Multiple FAS1 domains and the RGD motif of TGFBI act cooperatively to bind αvβ3 integrin,leading to anti-angiogenic and anti-tumor effects

TGFBI, a transforming growth factor β-induced extracellular matrix protein, circulates at a level of ~ 300 ng/ml in humans and modulates several integrin-mediated cellular functions. The protein contains an N-terminal EMI domain, four consecutive FAS1 domains, and the RGD motif. Each FAS1 domain and the RGD motif have been known to interact with avb3 integrin. Here, we found that the binding affinity (K_d) of TGFBI for αvβ3 integrin was approximately 3.8 × 10^? 8 M, a value ~ 2300-fold higher than that of a single FAS1 domain, and demonstrated that this greater affinity was due to the cooperative action of the four FAS1 domains and the RGD motif. Moreover, TGFBI exhibited more potent anti-angiogenic and anti-tumorigenic activities, even at a 100-fold lower molar dose than the reported effective dose of the FAS1 domain. Finally, our data showed that TGFBI specifically targeted the tumor vasculature and accumulated at the tumor site. Collectively, our results support the theory that TGFBI acts as a potent endogenous anti-tumor and anti-angiogenic molecule by targeting αvβ3 integrin, and highlights the importance of physiological circulating TGFBI levels in inhibiting tumor growth.     

Redox properties of a thioredoxin-like Arabidopsis protein,AtTDX

AtTDX is an enzyme present in Arabidopsis thaliana which is composed of two domains, a thioredoxin (Trx)-motif containing domain and a tetratricopeptide (TPR)-repeat domain. This enzyme has been shown to function as both a thioredoxin and a chaperone. The midpoint potential (E_m) of AtTDX was determined by redox titrations using the thiol-specific modifiers, monobromobimane (mBBr) and mal-PEG. A NADPH/Trx reductase (NTR) system was used both to validate these E_m determination methods and to demonstrate that AtTDX is an electron-accepting substrate for NTR. Titrations of full-length AtTDX revealed the presence of a single two-electron couple with an E_m value of approximately ?260 mV at pH 7.0. The two cysteines present in a typical, conserved Trx active site (WCGPC), which are likely to play a role in the electron transfer processes catalyzed by AtTDX, have been replaced by serines by site-directed mutagenesis. These replacements (i.e., C304S, C307S, and C304S/C307S) resulted in a complete loss of the redox process detected using either the mBBr or mal-PEG method to monitor disulfide/dithiol redox couples. This result supports the conclusion that the couple with an E_m value of ?260 mV is a disulfide/dithiol couple involving Cys304 and Cys307. Redox titrations for the separately-expressed Trx-motif containing C-domain also revealed the presence of a single two-electron couple with an E_m value of approximately ?260 mV at 20 °C. The fact that these two E_m values are identical, provides additional support for assignment of the redox couple to a disulfide/dithiol involving C304 and C307. It was found that, while the disulfide/dithiol redox chemistry of AtTDX was not affected by increasing the temperature to 40 °C, no redox transitions were observed at 50 °C and higher temperatures. In contrast, Escherichia coli thioredoxin was shown to remain redox-active at temperatures as high as 60 °C. The temperature-dependence of the AtTDX redox titration is similar to that observed for the redox activity of the protein in enzymatic assays.     

