Antitumor Activity of α-Linolenic Acid-Paclitaxel Conjugate Nanoparticles: In vitro and in vivo.

Purpose: Small molecule modified antitumor drug conjugate nanoparticles have the advantages of high drug loading, simple synthesis and preparation, and better biocompatibility. Due to the large demand for exogenous α-linolenic acid (ALA) by tumor cells, we synthesized α-linolenic acid-paclitaxel conjugate (ALA-PTX) and prepared α-linolenic acid-paclitaxel conjugate nanoparticles (ALA-PTX NPs), in order to obtain better tumor cellular uptake and antitumor activity in vitro and in vivo.

Methods: We synthesized and characterized ALA-PTX, and then prepared and characterized ALA-PTX NPs.

RANK/RANKL Acts as a Protective Factor by Targeting Cholangiocytes in Primary Biliary Cholangitis.

Background: Primary biliary cholangitis (PBC) is an autoimmune liver disease characterized by the highly selective autoimmune injury of small intrahepatic bile ducts. Studies reported that the cholangiocytes from PBC patients expressed significantly higher levels of both receptor activator of nuclear factor-kappa B (RANK) and its ligand RANKL. However, the accurate role of RANK/RANKL axis in PBC remains unclear.

Antitumor activity of the bioreductive prodrug 3-(2-nitrophenyl) propionic acid-paclitaxel nanoparticles (NPPA-PTX NPs) on MDA-MB-231 cells: in vitro and in vivo.

Background: 3-(2-Nitrophenyl) propionic acid-paclitaxel (NPPA-PTX) is a paclitaxel (PTX) bioreductive prodrug synthesized by our lab. We hypothesize that NPPA-PTX can self-assemble to form nanoparticles (NPs).

Materials And Methods: In the present research, the theoretical partition coefficient (XlogP) and Hansen solubility parameters of NPPA-PTX were calculated.

Anti-tumour activity of low molecular weight heparin doxorubicin nanoparticles for histone H1 high-expressive prostate cancer PC-3M cells.

Nucleus-targeting drug delivery systems (NTDDs) deliver chemotherapeutic agents to nuclei in order to improve the efficacy of anti-tumour therapy. Histone H1 (H1) plays a key role in establishing and maintaining higher order chromatin structures and could bind to cell membranes. In the present study, we selected H1 as a target to prepare a novel H1-mediated NTDD.

The theranostic efficiency of tumor-specific, pH-responsive, peptide-modified, liposome-containing paclitaxel and superparamagnetic iron oxide nanoparticles.

Background: In the present study, the tumor-specific, pH-responsive peptide HK(R)-modified, theranostic liposome-containing paclitaxel (PTX) and superparamagnetic iron oxide nanoparticles (SPIO NPs), PTX/SPIO-SSL-HK(R), was prepared by using HK(R) as the targeting ligand, SPIO NPs as the magnetic resonance imaging (MRI) agent, PTX as antitumor drug.

Methods: The PTX/SPIO-SSL-HK(R) was prepared by a thin film hydration method. The characteristics of PTX/SPIO-SSL-HK(R) were evaluated.

Effect of XlogP and Hansen Solubility Parameters on Small Molecule Modified Paclitaxel Anticancer Drug Conjugates Self-Assembled into Nanoparticles.

Small molecule modified anticancer drug conjugates (SMMDCs) can self-assemble into nanoparticles (NPs) as therapeutic NP platforms for cancer treatment. Here we demonstrate that the XlogP and Hansen solubility parameters of paclitaxel (PTX) SMMDCs is essential for SMMDCs self-assembling into NPs. The amorphous state of PTX SMMDCs will also affect SMMDCs self-assembling into NPs.

Comparative Effectiveness of Prophylactic Strategies for Perinatal Transmission of Hepatitis B Virus: A Network Meta-analysis of Randomized Controlled Trials.

Background: Perinatal transmission is the main route of hepatitis B virus (HBV) transmission. While several measures have been attempted as means of preventing perinatal HBV transmission, the optimal strategy remains inconclusive.

