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1.
J Pharm Sci ; 2024 Aug 15.
Artículo en Inglés | MEDLINE | ID: mdl-39151795

RESUMEN

Liver cancer is one of the aggressive primary tumors as evident by high rate of incidence and mortality. Conventional treatments (e.g. chemotherapy) suffer from various drawbacks including wide drug distribution, low localized drug concentration, and severe off-site toxicity. Therefore, they cannot satisfy the mounting need for safe and efficient cancer therapeutics, and alternative novel strategies are needed. Nano-based drug delivery systems (NDDSs) are among these novel approaches that can improve the overall therapeutic outcomes. NDDSs are designed to encapsulate drug molecules and target them specifically to liver cancer. Thus, NDDSs can selectively deliver therapeutic agents to the tumor cells and avoid distribution to off-target sites which should improve the safety profile of the active agents. Nonetheless, NDDSs should be well designed, in terms of the preparing materials, nanocarriers structure, and the targeting strategy, in order to accomplish these objectives. This review discusses the latest advances of NDDSs for cancer therapy with emphasis on the aforementioned essential design components. The review also entails the challenges associated with the clinical translation of NDDSs, and the future perspectives towards next-generation NDDSs.

2.
PLoS One ; 19(8): e0306132, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-39110692

RESUMEN

The past decade has witnessed a significant evolution in the role of the Internet, transitioning from individual connectivity to an integral aspect of various domains. This shift has prompted a move in IP paradigms from hierarchical to distributed architectures characterized by decentralized structures. This transition empowers efficient data routing and management across diverse networks. However, traditional distributed mobility management (DMM) protocols, reliant on tunneling mechanisms, incur overheads, costs, and delays, exacerbating challenges in managing the exponential growth of mobile data traffic. This research proposes Tunnel-Free Mobility for IPv6 (TFMIPv6) as a solution to address the shortcomings of existing DMM protocols. TFMIPv6 eliminates the need for tunneling, simplifying routing processes and reducing latency. A comprehensive cost analysis and performance evaluation are conducted, comparing TFMIPv6 with traditional protocols such as MIPv6, PMIPv6, FMIPv6, and HMIPv6. The study reveals significant improvements with TFMIPv6. Signaling costs are reduced by 50%, packet delivery costs by 23%, and tunneling costs are completely eliminated (100%). Real-world network traffic datasets are used for simulation, providing statistical evidence of TFMIPv6's efficacy in supporting an uninterrupted movement of IPv6 data across networks.


Asunto(s)
Costos y Análisis de Costo , Redes de Comunicación de Computadores/economía , Internet , Humanos , Algoritmos
3.
Metabolomics ; 20(4): 75, 2024 Jul 09.
Artículo en Inglés | MEDLINE | ID: mdl-38980562

RESUMEN

INTRODUCTION: Microbial communities affect several aspects of the earth's ecosystem through their metabolic interaction. The dynamics of this interaction emerge from complex multilevel networks of crosstalk. Elucidation of this interaction could help us to maintain the balance for a sustainable future. OBJECTIVES: To investigate the chemical language among highly abundant microbial genera in the rhizospheres of medicinal plants based on the metabolomic analysis at the interaction level. METHODS: Coculturing experiments involving three microbial species: Aspergillus (A), Trichoderma (T), and Bacillus (B), representing fungi (A, T) and bacteria (B), respectively. These experiments encompassed various interaction levels, including dual cultures (AB, AT, TB) and triple cultures (ATB). Metabolic profiling by LC-QTOFMS revealed the effect of interaction level on the productivity and diversity of microbial specialized metabolites. RESULTS: The ATB interaction had the richest profile, while the bacterial profile in the monoculture condition had the lowest. Two native compounds of the Aspergillus genus, aspergillic acid and the dipeptide asperopiperazine B, exhibited decreased levels in the presence of the AT interaction and were undetectable in the presence of bacteria during the interaction. Trichodermarin N and Trichodermatide D isolated from Trichoderma species exclusively detected during coexistence with bacteria (TB and ATB). These findings indicate that the presence of Bacillus activates cryptic biosynthetic gene clusters in Trichoderma. The antibacterial activity of mixed culture extracts was stronger than that of the monoculture extracts. The TB extract exhibited strong antifungal activity compared to the monoculture extract and other mixed culture treatments. CONCLUSION: The elucidation of medicinal plant microbiome interaction chemistry and its effect on the environment will also be of great interest in the context of medicinal plant health Additionally, it sheds light on the content of bioactive constituents, and facilitating the discovery of novel antimicrobials.


