Two novel 18,19-seco-ursane triterpenoid saponins, ilexasprellanosides J-K (1-2, resp.), 3-O-α-l-Rhamnopyranosyl-(1 → 2)-β-d-xylopyrannosyl-19-O-β-d-glucopyranosyl-16-β-hydroxyl-18,19-seco-13(18)-urs-ene-21, 28-lactone (1), 3-O-β-d-Xylopyrannosyl-19-O-α-l-rhamnopyran osyl-(1 → 2)-α-l-arabinopyranoside-16, 21-epoxy-18, 19-seco-13(18)-urs-ene-28-oic acid (2), five known compounds (3-7) were isolated from the leaves of Ilex asprella (Hook. et Arn.) Champ. ex Benth. (Gangmeiye). The chemical structures of these compounds were elucidated through UV, IR, ESI-MS, 1H NMR and 13C NMR analyses. In MTT and SRB assays, compounds 1-4 presented cytotoxic activities against several human cancer cell lines, namely, the HL-60 human acute promyelocytic leukaemia, Bel 7402 liver cancer, BGC-823 gastric cancer and KB human nasopharyngeal carcinoma cell lines. Compound 1 exhibited weak cytotoxic activities against the human tumour cell lines HL-60, Bel 7402 and KB with inhibition rates of 27.97%, 21.00% and 25.60%, respectively. Compound 2 exhibited weak cytotoxic activities against the human tumour cell lines HL-60, Bel 7402 and BGC-823 with inhibition rates of 19.34%, 7.50% and 4.26%. Respectively, the compounds exerted no statistically different effects on mast cell degranulation in rats. This result indicates that the compounds do not affect mast cell degranulation.
Keywords: Cell degranulation; Cytotoxic activity; Ilex asprella; Ilexasprellanoside; Triterpenoid saponins.
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