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1.
Pak J Pharm Sci ; 35(6(Special)): 1755-1760, 2022 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-36861239

RESUMEN

The present study was aimed to investigate the comparative antidiabetic potential of Nigella sativa seed extract and oil in an in vivo trial using rat animal model. The levels of antioxidants analysed in this study included catalase, vitamin C and bilirubin. NS methanolic extract and its oil were tested for their hypoglycemic effect against alloxanized diabetic rabbits (120mg/kg). The crude methanolic extract and the oil (2.5ml/kg/day) were given orally for 24 days that resulted in a significant reduction in glycaemia, particularly during the first 12 days of treatment (reductions of 58.09% and 73.27%, respectively), whereas the oil treated group normalised the levels of catalase (-69.23%), vitamin C (27.30%) and bilirubin (-51.48%) and the extract treated group normalised the levels of catalase (-65.38), vitamin C (24.15%) and bilirubin (-26.19%) at the end of the trial. The results have shown that the seed oil more significantly normalized the levels of serum catalase, serum ascorbic acid and total serum bilirubin as compared to the methanolic extract of Nigella sativa, so Nigella sativa seed oil (NSO) may be used as part of antidiabetic remedies against diabetes and utilized as a nutraceutical.


Asunto(s)
Diabetes Mellitus , Nigella sativa , Conejos , Animales , Ratas , Hipoglucemiantes/farmacología , Antioxidantes/farmacología , Catalasa , Ácido Ascórbico/farmacología , Vitaminas , Bilirrubina , Metanol , Extractos Vegetales/farmacología
2.
Pak J Pharm Sci ; 33(3): 987-995, 2020 May.
Artículo en Inglés | MEDLINE | ID: mdl-33191222

RESUMEN

Following the Claisen Schmidt condensation a series of chalcone, their allylidene derivatives and metallic complexes were produced and subsequently screened for antibacterial assay. The precursors were simple acetophenone and different substituted aryl benzaldehydes; which were made to react in basic ethanolic conditions. The structure of synthesized targets was established by IR, 1H-NMR and EIMS data. The antibacterial statistics showed that most of the bacterial strains particularly S. typhi and E. coli were potently inhibited by majority of the compounds like 3c, 5c, 7a & 7c. This structure activity relationship studies showed that these molecules possessed p-methoxy substituents in their framework and found active in rupturing the cell wall. These molecules might serve as potential drug candidates for future drug discovery and design. The presented manuscript highlights the pharmacological diversity of chalcones holding allylidene moiety and Zn+2 complexes.


Asunto(s)
Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Chalcona/farmacología , Chalconas/farmacología , Antibacterianos/síntesis química , Bacterias/crecimiento & desarrollo , Chalcona/análogos & derivados , Chalcona/síntesis química , Chalconas/síntesis química , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Relación Estructura-Actividad
3.
Pak J Pharm Sci ; 32(1): 205-212, 2019 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-30772810

RESUMEN

Synthetic drugs are associated with adverse side-effects and rapid increase in resistance to most of them inspires to evaluate plants for their therapeutic values. We have been aimed to suggest the medicinal use of Nigella sativa seed aqueous extract to minimize the severity of liver damage via its antioxidant properties and its role in maintenance of cell ion-homeostasis. Annoyances in serum levels of some antioxidants and trace metals in human hepatitis C infected patients were compared with that from acetaminophen-induced hepatotoxic rabbits. Serum analysis of human patients and that of hepatotoxic rabbits have exhibited the same trend of incidence of liver marker enzymes, antioxidant levels, and trace metal concentrations, except for the serum levels of cobalt. Significance of pre-/ or post-treatment of Nigella sativa to acetaminophen induced-hepatotoxic rabbit has also evaluated. NS post-treatment to rabbits has been found effective in normalizing the levels (P<0.001) of serum liver markers; especially the ALP levels, and the antioxidants; with significant effect on the serum catalase levels. However, NS pre-treatment has shown its role (P<0.001) in maintaining the serum nickel and cobalt concentrations. Therefore, we suggest the use of Nigella sativa seeds as pre-/ or post-treatment therapy, and also as supplement to the normal medications of liver infection to normalize the status of cell antioxidants and trace metal concentrations.


