The chemical constituents from the leaves of Ilex guayusa were investigated. Sixteen triterpenoids were isolated from the 95% ethanol extract of dried leaves of I. guayusa by silica gel, Sephadex LH-20, and ODS column chromatographies and semi-prepa-rative HPLC. Those triterpenoids were identified by NMR, HR-MS, and literature analysis: 3β-hydroxy-11α,12α-epoxy-24-nor-urs-4(23)-ene-28,13β-olide(1), 3β-hydroxy-24-nor-4(23),12-oleanadien-28-methyl ester(2), oleanolic acid(3), 3β,28-dihydroxy-12-oleanene(4), 2α,3β-dihydroxy-11α,12α-epoxy-24-'nor-olean-4(23)-ene-28,13β-olide(5), ursolic acid(6), 3β,23-dihydroxy ursolic acid(7), 3β,28-dihydroxy-12-ursene(8), 3β-28-nor-urs-12-ene-3,17-diol(9), 3β-hydroxyurs-11-ene-28,13β-olide(10), 13β,28-epoxy-3β-hydroxy-11-ursene(11), 3β-hydroxy-28,28-dimethoxy-12-ursene(12), 3β-hydroxy-24-nor-urs-4(23),12-dien-28-oic acid(13), 3β-hydroxy-24-nor-urs-4(23),12-dien-28-methyl ester(14), 2α,3β-dihydroxy-11α,12α-epoxy-24-nor-urs-4(23)-ene-28,13β-olide(15) and 2α,3β-dihydroxy-11α,12α-epoxy-24-nor-urs-4(23),20(30)-dien-28,13β-olide(16). Compounds 1-2 were new compounds, and compounds 4-5, 7 and 9-16 were isolated from I. guayusa for the first time.
Drugs, Chinese Herbal ; Ilex guayusa ; Molecular Structure ; Oleanolic Acid ; Plant Leaves ; Triterpenes

Yerba Mate, derived from the leaves of the tree, Ilex paraguariensis, is widely-used as a tea or as an ingredient in formulated foods. The aim of the present study was to evaluate the effects of Yerba Mate extract on weight loss, obesity-related biochemical parameters, and diabetes in high-fat diet-fed mice. To this end, by using in vivo animal models of dietary-induced obesity, we have made the interesting observations that Yerba Mate has the ability to decrease the differentiation of pre-adipocytes and to reduce the accumulation of lipids in adipocytes, both of which contribute to a lower growth rate of adipose tissue, lower body weight gain, and obesity. Our data from in vivo studies revealed that Yerba Mate treatment affects food intake, resulting in higher energy expenditure, likely as a result of higher basal metabolism in Yerba Mate-treated mice. Furthermore, in vivo effects of Yerba Mate on lipid metabolism included reductions in serum cholesterol, serum triglycerides, and glucose concentrations in mice that were fed a high fat diet. In conclusion, Yerba Mate can potentially be used to treat obesity and diabetes.
Adipocytes ; Adipose Tissue ; Animals ; Basal Metabolism ; Body Weight ; Cholesterol ; Diet, High-Fat ; Eating ; Energy Metabolism ; Food, Formulated ; Glucose ; Ilex paraguariensis ; Lipid Metabolism ; Mice ; Models, Animal ; Obesity ; Tea ; Trees ; Triglycerides ; Weight Loss

OBJECTIVETo establish a RP-HPLC method for the determination of tortoside A in Ilex pubences.

METHODKromasil-C18 (4.6 mm x 250 mm, 5 microm) column was used in HPLC with mobile phase acetonitrite-0.1% H3PO4 (17:83), the column temperature was 30 degrees C, the flow rate was 1 mL x min(-1), the detection wavelength was set at 210 nm, and inject volume was 10 microL RESULT: Tortoside A was well separated under the established conditions, the liner range of tortoside A was 26.05-521.00 microg (r = 0.999 9, n = 6), and the average recovery was 98.42%.

CONCLUSIONIt was the first time to establish the RP-HPLC method with accuracy, good reproducibility for determining the content of tortoside A in I. Pubescentis.

Chromatography, High Pressure Liquid ; methods ; Glycosides ; analysis ; Ilex ; chemistry

This study intends to develop a high performance liquid chromatography-diode array detection(HPLC-DAD) method for simultaneous determination of chlorogenic acid, 2-hydroxymethyl-3-hydroxyl-1-butene-4-O-β-D-(6″-O-caffeoyl)-glucopyranoside, pubescenoside B, huazhongilexone-7-O-β-D-glucopyranoside, rutin, isochlorogenic acid B, isochlorogenic acid A, isochlorogenic acid C in Ilex hainanensis. The HPLC conditions are as follows: Waters XBridge C_(18 )column(4.6 mm×250 mm, 5 μm), mobile phase of 0.5% formic acid in water(A)-acetonitrile(B), gradient elution(0-8 min, 5%-12% B; 8-18 min, 12%-18% B; 18-30 min, 18%-25% B; 30-40 min, 25%-30% B; 40-42 min, 30%-80% B; 42-45 min, 80% B) at the flow rate of 0.8 mL·min~(-1), detection wavelengths of 282, 324, and 360 nm, column temperature of 25 ℃, and injection volume of 5 μL. The content of the 8 phenols in 8 samples was 0.30-6.29, 0.29-3.27, 0.15-10.4, 0.51-5.85, 0.49-9.02, 0.51-4.68, 1.93-13.4, and 0.87-5.95 mg·g~(-1), respectively. Moreover, the content of phenols in the samples collected in October was higher than that of samples harvested in other months. The established method is accurate and sensitive for the determination of phenols in I. hainanensis, which is useful for the quality improvement of this herbal medicine.
Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; Ilex ; Phenols

OBJECTIVETo investigate the chemical constituents of Ilex cornuta.

