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Four previously unreported triterpenoid saponins named 3ß-hydroxy-23-oxours-12-en-28-oic acid 28-O-ß-D-glucopyranosyl ester (mannioside G) (1), 23-O-acetyl-3ß-hydroxyurs-12-en-28-oic acid 28-O-ß-D-glucopyranosyl ester (mannioside H) (2), ursolic acid 28-O-[α-L-rhamnopyranosyl-(1â4)-ß-D-glucopyranosyl-(1â6)-ß-D-glucopyranosyl] ester (mannioside I) (3), and 3ß-hydroxy-23-oxolup-20(29)-en-28-oic acid 28-O-ß-D-glucopyranosyl ester (mannioside J) (4) were isolated as minor constituents from the EtOAc soluble fraction of the MeOH extract of the leaves of Schefflera mannii along with the known compounds 23-hydroxyursolic acid 28-O-ß-D-glucopyranosyl ester (5), ursolic acid 28-O-ß-D-glucopyranosyl ester (6), pulsatimmoside B (7) betulinic acid 28-O-[α-L-rhamnopyranosyl-(1â4)-ß-D-glucopyranosyl-(1â6)-ß-D-glucopyranosyl] ester (8), 23-hydroxy-3-oxo-urs-12-en-28-oic acid (9), hederagenin (10), ursolic acid (11), betulinic acid (12), and lupeol (13). Their structures were elucidated by a combination of 1D and 2D NMR analysis and mass spectrometry. The MeOH extract, the EtOAc and n-BuOH fractions, and some of the isolated compounds were evaluated for their antibacterial activity against four bacteria: Staphylococcus aureus ATCC1026, Staphylococcus epidermidis ATCC 35984, Escherichia coli ATCC10536, and Klepsiella pnemoniae ATCC13882. They were also screened for their antioxidant properties, but no significant results were obtained.
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Antibacterianos , Saponinas , Triterpenos , Triterpenos/química , Triterpenos/farmacología , Triterpenos/aislamiento & purificación , Saponinas/química , Saponinas/farmacología , Saponinas/aislamiento & purificación , Antibacterianos/farmacología , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/química , Extractos Vegetales/farmacología , Estructura Molecular , Hojas de la Planta/química , Triterpenos Pentacíclicos/farmacología , Triterpenos Pentacíclicos/química , Triterpenos Pentacíclicos/aislamiento & purificación , Staphylococcus aureus/efectos de los fármacos , Araliaceae/químicaRESUMEN
Dorstenia psilurus is a widely used plant spice in traditional African medicine to treat pain-related conditions. However, the anti-inflammatory mechanisms underlying this activity and the main active ingredients of D. psilurus have not yet been fully characterized. This study aimed to isolate and identify the main active anti-inflammatory constituents of the D. psilurus extract and to investigate the underlying anti-inflammatory mechanisms in murine macrophages. Chromatographic techniques and spectroscopic data were used for compound isolation and structure elucidation. The Griess reagent method and the ferrous oxidation-xylenol orange assay were used to evaluate the inhibition of NO production and 15-lipoxygenase activity, respectively. Cyclooxygenase activity was assessed using the fluorometric COX activity assay kit, and Th1/Th2 cytokine measurement was performed using a flow cytometer. The results indicated that the extract and fractions of D. psilurus inhibit NO production and proliferation of RAW 264.7 macrophage cells. Bioguided fractionation led to the identification of psoralen, a furocoumarin, as the main bioactive anti-inflammatory compound. Psoralen inhibited NO production and 15-lipoxygenase activity and reduced pro-inflammatory Th1 cytokines (IFN-γ, TNF-α, and IL-2) while increasing the secretion of anti-inflammatory cytokines (IL-4, IL-6, and IL-10) in activated RAW 264.7 macrophage cells. The encouraging results obtained in this study suggest that psoralen-based multiple modulation strategies could be a useful approach to address the treatment of inflammatory diseases.
