24 (1R,5R)-1,5-epoxysalvial-4( 14)ene S. sclarea 49 2 salviadienol A S. chinensis 42 25 (2R,5E)-2,12-epoxycaryophyll-5ene S. sclarea 49 3 3β,6β,8a-triacetoxy-4β,5α-epoxy-1-oxogermacr-10(14)-ene S. roborowskii 43 26 (2R,5E)-caryophyll-5-en-12-al S. sclarea 49 4 3β,6β,8a-triacetoxy-4β,5α-epoxygermacr-1(10)E-ene S. roborowskii 43 27 (2S,5E)-caryophyll-5-en-12-al S. sclarea 49 5 3β,6β,8a-triacetoxy-4β,5α:1α,10β-diepoxygermacrane S. roborowskii 43 28 caryophyllene oxide S. sclarea 51, 47 6 salviadienol B S. chinensis 42 S. palaefolia 50 7 trijugin A S. trijuga 45 29 4,10-epoxy-6α-hydroxyguaiane (= buchariol) S. bucharica 343 8 trijugin B S. trijuga 45 30 isospathulenol S. sclarea 49 9 trijugin C S. trijuga 45 31 (1β,3β,4α,5α,6α,8α)-guai-10(14)ene-3,4,6,8-tetrol 3,6,8-triacetate S. roborowskii 48 10 trijugin D S. trijuga 45 32 spathulenol S. eupatorium 361 11 trijugin E S. trijuga 45 S. sclarea 51 12 trijugin F S. trijuga 45 33 nubiol S. nubicola 23 13 trijugin G S. trijuga 45 34 nubenolide S. nubicola 52 14 trijugin H S. trijuga 45 35 nubenolideacetate S. nubicola 52 15 trijugin I S. trijuga 45 36 bisnubidiol S. nubicola 23 16 (1aS*,6R*,6aS*,7aR*,9aR*)-1a,2,6,6a,7a,8,9,9a-octahydro-1a,5,7atrimethylbisoxireno[4,5:8,9]cyclodeca[1,2-b]furan-6-yl acetate (= castanin B) S. castanea 44 37 bisnubenolide S. nubicola 52 6-acetoxyglechomafuran S. roborowskii 43 38 1α,9β-dibenzoyloxy-2β,3β,4βtrihydroxydihydro-β-agarofuran S. palaefolia 50 17 glechomafuran S. palaefolia 47 39 lα-acetoxy-11-hydroxy-2,8-dioxoeudesman-3-en-12-oic acid methyl ester S. palaefolia 53 18 castanin C S. castanea 46 40 11-hydroxy-3,8-dioxo-eudesman-1,4-dien-12-oic acid methyl ester S. palaefolia 53 19 castanin D S. castanea 46 41 β-eudesmol S. microphylla 55 20 castanin E S. castanea 46 42 8α-hydroxy-β-eudesmol S. microphylla 55 21 castanin F S. castanea 46 43 1α-acetoxy-2-oxoeudesman-3,7(11)-dien-8β,12-olide S. palaefolia 53 22 (4R*,5R*,5aS*,8S*,8aR*,8bR*)-8-formyl-4,5,5a,6,7,8,8a,8b-octahydro-5,8b-dihydroxy-3,5a,8-trimethyl-2-oxo-2H-indeno[4,5-b]furan-4-yl acetate (= castanin A) S. castanea 44 44 1α-hydroxy-2-oxoeudesman-3,7(11)-dien-8β,12-olide S. palaefolia 53 23 (3β,4α,6α,8β,9β,10α)-8-(acetyloxy)-3,4:9,10-diepoxygermacr-7(11)-eno-12,6-lactone S. roborowskii 48 45 1α,8α-dihydroxy-2-oxoeudesman-3,7(11)-dien-8β,12-olide S. palaefolia 53, 54 46 1α-acetoxy-8α-hydroxy-2oxoeudesman-3,7(11)-dien-8,12olide S. palaefolia 54
Eight sesquiterpene lactones were isolated from the roots of Inula helenium and fl owers of I. japonica. Among them, isoalantolactone (3) and santamarine (6) exhibited signifi cant growth inhibitory activities against gynecologic cancer cell lines, while others weakly inhibited the growth of the cell lines (IC 50 100 μM). In addition, 3 signifi cantly inhibited the tumour growth of S180 tumour-bearing mice. Compounds 3 and 6 were not toxic to human embryonic lung fi broblast cells in vitro. These results demonstrated that the antitumour activities are closely related to the structures of the compounds, that is, an α-exomethylene-γ-lactone ring is necessary for these activities.
The Asteraceae family comprises ca. 1000 genera, mainly distributed in Asia and Europe. Saussurea DC., as the largest subgenus of this family, comprises ca. 400 species worldwide, of which ca. 300 species occur in China. Most plants in China grow wild in the alpine zone of the Qingzang Plateau and adjacent regions at elevations of 4000 m. Plants of the genus Saussurea (Asteraceae) are used in both traditional Chinese folk medicine and Tibet folklore medicine, since they are efficacious in relieving internal heat or fever, harmonizing menstruation, invigorating blood circulation, stopping bleeding, alleviating pain, increasing energy, and curing rheumatic arthritis. A large number of biologically active compounds have been isolated from this genus. This review shows the chemotaxonomy of these compounds (215 compounds) such as sesquiterpenoids (101 compounds), flavonoids (19 compounds), phytosterols (15 compounds), triterpenoids (25 compounds), lignans (32 compounds), phenolics (23 compounds), and chlorophylls (11 compounds). Biological activities (anti-inflammatory, anticancer, antitumor, hepatoprotective, anti-ulcer, cholagogic, immunosuppressive, spasmolytic, antimicrobial, antiparasitic, antifeedant, CNS depressant, antioxidant, etc.) of these compounds, including structure-activity relationships, are also discussed.
TRK-fused gene (TFG) is known to be involved in protein secretion and plays essential roles in an antiviral innate immune response. However, its function in LPS-induced inflammation and pyroptotic cell death is still unknown. Here, we reported that TFG promotes the stabilization of Unc-51 like autophagy activating kinase (ULK1) and participates in LPS plus nigericin (Ng) induced pyroptotic cell death. Our results showed that TFG-deficient THP-1 macrophages exhibit higher mitochondrial ROS production. LPS/Ng stimulation triggers a much higher level of ROS and induces pyroptotic cell death. ULK1 undergoes a rapid turnover in TFG-deficient THP-1 cells. TFG forms complex with an E3 ligase, tumor necrosis factor receptor-associated factor 3 (TRAF3), and stabilizes ULK1 via disturbing ULK1-TRAF3 interaction. Knockdown of TFG facilitates the interaction of ULK1 with TRAF3 and subsequent K48-linked ULK1 ubiquitination and proteasome degradation. Rescue of ULK1 expression blocks LPS/Ng-induced cell death in TFG-deficient THP-1 macrophages. Taken together, TFG plays an essential role in LPS/Ng-induced pyroptotic cell death via regulating K48-linked ULK1 ubiquitination in macrophages.
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