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Objective:To investigate the effect and mechanism of Chaihu Jia Longgu Mulitang （CJLM） on hippocampal NOD-like receptor protein 3 （NLRP3）inflammasome pathway in rats with depression. Method:Sixty male SD rats were randomly divided into a normal group，a model group， a MCC950 （1 mg·kg<sup>-1</sup>） group， and high- （13 g·kg<sup>-1</sup>）， medium- （6.5 g·kg<sup>-1</sup>）， and low-dose （3.25 g·kg<sup>-1</sup>） Chaihu Jia Longgu Mulitang groups， with 10 rats in each group．The depression model was induced by isolation combined with chronic unpredictable mild stimulation（CUMS） in rats except for those in the normal group. Rats were treated correspondingly for 21 days by intraperitoneal injection in the MCC950 group and gavage in other groups. The normal group and the model group received an equal volume of normal saline. The depression-like behaviors of rats were observed by sucrose preference test （SPT） and novelty-suppressed feeding test. Enzyme-linked immunosorbent assay （ELISA） was used to determine the levels of interleukin-1<italic>β </italic>（IL-1<italic>β</italic>） and IL-18 in the hippocampus of depressed rats. Western blot was used to detect the protein levels of NLRP3， apoptosis-associated speck-like protein containing a C-terminal caspase recruitment domain （ASC）， and Caspase-1. Result:Compared with the normal group， the model group showed decreased sucrose preference rate （<italic>P</italic><0.01）， prolonged novelty-suppressed feeding time （<italic>P</italic><0.01）， enhanced protein expression of NLRP3，ASC， and caspase-1<italic> </italic>（<italic>P</italic><0.05， <italic>P</italic><0.01）， and elevated expression of IL-1<italic>β</italic> and IL-18 （<italic>P</italic><0.01）. Conclusion:CJLM can alleviate depression-like behaviors in CUMS-induced model rats， and the underlying mechanism is related to the inhibition of the NLRP3 inflammasome pathway．
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Objective:To observe the effect of modified Erchentang on the expression of CXC chemokine ligand (CXCL) 8-CXC chemotaxis factor receptor (CXCR) 1/2 genes in the lung tissue of rats with chronic obstructive pulmonary disease (COPD), in order to explore the anti-inflammatory molecular mechanism of Erchentang on COPD. Method:Forty SD rats were randomly divided into normal group, model group, Jizhi syrup group and modified Erchentang group. COPD models in rats were prepared by cigarette smoke and dripping lipopolysaccharide (LPS) in the trachea. After modeling, normal and model groups were intragastrically given normal saline solution, Jizhi syrup group was given Jizhi syrup（10 g·kg-1），and modified Erchentang group was given intragastrically corresponding herbal drugs (10 g·kg-1) for 14 days. The levels of chemokines CXCL1, CXCL8 were detected by enzyme-linked immunosorbent assay in rat bronchoalveolar lavage fluid (BALF). The mRNA expressions of CXCL8, CXCR1 and CXCR2 were detected by quantitative real time PCR (Real-time PCR). Western blot was used to detect the levels of CXCL8, CXCR1 and CXCR2 protein, the pathological changes of lung tissues were observed by hematoxylin-eosin(HE) staining,and immunohistochemistry (IHC) method was used to detect the expressions of CXCL8, CXCR1 and CXCR2 protein in the lung tissue of all the groups. Result:The levels of chemokines CXCL1, CXCL8 in rats BALF were increased significantly (P<0.01), the expressions of CXCL8，CXCR1 and CXCR2 mRNA and protein were increased significantly (P<0.05, P<0.01) in model group compared with normal group. Compared with model group, the expressions of CXCL8, CXCR1 and CXCR2 mRNA and protein were decreased significantly (P<0.05), and the levels of chemokines CXCL1, CXCL8 in rats BALF were decreased significantly (P<0.01) in modified Erchentang. Conclusion:Modified Erchentang has an anti-inflammatory effect on COPD. The mechanism may be related to inhibiting the expressions of CXCL8, CXCR1, CXCR2 mRNA and protein, and reducing the release of chemokines CXCL1, CXCL8.
