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Xanthones from leaves of Calophyllum inophyllum Linn.

Yuan LI ; Zhan-Lin LI ; Ming-Sheng LIU ; Dan-Yi LI ; Hui ZHANG ; Hui-Ming HUA

Acta Pharmaceutica Sinica.2009;44(2):154-157.

To study the xanthones from the leaves of Calophyllum inophyllum Linn., several chromatography methods were employed to isolate the constituents. Investigation on the CHCl3 extract led to the isolation of a new xanthone named inophyxanthone A (1) and four known compounds, which were pancixanthone A (2), gerontoxanthone B (3), jacareubin (4) and pyranojacareubin (5). Among them, compound 2 was obtained from this plant firstly, and compound 3 was obtained for the first time from this genus. The structure of inophyxanthone A (1) was identified as 1, 3, 5-trihydroxy-2-(1, 1-dimethylallyl)xanthone by spectral analysis.
Calophyllum ; chemistry ; Molecular Structure ; Plant Leaves ; chemistry ; Plants, Medicinal ; chemistry ; Xanthones ; chemistry ; isolation & purification

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Seperation and structure elucidation of alkaloids from Chinese drug buzhaye, Folium Microcos.

Ji-Peng LUO ; Li-Ping ZHANG ; Shi-Ling YANG ; M F ROBERTS ; J D PHILLIPSON

Acta Pharmaceutica Sinica.2009;44(2):150-153.

From the chloroform extracts of the dried Folium Microcos, four compounds were isolated by using repeated column chromatography on silica gel and recrystallization and their structures were elucidated by physicochemical properties and UV, MS and NMR, separately. They are N-methyl-6alpha-(deca-1', 3', 5'-trienyl)-3beta-methoxy-2beta-methylpiperidine, 6-(deca-1', 3', 5'-trienyl)-3-methoxy-2-methylpiperidine, N-methyl-6-(deca-1', 3', 5'-trienyl)-2, 3-dimethylpiperidine and N-methyl-6-(deca-1', 3', 5'-trienyl)-2-methylpiperidine, named as micropiperidine A, micropiperidine B, micropiperidine C and micropiperidine D, respectively. The latter three are new compounds.
Alkaloids ; chemistry ; isolation & purification ; Molecular Structure ; Piperidines ; chemistry ; isolation & purification ; Plant Leaves ; chemistry ; Plants, Medicinal ; chemistry ; Tiliaceae ; chemistry

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Non-nucleoside reverse transcriptase inhibitors (Part 18): synthesis and anti-HIV activity of 4-allylamino or 4-azido substituted diaryltriazines.

Yuan-Zhen XIONG ; Hai-Rong HU ; Fen-Er CHEN ; Jan BALZARINI ; Christophe PANNECOUQUE ; Erik de CLERCQ

Acta Pharmaceutica Sinica.2009;44(2):145-149.

Eight new diaryltriazine derivatives containing 4-allylamino and 4-azido substitutes guided by molecular docking have been designed and synthesized based on our previous work. The evaluation of HIV inhibitory activity demonstrated that all compounds were potent against HIV-1 replication. The most active compound 7c exhibited activity against HIV-1 (IC50 = 0.034 micromol x L(-1), SI = 6,475) and the double mutant strain (IC50 = 9.39 micromol x L(-1)) in the micromolar range, which was more potent than nevirapine.
Anti-HIV Agents ; chemical synthesis ; chemistry ; pharmacology ; Catalytic Domain ; HIV-1 ; drug effects ; Inhibitory Concentration 50 ; Molecular Structure ; Reverse Transcriptase Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; Triazines ; chemical synthesis ; chemistry ; pharmacology

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Antitumor mechanism of Qinghaosu derivatives--molecular docking studies of Qinghaosu derivatives with transferrin.

Nai-Fang LIU ; Ling-Bo QU ; Bing-Ren XIANG ; Ran YANG

Acta Pharmaceutica Sinica.2009;44(2):140-144.

