ABSTRACT
Few sclerophyllous plants from the central coast of Chile have been systematically studied. This work describes the phytochemical composition and antimicrobial properties of Baccharis concava Pers. (sin. B. macraei), a shrub found in the first line and near the Pacific coast. B. concava has been traditionally used by indigenous inhabitants of today's central Chile for its medicinal properties. Few reports exist regarding the phytochemistry characterization and biological activities of B. concava. A hydroalcoholic extract of B. concava was prepared from leaves and small branches. Qualitative phytochemical characterization indicated the presence of alkaloids, steroids, terpenoids, flavonoids, phenolic, and tannin compounds. The antimicrobial activity of this extract was assessed in a panel of microorganisms including Gram-positive bacteria, Gram-negative bacteria, and pathogenic yeasts. The extract displayed an important antimicrobial effect against Gram-positive bacteria, Candida albicans, and Cryptococcus neoformans but not against Gram-negatives, for which an intact Lipopolysaccharide is apparently the determinant of resistance to B. concava extracts. The hydroalcoholic extract was then fractionated through a Sephadex LH-20/methanol-ethyl acetate column. Afterward, the fractions were pooled according to a similar pattern visualized by TLC/UV analysis. Fractions obtained by this criterion were assessed for their antimicrobial activity against Staphylococcus aureus. The fraction presenting the most antimicrobial activity was HPLC-ESI-MS/MS, obtaining molecules related to caffeoylquinic acid, dicaffeoylquinic acid, and quercetin, among others. In conclusion, the extracts of B. concava showed strong antimicrobial activity, probably due to the presence of metabolites derived from phenolic acids, such as caffeoylquinic acid, and flavonoids, such as quercetin, which in turn could be responsible for helping with wound healing. In addition, the development of antimicrobial therapies based on the molecules found in B. concava could help to combat infection caused by pathogenic yeasts and Gram-positive bacteria, without affecting the Gram-negative microbiota.
Subject(s)
Baccharis , Quercetin , Quinic Acid/analogs & derivatives , Chile , Tandem Mass Spectrometry , Phytochemicals/pharmacology , Flavonoids/pharmacology , Plant Extracts/pharmacologyABSTRACT
Medicinal plants are used to cure diseases, and their replacement is frequent and affects public health. The genus Baccharis has representatives within the medicinal flora of Argentina, although the replacement of the species of this genus known under the vulgar name of "carqueja" by Baccharis spicata has been detected i n herbalists or markets of herbal products. The genotoxic safety of this species has been established in previous work of our group. The aim of this study was to evaluate the antiviral activity of an infusion made from B. spicata leaves against hepatitis B virus with the HepG2.2.15 cellular system and to determine cytotoxicity in HepG2.2,15, A549 and Vero cell lines. Infusion of B. spicata was active to inhibit HBV replication with an EC 50 of 22.54 µg/mL and a CC 50 of 190 µg/mL.
Las plantas medicinales son empleadas para la cura de enfermedades, y su sustituc ión es frecuente y afecta a la salud pública. El género Baccharis posee representantes dentro de la flora medicinal de Argentina, aunque se ha detectado la sustitución de las especies de dicho género conocidas bajo el nombre vulgar de "carqueja" por Baccha ris spicata en herboristerías o mercados de productos herb arios . Se ha establecido la seguridad genotóxica de esta especie en trabajos previos de nuestro grupo. Este estudio buscó evaluar la actividad antiviral de una infusión elaborada a partir de hojas de B. spicata frente al virus de la hepatitis B con el sistema celular HepG2.2.15 y determinar la citotoxicidad en las líneas celulares HepG2.2.15, A549 y Vero. La infusión de B. spicata fue activa para inhibir la replicación del virus con un EC 50 de 22.54 µg/mL y un CC 50 de 190 µg/mL.
Subject(s)
Antiviral Agents/administration & dosage , Plant Extracts/administration & dosage , Baccharis/chemistry , Hepatitis B/drug therapy , Antiviral Agents/pharmacology , Virus Replication/drug effects , Plant Extracts/pharmacology , Cell Line/drug effects , Hepatitis B virus/drug effects , Plant Leaves , Asteraceae , Medicine, TraditionalABSTRACT
Baccharis vulneraria Baker is used popularly for the treatment of skin infections. So, this study aimed investigate the antimicrobial activity and chemical characterization of the essential oil (EO) against microorganisms that cause cutaneous infections. The EO was analyzed by GC-MS. The antimicrobial test was performed using the serial microdilution method, and the antimicrobial activity was determined by the minimum inhibitory concentration against Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Pseudomonas aeruginosa, Candida albicans, Trichophyton interdigitale, Trichophyton rubrum, Fusarium solani and Fusarium oxysporum within the 32-0.0625 mg/mL concentration range. Were identified 31 EO compounds. Its major compounds are bicyclogermacrene, trans-cadin-1,4-diene, ß-caryophyllene, and germacrene A. EO showed antifungal action against T. rubrum and T. interdigitale (2 and 4 mg/mL MIC, respectively). The growth of C. albicans, at 4 mg/mL, decreased by 50% compared to control. The oil had no significant potential for other microorganisms at the selected concentrations.
