药学学报最新文献

To study the metabolic products of main compounds of Chuankezhi injection in rat, 12 SpragueDawley rats were classed into 2 groups, a blank control group and an intermuscular administration group,respectively. Rat feces and urine samples were collected from 0−24 h and 24−48 h after administration. Allthe samples were ultrasonically treated with methanol and then analyzed using LC-LTQ Orbitrap MSn. Bycomparison with the total ion chromatogram of samples from the blank control group, the metabolites in thesamples of drug-treated group were screened. These metabolites were further analyzed by multistage production scanning and comparison of retention time with reference substances. As a result, a total of 12 flavonoidmetabolites were tentatively identified from the rat feces and no metabolite was discovered in the rat urine.Epimedin C and icariin were detected in the rat blood samples after 30 min of administration, but theirmetabolites and other original flavones were not detected. Furthermore, no original flavones and theirmetabolites were detected in rat blood samples after 2 and 4 h of administration. The potential metabolismpaths were further characterized and the principal in vivo transformation of flavones from Chuankezhi injectionwere deglycosylation, dehydration, methylation, oxidation and isomerization in rats.

Our research was designed for on-line detection of multi-index in the concentration process ofGanmaoling granules by integration of near infrared spectroscopy and automatic control system. First, on-linedetection system was set up in the concentration tank for Ganmaoling granules production. Spectra werescanned and values of chlorogenic acid, linarin, solid content and relative density were measured. Modelsof partial least squares regression were built and imported into near infrared workstation. By connectingthe control system, real-time multi-index values were determined automatically in the concentration process.Results showed that correlation coefficients of chlorogenic acid, linarin, solid content and relative density modelswere 0.963, 0.989, 0.993 and 0.918, respectively. Relative standard errors of prediction were 3.71%, 4.28%,4.17% and 0.24%, respectively, indicating a good performance and high accuracy of the models. Real-time datacollection during the whole process was measured by the near infrared detecting system in the control system.In conclusion, the near infrared detection system is able to perform real-time automatic determination of multiindexin the concentration process of Ganmaoling granules with significant advantages.

In this study, a novel brain-targeting carrier was made via conformational epitope imprinting.Acrylamide and N,N '-methylene bisacrylamide was used as carrier materials and the N-terminal epitope ofnicotinic acetylcholine receptor α7 (nAchR α7) was tested as a template molecule, and the polymer nanoparticleswere obtained after polymerization and template removal. The nanoparticles were investigated by particle sizeanalyzer and transmission electron microscopy (TEM). Their targeting capabilities were investigated with a celluptake assay in vitro and fluorescence imaging in vivo. The results suggest that the nanoparticles had a smallparticle size (42.1 ± 4.3 nm) with a homogeneous distribution, and good targeting properties in vitro and in vivo.We have made the molecularly imprinted polymer nanoparticles with brain targeting capability, which representsa new tool in the treatment of brain diseases.

The study aims to investigate the effective components of Semen Ziziphi Spinosae (SZR) innourishing the heart and tranquilizing the mind. A method of ultra high liquid chromatography (UHPLC)coupled with Q Exactive high resolution mass spectrometry (HR-MS) was developed. Based on the UV spectra,retention time and MS spectra, 25 compounds of SZR extract were identified or tentatively characterized,including 12 flavonoids, 8 triterpenoids saponins, 2 fatty acid and 3 alakoids. The study illuminated the majorchemical components. Twenty bioactive components were determined in rat urine after oral administration ofSZR extract by “in vitro to in vivo” translation approach, including 16 prototype compounds and 4 metabolites.Spinosin, swertisin, jujuboside A and B were considered as the effective and active constituents in SZR ofthe sedative and hypnotic effects, which emodies characteristics of multiple components. It was beneficialexploration for searching the effective and active constituents of SZR in nourishing the heart and tranquilizingthe mind.

A type Ⅱ ribosome inactivating protein (RIP) gene was cloned from Polyporus umbellatussclerotia by RT-PCR method. The full open reading frame cDNA sequence of this gene was 873 bp in lengthand encoded a 290-aa protein with a molecular weight of 32.33 kDa and an isoelectric point of 5.58. Multiplesequence alignment revealed that the deduced amino acids possessed conserved domains of RICIN superfamilyprotein. A neighbor joining phylogenetic analysis suggests that PuRIP was closely related to RIP in Marasmiusoreades. Real time PCR results showed that this gene expressed in all tested tissues of P. umbellatus. Meanwhile,the expression of this gene was significantly up-regulated in the part infected by Armillaria mellea. This resultsuggested that this PuRIP might played important role with potential biotic stress tolerance of P. umbellatus.Otherwise, we successfully constructed the pET15b-PuRIP plasmid, produced and purified the His-PuRIP fusionprotein, which would provide the basic material for polyclonal antibody preparation and gene function research.

Bile acids play critical roles in the regulation of metabolism and absorption of lipids. The ilealapical sodium-dependent bile acid transporter (ASBT) located at the enterocyte brush border is responsible forthe reuptake of bile acids and the maintenance of bile acid homeostasis. Recently, a number of investigationshave been made concerning the regulation and control of ASBT and the relationship between ASBT and intestinalinflammation, tumorigenesis, diabetes mellitus and hyperlipemia, which suggests ASBT as a potential therapeutictarget of these diseases. In this review, advances in the study of above-mentioned issues were summarized.

