Fluorescence enhancement reaction of flavoxate hydrochloride (FX) in strong alkali solution was studied, the mechanism of the reaction was investigated, and a novel fluorimetric method for analysis of FX in drug sample was established. FX has no intrinsic fluorescence, but it can slowly produce fluorescence in strong alkali solution. Heating can promote the fluorescence enhancement reaction. In 3D fluorescence spectra of the decomposition product of FX, two fluorescence peaks, located respectively at excitation wavelengths λex/ emission wavelength λem =223/410 nm, and 302/410 nm, were observed. Using quinine sulfate as a reference, fluorescence quantum yield of the decomposition product was measured to be 0.50. The structural characteriza- tion and spectral analysis of the decomposition product reveal that ester bond hydrolysis reaction of FX is firstly occurred during heating process, forming 3-methylflavone-8-carboxylic acid (MFA), then a cleavage reaction of the γ-pyrone ring of MFA occurred, producing α, β-unsaturated ketone. This product includes adjacent hydroxyl benzoic acid group in its molecule, which can form intramolecular hydrogen bond under alkaline condition, so that increase the conjugate degree and enhance the rigidity of the molecule, and thereby cause fluorescence enhancement. Based on this fluorescence enhancement reaction, a fluorimetric method was proposed for the determination of FX. A linear calibration curve covered the concentration range 0.020 3-0.487 µg · mL. The regression equation was I(F) = 23.9 + 5357.3 c, with correlation coefficient r = 0.999 7 (n = 8), detection limit D = 1.1 ng · mL(-1). The method was applied to the analysis of FX tablets, with a spiked recovery rate of 100.2%. The reliability of the method was verified by a UV-spectrophotometric method.
Alkalies ; Calibration ; Chemistry, Pharmaceutical ; Flavoxate ; analogs & derivatives ; chemistry ; Fluorescence ; Limit of Detection ; Reproducibility of Results ; Solutions ; Tablets

By summarizing the recent literatures on brain mechanisms with acupuncture intervention based on blood oxygenation level-dependent (BOLD)-functional magnetic resonance imaging (fMRI), the BOLD-fMRI examination and analysis methods, the points to be acupunctured, the corresponding meridian activation regions, the specific intensity range, functions and indications of the acupoints, the manifestation of 'bi-directional regulation' characteristics, fMRI performance of chronergy, laterality and needling qi of acupuncture were reviewed to provide the ideas for future research in this area.

Objective:To observe the lipid-lowering effect of different transdermal absorption enhancers applied to the herbal cake-partitioned moxibustion in hyperlipidemia model rabbits, and to explore the possible mechanism. Methods:Forty New-Zealand rabbits were randomly divided into 5 groups using the random number table method, with 8 rats in each group. Rabbits in the blank group were fed routinely with normal diet; rabbits in the other groups were fed with high-fat diet for 12 weeks to establish the hyperlipidemia model. Rabbits in the blank and the model groups were not treated. After the model was prepared, rabbits in the non-transdermal absorption enhancer group received herbal cake-partitioned moxibustion without transdermal absorption enhancer; rabbits in the laurocapram group and the borneol group received herbal cake-partitioned moxibustion with laurocapram or borneol respectively. After 4 weeks of treatment, serum was collected for enzyme-linked immunosorbent assay (ELISA), and the liver tissues were isolated for immunohistochemistry, quantitative polymerase chain reaction (qPCR) and Western-blotting (WB) detection. Results: Serum ELISA results showed that leptin was significantly decreased in the model group compared with the blank group (P＜0.05); compared with the model group, leptin was significantly increased in the non-transdermal absorption enhancer, the laurocapram and the borneol groups (all P＜0.05); compared with the non-transdermal absorption enhancer group, leptin was significantly increased in the laurocapram group and the borneol group (both P＜0.05); there was no significant difference in leptin between the laurocapram and the borneol groups (P＞0.05). The qPCR results of rabbit liver tissues showed that the mRNA expressions of leptin, Janus kinase 2 (JAK2) and signal transducer and activator of transcription 3 (STAT3) in the model group were significantly lower than those in the blank group (all P＜0.05); compared with the model group, the mRNA expressions of leptin, leptin receptor (LR), JAK2 and STAT3 in the non-transdermal absorption enhancer, the laurocapram and the borneol groups were significantly increased (all P＜0.05); compared with the non-transdermal absorption enhancer group, the mRNA expressions of leptin, LR, JAK2 and STAT3 in the laurocapram and the borneol groups were significantly increased (all P＜0.05); compared with the laurocapram group, the mRNA expressions of leptin, LR, JAK2 and STAT3 in the borneol group were significantly increased (P＜0.05). The trend of immunohistochemistry and WB detection results was basically consistent with the qPCR assay results. The immunohistochemistry and WB detection results of phosphorylated JAK2 (phospho-JAK2) and phosphorylated STAT3 (phospho-STAT3) were basically consistent with those of JAK2 and STAT3. Conclusion: The molecular expression of Leptin/JAK2/STAT3 pathway in the hyperlipidemia model rabbits was decreased. The molecular expression of Leptin/JAK2/STAT3 pathway was significantly increased after the herbal cake-partitioned moxibustion. The application of laurocapram and borneol, as transdermal absorption enhancers, in the herbal cake-partitioned moxibustion could more obviously up-regulate the factors of the Leptin/JAK2/STAT3 lipid-regulating pathway than the herbal cake-partitioned moxibustion alone.

