Phytochemical Profile of Alkaloid Extract from Dendrobium huoshanense and Inhibitory Effects against Oxidative Stress in H2 O2 -Induced PC12 Cells.

This study aimed to explore the alkaloid profile of Dendrobium huoshanense and determine the potential protective effect against oxidative damage. The crude D. huoshanense alkaloid extract (DHAE) was obtained by 70 % ethanol extraction and liquid-liquid partition. DHAE contained specific alkaloid components with abundant 6-hydroxynobiline (58.15 %) and trace dendrobine (3.23 %) in the preliminary HPLC fingerprint and GC-MS analysis, which was distinguished from D. officinale or D. nobile. Subsequently, six alkaloids including 6-hydroxynobiline, 2-hydroxy dendrobine, nobilonine, dendrobine, Findlayines D and trans-dendrochrysanine were identified in the purified DHAE (namely DHSAE-3, DHSAE-3') via further solid phase extraction coupled with UPLC-MS/MS analysis. Meanwhile, pretreatment with DHAE or DHSAE (0.5, 5 µg/mL) increased cell viability by 14.0-57.4 % compared to that of H2 O2 -induced PC12 Model cells. Among them, 5 µg/mL DHSAE-3-treated cells displayed a pronounced reversion than the positive vitamin E (p<0.01). Furthermore, a clear cellular morphological restoration and 38.4 % reduction in intracellular reactive oxidative species level were achieved. Our findings suggest that D. huoshanense has a characteristic alkaloid profile represented by abundant 6-hydroxynobiline, and DHAEs exhibit obvious protection against oxidative neuronal damage. Overall, this study indicates that DHAEs might be used to inhibit oxidative stress and provide a source to develop novel neuroprotective drugs.

Synthesis of Quercetin-Acid Esters and Its Reduction of H2 O2 -Triggered PC12 Cells Damage by Down-Regulating ROS.

Quercetin is a kind of polyphenolic flavonoid compounds which has perfect antioxidant properties. However, quercetin is not available in many situations due to its poor bioavailability. In this work, the QAEs with better solubility and even stronger antioxidant properties were synthesized, through the esterification between quercetin and the chlorinated cinnamic acid or its derivatives, whose chlorination were achieved by using SOCl2 . The protective effects of the QAEs were evaluated by the H2 O2 -induced apoptosis experiment in rat adrenal pheochromocytoma cells (PC12 cells) and its ability to remove ROS generated by oxidative stress. Compared with the original quercetin group, the QAEs groups showed much improved cell viability and capability of removing ROS, which means their higher bioavailability than the parent.

Okra pectin relieves inflammatory response and protects damaged intestinal barrier in caerulein-induced acute pancreatic model.

BACKGROUND: Protecting the intestinal mucosa from being destroyed helps reduce the inflammation caused by acute pancreatitis (AP). In this study, whether okra pectin (OP) could attenuate the inflammation of AP through protecting the intestinal barrier was investigated. RESULTS: OP was obtained from crude okra pectin (COP) through the purification by DEAE cellulose 52 column. Supplementation with OP or COP in advance reduced the severity of AP, as revealed by lower serum amylase and lipase levels, abated pancreatic edema, attenuated myeloperoxidase activity and pancreas histology. OP or COP inhibited the production of pancreatic proinflammatory cytokines, including tumor necrosis factor-α and interleukin-6. In addition, the upregulation of AP-related proteins including ZO-1, occludin, the antibacterial peptide-defensin-1 (DEFB1) and cathelicidin-related antimicrobial peptide (CRAMP), as well as the histological examination of colon injuries, demonstrated that OP or COP provision could effectively maintain intestinal barrier function. Ultimately, dietary OP or COP supplementation could inhibit AP-induced intestinal inflammation. For the above, the effect of OP was better than COP. CONCLUSION: Dietary OP supplementation could be considered as a preventive method that effectively interferes with intestinal damage and attenuates inflammatory responses trigged by AP. © 2020 Society of Chemical Industry.

Effect of high-pressure pre-soaking on texture and retrogradation properties of parboiled rice.