METHODThe chemical constituents were isolated by column chromatographic methods. And the structures were identified by spectral data.

RESULTSeven compounds were isolated and identified as follows: 2alpha-hydroxy ursolic acid (1), arjunolic acid (2), 23-hydroxy ursolic acid (3), 27-0-p-(Z) -coumaroyl ursolic acid (4), 27-O-p-(E)-coumaroyl ursolic acid (5), asiatic acid (6).

CONCLUSIONCompound 1, 2 were obtained from this genus for the first time and 3-6 from this plant for the first time.

Ilex ; chemistry ; Magnetic Resonance Spectroscopy ; Pentacyclic Triterpenes ; Plant Leaves ; chemistry ; Triterpenes ; chemistry

Nine compounds were isolated from the leaves of Ilex latifolia. Their structures were respectively identified as 5-hydroxy-6, 7, 8, 4'-tetramethoxyflavone (1), tangeretin (2), nobiletin (3), 5-hydroxy-6, 7, 8, 3', 4'-pentamethoxyflavone (4), 5, 6, 7, 8, 4'-pentamethoxyflavonol (5), 5, 6, 7, 8, 3', 4'-hexamethoxy-flavonol (6), 5-hydroxy-3', 4', 7-trimethoxyflavanone (7), soyacerebroside I (8), and soyacerebroside II (9) by their physicochemical properties and spectroscopic data Compounds 1-9 were isolated from this plant for the first time.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Ilex ; chemistry ; Plant Leaves ; chemistry

OBJECTIVETo develop a HPLC-ELSD method for determination of ilexside II in leaves of Ilex cornuta.

METHODThe separation was performed on a Waters Syemmetry Shield RP18 column (4.6 mm x 250 mm, 5 microm) and methanol-water was used as mobile phase in gradient elution. The flow was 1.0 mL x min(-1), and the temperature was set at 35 degrees C.

RESULTThe calibration curve showed good linearity in the test range (R2 = 0.9997). And the mean recovery was 101.3%, RSD was 2.0% (n=6).

CONCLUSIONThe developed HPLC-ELSD method was accurate and reproducible, and can be used for the determination of ilexside II in leaves of Ilex cornuta.

Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; analysis ; Glycosides ; analysis ; Ilex ; chemistry ; Plant Leaves ; chemistry ; Triterpenes ; analysis

OBJECTIVETo investigate the chemical constituents of Ilex pernyi.

METHODThe chemical constituents were isolated by various column chromatographic methods. The structures were identified by spectral data.

RESULTEight triterpenoid compounds were isolated and identified as ursolic acid (1), lupeol (2), alpha-amyrin (3), uvaol (4), 3beta-hydroxyurs-11-ene-13beta-olide (5), pomolic acid (6), lup-20 (29)-ene-3beta, 24-diol (7), 3beta, 23-dihydroxy-urs-12-en-28-oic acid (8).

CONCLUSIONThe eight compounds were obtained from this plant for the first time.

Ilex ; chemistry ; Oleanolic Acid ; analogs & derivatives ; chemistry ; isolation & purification ; Plant Leaves ; chemistry ; Plants, Medicinal ; chemistry ; Triterpenes ; chemistry ; isolation & purification

Cardio-cerebral vascular disease induced by atherosclerosis is a serious cause of human health. The pathogenesis of AS is very complex,and the oxidized low-density lipoprotein( ox LDL) induced foam cells formation is considered to be the most important cytological change in AS. Based on the definition of " TCM chemical biology",we clarified the chemical composition of Ilex hainanensis,the effective substances of I. hainanensis on the activity of anti-AS were screened. Then we found that saponin BF523 had the good inhibitory effect on foam cell formation. In this research,we studied the BF523 as the research object to clarify the molecular target of the active compound of I. hainanensis by foam cell formation model. The results showed that BF523 significantly inhibited the oxidation of ox LDL-induced macrophage foaming and decreased the lipid content in macrophages. BF523 had inhibited the phagocytosis of ox LDL in macrophages by reducing the mRNA and protein levels of scavenger receptor CD36,thereby inhibiting the occurrence and development of AS. These findings not only clarified the mechanism of the inhibition of foam cell formation by saponin BF523,but also provided a useful exploration for the enrichment of the theory of " TCM chemical biology".
Atherosclerosis ; CD36 Antigens ; metabolism ; Cells, Cultured ; Foam Cells ; cytology ; drug effects ; Humans ; Ilex ; chemistry ; Lipoproteins, LDL ; adverse effects

AIM: To study the chemical constituents of the roots of Ilex asprella Champ. ex Benth. METHODS: Compounds were isolated by silica gel, ODS, and Sephadex LH-20 column chromatography, and their structures were elucidated on the basis of physicochemical properties and spectroscopic analysis. RESULTS: Four triterpenoid glycosides were isolated and identified as (3β)-19-hydroxy-28-oxours-12-en-3-yl β-D-glucopyranosiduronic acid n-butyl ester (1), ilexasoside A (2), monepaloside F (3), and ilexoside A (4). CONCLUSION Compound 1 is a new triterpenoid glycoside, and compounds 3 and 4 were isolated from this plant for the first time.
Glycosides ; chemistry ; isolation & purification ; Ilex ; chemistry ; Molecular Structure ; Plant Extracts ; chemistry ; isolation & purification ; Plant Roots ; chemistry ; Triterpenes ; chemistry ; isolation & purification