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1.
BMC Plant Biol ; 24(1): 364, 2024 May 04.
Artigo em Inglês | MEDLINE | ID: mdl-38702592

RESUMO

BACKGROUND: This study aimed to investigate the alterations in biochemical and physiological responses of oat plants exposed to antimony (Sb) contamination in soil. Specifically, we evaluated the effectiveness of an arbuscular mycorrhizal fungus (AMF) and olive mill waste (OMW) in mitigating the effects of Sb contamination. The soil was treated with a commercial strain of AMF (Rhizophagus irregularis) and OMW (4% w/w) under two different levels of Sb (0 and 1500 mg kg-1 soil). RESULTS: The combined treatment (OMW + AMF) enhanced the photosynthetic rate (+ 40%) and chlorophyll a (+ 91%) and chlorophyll b (+ 50%) content under Sb condition, which in turn induced more biomass production (+ 67-78%) compared to the contaminated control plants. More photosynthesis in OMW + AMF-treated plants gives a route for phenylalanine amino acid synthesis (+ 69%), which is used as a precursor for the biosynthesis of secondary metabolites, including flavonoids (+ 110%), polyphenols (+ 26%), and anthocyanins (+ 63%) compared to control plants. More activation of phenylalanine ammonia-lyase (+ 38%) and chalcone synthase (+ 26%) enzymes in OMW + AMF-treated plants under Sb stress indicated the activation of phenylpropanoid pathways in antioxidant metabolites biosynthesis. There was also improved shifting of antioxidant enzyme activities in the ASC/GSH and catalytic pathways in plants in response to OMW + AMF and Sb contamination, remarkably reducing oxidative damage markers. CONCLUSIONS: While individual applications of OMW and AMF also demonstrated some degree of plant tolerance induction, the combined presence of AMF with OMW supplementation significantly enhanced plant biomass production and adaptability to oxidative stress induced by soil Sb contamination.


Assuntos
Antimônio , Micorrizas , Olea , Poluentes do Solo , Micorrizas/fisiologia , Olea/microbiologia , Poluentes do Solo/metabolismo , Antimônio/metabolismo , Adaptação Fisiológica , Resíduos Industriais , Fotossíntese/efeitos dos fármacos , Biodegradação Ambiental , Biomassa
2.
Saudi Pharm J ; 32(1): 101913, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38204591

RESUMO

To fully evaluate and define the new drug molecule for its pharmacological characteristics and toxicity profile, pre-clinical and clinical studies are conducted as part of the drug research and development process. The average time required for all drug development processes to finish various regulatory evaluations ranges from 11.4 to 13.5 years, and the expense of drug development is rising quickly. The development in the discovery of newer novel treatments is, however, largely due to the growing need for new medications. Methods to identify Hits and discovery of lead compounds along with pre-clinical studies have advanced, and one example is the introduction of computer-aided drug design (CADD), which has greatly shortened the time needed for the drug to go through the drug discovery phases. The pharmaceutical industry will hopefully be able to address the present and future issues and will continue to produce novel molecular entities (NMEs) to satisfy the expanding unmet medical requirements of the patients as the success rate of the drug development processes is increasing. Several heterocyclic moieties have been developed and tested against many targets and proved to be very effective. In-depth discussion of the drug design approaches of newly found drugs from 2020 to 2022, including their pharmacokinetic and pharmacodynamic profiles and in-vitro and in-vivo assessments, is the main goal of this review. Considering the many stages these drugs are going through in their clinical trials, this investigation is especially pertinent. It should be noted that synthetic strategies are not discussed in this review; instead, they will be in a future publication.

3.
Toxicol Appl Pharmacol ; 461: 116405, 2023 02 15.
Artigo em Inglês | MEDLINE | ID: mdl-36716865

RESUMO

Cancer is one of the leading causes of death worldwide, so pursuing effective and safe therapeutics for cancer is a key research objective nowadays. Doxorubicin (DOX) is one of the commonly prescribed chemotherapeutic agents that has been used to treat cancer with its antimitotic properties via inhibition of topoisomerase II (TOP2) activity. However, many problems hinder the broad use of DOX in clinical practice, including cardiotoxicity and drug resistance. Research in drug discovery has confirmed that natural bioactive compounds (NBACs) display a wide range of biological activities correlating to anticancer outcomes. The combination of NBACs has been seen to be an ideal candidate that might increase the effectiveness of DOX therapy and decreases its unfavorable adverse consequences. The current review discusses the chemo-modulatory mechanism and the protective effects of combined DOX with NBACs with a binding affinity (pKi) toward TOP2A more than pKi of DOX. This review will also discuss and emphasize the molecular mechanisms to provide a pathway for further studies to reveal other signaling pathways. Taken together, understanding the fundamental mechanisms and implications of combined therapy may provide a practical approach to battling cancer diseases.


