ReferenceID 3846
Selective cytotoxicity of the herbal substance acteoside against tumor cells and its mechanistic insights
Redox Biol
Natural products are characterized by extreme structural diversity and thus they offer a unique source for the identification of novel anti-tumor agents. Herein, we report that the herbal substance acteoside being isol
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- Reference Id
- 3846
- Evidence Id
- 20436
- Core Evidence Id
- 20436
- Source Reference Id
- 972
- Herb2 Reference Id
- HBREF001683
- Subject Paper Key
- HBIN014630_29505920
- Pubmed Id
- 29505920
- Doi
- 10.1016/j.redox.2018.02.015
- Paper Title
- Selective cytotoxicity of the herbal substance acteoside against tumor cells and its mechanistic insights
- Paper Abstract
- Natural products are characterized by extreme structural diversity and thus they offer a unique source for the identification of novel anti-tumor agents. Herein, we report that the herbal substance acteoside being isolated by advanced phytochemical methods from Lippia citriodora leaves showed enhanced cytotoxicity against metastatic tumor cells; acted in synergy with various cytotoxic agents and it sensitized chemoresistant cancer cells. Acteoside was not toxic in physiological cellular contexts, while it increased oxidative load, affected the activity of proteostatic modules and suppressed matrix metalloproteinases in tumor cell lines. Intraperitoneal or oral (via drinking water) administration of acteoside in a melanoma mouse model upregulated antioxidant responses in the tumors; yet, only intraperitoneal delivery suppressed tumor growth and induced anti-tumor-reactive immune responses. Mass-spectrometry identification/quantitation analyses revealed that intraperitoneal delivery of acteoside resulted in significantly higher, vs. oral administration, concentration of the compound in the plasma and tumors of treated mice, suggesting that its in vivo anti-tumor effect depends on the route of administration and the achieved concentration in the tumor. Finally, molecular modeling studies and enzymatic activity assays showed that acteoside inhibits protein kinase C. Conclusively, acteoside holds promise as a chemical scaffold for the development of novel anti-tumor agents.
- Journal
- Redox Biol
- Publish Year
- 2018
- Experiment Subject
- mouse
- Experiment Type
- Animal Experiment
- Phenotype Related
- Paper Title Cn
- Paper Title En
- Selective cytotoxicity of the herbal substance acteoside against tumor cells and its mechanistic insights
- Bilingual Status
- semi_complete