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1.
Luminescence ; 39(3): e4724, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38523053

RESUMEN

For white light-rendering research activities, interpretation by using colored emitting materials is an alternative approach. But there are issues in designing the white color emitting materials. Particularly, differences in thermal and decay properties of discrete red, green, and blue emitting materials led to the quest for the search of a single-phased material, able to emit primary colors for white light generation. The current study is an effort to design a simple, single-phase, and cost-effective material with the tunable emission of primary colors by a series of Mg1-xBaxAl2O4:Mn2+ nanopowders. Doping of manganese ion (Mn2+) in the presence of the larger barium cation (Ba2+) at tetrahedral-sites of the spinel magnesium aluminate (MgAl2O4) structure led to the creation of antisite defects. Doped samples were found to have lower bandgaps compared with MgAl2O4, and hybridization of 3d-orbitals of Mn2+ with O(2p), Mg(2s)/Al(2s3p) was found to be responsible for narrowing the bandgap. The distribution of cations at various sites at random results in a variety of electronic transitions between the valance band and oxygen vacancies as well as electron traps produced the antisite defects. The suggested compositions might be used in white light applications since they have three emission bands with centers at 516 nm (green), 464 nm (blue) and 622 nm (red) at an excitation wavelength of 380 nm. A detailed discussion to analyze the effects of the larger cationic radius of Ba2+ on the lattice strain, unit cell parameters, and cell volumes using X-ray diffraction analysis is presented.


Asunto(s)
Óxido de Aluminio , Óxido de Magnesio , Cristalografía por Rayos X , Electrónica
2.
Sci Prog ; 107(1): 368504241236026, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38490163

RESUMEN

Termites cause a serious menace to wooden structures all over the world. They rely mostly on entozoic fauna residing in their hindgut for the digestion of cellulosic and hemicellulosic materials. One of the ways to control termites is through their gut symbionts. The present study was designed to characterize the hindgut bacteria isolated from Odontotermes obesus and Heterotermes indicola. Furthermore, the growth inhibitory effect of eight tropical plant extracts was investigated to find out potential control agents for these bacterial isolates. The characterization of bacteria was carried out based on their morphology, Gram staining, biochemical and amplification of 16SrRNA gene. Amplified products were sequenced to confirm their relationship with bacterial isolates from termites of other regions. The growth inhibitory effect of ethanolic leaf extracts of eight plants was evaluated in an invitro agar well diffusion method. Qualitative and quantitative phytochemical analysis of the most effective plant was carried out to learn about bioactive agents. The results confirmed the presence of five bacteria from each termite species. The Bacillus cereus, Escherichia coli, and Lysinibacillus fusiformis were common to both termites whereas Lysinibacillus xylanilyticus and Lysinibacillus macrolides were found in O. obesus only and H. indicola harbor Bacillus subtilis and Shigella sonnei in addition to common three ones. Among the plant extracts of Carica papaya, Eucalyptus camaldulensis, Osmium basilicum, Grevillea robusta, Eucalyptus globulus, Pongamia pinnata, Mentha longifolia, and Melia azedarach, the G. robusta > E. camaldulensis > O. basilicum were found to have growth inhibitory effects with increasing concentrations from 100 to 2000 µg/mL. The biodiversity of the bacterial fauna is important for the biological control of termites. Leaf extracts of these medicinal plants can be used to control termite infestation in an environment-friendly manner to save huge economic loss.


Asunto(s)
Isópteros , Animales , Isópteros/microbiología , Bacterias/genética , Extractos Vegetales/farmacología , Biodiversidad
3.
Reprod Domest Anim ; 59(3): e14551, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38462999

RESUMEN

Cryopreservation is one of the reliable techniques for long-term storage of sperm. The success of this technique depends on the choice of cryoprotectant; therefore, a plethora of literature has reported the effects of different cryoprotective agents so far. Kappa-carrageenan (κ-carrageenan) is a hydrocolloid polysaccharide extracted from red marine seaweed. Its unique property makes it a promising option as a non-colligative cryoprotectant. The current study aims to evaluate the cryoprotective effect of k-carrageenan along with glycerol on ram sperm quality both after equilibration and freezing. Nine Kajli rams were utilized in this experiment for semen collection through an artificial vagina maintained at 42°C. Qualified samples were diluted in tris egg yolk glycerol (TEYG) extender containing different concentrations of k-carrageenan as 0 mg/mL (control), 0.2, 0.5, 0.8 and 1 mg/mL. Post-thaw assessment was done at 37°C after 24 h of storage, which showed a significant improvement (p < .05) in sperm viability, motility, membrane and acrosome integrity in an extender containing k-carrageenan at a concentration of 0.5 mg/mL compared to control. It is concluded from the current study that the combination of glycerol and 0.5 mg/mL concentration of k-carrageenan improved the sperm post-thaw quality.