Assuntos
DNA Topoisomerases Tipo II , Doxorrubicina , Humanos , Doxorrubicina/efeitos adversos , DNA Topoisomerases Tipo II/metabolismo , Cardiotoxicidade , Apoptose
4.
Molecules ; 28(7)2023 Apr 05.
Artigo em Inglês | MEDLINE | ID: mdl-37050006

RESUMO

In the present study, an attempt was made to investigate the in vitro antioxidant, anticancer, and antibacterial activities of Delonix regia, then in vivo evaluate its safety as a natural colorant and sweetener in beverages compared to synthetic colorant and sweetener in rats, then serve the beverages for sensory evaluation. Delonix regia flowers had high protein, polysaccharide, Ca, Na, Mg, K, and Fe contents. The Delonix regia pigment extract (DRPE) polysaccharides were separated and purified by gel permeation chromatography on Sephacryl S-200, characterized by rich polysaccharides (13.6 g/L). The HPLC sugar profile detected the monosaccharides in the extracted polysaccharides, composed of mannose, galactose, glucose, arabinose, and gluconic acid, and the structure of saccharides was confirmed by FTIR, which showed three active groups: carbonyl, hydrocarbon, and hydroxyl. On the other hand, the red pigment constituents of DRPE were detected by HPLC; the main compounds were delphinidin and cyanidin at 15 µg/mL. The DRPE contained a considerable amount (26.33 mg/g) of anthocyanins, phenolic compounds (64.7 mg/g), and flavonoids (10.30 mg/g), thus influencing the antioxidant activity of the DRPE, which scavenged 92% of DPPH free radicals. Additionally, it inhibited the population of pathogenic bacteria, including Staphylococcus aureus, Listeria monocyogenes, Salmonella typhimurum, and Pseudomonas aeruginosa, in the range of 30-90 µg/mL, in addition to inhibiting 85% of pancreatic cancer cell lines. On the in vivo level, the rats that were delivered a diet containing DRPE showed regular liver markers (AST, ALP, and ALT); kidney markers (urea and creatinine); high TP, TA, and GSH; and low MDA, while rats treated with synthetic dye and aspartame showed higher liver and kidney markers; lowered TP, TA, and GSH; and high MDA. After proving the safety of DRPE, it can be safely added to strawberry beverages. Significant sensorial traits, enhanced red color, and taste characterize the strawberry beverages supplemented with DRPE. The lightness and redness of strawberries were enhanced, and the color change ΔE values in DRPE-supplemented beverages ranged from 1.1 to 1.35 compared to 1.69 in controls, indicating the preservative role of DRPE on color. So, including DRPE in food formulation as a natural colorant and sweetener is recommended for preserving health and the environment.


Assuntos
Antioxidantes , Fabaceae , Ratos , Animais , Antioxidantes/química , Antocianinas/farmacologia , Antocianinas/análise , Edulcorantes , Extratos Vegetais/química , Polissacarídeos/química , Carboidratos/análise , Flores/química , Antibacterianos/farmacologia , Antibacterianos/análise , Fabaceae/química , Bebidas/análise
5.
Phytother Res ; 36(8): 3181-3201, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-35794729

RESUMO

Glycolysis is the primary source of energy for cancer growth and metastasis. The shift in metabolism from mitochondrial oxidative phosphorylation to aerobic glycolysis is called the Warburg effect. Cancer progression due to aerobic glycolysis is often associated with the activation of oncogenes or the loss of tumor suppressors. Therefore, inhibition of glycolysis is one of the effective strategies in cancer control. Pyruvate kinase M2 (PKM2) is a key glycolytic enzyme overexpressed in breast, prostate, lung, colorectal, and liver cancers. Here, we discuss published studies regarding PKM2 inhibitors from natural products that are promising drug candidates for cancer therapy. We have highlighted the potential of natural PKM2 inhibitors for various cancer types. Moreover, we encourage researchers to evaluate the combinational effects between natural and synthetic PKM2 inhibitors. Also, further high-quality studies are needed to firmly establish the clinical efficacy of natural products.


