Spinal CCL2 Promotes Central Sensitization, Long-Term Potentiation, and Inflammatory Pain via CCR2: Further Insights into Molecular, Synaptic, and Cellular Mechanisms / 神经科学通报·英文版

Mounting evidence supports an important role of chemokines, produced by spinal cord astrocytes, in promoting central sensitization and chronic pain. In particular, CCL2 (C-C motif chemokine ligand 2) has been shown to enhance N-methyl-D-aspartate (NMDA)-induced currents in spinal outer lamina II (IIo) neurons. However, the exact molecular, synaptic, and cellular mechanisms by which CCL2 modulates central sensitization are still unclear. We found that spinal injection of the CCR2 antagonist RS504393 attenuated CCL2- and inflammation-induced hyperalgesia. Single-cell RT-PCR revealed CCR2 expression in excitatory vesicular glutamate transporter subtype 2-positive (VGLUT2) neurons. CCL2 increased NMDA-induced currents in CCR2/VGLUT2 neurons in lamina IIo; it also enhanced the synaptic NMDA currents evoked by dorsal root stimulation; and furthermore, it increased the total and synaptic NMDA currents in somatostatin-expressing excitatory neurons. Finally, intrathecal RS504393 reversed the long-term potentiation evoked in the spinal cord by C-fiber stimulation. Our findings suggest that CCL2 directly modulates synaptic plasticity in CCR2-expressing excitatory neurons in spinal lamina IIo, and this underlies the generation of central sensitization in pathological pain.

In-silico investigation of tubulin binding modes of a series of novel antiproliferative spiroisoxazoline compounds using docking studies

Interference with microtubule polymerization results in cell cycle arrest leading to cell death. Colchicine is a well-known microtubule polymerization inhibitor which does so by binding to a specific site on tubulin. A set of 3, 4-bis [substituted phenyl]-4H-spiro [indene-2, 5-isoxazol]-1[3H]-one derivatives with known antiproliferative activities were evaluated for their tubulin binding modes. 3D structures of the derivatives were docked into the colchicine binding site of tubulin using GOLD 5.0 program under flexible ligand and semi-flexible receptor condition. The spiroisoxazoline derivatives bind tubulin in a similar manner to colchicine by establishing at least a hydrogen bonding to Cys[241] as well as hydrophobic interactions with Leu[255], Ile[378] and Lys[254] and few other residues at the binding pocket. It can be concluded that the spiroisoxazoline core structure common to the studied derivatives is a suitable scaffold for placing the antitubulin pharmacophoric groups in appropriate spatial positions required for tubulin binding activity

Pteridic acid hydrate and pteridic acid C produced by StreStreptomyces pseudoverticillus YN17707 induce cell cycle arrest / 中国天然药物

The present study aimed at identifying cell cycle inhibitors from the fermentation broth of Streptomyces pseudoverticillus YN17707. Activity-guided isolation was performed on tsFT210 cells. Compounds were isolated through various chromatographic methods and elucidated by spectroscopic analyses. Flow cytometry was used to evaluate the cell cycle inhibitory activities of the fractions and compounds. Two compounds were obtained and identified as pteridic acid hydrate (1) and pteridic acid C (2), which arrested the tsFT210 cells at the G0/G1 phase with the MIC values being 32.8 and 68.9 μmol·L(-1), respectively. These results provide a basis for future development of Compounds 1 and 2 as novel cell cycle inhibitors for cancer therapy.

Derivatives of 3H-spiro1-benzofuran-2, 1’-cyclohexanes: immunostimulants for veterinary use / Derivados de 3H-espiro1-benzofurano-2, 1’-ciclohexanos: inmunoestimulantes de uso veterinario

Four 3H-spiro1-benzofuran-2, 1’-cyclohexanes were synthesized from filifolinol, two of which are reported for the first time. Docking molecular studies were carried out to determine in silico whether these derivatives have similar immunostimulant activity to that reported for filifolinol, and its oxidation product, filifolinone. Through of the study of interactions of these compounds with the heterodimer of the protein present in teleost TLR1-TLR2, filifolinol, 3’-filifolinchloride and filifolinyl acetate shows similar interactions between them, allowing to predict that they would have similar immunostimulant activity, but different to filifolinone and filifolinane or that they would act by a different mechanisms.