Asunto(s)
Interacciones Microbianas , Plantas Medicinales , Rizosfera , Plantas Medicinales/metabolismo , Plantas Medicinales/microbiología , Aspergillus/metabolismo , Bacterias/metabolismo , Trichoderma/metabolismo , Bacillus/metabolismo , Hongos/metabolismo , Metabolómica , Técnicas de Cocultivo , Microbiología del Suelo
4.
Curr Issues Mol Biol ; 46(7): 6805-6819, 2024 Jul 02.
Artículo en Inglés | MEDLINE | ID: mdl-39057048

RESUMEN

Escherichia coli is a major cause of serious infections, with antibiotic resistance rendering many treatments ineffective. Hence, novel strategies to combat this pathogen are needed. Anti-virulence therapy is a promising new approach for the subsequent era. Recent research has examined the impact of sub-inhibitory doses of ascorbic acid and paracetamol on Escherichia coli virulence factors. This study evaluated biofilm formation, protease production, motility behavior, serum resistance, expression of virulence-regulating genes (using RT-PCR), and survival rates in a mouse model. Ascorbic acid significantly reduced biofilm formation, protease production, motility, and serum resistance from 100% in untreated isolates to 22-89%, 10-89%, 2-57%, and 31-35% in treated isolates, respectively. Paracetamol also reduced these factors from 100% in untreated isolates to 16-76%, 1-43%, 16-38%, and 31-35%, respectively. Both drugs significantly down-regulated virulence-regulating genes papC, fimH, ompT_m, stcE, fliC, and kpsMTII. Mice treated with these drugs had a 100% survival rate compared with 60% in the positive control group control inoculated with untreated bacteria. This study highlights the potential of ascorbic acid and paracetamol as anti-virulence agents, suggesting their use as adjunct therapies alongside conventional antimicrobials or as alternative treatments for resistant Escherichia coli infections.

5.
Vet Res Commun ; 2024 Jul 31.
Artículo en Inglés | MEDLINE | ID: mdl-39083180

RESUMEN

Hexaflumuron (HEX) insecticide is widely used in agriculture practices to fight crop insects. The toxicological effect of HEX on Nile tilapia (Oreochromis niloticus) was investigated in this study. Two hundred and forty fish (35.50 ± 1.45 g) were divided into six groups in four replicates (40 fish/group; 10 fish/replicate) and were exposed to six distinct HEX concentrations (0, 2, 4, 6, 8, and 10 mg L-1) for 96-h. The 96-h lethal concentration 50 (96-h LC50) of HEX was calculated to be 7.19 mg L-1. The fish exhibited reduced surface and middle swimming, aggressiveness, and tail-spreading behaviors with increasing bottom swimming and resting patterns after HEX exposure. HEX exposure resulted in body bleeding and fin rot. The erythrogram (red blood cell count, hemoglobin, and packed cell volume %) was significantly reduced with increased mean corpuscular volume by HEX exposure. HEX exposure decreased the white blood cells (WBCs) and differential WBC counts. Acute HEX exposure raised 8-hydroxy-2-deoxyguanosine level while lowering brain acetylcholine esterase activity. HEX exposure caused hepato-renal dysfunction and increased stress-related parameters (glucose and cortisol). Exposure to HEX reduced the immune responses (lysozyme, nitric oxide, immunoglobulin M, and complement 3). A substantial decrease in the antioxidant variables (reduced glutathione content and catalase) with increasing the malondialdehyde was noted by HEX exposure. Moreover, histopathological changes resulted from HEX exposure in the gills, liver, kidney, and spleen. These results indicate that HEX exposure induced behavioral changes, hepato-renal dysfunction, and immune-antioxidant disruption, indicating a possible physiological disruption in O. niloticus.