Assuntos
Produtos Biológicos , Neoplasias , Produtos Biológicos/metabolismo , Produtos Biológicos/farmacologia , Produtos Biológicos/uso terapêutico , Linhagem Celular Tumoral , Glicólise , Humanos , Mitocôndrias/metabolismo , Neoplasias/tratamento farmacológico , Neoplasias/metabolismo , Piruvato Quinase/metabolismo
6.
Molecules ; 27(15)2022 Jul 28.
Artigo em Inglês | MEDLINE | ID: mdl-35956775

RESUMO

Multiple biological functions of Mentha pulegium extract were evaluated in the current work. Phytochemical components of the M. pulegium extract were detected by Gas Chromatography-Mass Spectrometry (GC-MS) and High-performance liquid chromatography (HPLC). Moreover, M. pulegium extract was estimated for antioxidant potential by 2,2-Diphenyl-1-picryl-hydrazyl-hydrate (DPPH) free radical scavenging, antimicrobial activity by well diffusion, and anticoagulant activity via prothrombin time (PT) and activated partial thromboplastin time (APTT). GC-MS analysis detected compounds including cholesterol margarate, stigmast-5-en-3-ol, 19-nor-4-androstenediol, androstan-17-one, pulegone-1,2-epoxide, isochiapin B, dotriacontane, hexadecanoic acid and neophytadiene. Chrysoeriol (15.36 µg/mL) was followed by kaempferol (11.14 µg/mL) and 7-OH flavone (10.14 µg/mL), catechin (4.11 µg/mL), hisperdin (3.05 µg/mL), and luteolin (2.36 µg/mL) were detected by HPLC as flavonoids, in addition to ferulic (13.19 µg/mL), cinnamic (12.69 µg/mL), caffeic (11.45 µg/mL), pyrogallol (9.36 µg/mL), p-coumaric (5.06 µg/mL) and salicylic (4.17 µg/mL) as phenolics. Antioxidant activity was detected with IC50 18 µg/mL, hemolysis inhibition was recorded as 79.8% at 1000 µg/mL, and PT and APTT were at 21.5 s and 49.5 s, respectively, at 50 µg/mL of M. pulegium extract. The acute toxicity of M. pulegium extract was recorded against PC3 (IC50 97.99 µg/mL) and MCF7 (IC50 80.21 µg/mL). Antimicrobial activity of M. pulegium extract was documented against Bacillus subtilis, Escherichia coli, Pseudomonasaureus, Candida albicans, Pseudomonas aeruginosa, but not against black fungus Mucor circinelloides. Molecular docking was applied using MOE (Molecular Operating Environment) to explain the biological activity of neophytadiene, luteolin, chrysoeriol and kaempferol. These compounds could be suitable for the development of novel pharmacological agents for treatment of cancer and bacterial infections.


Assuntos
Anti-Infecciosos , Mentha pulegium , Antibacterianos/farmacologia , Anti-Infecciosos/farmacologia , Antioxidantes/química , Hemólise , Hemolíticos , Quempferóis , Luteolina , Mentha pulegium/química , Simulação de Acoplamento Molecular , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia
7.
Molecules ; 27(5)2022 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-35268707

RESUMO

Cisplatin (CISP) is one of the most widely used anti-cancer chemotherapeutic agents with remarkable efficacy against various types of cancers. However, it has been associated with nephrotoxicity amongst other undesirable side effects. Pomegranate (PE) is a potent antioxidant and anti-inflammatory agent effective against cancer, with a superior benefit of not being associated with the common toxicities related to the use of conventional chemotherapeutic agents. However, the application of PE is limited by its reduced solubility and decreased bioavailability. We investigated the potential of a novel nanoparticle (NP) enclosing PE to enhance its solubility and improve its bioavailability, and efficacy to prevent CISP-associated nephrotoxicity in a mice model of Ehrlich solid carcinoma (ESC). All mice were grouped into four cohorts: (I) control, (II) tumor, (III) CISP, and (IV) CISP + PE-NPs. The data obtained demonstrated that PE-NPs was beneficial in potently ameliorating CISP-induced nephrotoxicity in ESC mice. PE-NPs significantly attenuated CISP-induced oxidative stress and lipid peroxidation in the kidney via improving activities of antioxidants (SOD, GSH, and CAT). Additionally, PE-NPs considerably decreased CISP-induced inflammation in the kidney by decreasing the levels of NF-kB, IL-1ß, and TNF-α. Notably, PE-NPs did not assuage the antitumor efficacy of CISP as revealed by histological assessment and tumor weight data. In summary, PE-NPs may be a potent alternative anticancer therapy devoid of nephrotoxicity.