Asunto(s)
Antioxidantes/farmacología , Enfermedad Hepática Inducida por Sustancias y Drogas/prevención & control , Hígado/efectos de los fármacos , Nigella sativa , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/farmacología , Acetaminofén , Adulto , Anciano , Animales , Antioxidantes/aislamiento & purificación , Biomarcadores/sangre , Estudios de Casos y Controles , Enfermedad Hepática Inducida por Sustancias y Drogas/sangre , Enfermedad Hepática Inducida por Sustancias y Drogas/patología , Citoprotección , Modelos Animales de Enfermedad , Femenino , Hepatitis C Crónica/sangre , Hepatitis C Crónica/diagnóstico , Hepatitis C Crónica/virología , Humanos , Hígado/metabolismo , Hígado/patología , Masculino , Metales/sangre , Persona de Mediana Edad , Nigella sativa/química , Extractos Vegetales/aislamiento & purificación , Conejos , Semillas , Oligoelementos/sangre , Adulto Joven
4.
Pak J Pharm Sci ; 30(5): 1679-1690, 2017 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-29084690

RESUMEN

Dengue infection is rapidly spreading in most of the countries of south Asia. It is of utmost importance to explore the plants with "anti-thrombocytopenic activity" the dreadful response of dengue fever. The present study was conducted to investigate the potential of aqueous extract of Nigella sativa (black cumin) seeds in alleviating the severity of dengue disease by raising the platelet count (PLT). Serum samples of thirty patients with dengue hemorrhagic fever (DHF) were analysed for different biochemical parameters. When compared with control groups, the patients were found with very low PLT count (7.62 fold), reduced antioxidant levels; catalase (1.4 fold), ascorbic acid (1.1 fold), bilirubin (1.06 fold), and severe deficiency of micronutrient concentrations; cobalt (2.27 fold), iron (2.35 fold) and nickel (71.46 fold). Similar parameters were studied in albino rats to observe the changes in serum levels of biochemical markers, after administration of single dose of choloroquine phosphate (IM, 1.5 mL saline). The drug successfully induced thrombocytopenia along with significant decrease in levels of antioxidants and trace metals. Administration of N. sativa aqueous seed extract (15.25 mg/kg/bw) for 12 days resulted in an increase in PLT count (1.59 fold) as compared to control group. N. sativa post-treatment was found effective in elevating the serum levels of catalase, ascorbic acid, and bilirubin (1.06, 1.58 and 0.4 folds respectively). However, the N. sativa pre-treatment was useful in increasing the levels of micronutrients; iron, nickel and cobalt when compared to quinine-induced group. From the above findings it was suggested that N. sativa seed aqueous extract supplementation would be a promising solution for declined PLT count and associated consequences.


Asunto(s)
Antioxidantes/farmacología , Plaquetas/efectos de los fármacos , Cloroquina/análogos & derivados , Nigella sativa/química , Extractos Vegetales/farmacología , Semillas/química , Trombocitopenia/tratamiento farmacológico , Adolescente , Adulto , Animales , Antioxidantes/aislamiento & purificación , Estudios de Casos y Controles , Modelos Animales de Enfermedad , Femenino , Humanos , Masculino , Persona de Mediana Edad , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/aislamiento & purificación , Recuento de Plaquetas , Ratas , Dengue Grave/sangre , Dengue Grave/diagnóstico , Trombocitopenia/sangre , Trombocitopenia/inducido químicamente , Factores de Tiempo , Oligoelementos/sangre , Adulto Joven
5.
ACS Omega ; 8(24): 21642-21652, 2023 Jun 20.
Artículo en Inglés | MEDLINE | ID: mdl-37360421

RESUMEN

The current study focused on the antioxidant potential, α-amylase inhibitory activity, and hypoglycemic, hypolipidemic, and histoprotective (pancreas and kidney) effects of polyherbal emulsion on the alloxan-induced diabetic rats. Polyherbal formulations were prepared from extracts and oils of Nigella sativa (N. sativa), Citrullus colocynthis (C. colocynthis), and Silybum marianum (S. marianum). Out of nine stable formulations, one formulation named F6-SMONSECCE was found to be the best after its evaluation using antioxidant and in vitro α-amylase inhibition assay. The prepared herbal formulations showed significant (p < 0.05) antioxidant activity in terms of radical scavenging as 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric-reducing antioxidant power (FRAP) assays and also revealed the presence of a significant amount of total phenolic and flavonoid contents. "F6- SMONSECCE" (prepared with composition; Silybum marianum oil (SMO) + Nigella sativa extract (NSE) + Citrullus colocynthis extract CCE) was selected for an in vivo trial to ascertain its antidiabetic potential. The treatment dose was determined by using an acute toxicity trial on rats. Administration of alloxan (150 mg/kg b.w., i.p.) significantly (P < 0.05) augmented the blood glucose levels and lipid contents as total cholesterol (TC), triglycerides (TG), low-density lipoproteins (LDL-c), and very-low-density lipoproteins (VLDL-c). However, the levels of insulin and high-density lipoproteins (HDL-c) were found to be decreased, and the histopathological alterations were also found in the pancreas and kidney. The administration of the polyherbal formulation (F6-SMONSECCE) significantly attenuated the blood glucose levels (22.94%), TC (29.10%), TG (38.15%), LDL-c (27.58%), and VLDL-c (71.52%), whereas on the other side, the insulin (-149.15%) and HDL-c levels (-22.22%) were significantly increased. A significant histopathological normalization was observed in the pancreas and kidney tissues of the F6-SMONSECCE-treated rats. The current findings proposed that the prepared polyherbal formulation "F6-SMONSECCE" exhibited significant antioxidant, antilipidemic, and hypoglycemic potential and hence might be suggested as a remedy against diabetes or as a coadjuvant to synthetic medicines to maintain normal physiology.

