ABSTRACT
Autophagy is a degradation process that is evolutionarily conserved and is essential in maintaining cellular and physiological homeostasis through lysosomal removal and elimination of damaged peptides, proteins and cellular organelles. The dysregulation of autophagy is implicated in various diseases and disorders, including cancers, infection-related, and metabolic syndrome-related diseases. Propolis has been demonstrated in various studies including many human clinical trials to have antimicrobial, antioxidant, anti-inflammatory, immune-modulator, neuro-protective, and anti-cancer. Nevertheless, the autophagy modulation properties of propolis have not been extensively studied and explored. The role of propolis and its bioactive compounds in modulating cellular autophagy is possibly due to their dual role in redox balance and inflammation. The present review attempts to discuss the activities of propolis as an autophagy modulator in biological models in relation to various diseases/disorders which has implications in the development of propolis-based nutraceuticals, functional foods, and complementary therapies.
Subject(s)
Autophagy , Inflammation , Oxidation-Reduction , Propolis , Propolis/pharmacology , Humans , Autophagy/drug effects , Inflammation/drug therapy , Inflammation/metabolism , Inflammation/pathology , Animals , Oxidation-Reduction/drug effects , Anti-Inflammatory Agents/pharmacologyABSTRACT
A large series of chalcones were synthesized and studied for activity against Candida albicans. The SAR analysis showed that the antifungal activity was highly dependent on the substitution pattern of the aryl rings and correlated to a large extent with the ability of compounds to interact with sulfhydryl groups. The most active were the hydroxylated chalcones as their activity related to the location of the phenolic group in the aryl ring B as follows: o-OH>p-OH approximately 3,4-di-OH>m-OH. These and other correlations obtained strongly contribute to the knowledge for design of anticandidal chalcones.
Subject(s)
Antifungal Agents/chemical synthesis , Candida albicans/drug effects , Chalcones/chemical synthesis , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Chalcones/chemistry , Chalcones/pharmacology , Colony Count, Microbial , Microbial Sensitivity Tests , Structure-Activity RelationshipABSTRACT
Propolis is a beehive product with a very complex chemical composition, widely used in folk medicine because of its several therapeutic activities. Its biological properties and chemical composition may vary according to the geographic location and to the different plant sources. The possible mechanism of action of propolis as well as of its active compounds has been the subject of researchers in recent years. In this work, first we reported the results of our study on the seasonal effect of the immunomodulatory action of propolis on antibody production in bovine serum albumin (BSA)-immunized rats. Then, we compared the effect of Brazilian and Bulgarian propolis, some isolated compounds and Baccharis extract on anti-BSA antibody levels. Based on the results, we conclude that propolis stimulates antibody production, independently of the season and geographic origin. Caffeic acid, quercetin and Baccharis extract had no effect on antibody production, although the importance of isolated compounds is well reported in other biological assays. Propolis action is a consequence of plant-derived products with synergic effects, while isolated compounds or extracts from its plant sources had no effect in this assay.
Subject(s)
Anti-Infective Agents/pharmacology , Antibody Formation/drug effects , Antioxidants/pharmacology , Caffeic Acids/pharmacology , Immunologic Factors/pharmacology , Propolis/pharmacology , Quercetin/pharmacology , Animals , Anti-Infective Agents/immunology , Antioxidants/isolation & purification , Brazil , Bulgaria , Caffeic Acids/isolation & purification , Immunologic Factors/isolation & purification , Male , Propolis/immunology , Quercetin/isolation & purification , Rats , SeasonsABSTRACT
Paracoccidioidomycosis is the most important systemic mycosis in Latin America. Its etiological agent, Paracoccidoides brasiliensis, affects individuals living in endemic areas through inhalation of airborne conidia or mycelial fragments. The disease may affect different organs and systems, with multiple clinical features, with cell-mediated immunity playing a significant role in host defence. Peritoneal macrophages from BALB/c mice were stimulated with Brazilian or Bulgarian propolis and subsequently challenged with P. brasiliensis. Data suggest an increase in the fungicidal activity of macrophages by propolis stimulation, independently from its geographic origin.