Assuntos
Antineoplásicos , Carcinoma , Nanopartículas , Punica granatum , Animais , Antineoplásicos/efeitos adversos , Antineoplásicos/metabolismo , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Apoptose , Carcinoma/patologia , Cisplatino/farmacologia , Rim , Camundongos , Estresse Oxidativo
8.
Molecules ; 27(18)2022 Sep 14.
Artigo em Inglês | MEDLINE | ID: mdl-36144719

RESUMO

Emulgel is a new innovatory technique for drug development permitting controlled release of active ingredients for topical administration. We report a stable emulgel of 4% Piper nigrum extract (PNE) prepared using 80% ethanol. The PNE-loaded formulation had an antioxidant activity of 84% and tyrosinase inhibition was 82%. Prepared formulation rendered spherical-shaped globules with high zeta potential (-45.5 mV) indicative of a stable system. Total phenolic contents were 58.01 mg GAE/g of dry extract whereas total flavonoid content was 52.63 mg QE/g of dry extract. Sun protection factor for PNE-loaded emulgel was 7.512 and formulation was stable without any evidence of physical and chemical changes following 90 days of storage. Gas chromatography-mass spectroscopy (GC-MS) revealed seventeen bioactive compounds in the PNE including monoterpenoids, triterpenoids, a tertiary alcohol, fatty acid esters, and phytosterols. In silico studies of GC-MS identified compounds show higher binding affinity in comparison to standard kojic acid indicating tyrosinase inhibition. It can be concluded that PNE-loaded emulgel had prominent antioxidant and tyrosinase inhibition and can be utilized as a promising topical system for anti-aging skin formulation.


Assuntos
Fitosteróis , Piper nigrum , Triterpenos , Alérgenos , Antioxidantes/química , Antioxidantes/farmacologia , Preparações de Ação Retardada , Etanol , Álcoois Graxos , Flavonoides , Simulação de Acoplamento Molecular , Monofenol Mono-Oxigenase , Monoterpenos , Piper nigrum/química , Extratos Vegetais/química , Sementes
9.
Int J Mol Sci ; 22(13)2021 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-34202112

RESUMO

D-galactose (D-gal) administration causes oxidative disorder and is widely utilized in aging animal models. Therefore, we subcutaneously injected D-gal at 200 mg/kg BW dose to assess the potential preventive effect of thymoquinone (TQ) and curcumin (Cur) against the oxidative alterations induced by D-gal. Other than the control, vehicle, and D-gal groups, the TQ and Cur treated groups were orally supplemented at 20 mg/kg BW of each alone or combined. TQ and Cur effectively suppressed the oxidative alterations induced by D-gal in brain and heart tissues. The TQ and Cur combination significantly decreased the elevated necrosis in the brain and heart by D-gal. It significantly reduced brain caspase 3, calbindin, and calcium-binding adapter molecule 1 (IBA1), heart caspase 3, and BCL2. Expression of mRNA of the brain and heart TP53, p21, Bax, and CASP-3 were significantly downregulated in the TQ and Cur combination group along with upregulation of BCL2 in comparison with the D-gal group. Data suggested that the TQ and Cur combination is a promising approach in aging prevention.


Assuntos
Benzoquinonas/farmacologia , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Curcumina/farmacologia , Galactose/farmacologia , Miocárdio/metabolismo , Oxirredução/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Animais , Benzoquinonas/química , Curcumina/química , Imuno-Histoquímica , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Especificidade de Órgãos , Ratos , Relação Estrutura-Atividade
10.
J Therm Biol ; 93: 102683, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-33077109

RESUMO

BACKGROUND: Heat stress is a condition that is due to extreme heat exposure. It occurs when the body cannot keep its temperature healthy in response to a hot climate and associated with oxidative stress. Testicular hyperthermia can induce apoptosis of sperm cells, affect sperm production and decrease sperm concentration, leading to sperm disorder, for this reason, we examined the protective impact of pycnogenol that it has a wide range of biological benefits, including antioxidant, anti-inflammatory and anti-cancer activities against the oxidative alterations that happen in testicular and brain tissues due to heat stress in rats. STUDY DESIGN: Forty-eight Wistar male rats, approximately around 6 weeks age were allocated randomly into four groups (12 in each) of control, HS (subjected to heat stress and supplemented orally with 50 mg of pycnogenol/kg b. w./day dissolved in saline for 21 days), and pycnogenol (rats supplemented orally with 50 mg of pycnogenol/kg b. w./day dissolved in saline for 21 days). RESULTS: Data revealed a promising role of pycnogenol as an antioxidant, natural product to successfully reverse the heat-induced oxidative alterations in testicular and brain tissues of rats through significant upregulation of superoxide dismutase-2, catalase, reduced glutathione, and anti-apoptotic gene, while downregulating pro-apoptotic, and heat shock protein70. Pycnogenol treatment also reversed the reproductive hormone level and spermatogenesis to their normal values. CONCLUSION: Pycnogenol as a natural protective supplement could recover these heat stress-induced oxidative changes in testes and hypothalamus.


