Hepatoprotective activity of Zha Xun and its different solvent-eluting components / 药学学报

A pharmacophore-based study was conducted to investigate the therapeutic activity of the traditional Tibetan medicine Zha Xun (ZX) in liver diseases. In the present study, the protective effect of ZX on the acute liver injury induced by concanavalin A (ConA) and 0.15% carbon tetrachloride (0.15% CCl4) in ICR mice was evaluated, and the results showed that ZX significantly reduced serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in the ConA-induced acute immune liver injury model and the CCl4-induced acute oxidative liver injury model (P < 0.05). Subsequently, the protective effects of aqueous, 95% ethanol, 60% ethanol and 30% ethanol eluting fractions of ZX, and fulvic acid, the main water-soluble constituent of ZX, were evaluated against acute oxidative liver injury induced by 0.15% CCl4 in mice. The results showed that different solvent-eluting fractions of ZX showed certain hepatoprotective activities, among which the aqueous extract of ZX and 30% ethanol extract of ZX significantly reduced the serum levels of ALT, AST, and lactate dehydrogenase (LDH) in mice (P < 0.05), and the serum levels of LDH in mice were significantly reduced by fulvic acid (P < 0.05), which showed significant hepatoprotective activity. The protective activities and preliminary mechanisms of the total extract of ZX, the aqueous extract of ZX, the 30% ethanol extract of ZX, and fulvic acid against hepatocellular injury in vitro were further evaluated by using the H2O2-induced hepatocellular injury model. The results showed that the components could significantly inhibit H2O2-induced hepatocellular injury, reduce the levels of ALT, alkaline phosphatase (ALP), and LDH, improve the survival rate of hepatocellular cells, and reduce the content of intracellular reactive oxygen species (ROS) in cell culture. At the same time, it can inhibit hepatocyte apoptosis by increasing the expression ratio of Bcl-2/BAX protein and decreasing the expression ratio of cleaved caspase-3/pro caspase-3 protein. The present study showed that ZX has clear hepatoprotective activity in vitro and in vivo, and the different solvent elution fractions of ZX showed certain hepatoprotective activity, among which the aqueous extract of ZX, 30% ethanol extract of ZX had better hepatoprotective activity, and the activity of 60% ethanol extract of ZX was stronger than that of 95% ethanol extract of ZX. The activity of ZX and its water-soluble elution site exerted hepatoprotective effects by inhibiting hepatocyte apoptosis and oxidative stress. The animals used in this experiment and related disposal meet the requirements of animal welfare, and have been reviewed and approved by the Laboratory Animal Management and Use Committee of the Institute of Materia Medica, Chinese Academy of Medical Sciences (approval number: 00004018).

A new polycyclic polyprenylated acylphloroglucinol from Hypericum pseudohenryi / 药学学报

Eight polycyclic polyprenylated acylphloroglucinols (PPAPs) were isolated from the 95% ethanol extract of Hypericum pseudohenryi by MCI column, silica gel column and preparative HPLC. These compounds were defined as hypseudohenrin L (1), hyperbeanin P (2), furohyperforin (3), furoadhyperforin (4), ascyronone F (5), attenuatumione E (6), hyphenrone T (7) and hyperforatone N (8), compound 1 is a new compound. Compounds 1, 3, 5, 7 showed an inhibitory effect on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in macrophage cells.

Chemical constituents of triterpenoids from Euphorbia resinifera / 中国中药杂志

The combination of normal-phase silica gel column chromatography, octadecyl silica(ODS) column chromatography, semi-preparative high performance liquid chromatography(HPLC), etc. was employed to isolate and purify the chemical components from Euphorbia resinifera, and 7 triterpenoids were separated from the ethanol extract of the medicinal materials. Their structures were identified by various spectroscopy methods as cycloartan-1,24-diene-3-one(1), cycloartan-1,24-diene-3-ol(2), 3β-hydroxy-lanosta-8,24-diene-11-one(3), lnonotusane C(4), eupha-8,24-diene-3β-ol-7,11-dione(5), eupha-24-methylene-8-ene-3β-ol-7,11-dione(6), and eupha-8,24-diene-3β,11β-diol-7-one(7). Compounds 1 and 2 are new compounds, and compound 3 is obtained from nature for the first time.

Chemical constituents from Hypericum curvisepalum / 中国中药杂志

This study explored the chemical constituents of the aerial part of Hypericum curvisepalum. Sixteen compounds were isolated from the 95% ethanol extract of H. curvisepalum with various chromatographic techniques, including a new prenylated phenyl polyketide, mysorenone D(1). Other compounds were mysorenone-A(2), mysorenone-C(3), mysorenone-B(4), peplidiforone A(5), 4-methoxy-3-(2-methylbut-3-en-2-yl)-6-phenyl-2H-pyran-2-one(6), hyperenone-A(7), 4-(3,3-dimethylallyl)oxy-6-phenyl-α-pyrone(8), peplidiforone B(9), elegaphenone(10), hypercohin A(11), hyperisampsin G(12), spathulenol(13), quercetin(14), β-sitosterol(15), and β-amyrin(16).