BACKGROUND: The poor palatability, low digestibility, and unpleasant color of parboiled rice (PR) have severely hampered its acceptance by consumers. It is hence necessary and urgent to develop a new method for producing high-quality PR. In the current study, the effect of high hydrostatic pressure (HHP) pre-soaking on the color, textural properties, and the degree of retrogradation of PR was investigated. RESULTS: With HHP from 100 to 500 MPa, the water adsorption rate increased and cooking time decreased. Parboiled rice samples presented higher lightness scores (L) and had lower color intensity (B). Compared with a control group, PR samples treated with high-pressure pre-soaking showed a reduction of hardness values from 0.69% to 32.99%, and gumminess values also decreased from 8.58% to 33.62%. The differential scanning calorimetry (DSC) results indicated that the enthalpy values of PR samples decreased after high pressure pre-soaking. The molecular structure of PR characterized by Fourier transform infrared spectrometry confirmed that HHP pre-soaking could decrease the retrogradation level. CONCLUSION: The findings outlined above suggest that the texture and retrogradation properties of PR were improved after high-pressure pre-soaking. © 2021 Society of Chemical Industry.

Theoretical design, preparation, and evaluation of Ginkgolide B molecularly imprinted polymers.

Ginkgolide B is in great demand worldwide on account of its extensive and excellent pharmacological effects, however, it is difficult to separate and purify ginkgolide B. In this study, ginkgolide B molecularly imprinted polymers were prepared by combining software simulation and molecular imprinting technique, and its characterization and adsorption performed evaluation were performed to understand the adsorption behavior of the polymers. The adsorption equilibrium concentration of molecularly imprinted polymers was 0.70 mg/mL, and the adsorption equilibrium time was 4 h. Meanwhile, the adsorption isotherm of the polymers for ginkgolide B fitted well with the Langmuir model, and the adsorption kinetics was in line with the pseudo-second-order kinetics. In contrast, the adsorption capacity of molecularly imprinted polymers on ginkgolide B was higher than that of non-molecular imprinted polymers, with better selectivity and better adsorption after repeated use for six times. The application experiments showed that molecular imprinted polymers have a good adsorption effect in low purity samples. Therefore, the polymers reported herein can be expected to apply in the adsorption and separation of ginkgolide B samples.

Optimization on conditions of podophyllotoxin-loaded liposomes using response surface methodology and its activity on PC3 cells.

The purpose of this study was to optimize the preparation conditions of podophyllotoxin liposomes (PPT-Lips), and to investigate their effects on PC3 cells. PPT-Lips were prepared by using a thin-film dispersion method. In order to achieve maximum drug encapsulation efficiency (EE), the process and formulation variables were optimized by response surface methodology (RSM). The optimum preparation conditions were cholesterol to lecithin ratio of 3.6:40 (w/w), lipid to drug ratio of 15.8:1 (w/w), and the ultrasonic intensity of 35% (total power of 400 W). The experimental EE of PPT-Lips was 90.425%, which was consistent with the theoretically predicted value. The characterization studies showed that PPT-Lips were well-dispersible spherical particles with an average size of 106 nm and a zeta potential of -10.1 mV. A gradual and time-dependent pattern of PPT from liposomes was found in in vitro drug release with a cumulative release amount up to 70.3% in 24 h. Results of cell viability experiments on PC3 cells demonstrated that PPT-Lips exhibited more effective anticancer activity in comparison with free PPT. Therefore, PPT-Lips represent an efficient and promising drug delivery system for PPT.

Two macamide extracts relieve physical fatigue by attenuating muscle damage in mice.

BACKGROUND: Macamides, the main active components contained in maca, have attracted increasing attention due to their various bioactivities. In this study, crude macamide extract (CME) and purified macamide extract (PME) were prepared by enzyme-assisted extraction and macroporous resin separation, and the anti-fatigue effects of CME and PME were evaluated in a forced swimming model. RESULTS: The composition analysis results revealed that both CME and PME mainly contain eight kinds of macamide. Based on the results of a weight-loaded forced swimming test, compared with a control group, CME and and PME groups could prolong exhaustive swimming time, increase levels of liver glycogen (LG) and muscle glycogen (MG), accelerate fatty acid oxidation in serum to provide energy, eliminate the accumulation of blood lactic acid (BLA) and blood urea nitrogen (BUN), and decrease the serum biomarkers for muscle damage, such as lactate dehydrogenase (LDH) and creatine kinase (CK). Histological analysis also indicated that CME and PME attenuated damage to skeletal muscle and the myocardium in mice during exercise. CONCLUSION: Two macamide extracts have a beneficial effect on relieving physical fatigue by attenuating the damage of skeletal muscle and myocardium during exercise, and a better effect was observed in the PME group. © 2018 Society of Chemical Industry.