Assuntos
Antioxidantes/farmacologia , Flavonoides/farmacologia , Transtornos de Estresse por Calor/tratamento farmacológico , Extratos Vegetais/farmacologia , Transcriptoma , Animais , Antioxidantes/uso terapêutico , Apoptose , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Flavonoides/uso terapêutico , Glutationa/metabolismo , Proteínas de Choque Térmico HSP70/genética , Proteínas de Choque Térmico HSP70/metabolismo , Transtornos de Estresse por Calor/prevenção & controle , Masculino , Estresse Oxidativo , Extratos Vegetais/uso terapêutico , Proteínas Proto-Oncogênicas c-bcl-2/genética , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Ratos , Ratos Wistar , Espermatogênese , Superóxido Dismutase/genética , Superóxido Dismutase/metabolismo , Testículo/efeitos dos fármacos , Testículo/metabolismo
12.
Int J Mol Sci ; 18(5)2017 Apr 27.
Artigo em Inglês | MEDLINE | ID: mdl-28448463

RESUMO

Antioxidants have valuable effects on the process of spermatogenesis, particularly with diabetes mellitus (DM). Therefore, the present study investigated the impact and the intracellular mechanisms by which thymoquinone (TQ) works against diabetes-induced testicular deteriorations in rats. Wistar male rats (n = 60) were randomly allocated into four groups; Control, Diabetic (streptozotocin (STZ)-treated rats where diabetes was induced by intraperitoneal injection of STZ, 65 mg/kg), Diabetic + TQ (diabetic rats treated with TQ (50 mg/kg) orally once daily), and TQ (non-diabetic rats treated with TQ) for 12 weeks. Results revealed that TQ significantly improved the sperm parameters with a reduction in nitric oxide (NO) and malondialdehyde (MDA) levels in testicular tissue. Also, it increased testicular reduced glutathione (GSH) levels and superoxide dismutase (SOD) activity. Interestingly, TQ induced downregulation of testicular inducible nitric oxide synthase (iNOS) and nuclear factor kappa-B (NF-κB) and significantly upregulated the aromatase protein expression levels in testicles in comparison with the diabetic rats. In conclusion, TQ treatment exerted a protective effect against reproductive dysfunction induced by diabetes not only through its powerful antioxidant and hypoglycemic effects but also through its downregulation of testicular iNOS and NF-κB along with upregulation of aromatase expression levels in diabetic rats.


Assuntos
Antioxidantes/metabolismo , Aromatase/metabolismo , Benzoquinonas/farmacologia , Substâncias Protetoras/farmacologia , Espermatogênese/efeitos dos fármacos , Testículo/efeitos dos fármacos , Animais , Peso Corporal/efeitos dos fármacos , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/patologia , Glutationa/metabolismo , Masculino , Malondialdeído/metabolismo , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Ratos , Ratos Wistar , Estreptozocina/toxicidade , Superóxido Dismutase/metabolismo , Testículo/metabolismo , Testículo/patologia , Regulação para Cima/efeitos dos fármacos
13.
Pak J Pharm Sci ; 29(5 Suppl): 1881-1884, 2016 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28476718

RESUMO

Nigella sativa (N. sativa), remedial usage against different diseases associated with skeleton, cardiovascular, digestive and urinary systems has a long-standing history. At present, efforts are underway to study its effects against various cancers at both the cellular and molecular levels. In this review, the role of active constituents like thymoquinone (TQ) on different types of cancer has been explored. TQ putative involvement in metastasis has been assessed by elucidating its effects on cell proliferation, adhesion, invasion and angiogenesis. Up regulation of caspase 3, Smac and down regulation of p-AKT, p65, XIAP, Bcl-2, COX-2 is also influenced by N. sativa. These findings prove a significant positive correlation between TQ concentrations and induction of apoptosis, decrease in motility and a reduction in invasion and angiogenesis in cancerous cells. However, there are still quite a few unaddressed domains, which need to be understood. One of these may include target specificity of N. sativa against cancerous tissues, mode of administration, dosage and downstream regulators in mediating these effects. In reference to earlier findings and low cost availability, N. sativa may, also, be suggested as either a suitable sole remedy for cancer or as a complementary to ongoing conventional therapy based extensive and rigorous in vivo optimization and validation.