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Objective::To establish the HPLC fingerprint of carbonized ginger and to determine the contents of zingerone, 6-gingerol, 6-shogaol, 10-gingerol, 8-shogaol and 10-shogaol with quantitative analysis of multi-components by single marker (QAMS). Method::The fingerprint of carbonized ginger was established by HPLC. All samples were analyzed by Waters SymmetryShield™ RP18 column (4.6 mm×250 mm, 5 μm) with gradient elution by acetonitrile(A)-water(B) (0-30 min, 25%-70%A; 30-50 min, 70%-90%A; 50-60 min, 90%A), the flow rate was 1.0 mL·min-1, the detection wavelength was set at 240 nm and the column temperature was 30 ℃. Zingerone, 6-gingerol, 8-gingerol, 6-shogaol, 10-gingerol, 8-shogaol and 10-shogaol was chosen as marker ingredients to establish HPLC fingerprint of carbonized ginger decoction pieces. Taking 6-gingerol as internal reference standard, the contents of zingerone, 6-shogaol, 10-gingerol, 8-shogaol and 10-shogaol were determined at the detection wavelength of 220 nm and 280 nm according to the relative correction factor. Result::The HPLC fingerprint of carbonized ginger was obtained and 10 common peaks were designated, and 7 of them were identified as zingerone, 6-gingerol, 8-gingerol, 6-shogaol, 10-gingerol, 8-shogaol and 10-shogaol, respectively. And there were no significant differences between the quantitative results of external standard method and QAMS. It is suggested that the content limits of carbonized ginger should be not less than 0.020%of zingerone (C11H14O3), 0.050%of 6-gingerol (C17H26O4), 0.120%of 6-shogaol (C17H24O3), 0.080%of 10-gingerol (C21H34O4), 0.030%of 8-shogaol (C19H28O3) and 0.050%of 10-shogaol (C21H32O3) calculated with reference to the dried products, respectively. Conclusion::The developed method is accurate and feasible, which can provide a simple and effective method for the quality control of carbonized ginger.
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Objective:To study the effect of modified Erchentang on levels of interleukin-12 (IL-12), interferon-γ (IFN-γ), interleukin-9 (IL-9), interleukin-4 (IL-4) and interleukin-13 (IL-13) in plasma and bronchoalveolar lavage fluid (BALF) of all rats, as well as expressions of interleukin-4 (IL-4) receptor (IL-4R1) and interleukin-13 (IL-13) receptor (IL-13RA1) in bronchioles tissue of rats with chronic obstructive pulmonary disease (COPD). Method:Fifty SD rats were randomly divided into 5 groups, namely normal group, model group, and low, middle and high-dose modified Erchentang groups (5, 10, 20 g·kg-1), with 10 rats in each group. COPD in rat was prepared by using cigarette smoke combined with dripping lipopolysaccharide (LPS) in trachea. After the modeling, normal and model groups were given normal saline solution through intragastric (ig) administration, while other groups were given corresponding herbal drugs (5, 10, 20 g·kg-1) intragastrically (ig) for 14 days. The levels of IL-12, IFN-γ, IL-9, IL-4 and IL-13 in plasma and BALF were detected by Enzyme-linked immunosorbent assay (ELISA) method， and immunohistochemistry (IHC) method was used to detect the expressions of IL-4R1 and IL-13RA1 in bronchioles tissue of all of the groups. Result:Compared with the normal group, the levels of IL-12 and IFN-γ were decreased significantly (P<0.01), but the levels of IL-9, IL-4 and IL-13 in plasma and BALF were significantly increased (P<0.01), and the expressions of IL-4R1 and IL-13RA1 in bronchioles tissue were increased significantly (P<0.01) in model group. Compared with the model group, the levels of IL-12 and IFN-γ were increased significantly, while the levels of IL-9, IL-4 and IL-13 in plasma and BALF were decreased significantly (P<0.01), and the expressions of IL-4R1 and IL-13RA1 in bronchioles tissue were decreased significantly (P<0.01) in modified Erchentang groups (10, 20 g·kg-1). Conclusion:Modified Erchentang has effects in resisting inflammatory and protecting tissue structure of bronchioles. Its mechanism may be correlated with increasing the levels of IL-12, IFN-γ and reducing the levels of IL-9, IL-4 and IL-13 in plasma and BALF, and inhibiting the expressions of IL-4R1 and IL-13RA1 in bronchioles tissue.
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Objective:To study the effect of modified Xiao Chaihutang on the expressions of excitatory amino acid transporters（EAATs） and vesicle glutamate transporters（VGLUTs）in hippocampus of rats with chronic depression， in order to explore the anti-depressant mechanism of modified Xiao Chaihutang based on glutamate transport. Method:A total of 120 SD rats were randomly divided into normal group， model group， and low， middle and high-dose modified Xiaochaihutang groups （6.5， 13， 26 g·kg-1） and riluzole group， with 20 rats in each group．Except normal group， the depression model of rats was prepared through Chronic restraint stress（CRS）. The normal group and the model group were intragastrically （ig） given normal saline. The modified Xiao Chaihutang groups were intragastrically given corresponding herbal drugs （6.5， 13， 26 g·kg-1）， and the Riluzole group was given Riluzole 20 mg·kg-1 through intraoeritoneal injection for 21 days， once a day. Then the depressive behaviors of rats were observed by forced swimming test （FST） and tail suspension test （TST）. The level of glutamic acid （Glu） in rats hippocampus was determined by high performance liquid chromatography （HPLC）. The mRNA expressions of EAAT1， EAAT2 and EAAT3 in hippocampus were detected by Real-time fluorescence quantitative polymerase chain reaction （Real-time PCR）method. Western blot was used to detect the protein expressions of EAAT1， EAAT2， EAAT3， VGLUT1 and VGLUT2 in rat hippocampus tissue. Nissl staining was used to observe the morphology of hippocampal neurons in rats. Immunohistochemical（IHC）S-P method were used to detect the location expressions of EAAT1， EAAT2 and NeuN proteins in rat hippocampal CA1 region tissue. Result:The immobility times in FST and TST were increased significantly（P<0.01）， the mRNA and protein expressions of EAAT1，EAAT2，EAAT3 were decreased significantly （P<0.01）， and as well as the expressions of VGLUT1 and NeuN were decreased significantly（P<0.01）， while the level of Glutamate and the expression of VGLUT2 were increased significantly（P<0.01） in model group， compared with normal group. Compared with model group，the immobility times in FST and TST were decreased significantly（P<0.05， P<0.01）， mRNA and protein expressions of EAAT1，EAAT2，EAAT3 were increased significantly（P<0.01）， and expressions of VGLUT1 and NeuN were increased significantly（P<0.01）. However， the level of Glutamate and the expression of VGLUT2 were decreased significantly（P<0.01）， and the damage of hippocampal neurons in rats was mild in middle and high-dose modified Xiao Chaihutang groups. Conclusion:Modified Xiao Chaihutang has an anti-depressive effect. Its mechanism may be related to its up-regulation of expressions of EAAT1， EAAT2， EAAT3 genes and VGLUT1 protein in the hippocampus of depression model rats.
