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Development of gastric precancerous lesion animal model.

Chunying LI ; Aihua LIANG ; Shuangrong GAO ; Lianqiang HUI ; Ting LIU ; Chunyu CAO ; Yong ZHAO ; Ran HAO ; Yan YI ; Jing GUO

China Journal of Chinese Materia Medica.2012;37(1):89-93.

OBJECTIVETo establish a model of gastric precancerous lesion by using Aristolochic manshuriensis which contains aristolochic acids.

METHODThe SD rats were randomly divided into four groups: control and three different doses of ethanol extractive of A. manshuriensis (EEA) (corresponding to aristolochic acid I 2.5, 5.0, 10.0 mg x kg(-1)), respectively. EEA was intragastrically given to rats every other day. At the end of the 10th, 15th, 20th week, part of the rats in each group was sacrificed and the stomachs were weighed. The gastric tumor was assessed by the weight and the relative stomach weight to the body weight. The stomachs were fixed in 4% neutral formalin, and the paraffin imbedding tissues were sliced and HE stained. Histomorphology was observed under the light microscope to determine gastric hyperplasia, mucosa precancerosis (atypical hyperplasia) and gastric cancer formation.

RESULTThe rats treated with different doses of EEA for 10 weeks induced mucosa papillary, epithelioma hyperplasia. Histological observation showed mucosa precancerosis lesions characterized as atypical hyperplasia at the dose levels corresponding to aristolochic acid I 5.0 and 10.0 mg x kg(-1) treated for 10 weeks. The incidence rate of gastric precancerosis in those two groups was 100% at the 15th week. Malignant tumors were observed in most of the animals in 10.0 mg x kg(-1) group. The animals in 5.0 mg x kg(-1) group were well tolerant compared to 10.0 mg x kg(-1) group during the course of experiment, so the dose of aristolochic acid I 5.0 mg x kg(-1) and 10-15 weeks treatment were considered to be optimum to establish the model of gastric precancerosis.

CONCLUSIONA rat model of gastric precancerosis can be induced within a short duration by giving an oral administration of the ethanol extract of A. manshuriensis which contains aristolochic acids.

Animals ; Aristolochia ; chemistry ; Aristolochic Acids ; administration & dosage ; Disease Models, Animal ; Drugs, Chinese Herbal ; administration & dosage ; Humans ; Male ; Rats ; Stomach Neoplasms ; drug therapy ; pathology

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Inhibitory effects of astragaloside IV on cytochrome P450 enzyme of rat liver microsomes.

Wenya SHAN ; Yufeng ZHANG ; Jieqiang ZHU ; Qin SHAO ; Xiaohui FAN

China Journal of Chinese Materia Medica.2012;37(1):85-88.

OBJECTIVETo provide a scientific basis for the drug-combination and aim to examine whether astragaloside IV has the impact on the cytochrome P450 enzymes.

METHODTolbutamide, chlorzoxazone, coumarin, nifedipine, and phenacetin were as probe substrates of rat CYP2C9, CYP2E1, CYP2A6, CYP3A4, and CYP1A2, and were incubated in rat liver microsomes with astragaloside IV. Triplicate samples were run to generate IC50 value by incubating P450 probe substrates in the presence of five concentrations of astragaloside IV in the incubation mixture. The K(i) values were determined by fitting the probe substrate at various inhibitor concentrations to the equations for competitive inhibition, noncompetitive inhibition, noncompetitive inhibition, and mixed-type inhibition.

RESULTIC50 and K(i) values were estimated, and the types of inhibition were determined. Among the five probe substrates, astragaloside IV might not significantly affect CYP2E1, CYP2A6 and CYP1A2-mediated metabolism in rats, but was a competitive inhibitor of CYP2C9 (IC50 35.40 micromol x L(-1), K(i) 42.88 micromol x L(-1)), and was a uncompetitive inhibitor of CYP3A4 (IC50 88.24 micromol x L(-1), K(i) 33.31 micromol x L(-1)).

