Effects of length and type of the alkyl chain on the micellization behavior of mixed systems of HS15 with fatty acids.

Due to volatility, low solubility and instability, the application of SCFAs and MCFAs is limited, which is expected to be solved by micelles. Taking SCFAs and MCFAs as models, this paper aims to research the influences of alkyl chain length and type on HS15 micelles. The critical micelle concentration (CMC) of various acid-HS15 systems was determined firstly. Then some air-water interface parameters and thermodynamic parameters were analyzed. Subsequently, particle size, cloud points (CP) and fluorophore release curves were measured. With the increase of CMC and Gmin, the decrease of size and CP, and the rapid quenching of fluorophores, it is more difficult for acids with longer-chain to form stable micelles with HS15 because of the strength of iceberg structure. Showing smaller CMC and Gmin, smaller size, higher CP and slower release of fluorescers, branched molecules can bind more closely to the hydrophobic part of HS15 due to their spatial flexibility.

The complete mitochondrial genome of a planarian flatworm Girardia tigrina (Tricladida: Dugesiidae).

Girardia tigrina, a freshwater planarian species native to America and introduced to other continents, has been usually used as model organism in many research fields of biology. In this study, we determined the complete mitochondrial genome of G. tigrina using next-generation sequencing (NGS). The complete mitogenome was 15,938 bp in length, with 36 genes, including 12 protein-coding genes, 2 ribosomal RNAs and 22 transfer RNAs, and ATP8 was absent in the mitogenome of G. tigrina as in the mitogenomes of some other flatworms. The maximum-likelihood phylogenetic tree suggested that G. tigrina was closely related to genus Dugesia in the clade of Tricladida.

15-hydroxystearate micelles for the delivery of aprepitant: Preparation, characterization, pharmacokinetics and tissue distribution in mice.

This study developed a novel Aprepitant micells (APPT-Ms) formulation that uses a mixture of 15-hydroxystearate (HS15) as surfactant to solubilize AAPT. This article determines the content of APPT by HPLC. The in vitro test results show that the optimized APPT-Ms has small particle size, excellent stability and long-lasting release. At a test dose of 20mg/kg, the pharmacokinetic study of APPT-Ms showed that it accorded with first-order kinetics in mice, and its AUC value was higher than the pure AAPT about 6 times. The tissue distribution study of mice showed that the APPT-Ms had higher tissue binding ability than pure AAPT. The APPT-Ms could be rapidly distributed to various tissues and it was easier to pass through the blood-brain barrier than APPT. In this study, the APPT-Ms has high antiemetic activity and improves the compliance of patient. The pharmacokinetics and tissue distribution of APPT-Ms after injection administration were studied, which may be of guiding significance for further research.

New PTX-HS15/T80 Mixed Micelles: Cytotoxicity, Pharmacokinetics and Tissue Distribution.

Compared with single micelle, the new PTX-HS15/T80 mixed micelle system (PTX-HS15/T80 MMs) had achieved better results in solubilization, stability, and sensitization before. Therefore, we intend to further verify the potential advantages of the mixed micelle delivery system through in vitro cytotoxicity test and animal test to understand the anticancer effect and in vivo pharmaceutical behavior of the system. In vitro cytotoxicity test showed that the new PTX-HS15/T80 MMs had a stronger ability to inhibit the proliferation of cancer cells. The results of in vivo pharmacokinetics showed that the micelle had shorter half-life, higher clearance rate, and lower blood concentration and had good blood clearance characteristics. The results of in vivo tissue distribution showed that, compared with the single micelle Taxol®, the new PTX-HS15/T80 MMs had good distribution characteristics in the lung (AUC (lung 0-4 H) increased about 26%) and low concentration in the heart (AUC (Heart 0-4 H) decreased about 10%). Paclitaxel was mainly metabolized through the liver and kidney. The above results suggested that the new PTX-HS15/T80 MMs may have a certain therapeutic potential against lung cancer and reduce the toxic and side effects. In general, the mixed micelle delivery system was not only simple and cheap to prepare but also had certain advantages in vitro and in vivo, indicating that the combination of surfactants provides a good choice for solving the problem of insoluble drug delivery.

Kolliphor® HS 15-cyclodextrin Complex for the Delivery of Voriconazole: Preparation, Characterization, and Antifungal Activity.