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Objective:To study the effect of Chaihu Jia Longgu Mulitang on phosphatidylinositol-3-kinases （PI3K）/protein kinase B （Akt）/glycogen synthase kinase 3β （GSK3β）/β-catenin signaling pathway of hippocampus in rats with depression. Method:A total of 120 SD rats were randomly divided into normal group，model group， and low， middle and high-dose Chaihu Jia Longgu Mulitang groups（3.25，6.5，13 g·kg-1）， and fluoxetine group， with 20 rats in each group. Except normal group， the depression model was prepared through chronic unpredictable mild stimulation（CUMS）. The normal group and the model group were given normal saline with 6.5 g·kg-1 by gavage. Chaihu Jia Longgu Mulitang groups were intragastrically given corresponding herbal drugs 3.75，6.5，13 g·kg-1， while fluoxetine group was intragastrically given fluoxetine 10 mg·kg-1 for 21 days， once a day. Then the depressive behaviors of rats were observed by sucrose preference test （SPT） and forced swimming test （FST）. Western blot was used to detect the protein expressions of PI3K，Akt，GSK3β and phosphorylation level. Result:Compared with normal group，the sucrose preference index was decreased significantly，while the immobility time in FST was increased significantly（P<0.01）， the protein expressions of PI3K， p-PI3K p110， p-PI3K p85 were decreased significantly （P<0.01）， and expressions of Akt， p-Akt Thr308，p-Akt Ser473， p-GSK3β Ser9 and β-catenin were decreased significantly（P<0.01）， while the level of GSK3β， p-GSK3β Tyr216 were increased significantly in model group（P<0.05，P<0.01）. Compared with model group，Chaihu Jia Longgu Mulitang could increase sucrose preference index and decrease the immobility time in FST（P<0.01）， the protein expressions of PI3K p110 and PI3K p85 was increased significantly （P<0.01）， levels of Akt Thr308，Akt Ser473， p-GSK3β Ser9， β-catenin were increased significantly （P<0.01）， whereas levels of GSK3β， and GSK3β Tyr216 were decreased significantly. Conclusion:Chaihu Jia Longgu Mulitang could increase protein expression and activity of PI3K in rat hippocampus， activate Akt， inhibit GSK3β kinase activity and prevent β-catenin from degradation， so as to increase PI3K/Akt pathway activity in rat hippocampus， and protect hippocampal neurons.
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Objective: To study the effect of modified Erchentang on expressions of Toll-like receptor 4 (TLR4), myeloid differentiation factor (MyD88) and nuclear factor-κB (NF-κB) genes in the lung tissue homogenate of rats with chronic obstructive pulmonary disease (COPD). Method: Forty SD rats were randomly divided into normal group, model group, modified Erchentang group and EVP4593 (NF-κB inhibitor) group. Rat COPD models were prepared through cigarette smoke and tracheal dripping with lipopolysaccharide (LPS). After the modeling, normal and model groups were intragastrically given normal saline solution, EVP4593 group was given EVP4593(1 mg · kg-1) through subcutaneous injection, and modified Erchentang group was given corresponding herbal drugs intragastrically (10 g · kg-1) for 14 days. The levels of high mobility group box 1(HMGB1), chemokines CXCL-2, CXCL-3 and monocyte chemoattractant protein-1 (MCP-1) in rats serum were detected by enzyme-linked immunosorbent assay in rats serum. The expressions of Toll-like receptors 4(TLR4), myeloid differentiation factor (MyD88) and nuclear factor-κB p65 (NF-κB p65) mRNA were detected by Real-time fluorescence quantitative PCR (Real-time PCR) method. Western blot were used to detect the levels of TLR4, MyD88, NF-κB p65 and p-NF-κB p65 protein. Immunohistochemistry (IHC) method was used to detect the localization and expressions of TLR4, MyD88 and p-NF-κB p65 protein in the lung tissue. Result: The mRNA and protein expressions of TLR4, MyD88 and NF-κB p65 were increased significantly (PPκB p65 mRNA and protein were decreased significantly (PConclusion: Modified Erchentang may inhibit the inflammatory response of COPD effectively. The mechanism may be related to the inhibition of the expressions of the signal molecule genes involved in the TLR4/MyD88/NF-κB pathway and the reduction of the release of HMGB1, CXCL-2, CXCL-3 and MCP-1.
