2.Inhibition of curcumin on proliferative vitreoretinopathy in rabbit eye
Jian-bin, AN ; Jing-xue, MA ; Dan-yan, LIU ; Yan-jun, GAO ; Yue-xian, CUI ; Su-zhen, CAI ; Li-ya, LIU
Chinese Journal of Experimental Ophthalmology 2011;29(2):125-129
Background Our previous study demonstrated that curcumin can induce the apoptosis of retinal pigment epithelial (RPE) cells and herein inhibit the proliferation of RPE cells,and it is proved that the intravitreous injection of 0.1mg curcumin has less adverse effect to ocular tissue, inferring a good applicative prospect in clinic. Objective The goal of this experiment was to evaluate the effectiveness of curcumin on the prevention and treatment of experimental proliferative vitreoretinopathy (PVR). Methods PVR models were induced by injection of 0.1ml RPE cells (containing 2×106 cells) into vitreous cavity in 40 eyes of 20 healthy and mature New Zealand albino rabbits.0. 1ml curcumin(0. 1 mg) was then injected into lateral eye of each model rabbit immediately following the injection of RPE cells,and the equal volume of normal saline solution containing 0. 5‰ DMSO was injected into the fellow eye of each model rabbit as controls. On 1,3,7,14,21 and 28 days after injection, the changes of cornea, aqueous humor, lens, vitreous and fundus were examined and recorded by slit lamp biomicroscope, indirect ophthalmoscope,fundus color camera and B-type ultrasonograph to evaluate the inflammatory response. The incidence rate of retinal detachment was calculated and compared between curcumin group and control group. Results The inflammatory reaction in anterior chamber and misty opacity in vitreous were found from 1 day through 3 days after injection, but no obvious proliferative strap and retinal detachment in all of the experimental eyes. On the 7th day after injection, inflammatory reaction was extinct in the anterior chamber of rabbit eyes, and proliferative strap occurred in 14 eyes(75% ) in the control group but only 2 eyes (10% ) in curcumin group,showing significant difference between these two groups (P<0. 01). No retinal detachment was seen in both the two groups. On 14,21 and 28 days after injection, the incidence rate of retinal detachment was 55% ,80% ,95% respectively in control group and that of curcumin group was 10% ,15% ,15% respectively,presenting considerably differences between two groups (P<0. 01, P<0. 01 ,P<0. 01 ). Conclusion Injection of curcumin into vitreous cavity can effectively inhibit the occurrence and development of PVR in rabbit.
3.A study on the noninvasive prenatal diagnosis of fetal blood type by maternal blood
Zhen-Yong WANG ; Guo-Song SHEN ; Ping-Ya HE ; Su ZHANG ; Ya-Qin ZHANG
Journal of Preventive Medicine 2016;28(5):473-476
Objective ToexplorethevalueofprenataldiagnosisoffetalABObloodgroupsinthepreventionofABO-HDN,andtoprovideevidenceforpreventionofABO-HDN.Methods Atotalof3777sampleswerecollectedfromthe pregnant women whose ABO blood group is O,and we detected the ABO blood group by serological method to detect the titerofIgGanti-Aandanti-Binthematernalblood.Results Amongthe3777samplescollectedfromthepregnant women whose ABO blood group is O ,the titer of IgG anti-A to anti-B was 1 to1 024 in 27 samples(0.7%),1∶51 2 in 97 samples(2.6%),1∶256 in 1 63 samples(4.3%),1∶1 28 in 285 samples(7.5%)and 1:64 in 603 samples(1 6%). We followed the pregnancy and newborn outcome of 769 case whose antibody titer of 1∶64 or more ,and compared the fetal ABO blood group with results of the titer of IgG anti -A and/or anti -B.A total of 641 patients (83.3%) was corresponding resistance against A or B,and 1 28 patients (1 6.6%)was not corresponding resistance against A or B.The higher the antibody titer,the higher incidence of neonatal ABO hemolytic disease occurred.We extracted the fetal free DNA of peripheral blood plasma in 30 pregnant women, and the genotypes of fetal ABO blood group were detected by the polymerase chain reaction-sequence specific primer (PCR-SSP),and all the experiment presented success.Conclusion ThetiterofIgGanti-Atoanti-Bcouldbeusedtopreventtheoccurrenceofhemolyticdiseaseofnewborn. Considering the interference factors,the fetal free DNA in the maternal circulation could be used to prenatally detect fetal ABO blood groups.