CONCLUSIONThese results suggested that astragaloside IV inhibited CYP2C9 and CYP3A4, which provided useful information for safe and effective use of astragaloside IV.

Animals ; Cytochrome P-450 Enzyme Inhibitors ; Cytochrome P-450 Enzyme System ; chemistry ; metabolism ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Enzyme Inhibitors ; chemistry ; pharmacology ; Kinetics ; Male ; Microsomes, Liver ; chemistry ; drug effects ; enzymology ; Rats ; Rats, Sprague-Dawley ; Saponins ; pharmacology ; Triterpenes ; pharmacology

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Modulation of aberrant extracellular matrix degradation systems by astragali radix and angelicae sinensis radix decoction (A&A) in interstitial fibrotic kidney.

Liqiang MENG ; Aineng LIAO ; Lei QU ; Jiawei TANG ; Xiaomei LI

China Journal of Chinese Materia Medica.2012;37(1):79-84.

OBJECTIVEThe imbalance between extracellular matrix (ECM) synthesis and degradation induces the excessive ECM deposition and thus renal fibrosis. The decoction (A&A) which is a combination of two Chinese herbs, Astragalus membranaceus var. mongholicus and Angelica sinensis, has been shown to alleviate ECM production in animal models of chronic kidney diseases. In this paper, the effect of A&A on ECM degradation was investigated with interstitial fibrosis in rats.

METHODMale Wistar rats were randomly divided into sham, unilateral ureteral obstruction (UUO) and UAA (UUO plus A&A administration) groups. After administration of A&A (14 g x kg(-1) x d(-1)) by gavage for 3, 7 and 10 days, morphological changes were evaluated by HE, PAS and Sirius red staining technique. The expression of plasminogen activator inhibitor-1 (PAI-1) and tissue-type plasminogen activator (t-PA), the activity of PAI-1 and t-PA were determined by ELISA. The activity of matrix metalloproteinases (MMP-9, MMP-2), tissue inhibitor of matrix metalloproteinase-1 (TIMP-1) were evaluated by gelatin zymography or reverse gelatin zymography, respectively.

RESULTMorphological analysis showed severe interstitial mononuclear cells infiltration, tubular atrophy, renal fibrosis and collagen expression in kidneys of UUO group, which was reduced by A&A administration (P < 0.05, UAA vs UUO group). Compared with the sham group, the expression of PAI-1 was significantly increased in UUO group by 63%, 91% and 112% at day 3, 7 and 10 respectively; and there were a remarkable decrease in UAA group by 44%, 43% and 52% at day 3, 7 and 10. The expression of active PAI-1 was strikingly increased in UUO group at day 3 [(30.5 +/- 23.8) ng x g(-1) vs. (0.0 +/- 0.0) ng x g(-1), P < 0.05)], day 7 [(36.5 +/- 11.2) ng x g(-1) vs. (0.0 +/- 0.0) ng x g(-1), P < 0.05)], and day 10 [(54.5 +/- 14.2) ng x g(-1) vs. (0.5 +/- 0.5) ng x g(-1), P < 0.05)]. The active PAI-1 was decreased in UAA group at day 7 [(14.9 +/- 0.5) ng x g(-1) vs. (36.5 +/- 11.2) ng x g(-1), P < 0.05] and day 10 [(15.4 +/- 4.8) ng x g(-1) vs. (54.5 +/- 14.2) ng x g(-1), P < 0.05]. The expression of t-PA was increased in UUO group only at day 3 [(58.1 +/- 16.5) microg x g(-1) vs. (30.1 +/- 17.3) microg x g(-1)], P < 0.05), meanwhile decreased in UAA group [(26.3 +/- 8.7) microg x g(-1) vs. (58.1 +/- 16.5) microg x g(-1), P < 0.05)]. But the expression of active t-PA was shown no significantly difference among the three groups. For MMP-2 and MMP-9 activity, they were significantly higher compared with the sham group in UUO group, but no significantly change after A&A treatment. The TIMP-1 activity was significantly increased in UUO group by 28% and 63% at day 7 and 10 respectively, significantly decreased in UAA group by 40% and 39% at the same time point.

