Study On Chemical Constituents And Bioactivities Of Acanthus Ilicifolius

Mangrove plant Acanthus ilicifolius(Acanthaceae),which have pharmaceutical functions of cleanup heat detoxification and acesodyne,grows in tropical coastal areas.In Hainan province countryside of China,the water extract of root of A.ilicifolius was used as specific medicine for the disease hepatitis b virus(HBV).Previous work showed that A.ilicifolius contains the constituents such as sterols,triterpenes, flavonoids,alkaloids,phenylethanol glycosides,lignans,and their bioactivities included hepatoprotective,antioxidant,anti-tumor,to kill Leishmania donovani and so on.In the further search of bioactive constituents,particularly the ingredients against the HBV,A.ilicifolius Linn,collected from Hainan Province of China was chemically investigated.Thirty compounds were isolated and purified by thin-layer chromat-ography(TLC),preparative thin layer chromatography(PTLC),Si gel column chromatography(CC),gel(Sephadex LH-20)column chromatography, reverse phase column chromatography(ODS)and high performance liquid chromatography(HPLC)methods.On the basis of extensive spectroscopic analysis and comparison their spectral data with these reported in literatures,their structures were identified as stigmasta-4,22-dien-3-one(HP1),campest-4-en-3-one(HP2), stigmasta-4-en-3-one(HP3),Stigmast-4,22-diene-6β-ol-3-one(HP4),6β-hydroxystigmast-4-en-3-one(HP5), 3β-hydroxystigmasta-5,22-diene-7-one(HP6), 3β-hydroxystigmasta-5-en-7-one(HP7),Stigmast-4,22-diene-3,6-dione(HP8), Stigmast-4-en-3,6-dione(HP9),4-methyl-cholesta-7-ene-3β-ol(HP10),5α,8α-Epidioxy-(22E,24R)-ergosta-6, 22-dien-3β-ol(HP11),5α,8α-Epidioxy-(22E,24R)-ergosta-6, 9,22-tien-3β-ol(HP12),Ergosta-4,6,8(14),22-tetraene-3-one(HP13), 3α,5α-Dihydroxy-ergosta-7,22-diene(HP14),ergostra-7,22-diene-3β,5α,6β-triol (HP15),5α,6α-Epoxy-(22E,24R)-ergosta-8(14),22-diene-3β,7α-diol(HP16), 24-methylenecycloartenol(HP17),lupeol(HP18),cycloartenol(HP19), 24-methylenelanost-9(11)-en-3β-ol(HP20),19-Norlanost-5-en-3-ol(HP21),Phytol (HP22),2-benzoxazolinone(HP23),2,5-Piperazinedion(HP24),Neoechinulin A (HP25),Cryptoechinuline C(HP26),Preechinulin(HP27),(+)-syringare sinol(HP28), Hexadecanoic acid(HP29),Bis(2-methylpropyl)ester(HP30),respectively.Among them,HP4-HP6,HP8-HP10,HP13-HP16 and HP24-HP27 were obtained from A. ilicifolius Linn,for the first time.In the bioactivity assay,20 compouds were tested by MTT and SRB methods against tumor cell line P-388 and BEL-7402,compounds HP13,HP18 and HP22 showed potential anti-tumor activities.