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1.
Arq Bras Cardiol ; 121(4): e20230565, 2024.
Article Pt, En | MEDLINE | ID: mdl-38695472

Pulmonary veno-occlusive disease (PVOD) and pulmonary capillary hemangiomatosis are rare types of histopathological substrates within the spectrum of pulmonary arterial hypertension (PAH) with a very poor prognosis. They are characterized by a widespread fibroproliferative process of the small caliber veins and/or capillaries with sparing of the larger veins, resulting in a pre-capillary pulmonary hypertension phenotype. Clinical presentation is unspecific and similar to other PAH etiologies. Definitive diagnosis is obtained through histological analysis, although lung biopsy is not advised due to a higher risk of complications. However, some additional findings may allow a presumptive clinical diagnosis of PVOD, particularly a history of smoking, chemotherapy drug use, exposure to organic solvents (particularly trichloroethylene), low diffusing capacity for carbon monoxide (DLCO), exercise induced desaturation, and evidence of venous congestion without left heart disease on imaging, manifested by a classical triad of ground glass opacities, septal lines, and lymphadenopathies. Lung transplant is the only effective treatment, and patients should be referred at the time of diagnosis due to the rapid progression of the disease and associated poor prognosis. We present a case of a 58-year-old man with PAH with features of venous/capillary involvement in which clinical suspicion, prompt diagnosis, and early referral for lung transplantation were determinant factors for the successful outcome.


A doença veno-oclusiva pulmonar (DVOP) e a hemangiomatose capilar pulmonar são tipos raros de substratos histopatológicos dentro do espectro da hipertensão arterial pulmonar (HAP) com prognóstico muito ruim. Caracterizam-se por um processo fibroproliferativo generalizado das veias e/ou capilares de pequeno calibre com preservação das veias maiores, resultando em um fenótipo de hipertensão pulmonar pré-capilar. A apresentação clínica é inespecífica e semelhante a outras etiologias de HAP. O diagnóstico definitivo é obtido por meio de análise histológica, embora a biópsia pulmonar não seja aconselhada devido ao maior risco de complicações. No entanto, alguns achados adicionais podem permitir um diagnóstico clínico presuntivo de DVOP, especialmente história de tabagismo, uso de drogas quimioterápicas, exposição a solventes orgânicos (particularmente tricloroetileno), baixa capacidade de difusão do monóxido de carbono (DLCO), dessaturação ao esforço e evidências de doença venosa sem doença cardíaca esquerda no exame de imagem, manifestada por uma tríade clássica de opacidades em vidro fosco, linhas septais, e linfadenopatias. O transplante pulmonar é o único tratamento eficaz e os pacientes devem ser encaminhados no momento do diagnóstico, devido à rápida progressão da doença e ao prognóstico ruim. Apresentamos o caso de um homem de 58 anos com HAP com características de envolvimento venoso/capilar em que a suspeita clínica, o pronto diagnóstico e o encaminhamento precoce para transplante pulmonar foram determinantes para um bom desfecho.


Pulmonary Veno-Occlusive Disease , Humans , Male , Middle Aged , Pulmonary Veno-Occlusive Disease/diagnostic imaging , Pulmonary Arterial Hypertension/etiology , Hypertension, Pulmonary/etiology
2.
Food Res Int ; 184: 114239, 2024 May.
Article En | MEDLINE | ID: mdl-38609220