Partitioning of latent heat flux at a northern peatland

The partitioning of latent heat flux (Q_E) to vascular plant and moss surface components was assessed for a Sphagnum-dominated bog with a hummock–hollow surface having a sparse canopy of low shrubs. Results from porometry and eddy covariance measurements of Q_E showed evaporation from the moss surface ranged from greater than 50% of total Q_E early in the growing season to less than 20% after a dry period toward the end of the growing season. Both soil moisture and vapour pressure deficit (D_a) affected this partitioning with drier moss and peat, lower water table, and smaller D_a all reducing moss Q_E. Daily maximum moss Q_E ranged from greater than 200 W m⁻² early in the growing season to less than 100 W m⁻² during a dry period. In contrast, vascular contribution to total Q_E increased over the season from a daily maximum of about 150 W m⁻² to 250 W m⁻² due to increase in leaf area by leaf replacement and emergence and to drying of the moss surface. Porometry results showed average daily maximum conductance from bog shrubs was near 8 mm s⁻¹. These conductance values were smaller than those reported for vascular plants from more nutrient-rich wetlands. The effect of increases in D_a on vascular Q_E were moderated by decreases in stomatal conductance. At constant available energy, vascular leaf conductance was reduced by as much as 2 mm s⁻¹ and moss surface conductance was enhanced by up to 3 mm s⁻¹ by large D_a. Considering vascular and non-vascular water transport characteristics and frequency of water table position and given the observed variations of Q_E partitioning with water table location and moss and peat water content, it is suggested that modelling efforts focus on how dry hummocks and wet hollows each contribute to Q_E, especially as related to D_a and soil moisture dynamics.     

Structural–functional insights of single and multi-domain Capsicum annuum protease inhibitors

Pin-II protease inhibitors (PIs) are the focus of research interest because of their large structural–functional diversity and relevance in plant defense. Two representative Capsicum annuum PI genes (CanPI-15 and -7) comprising one and four inhibitory repeat domains, respectively, were expressed and recombinant proteins were characterized. β-Sheet and unordered structure was found predominant in CanPI-15 while -7 also displayed the signatures of polyproline fold, as revealed by circular dichroism studies. Inhibition kinetics against bovine trypsin indicated three times higher potency of CanPI-7 (K_i ～ 57 μM) than -15 (～184 μM). Activity and structural stability of these CanPIs were revealed under various conditions of pH, temperature and denaturing agent. Structure prediction, docking studies with proteases and mass spectroscopy revealed the organization of multiple reactive site loops of multi domain PIs in space as well as the steric hindrances imposed while binding to proteases due to their close proximity.     

Probing the active-site requirements of human intestinal N-terminal maltase glucoamylase: The effect of replacing the sulfate moiety by a methyl ether in ponkoranol,a naturally occurring α-glucosidase inhibitor

Ponkoranol is a naturally occurring glucosidase inhibitor isolated from the plant Salacia reticulata. The compound comprises a sulfonium ion with an internal sulfate counter ion. We report here an efficient synthetic route to 3′-O-methyl ponkoranol to test the hypothesis that occupation of a hydrophobic pocket by a methyl group instead of the polar sulfate ion within the active site of human N-terminal maltase glucoamylase would be beneficial. The synthetic strategy relies on the nucleophilic attack of 2,3,5-tri-O-benzyl-1,4-anhydro-4-thio-d-arabinitol at the C-6 position of benzyl 6-O-p-toluenesulfonyl β-d-glucopyranoside, followed by deprotection using boron trichloride and reduction with sodium borohydride. The target compound inhibited the N-terminal catalytic domain of intestinal human maltase glucoamylase (ntMGAM) with a K_i value of 0.50 ± 0.04 μM, higher than those of de-O-sulfonated ponkoranol (K_i = 43 ± 3 nM), or its 5′-stereoisomer (K_i = 15 ± 1 nM). We conclude that the interaction of the methyl group with hydrophobic residues in the active site is not as beneficial to inhibition of ntMGAM as the other interactions of the polyhydroxylated chain with active-site residues.     

Breast cancer aromatase expression evaluated by the novel antibody 677: Correlations to intra-tumor estrogen levels and hormone receptor status

