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.

[Electroacupuncture down-regulates expression of ADAMTS-4 of intervertebral disc in rats with lumbar intervertebral disc degeneration].

OBJECTIVE: To observe the effect of electroacupuncture (EA) stimulation on the levels of a disintegrin and metalloproteinase with thrombospondin motifs-4 (ADAMTS-4) protein in the lumbar intervertebral disc tissue and serum in prolapsed lumbar intervertebral disc degeneration (PLIDD) rats, so as to explore its mechanism underlying improvement of intervertebral disc degeneration (IDD). METHODS: A total of 48 Sprague-Dawley rats were divided into sham operation (n＝12), model (n＝18) and EA (n＝18) groups. The PLIDD model was established by puncturing the lumbar discs (L4-L5, L5-L6) with a gauge-22 syringe needle. After modeling, EA stimulation was applied to "Pangguangshu"(BL28), "Zusanli"(ST36) and "Zhijian"for 20 min, 6 times per week for 4 weeks. The lumbar intervertebral disc tissue and blood samples were collected at the 4th, 6th and 8th week after modeling, respectively. The expression of ADAMTS-4 in the lumbar intervertebral disc tissue was detected by immunohistochemistry and Western blot (WB), separately. The content of ADAMTS-4 in the serum was detected by ELISA. RESULTS: Both immunohistochemical stain and WB showed that the expression levels of lumbar ADAMTS-4 at the 4th, 6th and 8th week were significantly up-regulated in the model group relevant to the sham operation group (P<0.01). Following EA treatment, the expression levels of ADAMTS-4 on day 14 and 28 were notably lower in the EA group than in the model group (P<0.05). The serum ADAMTS-4 contents were significantly increased in the model group than in the sham operation group at the 3 time-points (P<0.05, P<0.01), and considerably decreased in the EA group than in the model group on day 28 after EA intervention(P<0.05)．. CONCLUSION: EA can down-regulate the ADAMTS-4 expression of lumbar intervertebral disc tissue in PLIDD rats, which may contribute to its effect in relieving lumbar intervertebral disc degeneration.