A novel drug-drug coamorphous system without molecular interactions: improve the physicochemical properties of tadalafil and repaglinide.

Tadalafil and repaglinide, categorized as BCS class II drugs, have low oral bioavailabilities due to their poorly aqueous solubilities and dissolutions. The aim of this study was to enhance the dissolution of tadalafil and repaglinide by co-amorphization technology and evaluate the storage and compression stability of such coamorphous system. Based on Flory-Huggins interaction parameter ( ≤ 0) and Hansen solubility parameter ( ≤ 7 MPa) calculations, tadalafil and repaglinide was predicted to be well miscible with each other.

[Drug syndrome of ephedra based on its property and pharmacology].

Ephedra is a classic herb in traditional Chinese medicine( TCM). The new effects of ephedra were gradually found,and the contraindications of the drug were broken in later ages. Because the principles of expanded application were not well elucidated,it is difficult to use in the clinical flexibility.

A carbon-rich nanofiber framework based on a conjugated arylacetylene polymer for photocathodic enzymatic bioanalysis.

Poly(1,3,5-triethynylbenzene) (PTEB), a newly developed conjugated arylacetylene polymer, was utilized for photoelectrochemical (PEC) enzymatic bioanalysis in this work. The porous nanofiber framework of PTEB film which produced an apparent cathodic photocurrent under visible light illumination was fabricated on an indium tin oxide (ITO) electrode copper-surface mediated interface Glaser polycondensation. As the photocurrent density of the metal-free photocathode displayed a characteristic O dependency, the consumption of dissolved oxygen caused by the modified glucose oxidase (GOx) in biocatalysis induced a depressed photoresponse in the presence of glucose.

[Screening for active components of Sophorae Flos on inhibiting AGEs formation based on non-enzymatic glycation reaction].

Sugar-poison caused blood-heat is the pathological basis of many complications of diabetes. Advanced glycation end products( AGEs) are considered as the potential glycotoxic factor that can cause blood-heat. Sophorae Flos hold the effect of removing pathogenic heat from blood.

Probiotics Ameliorate Colon Epithelial Injury Induced by Ambient Ultrafine Particles Exposure.

Diesel exhaust particles (DEPs) are common airborne ultrafine particles (UFPs); however, few studies have examined their effects on the gastrointestinal tract. To investigate the interaction of gut microbiota and DEPs-induced colonic injury, adult C57BL/6 mice are kept in whole-body inhalation chambers and exposed to filtered room air (FRA) or DEPs (300 µg m) 1 h per day for 28 consecutive days. DEPs exposure results in colon epithelial injury with inflammatory cell infiltration and mucus depletion.

[A new phenolic glycoside from honey-fried Eriobotrya japonica].

A total of twelve compounds were isolated from the ethyl acetate of the water extract of honey-fried Eriobotrya japonica through column chromatography over silica gel,Sephadex LH-20,RP-18,and preparative HPLC. Their structures were established by MS,1 D NMR and 2 D NMR data as japonicanoside A( 1),nerolidol-3-O-α-L-rhamnopyranosyl-( 1→2)-β-D-glucopyranoside( 2),nerolidol-3-O-α-L-rhamnopyranosyl-( l→4)-α-L-rhamnopyranosyl-( 1 → 2)-[α-L-( 4-trans-feruloyl)-rhamnopyranosyl-( 1 → 6) ]-β-D-glucopyranoside( 3),( +)-catechin( 4),(-)-epicatechin( 5),kaempferol 3-O-α-L-rhamnopyranoside( 6),quercitrin( 7),quercetin-3-O-β-D-galactopyranoside( 8),quercetin-3-O-β-glucopyranoside( 9),vanillin( 10),protocatechuic aldehyde( 11),and maltol( 12). Among them,1 is a new phenolic glycoside.

Mannose-Modified Multi-Walled Carbon Nanotubes as a Delivery Nanovector Optimizing the Antigen Presentation of Dendritic Cells.

Dendritic cells (DCs) based cancer immunotherapy is largely dependent on adequate antigen delivery and efficient induction of DCs maturation to produce sufficient antigen presentation and ultimately lead to substantial activation of tumor-specific CD8 T cells. Carbon nanotubes (CNTs) have attracted great attention in biomedicine because of their unique physicochemical properties. In order to effectively deliver tumor antigens to DCs and trigger a strong anti-tumor immune response, herein, a specific DCs target delivery system was assembled by using multi-walled carbon nanotubes modified with mannose which can specifically bind to the mannose receptor on DCs membrane.

Solvent-dependent regio- and stereo-selective reactions of 3-formylchromones with 2-aminobenzothiazoles and transacetalization efficiency of the product 3-((benzo[]thiazol-2-ylimino)butyl)-4-chromen-4-one.

Using 2-propanol as the solvent, 3-formylchromones and 2-aminobenzothiaoles formed corresponding imines, while 1° and 2°-alcohols formed the corresponding 2-alkoxy-3-enamines with selectivity for the -isomer. Changing the substrates with similar molecules such as 3-formylchromone with quinoline-, quinolone- and indole-3-carbaldehydes sometimes resulted in the formation of the corresponding imines, whereas replacing 2-aminobenzothiazole with amides resulted in the formation of acetals. Considering the effect of the solvent, replacing alcohols with the aprotic solvents THF and CHCl resulted in the formation of imines and enamines, which are the characteristic reactions of 2-propanol and other 1° and 2°-alcohols, respectively.

