20(S)-protopanaxadiol (PPD), a dammarane-type aglycone generated from the intestinal metabolism of Panax ginseng saponins, has attracted increasing attention as a pharmacologically active natural compound. Over the past decade, accumulating evidence has revealed various pharmacological activities of PPD including anti-tumor, anti-inflammatory, neuroprotective, and anti-fibrotic effects. Mechanistically, these pharmacological activities are mediated through multiple molecular mechanisms, including the regulation of oxidative stress, control of apoptosis and autophagy, and modulation of immune. And the related signaling pathways include AMPK/mTOR, NF-κB, and TGF-β/Smad, among others. This review summarizes the current advances in the pharmacological activities and molecular mechanisms of PPD. In addition, the pharmacokinetic characteristics of PPD are discussed, including its intestinal metabolism, moderate oral bioavailability, hepatic biotransformation and species-specific differences. Besides, recent advances in drug delivery strategies are also discussed for their potential to improve the solubility and absorption of PPD. Collectively, by combining pharmacological and pharmacokinetic characteristics, this review provides comprehensive and updated medicinal property of PPD and offers a valuable scientific basis for the further development and clinical translation of PPD.
He et al. (Fri,) studied this question.