Subject(s)
Anti-Infective Agents , Baccharis , Oils, Volatile , Oils, Volatile/chemistry , Anti-Infective Agents/pharmacology , Antifungal Agents/pharmacology , Candida albicans , Microbial Sensitivity TestsABSTRACT
New natural analgesic compounds that act in KORs are important alternatives for potential therapeutical use in medicine. In this work, we report and compare here the antinociceptive activity displayed by cyclic and linear diterpenes, obtained from the genus Baccharis. The antinociceptive activities determined were relatively strong, in comparison whit morphine. The antinociceptive mechanism of action was made through naloxone administration (a non-selective antagonist of opioid receptors). The more active compounds were vehiculized successfully in niosomes at nanometric scale. The observed antinociceptive activity for Bartemidiolide oxide (BARTO), obtain from Baccharis artemisioides, was greater than Flabeloic acid dimer (DACD), the first compound isolated from Baccharis flabellata that was reported possessing antinociceptive effects. We also conducted docking calculations and molecular dynamics simulations, which suggested that the newly identified diterpenes might share the molecular action mechanism reported for Salvinorin A (SalA). Molecular simulations have allowed us to appreciate some subtle differences between molecular interactions of these ligands stabilizing their respective complexes; such information might be useful for designing and searching for new inhibitors of KORs.
Subject(s)
Baccharis , Receptors, Opioid, kappa , Receptors, Opioid, kappa/agonists , Liposomes , Molecular Structure , Analgesics/pharmacology , Receptors, OpioidABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: Justicia procumbens L. (JP) (Oriental Water Willow, Shrimp plant, Acanthaceae) is a herbaceous plant that is commonly found in India, Taiwan, Australia, Southern China, Vietnam, and Korea. The plant has been primarily used to treat fever, asthma, edema, cough, jaundice, urinary tract infection, and sore throat, as well as for snake bites and as a fish-killer. In the present review, the reported phyto-chemical, ethno-pharmacological, biological, and toxicological studies on J. procumbens were summarized. Special focus had been given to its reported lignans, regarding their isolation, characterization, quantitative estimation, and biosynthesis. MATERIALS AND METHODS: A survey of the literature was done using assorted databases and publishers; Scopus, Sci-Finder, Web of Science, PubMed, GoogleScholar, ScienceDirect, Wiley, Taylors&Francis, Bentham, Thieme, and Springer. RESULTS: Currently, 95 metabolites have been separated fromJ. procumbens. Lignans and their glycosides were reported as main phyto-constituents of J. procumbens. Various methods are mentioned for quantitative estimation of these lignans. These phyto-constituents possessed wide pharmacological effectiveness, such as antiplatelet aggregation, antimicrobial, antitumor, and antiviral. CONCLUSIONS: Many of the stated effects are harmonious with the reported traditional uses of this plant. This data could further support J. procumbens's utilization as a herbal remedy and drug lead. However, further study of J. procumbens toxicity, as well as preclinical and clinical investigation is required to ensure the safe usage of J. procumbens.
Subject(s)
Baccharis , Justicia , Lignans , Animals , Justicia/chemistry , Medicine, Traditional , Plants , Phytochemicals/pharmacology , Phytochemicals/therapeutic use , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , EthnopharmacologyABSTRACT
This study proposes an unpreceded model of cardiovascular disease by combining alcohol and energy drink intake with hookah smoking to investigate the cardiovascular effects of Baccharis trimera (Less.) DC., a medicinal plant used to treat dyslipidemia. For 10 weeks, Wistar rats (n=8) received alcohol (10% ad libitum) and energy drink (2 mL/kg) and/or were exposed to hookah smoke (1 hour/day). In the last 4 weeks, the animals received daily treatment with vehicle (filtered water) or ethanol soluble fraction of B. trimera (30, 100 and 300 mg/kg). Electrocardiography was performed. Systolic, diastolic, and mean blood pressure, heart rate, and plasmatic cholesterol, triglycerides, urea, creatine, aspartate, and alanine aminotransferase levels were determinate. The heart, aorta, and kidneys were histopathological evaluated. In isolation the risk factors altered all the evaluated parameters and when the risk factors were associated, a synergistic effect was observed. Treatment with B. trimera reversed these cardiovascular changes.
