Paridis Rhizoma， a traditional valuable Chinese herbal medicine， has the functions of clearing heat and removing toxin， relieving edema and pain， cooling liver and calming convulsion， which can be used to treat various diseases such as mumps， abscess， burn， bleeding， and tumor. It has been used in folk medicine for a long time and is the main raw material of various Chinese patent medicines such as Gongxuening Capsules and Yunnan Baiyao. Polyphyllin Ⅰ， an isospirostanol saponin and one of the main active components in Paridis Rhizoma， is distributed in the rhizome， pericarp， and leaves of Paris polyphylla. With high polarity， polyphyllin Ⅰ is mainly extracted by n-butanol extraction and macroporous adsorption resin chromatography， separated by silica gel column chromatography and preparative high performance liquid chromatography， and purified with the combination of methods. With anti-tumor， anti-inflammatory， antibacterial， and anti-virus effects， it is generally employed to treat liver cancer， lung cancer， gastric cancer and other cancers as well as arthritis， influenza， sore toxin， and bacterial infection. However， polyphyllin Ⅰ may cause stomach irritation， hemolysis， liver damage， kidney damage， heart damage， and other adverse reactions. Pharmacokinetic studies show that it has problems such as low bioavailability and poor intestinal absorption and permeability， which affect the clinical application of polyphyllin Ⅰ. This paper summarizes the research on the plant sources， extraction and separation methods， pharmacological effects， adverse reactions， and pharmacokinetics of polyphyllin Ⅰ in recent years， which is expected to provide a reference for the rational clinical application and other in-depth research work of polyphyllin Ⅰ.