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Citocinas , Ficusina , Lipopolisacáridos , Macrófagos , Raíces de Plantas , Animales , Ratones , Células RAW 264.7 , Citocinas/metabolismo , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Raíces de Plantas/química , Lipopolisacáridos/farmacología , Ficusina/farmacología , Ficusina/química , Células TH1/efectos de los fármacos , Células TH1/metabolismo , Células Th2/metabolismo , Células Th2/efectos de los fármacos , Extractos Vegetales/farmacología , Extractos Vegetales/química , Óxido Nítrico/metabolismo , Antiinflamatorios/farmacología , Antiinflamatorios/químicaRESUMEN
The coupling reaction of diazonium ion of 2-amino-6-nitrobenzothiazole at 0-5 °C with distinctly substituted 2-aminobenzothiazole derivatives produced new 1,2,3,5-tetrazine derivatives. It was found that diazotized 2-amino-6-nitrobenzo[d]thiazol reacts with the ring nitrogen atom of varyingly substituted 2-aminobenzothiazole derivatives to yield tetrazine nucleus. The benzene ring of benzothiazole bearing electron donor group and annelated to the tetrazine was further substituted in situ by other 6-nitrobenzo[d]thiazol-2-yl) diazinyl to yield the final product. The structure of the prepared compounds was elucidated using their physical, elemental, and spectroscopic data. The synthesized compounds were tested for their antimicrobial and antibiofilm activities against Staphylococcus aureus and Escherichia coli bacteria. Two of the synthesis tetrazine derivatives exhibited interesting antibiofilm potential.
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Antibacterianos , Benzotiazoles , Biopelículas , Escherichia coli , Pruebas de Sensibilidad Microbiana , Staphylococcus aureus , Biopelículas/efectos de los fármacos , Antibacterianos/farmacología , Antibacterianos/síntesis química , Staphylococcus aureus/efectos de los fármacos , Escherichia coli/efectos de los fármacos , Benzotiazoles/farmacología , Benzotiazoles/química , Benzotiazoles/síntesis química , Compuestos de Diazonio/química , Compuestos de Diazonio/farmacologíaRESUMEN
Introduction: There is a growing interest in studying natural products for the identification of novel lead compounds for drug development for treating inflammatory diseases. Although some studies have focused anti-inflammatory activity of benzophenones and xanthones, exploring additional targets such as enzymes and cytokines, involved in their inflammatory response could provide more comprehensive understanding of the compounds' anti-inflammatory effects. In this study, four xanthones ananixanthone (1), smeathxanthone A (2), smeathxanthone B (3), and 1,3,5,8-tetrahydroxy-2-(3-methybut-2-enyl)-4-(3,7-dimethyloct-2,6-dienyl) xanthone (4); and three benzophenones guttiferone O (5), guttiferone M (6), and aristophenone A (7) from Garcinia smeathmannii (Planch. & Triana) Oliv. were investigated for their effect on nitric oxide production, cyclooxygenase, lipoxygenase inhibition, and Th1/Th2 cytokines production in activated RAW 264.7 macrophages. Methods: The Griess reagent method and the ferrous oxidation-xylenol orange assay were used to evaluate the inhibition of NO production and the 15-lipoxygenase activity respectively. Cyclooxygenase activity was assessed using the fluorometric COX activity assay kit and measurement of Th1/Th2 cytokines was performed using a flow cytometer. Results: All the tested compounds exhibited a dose-dependent inhibition of NO production with varying degrees of inhibitory effects on 15-LOX activity. Compound (6), displays the best inhibitory effect on COX-1/COX-2 activity. A general trend of the tested compounds on cytokines profiles revealed that compound (5) showed a pronounced enhancement of anti-inflammatory cytokines (IL-4 and IL-10). Conclusion: This observation supports future exploration of ananixanthone (1), guttiferone O (5), and guttiferone (6) as potential candidates for the development of anti-inflammatory drugs.
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Background: Candidiasis is the common name for diseases caused by yeast of the genus Candida. Candida albicans is one of the most implicated species in superficial and invasive candidiasis. Antifungals, polyenes, and azoles have been used to treat candidiasis. However, due to the development of antifungal resistance, research of natural substances with potential antifungal effects at low concentrations or combined is also a possibility. Methods: The broth microdilution method was used to evaluate the antifungal activity. The biofilm formation was assessed using the microtiter plate method. The antibiofilm activities were assessed using micro plaque tetrazolium salt assay (MTT). The combination effect of antifungal with natural substances was made using the checkerboard method. Results: Among our isolates, clotrimazole was the most resistant, but amphotericin B was the most effective antifungal. The biofilm was formed by all isolates of C. albicans. Curcumin and piperine displayed antibiofilm activity with minimum biofilm inhibitory concentration (MBIC) and minimum eradicating concentration (MBEC) ranging from 64 to 1024 µg/mL and 256 to 2048 µg/mL. In combination, piperine presented double synergistic effects compared to curcumin with all antifungals tested. Curcumin shows more synergistic effect when combined with polyenes than with azoles. However, piperine shows a more synergistic effect when combined with azoles compared to polyenes. Conclusion: C. albicans was susceptible to curcumin and piperine both on planktonic cells and biofilm. The combination of curcumin and piperine with antifungals has shown synergistic effects against multiresistant clinical isolates of Candida albicans representing an alternative drug research for the treatment of clinical candidiasis.