Este estudio propone un modelo sin precedentes de enfermedad cardiovascular mediante la combinación de la ingesta de bebidas energéticas y alcohol con fumar narguile para investigar los efectos cardiovasculares de Baccharis trimera (Less.) DC., una planta utilizada para tratar la dislipidemia. Durante 10 semanas, las ratas Wistar recibieron alcohol (10%) y bebida energética y/o fueron expuestas al humo de narguile. En las últimas 4 semanas, los animales recibieron tratamiento con vehículo, fracción soluble en etanol de B. trimera (30, 100, 300 mg/kg). Se realizó electrocardiografía. Se determinaron los niveles de presión arterial sistólica, diastólica y media, frecuencia cardíaca, colesterol plasmático, triglicéridos, aspartato y alanina aminotransferasa, urea y creatina. El corazón, la aorta y los riñones fueron evaluados histopatológicamente. De forma aislada los factores de riesgo alteraron todos los parámetros evaluados y cuando se asociaron los factores se observó un efecto sinérgico. El tratamiento con B. trimera revirtió estos cardiovasculares cambios.
Subject(s)
Baccharis/chemistry , Alcoholism/drug therapy , Cigar Smoking/drug therapy , Plant Extracts/chemistry , Rats, Wistar , Plant Leaves/chemistry , Energy Drinks/adverse effectsABSTRACT
Intestinal helminthiasis is a neglected disease that affects a significant portion of the global population, specifically in developing countries, where medicinal plants are widely used for therapeutic purposes. With the purpose to identify the native species used in traditional Brazilian medicine for the management of helminthiasis, ethnopharmacological books edited in Brazil documenting the folk use of medicinal plants were analyzed. The native species cited in at least three studies were selected, and bibliographic research was performed using electronic databases to identify their scientifically validated anthelmintic properties. The search retrieved 133 native species belonging to 88 genera and 43 families from all six Brazilian biomes. Fabaceae (14 Genera and 25 Species) and Asteraceae (7 Genera and 8 Species) were the most frequently cited families. The most reported native species were Baccharis crispa Spreng., Hymenaea courbaril L., Senna occidentalis (L.) Link, Carapa guianensis Aubl., Stachytarpheta cayennensis (Rich.) Vahl, Annona glabra L., Hymenaea stigonocarpa Mart. ex Hayne, Spigelia anthelmia L., Simarouba versicolor A.St.-Hil. and Anacardium occidentale L. Bark (19%) and leaves (17%) were the most commonly used plant parts, and decoction (27%) was the most preferred method of preparation. Evidence of the anthelmintic properties of most species was confirmed using in vitro assays for key human and animal parasites, including Haemonchus contortus, Hymenolepis diminuta, Schistosoma mansoni and Trichostrongylus spp. The species S. alata, S. occidentalis, A. occidentale, and S. anthelmia have been the subject of many biological studies, supporting their use as vermicides. The overall results obtained in this review revealed that Brazil is rich in traditional herbal medicines used to manage helminthiasis; however pharmacological investigations are lacking to confirm their therapeutic properties. Thus, this study could serve as a baseline to validate their use and encourage further clinical investigation of their vermifuge potential.
Subject(s)
Anthelmintics , Baccharis , Helminthiasis , Plants, Medicinal , Animals , Humans , Brazil , Phytotherapy/methods , Surveys and Questionnaires , Health Knowledge, Attitudes, Practice , Ethnobotany , Helminthiasis/drug therapy , Anthelmintics/pharmacology , Anthelmintics/therapeutic useABSTRACT
Endemic in 21 countries, Chagas disease, also known as American Trypanosomiasis, is a neglected tropical disease (NTD) caused by the protozoan parasite Trypanosoma cruzi. The available drugs for the treatment of this disease, benznidazole and nifurtimox, are outdated and display severe side effects. Thus, the discovery of new drugs is crucial. Based on our continuous studies aiming towards the discovery of natural products with anti-T. cruzi potential, the MeOH extract from aerial parts of Baccharis sphenophylla Dusén ex. Malme (Asteraceae) displayed activity against this parasite and was subjected to high-performance countercurrent chromatography (HPCCC), to obtain one unreported syn-labdane diterpene - sphenophyllol (1) - as well as the known compounds gaudichaudol C (2), ent-kaurenoic acid (3), hispidulin (4), eupafolin (5), and one mixture of di-O-caffeoylquinic acids (6-8). Compounds 1-8 were characterized by analysis of nuclear magnetic resonance (NMR) and mass spectrometry (MS) data. When tested against trypomastigote forms, isolated labdane diterpenes 1 and 2 displayed potent activity, with EC50 values of 20.1 µM and 2.9 µM, respectively. The mixture of chlorogenic acids 6-8, as well as the isolated flavones 4 and 5, showed significant activity against the clinically relevant amastigotes, with EC50 values of 24.9, 12.8, and 2.7 µM, respectively. Nonetheless, tested compounds 1-8 displayed no cytotoxicity against mammalian cells (CC50 > 200 µM). These results demonstrate the application of HPCCC as an important tool to isolate bioactive compounds from natural sources, including the antitrypanosomal extract from B. sphenophylla, allowing for the development of novel strategic molecular prototypes against tropical neglected diseases.
