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1.
Bioprocess Biosyst Eng ; 47(1): 75-90, 2024 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-38081951

RESUMEN

A significant waste (e.g., high oil content and pollutants such as heavy metals, dyes, and microbial contaminants) in water is generated during crude oil extraction and industrial processes, which poses environmental challenges. This study explores the potential of Ag@Fe3O4 nanocomposite (NC) biosynthesized using the aqueous leaf extract of Laurus nobilis for the treatment of oily wastewater. The NC was characterized using ultraviolet-visible (UV-Vis) spectrophotometry, Scanning Electron Microscopy (SEM), Fourier Transformed Infrared (FTIR) and X-Ray Diffraction (XRD) spectroscopies. The crystalline structure of the NC was determined to be face-centered cubic with an average size of 42 nm. Ag@Fe3O4 NC exhibited significant degradation (96.8%, 90.1%, and 93.8%) of Rose Bengal (RB), Methylene Blue (MB), and Toluidine Blue (TB), respectively, through a reduction reaction lasting 120 min at a dye concentration of 10 mg/L. The observed reaction kinetics followed a pseudo-first-order model, with rate constants (k-values) of 0.0284 min-1, 0.0189 min-1, and 0.0212 min-1 for RB, MB, and TB, respectively. The fast degradation rate can be attributed to the low band gap (1.9 eV) of Ag@Fe3O4 NC. The NC elicited an impressive effectiveness (99-100%, 98.0%, and 91.8% within 30 min) in removing, under sunlight irradiation, several heavy metals, total petroleum hydrocarbons (TPH), and total suspended solids (TSS) from the oily water samples. Furthermore, Ag@Fe3O4 NC displayed potent antibacterial properties and a good biocompatibility. These findings contribute to the development of efficient and cost-effective methods for wastewater treatment and environmental remediation.


Asunto(s)
Metales Pesados , Nanocompuestos , Aguas Residuales , Fotólisis , Antibacterianos/farmacología , Antibacterianos/química , Agua , Colorantes/química , Nanocompuestos/química , Catálisis
2.
Artículo en Inglés | MEDLINE | ID: mdl-39284929

RESUMEN

The synthesis of magnesium hydroxide nanoparticles (Mg(OH)2 NPs) using plant extracts are known to be a practical, economical, and an environmentally friendly approach. In this work, Mg(OH)2 NPs were synthesized using aqueous leaf extract of Tinospora cordifolia, a medicinal plant commonly found in India. The synthesized Mg(OH)2 NPs were characterized using various spectroscopic techniques. The ultraviolet-visible (UV-Vis) absorption peak of the Mg(OH)2 NPs was detected at 289 nm, Fourier transform infrared (FTIR) analysis confirmed the presence of various functional groups, and X-ray diffraction (XRD) patterns revealed the well-crystallized structure of the Mg(OH)2 NPs. High-resolution transmission electron microscopy (HR-TEM) and scanning electron microscopy (SEM) analyses depicted spherical morphology and an average particle size (PS) of 27.71 nm. The energy-dispersive X-ray (EDX) analysis confirmed the presence of C, O, and Mg elements, and the X-ray photoelectron spectroscopy (XPS) survey spectrum confirmed the elements for the Su 1 s peak at 280.2 eV. The dynamic light scattering (DLS) analysis displayed an average PS of 54.3 nm, and the Zeta potential (ZP) was of 9.89 mV. The fabricated Mg(OH)2 NPs displayed notable antibacterial activity against S. epidermidis, E. coli, and S. aureus. In addition, these NPs exhibited strong antioxidant properties (> 75%) based on DPPH, ABTS, and hydrogen peroxide (H2O2) assays. Further, the same NPs exerted a potent anti-inflammatory activity (> 65%) based on COX-1 and COX-2 evaluations. The anti-Alzheimer' disease (AD) potential of Mg(OH)2 NPs was assessed through effective inhibition (> 70%) of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities. Molecular docking (MD) studies confirmed that caryophyllene has higher binding affinity with AChE (-5.3 kcal/mol) and BuChE (-6.4 kcal/mol) enzymes. This study emphasizes the green synthesis of Mg(OH)2 NPs using T. cordifolia as a plant source and highlights their potential for biomedical applications.