Synthesis and evaluation of paeonol derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.

Alzheimer's disease (AD) is a progressive neurodegenerative brain disorder characterized by memory loss, language impairment, personality changes and intellectual decline. Taking into account the key pathological features of AD, such as low levels of acetylcholine, beta-amyloid (Aß) aggregation, oxidative stress and dyshomeostasis of biometals, a new series of paeonol derivatives 5a-5d merging three different functions, i.e., antioxidant, anti-acetylcholinesterase (AChE) activity, metal chelating agents for AD treatment have been synthesized and characterized. Biological assays revealed that compared with paeonol (309.7 µM), 5a-5d had a lower DPPH IC50 value (142.8-191.6 µM). 5a-5d could significantly inhibit hydrogen peroxide-induced neuronal PC12 cell death assessed by MTT assay in the concentration range of 5-40 µM. AChE activity was effectively inhibited by 5a-5d, with IC50 values in the range of 0.61-7.04 µM. 5a-5d also exhibited good metal-chelating ability. All the above results suggested that paeonol derivatives may be promising multifunctional agents for AD treatment.

Enhanced Brain Targeting Delivery of Salvianic Acid Using Borneol as a Promoter of Blood/Brain Transport and Regulator of P-gp.

BACKGROUND: Borneol can enhance the blood-brain barrier (BBB) permeability of some drugs and suppress the efflux transport of P-glycoprotein (P-gp), which will contribute to the brain delivery of salvianic acid A (SAA). OBJECTIVE: The study aimed to develop an approach to improve the brain targeting delivery of SAA with the aid of borneol. MATERIALS AND METHODS: "Borneol" was involved in SAA via esterified prodrug SAA borneol ester (SBE) and combined administration (SAA-borneol, SAA-B). Subsequently, the blood-brain transport of SAA through brain/blood distribution and P-gp regulation via expression and function assay were investigated in rats. RESULTS: The SBE and SAA-B-treated group received a three-fold brain concentration and longer t1/2 and retention period of active SAA than that of SAA alone (20.18/13.82 min vs. 6.48 min; 18.30/17.42 min vs. 11.46 min). In addition, blood to brain transport of active SAA in SBE was altered in comparison to that of SAA-B, ultimately resulting in a better drug targeting index (9.93 vs. 3.63). Further studies revealed that SBE-induced downregulation of P-gp expression occurred at the later stage of administration (60 min, P < 0.01), but SBE always showed a more powerful drug transport activity across BBB represented by Kp value of rhodamine 123 than SAA-B (30, 60 min, P < 0.05). CONCLUSION: The comparative results indicate that SBE exhibits prominent efficiency on SAA's targeting delivery through improved blood/brain metabolic properties and sustained inhibitory effect of "borneol" on P-gp efflux. Therefore, prodrug modification can be applied as a more effective approach for brain delivery of SAA.

Discovery of acylated isoquercitrin derivatives as potent anti-neuroinflammatory agents in vitro and in vivo.

Neuroinflammation is considered as an important pathological mechanism in neurodegenerative diseases. The natural isoquercitrin (IQ) was reported to have potential anti-neuroinflammatory activity. The acylation of glycoside in IQ enhanced its hydrophobicity, which was expected to enhance the protective effect against inflammation. In this study, three carboxylic acids with anti-neuroinflammatory effects including cinnamic acid, ibuprofen (IBU) and acetylsalicylic acid were introduced into the 6''-OH of IQ through the corresponding vinyl esters intermediates (8a-8c). Ultimately, the acylated IQ derivatives (Compound 9a-9c) were obtained with 35-42% yields using immobilized lipase Novozym 435 as catalyst. Subsequently, their anti-neuroinflammatory activities were evaluated in lipopolysaccharide (LPS)-induced BV2 cells. Compound 9b improved cell viability in the range of ≤50 µM and significantly decreased NO, PGE2 production and TNF-α, IL-1ß release and oxidative stress level with a concentration-dependent manner. Also, it could downregulate iNOS, COX-2, TNF-α and IL-1ß expression levels, approximately 40% reduction were achieved when 15µM compound 9b was employed. In addition, compound 9b resisted phosphorylation and degradation of IkBαs, suppressing the activation of NF-κB signaling pathway, exhibiting excellent neuroinflammatory inhibition. Moreover, the administration of compound 9b (30, 60 mg/kg) alleviated behavioral disorders and neuronal damages in LPS-induced neuroinflammatory mice. Meanwhile, the decreased TNF-α, IL-1ß release, expression and the inhibited glial cells activation were obtained in compound 9b-treated group, which was superior to that of IQ or IBU. Overall, these findings demonstrated that compound 9b, formed by the introduction of ibuprofen into IQ, can serve as a novel promising therapeutic agent for anti-neuroinflammation.