BACKGROUND: This study aimed to reduce the amount of sulfobutylether-ß-cyclodextrin (SBECD) used in the marketed voriconazole injections to meet the clinical needs of patients with moderate-to-severe renal impairment (creatinine clearance rate <50 mL/min). OBJECTIVE: This study found that the surfactant Kolliphor® HS 15 (HS 15) and SBECD had significant synergistic effects on solubilizing voriconazole, and a novel voriconazole complex delivery system (VRC-CD/HS 15) was established. METHODS: The complex system was characterized, and its antifungal activity was studied by dynamic light scattering, dialysis bag method, disk diffusion, and broth microdilution. RESULTS: Compared with the control, its encapsulation efficiency (90.07±0.48%), drug loading (7.37±0.25%) and zeta potential (-4.36±1.37 mV) were increased by 1.54%, 41.19%, and 296.36%, respectively; its average particle size (13.92±0.00 nm) was reduced by 15.69%, so the complex system had better stability. Simultaneously, its drug release behavior was similar to that of the control, and it was a first-order kinetic model. Antifungal studies indicated that the complex system had noticeable antifungal effects. With the increase of drug concentration, the inhibition zone increased. The minimum inhibitory concentrations of the complex system against Cryptococcus neoformans, Aspergillus niger and Candida albicans were 0.0313 µg/mL, 1 µg/mL and 128 µg/mL, respectively. CONCLUSION: It showed a significant inhibitory effect on C. neoformans and had a visible therapeutic effect on Kunming mice infected with C. neoformans. Consequently, VRC-CD/HS 15 had better physicochemical properties and still had an apparent antifungal effect, and was promising as a potential alternative drug for clinical application.

Distinct Roles of Smooth Muscle and Non-muscle Myosin Light Chain-Mediated Smooth Muscle Contraction.

Both smooth muscle (SM) and non-muscle (NM) myosin II are expressed in hollow organs such as the bladder and uterus, but their respective roles in contraction and corresponding physiological functions remain to be determined. In this report, we assessed their roles by analyzing mice deficient of Myl9, a gene encoding the SM myosin regulatory light chain (SM RLC). We find that global Myl9-deficient bladders contracted with an apparent sustained phase, despite no initial phase. This sustained contraction was mediated by NM myosin RLC (NM RLC) phosphorylation by myosin light chain kinase (MLCK). NM myosin II was expressed abundantly in the uterus and young mice bladders, of which the force was accordingly sensitive to NM myosin inhibition. Our findings reveal distinct roles of SM RLC and NM RLC in SM contraction.

Molecular cloning, antiserum preparation and expression analysis during head regeneration of α-crystallin type heat shock protein in Hydra vulgaris.

Our previous study based on the transcriptome profiling indicated that a fragment of α-crystallin type heat shock protein (α-Hsp) gene was one of the numerous cDNA sequences expressed differentially at various stages of head regeneration in Hydra vulgaris. To further investigate the role that which α-Hsp plays during hydra regeneration, a full-length cDNA of α-Hsp gene of H. vulgaris was isolated by the rapid amplification of cDNA ends (RACE) technique. The full-length cDNA of α-Hsp gene was 1156 bp, containing a 765 bp open-reading frame (ORF), which encodes a polypeptide of 254 amino acid residues with a molecular weight of 29.27 kDa. Further, the ORF was subcloned into the plasmid pET-42a(+), and the recombinant plasmid pET-42a(+)-α- Hsp was transformed to Escherichia coli BL21(DE3), then the fusion protein GST-α-Hsp was expressed mainly in the form of a soluble molecule after induction by isopropyl-ß-d-thiogalactopyranoside. In addition, BALB/Cmice were immunized with the fusion protein to prepare the polyclonal antiserum which was used as the primary antibody for whole-mount immunohistochemical assay. The results from the immunohistochemical assay showed that α-Hsp had expressedmainly at the wound site and nearby area of hydra after decapitation operation, and both quantitative real-time polymerase chain reaction (qPCR) analysis and immunohistochemical assay revealed that the expression level of α-Hsp increased gradually during the early period of hydra regeneration, then reached a peak at 24 h after decapitation operation, while decreased during the late regeneration period. Moreover, it indicated an important role of α-Hsp gene in hydra head regeneration that RNA interference (RNAi)-mediated α-Hsp silencing led to the obvious delay of the regeneration of head structures in H. vulgaris. In conclusion, our results gave the hint that α-Hsp could be related to wound healing and tissue remodelling at early regeneration stages, and may lay the foundation for further studies about the physiological function and role of α-Hsp during hydra regeneration.

