Bacteriostatic stimulus of meropenem on allelochemical-metabolizing Burkholderia sp. LS-044 mitigates ferulic acid autotoxicity in rice (Oryza sativa ssp. japonica cv. Tainung 71)

Plant and Soil - To screen plant-associated Burkholderia strains for plant probiotic traits including allelochemical metabolism and understand their role on rice allelopathy using a...     

Quantitation of tadalafil in human plasma by liquid chromatography-tandem mass spectrometry with electrospray ionization

A simple, rapid, sensitive and specific liquid chromatography-tandem mass spectrometry method was developed and validated for quantitation of tadalafil (I) in human plasma, a new selective, reversible phosphodiesterase 5 inhibitor. The analyte and internal standard (sildenafil, II) were extracted by liquid-liquid extraction with diethyl ether/dichloromethane (70/30, v/v) using a Glas-Col Multi-Pulse Vortexer. The chromatographic separation was performed on reverse phase Xterra MS C18 column with a mobile phase of 10mM ammonium formate/acetonitrile (10/90, v/v, pH adjusted to 3.0 with formic acid). The protonate of analyte was quantitated in positive ionization by multiple reaction monitoring with a mass spectrometer. The mass transitions m/z 390.4 --> 268.0 and m/z 475.5 --> 58.3 were used to measure I and II, respectively. The assay exhibited a linear dynamic range of 10-1000 ng/mL for tadalafil in human plasma. The lower limit of quantitation was 10 ng/mL with a relative standard deviation of less than 15%. Acceptable precision and accuracy were obtained for concentrations over the standard curve ranges. Run time of 1.2 min for each sample made it possible to analyze a throughput of more than 400 human plasma samples per day. The validated method has been successfully used to analyze human plasma samples for application in pharmacokinetic, bioavailability or bioequivalence studies.     

Indole-3-piperazinyl derivatives: novel chemical class of 5-HT(6) receptor antagonists

N₁-Arylsulfonyl-3-piperazinyl indole derivatives were designed and identified as a novel class of 5-HT₆ receptors ligands. All the compounds have high affinity and antagonist activity towards 5-HT₆ receptor. The compound 7a (K_i = 3.4 nM, functional assay IC₅₀ = 310 nM) shows enhanced cognitive effect when tested in NORT and Morris water maze models. Synthesis, SAR and PK profile of these novel compounds constitute the subject matter of this Letter.     

High-performance liquid chromatography method for the quantification of pantoprazole in human plasma

A sensitive and selective HPLC method with UV detection (290 nm) was developed and validated for quantitation of pantoprazole, proton-pump inhibitor, in human plasma. Following a single-step liquid-liquid extraction with methyl tert-butyl ether/diethyl ether (70/30, v/v), the analyte and internal standard (zonisamide) were separated using an isocratic mobile phase of 10mM phosphate buffer (pH 6.0)/acetonitrile (61/39, v/v) on reverse phase Waters symmetry C18 column. The lower limit of quantitation was 20 ng/mL, with a relative standard deviation of less than 4%. A linear range of 20-5000 ng/mL was established. This HPLC method was validated with between-batch and within-batch precision of 1.3-3.2% and 0.7-3.3%, respectively. The between-batch and within-batch bias was -0.5 to 8.2 % and -2.5 to 12.1%, respectively. This validated method is sensitive and repeatable enough to be used in pharmacokinetic studies.     

High-performance liquid chromatography method for the quantification of entacapone in human plasma

A simple, sensitive and selective HPLC method with UV detection (315 nm) was developed and validated for quantitation of entacapone in human plasma, the newest addition to the group of antiparkinsonian agents. Following a single-step liquid-liquid extraction (LLE) with ethyl acetate/n-hexane (30/70, v/v), the analyte and internal standard (rofecoxib) were separated using an isocratic mobile phase of 30 mM phosphate buffer (pH 2.75)/acetonitrile (62/38, v/v) on a reverse phase C18 column. The lower limit of quantitation was 25 ng/mL, with a relative standard deviation of less than 8%. A linear range of 25-2500 ng/mL was established. This HPLC method was validated with between-batch and within-batch precision of 2.2-4.2% and 1.7-7.8%, respectively. The between-batch and within-batch accuracy was 98.7-107.5% and 97.5-106.0%, respectively. Frequently coadministered drugs did not interfere with the described methodology. Stability of entacapone in plasma was excellent, with no evidence of degradation during sample processing (autosampler) and 30 days storage in a freezer. This validated method is sensitive, simple and repeatable enough to be used in pharmacokinetic studies.     

Design,synthesis and pharmacological evaluation of 4-(piperazin-1-yl methyl)-N1-arylsulfonyl indole derivatives as 5-HT6 receptor ligands

4-(Piperazin-1-yl methyl)-N₁-arylsulfonyl indole derivatives were designed and synthesized as 5-HT₆ receptor (5-HT₆R) ligands. The lead compound 6a, from this series shows potent in vitro binding affinity, good PK profile, no CYP liabilities and activity in animal models of cognition.     

