Comparison study of chitosan/β-cyclodextrin and carboxymethyl chitosan/β-cyclodextrin microspheres

To compare two microspheres of chitosan/β-cyclodextrin and carboxymethyl chitosan/β-cyclodextrin loaded theophylline as pulmonary sustained drug delivery carriers, the characteristics and ciliotoxicity were studied. The drug loadings of chitosan/β-cyclodextrin and carboxymethyl chitosan/β-cyclodextrin microspheres were 21.09% and 21.42%, and the encapsulation efficiencies were 91.40% and 92.80%. The distributions of 50% (d _0.5) of chitosan/β-cyclodextrin and carboxymethyl chitosan/β-cyclodextrin microspheres were 4.89 and 5.83 μm, respectively. Both microspheres showed spherical shape with smooth or wrinkled surfaces. FT-IR of chitosan/β-cyclodextrin microspheres demonstrated that theophylline had formed hydrogen bonds with chitosan and β-cyclodextrin, while for the carboxymethyl chitosan/β-cyclodextrin microspheres theophylline had interaction with carboxymethyl chitosan. The moisture absorption showed that an equilibrium was reached within 24 h. The two microspheres possessed better adaptability. In vitro release of theophylline from chitosan/β-cyclodextrin microspheres was slower than that from carboxymethyl chitosan/β-cyclodextrin microspheres at pH 6.8. Biography: LI Ruobao(1968–), male, Associate professor, research direction: foundation research of respiratory system.     

Formation of the inclusion complex of Orange II with β-Cyclodextrin and its photostability

Inclusion complex of Orange II with β-Cyclodextrin (β-CD) and the anti-photolysis effect under UV-light were investigated. The molar ratio of inclusion complex of β-Cyclodextrin and Orange II is 1∶1. The formation constantK = 1.236×10³ L/mol was determined by the UV and Fluorescence spectra respectively, which was quite in accordance with the calculation with a modified Benesi-Hildbrand equation. The inclusion complex was characterized by the IR spectra and the molar ratio of inclusion complex is 1∶1 too. The formation constantK = 1.266×10³ L/mol was determined by¹H NMR analysis and was nearly the same by UV and fluorescence spectra. The photocatalytic decolorization rate of Orange II solutions containing β-CD and TiO₂ was smaller by 51.9% than that of the Orange II solutions only containing TiO₂, while in the case of direct photolysis of Orange II solutions, β-CD can lower the photolysis rate by 48.1% under UV-light. This result indicates β-CD can inhibit the photolysis and photocatalytic decolorization of Orange II under UV-light. The β-CD inclusion complex was found to be persistent to UV-light photolysis. Foundation item: Supported by the National Natural Science Foundation of China (20177017) Biography: Lu Ping (1958), male. Associate professor, research direction: environmental photochemistry.     

Preparation of (R)- and (S)-2-Allyl-1, 3, 2-dinaphtho (α, β) [d.f] dioxaborepin and their reactions with aldehydes

(R)- and(S)-2-Allyl-1,3,2-dinaphtho (α,β) [d.f] dioxaborepin ((R)-2 and(S)-2) have been first prepared by the reaction of(R)-(+)- or(S)-(−)-1, 1′-bi-2-naphthol and triallylborane in THF at room temperature, respectively.(S)-2 and(R)-2 are sensitive to moisture and oxygen in air and disproportionate easily to triallylborane and 1,1′-bi-2 naphthyl bis (1,1′-bi-2-naphtholborate) at ambient temperature. However, THF is a stabilizer for them. The reactions of(R)-2 or(S)-2 and some aliphetic or aromatic aldehydes in CH₂Cl₂ at −78°C for several hours afforded β-alkylenyl alcohols in up to 84.8%ee. Among them, optically active 1-(3, 5-dichlorophenyl)-3-butenol and 1-(2-methoxyphenyl)-3-butenol were first prepared Foundation item: Supported by the National Natural Science Foundation of China (29972033) Biography: Liu Dejun (1973), male, Ph. D, research direction: asymmetric synthesis     

Synthesis,Structure and Antitumor Activities of [Ni（dien）2][Ni（CN）4] Complex

Ni(II)-dien complex was prepared and characterized by X-ray diffraction. The crystal belongs to triclinic system, space group P-1, with crystallographic parametersa=0.888 13(18) nm,b=0.890 10(18) nm,c=1. 591 8(3) nm, α=77.71(3)°, β=89.12(3)°, γ=61.24(3)°,Z=2. The two dien molecules coordinate to the central Ni atom, the six nitrogen atoms form a distorted octahedron. Preliminary pharmacological tests showed this complex had antitumor activity against HepG₂ and HL-60 cell linesin vitro. Foundation item, Supported by the National Natural Science Foundation of China (29972034) Biography: Li Tao (1976-), male, Ph. D candidate, research direction: ophthalmology and chemicalbiology.     