Cuatro 3H-spiro1-benzofuran-2, 1'-ciclohexanos se sintetizaron a partir de filifolinol, dos de los cuales son reportados por primera vez. Se llevaron a cabo estudios de docking molecular para determinar in silico si estos derivados tienen actividad inmunoestimulante similar a la reportada para filifolinol y su producto de oxidación, filifolinona. A través del estudio de las interacciones de estos compuestos con el heterodímero de la proteína presente en teleósteos TLR1-TLR2 se estableció que el filifolinol, 3'-cloruro de filifolinilo y acetato de filifolinilo tienen interacciones similares con el heterodímero, lo que permite predecir que entre ellos tendrían una actividad simi- lar, pero diferente a la de la filifolinona y filifolinano o que estos últimos actuarían por diferentes mecanismos.

Partial characterization of Plasmodium falciparum trophozoite proteome under treatment with quinine, mefloquine and the natural antiplasmodial diosgenone / Caracterización parcial del proteoma del trofozoíto de Plasmodium falciparum bajo tratamiento con quinina, mefloquina y el compuesto natural diosgenona

Introduction: Despite efforts to control malaria, around 10% of the world population is at risk of acquiring this disease. Plasmodium falciparum accounts for the majority of severe cases and deaths. Malaria control programs have failed due to the therapeutic failure of first-line antimalarials and to parasite resistance. Thus, new and better therapeutic alternatives are required. Proteomic analysis allows determination of protein expression levels under drug pressure, leading to the identification of new therapeutic drug targets and their mechanisms of action. Objective: The aim of this study was to analyze qualitatively the expression of P.falciparum trophozoite proteins (strain ITG2), after exposure to antimalarial drugs, through a proteomic approach. Materials and methods: In vitro cultured synchronized parasites were treated with quinine, mefloquine and the natural antiplasmodial diosgenone. Protein extracts were prepared and analyzed by two-dimensional electrophoresis. The differentially expressed proteins were selected and identified by MALDI-TOF mass spectrometry. Results: The following proteins were identified among those differentially expressed in the parasite in the presence of the drugs tested: enolase (PF10_0155), calcium-binding protein (PF11_0098), chaperonin (PFL0740c), the host cell invasion protein (PF10_0268) and proteins related to redox processes (MAL8P1.17). These findings are consistent with results of previous studies where the parasite was submitted to pressure with other antimalarial drugs. Conclusion: The observed changes in the P. falciparum trophozoite protein profile induced by antimalarial drugs involved proteins mainly related to the general stress response.

Introducción. A pesar de los esfuerzos para controlar la malaria, esta sigue siendo un problema de salud pública. Plasmodium falciparum es responsable de la mayoría de los casos graves y de las muertes. Los programas de control de la malaria han sido cuestionados debido al fracaso del tratamiento y a la resistencia del parásito a los antipalúdicos de primera línea, por lo que se requieren nuevas y mejores alternativas. El análisis proteómico permite identificar y determinar los niveles de expresión de las proteínas bajo la presión de los medicamentos, lo que posibilita la identificación de nuevos blancos terapéuticos y mecanismos de acción. Objetivo. Analizar cualitativamente la expresión diferencial de proteínas del citosol del trofozoíto de P. falciparum bajo tratamiento con quinina, mefloquina y el compuesto natural diosgenona mediante una aproximación proteómica. Materiales y métodos. Se trataron trofozoítos sincronizados y cultivados in vitro de P. falciparum (cepa ITG2) con quinina, mefloquina y el compuesto natural diosgenona. Los extractos proteicos se prepararon y analizaron por electroforesis bidimensional. Las proteínas con aparente expresión diferencial se seleccionaron e identificaron mediante espectrometría de masas MALDI-TOF. Resultados. Se encontraron las siguientes proteínas diferencialmente expresadas en el trofozoíto: la enolasa (PF10_0155), la proteína de unión a calcio (PF11_0098), la chaperonina (PFL0740c), la proteína de invasión a la célula del huésped (PF10_0268) y la proteína relacionada con procesos de reducción y oxidación (redox) (MAL8P1.17). Estos hallazgos son congruentes con resultados previos de estudios en los que el parásito fue presionado con otros medicamentos antipalúdicos. Conclusión. Los cambios observados en el perfil de proteínas del trofozoíto de P. falciparum tratado con antipalúdicos involucraron preferencialmente proteínas relacionadas con la respuesta al estrés general.

