Abstract
Antioxidants are substances that can prevent or slow damage to cells caused by free radicals, unstable molecules that the body produces as a reaction to environmental and other pressures. Free radicals may play a role in heart disease, cancer and other diseases. If the body cannot process and remove free radicals efficiently, oxidative stress can result. This can harm cells and body function. Free radicals are also known as reactive oxygen species (ROS). In this research, Triptorelin® (TRP) conjugates of triphenylmethanol derivatives (TPMs) were synthesized to evaluate their in vitro lipid peroxidation potency. Comparative lipid peroxidation assays between TRP-TPMs conjugates and the corresponding TPMs derivatives were measured using thiobarbituric reactive substance (TBARS) in a dose- and time-dependent manner following the Fenton’s pathway. Overall, TBARS decreased between 20% - 30% for the treated samples of synthesized conjugates compared to their respective control physical mixtures. These data suggest that TRP-TPMs derivatives can be used to improve the biological activity of TRP.
Highlights
Triptorelin® (TRP) is a synthetic analogue of the gonadotropin-releasing hormone (GnRH), first reported in 1976
The thiobarbituric acid (TBA) test can be performed (a) by directly heating the sample with TBA followed by separation of the pink complex produced (b) by distillation of the sample followed by reaction of the distillate with TBA (c) by extraction of the lipid portion of the sample with organic solvents and reaction of the extract with TBA and (d) by extraction of MDA using aqueous trichloroacetic or perchloric acid and reaction with TBA
Heating during distillation enhances the degradation of existing lipid hydroperoxides and, additional MDA and other TBA-reactive substances (TBARS) may be formed even in the presence of metal chelators or phenolic antioxidants
Summary
Triptorelin® (TRP) is a synthetic analogue of the gonadotropin-releasing hormone (GnRH), first reported in 1976. TRP stimulates the pituitary secretion of FSH and LH, prolonged stimulation (constant concentration of TRP in the blood) of the pituitary causes insensitive to the ac-. This reduces the level of gonadotropin in the blood, resulting in decreased levels of sex hormones to postcastration or menopausal levels. In addition to the usual side effects of the agonist analogs of LH-RH, other reported adverse effects include transient hypertension, dry mouth, excessive salivation, paraesthesia and increased dysuria [1]
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