Multidrug resistance (MDR) causes difficulties in the treatment of infections and cancer. Research and development studies have become increasingly important for the strategy of preventing MDR. There is a need for new multitarget drug research and advancement to reduce the development of drug resistance in drug‐drug interactions and reduce cost and toxic effects. This study aimed to determine the effects of multi‐target triazene compounds on antibacterial, antifungal, antiviral, cytotoxic, and larvicidal activities were investigated in vitro. A series of 12 novel of 1,3‐diaryltriazene‐substituted sulfadiazine (SDZ) derivatives were synthesized, and the obtained pure products characterized in detail by spectroscopic and analytic methods (FT‐IR, 1H‐NMR, 13C‐NMR, and melting points). The antibacterial and antifungal activities of these derivatives (AH1‐12) were determined by broth microdilution method. All derivatives have been evaluated in cell‐based assays for cytotoxic and antiviral activities against Modified Vaccinia Virus Ankara. The larvicidal efficacy of these chemical compounds was also investigated by using Lucilia sericata (L. sericata) larvae. Twelve 1,3‐diaryltriazene‐substituted SDZ derivatives (AH1‐12) were designed and developed as potent multitargeted compounds. Among them, the AH1 derivative showed the most antibacterial and antifungal activity. Besides, synthesized derivatives AH2, AH3, AH5, and AH7 showed higher antiviral activity than SDZ. All synthesized derivatives showed higher cytotoxic activity than SDZ. Also, they showed larvicidal activity at 72 h of the experiment. As a result, these compounds might be great leads for the development of next‐generation multitargeted agents.
• D. melanogaster was exposed to Acetazolamide (AAZ) and SLC-0111 against carbon tetrachloride-induced toxicity. • Feeding with AAZ and SLC-0111 increased development times. • The AAZ and SLC-0111 increased the activity of antioxidant enzymes thus reducing the high percentage of survival in adults caused by the CCl4 induced toxicity. • AAZ and SLC-0111 were reduced CCl4-induced oxidative stress in adipose tissue in D. melanogaster and were positively affect the development of organisms.
Aim: Cyclophosphamide (CP) is a commonly used chemotherapeutic agent despite its toxic adverse effects, including hepatotoxicity. Ellagic acid (EA) is an antioxidant agent and exhibits free radical scavenging activities. In this experimental study, the effects of EA on CP-induced liver injury were investigated.Material and Methods: Twenty-four Sprague-Dawley rats (180-220 gr) were separated into four equal groups. A single dose of 150 mg/kg CP was given intraperitoneally to generate hepatotoxicity. Different doses (50 and 75 mg/kg) of EA were administered orally 20 minutes before, 4 and 8 hours after CP administration. The histopathological evaluation of kidney tissues and immunohistochemical evaluation for caspase-3 were conducted as well as the serum biochemical analyses.Results: CP treated group exhibited a significant increase in serum hepatic enzymes, aspartate aminotransferase (AST) and alanine aminotransferase (ALT), compared to the control group. Similarly, the total triglycerides (TG) and very-low-density lipoprotein cholesterol (VLDL-C) levels increased significantly. Additionally, the high-density lipoprotein cholesterol (HDL-C) levels decreased, which was not significant, compared to the control group. At both EA doses, VLDL-C, AST, ALT levels decreased significantly while HDL-C level revealed a significant increase. 75 mg/kg EA treatment caused a non-significant elevation in total cholesterol (TC) concentration. Microscopic analysis showed a significant congestion, edema, degeneration and necrosis in the livers of CP administered group. However, edema, degeneration, and necrosis were significantly reduced in animals treated with EA-75. In addition, caspase-3 expression significantly decreased in EA-75 group.Conclusion: These results indicate the protective effects of EA in CP-induced hepatotoxicity in rats.
2 May 2023 in Journal of Biochemical and Molecular Toxicology
Schiff bases (imines or azomethines) are versatile ligands synthesized from the condensation of amino compounds with active carbonyl groups and used for many pharmaceutical and medicinal applications. In our study, we aimed to determine the cytotoxic, antifungal and larvicidal activities of biologically potent bis‐sulfonamide Schiff base derivatives that were re‐synthesized by us. For this aim, 16 compounds were re‐synthesized and tested for their cytotoxic, antifungal and larvicidal properties. Among this series, compounds A1B2, A1B4, A4B2, A4B3, and A4B4 were shown to have cytotoxic activity against tested cancer lung cell line (A549). The most potent antifungal activity was observed in compounds A2B1 and A2B2 against all fungi. A1B1 showed the strongest larvicidal effect at all concentrations at the 72nd h (100% mortality). These obtained results demonstrate that these type of bis‐substituted compounds might be used as biologically potent pharmacophores against different types of diseases.
< /B > Spinal cord injuries negatively affect the individuals and the life quality of their families due to neurological deficits caused by trauma. The prevalence of spinal cord injury is 15-45/1 million in the world. Caffeic acid phenethyl ester (CAPE) is the most active component of propolis and has neuroprotective, anti-oxidant and anti-apoptotic effects. Our aim was to determine the effects of CAPE on the prevention of secondary injury and to compare with methylprednisolone. Forty rats were divided into 4 groups. The control group did not undergo surgery (Group I), only trauma group (Group II), trauma+CAPE treatment group (Group III), and trauma+methylprednisolone treatment group (Group IV). Histopathological assessment was performed with two staining methods as hematoxylin-eosin (HE) and terminal deoxynucleotidyl Transferase Biotin - dUTP Nick End Labeling (TUNEL). The groups were statistically compared. The apoptotic cells decreased in treatment groups compared with the trauma. CAPE has more anti-apoptotic effect than methylprednisolone. The histological difference between the Group II, and Groups III and IV was statistically significant. CAPE has a positive effect on spinal cord injuries by preventing apoptosis.