CONCLUSIONThe anti-fibrosis effects of A&A might be associated with modulating the imbalance of PAs/PAIs system as well as MMPs/TIMPs system, thereby alleviate ECM accumulation and interstitial fibrosis.

Angelica sinensis ; chemistry ; Animals ; Astragalus Plant ; chemistry ; Drugs, Chinese Herbal ; administration & dosage ; Extracellular Matrix ; metabolism ; Fibrosis ; Humans ; Kidney ; enzymology ; metabolism ; pathology ; Kidney Diseases ; drug therapy ; enzymology ; metabolism ; pathology ; Male ; Matrix Metalloproteinase 1 ; metabolism ; Matrix Metalloproteinase 9 ; metabolism ; Plasminogen Activator Inhibitor 1 ; metabolism ; Rats ; Rats, Wistar ; Tissue Plasminogen Activator ; metabolism

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Simultaneous determination of hypocrellin A, hypocrellin B, and hypocrellin C by HPLC.

Ming KONG ; Zhanli CHEN ; Zhiqi YIN ; Jian ZHANG

China Journal of Chinese Materia Medica.2012;37(1):75-78.

OBJECTIVETo develop a high-performance liquid chromatography (HPLC) method for simultaneous determination of hypocrellin A, hypocrellin B, and hypocrellin C.

METHODThe separation was carried out on a Kromasil C18 (4.6 mm x 250 mm, 5 micrm) colum eluted with in mobile phases of water containing 0.5% glacial acetic acid and acetonitrile. The column temperature was 35 degrees C, and the flow rate was 1.0 mL x min(-1). The detection wavelength was set at 265 nm.

RESULTThe three compounds were well separated. Calibration curves of hypocrellin A, hypocrellin B, and hypocrellin C showed good linear relationship RSD > 2.0%. The average recoveries of the hypocrellin A, hypocrellin B, and hypocrellin C were 101.8%, 102.3%, 100.0%, respectively.

CONCLUSIONThe developed method is simple, accurate, and repeatable, and can be readily used as valid tool for the quality control of Hypocrella bambusae.

Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; analysis ; Hypocreales ; chemistry ; Perylene ; analogs & derivatives ; analysis ; Quinones ; analysis

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Simultaneous determination of three homoisoflavonoids in Ophiopogon japonicus by HPLC.

Pintao ZENG ; Hui ZHOU ; Yimin ZHENG ; Xiuying XU ; Shanquan FU

China Journal of Chinese Materia Medica.2012;37(1):71-74.

Three homoisoflavonoids, 6-aldehydo-3-ophiopogonanone A, methyl ophiopogonanone A and ophiopogonanone A from Ophiopogon japonicus were analyzed simultaneously by HPLC with acetonitrile-water containing 0.5% H3 PO4 (58:42) as the mobile phase, and the detection wavelength was set at 296 nm (0-14 min) and 275 nm (14-22 min). The mean recoveries of three homoisoflavonoids were 99.41%-99.86% (RSD 0.82%-1.05%). The linear response ranges of. 6-aldehydo-3-ophiopogonanone A, methyl ophiopogonanone A and ophiopogonanone A were 0.165-0.990 microg (r = 0.999 9), 0.153-0.918 microg (r = 0.999 9), and 0.270-1.620 microg (r = 0.999 9), respectively. This method was certified to be accurate and reliable and can be used for quality control of O. japonicus.
Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; analysis ; Isoflavones ; analysis ; Ophiopogon ; chemistry

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Antitumoral bibenzyl derivatives from tuber of Arundina graminifolia.

Meifeng LIU ; Haoran LV ; Yi DING

China Journal of Chinese Materia Medica.2012;37(1):66-70.