A comparative study of pectic polysaccharides from fresh and dried Dendrobium officinale based on their structural properties and hepatoprotection in alcoholic liver damaged mice.

In this study, two pectic polysaccharides from fresh and dried Dendrobium officinale, namely FDP and DDP, were obtained by sour-water extraction, ethanol precipitation and further purification with DEAE cellulose-52 and Sephadex G-100 column chromatography. FDP/DDP had eight similar glycosidic linkages including 1,4-linked-GlcAp, 1,4- and 1,3,4-linked-GalAp, 1,3,4- and T-linked-Glcp, 1,6- and T-linked-Galp, T-linked-Galp and T-linked-Xylp. Besides, FDP was marked by 1,6-, 1,2,6-linked-Manp and 1,2,4-, 1,2-linked-Rhap, and DDP consisted of unique 1,6-linked-GlcAp and 1,3,6-Manp. FDP with a molecular weight of 14.8 kDa generally showed stronger scavenging capacity against DPPH, ABTS and hydroxyl radicals than DDP (p < 0.05). Pretreatment with FDP/DDP alleviated the alcohol-induced liver injury in mice, and their serum aminotransferase and triglyceride levels were 10.3%-57.8% lower than those of the model group (MG). Meanwhile, the FDP/DDP-M and FDP/DDP-H groups (200 and 300 mg kg-1) displayed a remarkable increase in antioxidant enzyme activities and significant reduction in inflammatory cytokine levels in comparison with the MG. Further analysis revealed that FDP-treated mice generally exhibited lower transaminase levels and inflammatory cytokine expression as well as higher antioxidant enzyme activities than DDP-treated ones. The FDP-H group showed significant restoration, which was slightly less than or almost comparable to that of the bifendate-fed positive control. The above results indicate that D. officinale pectin can attenuate oxidative stress and inflammatory cytokine response, and ultimately ameliorate liver injury, and "fresh" pectin with specific structural characteristics is expected to be more promising as hepatoprotective food.

Antioxidant, anticancer activity and molecular docking study of lycopene with different ratios of Z-isomers.

The main purpose of this study was to compare the antioxidant and anticancer activities of lycopene samples with different ratios of Z-isomers. Lycopene samples containing 5%, 30%, and 55% Z-isomers were successfully prepared by using thermal treatment combined with anti-solvent crystallization. The in vitro bio-accessibility of lycopene was estimated by the determination of partition factor (PF) and the results showed that lycopene with 55% Z-isomers possessed the highest bio-accessibility. Moreover, DPPH and ABTS assays suggested that the antioxidant activity of lycopene increased with the Z-isomers content from 5% to 55%. However, lycopene inhibited the survival of human hepatocellular carcinoma cells (HepG2) in a dose and time-dependent manner. The highest inhibition of HepG2 cell lines was achieved by 55% Z-ratio of lycopene. The cell viability was 22.54% at 20 µg/mL after incubating for 24 h, the number of cells was significantly reduced and the morphology was shrunk. Furthermore, molecular docking was introduced to compare the binding ability between different lycopene isomers with Scavenger Receptor class B type I (SR-BI), and the results revealed that the affinity of (all-E)-lycopene with SR-BI was lower compared to 5Z-lycopene and 13Z-lycopene, providing the reasons for different bioavailability of the above-mentioned lycopene isomers. All the above results demonstrated that Z-isomers-rich lycopene could enhance bio-accessibility and biological functionality.

Comparison of prediction models for blood brain barrier permeability and analysis of the molecular descriptors.

To develop an in silico model for predicting blood brain barrier (BBB) permeability, and evaluate whether incorporation of two new biological descriptors, high affinity P-glycoprotein substrate probability (HAPSP) and plasma protein binding ratio (PPBR), could result in a better model, four different multiple linear regression (MLR) models have been constructed and compared with each other. The optimized model demonstrated predictive ability and simplicity, not only suitable for passive but also for active transport. Moreover, the molecular descriptors used here are discussed.