Asunto(s)
Preservación de Semen , Semen , Masculino , Ovinos , Animales , Carragenina/farmacología , Glicerol/farmacología , Motilidad Espermática , Espermatozoides , Crioprotectores/farmacología , Criopreservación/veterinaria , Criopreservación/métodos , Oveja Doméstica , Preservación de Semen/veterinaria , Preservación de Semen/métodos , Suplementos Dietéticos
4.
J Ethnopharmacol ; 323: 117671, 2024 Apr 06.
Artículo en Inglés | MEDLINE | ID: mdl-38163555

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Snake bites are a critical health issue in many parts of the world particularly in Asian countries lacking efficient health facilities in rural areas. Cobra is the most common snake type in Asia and is responsible for a large number of mortalities particularly in rural areas. Plants are usually considered the most effective and easy-to-approach treatment for snake bites in rural areas of various countries. Vitex negundo L. is an important medicinal plant traditionally used to treat snake bite envenomation in many countries of Asia. AIM OF THE STUDY: From literature survey of plants traditionally used in the treatment of snake bites in Asian countries including India, Pakistan and Sri Lanka, roots of V. negundo were selected for the present study. Anti-snake venom potential of its roots was assessed through various in vitro assays targeting the phospholipase A2 enzyme. MATERIALS AND METHODS: V. negundo roots were sequentially extracted in different organic solvents to get fractions and in methanol to get total extract. The extracts were evaluated for phospholipase A2 (PLA2) inhibitory potential through inhibition of venom-induced hemolysis, ADP-induced platelet aggregation, PLA2-induced fatty acid hydrolysis and anticoagulant effect of cobra venom. Antioxidant power was determined using DPPH and superoxide radical scavenging assays. GC-MS and HPLC analysis was performed for the total methanol extract. RESULTS: Strong PLA2 inhibitory effect was observed for all the extracts. The ethyl acetate, acetone and methanol fractions significantly inhibited toxic effects of cobra venom under in vitro conditions. Radical scavenging potential of these fractions was also significantly high as compared to non-polar fractions in both DPPH and superoxide scavenging assays. Phytochemical analysis indicated high phenolic and flavonoid contents in these fractions. GC-MS and HPLC analysis of total methanol extract confirmed the presence of bis(2-ethylhexyl) phthalate, phenol, o-Guaiacol, palmitic acid-methyl ester, methyl stearate, quercetin and kaempferol in the plant. CONCLUSION: The study concluded that the roots of V. negundo, particularly their polar extracts, have strong PLA2 inhibitory effect against cobra venom confirming their traditional use to manage snake bites. The roots of this plant can be further studied for isolation of plant-based antisera.


Asunto(s)
Mordeduras de Serpientes , Vitex , Humanos , Mordeduras de Serpientes/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Extractos Vegetales/química , Metanol/uso terapéutico , Antivenenos/farmacología , Venenos Elapídicos , Fosfolipasas A2 , Fitoquímicos/farmacología , Fitoquímicos/uso terapéutico , Fosfolipasas , Pakistán
5.
Ecotoxicol Environ Saf ; 268: 115699, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37979353

RESUMEN

This study investigated the physiological and molecular responses of rice genotype '9311' to Cd stress and the mitigating effects of silicon oxide nanoparticles (SiO NPs). Cd exposure severely hindered plant growth, chlorophyll content, photosynthesis, and Cd accumulation. However, SiO NPs supplementation, particularly the SiONP100 treatment, significantly alleviated Cd-induced toxicity, mitigating the adverse effects on plant growth while maintaining chlorophyll content and photosynthetic attributes. The SiONP100 treatment also reduced Cd accumulation, indicating a preference for Si uptake in genotype 9311. Complex interactions among Cd, Si, Mg, Ca, and K were uncovered, with fluctuations in MDA and H2O2 contents. Distinct morphological changes in stomatal aperture and mesophyll cell structures were observed, including changes in starch granules, grana thylakoids, and osmophilic plastoglobuli. Moreover, following SiONP100 supplementation, genotype 9311 increased peroxidase, superoxide dismutase, and catalase activities by 56%, 44%, and 53% in shoots and 62%, 49%, and 65% in roots, respectively, indicating a robust defense mechanism against Cd stress. Notably, OsNramp5, OsHMA3, OsSOD-Cu/Zn, OsCATA, OsCATB, and OsAPX1 showed significant expression after SiO NPs treatment, suggesting potential Cd translocation within rice tissues. Overall, SiO NPs supplementation holds promise for enhancing Cd tolerance in rice plants while maintaining essential physiological functions.


