Long noncoding RNAs HAND2-AS1 ultrasound microbubbles suppress hepatocellular carcinoma progression by regulating the miR-873-5p/tissue inhibitor of matrix metalloproteinase-2 axis

BACKGROUND Increasing data indicated that long noncoding RNAs(lncRNAs)were directly or indirectly involved in the occurrence and development of tumors,including hepatocellular carcinoma(HCC).Recent studies had found that the expression of lncRNA HAND2-AS1 was downregulated in HCC tissues,but its role in HCC progression is unclear.Ultrasound targeted microbubble destruction mediated gene transfection is a new method to overexpress genes.AIM To study the role of ultrasound microbubbles(UTMBs)mediated HAND2-AS1 in the progression of HCC,in order to provide a new reference for the treatment of HCC.METHODS In vitro,we transfected HAND2-AS1 siRNA into HepG2 cells by UTMBs,and detected cell proliferation,apoptosis,invasion and epithelial-mesenchymal transition(EMT)by cell counting kit-8 assay,flow cytometry,Transwell invasion assay and Western blotting,respectively.In addition,we transfected miR-837-5p mimic into UTMBs treated cells and observed the changes of cell behavior.Next,the UTMBs treated HepG2 cells were transfected together with miR-837-5p mimic and tissue inhibitor of matrix metalloproteinase-2(TIMP2)overexpression vector,and we detected cell proliferation,apoptosis,invasion and EMT.In vivo,we established a mouse model of subcutaneous transplantation of HepG2 cells and observed the effect of HAND2-AS1 silencing on tumor formation ability.RESULTS We found that UTMBs carrying HAND2-AS1 restricted cell proliferation,invasion,and EMT,encouraged apoptosis,and HAND2-AS1 silencing eliminated the effect of UTMBs.Additionally,miR-873-5p targets the gene HAND2-AS1,which also targets the 3’UTR of TIMP2.And miR-873-5p mimic counteracted the impact of HAND2-AS1.Further,miR-873-5p mimic solely or in combination with pcDNA-TIMP2 had been transformed into HepG2 cells exposed to UTMBs.We discovered that TIMP2 reversed the effect of miR-873-5p mimic caused by the blocked signalling cascade for matrix metalloproteinase(MMP)2/MMP9.In vivo results showed that HAND2-AS1 silencing significantly inhibited tumor formation in mice.CONCLUSION LncRNA HAND2-AS1 promotes TIMP2 expression by targeting miR-873-5p to inhibit HepG2 cell growth and delay HCC progression.

Identification and Distribution of the Clinical Isolates of Imipenem-resistant Pseudomonas aeruginosa Carrying Metallo-β-lactamase and/or Class 1 Integron Genes

To investigate the distribution of the genes of two major metallo-β-1actamases （MBL;i.e.,IMP and VIM） and class 1 integrons （intI） in the clinical imipenem-resistant Pseudomonas aeruginosa, a total of 65 isolates, from a university hospital in Sichuan between December 2004 and April 2005 were screened for MBL genes by PCR using primers specific for blaIMP-1, blaVIM and blaVIM-2 genes. The MBL-positive isolates were further assessed for class 1 integrons by PCRusing specific primers. The nucleotide sequences of several PCR products were also determined. The results revealed that the blaVIM gene was found in 81.5% （53/65） of all isolates, blaVIM-2 gene was found in only 1 isolate and the intl gene was observed in 45.3% （24/53） of blaVIM-positive isolates. One isolate carried simultaneously both blaIMP-1 and intl genes, and to the best of our knowledge this is the first report of such isolate in southwest China. These observations highlight that the genes for VIM β-1actamase and class 1 integrons were predominantly present among the imipenem-resistant P. aeruginosa tested, confirming the current widespread threat of imipenem-resistant, integron-borne P.aeruginosa.

