Sinteza, in vitro antitumorsko ispitivanje i radiosenzitirajuće vrednovanje novih derivata 4-[3-(supstituiranih)tioureido]-N-(kinoksalin-2-il)benzensulfonamida

Sulfonamides and quinoxaline derivatives possess many types of biological activities and have been recently reported to show substantial antitumor activity. This paper reports the synthesis of novel thioureidosulfaquinoxaline derivatives. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against a human liver cell line (HEPG2) and showed higher activity than the reference drug doxorubicin. 4-(3-(4-Ethylbenzoate)thioureido)-N-(quinoxalin-2-yl)benzenesulfonamide (9) (IC50 = 15.6 µmol L1), N-(pyridin-2-yl)-4-(3-(4-(N-quinoxalin-2-yl-sulfamoyl)phenyl)thioureido)benzene-sulfonamide (10) (IC50 = 26.8 µmol L1) and N-(quinoxalin-2-yl)-4-(3-(4-(N-thiazol-2-ylsulfamoyl)phenyl)thioureido)benzenesulfonamide (11) (IC50 = 24.4 µmol L1) were the most potent compared to doxorubicin (IC50 = 71.8 µmol L1). The most potent compounds 9, 10 and 11 were evaluated as radiosensitizing agents by subjecting the compounds to γ-irradiation (8 kGy).Derivati sulfonamida i kinoksalina imaju raznoliko biološko djelovanje, između ostalog i antitumorsko djelovanje. U radu je opisana sinteza novih derivata tioureido sulfakinoksalina. Svim novim spojevima ispitano je antitumorsko djelovanje in vitro na humanoj staničnoj liniji jetre (HEPG 2). Svi ispitani spojevi pokazuju jači učinak nego referentni lijek doksorubicin. Najjači učinak imali su 4-(3-(4-etilbenzoat)tioureido)-N-(kinoksalin-2-il)benzen-sulfonamid (9) (IC50 = 15,6 µmol L1), N-(piridin-2-il)-4-(3-(4-(N-kinoksalin-2-il-sulfamoil)fenil)tioureido)-benzen-sulfonamid (10) (IC50 = 26,8 µmol L1) i N-(kinoksalin-2-il)-4-(3-(4-(N-tiazol-2-ilsulfamoil)fenil)tioureido)benzen-sulfonamid (11) (IC50 = 24,4 µmol L1), dok je IC50 vrijednost bila 71,8 µmol L1. Najaktivniji spojevi 9, 10 i 11 evaluirani su kao radziosenzitirajuća sredstva nakon izlaganja spojeva γ-zračenju (8 kGy)

In-vitro cytotoxic and radiosensitizing evaluation of novel 2-pyridone, isoquinoline, chromene and chromenopyridone derivatives

On the account of the reported anticancer activity of 2-pyridone, a new series of ethyl-1,6-dihydropyridine-3-carboxylate (4a-j), 1-oxo-1,2-dihydroisoquinoline-7-carbonitrile (6a-h), 2H-chromene (7,8) and 3H-chromeno[3,4-c]pyridone derivatives (9,10) were synthesized and tested for in-vitro anticancer activity against Ehrlich Ascites Carcinoma (EAC) cell line and human liver cell line (HEPG2). The structures of the synthesized compounds were confirmed by analytical and spectral data. Furthermore, radiosensitization study was performed for the most potent compounds (4a, 4d, 6a, 6c, 6e and 10)

Bone Activity Biomarkers and Bone Mineral Density in Children with Chronic Kidney Disease

