The standardization of apiceutical products like as propolis extracts has been widely debated worldwide and variations in the propolis chemical composition are still very relevant topics for ...use-standardized of different propolis-type as medication by much of the world's population. The present manuscript discuss important issues related to the climate effect and variations in propolis metabolite-profiling changes, antioxidant capacity and variations of the antibacterial activity of the Brazilian red propolis metabolites using comprehensive multivariate correlations. It was observed the increasing of guttiferones concentrations during the intense drought period and drastic decreasing in rainy period. The climate variation induced the high concentration of flavonoids in rainy period with pronounced dropped in some rainy months. The Pearson´s analysis demonstrated correlation between IC
from DPPH and guttiferones and flavonoids concentrations. The PCA-X and Hotelling T2 test showed outliers during the months with lowest concentrations of formononetin and isoliquiritigenin was observed in antibacterial tests. The PLS-DA, OPLS-DA and VIP analysis demonstrate guttiferone E, guttiferone B, liquiritigenin, naringenin are considered important substances responsible by anti-staphylococcal activity in red propolis composition during the rainy season and drought period, but a synergistic effect with other flavonoids and isoflavonoids are not ruled out.
Lipases have key roles in insect lipid acquisition, storage, and mobilization and are also fundamental to many physiological processes in insects. Lipids are an important component of insect diets, ...where they are hydrolyzed in the midgut lumen, absorbed, and used for the synthesis of complex lipids. The South American palm weevil
is one of the most important pests on commercial palm plantations. However, there are few studies about lipid digestion for this insect. In this work, we have described the biochemical characterization of the lipase activity in the posterior midgut of the
palm weevil. Lipase activity was highest between the temperatures of 37 °C and 45 °C and at pH 6.5. Lipase activity was also sensitive to variations in salt and calcium concentrations. Lipases have been described structurally as enzymes with the Ser-His-Asp Catalytic Triad, containing an active serine. The serine protease inhibitor PMSF (phenylmethane sulfonyl fluoride) inhibited the lipases from
, demonstrating the importance of a serine residue for this activity. The ability of the lipases to hydrolyze
-Nitrophenyl esters with different chain lengths has revealed the activities of a broad range of substrates. The lipase activities of
increased in the presence of reduced glutathione (GSH) and dithiothreitol (DTT), while in the presence of oxidized glutathione (GSSG), activities were drastically reduced. To our knowledge, this study has provided the first information about lipase activity in the
palm weevil.
The ever-increasing demand for natural products and biotechnology derived from bees and ultra-modernization of various analytical devices has facilitated the rational and planned development of ...biotechnology products with a focus on human health to treat chronic and neglected diseases. The aim of the present study was to prepare and characterize polymeric nanoparticles loaded with Brazilian red propolis extract and evaluate the cytotoxic activity of “multiple-constituent extract in co-delivery system” for antileishmanial therapies. The polymeric nanoparticles loaded with red propolis extract were prepared with a combination of poly-ε-caprolactone and pluronic using nanoprecipitation method and characterized by different analytical techniques, antioxidant and leishmanicidal assay. The red propolis nanoparticles in aqueous medium presented particle size (200–280 nm) in nanometric scale and zeta analysis (−20 to −26 mV) revealed stability of the nanoparticles without aggregation phenomenon during 1 month. After freeze-drying method using cryoprotectant (sodium starch glycolate), it was possible to observe particles with smooth and spherical shape and apparent size of 200 to 400 nm. Attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR) and thermal analysis revealed the encapsulation of the flavonoids from the red propolis extract into the polymeric matrix. Ultra performance liquid chromatography coupled with diode array detector (UPLC-DAD) identified the flavonoids liquiritigenin, pinobanksin, isoliquiritigenin, formononetin and biochanin A in ethanolic extract of propolis (EEP) and nanoparticles of red propolis extract (NRPE). The efficiency of encapsulation was determinate, and median values (75.0 %) were calculated using UPLC-DAD. 2,2-Diphenyl-1-picryhydrazyl method showed antioxidant activity to EEP and red propolis nanoparticles. Compared to negative control, EEP and NRPE exhibited leishmanicidal activity with an IC50 value of ≅38.0 μg/mL and 31.3 μg/mL, 47.2 μg/mL, 154.2μg/mL and 193.2 μg/mL for NRPE A1, NRPE A2, NRPE A3 and NRPE A4, respectively. Nanoparticles loaded with red propolis extract in co-delivery system and EEP presented cytotoxic activity on
Leishmania (V.) braziliensis
. Red propolis extract loaded in nanoparticles has shown to be potential candidates as intermediate products for preparation of various pharmaceutical dosage forms containing red propolis extract in the therapy against negligible diseases such as leishmaniasis.
