Pachysandra (the family Buxaceae) is a small genus containing medicinal plants. This brief communication first describes its phytochemistry and pharmacological activities. More than 140 metabolites were separated, and steroidal alkaloids-based pregnane skeletons were the main compounds obtained. (+)-Axillaridine A, epipachysamines B and D-E, pachysandrines B-D, pachysamines A-B, pachystermine A, and (+)-spiropachysine are likely primary metabolites. Various compounds were identified as previously undescribed compounds. Non-alkaloids, such as sterols, triterpenoids, mono-phenols, coumarins, megastigmanes, and lignans, were also identified. Pachysandra steroidal alkaloids showed potential for drug development as they exhibited anticancer, antimicrobial, antiestrogenic, and gastric protective activities. The amine substituents at carbons C-3 and C-20 might cause differences in pharmacological results. The underlying mechanisms, such as the PI3K/Akt/mTOR signaling pathway, were proposed to explain pharmacological activities. Pachysandra phytotoxins exhibited antioxidative and antidiabetic activities. Synthetic products of Pachysandra steroidal alkaloids had higher cytotoxic effects than the natural compounds.