Subject(s)
Baccharis , Chagas Disease , Trypanosoma cruzi , Animals , Countercurrent Distribution , Plant Extracts/pharmacology , MammalsABSTRACT
O Diabetes desde a antiguidade tem sido uma das maiores causas de morte entre as populações do globo, e segundo a Organização Mundial da Saúde continua assolando nos nossos dias. Apesar das descobertas de tratamentos mais eficazes, a doença vem avançando em progressões assustadoras atualmente, com projeções preocupantes para a saúde pública. Como estratégia de acompanhamento terapêutico, estatístico direcionado a portadores de diabetes, o Governo Federal lançou o programa HIPERDIA (Hipertensos e Diabéticos), que faz o acompanhamento da evolução da doença e das complicações dos pacientes. E neste sentido, também são utilizadas terapêuticas mais acessíveis como as plantas medicinais. O objetivo desta pesquisa consiste em realizar uma revisão bibliográfica abordando as opções de terapias de controle do diabetes oferecidas no Sistema Único de Saúde e pesquisar fitoterápicos com potencial hipoglicêmico aprovados pela Anvisa. Através de levantamento bibliográfico, foram identificadas oito espécies vegetais utilizadas pela medicina popular no controle do diabetes, sendo estas: Bauhinia Forficata, Syzygium Cumini, Annona Muricata, Cynara Scolymus, Momordica Charantia, Eugenia Uniflora e Baccharis Trimera. Essas plantas do programa, embora tenham comprovação de seu efeito hipoglicêmico e redutores dos sintomas diabéticos, pelas suas propriedades antioxidantes e antiinflamatórias, colabora para uma melhor qualidade de vida aos pacientes.
Since antiquity, Diabetes has been one of the biggest causes of death amon-g populations around the globe, and according to the World Health Organization, it continues to plague our days. Despite discoveries of more effective treatments, the disease is currently advancing in frightening progressions, with worrying projections for public health. As a therapeutic, statistical follow-up strategy aimed at people with diabetes, the Federal Government launched the HIPERDIA (Hypertensive and Diabetic) program, which monitors the evolution of the disease and the complications of patients. And in this sense, more accessible therapies such as medicinal plants are also used. The objective of this research is to carry out a literature review addressing the options for diabetes control therapies offered in the Unified Health System and to search for herbal medicines with hypoglycemic potential approved by Anvisa. Through a bibliographical survey, eight plant species used by folk medicine to control diabetes were identified, namely: Bauhinia Forficata, Syzygium Cumini, Annona Muricata, Cynara Scolymus, Momordica Charantia, Eugenia Uniflora and Bacharis Trimera. These plants in the program, although they have evidence of their hypoglycemic effect and reduce diabetic symptoms, due to their antioxidant and anti-inflammatory properties, contribute to a better quality of life for patients.
La diabetes ha sido desde la antigüedad una de las principales causas de muerte entre las poblaciones del planeta, y según la Organización Mundial de la Salud sigue haciendo estragos en nuestros días. A pesar de los descubrimientos de tratamientos más eficaces, la enfermedad avanza actualmente con una progresión aterradora, con proyecciones preocupantes para la salud pública. Como estrategia de seguimiento terapéutico, estadísticamente dirigida a las personas con diabetes, el Gobierno Federal puso en marcha el programa HIPERDIA (Hipertensión y Diabetes), que controla la evolución de la enfermedad y las complicaciones de los pacientes. En este sentido, también se utilizan terapias más accesibles, como las plantas medicinales. El objetivo de esta investigación es realizar una revisión bibliográfica que aborde las opciones de terapias para el control de la diabetes ofrecidas en el Sistema Único de Salud y buscar fitoterapias con potencial hipoglucemiante aprobadas por Anvisa. Mediante un estudio bibliográfico, se identificaron ocho especies vegetales utilizadas por la medicina popular en el control de la diabetes, a saber: Bauhinia Forficata, Syzygium Cumini, Annona Muricata, Cynara Scolymus, Momordica Charantia, Eugenia Uniflora y Baccharis Trimera. Estas plantas del programa, aunque han demostrado su efecto hipoglucemiante y reductor de los síntomas diabéticos, por sus propiedades antioxidantes y antiinflamatorias, colaboran a una mejor calidad de vida para los pacientes.