Asunto(s)
Nanopartículas , Oryza , Cadmio/metabolismo , Oryza/metabolismo , Peróxido de Hidrógeno/metabolismo , Antioxidantes/farmacología , Antioxidantes/metabolismo , Clorofila/metabolismo , Raíces de Plantas/metabolismo , Plantones
6.
Plant Physiol Biochem ; 202: 107991, 2023 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-37660606

RESUMEN

High temperature (HT) stress at reproductive stage is one of most important environment negatively affecting spikelet fertility and rice yield. In this study, the effect of HT exposure on the sugar composition and carbohydrate metabolism in developing anthers and its relation to floret fertility and pollen viability were investigated by different temperature regimes under well-controlled climatic condition. Result showed that HT exposure during microspore development significantly reduced the starch deposition in developing anther and evidently disrupted the spatial distribution of sugar and starch concentrations in different compartments of rice anther, with the higher ratio of sucrose to hexose concentrations in HT-stressed anthers relative to the control ones. Under HT exposure, the amount of starch deposition in the fraction of sporophytic tissues dropped evidently, while the concentrations of sucrose and starch in anther wall tissue enhanced significantly, suggesting that HT exposure impaired the translocation of sucrose from the anther wall tissue to the sporophytic tissues inside rice anther. Furthermore, we presented possible contribution of various genes and key enzymes involving in sugar conversion and carbohydrate metabolism in developing anther to the formation of HT-induced pollen abortion by disrupting the sugar utilization in HT-stressed anther. HT exposure suppressed the activities of cell wall and vacuolar invertase, hexokinase, and ADP-glucose pyrophosphorylase in developing anther, while it was opposite for the effect of HT exposure on sucrose synthase and fructokinase. HT-induced suppression of OsCWIN3 in the anther walls might be strongly responsible for the HT-induced impairments of sugar utilization in HT-stressed anthers.


Asunto(s)
Oryza , Femenino , Embarazo , Humanos , Metabolismo de los Hidratos de Carbono , Pared Celular , Polen , Azúcares
7.
Saudi J Biol Sci ; 30(9): 103745, 2023 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-37588571

RESUMEN

Nanoparticles are beneficial in many aspects to human life but their excessive use can cause various abnormalities. They dispose in the environment through transport, industrial and agricultural usage and enter in living body through dermal, respiratory route or ingested with the lipsticks and there higher concentration produces toxicity. Therefore, current study characterized ZnO-NPs to evaluate toxic ability by X-rays diffraction (XRD) and Scanning Electron Microscopy (SEM) techniques and showed 29.83 and 35 nm size, respectively with hexagonal crystalline structure. LC50 value of ZnO-NPs was also evaluated as 72.48 ±â€¯10.33 mg/kg BW. Male Sprague Dawley (Post weaning) rats were divided into five groups with five rats in each group. Control (C) group received no treatment, placebo (S) group received normal saline (0.9% sodium chloride) intraperitoneally and three treated groups received different levels of ZnO- NPs intraperitoneally at the dose of either 10 or 20 or 30 mg/kg for 21 days on alternate days and named as 1G1, 1G2 and 1G3, respectively for the assessment of toxicity for better understanding of precautionary measures in future. Oxidative stress enzymes of liver and kidney, hepatorenal function enzymes and hematological parameters along with hepatic histology were measured at the end of the experiment. Results showed highly significant variations in all parameters in a dose dependent manner as compared to control group while groups receiving 10 or 20 mg/kg of ZnO-NPs showed low to moderate pathological changes in both organs. Liver histological analysis showed congestion, necrosis, hemorrhage, RBC's accumulations; inflammatory cells infiltration and severe abnormalities in high dose group while medium, low dose group showed moderate and least effects, respectively. It is concluded that ZnO-NPs are highly toxic at more concentration so their careful usage is needed in daily routine.

