By means of preparative HPTLC and column chromatography over silica gel and Sephadex LH-20, nine diterpenoids were isolated and purified from the whole plants of Scutellaria strigillosa. Based on the physico-chemical properties and spectral data, their structures were elucidated as: 6-O-acetyl-7-O-nicotinoylscutebarbatine G(1), 6-O-nicotinoyl-7-O-acetylscutebarbatine G(2), 6,7-di-O-nicotinoylscutebarbatine G(3), scutebarbatine K(4), scutebarbatine B(5), 6-O-acetylscutehenanine A(6), 6-O-nicotinoylbarba- tin A(7), 6,7-di-O-acetoxylbarbatin A(8), scutebarbatine F(9). Compound 1 is a new diterpenoid, and compounds 2-9 were isolated from Scutellaria strigillosa for the first time.
Diterpenes ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Scutellaria ; chemistry ; Spectrometry, Mass, Electrospray Ionization

Ten compounds were isolated and purified by column chromatography over silica gel, preparative TLC, and Sephadex LH-20 from the whole plant of Solanum lyratum. The structures were elucidated on the basis of physico-chemical properties and spectral data as 1beta-hydroxy-1 ,2-dihydro-alpha-santonin (1) , boscialin (2) , blumenol C (3), 3beta-hydroxy-5alpha, 6alpha-epoxy-7-megastigmen-9-one(4), dehydrovomifoliol(5) , blumenol A(6), (1'S,2R,5S, 10R) -2-(1', 2'-dihydroxy-l1'-methylethyl) -6,10-dimethylspiro[4,5] dec-6-en-8-one(7) , (1'R,2R,5S,10R)-2-( 1',2'-dihydroxy-l '-methylethyl) -6,1 l0-dimethylspiro[4,5]dec-6-en-8-one( 8) , 2-(1',2'-dihydroxy-1 '-methylethyl) -6,1 0-dimethyl-9-hydroxyspiro [4,5] dec-6-en-8-one (9) , and grasshopper ketone (10). Compounds 1-10 were isolated from this plant for the first time.
Drugs, Chinese Herbal ; chemistry ; Solanum ; chemistry ; Terpenes ; analysis ; isolation & purification

A colistin producing strain Paenibacillus polymyxa AS1.541 was treated by N-methyl-N-nitro-N-nitrosoguanidine(NTG) for increasing yields of the antibiotic colistin.High-yield strains were obtained by selection of deregulated mutant which grow on media containing colistin,a self second metabolite,and ethionine,an analogue of methionine.Some of these mutants have higher yield of colistin than that of the parent strain.

To investigate the secondary metabolites of endophytic fungi Pericinia sp. F-31. Column chromatography on silica gel, Sephadex LH-20 and semi-preparative HPLC were used to separate and purify the compounds. Two compounds were isolated from the fermentation broth of Periconia sp. Their structures were identified as 5-(1-hydroxyhexyl) -6-methyl-2H-pyran-2-one (1) and 2-(3-hydroxy-4-methylphenyl) -propanoic acid (2). Compound 1 was a new lactone compound, compound 2 was new natural product, and the NMR data of compound 2 was reported for the first time.
Annona ; microbiology ; Ascomycota ; chemistry ; genetics ; isolation & purification ; metabolism ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; metabolism ; Endophytes ; chemistry ; genetics ; isolation & purification ; metabolism ; Lactones ; chemistry ; isolation & purification ; metabolism ; Mass Spectrometry ; Molecular Structure

Aged ; Coal Mining ; Humans ; Male ; Middle Aged ; Pneumoconiosis ; complications ; diagnostic imaging ; Pulmonary Heart Disease ; diagnostic imaging ; etiology ; Sensitivity and Specificity ; Tomography, Spiral Computed ; methods

As the main medicinal powder for drawing out pus and removing necrotic tissue in external therapies of traditional Chinese surgery, Sheng Powder has made great contributions to the treatment of inflammatory wounds and has the unique bactericidal and decay-discharging function that can not be replaced by antibiotics. However, Sheng Powder has toxicity because it contains mercury. So far, there is no clinical research on the standards of dose and usage of Sheng Powder and there is a lack of objective and quantitative criteria for operating standards and monitoring of toxicity and side effects. Therefore, the authors choose Jiuyi Powder, one of the most commonly used Sheng Powder, to evaluate the safety of its external use, and form a standardization program for clinical implementation.

AIMTo study the preparation of hydroxypropyl methylcellulose phthalate (HPMCP) nanoparticles and compare its pharmacokinetic characteristics with Neoral.

METHODSHPMCP nanoparticles loaded cyclosporine A were prepared by solvent-nonsolvent method. CyA-HP50 nanoparticles, CyA-HP55 nanoparticles and Neoral were orally administered at the dosage of 15 mg x kg(-1) to rats. The CyA concentration in blood were determined by HPLC. Pharmacokinetic parameters were calculated by 3P97 program.

RESULTSThe concentration-time data of the three preparations were best fit by two compartment model. The relative bioavailability of CyA-HP50 and CyA-HP55 nanoparticles calculated by the AUC0-72 were 82.3% and 119.6%, bioequivalent to the reference of Neoral. The relative bioavailability of CyA-HP55 nanoparticles was 145.3% of CyA-HP50 nanoparticles.

CONCLUSIONCyA HPMCP nanoparticles could be prepared easily and reproducibly. It was found that the oral absorption of CyA can be increased by using the HPMCP nanoparticles.