The new K_V3.4 inhibitor BDS-I[1–8] as a potential pharmacological opportunity in Alzheimer’s disease therapy

Alzheimer's disease(AD)is the most common neurodegenerative disorder and the first cause of dementia in the elderly,with no treatment able to prevent or to block disease progression.AD is characterized by memory impairment and cognitive dysfunction,followed in the late phases of the disease by severe neurodegeneration and neuronal death.The amyloid-β(Aβ)peptide,generated upon the processing of the amyloid precursor protein,is considered the main initiator of AD pathology.Indeed,Aβpeptides,which aggregate and accumulate to form extracellular plaques and intraneuronal deposits.

Synthesis and Crystal Structure of a Novel Ethyl 5-(4-(2-Phenylacetamido)phenyl)-1H-pyrazole-3-carboxylate as an Acrosin Inhibitor

The title compound （ethyl5-（4-（2-phenylacetamido）phenyl）-lH-pyrazole-3-carboxylate, C20H19N3O3） was synthesized by the reaction of Claisen condensation, cyclization, reduction and acylation. The structure was characterized by X-ray diffraction, MS, NMR and IR. It belongs to the monoclinic system, space group C2/c with a = 22.723（9）, b = 9.324（4）, c = 18.890（8） A, β = 114.259（6）°, V = 3649（3） A^3, Dc = 1.272 Mg·m^3, Z = 8, Mr = 349.38, p = 0.087 mm^-1, F（000） = 1472, the final R = 0.0615 and wR = 0.1643. The biological test shows that the title compound has a moderate acrosin inhibition activity.

Effect of protease inhibitor from Agaricus bisporus on glucose uptake and oxidative stress in 3T3-L1 adipocytes

Objective:To explore the effect of the protease inhibitor from Agaricus bisporus(J.E.Lange)Imbach(AbPI)on glucose uptake and oxidative stress in 3 T3-L1 adipocytes.Methods:Adipocytes were differentiated and stained with OilRed-O staining to confirm adipogenesis.The toxic/protective effect of AbPI on the adipocytes was determined by MTT assay,intracellular reactive oxygen species generation through flow cytometry,and morphologically through confocal microscopy using propidium iodide,4,6-diamino-2-phenylindol dihydrochloride,and 2’,7’-dichlorofluorescein diacetate dyes.The uptake of fluorescent glucose analog,2-[N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino]-2-deoxy-d-glucose by adipocytes was also studied through confocal microscopy.Results:MTT assay showed that the cell survival rate was(28.00±3.00)%,(92.33±2.60)%,and(71.34±2.10)%in the presence of 2 mM H2O2,AbPI alone,and AbPI and H2O2 both,respectively,in comparison to the control.Oil-Red-O staining indicated that Ab PI enhanced adipogenesis.AbPI stimulated the glucose uptake by adipocytes similar to the drug rosiglitazone,and showed insulinsensitizing effect in the presence of insulin,but failed to stimulate the uptake in the absence of insulin.Intracellular reactive oxygen species generation was reduced in differentiating adipocytes upon Ab PI treatment.Confocal microscopy showed that the damaged cell population rose to 3.50%,117.84%,and 261.50%in the presence of Ab PI alone,AbPI with H2O2,and H2O2 alone,respectively.Conclusions:The protease inhibitor enhances glucose uptake by adipocytes and exhibits a cytoprotective effect on them.

Ⅲ期结肠癌辅助化疗过程中血清CEA和TIMP-1水平的变化

目的观察Ⅲ期结直肠癌患者化疗过程中癌胚抗原(CEA)和组织金属蛋白酶抑制剂-1(TIMP-1)水平的变化。方法选择接受结直肠癌根治性切除患者30例,以mFOLFOX6方案进行12周期化疗。化疗前(d0)、第1周期后(d4)、第2周期前后(d14、d18)、第6周期前后(d70、d74)分别采集血样,分别测定CEA和TIMP-1水平。结果血清CEA水平6个时间点分别为(1.66±0.35)、(1.16±0.26)、(1.71±0.28)、(1.69±0.51)、(1 63±0.16)、(1.61±0.20)μg/L,化疗中除d4与d0差异有统计学意义,其余各时点CEA水平与化疗前差异均无统计学意义。TIMP-1水平6个时点分别为(150.70±15.32)、(153.53±16.91)、(166.28±12.64)、(190.81±1 1.73)、(140.48±12.30)、(145_20±10 49)μg/L,d4、d14与d0的差异均无统计学意义,d18与d0相比升高,差异有统计学意义。结论辅助化疗过程中,CEA保持稳定,而TIMP-1在化疗开始第2周后有一过性升高。

