5-Methoxytryptophol

Anti-Inflammatory Effects of Melatonin and 5-Methoxytryptophol on Lipopolysaccharide-Induced Acute Pulpitis in Rats

Aim: The aim of this study was to investigate the possible therapeutic impacts of two pineal hormones, melatonin and 5-methoxytryptophol (5-MTX), in a rat model of acute pulpitis by analyzing biochemical and histopathological parameters. Methods: This research was done using 32 male and female Wistar albino rats with weight between 200 and 250 g. The rats were randomly divided into four groups: a control group (rats without any treatment), acute pulpitis (AP) group, AP+melatonin group, and AP+5-MTX group. In the AP-induced groups, the crowns of the upper left incisors were removed horizontally. Lipopolysaccharide solution was applied to the exposed pulp tissue before the canal orifices were sealed with a temporary filling material. Melatonin (10 mg/kg) and 5-MTX (5 mg/kg) were administered intraperitoneally. The rats were sacrificed 24 hours after pulp injury, and trunk blood and pulp samples were collected. The concentrations of TNF-α, IL-1β, MMP-1, and MMP-2 in sera and pulp samples were determined using ELISA assay kits. Results: TNF-α, IL-1β, MMP-1, and MMP-2 levels in the serum and pulp tissues were considerably higher in the AP group than the control group (p < 0.01-0.001). In the AP+melatonin and AP+5-MTX groups, TNF-α, IL-1β, MMP-1, and MMP-2 levels in the serum and pulp tissues were significantly lower than in the AP group (p < 0.05-0.001). Conclusions: Both melatonin and 5-MTX provided protective effects on acute pulpitis, which indicates they may be promising as a therapeutic strategy for oral disease.

Daylight is critical to preserve 5-methoxytryptophol levels in suspected and confirmed COVID-19 patients

Declared as a pandemic by the World Health Organization, COVID-19 causes damage to tissues with the cytokine storm. It even causes death in people who are fond of it. In this case, the role of the immune system is vital. In particular, the cycle of melatonin and 5-methoxytryptophol released from the pineal hormone ensures that immunity continues for 24 h. While 5-MTX is active in sunlight, melatonin secretion increases in the dark at night. 5-MTX, like melatonin, has shown antioxidant and immunomodulatory properties in studies. Therefore, people who are sick and those who are not must strictly comply with the 24-h circadian rhythm during this period. We think that it is crucial in terms of being protected from the disease that we should carry out our activities according to the circadian rhythm.

THE METABOLISM OF 5-METHOXYTRYPTOPHOL

A new role for 5-methoxytryptophol on bone cells function in vitro

The present study investigates the direct action of 5-methoxytryptophol (5-MTX) in both MC3T3-E1 and RAW264.7 cells and compares it with melatonin (MEL), another 5-methoxyindol known to play a significant role on bone metabolism. We first screened increasing doses of both 5-MTX and MEL to determine their effect on metabolic activity and viability of preosteoblastic MC3T3-E1 cells. The optimal dose was used to determine its effect on differentiation of MC3T3-E1 cells and preosteoclastic RAW264.7 cells. Finally, we investigated the mechanism of action by adding the melatonin receptor antagonist luzindole (LUZ) and detecting the immunostaining of phospho-ERK. In MC3T3-E1 cells, most of the 5-MTX doses reduced slightly the metabolic activity of osteoblasts compared with the control, while MEL only decreased it for the highest dose (2.5 mM). As regards to cytotoxicity, low doses (0.001-0.1 mM) of both indoles showed a protective effect on osteoblasts, while the highest dose of MEL showed a higher cytotoxicity than the 5-MTX one. After 14 days of cell culture, Rankl mRNA levels were decreased, especially for 5-MTX. 5-MTX also induced a higher osteocalcin secretion and mineralization capacity than MEL. In RAW264.7 cells, 5-MTX decreased the number of osteoclast formed and its activity whereas MEL did not affect significantly the number of multinucleated TRAP-positive cells formed and showed a lower activity. Finally, MEL and 5-MTX promoted activation of the ERK1/2 pathway through the phosphorylation of ERK, while LUZ addition suppressed this effect. In conclusion, the present study demonstrates a new role of 5-MTX inhibiting osteoclastogenesis and promoting osteoblast differentiation.

Physiological and pharmacological properties of 5-methoxytryptophol

5-methoxytryptophol (5-ML) is a pineal indoleamine derived from serotonin shown to be biologically active in a number of species. This indolamine exhibits a circadian pattern synchronized with the day-night cycle with significant increases during daylight, already recognized in vertebrates. The multiplicity of physiological and endocrine functions of 5-ML is remarkable; it is involved in circadian rhythms, reproduction and sexual processes. Furthermore, a number of pharmacological benefits of 5-ML have been reported, including immunomodulatory, antitumor and antioxidative activities. However, the molecular mechanisms of these pharmacological effects remain unclear. The purpose of this article is to provide an overview on the general properties and physiological functions of 5-ML. An attempt has been made to fully document all studies performed using 5-ML. In addition, this article aims to gain insight into the current state of knowledge regarding pharmacological and therapeutic effects of this indoleamine.