Abstract

Two new steroidal alkaloids, named hookerianine A (1) and hookerianine B (2) were isolated from the stems and roots of Sarcococca hookeriana Baill., along with two known compounds, sarcorucinine G (3) and epipachysamine D (4). On the basis of spectroscopic methods and by comparison with literature data, their structures were determined. As well as X-ray crystallography was performed to confirm compound 4. To identify novel antitumor inhibitors, all compounds were performed a CCK-8 assay against five human cancer cell lines SW480, SMMC-7721, PC3, MCF-7 and K562 in vitro. Compound 2 exhibited moderate cytotoxic activities to all cell lines with IC50 values in the range of 5.97–19.44 μM. Compound 3 was the most effective one against SW480 and K562 cell lines with IC50 values of 5.77 and 6.29 μM, respectively.

Highlights

  • The Sarcococca genus (Buxaceae) consists of about 20 species, widely distributed in the southwestern region of China and other south Asian countries [1]

  • The IC50 values of four compounds against five human cancer cell lines: SW480, SMMC-7721, PC3, MCF-7 and K562 are summarized in Table 2 (DDP and 5-FU was used as the positive control)

  • The relationships of compound 1 and 4 showed that steroidal alkaloids possessed a novel phenylacetyl structure-activity relationships of compound 1 and 4 showed that steroidal alkaloids possessed a group instead of benzoyl group located at C-3 can increase the cytotoxicity to human cancer cell lines: novel phenylacetyl group instead of benzoyl group located at C-3 can increase the cytotoxicity to

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Summary

Introduction

The Sarcococca genus (Buxaceae) consists of about 20 species, widely distributed in the southwestern region of China and other south Asian countries [1]. Previous investigations on several species of this genus indicated that steroidal alkaloids are the major chemical components with a broad spectrum of biological activities, such as cholinesterase inhibition [5,6,7], antitumor [8], antibacterial [9], antileishamanial [10], antidiabetic [11] and estrogen biosynthesis-promoting [12]. Dozens of steroidal alkaloids have been discovered from S. hookeriana of Nepal [13,14,15,16,17], there were few phytochemical or biological studies on this species which grows in China. Enlightened by the diverse bioactivities of steroidal alkaloids and the use of Sarcococca plants as folk medicine, S. hookeriana was chosen for searching antitumor agent by our research group and several cytotoxic steroidal alkaloids have been reported [18]. We describe the isolation, structure elucidation and cytotoxicity of the isolates

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