Synthesis of carbazole bearing pyridopyrimidine‐substituted sulfonamide derivatives and studies their carbonic anhydrase enzyme activity

The synthesis of carbazole containing pyridopyrimidine‐substituted sulfonamide derivatives ( 3a‐i ) and their inhibitory effects on human carbonic anhydrase (hCA) I and II were studied. Spectral data and elemental analysis confirmed the structures of the compounds synthesized. The results show that all the synthesized compounds inhibited the CA I and II activities. Among them, 3a was found to be the most active ( K _i: 14 µM) for hCA I and 3f ( K _i: 126 µM) for hCA II.     

Menadione sodium bisulphite regulates physiological and biochemical responses to lessen salinity effects on wheat (Triticum aestivum L.)

Salinity is a significant constraint for plant survival and productivity. Therefore, an immediate solution to this problem is sought to meet the human population''s food demands. Recently, Menadione sodium bisulphite (MSB) has emerged as a significant regulator of plant defense response under abiotic stress. Studies on MSB are scarce, and a few reports on salinity (Arabidopsis and okra) and cadmium stress (okra) are present in the literature. However, these studies did not include the impact of MSB on physiological and plant water relation attributes, critical mediators of plant survival, and yield production under stress. Our results studied the impact of MSB on wheat administered to NaCl salinity in hydroponics medium. We used two wheat cultivars (salt-sensitive MH-97 and salt-tolerant Millat-2011, based on our pre-experimental studies). Seeds were primed in different MSB doses [control (unprimed), hydroprimed, 5, 10, 20, and 30 mM]. Salinity significantly diminished growth, chlorophyll molecules, photosynthesis, total free amino acids, water and turgor potentials, K, Ca, and P contents of wheat when administered NaCl salinity in the nutrient solution. Besides, a noteworthy accretion was present in oxidative stress markers [hydrogen peroxide & malondialdehyde], proline, ascorbic acid, antioxidant enzyme activities, and Na⁺ accumulation under salinity. Moreover, MSB noticeably enhanced chlorophyll molecules, proline, and oxidative defense to improve photosynthesis, plant water relations, and diminish specific ions toxicity. Our results manifested better defense regulation in salt-administered plants primed with 5 and 10 mM MSB. Our findings strongly advocated the use of MSB in improving plant salinity tolerance, particularly in wheat.     

Effect of testosterone on epididymal proteins in castrated rhesus monkeys

The effect of testosterone on regulation of epididymal protein synthesis has been investigated in castrated rhesus monkeys (Macaca mulatta). The proteins in the treated monkeys were characterized using polyacrylamide gel electrophoresis (under nondenaturing and denaturing conditions) and electrofocusing. At least four distinct proteins have been shown to be synthesized by the monkey epididymis under testosterone influence. Two of these proteins were detected following two days of testosterone treatment while the other two proteins were detected after a six-day treatment period. None of these proteins was detectable in monkeys treated with estradiol for six days. Electrofocusing of epididymal cytosol proteins from untreated and testosterone-treated and castrated monkeys also confirmed the presence of four androgen-dependent proteins in this species. The isoelectric points of these proteins were shown to range between 5.8 and 6.4. The molecular weights of these proteins were found to vary between 47,500 and 66,000. The in vitro incorporation of ³H-labeled amino acids was markedly greater in the androgen-primed epididymis as compared with the control tissue.     

cis-Unsaturated fatty acids uncouple mitochondria and stimulate glycolysis in intact lymphocytes.

In intact lymphocytes, linoleic acid acts as a typical mitochondrial uncoupler: it substantially decreases the mitochondrial membrane potential and the cellular ATP level, while stimulating oxygen consumption and glycolysis. Under these conditions the inhibition of cellular functions by linoleic acid cannot be attributed to its postulated effects on lipid domains in the plasma membrane.     

The Effects of Sunitinib in Healthy and Cisplatin-Induced Rats

Sunitinib is a multitargeted kinase inhibitor that inhibits many receptor tyrosine kinases and has been used in the treatment of gastrointestinal stromal tumors, metastatic renal cell carcinoma, and pancreatic neuroendocrine tumors. In this study, the effects of sunitinib given to rats, both alone and after stress with cisplatin, were investigated. The animals were divided into four groups – (1) control group (C) administered interperitoneally with a single dose 0.9 % saline, (2) Cis group administered a single dose (7 mg/kg) of cisplatin, (3) Sun group administered 10 mg/kg sunitinib for seven days, and (4) Cis+Sun group administered 10 mg/kg sunitinib for seven days after a single dose (7 mg/kg) of cisplatin. After these applications, the rats were sacrificed, and blood and tissue samples were taken for biochemical and histopathological evaluations. Sunitinib did not show any effect on urea, creatine, and kidney IL1β and TGF-β3 expression levels when administered alone; it increased ALT, AST, and IL-38 levels. When sunitinib was given to the cisplatin-induced rats, it was observed that the increase in ALT, AST, and IL-38 levels increased more than the rats that was given only sunitinib. According to the data obtained, sunitinib does not cause a significant change in kidney tissue under both normal and stress conditions, while it creates stress in liver tissue. In addition, its toxicity in the liver becomes more certain as a result of its combination with cisplatin.