ABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: B. boliviensis and B. tola are used in traditional medicine in the Argentine Puna to treat skin and soft tissue infections and inflammatory processes in humans and animals. AIM OF THE STUDY: To assess the potential of phytotherapeutic preparations of Baccharis species as antifungal agents against clinically relevant fungi and to determine the chemical composition of the extracts. MATERIAL AND METHODS: Phytotherapeutic preparations of B. boliviensis and B. tola collected in Argentine Puna were evaluated as an antifungal agent against clinically relevant fungi (yeast, non-dermatophytes, and dermatophytes) isolated of patients from a local Hospital, and reference strains, using macrodilution and microdilution assays. The bioactivity was supported by UHPLC-OT-MS metabolome fingerprinting. RESULTS: The results revealed that the plant preparations were active against most of evaluated fungal strains; B. boliviensis was more active than B. tola. Dermatophyte fungi strains were the most sensitive isolates. The phytotherapeutic preparation showed Minimal Inhibitory Concentration (MIC) values between 25 and 400 µg GAE/mL and Minimum Fungicidal Concentration (MFC) values between 50 and 400 µg GAE/mL. Regarding the phytochemical analysis, total phenolic and total flavonoid contents of hydroalcoholic preparation of B. boliviensis were greater than those of the B. tola extract. Both Baccharis species showed similar chromatographic patterns, fifty-two compounds were identified based on UHPLC-OT-MS including several terpenoids, flavonoids and phenolic acids that have been identified in this two endemic South American Baccharis species for the first time. Several identified compounds present antifungal properties, the presence of these compounds support the bioactivity of the Baccharis extracts. CONCLUSIONS: In this work the traditional use of both Baccharis species as an antimicrobial against commercial products resistant fungal strains was validate, principally against dermatophytes fungi such as T. rubrum, T. mentagrophytes, M. canis, and M. gypseum. These results indicate that the hydroalcoholic preparations could be used for the treatment of fungal infectious.
Subject(s)
Antifungal Agents/pharmacology , Baccharis , Fungi/drug effects , Plant Extracts/pharmacology , Antifungal Agents/chemistry , Argentina , Flavonoids/analysis , Flavonoids/pharmacology , Microbial Sensitivity Tests , Phenols/analysis , Phenols/pharmacology , Phytochemicals/analysis , Phytochemicals/pharmacology , Plant Extracts/chemistryABSTRACT
The design of novel delivery systems to treat vaginal fungal infections is a topic of high interest. Chitosan, being itself antimicrobial and having good mucoadhesive properties, is an excellent candidate as a delivery matrix for active compounds. In this work, chitosan microcapsules containing dry extracts of Argentinean medicinal plants with proved biological properties (Larrea divaricata, L. cuneifolia, L. nitida, Zuccagnia punctata and Tetraglochin andina) were developed through electrospraying and compared with conventionally used tablets containing the same extracts. Total phenolics, loading efficacy, physical properties, morphology and particle size, molecular organization, water sorption capacity, release of bioactive compounds and biological properties were assessed. The encapsulation process or the inclusion in tablets did not degrade the bioactive compounds of the extracts. The release of phenolic compounds from chitosan microcapsules was faster than from tablets. The fingerprint of released phenolic compounds from microcapsules and tablets was similar to that from the dry extracts and the antioxidant and antifungal capacity remained unchanged. The FT-IR analysis suggested interactions between the chitosan and the extracts, which explained why the microcapsules kept the integrity in slightly acidic media. Increased solubility of the extracts when incorporated in the microcapsules was seen in simulated vaginal fluid, potentially increasing the bioavailability of bioactive compounds in the vaginal environment. This work highlights the potential of the chitosan-based delivery systems for phytomedicines with antifungal and antioxidant activity to be used in vulvovaginal candidiasis.