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Objective: To observe the effect of modified Erchentang on the expressions of NLRP3 inflammasome genes in peripheral blood mononuclear cells (PBMCs) and the levels of interleukin-1β(IL-1β)and interleukin-18(IL-18)and chemokine8 (CXCL8) in lung tissue of rats with chronic obstructive pulmonary disease (COPD), in order to explore the molecular mechanism of modified Erchentang against inflammation of COPD. Method: Forty SD rats were randomly divided into normal control group, model group, MCC950 (NLRP3 inhibitor) group and modified Erchentang group. The COPD model of rats was prepared by using cigarette smoke and dripping with lipopolysaccharide (LPS). During the modeling period (from the 1st to the 30th day), the MCC950 group received a single intraperitoneal injection with 60 mg · kg-1 on the first day of the experiment,and the modified Erchentang group was given intragastric administration with 10 g · kg-1, once every 2 days. From the 31st to the 45th day, the MCC950 group was intraperitoneally injected with 3 mg · kg-1, once every 2 days, the modified Erchentang group was given intragastric administration with 10 g · kg-1, twice a day, and the normal group and the model group received normal saline (NS) with 10 g · kg-1, twice a day. The levels of interleukin-1β(IL-1β), interleukin-18(IL-18) and chemokine8 (CXCL8) in rats lung tissue homogenate were detected by enzyme-linked immunosorbent assay (ELISA). The expressions of NLRP3, apoptosis-associated speck-like protein (ASC) and cysteinyl aspartate specific proteinase-1 (Caspase-1) mRNA in PBMCs were measured by Real-time fluorescence quantitative PCR (Real-time PCR). Western blot was used to detect the levels of NLRP3, ASC and Caspase-1 proteins in PBMCs. Immunohistochemical(IHC)method was used to detect the expressions of NLRP3, ASC and Caspase-1 proteins in lung tissues. Result: The expressions of NLRP3, ASC and Caspase-1 mRNA and protein were increased significantly (PPPβ and CXCL8 in lung tissue homogenate in model group were significantly higher than those in the control group. However, compared with model group, the levels of IL-18, IL-1β and CXCL8 were decreased significantly (PPConclusion: NLRP3 inflammasome is involved in the inflammatory response in COPD rats. Modified Erchentang may inhibit the inflammatory response of COPD effectively. The mechanism may be correlated with the reduction of NLRP3, ASC and Caspase-1 gene expressions, and the inhibition of the release of IL-18, IL-1β and CXCL8.
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Objective:To observe the clinical efficacy of modified Erchentang on CXC chemokine ligand receptors (CXCR1/2)and their ligands CXCL8,macrophage inflammatory protein -2(MIP-2) in patients of chronic obstructive pulmonary disease(AECOPD)at acute exacerbation stage,and assess the effect and mechanism of modified Erchentang on anti-inflammatory in patients of AECOPD. Method:This study was a multicenter, randomized single blind, controlled trial. The authors selected 200 cases in conformity to the standards of AECOPD. The AECOPD patients were randomly divided into modified Erchentang group and control group. In addition to the western medicine, modified Erchentang was also given to the modified Erchentang group, and Jizhitangjiang was given to the control group for 14 days. Each group was observed for the alleviation of the symptoms. Euzyme-linked immunosorbent assay (ELISA) was used to determine the levels of CXCL8 and MIP-2 in the patients' plasma of all groups before and after treatment. Western blot were used to detect the levels of CXCR1, CXCR2 and CXCL8 protein in peripheral blood mononuclear cells(PBMCs). Immunocytochemistry (ICC) method was used to detect the expressions of CXCL8, CXCR1 and CXCR2 protein in PBMCs. Result:The level of CXCL8 in plasma, and the expressions of CXCR1, CXCR2 and CXCL8 mRNA and protein in the modified Erchentang group were decreased significantly than those in the control group(PPConclusion:Modified Erchentang has an anti-inflammatory effect on AECOPD. Its mechanism may be related to the down-regulation of the expressions of CXCL8, CXCR1 and CXCR2, the reduction of synthesis and release of CXCL8 and MIP-2, the inhibition of the chemotaxis and activity of inflammatory cells, and the prevention of inflammation progress.
