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Chemical constituents of the rhizome of Matteuccia struthiopteris.

Lan YANG ; Man-yyan WANG ; Yu-ying ZHAO ; You-you TU

Acta Pharmaceutica Sinica.2005;40(3):252-254.

AIMTo study the chemical constituents of the rhizome of Matteuccia struthiopteris (L.) The constituents were separated and purified by column chromatography with normal Todaro.

METHODSphase silica gel and Sephadex LH-20. Their structures were identified on the basis of physical and spectral data (MS, NMR, HMBC and HMQC).

RESULTSFour compounds were isolated and identified as 1-O-beta-D-gl ucopyranosyl-(2S,3R,4E, 8Z) -2-N-(2'-hydroxydocosanoyl) eicosasphinga-4,8-dienine (1), 1-O-beta-D-galactosyl-(6-->1)-alpha-D-galactosyl-2,3-O-dihexadecanoyl-glycerol (2), succinic acid (3), D-mannitol (4).

CONCLUSIONCompounds 1 and 2 are new compounds. Compounds 3 and 4 were isolated from this plant for the first time.

Ferns ; chemistry ; Galactosides ; chemistry ; isolation & purification ; Glucosides ; chemistry ; isolation & purification ; Glycerides ; chemistry ; isolation & purification ; Mannitol ; chemistry ; isolation & purification ; Molecular Conformation ; Molecular Structure ; Plants, Medicinal ; chemistry ; Rhizome ; chemistry ; Succinic Acid ; chemistry ; isolation & purification

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Isolation and structure identification of chemical constituents from Anabasis brevifolia.

Hua CHEN ; Aisa HAJIA ; Zhong-duo YANG ; Yuan-chao LI

Acta Pharmaceutica Sinica.2005;40(3):248-251.

AIMTo study the chemical consitituents of the n-butanol-extracts of Anabasis salsa and Various chromatographic techniques were used to the chloroform-extract of Anabasis brevifolia.

METHODSseparate and purify the constituents. Their physico-chemical properties and spectral data were used to elucidate their structures.

RESULTSFive compounds were isolated and identified as 2-O-beta-D-glucopyranosyloxy-4,6-dimethoxy phenylenthanone (1), 2-O-(2)-beta-D-glucopyranosyloxy-4, 6-dimethoxy phenylenthanone (2), 3-methyl-but-2-enoic acid-[2-(4-methoxy phenyl)-ethyl]-amide (3), 5,6,7,2'-tetramethoxy isoflavonoid (4), 2'-hydroxy-5,6,7-trimethoxyisoflavonoid (5).

CONCLUSIONCompounds 2, 3, and 5 are new compounds. And the others were isolated from Anabasis L. for the first time.

Chenopodiaceae ; chemistry ; Crotonates ; chemistry ; isolation & purification ; Glucosides ; chemistry ; isolation & purification ; Isoflavones ; chemistry ; isolation & purification ; Molecular Structure ; Plants, Medicinal ; chemistry

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Synthesis and antitumor activity of A-ring modified hexacyclic analogues of camptothecin.

Di-zao LI ; Cun-ying WANG ; Xian-dao PAN ; Hong-yan LIU ; Zhao-di FU ; Song WU

Acta Pharmaceutica Sinica.2005;40(3):241-247.

AIMTo improve the biological activity of A-ring modified analogues of camptothecin.

METHODSA-ring modified camptothecins were synthesized from 10-hydroxycamptothecin or 7-ethyl-10-hydroxycamptothecin (SN-38) in three or four steps. Their cytotoxicity was evaluated using MTY assay, and their in vivo antitumnor activity against mouse liver cancer H22 was tested. Results Five hexacyclic camptothecins (6a, 6b, 6c, 7a and 7b) are target compounds, and ten camptothecin derivatives are new compounds.

CONCLUSIONThe modification of a 1,4-oxazine-2-one ring fused with positions 9 and 10 of A-ring will reduce the antitumor activity of camptothecins.

Animals ; Antineoplastic Agents ; chemical synthesis ; pharmacology ; Camptothecin ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology ; Carcinoma, Hepatocellular ; drug therapy ; pathology ; Cell Line, Tumor ; drug effects ; Female ; Humans ; Liver Neoplasms ; drug therapy ; pathology ; Mice ; Neoplasm Transplantation ; Polycyclic Compounds ; chemical synthesis ; pharmacology

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Location and relative quantity of coumarins in the stem of Dendrobium thyrsiflorum.

Yan ZHENG ; Luo-shan XU ; Zheng-tao WANG ; Chao-ying ZHANG

Acta Pharmaceutica Sinica.2005;40(3):236-240.