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Pseudomonas aeruginosa is one of the most frequently resistant and dangerous bacteria isolated from infected wounds of patients. This study aimed to determine the prevalence of P. aeruginosa from infected wounds of patients in the Dschang District Hospital to evaluate their antibiotic susceptibility profiles and their ability to swarm and swim and correlate pyocyanin production with biofilm formation. Wound swab samples were collected and the identification of P. aeruginosa was performed using microbiological and biochemical tests. Their antimicrobial susceptibility was determined by the broth microdilution method. Swarming and swimming were determined by measuring the diameters of motility in semisolid/low-viscosity media. Furthermore, pyocyanin production and biofilm formation were evaluated spectrophotometrically using a microtiter plate. The prevalence of P. aeruginosa from infected wounds in our study population was 26%. All P. aeruginosa isolates were resistant to streptomycin and paromomycin, and the frequency of multidrug resistance (MDR) was 65.8%. All P. aeruginosa isolates showed the ability to produce biofilm and pyocyanin. Out of the 37 isolates screened, 19 including the reference strains (51.4%) were strong biofilm producers. A significant positive correlation was observed among biofilm formation, pyocyanin production, and the antibiotic resistance profile of the isolates. Findings from this study suggest that infected wounds could act as a reservoir for MDR and virulent P. aeruginosa. The presence of strong biofilm producers of P. aeruginosa in infected wounds is a serious public health concern. Therefore, surveillance programs to monitor and control MDR P. aeruginosa in these patients are required to prevent their dissemination in hospital settings.
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Five unusual alkaloids featuring a pyrrolo[1,2-a]quinolone skeleton (pyrroloquinolones B-F, 1-5) were isolated from the ethanol extract of the whole plant of Vernonia glabra (Steetz) Vatke, along with sixteen known compounds. Their structures were established by means of spectroscopic (1D and 2D NMR, UV, IR, and ECD) and high resolution mass spectrometric techniques as well as by comparison of their spectroscopic data with those reported in the literature. The ethanol extract and some isolated compounds were assessed for their antibacterial activity against four bacterial strains. The extract was significantly active against Staphylococcus aureus ATCC1026 and S. epidermidis ATCC35984 (MIC = 64 µg/mL). All the tested compounds showed moderate activity against S. epidermidis (16 ≤ MIC ≤ 64 µg/mL). Furthermore, this is the first report on tricyclic pyrrolo[1,2-a]quinolone alkaloids from a plant source. A biosynthetic pathway for the formation of these compounds is also proposed.
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Alcaloides , Quinolonas , Vernonia , Vernonia/química , Extractos Vegetales/química , Pruebas de Sensibilidad Microbiana , Alcaloides/farmacología , Antibacterianos/farmacología , Antibacterianos/química , Quinolonas/farmacología , EtanolRESUMEN
Background Many plants are used to reduce the side effects of diabetes mellitus. These plants (including Vernonia amygdalina and Tamarindus indica) are rich in phytochemical compounds that have the ability to reduce glycemia and the effect of diabetes-related oxidative stress. In this study, we aimed to investigate the antioxidant and antidiabetic activities of combining V. amygdalina leaves and T. indica pulp extracts. Methodology We prepared a mixture by combining V. amygdalina leaves and T. indica pulp extracts, and we assessed antioxidant properties via the capacity of both extracts to reduce ferric ions, 2,2-diphenyl-1-picryl-hydrazyl (DPPH) radicals, and hydroxyl radicals. We also assessed antidiabetic properties through the capacity of the extracts' combination to inhibit alpha-amylase. We evaluated crude fiber, total phenols content (TPC), and total flavonoid content (TFC). Results From our findings, the combination at a concentration of 200 µg/mgE showed that a percentage of 55.17±1.2 could reduce DPPH radicals, 0.366±0.012 could scavenge ferric ions, and 0.233±0.0022 could reduce hydroxyl radicals. With regard to secondary metabolites, we obtained 16.96±0.17 mEGA/gE for total phenol content, 1.74±0.045 mECAT/gE for total flavonoid content, and crude fiber content in our combination at 6.87±1%. These results were obtained with a significant difference at the 5% threshold. The extract combination also showed an alpha-amylase inhibitory percentage of 23.56±4.6% at the concentration of 200 µg/mgE. Daily administration of the combination of extracts significantly lowered the fasting blood glucose, triglycerides, total cholesterol, LDL cholesterol, aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, creatinine, and malondialdehyde. However, there was a significant increase in serum proteins and HDL cholesterol. We did not observe an antagonistic effect between our combination and glybenclamide. Conclusion Our formulation, therefore, presents antioxidant and antidiabetic activity and could be used for the management of diabetic patients.
