINE | ID: mdl-28622712

ABSTRACT

The present study aimed to evaluate the antibacterial and modulatory potential of α-bisabolol, ß-cyclodextrin and α-bisabolol/ß-cyclodextrin complex. The minimum inhibitory concentration was determined through the broth microdilution technique using the bacterial strains: Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. The drugs norfloxacin, imipenem and gentamicin were used in the tests, and the compounds α-bisabolol and ß-cyclodextrin; all the compounds were diluted in DMSO. To obtain the minimum inhibitory concentration (MIC) a serial microdilution of the substances in volumes corresponding to the sub-inhibitory concentration (MIC/8), and microdilution with the antibiotic until the penultimate well were performed. The results showed that ß-cyclodextrin did not present synergistic effects when combined with the antibiotics. It was found that α-bisabolol presented a synergistic effect against S. aureus, when combined with the antibiotic norfloxacin. Moreover, α-bisabolol presented synergism against E. coli when combined with gentamicin. The results of this study show that α-bisabolol presents a modulatory synergistic effect for some antibiotics, as gentamicin, and this is an interesting result against multidrug resistant bacteria (MDR). By other side, the complexation of α-bisabolol with ß-cyclodextrin apparently reduces the modulatory effect, maybe due the polarity enhancement of the polarity of α-bisabolol, affecting the interaction of this compound with the cell membrane bilayer. However, more studies are necessary to demonstrate or not these interactions.


Subject(s)
Anti-Bacterial Agents/pharmacology , Sesquiterpenes/pharmacology , alpha-Cyclodextrins/pharmacology , beta-Cyclodextrins/pharmacology , Anti-Bacterial Agents/chemistry , Drug Compounding , Drug Resistance, Multiple, Bacterial , Drug Synergism , Escherichia coli/drug effects , Escherichia coli/growth & development , Gentamicins/pharmacology , Microbial Sensitivity Tests , Monocyclic Sesquiterpenes , Norfloxacin/pharmacology , Pseudomonas aeruginosa/drug effects , Pseudomonas aeruginosa/growth & development , Sesquiterpenes/chemistry , Staphylococcus aureus/drug effects , Staphylococcus aureus/growth & development , alpha-Cyclodextrins/chemistry , beta-Cyclodextrins/chemistry
16.
Biosci. j. (Online) ; 32(6): 1632-1643, nov./dec. 2016. tab, graf
Article in English | LILACS | ID: biblio-965822

ABSTRACT

The species Croton rhamnifolioides is a shrub popularly known as "quebra faca", utilized in teas or infusions for the treatment of gastrointestinal disorders as ulcers, gastric discomfort, vomiting and hemorrhagic diarrhea. This work has as its main objective to evaluate the chemical composition of the essential oil of the Croton rhamnifolioides leaves (EOC), antibacterial activity and modulatory activity of antibiotic resistance, against bacterial strains of Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa and, and antifungal activity against Candida albicans, Candida krusei and Candida tropicalis. The chemical composition was determined through chromatography with a gas phase coupled with mass spectrometry (CG/MS), whereas antimicrobial activity and modulation were determined by microdilution assay. The chemical composition of the oil revealed 21 compounds, with the major compounds being spathulenol (22.46%) and 1,8-cineol (18.32%). The antimicrobial activity was not significant with MIC>1024 µg/mL, however, was observed a synergistic interference when essential oil associated with the antibiotics aminoglycoside and -lactam, and the antifungal polyene.


Croton rhamnifolioides is é um arbusto conhecido popularmente como "quebra-faca" e utilizado como chá ou infusão para o tratamento de problemas gastro-intestinais como úlceras, desconforto gástrico, vômitos e diarréias hemorrágicas. O objetivo deste trabalho foi avaliar a composição química do óleo essencial das folhas de Croton rhamnifolioides (OEC), atividade antibacteriana, moduladora da resistência bacteriana, contra linhagens bacterianas de Escherichia coli, Staphylococcus aureus e Pseudomonas aeruginosa e, atividade antifúngica contra Candida albicans, C. krusei e C. tropicalis. A composição química foi determinada através de Espectroscopia de Massas acoplada a Cromatografia Gasosa (EM/CG), enquanto as atividades antimicrobianas e moduladoras foram determinadas pelo método de microdiluição. A composição química do OEC revelou a presença de 21 compostos, sendo os principais o Espatulenol (22,46%) e 1,8-cineol (18,32%). A atividade antimicrobiana não foi considerada significativa apresentando MIC > 1024 µg/mL, contudo, foi observado um sinergismo quando o óleo essencial foi associado com aminoglicosídios, -lactâmicos e antifúngicos poliênicos.