Introduction: Chronic kidney disease - mineral and bone disorder (CKD-MBD) is a spectrum of bone minerals changes that range from high turnover lesions of secondary hyperparathyroidism to the low turnover lesions of adynamic bone disease. Bone biopsy is the gold standard for the diagnosis, but it is not routinely performed because it is invasive technique. Methods: Fifteen CKD children on regular hemodialysis (group I) and 15 CKD children on conservative management (group II) were selected from the nephrology clinics of Zagazig University Hospitals along with 15 age and sex-matched healthy controls. Participants were subjected to biochemical assessment that included osteocalcin (OC), total and bone-specific alkaline phosphatase (tALP and bALP), isomerized beta form of type I collagen cross-linked telopeptide (β-Crosslaps) and intact parathyroid hormone (iPTH) levels. Patients with CKD also had their bone mineral density (BMD) measured using dual energy X-ray absorptiometry (DEXA) at lumbar spine and femoral neck. Results: Serum β-Crosslaps, OC and bALP were significantly higher in patient groups than controls and in group I compared to group II .There was a negative significant correlation between mean Z-score at lumbar spines and bALP, OC and iPTH in group I and with β-Crosslaps in both patient groups. The mean Z-score at femoral neck correlated negatively with bALP in group I, with OC in group II and with iPTH and β-Crosslaps in both groups. Conclusion: Biochemical bone markers and assessment of BMD in patients with CKD may have a role in the early detection of CDK-MBD. Keywords: chronic kidney disease; bone mineral density; bone biomarker

Primary colorectal small cell carcinoma: A clinicopathological and immunohistochemical study of 10 cases

Colorectal small cell carcinoma (SmCC) is a rare tumor with an aggressive course. The aim of this study is to summarize our experience with this tumor and to highlight its immunohistochemical profile. Ten cases of colorectal SmCC were identified in our files and a panel of immunostains was performed. Follow up was available for the average of 3 years, during which 7 patients died and 3 were alive with disease. All cases were positive for LMWK, CK 19 and pancytokeratin but were negative for TTF-1 and CA 125. EGFR was positive in 7 cases. TTF-1 negative staining may be valuable in differentiating it from its pulmonary counterpart. CDX2, mCEA, CD56, synaptophysin, NSE and chromogranin can help differentiate it from non-endocrine poorly differentiated adenocarcinoma. The expression of EGFR in a subset of patients has not been reported earlier and has to be evaluated in larger series to assess its role in the planning of targeted biologic therapy

Well as its Microcapsules in Rats

ABSTRACT Ketorolac is a potent non-steroidal analgesic drug. It is 36 times more potent than phenyl butazone, and twice as that of indomethacin. The oral administration of ketorolac is associated with high risk of adverse effects such as irritation, ulceration, bleeding of gastrointestinal tract, edema as well as peptic ulceration. These attributes make ketorolac a good candidate for controlled release dosage forms, so as to ensure slow release of the drug in the stomach. The present study reports on the formulation of ketorolac loaded Eudragit RS100, Eudragit RL100 as well as Ethyl cellulose as a controlled release drug delivery system. Solid dispersion and microencapsulation by air suspension method were the techniques of choice in order to coat the drug so as to improve bioavailability and stability and also target a drug at specific sites. The ratio of (1:3) drug to polymer from all polymers used was selected from solid dispersions systems as well as microcapsules to conduct further in vivo evaluation, since it was the best ratio which achieved significant reduction in the release of ketorolac at acidic pH of the stomach and maximal release at alkaline pH of the intestine. The effects of various formulations on ulcer index as well as ulcer incidence were studied. The obtained results indicate that microencapsulation technique was able to protect the stomach from ulcerogenic effect ketorolac compared to solid dispersion technique

Flavoring and Coating Technologies for Processing Methods, Packaging Materials, and Preservation of Food

The food sector addresses perhaps the main business with regard to degree, speculation, and variety. In a forever-evolving society, dietary requirements and inclinations are broadly factors. Alongside offering extraordinary mechanical help for inventive and valued items, the ongoing food industry ought to likewise cover the essential necessities of a consistently expanding populace. Active food packaging strategies have experienced a tremendous push forward in the last two decades. It is a great opportunity to decide which bioactive component will be more appropriate for each specific application once the microbiological hazards for each type of food item are recognized and the microbial targets are clearly differentiated. In order to improve Flavor delivery and preservation, the food industry and the science of Flavor are constantly creating new ingredients, processing techniques, and packaging materials. This improves the quality and acceptability of food by boosting Flavor stability. As most Flavors can be influenced by interactions with other food ingredients in addition to being volatile and chemically unstable to air, light, moisture, and high temperatures. The food sector will succeed in the long run if new technologies are quickly adopted and effectively used to meet both current and future consumer expectations