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1.
Biochem Genet ; 2024 Feb 20.
Article in English | MEDLINE | ID: mdl-38379038

ABSTRACT

Propofol has been found to have a protective effect against spinal cord injury (SCI). However, the underlying molecular mechanism of propofol regulating SCI process remains unclear. In this study, lipopolysaccharide (LPS)-induced PC12 cells were used to build SCI cell models. Cell viability and apoptosis were determined by cell counting kit 8 assay, flow cytometry, and caspase-3 activity detection. The protein levels of apoptosis-related markers and TNFAIP3 interacting protein 2 (TNIP2) were assessed using western blot analysis, and the levels of inflammatory factors were detected using ELISA. Cell oxidative stress was evaluated by measuring malondialdehyde (MDA) and reactive oxygen species (ROS) levels. The expression of microRNA (miR)-672-3p was examined by quantitative real-time PCR. SCI rat models were constructed to assess the effect of propofol in vivo. We found that propofol treatment promoted viability, while inhibited apoptosis, inflammation and oxidative stress of LPS-induced PC12 cells. Propofol decreased miR-672-3p expression, and miR-672-3p overexpression eliminated the inhibiting effect of propofol on LPS-induced PC12 cell injury. Besides, miR-672-3p targeted TNIP2, and TNIP2 knockdown reversed the protective effect of miR-672-3p inhibitor or propofol against LPS-induced PC12 cell injury. In vivo experiments, propofol treatment enhanced the motor function recovery and inhibited apoptosis of SCI rat models. In conclusion, propofol increased TNIP2 level by reducing miR-672-3p expression, thereby alleviating LPS-induced PC12 cell injury and improving the motor function of SCI rat models.

2.
Phys Chem Chem Phys ; 25(33): 22002-22010, 2023 Aug 23.
Article in English | MEDLINE | ID: mdl-37555282

ABSTRACT

Understanding the functional group modulation of electronic structure and excitation is pivotal to the design of organic small molecules (OSMs) for photoelectric applications. In this study, we employed density functional theory (DFT) and time-dependent DFT (TDDFT) calculations to explore the unique absorption character of four triphenylamine photosensitizers. The various conformations were investigated given the multiple single bonds in the compounds, and the resemblance in the electronic structure of different conformations is affirmed because the coplanarity and consequent long-range conjugation is maintained regardless of the orientation of the flexible blocks. Six functionals were evaluated, and MN15 was found to successfully reproduce the intense secondary absorption peak for the double 3,4-ethylenedioxythiophene (EDOT) modified sensitizer over B3LYP, PBE0, M062X, CAM-B3LYP, and ωB97XD. The introduction of EDOT gives rise to a new excited state S4, which is a local excitation constrained in the EDOT substituent triphenylamine block. This new excited state S4, in combination with inherent S2 and S3 derived from prototype molecule TPA-Pyc, jointly contributes to the hump of the secondary absorption peak of ETE-Pyc and finally affects the light-harvesting ability of the dye-sensitized TiO2 photoanode. The current findings provide guidance toward the rational design of OSMs with good light-harvest ability.

3.
Adv Mater ; 35(44): e2304820, 2023 Nov.
Article in English | MEDLINE | ID: mdl-37459472

ABSTRACT

Amorphous organic long-persistent luminescence materials (OLPLMs) can realize simpler solution processing and large-area uniform luminescence, where the luminescent properties are significantly influenced by the rigid environment. However, research on utilizing the rigidity to promote long-persistent luminescence (LPL) properties of amorphous OLPLMs is still relatively rare due to the lack of an unambiguous and effective strategy to construct the rigid environment. Here, a universal strategy is proposed to enhance the LPL performance of organic host-guest doping systems by UV curing, which utilizes the rigid environment constructed by UV curing to promote the interaction between host and guest, thus inducing a generation of materials with highly efficient LPL performance. This solution-processable, large-area, and "easy-to-realize" material fabrication strategy can make amorphous OLPLMs show broader application prospects in some fields, such as anti-counterfeiting, nondestructive detection, and pattern marking or indication.