Inhibition of phospholipase D2 induces autophagy in colorectal cancer cells

Autophagy is a conserved lysosomal self-digestion process used for the breakdown of long-lived proteins and damaged organelles, and it is associated with a number of pathological processes, including cancer. Phospholipase D (PLD) isozymes are dysregulated in various cancers. Recently, we reported that PLD1 is a new regulator of autophagy and is a potential target for cancer therapy. Here, we investigated whether PLD2 is involved in the regulation of autophagy. A PLD2-specific inhibitor and siRNA directed against PLD2 were used to treat HT29 and HCT116 colorectal cancer cells, and both inhibition and genetic knockdown of PLD2 in these cells significantly induced autophagy, as demonstrated by the visualization of light chain 3 (LC3) puncta and autophagic vacuoles as well as by determining the LC3-II protein level. Furthermore, PLD2 inhibition promoted autophagic flux via the canonical Atg5-, Atg7- and AMPK-Ulk1-mediated pathways. Taken together, these results suggest that PLD2 might have a role in autophagy and that its inhibition might provide a new therapeutic basis for targeting autophagy.

Medium optimization for palmarumycin C13 production in liquid culture of endophytic fungus Berkleasmium sp. Dzf12 using response surface methodology

Background: Berkleasmium sp. Dzf12, an endophytic fungus from Dioscorea zingiberensis, was a high producer of palmarumycin C13 with various bioactivities. In the present study, the experimental designs based on statistics were employed to evaluate and optimize the medium for palmarumycin C13 production in mycelia liquid culture of Berkleasmium sp. Dzf12. Results: Among various carbon and nitrogen sources, glucose, peptone and yeast extract were found to be the most favourable for palmarumycin C13 production based on the one-factor-at-a-time experiments. After Plackett-Burman test on the medium, glucose, peptone and yeast extract were further verified to be the most significant factors to stimulate palmarumycin C13 accumulation. These three factors (i.e., glucose, peptone and yeast extract) were then optimized through the experiments of central composite design (CCD) and analysis of response surface methodology (RSM). The optimized medium compositions for palmarumycin C13 production were determined as 42.5 g/l of glucose, 6.5 g/l of peptone, 11.0 g/l of yeast extract, 1.0 g/l of KH2PO4, 0.5 g/l of MgSO4 x 7H2O, 0.05 g/l of FeSO4 x 7H2O, and pH 6.5. Under the optimal culture conditions, the maximum palmarumycin C13 yield of Berkleasmium sp. Dzf12 was increased to 318.63 mg/l, which was about 2.5-fold in comparison with that (130.44 mg/l) in the basal medium. Conclusions: The results indicate that the optimum production of palmarumycin C13 in Berkleasmium sp. Dzf12 liquid culture can be achieved by addition of glucose, peptone and yeast extract with their appropriate concentrations in the modified Sabouraud medium.

Acortatarin A inhibits high glucose-induced extracellular matrix production in mesangial cells / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Diabetic nephropathy (DN) is the leading cause of end-stage renal disease. Various treatment regimens and combinations of therapies provide only partial renoprotection. Therefore new approaches are needed to retard the progression of DN. The aim of the present study was to evaluate the role of a novel spiroalkaloid from Acorus tatarinowii named acortatarin A (AcorA) in inhibiting high glucose-induced extracellular matrix accumulation in mesangial cells (MCs).</p><p><b>METHODS</b>The cytotoxity of AcorA on MCs was examined by 3-(4,5-dimethylthiazol-2-yl)-2.5-diphenyltetrazolium bromide (MTT) assay. The expression of fibronectin and collagen IV was examined by real time PCR and western blotting. The expression of p22(phox) and p47(phox) was detected by western blot. The interaction between p22(phox) and p47(phox) was examined by co-immunoprecipitation. The phosphorylation of p47(phox) was examined by immunoprecipitation. The phosphorylation of protein kinase C (PKC) α, PKCβ, phospholiase C gamma (PLCγ1), and the p85 subunit of PI3K was determined by Western blotting.</p><p><b>RESULTS</b>AcorA significantly inhibited high glucose-induced activation of NADPH oxidase, a ROS-generating enzyme, by increasing phosphorylation of p47(phox) and enhancing interaction between p22(phox) and p47(phox). Preincubation of AcorA with MCs inhibited high glucose-induced collagen IV and fibronectin production in a dose-dependent manner. Moreover, AcorA attenuated high glucose enhanced phosphorylation of PKCα, PKCβ, PLCγ1, and the p85 subunit of PI3K.</p><p><b>CONCLUSION</b>AcorA inhibits high glucose-induced extracellular matrix production via blocking NADPH oxidase activation.</p>

