Anti-colon cancer activity of amino acid ester betulinates: Apoptosis induction and IL1B gene expression in PBMCs by the lead compound
Betulinic acid (BA) is a natural pentacyclic triterpenoid with significant pharmaceutical potential. We found that converting BA into amino acid ethyl ester salts alters its cytotoxic effect on colorectal adenocarcinoma cells (HT-29). Among these salts, the estimated half-maximal inhibitory concentr...
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| Main Authors: | , , , , , , , |
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| Format: | Book |
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Pensoft Publishers,
2024-11-01T00:00:00Z.
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| Online Access: | Connect to this object online. |
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| Summary: | Betulinic acid (BA) is a natural pentacyclic triterpenoid with significant pharmaceutical potential. We found that converting BA into amino acid ethyl ester salts alters its cytotoxic effect on colorectal adenocarcinoma cells (HT-29). Among these salts, the estimated half-maximal inhibitory concentration (IC50) at 72 h varies by up to fifteenfold. The proline ethyl ester [ProOEt] salt, the most active compound, exhibited an IC50 value of 3.8 µM, which is 4.8 times lower than that of the parent BA. We observed that exposure to BA or [ProOEt][BA] induced apoptosis in HT-29 cells. Additionally, the proline-based salt led to a higher level of IL1B gene expression in PBMCs at a lower stimulation concentration. |
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| Item Description: | 10.3897/pharmacia.71.e136454 2603-557X |