摘要：

Objective: To investigate the chemical constituents of Heteroplexis micocephal and their bioactivities.Method: The constituents were isolated by using a combination of various chromatographic techniques including column chromatography over macroporous adsorbent resin,silica gel,Pharmadex LH-20,and C-18,as well as reversed-phase HPLC.Structures of the isolates were identified by spectroscopic data analysis.In vitro cytotoxic,HIV-1 replication,neuroprotective,and anti-inflammatory activities were screened by using cell-based models.Result: Thirty-one compounds were obtained.Twelve of them are phenylpropanols,and the structures were elucidated as(+)-(7S,8R)-guaiacylglycerol(1),ferulic acid(2),cinnamate methyl ester(3),1-eicosanyl 3,4-dihydroxycinnamate(4),morinin B(5),sinapyl diangelate(6),chlorogenic acid(7),4-O-caffeoylquinic acid(8),5-O-caffeoylquinic acid(9),5-O-caffeoylquinic acid methyl ester(10),1,5-di-O-caffeoylquinic acid(11) and 4,5-di-O-caffeoylquinic acid methyl ester(12).Three lignans,(+)-pinoresinol(13),prinsepiol(14) and(+)-pinoresinol-O-β-D-glucopyranoside(15).Four acetophenones,2,4-diacetylanisole(16),espeleton(17),viscidone(18) and 12-hydroxytremetone-12-O-β-D-glucopyranoside(19).Nine flavones,isosakuranetin(20),hesperetin(21),3-methoxy-5,7,3′,4′-tetrahydroxyflavone(22),acacetin(23),5-hydroxy-7,4′-dimethoxyflavone(24),7-methoxy-4′,5,6-trihydroxyflavone(25),3,3′-dimethylquercetin(26),kaempferol 3-O-rutinoside(27),rutin(28).And three coumarins scopoletin(29),umbelliferone(30) and ayapin(31).Compound 6 and 22 showed selective cytotoxicities against a human stomach cancer cell line(BGC-823) and a human lung cancer cell line(A549) with IC50 values of 3.74×10-5 and 7.17×10-5 mol·L-1,respectively.In addition,Compound 6 showed a potent activity inhibiting HIV-1 replication with an IC50 value of 4.04×10-6 mol·L-1,while 22 showed neuroprotective activity Against the MPP+ induced PC12-syn cell damage,with a relative protection ratio of 105.2%(P0.01) at a concentration of 10-5 mol·L-1.Compound 26 and 31 showed inhibitory activities against the release of β-glucuronidase of the polymorphous nuclear leukocytes induced by platelet activating factor(PAF),with inhibitory rates of 75.6%(P0.001) and 53.9%(P0.01),respectively.Conclusion: Compounds 1-31 were obtained from the genus Heteroplexis for the first time.Compound 6 and 22 possessed selective cytotoxicities against human cancer cell lines BGC-823 and A549,respectively.In addition,Compound 6 showed a potent activity inhibiting HIV-1 replication while 22 showed neuroprotective activity against the MPP+ induced PC12-syn cell damage.Compound 26 and 31 were potent anti-inflammatory agents.

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