Three types of oral administrated micronized zeolites [ZSM-5, zeolite A and Faujasite NaX (ZSM-5, ZA and ZX, respectively)] were prepared as anticancer 5-fluorouracil (5-Fu) delivery systems for colon cancer treatment. They were prepared by economically widespread and cheap natural resource, kaolin, at low temperatures, using microwave advanced tool. The obtained powders were characterized by XRD, SEM/EDX and BET; meanwhile, their degradation was investigated in two gastric fluids; FaSSGF (pH 1.6) and FeSSGF (pH 5), through concentration measurement of their solution disintegrated elemental constituents of Na
+
, Al
3+
and Si
4+
ions. Also, the processes of drug release and mechanism in both solutions were investigated. Moreover, the inhibition action of 5-Fu-free and 5-Fu-conjugated zeolites on colon cancer cells (CaCo-2) was estimated. The results showed that, the prepared zeolites possessed high surface areas of 526, 250, and 578 m
2
/g for ZSM-5, ZA and ZX, respectively. Although, zeolite structures seemed significantly stable, their frameworks seemed more likely reactive with time. The ions and drug release for zeolites occurred in successively two stages and found to be pH dependent, where the drug and zeolite ions were significantly of higher values in the more acidic media of the gastric solution (pH 1.6) than those of the mild acidic one (pH 5). The obtained activity indicated no cytotoxic affinity for all the prepared zeolite types. Accordingly, the synthesized zeolite frameworks are proposed to be of strong potential drug delivery vehicle for the treatment of gastrointestinal cancer.
Graphical abstract
The 1,3,4-thiadiazole derivatives (9a–i) were synthesized under solvent free conditions and their chemical composition was confirmed using different spectral tools (IR, Mass, and NMR spectrometry). All the synthesized compounds were screened for their anti-cancer potentiality over human breast carcinoma (MCF-7) and human lung carcinoma (A-549). Most of the tested compounds showed remarkable anti-breast cancer activity. However, compound 4 showed the most anti-lung cancer activity. Then, compounds with cytotoxic activity ≥ 80% over breast and lung cells were subjected to investigate their specificity on human normal skin cell line (BJ-1). Compounds 9b and 9g were chosen owing to their high breast anti-cancer efficacy and their safety, in order to study the possible anti-cancer mode of action. Otherwise, drug delivery provides a means to overcome the low solubility, un-targeted release, and limited bioavailability of the prepared 1,3,4-thiadiazole drug-like substances. Compounds 9b and 9g were chosen to be encapsulated in Na-alginate microspheres. The release profile and mechanism of both compounds were investigated, and the results revealed that the release profiles of both microspheres showed a sustained release, and the release mechanism was controlled by Fickian diffusion. Accordingly, these compounds are promising for their use in chemotherapy for cancer treatment, and their hydrophilicity was improved by polymer encapsulation to become more effective in their pharmaceutical application.
Twenty streptomycete strains were isolated from marine sediment samples collected from Nabq area, Sharm El-Sheikh, Red Sea Coast, Egypt. Four of them produce exopolysaccharides (EPS) showing marked in vitro antitumor activities. Morphological and cultural characteristics of the most significant strain (No. 3) were shown. Moreover, the sequence of this strain showed similarity with Streptomyces carpaticus. The results reveal that EPS produced by Streptomyces carpaticus No. 3 had high cytotoxicity reaching 51.7% and 59.1% against human tumor cells of breast and colon lines respectively. A chemical analysis of EPS indicated that the composing monosaccharides were galactouronic acid, glucose, xylose, galactose, mannose, and fructose with relative ratio of 3:1:1:2:2:1 respectively, with an average molecular weight (Mw) 1.180 × 105 g/mol and of a number average molecular weight (Mn) 1.052 × 105 g/mol. Also the EPS contained uronic acid (0.5072%) and monosaccharide sulphates (21.753%).
For a long time, plant secondary metabolites have been strongly examined for their antitumor and cytotoxic impacts. These days, there is another pattern of making utilization of the waste products of plants because of their extravagance of numerous phytochemical components and adequacy on human wellbeing. This research work is handling the effect of diversity of lipoidal and phenolic compounds found in the peels of two common edible plants in the Middle East; Pisum sativum and Vicia faba L. for their assesment as anticancer agents. The GC/MS of the n-hexane extract of both plant peels led to identification of twenty compounds (82.99%) and seventeen compounds (85.97%) of the total lipoidal contents from P. sativum and V. faba, respectively. While the HPLC analysis of the ethyl acetate fraction of the two plant peels resulted in recognition of 17 flavonoids and 18 phenolics from P. sativum and 16 flavonoids and 17 phenolics from V. faba. Moreover, four flavonoidal compounds were isolated to our knowledge for the first time from the peels and tested separately against different human cancer cell lines and the mode of action of the most potent compound has been determined. P. sativum ethyl acetate fraction possessed the highest scavenging activity (31.2%) as well as the most cytotoxic effect on breast carcinoma cell line. Apigenin proved to be the most potent tested compound on (MCF-7) and has no cytotoxic effect on normal human skin cell lines.
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