A new 2,3-dioxoflavonoid from the aerial part of Hypericum perforatum / 药学学报

Phytochemical study of the aerial parts of Hypericum perforatum L. resulted in the isolation of an undescribed compound, which was identified as Rel-(2S,3R)-2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-2-methoxy-3-(2-oxopropyl)chroman-4-one (1) by spectroscopic methods including UV, IR, HR-ESI-MS, 1D and 2D NMR spectra. Compound 1 is a new 2,3-dioxo-flavone with an acetonyl moiety, rarely found in nature. In addition, a plausible biogenetic pathway of 1 was proposed in this article.

Chemical constituents of Hypericum perforatum / 中国中药杂志

A chemical investigation on the aerial parts of Hypericum perforatum resulted in the isolation of a new phloroglucinol derivatives (1), and seven known compounds (2-8). The structures of the compounds were elucidated by means of spectroscopic methods (MS, IR, 1D NMR, and 2D NMR) as 3-methyl-4,6-di (3- methyl-2-butenyl)-3-(4-methyl-3-pentenyl)-2-(2-ethyl-1-oxobutyl)-cyclohexanone (1)，hyperforin (2)，(2R,3R,4S,6)-3-methyl-4,6-di(3-methyl-2-butenyl)-2-(2-methyl-1-oxo-propyl)-3-(4-methyl-3-pentenyl)-cyclohexanone (3)，hyperscabrin B (4)，hyperscabrin C (5)，furohyperforin isomer 1 (6)，furoadhyperforin (7)，and furohyperforin (8). Compound 1 was a new compound, and compounds 3-5 were obtained from H. perforatum for the first time.

Advances in secondary metabolites produced by actinobacteria derived from animal-microbe mutualism and their biological activities / 药学学报

Actinobacteria remain to be one of the major sources for new antibiotics, which historically play an essential role in human's fight against infectious diseases. Due to the emergence of resistant pathogenic microorganisms such as bacteria, fungi and viruses, it is imperative to develop new and effective drugs against these pathogens. The symbiotic actinobacteria residing inside the animals are becoming more and more important as a new source for drug discovery, as well as a "hotspot" in the field of microbial medicine. During the long period of evolution, a specific host-microbe mutualism is formed between the symbiotic bacteria and their hosts of animals. In this unique ecosystem, the secondary metabolites produced by bacteria are well tolerated by the hosts, meanwhile, are able to selectively suppress pathogenic microorganisms, thus providing a specific protection to their hosts. These secondary metabolites encompass a large variety of structural diversities of natural products, and so far, the reported biological activities are including antibacterial, antifungal, antiviral, antitumor, and immunomodulatory effects, which give them a great potential in the field of drug discovery. Herein, we review the secondary metabolites of animal symbiotic actinobacteria and their biological activities within the recent decade, by which to provide a viewpoint for future research of drug discovery from actinobacteria.

Chemical constituents of Myripnois dioica / 中国中药杂志

To study the chemical constituents of the aerial parts of Myripnois dioica. Twelve compounds were separated from the 95% ethanol extract of M. dioica by using various chromatographic techniques. Their stuctures were identified on the basis of their physicochemical properties and spectral data as 8-desoxyurospermal A(1), zaluzanin C(2), dehydrozaluzanin C(3), glucozaluzanin C(4), macrocliniside B(5), macrocliniside I(6), taraxinic acid-14-O-β-D-glucopyranoside(7), ainsliaside B(8), apigenin(9), luteolin(10), apigenin-7-O-β-D-glucopyranoside(11), and luteolin-7-O-β-D-glucopyranoside(12). Except for compound 8, the other compounds were isolated from this genus for the first time. Compound 8 was found to decrease blood glucose level properly in alloxan-induced diabetic mice.

A new lanostane-type triterpenoid from Cymbopogon citratus / 中国中药杂志

To study the chemical constituents of Cymbopogon citratus, isolation and purification of constituents were carried out on silica gel, Sephadex LH-20 and prepatative HPLC. The structures of the compounds were identified by physicchemical properties and spectral data analysis. Eight compounds were isolated and identified as 3beta-methoxy lanosta-9(11)-en-27-ol (1), 3beta-hydroxylanosta-9 (11)-en (2), (24S) -3beta-methoxylanosta-9(11), 25-dien-24-ol (3), 8-hydroxyl-neo-menthol (4), (2E)-3,7-dimethyl-2,7-octadiene-1, 6-diol (5), (+)-citronellol (6), 7-hydroxymenthol (7) and ethyl nonadecanoate(8). Compounds 1 is a new one. Compounds 2-3 are obtained from C. citratus for the first time.