6.
Sci Rep ; 14(1): 14452, 2024 Jun 24.
Artículo en Inglés | MEDLINE | ID: mdl-38914569

RESUMEN

The development of flame-retardant materials has become an important research direction. For the past dozen years, researchers have been exploring flame retardants with high flame-retardant efficiency, low toxicity, less smoke, or other excellent performance flame retardants. Therefore, this work aimed to synthesize new cyclodiphosph(V)azane derivatives and their Cu(II) and Cd(II) metal complexes and investigated their potential applications as high flame-retardant efficiency. Various techniques were used to characterize the prepared ligand H2L and its metal complexes, including elemental analyses, mass spectra, conductivity measurements, electronic spectral data UV-vis, FT-IR, 1H,13C-NMR, TGA, XRD, and molecular docking experiments studies were M. tuberculosis receptors (PDB ID: 5UHF) and the crystal structure of human topoisomerase II alpha (PDB ID: 4FM9). Wood-based paint was physically mixed with the ligand H2L and its metal complexes. The obtained results of mechanical characteristics of the dried paint layers were noticed to improve, such as gloss value, which ranged from 85 to 95, hardness 1.5-2.5 kg, adhesion 4B to 5B, and impact resistance, which improved from 1.3 to 2.5 J. Moreover, the obtained results of flame-retardant properties showed a significant retardant impact compared to the blank sample, such as ignitability, which includes the heat flux which increased from 10 to 25 kW/m2, and ignition time, ranging from 550 to 1200 s, respectively, and limiting oxygen index (LOI) (%) which has been increased from 21 to 130 compared with the plywood sample and sample blank. The ordering activity of the observed results was noticed that coated sample based on Cd(II) metal complexes > coated sample based on Cu(II) metal complexes of Cyclophosphazene ligand > coated sample based on phosphazene ligand H2L > coated sample without additives > uncoated sample. This efficiency may be attributed to (1) the H2L is an organophosphorus compound, which contains P, N, Cl, and aromatic six- and five-member ring, (2) Cu(II) and Cd(II) metal complexes characterized by high thermal stability, good stability, excellent performance flame retardants, and wide application.

7.
J Am Pharm Assoc (2003) ; 64(4): 102123, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38735392

RESUMEN

BACKGROUND: Inappropriate automated dispensing cabinet (ADC) overrides pose a significant risk to patient safety. Bypassing pharmacist review during these overrides removes a vital safety check, leaving nurses to review complex medication orders alone. This can lead to overlooking incorrect orders and significantly increasing the potential for medication errors. While Institute for Safe Medication Practices (ISMP) guidelines promote profiled ADCs and safe override practices, there is no national standard for acceptable override rates. OBJECTIVES: Assessing the appropriateness of ADC overrides of profiled ADCs at a tertiary hospital in Saudi Arabia in accordance with ISMP guidelines (third core safety process). METHODS: This retrospective observational study reviewed all override transactions for 13 profiled ADCs over a 3-month period, from 1 October 2022 until 31 December 2022. The target override rate was set at no more than 5%. After applying exclusions, the relevant data fields were extracted from electronic records of 2 integrated systems: the Omnicell dashboard and the BESTCare hospital information system. The study assessed whether the override transactions complying with the standard elements required for appropriate ADC overrides in accordance with ISMP recommendations and hospital regulations. RESULTS: Six hundred sixty-four override transactions from profiled ADCs were reviewed and evaluated. Although the overall override limit for profiled ADCs was met (1.9%), multiple inappropriate override practices were revealed. These inappropriate practices are missing physician orders (33.7%), undocumented verbal orders (31.5%), nonurgent physician orders (11%), missing (8.4%) or delayed (33.7%) administration records, and unrecognized override errors (5.3%). Only 3 (0.5%) met all the standard elements required for ADC overrides. CONCLUSION: The target override threshold of 5% is inadequate to demonstrate sufficient adherence to the standard elements of appropriate overrides or effectively prevent medication errors. Consequently, a significantly lower target threshold override limit, well below 5%, should be considered, especially with 24-hour pharmacy services and fully integrated computerized physician order entry with ADC system. A multidisciplinary override surveillance team is considered essential.


Asunto(s)
Errores de Medicación , Sistemas de Medicación en Hospital , Servicio de Farmacia en Hospital , Centros de Atención Terciaria , Arabia Saudita , Errores de Medicación/prevención & control , Errores de Medicación/estadística & datos numéricos , Estudios Retrospectivos , Humanos , Sistemas de Entrada de Órdenes Médicas/estadística & datos numéricos , Farmacéuticos/estadística & datos numéricos , Seguridad del Paciente , Automatización
9.
Bioorg Chem ; 148: 107414, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38733748