4.
Molecules ; 28(7)2023 Apr 06.
Article in English | MEDLINE | ID: mdl-37050045

ABSTRACT

A series of aggregation-induced emission (AIE)-featured phenylmethylene pyridineacetonitrile derivatives named o-DBCNPy ((Z)-3-(4-(di-p-tolylamino)phenyl)-2-(pyridin-2-yl)acrylonitrile), m-DBCNPy ((Z)-3-(4-(di-p-tolylamino)phenyl)-2-(pyridin-3-yl)acrylonitrile), and p-DBCNPy ((Z)-3-(4-(di-p-tolylamino)phenyl)-2-(pyridin-4-yl)acrylonitrile) have been synthesized by tuning the substitution position of the pyridine ring. The linkage manner of the pyridine ring had influences on the molecular configuration and conjugation, thus leading to different photophysical properties. The absorption and fluorescence emission peak showed a bathochromic shift when the linking position of the pyridine ring changed from the meta to the ortho and para position. Meanwhile, o-DBCNPy exhibited the highest fluorescence quantum yield of 0.81 and the longest fluorescence lifetime of 7.96 ns as a neat film among all three isomers. Moreover, non-doped organic light-emitting diodes (OLEDs) were assembled in which the molecules acted as the light-emitting layer. Due to the relatively prominent emission properties, the electroluminescence (EL) performance of the o-DBCNPy-based OLED was superior to those of the devices based on the other two isomers with an external quantum efficiency (EQE) of 4.31%. The results indicate that delicate molecular modulation of AIE molecules could endow them with improved photophysical properties, making them potential candidates for organic photoelectronic devices.

5.
Thorac Cancer ; 14(17): 1606-1617, 2023 06.
Article in English | MEDLINE | ID: mdl-37105940

ABSTRACT

BACKGROUND: Circular RNAs (circRNAs) are associated with propofol-mediated inhibitory effect on non-small cell lung cancer (NSCLC) progression. Circular hsa_circ_0003028 (circ_0003028) exerts a tumor-promoting role in NSCLC. However, it is unclear whether propofol can mediate NSCLC progression via regulating circ_0003028 expression. METHODS: A total of 36 NSCLC patients were recruited in the study. Cell viability, proliferation, apoptosis, migration, and invasion were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), colony formation, flow cytometry, and transwell assays. Relative expression of circ_0003028 in NSCLC samples and cells was detected by quantitative real-time polymerase chain reaction (RT-qPCR). Analysis of the latent binding of circ_0003028 to miR-1305 was done by bioinformatic analysis and confirmed by luciferase reporter and RNA immunoprecipitation (RIP) assays. Xenografting in mice was done to verify the relationship between propofol and circ_0003028. RESULTS: Significant upregulation of circ_0003028 was detected in NSCLC samples and cells. Functionally, propofol treatment reduced circ_0003028 expression in NSCLC cells, and circ_0003028 overexpression impaired propofol-mediated inhibitory effect on NSCLC cell proliferation, migration, and invasion. Interestingly, circ_0003028 could compete with miR-1305 as a competing endogenous RNA and upregulate CORO1C expression in NSCLC cells. CONCLUSION: Propofol-mediated inhibiting effect on NSCLC growth partly depended on the circ_0003028/miR-1305/CORO1C axis.


Subject(s)
Carcinoma, Non-Small-Cell Lung , Lung Neoplasms , MicroRNAs , Propofol , Humans , Animals , Mice , Apoptosis , Cell Proliferation
6.
Am J Transl Res ; 13(9): 10933-10941, 2021.
Article in English | MEDLINE | ID: mdl-34650774

ABSTRACT

OBJECTIVE: This study aimed to explore the application value of epidural and general anesthesia in total knee arthroplasty (TKA). METHODS: We first retrospectively analyzed 156 patients who underwent total knee arthroplasty in our hospital from January 2019 to January 2020 as subjects. The control group (CG) included 86 subject who were treated with general anesthesia. The remaining 70 subjects with epidural anesthesia were divided to a research group (RG). The recovery and adverse reactions after surgery were compared. The coagulation function before and after surgery was analyzed. The incidence of deep vein thrombosis (DVT) after surgery was observed. The expression of inflammatory factors and the improvement of cognitive function were assessed before surgery, followed by 6 and 12 h after surgery. The pain degree of patients was compared at 6 and 12 h after surgery. RESULTS: Compared with the CG, the recovery condition after surgery in the RG were dramatically lower, the concentrations of PLT, PT, and APTT in the RG were higher, while FBG was markedly lower. The incidence of postoperative venous thrombosis in the RG was lower. The TNF-α, IL-6 levels, and VAS scores in the RG were remarkably lower at 6 and 12 h after surgery. MMSE score was significantly higher than CG score. The total incidence of adverse reactions in the RG was markedly lower. CONCLUSION: Epidural anesthesia can improve blood coagulation and cognitive function in patients undergoing TKA and reduce the incidence of DVT and the degree of postoperative pain.

