Chemical Constituents Of The Roots Of Ilex Cornuta Lindl.Et Paxt <â…¡>

Ilex cornuta Lindl. et Paxt.(Aquifoliaceae) has been used as traditional Chinesemedicine to treat multiple common diseases such as rheumatic arthralgia, headacheand hypertension for thousands years in folk. Moreover, its roots, leaves and fruitsall possess various medicinal effects. The root of this plant, namely,“Mahonia root”,which can boost kidney-bone, expel wind-damp, relieve pain and can consequently be usedto cure lumbar muscle degeneration, icteric hepatitis, urticaria and so on. The modernpharmacology researches showed that I. cornuta has many efficacies, for instance,antisepsis, anti-inflammation, expansion of coronary artery and hypotensive,hypolipidemic and antifertility. In addition, phytochemical studies of Ilex genus havereported the occurrence of triterpenes, triterpenoid saponins, flavones, flavonoid glycosides,polyphenols and fatty acids, etc. However, almost all researches about this plant are limitedto its foliage while there is few reports about the roots, whose substance basis remains tobe further explored.Based on that, our team systematically experimented the chemical composition andscreened the effective parts of the roots of Ilex cornuta, which led to the conclusion that theextracts from the roots of the Ilex cornuta had remarkable bioactivities in antioxidant ofmyocardial cells, expansion of coronary artery and hypotensive, concentrating on the30%EtOH elute of D101macroporous resin column chromatography.To further investigate the constituents and to screen potentially active substances,bioassay-guided separation and purification of the30%active part were herein performed.As a result,32compounds were isolated through modern separating techniques such asresin, silica gel, Sephadex LH-20, medium pressure column chromatography, dynamicaxial compression chromatography and semi-preparative liquid chromatography. Moreover,their structures were elucidated via1D-and2D-NMR and MS spectra, etc. Among them,compounds GW-10，GW-11，GW-12，GW-26，GW-27，GW-31were obtained from thisgenus for the first time, compounds GW-2，GW-5，GW-6，GW-22，GW-24，GW-25，GW-30，GW-32were obtained from this species for the first time, and compounds GW-3，GW-4，GW-8，GW-9，GW-14，GW-15，GW-17，GW-18，GW-19，GW-21，GW-23 were novel, which were further determined as20a(H)-urs-12,18-dien-3β-O-β-D-glucuron-opyranoside-6-O-methyl ester (GW-3), Urs-12,18-dien-3β-O-β-D-glucuronopyranoside-6-O-methyl ester (GW-4),23-hydroxyl urs-12,18-dien-3β-O-a-L-arabinopyranoside(GW-8),23-hydroxyl urs-12,18-dien-3β-O-β-D-glucuro-nopyranoside-6-O-methyl ester(GW-9), Pomolic acid3β-O-β-D-glucuronic acid (GW-14), Pomolic acid3β-O-[a-L-ara-binopyranosyl (1→2)-β-D-glucuronopyranoside-6-O-methyl ester]-28-O-β-D-gluco-pyranosyl ester (GW-15),20a(H)-23-hydroxyl urs acid (GW-17),20a(H)-19a,23-dihyd-roxyl urs3β-O-a-L-arabinopyranoside (GW-18), Pomolic acid3β-O-[a-L-arabinopyran-osyl (1→2)-β-D-glucuronic acid]-28-O-β-D-glucopyranosyl ester (GW-19),20a(H)-23-hydroxyl urs-12,18-dien-3β-O-β-D-glucuronopyranoside (GW-21), Pomolic acid3β-O-a-L-arabinopyranosyl (1→2)-β-D-glucuronic acid (GW-23).Meanwhile, based on the previous pharmacodynamics experiments, we investigatedthe antioxidant activities and cardiomyocyte-protective effects of the11compounds, whichled to the conclusion that compounds1,13,14,15,19,23,31,32were the activesubstances from the roots of Ilex cornuta. Ulteriorly, this project revealed the materialfoundation for efficacy of the roots of Ilex cornuta, perfected their phytochemical studies,and provided experimental basis for investigation and utilization in future.