Tryptamine-Gallic Acid Hybrid Prevents Non-steroidal Anti-inflammatory Drug-induced Gastropathy

Abstract

Background: Non-steroidal anti-inflammatory drugs (NSAIDs) induce gastropathy by promoting mitochondrial pathology, oxidative stress, and apoptosis in gastric mucosal cells. Results: We have synthesized SEGA (3a), a tryptamine-gallic acid hybrid, which prevents NSAID-induced gastropathy by preventing mitochondrial oxidative stress, dysfunction, and apoptosis. Conclusion: SEGA (3a) bears an immense therapeutic potential against NSAID-induced gastropathy. Significance: This novel molecule is a significant addition in the discovery of gastroprotective drugs.

Synthesis and biological evaluation of primaquine–chloroquine twin drug: a novel heme-interacting molecule prevents free heme and hydroxyl radical-mediated protein degradation

“…The FRAP assay is based on the measurement of the ability of a substance to reduce Fe(III) to Fe(II); greater the reducing ability greater the antioxidant property. 2,3 Antioxidants reduce the colorless Fe (III)-TPTZ to a blue colored Fe (II)-TPTZ complex, which results in an increase in the absorbance at 595 nm giving a FRAP value. Higher FRAP value indicates greater reducing (i.e.…”

“…Iron chelating ability of PQCL at different concentrations was monitored by recording the absorbance of the Fe(II)-TPTZ complex immediately aer each addition in the quartz cells of 1 cm light-path in a Shimadzu UV/VIS spectrophotometer at 25 AE 1 C. The contents were mixed well before the spectrum was recorded. 2 Free radical scavenging activity in vitro (DPPH assay) 2,2-Diphenyl-1-picrylhydrazyl (DPPH) is a stable free radical that can accept hydrogen radical or an electron and become a stable diamagnetic molecule. The antioxidants can scavenge the DPPH by donating hydrogen as visualized by discoloration of the DPPH radical from purple to yellow.…”

“…1 Oxidative stress is a major contributing factor to the high mortality rates associated with several diseases, including malaria, gastropathy, cancer, diabetes, neuropathies, myopathies, cardiovascular disease, inammation, and hepatitis. [2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18][19] Although heme is an important molecule in human, 20 free heme is responsible for inammation, hemolysis and oxidative stress. 20 By generating reactive oxygen species (ROS) through oxidative stress, free heme induces toxic effects to tissues and organs.…”

Gallic Acid and Gallates in Human Health and Disease: Do Mitochondria Hold the Key to Success?

“…A tryptamine‐gallic acid derivative increases their stability in the serum and also exhibits promising gastroprotective effect against the NSAIDs. This is achieved through protecting mitochondrial membrane damage and respiratory capacity, inhibiting apoptosis with accelerated wound healing primarily by taking care of the mitochondrial ROS generation . Besides exhibiting antioxidant property, the prooxidative function of gallic acid is also augmented by a concomitant decrease in the cellular antioxidant enzymes including cytosolic and mitochondrial superoxide dismutases and thus accumulating ROS within the cellular milieu .…”

Association of Heme Oxygenase 1 with the Restoration of Liver Function after Damage in Murine Malaria by Plasmodium yoelii

“…The samples were centrifuged, and the absorbance of the supernatants was taken at 535 nm to measure the TBARS concentration. Tetraethoxypropane was considered the standard for this protocol (53)(54)(55)(56). For measurements of carbonylated proteins, a standard colorimetric method was followed as described previously (53,54,57).…”