Assuntos
Metástase Neoplásica/prevenção & controle , Nigella sativa , Plantas Medicinais , Humanos
14.
Front Bioeng Biotechnol ; 12: 1348365, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38544976

RESUMO

Biosurfactants are surface-active molecules with unique qualities and various uses. Many microorganisms produce secondary metabolites with surface-active characteristics that serve various antiviral functions. The HIV and Zika viruses were chosen for this study because they can spread from mother to child and result in potentially fatal infections in infants. Halophilic bacteria from the Red Sea solar saltern in Egypt were screened using drop collapse, emulsification activity, and oil displacement assays to produce biosurfactants and emulsifiers. Halobacterium jilantaiense strain JBS1 was the most effective strain of the Halobacteriaceae family. It had the best oil displacement test and emulsification activity against kerosene and crude oil, respectively. Among the ten isolates, it produced the most promising biosurfactant, also recognized by the GC-MASS library. This study evaluated biosurfactants from halophilic bacteria as potential antiviral drugs. Some of the computer methods we use are molecular docking, ADMET, and molecular dynamics. We use model organisms like the HIV reverse transcriptase (PDB: 5VZ6) and the Zika virus RNA-dependent RNA polymerase (ZV-RdRP). Molecular docking and molecular dynamics make the best complexes with 5VZ6 HIV-RT and flavone (C25) and 5wz3 ZV-RdRP and ethyl cholate (C8). Testing for ADMET toxicity on the complex revealed that it is the safest medicine conceivable. The 5VZ6-C25 and 5wz3-C8 complexes also followed the Lipinski rule. They made five hydrogen bond donors and ten hydrogen bond acceptors with 500 Da MW and a 5:1 octanol/water partition coefficient. Finally, extreme settings require particular adaptations for stability, and extremophile biosurfactants may be more stable.

15.
Front Bioeng Biotechnol ; 12: 1348344, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38544980

RESUMO

Active components in medicinal plants provide unlimited useful and traditional medicines. Antimicrobial activities are found in secondary metabolites in plant extracts such as argan oil. This experimental investigation aims to determine argan oil's volatile compounds and examine their in vitro antimicrobial properties. In silico simulations, molecular docking, pharmacokinetics, and drug-likeness prediction revealed the processes underlying the in vitro biological possessions. Gas chromatography-mass spectrometry (GC/MS) was used to screen argan oil's primary components. In silico molecular docking studies were used to investigate the ability of the selected bioactive constituents of argan oil to act effectively against Pseudomonas aeruginosa and Staphylococcus aureus (S. aureus) isolated from infections. The goal was to study their ability to interact with both bacteria's essential therapeutic target protein. The 21 chemicals in argan oil were identified by GC/MS. Docking results for all compounds with S. aureus and P. aeruginosa protease proteins ranged from -5 to -9.4 kcal/mol and -5.7 to -9.7 kcal/mol, respectively, compared to reference ligands. Our docking result indicates that the 10-octadecenoic acid, methyl ester was the most significant compound with affinity scores of -9.4 and -9.7 kcal/mol for S. aureus and P. aeruginosa proteins, respectively. The minimal bactericidal concentration (MBC) and minimal inhibitory concentration (MIC) of argan oil were 0.7 ± 0.03 and 0.5 ± 0.01 for S. aureus and 0.4 ± 0.01 and 0.3 ± 0.02 for P. aeruginosa, respectively. We confirmed the antimicrobial properties of argan oil that showed significant growth inhibition for S. aureus and P. aeruginosa.