Sodium tanshinone IIA silate increases melanin synthesis by activating the MAPK and PKA pathways and protects melanocytes from HO-induced oxidative stress.

Vitiligo is an intriguing depigmentation disorder that affects about 0.5-2% of the world population. In the past decade, first-line treatments of vitiligo have involved the use of calcineurin inhibitors and corticosteroids.

Colonic Injuries Induced by Inhalational Exposure to Particulate-Matter Air Pollution.

Particulate matter (PM) exposure has been associated with intestinal disorders. Therefore, there is an urgent need to understand the precise molecular mechanism involved and explore potential prevention strategies. In this study, inhaled PM is shown to activate inflammatory pathways in murine colon.

Antibiotic removal by agricultural waste biochars with different forms of iron oxide.

Pollution by antibiotics has become a serious threat to public health. In this study, agricultural waste, corn husk, in the form of biochar, was utilized for antibiotic removal from wastewater. Two kinds of iron-loaded biochars, impregnation-pyrolysis biochar (IP) and pyrolysis-impregnation biochar (PI), were synthesized to adsorb the typical antibiotics tetracycline (TC) and levofloxacin (LEV).

The magnetism of 1T-MX (M = Zr, Hf; X = S, Se) monolayers by hole doping.

The magnetism of hole doped 1T-MX (M = Zr, Hf; X = S, Se) monolayers is systematically studied by using first principles density functional calculations. The pristine 1T-MX monolayers are semiconductors with nonmagnetic ground states, which can be transformed to ferromagnetic states by the approach of hole doping. For the unstrained monolayers, the spontaneous magnetization appears once above the critical hole density (10 cm), where the p orbital of S or Se atoms contributes the most of the magnetic moment.

[Mining and discovery for active components of "Coptidis Rhizome-Magnoliae Officinalis Cortex" based on network pharmacology].

To mine and discover the active components of " Coptidis Rhizome-Magnoliae Officinalis Cortex( C&M) " based on the network pharmacology,integrate and analyze the potential targets and mechanisms. The TCMSP database was used to screen active ingredients. TTD and Drug Bank databases were used to predict the potential targets by referring to relevant literature,and the pathway annotation technology was used to enrich and analyze the active ingredients and potential targets of " C&M".

[Evaluation of scavenging activity of hydrogen peroxide in different origins of Liropes Radix by HPLC-UV-CL system].

The hydrogen peroxide generation system was used to analyze the scavenging activity of hydrogen peroxide by Liropes Radix from different origins by HPLC-UV-CL. The UV-CL fingerprints of Liropes Radix from different origins were evaluated,and the HPLC-UV and LC-CL fingerprints were systematically analyzed and evaluated. The results showed that the ether fractions of Liriope spicata var.

A novel analytical method based on HPLC-PDA coupled post-column derivatization to evaluate the ability to inhibit tyrosine nitration in lotus leaf extracts.

Protein tyrosine nitration plays a key role in many inflammatory and cardiovascular diseases and diabetes. Many natural products are used to treat these diseases through their ability to potentially interfere this reaction. Here, we describe a novel method to provide active fingerprinting of inhibition of tyrosine nitration by natural products based on post-column tyrosine nitration reaction analysis using high-performance liquid chromatography coupled to a photometric diode array.

A galactose-mediated targeting nanoprobe for intracellular hydroxyl radical imaging to predict drug-induced liver injury.

Drug-induced liver injury (DILI) is a serious concern in modern medicine due to its unpredictability. Currently, biochemical serum markers are being used in DILI detection. However, these biomarker-based methods lack sensitivity and specificity.

Three new cardiac glycosides obtained from the roots of Lour. and their cytotoxic and melanogenesis-inhibitory activities.

Three new cardiac glycosides strophanthidin-3--α-l-rhamnopyranosyl-(1→4)-6-deoxy-βd-allopyranoside (1), 5β-16β-acetylkamaloside (2), and mansonin-19-carboxylic acid (3) along with seven known steroids including five cardiac glycosides were isolated from the methanol extracts of Lour. roots. The structures of these compounds were established by spectroscopic analyses.

Novel steroidal saponins with cytotoxic activities from the roots of (L. f.) Ker-Gawl.

Six new steroidal saponins (1-6) and one known steroidal saponin (7) were obtained from the roots of (L. f.) Ker-Gawl.

Physiologically stable F127-GO supramolecular hydrogel with sustained drug release characteristic for chemotherapy and photothermal therapy.

A synthetic method for preparing a Pluronic F127 (F127)-stabilized graphene (GO) supramolecular hydrogel as a safe nanovehicle for combination treatment has been studied. Doxorubicin (DOX) as a model drug is non-covalently bound on the great surface area of GO due to strong π-π interaction, hydrophobic interaction, and the strongest hydrogen bonding. drug release experiments revealed that this F127-stabilized GO supramolecular hydrogel has a sustained drug release characteristic.