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Background Fungal infections mainly caused by Candida krusei are increasing rapidly and represent a serious public health problem in human immunodeficiency virus (HIV)-infected patients. This study aimed to investigate the antifungal susceptibility profile and virulence factors in C. krusei isolated from HIV-infected patients. Methodology Isolates were identified by biochemical and molecular methods. The antifungal resistance profile was established based on the antifungal susceptibility test performed using the Sensititre YeastOne™ (Thermo Fisher Scientific, Waltham, MA) microdilution technique. The production of phospholipase and proteinase was detected by standard methods. Biofilm formation was performed by the microtiter plate method. Results A total of 73 isolates of C. krusei were recovered from stool, oral swabs, vaginal swabs, and urine samples. The highest number of C. krusei isolates (49, 67.05%)was recovered from stool samples. A total of 32.56% of the C. krusei isolates were multidrug-resistant (MDR). The patients living with HIV and not receiving antiretroviral treatment displayed the highest number of C. krusei isolates (29, 39.76%), whereas the patients living with HIV on antiretroviral therapy exhibited the lowest number of C. krusei isolates (2, 2.72%). All isolates were categorized as strong biofilm producers. Among the production of hydrolytic enzymes, 25 (58.13%) and 24 (55.81%) of C. krusei isolates were classified as strong phospholipase and proteinase producers, respectively. Conclusion The C. krusei isolates obtained in this study were MDR and strongly expressed biofilm formation and both phospholipase and proteinase hydrolytic enzymes. The results show how pathogenic C. krusei is in the HIV-infected population and will contribute toward the management of C. krusei-related infections, which may help improve the life quality of people living with HIV.
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Background: Pseudomonas aeruginosa is an opportunistic human pathogen that causes infections that are mediated by both virulence factor production and biofilm formation. In addition, many antibiotics are increasingly losing their efficacy due to the development of resistance. The screening of potentially bioactive natural compounds that have both antivirulence and antibiofilm activities to enhance antibiotic efficacy and reverse antibiotic resistance is a good strategy to overcome these issues. In this study, the antibacterial, antibiofilm, and antivirulence factor activities of some bioactive natural products in combination with conventional antibiotics were evaluated against clinical isolates of P. aeruginosa. Methods: The broth microdilution method was used to determine the antibacterial and antibiofilm activities. The checkerboard method was used to evaluate the combination interactions. Spectrophotometric and agar plate techniques were used to assess the effect of the combination on the pyocyanin production and the motility in P. aeruginosa ATCC 27853 strain. Results: Out of the eighteen combinations tested, ten exhibited synergistic effects against planktonic cells, seven against biofilm inhibition, and five against the eradication of mature biofilm of P. aeruginosa biofilm. The best synergistic effect was the association of amikacin and sinapic acid against planktonic cells (FICI = 0.08) with a 70-fold reduction in the MIC value of amikacin. The same combination showed significant synergistic inhibition of biofilm formation (FICI = 0.1) and biofilm eradication (FICI = 0.15) reducing the MBIC and MBEC of amikacin by 32-fold. Some selected synergistic combinations showed statistically significant differences (p < 0.01 or p < 0.001) in the inhibition of virulence factors compared to the antimicrobials alone. Conclusion: In summary, this study revealed sinapic acid as an antibiotic adjuvant and antivirulence compound to overcome P. aeruginosa infections. This finding indicates that the combinations of amikacin plus sinapic acid, ceftazidime plus thymol, and norfloxacin plus curcumin could be considered promising candidates for the development of combination therapies targeting virulence factors against P. aeruginosa infections.
