Undescribed amino acid-sesquiterpene lactone adducts and sesquiterpene glycosides from the roots of Saussurea lappa and their anti-HBV activity.

Saussurea lappa (Asteraceae family), a traditional Chinese medicine, has been found to possess anti-inflammatory, immune-promoting, antibacterial, antitumor, anti-HBV, cholestatic, and hepatoprotective activities. Herein, two undescribed amino acid-sesquiterpene lactone adducts, saussureamines G and H (1 and 2), and two new sesquiterpene glycosides, saussunosids F and G (3 and 4), along with 26 known sesquiterpenoids (5-30) have been isolated from the roots of S. lappa. Their structures and absolute configurations of these compounds were established by physical data analyses such as HRESIMS, IR, 1D and 2D NMR and ECD calculations. All isolated compounds were tested for anti-hepatitis B virus (anti-HBV) activity. Ten compounds (5, 6, 12, 13, 17, 19, 23, 26, 29, and 30) exhibited activities against the secretions of HBsAg and HBeAg. In particular, compound 6 showed inhibition of HBsAg and HBeAg secretion with IC50 values of 11.24 and 15.12 μM, with SI values of 1.25 and 0.93, respectively. Molecular docking studies were also conducted on the anti-HBV compounds. Overall, this study provides insights into the potential therapeutic uses of the compounds found in the roots of S. lappa, particularly in the treatment of hepatitis B virus infections.

Cong XY ，He JY ，Shu TY ，Chen H ，Feng Y ，Su LH ，Xu M ... -  《-》

Lappanolides A-N, fourteen undescribed sesquiterpenoids from Saussurea costus (Syn. Saussurea lappa) and their anti HBV activity.

Lappanolides A-N (1-14), 14 undescribed sesquiterpenoids, along with 23 known ones (15-37), were isolated from the roots of Saussurea costus, which were primarily categorized into eudesmane, guaiane, and germacrane types. Lappanolide A (1) possessed an unprecedented pseudo-disesquiterpenoids. Their structures and absolute configurations were established using physical data analyses (HRESIMS, IR, 1D and 2D NMR) and ECD calculations. All isolated compounds were tested for anti-hepatitis B virus (anti-HBV) activity. Ten compounds (1, 9, 11, 12, 19, 22, 28, 29, 31, and 36) exhibited activities against HBsAg secretions as determined by ELISA assay, with IC50 values ranging from 5.2 to 45.7 μM. In particular, compounds 28 and 29 showed inhibition of HBsAg secretion with IC50 values of 5.28 and 5.30 μM, and CC50 values of 9.85 and 6.37 μM, respectively, though they all exhibited low selectivity. Several compounds displayed cytotoxicity in the MTT assay. Among them, compound 28 was the most notable and was chosen for further study using flow cytometry. The result showed that it significantly induced HepG2 cell arrest in the S phase and induced apoptosis.

Li HB ，Bai SQ ，Shu TY ，Wang Q ，Chen H ，Su LH ，Xu M ... -  《-》

Structure-Based Molecular Networking for the Discovery of Anti-HBV Compounds from Saussurea lappa (Decne.) C.B Clarke.

Wu T ，Yan XJ ，Yang TR ，Wang YF ，He JY ，Feng Y ，Su LH ，Chen H ，Xu M ... -  《-》

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 ... -  《-》

A new sesquiterpenoid from Saussurea lappa roots.

Cao K ，Qian W ，Xu Y ，Zhou Z ，Zhang Q ，Zhang X ... -  《-》