携TIMP-1基因RNAi慢病毒载体感染大鼠HSC-T6细胞抑制目的基因表达

目的验证构建成功的携基质金属蛋白酶组织抑制因子-1(TIMP-1)基因特异性小干扰RNA的慢病毒载体对目的基因表达的抑制效应。方法以慢病毒质粒感染HSC-T6细胞,在感染6天和8天后,观察慢病毒感染效率;采用定量PCR法检测TIMP-1 mRNA水平变化;采用免疫印迹法检测TIMP-1蛋白表达变化。结果在慢病毒载体感染6天时,TIMP-1 mRNA水平较正常对照组下降约0.668倍[2-ΔΔCt为(0.668±0.046)],下降程度明显高于阴性对照组[2-ΔΔCt为(1.001±0.041),(P<0.05)];在慢病毒感染6天和8天时,RNAi组对TIMP-1蛋白表达具有明显的抑制作用,且以感染第6天为显著。结论构建成功的携TIMP-1基因特异性RNAi慢病毒载体能有效感染HSC-T6细胞,并抑制目的基因的表达。

分化抑制因子-1与头颈部肿瘤关系的研究进展

近年研究表明,Id-1在人类多种头颈部恶性肿瘤诸如口腔鳞癌、鼻咽癌、喉癌、涎腺肿瘤等中过表达并通过多条信号通路推进细胞周期的演进,促进肿瘤细胞增殖、迁移、浸润,抑制细胞分化和诱导血管的发生,与肿瘤的预后密切相关,而且有望成为肿瘤治疗中的新靶点。

Combined Effects of Capsaicin and HA14-1 in Inducing Apoptosis in Melanoma Cells

Abnormal regulation of apoptosis is an important aspect of tumour development. Capsaicin, an extract of red chilli peppers, has been shown to inhibit growth of melanoma and other malignant cell lines and HA14-1 is an organic compound that directly induces apoptosis by binding to Bcl-2 protein. The aim of this work was to investigate whether combination therapy with capsaicin and HA14-1 might hold any promise for the treatment of melanoma. Three melanoma cell lines of a range of aggressive potential, melanocytes and fibroblasts were examined, looking at the effects of both drugs singly and in combination on cell viability and induction of apoptosis. This comparative study showed that melanoma cells and melanocytes have a similar sensitivity to capsaicin while fibroblasts are more resistant to it. HA14-1, as expected, induced apoptosis in all cells at relatively low concentrations. A combination of the two agents produced the expected results of an additive effect for 2 (HBL and A375SM) out of 3 melanoma cell lines in inducing apoptosis, but encouragingly for the most metastatically aggressive cancer cell line (C8161), a combination of the two showed a synergistic induction of apoptosis.

A new angiotensin-converting enzyme inhibitor from Peperomia pellucida(L.) Kunth

Objective:To isolate,identify,and evaluate a new angiotensin-converting enzyme inhibitor from Peperomia pellucida(L.)Kunth herbs.Methods:A dried sample of Peperomia pellucida herb was successively macerated with n-hexane and ethyl acetate.The ethyl acetate extract solution was evaporated to obtain the crude extract.Vacuum liquid column chromatography and thin layer chromatography were performed to obtain two pure compounds.Then,both compounds were elucidated and identified using the spectroscopic method.Angiotensin-converting enzyme inhibitory activity studies of both compounds were determined using angiotensin-converting enzyme kit WST-1 with spectrophotometer microplate reader 96-well at 450 nm wavelength.Results:Two bioactive compounds were successfully isolated from Peperomia pellucida herb,including a new compound of 2,3,5-trimethoxy-9-(12,14,15-trimethoxybenzyl)-1 H-indene and pellucidin A.Both compounds demonstrated angiotensin-converting enzyme inhibitory activity,with IC50 values of 72 μM(27.95 μg/mL)and 1 1μM(4.4 μg/mL),respectively.Conclusions:In the present study,two active angiotensin-converting enzyme inhibitors were successfully isolated and purified from Peperomia pellucida which is used as an antihypertensive in traditional medicine,and support its use as an angiotensin-converting enzyme-inhibiting drug.