High-performance liquid chromatography method for the quantification of rabeprazole in human plasma using solid-phase extraction

A simple, sensitive and selective HPLC method with UV detection (284 nm) was developed and validated for quantitation of rabeprazole in human plasma, the newest addition to the group of proton-pump inhibitors. Following solid-phase extraction using Waters Oasistrade mark SPE cartridges, the analyte and internal standard (Pantoprazole) were separated using an isocratic mobile phase of 5 mM ammonium acetate buffer (pH adjusted to 7.4 with sodium hydroxide solution)/acetonitrile/methanol (45/20/35, v/v) on reverse phase Waters symmetry C(18) column. The lower limit of quantitation was 20 ng/mL, with a relative standard deviation of less than 8%. A linear range of 20-1000 ng/mL was established. This HPLC method was validated with between- and within-batch precision of 2.4-7.2% and 2.2-7.3%, respectively. The between- and within-batch bias was -1.7 to 2.6% and -2.6 to 2.1%, respectively. Frequently coadministered drugs did not interfere with the described methodology. Stability of rabeprazole in plasma was excellent, with no evidence of degradation during sample processing (autosampler) and 3 months storage in a freezer. This validated method is sensitive, simple and repeatable enough to be used in pharmacokinetic studies.     

Siansivirga zeaxanthinifaciens gen. nov., sp. nov., a novel zeaxanthin-producing member of the family Flavobacteriaceae isolated from coastal seawater of Taiwan

A strictly aerobic, Gram-negative, rod-shaped bacterium (strain CC-SAMT-1(T)) showing gliding motility was isolated from coastal seawater of China Sea, Taiwan. Strain CC-SAMT-1(T) synthesizes all-trans-zeaxanthin (6.5 ± 0.5 mg g(-1) dry biomass) as a predominant xanthophyll carotenoid. As determined by 16S rRNA gene analysis, strain CC-SAMT-1(T) shared very high sequence similarity to the members of the genera Mariniflexile (96.1-95.3%) and Gaetbulibacter (96.0-95.9%); however, it formed a distinct phyletic lineage distantly associated with Mariniflexile species. Polar lipid profile constitutes phosphatidylethanolamine, four unidentified aminolipids, four unidentified lipids, and an unidentified glycolipid. Strain CC-SAMT-1(T) contains excessive unidentified aminolipid lipid (AL2-4) and glycolipid contents, and therefore clearly distinct from Mariniflexile species. Major fatty acids (> 5% of total fatty acids) were iso-C(15:0) (14.8%), iso-C(17:0) 3-OH (11.8%), iso-C(15:1) G (10.6%), anteiso-C(15:0) (9.7%), C(16:0) (8.1%), iso-C(16:0) 3-OH (7.9%), iso-C(15:0) 3-OH (7.5%), and summed feature 3 (containing C(16:1) ω6c and/or C(16:1) ω7c) (7.5%). Menaquinone-6 (MK-6) was major respiratory quinone. DNA G+C content was 33.7 mol%. Based on polyphasic taxonomy, strain CC-SAMT-1(T) represents a novel genus and species in the family Flavobacteriaceae for which the name Siansivirga zeaxanthinifaciens gen. nov., sp. nov. is proposed. The type strain is CC-SAMT-1(T) (= BCRC 80315(T) = JCM 17682(T)).     

Endophytic aquatic hyphomycetes in roots of riparian tree species of two Western Ghat streams

Bubble chamber incubation of surface sterilized segments of root bark and xylem of 10 riparian tree species of the Sampaje (475–500 m asl) and V?Badaga (765–800 m asl) stream reaches of the Western Ghats yielded 20 species of endophytic aquatic hyphomycetes. Anguillospora crassa, A. longissima and Cylindrocarpon sp. were among the top five species in streams. A two-way ANOVA showed significantly higher species richness and counts of conidium in the tree species of Sampaje compared to V?Badaga (p < 0.001), while two variables were not significantly different between bark and xylem. The total number of species recovered was slightly higher in bark than in xylem (14–19 vs. 13–17 spp.) and the average species richness between tissues did not differ significantly except for one tree species (Madhuca neriifolia: p < 0.05). The release of conidia from bark of only three tree species was significantly higher than from xylem (M. neriifolia and Canarium strictum: p < 0.05; Vateria indica: p < 0.01). Sørensen’s similarity index for bark as well as xylem between tree species was higher in Sampaje stream than in V?Badaga stream (0.45–0.78 vs. 0.25–0.61). The diversity of aquatic hyphomycetes in bark and xylem was higher in the trees of Sampaje than V?Badaga (3.1–3.3 vs. 2.7). A cluster analysis of aquatic hyphomycetes in bark and xylem resulted in two groups coinciding with the two streams. The results of this study revealed that assemblage and diversity of endophytic aquatic hyphomycetes in riparian tree roots are high in the mid-altitude Sampaje stream as previously documented for saprotrophic aquatic hyphomycetes.