In vitro immunostimulant activity of the aromatic geranyl derivative Filifolinone / Actividad inmunoestimulante in vitro del derivado aromático geranilado Filifolinona

The in vitro effect of the 3 H-spiro [1-benzofuran-2,1’-ciclohexane] derivative (Filifolinone), was evaluated on mouse dendritic cells through the level of expression of MHC molecules class II by flow cytometry. The results show that Filifolinone increases the expression of MHC promoting maturation of dendritic cells. The results suggest that Filifolinone is a potential immunomodulator for veterinary use.

La actividad in vitro del derivado 3H-espiro [1-benzofurano-2,1’-ciclohexano] (Filifolinona), fue evaluado en células dendríticas de ratón a través del nivel de expresión de moléculas MHC clase II utilizando citometría de flujo. Los resultados muestran que Filifolinona incrementa la expresión de MHC promoviendo la maduración de las células dendríticas. Estos resultados permiten sugerir que Filifolinona es un potencial inmunomodulador de uso veterinario.

In vitro antiproliferative activity of 3 H-spiro [1-benzofuran-2,1'-cyclohexane] derivatives / Actividad antiproliferativa in vitro de derivados de 3 H-spiro [1-benzofuran-2, 1'-cyclohexano]

The in vitro effect of the resinous exudate of Heliotropium filifolium, of the 3 H-spiro[1-benzofuran-2,1 '-cyclohexane] derivative called filifolinol 1, isolated from the resin and the semi-synthetic compounds filifolinone 2 and filifolinoic acid 3, obtained from filifolinol 1, were evaluated on the proliferation of an immortalized cell line, UCHT1, derived from rat thyroid. We evaluated the effect of these compounds on UCHT1 cell growth parameters by calculating doubling time; and toxicity using the LIVE/DEAD™ in vitro test. The results showed that the resin is not active, while filifolinone 2, filifolinoic acid 3 and filifolinol 1 produced a significant inhibition of cell doubling time, in concentrations equal or greater than 50, 25 and 75 uM, respectively. The LIVE/DEAD test showed no significant toxicity at these concentrations, compared to cultures kept in absence of compounds. These results suggest a possible cytostatic effect of these compounds, and could therefore constitute potential alternatives for antineoplasic therapy.

Se evaluó el efecto in vitro de la resina aislada desde Heliotropium filifolium y del derivado 3 H-spiro[1-benzofuran-2,1'-cyclohexano] llamado filifolinol 1, obtenido desde este exudado resinoso y los compuestos semi-sintéticos filifolinona 2 y ácido filifolinoico 3, obtenidos a partir de filifolinol 1, sobre la proliferación de la línea celular inmortal, UCHT1, derivada de tumor de tiroide de rata. Evaluamos el efecto de estos compuestos en el desarrollo celular de UCHT1 a través de los parámetros tiempo de doblaje y citotoxicidad usando el test LIVE/DEAD™ in vitro. Los resultados mostraron que la resina no presentó actividad y que filifolinona, ácido filifolinoico y filifolinol producen una inhibición significativa del tiempo de doblaje celular, en concentraciones iguales o superiores a 50, 25 y 75 uM, respectivamente. El test LIVE/DEAD no mostró toxicidad significativa en comparación con los cultivos mantenidos en ausencia de compuestos. Estos resultados sugieren un posible efecto citostático de estos compuestos y por lo tanto, constituirían alternativas potenciales para terapia antineoplásica.