3.
Molecules ; 28(4)2023 Feb 10.
Artículo en Inglés | MEDLINE | ID: mdl-36838699

RESUMEN

In this study, pEGFP-LUC was used as a model plasmid and three distinct cationic lipids (dioleyloxy-propyl-trimethylammonium chloride [DOTMA], dioleoyl trimethylammonium propane [DOTAP], and cetylpyridinium chloride [CPC]) were tested along with PEG 5000, as a nonionic surfactant, to prepare glyceryl monostearate (GMS)-based cationic solid lipid nanoparticles (cSLNs). Both the type and quantity of surfactant had an impact on the physicochemical characteristics of the cSLNs. Thermal analysis of the greater part of the endothermic peaks of the cSLNs revealed they were noticeably different from the individual pure compounds based on their zeta potential (ZP ranging from +17 to +56 mV) and particle size (PS ranging from 185 to 244 nm). The addition of cationic surfactants was required to produce nanoparticles (NPs) with a positive surface charge. This suggested that the surfactants and extensive entanglement of the lipid matrix GMS provided support for the behavioral diversity of the cSLNs and their capacity to interface with the plasmid DNA. Additionally, hemolytic assays were used to show that the cSLNs were biocompatible with the human colon cancer HCT-116 and human bronchial epithelial 16-HBE cell lines. The DOTMA 6-based cSLN was selected as the lead cSLN for further ex vivo and in vivo investigations. Taken together, these new findings might provide some guidance in selecting surfactants to prepare extremely efficient and non-toxic cSLN-based therapeutic delivery systems (e.g., gene therapy).


Asunto(s)
Nanopartículas , Compuestos de Amonio Cuaternario , Humanos , Compuestos de Amonio Cuaternario/química , Tensoactivos/química , Nanopartículas/química , Cationes
4.
Molecules ; 28(3)2023 Feb 03.
Artículo en Inglés | MEDLINE | ID: mdl-36771180

RESUMEN

Wilson's disease causes copper accumulation in the liver and extrahepatic organs. The available therapies aim to lower copper levels by various means. However, a potent drug that can repair the damaged liver and brain tissue is needed. Silymarin has hepatoprotective, antioxidant, and cytoprotective properties. However, poor oral bioavailability reduces its efficacy. In this study, a "thin film hydration method" was used for synthesizing silymarin-encapsulated liposome nanoparticles (SLNPs) and evaluated them against copper toxicity, associated liver dysfunction and neurobehavioral abnormalities in Wistar rats. After copper toxicity induction, serological and behavioral assays were conducted to evaluate treatment approaches. Histological examination of the diseased rats revealed severe hepatocyte necrosis and neuronal vacuolation. These cellular degenerations were mild in rats treated with SLNPs and a combination of zinc and SLNPs (ZSLNPs). SLNPs also decreased liver enzymes and enhanced rats' spatial memory significantly (p = 0.006) in the diseased rats. During forced swim tests, SLNPs treated rats exhibited a 60-s reduction in the immobility period, indicating reduced depression. ZSLNPs were significantly more effective than traditional zinc therapy in decreasing the immobility period (p = 0.0008) and reducing liver enzymes, but not in improving spatial memory. Overall, SLNPs enhanced oral silymarin administration and managed copper toxicity symptoms.


Asunto(s)
Degeneración Hepatolenticular , Silimarina , Ratas , Animales , Ratas Wistar , Silimarina/uso terapéutico , Cobre/farmacología , Liposomas/farmacología , Hígado , Degeneración Hepatolenticular/tratamiento farmacológico , Zinc/farmacología , Zinc/uso terapéutico
5.
Molecules ; 28(10)2023 May 17.
Artículo en Inglés | MEDLINE | ID: mdl-37241888

RESUMEN

Quercetin (QtN) displays low systemic bioavailability caused by poor water solubility and instability. Consequently, it exerts limited anticancer action in vivo. One solution to increase the anticancer efficacy of QtN is the use of appropriate functionalized nanocarriers that preferentially target and deliver the drug to the tumor location. Herein, a direct advanced method was designed to develop water-soluble hyaluronic acid (HA)-QtN-conjugated silver nanoparticles (AgNPs). HA-QtN reduced silver nitrate (AgNO3) while acting as a stabilizing agent to produce AgNPs. Further, HA-QtN#AgNPs served as an anchor for folate/folic acid (FA) conjugated with polyethylene glycol (PEG). The resulting PEG-FA-HA-QtN#AgNPs (further abbreviated as PF/HA-QtN#AgNPs) were characterized both in vitro and ex vivo. Physical characterizations included UV-visible (UV-Vis) spectroscopy, Fourier transform infrared (FTIR) spectroscopy, transmission electron microscopy (TEM), particle size (PS) and zeta potential (ZP) measurements, and biopharmaceutical evaluations. The biopharmaceutical evaluations included analyses of the cytotoxic effects on the HeLa and Caco-2 cancer cell lines using the MTT assay; cellular drug intake into cancer cells using flow cytometry and confocal microscopy; and blood compatibility using an automatic hematology analyzer, a diode array spectrophotometer, and an enzyme-linked immunosorbent assay (ELISA). The prepared hybrid delivery nanosystem was hemocompatible and more oncocytotoxic than the free, pure QtN. Therefore, PF/HA-QtN#AgNPs represent a smart nano-based drug delivery system (NDDS) and could be a promising oncotherapeutic option if the data are validated in vivo.


