Planta Med 2012; 78 - OP13
DOI: 10.1055/s-0032-1307491

Phytochemical, Pharmacological and Preclinical Investigation of Indole Alkaloids

XH Cai 1, T Feng 1, XN Li 1, YP Liu 1, Y Li 1, JH Shang 2, JK Wang 2, XD Luo 1
  • 1State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, People's Republic of China
  • 2Yunnan Institute of Medica Material, Kunming 650111, PR China

Alkaloids represent a highly diverse group of compounds that are related by the presence of a nitrogen atom in a heterocyclic ring. Plants are estimated to produce approximately 12,000 different alkaloids, and they can be organized into groups according to their carbon skeletal structures. Among them, Indole alkaloids might account for a quarter of this large group of natural products. Both their highly complex chemical structures and pronounced pharmacological activity have made research on alkaloids, including elucidation of their biosynthetic pathways, very attractive for many decades.

In our investigation in natural indoles from plants, 80 new compounds were isolated, in which 7 represented new subgroup skeleton. 10 compounds exhibited potent cytotoxicity against five human cancer cell lines, using the MTT assay method in vitro. Additionally, the bioactive compounds inhibited tubulin polymerization significantly.

Indole alkaloids from Alsotonia scholaris are valuable leads for the treatment of respiratory diseases in pharmacological studies. Then, total indole alkaloids from A. scholaris have been approved for clinical trials (phase I and II) by SFDA of China based on results of a serial of preclinical investigation.