Kurarinol induces hepatocellular carcinoma cell apoptosis through suppressing cellular signal transducer and activator of transcription 3 signaling.

Kurarinol is a flavonoid isolated from roots of the medical plant Sophora flavescens. However, its cytotoxic activity against hepatocellular carcinoma (HCC) cells and toxic effects on mammalians remain largely unexplored. Here, the pro-apoptotic activities of kurarinol on HCC cells and its toxic impacts on tumor-bearing mice were evaluated. The molecular mechanisms underlying kurarinol-induced HCC cell apoptosis were also investigated. We found that kurarinol dose-dependently provoked HepG2, Huh-7 and H22 HCC cell apoptosis. In addition, kurarinol gave rise to a considerable decrease in the transcriptional activity of signal transducer and activator of transcription 3 (STAT3) in HCC cells. Suppression of STAT3 signaling is involved in kurarinol-induced HCC cell apoptosis. In vivo studies showed that kurarinol injection substantially induced transplanted H22 cell apoptosis with low toxic impacts on tumor-bearing mice. Similarly, the transcriptional activity of STAT3 in transplanted tumor tissues was significantly suppressed after kurarinol treatment. Collectively, our current research demonstrated that kurarinol has the capacity of inducing HCC cell apoptosis both in vitro and in vivo with undetectable toxic impacts on the host. Suppressing STAT3 signaling is implicated in kurarinol-mediated HCC cell apoptosis.

Docking Design of the Different Microcapsules in Aqueous Solution and Its Quantitative On-Off Study.

To avoid risk, spacecraft docking technologies can transport batches of different astronauts or cargoes to a space station. Before now, spacecraft-docking multicarrier/multidrug delivery systems have not been reported on. Herein, inspired by spacecraft docking technology, a novel system including two different docking units, one made of polyamide (PAAM) and on of polyacrylic acid (PAAC), grafted respectively onto polyethersulfone (PES) microcapsules, is designed, based on intermolecular hydrogen bonds in aqueous solution. VB12 and vancomycin hydrochloride were chosen as the release drugs. The release results show that the docking system is perfect, and has a good responsiveness to temperature when the grafting ratio of PES-g-PAAM and PES-g-PAAC is close to 1:1. Below 25 °C, this system exhibited an "off" effect because the polymer chains on the microcapsule's surface produced intermolecular hydrogen bonds. Above 25 °C, when the hydrogen bonds were broken, the microcapsules separated from each other, and the system exhibited an "on" state. The results provide valuable guidance for improving the feasibility of multicarrier/multidrug delivery systems.

Controllable Fabrication and Oil-Water Separation Properties of Polyethylene Terephthaloyl-Ethylenediamine-IPN-poly(N-Isopropylacrylamide) Microcapsules.

In this paper, we report a microcapsule embedded PNIPAN in P (TPC-EDA) shell and it can be regarded as an interpenetrating polymer network (IPN) structure, which can accelerate the penetration of oily substances at a certain temperature, and the microcapsules are highly monodisperse and dimensionally reproducible. The proposed microcapsules were fabricated in a three-step process. The first step was the optimization of the conditions for preparing oil in water emulsions by microfluidic device. In the second step, monodisperse polyethylene terephthaloyl-ethylenediamine (P(TPC-EDA)) microcapsules were prepared by interfacial polymerization. In the third step, the final microcapsules with poly(N-isopropylacrylamide) (PNIPAM)-based interpenetrating polymer network (IPN) structure in P(TPC-EDA) shells were finished by free radical polymerization. We conducted careful data analysis on the size of the emulsion prepared by microfluidic technology and used a very intuitive functional relationship to show the production characteristics of microfluidics, which is rarely seen in other literatures. The results show that when the IPN-structured system swelled for 6 h, the adsorption capacity of kerosene was the largest, which was promising for water-oil separation or extraction and separation of hydrophobic drugs. Because we used microfluidic technology, the products obtained have good monodispersity and are expected to be produced in large quantities in industry.

Anti-inflammatory and blood stasis activities of essential oil extracted from Artemisia argyi leaf in animals.

Artemisia argyi leaf is a well-known species in traditional Chinese medicine. However, the anti-inflammatory and activating blood stasis activities of its essential oil (AAEO) have not been explored in vivo. The present study measured the contents of three chemical components by gas chromatography (GC). The anti-acute inflammatory effects of AAEO were investigated in dimethyl benzene, glacial acetic acid and carrageenan-induced animals through skin administration or by oral gavage, respectively. The effects of AAEO on haemorheology were studied in a rat acute blood stasis model. The contents of eucalyptol, camphor and borneol in AAEO were 254.4, 51.6 and 58.7 mg/g, respectively. All dosages of AAEO by skin administration significantly decreased the swelling in dimethyl benzene-induced ear oedema and carrageenan-induced paw oedema, and reduced the permeability in glacial acetic acid-induced abdominal blood capillary (p < 0.01). Meanwhile, haemorheology indexes such as whole blood viscosity and the erythrocyte aggregation index significantly decreased only in the high dosage group. In addition, the effects of AAEO by oral gavage were weaker than skin administration at the medium dose in the experiments. It suggests that AAEO has better absorption bioavailability and pharmacological effects through skin administration due to the better skin permeability of essential oil than gastrointestinal absorption.

Chemical composition of total flavonoids from Polygonum amplexicaule and their pro-apoptotic effect on hepatocellular carcinoma cells: Potential roles of suppressing STAT3 signaling.