16.
Appl Biochem Biotechnol ; 195(10): 5753-5776, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36705842

RESUMO

The green synthesis of selenium nanoparticles (Se NPs) had been synthesized by pomegranate peel extract (PPE). The antimicrobial, antioxidant, and anticancer activities of the synthesized Se NPs, as well as their hemocompatibility, were investigated. Se NPs were characterized by UV-Vis., SEM, XRD, HR-TEM, DLS, EDX, FTIR, and mapping techniques. HR-TEM image represented the spheroidal forms with moderately monodispersed NPs with a mean diameter 14.5 nm. The SEM image of Se NPs, incorporated with PPE, exhibits uniform NP surfaces, and the appearance was clear. The antimicrobial results confirmed the potential of Se NPs to hinder the growth of some tested pathogenic microbes. Results revealed that Se NPs exhibited promising antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, Staphylococcus aureus, and Streptococcus mutans where inhibition zones were 29, 16, 41, 22, and 54 mm, respectively. Likewise, it exhibited antifungal activity where the values of inhibition zones were 41, 40, 38, and 36 mm against Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus, and A. niger, respectively. The antioxidant activities of Se NPs at concentrations 250-4000 µg/mL were greater than 90% in all cases. Se NP concentrations of 500 µg/mL or less are safe in usage according to hemocompatibility study. Se NPs had an IC50 of 113.73 µg/mL in a cytotoxicity experiment. Results revealed that Se NPs have promising anticancer activities against MCF7 and Mg63 cancerous cell line, where IC50 was 69.8 and 47.9 µg/mL, respectively. In conclusion, Se NPs were successfully biosynthesized using PPE for the first time; these Se NPs had promising antimicrobial, antioxidant, and anticancer activities.


Assuntos
Anti-Infecciosos , Nanopartículas Metálicas , Punica granatum , Selênio , Antioxidantes/farmacologia , Selênio/farmacologia , Anti-Infecciosos/farmacologia , Antibacterianos/farmacologia , Extratos Vegetais/farmacologia , Testes de Sensibilidade Microbiana
17.
ACS Omega ; 8(36): 32458-32467, 2023 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-37720762

RESUMO

The present study aimed to assess the potential of plant growth-promoting Actinobacteria and olive solid waste (OSW) in ameliorating some biochemical and molecular parameters of wheat (Triticum aestivum) plants under the toxicity of high chromium levels in the soil. With this aim, a pot experiment was conducted, where the wheat plants were treated with a consortium of four Actinobacterium sp. (Bf treatment) and/or OSW (4% w/w) under two levels of nonstress and chromium stress [400 mg Cr(VI) per kg of soil] to estimate the photosynthetic traits, antioxidant protection machine, and detoxification activity. Both Bf and OSW treatments improved the levels of chlorophyll a (+47-98%), carotenoid (+324-566%), stomatal conductance (+17-18%), chlorophyll fluorescence (+12-28%), and photorespiratory metabolism (including +44-72% in glycolate oxidase activity, +6-72% in hydroxypyruvate reductase activity, and +5-44% in a glycine to serine ratio) in leaves of stressed plants as compared to those in the stressed control, which resulted in higher photosynthesis capacity (+18-40%) in chromium-stressed plants. These results were associated with an enhancement in the content of antioxidant metabolites (+10-117%), of direct reactive oxygen species-detoxifying enzymes (+49-94%), and of enzymatic (+40-261%) and nonenzymatic (+17-175%) components of the ascorbate-glutathione cycle in Bf- and OSW-treated plants under stress. Moreover, increments in the content of phytochelatins (+38-74%) and metallothioneins (+29-41%), as markers of detoxification activity, were recorded in the plants treated with Bf and OSW under chromium toxicity. In conclusion, this study revealed that the application of beneficial Actinobacteria and OSW as biofertilization/supplementation could represent a worthwhile consequence in improving dry matter production and enhancing plant tolerance and adaptability to chromium toxicity.