A stability-Indicating HPLC Method for Simultaneous Determination of Creatine Phosphate Sodium and its Related Substances in Pharmaceutical Formulation.

The objective of the study was to develop a simple, specific and stability-indicating HPLC method for the simultaneous determination of creatine phosphate sodium (CPS) and its related substances in pharmaceutical formulation. Separation of creatine phosphate sodium from its major process impurities and degradation products was achieved on a Hypersil BDS C18 column (250 × 4.6 mm, 5 µm) with an aqueous mobile phase containing 0.2% (w/v) tetrabutylammonium hydroxide (TAH) and 0.2% (w/v) monopotassium phosphate adjusted to pH 6.6 with orthophosphoric acid at a flow rate of 1.0 mL min(-1). The analytes were detected at 210 nm. Different chromatographic parameters were carefully optimized. The relative response factors for creatine, creatinine and creatinine phosphate disodium salt relative to CPS were determined. The method has been validated with respect to solution stability, system suitability, LOD, LOQ, linearity, accuracy, precision, specificity and robustness. The validation criteria were met in all cases. The developed method was successfully applied to determine the purity of CPS in pharmaceutical formulation.

The complete mitochondrial genome of Juema pig Sus scrofa (Suina: Suidae) from southern Gansu.

Juema pig is a kind of rare and special pig which is well adapted to high altitude, cold climate and harsh natural environment. The complete mitochondrial genome of Juema pig Sus scrofa is a circular molecule of 16 532 bp in length, containing 13 protein-coding genes, two ribosomal RNAs, 22 transfer RNAs, and a control region. The A + T content of the overall base composition of H-strand is 60.7% (T: 26.2%; C: 26.0%; A: 34.5%; G: 13.3%). ND4L gene begins with GTG as start codon, ND2, ND3, and ND5 genes begin with ATA as a start codon, and other nine protein-coding genes start with ATG. Cyt b gene is terminated with AGA as stop codon, ND1 and ND2 genes are terminated with TAG as stop codon, COII, COIII, ND3, and ND4 end with T, while ATP6, ATP8, COI, ND4L, ND5, and ND6 end with TAA. In addition, the phylogenetic relationships from neighbor-joining analyses based on the 13 concatenated PCGs indicated (Tylopoda (Suina (Ruminantia (Hippopotamidae, Cetacea)))).

Kolliphor® HS 15 Micelles for the Delivery of Coenzyme Q10: Preparation, Characterization, and Stability.

To enhance the stability of coenzyme Q10 (CoQ10), Kolliphor® HS 15 (HS15) was employed as a carrier to build up a stable CoQ10-loaded micelle delivery system. The impact of micellar compositions, the preparation condition, and the preparation method on size characteristics, the solubilization efficiency, and micellar stability were investigated. The optimal preparation conditions were 1:6, 4, 0.2%, 118°C, and 25 min for CoQ10/HS15 mass ratio, pH value, the concentration of glucose, and the sterilization conditions. Upon these conditions, the particle size, polydispersity index (PDI), zeta potential, the entrapment efficiency, drug loading, and the critical micelle concentration (CMC) of CoQ10-loaded micelles were 19.76 nm, 0.112, -3.405 mV, 99.39%, 13.77%, and 5.623 × 10(-4) g/mL, respectively. Differential scanning calorimetry (DSC) analysis collectively corroborated that CoQ10 was entrapped into the micelles in amorphous form. The release pattern of drug was analyzed and proved to follow the first order. Additionally, the samples were exposed to the temperatures of 30°C for 6 months with more significant impact on their stabilities as compared to 4 and 25°C based on particle size and PDI. Under constant humidity with light protection long-term (25 ± 2°C, relative humidity (RH) 60 ± 10%, 18 months) conditions, there was no variation except minor changes of CoQ10 content of the samples. The shelf life of the micellar samples could be predicted as 24 months based on the stability results. Consequently, the CoQ10-loaded micelles showed excellent stabilities below 25°C as a potential drug candidate for further clinical applications.