Subject(s)
Program Development , Diabetes Mellitus/therapy , Phytotherapeutic Drugs , Plants, Medicinal , Therapeutics , Unified Health System , Public Health , Health Strategies , Momordica charantia/chemistry , Syzygium/chemistry , Annona/chemistry , Baccharis/chemistry , Cynara scolymus/chemistry , Bauhinia/chemistry , Eugenia/chemistry , Hypertension/drug therapy , Hypoglycemic AgentsABSTRACT
INTRODUCTION: Capillary zone electrophoresis with direct UV detection (CZE-UV) was used to investigate the hypothesis about the extract of Baccharis trimera enzymatic activities as an analytical approach to monitoring the phenomenon. OBJECTIVE: The aim of this work was to investigate enzymatic bioactivities of the hydroalcoholic and infusion extracts of B. trimera through screening evaluation of the inhibition of the enzymes acetylcholinesterase (AChE) and α-glycosidase (α-GLY). METHOD: An alternative approach using CZE-UV to hydroalcoholic and infusion extracts of B. trimera monitoring was applied to evaluate the inhibition ability of the enzymes AChE and α-GLY. The result of the reaction of acetylthiocholine (AThCh) with AChE was thiocholine (TCh) and acetic acid, and from the amount of TCh generated, the AChE inhibition was calculated. For the inhibition study of the two enzymes, the reactions of the extracts were optimised to be performed in situ, inside the capillary column, and the introduction of the solutions was performed through ordered sequential plug injections. RESULTS: Samples extracted with 70% ethanol presented 7.80% inhibition for AChE and 0.51% for α-GLY, while samples extracted with 96% ethanol resulted in 6.89% inhibition for AChE and no inhibition activity for α-GLY. CONCLUSION: In the present work, the potentialities of CZE-UV for the study of hydroalcoholic and infusion extracts of B. trimera were demonstrated. The experimental results were useful for the calculation of the percentage of the inhibition activities of the AChE and α-GLY enzymes.
Subject(s)
Baccharis , Acetylcholinesterase , Plant Extracts/pharmacology , Ethanol , Acetic AcidABSTRACT
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
Plant microbiota is usually enriched with bacteria producers of secondary metabolites and represents a valuable source of novel species and compounds. Here, we analyzed the diversity of culturable root-associated bacteria of the medicinal native plant Baccharis trimera (Carqueja) and screened promising isolates for their antimicrobial properties. The rhizobacteria were isolated from the endosphere and rhizosphere of B. trimera from Ponta Grossa and Ortigueira localities and identified by sequencing and restriction analysis of the 16S rDNA. The most promising isolates were screened for antifungal activities and the production of siderophores and biosurfactants. B. trimera presented a diverse community of rhizobacteria, constituted of 26 families and 41 genera, with a predominance of Streptomyces and Bacillus genera, followed by Paenibacillus, Staphylococcus, Methylobacterium, Rhizobium, Tardiphaga, Paraburkholderia, Burkholderia, and Pseudomonas. The more abundant genera were represented by different species, showing a high diversity of the microbiota associated to B. trimera. Some of these isolates potentially represent novel species and deserve further examination. The communities were influenced by both the edaphic properties of the sampling locations and the plant niches. Approximately one-third of the rhizobacteria exhibited antifungal activity against Sclerotinia sclerotiorum and Colletotrichum gloeosporioides, and a high proportion of isolates produced siderophores (25%) and biosurfactants (42%). The most promising isolates were members of the Streptomyces genus. The survey of B. trimera returned a diverse community of culturable rhizobacteria and identified potential candidates for the development of plant growth-promoting and protection products, reinforcing the need for more comprehensive investigations of the microbiota of Brazilian native plants and habitats.
Subject(s)
Baccharis , Plants, Medicinal , Anti-Bacterial Agents/metabolism , Anti-Bacterial Agents/pharmacology , Antifungal Agents/metabolism , Antifungal Agents/pharmacology , Baccharis/metabolism , Bacteria , Humans , Plant Roots/microbiology , Rhizosphere , Siderophores/metabolismABSTRACT
The concern regarding the harm caused by biocides to human health has been increasing over the years, making the natural products an alternative to less toxic and more efficient biocides. Therefore, this paper reports the investigation of the disinfectant potential of extracts and isolated compounds from Baccharis dracunculifolia. For this purpose, extracts of aerial parts (BD-C), tricomial wash (BD-L) and roots (BD-R) of B. dracunculifolia were obtained by maceration. The extracts were submitted to different chromatographic techniques, including high-speedy countercurrent chromatography (HSCCC) furnishing nine isolated compounds. The extracts and isolated compounds were evaluated regarding their antimicrobial activity by the broth microdilution method, according to the Clinical and Laboratory Standards Institute, and regarding their sanitizing activity according to Standard Operating Procedure No. 65·3210·007 (INCQS, 2011), developed by the National Institute for Quality Control in Health (INCQS) - Oswaldo Cruz Foundation (FIOCRUZ). In the antimicrobial evaluation the BD-C extract showed minimum inhibitory concentration (MIC) values of 200 and 100 µg/ml against Staphylococcus aureus and Tricophyton mentagrophytes, respectively. BD-L extract showed MIC value of 200 µg/ml against S. aureus. The isolated compounds caffeic acid (MBC 2·22 µmol l-1 ), ferulic acid (MBC 2·06 µmol l-1 ) and baccharin (MBC 0·27 µmol l-1 ) showed significant inhibitory activity against S. aureus. All B. dracunculifolia isolated compounds were active with exception of aromadrendin-4´-O-methyl-ether for T. mentagrophytes. Additionally, isosakuranetin was active against Salmonella choleraesuis (MIC 1·4 µmol l-1 ). Regarding the sanitizing activity, the hydroalcoholic solution containing 0·2% of B. dracunculifolia extract in 40°GL ethanol was effective in eliminating the microbial contamination on all carrier cylinders and against all microorganisms evaluated in the recommended exposure time of 10 min. Therefore, B. dracunculifolia has potential for the development of sanitizing agents to be used in hospitals, food manufactures and homes.
