Ten new triterpenoids, schiglausins A-J (1-10), as well as four known compounds, were isolated from the stems of Schisandra glaucescens. Their structures were elucidated on the basis of spectroscopic methods, including extensive NMR spectra and CD experiment. Compound 8 was determined to be a norlanostane triterpenoid. The crystal structure of compound 1 has been determined using single-crystal X-ray analysis while its absolute configuration was assigned on the basis of the CD spectrum. All isolates were tested for their FXR agonistic and antagonistic effects.
"Schisandra glaucescens Diels (Schisandraceae) is a woodiness lianas, mainly distributed in Hubei and Sichuan provinces of China , which is used as folk medicine for the treatments of cough with dyspnea, spontaneous sweat, night sweat, chronic diarrhea, and neurasthenia . Previous chemical investigations of S. glaucescens proved the presence of lanostane triterpenoids  . "
[Show abstract][Hide abstract] ABSTRACT: Five new cycloartane triterpenoids, schiglausins K-O (1-5), including one hexanortriterpenoid (1) and one octanortriterpenoid (2), as well as two known compounds (6-7), were isolated from the stems of Schisandra glaucescens Diels. Their structures were elucidated on the basis of spectroscopic methods, including extensive NMR spectra. Compounds 2-7 were tested for their FXR agonistic and antagonistic effects. Compound 7 exhibited significant antagonistic effect against FXR with IC(50) of 1.50 μM.
[Show abstract][Hide abstract] ABSTRACT: Two new tetrahydrofuran lignans, schiglaucin A and B (1-2), together with eight known analogues (3-10), were isolated from the stems of Schisandra glaucescens Diels. Their structures were elucidated on the basis of spectroscopic techniques (HRESIMS, UV, IR, NMR, and CD experiments). All of the compounds were tested for their neuroprotective activities against H2O2- and CoCl2-induced cell injuries in SH-SY5Y cells, respectively. Compounds 1-10 showed significant neuroprotective effects against H2O2-induced SH-SY5Y cell death, while compounds 1-5 and 8-10 exhibited significant neuroprotective effects against CoCl2-induced SH-SY5Y cell injury.
[Show abstract][Hide abstract] ABSTRACT: Eleven compounds were identified as estrogen receptor modulators from an in-house natural product database (NPD) by structure-based virtual screening for ERα and ERβ. Among them, 3 compounds were confirmed as ER agonists and 8 compounds were confirmed as ER antagonists by yeast two-hybrid (Y2H) assay, with EC50 values ranging from several micromolar to 100 micromolar. In this study, a novel series of cycloartane triterpenoids isolated from Schisandra glaucescens Diels was found to have ER antagonistic effect, the most potent antagonist of which exhibited activity with EC50 value of 2.55 and 4.68μM for ERα and ERβ, respectively. Moreover, the types of modulation and subtype selectivity were also investigated through molecular docking simulation.
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