AIMTo determine the location and relative quantity of coumarins in the stem of Dendrobium thyrsiflorum Rchb. f. , and to provide a scientific basis for evaluating and utilizing the famous medicinal plant.

METHODSThe stems of one, two and three years old, separately, were collected in February. Location and relative quantity of coumarins in the top, middle and basal parts of each stem sample were determined by using laser scanning confocal microscopy (LSCM). ANOVA and Tukey's test were employed in the statistical analysis.

RESULTSThe coumarins located mainly in vascular bundles, especially on the walls of the outer fiber cells. There was significant difference or great significant difference exist in every part of the stem from different ages. The values of significant difference were as follows: basal part P = 0.004 (< 0.01); middle part P = 0.009 (< 0.01); top part P = 0.036( < 0.05).

CONCLUSIONTwo years old stem could be the best choice when collecting Dendrobium thyrsiflorum in Feburary.

Coumarins ; analysis ; Dendrobium ; chemistry ; Microscopy, Confocal ; Plant Stems ; chemistry ; Plants, Medicinal ; chemistry ; Time Factors

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Effect of epigallocatechingallate on acute lung injury induced by oleic acid in mice.

Guang-lin XU ; Lin YAO ; Shu-qin YU ; Dan BU ; Yan-fei WANG ; Zhu-nan GONG ; Shuang-quan ZHANG

Acta Pharmaceutica Sinica.2005;40(3):231-235.

AIMTo investigate the effect of epigallocatechingallate (EGCG) on acute lung injury induced by oleic acid in mice and the possible mechanism.

METHODSAcute lung injury was induced by oleic acid in mice. Light microscopy and electron microscopy were used to examine histological changes and lung index as well as wet to dry weight ratio was calculated. Serum TNF-a level was measured by enzyme linked immunosorbent assay (ELISA) and the phosphorylation of p38 MAPK was determined by Western blotting.

RESULTSPretreatment of EGCG significantly alleviated oleic acid induced lung injury accompanied by reduction of lung index and wet to dry weight ratio, decreased of TNF-a level in serum and inhibition of phosphorylation of p38 MAPK.

CONCLUSIONEGCG showed beneficial effect on acute lung injury induced by oleic acid in mice. The ultimate reduction of TNF-alpha in serum caused by inhibition of phosphorylated p38 MAPK is involved in the mechanism of action of EGCG.

Animals ; Catechin ; analogs & derivatives ; pharmacology ; Lung ; pathology ; ultrastructure ; Male ; Mice ; Oleic Acid ; Phosphorylation ; drug effects ; Protective Agents ; pharmacology ; Respiratory Distress Syndrome, Adult ; chemically induced ; metabolism ; pathology ; Tumor Necrosis Factor-alpha ; metabolism ; p38 Mitogen-Activated Protein Kinases ; metabolism

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Ginsenoside Rbl attenuates beta-amyloid peptide25-35 -induced tau hyperphosphorylation in cortical neurons.

Yu-qi ZENG ; Xiao-chun CHEN ; Yuan-gui ZHU ; Yong-kun LI ; Xiao-song PENG ; Li-min CHEN ; Jie SHEN ; Tian-wen HUANG

Acta Pharmaceutica Sinica.2005;40(3):225-230.

AIMTo explore the effect and the possible mechanism of ginsenoside Rb1 on beta-amyloid peptide (beta-AP)(25-35) -induced tau protein hyperphosphorylation in cortical neurons.

METHODSWestern blotting and immunocytochemical staining were used to detect tau phosphorylation level, total tau and glycogen synthase kinase-3beta (GSK-3beta) in cortical neurons.

RESULTSAfter exposure to beta-AP(25-35) (20 micromol x L(-1)) for 12 h, the levels of tau protein phosphorylation in the sites of Ser 396, Ser 199/202, Thr 231 and total tau were raised. Meanwhile, the expression of GSK-3beta also increased. Pretreatment with ginsenoside Rbl or lithium chloride, a specific inhibitor of GSK-3beta, markedly reduced beta-AP(25-35)-induced tau hyperphosphorylation and the expression of GSK-3beta.

CONCLUSIONGinsenoside Rb1 can attenuate beta AP(25-35)-induced tau protein hyperphosphorylation in cortical neurons by inhibiting the expression of GSK-3beta.

Amyloid beta-Peptides ; antagonists & inhibitors ; Animals ; Cerebral Cortex ; cytology ; metabolism ; Female ; Fetus ; Ginsenosides ; isolation & purification ; pharmacology ; Glycogen Synthase Kinase 3 ; metabolism ; Glycogen Synthase Kinase 3 beta ; Neurons ; metabolism ; Panax ; chemistry ; Peptide Fragments ; antagonists & inhibitors ; Phosphorylation ; Plants, Medicinal ; chemistry ; Rats ; Rats, Sprague-Dawley ; tau Proteins ; metabolism

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Protective effects of hydroxyethylpuerarin on cultured bovine cerebral microvascular endothelial cells damaged by hydrogen peroxide.