Mycotoxins can inflict harmful effects on diverse organs, and mounting evidence indicates their potential involvement in human neurodegenerative diseases. Given the common occurrence of these toxins in food, there is an increasing demand for a comprehensive assessment of their combined toxicity to enhance our understanding of their potential hazards. This research investigates mycotoxin exposure from widely consumed cereal-based products, including enniatin B (ENNB), sterigmatocystin (STG), aflatoxin B1 (AFB1), cyclopiazonic acid (CPZ), citrinin (CIT), and ochratoxin A (OTA). Employing the median-effect equation based on Chou and Talalay's mass-action law, we assessed their cytotoxicity in human SH-SY5Y neuronal cells. Notably, ENNB displayed the highest neurotoxicity (IC50 = 3.72 µM), followed by OTA (9.10 µM) and STG (9.99 µM). The combination of OTA + STG exhibited the highest toxicity (IC50 = 3.77 µM), while CPZ + CIT showed the least detrimental effect. Approximately 70 % of tested binary combinations displayed synergistic or additive effects, except for ENNB + STG, ENNB + AFB1, and CPZ + CIT, which showed antagonistic interactions. Intriguingly, the senary combination displayed moderate antagonism at the lowest exposure and moderate synergism at higher doses. OTA exhibited predominantly synergistic interactions, comprising approximately 90 %, a noteworthy finding considering its prevalence in food. Conversely, ENNB interactions tended to be antagonistic. The most remarkable synergy occurred in the STG and CIT combination, enabling a 50-fold reduction in CIT dosage for an equivalent toxic effect. These findings highlight the biological relevance of robust synergistic interactions, emphasizing the need to assess human exposure hazards accurately, particularly considering frequent mycotoxin co-occurrence in environmental and food settings.


Mycotoxins , Neuroblastoma , Humans , Mycotoxins/toxicity , Aflatoxin B1 , Edible Grain
3.
Antibiotics (Basel) ; 13(3)2024 Feb 28.
Article En | MEDLINE | ID: mdl-38534657

The importance of fungal infections, particularly those caused by yeasts, is increasing among the medical community. Candida albicans and Cryptococcus neoformans are amongst the high-priority fungal species identified by the World Health Organization (WHO) and are considered in the critical group, while Candida krusei is included in the medium-priority group. The cyclam salt H4[H2(4-CF3PhCH2)2Cyclam]Cl4 proved to be active against the growth of these three yeasts, and the aim of this work was to verify its interference with their virulence mechanisms, whether shared or unique. H4[H2(4-CF3PhCH2)2Cyclam]Cl4 significantly inhibited biofilm production and catalase activity, being able to interfere with C. albicans dimorphic transition and C. neoformans melanin production. At the minimal inhibitory concentration (MIC) values, H4[H2(4-CF3PhCH2)2Cyclam]Cl4 had no antioxidant effect, as determined by the DPPH method. When using the RAW264.7 macrophage cell line, H4[H2(4-CF3PhCH2)2Cyclam]Cl4 reduced nitric oxide (NO) detection (the Griess reaction), but this effect was associated with a significant toxic effect on the cells.

5.
Pharmaceuticals (Basel) ; 17(2)2024 Feb 06.
Article En | MEDLINE | ID: mdl-38399424

Global health faces a significant issue with the rise of infectious diseases caused by bacteria, fungi, viruses, and parasites. The increasing number of multi-drug resistant microbial pathogens severely threatens public health worldwide. Antibiotic-resistant pathogenic bacteria, in particular, present a significant challenge. Therefore, there is an urgent need to identify new potential antimicrobial targets and discover new chemical entities that can potentially reverse bacterial resistance. The main goal of this research work was to create and develop a library of 3,6-disubstituted xanthones based on twin drugs and molecular extension approaches to inhibit the activity of efflux pumps. The process involved synthesizing 3,6-diaminoxanthones through the reaction of 9-oxo-9H-xanthene-3,6-diyl bis(trifluoromethanesulfonate) with various primary and secondary amines. The resulting 3,6-disubstituted xanthone derivatives were then tested for their in vitro antimicrobial properties against a range of pathogenic strains and their efficacy in inhibiting the activity of efflux pumps, biofilm formation, and quorum-sensing. Several compounds have exhibited effective antibacterial properties against the Gram-positive bacterial species tested. Xanthone 16, in particular, has demonstrated exceptional efficacy with a remarkable MIC of 11 µM (4 µg/mL) against reference strains Staphylococcus aureus ATCC 25923 and Enterococcus faecalis ATCC 29212, and 25 µM (9 µg/mL) against methicillin-resistant S. aureus 272123. Furthermore, some derivatives have shown potential as antibiofilm agents in a crystal violet assay. The ethidium bromide accumulation assay pinpointed certain compounds inhibiting bacterial efflux pumps. The cytotoxic effect of the most promising compounds was examined in mouse fibroblast cell line NIH/3T3, and two monoamine substituted xanthone derivatives with a hydroxyl substituent did not exhibit any cytotoxicity. Overall, the nature of the substituent was critical in determining the antimicrobial spectra of aminated xanthones.

