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Title:

A Novel Molecule Effective for Non-steroidal Anti-inflammatory Drug Induced Gastropathy

Value Proposition:

A hybrid molecule SEGA (Synthesized tryptamine- gallic acid) against Non-steroidal anti-inflammatory drugs (NSAID: painkiller) induced gastropathy.

It is well tried and tested in vitro where in it was understood that SEGA has special property of preventing radicals from entering the mitochondria which in-turn protects gastric mucosa from injury.

The synthesis and evaluation of gastroprotective effect of different tryptamine derivatives were done. Tryptamine derivatives have been synthesized by formation of amide or ester with some known anti oxidant molecules. These derivatives show excellent antioxidant property in vitro. Among all the derivatives the compound SEGA (3a), that was prepared by the combination of serotonin with gallic acid shows the greater antioxidant property than the other synthesized compounds both in vivo and in vitro. SEGA(3a) shows the gastroprotective effect against NSAIDs (indomethacin or diclofenac)-induced gastropathy in dose dependent manner and also accelerates the healing from injury. It prevents the NSAIDs-induced mitochondrial oxidative stress in vivo. 
This derivative prevents NSAID-induced mitochondrial oxidative stress-mediated apoptosis in vivo by preventing the activation of caspase 9 and caspase-3 and restores NSAIDs-mediated collapse of mitochondroial transmembrane potential and dehydrogenase activity. SEGA (3a) plays an important role as an iron chelator as well as intra mitochondrial ROS scavenger. Thus, SEGA (3a) is a potent antioxidant antiapototic molecule, which efficiently prevents NSAID-induced gastropathy and stress or alcohol-mediated gastric damage.

Summary Application:

A novel small molecule which can prevent gastro trouble arising from use of pain killers.

Tryptamine derivatives are useful as antioxidant and anti-apoptotic effect to prevent gastropathy/gastric mucosal injury induced by Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), stress and ethanol.

Advantages:

Discovered indigenously.
Safe and stable.
Immense therapeutic potential.

These derivatives can chelate free iron, prevent oxidative stress by scavenging ROS and simultaneously offer anti-apoptotic effect in vitro. 
These derivatives have the ability to prevent the formation of iron-mediated .OH as well as scavenge ROS in vivo. We have shown that these derivatives can prevent gastric mucosal oxidative stress and gastropathy by preventing ROS-mediated activation of apoptosis in gastric mucosal cells induced by NSAIDs. 
This invention provides a new small molecule having gastroprotective efficacy and a new strategy for drug discovery in gastropathy

Tech. Readiness Level:
CSIR-Indian Institute of Chemical Biology
CSIR-Indian Institute of Chemical Biology[CSIR-IICB]
:  director[at]iicb[dot]res[dot]in
:91-33-24730492
:https://iicb.res.in/
Industrial Applications: Formulations [Drugs and Pharmaceuticals]
Patent Application(s): 2173/DEL/2010