ABSTRACT
Colorectal cancer (CRC) is the fourth most common cause of malignant tumor death. The development of novel, more effective drugs is desperately needed to treat CRC. Zingiber officinale is believed to possess anticancer properties due to its flavonoids and phenols. Using Soxhlet (SOXT) and maceration (MACR) techniques, the present study aimed to evaluate the amounts of quercetin, gallic acid, rutin, naringin, and caffeic acid in ginger capsules of Z. officinale. High-performance liquid chromatography (HPLC)/ultraviolet was used for separation and quantitation. In vitro toxicity evaluation of ginger capsules on the CRC cell line HT-29 was also conducted to assess the anticancer activity of the supplement. The cell line HT-29 (HTB-38) colorectal adenocarcinoma was utilized for the antiproliferative effect of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide. Ginger herbal supplement extract at dosages of 200 and 100 µg had strong cytotoxic effects (IC50 < 50 µg/mL) on HT-29 CRC cells via MACR. This extract is comparable to the SOXT extract, which has an IC50 of less than 50 µg/mL. The anticancer effect of ginger herbal supplement formulations against CRC lines was investigated, and the results obtained from both the MACR and SOXT extraction procedures were noteworthy. The quercetin content was the highest of all the extracts according to the HPLC data.
ABSTRACT
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.
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Subject(s)
Breast Neoplasms , Lung Neoplasms , Mebendazole , Mebendazole/pharmacology , Mebendazole/therapeutic use , Humans , Animals , Breast Neoplasms/drug therapy , Breast Neoplasms/pathology , Female , Cell Line, Tumor , Mice , Lung Neoplasms/drug therapy , Lung Neoplasms/pathology , Drug Carriers/chemistry , Lipids/chemistry , Mice, Inbred BALB C , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemistry , Mice, NudeABSTRACT
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 24â 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 (1.8â 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.
Subject(s)
Carcinoma , Rutin , Humans , Rutin/pharmacology , Liposomes , HT29 Cells , Polyethylene GlycolsABSTRACT
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.
Subject(s)
Antioxidants/administration & dosage , Neoplasms/drug therapy , Neovascularization, Pathologic/drug therapy , Plant Extracts/administration & dosage , Angiogenesis Inhibitors/administration & dosage , Angiogenesis Inhibitors/chemistry , Animals , Antioxidants/chemistry , Aorta/drug effects , Aorta/growth & development , Humans , Jordan/epidemiology , Neoplasms/epidemiology , Neovascularization, Pathologic/epidemiology , Plant Extracts/chemistry , Plants, Medicinal/chemistry , Rats , Saudi Arabia/epidemiologyABSTRACT
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.