RESUMEN

Spectroscopic, biochemical, and computational modelling studies have been used to assess the binding capability of a set of minor groove binding (MGB) ligands against the self-complementary DNA sequences 5'-d(CGCACTAGTGCG)-3' and 5'-d(CGCAGTACTGCG)-3'. The ligands were carefully designed to target the DNA response element, 5'-WGWWCW-3', the binding site for several nuclear receptors. Basic 1D 1H NMR spectra of the DNA samples prepared with three MGB ligands show subtle variations suggestive of how each ligand associates with the double helical structure of both DNA sequences. The variations among the investigated ligands were reflected in the line shape and intensity of 1D 1H and 31P-{1H} NMR spectra. Rapid visual inspection of these 1D NMR spectra proves to be beneficial in providing valuable insights on MGB binding molecules. The NMR results were consistent with the findings from both UV DNA denaturation and molecular modelling studies. Both the NMR spectroscopic and computational analyses indicate that the investigated ligands bind to the minor grooves as antiparallel side-by-side dimers in a head-to-tail fashion. Moreover, comparisons with results from biochemical studies offered valuable insights into the mechanism of action, and antitumor activity of MGBs in relation to their structures, essential pre-requisites for future optimization of MGBs as therapeutic agents.


Asunto(s)
ADN , ADN/química , ADN/metabolismo , Ligandos , Humanos , Antineoplásicos/química , Antineoplásicos/farmacología , Estructura Molecular , Conformación de Ácido Nucleico , Sitios de Unión , Relación Estructura-Actividad , Modelos Moleculares , Relación Dosis-Respuesta a Droga , Espectroscopía de Resonancia Magnética , Línea Celular Tumoral
10.
Ir J Med Sci ; 193(4): 1977-1983, 2024 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-38602618

RESUMEN

INTRODUCTION: Opioids are commonly added to local anaesthetic for subarachnoid block for caesarean section due to their synergistic effects. The physiochemical characteristics of opioids suggest premixing with hyperbaric bupivacaine may limit their distribution within the CSF. We studied the effect of a separate injection with a combination of bupivacaine, morphine and fentanyl on block characteristics, haemodynamic changes, postoperative pain and patient satisfaction. METHOD: Following ethical approval and informed consent, a prospective double-blinded randomised controlled trial was performed in a university hospital. A total of 126 patients undergoing caesarean section were randomised to two groups. In group M, the premixed group, patients received 12 mg of hyperbaric bupivacaine, 20 mcg of fentanyl and 100 mcg of morphine injected as a single mixture. In group S, the separate injection group, patients received the same drugs in separate injections. Measurements included haemodynamics, block distribution, intra- and postoperative pain, as well as patient satisfaction. RESULTS: Patients in both groups had similar block height, time to maximum sensory block, time to block regression and motor block. However, haemodynamics were different between the groups. The proportion of systolic hypotension episodes was greater in group S [159/1320 (12.05%)] than group M [113/1452 (7.78%)], with P = 0.0002. Moreover, a greater amount of ephedrine was administered in group S than group M, with values 12.09 (8.1) and 9.09 (8.5) mg respectively (P = 0.001). Additionally, postoperative pain, as measured by the Visual Analogue Scale (VAS), was greater in group M, with a VAS of 4.6 (1.7), vs. group S, which recorded a VAS of 3.8 (2.0) (P = 0.017). CONCLUSION: Sequential injection of intrathecal opioids and hyperbaric bupivacaine resulted in greater early haemodynamic instability and slightly better postoperative analgesia without any difference in block height or patient satisfaction. CLINICAL TRIAL REGISTRATION: NCT04403724.


Asunto(s)
Analgésicos Opioides , Anestésicos Locales , Bupivacaína , Cesárea , Fentanilo , Morfina , Dolor Postoperatorio , Humanos , Bupivacaína/administración & dosificación , Bupivacaína/uso terapéutico , Femenino , Analgésicos Opioides/administración & dosificación , Analgésicos Opioides/uso terapéutico , Adulto , Anestésicos Locales/administración & dosificación , Anestésicos Locales/uso terapéutico , Método Doble Ciego , Morfina/administración & dosificación , Morfina/uso terapéutico , Embarazo , Dolor Postoperatorio/tratamiento farmacológico , Dolor Postoperatorio/prevención & control , Fentanilo/administración & dosificación , Fentanilo/uso terapéutico , Espacio Subaracnoideo , Satisfacción del Paciente/estadística & datos numéricos , Estudios Prospectivos , Anestesia Raquidea/métodos , Bloqueo Nervioso/métodos , Hemodinámica/efectos de los fármacos
11.
Asian J Androl ; 26(4): 396-401, 2024 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-38639715