Subject(s)
Oils, Volatile , Croton/chemistry , Drug Resistance, Bacterial , Phytotherapy , Anti-Infective Agents
17.
Food Chem Toxicol ; 97: 297-306, 2016 Nov.
Article in English | MEDLINE | ID: mdl-27644596

ABSTRACT

1,8-cineole (eucalyptol) is widely used as an excipient in the pharmaceutical industry and as a food flavoring agent, thus providing significant potential for human exposure to the compound. We investigated the preclinical toxicity and reproductive toxicity of 1,8-cineole (CIN). In the repeated-doses toxicity study for 50 days, CIN (100, 500 or 1000 mg/kg) did not produce any signs of toxicity or deaths, but affected body weight gain during the first week of treatment. The hematological and biochemical profiles did not show significant differences except for increase in the MCV, platelet and urea levels or reduction in MCHC, MPV and alkaline phosphatase. Histopathological analysis showed weak changes in the lungs, liver, kidneys and uterus. In the reproductive toxicity, CIN (250, 500 or 1000 mg/kg) produced a reduction in body weight in pregnant rats treated during the pre-implantation or organogenesis periods. The highest doses induced a reduction in the mass of fetuses (pre-implantation) and dead fetuses (both periods) of pregnant rats. The results indicate that the treatment by repeated-doses showed occasional alterations in rats of both sexes. However, provide evidence that possibly 1,8-cineole presents maternal and fetal toxicity. This requires more detailed investigation to better characterize the toxic effects of this compound.


Subject(s)
Anti-Infective Agents/toxicity , Cyclohexanols/toxicity , Fetus/drug effects , Maternal Exposure/adverse effects , Monoterpenes/toxicity , Reproduction/drug effects , Toxicity Tests/methods , Animals , Body Weight/drug effects , Dose-Response Relationship, Drug , Eucalyptol , Female , Humans , Male , Organ Size/drug effects , Pregnancy , Rats , Rats, Wistar
18.
Revista Fitos Eletrônica ; 9(2): 101-112, 2015.
Article in Portuguese | MOSAICO - Integrative health | ID: biblio-881786

ABSTRACT

A utilização de plantas medicinais é uma prática comum nos países, fazendo parte da cultura popular como forma de tratamento de diferentes patologias. A planta Chenopodium ambrosioides L., conhecida popularmente como mastruz, é utilizada na medicina popular no tratamento de bronquite crônica, tuberculose, contusões, hérnias e fraturas, tendo algumas atividades comprovadas cientificamente como ação vermífuga e antimicrobiana. Dessa forma, o presente estudo teve como objetivo avaliar o perfil químico e investigar a atividade antibacteriana, moduladora de antibióticos e anti-inflamatória tópica do extrato metanólico obtido das folhas de Chenopodium ambrosioides L. Na prospecção fitoquímica do extrato, foram verificados diferentes metabólitos que possuem várias atividades biológicas, e na dosagem dos fenóis totais foram verificados 21,0 mg/g equivalente de ácido gálico, sendo a quantificação de flavonoides encontrado um total de 135,4 mg/g de quercetina. Não houve atividade antibacteriana, porém detectou-se modulação quando o extrato foi associado aos aminoglicosídeos contra cepas de E. coli e Staphylococcus aureus. Nos testes para inflamação aguda, o extrato apresentou um potencial antiedematogênico nas concentrações de 25 e 50 mg. Diante dos resultados, pode-se correlacionar o conhecimento empírico das pessoas, às propriedades biológicas observadas nessa pesquisa, esta podendo ser importante para futura validação dessas propriedades etnomedicinais.(AU)


The use of medicinal plants is a common practice in countries as part of popular culture as a treatment of different pathologies. The Chenopodium ambrosioides L. plant, popularly known as Mastruz, is used in folk medicine to treat chronic bronchitis, tuberculosis, bruises, fractures and hernias, and some activities scientifically proven as anthelmintic and antimicrobial action. Thus, this study aimed to evaluate the chemical profile and investigate the antibacterial activity, modulator of antibiotics and topical anti-inflammatory of methanol extract obtained from Chenopodium ambrosioides L. leaves. In the phytochemical extract prospecting, they were checked different metabolites that have multiple biological activity, and the dosage of total phenols were checked 21.0 mg / g gallic acid equivalent, and the quantification of flavonoids found a total of 135.4 mg / g quercetin. There was no antibacterial activity, but modulation was detected when the extract was associated with aminoglycosides against strains of E. coli and Staphylococcus aureus. In tests for acute inflammation, the extract showed an antiedematogenic potential at concentrations of 25 and 50 mg. Given the results, we can correlate the empirical knowledge of people; the biological properties observed in this study, this may be important for future validation of these ethnomedicinal properties.(AU)


Subject(s)
Humans , Animals , Male , Mice , Anti-Bacterial Agents/therapeutic use , Chenopodium ambrosioides/microbiology , Phytotherapy , Plant Extracts/therapeutic use , Chenopodium ambrosioides/chemistry , Flavonoids/chemistry , Models, Animal , Phenols/chemistry , Plant Extracts/chemistry
19.
J Ethnopharmacol ; 155(3): 1522-33, 2014 Sep 29.
Article in English | MEDLINE | ID: mdl-25086410