6.
Int Microbiol ; 2024 Jan 18.
Article En | MEDLINE | ID: mdl-38236380

The increase in global travel and the incorrect and excessive use of antibiotics has led to an unprecedented rise in antibiotic resistance in bacterial and fungal populations. To overcome these problems, novel bioactive natural products must be discovered, which may be found in underexplored environments, such as estuarine habitats. In the present work, estuarine actinomycetotal strains were isolated with conventional and iChip techniques from the Tagus estuary in Alcochete, Portugal, and analysed for different antimicrobial bioactivities. Extracts were produced from the isolated cultures and tested for bioactivity against Staphylococcus aureus ATCC 29213, Escherichia coli ATCC 25922, Aspergillus fumigatus ATCC 240305, Candida albicans ATCC 10231 and Trichophyton rubrum FF5. Furthermore, bioactive extracts were subjected to dereplication by high-performance liquid chromatography (HPLC) and high-resolution mass spectrometry (HRMS) to putatively identify their chemical components. In total, 105 isolates belonging to 3 genera were obtained. One which was isolated, MTZ3.1 T, represents a described novel taxon for which the name Streptomyces meridianus was proposed. Regarding the bioactivity testing, extracts from 12 strains proved to be active against S. aureus, 2 against E. coli, 4 against A. fumigatus, 3 against C. albicans and 10 against T. rubrum. Dereplication of bioactive extracts showed the presence of 28 known bioactive molecules, 35 hits have one or more possible matches in the DNP and 18 undescribed ones. These results showed that the isolated bacteria might be the source of new bioactive natural products.

7.
Antonie Van Leeuwenhoek ; 117(1): 26, 2024 Jan 23.
Article En | MEDLINE | ID: mdl-38261060

An appealing strategy for finding novel bioactive molecules in Nature consists in exploring underrepresented and -studied microorganisms. Here, we investigated the antimicrobial and tumoral anti-proliferative bioactivities of twenty-three marine and estuarine bacteria of the fascinating phylum Planctomycetota. This was achieved through extraction of compounds produced by the Planctomycetota cultured in oligotrophic medium followed by an antimicrobial screening against ten relevant human pathogens including Gram-positive and Gram-negative bacteria, and fungi. Cytotoxic effects of the extracts were also evaluated against five tumoral cell lines. Moderate to potent activities were obtained against Enterococcus faecalis, methicillin-sensitive and methicillin-resistant Staphylococcus aureus and vancomycin-sensitive and vancomycin-resistant Enterococcus faecium. Anti-fungal effects were observed against Trichophyton rubrum, Candida albicans and Aspergillus fumigatus. The highest cytotoxic effects were observed against human breast, pancreas and melanoma tumoral cell lines. Novipirellula caenicola and Rhodopirellula spp. strains displayed the widest spectrum of bioactivities while Rubinisphaera margarita ICM_H10T affected all Gram-positive bacteria tested. LC-HRMS analysis of the extracts did not reveal the presence of any known bioactive natural product, suggesting that the observed activities are most likely caused by novel molecules, that need identification. In summary, we expanded the scope of planctomycetal species investigated for bioactivities and demonstrated that various strains are promising sources of novel bioactive compounds, which reenforces the potential biotechnological prospects offered by Planctomycetota.


Methicillin-Resistant Staphylococcus aureus , Planctomycetes , Humans , Gram-Negative Bacteria , Anti-Bacterial Agents/pharmacology , Vancomycin , Gram-Positive Bacteria
9.
Mar Drugs ; 21(12)2023 Nov 25.
Article En | MEDLINE | ID: mdl-38132930

Parasitic diseases still compromise human health. Some of the currently available therapeutic drugs have limitations considering their adverse effects, questionable efficacy, and long treatment, which have encouraged drug resistance. There is an urgent need to find new, safe, effective, and affordable antiparasitic drugs. Marine-derived cyclic peptides have been increasingly screened as candidates for developing new drugs. Therefore, in this review, a systematic analysis of the scientific literature was performed and 25 marine-derived cyclic peptides with antiparasitic activity (1-25) were found. Antimalarial activity is the most reported (51%), followed by antileishmanial (27%) and antitrypanosomal (20%) activities. Some compounds showed promising antiparasitic activity at the nM scale, being active against various parasites. The mechanisms of action and targets for some of the compounds have been investigated, revealing different strategies against parasites.