Studies on chemical constituents from Davidia involucrata var. vilmoriniana / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Davidia involucrata var. vilmoriniana.</p><p><b>METHOD</b>The chemical constituents were isolated by column chromatography on silical gel and sephadex LH -20. Their structures were elucidated on the basis of spectral analysis and physical constants.</p><p><b>RESULT</b>Seven compounds were isolated from this plant and the structures of them were identified as 3, 4, 5-trihydroxybenzoic acid (1), ellagic acid (2), maleic acid (3), quercetin (4), quercetin-3-O-beta-D-galactoside (5), 2alpha, 3alpha, 19alpha, 23-tetrahydroxyurs-12-en-28-oic-acid-28-O-beta-D-glucopyranosyl ester (6), ethyl brevifolin carbosylate (7), respectively.</p><p><b>CONCLUSION</b>Compounds 1-7 were isolated from this plant for the first time.</p>

Studies on chemical constituents of Artemisia rupestris (II) / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Artemisia rupestris.</p><p><b>METHOD</b>The chemical constituents were isolated by column chromatography on silica gel, polyamide and Sephadex LH-20. Their structures were elucidated on the basis of spectral analysis.</p><p><b>RESULT</b>11 compounds have isolated from this plant, and the structure of them have identified as robinin (1), quercetin (2), linearin (3), luteolin (4), sucrose (5), tilianin (6), luteolin-7-glucoside (7), beta-D-3'-methoxy-4'-O-P-coumaroylglucoside (8), hirsutine (9), 3-(4-methoxy phenyl)-(E)-2-propenoic acid ethyl ester (10), rutin (11).</p><p><b>CONCLUSION</b>All this compounds have been isolated from this plant for the first time.</p>

Studies on hypoglycemic effect of extract of Balaophora polyandra in mice / 中国中药杂志

<p><b>OBJECTIVE</b>To study the hypoglycemic effect of the extract of B. polyandra (SHG).</p><p><b>METHOD</b>The diabetic mice were induced by alloxan in ICR mice. The blood glucose concentration was measured by glucose oxidase method. The serum insulin level was determined by 125I-insulin radioimmunoassay kit. The hypoglycemic effect was evaluated by the levels of both fasting and no-fasting blood glucose. The effect on serum insulin level was estimated by the values of the blood insulin and the changes of the blood glucose induced by the glucose intraperitoneal injection. The effect on the glucose absorption was investigated by the oral sucrose or starch tolerance test.</p><p><b>RESULT</b>Both of the fasting and no-fasting blood glucose levels were decreased significantly by the treatment of 20 or 30 g raw materials crude drug x kg (-1) SHG orally for 7-10 d in ICR mice or in alloxan diabetic mice. In the oral sucrose tolerance test or oral starch tolerance test, the administration of SHG reduced significantly the peak value of the blood glucose and the area under the blood glucose-time curve (AUC) in normal or alloxan diabetic mice, respectively. These effects of SHG were similar to those of acarbose, a kind of alpha-glucosidase inhibitors. In the oral glucose tolerance test in normal and alloxan diabetic mice, SHG decreased both the blood glucose peak and the AUC induced by the glucose loading. But in the intraperitoneal injection glucose tolerance test the levels of insulin in both SHG and control mice were similar, however, the changes of the blood glucose level after the glucose-loading for 30 min in SHG mice was much lower than that in control mice.</p><p><b>CONCLUSION</b>With the treatment of SHG, the fasting and no-fasting blood glucose concentrations were decreased and the glucose tolerance improved significantly in both normal and alloxan diabetic mice, and the inhibition of a-glucosidase might be one of its major mechanisms.</p>

Studies on chemical constituents in herb from Artemisia rupestris / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Artemisia rupestris.</p><p><b>METHOD</b>The chemical constituents were isolated by column chromatography on silical gel and sephadex LH - 20. Their structures were elucidated on the basis of spectral analysis.</p><p><b>RESULT</b>8 compounds have isolated from this plant, and the structures of them have identified as rupestonic acid (1), chrysosplenetin B (2), artemetin (3), herniarin (4), isokaempferide (5), vanillic acid (6), kaempferol 3, 3', 4'-trimethyl ether (7) and ermanine (8).</p><p><b>CONCLUSION</b>Compounds 2-8 have been isolated from this plant for the first time.</p>