Two New β-Dihydroagarofuran Sesquiterpenes from Celastrus orbiculatus Thunb and Their Anti-Proliferative Activity

Abstract

Two new β-dihydroagarofuran-type sesquiterpenes (1–2) were isolated and identified from the fruit of Celastrus orbiculatus Thunb, together with seventeen known compounds (3–19). The structures of the isolated new compounds were elucidated based on extensive spectroscopic analyses. The cytotoxic activities of the 19 sesquiterpenes on three cell lines, human acute promyelocytic leukemia HL-60, human leukemic K562, and human colon cancer HCT-116 cells, were evaluated in vitro. Compound 4 exhibited potent cytotoxic activity against HL-60, K562, and HCT116 cell lines with IC50 values of 3.61 μΜ, 17.13 μΜ and 10.15 μΜ, respectively, and the other compounds displayed moderate activity.

Inhibition or Reversal of the Epithelial-Mesenchymal Transition in Gastric Cancer: Pharmacological Approaches

“…It has been used in rheumatoid arthritis, insomnia, and contusion [ 159 ]. In addition, it has properties analgesic [ 159 ], hypnotic [ 159 ], and anti-tumor [ 160 , 161 , 162 , 163 ] properties. Zhou et al demonstrated that β-dihydroagarofuran sesquiterpenes from COE exhibited antiproliferative activity, directed against human colon cancer HCT-116 cells, human acute promyelocytic leukemia HL-60 cells, and human leukemic K562 cells [ 160 ].…”

“…In addition, it has properties analgesic [ 159 ], hypnotic [ 159 ], and anti-tumor [ 160 , 161 , 162 , 163 ] properties. Zhou et al demonstrated that β-dihydroagarofuran sesquiterpenes from COE exhibited antiproliferative activity, directed against human colon cancer HCT-116 cells, human acute promyelocytic leukemia HL-60 cells, and human leukemic K562 cells [ 160 ]. Qian et al demonstrated the existence of a synergistic inhibition of hepatocellular carcinoma growth through low mTOR expression and COE-induced cell apoptosis in HepG2/mTOR-in vitro [ 161 ].…”

Structure elucidation and NMR assignment of two new hydroxywilfordate‐type alkaloids from the stems of Tripterygium hypoglaucum and activity evaluation

“…Hutch (THH) is an endemic liana shrub (Celastraceae) indigenous in southwest China and distributed mainly in Yunnan, Sichuan, and Guizhou Provinces. [ 1–4 ] Previously published research results suggest that a broad variation of dihydroagarofuran sesquiterpene derivatives appears to be the most common and representative of the bioactive metabolites found in Celastraceae species, [ 5–7 ] and many are considered to be important as chemotaxonomic indicators. [ 8 ] The macrolide sesquiterpene pyridine alkaloids (MSPASs) represent a structurally specific class of macrolactone alkaloids that contain a pyridine dicarboxylic acid substructure, including wilfordic, hydroxywilfordic, evoninic, cassinic, and edulic, which bridge the C 3 and C 15 positions of the highly functionalized sesquiterpenoid core, for example, evoninol, euonyminol, or isoeuonyminol.…”