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Traditional medical systems represent an important source of knowledge about the use of biodiversity. Ethnobotanical and ethnopharmacological studies can encourage bioprospecting in the pursuit and selection of promising medicinal plants. This study investigated the diversity of medicinal plants in a disjunct area of cerrado in Chapada do Araripe, Ceará, Brazil, and assessed the species of interest for bioprospecting. MATERIALS AND METHODS: Structured and semi-structured interviews were conducted through free listing, and the informants were recruited using the "snowball" technique. The relative importance and informant consensus factor were analyzed for the selection of plant species with therapeutic potential. RESULTS: A total of 68 species were recorded and cited for 91 therapeutic purposes. Of these, 10 species showed great versatility of use, including Copaifera langsdorffii Desf., Caryocar coriaceum Wittn., Himatanthus drasticus (Mart.) Plumel, Stryphnodendron rotundifolium Mart., and Dimorphandra garderiana Tull. The therapeutic citations were grouped into 16 categories of body systems, of which Injuries, Poisonings and Other Consequences of External Causes, and Neoplasias showed the highest agreement of use. CONCLUSIONS: Regarding the diversity of the species, some including Tocoyena Formosa (Cham. & Schlecht.) Schum., Himatanthus drasticus, Caryocar coriaceum, Roupala montana Aubl. and Stryphnodendron rotundifolium showed both high relative importance and strong consensus among informants, and although many have already been investigated scientifically, others are almost unknown with respect to their medicinal properties and can be targets for bioprospecting.


Subject(s)
Plants, Medicinal , Adult , Aged , Aged, 80 and over , Brazil , Ethnobotany , Female , Health Knowledge, Attitudes, Practice , Humans , Male , Medicine, Traditional , Middle Aged , Young Adult
20.
REME rev. min. enferm ; 17(1): 76-84, jan.-mar. 2013.
Article in Portuguese | LILACS, BDENF - Nursing | ID: lil-684229

ABSTRACT

A utilização de plantas medicinais é bastante difundida em todo o mundo inclusive no Brasil, onde há grande variedade de espécies e extensa tradiçãoem sua utilização. Objetivou-se, com esta pesquisa, conhecer a percepção dos enfermeiros sobre o uso da fitoterapia na Estratégia Saúde da Família.Trata-se de estudo descritivo exploratório, de abordagem qualitativa, desenvolvido em Crato-CE, com 15 enfermeiros. Empregou-se o método deanálise temático-categorial. Foram construídas seis categorias e duas subcategorias, nas quais foram descritos o conhecimento dos profissionais sobrea fitoterapia, a visão deles sobre o uso na atenção básica, a utilização dessa prática e as estratégias desenvolvidas para seu uso. Os resultados revelaramque o conhecimento dos entrevistados é, na maioria das vezes, restrito e informal e que eles encontram dificuldades para a implantação de práticasfitoterápicas, como a não valorização por parte da gestão e do restante da equipe de saúde. Ressalte-se assim, a importância do desenvolvimento deestratégias que viabilizem a inserção segura e eficiente da fitoterapia na assistência e, consequentemente, a valorização da cultura local.


The use of medicinal plants is widespread around the world including Brazil, where there are several species and a large tradition in their use. It wasaimed to know the perception of the nurses about the use of phytotherapy in Health Family Strategy (HFS). Exploratory descriptive study, qualitativeapproach, developed in Crato-CE with fifteen nurses from HFS. It was employed the Theme-Category Analysis. It were constructed six categories and twosubcategories which were described the knowledge of professionals about phytotherapy, their views about use in primary care, the use of this practice andthe strategies developed for this use. The results revealed that the knowledge of the interviewees mostly is narrow and informal, and they find difficultiesto implement phytotherapic practices such as no valuation by the management and the rest of the health group. It should be emphasized as well theimportance of developing strategies that enable the safe and efficient integration of phytotherapy in care and thus the appreciation of local culture.


El empleo de plantas medicinales está bastante difundida en todo el mundo, inclusive en Brasil, donde hay gran variedad de especies y largatradición de uso. Con esta investigación se buscó conocer la percepción de los enfermeros sobre el uso de la fitoterapia en la Estrategia Salud de laFamilia (ESF). Se trata de un estudio exploratorio descriptivo de enfoque cualitativo desarrollado en Crato-CE con quince enfermeros de la ESF. Seempleó el método de análisis temático-categorial. Se construyeron seis categorías y dos subcategorías en las cuales se describieron el conocimientode los profesionales sobre fitoterapia, su visión del empleo de dicha práctica en la atención primaria, el ejercicio de esta práctica y las estrategiasdesarrolladas para tal ejercicio. Los resultados revelaron que el conocimento de los entrevistados era, en su mayoría, limitado e informal y queencuentran ciertas dificultades para establecer prácticas fitoterápicas, tales como falta de valoración por parte de la gestión y del resto del person...


Subject(s)
Humans , Primary Health Care , Community Health Nursing , Phytotherapy , Plants, Medicinal
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