Objective: To study the structures and cytotoxic activity of sesquiterpene from Kadsura heteroclite rhizome. Method: Dried rhizomes of K. heteroclite rhizome were smashed and extracted with 95% ethanol for three times (150 L×1 h×3). The ethanol extract was concentrated and separated with water through polyamide chromatography into 30% ethanol

60% ethanol and 95% ethanol

respectively. The eluate of 30% ethanol was separated by MCI chromatography with water into 30% ethanol

50% ethanol

and 95% ethanol

respectively. The 50% ethanol was enriched sesquiterpenes. With methanol and water as mobile phase

MPLC was used to separate sesquiterpenes

and TLC and HPLC were used to combine the components. The components containing sesquiterpenes were separated with HPLC into monomeric compounds

which were by ESI-MS and NMR. Result: In vitro antitumor screening suggests that 8 sesquiterpenes were isolated from the plant and identified as 1α-hydroxy-9-deoxycacalol (1)

balsamiferine B (2)

balsamiferine D (3)

chaetopenoid A (4)

chaetopenoid B (5)

asterothamnone A (6)

asterothamnone B (7)

and 10-dehydroxy-melleoliede B (8). Compounds 2

6

7 exhibited a cytotoxic activity against SMMC7721

with IC50 values of 10.6

9.5

15.5 μmol·L-1

respectively. Conclusion: Compounds 1-8 were obtained from Kadsura for the first time.