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1.
Molecules ; 27(18)2022 Sep 09.
Artículo en Inglés | MEDLINE | ID: mdl-36144585

RESUMEN

This work was undertaken to explore the phytochemical composition, antioxidant, and enzyme-inhibiting properties of Neurada procumbens L. extracts/fractions of varying polarity (methanol extract and its fractions including n-hexane, chloroform, n-butanol, and aqueous fractions). A preliminary phytochemical study of all extracts/fractions, HPLC-PDA polyphenolic quantification, and GC-MS analysis of the n-hexane fraction were used to identify the phytochemical makeup. Antioxidant (DPPH), enzyme inhibition (against xanthine oxidase, carbonic anhydrase, and urease enzymes), and antibacterial activities against seven bacterial strains were performed for biological investigation. The GC-MS analysis revealed the tentative identification of 22 distinct phytochemicals in the n-hexane fraction, the majority of which belonged to the phenol, flavonoid, sesquiterpenoid, terpene, fatty acid, sterol, and triterpenoid classes of secondary metabolites. HPLC-PDA analysis quantified syringic acid, 3-OH benzoic acid, t-ferullic acid, naringin, and epicatechin in a significant amount. All of the studied extracts/fractions displayed significant antioxidant capability, with methanol extract exhibiting the highest radical-scavenging activity, as measured by an inhibitory percentage of 81.4 ± 0.7 and an IC50 value of 1.3 ± 0.3. For enzyme inhibition experiments, the n-hexane fraction was shown to be highly potent against xanthine oxidase and urease enzymes, with respective IC50 values of 2.3 ± 0.5 and 1.1 ± 0.4 mg/mL. Similarly, the methanol extract demonstrated the strongest activity against the carbonic anhydrase enzyme, with an IC50 value of 2.2 ± 0.4 mg/mL. Moreover, all the studied extracts/fractions presented moderate antibacterial potential against seven bacterial strains. Molecular docking of the five molecules ß-amyrin, campesterol, ergosta-4,6,22-trien-3ß-ol, stigmasterol, and caryophyllene revealed the interaction of these ligands with the investigated enzyme (xanthine oxidase). The results of the present study suggested that the N. procumbens plant may be evaluated as a possible source of bioactive compounds with multifunctional therapeutic applications.


Asunto(s)
Anhidrasas Carbónicas , Catequina , Plantas Medicinales , Triterpenos , 1-Butanol , Antibacterianos/farmacología , Antioxidantes/química , Ácido Benzoico , Cloroformo , Ácidos Grasos , Flavonoides/análisis , Flavonoides/farmacología , Hexanos , Ligandos , Metabolómica , Metanol/química , Simulación del Acoplamiento Molecular , Fenoles/análisis , Fitoquímicos/análisis , Fitoquímicos/farmacología , Extractos Vegetales/química , Plantas Medicinales/metabolismo , Estigmasterol , Terpenos , Trientina , Ureasa , Xantina Oxidasa
2.
Biomed Res Int ; 2022: 1662194, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35372569

RESUMEN

The study was aimed at designing and characterizing the ondansetron hydrochloride (OND) bearing agarose (AG), and hydroxypropyl methyl cellulose (HPMC) mucoadhesive buccal films employing glycerol as a plasticizer. The buccal delivery of ondansetron hydrochloride was remarkably boosted by employing physical (iontophoresis) and chemical enhancement approaches (chemical penetration enhancers). To explore the influence of different formulation components, i.e., agarose, hydroxypropyl methyl cellulose (HPMC), and glycerol on various evaluating parameters, i.e., tensile strength, swelling index, ex vivo mucoadhesion time, and subsequently on in vitro drug release, a D-optimal design was opted. A buccal film bearing OND was mounted on bovine buccal mucosa for ex vivo permeation studies and impact of chemical and physical enhancement techniques on the permeation profile was also analysed. A linear release profile was revealed in in vitro drug release of OND over 60 minutes and outcomes ascertained the direct relationship between HPMC content and in vitro drug release and inverse relationship was depicted by AG content. The FTIR and DSC thermal analysis was executed to determine the physicochemical interactions and results exposed no chemical interactions between drug and polymers. The drug (OND) appeared as tiny crystals on smooth film surface during scanning electron microscopy (SEM) analysis. A notable enhancement in permeation flux, i.e., 761.02 µg/min of OND during ex vivo permeation studies was witnessed after the application of current (0.5-1 mA) without any time lag and with enhancement ratio of 3.107. A time lag of 15 minutes, 19 minutes, and 26 minutes with permeation flux of 475.34 µg/min, 399.35 µg/min, and 244.81 µg/min was observed after chemical enhancer pretreatment with propylene glycol, Tween 80, and passive, respectively. Rabbit was employed as the experimental animal for pharmacokinetic studies (in vivo) and cats for pharmacological activity (in vivo), and the results illustrated the enhanced bioavailablity (2.88 times) in the iontophoresis animal group when compared with the rabbits of control group. Likewise, a remarkable reduction in emesis events was recorded in cats of iontophoresis group. Conclusively, the histopathological examinations on excised buccal mucosa unveiled no severe necrotic or cytopathetic outcomes of current.


Asunto(s)
Iontoforesis , Ondansetrón , Animales , Gatos , Bovinos , Sistemas de Liberación de Medicamentos/métodos , Glicerol , Derivados de la Hipromelosa/química , Metilcelulosa , Mucosa Bucal , Ondansetrón/farmacología , Conejos , Sefarosa
3.
J Pak Med Assoc ; 71(Suppl 7)(11): S12-S19, 2021 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-34793424

RESUMEN

Investing in voluntary family planning services and commodities is a cost-effective intervention for socio-economic development. Every dollar spent on family planning results in reductions in child and maternal deaths, returns in savings in other development areas, and environmental benefits. Investments in family planning yield demonstrated social and economic returns in all sectors - food, water, health, and economic development. Our analysis suggests that achieving universal access to contraception could contribute in the long term to achieving some of the Sustainable Development Goals (SDGs). We applied the Family Planning-Sustainable Development Goals (FP-SDGs) Model that quantifies the benefits voluntary contraceptive use offers for realizing 13 of the SDG indicators which are related to 7 out of the 17 SDGs Goals. The model unravelling the multi-sectoral benefits of contraceptive use and shows that family planning can accelerate progress across the 7 SDG. Further, it shows that family planning does not only empower women to choose the number, timing, and spacing of their pregnancies but also touches on many multisectoral determinants vital to sustainable development. We show that in the case of Pakistan, without universal access to family planning and reproductive health, the impact and effectiveness of other interventions will be less, will cost more, and will take longer to achieve. In the end, we put some key recommendations to prioritize family planning as one of the strategic national development investments.


Asunto(s)
Servicios de Planificación Familiar , Desarrollo Sostenible , Niño , Anticoncepción , Femenino , Objetivos , Humanos , Pakistán , Embarazo
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