Brazilian green and red propolis stand out as commercial products for different medical applications. In this article, we report the antimicrobial activities of the hydroalcoholic extracts of green ...(EGP) and red (ERP) propolis, as well as guttiferone E plus xanthochymol (8) and oblongifolin B (9) from red propolis, against multidrug‐resistant bacteria (MDRB). We undertook the minimal inhibitory (MIC) and bactericidal (MBC) concentrations, inhibition of biofilm formation (MICB50), catalase, coagulase, DNase, lipase, and hemolysin assays, along with molecular docking simulations. ERP was more effective by displaying MIC and MBC values <100 μg mL−1. Compounds 8 and 9 displayed the lowest MIC values (0.98 to 31.25 μg mL−1) against all tested Gram‐positive MDRB. They also inhibited the biofilm formation of S. aureus (ATCC 43300 and clinical isolate) and S. epidermidis (ATCC 14990 and clinical isolate), with MICB50 values between 1.56 and 6.25 μg mL−1. The molecular docking results indicated that 8 and 9 might interact with the catalase's amino acids. Compounds 8 and 9 have great antimicrobial potential.
The aim of this study was to evaluate the antimicrobial efficacy of polyhexamethylene hydrochloride guanidine (PHMGH) compared to chlorhexidine digluconate (CLX) for use as an oral antiseptic during ...dental procedures in wild cats. This research is crucial due to limited information on the diversity of oral microorganisms in wild cats and the detrimental local and systemic effects of oral diseases, which highlights the importance of improving prevention and treatment strategies. Samples were collected from the oral cavities of four
Puma concolor
, one
Panthera onca
, and one
Panthera leo
, and the number of colony-forming units per milliliter (CFU/mL) was counted and semi-automatically identified. The antimicrobial susceptibility profile of bacterial isolates was determined using minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and time-kill kinetics of PHMGH and CLX. A total of 16 bacterial isolates were identified, consisting of six Gram-positive and 10 Gram-negative. PHMGH displayed MIC and MBC from 0.24 to 125.00 μg/mL, lower than those of CLX against three isolates. Time-kill kinetics showed that PHMGH reduced the microbial load by over 90% for all microorganisms within 30 min, whereas CLX did not. Only two Gram-positive isolates exposed to the polymer showed incomplete elimination after 60 min of contact. The results could aid in the development of effective prevention and treatment strategies for oral diseases in large felids. PHMGH showed promising potential at low concentrations and short contact times compared to the commercial product CLX, making it a possible active ingredient in oral antiseptic products for veterinary use in the future.
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•The Plinia cauliflora Essential Oil act as natural leishmanicide activity.•Essential oils can be used for oral antibacterial control.•Essential oils in development of new drugs.
The ...essential oils of Eugenia uniflora L. (EuEO), Plinia cauliflora (Mart.) (PcEO) and Syzygium cumini (L.) (ScEO), of the Myrtaceae family, were analyzed in gas chromatography with mass spectrometry in order to identify their volatile components, as well as their in vitro leishmanicidal, antibacterial and cytotoxic activities. A total of 34 compounds were identified from EuEO. The major compounds found in EuEO were germacrone (8.52%), spathulenol (8.20%), α-selinene (7.50%) and (Z)-β-elemenone (4.88%). PcEO contained 52 compounds, with the major compounds being (E)-cariophene (14.69%), β-bisabolene (9.36%), (E, E)-α-farnecene (8.07%) and globulol (7.86%). ScEO contained 38 compounds, with the major compounds being α-pinene (21.20%), globulol (15.30%), eugenol (11.20%), and α-terpineol (8.88%). Our results demonstrated that EuEO, PcEO and ScEO, tested against Leishmania amazonensis, affected promastigote growth in a dose-dependent manner. The IC50 of EuEO, PcEO and ScEO were 0.99, 0.46 and 8.78 μg/mL, respectively, while the IC50 of Amphotericin B was 0.60 μg/mL. All the EO of the species evaluated presented moderate inhibitory activity, with Minimum Inhibitory Concentration (MIC) variation of 100 to 400 μg/mL for the following bacteria tested: Streptococcus mutans, Streptococcus mitis, Streptococcus sanguinis, Streptococcus sobrinus, Streptococcus salivarius, Actinomyces naeslundii, Bacteroides fragilis, Bacteroides thetaiotaomicron, Prevotella nigrescens and Porphyromonas gingivalis. Our results showed that the IC50 values for the treated tumor cell lines ranged from 76.5 to 106.2 μg/mL for EuEO and 76.6 to 116.2 μg/mL for PcEO. ScEO was not tested on the tumor cell lines because it presented an IC50 > 400 μg/mL on normal cell lines. These results highlight the variability of the chemical composition of essential oils and the high potential of their bactericidal and leishmanicidal activities.
