Planta Medica Letters 2015; 2(01): e48-e51
DOI: 10.1055/s-0035-1557861
Letter
Georg Thieme Verlag KG Stuttgart · New York

Semi-Synthesis of Kaurenoic Acid Derivatives and Their In Vitro Cytotoxic Activities

Lei Zhang
1  Key Laboratory of Natural Drug Pharmacology in Fujian Province, School of Pharmacy, Fujian Medical University, Fuzhou, P. R. China
,
Fei Wang
1  Key Laboratory of Natural Drug Pharmacology in Fujian Province, School of Pharmacy, Fujian Medical University, Fuzhou, P. R. China
,
Xin-hua Ma
1  Key Laboratory of Natural Drug Pharmacology in Fujian Province, School of Pharmacy, Fujian Medical University, Fuzhou, P. R. China
,
Fang Zhou
1  Key Laboratory of Natural Drug Pharmacology in Fujian Province, School of Pharmacy, Fujian Medical University, Fuzhou, P. R. China
,
Sheng-mei Wen
1  Key Laboratory of Natural Drug Pharmacology in Fujian Province, School of Pharmacy, Fujian Medical University, Fuzhou, P. R. China
,
Tian-hua Zhong
2  Key Laboratory of Marine Biogenetic Resources, Third Institute of Oceanography, State Oceanic Administration, Xiamen, P. R. China
,
Quan-yu Liu
1  Key Laboratory of Natural Drug Pharmacology in Fujian Province, School of Pharmacy, Fujian Medical University, Fuzhou, P. R. China
,
Shi-wu Chen
3  School of Pharmacy, Lanzhou University, Lanzhou, P. R. China
,
Yong-hong Zhang
1  Key Laboratory of Natural Drug Pharmacology in Fujian Province, School of Pharmacy, Fujian Medical University, Fuzhou, P. R. China
› Author Affiliations
Further Information

Publication History

received 11 November 2014
revised 22 June 2015

accepted 09 July 2015

Publication Date:
06 November 2015 (online)

Abstract

The cytotoxic activities of the diterpene kaurenoic acid (1) and its 15 semi-synthesis derivatives were assessed on human cell cultures. The human tumor cells used comprised colon (SW620 and SW480), pancreatic (PANC-1 and BxPC-3), stomach (SGC-7901), esophageal (Eca-109), and leukemia (K562 and HL-60). Kaurenoic acid was inactive against the tumor cell lines; however, its derivatives which contain α,β-unsaturated ketone rendered compounds with cytotoxic activity. Compounds 514, 1719, and 24 with a substitution at the C-4 position showed significant inhibitory activity against the tested cell lines, while compound 3, without a substitution at the C-4 position, was slightly less active in these cell lines. The SW620 colon cancer cell was highly susceptible to all of the tested derivatives.

Supporting Information