| Objective:Xanthium sibiricum (X. sibiricum）, an annual herb plant of the genus Xanthium,Asteraceae family. Mainly contains sesquiterpene lactones, glycosides, and other compounds,according to previous studies. And pharmacology research show that this genus possesseseffects of anti-inflammatory, analgesic, antibacterial, antitumor, ant oxidation action and theeffect of cardiovascular. Therfore, X. sibiricum is popularly approached for its antipyretic,detoxific, diuretic, emetic, as well as purgative effects and commonly used to cure prostateand lymphatic system diseases, hepatitis, skin pruritus, leprosy and sore ulcer, etc. However,most previous studies linger on the fruits or stems of Xanthium, leaving the probing to thechemical constituents and pharmacological effects of the roots rarely conducted. So that,through systematical studies on the chemical composition and pharmacological effects of theroots of X. sibiricum, this paper was brought out with an aim to provide theoretical basises fortheir utilization.Method:The dry roots were comminutd and extracted with75%aqueous ethanol, then the crudeextract was filtered and concentrated under the reduced pressure to yield dark residue. Afterthe dispersion of the water, the residue was partitioned respectively with petroleum ether,yielded a petroleum ether extract. Dried the remaining portion, uniformly mied on silica,Meanwhile, loaded onto the column, eluting with EtOAc, and the eluate was concentrated toobtain the EtOAc extract. Compounds of each extract were obtained using silica gel columnchromatography, reverse phase silica gel column chromatography, Sephadex LH-20,preparation TLC and so on. The structures of the isolated compounds were determined byspectroscopic methods, including1D/2DNMR, MS, IR, UV, and their physicochemicalproperties. The chemical composition of the essential oil from the leaves、roots of X. sibiricumwere identified by gas chromatography-mass spectrometry (GC-MS)，Finally, the antibacterialand anti-tumor activities were tested.Results:29compounds were isolated and puried from the roots of X. sibiricum,21compoundsincluding one naphthoquinone,one diarylheptanoids, three triterpenes, seven steroids, five Benzene derivatives, one diacid, and three fatty acid esteres were identified using the modernspectrum technology, unifies physicochemical method and literature comparison as5-hydroxy-3,6-dimethoxy-7-methyl-1,4-naphthalenedione(1),7-(4-hydroxy-3-methoxy-phenyl)-1-phenylhept-4-en-3-one(2), betlinc acid(3), betulin(4), erythrodiol(5),β-sitosterol(6),β-stigmasterol(7),6-hydroxystigmast-4-en-3-one(8),7-ketositosterol(9),6-hydroxystigmast-4,22-dien-3-one(10),3-oxo-Δ(4,5)-sitostenone(11), β-daucosterol(12),4-Ketopinoresinol(13), scopoletin(14), p-methoxy cinnamic acid (15), vanillin(16),2-hydroxybenzoic acid(17), suberic acid(18), nonadecyenoic acid (19), linoleic acidmonoglyceride(20), myristic acid monoglyceride(21). Compound1and13are newcompounds, which have not been reported. This is the first report of the compound1，2and13have been isolated from this genus.4,5,9,10,15,18were first isolated from the plant.GC-MS analysed the chemical constituents of the volatile oil from the leaves and roots of X.sibiricum, the petroleum ether extract and the EtOAC extract of the roots of X. sibiricum,including terpenes, esters, fatty acids, alkanes, aldehydes, ketones, alcohols, and phenols. Inthe pharmacological activity test, the petroleum ether extraction of X. sibiricum leavesinhibitory had a best effect on Escherichia coli (MIC4.8μg/ml), and the chloroformextraction of the roots showed significant influence on Bacillus subtilis, Escherichia coli,Staphylococcus and Staphylococcus aureus (MIC39,39,39,19μg/ml). The volatile oil fromthe leaves showed better inhibitory effect on Bacillus cereus (MIC31.3μg/ml), the volatile oilfrom the roots effectively inhibition of human gastric cancer cell SGC-7901, and human lungadenocarcinoma cells SPC-A-1,which IC50values were5.44and0.65μg/ml. |
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