Subject(s)
Anti-Infective Agents , Baccharis , Disinfectants , Anti-Infective Agents/pharmacology , Baccharis/chemistry , Disinfectants/pharmacology , Humans , Microbial Sensitivity Tests , Plant Extracts/chemistry , Staphylococcus aureusABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: Popularly known as "escoba" (broom) or "escobilla china" (Chinese brush), Baccharis conferta Kunth (Asteraceae), is a plant widely used in Mexican folk medicine for alleviating muscular and rheumatic pain. A recent study described that dichloromethane extract as well as fractions and isolated compounds, possess anti-inflammatory activity in TPA-induced acute edema. AIM OF THE STUDY: Based on the popular medicinal uses of B. conferta as well as previous studies on its anti-inflammatory activity, the aim of this research was to evaluate the anti-arthritic and anti-inflammatory effects of dichloromethane extract, fractions, and compounds from B. conferta in a monoarthritis model induced with kaolin/carrageenan (K/C). MATERIALS AND METHODS: Aerial parts of B. conferta were collected, dried, and macerated with dichloromethane. The dichloromethane extract (BcD) was separated by open column chromatography to obtain the BcD2 fraction where the diterpene kingidiol (KIN) was isolated and from the BcD3 fraction the flavonoid cirsimaritin (CIR), which are the most active compounds in the TPA model. In addition, the flavonoids acacetin, pectolinaringenin and 6-methoxykaempferide were identified and isolated from the BcD2 fraction. The content of the main compounds was estimated in BcD, BcD2 and BcD3. The anti-arthritic and anti-inflammatory effects of B. conferta were investigated by evaluating ankle joint inflammation, hyperalgesia using the hot plate test, and pro- and anti-inflammatory cytokine levels in the synovial capsule as well as histological changes in ankle joint tissue in a monoarthritis model induced with K/C in Balb/c mice. RESULTS: Oral administration of BcD2 fraction (25 mg/kg) and KIN (10 mg/kg) reduced the ankle thickness induced by K/C and decreased the levels of TNF-α, IL-1ß, IL-6 and IL-17, while BcD2 increased IL-10. In addition, BcD2 and KIN showed significant edema attenuation of the synovial membrane and decreased inflammatory infiltration and cartilage erosion compared to the VEH group. Finally, BcD (50 mg/kg), KIN (10 mg/kg) and CIR (5 mg/kg) decreased hyperalgesia. CONCLUSIONS: B. conferta constitutes a therapeutic or preventive candidate for osteoarthritis, because of decreased articular inflammation and pain accompanied with the modulation of cytokine concentrations, which confirms the anti-arthritic and anti-inflammatory activities of B. conferta and support its popular use.
Subject(s)
Anti-Inflammatory Agents/pharmacology , Arthritis, Experimental/drug therapy , Baccharis/chemistry , Plant Extracts/pharmacology , Animals , Anti-Inflammatory Agents/isolation & purification , Arthritis, Experimental/pathology , Carrageenan , Disease Models, Animal , Hyperalgesia/drug therapy , Inflammation/drug therapy , Inflammation/pathology , Kaolin , Male , Medicine, Traditional , Mice , Mice, Inbred BALB C , Plant Extracts/chemistryABSTRACT
Natural products have been largely explored as treatments for leishmaniasis, neglected diseases with few toxic therapeutic options, as scaffolds for the development of new drugs. Herein, derivatives from the aerial parts of Baccharis trimera (Less.) DC (extract and its fractions) were evaluated against Leishmania amazonensis and macrophage cells. The ethyl acetate extract was fractionated by solid-phase extraction, resulting in eight fractions (F1-F8). Fractions F3-4 were further separated into 149 subfractions; subfraction 148 (IC50-PRO = 1.56 ± 0.1 µg mL-1) was selected for purification and constituent(s) characterization by high-performance liquid chromatography, as well as 1H and 13C nuclear magnetic resonance spectroscopy. The flavonoid eupatorin (3',5-dihydroxy-4',6,7-trimethoxyflavone) was identified. This compound was 3.7 times more effective against intracellular amastigotes (IC50-AMA = 1.6 ± 0.1 µM) than amphotericin B and presented low cytotoxicity (CC50 > 100 µM), being almost 62 times more selective for the parasite, showing great potential in drug development for cutaneous leishmaniasis treatment.