Antiprotozoal Agents , Leishmaniasis , Parasitic Diseases , Humans , Antiparasitic Agents/chemistry , Peptides, Cyclic/pharmacology , Peptides, Cyclic/therapeutic use , Leishmaniasis/drug therapy , Antiprotozoal Agents/chemistry , Parasitic Diseases/drug therapy
10.
Mar Drugs ; 21(11)2023 Oct 24.
Article En | MEDLINE | ID: mdl-37999375

Natural products are a very rich source for obtaining new compounds with therapeutic potential. In the search for new antiparasitic and antimicrobial agents, molecular hybrids were designed based on the structures of antimicrobial marine quinazolinones and eugenol, a natural phenolic compound. Following reports of the therapeutic potential of quinazolinones and eugenol derivatives, it was expected that the union of these pharmacophores could generate biologically relevant substances. The designed compounds were obtained by classical synthetic procedures and were characterized by routine spectrometric techniques. Nine intermediates and final products were then evaluated in vitro against Trypanosoma brucei and Leishmania infantum. Antifungal and antibacterial activity were also evaluated. Six compounds (9b, 9c, 9d, 10b, 10c, and 14) showed mild activity against T. brucei with IC50 in the range of 11.17-31.68 µM. Additionally, intermediate 9c showed anti-Leishmania activity (IC50 7.54 µM) and was six times less cytotoxic against THP-1 cells. In conclusion, novel derivatives with a simple quinazolinone scaffold showing selectivity against parasites without antibacterial and antifungal activities were disclosed, paving the way for new antitrypanosomal agents.


Anti-Infective Agents , Antiprotozoal Agents , Leishmania infantum , Trypanosoma brucei brucei , Antifungal Agents/pharmacology , Eugenol , Antiprotozoal Agents/chemistry , Anti-Bacterial Agents/pharmacology , Quinazolinones/chemistry , Structure-Activity Relationship
11.
Antibiotics (Basel) ; 12(9)2023 Sep 16.
Article En | MEDLINE | ID: mdl-37760747

Tanacetum annuum L. is a Mediterranean plant, commonly known as Blue Tansy due to its blue colour as an essential oil, which is widely used for medicinal purposes. However, there are no studies on the bioactive compounds (especially, phenolic compounds) and the biological properties of their organic extracts. Herein, the purpose of the present work was to investigate the chemical composition of the essential oil and crude extracts of the T. annuum aerial parts collected from northern Morocco and to evaluate their antioxidant and antifungal activity against Fusarium oxysporum f. sp. albedinis, an agent causing Bayoud disease of the date palm, an important food source and commercial perennial crop in the Sahara and North Africa. Chemically, Folin-Ciocalteu and aluminium chloride colourimetric methods were used to determine the total phenolic (TPC) and total flavonoid (TFC) contents, respectively; polyphenols were characterized using HPLC-MS, while GC-MS was used to analyse the essential oil composition. Moreover, the evaluation of antioxidant and antifungal activities was carried out using the DPPH test and microdilution method, respectively. The results showed that the three T. annuum parts (stems, leaves and flowers) extracts contained important TPC and TFC with values varied between 51.32 and 116.32 mg/g of dry crude extract (DCE). HPLC-MS analysis revealed the identification and quantification of 19 phenolic acids and flavonoids with an emphasis on apigenin 7-glucoside (4540 µg/g of dry weight (DW)), luteolin 7-glucoside (2804 µg/g DW) and salicylic acid (1878 µg/g DW). Additionally, 39 biomolecules were identified in the essential oil using GC-MS, which were predominated by camphor (16.69%), α-pinene (12.37%), bornyl acetate (11.97%) and limonene (11.10%). The methanolic and hydro-methanolic extracts of T. annuum parts demonstrated a strong antioxidant property with IC50 values ranging between 0.22 and 0.65 mg/mL. Concerning antifungal activity, the essential oil and crude extracts of the Moroccan Blue Tansy exhibited a potent capacity against F. oxysporum f. sp. albedinis at low concentrations, with MIC and MFC values of 3.33 and 4.58 µL/mL for the essential oil and values of 3.33 and 9.17 mg/mL for crude extracts, respectively. Overall, these results demonstrated T. annuum as an important source of bioactive compounds and contribute significantly to the potential of using essential oils and extracts for controlling the Bayoud disease of date palms. Moreover, the finding suggests that T. annuum can be highly useful for phytosanitary and pharmaceutical industries.

