| Celastrus orbiculatus Thunb. is a member of family Celastraceae. It is a traditional herbal medicine which is widely distributed in China. The constituents of Celastrus orbiculatus are complicated, such as sesquiterpenes, flavonoids, tripenes et al. Its fruits had activities in tranquilization, hypnogenesis, antiinflammation, antitumor, antifeedant, and had been used as the substitute of flowers of Albizia julibrissin. In order to find the active constituents, the systemic studies on its chemistry and pharmacology were carried out.42 constituents were isolated from the fruits of Celastrus orbiculatus by using open-column chromatograph, and PHPLC methods et al. On the basis of analysis of UV, NMR, MS data and physico-chemical constants, the structures of 37 compounds were identified as following: 1β, 6a-diacetoxy-9a-benzoyloxy-p-dihydroagarofuran (1), 6a, 13-diacetoxy-1β, 8β, 9a-tribenzoyloxy-p-dihydroagarofuran (2) , 1β, 2β, 13-diacetoxy-9β-benzoyloxy-β-dihydro-agarofuran (3), lβ-acetoxy-9a-cinnamoyloxy-p-dihydroagarofuran (4), 1 B-acetoxy-6a, 9a-dibenzoyloxy-β-dihydroagarofuran (5), 1β, 6a 8B-triacetoxy-9a-benzoyloxy-β-dihydroagaro-furan (6), 1β, 6a-diacetoxy-9β-benzoyloxy-8β-cinnamoyloxy-p-dihydroagarofuran (7), la, 2a-diacetoxy-9β-cinnamoyloxy-β-dihydroagarofuran (8), 1β, 2β, 6a-triacetoxy- 9β-benzoyloxy-β-dihydroagarofunan (9), 6a-acetoxy-1β, 8β, 9β-tribenzoyloxy-β- dihydroagarofuran (10), 1B, 6a,13-triacetoxy-9a-benzoyloxy-p-dihydroagarofuran (11), 1β, 6a-diacetoxy-8β, 9β-dibenzoyloxy-β-dihydroagarofuran (12), 6a-acetoxy-9β-benzoyloxy-1β-cinnamoyloxy-8p-butanoyloxy-β-dihydroagarofuran (13), 1β, 2β-diacetoxy-6a-benzoyloxy-9a-cinnamoyloxy-p-dihydroagaro-furan (14), 1β, 8β-diacetoxy-9β-cinnamoyloxy-2β-hexanoyloxy-p-dihydroagarofiiran (15), 6a-acetoxy-9p-benzoyloxy-lp-cinnamoyloxy-8β-(2-methylbutanoyloxy)-β-dihydroagarofuran (16), la, 2a, 8p-triacetoxy-9p-cinnamoyloxy-8β-(2-methylbutanoyloxy)-β-dihydroagarofuran (17), 6a-acetoxy-lβ, 9β-dibenzoyloxy-8p-hydroxy-β-dihydroagarofuran (18), iβ, 2β, 6a-triacetoxy-9β-cinnamoyloxy-p-dihydroagarofuran (19),1β, 2β, 6a-triacetoxy-9β-cinnamoyloxy-β-dihydroagarofuran (20), 1β, 2β, 6a, 13-tetraacetoxy-9p-cinnamoyloxy-p-dihydroagarofuran (21), 6a-acetoxy-1β, 8β-dibenzoyloxy-9β-hydroxy-p-dihydroagarofuran (22), kaempferol (23), quercetin (24), kaempferol-7-O-a-L-rhamnoside (25), quercetin-7-O-a-L-rhamnoside (26) , kaempferol-3,7-O-a-L-dirhamnoside (27), kaempferol-7-O-a-L-rhamnosyl-3-O-β-D-glucopyranoyl(1-4)-a-L- dirhamnoside (28), benzoic acid (29), 2-hydroxy benzoicacid, (30), 3, 4-dihydroxy benzoic acid (31), 4-hydroxy benzaldehyde (32), vanillic acid (33), (6S, 7aR)-6-hydroxy-4, 4, 7a-trimethyl-5, 6, 7, 7a-tetradihydrobenzofuran- 2(4H)-one (34), 3, 4-dihydro-3-oxo-4-benzyl-lH-pyrrolo[2, l-c][1, 4]oxazine-6-carboxaldehyde (35), p-sitosterol (36), daucosterol (37).Among them, compound 2 , 3, 13, 15, 16, 20, 21 and 22 are new compounds; compound 35 is a new natural product; compounds 28~34 were first isolated from this genus.A review on the type of structures, the spectral characters and so on of p-dihydroagarofuran was given based on the literatures and our research work.The pharmacological experiments showed that the extract of fruits of C. orbiculatus had no effects on spontaneous movements of mice, so the use of fruits should be discussed further instead ofAlbiziajulibrissin flowers.The experiments inhibiting the proliferation of tumor cells indicated that p-dihydroagarofuran sesquiterpene esters, isolated from the fruits of Celastrus orbiculatus, had obvious activity of inhibiting the proliferation in Hela and A375-S2 cells at the concentration of 40ug/ml.In vitro experiments of anti-inflammation, the ethanol extract of the fruits of Celastrus orbiculatus suppressed the NF-kB activation and NO production and the active part should be the petroleum ether partition of fruits extract. Extended research showed that the main chemical constituents of petroleum ether part, β-dihydroagarofuran se...
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