Subject(s)
Antiprotozoal Agents , Baccharis , Leishmania mexicana , Leishmaniasis, Cutaneous , Antiprotozoal Agents/pharmacology , Baccharis/chemistry , Flavonoids/analysis , Leishmaniasis, Cutaneous/drug therapy , Plant Extracts/chemistry , Plant Leaves/chemistryABSTRACT
BACKGROUND: In the present work the bioactivity-guided fractionation of n-hexane extract from aerial parts of Baccharis sphenophylla (Asteraceae) against trypomastigote forms of Trypanosoma cruzi was performed. PURPOSE: To evaluate the antitrypanosomal potential of diterpenes entkaurenoic (1), grandifloric (2). and 15ß-tiglinoyloxyent-kaurenoic (3) acids, isolated from n-hexane extract from aerial parts of B. sphenophylla, and elucidate their mechanism of action against T. cruzi. METHODS/STUDY DESIGN: n-Hexane and MeOH extracts from aerial parts of B. sphenophylla were prepared and caused, respectively, 100% and 50% of death of trypomastigote forms of T. cruzi. Based on these results, the n-hexane extract was subjected to bioactivity-guided fractionation procedures to afford three related entkaurane diterpenoids (1-3). Based on spectrofluorometric assays and flow cytometry analysis, the mechanism of action of compounds 1 and 3 was investigated. RESULTS: Compounds 1 and 3, isolated from n-hexane extract from aerial parts of B. sphenophylla, showed potent activity against parasites with EC50 values of 10.6 µM (SI > 18.8) and 2.4 µM (SI = 34.8), respectively. On the other hand, compound 2 was inactive against trypomastigotes. In mechanism of action studies using the fluorescent probe SYTOX Green, the plasma membrane permeability was unaltered after treatment with compounds 1 and 3, but compound 1 induced a depolarization of the plasma membrane electric potential (ΔΨp). No substantial alterations were observed in the mitochondria after treatment with compound 3, but a transient hyperpolarization of the mitochondrial membrane potential (ΔΨm) by compound 1. Despite the increased ATP levels induced by compounds 1 and 3, no alterations of ROS and Ca2+ levels were registered. However, both compounds promoted a time-dependent alkalinization of the acidocalcisomes, probably contributing to an osmotic imbalance of the cell. In silico physicochemical studies of compounds 1-3 suggested that lipophilicity and molecular complexity may play an important role in the antitrypanosomal activity. Moreover, no pan-assay interference compounds (PAINS) alerts were detected for compounds 1-3. CONCLUSION: Obtained data indicated that the isolated entkaurane diterpenes from n-hexane extract from aerial parts of B. sphenophylla, especially compound 3, could be considered interesting prototypes for further modifications aiming the discovery of new hits against T. cruzi.
Subject(s)
Baccharis , Diterpenes, Kaurane , Diterpenes , Trypanosoma cruzi , Diterpenes/pharmacology , Diterpenes, Kaurane/pharmacology , HexanesABSTRACT
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
Cardiovascular diseases are associated with high morbidity and mortality worldwide and have several risk factors, including dyslipidemia, smoking, and hypertension. Studies have evaluated isolated risk factors in experimental models of cardiovascular disease, but few preclinical studies have assessed associations between multiple risk factors. In the present study, hypertensive Wistar rats (Goldblatt 2K1C model) received a 0.5% cholesterol diet and were exposed to tobacco smoke for 8 weeks. During the last 4 weeks, the animals were treated with vehicle, an ethanol-soluble fraction of B. trimera (30, 100, and 300 mg/kg), or simvastatin + enalapril. A group of normotensive, non-dyslipidemic, and non-smoking rats was treated with vehicle. The levels of aspartate aminotransferase, alanine aminotransferase, urea, creatinine, and hepatic and fecal lipids, blood pressure, and mesenteric arterial bed reactivity were evaluated. Cardiac, hepatic, and renal histopathology and tecidual redox state were also investigated. Untreated animals exhibited significant changes in blood pressure, lipid profile, and biomarkers of heart, liver, and kidney damage. Treatment with B. trimera reversed these changes, with effects that were similar to simvastatin + enalapril. These findings suggest that B. trimera may be promising for the treatment of cardiovascular and hepatic disorders, especially disorders that are associated with multiple risk factors.