Hong-mei GUANG ; Xiu-mei ZHANG ; Ying-quan LI ; Xin-bing WEI ; Zi-ying WANG ; Hui-qing LIU

Acta Pharmaceutica Sinica.2005;40(3):220-224.

AIMTo observe the damages induced by hydrogen peroxide in cultured bovine cerebral microvascular endothelial cells (BCMEC) and evaluate the protective effects of hydroxyethylpuerarin on hydrogen peroxide-injured BCMEC.

METHODSBCMEC were cultured and transferred into modified Eagle medium (MEM). The viability of cells was detected by MTT assay. Cell injury was determined by lactate dehydrogenase (LDH) activity in the extracellular medium. Flow cytometry was employed to observe the occurrence of apoptosis. Morphologic changes of cells were visualized under phase contrast and electron microscopes.

RESULTSHydrogen peroxide (200 micromol x L(-1) for 4 hours) inhibited the viability of cultured BCMEC and stimulated LDH release. Hydrogen peroxide (100 micromol x L(-1) for 4 hours) induced the occurrence of apoptosis. Hydroxyethylpuerarin was shown to increase the survival rate and decrease the activity of LDH of BCMEC damaged by hydrogen peroxide. Hydroxyethylpuerarin was also found to protect BCMEC against apoptosis induced by hydrogen peroxide.

CONCLUSIONHydrogen peroxide induces BCMEC injury either by apoptosis or through necrosis. Hydroxyethylpuerarin protects BCMEC against hydrogen peroxide-induced injury in a concentration-dependent manner. Its antioxidant effects might be involved as the mechanism protection.

Animals ; Antioxidants ; administration & dosage ; isolation & purification ; pharmacology ; Apoptosis ; drug effects ; Brain ; blood supply ; Cattle ; Cell Survival ; drug effects ; Cells, Cultured ; Dose-Response Relationship, Drug ; Drugs, Chinese Herbal ; administration & dosage ; isolation & purification ; pharmacology ; Endothelial Cells ; drug effects ; metabolism ; Hydrogen Peroxide ; toxicity ; Isoflavones ; administration & dosage ; isolation & purification ; pharmacology ; Microcirculation ; drug effects ; metabolism ; Neuroprotective Agents ; administration & dosage ; isolation & purification ; pharmacology ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Pueraria ; chemistry

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Effects of gingko biloba extract on glutamate-induced Ca2+i changes in cultured cortical astrocytes after hypoxia/reoxygenation, H2O2 or L-glutamate injury.

Zhen LI ; Xian-ming LIN ; Pei-li GONG ; Guan-hua DU ; Fan-dian ZENG

Acta Pharmaceutica Sinica.2005;40(3):213-219.

AIMTo investigate glutamate-induced [Ca2+]i changes in cultured rat neonatal cortical astrocytes after hypoxia/reoxygenation, H2O2 or high concentration of L-glutamate injury. In the meantime, the effects of Gingko biloba extract (GbE) were examined.

METHODS[Ca2+]i changes in astrocytes were monitored by laser scanning confocal microscopy with the Ca2+ sensitive fluorescent probe fluo-3.

RESULTSAfter astrocytes were impaired by hypoxia/reoxygenation, H2O2 (50 micromol x L(-1)) or L-glutamate (0.25 mmol x L(-)), the exogenous glutamate (27 micromol x L(-1)) could not induce increase of [Ca2+]i, but decrease by (3.3 +/- 1.6)%, (81 +/- 11)% and (81 +/- 7)%, respectively. Pretreatment with GbE (10 mg x L(-1)) could not improve injured astrocytic glutamate response. But after pretreatment with GbE (100 mg x L(-1)), glutamate-induced [Ca2+]i elevation of astrocytes after hypoxia/reoxygenation, H2O2 or high concentration of L-glutamate injury were (135 +/- 98)%, (117 +/- 93)% and (89 +/- 36)%, respectively. Nimodipine (1.6 mg x L(-1)) could also reverse the abnormal response of astrocytes after different injury.

CONCLUSIONHypoxia/reoxygenation, H2O2 and high concentration of L-glutamate impaired astrocytes' response to exogenous L-glutamate, and then bidirectional communication between astrocytes and neurons could not take place. GbE could improve the abnormal responses and maintain the normal function of astroglical network. These effects support that GbE has potential beneficial actions against brain injury.