The complete mitochondrial genome of stretch spider Tetragnatha maxillosa (Araneae: Tetragnathidae).

The stretch spider Tetragnatha maxillosa (Araneae: Tetragnathidae) is found all over the world. In the present study, we investigated the complete mitochondrial genome of T. maxillosa and the mitogenome is a circular molecule of 14 414 bp in length, consists of 13 protein-coding genes, two ribosomal RNAs, 22 transfer RNAs, and a control region. The A + T content of the overall base composition of H-strand is 74.5% (T: 40.4%; C: 9.6%; A: 34.1%; G: 15.9%). COI gene begins with TTT as start codon, COII and COIII genes begin with TTG as start codon, ATP8, Cyt b, ND2, and ND4L genes begin with ATT as start codon, and other six protein-coding genes start with ATA. ATP6, ATP8, COI, COIII, ND1, ND3, and ND6 genes are terminated with TAA as stop codon, Cyt b, ND2, ND4, ND4L, and ND5 end with T, and COII ends with TAG. In addition, the phylogenetic relationships from neighbor-joining analyses based on the 13 concatenated PCGs indicated (Tetragnatha (Nephila (Argiope (Araneus, Neoscona)))).

The complete mitochondrial genome of pantropical jumping spider Plexippus paykulli (Araneae: Salticidae).

The complete mitochondrial genome of Plexippus paykulli is a circular molecule of 14,316 bp in length, containing 13 protein-coding genes, 2 ribosomal RNAs, 22 transfer RNAs and a control region. The A + T content of the overall base composition of H-strand is 73.5% (T: 40.6%; C: 9.0%; A: 32.9%; G: 17.5%). ATP6, Cyt b, ND2, ND5 and ND4 genes begin with ATA as start codon; ATP8, ND1, ND3 and ND4L genes begin with ATT as start codon; COII and COIII genes begin with TTG as start codon; COI gene begins with AGA as start codon, while ND6 gene start with a typical ATG initiation codon. ATP6, COI, COII, COIII and ND3 genes are terminated with TAA as stop codon, ND6 ends with TA, ATP8, ND1 and ND2 end with TAG, Cyt b, ND5, ND4 and ND4L end with T.

The complete mitochondrial genome of flat spider Selenops bursarius (Araneae: Selenopidae).

The complete mitochondrial genome of Selenops bursarius is a circular molecule of 14,272 bp in length, containing 13 protein-coding genes, 2 ribosomal RNAs, 22 transfer RNAs and a control region. The A + T content of the overall base composition of H-strand is 74.4% (T: 41.8%; C: 8.7%; A: 32.6%; G: 16.9%). COI gene begins with TTA as start codon; COII gene begins with GTG as start codon; ATP6 and ATP8 genes begin with ATA as start codon; COIII and ND4 genes begin with TTG as start codon; ND1 and ND5 genes begin with ATC as start codon, while other five protein-coding genes start with ATT. ATP6, ATP8, COII, COIII, ND2, ND3, ND4 and ND5 genes are terminated with TAA as stop codon, ND1 ends with TAG, COI ends with TG, Cyt b, ND4L and ND6 end with T.

The complete mitochondrial genome of the writing spider Argiope amoena (Araneae: Araneidae).

The complete mitochondrial genome of Argiope amoena is a circular molecule of 14,121 bp in length, contains 13 protein-coding genes, 2 ribosomal RNAs, 21 transfer RNAs genes and a control region. The A + T content of the overall base composition of H-strand is 72.1% (T: 38.2%; C: 10.6%; A: 33.9%; G: 17.3%). ND1, ND4, ND6 and ATP6 begin with ATA as start codon, ND4L begins with ATG, ATP8, Cyt b, ND2 and ND3 genes begin with ATT, and the other two protein-coding genes begin with TTG. ATP6, ATP8, COI, COII, COIII, Cyt b, ND1, ND2, ND3, ND4L and ND5 genes are terminated with TAA as stop codon, ND6 ends with TAG, and ND4 ends with T.

The complete mitochondrial genome of striped lynx spider Oxyopes sertatus (Araneae: Oxyopidae).

