UPLC/MS/MS method for quantification and cytotoxic activity of sesquiterpene lactones isolated from Saussurea lappa.

Saussurea lappa (Asteraceae) roots have been reputed for the usage in traditional medicinal systems of India, China and Japan for the treatment of various kinds of disorders such as anti-ulcer, anti-convulsant, anti-cancer, hepatoprotective, anti-arthritic and anti-viral activities. Compounds were isolated using a column chromatographic technique. The root extract, fractions and isolated compounds were tested for cytotoxicity against A549 (human lung carcinoma) and C-6 (rat glioma) cells using the Sulphorhodamine B assay. Chromatographic separations of active sesquiterpene lactones were accomplished on BEH-HSS-T3 column at 25°C. Phytochemical investigation of Saussurea lappa root extract resulted in the isolation of isoalantolactone (1), β-cyclocostunolide (2) α-cyclocostunolide (3), 4-hydroxy-3,5-dimethoxycinnamyl-9-O-β-D-glucopyranoside (4), sucrose (5), and alantolactone (6). Their structures were determined by spectroscopic means. Ethanolic extract, chloroform fraction, compounds 1, 2, 3 and 6 possessed significant activity against both tested cells. The quantification was performed using the transitions of m/z 233/105 for isoalantolactone and m/z 233/105 for alantolactone respectively. Costunolide and dehydrocostus lactone were also characterised by comparison of MS/MS fragmentation pattern. This is the first study on simultaneous quantification of isoalantolactone and alantolactone by the UPLC/MS/MS method in Saussurea lappa. Our study against A549 and C-6 cells showed higher cytotoxicity. It is suggested that roots of Saussurea lappa might be a potential source of anticancer compounds.

Kumar A ，Kumar S ，Kumar D ，Agnihotri VK ... -  《-》

Cytotoxic sesquiterpene lactones from the root of Saussurea lappa.

Sun CM ，Syu WJ ，Don MJ ，Lu JJ ，Lee GH ... -  《JOURNAL OF NATURAL PRODUCTS》

Sesquiterpene lactones from Saussurea involucrata.

Bioassay-directed separation of the ethyl acetate extract from the aerial parts of Saussurea involucrata (Kar. et Kir. ex Maxim) led to the isolation of three new sesquiterpene lactones sausinlactones A (1), B (2), C (3) and six known ones (4-9). The structures were established by spectroscopic data (UV, IR, HRESIMS, 1D and 2D NMR). CD technique was also employed to determine the absolute configurations of new compounds 1-3. The anti-inflammatory activities of compounds 1-9 and antitumor activities of new compounds 1-3 were tested. The results presented that compounds 5 and 6 were responsible for anti-inflammatory activities, and compounds 1 and 2 showed significant cytotoxic activities against A549 cells.

Xiao W ，Li X ，Li N ，Bolati M ，Wang X ，Jia X ，Zhao Y ... -  《-》

A new sesquiterpene lactone from the roots of Saussurea lappa: structure-anticancer activity study.

Robinson A ，Kumar TV ，Sreedhar E ，Naidu VG ，Krishna SR ，Babu KS ，Srinivas PV ，Rao JM ... -  《-》

Antitrypanosomal sesquiterpene lactones from Saussurea costus.

In the course of a larger screen of 1800 plant and fungal extracts, the ethyl acetate extract of Saussurea costus roots potently inhibited the growth of Trypanosoma brucei rhodesiense. Subsequent HPLC based activity profiling led to the identification of the sesquiterpene lactones arbusculin B (1), α-cyclocostunolide (2), costunolide (3), and dehydrocostuslactone (4). They were tested for in vitro antitrypanosomal activities and cytotoxicity alongside the structurally related sesquiterpene lactones parthenolide (5), zaluzanin D (6), and eupatoriopicrin (7), and had IC(50)s between 0.8 and 22 μM. Cytotoxic IC(50)s were from 1.6 to 19 μM, and selectivity indices from 0.5 to 6.5.

Julianti T ，Hata Y ，Zimmermann S ，Kaiser M ，Hamburger M ，Adams M ... -  《-》