Breast cancer tissue estrogen levels on an average exceed plasma as well as benign breast tissue levels. To evaluate the contribution of intra-tumor aromatization to individual tumor estrogen levels (estradiol, E₂; estrone, E₁; estrone sulfate, E₁S), breast cancer tissue sections obtained during mastectomy in 28 postmenopausal breast cancer patients were stained for aromatase protein expression using the aromatase antibody 677. The findings were correlated to intra-tumor estrogen levels determined with a highly sensitive HPLC-RIA. Staining with 677 alone (irrespective of the hormone receptor status) revealed no difference in tumor E₂ levels comparing 677+ versus 677? tumors, although a non-significant trend towards higher tumor E₁ and E₁S levels was observed in 677+ breast cancers. In contrast, tumor levels of E₂ were significantly higher in ER+ tumors compared to ER? tumors (P < 0.001) and to benign breast tissue from the same breast (P < 0.001). Analysing the additional effect of positive staining with the aromatase antibody 677 on tumor estrogen levels in the subgroup of ER+ tumors, revealed significantly higher tumor levels of E₂ (mean level of 544.7 versus 197.1 fmol/g tissue) as well as a non-significant trend concerning tumor E₁ (mean level of 296.9 versus 102.1 fmol/g tissue). The mean tumor tissue E₁S level was observed somewhat lower in ER+677+ (103.5 fmol/g) versus ER+677? tumors (190.1 fmol/g). In the subgroup of ER+PgR+ tumors, tissue levels of E₂ were also found to be significantly higher among 677+ compared to 677? tumors: 873.2 fmol/g (95% CI 395.9–1925.6) versus 217.9 fmol/g (95% CI 88.8–534.9) (P = 0.015).In conclusion, our results indicate a moderate effect of aromatase enzyme expression evaluated by IHC using the antibody 677 on intra-tumor estrogen levels among ER+ breast cancers. A substantial interindividual variation in the ratios between the individual estrogen fractions suggests additional effects, like alterations in other enzymes to be involved in the intra-tumor estrogen homeostasis.     

Overexpression of the TIR-X gene results in a dwarf phenotype and activation of defense-related gene expression in Arabidopsis thaliana

The Arabidopsis genome encodes various proteins with a Toll/interleukin-1 receptor (TIR) domain. Many of these proteins also contain nucleotide-binding site (NBS) and leucine-rich repeat (LRR) domains and function as resistance (R) proteins. However, the protein encoded by At2g32140 (a TIR-X gene) contains a TIR domain but lacks NBS and LRR domains. We found that transgenic plants overexpressing At2g32140 displayed a dwarf phenotype and showed increased expression of defense-related genes. In general, the growth defect caused by activation of defense responses is suppressed under high-temperature conditions. However, transgenic plants overexpressing At2g32140 displayed a much stronger dwarf phenotype at 28 °C than at 22 °C. This dwarf phenotype was suppressed under the combination with known salicylic-acid pathway mutants. These findings suggest that At2g32140 encodes a protein involved in the plant defense response.     

Mechanical asymmetry during articulation of tibial and femoral cartilages: Local and overall compressive and shear deformation and properties

During knee movement, femoral cartilage articulates against cartilage from the tibial plateau, and the resulting mechanical behavior is yet to be fully characterized. The objectives of this study were to determine (1) the overall and depth-varying axial and shear strains and (2) the associated moduli, of femoral and tibial cartilages during the compression and shearing of apposing tibial and femoral samples. Osteochondral blocks from human femoral condyles (FCs) characterized as normal and donor-matched lateral tibial plateau (TP) were apposed, compressed 13%, and subjected to relative lateral motion. When surfaces began to slide, axial (?E_zz) and shear (E_xz) strains and compressive (E) and shear (G) moduli, overall and as a function of depth, were determined for femoral and tibial cartilages. Tibial ?E_zz was ～2-fold greater than FC ?E_zz near the surface (0.38 versus 0.22) and overall (0.16 versus 0.07). Near the surface, E_xz of TP was 8-fold higher than that of FC (0.41 versus 0.05), while overall E_xz was 4-fold higher (0.09 versus 0.02). For TP and FC, ?E_zz and E_xz were greatest near the surface and decreased monotonically with depth. E for FC was 1.7-fold greater than TP, both near the surface (0.40 versus 0.24 MPa) and overall (0.76 versus 0.47 MPa). Similarly, G was 7-fold greater for FC (0.22 MPa) than TP near the surface (0.03 MPa) and 3-fold higher for FC (0.38 MPa) than TP (0.13 MPa) overall. These results indicate that tibial cartilage deforms and strains more axially and in shear than the apposing femoral cartilage during tibial–femoral articulation, reflecting their respective moduli.     