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Antibacterianos , Productos Biológicos , Humanos , Antibacterianos/farmacología , Amicacina , Pseudomonas aeruginosa , Biopelículas , Productos Biológicos/farmacologíaRESUMEN
Background Enteric fever is a systemic infection in humans caused by the Gram-negative bacilliSalmonella enterica serovars Typhi and Paratyphi. Although the diagnosis typically involves the isolation of Salmonella enterica serovars, it is often determined based on laboratory findings and clinical observations. However, due to the wide variety and the non-specific character of clinical features, making a definitive diagnosis presents numerous challenges. Therefore, the aim of this study was to find the predictive hematological and biochemical parameters which would serve in the diagnosis, prognosis, and treatment of typhoid fever cases. Methodology A cross-sectional study was conducted from November 2020 to September 2021 on1076consented volunteerparticipants. Stool culture and identification tests enabled us to distinguish three groups including 423 Salmonella Typhi positive patients, 115 S. Paratyphi positive patients, and 538 Salmonella negative participants. Biochemical and hematological parameters were evaluated using standard methods from commercial kits and Sysmex KX-21N automated hematology analyzer, respectively. A multiple logistic regression analysis was performed to identify the validity of the hematological and biochemical characteristics for enteric fever diagnosis. Results Multiple logistic regression showed hyper creatininemia, hypoalbuminemia, hyper total proteinemia, hyper alkaline phosphatase (ALP), hyper alanine aminotransferase (ALT), hyper total bilirubinemia, hyper conjugated bilirubinemia, hyper triglyceridemia, hyper C-reactive protein (CRP), leukopenia, thrombocytopenia, lymphopenia, monocytopenia, low hemoglobin, low hematocrit, low mean corpuscular volume (MCV), low mean corpuscular hemoglobin (MCH), low platelet, low platelet crit level, high platelet distribution width (PDW) level, high erythrocyte sedimentation rate 1 (ESR1) level as significant biological abnormalities associated (odds ratio {OR} > 1; p < 0.05) with enteric fever infection. Similarly, hyper ESR2 was an independent predictor (OR > 1; p < 0.05) of S. Typhi infection. However, a negative and significant association (OR < 1; p < 0.05) was recorded between enteric fever infection and high mean platelet volume (MPV). Conclusion Overall the results of the biochemical and hematological profiles can serve as potential diagnostic markers for typhoid fever. These markers can also be useful in the appropriate management of those with enteric fever, preventing severity and limiting outcomes of mortality.
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Background Staphylococcus spp. is one of the most causative agents of urinary tract infections (UTIs). This study aimed to investigate the antibiotic resistance profile and the virulence factors, including the biofilm formation ability of Staphylococcus spp. isolates from urine. Methodology The agar disk diffusion method was used to test the susceptibility of Staphylococcus isolates to ten antibiotics. The biofilm formation ability was determined using the safranin microplate-based method, and the phospholipase, esterase, and hemolysin activities were assessed by the agar plate method. Results During the study period, a prevalence of 18.12% of urinary tract infections caused by the identified Staphylococci was obtained. All the isolated Staphylococcus aureus and S. epidermidis were resistant to cefazolin. Multi-drug resistance (MDR) was recorded in 80.01%, 81.49%, and 76.20% of S. aureus, S. epidermidis, and S. saprophyticus isolates, respectively. Most of the isolates were moderate biofilm formers, while 44.44%, 31.75%, and 30.16% were positive for phospholipase, esterase, and hemolysin activities, respectively. No relevant correlations were observed between the ability of biofilm formation and the resistance to antibiotics or the expression of virulence factors investigated. Conclusion This study shows that Staphylococcus spp. isolates from patients with clinical manifestations of UTIs expressed a high degree of virulence factors, including the ability of biofilm formation, and exhibited multi-drug resistance to the majority of antimicrobials commonly used for the treatment of Staphylococcal infections.