A novel class of apical sodium–dependent bile salt transporter inhibitors:1-(2,4-bifluorophenyl)-7-dialkylamino-1,8-naphthyridine-3-carboxamides

The apical sodium-dependent bile acid transporter(ASBT) is the main transporter to promote re-absorption of bile acids from the intestinal tract into the enterohepatic circulation.Inhibition of ASBT could increase the excretion of bile acids,thus increasing bile acid synthesis and consequently cholesterol consumption.Therefore,ASBT is an attractive target for developing new cholesterol-lowering drugs.In this report,a series of 1-(2,4-bifluorophenyl)-7-dialkylamino-1,8-naphthyridine-3-carboxamides were designed as inhibitors of ASBT.Most of them demonstrated potency against ASBT transport of bile acids.In particular,compound 4a_1 was found to have the best activity,resulting in 80.1%inhibition of ASBT at10μmol/L.

Recurrent Glioblastoma Multiforme—A Strategy for Long-Term Survival

Recurrent GBM (RGBM) has a highly unfavorable prognosis with majority of patients dying within 6 months and no standard treatments available. Antineoplaston (ANP) A10 and AS2-1 injections underwent Phase II trials in RGBM patients, which reported a long-term overall survival (OS) in a small percentage of patients. The additional Phase II studies BT-07, and BT-21 with ANP in GBM also revealed cases of a long-term OS. ANP shares active ingredients with metabolites of sodium phenylbutyrate (PB), which was used in private practice setting in combination of targeted and chemotherapeutic agents for the treatment of RGBM. The treatment contributed to cases of rapid complete response (CR) and significant OS. This paper provides case studies of three patients treated with ANP under Phase II protocols and two patients treated with PB in combination with targeted therapy, who obtained CR and long-term OS. Based on these studies and basic research on the effects of ANP and PB on the genome of GBM and review of results of preclinical and clinical research on targeted agents, the authors suggest a new strategy for successful treatment of RGBM. They propose Phase I/II clinical trials with ANP and PB in combination with targeted agents, bevacizumab (BVZ), pazopanib, dasatinib and everolimus in patients with RGBM after failure of standard surgery, radiation therapy (RT) and chemotherapy including temozolomide (TMZ) to be conducted to evaluate survival, response and toxicity in these patients.

Design, Synthesis, and Evaluation of 3-（（4-（t-Butyl）-2-（2- benzylidenehydrazinyl）thiazol-5-yl）methyl）quinolin- 2（1H）-ones as Neuraminidase Inhibitors

A series of novel 3-（（4-（t-buty-）-2-（2-benzylidenehydrazinyl）thiazol-5-yl）methyl）quinolin-2（1H）-ones （7a--7z） were designed, synthesized and evaluated for their ability of inhibiting neuraminidase （NA） of influenza H1N1 virus. Some compounds displayed moderate influenza NA inhibitory activity. Compound 71 with the scaffold of 2-（2-（2-methoxybenzylidene）hydrazinyl）thiazole was the best one, exhibiting moderate NA inhibitory activity with ICs0 of 44.66 ~tmol/L. Structure-activity relationship showed that compounds with methoxy or hydroxy groups at the ortho position, fluorine and nitro groups at the meta position and chlorine and bromine groups at the para posi- tion of phenyl ring were more active. Docking study indicated that compound 71 has important interactions with some key residues （including Asp151, Glu119, Arg292, Tyr406, and Asn347） and binds to 430-cavity adjacent to NA active site.