Animals ; Astrocytes ; cytology ; metabolism ; Calcium ; metabolism ; Cell Hypoxia ; Cells, Cultured ; Cerebral Cortex ; cytology ; metabolism ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Ginkgo biloba ; chemistry ; Glutamic Acid ; toxicity ; Hydrogen Peroxide ; toxicity ; Plant Leaves ; chemistry ; Plants, Medicinal ; chemistry ; Rats ; Reperfusion Injury

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Effects of enalapril on plasma Ang II level and the expression of AT1 in blood vessel and kidney of type 2 diabetic rats.

Jian YANG ; Chun XUE ; Gang HU

Acta Pharmaceutica Sinica.2005;40(3):208-212.

AIMTo study the plasma angiotensin II (Ang II) levels and the expressions of angiotensin II1 receptor (AT1) in blood vessels and kidneys in diabetic and high fat diet rats, and the effects of enalapril on plasma Ang II levels and the expressions of AT1 in blood vessels and kidneys in diabetic rats.

METHODSThe plasma Ang II level was assayed with 125I-Ang II radioimmunoassay, and the expression of AT1 in blood vessel and kidney was analyzed with immunohistochemical technique.

RESULTSThe plasma Ang II level was significantly higher in type 2 diabetic rats (241 +/- 49) pg x mL(-1) than that in the control (71 +/- 22) pg x mL , high fat diet group (151 +/- 29) pg x mL(-1) (P < 0.01) , and enalapril-treated groups (136 +/- 25) pg x mL(-1) (P < 0.05). The plasma Ang II levels in high fat diet and in enalapril-treated groups were also significantly higher than that in control group ( P < 0.01 ). With immunohistochemical technique, it was found that the expression of AT1 in endothelial cells of blood vessels, vascular smooth muscle cells, and kidneys in diabetic group increased. The expression of AT1 in endothelial cells of blood vessels, vascular smooth muscle cells, and kidney in enalapril-treated group was similar to that in control group.

CONCLUSIONThe plasma Ang II levels and the expression of AT1 in type 2 diabetic and high fat diet rats increased. Enalapril was shown to decrease the plasma Ang II level and downregulate the expression of AT1 in blood vessels and kidneys in type 2 diabetic rats.

Angiotensin II ; blood ; Angiotensin-Converting Enzyme Inhibitors ; pharmacology ; Animals ; Blood Vessels ; cytology ; metabolism ; Diabetes Mellitus, Type 2 ; blood ; metabolism ; Dietary Fats ; administration & dosage ; Enalapril ; pharmacology ; Endothelial Cells ; metabolism ; Kidney ; metabolism ; Male ; Myocytes, Smooth Muscle ; metabolism ; Rats ; Rats, Sprague-Dawley ; Receptor, Angiotensin, Type 1 ; metabolism

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Reversal of multidrug resistance in drug-resistant cell line EAC/ADR by cepharanthine hydrochloride and its mechanism.

Yu-cheng SONG ; Wei XIA ; Jin-hua JIANG ; Qing-duan WANG

Acta Pharmaceutica Sinica.2005;40(3):204-207.

AIMTo investigate the correlation between reversal effect of cepharanthine hydrochloride (CH) on multidrug resistance (MDR) in drug-resistant cell line EAC/ADR and the nuclear transcription factor-KB (NF-KB).

METHODSCytotoxicity was determined by the tetrazolium (MTT) assay in vitro. An EAC/ADR cell homograft model was established to investigate the effect of CH on reversing MDR in vivo. The constitutive activity and activation of NF-KB by drugs were measured by Dot-Enzyme-linked Immune Sorbent Assay (Dot-ELISA).

RESULTSCH was shown to potentiate the cytotoxicity of ADR, a 13- fold reversal effect of resistance was achieved in vitro. In mice bearing EAC/ADR cell homografts, CH was found to prolong the survival time of animals bearing tumor. Increase in life span over control was 75. 37%. In addition, the constitutive activity of NF-KB and activation of NF-KB by chemotherapy were lowered by CH.

CONCLUSIONThe findings suggest that CH is able to reverse drug resistance and its mechanism may be related to suppressing the constitutive activity and activation of NF-KB by drugs.

Alkaloids ; isolation & purification ; pharmacology ; Animals ; Antineoplastic Agents, Phytogenic ; isolation & purification ; pharmacology ; Benzylisoquinolines ; Carcinoma, Ehrlich Tumor ; drug therapy ; metabolism ; pathology ; Cell Line, Tumor ; Drug Resistance, Multiple ; drug effects ; Drug Resistance, Neoplasm ; drug effects ; Female ; Male ; Mice ; NF-kappa B ; metabolism ; Neoplasm Transplantation ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Random Allocation ; Stephania ; chemistry

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