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Ginsenosides (mainly, dammarane saponins) and dammarane sapogenins are main active ingredients in ginseng, and exhibit various anti-cancer activities in in-vitro cell cultures, animal models and human studies.
Through comprehensive review of hundreds of publications in the past 10 years, we have discovered a general law which applies to most, if not all, ginsenosides.
- Protopanaxatriol-type ginsenosides (Rg1, Rg2, Re) can be metabolized into aglycone protopanaxatriol (dammarane sapogenin PPT) after glucose cleavage from side chains, and protopanaxadiol-type ginsenosides (Rb1, Rb2, Rd, Rg3, compound K, Rh2) are converted into aglycone protopanaxadiol (PPD) correspondingly.
- With the cleavage of side-chain glucose moieties, the anti-cancer activity of ginsenosides increase, with the strongest anti-cancer activity attributed to PPD.
- In general, the anti-cancer activity of PPD-type ginsenosides is greater than those PPT-type ginsenosides.
- The ranking of specific ginsenosides or dammarane sapogenins is: PPD>compound K and Rh2 > Rb1 > Rg3 > PPT > Rg1.
- In cell cultures, the minal concentration to trigger apoptosis of various cancer cells (e.g., lung cancer, hepatocellular cancer, lymphoma, pancreatic cancer, leukemia, glioma, breast cancer, prostate cancer, etc.) is ~ 10ug/ml for PPD. The concentration of 1~5ug/ml PPD can cause cell division arrest in most cancer cells.
- In animal tumor models, the effective PPD dose for tumor growth inhibition is 60～200mg/kg, converted into 5～20mg/kg for human body.
- Oral ginsenosides, especially dammarane sapogenins, at the dose of 600mg～2000mg/day could deliver perceptible benefits to cancer patients.