8.
Sci Rep ; 13(1): 4514, 2023 03 18.
Artículo en Inglés | MEDLINE | ID: mdl-36934168

RESUMEN

Plants provide humans with more than just food and shelter; they are also a major source of medications. The purpose of this research was to investigate the antioxidant and hypoglycemic potential of green synthesized CeONPs using Mentha royleana leaves extract. The morphological and physicochemical features of CeONPs were evaluated by UV-Visible spectrophotometry, Scanning Electron Microscopy, Energy Dispersive X-rays and Fourier-transform infrared spectrometry, Dynamic light scattering, Atomic Force Microscopy, Zeta Potential. The average size range of synthesized CeONPs diameter between 46 and 56 nm, crystalline in shape, with Polydispersity index value of 0.2 and subatomic particles mean diameter was 4.5-9.1 nm. The antioxidant capability of CeONPs was assessed using DPPH, ABTS+, hydrogen peroxide, hydroxyl radical scavenging, and reducing power tests. The hypoglycemic potential of CeONPs was investigated using alpha-amylase, alpha-glucosidase, glucose absorption by yeast cells, and antisucrase. The effective concentrations were 500 and 1000 µg/ml found good in suppressing radical species. To explore the hypoglycemic potential of CeONPs, alpha-amylase, alpha-glucosidase, glucose absorption by yeast cell, and antisucrase assays were performed. Glucose absorb by yeast cells assay was tested for three distinct glucose concentrations: 5 mmol/L, 10 mmol/L, and 25 mmol/L. Green synthesize CeONPs showed a dose-dependent response, higher concentrations of CeONPs imposed a stronger inhibitory impact on the catalytic site of enzymes. This study suggest that CeONPs could possibly binds to the charge carrying species and act as competitive inhibitor which slow down the enzyme substrate reaction and prevents enzymatic degradation. The study's findings were outstanding, which bodes well for future medicinal applications of CeONPs.


Asunto(s)
Cerio , Nanopartículas del Metal , alfa-Glucosidasas , Antioxidantes/farmacología , Cerio/química , Glucosa , Hipoglucemiantes/farmacología , Hipoglucemiantes/química , Nanopartículas del Metal/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Saccharomyces cerevisiae
9.
Plant Cell Environ ; 46(5): 1453-1471, 2023 05.
Artículo en Inglés | MEDLINE | ID: mdl-36691352

RESUMEN

High temperatures (HT) cause pollen abortion and poor floret fertility in rice, which is closely associated with excessive accumulation of reactive oxygen species (ROS) in the developing anthers. However, the relationships between accumulation of abscisic acid (ABA) and ROS, and their effects on tapetum-specific programmed cell death (PCD) in HT-stressed anthers are poorly characterised. Here, we determined the spatiotemporal changes in ABA and ROS levels, and their relationships with tapetal PCD under HT exposure. Mutants lacking ABA-activated protein kinase 2 (SAPK2) functions and exogenous ABA treatments were used to explore the effects of ABA signalling on the induction of PCD and ROS accumulation during pollen development. HT-induced pollen abortion was tightly associated with ABA accumulation and oxidative stress. The higher ABA level in HT-stressed anthers resulted in the earlier initiation of PCD induction and subsequently abnormal tapetum degeneration by activating ROS accumulation in developing anthers. Interactions between SAPK2 and DEAD-box ATP-dependent RNA helicase elF4A-1 (RH4) were required for ABA-induced ROS generation in developing anthers. The OsSAPK2 knockout mutants showed the impaired PCD responses in the absence of HT. However, the deficiency of SAPK2 functions did not suppress the ABA-mediated ROS generation in HT-stressed anthers.


Asunto(s)
Oryza , Especies Reactivas de Oxígeno/metabolismo , Oryza/fisiología , Ácido Abscísico/farmacología , Ácido Abscísico/metabolismo , Proteína Quinasa 11 Activada por Mitógenos/genética , Proteína Quinasa 11 Activada por Mitógenos/metabolismo , Polen/fisiología , Apoptosis/genética , Respuesta al Choque Térmico , Regulación de la Expresión Génica de las Plantas
10.
3 Biotech ; 11(11): 469, 2021 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-34745820

RESUMEN

Dry tubers of Pinellia ternata (Thunb.) Breit are used in traditional Chinese medicine. Commonly known as "banxia" in China, the tubers contain valuable compounds, including alkaloids and polysaccharides that are widely used in pharmaceuticals. The quantity and quality of these important compounds are affected by whether P. ternata is grown as a sole crop or as an intercrop, and P. ternata cultivation has become challenging in recent years. By intercropping P. ternata, its maximum yield, as well as large numbers of chemical components, can be realized. Here, a large data set derived from next-generation sequencing was used to compare changes in the bacterial communities in rhizosphere soils of P. ternata and maize grown as sole crops and as intercrops. The overall microbial population in the rhizosphere of intercropped P. ternata was significantly larger than that of sole-cropped P. ternata, whereas the numbers of distinct microbial genera, ranging from 552 to 559 among treatments, were not significantly different between the two rhizospheres. The relative abundances of the genera differed. Specifically, the numbers of Acidobacteria and Anaerolineaceae species were significantly greater, and those of Bacillus were significantly lower, in the intercropped P. ternata rhizosphere than in the sole-cropped rhizosphere. SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at 10.1007/s13205-021-03011-3.

