| Acorus calamus Linn.(Araceae) is a perennial aquateic herb and its rhizomes can be used as Traditional Chinese Medicine. It is widely distributed among the northern temperate and subtropical regions of North America, Europe, and Asia. In China, it is mainly distributed in Hunan, Hubei, Liaoning, and Sichuan Provinces. Its rhizome is one source of the traditional Chinese Medicine "Chang Pu". Chang Pu was first recorded in Shen Nong Ben Cao Jing and top graded. It can be used to treat kinds of psychosis, It has been reported to possess extensive antidiabetic, nootropic, antioxidant, antimicrobial, anti-inflammatory, antispasmodic, antiulcer, and hypolipidemic activities. In addition, it contains a wide variety of sesquiterpenoids, phenylpropanoids, lignans, flavonoids, steroids, and triterpenoid saponins. In this thesis, we screened the petroleum ether, ethyl acetate, n-butanol and water parts of its95%ethonal extract and ten silica gel chromatographied parts of ethyl acetate fraction of their bioactivities. At the concentration of10ug/ml, the fractions Shui-1, Shui-2, Shui-3, Et-3, Et-4, Et-7, Et-8, Et-9, and Et-10exhibited significant GK-activation activity; Shui-0and Et-8displayed slight aldose reductase inhibition activity (At10ug/ml, the aldose reductase inhibition rations were51.3%and52.2, respectively.). Additionally, in the MTT test, Et-1, Et-5, Et-7, Et-10, Shui-0, and Shui-4exhibited hepatoprotective activities to the CCl4and APAP-induced hepatic injury at the concentration of50ug/mL. Among them, Et-5, Et-7, and Shui-0exhibited significant hepatoprotective activities.In this thesis, kinds of chromatographic and spectral methods were used to isolate the compounds from95%ethanol extract of A. calamus and elucidate their structures. In addition, the compounds isolated were screened of their bioactivities.79compounds were isolated from A. calamus and elucidated, including30new ones (compounds1-19and21-31) and a new natural product (compoun d20). These compounds include21sesquiterpenes (compounds1-17and32-46),14alkaloids (compounds18-22and47-55),10phenylpropanoids (compoun ds23-27and56-60),8lignans (compounds28-29and61-66), and15other compounds (compounds30-31and67-79). These compounds are listed as foll ows:calamusin A (1), calamusin B (2), calamusin C (3), calamusin D (4), cala musin E (5), calamusin F (6), calamusin G (7), calamusin H (8), calamusin I (9), calamusin J (10), calamusin K (11), calamusin L (12), calamusin M (13), calamusin N (14), calamusin O (15), calamusin P (16), calamusin Q (17), cala musine A (18), calamusine B (19), calamusine C (20), calamusine D (21), cala musine E (22),threo-2,4,5-trimethoxy-7-O-(1-α-allofuranosyl)-8-hydroxypropane (23),threo-2,4,5-trimethoxy-7-O-(1-β-fructofuranosyl)-8-hydroxypropane (24), thre o-3,4-dimethoxy-7-O-(1-α-allofuranosyl)-8-hydroxypropane (25),threo-2,4,5-trimet hoxy-7-O-(1-α-tagatofuranosyl)-8-hydroxypropane (26), threo-4,7,8-trihydroxyl-met hyl phenylproianate (27),(+)-7R,8S-4,3’,4’-trihydroxy-3,5-dimethoxy-9’-nor-7,8’-ox y-neolignan-8,9-diol (28),(+)-4-hydroxy-3,5’-dimethoxy-4,7’-epoxy-8,3’-neolignan-9-ol-9’-methyl ester (29), picidic acid1-methyl-5-ethyl ester (30),2’R-2-acetoxy-3-(2,3-dihyxoxypropoxy)furan (31), hedytriol (32),(-)-1β,4β,7α-trihydroxyeudesm ane (33), oplodiol (34),6-eudesmene-1β,4β-diol (35),4β,5α,10β-Trihydroxycadin an (36), tatarinowin A (37), bullatantriol (38), homalomenol A (39),(E)-4’-di hydrophaseic acid (40),4’-dihydrophaseic acid (41),(6S,9S)-9-hydroxy-4-megasti gmen-3-one (42),(6R,9S)-9-hydroxy-4-megastigmen-3-one (43),(+)-dehydrovomif oliol (44),1,10-seco-4ξ-hydroxy-muurol-5-ene-1,10-diketone (45),2-hydroxyacore none (46),2-oxo-l-pyrrolidineacetic acid (47), N-ethoxycarbonylmethylpyrrolidin-2-one (48), α-pyrrolidone acetic methyl ester (49), tatarine A (50), telitoxine (51), paprazine (52), N-trans-feruloyl tyramine (53),3-(4-hydroxy-3-methoxyphenyl)-N-[2-(4-hydroxyphenyl)-2-methoxyethyl]acrylamide (54),4-pyrazin-2-yl-but-3-en e-1,2-diol (55),1-(3,4-dimethoxyphenyl)propane-1,2-diol (56),2-hydroxy-l-metho xy-1-(2’,4’,5’-trimethoxyl)propane (57), acoramone (58), trans-4-hydroxycinnamic acid (59), trans-3-hydroxycinnamic acid (60),(-)-syringaresinol (61), ceplignan (62),threo-guaiacylglycerol-β-ferulic acid ether (63),(+)-isolariciresinol (64),(7S,8R)-4,9,9’-trihydroxy-3,3’-dimethoxy-7,8-dihydrobenzofuran-1’-propylneolignan (65), huazhongilexin (66),5-hydroxymethyl-2-furfural (67), diisobutyl phthalate (68), dibutyl phthalate (69), phenol (70),4-hydroxybenzoic acid (71),3-hydroxybe nzoic acid (72), succinic acid (73),4-hydroxyphenethyl alcohol (74),(-)-eucomi c acid (75),(E)-4-[5-(Hydroxymethyl)furan-2-yl]but-3-en-2-one (76),3,4-dimet hoxybenzaldehyde (77), asarylaldehyde (78), isorhamnetin-7-O-α-L-rhamnopyrano side (79).The bioactive screening was taken of25compounds isolated from the95%ethanol extract of A. calamus. At the concentration of10-6mol/L, compound18exhibited significant PPARγ transcription activity, the activation multiple to PPARγ transcription is3.6, who is better then the positive control rosiglitazone. Compound 18also exhibited significant PPARa transcription activity at the concentration of10-6mol/L, the activation multiple to PPARa transcription is1.52. In addition, compounds18and29exhibited significant GK activation activity at10"5mol/L, the activation multiple was1.6and EC1.5values were5.86μM and1.29μM, respectively. Additionally, compounds1,5,11,17,21and31exhibited moderate hepatoprotective activities at10μM to the APAP-induced hepatic injury. In addition, compounds2,5,6,9,10,12,13,18,19,21,29,30, and31aggravated serum-deprived injuries of PC12cells at10μM; compounds21and30aggravated rotenone-induced injuries of PC12cells at10μM; compounds1,2,3,11,12,13, and29exhibited protective activities to the OGD-induced injuries of PC12cells. |
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