The mechanism of anestrus in rats treated with losulazine, a peripheral sympatholytic antihypertensive agent, was investigated by determining its effect on hypothalamic catecholamines and serum sex hormones and by evaluating the influence of bromocriptine on the reproductive functions of rats tr...
Losulazine, a hypotensive agent, was given orally by gastric intubation to Sprague-Dawley rats in doses of 0, 2, 4, or 8 mg/kg/day in a study of fertility and general reproductive performance. Eighteen males per group were treated for 67 days before cohabitation, then daily until killed. Thirty-...
Losulazine hydrochloride, an antihypertensive agent, was administered intraperitoneally to adult male Wistar rats in doses of 1, 2 and 5 mg/kg/day for 1 seminiferous epithelium cycle to determine its effects on testicular steroidogenesis, spermatogenesis and accessory sex gland function. Adminis...
Different benzylidene derivatives (15a-o and 16a-o) of betulinic acid were designed and synthesized in an effort to develop potent anticancer agents. All the synthesized derivatives along with betulinic acid were evaluated for cytotoxicity against a panel of five different human cancer cell line...
Carbonic anhydrase enzymes (EC 4.2.1.1, CAs) are metalloenzyme families that catalyze the rapid conversion of H2O and CO2 to HCO3– and H+. CAs are found in different tissues where they participate in various significant biochemical processes such as ion transport, carbon dioxide respiration, ur...
A new series of octadec-9-enoic acid schiff base entities (S1-S30) were designed and synthesized targeting peroxisome proliferator activated receptor-gamma for agonist action. Molinspiration software (online) was used to estimate drug like molecular properties of the metabolites. Docking disquis...
Tyrosinase enzyme plays a crucial role in melanin biosynthesis and enzymatic browning process of vegetables and fruits. A series of veratric acid derivatives containing benzylidene-hydrazine moieties with different substitutions were synthesized and their inhibitory effect on mushroom tyrosinase...
Herein, we report photoluminescence properties by embedding a purely organic fluorophore into a polymer matrix. Biopolymer-polylactic acid [PLA] doped with bischalcone, [1, 3-bis (4-bromobenzylidene) cyclohexan-2-one] is found to show exciting properties for applications in optoelectronics. This...
Electrochemical measurements as well as the weight loss method were investigated to determine the mechanism and performance of inhibition of (Z) -4 - ((2-bromobenzylidene) amino) -5-methyl-2-4-dihydro -3H-1,2,4-triazole-3-thione (2i) and (Z) -4 - ((3-bromobenzylidene) amino) -5-methyl-2-4-dihydr...
1-(4-Methoxyphenyl)-12-hydroxymethyl-p-carborane (2a), which is a precursor to the previously developed potent carborane-containing ER agonist BE120, exhibited weak cell growth inhibitory activity against four human cancer cell lines (MCF-7, MDA-MB-453, LNCaP, and PC-3). The biological evaluatio...
Using new experimental methods, 1-(4-chloro-3-nitrophenyl)-3-(2-methoxyphenyl) triazene, (CNPMPT) structure was synthesized in the laboratory. The structure has two E and Z conformational states that E is a more stable state than the Z. After synthesis of the structure, crystallization process w...
Tetrahydropyranylation of methyl-4-hydroxybenzoate proceeds with formation of its corresponding THP aromatic ether THP–O–p-C6H4CO2CH3 (1; THP = tetrahydropyranyl, C5H9O). Reaction with in situ generated carbanion of acetylferrocene gave the protected organometallic complex Fc–C(O)CHC(OH)(p-C6...
Technical lignins are structurally heterogeneous and polydisperse. This work describes the use of a simple and green method for lignin fractionation, using different proportions of acetone (40 and 60%) in water. Lignins from three different sources (wheat straw organosolv lignin, wheat straw sod...
Five polycyclic aromatic hydrocarbons (PAHs), benzo[a]pyrene (B[a]P), benzo[b]fluoranthene (B[b]F), dibenz[a,h]anthracene (DBA), 5-methylchrysene (5MC), and cyclopenta[cd]pyrene (CPP) were examined for their lung tumorigenic activities in strain A/J mice, their ability to form PAH-DNA adducts in...
DNA has been incubated in vitro with dibenz[a,h]anthracene (DB[a,h]A) and the related 5,6-diol and 3,4-diol in the presence of 3-methylcholanthrene- or Aroclor 1254-induced rat liver microsomes. After incubation, the DNA was extracted and examined for the presence of aromatic adducts using the n...
The formation of trans-dihydrodiols from dibenz[a,c]anthracene, dibenz[a,h]anthracene and chrysene by chemical oxidation in an ascorbic acid-ferrous sulphate-EDTA system and by rat-liver microsomal fractions has been studied using a combination of thin-layer (TLC) and high pressure liquid chroma...
An unequivocal synthesis of dihydrodiols of the mutagenic polycyclic aromatic hydrocarbon, dibenz(a,c)anthracene is described
The mutagenic activities of dibenz[a,c]anthracene (DB[a,c]A), and its 11 derivatives, including 3 diols, 6 phenols and 2 oxepines, were studied in the TA100 strain of Salmonella typhimurium at doses varying from 0 to 20 μg/plate in the presence of a rat-liver S9 (9000 × g) preparation. Among t...
Fluorescence spectroscopic techniques were developed and employed in the identification and quantitation of the metabolites of the carcinogenic pollutants 7H-dibenzo[c,g]carbazole (DBC) and dibenz[a,j]acridine (DBA) after HPLC separation. Metabolites formed in vitro with 3-methylcholanthrene (3-...
N-Heterocyclic polynuclear aromatics are widely-occurring environmental pollutants formed during the pyrolysis of nitrogen-containing organic chemicals. Dibenz[a,j]acridine (DBA), a member of this class, has been shown to be a skin carcinogen in mice. We undertook studies to determine the organ ...
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