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1.
Nanomedicine (Lond) ; 19(12): 1087-1101, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38661720

RESUMEN

Aim: To investigate the therapeutic potential of mebendazole (MBZ)-loaded nanostructured lipid carriers (NLCs). Methodology: NLC-MBZ was prepared and characterized to evaluate the in vitro and in vivo anticancer effects and the inhibitory effect on RanGTP and its potential as an antimetastatic treatment in vivo. Results: NLC-MBZ exhibited a size and charge of 155 ± 20 nm and -27 ± 0.5 mV, respectively, with 90.7% encapsulation. Free MBZ and NLC-MBZ had a 50% inhibitory concentration of 610 and 305 nM, respectively, against MDA-MB-231 cell lines. NLC-MBZ decreased tumor size, suppressed tumor lung metastases, and lowered the expression of CDC25A, SKP2, RbX1 and Cullin1 while boosting the Rb proteins. Conclusion: NLC-MBZ displayed antiangiogenic potential and resulted in a reduced rate of lung metastasis in vivo.


[Box: see text].


Asunto(s)
Neoplasias de la Mama , Neoplasias Pulmonares , Mebendazol , Mebendazol/farmacología , Mebendazol/uso terapéutico , Humanos , Animales , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/patología , Femenino , Línea Celular Tumoral , Ratones , Neoplasias Pulmonares/tratamiento farmacológico , Neoplasias Pulmonares/patología , Portadores de Fármacos/química , Lípidos/química , Ratones Endogámicos BALB C , Antineoplásicos/farmacología , Antineoplásicos/química , Ratones Desnudos
2.
Chem Biodivers ; 20(11): e202301167, 2023 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-37781742

RESUMEN

The abstract discusses the development of rutin-loaded nanoliposomes and their anti-colorectal cancer activity against human carcinoma cells (HT-29). The study characterizes the nanoliposomes using the thin-film hydration method and analyzes their size, charge, and polydispersity index. The encapsulation efficiency and drug loading ability of rutin at different concentrations were investigated. The nanoliposomes were found to be stable for up to one month at 4 °C and showed sustained drug release for up to 24 h. The anti-cancer activity of the rutin-loaded nanoliposomes was found to be concentration-dependent and significantly improved compared to free rutin. PEGylated nanoliposomes with rutin (1.8 mg/ml) showed the highest encapsulation efficiency and drug loading ability, along with improved selectivity against cancer cells. Overall, the study provides important insights into the potential use of rutin-loaded nanoliposomes for the treatment of colorectal cancer.


Asunto(s)
Carcinoma , Rutina , Humanos , Rutina/farmacología , Liposomas , Células HT29 , Polietilenglicoles
3.
Mol Med Rep ; 18(2): 2441-2448, 2018 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-29901194

RESUMEN

Angiogenesis plays a crucial role in malignant tumor progression and development. The present study aimed to identify lead plants with selective anti-angiogenic properties. A total of 26 methanolic extracts obtained from 18 plants growing in Saudi Arabia and Jordan that belong to the Lamiaceae family were screened for their cytotoxic and anti-angiogenic activities using MTT and rat aortic ring assays, respectively. Four novel extracts of Thymbra capitata (L.) Cav., Phlomis viscosa Poir, Salvia samuelssonii Rech.f., and Premna resinosa (Hochst.) Schauer were identified for their selective anti-angiogenic effects. These extracts did not exhibit cytotoxic effects on human endothelial cells (EA.hy926) indicating the involvement of indirect anti-angiogenic mechanisms. The active extracts are potential candidates for further phytochemical and mechanistic studies.


Asunto(s)
Antioxidantes/administración & dosificación , Neoplasias/tratamiento farmacológico , Neovascularización Patológica/tratamiento farmacológico , Extractos Vegetales/administración & dosificación , Inhibidores de la Angiogénesis/administración & dosificación , Inhibidores de la Angiogénesis/química , Animales , Antioxidantes/química , Aorta/efectos de los fármacos , Aorta/crecimiento & desarrollo , Humanos , Jordania/epidemiología , Neoplasias/epidemiología , Neovascularización Patológica/epidemiología , Extractos Vegetales/química , Plantas Medicinales/química , Ratas , Arabia Saudita/epidemiología
4.
Mol Med Rep ; 17(4): 6059-6067, 2018 04.
Artículo en Inglés | MEDLINE | ID: mdl-29484402

RESUMEN

Huernia Sp. Nov. aff. Boleana, Apocynaceae, grows in the high mountains of southwest Saudi Arabia and is widely used as a remedy for the treatment of diabetes. The present study investigated the anti­inflammatory, wound healing and inhibitory effects on migration of Huernia Sp. Nov. aff. Boleana. The anti­inflammatory effect was assessed in mice using formalin­induced edema. Wound healing effects were assessed in rats using a circular excision wound model. An in vitro 'scratch' test was used to investigate the inhibitory effects on melanoma cell (B16­F10) migration. The anti­inflammatory effects of total extract, hexane and chloroform fractions were greater or equal to indomethacin (control). The relatively non­polar fractions (hexane and chloroform) exhibited higher anti­inflammatory activities compared with the aqueous fraction. The percentage of wound contraction among animals treated with the plant extract was higher compared with the control; however, this difference was not statistically significant (P>0.05). The total plant extract increased wound healing by inhibiting the inflammatory response, promoting angiogenesis, and significantly promoting the proliferation of fibroblasts, particularly on days 7 and 14 post­wounding. Furthermore, the plant extract promoted wound repair via the enhancement of collagen synthesis, and complete epithelization with well­formed and differentiated epithelial tissues. The in vitro 'scratch' test indicated the inhibitory effects of this plant on melanoma cell migration in a dose­dependent manner. The present study indicated that Huernia Sp. Nov. aff. Boleana may have potential as an anti­inflammatory, wound-healing and migration-inhibiting ethno medicine.


Asunto(s)
Antiinflamatorios/farmacología , Apocynaceae/química , Extractos Vegetales/farmacología , Animales , Movimiento Celular/efectos de los fármacos , Colágeno/metabolismo , Edema/inducido químicamente , Edema/tratamiento farmacológico , Edema/metabolismo , Edema/patología , Femenino , Fibroblastos/efectos de los fármacos , Fibroblastos/metabolismo , Melanoma Experimental , Ratones , Neovascularización Fisiológica/efectos de los fármacos , Arabia Saudita , Cicatrización de Heridas/efectos de los fármacos
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