Subject(s)
Antifungal Agents/pharmacology , Macrophages, Peritoneal/drug effects , Paracoccidioides/drug effects , Propolis/pharmacology , Animals , Bees , Brazil , Bulgaria , Interferon-gamma , Macrophage Activation/immunology , Macrophages, Peritoneal/immunology , Macrophages, Peritoneal/microbiology , Male , Mice , Mice, Inbred BALB C , Paracoccidioides/growth & development , Propolis/isolation & purificationABSTRACT
Propolis samples from different geographic origins were investigated for their antibacterial (against Staphylococcus aureus and Escherichia coli), antifungal (against Candida albicans) and antiviral (against Avian influenza virus) activities. All samples were active against the fungal and Gram-positive bacterial test strains, and most showed antiviral activity. The activities of all samples were similar in spite of the differences in their chemical composition. In samples from the temperate zone, flavonoids and esters of phenolic acids are known to be responsible for the above mentioned activities of bee glue; tropical samples did not contain such substances but showed similar activities. Obviously, in different samples, different substance combinations are essential for the biological activity of the bee glue. It seems that propolis has general pharmacological value as a natural mixture and not as a source of new powerful antimicrobial, antifungal and antiviral compounds.
Subject(s)
Candida albicans/drug effects , Escherichia coli/drug effects , Influenza A virus/drug effects , Propolis/pharmacology , Staphylococcus aureus/drug effects , Animals , Anti-Bacterial Agents , Anti-Infective Agents/pharmacology , Antifungal Agents/pharmacology , Antiviral Agents/pharmacology , Antiviral Agents/toxicity , Cell Culture Techniques , Chick Embryo , Fibroblasts/virology , Flavonoids/analysis , Phenols/analysisABSTRACT
The behavior of microorganisms towards the antibiotic action of propolis has been widely investigated. Since reports dealing with seasonal effect on propolis activity are not available, this assay was carried out aiming to observe the in vitro antimicrobial activity of propolis, collected during the four seasons, on bacterial strains isolated from human infections. Dilution of ethanolic extract of propolis (EEP) in agar was the method performed, with serial concentrations ranging from 0.4 to 14.0% (% v/v). The behavior of some bacteria was analysed according to the incubation period in medium plus propolis, and the survival curve was plotted. It was verified that the growth of Gram-positive bacteria is inhibited by low propolis concentrations (0.4%) whereas Gram-negative bacteria were less susceptible to this substance, the minimal inhibitory concentration ranging from 4.5 to 8.0%. There was no significant difference with regards to the seasonal effect on the survival curve of Staphylococcus aureus and Escherichia coli; after incubation with propolis, there was an efficient antimicrobial action, mainly towards Gram-positive bacteria.
Subject(s)
Anti-Bacterial Agents/pharmacology , Bacteria/drug effects , Propolis/pharmacology , Bacteria/isolation & purification , Brazil , Humans , Microbial Sensitivity Tests , SeasonsABSTRACT
The effect of a water-soluble derivative (WSD) of propolis on the classical pathway (CP) and the alternative (AP) complement activity has been investigated. The in vitro experiments show that WSD inhibits both pathways and the effect depends on the source of complement. The suppression of complement-mediated haemolysis proves to be time- and temperature-related. High WSD concentrations cause direct damage of the target erythrocytes. The estimation of C3-residual activity indicates that the preparation diminishes C3 functional activity.
Subject(s)
Complement C3/antagonists & inhibitors , Complement Inactivator Proteins/pharmacology , Propolis/pharmacology , Animals , Buffers , Complement Hemolytic Activity Assay , Dose-Response Relationship, Drug , Erythrocytes/drug effects , Guinea Pigs , Hemolysis/drug effects , Humans , Mice , Propolis/chemistry , Solubility , Water/chemistryABSTRACT
The water soluble derivative (WSD) of propolis in a dose of 150 mg/kg was administered intravenously (i.v.), intraperitoneally (i.p.) and orally (p.o.) to mice. The alteration of serum alternative pathway (AP) complement level was observed. The WSD also influenced the process of acute inflammation provoked by zymosan in mice. The effect was strongly dependent on the route of WSD administration.