18.
Microorganisms ; 11(3)2023 Mar 06.
Artigo em Inglês | MEDLINE | ID: mdl-36985234

RESUMO

Hypervirulent Klebsiella pneumoniae (hvKp) is a new emerging variant of K. pneumoniae that is increasingly reported worldwide. The variant hvKp is known to cause severe invasive community-acquired infections such as metastatic meningitis, pyogenic liver abscesses (PLA) and endophthalmitis, but its role in hospital-acquired infections (HAIs) is little known. The aim of this study was to evaluate the prevalence of hvKp among hospital-acquired (HA) K. pneumoniae infections in the intensive care unit (ICU) and to compare between hvKp and classical K. pneumoniae (cKP) regarding antimicrobial resistance pattern, virulence and molecular characteristics. The study was cross-sectional and included 120 ICU patients suffering from HA K. pneumoniae infections between January and September 2022. K. pneumoniae isolates were subjected to antimicrobial susceptibility testing and detection of extended-spectrum-ß-lactamase (ESBL) production by the Phoenix 100 automated microbiology system, string test, biofilm formation, serum resistance assay, and detection of virulence-associated genes (rmpA, rmpA2, magA, iucA) and capsular serotype-specific genes (K1, K2, K5, K20, K57) by polymerase chain reaction (PCR). Of 120 K. pneumoniae isolates, 19 (15.8%) were hvKp. The hypermucoviscous phenotype was more significantly detected in the hvKp group than in the cKP group (100% vs. 7.9%, p ≤ 0.001). The rate of resistance to different antimicrobial agents was significantly higher in the cKP group than that in the hvKp group. Fifty-three strains were identified as ESBL-producing strains, which was more frequent in the cKP group than in the hvKp group (48/101 [47.5%] vs. 5/19 [26.3%], respectively, p ≤ 0.001). The hvKP isolates were highly associated with moderate and strong biofilm formation than cKP isolates (p = 0.018 and p = 0.043 respectively). Moreover, the hvKP isolates were highly associated with intermediate sensitivity and re sistance to serum in the serum resistance assay (p = 0.043 and p = 0.016 respectively). K1, K2, rmpA, rmpA2, magA and iucA genes were significantly associated with hvKp (p ≤ 0.001, 0.004, <0.001, <0.001, 0.037 and <0.001, respectively). However, K5, K20 and K57 were not associated with hvKp. The hvKp strains have emerged as a new threat to ICU patients because of their ability to cause more severe and life-threatening infections than cKP. The string test alone as a laboratory test for screening of hvKp has become insufficient. Recently, hvKp was defined as hypermucoviscous- and aerobactin-positive. It is important to improve the awareness towards the diagnosis and management of hvKp infections.

19.
Infect Drug Resist ; 16: 4397-4408, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37431447

RESUMO

Background: Otitis externa and otitis media are two types of ear infections that affect people of all ages, although they are more common in newborns and young children. Antibiotic usage, healthcare, and advanced age all play a role in the development of this illness. Methods: Fifty-eight patients with various kinds of infections of the ears were voluntary patients attending the outpatient clinics of the Prince Mutaib Bin Abdulaziz Hospital in Sakaka, Al Jouf, Saudi Arabia, examined to evaluate the role of bacteria and the likely significance of plasmids in their antibiotic resistance as ear infectious agents. Results: Staphylococcus aureus and Pseudomonas aeruginosa are the most prevalent bacteria found in ear infections. The greatest number of major bacterial isolates were S. aureus (54%), followed by P. aeruginosa (13%), whereas a smaller number of isolates (3%) were from Streptococcus pyogenes, Bacillus subtilis, and Proteus vulgaris, respectively. Mixed growth was noted in 3.4% of instances. The isolation rate for Gram-positive organisms was 72%, while the rate for Gram-negative species was 28%. All the isolates had DNA greater than 14 kilobases. Hind III analysis of the plasmid DNA extracted from the resistant strains of ear infection demonstrated that antibiotic-resistance plasmids were extensively dispersed. Exotoxin A PCR amplification indicated 396 pb PCR-positive DNA for all identified samples, with the exception of three strains for which no band was observed. Patients in the epidemiological study ranged in number, but all were linked together for the purposes of the study because of their shared epidemiological characteristics. Conclusion: Vancomycin, linezolid, tigecycline, rifampin, and daptomycin are all antibiotics that have been shown to be effective against S. aureus and P. aeruginosa. Microbiological pattern evaluation and antibiotic sensitivity patterns of the microorganisms providing empirical antibiotics are becoming increasingly crucial to minimize issues and the development of antibiotic-resistant strains.

20.
Poult Sci ; 102(9): 102786, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37454641

RESUMO

Avian campylobacteriosis is a vandal infection that poses human health hazards. Campylobacter is usually colonized in the avian gut revealing mild signs in the infected birds, but retail chicken carcasses have high contamination levels of Campylobacter spp. Consequently, the contaminated avian products constitute the main source of human infection with campylobacteriosis and result in severe clinical symptoms such as diarrhea, abdominal pain, spasm, and deaths in sensitive cases. Thus, the current review aims to shed light on the prevalence of Campylobacter in broiler chickens, Campylobacter colonization, bird immunity against Campylobacter, sources of poultry infection, antibiotic resistance, poultry meat contamination, human health hazard, and the use of standard antimicrobial technology during the chicken processing of possible control strategies to overcome such problems.


Assuntos
Infecções por Campylobacter , Campylobacter , Gastroenterite , Animais , Humanos , Infecções por Campylobacter/epidemiologia , Infecções por Campylobacter/veterinária , Aves Domésticas , Galinhas , Prevalência , Gastroenterite/veterinária , Resistência Microbiana a Medicamentos , Carne , Microbiologia de Alimentos , Contaminação de Alimentos
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