12.
Article En | MEDLINE | ID: mdl-37711123

INTRODUCTION: Fabry disease is an X-linked lysosomal storage disorder caused by pathogenic variants in the GLA gene, leading to decreased/absent α-galactosidase activity. In clinical practice, enzyme activity and substrate/byproduct accumulation play a role in diagnosis and disease-monitoring biomarkers. However, interpreting biomarker levels is not straightforward and can change according to the underlying GLA protein abnormality. OBJECTIVE: Our goals were to understand how disrupting specific protein regions changes biomarker behaviour and to establish specific patterns for individual variants. METHODOLOGY: We analysed data from the Biochemical Genetics Laboratory regarding GLA variants, GLA enzyme activity (in dried blood spots, plasma or white blood cells), plasma LysoGb3 accumulation, and urinary Gb3 excretion. We assessed correlations, trends, and potential predictor models of biomarker behaviour. RESULTS: We assessed 169 hemizygous male and 255 heterozygous female patients. For both groups, substrate accumulation correlates inversely with GLA activity. Variants affecting residues buried within the protein core or the active site were associated with more severe biomarker changes, while those affecting residues that establish disulfide bonds or are glycosylated were similar to other variants. For each non-truncating variant, we also established specific profiles of biomarker behaviour. Finally, we also designed predictor models of biomarker behaviour based on structural variant information. This study provides the groundwork for the impact of GLA protein variation on GLA activity and substrate accumulation. CONCLUSION: This knowledge is of extreme relevance for diagnostic labs and clinicians, as some genetic variants are challenging to interpret regarding pathogenicity. Assessing whether biomarker changes are in the expected range for a specific variant may help diagnostic evaluation. This study also contributes to recognising non-disease-causing variants, considering their overall biochemical impact, and providing a comparative reference for biomarker discovery studies. In the future, the correlation of these findings with disease severity may be of great relevance for diagnosis and monitoring progression.

13.
J Mater Chem B ; 11(36): 8697-8716, 2023 09 20.
Article En | MEDLINE | ID: mdl-37646077

Currently, multidrug-resistant (MDR) infections are one of the most important threats, driving the search for new antimicrobial compounds. Cationic peptide antibiotics (CPAs) and ceragenins (CSAs) contain in their structures cationic groups and adopt a facially amphiphilic conformation, conferring the ability to permeate the membranes of bacteria and fungi. Keeping these features in mind, an amine steroid, DOCA-NH2, was found to be active against reference strains and MDR isolates of Gram-positive Enterococcus faecalis and Staphylococcus aureus and Gram-negative Escherichia coli and Pseudomonas aeruginosa. The compound was active against all the tested microorganisms, having bactericidal and fungicidal activity, displaying minimal inhibitory concentrations (MICs) between 16 and 128 µg mL-1. No synergy with clinically relevant antibacterial drugs was found. However, the compound was able to completely inhibit the biofilm formation of bacteria exposed to the MIC of the compound. For E. coli and E. faecalis, inhibition of biofilm formation occurred at half the MIC. Besides, DOCA-NH2 inhibited the dimorphic transition of Candida albicans at concentrations 4 times lower than the MIC, and can reduce the microorganism virulence and biofilm formation was significantly reduced at both MIC and half the MIC. Polydimethylsiloxane-based coatings containing DOCA-NH2 (0.5, 1.0, and 1.5 wt%) were prepared and tested against the E. coli biofilm formation under hydrodynamic conditions similar to those prevailing in ureteral stents. A biofilm reduction of approximately 80% was achieved when compared to the control.