The complete mitochondrial genome of Oxyopes sertatus is a circular molecule of 14,442 bp in length, containing 13 protein-coding genes, 2 ribosomal RNAs, 22 transfer RNAs, and a control region. The A + T content of the overall base composition of H-strand is 75.9% (T: 42.9%; C: 8.2%; A: 33.0%; G: 15.9%). COII, COIII and ND4 genes begin with TTG as start codon; ATP6, COI, ND1 and ND5 genes begin with ATA as start codon, ATP8, Cyt b, ND2 and ND3 genes begin with ATT as start codon, ND6 gene begins with GTG as start codon, while ND4L gene start with a typical ATG initiation codon. ND2 gene is terminated with TAG as stop codon, Cyt b and ND5 end with TA, COI, ND1 and ND4L end with T, ATP6, ATP8, COII, COIII, ND3, ND4 and ND6 end with TAA.

The complete mitochondrial genome of the leopard spider Pardosa laura (Araneae: Lycosidae).

The complete mitochondrial genome of Pardosa laura is a circular molecule of 14,513 bp in length, containing 13 protein-coding genes, 2 ribosomal RNAs, 22 transfer RNAs, and a control region. The A + T content of the overall base composition of H-strand is 77.4% (T: 42.9%; C: 8.1%; A: 34.5%; G: 14.5%). ATP6, COII and COIII genes begin with TTG as start codon; ND4 and ND6 genes begin with ATA as start codon, while other eight protein-coding genes start with ATT. COII, COIII, ND2 and ND6 genes are terminated with TAG as stop codon, COI and ND4L end with T, ND4 ends with TA, ATP6, ATP8, Cyt b, ND1, ND3and ND5 end with TAA.

The complete mitochondrial genome of Chinese pond mussel Sinanodonta woodiana (Unionoida: Unionidae).

The complete mitochondrial genome of Sinanodonta woodiana is a circular molecule of 16256 bp in length, containing 14 protein-coding genes, 2 ribosomal RNAs, 22 transfer RNAs, and 2 control regions. The A + T content of the overall base composition of H-strand is 65.9% (T: 28.0%; C: 22.3%; A: 37.9%; G: 11.8%). F ORF (Female-specific open reading frame) begins with ATA, Cyt b begins with ATC, ATP6, ATP8, COII, COIII, ND1, ND2, ND3 and ND5 begin with ATG, ND4L begins with GTG, COI begins with TTG, and other two protein-coding genes begin with ATT as start codon. COII, COIII, F ORF, ND1, ND3, ND5 and ND6 genes are terminated with TAA as stop codon, ATP6, ATP8, COI, Cyt b, ND4 and ND4L end with TAG, and ND2 gene ends with T.

The complete mitochondrial genome of long-legs spider Pholcus sp. (Araneae: Pholcidae).

The complete mitochondrial genome of Pholcus sp. is a circular molecule of 14,279 bp in length, containing 13 protein-coding genes, 2 ribosomal RNAs, 22 transfer RNAs, and a control region. The A + T content of the overall base composition of H-strand is 65.8% (T: 39.1%; C: 10.7%; A: 26.7%; G: 23.5%). COII and ND2 genes begin with GTG as start codon, COI, ND4L and ND5 genes begin with ATA as start codon, ATP8, ND1 and ND3 genes begins with ATT as start codon, while other five protein-coding genes start with a typical ATG initiation codon. ATP6, ATP8, COIII, ND2, ND4, ND4L and ND6 genes are terminated with TAA as stop codon, COI, Cyt b, ND1 and ND3 end with TAG, while COII and ND5 end with T.

The complete mitochondrial genome of the wasp spider Argiope bruennichi (Araneae: Araneidae).

The complete mitochondrial genome of Argiope bruennichi is a circular molecule of 14,063 bp in length, containing 13 protein-coding genes, 2 ribosomal RNAs, 21 transfer RNAs, and a control region. The A + T content of the overall base composition of H-strand is 73.4% (T: 38.0%; C: 9.8%; A: 35.4%; G: 16.8%). ND6 begins with ATG, ND4 and ATP6 begin with ATA, ND5 and COI begin with TTA, ND1, COII and COIII begin with TTG, and other five protein-coding genes begin with TTG as start codon. ND5, ND4L, ND6, COI, COII, COIII, ATP6 and ATP8 genes are terminated with TAA as stop codon, Cyt b, ND1 and ND2 end with TAG, and other two protein-coding genes end with T.