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Constituents from Entada scandens with TRAIL-resistance Overcoming Activity
Abstract:
Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) has emerged as a promising anticancer agent because of its ability to selectively kill tumor cells. But TRAIL-resistance is a major problem of its therapy. A search for compounds for abrogating TRAIL-resistance has, thus, become an important strategy for anticancer drug discovery. In search of bioactive natural products for overcoming TRAIL-resistance, we previously reported some compounds with TRAIL-resistance overcoming activity. Bioassay guided fractionation of Entada scandens led to the isolation of four compounds (1-4). Of the isolates, compounds 1 and 3 showed moderate TRAIL-resistance overcoming activity in TRAIL-resistant human gastric adenocarcinoma (AGS) cells.
Insights
Researchers explored natural products to overcome cancer therapy resistance. Compounds from Entada scandens showed moderate activity in overcoming tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) resistance in gastric cancer cells.
Area of Science:
- Natural Product Chemistry
- Cancer Biology
- Pharmacology
Background:
- Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) is a promising anticancer agent due to its selective tumor cell-killing ability.
- TRAIL resistance significantly hinders its therapeutic efficacy, necessitating the discovery of novel compounds to overcome this challenge.
- Natural products represent a valuable source for identifying bioactive compounds with potential anticancer properties.
Purpose of the Study:
- To identify natural products capable of overcoming TRAIL resistance in cancer therapy.
- To investigate the TRAIL-resistance overcoming activity of compounds isolated from Entada scandens.
Main Methods:
- Bioassay-guided fractionation of the plant extract Entada scandens.
- Isolation and characterization of four compounds from the plant.
- Evaluation of the isolated compounds' activity in overcoming TRAIL resistance using TRAIL-resistant human gastric adenocarcinoma (AGS) cells.
Main Results:
- Four compounds (1-4) were isolated from Entada scandens.
- Compounds 1 and 3 demonstrated moderate activity in overcoming TRAIL resistance.
- The activity was observed in TRAIL-resistant human gastric adenocarcinoma (AGS) cells.
Conclusions:
- Entada scandens is a source of compounds with TRAIL-resistance overcoming potential.
- Compounds 1 and 3 show promise as lead compounds for developing strategies to enhance TRAIL-based cancer therapy.
- Further research is warranted to explore the mechanisms and optimize the efficacy of these compounds.
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