Asunto(s)
Productos Biológicos , Nanopartículas del Metal , Neoplasias , Humanos , Ácido Hialurónico/química , Quercetina/farmacología , Nanopartículas del Metal/química , Células CACO-2 , Plata , Polietilenglicoles/química , Agua , Espectroscopía Infrarroja por Transformada de Fourier
6.
Saudi Pharm J ; 31(12): 101839, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37965489

RESUMEN

Itraconazole (ITZ) is a renowned antifungal medication, however its therapeutic efficacy is limited by low solubility and oral bioavailability. The current research work attempted to augment the oral bioavailability of ITZ by incorporating into self-emulsifying micelles (SEMCs). To fabricate the SEMCs, various preparation techniques including physical mixture, melt-emulsification, solvent evaporation and kneading, were opted by using different weight ratio of drug and solubilizers i.e. Gelucire-50/13 or Gelucire-44/14 and characterized both in vitro and in vivo. The prepared SEMCs were found to be in the size range from 63.4 ± 5.2 to 284.2 ± 19.5 nm with surface charges ranging from -16 ± 1.2 to -27 ± 2.0 mV. The drug solubility was improved to a reasonable extent with all investigated formulations, however, SEMCs in group 6 prepared by kneading method (KMG6) using Gelucire-44/14: drug (10:1 presented 87.6 folds' increase (964.93 ± 2 µg/mL) compared to solubility of crystalline ITZ (11 ± 2 µg/mL) through kneading method. In addition, KMG6 SEMCs shows the fast drug release compared to other SEMCs. Further, KMG6 SEMCs also exhibited 5.12-fold higher relative intestinal serosal fluid absorption compared to crystalline ITZ. The pharmacokinetic parameters such Cmax, AUC and Tmax of KMG6 SEMCs significantly improved compared to crystalline ITZ. In conclusion, the manipulation of ITZ solubility, dissolution rate and absorption using SEMCs is a promising strategy for bioavailability enhancement.

7.
Int J Mol Sci ; 23(24)2022 Dec 14.
Artículo en Inglés | MEDLINE | ID: mdl-36555575

RESUMEN

Antibacterial restorative materials against caries-causing bacteria are highly preferred among high-risk patients, such as the elderly, and patients with metabolic diseases such as diabetes. This study aimed to enhance the antibacterial potential of resin composite with Magnesium-doped Zinc oxide (Mg-doped ZnO) nanoparticles (NPs) and to look for their effectiveness in the alloxan-induced diabetic model. Hexagonal Mg-doped ZnO NPs (22.3 nm diameter) were synthesized by co-precipitation method and characterized through ultraviolet-visible (UV-Vis), Fourier transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD), scanning electron microscopy (SEM), and energy dispersive spectroscopy (EDS) analysis. The Mg-doped ZnO NPs (1, 2.5 and 5% w/w) were then evaluated for antibacterial activity using a closed system in vitro biofilm model. Significant enhancement in the antibacterial properties was observed in composites with 1% Mg-doped ZnO compared to composites with bare ZnO reinforced NPs (Streptococcus mutans, p = 0.0005; Enterococcus faecalis, p = 0.0074, Saliva microcosm, p < 0.0001; Diabetic Saliva microcosm, p < 0.0001). At 1−2.5% Mg-doped ZnO NPs concentration, compressive strength and biocompatibility of composites were not affected. The pH buffering effect was also achieved at these concentrations, hence not allowing optimal conditions for the anaerobic bacteria to grow. Furthermore, composites with Mg-doped ZnO prevented secondary caries formation in the secondary caries model of alloxan-induced diabetes. Therefore, Mg-doped ZnO NPs are highly recommended as an antibacterial agent for resin composites to avoid biofilm and subsequent secondary caries formation in high-risk patients.


Asunto(s)
Diabetes Mellitus , Nanopartículas del Metal , Nanopartículas , Óxido de Zinc , Humanos , Anciano , Óxido de Zinc/farmacología , Óxido de Zinc/química , Zinc , Aloxano , Magnesio/farmacología , Óxido de Magnesio/farmacología , Óxido de Magnesio/uso terapéutico , Susceptibilidad a Caries Dentarias , Nanopartículas/química , Antibacterianos/farmacología , Antibacterianos/uso terapéutico , Antibacterianos/química , Nanopartículas del Metal/química , Espectroscopía Infrarroja por Transformada de Fourier , Difracción de Rayos X , Pruebas de Sensibilidad Microbiana
8.
Int J Mol Sci ; 23(6)2022 Mar 15.
Artículo en Inglés | MEDLINE | ID: mdl-35328564

RESUMEN

Chronic liver disease (CLD) is a global threat to the human population, with manifestations resulting from alcohol-related liver disease (ALD) and non-alcohol fatty liver disease (NAFLD). NAFLD, if not treated, may progress to non-alcoholic steatohepatitis (NASH). Furthermore, inflammation leads to liver fibrosis, cirrhosis, and hepatocellular carcinoma. Vitexin, a natural flavonoid, has been recently reported for inhibiting NAFLD. It is a lipogenesis inhibitor and activates lipolysis and fatty acid oxidation. In addition, owing to its antioxidant properties, it appeared as a hepatoprotective candidate. However, it exhibits low bioavailability and low efficacy due to its hydrophobic nature. A novel rat model for liver cirrhosis was developed by CCL4/Urethane co-administration. Vitexin encapsulated liposomes were synthesized by the 'thin-film hydration' method. Polyethylene glycol (PEG) was coated on liposomes to enhance stability and stealth effect. The diseased rats were then treated with vitexin and PEGylated vitexin liposomes, administered intravenously and orally. Results ascertained the liposomal encapsulation of vitexin and subsequent PEG coating to be a substantial strategy for treating liver cirrhosis through oral drug delivery.