Administration, Oral ; Animals ; Area Under Curve ; Biological Availability ; Cyclosporine ; administration & dosage ; pharmacokinetics ; Immunosuppressive Agents ; administration & dosage ; pharmacokinetics ; Male ; Methylcellulose ; administration & dosage ; analogs & derivatives ; Nanostructures ; Particle Size ; Rats ; Rats, Sprague-Dawley

The tumor multidrug resistance reversal effect of NPB304, a novel taxane, was studied. MTT assay was used to determine the IC50 of chemotherapy drugs. Western blotting assay was applied to analyze the expression of P-glycoprotein (P-gp). The effect of compounds on the P-gp function and P-gp ATPase activity was determined by rhodamine 123 (Rh123) accumulation assay and analysis kit, respectively. Molecular docking was employed to predict the binding force between compounds and P-gp. Transmembrane transport of NPB304 was analyzed using MDCK II and MDR1-MDCK II cell model. NPB304 displayed multidrug resistance reversal effect on KBV cells and MCF-7/paclitaxel cells, NPB304 collaborative with P-glycoprotein (P-gp) inhibitors verapamil enhanced the reversal activity, specifically, 10 μmol x L(-1) verapamil in combination with paclitaxel reversed resistance by 56.5-fold, while combined with NPB304 increased the reversal fold; NPB304 synergistically increased Rh123 accumulation in the resistant cells when combined with verapamil, and NPB304 at 0-1 μmol x L(-1) enhanced the ATPase activity activated by verapamil was observed. NPB304 existed the hydrophobic interactions with the TM regions of P-gp, and the binding force between NPB304 and the A chain of the TM region was stronger. P-gp ATPase activity assay demonstrated NPB304 at lower concentrations (0-1.5 μmol x L(-1)) could activate the P-gp ATPase, playing a role on inhibition of P-gp function. However, NPB304 did not have an obvious feature of P-gp substrate. NPB304 exerted itself and synergy with verapamil activity on reversing tumor resistance via inhibiting the P-gp function.
ATP-Binding Cassette, Sub-Family B, Member 1 ; metabolism ; Antineoplastic Agents ; pharmacology ; Biological Transport ; Drug Resistance, Multiple ; Drug Resistance, Neoplasm ; Drug Synergism ; Humans ; MCF-7 Cells ; Rhodamine 123 ; Taxoids ; pharmacology ; Verapamil ; pharmacology

Naringenin (1) was transformed to three metabolites (2-4) by Mucor sp. Based on LCMS(n)-IT-TOF and NMR spectroscopic data, 2-4 were identified as naringenin-7-O-sulphate, naringenin-4'-O-sulphate, and naringenin-5-O-sulphate, respectively. These results might provide hints to the mammalian/human metabolism of naringenin.
Biotransformation ; Drugs, Chinese Herbal ; chemistry ; metabolism ; Flavanones ; chemistry ; metabolism ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Mucor ; metabolism ; Sulfates ; metabolism

OBJECTIVEThe purpose of this study was to observe the endothelial progenitor cells (EPCs) related gene expression changes before and early after revascularization in patients with acute myocardial infarction.

METHODSPeripheral blood samples were taken from patients with acute anterior myocardial infarction 6 hours and 7 days after PCI and stenting. Mononuclear cells (MNCs) were isolated by Ficoll-density centrifugation and cultured in M-199 medium. After 14 days culture, attaching cells incorporated DiI-acetylated low-density lipoprotein (EPCs) were collected and RNA was isolated by Trizol for microarray analysis on 24 genes associated with permissibility/vessel tone (angiotensin system: ACE, AGTR-1, AGTR-2; NO system: eNOS; prostacyclin system: COX-2; endothelin system: ET-1, ETA, ETB; superoxide anions system: SOD-1), angiogenesis (adhesion molecule: CDH5; growth factors and receptors: VEGFR1, VEGFR2, VEGF) and endothelial cell activation (adhesion molecules expression: ICAM1, ICAM2, ICAM3, PECAM-1, E-Selectin, L-Selection, VCAM1; change phenotype from antithrombotic to prothrombotic: tPA, uPA, PAI, vWF). VEGFR2, PECAM-1 and VE-cadherin positive cells were identified by flow cytometry.

RESULTEight gene expressions (AGTR-1, AGTR-2, COX-2, eNOS, ET-1, ETA, VEGF) were significantly downregulated 7 days post PCI compared to pre-PCI (P < 0.05). Flow cytometry results showed that VEGFR2 positive cells were also significantly reduced post PCI than that of before PCI (P < 0.05).

CONCLUSIONPCI down-regulated endothelial progenitor cells related gene expressions in patients with acute myocardial infarction.

Aged ; Aged, 80 and over ; Centrifugation, Density Gradient ; Endothelial Cells ; cytology ; Endothelium, Vascular ; cytology ; Female ; Gene Expression ; Humans ; Male ; Middle Aged ; Myocardial Infarction ; metabolism ; therapy ; Myocardial Reperfusion ; Myocardial Revascularization ; Oligonucleotide Array Sequence Analysis ; Receptor, Angiotensin, Type 1 ; biosynthesis ; genetics ; Receptor, Endothelin A ; biosynthesis ; genetics ; Stem Cells ; cytology ; Superoxide Dismutase ; biosynthesis ; genetics