Toxicidad de spiromesifen en los estados biológicos de Bactericera cockerelli (Sulc) (Hemiptera: Triozidae) / Toxicity of spiromesifen to the developmental stages of Bactericera cockerelli (Sulc) (Hemiptera: Triozidae)

Spiromesifen is an insecticide that inhibits the synthesis of lipids and, in Mexico, its use against the Tomato-Potato Psyllid, Bactericera cockerelli (Sulc), on chili pepper (Capsicum annum), tomato (Lycopersicon sculentum) and potato (Solanum tuberosum) began in 2005; however more information is needed to understand its toxicity on this insect pest. The aim of this research was to determine the toxicity of spiromesifen against each of the biological stages of tomato-potato psyllid, its effect on fertility and viability of eggs deposited by treated females, as well as the female preference to lay eggs on treated and non treated plants. The relative toxicity at 95 percent mortality (highest LC95 value /LC95 value of the respective biological stage) of spiromesifen in egg, nymph 1, nymph 2, nymph 3, nymph 4, and nymph 5 were 517.5; 31316.2; 2950.1; 315.6; 18.2 and 1-fold, respectively. There were no differences in the toxicity of spiromesifen between adult males and females. The number of laid eggs was reduced as the spiromesifen concentration used to treat female increased and egg hatch was reduced in all tested doses. In the "no choice" test, females deposited 38.6 ± 2.01 eggs by leaf of non treated chili pepper type jalapeño, while in the treated with 360 mg L-1 we observed 0.3 ± 0.08 eggs by leaf. In the "choice" test, the oviposition decreased as the dose increased. There were no eggs on plants treated with 2400 mg L-1 of spiromesifen.

Two new sesquiterpene lactones from the pericarp of Illicium macranthum / 药学学报

Silica gel column chromatography was used for the isolation and purification of the chemical constituents of the pericarp of Illicium macranthum. From dichloromethane-EtOAc (1:1) fraction and EtOAc fraction of the methanol extracts, eleven compounds were identified on the basis of chemical and spectral data. Two new compounds were elucidated to be 6-deoxyneomajucin (1) and 2-oxo-6-deoxyneomajucin (2), along with nine known compounds 6-deoxypseudoanisatin (3), pseudoanisatin (4), anisatin (5), pseudomajucin (6), protocatecheuic acid (7), shikimic acid (8), shikimic acid methylester (9), beta-sitosterol (10) and daucosterol (11). Compounds 1 and 2 are new majucin-type sesquiterpene lactones.

Simultaneous determination of atractylone, hinesol, beta-eudesmol, atrctylodin in Atractylodes lancea and hierarchical cluster analysis / 中国中药杂志

<p><b>OBJECTIVE</b>To develop a GC method for simultaneous determination of 4 compounds (atractylone, hinesol, beta-eudesmol and atractylodin) in Atractylodes lancea.</p><p><b>METHOD</b>A HP-1 capillary column (0.25 mm x 30 m, 0.25 microm) was used. The detector was FID:Inlet temperature was 250 degrees C. The detector temperature was 250 degrees C. The column temperature was set at 145 degrees C and held for 25 min after injection, then programmed at 10 degrees C x min(-1) to 250 degrees C and held for 10 min at the temperature. The carrying gas was nitrogen, split ratio was 40:1. Injection volume was 2 microL, Cluster analysis was performed by SPSS13.0 software.</p><p><b>RESULT</b>The linear ranges for atractylone, hinesol, beta-eudesmol and atractylodin were 0.0122. 32 (r = .9998), 0.008-1.68 (r = 0.9998), 0.009-1.76 (r = 0.9999), 0.016-3.20 g x L(-1) (r = 0.9997), respectively. The average recoveries (n = 3) of atractylone, hinesol, beta-eudesmol and atractylodin were 98.0%-99.0%, 97.7%-99.4%, 98.4%-99.2%, 97.8%-99.7%, respectively. The samples analyzed were divided into two classes.</p><p><b>CONCLUSION</b>This method is simple, specific, repeatable and stable. It can be applied for the simultaneous determination of 4 compounds (atractylone, hinesol, beta-eudesmol and atractylodin) in A. lancea, which will provide the basis for the quality control of A. lancea. The contents of 4 active compounds were significantly different between geo-authentic and non-authentic producing areas.</p>

Action of protein phosphatase-1 on Tat-dependent HIV-1 transcription and its related inhibitors / 药学学报

Host cell protein phosphatase-1 (PP1) is an important regulator of human immunodeficiency virus-1 (HIV-1) transcription. PP1 is involved in the regulation of HIV-1 transcription, and dephosphorylates RNA polymerase II C-terminal domain (RNAPII CTD) or CycT1-dependent kinase 9 (CDK9) to increase Tat-dependent HIV-1 transcription. In this review, we discuss the action of PP1 in Tat-induced HIV-1 transcription and related to PP1 inhibitors.