Subject(s)
Adjuvants, Immunologic/pharmacology , Complement Pathway, Alternative/drug effects , Propolis/pharmacology , Adjuvants, Immunologic/administration & dosage , Adjuvants, Immunologic/therapeutic use , Administration, Oral , Animals , Complement Hemolytic Activity Assay , Edema/drug therapy , Female , Hindlimb , Inflammation/chemically induced , Inflammation/drug therapy , Injections, Intraperitoneal , Injections, Intravenous , Male , Mice , Mice, Inbred ICR , Propolis/administration & dosage , Propolis/therapeutic use , Solubility , Water/chemistry , Zymosan/administration & dosage , Zymosan/toxicityABSTRACT
Four compounds were isolated from Brazilian propolis. They are identified as: (1) 3-prenyl-4-hydroxycinnamic acid (PHCA), (2) 2,2-dimethyl-6-carboxyethenyl-2H-1-benzopyrane (DCBEN), (3) 3,5-diprenyl-4-hydroxycinnamic acid (DHCA), and (4) 2,2-dimethyl-6-carboxyethenyl-8-prenyl-2H-1-benzopyran (DPB). The structures of the compounds were determined by MS and NMR techniques. All compounds were assayed against Trypanosoma cruzi and the bacteria Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Streptococcus faecalis. Compounds (1) to (4) were active against T. cruzi. Except (1), all compounds presented activity against the bacteria tested. When compounds (1)-(3) were tested in the guinea pig isolated trachea, all induced a relaxant effect similar to propolis extract.
Subject(s)
Anti-Bacterial Agents/pharmacology , Phenols/pharmacology , Propolis/chemistry , Animals , Anti-Bacterial Agents/isolation & purification , Brazil , Chromatography, High Pressure Liquid , Female , Guinea Pigs , In Vitro Techniques , Magnetic Resonance Spectroscopy , Male , Muscle Relaxation/drug effects , Muscle, Smooth/drug effects , Phenols/isolation & purification , Spectrophotometry, Ultraviolet , Trypanocidal Agents/isolation & purification , Trypanocidal Agents/pharmacology , Trypanosoma cruzi/drug effectsABSTRACT
Three ent-kaurene diterpenoids, not previously described as constituents of propolis, were isolated from a sample collected by Brazilian native bees Melipona quadrifasciata anthidioides. One of them, kaurenoic acid, as well as the total extract, displayed moderate antibacterial activity.
Subject(s)
Anti-Bacterial Agents/pharmacology , Bees , Diterpenes/pharmacology , Escherichia coli/drug effects , Propolis/chemistry , Staphylococcus aureus/drug effects , Animals , Anti-Bacterial Agents/isolation & purification , Brazil , Diterpenes/isolation & purification , Humans , Microbial Sensitivity TestsABSTRACT
Alkaloids isolated from Crinum species have been reviewed for the period 1985-2000. Non-nitrogenous compounds have been surveyed for the first time. Botanical classification and biological activity are discussed. Spectral data literature sources are listed.
Subject(s)
Alkaloids/isolation & purification , Liliaceae/chemistry , Plants, Medicinal/chemistry , Alkaloids/chemistry , Alkaloids/pharmacology , Animals , Anti-Infective Agents/chemistry , Anti-Infective Agents/isolation & purification , Anti-Infective Agents/pharmacology , Antineoplastic Agents/chemistry , Antineoplastic Agents/isolation & purification , Antineoplastic Agents/pharmacology , Insecticides/chemistry , Insecticides/isolation & purification , Insecticides/pharmacology , Liliaceae/classification , Molecular Structure , Phytotherapy , Plants, Medicinal/classificationABSTRACT
Several phenolic constituents of propolis and their synthetic analogs were derivatized with L-lysine. The ability of these complexes to alter complement activity was estimated in vitro in human serum. The influence of selected complexes on C3 hemolytic activity via classical pathway (CP) and alternative pathway (AP) and on zymosan-induced AP activation was determined. The results suppose that the anticomplement effect of the complexes might be related to the interaction with C3 complement component.
