Three new triterpenoids isolated from the aerial parts of Ilex cornuta and protective effects against HO-induced myocardial cell injury / 中国天然药物

In the present study, three new triterpenoids, 23-hydroxyurs-12, 18-dien-28-oic acid 3β-O-α-L-arabinopyranoside (1), 23-hydroxyurs-12, 18-dien-28-oic acid 3β-O-β-D-glucuronopyranoside-6-O-methyl ester (2), and urs-12, 18-dien-28-oic acid 3β-O-β-D-glucuronopyranoside-6-O-methyl ester (3), and a known triterpenoid, 3β-hydroxy-urs-2, 18-dien-28-oic acid (4, randialic acid B), were isolated from the aerial parts of Ilex cornuta. Their structures were identified by the spectroscopic analyses (IR, ESI-MS, HR-ESI-MS, and 1D and 2D NMR) and chemical reactions. Compound 4 showed significant cell-protective effects against HO-induced H9c2 cardiomyocyte injury. Compounds 1-4 did not show any significant DPPH radical scavenging activity.

Antioxidant and cardioprotective effects of Ilex cornuta on myocardial ischemia injury / 中国天然药物

Previous studies have indicated that the Ilex genus exhibits antioxidant, neuroprotective, hepatoprotective, and anti-inflammatory activities. However, the pharmacologic action and mechanisms of Ilex cornuta against cardiac diseases have not yet been explored. The present study was designed to investigate the antioxidant and cardioprotective effects of Ilex cornuta root with in vitro and in vivo models. The anti-oxidative effects of the extract of Ilex cornuta root (ICR) were measured by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging and MTT assays as well as immunoassay. Furthermore, a rat model of myocardial ischemia was established to investigate the cardioprotective effect of ICR in vivo. Eight compounds were isolated and identified from ICR and exhibited DPPH free-radical scavenging activities. They also could increase cell viability and inhibit morphological changes induced by HO or NaSO in H9c2 cardiomyocytes, followed by increasing the SOD activities and decreasing the MDA and ROS levels. In addition, it could suppress the apoptosis of cardiomyocytes. In the rat model of myocardial ischemia, ICR decreased myocardial infarct size and suppressed the activities of LDH and CK. Furthermore, ICR attenuated histopathological alterations of heart tissues and the MDA levels, while increasing SOD activities in serum. In conclusion, these results suggest that ICR has cardioprotective activity and could be developed as a new food supplement for the prevention of ischemic heart disease.

Chemical constituents in stems of Ilex cornuta / 中草药

Objective: To investigate the chemical constituents in the stems of Ilex cornuta and the ability of scavenging free radicals of compounds 1-9. Methods: The compounds were isolated and purified by silica gel, medium pressure column chromatography, and semi-preparative liquid chromatography, and their structures were elucidated by chemical properties and spectroscopic analyses. The antifreeradical efficiency of compounds 1-9 was evaluated by DPPH radical scavenging assay. Results: Fifteen compounds were isolated and their structures were identified as isochlorogenic acid B (1), 3,4,5-tricaffeoylquinic acid (2), 4,5-di-O-caffeoyl quinic acid methyl ester (3), 3,4-di-O-caffeoyl quinicacid methyl ester (4), 3,5-di-O-caffeoyl quinicacid methyl ester (5), 3,4,5-tri-O-caffeoyl quinic acid methyl ester (6), 3,5-dimethoxy-4-hydroxybenzaldehyde (7), ethyl gallate (8), dihydrosyringenin (9), 2,6-dimethoxy-1,4-benzoquinone (10), arctigenin (11), 1-O-(vanillic acid)-6-O-(3″, 5″-dimethoxy-galloyl)-β-D-glycoside (12), (+)-1-hydroxypinoresinol-1-O-β-D-glucopyranoside (13), (+)-(7S,8S)-syringylglycerol 8-O-β-D-glucopyranoside (14), and schaftoside (15). Compounds 1-7 had good antifreeradical efficiency. Conclusion: Compounds 6,8-10,14, and 15 are obtained from the plants of Ilex L. the first time, and compounds 2,7,11, and 12 are obtained from this plant for the first time. Compounds 1-6 have good antifreeradical efficiency.

Identification of “Gonglao Leaf” and Its Sibling Adulterants Based on ITS2 Sequence / 世界科学技术-中医药现代化

Objective: The Phenomenon of different species with the same name has created potential threats to cinical safety of medication. Because of that, two kinds of “gonglao leaf” and their sibling adulterants have been identified by molecular methods in this study, to secure its safety in medication. Methods: Ilexcornuta, Mahoniabealei, Mahoniafortuneiand their sibling adulterants total of 9 species 45 samples were collected in this experiment,Total genomic DNA was extracted from them by the method of improved CTAB, ITS2 sequences were amplified, and the PCR products were sequenced. Sequence assembly and consensus sequence generation were performed by the CodonCode Aligner V 4.2.4.. The genetic distances were computed by MEGA 6.0 in accordance with the Kimura 2-Parameter (K2P) model and the phylogenetic tree constructed by the neighbor-joining (NJ) method. Results: The analysis results of the genetic distances, variable sites and the NJ phylogenetic tree showed that Ilexcornuta, Mahoniabealei, Mahoniafortunei were seperated from their sibling adulterants obviously. Conclusion: ITS2 sequence was able to identify two kinds of “gonglao leaf” and their sibling adulterants which can provide a basis for clinical accurate medication.

Chemical constituents in roots of Ilex cornuta / 中草药

Objective: To study the chemical constituents of the roots of Ilex cornuta. Methods: The compounds were isolated and purified by silica gel, Sephadex LH-20, medium pressure column chromatography, and semi-preparative liquid chromatography, and their structures were elucidated by chemical properties and spectroscop analyses. Results: Eight compounds were isolated and their structures were identified to be β-sitosterol (1), lupeol (2), betulonic acid (3), hede-ragenin (4), 3β-acetoxy-28-hydroxyurs-12-ene (5), ursolic acid (6), 19α-hydroxy ursolic acid (7), 3β-acetoxy-ursolic acid (8), 23-hydroxyl-methyl ursolate (9), heptanoic acid (10), β-daucosterol (11). Conclusion: Compounds 4,5,8, and 9 are obtained from this genus for the first time, and compound 3 is obtained from this plant for the first time.