Asunto(s)
Neoplasias Hepáticas , Enfermedad del Hígado Graso no Alcohólico , Animales , Apigenina , Etanol , Liposomas/uso terapéutico , Hígado/patología , Cirrosis Hepática/patología , Neoplasias Hepáticas/patología , Enfermedad del Hígado Graso no Alcohólico/patología , Polietilenglicoles/uso terapéutico , Ratas , Ratas Sprague-Dawley
9.
Molecules ; 27(24)2022 Dec 17.
Artículo en Inglés | MEDLINE | ID: mdl-36558144

RESUMEN

This study aimed to establish the phytochemical profile of Glochidion velutinum and its cytotoxic activity against prostate cancer (PC-3) and breast cancer (MCF-7) cell lines. The phytochemical composition of G. velutinum leaf extract and its fractions was established with the help of total phenolic and flavonoid contents and LC-MS/MS-based metabolomics analysis. The crude methanolic extract and its fractions were studied for pharmacological activity against PC-3 and MCF-7 cell lines using the MTT assay. The total phenolic content of the crude extract and its fractions ranged from 44 to 859 µg GAE/mg of sample whereas total flavonoid contents ranged from 20 to 315 µg QE/mg of sample. A total of forty-eight compounds were tentatively dereplicated in the extract and its fractions. These phytochemicals included benzoic acid derivatives, flavans, flavones, O-methylated flavonoids, flavonoid O- and C-glycosides, pyranocoumarins, hydrolysable tannins, carbohydrate conjugates, fatty acids, coumarin glycosides, monoterpenoids, diterpenoids, and terpene glycosides. The crude extract (IC50 = 89 µg/mL), the chloroform fraction (IC50 = 27 µg/mL), and the water fraction (IC50 = 36 µg/mL) were found to be active against the PC-3 cell line. However, the crude extract (IC50 = 431 µg/mL), the chloroform fraction (IC50 = 222 µg/mL), and the ethyl acetate fraction (IC50 = 226 µg/mL) have shown prominent activity against breast cancer cells. Moreover, G. velutinum extract and its fractions presented negligible toxicity to normal macrophages at the maximum tested dose (600 µg/mL). Among the compounds identified through LC-MS/MS-based metabolomics analysis, epigallocatechin gallate, ellagic acid, isovitexin, and rutin were reported to have anticancer activity against both prostate and breast cancer cell lines and might be responsible for the cytotoxic activities of G. velutinum extract and its bioactive fractions.


Asunto(s)
Neoplasias de la Mama , Malpighiales , Humanos , Femenino , Extractos Vegetales/farmacología , Extractos Vegetales/química , Cromatografía Liquida , Antioxidantes/química , Cloroformo , Espectrometría de Masas en Tándem , Células MCF-7 , Neoplasias de la Mama/metabolismo , Flavonoides/farmacología , Flavonoides/análisis , Fitoquímicos/farmacología , Fitoquímicos/análisis , Glicósidos
10.
Molecules ; 27(21)2022 Oct 24.
Artículo en Inglés | MEDLINE | ID: mdl-36364007

RESUMEN

Resin composites have been widely used in dental restoration. However, polymerization shrinkage and resultant bacterial microleakage are major limitations that may lead to secondary caries. To overcome this, a new type of antibacterial resin composite containing ciprofloxacin-loaded silver nanoparticles (CIP-AgNPs) were synthesized. The chemical reduction approach successfully produced CIP-AgNPs, as demonstrated by FTIR, zeta potential, scanning electron microscopy, and ultraviolet-visible (UV-vis) spectroscopy. CIP-AgNPs were added to resin composites and the antibacterial activity of the dental composite discs were realized against Enterococcus faecalis, Streptococcus mutans, and the Saliva microcosm. The biocompatibility of modified resin composites was assessed and mechanical testing of modified dental composites was also performed. The results indicated that the antibacterial activity and compressive strength of resin composites containing CIP-AgNPs were enhanced compared to the control group. They were also biocompatible when compared to resin composites containing AgNPs. In short, these results established strong ground application for CIP-AgNP-modified dental composite resins.


