Anthraquinones constitute an important class of natural and synthetic compounds with a broad scope of pharmacological including anti-bacterial, antioxidant, laxative, anti-tumor and other activities. Physcion and physcion 8-O-β-glucopyranoside (PG) are common anthraquinones existed in various plants. Emerging studies suggested that physcion and PG not only exert anti-tumor, anti-microbial, anti-inflammatory, anti-oxidant, optical-related, enzyme inhibitory, lipid regulation and neuroprotective activities, but also lead to hepatotoxicity, renal toxicity and genetic damage. Besides, a growing number of pharmacokinetics researches of physcion and PG also have been conducted. However, no review of physcion or PG have been published by now, so the aim of present review is to give a comprehensive summary and analysis of the pharmacology, toxicity and pharmacokinetics of physcion and PG by consulting all the currently available literatures published in PubMed then give a future prospects about it.