Subject(s)
Antifungal Agents , Candida/growth & development , Chitosan , Drug Carriers , Plant Extracts , Plants, Medicinal/chemistry , Saccharomyces cerevisiae/growth & development , Administration, Intravaginal , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Capsules , Chitosan/chemistry , Chitosan/pharmacology , Drug Carriers/chemistry , Drug Carriers/pharmacology , Female , Humans , Plant Extracts/chemistry , Plant Extracts/pharmacologyABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: The Argentinean medicinal plant Tetraglochin andina Ciald, formerly classified as T. cristatum (Britton) Rothm is used in traditional medicine by inhabitants from Argentinean northwestern highlands (Puna) to treat candidiasis and as anti-inflammatory. AIM OF THE STUDY: To assess the potential of the crude drug as an anti-Candida agent with anti-inflammatory properties. The bioactivity and phytochemical composition of a dry extract of the plant was investigated. MATERIAL AND METHODS: The pharmacognostic description of the crude drug is carried out for the first time, including macroscopic and microscopic examinations of the different organs, physicochemical and extractive values (petroleum ether-, ethanol- and water-soluble). The dry extract from T. andina was evaluated as antifungal against pathogenic Candida sp. and Saccharomyces cerevisiae isolated from vaginal infections and reference strains, by the macrodilution and microdilution assays. The normal vaginal microbiome in women is characterized by the dominance of lactic acid-producing bacteria, mainly Lactobacillus spp. The effect of T. andina extract on Lactobacillus strains was also assayed. The inhibitory effect on proinflammatory enzymes (cyclooxygenase, lipoxygenase and phospholipase A2) and antioxidant capacity was studied. The chemical profile was analyzed by HPLC-ESI-MS. RESULTS: The hydroalcoholic extract inhibited the growth of all yeasts with Minimal Inhibitory Concentration (MIC) values between 12.5 and 400⯵g GAE/mL and the MIC values on Lactobacillus were higher than the MIC values against Candida isolates ( > 400⯵g GAE/mL). These results indicate that the hydroalcoholic extract could be used without affecting the normal microbiota of vaginal fluid. The extract showed antioxidant activity and could modulate the inflammatory process by three pathways (sPLA2, COX-2, LOX). The plant extract contained high total phenolic levels (386.9±1.7â¯mg GAE/g dry extract) and flavonoid levels (260.4±2.7â¯mg GAE/g dry extract). Fifty phenolic compounds were identified by HPLC-ESI-MS. They were mainly hydrolysable and condensed tannins. The dry extract was chemically and biologically stable during one year at room temperature or 4⯰C. CONCLUSIONS: The presence of anti-Candida and anti-inflammatory activities in Tetraglochin andina extracts give support to their traditional use for treating conditions associated with microorganism infections and inflammatory process in humans. This plant preparation could be used to design phytopharmaceutical preparations to inhibit yeast growth and moderate the inflammatory and oxidative process.
Subject(s)
Anti-Inflammatory Agents/pharmacology , Antifungal Agents/pharmacology , Candida/drug effects , Candidiasis, Vulvovaginal/drug therapy , Plant Extracts/pharmacology , Rosaceae , Anti-Inflammatory Agents/isolation & purification , Antifungal Agents/isolation & purification , Antioxidants/isolation & purification , Antioxidants/pharmacology , Argentina , Candida/classification , Candida/growth & development , Candidiasis, Vulvovaginal/microbiology , Cyclooxygenase Inhibitors/isolation & purification , Cyclooxygenase Inhibitors/pharmacology , Erythrocytes/drug effects , Erythrocytes/metabolism , Female , Hemolysis/drug effects , Humans , Lactobacillus/drug effects , Lactobacillus/growth & development , Lipoxygenase Inhibitors/isolation & purification , Lipoxygenase Inhibitors/pharmacology , Microbial Sensitivity Tests , Oxidative Stress/drug effects , Phospholipase A2 Inhibitors/isolation & purification , Phospholipase A2 Inhibitors/pharmacology , Phytotherapy , Plant Components, Aerial , Plant Extracts/isolation & purification , Plants, Medicinal , Rosaceae/chemistry , Saccharomyces cerevisiae/drug effects , Saccharomyces cerevisiae/growth & developmentABSTRACT
The aim of this work was to assess the nutritional and functional components of powder obtained by lyophilization of whole fruits, seeds, pulp and skin from chilto (Solanum betaceum Cav) cultivated in the ecoregion of Yungas, Argentina. The powders have low carbohydrate and sodium content and are a source of vitamin C, carotenoid, phenolics, potassium and fiber. The HPLC-ESI-MS/MS analysis of the fractions enriched in phenolics allowed the identification of 12 caffeic acid derivatives and related phenolics, 10 rosmarinic acid derivatives and 7 flavonoids. The polyphenols enriched extracts before and after simulated gastroduodenal digestion inhibited enzymes associated with metabolic syndrome, including α-glucosidase, amylase and lipase and exhibited antioxidant activity by different mechanisms. None of the analyzed fruit powders showed acute toxicity or genotoxicity. The powders from the three parts of S. betaceum fruit may be a potential functional food and the polyphenol enriched extract of seed and skin may have nutraceutical properties.