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Kyrgyzstan is a mountainous country in the northeastern part of Central Asia which shares borders to the southeast with China. Due to their extreme environment and climate, there are a diverse range of species of plants. Many of the plants used in Kyrgyz folk medicine have not been studied using modern scientific techniques. This paper introduced the basic situation of medicinal herbs in Kyrgyzstan by comparing the differences traditional use between China and Kyrgyzstan, and looked for traditional medicinal plant research to provide basis for the development and cooperation of China and Kyrgyzstan.
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Humans , China , Kyrgyzstan , Medicine, Traditional , Methods , Plants, Medicinal , Chemistry , ClassificationABSTRACT
<p><b>OBJECTIVE</b>To compare the efficacy on vertebrobasilar insufficiency (VBI) between auricular acupuncture therapy and oral administration of medicine.</p><p><b>METHODS</b>Sixty patients of VBI were randomized into an auricular acupuncture therapy group and a medicine group, 30 cases in each one. In the auricular acupuncture group, acupuncture was applied bilaterally to gan (CO12) and jiejie (HX8) on the ears and needles were retained for 15 min. After needle withdrawal, the vaccariae semen were fixed with plaster at naogan (AT3, 4i), zhen (AT3), jing (AH12), shen (CO10) and pi (CO13) on the ears. In the medicine group, flunarizine hydrochloride capsules (Sibelium), 5mg were prescribed for oral administration, once every night. The treatment lasted continuously for 2 weeks (14 days) in the two groups. In 2 weeks, the clinical efficacy was assessed and the transcranial doppler (TCD) examination was performed.</p><p><b>RESULTS</b>After treatment, the symptom scores were all apparently reduced in the patients of the two groups (P < 0.01, P < 0.05). Compared with the medicine group, the reduced score was much more obvious in the auricular acupuncture group (P < 0.05), indicating the significant difference. After treatment, with TCD examination, the blood velocity was increased to different degrees in the patients of low velocity type in the auricular acupuncture group and the medicine group; that was reduced to different degrees in the patients of high velocity type in the auricular acupuncture group and the medicine group. All of them were different significantly as compared with those before treatment (all P < 0.05). But the difference was not significant between the two groups (both P > 0.05). In comparison of clinical efficacy between the two groups, the effective rate was 93.3% (28/30) in the acupuncture group and better than 76.7% (23/30) in the medicine group, indicating the significant difference in comparison (P < 0.05).</p><p><b>CONCLUSION</b>The auricular acupuncture therapy achieves the definite efficacy on VBI and the efficacy is better than flunarizine hydrochloride capsules.</p>
Subject(s)
Adult , Aged , Female , Humans , Male , Middle Aged , Acupuncture Points , Acupuncture, Ear , Treatment Outcome , Vertebrobasilar Insufficiency , TherapeuticsABSTRACT
<p><b>OBJECTIVE</b>To Systematic review and meta-analysis of short and long term efficacy and safety of procedure for prolapse and hemorrhoids.</p><p><b>METHODS</b>Electronic databases including Cochrane Library, PubMed, OVID, SpringerLinker, ScinceDirect, EBSCO, CNKI, VIP, WanFang Data and CBM were searched. The date of search was between January 2000 and January 2013. Randomized controlled trials (RCTs) were indentified studying association of Compare PPH and Milligan-Mogan (MMH) treatment. Study selection and meta-analysis were conducted according to the Cochrane Handbook for RevMan 5.1 software.</p><p><b>RESULTS</b>The trials involving 1343 patients were included. The results of meta-analysis indicated: compared with MMH, PPH operative time (OR = -11.05, 95%CI: -15.15--6.95, P < 0.01), duration of hospitalization (OR = -3.07, 95%CI: -4.46--1.69, P < 0.01) and return to normal activity time (OR = -7.17, 95%CI: - 9.13--5.20, P < 0.01) was short, postoperative pain light (OR = -3.13, 95%CI: -4.38--1.88, P < 0.01), but the high cost of treatment (OR = 2534.2, 95%CI: 509.0-4559.4, P = 0.01). Long-term efficacy, PPH was higher patient satisfaction (OR = 2.21, 95%CI: 1.03-4.75, P = 0.04), but the recurrence rate of prolapse (OR = 3.75, 95%CI: 1.75-8.06, P < 0.01) and reoperation rate (OR = 7.90, 95%CI: 1.78-35.03, P < 0.01) higher. The incidence of anal stenosis and anal incontinence postoperative were higher than MMH (P > 0.05). The difference of post operative anal stenosis and anal incontinence and residual skin tag rate were not statistically significant (all P > 0.05).</p><p><b>CONCLUSIONS</b>PPH surgery can be used as replacement therapy of MMH for III°-IV° prolapsed hemorrhoids. But we should inform patients of prolapse recurrence and reoperation risk of PPH in the long term.</p>
