Construction of 3D network aluminum sludge-based hydrogel beads: combination of macroization, amino functionalization, and resource utilization.

An aluminum sludge-based composite material was constructed against the problems of phosphorus pollution and the waste of aluminum sludge resources. Utilizing metal Ce doping and hydrogel microbeads with pore preparation, the adsorption performance of the original sludge was improved. Meanwhile, the macroscopic body was constructed, and on this basis, polyethyleneimine (PEI) was introduced to complete the amino functionalization further to enhance the adsorption of phosphorus by the adsorbent, and NH-CeAIS-10 microbeads were successfully prepared. In adsorption, microbeads with larger specific surface area and richer functional groups are better choice compared to original sludge. The results of SEM, BET, FT-IR, and XPS analyses indicate that the adsorption of phosphorus by the microbeads is mainly achieved through electrostatic interactions, ligand exchange, and the formation of inner-sphere complexes. According to the Langmuir model, the maximum phosphorus adsorption capacity of NH-CeAIS-10 was 29.56 mg g-1, which was four times higher compared to native aluminum sludge. This also confirms the significant enhancement of phosphorus adsorption through the modification of aluminum sludge. Besides, in dynamic adsorption column experiments, the material exhibited up to 99% removal in simulated wastewater for up to 30 days, demonstrating the great adsorption potential of NH-CeAIS-10 in engineering applications.

A chemo-photothermal synergetic antitumor drug delivery system: Gold nanoshell coated wedelolactone liposome.

In this study, an antitumor drug delivery system, gold nanoshell coated wedelolactone liposomes (AuNS-Wed-Lip), were designed and synthesized. In the drug delivery system, wedelolactone liposome and gold-nanoshell were linked by l-cysteine, which had been shown an effective nanocarrier for antitumor drug delivery, on-demand drug release, and phototherapy under near-infrared (NIR) light irradiation. It was capable of absorbing 780-850 nm NIR light and converting light energy to heat rapidly. The hyperthermia promoted wedelolactone release rapidly from the systems. The release amount of AuNS-Wed-Lip under NIR irradiation reached up to 97.34% over 8 h, achieving the on-demand drug release. Moreover, a high inhibition rate up to 95.73% for 143B tumor cells by AuNS-Wed-Lip upon laser irradiation at 808 nm was observed. The excellent inhibition efficacy was also displayed in vivo antitumor study with S180 tumor-bearing mice. The results demonstrated that AuNS-Wed-Lip, as an antitumor drug delivery system, achieved chemo-photothermal synergetic effect, which has great potential in cancer therapy.

Doxorubicin/gold nanoparticles coated with liposomes for chemo-photothermal synergetic antitumor therapy.

Hybrid liposome/metal nanoparticles are promising candidate drug-carriers for therapy of various diseases due to their unique photothermal effect. In this study, self-crystallized gold nanoparticles (Au NPs) and doxorubicin (DOX) were co-encapsulated within liposomes (Au/DOX-Lips) by thin film hydration and gel separation technology. The surface plasmon resonance bands of drug-carriers were controllable in the near-infrared (NIR) zone. When the complex liposome/metallic hybrids were irradiated by NIR light, they displayed higher endocytosis efficiency following the fracture of liposomal membranes and the release of Au NPs. Then, the Au NPs penetrated further into deeper tumor tissue to accomplish photothermal treatment. The Au/DOX-Lips showed an excellent antitumor effect, whose inhibition rate for tumor cells was up to 78.28%. In experiments on mice bearing tumors, the Au/DOX-Lips treated mice exhibited superior tumor suppression. This novel drug system provides huge potential for biomedical application.

Combining nanoscale magnetic nimodipine liposomes with magnetic resonance image for Parkinson's disease targeting therapy.

AIM: To enhance drug targeting and blood-brain barrier penetration for Parkinson's disease (PD), a novel nanoscale magnetic nimodipine (NMD) delivery system was designed and prepared. MATERIALS & METHODS: The PD rats were established and treated with free NMD or Fe3O4-modified NMD liposomes (Fe3O4-NMD-lips). Then, factional anisotropy values were measured by MRI to evaluate therapy efficacy. RESULTS: Fe3O4-NMD-lips showed the best neuroprotective effect, and the NMD concentration of lesions was 2.5-fold higher in Fe3O4-NMD-lips group than that of free NMD group. CONCLUSION: These results demonstrated that the magnetic drug system had a great potential to cross the blood-brain barrier and provided a noninvasive and effective therapeutic strategy for PD.