6.
Molecules ; 17(5): 5803-15, 2012 May 16.
Artículo en Inglés | MEDLINE | ID: mdl-22592086

RESUMEN

Expression analysis of crop plants has improved our knowledge about the veiled underlying mechanisms for salt tolerance. In order to observe the time course effects of salinity stress on gene expression for enzymes regulating proline metabolism, we comparatively analyzed the expression of specific genes for proline metabolism in root and shoot tissues of salt-tolerant (cv. Dunkled) and salt-sensitive (cv. Cyclone) canola (Brassica napus L.) cultivars through reverse-transcriptase polymerase chain reaction (RT-PCR); following the NaCl treatment for various durations. Both lines showed an increase in ∆¹-pyrroline-5-carboxylate synthase1 (P5CS1) gene expression after induction of salt stress with enhanced expression in the root tissue of the tolerant line, while maximum expression was noted in the shoot tissues of the sensitive line. We observed a much reduced proline dehydrogenase (PDH) expression in both the root and shoot tissues of both canola lines, with more marked reduction of PDH expression in the shoot tissues than that in the root ones. To confirm the increase in P5CS1 gene expression, total proline content was also measured in the root and shoot tissues of both the canola lines. The root tissues of canola sensitive line showed a gradually increasing proline concentration pattern with regular increase in salinity treatment, while an increase in proline concentration in the tolerant line was noted at 24 h post salinity treatment after a sudden decrease at 6 h and 12 h of salt treatment. A gradually increasing concentration of free proline content was found in shoot tissues of the tolerant canola line though a remarkable increase in proline concentration was noted in the sensitive canola line at 24 h post salinity treatment, indicating the initiation of proline biosynthesis process in that tissue of sensitive canola.


Asunto(s)
Brassica napus/metabolismo , Raíces de Plantas/metabolismo , Brotes de la Planta/metabolismo , Prolina/metabolismo , Plantones/metabolismo , Brassica napus/genética , Regulación de la Expresión Génica de las Plantas , Fosfotransferasas (Aceptor de Grupo Alcohol)/genética , Fosfotransferasas (Aceptor de Grupo Alcohol)/metabolismo , Raíces de Plantas/genética , Brotes de la Planta/genética , Prolina/genética , Prolina Oxidasa/genética , Prolina Oxidasa/metabolismo , Pirroles/metabolismo , Reacción en Cadena de la Polimerasa de Transcriptasa Inversa , Salinidad , Tolerancia a la Sal/fisiología , Plantones/genética , Cloruro de Sodio
7.
ACS Omega ; 7(51): 47755-47763, 2022 Dec 27.
Artículo en Inglés | MEDLINE | ID: mdl-36591203

RESUMEN

The current study investigates the antioxidant, antidiabetic, hepatoprotective, and nephroprotective potentials of a polyherbal mixture containing the methanolic extracts of seeds from Nigella sativa, Cicer arietinum, Silybum marianum, and Citrullus colocynthis and the rhizome of Zingiber officinale. The polyherbal extract (PHE) showed significant total phenolic contents (187.17 GAE/g), ferric reducing power (28%), and radical-scavenging activity (86.16%). The PHE also showed a substantial hypoglycemic effect in alloxan-induced diabetic rats by reducing the blood glucose level of the PHE-treated rats (-48.64%) and increasing the insulin level (107.5%) as compared with the diabetic control group. Likewise, an increase in high-density lipoprotein (HDL) contents (22.95%) with an associated decrease in low-density lipoprotein (LDL) levels (-43.93%) was also noted. A significant decrease in serum levels of liver marker enzymes, e.g., SGPT (-36%), SGOT (-31%), and serum ALP (-12%), was also observed as compared with the standard drug-treated group. Based on the findings of the study, it may be suggested that PHE helps ameliorate the severity of diabetes as a herbal remedy and might be employed in nutra-pharmaceuticals, replacing synthetic antidiabetic compounds.