Dexmedetomidine (DEX) has neuroprotective effects and its efficacy was determined in propofol-treated pups. Postnatal day (P) 7 rats were exposed to propofol and DEX to investigate the induced apoptosis-related gene expression. Furthermore, synaptic structural changes at the cellular level were observed by electron microscopy. Induction of hippocampal long-term potentiation (LTP) of P30 rats and long-lasting performance of spatial discrimination at P30 and P60 were evaluated. After a single propofol exposure to P7 rats, DEX pretreatment effectively rescued the profound apoptosis seen in hippocampal neurocytes, and strongly reversed the aberrant expression levels of Bcl2-like 1 (BCL2L1), matrix metallopeptidase 9 (MMP-9) and cleaved caspase 3 (CC3), and sharply enhanced synaptic plasticity. However, there were no significant differences in escape latency or crossing times in a probe test. This was accompanied by no obvious reduction in search strategies among the rat groups. No impairment of long-term learning and memory in P30 or P60 rats was detected when using a single dose propofol treatment during the most vulnerable period of brain development. DEX was shown to ameliorate the rodent developmental neurotoxicity caused by a single neonatal propofol challenge, by altering MMP-9, BCL2L1 and CC3 apoptotic signaling.

Five structural important residues of rice nonspecific lipid transfer protein LTP110 were mutated by site-directed mutagenesis. Sequence results showed that they were all mutated successfully. After trying various E. coli expression systems, thioredoxin fusion expression system was found to be a proper system to express wild type and mutant LTP110. cDNA sequences encoding wild type LTP110 and the mutants Y17A, P72L, R46A, D43A, C50A were cloned into two kinds of thioredoxin fusion expression vectors. The expression results were compared. In pTrxFus/GI724 expression system, wild type LTP110 and the mutants Y17A, P72L, R46A could be expressed at low level while D43A and C50A could not be expressed normally; in pET32a(+)/BL21 (DE3) trxB- expression system, wild type LTP110 and all mutant proteins could be expressed very well and the levels were higher than that in pTrxFus/GI724 system. LTP110 fusion protein expressed in pET32a(+) vector was purified and its activity was checked by fluorescence labeled fatty acid. Results indicated that the recombinant LTP110 fusion protein has lipid binding activity. This work provides good basis for the further study.
Amino Acid Sequence ; Carrier Proteins ; genetics ; isolation & purification ; metabolism ; Gene Expression ; Genetic Engineering ; Genetic Vectors ; Molecular Sequence Data ; Mutagenesis, Site-Directed ; Oryza ; genetics ; Plant Proteins ; genetics ; isolation & purification ; metabolism ; Recombinant Fusion Proteins ; genetics ; isolation & purification ; metabolism ; Thioredoxins ; genetics

OBJECTIVETo evaluate the effect of topical corticosteroid for treatment of moderate or severe dry eye.

METHODSSixty eyes of 30 patients with moderate or severe dry eye, who were not sensitive to artificial tears, were treated with 0.1% fluorometholone eye drops. Subjective symptom and objective tests were used to evaluate the efficacy of treatment before and after application of 0.1% fluorometholone eye drops for 1 week and 1 month. Side effects were also evaluated.

RESULTSAfter 1 week of treatment, subjective symptoms were improved in all dry eye patients; objective tests were improved in all dry eye patients 1 month after treatment, and the difference was significant.

CONCLUSIONTopical corticosteroid drops can rapidly and effectively relieve the symptoms and signs of moderate or severe dry eye.

Administration, Topical ; Adult ; Dry Eye Syndromes ; drug therapy ; Female ; Fluorometholone ; administration & dosage ; adverse effects ; Glucocorticoids ; administration & dosage ; Humans ; Male ; Middle Aged

Adult ; Base Sequence ; Drug Resistance, Multiple, Viral ; Genome, Viral ; Hepatitis B virus ; genetics ; Hepatitis B, Chronic ; drug therapy ; virology ; Humans ; Male ; Mutation ; Phylogeny

Objective To investigate the effects of standardized tertiary rehabilitation (STR) on limb motor function (LMF) after stroke.Methods Eighty-two patients were divided into a primary cerebral infarction group (PCI group) and a primary cerebral hemorrhage group (PCH group),and then randomly further divided into experi- mental and control sub-groups.All patients received routine internal medicine treatment,supplemented with stand- ardized tertiary" rehabilitation in the experimental groups.All patients were assessed with the simplified Fugl-Meyer motor function assessment (S-FMMFA) at enrollment,and 1,3 and 6 months after their stroke.Results The scores of the experimental groups were higher than those of the controls.The experimental groups scores were 26.10% of normal at the time of the enrollment,and improved to 42.52%,65.62% and 83.71% by the end of the 1st,3rd and 6th month,respectively.The control groups started at 18.51%,and progressed to 24.85% ,37.24% and 45.84% over the same interval.Conclusion STR was associated with improved LMF scores of stroke pa- tients.

