Chemosensitizing effect and mechanism of imperatorin on the anti-tumor activity of doxorubicin in tumor cells and transplantation tumor model.

Multidrug resistance of tumors has been a severe obstacle to the success of cancer chemotherapy. The study wants to investigate the reversal effects of imperatorin (IMP) on doxorubicin (DOX) resistance in K562/DOX leukemia cells, A2780/Taxol cells and in NOD/SCID mice, to explore the possible molecular mechanisms. K562/DOX and A2780/Taxol cells were treated with various concentrations of DOX and Taol with or without different concentrations of IMP, respectively.

[Co-amorphous technology to improve dissolution and physical stability of silybin].

The present study explored the effect of co-amorphous technology in improving the dissolution rate and stability of silybin based on the puerarin-silybin co-amorphous system prepared by the spray-drying method. Solid-state characterization was carried out by powder X-ray diffraction(PXRD), polarizing microscopy(PLM), Fourier transform infrared spectroscopy(FT-IR), differential scanning calorimetry(DSC), etc. Saturated powder dissolution, intrinsic dissolution rate, moisture absorption, and stability were further investigated.

Nrf2 expands the intracellular pool of the chaperone AHSP in a cellular model of β-thalassemia.

In β-thalassemia, free α-globin chains are unstable and tend to aggregate or degrade, releasing toxic heme, porphyrins and iron, which produce reactive oxygen species (ROS). α-Hemoglobin-stabilizing protein (AHSP) is a potential modifier of β-thalassemia due to its ability to escort free α-globin and inhibit the cellular production of ROS. The influence of AHSP on the redox equilibrium raises the question of whether AHSP expression is regulated by components of ROS signaling pathways and/or canonical redox proteins.

Improvement of the bioavailability of curcumin by a supersaturatable self nanoemulsifying drug delivery system with incorporation of a hydrophilic polymer: in vitro and in vivo characterisation.

Objectives: The current study was focused on preparing curcumin (CUR) supersaturated self-nano-emulsion (PI-CUR-SNEDDS) using hydrophilic polymer and to study the influence of polymer precipitation inhibitor on the physicochemical and biopharmaceutical properties of the PI-CUR-SNEDDS.

Methods: PI-CUR-SNEDDS were prepared using hydrophilic polymer in order to maintain the supersaturation of CUR in nano-emulsion solution, artificial gastrointestinal fluid (AGF), and the precipitates formed, and characterised by in vitro dispersion tests, in vitro intestinal absorption and in vivo pharmacokinetic and compared with CUR-SNEDDS.

Key Findings: PI-CUR-SNEDDS prepared with 2% hydroxypropyl methylcellulose 55-60 (HPMC55-60) as precipitation inhibitor (PI) significantly improved the viscosity, physical stability and CUR's equilibrium solubility of nanoemulsion.

Reversal Effect of Oxypeucedanin on P-glycoprotein-mediated Drug Transport.

P-glycoprotein affects the transport of numerous drugs including chemotherapeutic drugs vincristine sulfate (VCR) and docetaxel (DTX), and is one of the main causes for multidrug resistance. Our previous studies have shown that oxypeucedanin (OPD) can enhance the intestinal transit of puerarin and VCR. However, the underlying mechanism is unclear.

[Effect investigation of coumarin constituents in Angelica dahurica on pharmacokinetics of docetaxel by LC-MS].

The study was aimed to establish a liquid chromatography-tandem mass spectrometric method for the determination of the docetaxel concentration in rat plasma, and study the effect of coumarin constituents (imperatorin, isoimperatorin and oxypeucedanin) in Angelica dahurica on pharmacokinetics of docetaxel.Plasma was precipitated with acetonitrile and determined by LC-MS method with Paclitaxel as an internal standard. The specificity, linearity, range, accuracy, precision and stability of the method were suitable for the determination of docetaxel in plasma.

[Key physical parameters of hawthorn leaf granules by stepwise regression analysis method].

The purpose of this study was to investigate the effect of key physical properties of hawthorn leaf granule on its dissolution behavior. Hawthorn leaves extract was utilized as a model drug. The extract was mixed with microcrystalline cellulose or starch with the same ratio by using different methods.

[Correlation between four properties of traditional Chinese medicine and function of reversing multidrug resistance of tumor cells].

To study the correlation of four properties of traditional Chinese medicine and the function of reversing multidrug resistance (MDR) of tumor cells, with 580 herbs in Chinese Pharmacopoeia 2015 version as the research objects. CNKI, CBA, Wanfang, VIP, and PubMed were searched to screen the documents related to the reversal of MDR for collection, summarizing and analysis. The results of the research showed that a total of 114 species Chinese herbs had been reported to be associated with reversal of MDR in tumor cells.

Improvement of Transmembrane Transport Mechanism Study of Imperatorin on P-Glycoprotein-Mediated Drug Transport.

P-glycoprotein (P-gp) affects the transport of many drugs; including puerarin and vincristine. Our previous study demonstrated that imperatorin increased the intestinal absorption of puerarin and vincristine by inhibiting P-gp-mediated drug efflux. However; the underlying mechanism was not known.

[Improvement of powder flowability and hygroscopicity of traditional Chinese medicine extract by surface coating modification technology].