Graphical Abstract
Some biochemical mechanisms of cellular debridement of
Leishmania (V.) braziliensis
species by the flavonoids of red propolis extract (EEP) or NRPE loaded with red propolis extract
This study aimed to evaluate the physical–chemical properties (particle size, zeta potential, encapsulation, and thermal stability), antioxidant properties, antibacterial properties and ...casein-flavonoid interaction studies of soluble complexes, called caseinates of red propolis. The caseinates of red propolis were successfully prepared using the spray-dryer technique, which presented two populations of nanometre and micrometre particles, and were able to encapsulate flavonoids and isoflavonoids from the red propolis extract as a soluble complex. SEM analysis demonstrated casein nanoparticles and fat globules combined with lipophilic compounds (terpenes) from red propolis extract. FTIR analysis proved the encapsulation of flavonoids into caseinates. The thermogravimetric assays demonstrated thermal stability of red propolis caseinates and DTA analysis observed the denaturation during the coagulation temperature. The fluorescence, antioxidant, Folin–Ciocalteu method and chromatographic assays have shown that flavonoids bind to the amino acid residues present in the casein protein matrix, demonstrating a reversible interaction between flavonoids and casein amino acids. Dissolution studies prove the formation of a casein-flavonoids soluble complex and can bring benefits and increase the process of absorption of flavonoids by biological membranes. Despite the interaction of flavonoids with casein amino acids, caseinates of red propolis demonstrated antimicrobial activity against
Staphylococcus aureus
and
Pseudomonas aeruginosa
. The caseinates of red propolis can be easily incorporated in foods such as cakes, pies, dairy and cocoa such as foods bio-preservatives. The caseinates of red propolis can be manufactured by the pharmaceutical and nutraceuticals industries as intermediary bioproduct in the powder form for supplements, capsules and oral emulsion systems for beverages as yogurts.
The chitosan microcapsules containing Brazilian red propolis extract (RPE) obtained by spray-drying also called chitosanates of red propolis extract were prepared and characterized using techniques ...of particle size, scanning electron microscopy, infrared spectroscopy, thermal analysis, dissolution studies and antibacterial activity. An amount of five compositions of chitosanate hydrogels which were prepared at the concentrations between 16 and 75% of red propolis extract and characterized by particle size analysis showed 2 subpopulations of particle between 0.30 and 8.00 μm. The chitosanates in solid state obtained by spray-drying showed a rounded shape and particle diameter between 1.0 and 30 μm by SEM analysis. The thermal analysis and FTIR data demonstrate encapsulation of the bioactive red propolis extract into chitosan bio-polymeric system, and chemical reaction between chitosan and RPE was not detected. The chitosanates containing 35%, 50% and 75% of red propolis extract demonstrated in vitro release of flavonoids following a concentration-dependent and pH-dependent model. The modified release in simulate gastrointestinal tract conditions was proved. The chitosanates of red propolis extract obtained in the solid state were reversibly dissolved in chitosanate hydrogels in an appropriate dissolution medium to release the active flavonoids from the Brazilian red propolis extract. Antibacterial activity of chitosanates against
Staphylococcus aureus
was demonstrated. The chitosanates loaded with red propolis extract can be easily incorporated into food, in the production of biodegradable films, as a bio-preservative and can be manufactured by the pharmaceutical and nutraceutical industries as an intermediate bio-product in the form of powder for supplements, capsules and oral emulsifying systems.