Subject(s)
Fruit/chemistry , Metabolic Syndrome/drug therapy , Oxidative Stress/drug effects , Plant Preparations/pharmacology , Seeds/chemistry , Solanum/chemistry , Antioxidants/analysis , Antioxidants/pharmacology , Argentina , Ascorbic Acid/analysis , Carotenoids/analysis , Cinnamates/analysis , Depsides/analysis , Dietary Fiber/analysis , Female , Flavonoids/analysis , Flavonoids/pharmacology , Glycoside Hydrolase Inhibitors/analysis , Glycoside Hydrolase Inhibitors/pharmacology , Humans , Inhibitory Concentration 50 , Lipase/antagonists & inhibitors , Lipase/metabolism , Male , Phytochemicals/analysis , Phytochemicals/pharmacology , Plant Preparations/chemistry , Polyphenols/analysis , Potassium, Dietary/analysis , Powders/chemistry , Recommended Dietary Allowances , Tandem Mass Spectrometry , alpha-Amylases/antagonists & inhibitors , alpha-Amylases/metabolism , alpha-Glucosidases/metabolism , Rosmarinic AcidABSTRACT
Zuccagnia punctata Cav. (Fabaceae) is an Argentine medicinal aromatic shrub (jarilla pispito, puspus, lata and jarilla macho). The chalcones were identified as pigments responsible for the yellow color of the flowers. Hydroethanolic extracts were obtained both from fresh flowers and from flowers dried by lyophilization. The extracts were standardized by their phenolic and flavonoids content. Their fingerprints by HPLC-DAD indicated the presence of two chalcones as major compounds (2',4'-dihydroxychalcone and 2',4'-dihydroxy-3'-methoxychalcone). Both extracts showed the same total phenolic, non-flavonoid phenolic and flavonoid phenolic content and their phenolic profiles were similar. The polyphenolic extracts exhibited antioxidant (free radical scavenging and inhibitory activity on lipoperoxidation) and anti-inflammatory (inhibition of lipoxygenase and cyclooxygenase enzymes) activities. The flower extracts were active against six Candida species with MIC values between 60 and 120 µg GAE x mL(-1) and were also active on methicillin-resistant Staphylococcus aureus (MIC: 250 µg GAE x mL(-1)) and Enterococcus faecalis (MIC: 500 µg GAE x mL(-1)). The extracts were neither toxic (Artemia salina test) nor mutagenic (Ames test). Jarilla flowers could be considered as a new dietary supplement that could help to prevent pathologies associated with oxidative stress and the polyphenolic extract obtained from them could be considered as a standardized phytotherapeutic product with antimicrobial, antioxidant and anti-inflammatory activities. The aim of this work was to determine the pigments responsible for the yellow color of the flowers of Z. punctata and to evaluate the functional properties of the polyphenolic extract of the flowers. The toxicity (Artemia salina) and mutagenic activity (Ames test) of the extract were also evaluated.
Subject(s)
Anti-Infective Agents/pharmacology , Anti-Inflammatory Agents/pharmacology , Antioxidants/pharmacology , Fabaceae/chemistry , Plant Extracts/pharmacology , Plants, Medicinal/chemistry , Anti-Infective Agents/chemistry , Anti-Infective Agents/isolation & purification , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/isolation & purification , Antioxidants/chemistry , Antioxidants/isolation & purification , Argentina , Bacteria/drug effects , Flowers/chemistry , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Yeasts/drug effectsABSTRACT
Zuccagnia punctata Cav. has been used as a traditional medicine in Argentina for the treatment of bacterial and fungal infections. In this study, we evaluated the ability of Z. punctata extract (ZpE) and compounds isolated from it to inhibit the growth and virulence factors of Candida species. ZpE showed inhibitory activity against planktonic cells of all assayed Candida species with MIC values of 400 microg/mL and with MFC values between 400 and 1,200 microg/mL. The principal identified compounds by HPLC-MS/MS and UV-VIS were chalcones (2',4'-dihydroxy-3'-methoxychalcone, 2',4'- dihydroxychalcone), flavones (galangin, 3,7-dihydroxyflavone and chrysin) and flavanones (naringenin, 7-hydroxyflavanone and pinocembrine). These compounds were more effective as inhibitors than the extracts upon biofilm formation as well as on preformed Candida biofilm and yeast germ tube formation. Furthermore, ZpE and chalcones are able to inhibit exoenzymes, which are responsible for the invasion mechanisms of the pathogens. All these effects could moderate colonization, thereby suppressing the pathogen invasive potential. Our results indicate that ZpE and chalcones could be used in antifungal therapy.
