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2000
Volume 32, Issue 42
  • ISSN: 0929-8673
  • E-ISSN: 1875-533X

Abstract

Introduction

Arjunolic acid, a well-known natural product with various medicinal properties, was isolated from the heartwood of . Various amides of arjunolic acid were synthesized using different aryl and cyclic amines, characterized, and evaluated for their anti-cancer activities at the National Cancer Institute (NCI).

Methods

All the derivatives were active against all the cell lines of NCI compared to the parent molecule arjunolic acid. Eight compounds were selected for dose-dependent activity based on the preliminary results. IC of selected eight compounds was evaluated. Based on IC values against various cell lines, compound was further investigated to understand the mechanism of action against HCT-116 and CT-26 colon cancer cell lines.

Results

Mechanistic studies of compound in these two cell lines demonstrated that compound arrested the colon cancer cells at the G/G phase. Compound -treated cells were also found to have an increased percentage of ROS compared to untreated cells. It induced apoptosis in both these cell lines.

Conclusion

Compound was found to inhibit cancer growth in the mice model and was very effective against all the cancer cell lines. Therefore, it could be used for further development to treat colon cancer.

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Amide Derivative of Arjunolic Acid TA-1,4-BiP Enhances ROS- mediated Apoptosis in Colorectal Cancer Cells
Curr. Med. Chem. 32, 9756 (2025); https://doi.org/10.2174/0109298673348718250109142630
/content/journals/cmc/10.2174/0109298673348718250109142630
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  • Article Type:     Research Article
Keyword(s): amides; apoptosis; arjunolic acid; colon cancer; synthesis; Terminalia arjuna

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