Subject(s)
Humans , Anal Canal , General Surgery , Colorectal Surgery , Hemorrhoids , General Surgery , Randomized Controlled Trials as Topic , Recurrence , Reoperation , Risk FactorsABSTRACT
Ginsenoside Rb1 is an active component in ginseng. Previous in vitro experiments showed that ginsenoside Rb1, could inhibit lipolysis and promote glucose transporter in adipocytes. This study focused on the effect of ginsenoside Rb1 in insulin resistance and ectopic fat deposit in obese mice induced by high fat diet and its molecular mechanism. Obese male C57/L mice induced by high fat diet were randomly divided into the diet-induced obesity group (DIO group), the ginsenoside Rb1 group (Rb1 group) and the rosiglitazone group (Rog group), and continuously fed with high fat diet. In addition, male C57/L mice fed with normal diet were selected as the normal group (NC group). Mice in Rb1 group and Rog groups were intraperitoneally injected with ginsenoside Rb1 and rosiglitazone with the dosage of 20 mg x kg(-1) and 10 mg x kg(-1), respectively. NC and DIO groups were intraperitoneally injected with the same amount of saline. Two weeks later, the intraperitoneal glucose tolerance test (IPGTT) was performed. Three days later, the mice were killed, and their serum samples were collected to detect insulin and free fatty acid (FFA). Their livers were weighed to examine the triglyceride content, and a pathological detection was performed. Epididymal adipose tissues were weighed, and PDE3B, HSL and perilipin were detected by Western blotting. The results showed that the treatment with ginsenoside Rb1 for two weeks could improve the glucose tolerance of obese mice. Except for 0-120 min, the areas under the glucose tolerance curve (0-30 min, 0-60 min and 0-90 min) in the Rb1 group were less than that in the DIO group (P < 0.05, n = 5), with a much lower HOMA-IR (P < 0.05, n = 5). The fat level of obese mice was significantly reduced by Rbl (P < 0.05, n = 5), and so were liver weight/weight (P < 0.05, n = 8). The increased serum FFA of obese mice declined after the treatment of Rb1 (P < 0.05, n = 8). Rb1 could partially recover the expression of perilipin in adipose tissues, but without obvious change in the expressions of PDE3B and HSL and the phosphorylated activation. The above findings indicated that ginsenoside Rb1 could reduce the release of FFA and alleviate the ectopic deposit of triglyceride by up-regulating the expression of perilipin in adipose tissue, which may be one of its mechanisms for improving the insulin resistance and abnormal glucose metabolism of organisms.
Subject(s)
Animals , Male , Mice , Adipose Tissue , Pathology , Body Weight , Diet, High-Fat , Dose-Response Relationship, Drug , Fatty Acids, Nonesterified , Blood , Gene Expression Regulation , Ginsenosides , Pharmacology , Glucose Tolerance Test , Insulin , Blood , Insulin Resistance , Liver , Metabolism , Mice, Inbred C57BL , Obesity , Blood , Metabolism , Pathology , Organ Size , Triglycerides , MetabolismABSTRACT
An efficient modified route based on the targeting mechanism of antibacterial fluoroquinolones for the shift from the antibacterial activity to the antitumor one was further developed. Using a fused heterocyclic ring, s-triazolothiadiazine as a carboxyl bioisostere of ciprofloxacin, the title compounds, 1-cyclopropyl-6-fluoro-7-piperazin-1-yl-3-(6-substituted-phenyl-7H-[1, 2, 4]triazolo[3, 4-b][1, 3, 4]thiadiazin-3-yl)-quinolin-4(1H)-ones (5a-5e) and their corresponding N-acetyl products (6a-6e), were designed and synthesized, separately. Meaningfully, a ring-contraction of fused six-membered thiadiazine occurred by a sulfur extrusion reaction gave new tri-acetylated fused heterocycles related to pyrazolo[5, 1-c][1, 2, 4] triazoles (7a-7e). The in vitro antitumor activity against L1210, CHO and HL60 cell lines was also evaluated for the synthesized fifteen heterocycles compared to parent ciprofloxacin by methylthiazole trazolium (MTT) assay. Interestingly, the results displayed that fifteen fused heterocyclic compounds showed more significant growth inhibitory activity (IC50 < 25.0 micromo x L(-1)) than that of parent ciprofloxacin (IC50 > 150.0 micromol x L(-1)), and the active order decreased from 7a-7e to 5a-5e to 6a-6e, respective.