OBJECTIVETo isolate the bibenzyl derivatives from the tuber of Arundina graminifolia and evaluate the anti-tumor activity of these compounds in vitro.

METHODThe constituents have been extracted by 95% alcohol and then isolated by column chromatography on silica gel and Sephedax LH-20. The structures were determined by UV, IR, NMR and MS spectral analysis.

RESULTSix constituents have been isolated, and their structures have been established as 2,7-dihydroxy-1-(p-hydroxylbenzyl)-4-methoxy-9, 10-dihydrophenanthrene (1), 4,7-dihydroxy-1- (p-hydroxylbenzyl)-2-methoxy-9,10-dihydrophenanthrene (2), 3, 3'-dihydroxy-5-methoxybibenzyl (3), (2E) -2- propenoic acid-3-(4-hydroxy-3-methoxyphenyl) -tetracosyl ester (4), (2E) -2-propenoic acid-3- (4-hydroxy-3- methoxyphenyl) -pentacosyl ester (5) and pentadecyl acid (6), respectively.

CONCLUSIONAll compounds except for 3 were isolated from the tuber of A. graminifolia for the first time. Compound 3 with bibenzyl ring opening exhibits stronger anti-tumor activity than that of compounds 1 and 2 with bibenzyl ring closing.

Antineoplastic Agents ; chemistry ; isolation & purification ; pharmacology ; Bibenzyls ; chemistry ; immunology ; isolation & purification ; Cell Line, Tumor ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Humans ; Magnetic Resonance Spectroscopy ; Orchidaceae ; chemistry

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Compounds from fraction with cardiovascular activity of Chrysanthemum indicum.

Yu SUN ; Xiaobin MA ; Jianxun LIU

China Journal of Chinese Materia Medica.2012;37(1):61-65.

In order to investigate the chemical constituents from the fraction with cardiovascular activtiy of Chrysanthemum indicum, the isolation and purification of compounds from this active fraction were performed, and the chemical structures were elucidated by spectral analysis and comparison of the spectral data with those reported in the literature. As a result, twelve compounds were obtained and identified as (2S) -eriodictyol-7-O-beta-D-glucuronide (1), (2S) -eriodictyol-7-O-beta-D-glucoside (2), (2S) -hesperetin-7-O-beta-D-glucuronide (3), luteolin-7-O-beta-D-glucoside (4), luteolin-7-O-beta-D-glucuronide (5), diosmetin-7-O-beta-D-glucuronide (6), quercetin -7-O-beta-D-glucoside (7), (2S)-eriodict-dicaffeoylquinate (8), 3, 5-dicaffeoylquinic acid(9), 3, 5-cis-dicaffeoylquinic acid (10), 1, 5-dicaffeoylquinic acid (11), and 1, 3-dicaffeoylquinic acid (12). The above result indicated that flavonoids were the ma-dicaffeoylquinate (8), 3, 5-dicaffeoylquinic acid (9), 3, 5-cis-dicaffeoylquinic acid (10), 1, 5-dicaffeoylquinic acid (11), and 1, 3-dicaffeoylquinic acid (12). The above result indicated that flavonoids were the major components of the active fraction. Compounds 2, 3, 7, 8 and 10 were obtained from this genus for the first time, and compounds 5, 6, 9, 11, and 12 were first isolated from C. indicum.
Cardiovascular Agents ; chemistry ; isolation & purification ; Chromatography, High Pressure Liquid ; Chrysanthemum ; chemistry ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Magnetic Resonance Spectroscopy ; Molecular Structure

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Studies on chemical constituents from fruits of Forsythia suspense.

Qiongyu ZOU ; Wenlong DENG ; Shunyuan JIANG ; Lei ZHANG ; Shulin PENG ; Lisheng DING

China Journal of Chinese Materia Medica.2012;37(1):57-60.