Anti-Infective Agents , Desoxycorticosterone Acetate , Urinary Tract Infections , Humans , Escherichia coli , Anti-Bacterial Agents/pharmacology , Urinary Tract Infections/drug therapy , Amines , Biofilms , Cations
14.
Life (Basel) ; 13(5)2023 May 19.
Article En | MEDLINE | ID: mdl-37240862

Ganoderma lucidum is an extensively famous medicinal mushroom distributed worldwide. Despite being widely grown in Moroccan forests, there are no studies on its nutritional, nutraceutical and pharmaceutical values. Herein, the objective of this study was to investigate the chemical characterization and antimicrobial properties of G. lucidum methanolic extract. Total phenolic, flavonoid, tannin, ascorbic acid and carotenoid contents were determined by spectrophotometry. The results revealed that the most prevalent bioactive compounds were phenolics and flavonoids, with total values of 154.60 mg GAE/g of dry methanolic extract (dme) and 60.55 mg CE/mg of dme, respectively. A GC-MS analysis identified 80 biologically active molecules, which were mainly divided into the following major groups: sugars (49.49%), organic acids (8.89%), fatty acids (7.75%), amino acids (7.44%), steroids (7.32%), polyphenols (5.92%), and others (13.16%). Additionally, 22 individual phenolic compounds were identified and quantified using HPLC-MS, with emphasis on kaempferol (1714 µg/g of dry weight (dw)), apigenin (1955 µg/g dw) and quercetin (947.2 µg/g dw). The methanolic extract of G. lucidum indicated strong antioxidant capacity by means of the following: DPPH radical-scavenging activity (53.7 µg/mL), ß-carotene/linoleate assay (43.75 µg/mL), and reducing power assay (76.62 µg/mL). Furthermore, the extract exhibited potent antimicrobial properties against seven human pathogenic microorganisms, including two bacteria and five fungal strains, at concentrations ranging from 1 to 16 mg/mL. The most sensitive pathogen was Epidermophyton floccosum (MIC = MFC = 1 mg/mL), while Aspergillus fumigatus was the most resistant one (MIC = 16 mg/mL and MFC ≥ 16 mg/mL). Overall, our findings demonstrated valuable nutritional and bioactive compound attributes, and potent antioxidant and antimicrobial properties, of G. lucidum growing in Moroccan forests. Moreover, these findings suggest that the Moroccan mushroom can be extremely useful for the food and medicinal industries to positively affect socioeconomic status.

15.
Antibiotics (Basel) ; 12(5)2023 May 08.
Article En | MEDLINE | ID: mdl-37237772

Pest resistance against fungicides is a widespread and increasing problem, with impact on crop production and public health, making the development of new fungicides an urgent need. Chemical analyses of a crude methanol extract (CME) of Guiera senegalensis leaves revealed the presence of sugars, phospholipids, phytosterols, guieranone A, porphyrin-containing compounds, and phenolics. To connect chemical composition with biological effects, solid-phase extraction was used to discard water-soluble compounds with low affinity for the C18 matrix and obtain an ethyl acetate fraction (EAF) that concentrates guieranone A and chlorophylls, and a methanol fraction (MF) dominated by phenolics. While the CME and MF exhibited poor antifungal activity against Aspergillus fumigatus, Fusarium oxysporum and Colletotrichum gloeosporioides, the EAF demonstrated antifungal activity against these filamentous fungi, particularly against C. gloeosporioides. Studies with yeasts revealed that the EAF has strong effectiveness against Saccharomyces cerevisiae, Cryptococcus neoformans and Candida krusei with MICs of 8, 8 and 16 µg/mL, respectively. A combination of in vivo and in vitro studies shows that the EAF can function as a mitochondrial toxin, compromising complexes I and II activities, and as a strong inhibitor of fungal tyrosinase (Ki = 14.40 ± 4.49 µg/mL). Thus, EAF appears to be a promising candidate for the development of new multi-target fungicides.