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Background: Cryptococcosis is one of the most common fungal infections in immunocompromised patients, which is caused by Cryptococcus neoformans. However, relatively little is known about the virulence factors of C. neoformans and the incidence of antifungal drug resistance in C. neoformans is rapidly increasing. This study was undertaken to investigate the virulence factors in C. neoformans, thymol, curcumin, piperine, gallic acid, eugenol, and plumbagin for their potential antimicrobial activity against C. neoformans. Methods: The production of phospholipase and proteinase was detected using standard methods. Biofilm formation was determined using the microtiter plate method. The broth microdilution method was used to determine the antifungal activity. The antibiofilm activity was assessed using the safranin staining method. Results: All isolates of C. neoformans produced biofilms with optical density values ranging from 0.16 to 0.89. A majority of C. neoformans isolates that were tested exhibited strong phospholipase (7/8) and proteinase (5/8) production. Plumbagin (with minimum inhibitory concentration values ranging from 4 to 16 µg/mL) showed the highest antifungal activity followed by thymol (with minimum biofilm inhibitory concentration values ranging from 8 to 64 µg/mL). In addition, plumbagin showed the highest antibiofilm activity with minimum biofilm inhibitory concentration and minimum biofilm eradication concentration values ranging from 4 to 16 µg/mL and 32 to 256 µg/mL, respectively. Conclusion: Plumbagin, compared to other natural products studied, was the most efficient in terms of antifungal and antibiofilm activities. Hence, plumbagin could be used in combination with antifungals for the development of new anticryptococcal drugs.
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Criptococosis , Cryptococcus neoformans , Humanos , Antifúngicos/farmacología , Péptido Hidrolasas , Timol , Fosfolipasas , Criptococosis/tratamiento farmacológico , Criptococosis/epidemiología , Criptococosis/microbiología , Pruebas de Sensibilidad Microbiana , Factores de Virulencia , BiopelículasRESUMEN
A new 3-arylcoumarin, 7-hydroxy-6-(1,1-dimethylallyl)-2',5'-dihydroxy-4'-(3,3dimethylprenyl)-3-arylcoumarin (desmoarylcoumarin) 1, a previously unreported oleanane-type triterpenoid, 3ß,22ß,23-trihydroxyolean-12-en (episoyasapogenol B) 2, together with five known flavonoids including darbergioidin (3), isoferreirin (4), quercetin (5), vitexin (6), swertizin (7), and one carbohydrate, sucrose (8) were isolated from the methanolic extract of the roots of Desmodium salicifolium. Their structures were elucidated mainly by extensive spectroscopic analysis (1D and 2D) and mass spectrometric (HRFAB-MS) data. The methanolic extract, EtOAc and n-BuOH fractions as well as some isolated compounds were assessed for their antibacterial and antioxidant activities. The EtOAc fraction exhibited moderate activity against Enterococcus faecalis with MIC value of 128 µg/mL. The methanolic extract and the EtOAc fraction displayed DPPH scavenging activity with EC50 values of 5.99 and 2.06 µg/mL, respectively. Compound 1 showed a moderate antibacterial activity against Enterococcus faecalis with a MIC of 16 µg/mL. It also showed moderate DPPH scavenging activity.
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Background: Salmonella species are frequently linked to biofilm-associated infections. Biofilm formation intensively reduces the efficacy of antibiotics and the host immune system. Therefore, new therapeutic strategies are needed. Thymol, the main monoterpene phenol found in Thymus vulgaris, has been shown to possess potent antibiofilm activity. Our previous findings showed that thymol enhanced the antibiofilm activity of aminoglycosides against Salmonella enterica serovars. However, the clinical potential of thymol has not yet been realized due to its low aqueous solubility and high volatility. Nano-based drug delivery systems have emerged as a novel strategy to resolve these problems. This study aimed to investigate the antibiofilm activity of thymol-loaded poly (lactic-co-glycolic acid) nanoparticles (TH-NPs) and their synergism when used in combination with amikacin antibiotics. Methods: The antibacterial activity of TH-NPs was evaluated using the broth microdilution method. Biofilm formation and antibiofilm assays were performed by the miniaturized microtiter plate method. Interaction studies between TH-NPs and amikacin against biofilm were determined using the checkerboard method. Results: TH-NPs exhibited antibacterial activity against planktonic cells of S. enterica serovars that were more efficient (8 to 32 times) than free thymol alone. S. Typhimurium and S. Choleraesuis isolates were considered strong biofilm producers. The combination of TH-NPs with amikacin showed synergistic activity in the inhibition and eradication of S. enterica serovar biofilm. The minimum biofilm inhibitory concentration (MBIC) and minimum biofilm eradication concentration (MBEC) of amikacin were reduced by 32 to 128-fold when used in combination with TH-NPs. Time-kill kinetic studies showed that the combination of TH-NPs with amikacin possesses bactericidal action. Conclusion: This study suggests that the combination of TH-NPs with amikacin can be an alternative to overcome biofilm-associatedSalmonella diseases and therefore should be further explored as a model to search for new antibiofilm drugs.
