摘要：Microneedles(MNs)are an innovative and viable option for drug delivery that offer the distinct advantages of minimal invasiveness,painlessness,stable drug loading,efficient drug permeation,and *** were first used to penetrate the skin surface and facilitate transcutaneous drug delivery with great *** applications of MNs have extended to non-transdermal drug delivery,specifically,to various tissues and *** review captures the fabrication methods for MNs,discusses advanced design strategies for achieving controlled drug release,and summarizes current MN applications in delivering multiple therapeutic agents to the cardiovascular,digestive(e.g.,oral cavity),reproductive,and central nervous *** findings in this review would contribute toward the improved designs of MN systems that can be modified according to purpose,including material selection,structural design,choice of fabrication methods,and tissue considerations,to determine the optimal therapeutic regimen for the target treatment area.

摘要：Obesity has become a global threat to health;however,the available drugs for treating obesity are *** investigated the anti-obesity effect of hydroxy-α-sanshool(HAS),an amide derived from the fruit of Zanthoxylum bungeanum,which promotes the management of obesity by triggering the browning of white adipose tissue(WAT)targeting the membrane receptor of transient receptor potential vanilloid 1(TRPV1).However,HAS easily undergoes configuration transformation and oxidative *** short peptide CKGGRAKDC or adipose-targeting sequence(ATS)binds specifically to prohibitin on the surface of WAT cells and can be used as recognition assembly to enhance adipocyte ***,mesoporous silica nanoparticles(MSNs)are widely used in drug delivery systems because of their large specific surface area and pore ***,HAS-loaded adipose-targeted MSNs(MSNs-ATS)were developed to enhance the adipocyte targetability,safety,and efficacy of HAS,and tested on mature 3T3-L1 cells and obese mouse ***-ATS showed higher specificity for adipocyte targetability without obvious ***-loaded MSNs-ATS showed anti-obesity effects superior to those of HAS *** conclusion,we successfully developed adipocyte-targeted,HAS-loaded MSNs with good safety and anti-obesity effects.

摘要：Acidic oligosaccharide sugar chain （AOSC）, a D-mannuronic acid oligosaccharide, derived from brownalgaepolysaccharide, has been completed Phase I clinical trial in China as an anti-Alzheimer＇s Disease （AD） drug candidate. The identification of AOSC-binding protein（s） in neurons is very important for understanding its action mechanism. To determine the binding protein（s） of AOSC in neurons mediating its anti-AD activities, confocal microscopy, affinity chromatography, and liquid chromatography-tandem mass spectrometry （LC-MS/MS） analysis were used. Confocal microscopy analysis shows that AOSC binds to SH-SY5Y cells in concentration-, time-, and temperature-dependent fashions. The AOSC binding proteins were purified by affinity chromatography and identified by LC-MS/MS analysis. The results showed that there are 349 proteins binding AOSC, including clathrin, adaptor protein-2 （AP-2） and amyloid precursor protein （APP）. These results suggest that the binding/entrance of AOSC to neurons is probably responsible for anti-AD activities.

摘要：A series of 3-substituted quinazolinones,2-substituted quinoxalines and 2-substituted benzopyrans were synthesized and evaluated for their antifungal activity in *** new compounds revealed excellent in vitro antifungal activity with broad *** structure-activity relationships（SARs） of the derivatives were *** 9A2 exhibits better antifungal activity against 5 tested fungi in vitro than fluconazole,especially against Trichophyton rubrum and Microsporum *** study provides a series of novel lead compounds for the development of non-azole antifungal agents.

摘要：Hydrophobic fluorescence:Tan and his colleagues recently introduced a brand new chemotype of environment-sensitive fluorescent turn-on probes to detect the hydrophobic ligand-binding domain by using SBD *** design strategy described in this report generalized the environment sensitivity turn-on mechanism to recognize a specific protein,which provides a robust breakthrough for interchanging fluorescence in conventional small-molecule fluorescent imaging.

摘要：A novel series of eight SMS and sPLA2 dual inhibitors containing indole and a-amino cyanide fragments of different length and substitution position was synthesized and evaluated by three different in vitro assays. Biological evaluation showed that all compounds provided inhibitory effects against SMS （about 50% inhibition at 100 μmol/L） and sPLA2 （14-32 μmol/L）. All the compounds had the SMS activity better than the positive control compound D609 in SMS2 homogenate, with compounds 5b and fie ideal for liver homogenate and SMS2 high expression cell homogenate, respectively.

摘要：Several novel fluorescent probes targeting α_1-adrenergic receptors were well designed and synthesized by conjugating phenylpiperazine pharmacophore with coumarin and fluorescein fluorophores. These compounds showed suitable fluorescence property, high receptor affinity, and low cytotoxicity. Moreover, the cell imaging results displayed that these probes can be effective tools for the real-time detection of ligand-receptor interactions, as well as the visualization and location of α_1-adrenergic receptors in living cells.

摘要：By integrating photoinduced electron transfer（PET） into the design of functional bioluminogenic probes,Urano and his coworkers recently developed a new rational design strategy, BioLeT. It is expected that this BioLeT strategy will enable us to design and develop new bioluminescence probes for detecting various biomolecules with no catalytic or reactive activity.

摘要：A new series of isatin semicarbazide derivatives（7a-7j） were synthesized and characterized by spectroscopic means and elemental *** and anti-inflammatory screening was performed using tail-flick technique and the carrageenan-induced foot paw edema test *** ulcerogenicity was also determined for all the *** of the compounds showed moderate enhancement of the *** the synthesized derivatives,compound 7d showed higher analgesic, antiinflammatory and one-third of ulcer index of the reference drug.

摘要：Gatifloxacin eye drops are frequently used in eye *** such formulations have a major drawback *** duration of action and usually require 4e6 times installations daily.A chitosan coated niosomal formulation of gatifloxain was purposed to show a longer retention time on eyes and subsequent reduction in dosing *** were prepared by solvent injection method using cholesterol and *** extensive optimization of formulation was done using different ratios of cholesterol,Span-60 and drug,revealed NS60-5(cholesterol:span-6050:50 and drug content of 20 mg)to be the optimized niosome ***60-5 had shown a highest entrapment efficiency of 64.9±0.66%with particle size 213.2±1.5 nm and zeta potential
34.7±2.2 *** niosomes were also coated with different concentrations of chitosan and *** studies had revealed that optimized niosomes(86.77±1.31%)had increased the transcorneal permeation of Gatifloxacin more than two fold than simple drug solution(37.19±1.1%).Longer retention potential of the coated niosomes was further verified by fluorescence *** revealed that simple dye solution got easily washed out with in 6 *** uncoated niosomes(NS60-5)showed a longer retention(more than 6 h),which was further enhanced in case of coated niosomes ***60-1(more than 12 h).Antimicrobial studies had shown the better efficacy of CNS60-1(zone of inhibition)when compared to marketed *** final chitosan formulation was found to have shown better ocular tolerability as demonstrated by corneal hydration test histopathology investigations.