RESUMEN

Thyroid hormones play essential roles in spermatogenesis, but their effects on infertile males remain poorly understood. This study aimed to evaluate the impact of combining carbimazole (CBZ) with vitamin E (VE) on testicular injury induced by experimental hyperthyroidism in adult albino rats, focusing on oxidative, inflammatory, and apoptotic pathways. In this experimental study, 64 adult male albino Wistar rats were divided into eight groups: Group I (control-untreated), Group II (CBZ-control), Group III (VE-control), Group IV (CBZ + VE-control), Group V (levothyroxine-induced testicular injury), Group VI (levothyroxine + CBZ-treated), Group VII (levothyroxine + VE-treated), and Group VIII (levothyroxine + CBZ + VE-treated). The study was conducted in the Faculty of Medicine, Suez Canal University (Ismailia, Egypt). After cervical decapitation, both testes and epididymis were examined histopathologically and immunohistochemically. Significant differences were observed among groups concerning malondialdehyde (MDA), glutathione (GSH), superoxide dismutase (SOD), and catalase (CAT; all P < 0.001). Polymerase chain reaction analysis showed significant differences in tumor necrosis factor-α (TNF- α ), interleukin-10 (IL-10), Bcl-2-associated X protein (BAX), B-cell lymphoma 2 protein (Bcl2), p53, Caspase-3, Caspase-8, Caspase-9, and nuclear factor-kappa B (NF- κ B) mRNA levels (all P < 0.001). Hyperthyroid group treated with CBZ alone (Group VI) exhibited testicular side effects, affecting seminiferous tubules and spermatogenesis. However, the Group VIII showed improved spermatogenesis and a decrease in testicular side effects. The addition of VE to the treatment of hyperthyroid rats with CBZ reduced testicular side effects and seminiferous tubular affection when potentially improving spermatogenesis. Further research is needed to elucidate the underlying mechanisms fully.


Asunto(s)
Apoptosis , Carbimazol , Hipertiroidismo , Estrés Oxidativo , Ratas Wistar , Testículo , Vitamina E , Masculino , Animales , Hipertiroidismo/tratamiento farmacológico , Ratas , Testículo/efectos de los fármacos , Testículo/patología , Testículo/metabolismo , Carbimazol/uso terapéutico , Estrés Oxidativo/efectos de los fármacos , Apoptosis/efectos de los fármacos , Vitamina E/farmacología , Vitamina E/uso terapéutico , Antitiroideos , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Malondialdehído/metabolismo , Glutatión/metabolismo , Superóxido Dismutasa/metabolismo , Espermatogénesis/efectos de los fármacos , Epidídimo/efectos de los fármacos , Epidídimo/metabolismo , Epidídimo/patología , Quimioterapia Combinada
12.
Heliyon ; 10(8): e28714, 2024 Apr 30.
Artículo en Inglés | MEDLINE | ID: mdl-38638997

RESUMEN

MIMO (Multiple-Input-Multiple-Output) antenna systems are promising for fifth-generation (5G) networks, offering lower latency and higher data rates. These systems utilize millimeter-wave (mmWave) frequency bands for efficient transmission and reception of multiple data simultaneously, enhancing overall efficiency and performance. This article presents a compact size, wide band tri-circular ring mmWave MIMO antenna with suitable performance characteristics for next-generation communication systems. The MIMO system consists of a tri-circular ring patch with slots on a ground plane. The four elements of the antenna are arranged together in the polarization diversity configuration with overall dimensions of 23×18×0.254 mm3, and designed on a 0.254 mm thin, flexible RO5880 substrate with a relative permittivity of 2.3 using Computer Simulation Technology (CST) 2022. The proposed antenna design shows the impedance bandwidth of 14 GHz with isolation >18 dB throughout the 26-40 GHz resonance band. The obtained gain is 6.6 dBi at 28 GHz with radiation efficiency > 90%. Several MIMO parameters are also investigated, such as Envelope Correlation Coefficient (ECC), Mean Effective Gain (MEG), Diversity Gain (DG), Total Active Reflection Co-efficient (TARC), and Channel Capacity Loss (CCL), and are found to be within the accepted limits for a practical MIMO system. Furthermore, the fabricated MIMO antenna was tested, and the measured results aligned favorably with the simulated results, confirming the suitability of the proposed design. Through the obtained results, the mmWave MIMO antenna is suitable for practical 5G as well as mmWave applications due to its lightweight, simple design, and wideband characteristics, which cover the 5G frequency bands of 26, 28, 32, and 38 GHz.