HPLC determination of 2-hydroxy-1-methoxyaporphine, pronuciferine, nuciferine and roemerine in Nelumbo nucifera and its alkaloid fraction / 中国中药杂志

<p><b>OBJECTIVE</b>To establish an HPLC method for the determination of four alkaloids, i.e., 2-hydroxy-1-methoxyaporphine, pronuciferine, nuciferine and roemerine, in Nelumbo nucifera and its alkaloid fraction.</p><p><b>METHOD</b>The determination was carried out at 35 degrees C on a Hypersil C18 column (4.6 mm x 250 mm, 5 microm), eluting with acetonitrile-water containing 0.1% triethylamine as mobile phases in gradient mode. The flow rate was 1.0 mL x min(-1) and detection at the wavelength was set at 270 nm.</p><p><b>RESULT</b>The linear ranges of 2-hydroxy-1-methoxyaporphine, pronuciferine, nuciferine and roemerine were 0.110-0.658 microg (r = 0.9995), 0.0210-0.126 microg (r = 0.9995), 0.103-0.618 microg (r = 0.9998), 0.085 6-0.514 microg (r = 0.9995), with the average recoveries (n=6) were 101.5%, 99.14%, 99.21% and 98.41% for the alkaloid fraction of N. nucifera and 99.53%, 100.5%, 97.51% and 100.1% for N. nucifera respectively.</p><p><b>CONCLUSION</b>The determination results of the three batches of samples showed that the method was easy and accurate which could be used to determine the contents of four components in N. nucifera and its alkaloid fraction.</p>

Five alkaloids from vine stems of Diploclisia affinis / 中国中药杂志

<p><b>OBJECTIVE</b>To study alkaloid constituents of Diploclisia affinis.</p><p><b>METHOD</b>The air-dried vine stems of D. affinis were extracted with 90% EtOH three times at room temperature. The EtOH extract was suspended in H2 O and adjusted to pH 2 with 5% HCl solution. After extracted with petroleum ether and CHCl3 successively, the aqueous fraction was adjusted to pH 9 with 10% NH3 x H2O and extracted with CHCl3 again to afford the total alkaloids fraction. The compounds were isolated through column chromatography from the total alkaloids fraction. Their structures were determined on the basis of spectral analysis (MS, 1H-NMR, 13C-NMR).</p><p><b>RESULT</b>Five alkaloids was identified as reticuline (1), asimilobine (2), acutumine (3), dihydroxyprotoberberine (4), stepholidine (5), were isolated from the vine stems of D. affinis.</p><p><b>CONCLUSION</b>All the compounds were obtained from D. affinis for the first time.</p>

Fingerprint of volatile oil of Atractylodes lancea by GC-MS / 药学学报

To study the fingerprint of the volatile oil of Atractylodes lancea (Thunb.) DC., and to offer the characteristic data for the quality evaluation, GC-MS analysis was performed for 17 samples of different areas used as Atractylodes lancea (Thunb.) DC. Nine kinds of same components were selected. TIC profiles were evaluated by "Computer Aided Similarity Calculation". The characteristic peaks in chromatograms were identified by comparing mass data with literatures. Hierarchical clustering analysis was performed by SPSS based on the relative peak area (RPA) of identified peak to atractydin in 17 samples. The mutual mode fingerprint plots of genuine Atractylodes lancea (Thunb.) DC. have been established, the matching of active components was characteristic that atractylon, hinesol, beta-eudesmol, atractydin as (0.89 - 1.12): (0.11 - 0.15) : (0.48 - 0.61) : 1. The difference of resemblance of not genuine samples with genuine samples was remarkable. Two categorizations were clustered. Atractylodes lancea (Thunb.) DC. from genuine and Tangshan and Nanshan, Jiangsu Prov. were in a group, while those from Anhui and Hubei Prov. were in another group. The characteristic fingerprint of genuine Atractylodes lancea (Thunb.) DC. combined with the study of the matching of active components for the quality control and the resemblance calculation of fingerprints and SPSS hierarchical clustering analysis provided a new analytic method for the quality evaluation and discrimination of Atractylodes lancea (Thunb.) DC.