To investigate the antitumor mechanism of artemisninin, a flexible docking analysis was used to score all kinds of functions of 11 Qinghaosu derivatives and transferrin with different resolutions. The distances of Asp-63, Tyr-188, His-249, Arg-124 and Lys-296 with Qinghaosu were less than 0.5 nm, separately. Meanwhile, the higher is the activity of Qinghaosu derivatives the higher is the score. Our model explains that Fe2+ is more feasible to react with Qinghaosu, and not involved in other metabolism in presence of transferrin. Docking results unveil that Iron(II)-transferrin increased the cytotoxicity of Qinghaosu derivatives and provide a rational basis for further design and synthesis of novel Qinghaosu derivatives.
Antineoplastic Agents, Phytogenic ; chemical synthesis ; chemistry ; pharmacology ; Artemisinins ; chemical synthesis ; chemistry ; pharmacology ; Catalytic Domain ; Drug Discovery ; Models, Chemical ; Molecular Structure ; Protein Binding ; Transferrin ; chemistry

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Mechanisms of gross saponins of Tribulus terrestris via activating PKCepsilon against myocardial apoptosis induced by oxidative stress.

Si-Si WANG ; Ying-Shi JI ; Hong LI ; Shi-Jie YANG

Acta Pharmaceutica Sinica.2009;44(2):134-139.

This study is to observe the effect of gross saponins of Tribulus terrestris (GSTT) on protein kinase Cepsilon (PKCepsilon) and apoptosis-associated protein in the apoptosis of cultured cardiocyte apoptosis induced by hydrogen peroxide (H2O2), and to explore the mechanisms of GSTT against myocardial apoptosis. Primary cardiocytes were isolated and cultured. Myocardial apoptosis was induced by H2O2 and analyzed with flow cytometry. Protein content of phospho-PKCepsilon, Bcl-2, and Bax were detected with Western blotting analysis. Cleaved caspase-3 protein content was determined with immunocytochemical technique. After the pretreatment of 100 mg x L(-1) GSTT, compared with H2O2 group, GSTT could not only decrease the apoptotic percentage in cardiocytes damaged by H2O2 (P < 0.01), but also reduce protein contents of Bax and cleaved caspase-3 (P < 0.01), and increase protein content of phospho-PKCepsilon and Bcl-2 significantly (P < 0.01). PKC inhibitor chelerythrine (Che) could prevent partly the effect of GSTT against myocardial apoptosis (P < 0.05 and P < 0.01). Mechanisms of GSTT against myocardial apoptosis might be associated with inhibition of mitochondrial apoptosis pathway after PKCepsilon activation.
Animals ; Apoptosis ; drug effects ; Benzophenanthridines ; pharmacology ; Caspase 3 ; metabolism ; Cells, Cultured ; Dose-Response Relationship, Drug ; Enzyme Activation ; Female ; Hydrogen Peroxide ; toxicity ; Male ; Myocytes, Cardiac ; cytology ; drug effects ; metabolism ; Oxidative Stress ; Phosphorylation ; Plants, Medicinal ; chemistry ; Protein Kinase C ; antagonists & inhibitors ; Protein Kinase C-epsilon ; metabolism ; Proto-Oncogene Proteins c-bcl-2 ; metabolism ; Rats ; Rats, Wistar ; Saponins ; administration & dosage ; isolation & purification ; pharmacology ; Tribulus ; chemistry ; bcl-2-Associated X Protein ; metabolism

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Protective effect of calcium dobesilate against early diabetic nephropathy of rat kidney.

Mei-Juan GAO ; Ming LIU ; Bo LI ; Ming-Long LI ; Li-Xiang BIAN ; Gui-Na YU

Acta Pharmaceutica Sinica.2009;44(2):126-133.