13.
Chem Biodivers ; 21(6): e202400451, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38556464

RESUMEN

Five types of heterocyclic compounds containing trifloromethylpyridine scaffold namely; 3-cyano-2-(N-phenyl)carbamoylmethylthio-6-(thiophen-2-yl)-4-trifluoromethyl-pyridine (6a), thieno[2,3-b]pyridines 3-5 and 7a-c, pyrido[3',2':4,5]thieno[3,2-d] pyrimidines 8-13 and 15a-c, pyrido[3',2':4,5]thieno[3,2-d][1,2,3]triazines 16a,b, and 9-(thiophen-2-yl)-7-(trifluoromethyl) pyrido [3',2':4,5]thieno[2,3-e][1,2,4]triazolo[1,5-c]pyrimidine (14) were synthesized in excellent yields and very pure state. The structures of these compounds were confirmed by elemental and spectral analyses. Most of the synthesized compounds were evaluated as insecticidal agents toward Aphis gossypii insects and promising results obtained. Among all tested compounds, only 6, 7a, 7c and 15c being the most potent compounds against nymphs and adults of Aphis gossypii and their activities are nearly to that of acetamiprid as a reference. The effect of 6a compounds 7a, 7c and 15c on the Aphis digestive system from histological point of view was also included.


Asunto(s)
Áfidos , Compuestos Heterocíclicos , Insecticidas , Piridinas , Animales , Insecticidas/química , Insecticidas/farmacología , Insecticidas/síntesis química , Piridinas/química , Piridinas/síntesis química , Compuestos Heterocíclicos/química , Compuestos Heterocíclicos/síntesis química , Compuestos Heterocíclicos/farmacología , Áfidos/efectos de los fármacos , Relación Estructura-Actividad , Estructura Molecular
14.
PeerJ ; 12: e16826, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38313021

RESUMEN

This study aimed to investigate the potential of patuletin, a rare natural flavonoid, as a virulence and LasR inhibitor against Pseudomonas aeruginosa. Various computational studies were utilized to explore the binding of Patuletin and LasR at a molecular level. Molecular docking revealed that Patuletin strongly interacted with the active pocket of LasR, with a high binding affinity value of -20.96 kcal/mol. Further molecular dynamics simulations, molecular mechanics generalized Born surface area (MM/GBSA), protein-ligand interaction profile (PLIP), and essential dynamics analyses confirmed the stability of the patuletin-LasR complex, and no significant structural changes were observed in the LasR protein upon binding. Key amino acids involved in binding were identified, along with a free energy value of -26.9 kcal/mol. In vitro assays were performed to assess patuletin's effects on P. aeruginosa. At a sub-inhibitory concentration (1/4 MIC), patuletin significantly reduced biofilm formation by 48% and 42%, decreased pyocyanin production by 24% and 14%, and decreased proteolytic activities by 42% and 20% in P. aeruginosa isolate ATCC 27853 (PA27853) and P. aeruginosa clinical isolate (PA1), respectively. In summary, this study demonstrated that patuletin effectively inhibited LasR activity in silico and attenuated virulence factors in vitro, including biofilm formation, pyocyanin production, and proteolytic activity. These findings suggest that patuletin holds promise as a potential therapeutic agent in combination with antibiotics to combat antibiotic-tolerant P. aeruginosa infections.


Asunto(s)
Biopelículas , Cromonas , Flavonas , Virulencia , Pseudomonas aeruginosa , Percepción de Quorum , Simulación del Acoplamiento Molecular , Piocianina/metabolismo , Flavonas/farmacología
15.
Sci Rep ; 14(1): 4601, 2024 Feb 26.
Artículo en Inglés | MEDLINE | ID: mdl-38409208

RESUMEN

A novel hybrid ternary metallic electrocatalyst of amorphous Mo/Co oxides and crystallized Cu metal was deposited over Ni foam using a one-pot, simple, and scalable solvothermal technique. The chemical structure of the prepared ternary electrocatalyst was systematically characterized and confirmed via XRD, FTIR, EDS, and XPS analysis techniques. FESEM images of (Mo/Co)Ox-Cu@NF display the formation of 3D hierarchical structure with a particle size range of 3-5 µm. The developed (Mo/Co)Ox-Cu@NF ternary electrocatalyst exhibits the maximum activity with 188 mV and 410 mV overpotentials at 50 mA cm-2 for hydrogen evolution reaction (HER) and oxygen evolution reaction (OER), respectively. Electrochemical impedance spectroscopy (EIS) results for the (Mo/Co)Ox-Cu@NF sample demonstrate the minimum charge transfer resistance (Rct) and maximum constant phase element (CPE) values. A two-electrode cell based on the ternary electrocatalyst just needs a voltage of about 1.86 V at 50 mA cm-2 for overall water splitting (OWS). The electrocatalyst shows satisfactory durability during the OWS for 24 h at 10 mA cm-2 with an increase of only 33 mV in the cell potential.