Subject(s)
Animals , Cricetinae , Humans , Mice , Antineoplastic Agents , Chemistry , Pharmacology , CHO Cells , Cell Line, Tumor , Ciprofloxacin , Pharmacology , Cricetulus , Fluoroquinolones , Chemistry , Pharmacology , HL-60 Cells , Inhibitory Concentration 50 , Leukemia L1210 , Pathology , Structure-Activity Relationship , Thiadiazines , Chemistry , Pharmacology , Triazoles , Chemistry , PharmacologyABSTRACT
<p><b>OBJECTIVE</b>To analyze the clinicopathological features and prognosis of colorectal cancer patients with preoperative cancer-related anemia.</p><p><b>METHODS</b>Clinical data of 354 patients with colorectal cancer in the Second Affiliated Hospital of Guangzhou Medical College from January 2003 to July 2009 were analyzed retrospectively. Those with hemoglobin(Hb)<120 g/L before surgery were defined as cancer-related anemia.</p><p><b>RESULTS</b>Of the 354 colorectal cancer cases, 195 were males and 159 were females. The median age was 65(range 22-92) years. Preoperative cancer-related anemia tended to be occurred in female(P<0.01) and those with preoperative albumin ≤35 g/L (P<0.01), right colon cancer(P<0.01) and full-thickness invasion(P<0.05). Cox regression analysis showed preoperative cancer-related anemia was an independent unfavorable factor for overall survival (HR=1.60, 95% CI:1.05-2.44; P<0.05), but not for disease-free survival (HR=1.43, 95% CI:0.97-2.12; P>0.05) in colorectal cancer.</p><p><b>CONCLUSIONS</b>Preoperative cancer-related anemia plays an important role in the development and prognosis of colorectal cancer and great attention should be paid to clinical practice.</p>
Subject(s)
Adult , Aged , Aged, 80 and over , Female , Humans , Male , Middle Aged , Young Adult , Anemia , Colorectal Neoplasms , General Surgery , Prognosis , Retrospective StudiesABSTRACT
To explore an efficient strategy for further development of anticancer fluoroquinolone candidates derived from ciprofloxacin, a heterocyclic ring as the bioisosteric replacement of C3 carboxyl group led to a key intermediate, oxadiazole thiol (5), which was further modified to the bis-oxadiazole methylsulfides (7a-7h) and the corresponding dimethylpiperazinium iodides (8a-8h), respectively. Structures were characterized by elemental analysis and spectra data, and their anticancer activities in vitro against CHO, HL60 and L1210 cancer cells were also evaluated by MTT assay. The preliminary results show that piperazinium compounds (8) possess more potent activity than that of corresponding free bases (7).
Subject(s)
Animals , Cricetinae , Humans , Antineoplastic Agents , Chemistry , Pharmacology , CHO Cells , Cell Line, Tumor , Cell Proliferation , Ciprofloxacin , Chemistry , Cricetulus , Drug Design , HL-60 Cells , Inhibitory Concentration 50 , Leukemia L1210 , Molecular Structure , Oxadiazoles , Chemistry , Pharmacology , Piperazines , Chemistry , PharmacologyABSTRACT
<p><b>BACKGROUND</b>Domestic violence (DV) is not only a devastating societal problem, but also a severe medical and mental health problem worldwide. Our previous study has shown that perpetrators were with higher prevalence of self-reported symptoms than that of controls. This study based on our former large scale population-based samples is aimed to further explore the correlations between the symptoms and psychosocial factors of the perpetrators with DV. It was helpful to provide some insight into possible strategies for clinicians to reduce the symptoms of the perpetrators with DV in China.</p><p><b>METHODS</b>From our former population-based epidemiological samples, 1098 households with a history of DV in preceding year, 318 perpetrators with DV were randomly selected. Face-to-face interviews were conducted. Symptom Checklist-90 (SCL-90) was administrated to check and classify the symptoms of perpetrators, Eysenck's personality questionnaire (EPQ), trait coping style questionnaire (TCSQ), life events scale (LES) and social supporting rating scale (SSRS) were administrated to evaluate the psychosocial factors of perpetrators. The correlation analysis was used to analyze the relationships between the symptoms and psychosocial factors of perpetrators of DV.</p><p><b>RESULTS</b>The global and all subscale scores of SCL-90 were significantly positively correlated with EPQ-N, negative TCSQ and negative LES scores (P < 0.01). The global score of SCL-90 was negatively correlated with both objective and subjective SSRS (P < 0.01). The negative LES and negative TCSQ were significantly positively correlated with EPQ-N (P < 0.01). Negative TCSQ was significantly positively correlated with negative LES and negatively correlated with subjective SSRS (P < 0.01).</p><p><b>CONCLUSIONS</b>The self-reported symptoms of perpetrators with DV were strongly correlated with their psychosocial factors, such as the neurotic personality, negative coping style, more negative life events and less subjective social supports. It suggested bio-psycho-socially oriented interventions were necessary to buffer the symptoms of perpetrators with DV.</p>
Subject(s)
Adult , Female , Humans , Male , Middle Aged , China , Domestic Violence , Psychology , Surveys and QuestionnairesABSTRACT
