Paris polyphylla Smith var. yunnanensis, has been used in traditional Chinese medicine for its antibiotic and anti-inflammatory properties; in addition it has been used to cure liver cancer in particular. In this current study, β-ecdysterone (1) and three pennogenin steroidal saponins (2-4) were isolated from the EtOH extract of Paris polyphylla var. yunnanensis, and then tested for their antitumor and antifungal activities. Spectroscopic data was used to confirm their structures. Their antitumor properties were determined by using an MTT assay in addition to ethidium bromide and acridine orange staining techniques. Compounds 2, 3 and 4 exhibited significant anti-proliferation activities against HepG2 cells, with IC50 values of 13.5 μM, 9.7 μM and 11.6 μM respectively, obtained following 48 h treatment. Furthermore, we found these pennogenin steroidal saponins could induce HepG2 cells apoptosis at a concentration of 20 μM after 48 h treatment. Compounds 2, 3 and 4 were confirmed to exhibit moderate antifungal activity. The minimum inhibitory concentration (MIC) of compounds 2, 3 and 4 against saccharomyces cerevisiae hansen were 2.5 mg.mL(-1), 0.6 mg.mL(-1) and 0.6 mg.mL(-1), respectively. The MIC of compounds 2, 3 and 4 against Candida albicans were 1.2 mgmL(-1), 0.6 mg.mL(-1) and 1.2 mg.mL(-1), respectively. The analysis of the bioactivity-structure relationship shows that the sugar moiety plays a critical role in the activity of steroid moiety. Our results suggest that these three pennogenin steroidal saponins could be utilized to develop anticancer medicines.
Keywords: Antifungal activity; Antitumor activity; Paris polyphylla var. yunnanensis; Pennogenin steroidal saponins.