11.
Pak J Pharm Sci ; 34(1(Special)): 387-395, 2021 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-34275784

RESUMEN

The current study assessed the ameliorative effect of Trigonella foenum graceum extract against copper oxide nanoparticles (CuO-NPs) induced toxicity in Oreochromis mossambicus. For this purpose 100 healthy fish weighing 20±2.34g were randomly divided into five different groups in duplicates and designated as control (C) no treatment, positive control (G*) treated with 0.12mg/L of CuO-NPs, experimental co-treated groups G1, G2 and G3 were treated with Trigonella foenum-graecum extract @ 18, 26 and 52mg/L along with 0.12 mg/L of CuO-NPs, respectively. In this study significant (P<0.05) changes were observed in the antioxidant activity of enzymes and histological alterations in the liver and intestine of fish in G*, G1 and G2 groups while a good ameliorative response of Trigonella foenum-graecum was observed in G3. Dose dependent alterations in glutathione, lipid peroxides, catalase, and malondialdehyde as well as histological architecture of liver and intestine were observed in treated groups, where more alterations were observed in positive control and low dose treated groups of Trigonella foenum-graecum. Moreover, more ameliorative effect was observed in high dose of Trigonella foenum-graecum treated group (G3). This study is novel as no previous data is available on the amelioration of Trigonella foenum-graecum extract against CuO-NPs induced toxicity in fish.


Asunto(s)
Cobre/toxicidad , Intestinos/efectos de los fármacos , Hígado/efectos de los fármacos , Nanopartículas del Metal/toxicidad , Extractos Vegetales/farmacología , Trigonella , Animales , Antioxidantes/metabolismo , Catalasa/efectos de los fármacos , Catalasa/metabolismo , Glutatión/efectos de los fármacos , Glutatión/metabolismo , Intestinos/enzimología , Intestinos/patología , Peroxidación de Lípido/efectos de los fármacos , Hígado/enzimología , Hígado/patología , Malondialdehído/metabolismo , Distribución Aleatoria , Tilapia
12.
Turk J Pharm Sci ; 18(3): 319-325, 2021 06 18.
Artículo en Inglés | MEDLINE | ID: mdl-34157821

RESUMEN

Objectives: Many agents, including those from herbal sources, have been sought as preventives or cures for hepatotoxicity. The pollen of Pinus brutia Ten., known as red pine (Pinaceae), is used against liver diseases in Anatolian folk medicine. Materials and Methods: In the current study, pollen ethanol extract of P. brutia was investigated for its possible hepatoprotective activity using a mouse model of CCl4-induced hepatotoxicity. Swiss albino mice were divided into five groups, and extract-treated groups were compared with a silymarin-treated group as the reference. The extract was tested at 100, 200, and 300 mg/kg (b.w.). Phenolic acids were analyzed using high-performance column chromatography (HPLC) in the extracts as pollens are usually known to be rich in phenolics. Results: Our data revealed that the extract displayed the best hepatoprotection at a dose of 100 mg/kg when compared with silymarin (Legalon®), the reference drug. HPLC analysis indicated presence of protocatechuic acid (0.176 mg/g extract), p-hydroxybenzoic acid (0.001 mg/g extract), vanillic acid (VA) (0.537 mg/g extract), syringic acid (0.050 mg/g extract), and tr-cinnamic acid (0.310 mg/g extract), while the major phenolic acid was VA. Conclusion: The outcomes of this study allow us to conclude that red pine pollen extract can serve as a promising hepatoprotective agent. Among the phenolic acids analyzed in the pollen extract, vanillic acid as the major one besides some other phenolic acids detected seems to be responsible for its remarkable hepatoprotective effect.

13.
Biomed Res Int ; 2021: 6618349, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33816618

RESUMEN

Snakebite is one of the most neglected diseases of developing countries. Deaths due to snakebite envenoming are quite high in Pakistan, and many deaths are caused by Echis carinatus envenomation. Traditional use of medicinal plants against snakebites is a common practice in Pakistan due to countless benefits. The current study was performed with the objective to evaluate eighteen Pakistani medicinal plants inhibitory potential against hyaluronidase and alkaline phosphatase enzymes of Pakistani Echis carinatus venom. Hyaluronidase activity (0.2-1.6 mg/0.1 mL) and alkaline phosphatase activity (0.1-0.8 mg/0.1 mL) were measured in dose-dependent manner. Crude methanolic extracts of medicinal plants were used for in vitro investigation of their inhibitory activity against toxic enzymes. All active plants were fractioned using different solvents and were again analyzed for inhibitory activity of same enzymes. Results indicated all plants were able to neutralize hyaluronidase that Swertia chirayita (Roxb. ex Flem.) Karst., Terminalia arjuna Wight and Arn, Rubia cordifolia Thumb., and Matthiola incana (L.) R.Br. inhibited maximum hyaluronidase activity equivalent to standard reference (p > 0.5). Pakistani medicinal plants are dense with natural neutralizing metabolites and other active phytochemicals which could inhibit hyaluronidase activity of Pakistani Echis carinatus venom. Further advanced studies at molecular level could lead us to an alternative for envenoming of Pakistani Echis carinatus venom.