Magnetic-Field-Induced Improvement of Photothermal Sterilization Performance by Fe3O4@SiO2@Au/PDA Nanochains.

Due to the abuse of antibiotics, the sensitivity of patients to antibiotics is gradually reduced. This work develops a Fe3O4@SiO2@Au/PDA nanochain which shows an interesting magnetic-field-induced improvement of its photothermal antibacterial property. First, SiO2 was wrapped on Fe3O4 nanospheres assembled in a chain to form a Fe3O4@SiO2 nanocomposite with a chain-like nanostructure. Then, the magnetic Fe3O4@SiO2@Au/PDA nanochains were prepared using in situ redox-oxidization polymerization. Under the irradiation of an 808 nm NIR laser, the temperature rise of the Fe3O4@SiO2@Au/PDA nanochain dispersion was obvious, indicating that they possessed a good photothermal effect. Originating from the Fe3O4, the Fe3O4@SiO2@Au/PDA nanochain showed a typical soft magnetic behavior. Both the NIR and magnetic field affected the antimicrobial performance of the Fe3O4@SiO2@Au/PDA nanochains. Escherichia coli and Staphylococcus aureus were used as models to verify the antibacterial properties. The experimental results showed that the Fe3O4@SiO2@Au/PDA nanochains exhibited good antibacterial properties under photothermal conditions. After applying a magnetic field, the bactericidal effect was further significantly enhanced. The above results show that the material has a broad application prospect in inhibiting the growth of bacteria.

The impact of quick-freezing methods on the quality, moisture distribution and microstructure of prepared ground pork during storage duration.

The aim of present study was to investigate the influences of ultrasound-assisted immersion freezing (UIF), immersion freezing (IF) and air freezing (AF) on the quality, moisture distribution and microstructure properties of the prepared ground pork (PGP) during storage duration (0, 15, 30, 45, 60, 75 and 90 days). UIF treatment significantly reduced the freezing time by 60.32% and 39.02%, respectively, compared to IF and AF (P < 0.05). The experimental results of quality evaluation revealed that the L* and b* values, juice loss, cooking loss, TBARS values and carbonyl contents were decreased in the UIF treated samples, while the a* value, peak temperatures (Tm), enthalpy (ΔH) and sulfhydryl contents were significantly higher than those of IF and AF treated samples (P < 0.05). In addition, low-field nuclear magnetic resonance (LF-NMR) and differential scanning calorimetry (DSC) analysis demonstrated that UIF inhibited the mobility of immobilized water and reduced the loss of immobilized and free water, and then a high water holding capacity (WHC) was achieved. Compared to the IF and AF treatments, the UIF treated PGP samples possessed better microstructure. Therefore, UIF could induce the formation of ice crystals with smaller size and more even distribution during freezing process, which contributed to less damage to the muscle tissue and more satisfied product quality.

Preparation, characterization, antioxidant and anti-inflammatory activities of acid-soluble pectin from okra (Abelmoschus esculentus L.).

Currently, there are few studies on acid-soluble pectin from okra, especially in biological activity for antioxidant and anti-inflammatory. In this study, the antioxidant properties of acid-soluble okra pectin components and their anti-inflammatory were explored. Firstly, two acid-soluble okra pectic fractions, namely crude acid-soluble okra pectin (CAOP) and acid-soluble okra pectin (AOP), were obtained and exhibited structural and compositional variation. The two pectic fractions contained a low degree of esterification (42.0-46.5%) and a relatively high uronic acid content (31.6-37.3%). AOP was composed of galacturonic acid (79.1 mol/%), galactose (4.3 mol/%), rhamnose (14.5 mol/%) and xylose (2.1 mol/%), and the molecular weight was 92.8 kDa. Morphological and thermal properties of acid-soluble okra pectin components were also investigated. Compared to CAOP, AOP expressed better antioxidant activity, and suppressed the NO production in LPS-induced RAW 264.7 macrophages. All the above results indicated that AOP had the potential to act as a natural antioxidant or a functional anti-inflammatory food, which would broaden the development and utilization of okra resources.

Computer simulation aided preparation of molecularly imprinted polymers for separation of bilobalide.