Insecticide susceptibility of Ephemera orientalis (Ephemeroptera: Ephemeridae) and two mosquito species,Anopheles sinensis and Culex pipiens in the Republic of Korea

Field-collected populations of mayflies, Ephemera orientalis were tested for susceptibility to 10 different insecticides using a direct-contact mortality bioassay. Ephemera orientalis subimagoes were susceptible to the insecticides chlorpyrifos, fenitrothion and chlorfenapyr with LD₅₀ values of 69.7, 78.8 and 81.9 μg/♀, and adults had LD₅₀ values of 71.9, 78.8 and 85.4 μg/♀, respectively. Susceptibility ratios (SRs) of subimagoes and adults of E. orientalis to the 10 insecticides were 1.0 to1.2 folds. The mayflies showed higher susceptibility to organophosphates than to pyrethroids. The SRs of Anopheles sinensis to E. orientalis were 514 to 1438 folds higher for organophosphates (LD₅₀ values of 0.05 to 0.23 μg/♀) and 62 to 1155 folds higher for pyrethroids (LD₅₀ values of 0.13 to 2.41 μg/♀). The SRs of Culex pipiens to E. orientalis were 606 to 3595 folds higher for organophosphates with LD₅₀ values of 0.02–0.17 μg/♀ and 81 to 1365 folds higher for pyrethroids with LD₅₀ values of 0.11–1.83 μg/♀. These results indicate that the use of ineffective insecticides will result in unsatisfactory control against field populations of the subimagoes and adults of E. orientalis.     

Antimicrobial activities of Dilobeia thouarsii Roemer and Schulte,a traditional medicinal plant from Madagascar

The leaves of Dilobeia thouarsii (Roemer and Schulte), a tree that is endemic to Madagascar (Proteaceae), are used in traditional Malagasy medicine to treat bacterial skin infections and wounds. This study investigated the in vitro antibacterial activities of D. thouarsii leaf extracts and identified the bioactive compounds with the aim of providing a scientific basis for its use against skin diseases. Using broth microdilution method for leaf crude extract and its compounds, we investigated inhibition of the growth of Bacillus cereus, Bacillus megaterium, Staphylococcus aureus, Enterococcus faecalis, Vibrio harveyi, Vibrio fisheri, Salmonella Typhimurium, Salmonella antarctica, Escherichia coli, and Klebsiella pneumoniae. The two purified phenolic compounds from leaf ethyl acetate extracts (1, 2) were found to be more active than the crude extract itself. The structure of the two compounds was elucidated by NMR and mass spectrometry: compound 1 was identified as 4-aminophenol and compound 2 as 4-hydroxybenzaldehyde. A marked inhibitory effect (MIC < 0.1 mg/ml) was found against S. aureus, which is a major agent in skin infections. We observed moderate activities (MIC values of between 0.1 and 0.5 mg/ml) for E. faecalis, Vibrio spp., and Bacillus spp. Neither compound was active against Salmonella spp., E. coli and K. pneumoniae (MICs > 1 mg/ml). To conclude, the high antimicrobial activity of D. thouarsii leaf extracts against S. aureus supports its traditional use to treat skin infections.     

Esculentin-2CHa: A host-defense peptide with differential cytotoxicity against bacteria,erythrocytes and tumor cells