Asunto(s)
Fosfatasa Alcalina , Hialuronoglucosaminidasa , Extractos Vegetales/química , Plantas Medicinales/química , Proteínas de Reptiles , Venenos de Víboras/enzimología , Viperidae , Fosfatasa Alcalina/antagonistas & inhibidores , Fosfatasa Alcalina/química , Animales , Hialuronoglucosaminidasa/antagonistas & inhibidores , Hialuronoglucosaminidasa/química , Proteínas de Reptiles/antagonistas & inhibidores , Proteínas de Reptiles/química
14.
Biomed Res Int ; 2021: 6685806, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33816628

RESUMEN

Carbamazepine (CBZ) is an antiepileptic drug having low bioavailability due to its hydrophobic nature. In the current study, efforts are made to investigate the effect of dicarboxylic acid coformer spacer groups (aliphatic chain length) on physicochemical properties, relative humidity (RH) stability, and oral bioavailability of CBZ cocrystals. Slurry crystallization technique was employed for the preparation of CBZ cocrystals with the following coformers: adipic (AA), glutaric (GA), succinic (SA), and malonic acid (MA). Powder X-ray diffractometry and Fourier-transform infrared spectroscopy confirmed cocrystal preparation. Physicochemical properties, RH stability, and oral bioavailability of cocrystals were investigated. Among the prepared cocrystals, CBZ-GA showed maximum solubility as well as improved dissolution profile (CBZ-GA > CBZ-MA > CBZ-AA > pure CBZ > CBZ-SA) in ethanol. Maximum RH stability was shown by CBZ-AA, CBZ-SA, and CBZ-MA. In vivo studies confirmed boosted oral bioavailability of cocrystals compared to pure CBZ. Furthermore, in vivo studies depicted the oral bioavailability order of cocrystals as CBZ-GA > CBZ-MA > Tegral® > CBZ-AA > CBZ-SA > pure CBZ. Thus, pharmaceutical scientists can effectively employ cocrystallization technique for tuning physicochemical properties of hydrophobic drugs to achieve the desired oral bioavailability. Overall, results reflect no consistent effect of spacer group on physicochemical properties, RH stability, and oral bioavailability of cocrystals.


Asunto(s)
Carbamazepina , Animales , Disponibilidad Biológica , Rastreo Diferencial de Calorimetría , Carbamazepina/química , Carbamazepina/farmacocinética , Carbamazepina/farmacología , Cristalización , Evaluación Preclínica de Medicamentos , Estabilidad de Medicamentos , Conejos
15.
Curr Drug Deliv ; 18(7): 922-934, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33726649

RESUMEN

BACKGROUND: Bistorta amplexicaulis of the genus Polygonum (Polygonaceae) has been reported for its antioxidant and anticancer activities. However, the low cellular uptake of the compounds in its extract limits its therapeutic application. OBJECTIVES: The present study aimed at developing a nanoliposomal carrier system for B. amplexicaulis extracts for improved cellular uptake, thus resulting in enhanced anticancer activity. METHODS: Ultra Pressure Liquid Chromatography (UPLC) was used to identify major compounds in the plant extract. Nanoliposomes (NLs) were prepared by employing a thin-film rehydration method using DPPC, PEG2000DSPE and cholesterol, followed by characterization through several parameters. In vitro screening was performed against breast cancer cell line (MCF-7) and Hepatocellular carcinoma cell line (HepG-2) using MTT-assay. Raw extract and nanoliposomes were tested on Human Umbilical Vein Endothelial Cells (HUVEC). Moreover, molecular docking was performed to validate the data obtained through wet lab. RESULTS: The UHPLC method identified gallic acid, caffeic acid, chlorogenic acid and catechin as the major compounds in the extract. The NLs with a size ranging between 140-155 nm, zeta potential -16.9 to -19.8 mV and good polydispersity index of < 0.1 were prepared, with a high encapsulation efficiency of 81%. The MTT assay showed significantly (p > 0.05) high uptake and cytotoxicity of NLs as compared to the plant extract. Moreover, reduced toxicity against HUVEC cells was observed as compared to the extract. Also, the docking of identified compounds suggested a favorable interaction with the SH2 domain of both STAT3 and STAT5. CONCLUSION: Overall, the results suggest NLs as a potential platform that could be developed for the improved intracellular delivery of plant extract, thus increasing the therapeutic outcomes.