16.
Molecules ; 28(7)2023 Apr 03.
Article En | MEDLINE | ID: mdl-37049958

The purpose of this work was to investigate, for the first time to our knowledge, the chemical composition and bioactivity of methanolic extracts (roots, stems, leaves, and flowers) from Cladanthus mixtus (L.) Chevall. that grows wild in northern Morocco (the Tangier-Tetouan-Al Hoceima region). The phenolic and flavonoid contents were determined by spectrophotometer methods, and the composition of derivatized methanolic extracts from C. mixtus using N-O-bis(trimethylsilyl) trifluoroacetamide (BSTFA) was analyzed by gas chromatography-mass spectrometry (GC-MS). The antioxidant activity was carried out by applying the 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and DPPH (2,2-diphenyl-1-picrylhydrazyl) tests. The micro-dilution technique was chosen to investigate the antimicrobial activity of methanolic extracts against two bacterial strains and three fungal species. The results showed that the values of total phenolic and flavonoid contents were found to be higher in flower extracts (30.55 ± 0.85 mg of gallic acid equivalents (GAE)/g of dried weight (DW) and 26.00 ±1.34 mg of quercetin equivalents (QE)/g DW, respectively). Other groups of chemical compounds were revealed by GC-MS, such as carbohydrates (27.25-64.87%), fatty acids (1.58-9.08%), organic acids (11.81-18.82%), and amino acids (1.26-7.10%). Root and flower methanolic extracts showed the highest antioxidant activity using ABTS (39.49 mg of Trolox equivalents (TE)/g DW) and DPPH (36.23 mg TE/g DW), respectively. A positive correlation between antioxidant activity and polyphenol and flavonoid amounts was found. Antibacterial tests showed that the best activity was presented by the leaf extract against Staphylococcus aureus (minimum inhibitory concentration (MIC) = minimum bactericidal concentration (MBC) = 20 mg/mL) and Escherichia coli (MIC of 30 mg/mL and MBC of 35 mg/mL). S. aureus was more sensitive to the extracts compared to E. coli. All extracts showed antifungal activity against Trichophyton rubrum, with the best efficacy reported by the flower and leaf extracts (MIC = 1.25 mg/mL and minimum fungicidal concentration (MFC) = 2.5 mg/mL). In general, extracts of C. mixtus appeared less effective against Candida albicans and Aspergillus fumigatus.


Antioxidants , Plant Extracts , Plant Extracts/pharmacology , Plant Extracts/chemistry , Antioxidants/pharmacology , Antioxidants/chemistry , Staphylococcus aureus , Escherichia coli , Morocco , Flavonoids/pharmacology , Flavonoids/analysis , Phenols/pharmacology , Phenols/analysis , Methanol/pharmacology
17.
Polymers (Basel) ; 15(7)2023 Mar 30.
Article En | MEDLINE | ID: mdl-37050344

Textiles are important components for the development of lightweight and flexible displays useful in smart materials. In particular, halochromic textiles are fibrous materials with a color-changing ability triggered by pH variations mainly based on pH-sensitive dye molecules. Recently, a novel class of 2-aminoimidazole azo dyes was developed with distinct substituent patterns. In this work, silk fabric was functionalized through exhaustion for the first time with one of these dyes (AzoIz.Pip). The halochromic properties of the dye were assessed in an aqueous solution and after silk functionalization. The solutions and the fabrics were thoroughly analyzed by ultraviolet-visible (UV-vis) spectra, color strength (K/S), color difference (∆E), CIE L*a*b* coordinates, and the ultraviolet protection factor (UPF). The dyeing process was optimized, and the halochromic performance (and reversibility) was assessed in universal Britton-Robinson buffers (ranging from pH 3 to 12) and artificial body fluids (acid and alkaline perspiration, and wound exudate). AzoIz.Pip showed vibrant colors and attractive halochromic properties with a hypsochromic shift from blue (557 nm) to magenta (536 nm) in aqueous buffered solutions. Similarly, the functionalized silk showed a shift in wavelength of the maximum K/S value from 590 nm to 560 nm when pH increases. The silk fabric showed a high affinity to AzoIz.Pip, and promoted additional color stabilization of the dye, avoiding color loss as observed when the dye is in solution at alkaline pH after 24 h. The color reversibility was effective up to the fourth cycle and the fastness tests denoted suitable results, except washing fastness. The cytotoxicity of the silk fabric extracts was assessed, depicting reduced viability of HaCaT cells to <70% only when the dye concentration in the fabric is higher or equal to 64 µg·mL-1. Nevertheless, lower concentrations were also very effective for the halochromic performance in silk. These materials can thus be a helpful tool for developing sensors in several sectors such as biomedicine, packaging, filtration, agriculture, protective apparel, sports, camouflage, architecture, and design.

