LPS-induced oxidative inflammation and hyperlipidemia in male rats: The protective role of Origanum majorana extract

The antimicrobicidal activity of the phenolic compounds in the methanolic extract of Origanum majorana was recommended. The present study aimed to investigate the protective effect of Origanum majorana against LPS-induced toxicity in rats. Forty-eight male Sprague-Dawley rats were randomly divided into four equal groups, with 12 rats each group. Group C was used as control, while group E was treated with plant extract orally for 10 days (0.5 mg/kg/day). Group I was given LPS at a single i.p. dose (10 mg/kg BW) and group E + I was treated with plant extract (0.5 mg/kg/day) for 10 days, followed by a single i.p. dose of LPS (10 mg/kg BW). The WBC count and the number of macrophages in addition to the nitric oxide level in the peritoneal fluid were determined. Also, the lipids profile and the levels of urea and creatinine were detected. In addition, the MDA, glutathione and total proteins, as well as AST and ALT activities, were measured in all groups. The results indicated that the LPS injection caused significant decrease in the WBC count, hepatic glutathione and the total proteins, as well as serum HDL-c. On the other hand, LPS injection showed significant increase in the number of peritoneal macrophages, the levels of nitric oxide and MDA. Moreover, the total lipids, total cholesterol, triglycerides, urea, and creatinine concentrations, as well as AST and ALT activities, were significantly elevated. The pretreatment with Origanum majorana extract prior to LPS antagonized and alleviated its toxic effects in the treated animals. The results indicated that the treatment with Origanum majorana extract alone did not affect the tested parameters, except the number of peritoneal macrophages, which were significantly decreased

5-(5-Aryl-1,3,4-oxadiazole-2-carbonyl)furan-3-carboxylate and New Cyclic <em>C</em>-Glycoside Analogues from Carbohydrate Precursors with MAO-B, Antimicrobial and Antifungal Activities

Cyclization of acyclic <em>C</em>-glycoside derivatives <strong>1a,b</strong> to <strong>2a,b</strong> as the major isomers, and <strong>4a,b</strong> as the minor isomers were carried out. The isopropylidene derivatives <strong>3a,b</strong> were prepared, as well as the hydrazide derivative <strong>6</strong>, which was condensed with a variety of aldehydes to give hydrazones <strong>7a–e</strong> which were also prepared from the compounds <strong>12a–e</strong>. Acetylation of <strong>7a,d</strong> gave the corresponding acetyl derivatives <strong>8a,d</strong>, respectively. In addition, the dicarbonyl compound <strong>9</strong> was prepared in the hydrate form, which reacted with a number of aroylhydrazines to give the corresponding bisaroyl-hydrazones <strong>10a–d</strong>, which were cyclized into 1,3,4-oxadiazoles <strong>11a–d</strong>. Furthermore, two of the prepared compounds were examined to show the ability to activate MAO-B. In addition a number of prepared compounds showed antibacterial and antiviral activities

Synthesis and Biological Evaluation of New Imine- and Amino-Chitosan Derivatives

N-substituted chitosan derivatives were synthesized through condensation with a number of selected aryl and heteroaryl aldehydes. The synthesis of the amino-derivatives has been carried out by reductive amination with sodium borohydride as reducing agent. Their structures were characterized by (FT-IR, 1HNMR, and XRD). The antimicrobial activity of Chitosan Schiff’s base (CSB) derivatives were investigated against four types of bacteria and two crop-threatening pathogenic fungi, and the results indicated that the antibacterial and antifungal activities of the investigated derivatives are very promising. Additionally, different concentrations of the triazolo-Schiff’s base derivative 3c were used for cytotoxicity screening against Human Breast Adenocarcinoma Cells (MCF-7), Human Colon Carcinoma Cells (HCT-116), and Human Hepatocellular Liver Carcinoma Cells (HepG-2), and the obtained data revealed that the examined compounds have an excellent cell growth inhibitory effects on the cell lines as compared to standard

Potential anti-proliferative activity of Salix mucronata and Triticum spelta plant extracts on liver and colorectal cancer cell lines

Abstract Cancer’s etiology is linked to oxidative stress. As a result, it's vital to find effective natural antioxidant remedies. Salix mucronata and Triticum spelta plant extracts were prepared using five different solvents and examined for their cytotoxicity against liver HepG2 cancer cell line. It was found that Salix mucronata ethanolic extract is high in antioxidant mediated anti-cancer activity. The functional constituents (phenolic and flavonoids) as well as preparation of different ethanolic concentrations used to study their properties that include DPPH, oxygen, hydroxyl, nitrogen radical scavenging activities, ferric reducing power and metal chelating activities. The MTT assay was used to determine antioxidant-mediated anti-cancer activity against human liver (HepG2) and colorectal (Caco-2) cancer cells to calculate the half-maximal growth inhibitory concentration (IC50). Moreover, flow cytometry analysis was used to quantify the apoptotic effect on the treated cancer cells. Additionally, qRTPCR of p53, BCL2, Cyclin D, MMP9 and VEGF were measured. Furthermore, HPLC was used to assess the most effective ingredients of the plant extract. Salix mucronata 50% ethanol extract had the highest polyphenolic content, anti-oxidant, and anti-proliferative activity. Salix mucronata increased the number of total apoptotic cells, and caused an upregulation of p53 gene expression by more than five folds and a downregulation of gene expression level of BCL2, Cyclin D, MMP9 and VEGF by more than five folds. Consequently, that could modulate oxidative stress and improve the effectiveness of cancer therapy. Results, also, showed that Triticum spelta ethanolic extract was less effective than Salix mucronata. Therefore, Salix mucronata ethanolic extract represents promising surrogate natural therapy for apoptosis-mediated cancer and recommended for further investigation using animal model

Synthesis of New 1,3,4-Thiadiazole and 1,2,3,4-Oxathiadiazole Derivatives from Carbohydrate Precursors and Study of Their Effect on Tyrosinase Enzyme

5-(1,2,3,4-Tetrahydroxybutyl)-2-methylfuran-3-carbohydrazide (<strong>2</strong>) was condensed with a variety of ketones to afford carbohydrazide derivatives <strong>3</strong>–<strong>6</strong>. Acetylation of <strong>3</strong>–<strong>5</strong> afforded the acetyl derivatives <strong>7</strong>–<strong>9</strong>, while periodate oxidation of <strong>3</strong>–<strong>6</strong> afforded the formyl derivatives <strong>10</strong>–<strong>13</strong>. Acid catalyzed condensation of thiosemicarbazide or <em>o</em>-tolylthiosemicarbazide with the prepared aldehydes <strong>10</strong>–<strong>12</strong> gave thiosemicarbazone derivatives <strong>14</strong>–<strong>19</strong>. Cyclization of the latter with acetic anhydride afforded 4,5-dihydro-1,3,4-thiadiazolyl derivatives <strong>20</strong>–<strong>25</strong>. On the other hand, condensation of <em>p</em>-tosylhydrazine with the prepared aldehydes <strong>10</strong>–<strong>12</strong> afforded <em>p</em>-tosylhydrazone derivatives <strong>26</strong>–<strong>28</strong>. Cyclization of <strong>26</strong>–<strong>28</strong> with acetic anhydride afforded 1,2,3,4-oxathiadiazole derivatives <strong>29</strong>–<strong>31</strong> respectively. Moreover, the obtained results regarding to the effect of some of the prepared compounds on tyrosinase enzyme showed that the majority of these compounds having an inhibitory effect; especially compounds <strong>12</strong>, <strong>16</strong>, <strong>17</strong>, and <strong>28</strong>