Asunto(s)
Nanopartículas del Metal , Nanopartículas , Plata/farmacología , Plata/química , Ciprofloxacina/farmacología , Streptococcus mutans , Antibacterianos/farmacología , Antibacterianos/química , Resinas Compuestas/farmacología , Resinas Compuestas/química , Ensayo de Materiales , Nanopartículas/química
11.
Molecules ; 27(23)2022 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-36500511

RESUMEN

Background: Nickel stannate nanocomposites could be useful for removing organic and toxic water pollutants, such as methyl orange (MO). Aim: The synthesis of a nickel oxide-tin oxide nanocomposite (NiO-SnO2 NC) via a facile and economically viable approach using a leaf extract from Ficus elastica for the photocatalytic degradation of MO. Methods: The phase composition, crystallinity, and purity were examined by X-ray diffraction (XRD). The particles' morphology was studied using scanning electron microscopy (SEM). The elemental analysis and colored mapping were carried out via energy dispersive X-ray (EDX). The functional groups were identified by Fourier transform infrared spectroscopy (FTIR). UV-visible diffuse reflectance spectroscopy (UV-vis DRS) was used to study the optical properties such as the absorption edges and energy band gap, an important feature of semiconductors to determine photocatalytic applications. The photocatalytic activity of the NiO-SnO2 NC was evaluated by monitoring the degradation of MO in aqueous solution under irradiation with full light spectrum. The effects of calcination temperature, pH, initial MO concentration, and catalyst dose were all assessed to understand and optimize the physicochemical and photocatalytic properties of NiO-SnO2 NC. Results: NiO-SnO2 NC was successfully synthesized via a biological route using F. elastica leaf extract. XRD showed rhombohedral NiO and tetragonal SnO2 nanostructures and the amorphous nature of NiO-SnO2 NC. Its degree of crystallinity, crystallite size, and stability increased with increased calcination temperature. SEM depicted significant morphological changes with elevating calcination temperatures, which are attributed to the phase conversion from amorphous to crystalline. The elemental analysis and colored mapping show the formation of highly pure NiO-SnO2 NC. FTIR revealed a decrease in OH, and the ratio of oxygen vacancies at the surface of the NC can be explained by a loss of its hydrophilicity at increased temperatures. All the NC samples displayed significant absorption in the visible region, and a blue shift is seen and the energy band gap decreases when increasing the calcination temperatures due to the dehydration and formation of compacted large particles. NiO-SnO2 NC degrades MO, and the photocatalytic performance decreased with increasing calcination temperature due to an increase in the crystallite size of the NC. The optimal conditions for the efficient NC-mediated photocatalysis of MO are 100 °C, 20 mg catalyst, 50 ppm MO, and pH 6. Conclusions: The auspicious performance of the NiO-SnO2 NCs may open a new avenue for the development of semiconducting p-n heterojunction catalysts as promising structures for removing undesirable organic pollutants from the environment.


Asunto(s)
Compuestos Azo , Nanocompuestos , Compuestos Azo/química , Nanocompuestos/química , Catálisis , Extractos Vegetales
12.
Mar Drugs ; 19(9)2021 Aug 26.
Artículo en Inglés | MEDLINE | ID: mdl-34564146

RESUMEN

Marine algae are rich in bioactive nutraceuticals (e.g., carbohydrates, proteins, minerals, fatty acids, antioxidants, and pigments). Biotic (e.g., plants, microorganisms) and abiotic factors (e.g., temperature, pH, salinity, light intensity) contribute to the production of primary and secondary metabolites by algae. Easy, profitable, and sustainable recovery methods include novel solid-liquid and liquid-liquid extraction techniques (e.g., supercritical, high pressure, microwave, ultrasound, enzymatic). The spectacular findings of algal-mediated synthesis of nanotheranostics has attracted further interest because of the availability of microalgae-based natural bioactive therapeutic compounds and the cost-effective commercialization of stable microalgal drugs. Algal extracts can serve as stabilizing/capping and reducing agents for the synthesis of thermodynamically stable nanoparticles (NPs). Different types of nanotherapeutics have been synthesized using physical, chemical, and biological methods. Marine algae are a fascinating source of lead theranostics compounds, and the development of nanotheranostics has been linked to enhanced drug efficacy and safety. Indeed, algae are remarkable nanobiofactories, and their pragmatic properties reside in their (i) ease of handling; (ii) capacity to absorb/accumulate inorganic metallic ions; (iii) cost-effectiveness; and (iv) capacity of eco-friendly, rapid, and healthier synthesis of NPs. Preclinical and clinical trials shall enable to really define effective algal-based nanotherapies. This review aims to provide an overview of the main algal compounds that are nutraceuticals and that can be extracted and purified for nanotheranostic purposes.


Asunto(s)
Productos Biológicos/metabolismo , Chlorophyta/metabolismo , Phaeophyceae/metabolismo , Rhodophyta/metabolismo , Algas Marinas/metabolismo , Animales , Productos Biológicos/química , Productos Biológicos/farmacología , Humanos , Nanomedicina
13.
Molecules ; 27(1)2021 Dec 24.
Artículo en Inglés | MEDLINE | ID: mdl-35011342