New neo-lignan from Acanthopanax senticosus with protein tyrosine phosphatase 1B inhibitory activity.

New neo-lignan, (7S, 8R)-3-hydroxyl-4-methoxyl-balanophonin (1), together with seven known compounds (2-8) were isolated from the EtOAc-soluble extract of Acanthopanax senticosus. The structure of the new neo-lignan was elucidated with spectroscopic and physico-chemical analyses. All the isolates were evaluated for in vitro inhibitory activity against PTP1B, VHR and PP1. Among them, the new compound (1) was found to exhibit selective inhibitory activity on PTP1B with IC50 value 15.2 ± 1.4 µM.

Gold Nanoshells: Combined Near Infrared Photothermal Therapy and Chemotherapy Using Gold Nanoshells Coated Liposomes to Enhance Antitumor Effect (Small 30/2016).

Gold nanoshell coated oleanolic acid liposomes mediating by chitosan (GNOLs), are designed and successfully synthesized for the first time by D. Gao and co-workers on page number 4103. An excellent near infrared (NIR) photothermal effect, pH-responsive drug controlled release and tumor targeting properties are demonstrated. By combining NIR photothermal therapy and chemotherapy, the smart drug delivery system exhibits a superior antitumor property in vitro and in vivo.

Combined Near Infrared Photothermal Therapy and Chemotherapy Using Gold Nanoshells Coated Liposomes to Enhance Antitumor Effect.

Novel antitumor system based on the targeting photothermal and pH-responsive nanocarriers, gold nanoshells coated oleanolic acid liposomes mediating by chitosan (GNOLs), is designed and synthesized for the first time. The GNOLs present spherical and uniform size (172.03 nm) with zeta potential (20.7 ± 0.4 mV), which are more easily accumulated in tumor. Meanwhile, the GNOLs exhibit a slow and controlled release of oleanolic acid at pH 7.4, as well as a rapid release at pH 5.5, which is beneficial for tumor-targeting drug release. Under near infrared (NIR) irradiation, hyperthermia can be generated by activated gold nanoshells to perform photothermal therapy effect, which triggers drug release from the carriers by activating the gel to liquid crystalline phase transition of the liposomes. Moreover, the NIR assisting drug release can be easily and selectively activated locally due to the spatially and real-timely controllable property of light. The experimental results also verify that the GNOLs with NIR irradiation achieve more ideal antitumor effects than other oleanolic acid formulations in vitro and in vivo. Hence, the drug delivery system exhibits a great potential in chemo-photothermal antitumor therapy.

Four new sesqui-lignans isolated from Acanthopanax senticosus and their diacylglycerol acyltransferase (DGAT) inhibitory activity.

Four new sesqui-lignans, (7R, 7'R, 7″S, 8S, 8'S, 8″S)-4',5″-dihydroxy-3,5,3',4″-tetramethoxy-7,9':7',9-diepoxy-4,8″-oxy-8,8'-sesquineo-lignan-7″,9″-diol (1), (7R, 7'R, 7″S, 8S, 8'S, 8″S)-4',3″-dihydroxy-3,5,3',5',4″-pentamethoxy-7,9':7',9-diepoxy-4,8″-oxy-8,8'-sesquineo-lignan-7″,9″-diol (2), (7R, 7'R, 7″S, 8S, 8'S, 8″S)-3',4″-dihydroxy-3,5,4',5″-tetramethoxy-7,9':7',9-diepoxy-4,8″-oxy-8,8'-sesquineo-lignan-7″,9″-diol (3) and acanthopanax A (7) together with three known compounds (4-6) were isolated from the EtOAc-soluble extract of Acanthopanax senticosus. Their structures were elucidated on the basis of spectroscopic and physicochemical analyses. All the isolates were evaluated for in vitro inhibitory activity against DGAT1 and DGAT2. Among them, compounds 1-6 were found to exhibit selective inhibitory activity on DGAT1 with IC50 values ranging from 61.1 ± 1.3 to 97.7 ± 1.1 µM and compound 7 showed selective inhibition of DGAT2 with IC50 value 93.2 ± 1.2.

Effects of Morus root bark extract and active constituents on blood lipids in hyperlipidemia rats.