Twenty-four compounds in the fruits of Forsythia suspensa were isolated and purified by column chromatography and preparative TLC. On the basis of comprehensive spectroscopic methods including IR, ESI-MS/MS, 1D and 2D NMR, these compounds were identified as ten ceremides (1-10), six triterpenes (11-16), one steroids (17), three flavonoids (18-20), two C6-C2 alcohols (21-22) and two lignans (23-24). Compounds 1-10 were reported from F. suspense for the first time, among which 1, 2, 4 and 5 were new ones.
Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Forsythia ; chemistry ; Fruit ; chemistry ; Magnetic Resonance Spectroscopy ; Molecular Structure

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Pharmacokinetics effect of shaoyao gancao compound with different decocting methods on characteristic ingredients in rat plasma after oral administration.

Lan SHEN ; Rongwan HU ; Xiao LIN ; Yanlong HONG ; Yi FENG ; Desheng XU ; Kefeng RUAN

China Journal of Chinese Materia Medica.2012;37(1):52-56.

OBJECTIVETo observe the pharmacokinetic effect of Shaoyao Gancao compound on rats using different decocting methods, and to pharmacokinetically detect the the compatibility of the component compounds of the Shaoyao Gancao compound from the pharmacokinetic viewpoint.

METHODBased on the established HPLC analytical method of plasma effective constituents, rats were orally administered with a single or mixed decoction of Shaoyao and Gancao. Blood at different times after administering these decoctions were collected, and then variance analysis was made for pharmacokinetic parameters.

RESULTThe results of all six rats indicated that the absorption of the mixed decoction of Shaoyao and Gancao was greater than that of the single decoction. While, the absorption of the characteristic peaks at the retention time of 5.2, 11.0, 12.0, 14.6 min had statistical significance.

CONCLUSIONShaoyao Gancao compound was proved better than that of the single decoction from the pharmacokinetic viewpoint.

Administration, Oral ; Animals ; Biological Availability ; Chromatography, High Pressure Liquid ; Drug Compounding ; methods ; Drugs, Chinese Herbal ; administration & dosage ; analysis ; pharmacokinetics ; Male ; Paeonia ; chemistry ; Plasma ; chemistry ; Rats ; Rats, Sprague-Dawley

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Study on preparation of Dange Mingmu in-situ forming eye gel.

Zhigang WANG ; Yanjiao WANG ; Hui LI ; Chen ZANG ; Baoxian ZHANG

China Journal of Chinese Materia Medica.2012;37(1):46-51.

OBJECTIVETo prepare Dange Mingmu in-situ forming eye gel.

METHODThe viscosity of Dange Mingmu in-situ forming eye gel was tested by adopting poloxamer 407 and 188 as thermosensitive materials, and optimizing by uniform design. Drug release in vitro was studied using a novel membraneless model. Eye irritation experiments were performed with rabbits. The duration of residence time in rabbit eyes was observed using fluorescence tracer method.

RESULTThe gelation temperature of in-situ thermosensitive gel was lowered as the P407 concentration increased. In a certain range, the gelation temperature slowly increased with the increase of P188's concentration, and the effect of P407 was greater than that of P188. The optimized concentration of P407/P188 was 19%/1%. Based the adjusted concentration, Dange Mingmu in-situ forming eye gel. was converted into freely flowing liquid below 26.9 degrees C and became gel at 34.5 degrees C after being diluted with STF. In line with zero-order kinetics, drug release in vitro depends on gel erosion. The residence time on the surface of eyes was proved to be relatively long was and nonirritant.

CONCLUSIONUniform design is available for optimizing the formulation of thermosensitive gel for eye. The gel satisfies the requirement for ophthalmic application, and is expected to be applied in clinical practice in the future.

Animals ; Drug Compounding ; methods ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Eye Diseases ; drug therapy ; Gels ; chemistry ; pharmacology ; Humans ; Ophthalmic Solutions ; chemistry ; pharmacology ; Rabbits ; Temperature ; Viscosity

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