Daphnetin is quickly eliminated in rats after dosing, but the mechanism remains unclear. Thisstudy was aimed to investigate the in vitro metabolism of daphnetin using rat liver S9 fractions (RLS9). Themetabolites formed in RLS9 were identified and the kinetic parameters for different metabolic pathwayswere determined. HPLC-DAD-MS analysis showed that daphnetin was biotransformed to six metabolites,which were identified as 7 or 8 mono-glucuronide and mono-sulfate, 8-methylate, and 7-suflo-8-methylate.Methylation and glucuronidation of daphnetin exhibited the Michaelis-Menten kinetic characteristics, whereasthe substrate inhibition kinetic and the two-site kinetic were observed for 8-sulfate and 7-sulfate formations. Ofthe 3 conjugation pathways, the intrinsic clearance rate for sulfation was highest, followed by methylation andglucuronidation. By in vitro-in vivo extrapolation of the kinetic data measured in RLS9, the hepatic clearancewere estimated to be 54.9 mL·min−1·kg−1 which is comparable to the system clearance (58.5 mL·min−1·kg−1)observed in rats. In conclusions, the liver might be the main site for daphnetin metabolism in rats. Sulfation,methylation and glucuronidation are important pathways of the hepatic metabolism of daphnetin in rats.

The binding of rhaponticin to bovine serum albumin (BSA)-bovine lactoferrin (BLF) and thefactors that affect BSA-BLF interaction have been studied by fluorescence spectroscopy and Fourier transforminfrared spectroscopy. In the fluorescence experiment, RT quenched the fluorescence intensity of mixedproteome and the maximum emission wavelength of BSA, BLF and BSA-BLF proteins system. RT causedobvious red-shift fluorescence for an interaction between RT and proteome. The interaction between RT andproteome was impacted by single-component protein molecular interactions and the interaction between RT-BSAand RT-BLF, the microenvironment of solutions were the factors impacting the interactions between RT andproteome, which impacted quantitative expression of the general environment micro environmental factors.In the Fourier transform infrared spectroscopy, the secondary conformation of protein molecules of singlecomponent in the protein group were changed, and the difference of the molecules ’ structure was responsible forthe differences in the molecular conformation changes. The molecules ’ interaction in the single-componentprotein affected secondary conformation of the proteins’ molecule. The proteins’ concentration ratio and theinteraction were different in degree of molecular conformational change. These data demonstrates an exampleof combination of fluorescence spectrum experiment with Fourier transform infrared spectroscopy in the study ofprotein structura.

Puerarin (PUE), an isoflavone with anti-inflammation, anti-oxidation and neuroprotection effects,has been widely applied to the treatment of cardiovascular diseases in clinics in China. In the current study, wereported that the active pharmaceutical ingredient (API) of marketed products was the PUE monohydrate(PUEMH). During its supersaturated dissolution, the PUE concentration quickly reached a plateau, followed bya gradually concentration decrease to another lower plateau. In order to explore the internal mechanism of abovephenomenon, the solid residues after saturated dissolution test were characterized by powder X-ray diffraction(PXRD), thermal gravity analysis (TGA) and Karl Fisher titration (KFT). PXRD suggested that a novel PUEcrystal different from PUEMH formed during its dissolution, the following TGA and KFT confirmed the generationof PUE dihydrate (PUEDH) with much lower solubility. Moreover, polyvinylpyrrolidones (PVPK12, PVPK30and PVPK90) were added in the dissolution medium to investigate their potential inhibition effects on suchcrystal transformation during dissolution process. We observed that polymers could inhibit the transformationfrom PUEMH to PUEDH and result in much higher PUE concentration level than that in pure water.

Licorice is one of the most common herbs in traditional Chinese medicine, and classified as topgrade in Shen Nong Ben Cao Jing. There are three different original plants of licorice stipulated in ChinesePharmacopeia, Glycyrrhiza uralensis Fisch., Glycyrrhiza glabra L., and Glycyrrhiza inflata Bat. However,previous investigation showed that the pharmacodynamic effects of the three licorices were quite different. It isvery difficult to identify them by the classical identification methods. In order to establish a fast and effectiveidentification method, we collected 240 licorice plants from 21 populations of 7 provinces, and amplified theirITS and psbA-trnH sequences. ITS sequences with a full length of 616 bp and psbA-trnH sequences with a fulllength of 389 bp were obtained separately. Using DNAMAN to analyze these sequences, 4 variable sites werefound in ITS sequences and 2 ITS haplotypes were determined, and 3 variable sites were found in psbA-trnHsequences and 4 psbA-trnH haplotypes were determined. With the combination analysis of ITS and psbA-trnHsequences, the molecular identification method of original licorice was established. Using this method, 40samples of licorice slices collected from 4 main herbal material markets in China were identified successfully.Furthermore, the contents of 2 triterpenes, 18α-glycyrrhizic acid and 18β-glycyrrhizic acid, and 4 flavonoids,liquiritin, isoliquiritin, liquiritigenin, and isoliquiritigenin in these licorice pieces were examined by HPLC andthe results were analyzed using SPSS 21.0. This study provides a new method in identification of licorice,which may serve as a guideline for quality control of licorice slices.