8.
ACS Omega ; 7(51): 48506-48519, 2022 Dec 27.
Artículo en Inglés | MEDLINE | ID: mdl-36591136

RESUMEN

The dose frequency of drugs belonging to class II is usually high and associated with harmful effects on the body. The study aimed to enhance the solubility of the poorly water-soluble drug amoxicillin (AM) by the solid dispersion (SD) technique. Six different SDs of AM, F1-F6, were prepared by the spray drying technique using two other carriers, HP-ß-CD (F1-F3) and HPMC (F4-F6), in 1:1, 1:2, and 1:3 drug-to-polymer ratios. These SDs were analyzed to determine their practical yield, drug content, and aqueous solubility using analytical techniques such as Fourier transform infrared spectroscopy, scanning electron microscopy, thermogravimetric analysis, and powder X-ray diffraction. The effect of polymer concentration on SDs was determined using aqueous solubility, in vitro dissolution, and in vivo studies. The results showed no drug-polymer interactions in SDs. Solubility studies showed that SDs based on the drug-to-polymer ratio of 1:2 (F2 and F5) were highly soluble in water compared to those with ratios of 1:1 and 1:3. In vitro dissolution studies also showed that SDs with a ratio of 1:2 released the highest drug concentration from both polymeric systems. The SDs based on HPMC confirmed the more sustained release of the drug as compared to that of HP-ß-CD. All the SDs were observed as stable and amorphous, with a smooth spherical surface. In vivo studies reveal the enhancement of pharmacokinetics parameters as compared to standard AM. Hence, it is confirmed that spray drying is an excellent technique to enhance the solubility of AM in an aqueous medium. This may contribute to the enhancement of the pharmacokinetic behaviors of SDs.

9.
Appl Biochem Biotechnol ; 170(4): 980-7, 2013 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-23636650

RESUMEN

Gene expression pattern of two important regulatory proteins, salt overly sensitive 2 (SOS2) and plasma membrane protein 3-1 (PMP3-1), involved in ion homeostasis, was analyzed in two salinity-contrasting sunflower (Helianthus annuus L.) lines, Hysun-38 (salt tolerant) and S-278 (moderately salt tolerant). The pattern was studied at selected time intervals (24 h) under 150 mM NaCl treatment. Using reverse transcription PCR, SOS2 gene fragment was obtained from young leaf and root tissues of opposing lines while that for PMP3-1 was obtained only from young root tissues. Both tolerant and moderately tolerant lines showed a gradual increase in SOS2 expression in sunflower root tissues. Leaf tissues showed the gradually increasing pattern of SOS2 expression in tolerant plants as compared to that for moderately tolerant ones that showed a relatively lower level of expression for this gene. We found the highest level of PMP 3-1 expression in the roots of tolerant sunflower line at 6 and 12 h postsalinity treatment. The moderately tolerant line showed higher expression of PMP3-1 at 12 and 24 h after salt treatment. Overall, the expression of genes for both the regulator proteins varied significantly in the two sunflower lines differing in salinity tolerance.


Asunto(s)
Regulación de la Expresión Génica de las Plantas , Helianthus/metabolismo , Proteínas de la Membrana/metabolismo , Proteínas Serina-Treonina Quinasas/metabolismo , Plantas Tolerantes a la Sal/metabolismo , Membrana Celular/genética , Membrana Celular/metabolismo , Genes de Plantas , Helianthus/efectos de los fármacos , Helianthus/genética , Proteínas de la Membrana/genética , Hojas de la Planta/efectos de los fármacos , Hojas de la Planta/genética , Hojas de la Planta/metabolismo , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Raíces de Plantas/efectos de los fármacos , Raíces de Plantas/genética , Raíces de Plantas/metabolismo , Proteínas Serina-Treonina Quinasas/genética , ARN de Planta/análisis , ARN de Planta/genética , Plantas Tolerantes a la Sal/efectos de los fármacos , Plantas Tolerantes a la Sal/genética , Cloruro de Sodio/farmacología , Especificidad de la Especie
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