The aim of this study is to study the effect of calcium dobesilate on streptozotocin (STZ)-induced early diabetic nephrophathy (DN) in rats. All male Wistar rats were randomly divided into six groups: normal group; DN blank group; calcium dobesilate 75, 150, and 300 mg x kg(-1) groups and perindopril 0.4 mg x kg(-1) group. Blood glucose and the 24 h urinary albumin were measured dynamically during the experiment, after 8 weeks administration, the level of glycosylated hemoglobin (HbA1c) was determined, the expressions of plasminogen activator inhibitor-1 (PAI-1) and matrix metalloprotein-9 (MMP-9) in cortex of kidney were examined with immunohistochemical staining. The endothelin (ET) in plasma and kidney cortex was measured with radioimmunoassay, renal pathomorphism was observed with light and electron microscopes. Calcium dobesilate could decrease the 24 h urinary albumin and ET in plasma and kidney cortex, down-regulate the expression of PAI-1, and up-regulate MMP-9 in kidney. These findings suggested that calcium dobesilate could protect blood vessel endothelium, inhibit kidney fibrous degeneration, ameliorate renal pathological damage, and protect kidney function in many ways.
Albuminuria ; Animals ; Blood Glucose ; metabolism ; Calcium Dobesilate ; pharmacology ; Diabetes Mellitus, Experimental ; blood ; metabolism ; pathology ; Diabetic Nephropathies ; blood ; metabolism ; pathology ; Endothelins ; blood ; metabolism ; Glycated Hemoglobin A ; metabolism ; Hemostatics ; pharmacology ; Kidney Cortex ; metabolism ; ultrastructure ; Male ; Matrix Metalloproteinase 9 ; metabolism ; Plasminogen Activator Inhibitor 1 ; metabolism ; Random Allocation ; Rats ; Rats, Wistar

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Effects of fluvastatin on the activation of p38 mitogen-activated protein kinase in glomerular mesangial cells under high concentration of glucose.

Li-Hui WANG ; Guang-Li WU ; Li-Xia ZHANG ; Xu-Dong HUANG ; Sai LI

Acta Pharmaceutica Sinica.2009;44(2):121-125.

This study is to investigate the effects of fluvastatin on the activation of p38 mitogen-activated protein kinase (p38 MAPK) and cAMP response element-binding protein (CREB1) in glomerular mesangial cells under high concentration of glucose. High concentration glucose and fluvastatin were used to stimulate the cultured rat glomerular mesangial cells (GMCs) in vitro. The protein expressions of p38 MAPK, CREB1, p-p38 MAPK and p-CREB1 were observed with Western blotting. TGF-beta1 and fibronectin (FN) mRNA were measured with reverse transcription and polymerase chain reaction (RT-PCR). The protein synthesis of laminine (LN) and type IV collagen in the supernatants of the GMCs were detected with radioimmunoassay. Compared with low glucose control group, the expressions of p-p38 MAPK, p-CREB1 were increased obviously in high glucose group, TGF-beta1 mRNA and FN mRNA, LN and type IV collagen in the supernatants were increased significantly in GMCs under high concentration glucose medium. The expression levels of p-p38 MAPK, p-CREB1, TGF-beta1 mRNA, and FN mRNA, LN and type IV collagen in the supernatants were significantly lower in the fluvastatin group than those in the high concentration glucose group. It is concluded that fluvastatin can inhibit over production of TGF-beta1 and ECM proteins in GMCs under high concentration of glucose, partly by regulating the phosphorylation of p38 MAPK and CREB1.
Amino Acids, Diamino ; metabolism ; Animals ; Cell Proliferation ; Cells, Cultured ; Collagen Type IV ; metabolism ; Cyclic AMP Response Element-Binding Protein ; metabolism ; Fatty Acids, Monounsaturated ; pharmacology ; Fibronectins ; genetics ; metabolism ; Glucose ; administration & dosage ; Hydroxymethylglutaryl-CoA Reductase Inhibitors ; pharmacology ; Indoles ; pharmacology ; Male ; Mesangial Cells ; cytology ; metabolism ; Phosphorylation ; RNA, Messenger ; metabolism ; Rats ; Rats, Wistar ; Transforming Growth Factor beta1 ; genetics ; metabolism ; p38 Mitogen-Activated Protein Kinases ; metabolism

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The effect of chelerythrine on the hypertrophy of cardiac myocytes of neonatal rats induced by different glucose levels and its mechanism.

Wen-Bin ZHANG ; Min WANG ; Bin-Quan ZHOU ; Jun-Hui ZHU ; Guo-Sheng FU

Acta Pharmaceutica Sinica.2009;44(2):115-120.