7.
Anal Chim Acta ; 1153: 338278, 2021 Apr 08.
Article in English | MEDLINE | ID: mdl-33714447

ABSTRACT

Increased utilization of platinum ions in chemicals and drugs escalates environmental pollution and toxicity associated with Pt ions. However, current analysis and detection strategies of Pt ions display limited sensitivity due to the similar inert metal nature of platinum to gold. Herein, a photoinduced charge-separated molecule (MTPA)2Ab was synthesized as a probe for enhanced sensitive selection of Pt ions. Long-lived charge-separated states generated upon exposure to 365 nm light lead to a stable complex between (MTPA)2Ab and PtCl2/PtCl4 with highly-selectivity via sequential photoinduced electron transfers. Owing to the linear relationship of complex characteristic absorption and fluorescence emission intensities to Pt2+/Pt4+ concentrations, ultrasensitive spectrum analysis of Pt ions is achieved with a detection limit of 14.2 nM (2.8 ppb) for Pt2+ and 12.6 nM (2.5 ppb) for Pt4+ by an absorption spectrometer and 9.8 nM (1.9 ppb) for Pt ions (Pt2+/Pt4+) by a fluorescence spectrometer, far less than the reported values. Furthermore, a portable test box is developed based on (MTPA)2Ab test strips due to distinguishable color change with Pt2+/Pt4+ concentrations for rapid colorimetric detection of Pt ions. The results highlight the promise of photoinduced charge-separated molecular probe in ultrasensitive and rapid detection of Pt ions to overcome current limitations of detection strategies.

8.
Zhonghua Yi Xue Yi Chuan Xue Za Zhi ; 37(12): 1384-1386, 2020 Dec 10.
Article in Chinese | MEDLINE | ID: mdl-33306828

ABSTRACT

OBJECTIVE: To explore the clinical and genetic characteristics of a child featuring developmental delay. METHODS: The child was subjected to whole exome sequencing. Candidate variant was verified by Sanger sequencing. RESULTS: Whole genome sequencing revealed that the child has carried compound heterozygous variants c.2607-1G>C and c.899 + 2dupT of the RAB3GAP1 gene, which were respectively derived from her mother and father. CONCLUSION: A rare case of Warburg micro syndrome type 1 was diagnosed. The phenotype of the child was consistent with the literature, in addition with dysplasia of palatine arch, prominent high palatal arch and tooth dysplasia. Above finding has provided a basis for genetic counseling and prenatal diagnosis for the family.


Subject(s)
Abnormalities, Multiple , Cataract/congenital , Cornea/abnormalities , Hypogonadism , Intellectual Disability , Microcephaly , Optic Atrophy , rab3 GTP-Binding Proteins , Abnormalities, Multiple/genetics , Adult , Cataract/genetics , Child , Female , Humans , Hypogonadism/genetics , Intellectual Disability/genetics , Male , Microcephaly/genetics , Mutation , Optic Atrophy/genetics , Exome Sequencing , rab3 GTP-Binding Proteins/genetics
9.
Spectrochim Acta A Mol Biomol Spectrosc ; 229: 118016, 2020 Mar 15.
Article in English | MEDLINE | ID: mdl-31923789

ABSTRACT

In spite of the pivotal role of excited state electronic structures as regulation of photoinduced electron transfer (PET) process, the effect of excited state conformation on PET remains elusive. Here we exploit distinguishable emission characters of trans and cis singlet excited states of donor-acceptor-donor ensemble MTPAAZO to reveal that its PET efficiency and rate are closely depended on its singlet excited state conformation. The PET process occurs solely in cis conformation of MTPAAZO singlet excited states. Novel molecule (MTPA)2Ab as-designed with similar structure of MTPAAZO cis singlet excited states shows high PET efficacy and rate, leading to long-lived CS states. Our findings enable the rational design of the novel molecules with highly efficient PET process suitable for charge separation applications.