Total Alkaloids from Sophora Alopecuroides L.Increase Susceptibility of Extended-Spectrum β-Lactamases Producing Escherichia coli Isolates to Cefotaxime and Ceftazidime

Objective： To evaluate the antimicrobial activity of total alkaloids extracted from Sophorea alopecuroides L. （TASA） against clinical isolated extended-spectrum beta-lactamases （ESBLs） producing Escherichia coil （E.. coil） strains. Methods： The antibacterial activity of TASA either itself or in combination with cefotaxime （CTX） or ceftazidime （CAZ） was investigated by using the microbroth dilution method and phenotypic confirmatory disk diffusion test against three clinical isolated ESBLs-producing E. coil strains; the interactions of TASA and C＇I＇X or CAZ were ascertained by evaluating the fractional inhibitory concentration index （FICI）. Results： The antibacterial activity of either TASA itself or in combination with C＇IX or CAZ was found. The minimum inhibitory concentration （MICs） of TASA against the ESBLs producing isolates was 12.5 mg/mL. In the combinations with a sub-inhibitory concentration of TASA, a synergistic effect on CTX and CAZ against the ESBLs producing isolates was observed. Similarly, the isolates exposed to lower dose of TASA yielded an increased susceptibility to CTX and CAZ by 8-16 folds determined by microdilution assay. Moreover, enzymatic detection of ESBLs demonstrated that TASA induced reversal resistance to CTX and CAZ partially by a mechanism of inhibition of ESBLs activity in these isolates. Additionally, in the tested isolates following the exposure of TASA, molecular analysis verified the SHV-type beta-lactamase encoding ESBL gene in these isolates, and no mutation was introduced into the ESBL gene. Conclusions： These results suggest that TASA could be used as a source of natural compound with pharmacological activity of reversal resistance to antimicrobial agent. These findings also indicated that the application of the TASA in combination with antibiotics might prove useful in the control and treatment of infectious diseases caused by the ESBLs producing enterobacteriaceae.

Effects of Biejia Ruangan Tablet(复方鳖甲软肝片)-Containing Serum on Matrix Metalloproteinase-9 and Tissue Inhibitor of Metalloproteinase-1 Expression in Cultured Renal Interstitial Fibroblasts

Objective： To investigate the effects of Biejia Ruangan Tablet （复方鳖甲软肝片, BRT）- containing serum on the expression of matrix metalloproteinase （MMP-9） and tissue inhibitor of metalloproteinase （TIMP-1） in cultured renal interstitial fibroblasts. Methods： Different BRT-containing sera were prepared by gastric gavages to rats with the high-dose （7 g/kg）, mid-dose （3.5 g/kg）, and low-dose （1.75 g/kg） BRT respectively. The expression of extracellular matrix in NRK-49F cells was induced by treatment with human transforming growth factor-β1 （recombined human TGF-β 1）, and BRT-containing serum. Western blotting and Northern blotting were used to measure type I and III procollagen, MMP-9, and TIMP-1. Results： The high dose BRT-containing serum could decrease the type Ⅰ and Ⅲ procollagen gene expression which boosted by TGF- 13 1, at the same time cut down TIMP-1 protein and gene expression which increased by TGF- β1 （P〈0.05）. Treatment of cells with recombined human TGF-β 1 had no significant effect on MMP-9 expression and BRT- containing serum also had no effect on MMP-9 expression. Conclusions： High dose BRT has anti-fibrosis effects in NRK-49F cells, as indicated by its inhibition of type Ⅰ and Ⅲ procollagen and TIMP-1 expression.