RESUMEN

Green synthesis of silver nanoparticles (AgNPs) was synthesized from fresh garlic extract coupled with isoniazid hydrazide (INH), a commonly used antibiotic to treat tuberculosis. A molecular docking study conducted with the selected compounds compared with anthranilate phosphoribosyltransferase (trpD) from Mycobacterium tuberculosis. The aqueous extract of garlic was prepared and mixed with silver nitrate (AgNO3) solution for the superfast synthesis of stable AgNPs. INH was then conjugated with AgNPs at different ratios (v/v) to obtain stable INH-AgNPs conjugates (AgNCs). The resulting AgNCs characterized by FTIR spectra revealed the ultrafast formation of AgNPs (<5 s) and perfectly conjugated with INH. The shifting of λmax to longer wavelength, as found from UV spectral analysis, confirmed the formation of AgNCs, among which ideal formulations (F7, F10, and F13) have been pre-selected. The zeta particle size (PS) and the zeta potential (ZP) of AgNPs were found to be 145.3 ± 2.1 nm and -33.1 mV, respectively. These data were significantly different compared to that of AgNCs (160 ± 2.7 nm and -14.4 mV for F7; 208.9 ± 2.9 nm and -19.8 mV for F10; and 281.3 ± 3.6 nm and -19.5 mV for F13), most probably due to INH conjugation. The results of XRD, SEM and EDX confirmed the formation of AgNCs. From UV spectral analysis, EE of INH as 51.6 ± 5.21, 53.6 ± 6.88, and 70.01 ± 7.11 %, for F7, F10, and F13, respectively. The stability of the three formulations was confirmed in various physiological conditions. Drug was released in a sustainable fashion. Besides, from the preferred 23 compounds, five compounds namely Sativoside R2, Degalactotigonin, Proto-desgalactotigonin, Eruboside B and Sativoside R1 showed a better docking score than trpD, and therefore may help in promoting anti-tubercular activity.


Asunto(s)
Ajo/química , Hidrazinas/química , Isoniazida/síntesis química , Isoniazida/farmacología , Nanopartículas del Metal/química , Extractos Vegetales/química , Plata/química , Antituberculosos/química , Antituberculosos/farmacología , Sitios de Unión , Técnicas de Química Sintética , Estabilidad de Medicamentos , Tecnología Química Verde , Isoniazida/química , Ligandos , Nanopartículas del Metal/ultraestructura , Simulación del Acoplamiento Molecular , Simulación de Dinámica Molecular , Fitoquímicos/química , Fitoquímicos/farmacología , Unión Proteica , Análisis Espectral , Relación Estructura-Actividad
14.
Mar Drugs ; 18(12)2020 Dec 14.
Artículo en Inglés | MEDLINE | ID: mdl-33327517

RESUMEN

Seaweeds are broadly distributed and represent an important source of secondary metabolites (e.g., halogenated compounds, polyphenols) eliciting various pharmacological activities and playing a relevant ecological role in the anti-epibiosis. Importantly, host (as known as basibiont such as algae)-microbe (as known as epibiont such as bacteria) interaction (as known as halobiont) is a driving force for coevolution in the marine environment. Nevertheless, halobionts may be fundamental (harmless) or detrimental (harmful) to the functioning of the host. In addition to biotic factors, abiotic factors (e.g., pH, salinity, temperature, nutrients) regulate halobionts. Spatiotemporal and functional exploration of such dynamic interactions appear crucial. Indeed, environmental stress in a constantly changing ocean may disturb complex mutualistic relations, through mechanisms involving host chemical defense strategies (e.g., secretion of secondary metabolites and antifouling chemicals by quorum sensing). It is worth mentioning that many of bioactive compounds, such as terpenoids, previously attributed to macroalgae are in fact produced or metabolized by their associated microorganisms (e.g., bacteria, fungi, viruses, parasites). Eventually, recent metagenomics analyses suggest that microbes may have acquired seaweed associated genes because of increased seaweed in diets. This article retrospectively reviews pertinent studies on the spatiotemporal and functional seaweed-associated microbiota interactions which can lead to the production of bioactive compounds with high antifouling, theranostic, and biotechnological potential.


Asunto(s)
Ecología , Industrias , Microbiota , Algas Marinas/química , Animales , Humanos
15.
AAPS PharmSciTech ; 21(8): 323, 2020 Nov 16.
Artículo en Inglés | MEDLINE | ID: mdl-33200249

RESUMEN

Crude ginger has been used to treat wounds since ancient times till nowadays. The present study aimed at designing and characterizing topical hydrogel films loaded with ginger extract for wound healing in animal model. The hydrogel films were prepared using PVA and gelatin. The prepared films were evaluated for FTIR analysis, surface morphology, pH, swelling behavior, in vitro release, and % drug content. The wound-healing activity of the extract-loaded hydrogel films was compared with commercially available Silver Sulfadiazine® cream. The drug was compatible with the selected polymers and indicated the suitability of the selected polymers for preparation of topical hydrogel films. The SEM images clearly indicated porous structure of the prepared hydrogel films. Slight changes were observed in pH, ranging from 4.98 ± 0.079 in the beginning of the study to 4.9 ± 0.58 in the end. The swelling percentage after 8 h was 257.7%. The films released 78.7 ± 1.7% of the drug in 250 min. The percent drug content was 97.78 ± 5% which did not change significantly during the storage period. The hydrogel films showed similar wound-healing activity as compared to the commercial product (p > 0.05; ANOVA), while greater wound-healing activity as compared to the control group (p < 0.05; ANOVA) evidenced by intensive collagen formation in histopathological analysis.