4.Design, synthesis and evaluation of tacrine-methoxybenzene hybrids as cholinesterases inhibitors.
Wen LUO ; Yong-Mei ZHAO ; Zhen ZHANG ; Ya-Bin SU ; Chao-Jie WANG
Acta Pharmaceutica Sinica 2012;47(7):916-921
A series of tacrine-methoxybenzene hybrids (5a-5i) were designed, synthesized and evaluated as inhibitors of cholinesterases (ChEs). All the compounds had better ChEs inhibitory activities than tacrine with IC50 values at the nanomolar range. Compound 5h exhibited the strongest inhibition on acetylcholinesterase (AChE) with an IC50 value of 6.74 nmol x L(-1) and compound 5f showed the most potent inhibition on butyrylcholinesterase with IC50 value of 3.83 nmol x L(-1). Kinetic and molecular modeling studies showed that these hybrids targeted both the catalytic active site and the peripheral anionic site of AChE.
Acetylcholinesterase
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metabolism
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Anisoles
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chemical synthesis
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chemistry
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pharmacology
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Binding Sites
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Butyrylcholinesterase
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metabolism
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Catalytic Domain
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Cholinesterase Inhibitors
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chemical synthesis
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chemistry
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pharmacology
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Drug Design
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Inhibitory Concentration 50
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Tacrine
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chemical synthesis
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chemistry
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pharmacology
5.Isolation and elucidation of antioxidant constituents from acetone extract in root of Scutellaria rehderiana.
Ya-lun SU ; Yu HUANG ; Zhen-yu CHEN
China Journal of Chinese Materia Medica 2004;29(9):863-864
OBJECTIVETo isolatate and elucidate the antioxidant constituents from acetone extract of Scutellaria rehderiana.
METHODChemical constituents were isolated by several column chromatographies and their structures were elucidated on the basis of standard compounds and spectral analysis.
RESULTFive compounds, oroxylin A, wogonin, baicalein, ganhuangenin, ganhuangemin were isolated from acetone extract of S. rehderiana. Baicalin was obtained from methanol extract of S. rehderiana.
CONCLUSIONGanhuangemin was isolated from the plant for the first time. Baicalein and ganhuangenin have stronger antioxidant activity than that of BHT (butylated hydroxytoluene).
Antioxidants ; chemistry ; isolation & purification ; pharmacology ; Flavanones ; chemistry ; isolation & purification ; pharmacology ; Flavonoids ; chemistry ; isolation & purification ; pharmacology ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Scutellaria ; chemistry
6.Intestinal absorption of pulchinenosides from Pulsatilla chinensis in rats.
Ya-li LIU ; Yong-gui SONG ; Zhi-yu GUAN ; Ling ZHANG ; Shi-lin YANG ; Meng WANG ; Zhen-hua CHEN ; Dan SU
China Journal of Chinese Materia Medica 2015;40(3):543-549
HPLC-ELSD was applied to explore the absorption mechanism of pulchinenosides (B3, BD, B7, B10, B11) in rats. The experimental results showed that the absorption rate constant, Ka value (B3, BD) and Permeability coefficient, Peff value (B3, B7) displayed significant difference (P <0.05) in various intestinal segments, The Ka value and Peff value of PRS was different from each other with the highest absorption in duodenum (duodenum > jejunum > colon > ileum); The PRS displayed excessive satuation as the concentration increased over 0.05-2.5 g · L(-1). There were no obvious linear correlations between Peff values and concentrations in duodenum (0.6007 ≤ R2 ≤ 0.7727); Ka and Peff value declined when the PRS was perfused with P-glycoprotein promoter digoxin, on the other hand, inclined when perfused with P-glycoprotein inhibitor verapamil with significant difference among PRS B3, BD, B7, B11 (P <0.05). All the above results demonstrated that B3, BD, B7 were greatly influenced by absorption sites, duodenum was the main absorption site; PRS didn't entirely transported in a concentration dependent manner, and the transporter-protein involved the transportation, so the intestinal absorption of the five pulchinenosides was not entirely passive diffusion; and PRS might be the substrates of P-glycoprotein.
ATP-Binding Cassette, Sub-Family B, Member 1
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physiology
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Animals
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Intestinal Absorption
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Male
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Oleanolic Acid
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pharmacokinetics
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Pulsatilla
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chemistry
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Rats
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Rats, Wistar
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Saponins
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pharmacokinetics
7.Relationship between cognition function and hippocampus structure after long-term microwave exposure.