10.
Zhonghua Wei Zhong Bing Ji Jiu Yi Xue ; 30(5): 484-485, 2018 May.
Article in Chinese | MEDLINE | ID: mdl-29764557

ABSTRACT

OBJECTIVE: The common negative pressure drainage bottle used in the vacuum sealing drainage (VSD) cannot quantitative and automatically cut off. Excessive drainage damages the negative pressure source, causes drainage interruption, so once drainage was continuously performed, medical staff need to closely observe drainage bottle calibration. It was also important to known whether there was a large amount of fresh blood sucked out during continuous drainage because it could lose too much blood. To solve these two problems, we designed a kind of negative pressure drainage device, which volume was constant, with the function of automatic cutting off continuous drainage. It can not only prevent drainage fluid flowing back to the negative pressure source and cause drainage interruption, but also prevent massive blood loss from continued drainage after the hemorrhage. We could benefit from this device, which possess many advantages, such as simple structure, security and reliability. It is worthy promoting in the clinical work.


Subject(s)
Drainage , Negative-Pressure Wound Therapy , Pressure , Reproducibility of Results , Vacuum
11.
ACS Appl Mater Interfaces ; 9(11): 9880-9891, 2017 Mar 22.
Article in English | MEDLINE | ID: mdl-28256820

ABSTRACT

Effective charge separation is one of the key determinants for the photovoltaic performance of the dye-sensitized solar cells (DSSCs). Herein, two charge-separated (CS) sensitizers, MTPA-Pyc and YD-Pyc, have been synthesized and applied in DSSCs to investigate the effect of the CS states of the sensitizers on the device's efficiency. The CS states with lifetimes of 64 and 177 ns for MTPA-Pyc and YD-Pyc, respectively, are formed via the photoinduced electron transfer (PET) from the 4-styryltriphenylamine (MTPA) or 4-styrylindoline (YD) donor to the pyrimidine cyanoacrylic acid (Pyc) acceptor. DSSCs based on MTPA-Pyc and YD-Pyc exhibit high internal quantum efficiency (IQE) values of over 80% from 400 to 600 nm. In comparison, the IQEs of the charge transfer (CT) sensitizer cells are 10-30% lower in the same wavelength range. The enhanced IQE values in the devices based on the CS sensitizers are ascribed to the higher electron injection efficiencies and slower charge recombination. The results demonstrate that taking advantage of the CS states in the sensitizers can be a promising strategy to improve the IQEs and further enhance the overall efficiencies of the DSSCs.

12.
Neuromolecular Med ; 18(2): 232-8, 2016 Jun.
Article in English | MEDLINE | ID: mdl-27114095

ABSTRACT

Cerebral palsy (CP) is a neurological disorder affecting movement and posture that develops as a complication of prenatal, perinatal, and postnatal brain injury. Such non-progressive brain injury is often accompanied by neonatal encephalopathy and inflammation. The widely expressed soluble cytokine osteopontin (OPN) plays an important role in inflammation and neurological protection. Therefore, it is of great interest to study the relationship between CP and genetic variants of OPN. To explore the genetic association between OPN gene single nucleotide polymorphisms (SNPs) and CP in the Chinese Han population, five SNPs (rs2853744, rs2853749, rs11728697, rs4754, and rs1126616) were genotyped among 715 CP patients and 658 healthy controls using the MassArray platform. Statistical analysis was performed using the online SHEsis program, and Bonferroni correction was applied as necessary. We found an association between rs1126616 and global CP (corrected allelic P = 0.0006 and genotypic P = 0.0011 after Bonferroni correction). The other SNPs were not statistically associated with CP or any of its subgroups. By testing a relatively large sample size, our study demonstrates that the OPN gene SNP rs1126616 is statistically associated with CP. We suspect that the OPN gene might be a susceptibility factor for CP.


Subject(s)
Cerebral Palsy/genetics , Genetic Predisposition to Disease , Osteopontin/genetics , Case-Control Studies , China , Gene Frequency , Humans , Polymorphism, Single Nucleotide
13.
Zhongguo Zhen Jiu ; 36(1): 12-6, 2016 Jan.
Article in Chinese | MEDLINE | ID: mdl-26946726