The host-defense peptide, esculentin-2CHa (GFSSIFRGVA¹⁰KFASKGLGK D²⁰LAKLGVDLVA³⁰ CKISKQC) shows potent (MIC ≤ 6 μM) growth inhibitory activity against clinical isolates of multidrug-resistant strains of Staphylococcus aureus, Acinetobacter baumannii, and Stenotrophomonas maltophilia and differential cytotoxic activity against human erythrocytes (LC₅₀ = 150 μM) and human non-small cell lung adenocarcinoma A549 cells (LC₅₀ = 10 μM). Esculentin-2CHa significantly (P < 0.01) stimulates the release of the anti-inflammatory cytokine IL-10 by mouse lymphoid cells and elevates its production after stimulation with concanavalin A and significantly (P < 0.05) stimulates TNF-α production by peritoneal macrophages. Effects on IL-6 and IL-1β production were not significant. Removal of the hydrophobic N-terminal hexapeptide (GFSSIF) from esculentin-2CHa results in abolition of growth inhibitory activity against S. aureus and cytotoxic activity against erythrocytes and A549 cells as well as a marked (≥16-fold) reduction in potency against A. baumannii and S. maltophilia. The primary structure of esculentin-2 has been poorly conserved between frog species but evolutionary pressure has acted to maintain the hydrophobic character of this N-terminal hexapeptide sequence. Removal of the cyclic C-terminal domain (CKISKQC) and replacement of the Cys³¹ and Cys³⁷ residues by serine resulted in appreciable decreases in cytotoxicity against all microorganisms and against mammalian cells. The more cationic [D20K, D27K] analog showed a modest increase in potency against all microorganisms (up to 4-fold) but a marked increase in cytotoxicity against erythrocytes (LC₅₀ = 11 μM) and A549 cells (LC₅₀ = 3 μM).     

Synthesis,EPR, electrochemistry and EXAFS studies of ruthenium(III) complexes with a symmetrical tetradentate N2O2 Schiff base

A series of new hexa-coordinated ruthenium(III) complexes of the type [RuX(Nap-o-phd)(EPh₃)] (where, H₂-Nap-o-phd = N,N′-bis(2-hydroxy-1-naphthaldehyde) o-phenylene diamine; X = Cl or Br; E = P or As) have been prepared by reacting [RuX₃(EPh₃)₃] and [RuBr₃(PPh₃)₂(MeOH)] (where X = Cl or Br; E = P or As) with tetradentate Schiff base ligand (H₂-Nap-o-phd) in 1:1 molar ratio. The complexes have been characterized by elemental analyses, infra red, electronic, electron paramagnetic resonance spectroscopy and cyclic voltammetry. The coordination geometry and structure of the complexes have been investigated by extended X-ray absorption fine structure (EXAFS) spectroscopy and an octahedral structure has been proposed.     

Glutathione redox dynamics and expression of glutathione-related genes in the developing embryo

Embryonic development involves dramatic changes in cell proliferation and differentiation that must be highly coordinated and tightly regulated. Cellular redox balance is critical for cell fate decisions, but it is susceptible to disruption by endogenous and exogenous sources of oxidative stress. The most abundant endogenous nonprotein antioxidant defense molecule is the tripeptide glutathione (γ-glutamylcysteinylglycine, GSH), but the ontogeny of GSH concentration and redox state during early life stages is poorly understood. Here, we describe the GSH redox dynamics during embryonic and early larval development (0–5 days postfertilization) in the zebrafish (Danio rerio), a model vertebrate embryo. We measured reduced and oxidized glutathione using HPLC and calculated the whole embryo total glutathione (GSH_T) concentrations and redox potentials (E_h) over 0–120 h of zebrafish development (including mature oocytes, fertilization, midblastula transition, gastrulation, somitogenesis, pharyngula, prehatch embryos, and hatched eleutheroembryos). GSH_T concentration doubled between 12 h postfertilization (hpf) and hatching. The GSH E_h increased, becoming more oxidizing during the first 12 h, and then oscillated around −190 mV through organogenesis, followed by a rapid change, associated with hatching, to a more negative (more reducing) E_h (−220 mV). After hatching, E_h stabilized and remained steady through 120 hpf. The dynamic changes in GSH redox status and concentration defined discrete windows of development: primary organogenesis, organ differentiation, and larval growth. We identified the set of zebrafish genes involved in the synthesis, utilization, and recycling of GSH, including several novel paralogs, and measured how expression of these genes changes during development. Ontogenic changes in the expression of GSH-related genes support the hypothesis that GSH redox state is tightly regulated early in development. This study provides a foundation for understanding the redox regulation of developmental signaling and investigating the effects of oxidative stress during embryogenesis.     

