Effect of tamibarotene on innate immune response in the model of Porphyromonas gingivalis induced periodontitis / 中华口腔医学杂志

<p><b>OBJECTIVE</b>To investigate the effect of Am80 on innate immune response of Porphyromonas gingivalis (Pg) W83-induced periodontitis in mice.</p><p><b>METHODS</b>Twenty-five mice were randomly divided into five groups, control group, PgW83-induced periodontitis group (periodontitis), Am80 (10 µg/d) treatment group (low-dose group), Am80 (50 µg/d) treatment group (middle-dose group), Am80 (100 µg/d) treatment group (high-dose group). The distance of alveolar bone resorption in each mouse was observed and measured by a dissecting microscope. Enzyme-linked immunosorbent assay (ELISA) was used to detect the level of serum anti-Pg specific IgG. The mRNA expression of interferon-γ (IFN-γ) and interleuking-12 (IL-12) in gingival tissues, draining lymph node and spleen were detected by real-time reverse transcriptase polymerase chain reaction (RT-PCR). The measurement data were statistically analyzed.</p><p><b>RESULTS</b>The resorption rate in Am80 group [(121 ± 10)%] and high-dose of Am80 group [(108 ± 8)%] was significantly different with that in periodontitis mice [(133 ± 10)% ] (P < 0.05). The serum levels of anti-Pg specific IgG of the Am80 groups of different doses (0.437 ± 0.083, 0.566 ± 0.012, and 0.386 ± 0.078) were significantly lower than that of the periodontitis group (1.151 ± 0.433) (P < 0.001). Real-time quantitative PCR assay showed that after Am80 treatment, the IL-12 mRNA levels in the gingival tissues, lymph nodes and spleen of mice were reduced to 1.107 ± 0.088, 0.806 ± 0.220, and 0.668 ± 0.756, which were all significantly different with those in periodontitis (P < 0.01). Similarly, the relative expression of IFN-γ mRNA levels in gingival tissue, lymph nodes and spleen of mice were reduced to 8.898 ± 0.427, 16.654 ± 5.995, and 1.482 ± 0.033, which were significantly different with periodontitis (P < 0.001).</p><p><b>CONCLUSIONS</b>Am80 can reduce the extent of inflammation and alleviate alveolar bone resorption by modulating innate immune response.</p>

Rotigotine in the treatment of primary restless legs syndrome: A meta-analysis of randomized placebo-controlled trials / 华中科技大学学报（医学）（英德文版）

The aim of this study was to summarize the efficacy and tolerability of rotigotine in the treatment of primary restless legs syndrome (RLS). PubMed, EMBASE, and Cochrane Central Register of Controlled Trials (CENTRAL) were searched for English-language randomized controlled trials (RCTs) that assessed the effectiveness of rotigotine for RLS. The pooled mean change from baseline in International RLS (IRLS) Study Group Rating Scalescore and relative risk (RR) of response based on the Clinical Global Impression-Improvement (CGI-I) scale score were applied to evaluate the outcomes. The pooled proportions of adverse events (AEs) were also estimated. Six RCTs were included. The meta-analysis showed a favorable effectiveness of rotigotine versus placebo on RLS [mean change on IRLS score: mean difference (MD)=-4.80; 95% confidence interval (CI): -5.90 to -3.70; P<0.00001 and RR of response on CGI-I was 2.19; 95% CI: 1.86 to 2.58, P<0.00001]. The most common AEs were application site reactions, nausea, headache and fatigue. In general, rotigotine was well-tolerated in patients with primary RLS. Based on the findings from the meta-analysis, rotigotine was more significantly efficacious in the treatment of RLS than placebo. Nevertheless, long-term studies and more evidence of comparisons of rotigotine with other dopamine agonists are needed.