Asunto(s)
Carcinoma Hepatocelular , Polygonaceae , Carcinoma Hepatocelular/tratamiento farmacológico , Células Endoteliales , Humanos , Liposomas , Células MCF-7 , Simulación del Acoplamiento Molecular , Extractos Vegetales/farmacología
16.
Biomed Res Int ; 2021: 6631042, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33614782

RESUMEN

Echis carinatus is one of the highly venomous snakes of Pakistan that is responsible for numerous cases of envenomation and deaths. In Pakistan, medicinal plants are commonly used traditionally for snakebite treatment because of their low cost and easy availability in comparison with antivenom. The current research is aimed at evaluating the inhibitory activity of Pakistani medicinal plants against acetylcholinesterase and 5'-nucleotidases present in Echis carinatus venom. Acetylcholinesterase and 5'-nucleotidase enzymatic assays were performed at different venom concentrations to check the activity of these enzymes. Methanolic extracts from different parts of plants were used for in vitro determination of their inhibitory activity against 5'-nucleotidases in snake venom. Active methanolic extracts were subsequently fractioned using different solvents, and these fractions were also assessed for their anti-5'-nucleotidase activity. Results of this study exhibited that Eugenia jambolana Willd. ex O. Berg, Rubia cordifolia L., Trichodesma indicum (L.) R. Br., Calotropis procera (Wild.) R. Br., Curcuma longa L., and Fagonia arabica L. were able to significantly (p > 0.5) neutralize the 5'-nucleotidase activity by 88%, 86%, 86%, 85%, 83.7%, and 83%, respectively, compared with a standard antidote (snake venom antiserum). Thus, this study indicates that these plants possess the potential to neutralize one of the toxic enzymatic components of Echis carinatus venom and hence can help to augment the future efforts of developing alternative therapy for the management of snakebites.


Asunto(s)
5'-Nucleotidasa/antagonistas & inhibidores , Inhibidores de la Colinesterasa/farmacología , Extractos Vegetales/farmacología , Plantas Medicinales/química , Venenos de Víboras/antagonistas & inhibidores , Pakistán , Fitoquímicos/análisis , Fitoquímicos/química , Extractos Vegetales/química
17.
Phytother Res ; 34(12): 3089-3112, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32478964

RESUMEN

Alzheimer's disease (AD) is clinically characterized as memory deficits, altered behavior and impaired cognitive functions. The most important risk factor for AD is aging and mounting. Evidences suggested in different studies that traditionally used plants in Asia, China, and Europe significantly affect aging and AD involved neurodegeneration pathways. Research into ethnobotanicals for impaired memory and cognition has been burgeoned in last decades. The inclusion and exclusion criteria for the plant selection were based on reputed herbs recommended for treatment of neurological disorders and their scientific validation to cure neurodegenerative disorders. A range of traditional plants imparts effects via acetylcholinesterase activity, ß-amyloid peptide formation in plaques, neurotrophic factors and through antioxidant activity. On one side preclinical investigations identified promising drug candidates for AD, on the other side, clinical evidences are still pending. Presently, according to WHO, around more than 80% world population relay on natural remedies to cure their health related issues. Plants contain rich source of primary and secondary metabolites for improving health problems. Pharmaceutical industry is facing intriguing challenges like elevated cost and unendurable risk management due to the high burden of neurodegenerative disorders. A significant shift of drug discovery is being witnessed from synthetic moieties to herbal formulation.


Asunto(s)
Desarrollo de Medicamentos , Medicina Tradicional , Enfermedades Neurodegenerativas/tratamiento farmacológico , Plantas Medicinales , Envejecimiento/efectos de los fármacos , Envejecimiento/fisiología , Enfermedad de Alzheimer/tratamiento farmacológico , Enfermedad de Alzheimer/epidemiología , Antioxidantes/uso terapéutico , Asia/epidemiología , China/epidemiología , Cognición/efectos de los fármacos , Desarrollo de Medicamentos/métodos , Desarrollo de Medicamentos/tendencias , Europa (Continente)/epidemiología , Humanos , Medicina Tradicional/métodos , Medicina Tradicional/tendencias , Enfermedades Neurodegenerativas/epidemiología , Fitoterapia/métodos , Fitoterapia/tendencias
18.
Biomed Res Int ; 2020: 2096947, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32566667

RESUMEN

The objective of this study was to authenticate the ethnobotanical claims of the Nepeta ruderalis Buch.-Ham. (N. ruderalis) extract in the traditional system of medicine. Crude extract was prepared via a simple maceration process. DPPH free radical scavenging and carrageenan-induced rat paw edema models were used to monitor antioxidant and anti-inflammatory responses of the N. ruderalis extract. Furthermore, it was tested for antiplatelet aggregation, cardioprotective, and calcium channel antagonistic activities via standard documented protocols. The N. ruderalis extract exhibited 80.82% antioxidant activity (IC50 = 207.51 ± 4.36 µg) while the anti-inflammatory response was significant (p < 0.05 to p < 0.01) at 50 mg/kg (45.58%) and 100 mg/kg (60.90%) doses. Moreover, it was found to inhibit platelet aggregation (IC50 = 1.06 and 0.91 mg/mL) and, in addition, to increase the force of contraction at the concentration of 3.0-10 mg/mL with a decrease in the heart rate on isolated paired atria (EC50 = 11.78 mg/mL). Relaxant activity was observed on the isolated rabbit jejunum (EC50 = 0.96 mg/mL) and trachea (EC50 = 0.89 mg/mL). However, in a cumulative way, an 80-millimolar potassium-induced contraction was evaluated (EC50 = 1.31 mg/mL). The N. ruderalis extract exhibited antioxidant, anti-inflammatory, platelet aggregating, cardiotonic, and calcium channel antagonistic activities, therefore proving scientifically its effectiveness in the traditional system of medicine.


