Abstract

Tupistra chinensis is widely distributed in southwestern China and its rhizome is a famous folk medicine for the treatment of carbuncles and pharyngitis. Its chemical identity of potent antiproliferative and anti-inflammatory constituents has been carried out in this study. Twenty-three polyhydroxylated spirostanol saponins, including nine novels, were isolated and identified. The new spirostanol saponins were elucidated as spirost-25(27)-en-1β,2β,3β,4β,5β-pentol-2-O-β-D-xylopyranoside (1), spirost-25(27)- en-1β,2β,3β,4β,5β-pentol-2-O-α-L-arabinopyranoside (2), spirost-25(27)-en- 1β,3α,5β-triol (12), spirost-25(27)-en-1β,3α,4β,5β,6β-pentol (13), spirost-25(27)-en- 1β,2β,3β,5β-tetraol-5-O-β-D-glucopyranoside (16), 5β-spirost-25(27)-en-1β,3β-diol- 3-O-β-D-glucopyranosyl-(1 → 4)-β-D-glucopyranoside (17), (25R)-5β-spirostan- 1β,3β-diol-3-O-β-D-glucopyranosyl-(1 → 6)-β-D-glucopyranoside (18), (25R)-5β- spirostan-1β,3β-diol-3-O-β-D-fructofuranosyl-(2 → 6)-β-D-glucopyranoside (19), 5β-spirost-25(27)-en-3β-ol-3-O-β-D-glucopyranosyl-(1 → 4)-β-D-glucopyranoside (20). The antiproliferative effects against seven human cancer cell lines and inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in a macrophage cell line RAW 264.7 were assayed for all the isolated compounds. Compounds 17, 19 and 21 exhibited potential antiproliferative activities against all of human cancer cell lines tested. Compounds 21 showed significant inhibition on NO production with IC50 values of 11.5 μM. These results showed that the spirostanol saponins isolated from the dried rhizomes of T. chinensis have potent antiproliferative and anti-inflammatory activities and T. chinensis might be used as anticancer and.anti-inflammatory supplement.

Highlights

  • Tupistra chinensis is widely distributed in southwestern China and its rhizome is a famous folk medicine for the treatment of carbuncles and pharyngitis

  • Medicinal plants have been used for treating human diseases and they produced a large variety of secondary metabolites such as alkaloids, flavonoids, triterpenoids and steroidal glycosides1

  • In the course of our continuing search for bioactive leading compounds from the medicinal herbs, we focused on steroidal saponins from the dried rhizomes of T. chinensis and obtained twenty-three polyhydroxylated spirostanol saponins including nine new compounds

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Summary

Introduction

Tupistra chinensis is widely distributed in southwestern China and its rhizome is a famous folk medicine for the treatment of carbuncles and pharyngitis. Compounds 21 showed significant inhibition on NO production with IC50 values of 11.5 μM These results showed that the spirostanol saponins isolated from the dried rhizomes of T. chinensis have potent antiproliferative and anti-inflammatory activities and T. chinensis might be used as anticancer and. Steroidal glycosides as the important secondary metabolites of medicinal plants have been reported to possess a wide range of biological activities including anticancer, anti-inflammatory, platelet aggregation inhibition, antihypertensive, cholesterol lowering, antifungal and antiviral. Tupistra chinensis is widely distributed in southwestern China and its dried rhizome is a famous folk medicine for the treatment of carbuncles and pharyngitis. Previous phytochemical investigations on T. chinensis have led to the isolation of a variety of biologically active compounds, including steroidal www.nature.com/scientificreports/. Steroidal saponins that consist of spirostanol saponins and furostanol saponins were the most abundant active constituents in T. chinensis

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