Chemical Constituents Of The Stem Of Ilex Cornuta Lindl. Et Paxt

Ilex cornuta Lindl.(aquifoliaceae) is an evergreen arbor growing in Eastern and SouthernChina and its leaves have been used as one of the original materials of Kudingcha. Thebitter taste is known to be caused by terpenes and their glycosides. It has been consumed asa popular functional bitter tea beverage in China for nearly2000years because of itspotential health and economic significance. The botanicals made from Ilex cornuta hasbeen used traditionally as a contraceptive, cardiovascular and antibacterial agent.Phytochemical studies of Ilex cornuta have led to the isolation of triterpenes, triterpenoidsaponins, flavones, flavonoid glycosides, polyphenols and fatty acids. Many beneficialfunctions related to these compounds have been reported such as sore throat and an aid toweight loss, relief of hypertension, and for its potential cardiovascular benefits as well aspossessing antioxidant, antidiabetic, and anti-bacterial properties.In our effort to develop the extract of Ilex cornuta as a herbal dietary supplement forprevention of coronary artery disease, a phytochemical investigation on the aerial parts ofIlex cornuta was undertaken, which led to the isolation of thirty compounds and purifiedby resin, silica gel, medium pressure column chromatography, ODS silica gel, SephadexLH-20, and semi-preparative liquid chromatography, from50%ethanol extraction of I.Cornuta. In the thirty substances, compounds GS-2, GS-3, GS-4, GS-5, GS-7, GS-8,GS-12, GS-13, were obtained from this genus for the first time, compounds GS-6, GS-16,GS-17, GS-22, GS-23, GS-25, GS-27, GS-28, GS-29, GS-30were the previouslyunknown compounds, and their structures were identified as:3β-O-[α-L-arabinopyranosyl-(1→2)-β-D-glucuronic acid]-oleanolic acid28-O-β-D-glucopyranosyl ester (GS-6),19α,23-dihydroxyurs-12-en-28-oic acid3β-O-β-D-glucuronopyranoside-6-O-methyl ester (GS-16),19α,23-dihydroxyurs-12-en-28-oic acid3β-O-[β-D-glucuronopyranoside-6-O-methyl ester]-28-O-β-D-glucopyranosyl ester(GS-17),3β-O-α-L-arabinopyranosyl-19α,23-dihydroxy-20α-urs-12-en-28-oic acid28-O-β-D-glucopyranosyl ester (GS-22),3β-O-β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl-19-hydroxy-20α-urs-12-en-28-oic acid28-O-β-D-glucopyranosyl ester(GS-23), urs-12,18-dien-28-oic acid3β-O-β-D- glucuronopyranoside-6-O-methylester(GS-25),3β,23-dihydroxy-20α-urs-12,18-dien-28-oicacid(GS-27),3β-O-α-L-arabinopyranosyl-23-hydroxy-20α-urs-12,18-dien-28-oicacid(GS-28),20α-urs-12,18-dien-28-oic acid3β-O-β-D-glucuronopyranoside-6-O-methylester(GS-29),23-hydroxy-20α-urs-12,18-dien-28-oicacid3β-O-β-D-glucuronopyranoside-6-O-methyl ester (GS-30).Protective effects of compounds GS-1, GS-2, GS-6, GS-7, GS-9, GS-10,GS-11，GS-12,GS-14, GS-15, GS-16, GS-17, GS-20, GS-22, GS-24were tested against H2O2-inducedH9c2cardiomyocyte injury, and the data showed that compounds GS-15, GS-17, GS-20,GS-22had significant cell-protective effects. No significant DPPH radical scavengingactivity was observed for the compounds.