Search

Aspidosperma pyrifolium Mart., Apocynaceae, is a species popularly known with the popular Brazilian names of “pereiro” and “pau-pereiro.” It is a native tree from the Caatinga biome, and the flowers frequently attract bees. The species is known for the presence of plumeran indole alkaloids. In this study, the alkaloidal fraction of A. pyrifolium flowers resulted in the characterization of eighteen plumeran indolic alkaloids via ultra-performance liquid chromatography coupled with diode array and quadrupole time-of-flight mass spectrometry. Four of these alkaloids were isolated, and their structures were established by different spectroscopic methods. The novel indole alkaloid N-formyl-15-methoxy-aspidofractinin, in addition to the known alkaloids pyrifoline, aspidospermine, and 15-methoxy-aspidospermine, was identified from the analyzed plant.

Ethnopharmacological relevance Commiphora leptophloeos (Mart.) J.B. Gillett, popularly known as “imburana”, “imburana-de-cheiro” or “imburana-de-espinho”, has been used in folk medicine for the treatment of gastrointestinal diseases, such as diarrhea. The indian tribes “Kairir-Shoko and shoko use the bark to treat diarrhea. However, there is no scientific evidence to justify the therapeutic use of this species. Aim of the study To investigate the ethnomedicinal use of Commiphora leptophloeos, with respect to the antimicrobial, antisecretory, antimotility and antispasmodic activities of the crude ethanolic extract obtained from its leaves (CL-EtOHL) and the mechanism underlying this action in rodents. Material and methods In the evaluation of antibacterial and antifungal activities was determined the minimum inhibitory concentration (MIC) of the extract, against different strains of bacteria and fungi. All experimental protocols were approved by the Animal Ethics Committee of the Federal University of Paraiba (045/2016). In addition, behavioral screening and acute toxicity assessment of CL-EtOHL were performed in female mice (n = 6). In the investigation of antidiarrheal activity (n = 6), frequency of defecation and number of liquid stools, were classified during 4 h, and intestinal fluid and transit were measured. In addition, the antispasmodic effect on rat ileum (n = 5) was also investigated. Results The ethanolic extract is rich in flavonoids and the main were identified as C-glycosylated flavonoids (isoorientin, orientin, and vitexin). In the evaluation of antimicrobial and antifungal activity, the extract showed moderate efficacy only against the tested strains of Candida krusei ATCC-6258, Candida parapsilosis ATCC-22019 and Candida glabrata ATCC-90030. The extract had no toxic effect until 2000 mg/kg. In castor oil-induced diarrhea, CL-EtOHL inhibited, in a dose-dependent manner, both total defecation frequency (ED50 = 380.4 ± 145.4 mg/kg) and the number of watery stools (ED50 = 151.2 ± 76.3 mg/kg). The extract showed no effect on fluid accumulation or normal intestinal transit. On the other hand, when the animals were pretreated with castor oil, the extract decreased the distance traveled by the activated charcoal (ED50 = 177.0 ± 50.3 mg/kg). In the investigation of antispasmodic effect, CL-EtOHL antagonized the contractions induced by KCl 30 mM (IC50 = 208.2 ± 25.9 μg/mL) and CCh 10−6 M (IC50 = 95. ± 22.0 μg/mL). To verify the participation of muscarinic receptors in this effect, cumulative carbachol curves were performed in the absence and presence of the extract, and a non-competitive pseudo-irreversible antagonism of these receptors was observed. Conclusion The data indicate that ethanol extract obtained from the leaves of Commiphora leptophloeos has an antidiarrheal effect due to inhibition of the intestinal motility and antispasmodic effect, through the antagonism of muscarinic receptors. In addition, we suggest that flavonoids isolated from CL-EtOHL may be responsible for antidiarrheal activity of this extract. This explains its ethnomedicinal use in the treatment of diarrhea.

