Objective: Zerumbone (ZER) is a well-known natural compound that has been reported to have anti-cancer effect. Thus, this study investigated the ZER potential to inhibit Thymidine Phosphorylase (TP) and the ability to trigger Reactive oxygen species (ROS)-mediated cytotoxicity in non-small cell lung cancer, NCI-H460, cell line. Material and Method: The antiangiogenic activity for ZER was evaluated by using the thymidine phosphorylase inhibitory test. Reactive oxygen species (ROS) production was determined via DCFDA dye by using flow cytometry. Result and Discussion: ZER was found to be potent TP inhibitory with the IC50 value of 50.3± 0.31 μg/ml or 230±1.42 µM. NCI-H460 cells upon treatment with ZER produced significant ROS by 55.7%. Consequently, ZER exerts anti-angiogenic properties and modulates ROS production in lung cancer cells, serving as leads for better therapeutic index in cancer drug.
Amoxicillin 1 was treated with thiosemicarbazide and Phosphoryl chloride to obtain a new derivatives that contains 1,3,4-thiadiazole moiety 2. Schiff bases compounds were synthesized by the reaction of compound 2 with different aldehydes such as benzaldehyde and some substituted Benzaldehyde; p-hydroy, p-Chloro, p-Nitro, p-Dimethylamino, p-Methyl, p-Methoxy, p-Ethoxy to give compounds 3a-h. The obtained compounds have tested towards gram -ve and gram +ve bacteria. The compound shows good to moderate result towards the bacteria.
In this work, a series of new maleimides linked to substituted benzothiazole moiety were synthesized. Synthesis of these new cyclic imides were performed via three steps, the first one involved preparation of a series of 2-aminobenzothiazole substituted with different substituents via reaction of different primary aromatic amines with ammonium thiocyanate and bromine in glacial acetic acid. The prepared 2- amino benzothiozoles were introduced in the second step in reaction with maleic anhydride producing a series of N-(substituted benzothiazole-2-yl) maleamic acids.The resulted maleamic acids were dehydrated in the third step via treatment with acetic anhydride and anhydrous sodium acetate to afford a series of the desirable N-(substitu
... Show MoreAn International Publisher for Academic and Scientific Journals The mucilage of white and black chia seeds were extracted and determining their contents of bioactive compounds such as tannins, glycosides, flavonoids, phenols, and studying their activity as anti-filamentary and anticancer. Results showed that tannins exist in white chia seeds with 35%while it is 38% in black seeds, flavonoids represent 0.98mg/ml in white chia seeds and 1.5 mg/ml for black seeds. Both kinds of seeds showed anti-filamentaryactivity, the inhibition ratio was 86.5% for white seeds and 97.3% for black seeds. Chia black seeds showed anticancer activity and the inhibition of the tumor muscle cell line ratio (GI%) was 34.8% at 50mg/ml concentration and 88.4%
... Show MoreIt is known that the oral administration of ibuprofen caused an irritation of stomach as a side effect due to its carboxylic moiety. Ibuprofen ester was synthesized by linking the carboxylic moiety of ibuprofen and the hydroxylic group of paracetamol to reduce its side effect. Study the kinetic hydrolysis of prepared ester was examined at different values of physiological pH (1.0, 5.8, 6.4 and 7.4) at 37 ± 0.1 of 1 hour period. Measurements of absorbance were carried out by UV-Visible spectrophotometer to follow the stability of ester, it showed Pseudo first order hydrolysis. The pH- apparent rate profiles of ester was exhibited a good stability at pH 1.0 and pH 5.8. Pharmacological activity in vivo of prepared ester was evaluated in re
... Show MoreGiardia lamblia is one of most common protozoan cause diarrheas, and the most health problem in development countries worldwide. Our work aimed to assess activity and toxicity of metronidazole loaded silver nanoparticles in treatment of acute giardiasis in mice. After inoculated mice with Giardia cysts in a dose of 105 cyst for acute infection, treatments were given for eight days. Number Giardia cysts in stool were discovered. Toxicity nanoparticles was estimated by Measurement oxidative stress markers (GSH) and (MDA) in liver, kidney tissue homogenate. The results showed single therapy was better effect by silver nanoparticles, highest percentages of reduction in number of cysts Giardia lamblia of infected mice treated with silver nanopar
... Show MoreVitamin E, having the well known antioxidant activity through scavenging free radicals و it occurs in several isomeric forms , these isomers have relatively different functions . One of these actions is related to its ability to inhibit platelets aggregation and hence thrombosis. The present study included a total number of apparently healthy 62 males . 11of them served as standard group , treated with 100 mg aspirin /day for more than one month . Another 31 subjects were randomly grouped into 5 groups that received different daily doses of α – tocopherol : 400 IU , 800 IU and 1200 IU for 2-6 months.The remainder ( 20 ) subjects served
... Show MoreOur goal in this research, some new nucleoside analogues was synthesized. Starting from ?-D glucose which was converted to per acetylated ?-D gluco pyronoside then converted to active from(1-Bromo Sugar (2) as a sugar moiety.The base moiety 2-substituted benzimidazole was prepared from condensation of phenylene diamine with different aromatic aldehydes, which were subjected to amino alkylation via Mannich reaction forming new nucleobase derivatives. Condensation of nucleobase with bromo sugar through nucleophilic substitution of anomeric carbon with nitrogen forming new protected nucleoside analogues then hydrolyzed with sodium methoxide in methanol to obtain our target, the free nucleoside analogues. All prepared compound were identified b
... Show MoreBackground: Chemotherapeutic medication treatment for cancer is typically used in conjunction with other techniques as part of a routine regimen. It is well established that the capacity of different chemotherapeutic drugs to induce apoptosis is correlated with their anticancer efficacy. Quinazolinone-based drugs have demonstrated excellent responses from several cancer cell types. These substances have a lot of potential for use as building blocks in the creation of apoptosis inducers. Objective: To assess the new quinazolinone derivatives (M1 and M2) that were recently synthesized for their potential to halt wound healing and to use the acridine orange/propidium iodide (AO/PI) double stain to assess their capacity to induce apopto
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