Asunto(s)
Quemaduras/patología , Gelatina/química , Metilgalactósidos/química , Cicatrización de Heridas , Animales , Técnicas In Vitro , Modelos Animales , Extractos Vegetales , Sulfadiazina de Plata
16.
Pak J Pharm Sci ; 30(5): 1779-1781, 2017 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-29084701

RESUMEN

The rational use of plants as medicine is traced back over five epochs to ancient documents of early civilizations and is certainly as old as mankind. These medicines originally developed from crude drugs like tinctures and tinctures. Minimum 119 chemical substances are derived from 90 plant species and used all over the world as medicines, several of them containing compounds derived from or modelled after naturally occurring lead molecules and 74% of these derived from orthodox medicinal plants. 252 drugs (11%) are believed to be basic and essential by the WHO and are exclusively of plant origin. We have examined anti-urease activity of ethyl alcohol (Et-OH) and methyl alcohol (Me-OH) extracts of H. rhamnoides and Cassia fistula. Berthelot assay was used for the determination of anti-urease activity. The enzyme activity and inhibition was measured through catalytic effects of urease on urea by measuring change in absorbance in the absence and in the presence of inhibitor at 625nm using UV spectrophotometer. In the study, both Et-OH and Me-OH extracts of H. rhamnoides (91.69%±1.21) and C. fisstula (79.44%±0.55) showed stronger action against urease activity. An overview on the medicinal uses of H. rhamnoides and C. fisstula showing anti-urease activity may predict their possible alternative use for stomach problems. This study may help to explain the beneficial effects of these plants against stomach infection associated with pathogenic strains of H. pylori as Urease is the most prominent protein component of H. pylori.


Asunto(s)
Cassia/química , Inhibidores Enzimáticos/farmacología , Hippophae/química , Extractos Vegetales/farmacología , Ureasa/antagonistas & inhibidores , Catálisis , Inhibidores Enzimáticos/aislamiento & purificación , Etanol/química , Metanol/química , Extractos Vegetales/aislamiento & purificación , Solventes/química , Urea/metabolismo , Ureasa/metabolismo
17.
Pak J Pharm Sci ; 28(5): 1745-55, 2015 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-26408874

RESUMEN

The present study was conducted to formulate controlled release dosage forms containing Ibuprofen with Eudragit® S 100 polymer. The tablets were formulated at three different ratios with the polymer to investigate the effect of different concentrations of polymer on in vitro drug release patterns/kinetics and in vivo absorption/pharmacokinetics. Pre-formulation studies were conducted including bulk density, tapped density, compressibility index, Hausner ratio and angle of repose. In vitro studies were conducted using phosphate buffer (pH 7.4) as dissolution medium. In vivo performance was evaluated using albino rabbits. Physico-chemical characteristics (i.e. dimensional tests, weight variation, hardness, friability and drug content determination) fell in the USP acceptable limits. The compressibility index was found to range between 12.02 ± 0.01% and 18.66 ± 0.03%, the Hausner ratio varied between 1.02 ± 0.01 and 1.19 ± 0.10 and the angle of repose ranged from 15.19 ± 0.01 to 24.52 ± 0.10, all indicating better flow properties than the bulk-reference standard. Both bulk and tapped densities also fell in the USP acceptable range. Ibuprofen market tablets showed Tmax of 2.1 ± 0.4h, which was significantly (P-value <0.05) lower compared to that of the reference standard (i.e. 4.09 ± 1.3h). Ibuprofen test formulation has a half-life (t1/2) of 16.9 ± 2.5h, which was significantly (P-value<0.001) higher compared to that of the reference standard (i.e. 9.23 ± 2.9h). Eudragit® S 100 polymers can be used efficiently to develop directly compressed prolonged release tablets.


Asunto(s)
Antiinflamatorios no Esteroideos/farmacocinética , Ibuprofeno/farmacocinética , Animales , Antiinflamatorios no Esteroideos/administración & dosificación , Preparaciones de Acción Retardada , Excipientes , Interacciones Hidrofóbicas e Hidrofílicas , Ibuprofeno/administración & dosificación , Ácidos Polimetacrílicos/administración & dosificación , Conejos
18.
J Cosmet Dermatol ; 23(3): 1015-1028, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38268219