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Phytochemical investigation of the methanol extracts from the leaves and bark of Senna siamea resulted in the isolation of one new flavone C-glycoside: apigenin-8-C-[6''-(E)-feruloyl]-ß-D-glucopyranoside] (1), together with sixteen known compounds including quercetin-3-O-α-L-rhamnoside (2), vitexin (3), isovitexin (4), quercetin-3-O-ß-D-glucopyranoside (5), quercetin-3-O-ß-D-arabinopyranoside (6), quercetin (7), kaempferol (8), methyl inositol (9), sucrose (10), betulinic acid (11), vanillic acid (12), stigmastane-3ß,6α-diol (13), aurantiamide acetate (14), robinetinidol (15), catechin (16) and epicatechin (17). The structures of these compounds were established on the basis of their spectroscopic (1 D and 2 D NMR) and mass spectrometric (ESI-TOF-MS) data. The methanol extracts, fractions and some of the isolated compounds were screened for their antimicrobial properties against five microbial strains. The methanol extract and the ethyl acetate fraction from the bark showed very weak antifungal activity against C. glabrata with the same MIC value of 128 µg/mL. Compound 7 was weakly active against C. albicans with MIC of 32 µg/mL.
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A previously unreported gallocatechin glycoside, (2 R,3S) 4'-O-methyl-gallocatechin-3-O-α-Ê-rhamnopyranoside (1) and an unseparable mixture of two previously undescribed dihydromyricetin glycosides, (2 R,3R) 4'-O-methyl-dihydromyricetin-3-O-α-Ê-rhamnopyranoside (2a) and (2 R,3S) 4'-O-methyl-dihydromyricetin-3-O-α-Ê-rhamnopyranoside (2 b) along with three known compounds were isolated from the n-butanol soluble fraction of the stem bark of Olax subscorpioidea Oliv. Their structures were elucidated by detailed spectroscopic analyses, including 1H NMR, 13C NMR, 1H-1H COSY, HSQC, HMBC, NOESY, HR-ESI-MS and chemical methods. The crude ethanol extract, the fractions, and some of the isolated compounds were screened for their antioxidant and antibacterial activities. They showed significant antioxidant activities with EC50 ranging from 6.29 to 18.19 µg/mL in 2,2-diphenyl-1-picrylhydrazyl (DPPH) method and EC50 ranging from 85.77 to 86.39 mmol FeSO4/g in ferric reducing antioxidant power (FRAP) methods compared with 2.29 µg/mL and 3.52 mmol FeSO4/g for the positive control (Ê-ascorbic acid). Nevertheless, no inhibition was observed against the tested bacterial strains at a MIC less than 256 µg/mL.
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Antioxidantes , Flavonoides , Flavonoides/química , Antioxidantes/química , Corteza de la Planta/química , Extractos Vegetales/química , Glicósidos/químicaRESUMEN
A new triterpenoid saponin (Mimonoside D: 3-O-α-L-arabinopyranosyl-3ß-hydroxyolean-12-en-28-oic acid 28-O-ß-D-xylopyranosyl-(1â2)-ß-D- glucopyranoside ester (1)) was isolated from the aerial parts of Mimosa diplotricha Sauvalle together with nine known compounds: 7,4'-dihydroxyflavone (2), kaempferol (3), lupeol (4), betulinic acid (5), ß-sitosterol (6), ß-sitosterol-3-O-ß-D-glucopyranoside (7), lutein (8), 5,2'-dihydroxy-7,4',5'-trimethoxyflavone (9) and vitexin (10). Their structures were elucidated on the basis of spectroscopic (1 D and 2 D nuclear magnetic resonance) and high-resolution mass spectrometric data as well as by comparison of their spectral data with those of related compounds. Compounds 2, 7 and 8 had already been isolated from M. diplotricha, while compounds 3, 4, 5 and 6 have been isolated from other Mimosa species. Compound 2 moderately inhibited Proteus mirabilis (MIC = 32 µg/mL), weakly inhibited Pseudomonas aeruginosa (MIC = 64 µg/mL) and very weakly inhibited Staphylococcus aureus (MIC = 128 µg/mL) and Enterococus faecalis (MIC = 128 µg/mL).