Asunto(s)
Antiinflamatorios/farmacología , Antioxidantes/farmacología , Fármacos Cardiovasculares/farmacología , Nepeta/química , Extractos Vegetales/farmacología , Animales , Compuestos de Bifenilo/metabolismo , Edema/patología , Atrios Cardíacos/efectos de los fármacos , Frecuencia Cardíaca/efectos de los fármacos , Yeyuno/efectos de los fármacos , Picratos/metabolismo , Inhibidores de Agregación Plaquetaria/farmacología , Conejos , Ratas , Tráquea/efectos de los fármacos
19.
Pak J Pharm Sci ; 33(2): 531-535, 2020 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-32276894

RESUMEN

Various extrinsic and intrinsic origins slant skins and pledge evident vicissitudes of the skin surface. We explored the effects of dermocosmetic loaded medical Cannabis seed extract and evaluate the improvement on the skin surface in Asian and male volunteers in a split face topographic study. Dermocosmetic and base (without extract) fabricated were directed to apply by volunteers (Asian male) on their right and left cheek, respectively, in the split face skin topographic study up to three months. Efficacy of dermocosmetic versus base was assessed by non- invasive diagnostic technique focusing on skin texture parameters (energy, contrast and variance) and surface evaluation of the living skin (SELS), SEr (skin roughness), SEsc (skin scaliness), SEsm (skin smoothness), SEw (skin wrinkles). Unlike base, dermocosmetic showed significant effects on skin texture parameters (energy, variance and contrast) and SELS (SEr, SEsc, SEsm and SEw) parameters in Asian male volunteers when ANOVA applied. The level of significance was 5%. Dermocosmetic ultimately improved on skin surface and advocacies for anti-aging effects on skin appearance.


Asunto(s)
Cannabis , Cosméticos/administración & dosificación , Fármacos Dermatológicos/administración & dosificación , Extractos Vegetales/administración & dosificación , Envejecimiento de la Piel/efectos de los fármacos , Piel/efectos de los fármacos , Administración Tópica , Adulto , Cosméticos/aislamiento & purificación , Fármacos Dermatológicos/aislamiento & purificación , Humanos , Masculino , Extractos Vegetales/aislamiento & purificación , Semillas , Envejecimiento de la Piel/fisiología , Adulto Joven
20.
IET Nanobiotechnol ; 14(1): 33-39, 2020 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-31935675

RESUMEN

Magnetic manotheranostics can be a fascinating charm to diagnose a tumour with MRI, and treatment through hyperthermia. This study aims to synthesise and characterise magnetically responsive polymer colloids (MRPCs). Healthy tissue damage done by chemotherapy session could be minimised by MRPCs. For the colloidal formulation of MRPCs, the oil in water emulsion technique was employed with the aid of sonication and stirring. The organic phase of emulsion contained methotrexate (MTX) drug, Eudragit E100 and CoFe2O4 (synthesised by co-precipitation) in ethanol, and the aqueous phase contained tween 80 in deionised water. The emulsion was optimised by studying/adjusting two different parameters, i.e. the concentration of constituents and sonication cycles. Multiple formulations were produced at sonication amplitude of 60% at 20 kHz, followed by centrifugation and lyophilisation. Characterisation of MRPCs was done for morphology, size measurement (23-25 nm), surface charge (∼15.12), coercivity (∼1549.6 G), magnetisation (2.6 emu) and retentivity (1.34 emu). Drug release in simulating physiological environment (pH = 7.4), was observed for up to 48 h, and, to determine the best release kinetic mechanism results were compared with kinetic models. Magnetic hyperthermia studies showed that MRPCs achieved an acceptable temperature of 42°C, for hyperthermia treatments in cancer patients.


Asunto(s)
Cobalto/química , Coloides/química , Composición de Medicamentos/métodos , Compuestos Férricos/química , Metotrexato/química , Acrilatos/química , Hipertermia Inducida , Nanopartículas de Magnetita/química , Metotrexato/farmacocinética , Tamaño de la Partícula , Polímeros/química
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