18.
Pharmaceutics ; 15(3)2023 Mar 13.
Article En | MEDLINE | ID: mdl-36986787

The combination of two or more agents capable of acting in synergy has been reported as a valuable tool to fight against pathogens. Silver nanoparticles (AgNPs) present a strong antimicrobial action, although their cytotoxicity for healthy cells at active concentrations is a major concern. Azoimidazole moieties exhibit interesting bioactivities, including antimicrobial activity. In this work, a class of recently described azoimidazoles with strong antifungal activity was conjugated with citrate or polyvinylpyrrolidone-stabilized AgNPs. Proton nuclear magnetic resonance was used to confirm the purity of the compounds before further tests and atomic absorption spectroscopy to verify the concentration of silver in the prepared dispersions. Other analytical techniques elucidate the morphology and stability of AgNPs and corresponding conjugates, namely ultraviolet-visible spectrophotometry, scanning transmission electron microscopy and dynamic light scattering analysis. The synergistic antimicrobial activity of the conjugates was assessed through a checkerboard assay against yeasts (Candida albicans and Candida krusei) and bacteria (Staphylococcus aureus and Escherichia coli). The conjugates showed improved antimicrobial activity against all microorganisms, in particular towards bacteria, with concentrations below their individual minimal inhibitory concentration (MIC). Furthermore, some combinations were found to be non-cytotoxic towards human HaCaT cells.

19.
Microorganisms ; 11(2)2023 Jan 20.
Article En | MEDLINE | ID: mdl-36838237

(1) Background: Superficial, including cutaneous and mucocutaneous infections are a current public health problem with universal distribution. One of the main concerns, in the present/future, is fungal/bacterial infections by resistant microorganisms. This study aimed to verify if decoctions of coptidis (Coptis chinensis, Ranunculaceae family), neem (Azadirachta indica, Meliaceae family), and their essential oils (EOs), as well as the EO of manuka (Leptospermum scoparium, Myrtaceae family) have antimicrobial activity against prevalent species of microorganisms responsible for superficial infections. (2) Methods: The antimicrobial activity was determined by the minimum inhibitory concentration (MIC), using broth microdilution method, and minimum lethal concentration (MLC) was determined from subculture of MIC plates. (3) Results: C. chinensis EO and decoction demonstrated some antifungal action against the yeasts and dermatophytes tested. Greatest bactericidal effect against Propionibacterium acnes and some action against Staphylococcus aureus was observed. For A. indica only EO proved activity against dermatophytes and P. acnes. L. scoparium EO showed the broadest antimicrobial spectrum with activity against bacteria, yeasts, and dermatophytes showing greater activity against P. acnes and S. aureus. (4) Conclusions: C. chinensis (EO/decoction), EOs of L. scoparium and A. indica proved in vitro efficacy against fungal, bacterial, or mixed agents of superficial infections, either by sensitive or resistant strains.

20.
Chem Commun (Camb) ; 59(19): 2791-2794, 2023 Mar 02.
Article En | MEDLINE | ID: mdl-36789540

A novel route is described to obtain 2-aminoimidazole azo dyes with a unique substituent pattern in the heteroaryl unit that provides halochromic properties, exhibiting vibrant colours that change from magenta to deep blue. Potent antimicrobial properties against infectious yeasts were demonstrated. No cytotoxicity was detected for concentrations lower than 16 µg mL-1.


Azo Compounds , Coloring Agents , Imidazoles , Hydrogen-Ion Concentration
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