Methods: We conducted a comprehensive search, through December 2016, for randomized controlled trials (RCTs) that compared the following measures among pregnant women with HBV infection: placebo/none, active immunoprophylaxis (hepatitis B vaccine series starting at birth [HBVac]), passive-active immunoprophylaxis (hepatitis B immunoglobulin and vaccine [HBIG+HBVac]), prenatal HBIG administration (HBIG/HBIG+HBVac), and prenatal antiviral therapy (AVT/HBIG+HBVac).

Clinical course and perinatal transmission of chronic hepatitis B during pregnancy: A real-world prospective cohort study.

Objective: To determine the clinical course and perinatal transmission of chronic hepatitis B during pregnancy in a real life setting.

Methods: A total of 221 singleton pregnant women with detectable HBV-DNA levels (≥10 copies/mL) were enrolled during January 2011 to June 2015. Forty-three high viraemic patients (≥10 copies/mL) received telbivudine in the 2 or 3 trimester according to their intention, while 89 high viraemic and 79 low viraemic (≥10 and <10 copies/mL) patients were the control cohorts.

[Effect of rapid eye movement sleep deprivation on anxiety behavior and hippocampus NO level: different responses of adolescent and adult C57BL/6J mice].

Objective: To explore the difference between adolescent and adult C57BL/6J mice in response to rapid eye movement sleep (REMS) deprivation in terms of anxiety behavior and hippocampal NO level.

Methods: Both adolescent and adult C57BL/6J mice were divided into normal control (NC) group, wide platform (WP) group, and 24-hour REMS deprivation group, each group consisting of 15 mice. REMS deprivation models were established using a small platform in water tank, and the elevated plus maze test was used to examine anxiety behavior of the mice.

Ultrasound-guided percutaneous microwave ablation for adenomyosis: efficacy of treatment and effect on ovarian function.

A total of 142 premenopausal women with symptomatic adenomyosis underwent ultrasound (US)-guided percutaneous microwave ablation (PMWA) at the Chinese PLA General Hospital. This study aimed to evaluate changes in serum pituitary, gonadal hormone and cancer antigen 125 (CA125) levels after US-guided PMWA. Therefore, estradiol (E2), follicle-stimulating hormone (FSH), prolactin (PRL) and CA125 levels were evaluated before ablation and at 3, 6, 9 and 12 months after ablation.

Research of dose-effect relationship parameters of percutaneous microwave ablation for uterine leiomyomas--a quantitative study.

Eighty eight patients with 91 uterine leiomyomas who underwent ultrasound-guided percutaneous microwave ablation (PMWA) treatment were prospectively included in the study in order to study the dose-effect relationship parameters (DERP) of PMWA for uterine leiomyomas and its relationship with T2-weighted MR imaging (T2WI). Based on the signal intensity of T2WI, uterine leiomyomas were classified as hypointense, isointense, and hyperintense. During ablation, leiomyomas were treated with quantitative microwave ablation (QMWA) energy of 50 w × 300 s or 60 w × 300 s.

Ultrasound-guided percutaneous microwave ablation for submucosal uterine fibroids.

Study Objective: To prospectively evaluate the efficiency and safety of ultrasound-guided percutaneous microwave ablation (PMWA) in treating symptomatic submucosal uterine myomas.

Design: Self-controlled study (Canadian Task Force classification II-1).

Setting: Single center.

Chemical constituents from Solidago canadensis with hypolipidemic effects in HFD-fed hamsters.

Two new compounds, 8-dehydroxymethylvisanol (1) and 9-O-[3-O-acetyl-β-d-glucopyranosyl]-4-hydroxy-cinnamic acid (4), together with two known lignans, visanol (2) and 9-aldehydevibsanol (3), were isolated from the 80% EtOH extract of Solidago canadensis. The structures of the two new compounds were elucidated on the basis of 1D, 2D NMR, and mass spectral analysis. All the lignans exhibited moderate hypolipidemic activity in high-fat diet-fed hamsters.

[Study on the anti-tumor effect of paclitaxel mixed micelle by using in vivo optical imaging technique].