RESUMEN

BACKGROUND: Tocopherols are well-known antioxidant and moisturizing agent. Tocopherol succinate (TS) are widely used in many skin products especially used in anti-aging and skin whitening product formulation. AIM: We previously reported the successful synthesis and preliminary characterizations of stable TS ethosomal gels (TSEG) (DOI: 10.1111/jocd.14907). Herein, we develop and further characterize TSEG to enhance the stability of the developed formulation with increased permeation through skin. METHODS: Cold method technique was used to prepare TS ethosomes. The developed ethosomal vesicle size was 250 nm, which allowed TS to penetrate through the stratum corneum layer and act on melanocytes. For stability study was assessed by thermogravimetric analysis (TGA) by placing TSEG and unloaded/control ethosomal gel (CEG) at various temperature conditions, that is, 8°C, 25°C, 40°C, and 40°C ± 75% RH for 3 months. Organoleptic evaluation was done in terms of color, odor, and phase separation. Transmission electron microscopy (TEM), Fourier Transform infrared spectroscopy (FTIR), x-ray diffraction spectroscopy (XRD), zeta potential (ZP) and particle size (PS) was used for TSEG physical characterizations. In vitro dissolution and ex-vivo permeation studies (using Franz diffusion cell) were performed for both TSEG and CEG formulations. Human women (N = 34) were used to evaluate in vivo biophysical parameters including erythema, melanin, moisture content, sebum level, and skin elasticity. RESULTS: Developed formulation was highly thermostable during the 3 months. Erythema, melanin, and sebum level decreased while marked improvement (p < 0.05) in moisture content and elasticity have been observed for the developed TSEG. CONCLUSION: The developed TSEG formulation was found to be efficient, safe (no adverse effects observed), stable (at least for 3 months), and easy to use for topical application with improved skin complexation and skin integrity.


Asunto(s)
Absorción Cutánea , alfa-Tocoferol , Humanos , Femenino , alfa-Tocoferol/metabolismo , Administración Cutánea , Melaninas/metabolismo , Liposomas/metabolismo , Piel/metabolismo , Eritema , Geles/metabolismo
19.
PLoS One ; 19(6): e0303285, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38917154

RESUMEN

Typhoid fever, caused by Salmonella enterica serovar typhi, presents a substantial global health threat, particularly in regions with limited healthcare infrastructure. The rise of multidrug-resistant strains of S. typhi exacerbates this challenge, severely compromising conventional treatment efficacy due to over activity of efflux pumps. In our study, a comprehensive exploration of two fundamental aspects to combat MDR in S. typhi is carried out; i.e. employing advanced bioinformatics analyses and AlphaFold AI, We successfully identified and characterised a putative homologue, ABC-TPA, reminiscent of the P-glycoprotein (P-gp) known for its role in multidrug resistance in diverse pathogens. This discovery provides a critical foundation for understanding the potential mechanisms driving antibiotic resistance in S. typhi. Furthermore, employing computational methodologies, We meticulously assessed the potential of lignans, specifically Schisandrin A, B, and C, as promising Efflux Pump Inhibitors (EPIs) against the identified P-gp homologue in S. typhi. Noteworthy findings revealed robust binding interactions of Schisandrin A and B with the target protein, indicating substantial inhibitory capabilities. In contrast, Schisandrin C exhibited instability, showing varied effectiveness among the evaluated lignans. Pharmacokinetics and toxicity predictions underscored the favourable attributes of Schisandrin A, including prolonged action duration. Furthermore, high systemic stability and demanished toxicity profile of SA and SB present their therapeutic efficacy against MDR. This comprehensive investigation not only elucidates potential therapeutic strategies against MDR strains of S. typhi but also highlights the relevance of computational approaches in identifying and evaluating promising candidates. These findings lay a robust foundation for future empirical studies to address the formidable challenges antibiotic resistance poses in this clinically significant infectious diseases.


Asunto(s)
Antibacterianos , Farmacorresistencia Bacteriana Múltiple , Lignanos , Salmonella typhi , Salmonella typhi/efectos de los fármacos , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Lignanos/farmacología , Lignanos/química , Antibacterianos/farmacología , Antibacterianos/química , Proteínas Bacterianas/metabolismo , Proteínas Bacterianas/antagonistas & inhibidores , Proteínas Bacterianas/genética , Humanos , Pruebas de Sensibilidad Microbiana , Biología Computacional/métodos
20.
ACS Omega ; 9(15): 16893-16903, 2024 Apr 16.
Artículo en Inglés | MEDLINE | ID: mdl-38645323

RESUMEN

Wine has been utilized as a source for medicinal preparations, combined with various herbs, to treat particular ailments and disorders. By utilizing herb extracts, regular but limited consumption of these herbal wines helps to decrease the need for prescription medications to treat a variety of ailments. The diversity and the composition of the yeast micropopulation significantly contribute to the sensory characteristics of wine. A particular metabolic activity characterizes the growth of each wine yeast species, which determines the concentrations of flavor compounds in the final wine. Numerous herbs, such as tulsi, ginger, aloe vera, tea, amla, lemongrass, and peppermint, are used in the preparation of herbal wines, where either the herb or herbal blends are primarily used as the substrate. The variants provided improved accuracy, increased acceptability, and broader uses for the novel product. Herbal wines pave the way to provide nutraceuticals to consumers and protection against pathogenic microorganisms and inflammation through their richness in antioxidants. The existing herbal wines and their health advantages are discussed in this Review, along with some new directions for the herbal wine business.

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