<p><b>OBJECTIVE</b>The aim of this study is to observe the effect of combined amiodarone and antiarrhythmic peptide (AAP10) use on the incidence of induced ventricular arrhythmias in healed myocardial infarction (MI) rabbits.</p><p><b>METHODS</b>Twenty Japanese rabbits underwent thoracotomy without coronary artery ligation (Sham, group A), the middle left circumflex branch were ligated to induce MI in 180 Japanese rabbits. Eight weeks after operation, 124 rabbits survived MI operation and were divided into four groups: control group (group B, n = 31), amiodarone group (group C, n = 31), AAP10 group (group D, n = 31) and amiodarone plus AAP10 group (group E, n = 31). The A and B and D groups were treated with saline 2 ml/d, the C and E groups were treated with 2 ml saline containing amiodarone 100 mg×kg(-1)×d(-1). All rabbits were examined by echocardiogram at 12 weeks after operation, then anesthetized by sodium barbital, the left wedge ventricular preparations were cannulated and artery perfused by Tyrode's solution in vitro in the absence (Group A, B and C) and presence of AAP10 (500 nmol/L, Group D and E). The volume electrocardiogram, QT Interval, QRS interval, effective refractory period (ERP), the T-peak to T-end interval (T(p-e)), and ventricular tachycardia episodes induced by programmed stimulation were recorded. The T(p-e)/QT ratio was calculated. After perfusion, gap junctions protein connexin 43 (Cx43) expression was detected by Western blot and immunofluorescence.</p><p><b>RESULTS</b>The incidence of induced ventricular tachycardia episodes of group A, B, C, D, E was 0, 62.5%, 26.9%, 40.0%, 22.2% respectively. The incidence of induced ventricular tachycardia episodes of group E was less than group B. The T(p-e)/QT ratio in group B, C, D were greater than in group A. The T(p-e)/QT ratio of group E was less than group B. The myocardial Cx43 in the group B was down-regulated and disorganized compared to group A, up-regulated in group C and E compared to group B, up-regulated in group E compared to group D. The Cx43 in the heart of group D and E were well organized than in group B and C.</p><p><b>CONCLUSIONS</b>The artery perfused rabbits wedge preparations with healed myocardial infarction with high incidence of induced ventricular tachycardia episodes are good platform for ventricular arrhythmias research. Combined amiodarone and AAP10 use could decrease the T(p-e)/QT ratio and the incidence of induced ventricular tachycardia episodes. Amiodarone and AAP10 have synergistic effects on upregulating Cx43 and preventing ventricular arrhythmias in this rabbit model of healed myocardial infarction.</p>
Subject(s)
Animals , Male , Rabbits , Amiodarone , Pharmacology , Therapeutic Uses , Anti-Arrhythmia Agents , Pharmacology , Therapeutic Uses , Arrhythmias, Cardiac , Connexin 43 , Metabolism , Myocardial Infarction , Drug Therapy , Metabolism , Oligopeptides , Pharmacology , Therapeutic Uses , Treatment OutcomeABSTRACT
<p><b>OBJECTIVE</b>To clone the sequence of human Angiostatin cDNA and obtain the protein of recombinant angiostatin for further development.</p><p><b>METHODS</b>Fresh human liver tissue was used for the extraction of total RNA and amplified the Angiostatin cDNA through RT-PCR method . After the recombinant plasmid pET30a-Angiostatin was constructed and confirmed, it was transduced into Rosetta (DE3). Then the transformation was used for fermentation and induced expression. The protein was identified by Western Blot and purified by Ni-NTA affinity chromatography.</p><p><b>RESULTS</b>The sequence of human Angiostatin cDNA was identical with genebank. Angiostatin (K1-3) was expressed and purified. The target protein made up 30% of the total bacterial protein. The purity is above 90%.</p><p><b>CONCLUSION</b>Angiostatin K (1-3) can be reached using fusion vector pET30a. The product have the biological activity.</p>
Subject(s)
Humans , Angiostatins , Genetics , Metabolism , Cloning, Molecular , Escherichia coli , Genetics , Metabolism , Gene Expression , Liver , Metabolism , Recombinant Fusion Proteins , Genetics , MetabolismABSTRACT
<p><b>OBJECTIVE</b>To construct antisense c-Jun N-terminal kinase 1 (JNK1) eukaryotic fluorescent expressing vector and JNK1-/- human embryo lung fibroblasts cell line.</p><p><b>METHODS</b>Trizol reagent was used to extract total RNA in HELF. The proper primers of JNK1 were chosen and synthesized. RT-PCR and gene recombinant techniques were used to construct the fragment of JNK1. After purification, the PCR products were cut, and JNK1 were inserted reversely into eukaryotic fluorescent expressing vector pEGFP-C1. Enzyme-cutting and DNA auto-sequencing were used to prove the successful construction of JNK1 eukaryotic expressing vector. Then plasmids were extracted and transfected into HELF cells and screen by G418 24 h later. Monoclone was chosen and cultured. Fluorescent imaging and Western blot were used to identify the JNK1-/- HELF cell line.</p><p><b>RESULTS</b>Sequence analysis of pEGFP-C1-as JNK1 plasmids was same as expected. The expression level of JNK1 was inhibited markedly.</p><p><b>CONCLUSION</b>Construction of antisense JNK1 eukaryotic fluorescent expressing vectors and JNK1-/- HELF cell line is successful.</p>