ABSTRACT

OBJECTIVE: To compare the effects between moxibustion at Guanyuan (CV 4), Shenshu (BL 23), Zusanli (ST 36) and western medication on immune function in children with cerebral palsy. METHODS: A total of 230 children with cerebral palsy were randomly divided into an observation group and a control group, 115 cases in each one. Patients in the observation group were treated with warm moxibustion at Guanyuan (CV 4), Shenshu (BL 23) and Zusanli (ST 36). Patients in the control group were treated with oral administration of pidotimod 10 mL every time. The treatment was given once a day, and 30 days were considered as one session for total 90 days. The changes of T-lymphoctyte subgroups, serum immunoglobulin and development quotient were compared 30 days, 60 days and 90 days into treatment respectively; also the occurrence rate.of disease was observed during 6-month and 12-month follow-up visit. RESULTS: The T-lymphoctyte subgroups (CD3+, CD4+, CD4+/CD8+), serum immunoglobulin (IgG, IgA) and development quotient were significantly improved 30 days, 60 days and 90 days into treatment (P < 0.01, P < 0.05). Regarding the changes of CD3+, CD4+, CD4+/CD4+, IgG, IgA and development quotient, the control group was superior to the observation group 30 days into treatment (all P < 0.05), and the control group was similar to the observation group 60 days into treatment (all P > 0.05), and the observation group was superior to the control group 90 days into treatment (all P < 0.05). There was no significant difference of CD8+ and IgM before and after treatment in two groups (all P > 0.05). The rate of adverse events was 7.0% (8/115) in the observation group, which was lower than 23.5% (27/115) in the control group (P < 0.01); during 6-month and 12-month follow-up visit, the occurrence rate of disease in the observation group was lower than that in the control group (P < 0.05). CONCLUSION: Moxibustion at Guanyuan (CV 4), Shenshu (BL 23) and Zusanli (ST 36) can improve immune function of children with cerebral palsy, which is superior to pidotimod.


Subject(s)
Cerebral Palsy/immunology , Cerebral Palsy/therapy , Moxibustion , Acupuncture Points , Child, Preschool , Female , Humans , Immunoglobulin A/immunology , Immunoglobulin G/immunology , Infant , Male , T-Lymphocyte Subsets/immunology , Treatment Outcome
14.
J Inorg Biochem ; 125: 9-15, 2013 Aug.
Article in English | MEDLINE | ID: mdl-23665090

ABSTRACT

Tiopronin, a synthetic thiol-containing drug being used in treatments of cystinuria and certain types of rare arthritis, is also a hepatoprotective and a detoxifying agent. Many analytical methods have been developed based on its redox chemistry with metal ions/complexes, but the kinetic and mechanistic aspects are poorly understood. In this work, the oxidation of tiopronin by cisplatin prodrug and a model compound, cis-[Pt(NH3)2Cl4] and trans-[PtCl2(CN)4](2-), was investigated. The oxidation kinetics was followed by a stopped-flow spectrophotometer over a wide pH range under the pseudo first-order conditions of [Tiopronin]≫[Pt(IV)]. Time-resolved spectra were also recorded for both Pt(IV) complexes, enabling to establish an overall second-order rate law: -d[Pt(IV)]/dt=k'[Tiopronin][Pt(IV)], where k' pertains to observed second-order rate constants. Under the kinetic conditions, tiopronin was oxidized to form the tiopronin-disulfide exclusively as identified by mass spectrometry. A reaction mechanism was proposed, involving parallel reductions of the Pt(IV) complexes by the three protolytic tiopronin species as rate-determining steps. The rate constants for the rate-determining steps were derived. The fully deprotonated tiopronin is about 4×10(4) more reactive than its corresponding thiol form for both Pt(IV) complexes; the huge reactivity difference orchestrates closely with the fact that the nucleophilicity of thiolate is much higher than the corresponding thiol. Hence, the attack of the sulfur atom in thiol/thiolate of tiopronin on the axially-coordinated chloride in the Pt(IV) complexes is nucleophilic in nature in the rate-determining steps, resulting in a bridge formation and a subsequent bridged electron-transfer.


Subject(s)
Organoplatinum Compounds/chemistry , Tiopronin/chemistry , Cisplatin/chemistry , Hydrogen-Ion Concentration , Kinetics , Mass Spectrometry , Oxidation-Reduction , Prodrugs/chemistry
15.
J Phys Chem B ; 116(22): 6522-8, 2012 Jun 07.
Article in English | MEDLINE | ID: mdl-22574871