Synthesis and characterization of a fluorescent probe for α-tocopherol suitable for fluorescence microscopy

Previously prepared fluorescent derivatives of α-tocopherol have shown tremendous utility in both in vitro exploration of the mechanism of ligand transfer by the α-tocopherol transfer protein (α-TTP) and the intracellular transport of α-tocopherol in cells and tissues. We report here the synthesis of a 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (BODIPY) containing α-tocopherol analog having extended conjugation with an alkenyl thiophene group that extends the absorption and emission maxima to longer wavelengths (λ_ex = 571 nm and λ_em = 583 nm). The final fluorophore thienyl-ene-BODIPY-α-tocopherol, 2, binds to recombinant human α-TTP with a K_d = 8.7 ± 1.1 nM and is a suitable probe for monitoring the secretion of α-tocopherol from cultured Mcf7#189 cells.     

Cloning,heterologous expression and characterization of two keratinases from Stenotrophomonas maltophilia BBE11-1

The keratin-degrading strain Stenotrophomonas maltophilia BBE11-1 secretes two keratinolytic proteases, KerSMD and KerSMF. However, the genes encoding these proteases remain unknown. Here, we have isolated these two genes with a modified TAIL-PCR (thermal asymmetric interlaced PCR) method based on the N-terminal amino acid sequences of mature keratinases. These two keratinase genes encode serine proteases with PPC (bacterial pre-peptidase C-terminal) domain, which are successfully expressed with the help of pelB leader in Escherichia coli cells. Recombinant KerSMD (48 kDa) shows a better activity in feather degradation, higher thermostability and substrate specificity than KerSMF (40 kDa). KerSMD has a t_1/2 of 90 min at 50 °C and 64 min at 60 °C, and a better tolerance to surfactants SDS and triton X-100. The predicted model of KerSMD helps to explain the phenomenon of auto-catalytic C-terminal propeptide truncation, the special function of PPC domain, and the molecular weight of the C-terminal-processed mature keratinase KerSMD. This work not only provides a new way to overproduce keratinases but also helps to explore keratinases folding mechanism.     

Inventory and input–output analysis of CO2 emissions by fossil fuel consumption in Beijing 2007

With the most recent statistics available, a concrete emissions inventory is compiled for an input–output analysis to investigate the embodied CO₂ emissions induced by fossil fuel combustion of Beijing economy in 2007. Results show that the total direct CO₂ emissions amount to 9.45E + 07 t, within which 56.81% are released from coal combustion, 11.50% from coke combustion, 9.03% from kerosene combustion, 8.70% from natural gas and 6.40% from diesel, respectively. The average intensity of secondary industries (3.12 t/1E + 4 Yuan) is 0.65 times larger than that of primary industries (1.89 t/1E + 4 Yuan) and 1.58 times larger than that of tertiary industries (1.21 t/1E + 4 Yuan). The sector of Construction Industry contributes the largest share (21.98%) of CO₂ emissions embodied in final demand for Beijing due to its considerable capital investment. Beijing is a net importer of embodied CO₂ emissions with total import and export of 3.06E + 08 and 2.00E + 08 t, respectively. Results of this study provide a sound scientific database for effective policy making in Beijing to reduce CO₂ emissions.     

Growth and antrum formation of bovine primary follicles in long-term culture in vitro

Successful antral formation in vitro from bovine preantral follicles (145–170 μm) has been described previously, but antrum formation from the primary follicle (50–70 μm) has not yet been achieved in vitro. The aim of the study was to establish an optimal culture system supporting the growth and maturation of bovine primary follicles (50–70 μm) in vitro. Bovine primary follicles were cultured in a three-dimensional culture system for 13 or 21 days in alpha-minimum essential medium. Various treatments including follicle stimulating hormone (FSH), luteinizing hormone (LH), 17β-estradiol (E₂), basic fibroblast growth factor (bFGF) and epidermal growth factor (EGF) were tested. The follicular diameter and antrum formation rate were recorded, and follicular maturation markers (P450 aromatase, CYP19A1; anti-Mullerian hormone, AMH; growth differentiation factor-9, GDF9; bone morphogenetic protein-15, BMP15; and type III transforming growth factor β receptor, TGFβR3) were analyzed by real-time RT-PCR. After 21 days of culture under each treatment condition, the follicular diameter was significantly enlarged in the presence of FSH + LH + E₂ + bFGF or FSH + LH + E₂ + bFGF + EGF (p < 0.05). An addition of 50 ng/ml bFGF or bFGF + 25 ng/ml EGF initiated antrum formation by day 19 and day 17 of culture, and the antral cavity formation rate was 16.7% and 33.3% by 21 days of culture, respectively. The expression of follicular maturation markers (CYP19A1, AMH, GDF9, BMP15 and TGFβR3) was significantly altered. We conclude that addition of 50 ng/ml bFGF + 25 ng/ml EGF to media containing FSH + LH + E₂ turned out to be the most effective optimized culture conditions to support the growth and maturation of bovine primary follicles in vitro.     

