Abstract
The aim of this study was to evaluate the safety, tolerability and pharmacokinetics of single dose of Melissa officinalis extract which contained rosmarinic acid, including food-effects in healthy individuals. A total of eleven healthy individuals were randomly assigned to treatment arms in the two studies [Study 1 (fasted state) and Study 2 (fed state)]. Rosmarinic acid in serum was measured by a coulometric detection method using High-Performance Liquid Chromatography electrochemical detector. The serum concentration of total rosmarinic acid peaked at 1 hour after administration of Melissa officinalis extract containing 500mg rosmarinic acid in fasted state, with a maximum serum concentration 162.20 nmol/ L. The area under the curve for intact rosmarinic acid was calculated from the serum concentration-time profile to be 832.13 nmol • hour/ L. Food intake increases area under the curve and delayed time at which the maximum serum concentration. Rosmarinic acid supplementation did not affect liver, kidney, or blood cell function parameters. No adverse event was reported by any of the participants due to the study treatment. Single dose of Melissa officinalis extract containing 500 mg rosmarinic acid appears to be safe and tolerable in healthy individuals. Food intake increased the exposure of rosmarinic acid and delayed absorption of rosmarinic acid in healthy individuals.Trial RegistrationTrial Registration: UMIN-CTR UMIN000004997
Highlights
An estimated 24 million people worldwide have dementia, the majority of whom are thought to have Alzheimer’s disease (AD) [1]
With the exception of one, none of the participants withdrew before the end of the study; the withdrawing participant in the M. officinalis extract containing 100mg Rosmarinic acid (RA) arm in fasted state dropped out halfway through the study because of illness induced by insufficient sleep
Because no adverse effects were recorded in the other intervention periods in which he took M. officinalis extract containing 500 mg RA and placebo in fasted state, and M. officinalis extract containing 100 mg, 500 mg RA and placebo in fed state
Summary
An estimated 24 million people worldwide have dementia, the majority of whom are thought to have Alzheimer’s disease (AD) [1]. Continuing investigations of the pathogenic relationships of tau, Aβ, and AD suggest that oligomeric forms of Aβ play a seminal role in the disease causation [3, 4]. The most efficacious therapeutic agents would target the aggregation or neurotoxic activity of these structures. This suggestion is consistent with the fact that current AD treatments, which block brain acetylcholine degradation or N-methyl-D-aspartate receptors, are not preventive or curative and produce only modest and temporary symptomatic effects [5]. Rosmarinic acid (RA) is an ester of caffeic acid and 3,4-dihydroxiphenyllactic acid It has several interesting biological activities, e.g., antioxidant, anti-inflammatory, antimutagen, antibacterial, and antiviral [6]. With anti-oligomeric effect in our previous in vivo study [12], RA was very promising because it inhibited both Aβ oligomerization and Aβ deposition
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