Summary: | 碩士 === 中國醫藥大學 === 藥物化學研究所碩士班 === 100 === Echinops grijisii Hance (Echinops) is a folk medicine used in Taiwain to treat inflammation and detoxification.Our preliminary bioassay test in dicated that the methanol extract of radix of this plant showed a dose-dependent effect to NO inhibition.We continue in the study on chemical constituents of this plant.
These dried stems of Echinops grijisii Hance were extracted with methanol.The extracts were further separated by chromathography.Tirty six compounds have been isolated and purified. Those include :
Six aromatics:
Methyl caffeate (AR 1), 4,5-dimethoxybenzene-1,2-dicarbaldehyde (AR 2**), Methyl paraben (AR 3), 3-(4’-Hydroxyphenyl)-(E)-propenoic acid methyl ester (AR 4), Methyl veratrate (AR 5), and Vanillin (AR 6)
Five anthraquinone:
Chrysoobtusin (AQ 1), Obtusin (AQ 2) , Aurantio-obtusin (AQ 3) , 1-desmethylobtusin (AQ 4) , and Obtusifoline (AQ 5)
Eigteen thiophens:
2,2''-bithiophene -5''-carboxylic-acid (TH 1**), 2-(3,4-dihydroxybut-1-ynyl)-5-(penta-1,3-diynyl) –thiophene (TH 2), α-Terthienyl (TH 3) , 5’-(3,4-Dihydroxybut-1-ynyl)-2,2’-bithiophene
(TH 4) , 5-acetyl-2,2''-bithiophene (TH 5) , 5-formyl-2,2''-bithiophene(TH 6**) , methyl-5,2''-bithiophene-2-carboxylate (TH 7**) , 5''-(But-3-en-1-ynyl)-2,2''-bithiophene (TH 8) , 5''-(4-hydroxy-1-butynyl)-2,2''-bithiophene (TH 9) , Cardopatine (TH 10) , Isocardopatine (TH 11) , 5''-(3-Hydroxy-4-isovaleroyloxybut-1-ynyl)-2,2’-bithiophene (TH 12) , 5''-(3-Hydroxy-4-isovaleroyloxybut-1-ynyl)-2,2''-bithiophene (TH 13) , 5-(4-hydroxy-1-butynyl)-2,2''-bithiophene (TH 14) , 5’-(4-acetoxy -1-butynl)bithiophene (TH 15) , 5’-(4- hydroxy -3-methoxy-1-butyny)bithiophene (TH 16*) , 2-(penta-1, 3-diynyl)-5-(4-hydroxybut-1-ynyl)-thiophene(TH 17), 5’-(3- Hydroxy -4-acetoxybutyl-1-butyny)2,2’bithiophene(TH 18)
Four steroids:
β-Sitosterol (ST 1), Stigmasterol (ST 2), β-Sitosterol-O-D-Glucoside (ST 3), β-Stigmasterol-O-D-Glucoside (ST 4)
one lignan:
Pinoresinol (LI 1)
Two Sesquiterpenes:
Dihydrosantamarine ( SQ 1), Santamarine ( SQ 2)
According to bioassay result , compound AQ 1(Chryso obtusin ) showed the best cell viability to RAW 264.7 cell;compound SQ 2 (Santamarine ) showed the most inhibitory activity against LPS-induced NO production with IC50 value of 4.59 ± 0.17 μg/mL.
*New compound
** First isolation from natural source
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