Glycolipid ester-type heterodimers from Ipomoea tyrianthina and their pharmacological activity

Tyrianthins A (1) and B (2), two new partially acylated glycolipid ester-type heterodimers were isolated from Ipomoea tyrianthina. Scammonic acid A was determined as the glycosidic acid in both monomeric units. Tyrianthin A (1) (IC₅₀ 0.24 ± 0.09 μM and E_max 81.80 ± 0.98%), and tyrianthin B (2) (IC₅₀ 0.14 ± 0.08 μM and E_max 87.68 ± 0.72%) showed significant in vitro relaxant effect on aortic rat rings, in endothelium- and concentration-dependent manners. Also, these compounds were able to increase the release of GABA and glutamic acid in brain cortex, and displayed weak antimycobacterial activity.     

Photoactivated disinfection (PAD) of dental root canal system – An ex-vivo study

AimTo investigate the efficacy of photo activated disinfection (PAD) in reducing colony-forming unit (CFU) counts of Enterococcus faecalis (E. faecalis) in infected dental root canals. The study compared the efficacy of PAD with conventional endodontic treatment (CET) and also a combination of CET along with PAD.Material and Methods53 maxillary incisors were taken for the study. Teeth were divided into 3 groups, CET (Group I) (n = 11), PAD (Group II) (n = 21), and a combination of CET and PAD (Group III) which consisted of (n = 21) samples, Group II and Group III were further divided into 2 subgroups, Group IIa, IIb and Group IIIa, IIIb. Strains of E. faecalis were inoculated in all the root canals. CET group samples were treated by chemo-mechanical preparation (CMP) alone, PAD samples were treated with laser alone at 2 different exposure time (4 min and 2 min). In the combination treatment, samples were treated initially by CET and then by PAD for a time period of 4 min and 2 min. Contents of the root canal were aspirated, diluted and plated in Tryptone Soya Broth (TSB) and plates were incubated for 24 h to observe the bacterial regrowth.ResultsShowed PAD used along with CMP reduced the bacterial load of E. faecalis by 99.5% at 4 min and 98.89% at 2 min.ConclusionPAD may be an adjunctive procedure to kill residual bacteria in the dental root canal systems after standard endodontic root canal preparation.     

The structural definition of some novel adducts of stoichiometry CuX:dpex:MeCN (2:1:1)(n), X = (pseudo-) halogen,dppx = Ph2E(CH2)xEPh2, E = P,As, Sb

Single-crystal X-ray studies have defined the structures of a number of novel adducts of the form CuX:dpex (2:1), X = (pseudo-)halide, dpex = bis(diphenylpnicogeno)alkane, Ph₂E(CH₂)_xEPh₂, E = P, As, of diverse types, solvated with acetonitrile. CuBr:dpem (2:1)₂. 2MeCN (E = both P, As) are tetranuclear, derivative of the familiar ‘step’ structure, while CuCl:dpph (MeCN solvate) and CuBr:dppe (MeCN solvate) yield one-dimensional polymers (i.e., x = 1, 2, 6 for dppx, x = m, e, h), as also does CuSCN:dpam (MeCN solvate). In CuI:dpsm:MeCN (3:1:2) (‘dpsm’ = Ph₂Sb(CH₂)SbPh₂), CuI:dpsm (2:1)₂ ‘step’ units are connected into an infinite ‘stair’ polymer by interspersed (MeCN)CuI linkers.