miR-24-3p/S1PR2信号轴对大鼠RMECs损伤的作用与机制研究

目的研究miR-24-3p/1-磷酸鞘氨醇受体2(S1PR2)信号轴对肾小球内皮细胞(RMECs)损伤的作用及影响机制。方法原代分离获得大鼠RMECs,制备急性肾损伤(AKI)模型。采用CCK8检测细胞增殖能力,流式细胞术检测细胞凋亡情况、活性氧(ROS)水平,酶联免疫吸附试验(ELISA)检测肿瘤坏死因子(TNF)-α和白细胞介素(IL)-1β的表达;生化试剂盒检测超氧化物歧化酶(SOD)、丙二醛(MDA)水平;实时荧光定量PCR检测细胞中S1PR2(NM_017192.2)的mRNA表达水平,Western blot检测S1PR2和凋亡相关基因caspase-3和caspase-9、血管内皮细胞损伤相关因子细胞分裂周期蛋白20(CDC20)和血管内皮生长因子(VEGF)的表达水平。结果LPS组TNF-α、IL-1β水平高于control组,miR-24-3p inhibitor+LPS组TNF-α、IL-1β水平高于inhibitor NC+LPS组,差异有统计学意义(P<0.05)。LPS组MDA、SOD水平高于control组,miR-24-3p inhibitor+LPS组MDA水平高于inhibitor NC+LPS组,但SOD水平低于inhibitor NC+LPS组,差异有统计学意义(P<0.05)。LPS组S1PR2 mRNA表达水平高于control组,miR-24-3p inhibitor+LPS组S1PR2 mRNA表达水平低于inhibitor NC+LPS组,差异有统计学意义(P<0.05)。LPS组S1PR2、caspase-9、caspase-3蛋白表达水平高于control组,CDC20、VEGF蛋白表达水平低于control组,差异有统计学意义(P<0.05);miR-24-3p inhibitor+LPS组S1PR2、caspase-3、caspase-9蛋白表达水平低于inhibitor NC+LPS组,CDC20、VEGF蛋白表达水平高于inhibitor NC+LPS组,差异有统计学意义(P<0.05)。结论miR-24-3p inhibitor通过联动抑制S1PR2表达,下调caspase-3、caspase-9表达,上调CDC20、VEGF表达,实现抑制TNF-α、IL-1β与MDA表达、降低AKI模型对细胞造成损伤的作用。

Effects of (-)-epigallocatechin-3-gallate on expression of matrix metalloproteinase-1 and tissue inhibitor of metalloproteinase-1 in fibroblasts irradiated with ultraviolet A

Background It is known that ultraviolet irradiation can affect cellular function through a number of signaling pathways ( ) epigallocatechin 3 gallate (EGCG) is the major effective component in green tea and can offer protection from ultraviolet induced damage In this study, we investigated the protective mechanism of EGCG on human dermal fibroblasts damaged by ultraviolet A (UVA) in vitro Methods Transcription factor Jun protein levels were measured by Western blot Matrix metalloproteinase 1 (MMP 1) and tissue inhibitor of metalloproteinase 1 (TIMP 1) mRNA were studied by reverse transcription polymerase chain reaction (RT PCR) analysis in conjunction with computer assisted image analysis MMP 1 and TIMP 1 proteins were quantified by enzyme linked immunosorbent assay (ELISA) Results EGCG decreased transcription activity of Jun protein after induction by UVA Both the mRNA and protein levels of MMP 1 were increased by UVA irradiation, while no significant changes were observed in TIMP 1 levels The ratio of MMP 1 to TIMP 1 showed statistically significant differences compared with the control EGCG decreased the ratio of MMP 1 to TIMP 1 by inhibiting UVA induced MMP 1 expression ( P <0 05) Conclusion EGCG can protect human fibroblasts against UVA damage by downregulating the transcription activity of Jun protein and the expression of MMP 1 The ratio of MMP 1 to TIMP 1, rather than the levels of MMP 1 or TIMP 1 alone, may play a significant role in human skin photodamage

Synthesis and anti-HIV activities of phorbol derivatives

In this study,37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated,building upon our previous synthesis of 51 phorbol derivatives.12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out,demonstrating remarkable anti-HIV-1 activities and inhibitory effects on syncytia formation.These derivatives exhibited a higher safety index compared with the positive control drug.Among them,12-(trans-4-fluorocinnamoyl)-13-decanoyl phorbol,designated as compound 3c,exhibited the most potent anti-HIV-1 activity(EC_(50)2.9 nmol·L^(−1),CC50/EC_(50)11117.24)and significantly inhibited the formation of syncytium(EC_(50)7.0 nmol·L^(−1),CC50/EC_(50)4891.43).Moreover,compound 3c is hypothesized to act both as an HIV-1 entry inhibitor and as an HIV-1 reverse transcriptase inhibitor.Isothermal titration calorimetry and molecular docking studies indicated that compound 3c may also function as a natural activator of protein kinase C(PKC).Therefore,compound 3c emerges as a potential candidate for developing new anti-HIV drugs.