Li ZHAO ; Rui Yun PENG ; Shui Ming WANG ; Li Feng WANG ; Ya Bing GAO ; Ji DONG ; Xiang LI ; Zhen Tao SU
Biomedical and Environmental Sciences 2012;25(2):182-188
OBJECTIVETo analyze the effects of long-term microwave exposure on hippocampal structure and function in the rat.
METHODSExperiments were performed on 184 male Wistar rats (three exposure groups and a sham group). Microwaves were applied daily for 6 min over 1 month at average power densities of 2.5, 5, and 10 mW/cm2. Learning and memory abilities were assessed by Morris water maze. High performance liquid chromatography was used to detect neurotransmitter concentrations in the hippocampus. Hippocampal structures were observed by histopathological analysis.
RESULTSFollowing long-term microwave exposure there was a significant decrease in learning and memory activity in the 7 d, 14 d, and 1 m in all three microwave exposure groups. Neurotransmitter concentrations of four amino acids (glutamate, aspartic acid, glycine, and gamma-aminobutyric acid) in hippocampus were increased in the 2.5 and 5 mW/cm2 groups and decreased in the 10 mW/cm2 group. There was evidence of neuronal degeneration and enlarged perivascular spaces in the hippocampus in the microwave exposure groups. Further, mitochondria became swollen and cristae were disordered. The rough endoplasmic reticulum exhibited sacculated distension and there was a decrease in the quantity of synaptic vesicles.
CONCLUSIONThese data suggest that the hippocampus can be injured by long-term microwave exposure, which might result in impairment of cognitive function due to neurotransmitter disruption.
Animals ; Chromatography, High Pressure Liquid ; Cognition ; Hippocampus ; pathology ; physiopathology ; radiation effects ; Learning ; Male ; Memory ; Microscopy, Electron, Transmission ; Microwaves ; Rats ; Rats, Wistar
10.Rhein lysinate induces apoptosis in breast cancer SK-Br-3 cells by inhibiting HER-2 signal pathway.
Ya-Jun LIN ; Yun-Hong HUANG ; Yong-Zhan ZHEN ; Xiu-Jun LIU ; Yong-Su ZHEN
Acta Pharmaceutica Sinica 2008;43(11):1099-1105
This study is to investigate the effect of rhein lysinate on inducing human breast cancer cell line SK-Br-3 apoptosis and the role of HER-2 signal pathway in the apoptosis. MTT assay was used to detect SK-Br-3 cell proliferation. Cell cycle and apoptosis were analyzed by flow cytometry. The protein expression and the protein phosphorylation of HER-2 signal pathway were detected by Western blotting. The level of HER-2 mRNA was detected by RT-PCR and the level of HER-2 expression was also detected by immunofluorescence cytochemical methods. The results showed that rhein lysinate remarkably inhibited breast cancer SK-Br-3 cell proliferation. The IC50 value for 48 h treatment was 85 micromol x L(-1). Apoptosis in SK-Br-3 cells was induced by rhein lysinate in a dose dependent manner. The protein expressions of HER-2, NF-KB, and the protein phosphorylation of HER-2 were downregulated, however the protein expression of p53 and p21 was upregulated after rhein lysinate treatment. The level of HER-2 mRNA decreased by using RT-PCR assay and the level of HER-2 expression was also decreased by using immunofluorescence cytochemical assay after rhein lysinate treatment. It can be concluded that rhein lysinate could inhibit SK-Br-3 cell proliferation and induce apoptosis. HER-2/NF-kappaB/p53/p21 signal pathway might be involved in this process. Rhein lysinate has a good prospect to be an adjuvant chemotherapeutic drug.
Anthraquinones
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pharmacology
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Antineoplastic Agents
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pharmacology
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Apoptosis
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drug effects
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Breast Neoplasms
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metabolism
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pathology
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Cell Line, Tumor
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Cell Proliferation
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drug effects
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Cyclin-Dependent Kinase Inhibitor p21
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metabolism
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Female
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Humans
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Inhibitory Concentration 50
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Lysine
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pharmacology
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NF-kappa B
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metabolism
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RNA, Messenger
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metabolism
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Receptor, ErbB-2
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genetics
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metabolism
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Signal Transduction
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Tumor Suppressor Protein p53
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metabolism