Subject(s)
Complement Inactivator Proteins/pharmacology , Complement Pathway, Alternative/drug effects , Complement Pathway, Classical/drug effects , Flavanones , Hemolysis/drug effects , Lysine , Phenols/pharmacology , Propolis/pharmacology , Esters , Flavonoids/pharmacology , Humans , Structure-Activity Relationship , Zymosan/pharmacologyABSTRACT
Two diterpene glycosides, ent-8(17)-labden-15-O-alpha-L-rhamnoside and ent-8(17)-labden-15-O-(3'-O-acetyl)-alpha-L-rhamnoside (new natural compounds) were isolated from propolis from El Salvador. The compounds showed significant antibacterial activity and moderate toxicity to Artemia salina nauplii. These are the first glycosides reported in bee glue.
Subject(s)
Diterpenes/chemistry , Glycosides/chemistry , Propolis/chemistry , Rhamnose/chemistry , Animals , Artemia/drug effects , Decapoda/drug effects , Diterpenes/isolation & purification , Diterpenes/toxicity , Glycosides/isolation & purification , Glycosides/toxicity , Models, Molecular , Ovum/drug effects , Rhamnose/isolation & purificationABSTRACT
Twenty-one propolis samples produced by 12 different Meliponinae species were analyzed by GC-MS. Several chemical types of stingless bees' propolis could be grouped, according to the prevailing type of compounds like: 'gallic acid", "diterpenic" and "triterpenic" types. The results confirm that neither the bee species nor the geographical location determine the chemical composition of Meliponinae propolis and the choice of its plant source, respectively. This could be explained by the fact that Meliponinae forage over short distances (maximum 500 m) and thus use as propolis source the first plant exudate they encounter during their flights. The antibacterial, antifungal and cytotoxic activities of the samples were also investigated. Most samples had weak or no activity against E. coli, weak action against Candida albicans. Some of them showed significant activity against St. aureus., presumably connected to the high concentration of diterpenic acids. Samples rich in diterpenic acids possessed also high cytotoxic activity (Artemia salina test).
Subject(s)
Bees , Candida albicans/drug effects , Escherichia coli/drug effects , Propolis/chemistry , Propolis/pharmacology , Staphylococcus aureus/drug effects , Animals , Brazil , Candida albicans/growth & development , Diterpenes/analysis , Escherichia coli/growth & development , Gallic Acid/analysis , Gas Chromatography-Mass Spectrometry , Microbial Sensitivity Tests , Species Specificity , Staphylococcus aureus/growth & development , Triterpenes/analysisABSTRACT
Four samples of Brazilian propolis were investigated by GC/MS of different fractions. 32 volatile compounds, (10 of them new for propolis), as well as 12 more polar compounds (one of them new for propolis) were identified. Antibacterial activity was found in some propolis fractions.
Subject(s)
Anti-Bacterial Agents/pharmacology , Propolis/chemistry , Propolis/pharmacology , Staphylococcus aureus/drug effects , Aldehydes/analysis , Animals , Anti-Bacterial Agents/chemistry , Bees , Carboxylic Acids/analysis , Esters/analysis , Hydrocarbons/analysis , Ketones/analysis , Microbial Sensitivity Tests , Terpenes/analysisABSTRACT
2',3'-Dihydroxy-4,4'-dimethoxychalcone (1) and 2',3',4-trihydroxy-4'-methoxy-chalcone, two new chalcones, were isolated from propolis from El Salvador. The compounds showed significant antibacterial and antifungal activity and moderate toxicity to Artemia salina nauplii.