This work prepared and characterized microcapsule of
Uncaria tomentosa
(UT) in order to standardize a spray-dryer
Uncaria tomentosa
extract. The UT bark powder was subjected to extraction by ...maceration using hydro-ethanol solution. The
Uncaria tomentosa
extract was used to prepare the spray-dryer microcapsules UT-F1. The UT extract and microcapsules UT-F1 were submitted to chemical and physicochemical characterization tests. The phytochemical tests revealed the presence of alkaloids and phenolic compounds such as catechin. The UT extract and microcapsules UT-F1 showed high content of total phenols (28.48% ± 0.76 and 36.34% ± 0.22), high catechin content (47.95% ± 4.90 and 51.15% ± 4.20) and high antioxidant activity with IC
50
values of 5.80 and 5.03 µg cm
−3
. The SEM, FTIR and TG analysis confirmed the morphology of spherical particles, the microencapsulation of the constituents of the UT extract, low moisture content, as well as stability of the microcapsules UT-F1. The DSC analysis and dissolution tests showed the technological influence of spray-dried starch combined UT extract considered water-poorly soluble resulting in vitro release (52.9%) of polyphenolic compounds from
Uncaria tomentosa
microcapsules. The combined use of disintegrants with a natural surfactant in the UT microcapsules has improved the release of polyphenols (catechin) from spray-dryer herbal composition reaching an equivalent release of 78.6% of catechin after 240 min. The in vitro release of microcapsules UT-F1 responds depending on the concentration of pharmaceutical excipients considered disintegrating and can easily achieve release greater than 80%. The microcapsules UT-F1 can be used as bulk material for herbal products in pharmaceutical industry.
The aim of this study was to investigate the chemical composition of
Origanum vulgare L. essential oil, the inhibitory effect of the oil on the cell viability of
Staphylococcus aureus strains ...isolated from foods, and the influence of sub-inhibitory concentrations of the oil on some physiological attributes of these strains. GC–MS analysis showed that carvacrol (57.71%) was the most prevalent compound in the oil, followed by
p-cymene (10.91%), γ-terpinene (7.18%), terpinen-4-ol (6.68%) and thymol (3.83%). The results showed that
O. vulgare essential oil at 0.03, 0.6 and 0.12
μL
mL
−1 inhibited the cell viability of
Staph. aureus. At 0.12
μL
mL
−1 the oil caused cidal effect with decrease ≥3
log cycles of the initial inoculum after 15
min of exposure. Sub-inhibitory concentrations (0.03 and 0.015
μL
mL
−1) of the oil suppressed some physiological attributes of the
Staph. aureus strains such as coagulase, lipase and salt tolerance. The oil interfered on the microbial metabolic activity in a dose-dependent manner.
O. vulgare essential oil could be a novel antimicrobial with capability to suppress some physiological characteristics, in addition to inhibit the growth and survival of pathogen bacteria in foods, particularly
Staph. aureus.
Clozapine is an antipsychotic drug used for refractory schizophrenia and severe psychiatric disorders associated with several side effects. Studies on standardization of raw material and bulk ...products are necessary to ensure reproducibility batch to batch during all stages of the industrial pharmaceutical process. The aim of this study was to conduct studies of polymorphic characterization and compatibility study of clozapine. Different solvatomorphic forms of clozapine were obtained by recrystallization technique. Polymorphic characterization was performed using optical microscopy, SEM, intrinsic dissolution, and thermal analysis. Compatibility studies of clozapine:excipients were performed by TG and DSC techniques. The polymorphic characterization obtained by analytical and thermal techniques showed the formation of a solvatomorphic form of clozapine (clozapine monohydrate) when recrystallized in aqueous solvents and in alkaline medium. The polymorphic form (clozapine anhydrate) showed higher intrinsic dissolution rate compared to solvatomorphic form (clozapine monohydrate). All industrial batches of clozapine presented in anhydrate form. The DSC/TG data demonstrated similar melting peaks for 2 polymorphic forms, but desolvation peaks characteristic of monohydrate form was observed in clozapine monohydrate. Studies of binary mixtures showed no incompatibilities between clozapine and excipients, except for clozapine:lactose which can reduce the stability of bulk and tablets of clozapine. Tablets of clozapine presented the same thermal analysis profile of clozapine:lactose but did not contribute in decreasing shelf life of clozapine tablets before 24 months of storage. Dissolution studies of the tablets did not show variability between batches of clozapine during 24 months but presented decreasing on stability for 36 months of storage.