Synthesis and antibacterial activity of 7-(7-aminomethyl-5-azaspiro 2,4 hept-5-yl)-1-cyclopropyl-6-fluoro-8-methoxy-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid and its analogues / 药学学报

<p><b>AIM</b>To find new antibacterial agents of quinolone with high activity and low toxicity.</p><p><b>METHODS</b>To design and synthesize 7-(7-aminomethyl-5-azaspiro [2,4] hept-5-yl)-1-cyclopropyl-6-fluoro-8-methoxy-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid and its analogues, and to study their antibacterial activity in vitro and in vivo.</p><p><b>RESULTS</b>Twenty new compounds (2 - 11, 17 - 26) were obtained including five targeted compounds (22 - 26). The structures of the compounds were confirmed by 1HNMR, MS and HRMS. Compounds 22 - 26 showed broad spectrum of antibacterial activity against Gram-positive and Gram-negative organisms. Especially for compound 24, the relevant MIC values for 13 strains of Gram-positive organisms were < 0.001 - 0.03 mg(-1), including 4 strains of S. pneumoniae, 2 strains of S. pyogenes, 3 strains of S. aureus and 2 strains of Enterococci which exhibited more potent activity than contrast agents (clinafloxacin and gatifloxacin). The MIC values of 24 for 6 strains Gram-positive organisms were 0.01 - 1 mg x L(-1), which exhibited equal or lower activity than contrast agents. They were more effective than ciprofloxacin and gatifloxacin against intraperitoneal infections caused by S. pneumoniae and S. aureus in mice.</p><p><b>CONCLUSION</b>Compounds (23, 24 and 26) showed excellent antibacterial activity in vitro and in vivo and should be worth further investigation.</p>

The naphtha composing characteristics of geoherbs of Atractylodes lancea / 中国中药杂志

<p><b>OBJECTIVE</b>To find the chemical diversity and characteristics of A. lancea on two levels--individuals and populations, and to discover the chemical essentials for forming geoherbs.</p><p><b>METHOD</b>47 rhizomes of A. lancea were collected in 7 populations, and 6 naphtha components (1. elemol, 2. hinesol, 3. beta-eudesmol, 4. atractylone, 5. atractylodin, 6. atractylenolid I) in the rhizomes were determined by GC-MS combination. Principal Component Analysis and Cluster Analysis were carried out by SPSS.</p><p><b>RESULT</b>Cluster Analysis of the 6 main components indicated that the chemical components of geoherbs were different from those of the non-geonerbs of A. lancea. Other analysis showed as follows: 1. The general oil of geoberbs were lower than that of non-geoherbs(P < 0.01), but components yielding more than 1% (% of the total oil) were more than non-geoherbs(P < 0.01); 2. Hinesol mixing beta-eudesmol was more in non-geoherbs, which atractylodin mixing atractylone was more in geoherbs(P < 0.001); 3. Principal Component Analysis implied that atractylone was the most important component to discriminate geoherbs and non-geoherbs of A. Lancea.</p><p><b>CONCLUSION</b>The naphtha composing characteristics of geoherbs was the special proportionment sale, viz. atractylone: hinesol: beta-eudesmol: atractylodin being(0.70~2.00):(0.04~0.35):(0.09~0.40):1.</p>

Studies on chemical constituents of two plants from Costus / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Costus speciosus and C. tonkinensis (Zingiberaceae) distributed in Yunnan province.</p><p><b>METHOD</b>Chromatography and spectral analyses were used to isolate the constituents and elucidate their structure.</p><p><b>RESULT</b>Six compounds were isolated from the rhizome of C. speciosus and elucidated as diosgenin(1), prosapogenin B of dioscin(2), diosgenone(3), cycloartanol(4), 25-en-cycloartenol(5) and octacosanoic acid(6). Four compounds were isolated from the rhizome of Costus tonkinensis and elucidated as tetracosanoic acid(7), succinic acid(8), beta-sitosterol(9) and daucosterin(10).</p><p><b>CONCLUSION</b>Compounds of 3-6 were obtained from C. speciosus for the first time and compounds of 7-10 were obtained from C. tonkinensis for the first time too.</p>