Early Renal Morphological Changes in High-Cholesterol Diet Rats Model

In rats fed with high-cholesterol （HC） chow, the renal specimens were investigated by microscopy and enzymehistochemistry. The levels of serum lipids, 24 h urinary protein excretion （ UPE ）, N-acetyl-β-D-glucosaminidase （NAG） and Nitric Oxide （NO） were evaluated. Histological examination showed cell swelling, break-down and massive lipid deposition in renal tubules; perivascular and interstitial cell infiltration and mesangial cell proliferation. Enzymehistochemistry demonstrated that lactate dehydrogenase （LDH） activity in proximal tubular epithelial cells increased but succino dehydrogenase （SDH） activity decreased. The NO level in serum, urine and renal cortex were all decreased （p〈0.01）. Urinary NO, was negatively correlated with urinary NAG and UPE （r is -0. 525, 0. 529 respectively, p〈0.01）. This study shows that a HC diet can induce the early morphological changes in the whole kidney, particularly in the renal tubules. The decrease of NO is associated with the pathogenesis of hypercholesterolemia-induced renal injury.     

Research of Inclusion Complexation of 4,4＇-Thiodiphenol Effected by β-Cyclodextrin in Aqueous Solutions and the Effect on Photodegradation

The inclusion behavior of 4, 4＇ -Thiodiphenol （TDP）, a typical bisphenol and endocrine disruptor, reacts with β-cyclodextrin （β-CD） in aqueous solutions has been investigated by means of UV absorption spectrum and quantum-chemical calculation with Gaussian 98 software. The results show that the inclusion behavior of TDP is quite different in acidic solutions （pH 5.9） from that in alkaline solutions （pH 10.0）. This behavior difference is attributed to the different formula structures in aqueous solutions at acidic and alkaline pH values that are demonstrated by quantum- chemical modeling and calculation. TDP forms a 1 ： 1 fl-CD inclusion complex in aqueous solutions. The equiiibrium constant K was calculated to be 553.49 L/mol at pH 5.9 and 1 318.20 L/mol at pH 10.0 respectively for the inclusion complex reaction by using the modified Benesi-Heldbrand equation. After inclusion TDP＇s structure is changed especially at the inclusion part with the bond order becoming larger, which results in inhibitive photodegradation during direct photooxidation and H2O2 assisted photooxidation.     

Synthesis and Characterization of Polyamide-Containing 2, 6- （Substituded） pyridine Derivatives

0 IntroductionPayrriodminaetiics hoenteer oofc ythcleics m .os tC oambupnoduanndts a cnodn tbaeisntin kgno twhnepyridine ring are widely distributedin nature,principally asenzymes and alkaloids . Pyridine enzymes have been foundintissues of all plants and ani mals examined thus far ,andare derivedfromeither nicotinic acid or Vitamin B6[1].Pyr-idine derivatives are also the building block of many phar-maceuticals with a wide range of functionalities that includeantitubercular compounds ,antivi…     

NMR and IR investigations of ternary inclusion complexes among β-cyclodextrin, rare earth metal ions, and naphthalenediamines

Ternary inclusion complexes β-cyclodextrin (β-CD), rare earth metal ions (YbCl₃, YCl₃), and 1,8-naphthalene- diamine/1,5-naphthalenediamine are synthesized in basic aqueous media, which are characterized via ¹H NMR and IR spectroscopy. The stoichiometric proportion of β-CD:YbCl₃:1,5-naphthalenediamine is 2:1:2, that of β-CD:YCl₃:1,8-naphthalenediamine is 2:1:1, and that of β-CD:YbCl₃:1,8-naphthalenediamine is 2:1:1. The IR spectroscopy of the ternary inclusion complexes in the range of 935–1 000 cm⁻¹ reveals the existence of the coordinate bond M—O or M—N. The possible conformations of the ternary inclusion complexes are depicted. Biography: JIANG Huiming(1972–), male, Associate professor, research direction: molecular complex chemistry, supramolecular chemistry.     

Existence of single-peaked solution of a semilinear elliptic problem

We discussed the Dirichlet problem of semilinear elliptic equationin (Pβ,α)D;-β△u=uε+εu,u>0,in Ω u=0, on(e),Ω where Ω(∪)RN(N≥4) is smooth and bounded domain,P=N+2/N-2,β,ε>0. We have proved that there exist positive ε0 and ε1 , such that when 0≤ε≤ε0,β>√ε1,(P0,1)has a single-peaked solution uβ, furthermore, |▽μβ|-0in the sense of measure as ε→0 and β→0.     

Spectrofluorimetric method for the determination of triamcinolone acetonide

0　IntroductionTriamcinoloneAcetonide,9 fluoro 11β,2 1 dihydroxy 16α,17[(1 methylethylidene)bis (oxy) ] pregn 1,4 diene 3,2 0 dione,Mris 4 34.4 8(abr.TA ) .Itbelongstoaclassofadrenalcortexhormonedrug ,whosefunctionsareaffectionofsugarmetabolism ,anti inflammationandresistancehypersusceptibilityetc.TAcanbesuitabletorheumatoidarthritisanddermatosissuchashypersusceptibilityandneuropathicdermatitis .ThefunctionsofTAisstrongerandlongerthantriamcinolone[1 ,2 ] .ThecommonmethodsofdetectingTAm…