To study the improvement of powder flowability and hygroscopicity of traditional Chinese medicine extract by surface coating modification technology. The 1% hydrophobic silica nanoparticles were used as surface modifier, and andrographis extract powder was taken as a model drug. Three different techniques were used for coating model drugs, with angle of repose, compressibility, flat angle and cohesion as the comprehensive evaluation indexes for the powder flowability.

Quantitative Evaluation of the Mechanism Underlying the Biotransportation of the Active Ingredients in Puerariae lobatae Radix and Chuanxiong rhizoma.

The objective of this study was to establish a quantitative method to evaluate the biotransportation of a drug across the cell membrane. Through the application of the law of mass conservation, the drug transportation rate was calculated based on Fick's law of passive diffusion and the Michaelis-Menten equation. The overall membrane-transportation rate was the sum of the passive diffusion rate and the carrier-mediated diffusion rate, which were calculated as the transportation mass divided by the respective rate.

[Correlations between micromeritic properties of mixing powders of danshen extract and formability of their pellets].

It was difficult to prepare traditional Chinese medicine pellets due to the adverse characteristics of the herbal extract. In this study, Danshen extract (DS) powder mixed with different proportions of microcrystalline cellulose (MCC), lactose and starch were made into pellets by extrusion-spheronization. Particle size, span, bulk density, tapping density, compressibility, Hausner ratio and angle of repose were used to evaluate the micromeritic properties of mixing powders.

Mechanisms of improvement of intestinal transport of baicalin and puerarin by extracts of Radix Angelicae Dahuricae.

Radix Angelicae Dahuricae is the dried root of Angelicae Dahurica (Fisch.ex Hoffm.)Benth.

A new flavonol C-glycoside and a rare bioactive lignanamide from Piper wallichii Miq. Hand.-Mazz.

This study was conducted to investigate the chemical constituents of Piper wallichii (Miq.) Hand.-Mazz.

Transport properties of puerarin and effect of extract of Radix Angelicae dahuricae on puerarin intestinal absorption using in situ and in vitro models.

The root of Angelica dahurica (Radix Angelicae Dahuricae, RAD), which contains coumarins and volatile oil as its main classes of active components, is often given in conjunction with Pueraria root (Radix Puerariae, RP), which contains the phytoestrogen puerarin. The two herbs are considered to be compatible 'herb-pairs' in traditional Chinese medicine. The present investigation investigates the absorption of puerarin from RP and the effect of the total coumarins and volatile oil from RAD on its absorption.

Activation of STAT3 stimulates AHSP expression in K562 cells.

Studies on the chaperone protein α-hemoglobin stabilizing protein (AHSP) reveal that abundant AHSP in erythroid cells enhance the cells' tolerance to oxidative stress imposed by excess α-hemoglobin in pathological conditions. However, the potential intracellular modulation of AHSP expression itself in response to oxidative stress is still unknown. The present study examined the effect and molecular mechanism of STAT3, an oxidative regulator, on the expression of AHSP.

Elucidation of the transport mechanism of baicalin and the influence of a Radix Angelicae Dahuricae extract on the absorption of baicalin in a Caco-2 cell monolayer model.

Ethnopharmacological Relevance: Angelicae Dahurica (Hoffm.) Benth. & Hook.

Lysine-specific demethylase 1 represses THP-1 monocyte-to-macrophage differentiation.

Objective: To investigate the role of lysine-specific demethylase 1 (LSD1) in the process of THP-1 monocyte-to-macrophage differentiation.

Methods: Quantitative reverse transcription-polymerase chain reaction (qRT-PCR) and Western blotting were performed to analyze the expression of LSD1 and interleukin-6 (IL-6) in THP-1 monocytes and THP-1-derived macrophages. Chromatin immunoprecipitation (ChIP) assay was applied to detect the occupancy of LSD1 and H3K4 methylation at IL-6 promoter during THP-1 monocyte-to-macrophage differentiation.

miR-451 regulates dendritic cell cytokine responses to influenza infection.

MicroRNAs (miRNAs) are important posttranscriptional regulators in immune cells, but how viral infection regulates miRNA expression to shape dendritic cell (DC) responses has not been well characterized. We identified 20 miRNAs that were differentially expressed in primary murine DCs in response to the dsRNA agonist polyinosinic-polycytidylic acid, a subset of which were modestly regulated by influenza infection. miR-451 was unique because it was induced more strongly in primary splenic and lung DCs by live viral infection than by purified agonists of pattern recognition receptors.

Transport properties of puerarin and effect of Radix Angelicae Dahuricae extract on the transport of puerarin in Caco-2 cell model.

Ethnopharmacological Relevance: Angelicae Dahurica (Hoffm.)Benth.& Hook.

Mitofilin regulates cytochrome c release during apoptosis by controlling mitochondrial cristae remodeling.

Mitochondria amplify caspase-dependent apoptosis by releasing proapoptotic proteins, especially cytochrome c. This process is accompanied by mitochondrial cristae remodeling. Our studies demonstrated that mitofilin, a mitochondrial inner membrane protein, acted as a cristae controller to regulate cytochrome c release during apoptosis.