Design, synthesis and MAO inhibitory activity of 2-(arylmethylidene)-2,3-dihydro-1-benzofuran-3-one derivatives

A series of 2-（arylmethylidene）-2,3-dihydro-1-benzofuran-3-one derivatives（aurones, 1–20） were synthesized and screened for their inhibitory activity against h MAO. Seventeen compounds（1–5, 7–17,19） were found to be selective towards h MAO-B, while two were non-selective（6 and 20） and one（18）selective towards h MAO-A. Compound 17（Ki = 0.10 0.01 mmol/L） was found to be equally potent and selective towards h MAO-B, when compared with the standard drug Selegiline（Ki = 0.12 0.01 mmol/L）.Nature and position of substitution in aryl ring at 2nd position of benzofuranone influences h MAO-B inhibitory potency, while their structural bulkiness influences selectivity between h MAO-A and h MAO-B.Molecular docking simulation was also carried out to understand the interaction of inhibitor with the enzyme at molecular level, and we found the docking results were in good agreement with the experimental values. Comparison of the activity profile of the aurones with their corresponding flavones reported earlier by our group revealed that there exists no difference in potency as well as selectivity.

布地奈德联合槐杞黄颗粒治疗小儿哮喘的疗效及对血清LTD4、NGF、TIMP-1水平的影响

目的:研究布地奈德联合槐杞黄颗粒治疗小儿哮喘的临床疗效及对患儿血清白细胞三烯D4(LTD4)、神经生长因子(NGF)、基质金属蛋白酶抑制剂-1(TIMP-1)水平的影响。方法:选取2014年3月至2015年3月我院接诊的支气管哮喘患儿90例作为本次研究对象,按照随机数表法分为观察组和对照组。每组45例。两组患儿均在入院后给予支气管解痉剂、吸氧、抗生素、糖皮质激素等常规治疗,对照组患儿在此基础上采用雾化吸入布地奈德混悬液治疗,每次0.5 mg,加入3 mL生理盐水进行持续吸入,每天两次。观察组患儿在对照组的基础上加用槐杞黄颗粒治疗,每天两次。治疗12周后,观察和比较两组患儿的治疗疗效,喘憋、咳嗽、肺部湿罗音、肺部哮鸣音等临床症状消失时间,肺功能用力肺活量(FVC)、一秒用力呼气容积(FEV1),血清LTD4、NGF、TIMP-1水平及T淋巴亚群CD3+、CD4+、CD8+。结果:治疗后,观察组总有效率显著高于对照组[93.33%(42/45)vs77.77%(35/45)](P<0.05);喘憋消失、咳嗽缓解、肺部湿罗音、肺部哮鸣音消失时间显著短于对照组[(4.32±1.03)d vs(6.08±1.24)d,(5.60±1.12)d vs(7.21±1.30)d,(3.19±0.98)d vs(4.98±1.02)d,(3.25±1.03)d vs(5.89±1.35)d](P<0.05);FEV1、FEV1/FVC显著高于对照组[(92.63±10.01)L/s vs(78.36±9.19)L/s,(95.37±11.72)%vs(80.19±10.23)%](P<0.05);血清LTD4、NGF、TIMP-1水平显著低于对照组[(7.24±0.86)ng/ml vs(12.68±1.01)ng/mL,(68.18±9.01)pg/mL vs(80.78±10.24)pg/mL,(34.16±5.06)ng/mL vs(49.76±5.47)ng/mL](P<0.05);CD3+、CD4+显著高于对照组[(66.15±7.20)%vs(62.03±6.85)%,(45.13±7.90)%vs(37.42±7.06)%](P<0.05),CD8+显著低于对照组[(34.16±5.06)%vs(49.76±5.47)%](P<0.05)。结论:布地奈德联合槐杞黄颗粒治疗小儿哮喘的疗效显著,能够增强患儿的免疫功能,改善肺功能,降低血清LTD4、NGF、TIMP-1的水平。