The purpose of this study is to investigate the effect of chelerythrine on the hypertrophy of cardiomyocytes of neonatal rats induced by different glucose levels and its mechanism. Using cultured neonatal ventricular myocytes as a model, groups were divided as: control (5 mmol x L(-1)); high glucose level (10, 15, 20, and 25.5 mmol x L(-1)); high glucose level (25.5 mmol x L(-1)) add different concentrations of chelerythrine (1 and 8 micromol x L(-1)); and control glucose level (5 mmol x L(-1)) add different concentrations of chelerythrine (1 and 8 micromol x L(-1)). Different groups of cardiomyocytes after adding corresponding treat factors were cultured for 48 hours. Cardiomyocytes' diameters and protein level were measured and the expression of PKC-alpha, PKC-beta2, p-PKC-alpha, and p-PKC-beta2 were measured by Western blotting. Compared with control group, neonatal myocytes cultured in high glucose levels showed increased cellular volumes, protein level and expression of PKC-alpha, PKC-beta2, p-PKC-alpha, p-PKC-beta2. When chelerythrine was added, cellular volumes, protein level and expression of PKC-alpha, PKC-beta2, p-PKC-alpha, p-PKC-beta2 were significantly reduced. But in 1 micromol x L(-1) chelerythrine group, the expression of PKC-beta2 was not significantly reduced. The result suggested that chelerythrine can reverse the hypertrophy induced by different glucose levels on the cardiac myocytes, it may have protective effect against diabetic cardiomyopathy via PKC passageway.
Animals ; Animals, Newborn ; Benzophenanthridines ; pharmacology ; Cells, Cultured ; Diabetes Mellitus, Experimental ; drug therapy ; metabolism ; Dose-Response Relationship, Drug ; Glucose ; administration & dosage ; Hypertrophy ; chemically induced ; pathology ; Hypoglycemic Agents ; pharmacology ; Myocytes, Cardiac ; drug effects ; pathology ; Phosphorylation ; Protein Kinase C ; antagonists & inhibitors ; metabolism ; Protein Kinase C beta ; Protein Kinase C-alpha ; metabolism ; Rats ; Rats, Sprague-Dawley

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Folate receptor-mediated antitumor drugs.

Jie ZHAO ; Sheng-Li CAO ; Xiao-Lin ZHENG ; Bo ZHAO

Acta Pharmaceutica Sinica.2009;44(2):109-114.

Folate receptor (FR) is over-expressed in a variety of human cancers and it is seldom expressed or found in normal tissues. Therefore, folate receptor-mediated antitumor drugs can be targeted specially to the FR-positive tumor cells. This strategy improves the selectivity of drugs which may destroy the normal tissues in traditional chemotherapeutics. This review provides the delivery mechanism of FR-mediated antitumor drugs and highlights the novel folate-drug conjugates and their activities.
Animals ; Antineoplastic Agents ; administration & dosage ; chemistry ; pharmacology ; Carrier Proteins ; metabolism ; Cell Line, Tumor ; Drug Carriers ; Drug Delivery Systems ; Folate Receptors, GPI-Anchored ; Folic Acid ; administration & dosage ; analogs & derivatives ; chemistry ; pharmacology ; Humans ; Neoplasms ; metabolism ; pathology ; Receptors, Cell Surface ; metabolism

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Recent advances in the structure-activity relationship study of small-molecule sodium channel blockers with analgesic effects.

Wen LI ; You ZHOU ; Hong-Min LIU ; Qi-Dong YOU

Acta Pharmaceutica Sinica.2009;44(2):101-108.

Pain is one of the common clinical symptom, previous studies have implicated sodium channels as a key constituent in pain signaling. Sodium channel blockers with efficient sodium channel blockade effect play an important role in analgesic treatment. However, most drugs used in clinic have many drawbacks and can not meet the demand of the clinical use. Therefore, for the development of new generation of sodium channel blockers, it is of great significance to find small molecule sodium channel blocking lead compounds with novel chemical scaffolds and new structures, sodium channel blocking activity and structure-activity relationship are discussed in detail, and current problems and trends in future research are also emphasized.
Analgesics ; chemistry ; pharmacology ; therapeutic use ; Animals ; Drug Design ; Humans ; Molecular Structure ; Neuralgia ; drug therapy ; Pain ; drug therapy ; Pain Measurement ; Sodium Channel Blockers ; chemistry ; pharmacology ; therapeutic use ; Sodium Channels ; drug effects ; Structure-Activity Relationship

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