Invasion of periodontal tissues by Porphyromonas gingivalis and Aggregatibacter actinomycetemcomitans can be associated with aggressive forms of periodontitis. Oleoresins from different copaifera ...species and their compounds display various pharmacological properties. The present study evaluates the antibacterial and antivirulence activity of oleoresins obtained from different copaifera species and of ten isolated compounds against two causative agents of periodontitis. The following assays were performed: determination of the minimum inhibitory concentration (MIC), determination of the minimum bactericidal concentration (MBC), and determination of the antibiofilm activity by inhibition of biofilm formation and biofilm eradication tests. The antivirulence activity was assessed by hemagglutination, P. gingivalis Arg-X and Lis-X cysteine protease inhibition assay, and A. actinomycetemcomitans leukotoxin inhibition assay. The MIC and MBC of the oleoresins and isolated compounds 1, 2, and 3 ranged from 1.59 to 50 μg/mL against P. gingivalis (ATCC 33277) and clinical isolates and from 6.25 to 400 μg/mL against A. actinomycetemcomitans (ATCC 43717) and clinical isolates. About the antibiofilm activity, the oleoresins and isolated compounds 1, 2, and 3 inhibited biofilm formation by at least 50% and eradicated pre-formed P. gingivalis and A. actinomycetemcomitans biofilms in the monospecies and multispecies modes. A promising activity concerning cysteine protease and leucotoxin inhibition was also evident. In addition, molecular docking analysis was performed. The investigated oleoresins and their compounds may play an important role in the search for novel sources of agents that can act against periodontal pathogens.
•Kisspeptin/Kiss1R is expressed during the folliculogenesis and luteogenesis of the cat.•Pregnancy stimulates the luteal expression of Kiss1 and KissR in the cat.•Pregnancy influences angiogenic and ...immune factors in the cat's corpus luteum.•Luteolysis reduces the luteal expression of Kiss1, Kiss1r, Vegf and Mif in the cat.
The Kisspeptin/Kiss1r system has been studied in mammalian ovaries. However, there are still no studies on the modulation of this system and its relationship with angiogenic and immunological mediators in the ovary of domestic cats, especially during pregnancy. We evaluated the expression of Kisspeptin/Kiss1r and angiogenic and immunological mediators during folliculogenesis, luteogenesis and luteal regression of cyclic and pregnant cats. The ovary exhibited moderate to intense expression for Kiss1, VEGF, Flk-1, INFγ and MIF in oocytes and the follicular wall, while Kiss1r expression was low in granulosa cells. In these cells, there was also a greater expression of Kiss1, INFγ and MIF, mainly in secondary follicles, while tertiary and preovulatory follicles exhibited greater expression of VEGF and Flk-1 in this layer. In luteogenesis, Kiss1 immunostaining was higher in mature corpora lutea (MCL) of pregnant cats compared to vacuolated CL (VCL) and corpus albicans (CA). Pregnancy also increased the luteal gene expression of Kiss1 as well as Kiss1, Kiss1r, Flk-1, and MIF immunostaining in MCL, while reduced the area of VEGF expression in VCL and luteal mRNA expression of Mif when compared to non-pregnant animals. In addition, positive gene correlation between Kiss1r and Mif was observed in the CL. Kiss1, Kiss1r, Vegf and Mif expression were lower in the CA of cats in anestrus. These findings reveal that the expression of Kisspeptin/Kiss1r and angiogenic and immunological mediators, in the ovary of domestic cats, depend on the follicular and luteal stage, and the luteal expression of these mediators is influenced by pregnancy.
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A new method of screening was developed to generate 770 organic and water-soluble fractions from extracts of nine species of marine sponges, from the growth media of 18 species of marine-derived ...fungi, and from the growth media of 13 species of endophytic fungi. The screening results indicated that water-soluble fractions displayed significant bioactivity in cytotoxic, antibiotic, anti-Leishmania, anti-Trypanosoma cruzi, and inhibition of proteasome assays. Purification of water-soluble fractions from the growth medium of Penicillium solitum IS1-A provided the new glutamic acid derivatives solitumine A (1), solitumine B (2), and solitumidines A–D (3–6). The structures of compounds 1–6 have been established by analysis of spectroscopic data, chemical derivatizations, and vibrational circular dichroism calculations. Although no biological activity could be observed for compounds 1–6, the new structures reported for 1–6 indicate that the investigation of water-soluble natural products represents a relevant strategy in finding new secondary metabolites.
It is estimated that 10 to 20% of all genes in the human genome encode cell surface proteins and due to their subcellular localization these proteins represent excellent targets for cancer diagnosis ...and therapeutics. Therefore, a precise characterization of the surfaceome set in different types of tumor is needed. Using TCGA data from 15 different tumor types and a new method to identify cancer genes, the S-score, we identified several potential therapeutic targets within the surfaceome set. This allowed us to expand a previous analysis from us and provided a clear characterization of the human surfaceome in the tumor landscape. Moreover, we present evidence that a three-gene set—WNT5A, CNGA2, and IGSF9B—can be used as a signature associated with shorter survival in breast cancer patients. The data made available here will help the community to develop more efficient diagnostic and therapeutic tools for a variety of tumor types.
