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This study investigated the druggability, pharmacokinetics and ethyl acetate extract of Teucrium polium (EA T. polium) and the protective effect against carbon tetrachloride (CCl4) induced liver cirrhosis in rats. The total antioxidant capacity (TAC) and scavenging activity of the extract were examined. The in vivo protective study was based on the use of an animal model of CCl4-induced liver cirrhosis. Four groups of rats have been used: Group I: control rats; Group II: received CCl4 in olive oil (0.5 mL/kg); Group III: received the EA T. polium (25 mg/kg) of pretreatment for seven days by gavage then CCl4 in olive oil by gavage for 15 days. Group IV: received the EA of T. polium for seven days (25 mg/kg). EA T. polium was found to possess significant antioxidant capacity. CCl4 caused a hepatotoxicity associated increase in both levels of AST and ALT, which were reduced back to normal values following EA T. polium pretreatment. Hepatotoxicity associated structural modifications of liver tissues and increase in thiobarbituric acid reactive substances (TBARS), conjugated dienes (CD) and carbonyl proteins (CP), associated decreases in several assessed antioxidant enzymes such as superoxide dismutase (SOD), glutathione peroxidase (GPx) and catalase (CAT). The in vivo findings on the protective effect of T. polium were supported by its druggability, its pharmacokinetic properties and molecular docking assays. These results confirm the modulatory antioxidant and hepatoprotective potential of T. polium in this experimental liver cirrhosis model. T. polium phytochemicals are good candidates for further pharmaceutical explorations and drug design. [ABSTRACT FROM AUTHOR]

Sm-p80, the large subunit of Schistosoma mansoni calpain, is a leading candidate for a schistosomiasis vaccine. The prophylactic and antifecundity efficacy of Sm-p80 has been tested in three animal models (mouse, hamster and baboon) using a multitude of vaccine formulations and approaches. In our continual effort to enhance the vaccine efficacy, in this study, we have utilized the adjuvant, synthetic hexa-acylated lipid A derivative, glucopyranosyl lipid A (GLA) formulated in aluminum (GLA-Alum) with recombinant Sm-p80. The rSm-p80+GLA-Alum immunization regimen provided 33.33%-53.13% reduction in worm burden in the mouse model and 38% worm burden reduction in vaccinated baboons. Robust Sm-p80-specific immunoglobulin (Ig)G, IgG1, IgG2a and IgM responses were observed in all immunized animals. The rSm-p80+GLA-Alum coadministration induced a mix of T-helper (Th) cells (Th1, Th2 and Th17) responses as determined via the release of interleukin (IL)-2, IL-4, IL-18, IL-21, IL-22 and interferon-γ. [ABSTRACT FROM AUTHOR]

The synthesis, X-ray single crystal, and optical properties of a novel sulfate-bridged copper complex have been investigated. Moreover, the biological activities of our complex were explored for the development of both antioxidant and anti-tumoral drugs. [Display omitted] • Single crystals of a novel sulfate-bridged complex were grown by the slow evaporation method. • Its structure self-organizes in μ 2 -SO 4 cross-linked 1D infinite chains that are further implicated in hydrogen bonding engendering a 3D supramolecular network. • Thermal analyses pointed out the high thermal stability of our complex. • Optical measurements highlight the presence of a hypsochromic shift in the absorption and photoluminescence spectra. • The biochemical and histological studies invigorated further analyses of our complex for the development of both antioxidant and anti-tumoral drugs. A sulfate-bridged complex [Cu(µ 2 -SO 4)(Im) 4 ] (1) was prepared and structurally characterized, where Im: imidazole. The X-ray structure analysis reveals that 1 crystallizes in the monoclinic system with space group C2/c. The octahedral coordination around the metal center is made up of four distinct imine nitrogen atoms in the equatorial plane, and two sulfate oxygen atoms occupying the axial sites. The covalent linkage between metals via the sulfate group, forming infinite 1D zigzag chains, ensures the entanglement of the structure. These chains, in turn, are further assembled into a 2D network through N H⋯O hydrogen bonding. Thermal analyses underline the high thermal stability of our complex, which starts to decompose at 200 °C. The infrared spectrum confirms the results obtained from the crystallographic analysis. Optical studies reveal the presence of a hypsochromic effect noticed in the absorption and photoluminescence spectra. The synthesized compound was found to reduce both oxidative injury and histopathological features, which are associated with skeletal metastases as a result of malignant Walker 256/B breast cancer cells. [ABSTRACT FROM AUTHOR]

Diabetes mellitus has become a serious problem associated with health complications, such as metabolism disorders and liver-kidney dysfunction. The inadequacies associated with conventional medicines have led to a determined search for alternative natural therapeutic agents. The present study was conducted to evaluate the hypoglycemic, antilipidemic, and antioxidant effects of EGCG in surviving diabetic mice. Alloxan diabetic mice were treated with EGCG. Their bloods were collected and submitted to various biochemical measurements, including blood glucose, cholesterol, triglycerides, urea, creatinine, and transaminases. Their livers and kidneys were isolated to assess oxidative damage and to perform histological analysis. Both EGCG and insulin treatment of diabetic mice resulted in a significant reduction in fasting blood glucose levels. EGCG supplementation also ameliorated hepatic as well as renal toxicity indices. Moreover, diabetic mice injected with EGCG exhibited significant changes in antioxidant enzyme activities in the liver and kidney. Histological analyses also showed that it exerted an ameliorative action on these organs and efficiently protected the liver-kidney functions of diabetic mice. EGCG was found to bind α-amylase, PTP1B, and α-glucosidase with good affinities ranging from -6.1 to -8.4 kcal/mol. The findings revealed that EGCG administration induced attractive curative effects on diabetic mice, particularly in terms of liver-kidney function. EGCG can, therefore, be considered as a potential strong candidate for future applications to treat and alleviate diabetic burden. Its pharmacokinetics, high affinities, and molecular interactions with the targeted receptors satisfactory explain the in vivo findings., Competing Interests: Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Riadh Badraoui reports financial support was provided by University of Hail., (Copyright © 2022 Elsevier B.V. All rights reserved.)