Commiphora leptophloeos is known as “amburana-de-espinhos” or “Imburana” in Brazil. This plant species has been used as a material for combustion and construction, as well as medicinally. Traditional communities use this plant in the treatment of such as flu, urinary diseases and injuries, its pharmacological properties are attributed to the presence of tannins, saponins, flavonoids and alkaloids. Thus, this study aimed to evaluate the antimicrobial and antibiotic-modulating activity of the ethanolic extract of C. leptophloeos leaves. The chemical characterization of the extract was performed by UPLC-QTOF-MS/MS, confirming the presence of phenols and flavonoids of recognized pharmacological activity. To evaluate the antibacterial activity and ability of the extract to modulate the antibiotic activity of aminoglycosides towards resistant bacteria, the microdilution method was used in broth with determination of Minimum Inhibitory Concentration (MIC). The microorganisms used in the assays included standard and multi-drug resistant strains of Peudomonas aeruginosa and Staphylococcus aureus. The results were analyzed by ANOVA and Bonferroni’s posttest. The ethanolic extract of the leaves of Commiphora leptophloeos presented no clinically relevant intrinsic antibacterial activity with MIC ≥ 2048 μg/mL. However, modulation tests revealed that the extract significantly reduced the MIC values ​​of the antibiotics, indicating that the extract enhanced the action of the antibiotics against resistant microorganisms. In conclusion, C. leptophloeos has antibiotic-modulating potential. However, further research is recommended to better clarify the mechanism of action of the tested plant extract, guiding the development of new alternatives for the treatment of infections resistant to conventional therapies.

Melissopalynological, physicochemical analysis, mineral content, antiradical activity and profile of compounds by Ultra-Performance Liquid Chromatography coupled with a Diode Array Detector and quadrupole Time of Flight Mass Spectrometry (UPLC-DAD-qTOF-MS/MS) of Frieseomelitta doederleini honeys from semiarid region of the Northeast of Brazil are presented. The melissopalynological analysis showed two principal pollen types of Mimosa tenuiflora (jurema preta) and Shinus sp (aroeira). The chemical profile data obtained by UPLC-DAD-qTOF-MS/MS of the Mimosa tenuiflora flowers (principal pollen of honey) and the five samples of F. doederleini honeys both flowers and honey showed similar profile. Abelha branca honeys samples had similar characteristic profile of phenolic compounds (flavonoids), and also antiradical activity. The main flavonoids identified in the honey samples in the jurema preta flowers were flavonols/flavone and flavanols/flavanones aglycones. All the flavonoids identified showing that the nectar collected by the bees may be from this plant species. The antiradical activity of the honey samples strongly correlated with their phenolic content. Among the minerals analyzed, potassium was the most abundant, followed by magnesium.

The geopropolis produced by the stingless bee Melipona subnitida (popularly called “jandaíra” in Brazil) is a mixture of resin, wax, and mud. This study analyzed the antifungal activity of the geopropolis extract from Candida spp., developed a gel formulation with this extract and analyzed the delivery of bioactives (kinetics release) in the formulation and their chemical profile by UHPLC-PDA-qTOF-MS/MS. Three different gels were prepared using the geopropolis extract, carbomer, propylene glycol, and water. Formulations with different amounts of propylene glycol were investigated. Physical, visual, pH, viscosity, adhesion, spreadability, leakage, and in vitro release tests were performed in the proposed formulations. Antifungal tests with the geopropolis ethanolic extract were carried out against six Candida species. The chemical profile of the geopropolis extract and compounds released from the formulations were analyzed after the release test. The formulations had a pH between 4.6 and 4.8 and viscosity between 535,600 and 920,400 cPs. The geopropolis extract presented excellent antifungal activity against the tested yeasts. The results of the release test in semipermeable cellulose membrane showed that all formulations containing 5%, 10% and 40% propylene glycol presented release of geopropolis extract. For adhesion and leakage tests, the gel formulation with 5% propylene glycol was more effective. Both geopropolis ethanolic extract and the liquid obtained in the release test showed the presence of flavonoids (flavonol/flavone, flavanone, and chalcones). Gel formulations with geopropolis extract that are rich in flavonoids are promising as an adjuvant treatment of vaginal candidiasis. Keywords: Geopropolis, Melipona subnitida, Jandaíra, Flavonoids, Delivery system, Candidiasis

Phytochemical investigation of flowers from Geoffroea spinosa via ultra-performance liquid chromatography coupled with diode array and quadrupole time-of-flight mass spectrometry (UPLC-DAD-TOF-MS/MS) resulted in the characterization of fourteen compounds: six flavonoids, three hydroxycinnamic acid derivatives, and five hydroxycinnamic acid amide derivatives. This is the first report on the identification of hydroxycinnamic acid amide derivatives from the genus Geoffroea. The chemotaxonomic significance of the identified compounds is discussed.