Subject(s)
Anti-Infective Agents/chemistry , Artemia , Chalcone/chemistry , Propiophenones/chemistry , Propolis/chemistry , Animals , Anti-Bacterial Agents , Anti-Infective Agents/isolation & purification , Anti-Infective Agents/pharmacology , Antifungal Agents/chemistry , Antifungal Agents/isolation & purification , Antifungal Agents/pharmacology , Caffeic Acids/toxicity , Candida albicans/drug effects , Chalcone/isolation & purification , Chalcone/toxicity , Chromatography, Thin Layer , El Salvador , Escherichia coli/drug effects , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Models, Molecular , Molecular Conformation , Molecular Structure , Propiophenones/isolation & purification , Propiophenones/toxicity , Staphylococcus aureus/drug effectsABSTRACT
Four labdane-type diterpenic acids and syringaldehyde were isolated and identified from Brazilian propolis. All the compounds exhibit antibacterial activity. The diterpenes, found for the first time in propolis, are typical for some Araucaria species and thus indicate a possible plant source of Brazilian propolis.
Subject(s)
Anti-Bacterial Agents/isolation & purification , Diterpenes/isolation & purification , Plants , Propolis , Animals , Anti-Bacterial Agents/pharmacology , Bees , Brazil , Diterpenes/pharmacology , Microbial Sensitivity Tests , Staphylococcus aureus/drug effectsABSTRACT
The chemical composition of propolis from Bulgaria, Turkey, Greece and Algeria was investigated by GC-MS. All of them contained mainly flavonoids and esters of caffeic and ferulic acids, which indicated that their main source are buds of poplars of the taxonomic section Aegieros. Some Turkish samples contained a low percent of diterpenic acids, while in Algerian samples significant amounts of a hydroxyditerpenic acid (M=322, its structure not determined by its MS) were found. All samples showed significant antibacterial and weak to moderate antifungal activity.
Subject(s)
Anti-Bacterial Agents , Escherichia coli/drug effects , Propolis/chemistry , Propolis/pharmacology , Staphylococcus aureus/drug effects , Algeria , Animals , Bees , Bulgaria , Carbohydrates/analysis , Carboxylic Acids/analysis , Cycadopsida , Diterpenes/analysis , Escherichia coli/growth & development , Esters/analysis , Fatty Acids/analysis , Flavonoids/analysis , Gas Chromatography-Mass Spectrometry , Greece , Mediterranean Region , Staphylococcus aureus/growth & development , Trees , TurkeyABSTRACT
Chemometrics has been shown quite efficient to uncover relationships between chemical composition of a sample and its geographical origin. Forty propolis samples originated from the the South and South East of Brazil were analyzed by HPLC and 18 compounds of interest were studied which included: caffeic, p-coumaric and ferulic acids, and some of their derivatives, pinobanksin, a derivative of kaempferol and five phenolic compounds (assigned as 3-prenyl4-hydroxycinnamic acid (PHCA); 2,2-dimethyl-6-carboxyethnyl-2H-1-benzopyran (DCBE); 3,5-diprenyl-4-hydroxycinnamic acid (DHCA); compound E (still unknown) and 6-propenoic-2,2-dimethyl-8-prenyl-2H-1-benzopyran acid (DPB). Principal Component Analysis (PCA) indicated three different groups of propolis samples, having the same typical chromatogram, evaluated by HPLC. Samples from the South East group were rich in derivatives of kaempferol. Samples from the South group I had a high content of DPB compound, but a low concentration of kaempferol derivatives and of DCBEN compound. Samples from the South group II were characterized by a high concentration of DCBEN, DHCA, p-coumaric and DPB compounds. Therefore, the identification of new compounds in Brazilian propolis can give, useful information about the plant sources of a given geographic region.
Subject(s)
Flavonoids , Kaempferols , Phenols/analysis , Propolis/chemistry , Brazil , Chromatography, High Pressure Liquid , Geography , Quercetin/analogs & derivatives , Quercetin/analysisABSTRACT
The two investigated algae had almost identical sterol composition, but there were significant differences in the composition of the polar components and especially in the composition of the volatiles. P. denudata f. fragilis extracts possessed a stronger biological activity (antibacterial, antifungal and toxicity against Artemia salina). Despite the minute morphological differences between the two algae, we recommend P. denudata f. fragilis to be regarded as P. denudata subsp. fragilis.