ABSTRACT

Thioredoxins are small redox proteins and have the active sites of Cys-Xaa-Yaa-Cys; they are overexpressed by many different cancer cells. Cisplatin and Pt(II) analogues could bind to the active sites and inhibit the activities of the proteins, as demonstrated by other researchers. Platinum(IV) anticancer drugs are often regarded as prodrugs, but their interactions with thioredoxins have not been studied. In this work, 3,6-dioxa-1,8-octanedithiol (dithiol) was chosen as a model compound for the active sites of thioredoxins, and its reactions with cis-[Pt(NH(3))(2)Cl(4)] and trans-[PtCl(2)(CN)(4)](2-) (cisplatin prodrug and a model complex) were studied. The pK(a) values for the dithiol were characterized to be 8.7 ± 0.2 and 9.6 ± 0.2 at 25.0 °C and an ionic strength of 1.0 M. The reaction kinetics was followed by a stopped-flow spectrophotometer over a wide pH range. An overall second-order rate law was established, -d[Pt(IV)]/dt = k'[Pt(IV)][dithiol], where k' stands for the observed second-order rate constants. Values of k' increased several orders of magnitude when the solution pH was increased from 3 to 9. A stoichiometry of Δ[Pt(IV)]/Δ[dithiol] = 1:1 derived for the reduction process and product analysis by mass spectrometry indicated that the dithiol was oxidized to form an intramolecular disulfide, coinciding with the nature of thioredoxin proteins. All of the reaction features are rationalized in terms of a reaction mechanism, involving three parallel rate-determining steps depending on the pH of the reaction medium. Rate constants for the rate-determining steps were evaluated. It can be concluded that Pt(IV) anticancer prodrugs can oxidize the reduced thioredoxins, and the oxidation mechanism is similar to those of the oxidations of biologically important reductants by some reactive oxygen species (ROS) such as hypochlorous acid/hypochlorite and chloramines.


Subject(s)
Antineoplastic Agents/chemistry , Ethyl Ethers/chemistry , Organoplatinum Compounds/chemistry , Platinum/chemistry , Prodrugs/chemistry , Sulfhydryl Compounds/chemistry , Kinetics , Models, Molecular , Molecular Structure , Oxidation-Reduction
16.
J Pharm Sci ; 99(7): 2991-8, 2010 Jul.
Article in English | MEDLINE | ID: mdl-20091820

ABSTRACT

The aim of this work was to evaluate the low molecular weight chitosans (LMWCs) as enhancers of transdermal administration of baicalin, an useful drug for the treatment of atopic dermatitis, viral hepatitis, and HIV infection. Permeation experiments were performed in vitro through mouse skin by using Franz cells. Improved baicalin skin penetration was obtained with the addition of LMWCs or D-glucosamine (beta-D-GlcNH(2)) to the donor solutions. Chitosan molecular weight, degree of deacetylation, pH of donor baicalin solutions, and enhancer concentration all affected LMWC enhancement effects. Significant enhancement was observed at pH 7.0 or 7.5 for CS80-1000, and the enhancement factor (EF) in the co-delivery method was calculated as 11.7 or 15.9, respectively. Simultaneously, beta-D-GlcNH(2) showed greatest enhancement at pH 7.0 with an EF of 11. Moreover, there was an optimal concentration range (0.5-1% by weight for CS80-1000 and 1.0-1.5% for beta-D-GlcNH(2)) to enhance baicalin transdermal delivery. It was concluded that the effective fractions for the enhancement of LMWCs were beta-D-GlcNH(2) oligomers, and the repeated number of beta-D-GlcNH(2) was suggested to be in the range 2-6. Enhancement mechanism of LMWCs was also discussed and suggested to be relative to the interactions of LMWC with both baicalin and the lipid of stratum corneum.


Subject(s)
Anti-Infective Agents/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Chitosan/metabolism , Flavonoids/administration & dosage , Skin Absorption , Skin/metabolism , Administration, Cutaneous , Animals , Chitosan/chemistry , Drug Delivery Systems , Mice
17.
J Biomater Sci Polym Ed ; 20(4): 529-42, 2009.
Article in English | MEDLINE | ID: mdl-19228452