The aim of this study was to characterize tinctures and microcapsules loaded with an ethanol extract of red propolis through chemical, physicochemical and microbiological assays in order to establish ...quality control tools for nutraceutical preparations of red propolis. The markers (isoflavonoids, chalcones, pterocarpans, flavones, phenolic acids, terpenes and guttiferones) present in the tinctures A and B were identified and confirmed using LC/ESI/FTMS/Orbitrap. Four compositions (A, B, C and D) were prepared to contain B tincture of the red propolis with some pharmaceutical excipients and submitted to two drying processes, i. e. spray-drying and freeze-drying to obtain microcapsules loaded with the red propolis extract. The tinctures and microcapsules of the red propolis were submitted to the total flavonoid content and antioxidant activity tests. The antibacterial activity and minimum inhibitory concentration (MIC) were tested using Staphylococcus aureus ATCC 25293 and Pseudomonas aeruginosa ATCC 27853 strains. The tinctures and microcapsules presented high flavonoid quantities from 20.50 to 40.79 mg/100 mg of the microcapsules. The antioxidant activity and IC50 were determined for the tinctures A and B (IC50: 6.95 μg/mL and 7.48 μg/mL), the spray-driedmicrocapsules (IC50: 8.89-15.63 μg/mL) and the freeze-dried microcapsules (IC50: 11.83-23.36 μg/mL). The tinctures and microcapsules were proved to be bioactive against gram-positive and gram-negative bacteria with inhibition halos superior to 10 mm at concentration of 200 μg/mL and MIC values of 135.87-271.74 μg/mL using gram-positive strain and 271.74-543.48 μg/mL using gram-negative strain. The tinctures and microcapsules of the red propolis have a potential application for nutraceutical products.
Purpose: Quercetin is a flavonoid known for its therapeutic properties and for forming complexes. Although the antimony-quercetin (SbQ) complex has been produced before, no previous exploration of ...its characteristics has been published in literature. Thus, this study aimed to characterize this complex, assess its stability and investigate its complexation site through its antibacterial activity. Methods: The SbQ complex was synthetized using Sb(III) potassium tartrate trihydrate and quercetin anhydrous (1:1) (v/v) as a solution and dried using three methods: rotaevaporation, lyophilization and spray drying. The material, in solution, was analyzed by UV-vis and fluorimetry; and, in the powder, by X-ray diffraction (XRD), both scanning electronic and fluorescence microscopy and infrared spectroscopy (FT-IR). Antimicrobial activity was evaluated via broth microdilution. Results: UV-vis exhibited a shoulder peak at 291 nm indicating metal chelation at C-ring of quercetin and confirmed 1:1 stoichiometry. Spectrofluorimetry showed an increase of intensity with the complex formation with an emission band (525 nm). After drying, XRD and SEM indicated loss of crystallinity and a difference in shape and size of the complex compared to its precursors. FT-IR suggested by a shift of frequency of the carbonyl group (1661 cm-1) that the quercetin bond to antimony by the C-3, followed by positions C-5 and C-4 carbonyl, which has been confirmed by MIC through the structure-activity relationship of the antibacterial activity of quercetin. Conclusion: These results provided a characterization of SbQ complex with the confirmation of its binding site, working as a guide for future studies involving this complex.
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