Polygonum amplexicaule D. Don var. sinense Forb (P. amplexicaule) is a medical plant traditionally used in the treatment of malignant diseases including hepatocellular carcinoma (HCC), but the scientific basis underlying its anti-HCC activity remains poorly understood. Here, we explored the chemical profile of total flavonoids from P. amplexicaule (TFPA). Nine compounds that constituted the major components of TFPA were separated and identified. Further investigations revealed that TFPA dose-dependently induced HepG2, Huh-7 and H22 HCC cell apoptosis. In HCC cells, TFPA dramatically inhibited the transcriptional activity of signal transducer and activator of transcription 3 (STAT3). In addition, TFPA increased the expression of SHP-1, a protein tyrosine phosphatase catalyzing STAT3 dephosphorylation, in HCC cells. Animal studies showed that TFPA considerably provoked transplanted H22 cell apoptosis with undetectable toxicological effects on tumor-bearing mice. Consistently, TFPA dose-dependently inhibited transcriptional activity of STAT3 in transplanted tumor tissues. This study collectively demonstrated that TFPA has the capacity of inducing HCC cell apoptosis both in vitro and in vivo with low toxic effects on normal hepatocytes and vital organs of tumor-bearing mice. Suppressing STAT3 signaling is implicated in TFPA-mediated HCC cell apoptosis.

Selenium-dependent antitumor immunomodulating activity of polysaccharides from roots of A. membranaceus.

Roots of Astragalus membranaceus (Fish.) Bge. var. mongholicus (Bge.) Hsiao (A. membranaceus) have been long used as an auxiliary reagent supporting cancer treatment. Here, we compared the chemical composition and antitumor immunomodulating activity of polysaccharides from roots of A. membranaceus (PAMs) from five major habitats in Inner Mongolia, PR China. We revealed that compositions of monosaccharides and amino acids were comparable among PAMs from different habitats. However, amounts of selenium varied widely in roots of A. membranaceus and PAMs. PAMs selenium-dependently repressed the in vivo proliferation of transplanted H22 ascitic hepatoma and S180 sarcoma cells with low toxic impacts on tumor-bearing mice. Selenium-containing PAMs ameliorated host CD4+ T cell apoptosis and serum cytokine dysregulation induced by tumor transplantation, leading to the enhancement of cytotoxic activities of natural killer and CD8+ T cells. Moreover, PAMs also selenium-dependently improved the phagocytotic function of intra-abdominal macrophages and suppressed M2-like polarization of tumor-associated macrophages. These data suggested that the selenium content varies in the roots of A. membranaceus and PAMs from different geographical origins dramatically and selenium is an important contributor to the antitumor immunomodulation activities of PAMs.

[Study on moxa sticks burning temperature-time-space curves].

OBJECTIVE: To study the burning characteristics of moxa stick. METHODS: A self-designed moxa stick burning temperature measuring device, which was assembled with ALTEC intelligence digital setter and SJ-600 thermocouple, was used to conduct next four experiences: 1) embedding a thermocouple inside a moxa stick to measure peak burning temperature; 2) pulling a thermocouple embedded in the moxa stick at the proper rate to detect combustion stability; 3) elucidating temperature distribution of transverse section by measuring the temperature in the center, radius midpoint and lateral; 4) drawing temperature-time-space curves by pulling the thermocouples in the former three observation points. RESULTS: The experiment indicated that the burning temperature peak of three-year moxa stick (Hubei Herbal Medicine St. Qichun Technology Co., Ltd.) was 848 degrees C which had good combustion stability. Furthermore, the temperature in the center, radius midpoint and lateral of transverse section were 843 degrees C, 731 degrees C and 410 degrees C, respectively, and its burning temperature-time-space curves was drawn, which showed the real-time burning temperature and the peak burning temperature and were regarded as ultimate indice to integrate the formers. CONCLUSION: The measuring system elaborately reflecting the burning features of moxa stick may provide reference for manufacture industry of moxa stick quality criteria for its convenience and accuracy.

Firstborn microcrystallization method to prepare nanocapsules containing artesunate.

We developed a novel method to prepare nanocapsules. A solute often crystallizes when its solubility alters from one solvent to another, and its firstborn crystals are used as templates to prepare nanocapsules for the first time, which is called firstborn microcrystallization method. By using this method, the maximum diameter of the nanocapsules including artesunate is about 76 nm, and wrapping state is well. One important advantage of our method is that the preparation of the nanocapsules operates easily and is a one-time process with no other cumbersome processes necessary, therefore avoiding secondary pollution. The proposed method provides a new route to prepare monodisperse nanocapsules to increase bioavailability of hydrophobic solutes.

[Observation on scavenging free radical function of Artemisia burning products].

OBJECTIVE: To study the pharmacologic action of Artemisia burning products. METHODS: The extractions of Artemisia burning products were determined by spectrophotometry. The scavenging ability of Artemisia burning products on DPPH was evaluated. The chemical components and structures of Artemisia burning products were analyzed by Gas Chromatography and Mass Spectrometry (GC-MS). RESULTS: The scavenging ability of extractions from Artemisia burning products was the strongest. Thirty-six chemical components were detected, and the 5-tert-Butylpyrogallol among them had a stronger anti-oxygen capacity, its scavenging free radical ability was 1.55 times and 1.21 times as strong as VitC and BHT, respectively. CONCLUSION: The scavenging free radical ability of 5-tert-Butylpyrogallol extracted from Artemisia burning products is stronger than the natural antioxidant of VitC and artificial synthetic of BHT.