Siparuna guianensis is a Brazilian plant with extensive ethnobotanical indication and identified as one of the priority species that should be preserved in the Brazilian Cerrado. This work aimed to ...investigate the chemical composition and the antibacterial effects of the essential oil from leaves of S. guianensis (SG-EO) grown in southeastern Brazil against a representative panel of oral pathogens and mycobacteria. Anticariogenic and antimycobacterial activities of SG-EO were evaluated in terms of their minimum inhibitory concentrations (MICs). The essential oil from leaves of S. guianensis was analyzed by gas chromatography coupled to mass spectrometry (GC-MS). Forty one compounds were identified, accounting for 92.7 % of the SG-EO composition. E,E-famesol (18.0 %), P-myrcene (16.0 %), germacrene-D (10.0 %) and siparunone (14.6 %) were the major SG-EO constituents. SG-EO showed the strongest anticariogenic activity against the aerobic bacterium Streptococcus mutans (MIC of 50 microg/mL). SG-EO was also evaluated for its antimycobacterial activity, and showed MIC values of 250 microg/mL against Mycobacterium avium and 500 microg/mL against M. tuberculosis and M. kansasii. These results imply that S. guianensis may be a new alternative source of substances of medicinal interest. This is the first report of anticariogenic and antimycobacterial activities of essential oil of S. guianensis. Keywords: antimycobacterial activity; cariogenic bacteria; essential oil; Mycobacterium tuberculosis; Siparuna guianensis; Streptococcus mutans
Natural products are a very important source of bio-molecules for drug to treat infectious diseases. The essential oil of Eugenia dysenterica DC. dried leaves (Ed-EO), of the Myrtaceae family, was ...analyzed by gas chromatography with flame ionization detector (GC/FID) and by mass spectrometry (GC/MS) in order to identify their volatile components. A total of 24 compounds were identified from Ed-EO. The major compounds found in Ed-EO were limonene (16.0 %), caryophyllene oxide (15.0 %), citral (9.0 %), trans-caryophyllene (8.0 %), and 1,8-cineole (7.3 %). The in vitro biological activities of Ed-EO were investigated against trypomastigote forms of Trypanosoma cruzi and bacteria of the genus Streptococcus. Our results demonstrated that Ed-EO, tested against T. cruzi, affected trypomastigote growth in a dose-dependent manner. The IC
50
of Ed-EO was 9.5 μg/mL, while the IC
50
of benznidazole (positive control) was 9.8 μg/mL, revealing remarkable trypanocidal action. The minimum inhibitory concentrations (MICs) were determined by the broth dilution method in 96-well microplates. The Ed-EO displayed moderate antibacterial activity against Streptococcus mitis (MIC = 250 μg/mL), S. sanguinis (MIC = 200 μg/mL), S. sobrinus (MIC = 400 μg/mL), and S. salivarius (MIC = 400 μg/mL), and strong activity against S. mutans (MIC = 31.2 μg/mL). These results suggest that the oil of E. dysenterica dried leaves could be tested in future studies for the treatment of Chagas disease and dental caries.
Solanum paniculatum L. is widely used in Brazilian folk medicine for the treatment of liver and gastrointestinal disorders as well as for culinary purposes and beverage production. Fractionation of ...hydroalcoholic ethanol (EtOH) 70% tincture from S. paniculatum leaves led to the isolation of six new spirostanic saponins which included 6-O-α-l-rhamnopyranosyl-(1′′→3′)-β-d-quinovopyranosyl-(22S,23R,25S)-3β,6α,23-trihydroxy-5α-spirostane (1), 6-O-β-d-xylopyranosyl-(1′′→3′)-β-d-quinovopyranosyl-(22S,23R,25R)-3β,6α,23-trihydroxy-5α-spirostane (4), 3-O-α-l-rhamnopyranosyl-(1′′→3′)-β-d-quinovopyranosyl-(22S,23S,25R)-3β,6α,23-trihydroxy-5α-spirostane (5), 3-O-β-d-xylopyranosyl-(1′′→3′)-β-d-quinovopyranosyl-(22S,23S,25R)-3β,6α,23-trihydroxy-5α-spirostane (6), 6-O-α-l-rhamnopyranosyl-(1′′→3′)-β-d-quinovopyranosyl-(22S,25S)-1β,3β,6α-trihydroxy-5α-spirostane (7), and 6-O-β-d-xylopyranosyl-(1′′→3′)-β-d-quinovopyranosyl-(22S,25S)-3β,4β,6α-trihydroxy-5α-spirostane (8) together with two known spirostanic saponins (2, 3). The structures of these compounds were determined by one-dimensional (1D) and two-dimensional (2D) NMR experiments in addition to high-resolution electrospray ionization mass spectrometry (HRESIMS) analyses. The 70% alcohol tincture, used as phytomedicine, exhibited promising activities against oral pathogens, including, Steptococcus sanguinis, St. oralis, St. mutans, St. mitis, and Lactobacillus casei with minimal inhibitory concentration (MIC) values ranging from 6.25 to 50 μg/mL. The saponin fraction, nonetheless, showed lower activity against all the strains tested (from 100 to >400 μg/mL).
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