Asunto(s)
Fabaceae , Mimosa , Saponinas , Triterpenos , Saponinas/farmacología , Saponinas/química , Triterpenos/farmacología , Triterpenos/química , Extractos Vegetales/química , Estructura MolecularRESUMEN
The development of resistance of microorganisms to conventional antibiotics is a major global health concern; hence, there is an increasing interest in medicinal plants as a therapeutic option. This study aimed to evaluate the antibacterial, anti-biofilm, and anti-quorum activities of crude extracts prepared using various solvents of nine indigenous South African plants used locally for the treatment of diarrhoea. The minimum inhibitory concentration (MIC) was determined using the broth microdilution method and the crystal violet assay was used to test the anti-biofilm activity of the extracts against a panel of bacteria. Anti-quorum sensing activity of the extracts was assessed via inhibition of violacein production in Chromobacterium violaceum ATCC 12472. Preliminary screening of extracts against E. coli ATCC 25922 revealed that the acetone extracts had significant activity, with MIC values ranging from 0.04 to 0.63 mg/mL. Further screening against a panel of bacterial pathogens showed that the acetone extract of Bauhinia bowkeri was the most active with MIC of 0.01 mg/mL against Salmonella enteritidis, followed by Searsia lancea with MIC of 0.03 mg/mL against Bacillus cereus. All the plant extracts prevented the attachment of biofilms by more than 50% against at least one of the tested bacteria. However, only the mature biofilm of B. cereus was susceptible to the extracts, with 98.22% eradication by Searsia pendulina extract. The minimum quorum sensing inhibitory concentration of the extracts ranged from 0.08 to 0.32 mg/mL with S. lancea having the most significant activity. The extract of S. lancea had the best violacein production inhibitory activity with IC50 value of 0.17 mg/mL. Overall, the results obtained indicate that acetone extracts of S. leptodictya, S. lancea, S. batophylla, S. pendulina, B. galpinii, and B. bowkeri possess antibacterial and anti-biofilm activities and can modulate quorum sensing through the inhibition of violacein production. Therefore, these results signify the potential of the selected plant extracts in treating diarrhoea through inhibition of bacterial growth, biofilm formation inhibition, and quorum sensing antagonism, supporting their medicinal use.
RESUMEN
Background: Plants are a rich source of therapeutic compounds that have tremendous applications in the pharmaceutical industry. This study aimed to identify the phytochemicals present in the seven selected medicinal plants as well as their antioxidant and antimicrobial activities. Methods: Phytochemical screening, total phenolic, and flavonoid contents were determined using standard methods. The antioxidant activity of plant extracts was determined using 2, 2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl (OH), and nitric oxide (NO) radical scavenging assays. The antimicrobial activity of the plant extracts was determined by the broth microdilution method. Results: The results of phytochemical analysis showed the presence of phenols, flavonoids, and steroids in all plant extracts. The extract of Psychotria peduncularis showed the highest total phenolic and flavonoid contents (5.57 ± 0.22 mg GAE/g and 1.38 ± 0.06 mg QE/g, respectively). All plant extracts showed very strong antioxidant activity against DPPH and NO radical scavenging with IC50 values ranging from 0.55 to 49.43 µg/mL and 0.65 to 13.7 µg/mL, respectively. The extracts of Tristemma mauritianum and P. peduncularis displayed significant antibacterial activity with MIC values ranging from 16 to 1024 µg/mL. T. mauritianum extract showed bactericidal activity against all tested species. The extracts of Alsophila manianna and P. peduncularis showed significant antifungal activity (MIC = 64 µg/mL) against Candida albicans strain. Conclusion: The screened extracts of medicinal plants used in our study can be used as potential antioxidant and antimicrobial agents, and resources for the development of new drugs.