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Isolation of two sesquiterpene glycosides from Gaertn. with cytotoxic properties and analysis of their mechanism based on network pharmacology. | LitMetric

AI Article Synopsis

  • Two sesquiterpene glycosides, Mukurozioside IIa and Mukurozioside IIb, were purified from *Gaertn.* and showed significant anti-tumor effects on breast cancer.
  • In experiments, these compounds inhibited three breast cancer cell lines (MCF-7, MDA-MB-231, and MDA-MB-435s) by about 80% at a concentration of 200 μg/mL, outperforming cyclophosphamide.
  • The study identified 22 relevant molecular targets related to their anti-cancer mechanism, suggesting that while effective, these compounds do not fully express the activity of their original parent fraction.

Article Abstract

The anti-tumor effects of two compounds purified from Gaertn. (.) on breast cancer were observed. Their chemical structures were identified as sesquiterpene glycosides, namely, Mukurozioside IIa and Mukurozioside IIb. The results of XTT assay indicated that their inhibition rates against three cancer cell lines (MCF-7, MDA-MB-231 and MDA-MB-435s) reached approximately 80% at a concentration of 200 μg/mL, which were higher than that of cyclophosphamide (below 40% at 200 μg/mL), and their 50% inhibiting concentrations were ranged from 120.73 to 154.01 μg/mL, indicating their inhibition were weaker than their parent fraction. Furthermore, the mechanism on breast cancer was predicted, and 22 targets including PTPN1, IL2 and VEGFA were relatively important. These results illustrated the anti-breast cancer activity of was related to the two compounds with the structure of sesquiterpene glycosides, but they did not represent the full activity of their parent fraction.

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Source
http://dx.doi.org/10.1080/14786419.2020.1713120DOI Listing

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