16.
Chem Biodivers ; 21(2): e202301390, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38179826

RESUMEN

Overcoming or reducing the majority of difficulties caused by the use of common pesticides requires the use of developed, secure, unique and selective organic compounds. Due to their clear mechanism of action on pests and lower poisonousness towards vertebrates than conventional insecticides, juvenile hormone analogues as an example of insect growth regulators appear promising. Thus, a unique set of pure insect growth regulators has been synthesized. The structure of these synthesized compounds, which were related to the most well-known insect growth regulator insecticides, was confirmed by elemental and contemporary spectroscopic investigations (IR, UV, 1 H-NMR, 13 C NMR, and Dept 135 spectrum). Under laboratory conditions, the effectiveness of a chemically newly synthesized products was tested against the cotton mealybug, Phenacoccus solenopsis, and compared with Fenoxycarb as a reference insecticide. Compound 7 was discovered to be more effective than the other synthetic compounds, with LC50 values of 0.907 mg/L for adult female P. solenopsis and 0.377 mg/L for third instar nymphs. Furthermore, this results concluded that the adult female's stage of P. solenopsis was less sensitive to the checked treatments as matched to the third instar nymphs.


Asunto(s)
Hormigas , Hemípteros , Insecticidas , Animales , Femenino , Insecticidas/farmacología
17.
Heliyon ; 10(2): e24075, 2024 Jan 30.
Artículo en Inglés | MEDLINE | ID: mdl-38293404

RESUMEN

Staphylococcus aureus is a highly prevalent and aggressive human pathogen causing a wide range of infections. This study aimed to explore the potential of Patuletin, a rare natural flavone, as an anti-virulence agent against S. aureus. At a sub-inhibitory concentration (1/4 MIC), Patuletin notably reduced biofilm formation by 27 % and 23 %, and decreased staphyloxanthin production by 53 % and 46 % in Staphylococcus aureus isolate SA25923 and clinical isolate SA1, respectively. In order to gain a more comprehensive understanding of the in vitro findings, several in silico analyses were conducted. Initially, a 3D-flexible alignment study demonstrated a favorable structural similarity between Patuletin and B70, the co-crystallized ligand of CrtM, an enzyme that plays a pivotal role in the biosynthesis of staphyloxanthin. Molecular docking highlighted the strong binding of Patuletin to the active site of CrtM, with a high affinity of -20.95 kcal/mol. Subsequent 200 ns molecular dynamics simulations, along with MM-GBSA, ProLIF, PLIP, and PCAT analyses, affirmed the stability of the Patuletin-CrtM complex, revealing no significant changes in CrtM's structure upon binding. Key amino acids crucial for binding were also identified. Collectively, this study showcased the effective inhibition of CrtM activity by Patuletin in silico and its attenuation of key virulence factors in vitro, including biofilm formation and staphyloxanthin production. These findings hint at Patuletin's potential as a valuable therapeutic agent, especially in combination with antibiotics, to counter antibiotic-resistant Staphylococcus aureus infections.

18.
Int J Biol Macromol ; 257(Pt 2): 128817, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38103663

RESUMEN

A novel smart biochromic textile sensor was developed by immobilizing anthocyanin extract into electrospun cellulose acetate nanofibers to detect bacteria for numerous potential uses, such as healthcare monitoring. Red-cabbage was employed to extract anthocyanin, which was then applied to cellulose acetate nanofibers treated with potassium aluminum sulfate as a mordant. Thus, nanoparticles (NPs) of mordant/anthocyanin (65-115 nm) were generated in situ on the surface of cellulose acetate nanofibrous film. The pH of a growing bacterial culture medium is known to change when bacteria multiply. The absorbance spectra revealed a bluish shift from 595 nm (purple) to 448 nm (green) during the growth of Gram-negative bacteria (E. coli) owing to the discharge of total volatile basic amines as secretion metabolites. On the other hand, the absorption spectra of a growing bacterial culture containing Gram-positive bacteria (L. acidophilus) showed a blue shift from 595 nm (purplish) to 478 nm (pink) as a result of releasing lactic acid as a secretion metabolite. Both absorbance spectra and CIE Lab parameters were used to determine the color shifts. Various analytical techniques were utilized to study the morphology of the anthocyanin-encapsulated electrospun cellulose nanofibers. The cytotoxic effects of the colored cellulose acetate nanofibers were tested.