OBJECTIVE: Chinese crude drug Mori Cortex Radicis (the root cortex of Morus species) has been used as a folk medicine to treat hypertension, diabetes, as well as in expectorant, diuretic agents. This investigation aims to study the anti-hyperlipidemia effects of Mori Cortex Radicis (MCR) extracts in hyperlipidemic rat models and the potential therapeutic activities of compounds isolated from the extracts. MATERIALS AND METHODS: The effects of MCR on hypolipidemic parameters were investigated using Wistar rats induced by high-lipid emulsion. Sixty healthy Wistar rats were randomly divided into 6 groups: normal group, hyperlipidaemia model group, simvastatin, and high-, medium- and low-dose MCR extracts. After four weeks, body weight, total cholesterol (TC), triglycerides (TG), high and low-density lipoproteins (HDL, LDL), as well as aspartate aminotransferase (AST), alanine aminotransferase (ALT) were measured. To further investigation, four major active compounds were isolated from extracts through high performance liquid chromatography (HPLC) and their diacylglycerol acyltransferase 1 (DGAT1) inhibitory activity was evaluated. RESULTS: MCR dose-dependently reduced serum TC, TG, LDL-C, inhibited the activity of ALT, AST, and increased HDL-C. Furthermore, in vitro biochemistry tests revealed that four active isolates showed moderate inhibitory activity against DGAT1 with IC50 values ranging from 62.1 ± 1.2 to 99.3 ± 2.3 µM. CONCLUSIONS: The results demonstrated that MCR could effectively ameliorate hyperlipidaemia and inhibit DGAT1 that a key enzyme closely related to hyperlipidaemia and type 2 diabetes. It may provide a new pharmacological basis for treating hyperlipidaemia and related diseases using MCR.

Two new lignans from Saururus chinensis and their DGAT inhibitory activity.

Two new lignans were isolated from Saururus chinensis, along with eight known compounds. Their structures were elucidated on the basis of spectroscopic and physico-chemical analyses. All the isolates were evaluated for in vitro inhibitory activity against DGAT1 and DGAT2. Among them, compounds 2, 3, 5 and 7 were found to exhibit selective inhibitory activity on DGAT1 with IC50 values ranging from 44.3±1.5 to 87.5±1.3µM.

Ginkgo biloba attenuates oxidative DNA damage of human umbilical vein endothelial cells induced by intermittent high glucose.

Intermittent high glucose (IHG), one of the general and important symptoms of patients with diabetes, has greater effect than sustained high glucose on the development of diabetic cardiovascular complications, in which endothelial dysfunction caused by oxidative stress is regarded as the initiation. However, no study investigated either the degree of endothelial DNA oxidation caused by IHG or the potential protective effects of antioxidants. In this study, DNA oxidation, including 8-hydroxy-2'-deoxyguanosine (8-OHdG) concentration and comet assay, was studied in human umbilical vein endothelial cells (HUVECs) under IHG with or without treatment of Ginkgo biloba extract (EGb 761). We found that high glucose, especially IHG, increased reactive oxygen species generation, 8-OHdG content and oxidative DNA damage in HUVECs. These high glucose-induced oxidative stress could be suppressed by EGb 761 (25-100 microg/ml) in a dose-dependent manner through the improvement of total antioxidant capacity. Our results indicated that the presence of significant DNA oxidation in HUVECs exposed to high glucose, and especially higher in the cells in IHG conditions. EGb 761, an antioxidant herbal medicine, can remarkably alleviate endothelial DNA oxidation caused by IHG, which may provide a novel approach for endothelial protection in the presence of IHG.

Felodipine reduces cardiac expression of IL-18 and perivascular fibrosis in fructose-fed rats.

Metabolic syndrome is associated with accelerated macrovascular and microvascular coronary disease, cardiomyopathy, and elevated inflammatory status. To determine whether metabolic syndrome-associated elevation of the inflammatory cytokine interleukin-18 (IL-18) in serum and cardiac tissue, and its potential sequelae could be attenuated pharmacologically, we studied fructose-fed rats. The fructose-fed rats exhibited increases in systolic blood pressure (SBP), body weight, heart weight, left ventricular weight, and blood insulin. Serum IL-18 levels in these rats were also elevated significantly. These changes were significantly different compared to those in control rats. Perivascular fibrosis around coronary arterioles was evident in the fructose-fed rats, accompanied by a paralleled increase in IL-18 by immunohistochemical analysis and real time polymerase chain reaction. Felodipine attenuated the increased levels in serum IL-18 and cardiac IL-18 mRNA as well as coronary perivascular fibrosis. Thus, augmented IL-18 in serum and cardiac tissue in metabolic syndrome may contribute to the coronary perivascular fibrosis; felodipine administration can attenuate the inflammatory and fibrosis process.