In vivo tumor imaging technique method based on bioluminescence principle was established to evaluate the anti-tumor effect of paclitaxel mixed micelle (PMM). MDA-MB-231 tumor cells with luciferase reporter vectors were firstly implanted into nude mice, and subsequently the luciferase substrate was regularly injected during intraperitoneal administration of PMM. Then the tumor size, growth and the intensity of light signals were monitored with in vivo imaging technique.

Investigation of structural requirements for inhibitory activity at the rat and housefly picrotoxinin binding sites in ionotropic GABA receptors using DISCOtech and CoMFA.

A number of widely diverse compounds that show inhibitory activities at the picrotoxinin binding sites in housefly and rat GABA receptors were investigated by using the distance comparison technique (DISCOtech) and comparative molecular field analysis (CoMFA) methods to explore the pharmacophore models and the three-dimensional quantitative structure-activity relationships (3D-QSAR) of the compounds. These compounds consist of three diverse types of noncompetitive GABA receptor antagonists, i.e.

[Changes of Smoothened expression during retinofugal pathway development in mouse embryos].

Objective: To examine the change of Smoothened (Smo) expression in the retinofugal pathway and in the growth cones during the period of embryonic day 13 (E13) to E15.

Methods: Smo expression in the chiasm and growth cones was observed by fluorescent immunostaining and retinal explant culture.

Results: On E13 and E14, Smo was expressed moderately in the retina and optic disc, and in the corner of the retina, Smo expression was especially dense.

Changes of retinofugal pathway development in mouse embryos after Sonic hedgehog antibody perturbation.

Objective: To understand the function of Sonic hedgehog in chiasm development in mouse embryos of embryonic day 13 (E13) to E15.

Methods: Brain slices of E13-E15 mouse embryos containing the optic pathway from the eyes to the optic tract were prepared and cultured in DMEM/F12 in the presence of 10% fetal bovine serum at 37 degrees in a rolling incubator for 5 h. The antibody to Shh was added into the culture medium of the slices in the treatment group, while no additional chemical or only normal mouse IgG was added in the control groups.

In-vitro cytotoxicity, in-vivo biodistribution and anti-tumour effect of PEGylated liposomal topotecan.

In attempt to increase the accumulation of topotecan in tumours and improve its anti-cancer activity, PEGylated liposome (H-PEG) containing topotecan was prepared. The in-vitro cytotoxicity, in-vivo biodistribution pattern and anti-tumour effect of H-PEG were studied systemically. Compared with free topotecan or conventional liposome (H-Lip), H-PEG improved the cytotoxic effect of topotecan against human ovarian carcinoma A2780 and human colon carcinoma HCT-8 cells.

[Preparation of cardiomyocyte-targeting liposomes and their targeting ability in vitro].

Aim: To prepare the cardiomyocyte-targeting liposomes and investigate their cardiomyocyte targetability in vitro.

Methods: Liposomes modified with compound PAC were prepared (PAC-L); The uptake of PAC-L by cardiomyocytes was studied by incubating fluorescence labeled liposomes with cardiomyocytes in vitro and measuring the association of liposomes by a fluorescence spectrophotometer.

Results: A high affinity of PAC-L to the cardiomyocytes was observed, the amount of cell uptake of PAC-L by cardiomyocytes was higher than that by nonmyocyte (P < 0.

In vitro and in vivo studies of different liposomes containing topotecan.

Liposome as a carrier of topotecan (TPT), a promising anticancer drug, has been reported in attempt to improve the stability and antitumor activity of TPT. However, the biodistribution pattern of TPT liposome in vivo and PEG-modified liposome containing TPT have not been studied systemically. In this paper, the in vitro stability and in vivo biodistribution behavior of several liposomes containing TPT with different lipid compositions and PEG-modification were studied.

Regionally specific expression of L1 and sialylated NCAM in the retinofugal pathway of mouse embryos.

We have examined expression of L1 and the polysialic acid-associated form of the neural cell adhesion molecule (PSA-NCAM) in mouse embryos during the major period of axon growth in the retinofugal pathway to determine whether they are expressed in patterns that relate to the changes in axon organization in the pathway. Immunostaining for L1 and PSA-NCAM was found on all axons in the retina and the optic stalk. In the chiasm, while L1 immunoreactivity remained high on the axons, PSA-NCAM staining was obviously reduced.