Asunto(s)
Nanofibras , Antocianinas/farmacología , Escherichia coli , Colorimetría , Celulosa , Lactobacillus acidophilus
19.
Int J Biol Macromol ; 253(Pt 8): 127460, 2023 Dec 31.
Artículo en Inglés | MEDLINE | ID: mdl-37866559

RESUMEN

Conventional cancer mono-therapeutic approaches including radiotherapy, surgery, and chemotherapy don't always achieve satisfactory outcomes and are frequently associated with significant limitations. Although chemotherapy is a vital intervention, its effectiveness is frequently inadequate and is associated with metastasis, multidrug resistance, off-target effect, and normal cells toxicity. Phototherapies are employed in cancer therapy, encompassing photo-dynamic and photo-thermal therapies which under favorable NIR laser light irradiation initiate the included photosensitizers and photo-thermal agents to generate ROS or thermal heat respectively for cancer cells destruction. Photo-therapy is considered noninvasive, posing no resistance, but it still suffers from several pitfalls like low penetration depth and excessive heat generation affecting neighboring tissues. Improved selectivity and tumor-homing capacity could be attained through surface modulation of nanoparticles with targeting ligands that bind to receptors, which are exclusively overexpressed on cancerous cells. Developing novel modified targeted nanoparticulate platforms integrating different therapeutic modalities like photo-therapy and chemotherapy is a topic of active research. This review aimed to highlight recent advances in proteins, nucleic acids, and biological cell membranes functionalized nanocarriers for smart combinatorial chemotherapy/photo-therapy. Nanocarriers decorated with precise targeting ligands, like aptamers, antibody, and lactoferrin, to achieve active tumor-targeting or camouflaging using various biological cell membrane coating are designed to achieve homologous tumor-targeting.


Asunto(s)
Nanopartículas , Neoplasias , Ácidos Nucleicos , Humanos , Neoplasias/tratamiento farmacológico , Neoplasias/patología , Sistemas de Liberación de Medicamentos , Fármacos Fotosensibilizantes/farmacología , Membrana Celular
20.
Open Vet J ; 13(6): 772-781, 2023 06.
Artículo en Inglés | MEDLINE | ID: mdl-37545698

RESUMEN

Background: The fertility and genetic value of the flock can be enhanced by selecting lambs with highly developed early puberty characteristics. Spirulina (SP) has been evaluated as a natural product supplement to boost lamb growth, immunity, and productivity. Aim: Study growth performance, blood metabolites, puberty development traits, semen quality, and seminal plasma biochemical concentrations of growing Barki lambs when supplemented with SP at different levels. Methods: in a 24 weeks study, 30 Barki male lambs weighing an average of 21.78 ± 2.56 kg, with a body condition score of 3.20 ± 0.55 and an age of about 16 ± 0.24 weeks were used. The lambs were randomly assigned to three groups (10 lambs each) of daily SP supplementation levels per lamb of 0 ml (control), 50 ml (SP1), and 100 ml (SP2). The SP powder was made into a water suspension using SP to water ratio of 1 g:10 ml. The growth characteristics, as well as the development of puberty, blood metabolites, and semen quality analysis of every lamb, were measured. Results: The growth performance was greater (p < 0.05) in SP2 lambs compared with other lambs. While daily dry matter intake was not affected by SP treatment, feed efficiency had significantly improved in SP2 groups. Furthermore, the SP2 lambs have attained puberty at early ages than the control lambs. The testes volume of SP2 lambs was bigger (p < 0.05) than other groups throughout the pre-pubertal up to the puberty stage. The addition of SP had no effects on the total protein, glucose, and triglycerides concentrations. Meanwhile, the cholesterol concentration was lowest (p < 0.05) in the SP2 lambs. The blood and seminal plasma levels of alanine aminotransferase and aspartate aminotransferase decreased (p < 0.05) in the SP lambs more than their control counterparts. The levels of superoxide dismutase reduced glutathione, and total antioxidants had increased (p < 0.05) in the treated lambs compared with the control group. Further, the malondialdehyde levels decreased (p < 0.05) in the SP-treated lambs. Additionally, the SP2 lambs produced better semen quality than the control lambs. Conclusion: SP supplementation (100 ml/head/day) enhanced growth performance, feed efficiency, and antioxidative status, exerting a positive influence on the physiological parameters and sexual behavioral patterns at puberty in Barki lambs.


Asunto(s)
Análisis de Semen , Spirulina , Ovinos , Animales , Masculino , Análisis de Semen/veterinaria , Testosterona , Maduración Sexual , Suplementos Dietéticos , Oveja Doméstica
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