(R1671) Anti-cancer effects of periplognenin, levistolide A and scutellarin in vitro and in vivo

Jizhong Zhao (Jiangsu Normal University)| Shao Lee (Jiangsu Normal University)

Chemotherapy is one of major interventions against cancer. However, the therapeutic outcome is commonly unsatisfactory and more agents are required. Natural compounds provide a large pool of candidates for drug development. Periplogenin, levistolide A and scutellarin are chemically defined compounds derived from different herbs that have been used in China for treating cancer for long. In the present study, we investigated their anti-cancer effects in vitro and in vivo using HCT116 colon cancer cells as an experimental model. Both periplogenein and lesvitolide A inhibited cancer cell viability in a dose- and time-dependent manner, and caused apoptosis via ROS and ER stress pathways. They showed combinational effects in the induction of apoptosis, when used in combination with 5-fluorouracil or oxaliplatin. Scutellarin neither affect the cell viability nor triggered apoptosis of the cancer cell. However, it sensitized the cancer cells to apoptosis induced by 5-fluorouracil. In nude mice, periplogenein and lesvitolide A inhibited the cancer cell growth substantially when used alone. They also showed combinational growth inhibition effects when used in combination with 5-fluorouracil. In contract, scutellarin did not sensitize the cancer cells to the growth inhibitory effect of 5-fluorouacial or oxaliplatin. In conclusion, our results showed that periplogenein and lesvitolide A inhibited the colon cancer cell growth in vitro and in vivo, when used alone or in combination with clinical drugs, suggesting that they are candidates for colon cancer chemotherapeutic development.





Fig. 1 showed that PPG and LA but not SC inhibited the cell viability.
Fig. 2 showed that PPG and LA caused apoptosis via ROS production.
Fig .3 showed that PPG and LA caused apoptosis via ER stress.
Fig.4 showed that PPG or LA had combinational apoptotic effect when used with 5-FU or OXA. PPG: Periplogenin; LA: Levistolide A; 5-FU: 5-fluorouracil; OXA: Oxaliplatin; SC: Scutellarin
Fig. 5 showed that SC sensitized apoptosis by 5-FU.
Fig. 65 showed that PPG alone inhibited the cancer cell growth in nude mice, It had combinational effect when used with 5-FU.
Fig. 7 showed that LA alone inhibited the cancer cell growth in nude mice, It had combinational effect when used with 5-FU.
Fig. 8 showed that SC did not sensitize the growth inhibition effect of 5-FU or OXA. PPG: Periplogenin; LA: Levistolide A; 5-FU: 5-fluorouracil; OXA: Oxaliplatin; SC: Scutellarin.