Subject(s)
Baccharis , Noncommunicable Diseases , Animals , Plant Extracts , Rats , Rats, Wistar , Risk FactorsABSTRACT
The diverse flora of the Atlantic Forest is fertile ground for discovering new chemical structures with insecticidal activity. The presence of species belonging to the genus Baccharis is of particular interest, as these species have shown promise in pest management applications. The objective of this study is to chemically identify the constituents expressed in the leaves of seven species of Baccharis (B. anomala DC., B. calvescens DC., B. mesoneura DC., B. milleflora DC., B. oblongifolia Pers., B. trimera (Less) DC. and B. uncinella DC.) and to evaluate the toxicological and morphological effects caused by essential oils (EOs) on the larvae and adults of Drosophila suzukii (Diptera: Drosophilidae). Chemical analysis using gas chromatography-mass spectrometry (GC-MS) indicated that limonene was the main common constituent in all Baccharis species. This constituent in isolation, as well as the EOs of B. calvescens, B. mesoneura, and B. oblongifolia, caused mortality in over 80% of adults of D. suzukii at a discriminatory concentration of 80 mg L-1 in bioassays of ingestion and topical application. These results are similar to the effect of spinosyn-based synthetic insecticides (spinetoram 75 mg L-1) 120 h after exposure. Limonene and EOs from all species had the lowest LC50 and LC90 values relative to spinosyn and azadirachtin (12 g L-1) in both bioassays. However, they showed the same time toxicity over time as spinetoram when applied to adults of D. suzukii (LT50 ranging from 4.6 to 8.7 h) in a topical application bioassay. In olfactometry tests, 92% of D. suzukii females showed repellent behavior when exposed to the EOs and limonene. Likewise, the EOs of B. calvescens, B. mesoneura, and B. oblongifolia significantly reduced the number of eggs in artificial fruits (â 7.6 eggs fruit-1), differing from the control treatment with water (17.2 eggs fruit-1) and acetone (17.6 eggs fruit-1). According to histological analyses, the L3 larvae of D. suzukii had morphological and physiological alterations and deformations after exposure to treatments containing EOs and limonene, which resulted in high larval, pupal, and adult mortality. In view of the results, Baccharis EOs and their isolated constituent, limonene, proved to be promising alternatives for developing bioinsecticides to manage of D. suzukii.
Subject(s)
Baccharis/metabolism , Drosophila/drug effects , Insecticides/pharmacology , Animals , Drosophila/metabolism , Drosophila/physiology , Fruit/drug effects , Gas Chromatography-Mass Spectrometry/methods , Insect Repellents/chemistry , Insect Repellents/pharmacology , Insecticides/chemistry , Larva/drug effects , Limonene/pharmacology , Oils, Volatile/pharmacology , Oviposition/drug effects , Plant Extracts/pharmacology , Plant Leaves/metabolism , Pupa/drug effectsABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: Baccharis trimera (Less.) DC known as "carqueja" in Brazil has been acknowledged as a medicinal plant in folk medicine for the treatment of stomach aches and gastrointestinal disorders. AIM OF THE STUDY: The present study aimed to evaluate the gastroprotective and healing effects of essential oil from B. trimera (EOBT) against gastric ulcer lesions caused by absolute ethanol and acetic acid, respectively, and to identify the mechanism of action of this essential oil in male Wistar rats. MATERIALS AND METHODS: The plant material used to obtain EOBT was collected in the southern region of Brazil and was analyzed by chromatography-mass spectrometry (GCMS) demonstrate its characteristic chemical composition, with carquejyl acetate as its main component. Different doses of EOBT (50, 100, and 200 mg/kg) were administered orally in male Wistar rats as an acute treatment against absolute ethanol-induced gastric lesions. The gastric healing effect of EOBT (100 mg/kg) was evaluated once a day after 7, 10, and 14 days of treatment. After treatment, the stomachs of rats from all groups were collected to measure the lesion area (mm2), the activity of myeloperoxidase (MPO), and the relative expression of caspases -3, -8, -9, cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2), vascular endothelial growth factor (VEGF), and epidermal growth factor (EGF). The zymography method was used to elucidate the activity of matrix metalloproteinase-2 (MMP-2) and -9 (MMP-9) in the healing action of EOBT. We also analyzed toxicological parameters (body weight evolution and biochemical parameters) that could result after treatment with this essential oil for 14 days. RESULTS: Pretreatment with EOBT (100 and 200 mg/kg) significantly decreased the severity of gastric damage induced by absolute ethanol and decreased MPO activity in gastric tissue. After 10 and 14 days of treatment with EOBT (100 mg/kg) once a day, the lesion area was significantly reduced by 61% and 65.5%, respectively, compared to the negative control group. The gastric healing effect of EOBT was followed by a decrease in the expression of COX-1 compared to that in the negative control group. Notably, treatment with EOBT for 14 days increased the expression of VEGF compared to that using an anti-ulcer drug (lansoprazole). Additionally, analyses of MMP-2 and MMP-9 activities in the gastric mucosa confirmed the accelerated gastric healing effect of EOBT, with a significant decrease in the activity of pro-MMP-2. No sign of toxicity was observed after treatment with EOBT for 14 consecutive days. CONCLUSION: These findings indicated that EOBT was effective in preventing and accelerating ulcer healing by decreasing MPO activity, increasing VEGF expression, and decreasing MMP-2 activity. These actions collectively contribute to the rapid recovery of gastric mucosa following treatment with EOBT, without any observed toxicity.