海芋的活性成分研究.pdf

1、海芋(Alocasia macrorrhiza(L.) Schott)是天南星科海芋屬多年生草本植物，是嶺南地區(qū)常用中草藥，其根莖入藥用于治療乳腺癌、鼻咽癌、闌尾炎、肺結(jié)核、流行性感冒、關(guān)節(jié)炎和毒蛇咬傷等疾病。在我國，海芋主要分布在廣東、云南、臺灣、海南等省份?，F(xiàn)代藥理學(xué)研究表明，海芋具有抗腫瘤、抗炎和解熱鎮(zhèn)痛等藥理活性。海芋的化學(xué)成分研究始于20世紀五、六十年代，到目前為止已經(jīng)從該植物的鮮葉和根莖中共分離得到了40多個化合物，其中生物

2、堿類化合物21個，黃酮類化合物5個，其它類型化合物15個。
　　本研究利用多種色譜分離純化方法和各種波譜學(xué)技術(shù)從海芋的根莖中分離鑒定了71個化合物，包括生物堿類34個：(E)-3-(2-(3-hydroxy-5-methoxyphenyl)-3-(hydroxyl methyl)-7-methoxy-2,3-dihydrobenzofuran-5-yl)-N-(4-hydroxyphenethyl)acrylamide(1*),(

3、E)-3-(2-(4-hydroxy-3,5-dimethoxyphenyl)-3-(hydroxymethyl)-7-methoxy-2,3-dihydrobenzo furan-5-yl)-N-(4-hydroxyphenethyl)acrylamide(2*),(Z)-3-(2-(3-hydroxy-5-methoxyphenyl)-3-(hydroxymethyl)-7-methoxy-2,3-dihydrobenzofuran

4、-5-yl)-N-(4-hydroxyphenethyl)acryl amide(3*),(Z)-3-(2-(4-hydroxy-3,5-dimethoxyphenyl)-3-(hydroxymethyl)-7-methoxy-2,3-dihydrobenzofuran-5-yl)-N-(4-hydroxyphenethyl)acrylamide(4*), grossamide(5), cis-grossamide(6＃),4-(eth

5、oxy(4-hydroxy-3-methoxyphenyl) methyl)-2-(4-hydroxy-3-methoxy phenyl)-N-(4-hydroxyphenethyl)tetrahydrofuran-3-carboxamide(7*),(2S,3R,6R)-2-methyl-6-(1-phenylnonan-4-one-9-yl)piperidin-3-ol(8*),(2S,3R,6R)-2-methyl-6-(1-ph

6、enylnonan-5-one-9-yl)piperidin-3-ol(9*),(2S,3R,6R)-2-methyl-6-(9-phenylnonyl)piperidin-3-ol(10*),(2R,3R,4S,6S)-2-methyl-6-(9-phenylnonyl)piperidine-3,4-diol(11*),(2S,3S,6S)-2-methyl-6-(9-phenylnonyl)piperidin-3-ol(12*),(

7、2R,3R,5R,6R)-2-methyl-6-(9-phenylnonyl)piperidine-3,5-diol(13*),1-(2-(5-hydroxy-1H-indol-3-yl)-2-oxoethyl)-1H-pyrrole-3-carbaldehyde(14*), hyrtiosin B(15),5-hydroxy-1H-indole-3-glyoxylate methyl ester(16＃),5-hydroxy-1H-i

8、ndole-3-glyoxylate ethyl ester(17＃),1H-indole-3-carbaldehyde(18＃),1H-indole-3-carboxylic acid(19＃),5-hydroxy-1H-indole-3-carbaldehyde(20＃),5-hydroxy-1H-indole-3-carboxylic acid ethyl ester(21＃),7,8-dimethylbenzo[g]pterid

9、ine-2,4(1H,3H)-dione(22＃), cyclo-(L-Val-L-Pro)(23＃), L-pyroglutamicacid methyl ester(24＃),(R)-5-hydroxypyrrolidin-2-one(25＃), uracil(26),5-methyluracil(27＃), thymidine(28＃), adenosine(29＃), trans-N-feruloyltyranine(30),

10、cis-N-feruloyltyranine(31＃),(E)-ferulamide(32＃），5-hydroxypyridine(33＃), methyl-5-hydroxy-2-pyridinecarboxylate(34＃)；萜類8個：(6S,7E)-6-hydroxy-4,7-megastigmadien-3,9-dione(35＃),(6R,9R)-blumenol B(36＃), blumenol A(37＃),(E)-6-

11、hydroxy-2,6-dimethylocta-2,7-dienoicacid(38＃),(+)-sporogen AO-2(39＃), phaseic acid(40＃), cannabiside D(41＃), ursolic acid(42＃)；木脂素類5個：(+)-lyoniresinol-3α-O-β-D-glucopyranoside(43＃),(+)-lyoniresinol(44＃),(+)-lyoniresin-4-

12、ylβ-D-glucopyranoside(45＃), syringaresinol(46＃),8,8’-bisdihydro siringenin glucoside(47＃)；苯丙素類9個：siringenin(48＃), dihydrosiringenin(49＃), dihydroconiferin(50＃), threo-1-C-syringylglycerol(52＃),β-hydroxypropiovanillone(53

13、＃), trans-cinnamic acid(54＃), dihydroferulic acid methyl ester(55＃), dihydroferulic acid(56＃), ferulic acid(57＃)；酚類7個：2,6-dimethoxy p-hydroquinone1-O-β-D-glucopyranoside(51＃),3-methoxy-4-hydroxybenzoic acid(63),3,4-dihyd

14、roxybenzoic acid(64), syringic acid(65＃), p-hydroxy benzaldehyde(66＃), p-hydroxybenzoic acid(67), anisic acid(68＃)；其它類8個：icariside F2(58＃), isopentenol1-O-β-D-apiofuranosyl-(1→6)-β-D-glucopyranoside(59＃),5α,8α-epidioxyer

15、gosta-6,22-diene-3β-ol(60＃), decumbic acid(61＃),5-(hydroxymethyl) furan-2-carbaldehyde(62＃), butanedioic acid monoethyl ester(69＃),(9Z,12Z,15Z)-2,3-dihydroxypropyl octadecadienoate(70＃),(9Z,12Z)-2,3-dihydroxypropyl octad

16、ecadienoate(71＃).。其中，化合物1–4、7為5個新木脂素類生物堿，化合物8–13為6個新哌啶類生物堿，化合物14為一個新吲哚類生物堿；化合物6、16–25、27–29、31–62、65–66、68–71等52個化合物均為屬首分化合物。
　　此外，本研究還對從海芋中分得的化合物進行了抗腫瘤細胞細胞增殖活性和抗炎活性測試。
　　結(jié)果表明，新化合物10–13，已知化合物39、42對CNE-1、Detroit562、