Objective: To observe the effects of laurocapram and borneol as transdermal penetration enhancers applied to herbal cake-partitioned moxibustion on liver lipids, hormone-sensitive lipase (HSL) and hydroxymethylglutaryl CoA (HMG-CoA) reductase in hyperlipidemia rabbits.Methods: Forty New-Zealand rabbits were randomly divided into 5 groups using the random number table method, with 8 rats in each group. Rabbits in the blank group were fed routinely with a normal diet; rabbits in the other groups were fed with high-fat diet for 12 weeks to establish the hyperlipidemia model. Rabbits in the blank and the model groups were not given any intervention. After the model was prepared successfully, rabbits in the non-transdermal penetration enhancer group received herbal cake-partitioned moxibustion without transdermal penetration enhancers; rabbits in the laurocapram group and the borneol group received herbal cake-partitioned moxibustion with laurocapram or borneol respectively. After 4 weeks of treatment, the serum was isolated and enzyme-linked immunosorbent assay (ELISA) was applied for the detection of HSL and HMG-CoA reductase. The liver tissues were isolated, and total cholesterol (TC) and triglycerides (TG) were measured by enzymatic methods. One-step method was applied for high-density lipoprotein cholesterol (HDL-C) and low-density lipoprotein cholesterol (LDL-C) detection, and transmission turbidimetry was for apolipoprotein A1 (Apo-A1) and apolipoprotein B (Apo-B) detection. Results: The serum concentrations of the drugs in the laurocapram and the borneol groups were significantly higher than those in the non-transdermal penetration enhancer group (both P<0.05); all drug penetrations in the borneol group were significantly higher than those in the laurocapram group (both P<0.05), except for tanshinone ⅡA. Compared with the non-transdermal penetration enhancer group, the HSL was significantly increased while the HMG-CoA reductase was significantly decreased in the laurocapram and the borneol groups (both P<0.05); between groups, the HSL in the borneol group was significantly higher than that in the laurocapram group (P<0.05). Compared with the blank group, the levels of LDL-C, TG, TC and Apo-B in rabbit liver were significantly increased in the model group (P<0.05); compared with the model group, the levels of LDL-C, TG, TC and Apo-B in the non-transdermal penetration enhancer, the laurocapram, and the borneol groups were significantly decreased (all P<0.05); between groups, the TG and TC in the laurocapram group and the LDL-C, TG, TC and Apo-B in the borneol group were significantly lower than those in the non-transdermal penetration enhancer group (all P<0.05), and the TG, LDL-C and Apo-B in the borneol group were significantly lower than those in the laurocapram group (all P<0.05). Compared with the blank group, the HDL-C and Apo-A1 were significantly decreased in the model group (both P<0.05), while compared with the model group, the HDL-C and Apo-A1 were significantly increased in the non-transdermal penetration enhancer, the laurocapram, and the borneol groups (all P<0.05). Between groups, the Apo-A1 in the laurocapram group, the HDL-C and Apo-A1 in the borneol group were significantly higher than those in the non-transdermal penetration enhancer group (all P<0.05).Conclusion: The application of laurocapram and borneol, as transdermal penetration enhancers, in herbal cake-partitioned moxibustion can promote the penetration of the drugs in the herbal cake, increase the levels of HDL-C and Apo-A1, improve the metabolism of HSL and HMG-CoA reductase, and also simultaneously reduce the levels of TC, TG, LDL-C and Apo-B in the liver. The transdermal penetration enhancement effect of borneol is slightly better than or equivalent to that of laurocapram.

Objective To establish the quality standard for Yiwei Xiaoyu Granules.Methods TLC was used for the qualitative analyses of Atractylodis Macrocephalae Rhizoma, Angelicae Sinensis Radix and Dendrobii Caulis; HPLC was applied to determine the contents of notoginsenoside R1, ginsenoside Rg1, ginsenoside Rb1and ginsenoside Re. Results The TLC spots were clear and free from negative interference. Notoginsenoside R1, ginsenoside Rg1, ginsenoside Rb1and ginsenoside Re showed good linear relationships within the ranges of 0.067 2–0.672 μg (r=0.999 6), 0.501 2–5.012 μg (r=0.999 6), 0.326 5–3.265 μg (r=0.999 6), 0.098 3–0.983 μg (r=0.999 7), whose average recoveries were 96.32% (RSD=1.3%), 96.45% (RSD=1.5%), 101.23% (RSD=1.7%), and 97.89% (RSD=1.7%), respectively. Conclusion This method is accurate, reliable, and reproducible, which can be used for the quality control of Yiwei Xiaoyu Granules.