ABSTRACT

The aim of this work was to evaluate the feasibility and efficacy of flexible adhesive electrodes (FAEs) prepared with adhesive matrices for iontophoretic delivery of baicalin, a drug used for the treatment of atopic dermatitis, viral hepatitis and HIV. Single-layer adhesive matrices (SLAMs) and double-layer adhesive matrices (DLAMs) were prepared from carbomer 940, sodium alginate and polyvinyl alcohol with appropriate mechanical and high baicalin release properties. During the direct-current (DC) iontophoresis with SLAM FAEs, electrochemical reaction caused a clear decrease of pH value at the interface IF(+,FCL) and an increase of pH value at the interface IF(-,FCL). An additional pH-controlling layer in DLAMs could adjust the pH value of interfaces. Thus, deterioration of baicalin stability and the competitive delivery of hydroxyl ions produced with baicalin anions would be avoided during iontophoresis. Iontophoretic flux of baicalin from a DLAM FAE cathode increased proportionally to the time from the onset and affected by the current density and the frequency of pulsed DC. Increasing the applied current or the frequency could enhance the skin permeation flux of baicalin. Moreover, the baicalin skin permeation flux could be further improved from 0.22 microg/cm(2) per h in iontophoresis alone to 0.43 microg/cm(2) per h in the combined approach of iontophoresis and Azone.


Subject(s)
Anti-Infective Agents/administration & dosage , Anti-Infective Agents/metabolism , Drug Delivery Systems , Flavonoids/administration & dosage , Flavonoids/metabolism , Iontophoresis , Acrylic Resins/chemical synthesis , Acrylic Resins/chemistry , Administration, Cutaneous , Alginates/chemical synthesis , Alginates/chemistry , Azepines/pharmacology , Electrochemistry , Electrodes , Glucuronic Acid/chemical synthesis , Glucuronic Acid/chemistry , Hexuronic Acids/chemical synthesis , Hexuronic Acids/chemistry , Humans , Hydrogen-Ion Concentration , Polyvinyl Alcohol/chemical synthesis , Polyvinyl Alcohol/chemistry , Skin/drug effects , Skin/metabolism , Tensile Strength
18.
Acta Crystallogr Sect E Struct Rep Online ; 64(Pt 7): o1234, 2008 Jun 07.
Article in English | MEDLINE | ID: mdl-21202871

ABSTRACT

The title compound, C(17)H(19)N(3)O(2)·2H(2)O, is particularly useful in the preparation of mirtaza-pine, which is the active agent in a new class of anti-depressants. It crystallized as a zwitterion with two mol-ecules of water in the asymmetric unit. The crystal structure is dominated by a system of hydrogen bonds involving the positively charged N atom and both water mol-ecules.

19.
Acta Crystallogr Sect E Struct Rep Online ; 64(Pt 1): o128, 2007 Dec 06.
Article in English | MEDLINE | ID: mdl-21200692

ABSTRACT

The title compound, C(16)H(12)Cl(2)O, was synthesized from 1-naphthol and 1,2-dichloro-benzene with anhydrous aluminium chloride as a cataylst. In the mol-ecule, the two ring systems are approximately perpendicular to one other with a dihedral angle of 82.06 (4)°. There are two CH-type hydrogen bonds.

20.
J Biomater Sci Polym Ed ; 16(5): 563-74, 2005.
Article in English | MEDLINE | ID: mdl-16001716

ABSTRACT

The interactions of 1-dodecyl-azacycloheptan-2-one (Azone), a penetration enhancer, with mouse skin were analyzed by fluorescence microscopy, solid-state 13C-CP/MAS-NMR spectroscopy and Attenuated Total Reflectance Fourier-transform infrared (ATR-FT-IR) spectroscopy. Ferulic acid was employed as fluorescent probe to observe the delivery pathway in the stratum corneum (SC) after treatment with Azone. Results suggested that the interaction between Azone and the SC occurs in the lipid domains as well as the protein domains. FT-IR measurements show that treatment with Azone results in significant shifts toward larger wavenumbers at v(as)CH2 and v(s)CH2, indicating an increased gauche conformational isomer content of lipid CH2. Further, a decrease of (13C)T1 values and a shift of the SC protein amide-II band to a short wavenumber were found when the SC was pretreated with Azone. It is concluded that Azone can partially convert the SC protein from an alpha-helix conformation to a beta-sheet conformation and loosen the aggregating SC keratins at room temperature.


Subject(s)
Adjuvants, Pharmaceutic/pharmacology , Azepines/pharmacology , Skin Absorption , Skin/drug effects , Adjuvants, Pharmaceutic/pharmacokinetics , Administration, Cutaneous , Animals , Azepines/pharmacokinetics , Coumaric Acids/chemistry , Diffusion , Fluorescent Dyes , In Vitro Techniques , Keratins/chemistry , Lipids/chemistry , Magnetic Resonance Spectroscopy , Mass Spectrometry , Mice , Microscopy, Fluorescence , Protein Structure, Secondary , Skin/metabolism , Spectroscopy, Fourier Transform Infrared
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