Subject(s)
Antifungal Agents/pharmacology , Candida/drug effects , Candida/metabolism , Fabaceae/chemistry , Plant Extracts/pharmacology , Plants, Medicinal/chemistry , Virulence Factors/metabolism , Antifungal Agents/chemistry , Argentina , Biofilms/growth & development , Candida/physiology , Gene Expression Regulation, Fungal/drug effects , Models, Molecular , Plant Components, Aerial/chemistry , Plant Extracts/chemistry , StereoisomerismABSTRACT
We report a new colorimetric assay to quantify endo-polygalacturonase activity, which hydrolyzes polygalacturonic acid to produce smaller chains of galacturonate. Some of the reported polygalacturonase assays measure the activity by detecting the appearance of reducing ends such as the Somogyi-Nelson method. As a result of being general towards reducing groups, the Somogyi-Nelson method is not appropriate when studying polygalacturonase and polygalacturonase inhibitors in plant crude extracts, which often have a strong reducing power. Ruthenium Red is an inorganic dye that binds polygalacturonic acid and causes its precipitation. In the presence of polygalacturonase, polygalacturonic acid is hydrolyzed bringing about a corresponding gain in soluble Ruthenium Red. The described assay utilizes Ruthenium Red as the detection reagent which has been used previously in plate-based assays but not in liquid medium reactions. The new method measures the disappearance of the substrate polygalacturonic acid and is compared to the Somogyi-Nelson assay. The experimental results using lemon peel, a fern fronds and castor leaf crude extracts demonstrate that the new method provides a way to the quickly screening of polygalacturonase activity and polygalacturonase inhibitors in plant crude extracts containing high amounts of reducing power. On the other hand, the Ruthenium Red assay is not able to determine the activity of an exo-polygalacturonase as initial velocity and thus would allow the differentiation between endo- and exo-polygalacturonase activities.
Subject(s)
Colorimetry/methods , Daucus carota/enzymology , Pectins/metabolism , Polygalacturonase/metabolism , Ruthenium Red/metabolism , Plant Extracts/metabolism , Plant Proteins/metabolismABSTRACT
In this study, antioxidant activities in free-radical-mediated oxidative systems and the genotoxic/antigenotoxic effects of two proteins with molecular mass around 17 kDa, purified from Solanum betaceum fruits (cyphomine) and Solanum tuberosum tubers (solamarine), were investigated. Both proteins inhibited uric acid formation with IC(50) values between 55 and 60 µg/mL, and both proteins were able to reduce oxidative damage by scavenging hydroxyl radicals and superoxide anion in a dose-dependent manner. Furthermore, the DPPH⢠reduction assay showed SC(50) values of 55-73 µg/mL. Cyphomine and solamarine were able to retain their antioxidant activity after heat treatment at 80 °C for 15 min. Allium cepa and Salmonella /microsome assays showed no genotoxic and mutagenic effects. Solamarine showed an antimutagenic effect against a direct mutagen (4-nitro-o-phenylenediamine). Consequently, the present study showed that the investigated proteins are promising ingredients for the development of functional foods with a beneficial impact on human health and an important source for the production of bioactive peptides.
Subject(s)
Antimutagenic Agents/pharmacology , Antioxidants/pharmacology , Plant Proteins/pharmacology , Solanum tuberosum/chemistry , Solanum/chemistry , Free Radical Scavengers/pharmacology , Fruit/chemistry , Mutagenicity Tests , Plant Proteins/isolation & purification , Plant Tubers/chemistry , Salmonella typhimurium/drug effects , Salmonella typhimurium/geneticsABSTRACT
Propolis was included in the Argentine Food Code as a functional food. The chemical parameters and antioxidant properties of propolis samples from the same colonies of Apis mellifera in San Juan (Cuyo region, Western Argentine) were compared every month for 1 year using two collection methods. Chemical parameters were analyzed by the spectrophotometric method and fingerprinting using high-performance liquid chromatography with ultraviolet detection. The antioxidant activities of propolis samples were measured using model systems including the analysis of the scavenging activities for 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals and the beta-carotene bleaching assay. The results showed that propolis had a higher free radical scavenging and lipid peroxidation inhibitory capacity than butylated hydroxytoluene and quercetin, antioxidants used in the pharmaceutical and food industries. The concentration required to scavenge 50% of free radicals (SC(50)) values differed depending on the sample collection month. Samples collected in November had the highest antioxidant capacity. In all cases, SC(50) values of propolis samples obtained by scraping were similar to those collected from a wire mesh (5 microg/mL for ABTS and 20-30 microg/mL for DPPH radicals). A significant positive correlation was found between the antioxidant capacity and flavonoid content of each analyzed extract. The chemical profiles were very similar. Galangin (3,5,7-trihydroxyflavone), an antioxidant compound, was detected in all samples as a major compound. The chromatographic profile suggests that of Baccharis sp., which would be one of the botanical sources of propolis from western Argentina, and the content of galangin can be used as a parameter for evaluating propolis quality. Our results suggest that Argentine propolis from Cuyo is a promising source of bioactive compounds as ingredients for developing functional foods with a beneficial impact on oxidative stress.