In this study, the preparation of molecularly imprinted polymers for bilobalide (BBMIPs) was successfully achieved by bulk polymerization with methacrylamide (MAM), trimethylolpropane triacrylate (TMPTA), and acetonitrile (ACN) as functional monomer, cross-linker, and solvent, respectively. After Gaussian software simulation and single factor experiments, the prepared MIPs with a molar ratio of 1:4:15 for BB-MAM-TMPTA were systematically characterized. The hydrogen bonding interaction between BB and MAM was confirmed by a combination of FTIR and NMR analysis. Thermal gravimetric analysis results displayed that MIPs have excellent thermal stability under high temperature. Additionally, the average pore size and surface area of MIPs were found to be higher than those of NIPs through nitrogen adsorption results. The results of static adsorption and kinetic adsorption suggested that the adsorption equilibrium concentration was 0.6 mg/mL and the equilibrium time was 5 h, and the Langmuir and pseudo-second-order kinetic models were proven to fit with static and kinetic adsorption behaviors, respectively. Meanwhile, the selective adsorption study revealed that MIPs show high adsorption and great selectivity towards BB in comparison with other substances having similarly structure. MIPs also possessed a good performance on reusability, maintaining a high recovery rate after being reused 5 times. The application experiment further indicated that MIPs can effectively separate BB from low purity samples. Therefore, the prepared MIPs had a great potential for BB separation.

Purification, characterization and anti-fatigue activity of polysaccharide fractions from okra (Abelmoschus esculentus (L.) Moench).

The aim of this study was to investigate the anti-fatigue activity of polysaccharide fractions from Abelmoschus esculentus (L.) Moench (AE) in mice. After crude polysaccharide (CAEP) was extracted from AE and purified by DEAE cellulose-52 column, two polysaccharide fractions (AEP-1 and AEP-2) were obtained. The structural analysis suggested that AEP-1 and AEP-2 were a RG-I polysaccharide and an AG-II polysaccharide, respectively. According to the results of the weight-loaded swimming test, compared with the negative control group, the CAEP, AEP-1 and AEP-2 treatment groups could prolong the swimming time, decrease serum urea nitrogen (SUN) and blood lactic acid (BLA), and increase hepatic glycogen (HG) and muscle glycogen (MG), which indicated that okra polysaccharides have an effective anti-fatigue activity. Furthermore, our study exhibited the anti-fatigue mechanism of okra polysaccharide was correlated with retarding the accumulation of creatine kinase (CK) and lactate dehydrogenase (LDH) in serum, and enhancing succinate dehydrogenase (SDH), adenosine triphosphate (ATP) and adenosine triphosphatase (ATPase) levels. In addition, the anti-fatigue activity of AEP-1 was stronger than that of AEP-2, and significantly better than that of CAEP. Therefore, AEP-1 and AEP-2 may be the main active anti-fatigue functional substances of AE.

Enhancement of brain-targeting delivery of danshensu in rat through conjugation with pyrazine moiety to form danshensu-pyrazine ester.

Tetramethylpyrazine was introduced to the structure of danshensu (DSS) as P-glycoprotein (P-gp)-inhibiting carrier, designing some novel brain-targeting DSS-pyrazine derivatives via prodrug delivery strategy. Following the virtual screening, three DSS-pyrazine esters (DT1, DT2, DT3) were selected because of their better prediction parameters related to brain-targeting. Among them, DT3 was thought to be a promising candidate due to its appropriate bioreversible property in vitro release assay. Further investigation with regard to DT3's brain-targeting effects in vivo was also reported in this study. High-performance liquid chromatography-diode array detection (HPLC-DAD) method was established for the quantitative determination of DT3 and DSS in rat plasma, brain homogenate after intravenous injection. In vivo metabolism of DT3 indicated that it was first converted into DT1, DT2, then the generation of DSS, which could be the result of carboxylesterase activity in rat blood and brain tissue. Moreover, the brain pharmacokinetics of DT3 was significantly altered with 2.16 times increase in half-life compared with that of DSS, and its drug targeting index (DTI) was up to 16.95. Above these data demonstrated that DT3 had better tendency of brain-targeting delivery, which would be positive for the treatment of brain-related disorders.

A recyclable electrochemical allylation in water.

To develop environmentally benign processes for C-C bond formation, electrochemistry is applied in a tin-mediated allylation reaction in water. In this electrochemical process, the corresponding homoallylic alcohols are prepared in excellent yields, while both tin salt and water can be recycled and electrode materials are not consumed.