Application of patient-controlled intravenous analgesia of dezocine combined with sufentanil in burn patients after surgery / 中华烧伤杂志

<p><b>OBJECTIVE</b>To evaluate the efficacy and safety of patient-controlled intravenous analgesia (PCIA) of dezocine combined with sufentanil in burn patients after escharectomy or tangential excision followed by autologous skin grafting.</p><p><b>METHODS</b>Sixty burn patients hospitalized in Department of Burns and Plastic Surgery of our hospital from February 2011 to December 2013, conforming to the study criteria and going to have escharectomy or tangential excision followed by autologous skin grafting, were divided into sufentanil group (S, n = 30) and dezocine+sufentanil group (DS, n = 30) according to the random number table. Patients in group S were given 150 mL normal saline containing 2.5 µg/kg sufentanil citrate and 6 mg tropisetron after skin grafting for 48 hours. Patients in group DS were given 150 mL normal saline containing 0.25 mg/kg dezocine, 1.5 µg/kg sufentanil citrate, and 6 mg tropisetron for 48 hours. Visual Analog Scale (VAS), Bruggrmann Comfort Scale (BCS), and Ramsay Sedation Scale were used to evaluate the sedative effect or analgesic effect, and their scores were recorded at administration hour (AH) 2, 6, 12, 24, and 48. The times of efficient injection and incidence of adverse effect within the 48 AH were recorded. Data were processed with analysis of variance for repeated measurement, t test, chi-square test, and Fisher's exact test.</p><p><b>RESULTS</b>There were no obvious differences in the scores of VAS and BCS between two groups at each time point (with t values from -0.426 to 0.864, P values above 0.05). The scores of Ramsay Sedation Scale in group S at AH 2, 6, 12, 24, and 48 were respectively (3.2 ± 0.6), (3.2 ± 0.5), (3.3 ± 0.7), (3.2 ± 0.4), and (3.3 ± 0.4) points, which were higher than those in group DS [(2.4 ± 0.6), (2.5 ± 0.5), (2.4 ± 0.6), (2.4 ± 0.4), and (2.4 ± 0.5) points, with t values from 5.302 to 8.391, P values below 0.001]. The times of efficient injection within the 48 AH was 6.8 ± 0.7 in group S and 6.5 ± 0.9 in group DS, showing no significantly statistical difference (t = 1.260, P > 0.05). Respiratory depression was not observed in both groups; the incidence of pruritus was the same, and that of urine retention was similar between the 2 groups within the 48 AH (with P values above 0.05). Within the 48 AH, the incidence of nausea and vomiting in group S was 26.7% (8/30), which was obviously higher than that in group DS (6.7%, 2/30, P < 0.05); the incidence of drowsiness in group S was 20.0% (6/30), which was significantly higher than that in group DS (no patient, P < 0.05).</p><p><b>CONCLUSIONS</b>Dezocine combined with sufentanil can provide effective postoperative analgesia with little adverse effect for PCIA in burn patients after escharectomy or tangential excision followed by autologous skin grafting, therefore it can be widely used.</p>

Research on UPLC-PDA fingerprint of andrographis paniculata and quantitative determination of 4 major constituents / 中国中药杂志

Andrographis paniculata from different parts and origins were analyzed by UPLC-PDA fingerprint to provide refererice for related preparation technology. Using the peak of andrographolide as reference, 27 common peaks were identified, and digitized UPLC-PDA fingerprints for 23 batches of andrographis paniculata were established in this research. Principal component analysis (PCA) was carried out after feature extraction. The contents of andrographolide, neoandrographolide, deoxyandrographolide, dehydroandrographolide were determined by external standard method. The Plackett-Burman design combined with pareto chart was used to analyze the factors influencing the robustness of the method. It was found that the medicinal part has a more remarkable influence on the quality of andrographis paniculata than the origin. The contents of the 4 lactones the differ greatly in the different parts of andrographis paniculata, and the pH of the mobile phase is an important factor that influenced the robustness of the method.

Effects and related mechanism of retinoid X receptor agonist bexarotene on atherosclerosis progression in diabetic apoE(-/-) mice / 中华心血管病杂志

<p><b>OBJECTIVE</b>To explore the effect of retinoid X receptor (RXR) agonist bexarotene on atherosclerosis and the potential mechanism in streptozotocin (STZ) induced diabetic apolipoprotein E knockout (apoE(-/-)) mice.</p><p><b>METHODS</b>Eight C57BL/6 mice served as control, 46 apoE(-/-) mice were randomized into 4 groups: apoE(-/-) group (n = 10), STZ+apoE(-/-) group (n = 12), STZ+apoE(-/-)+Bex 10 (10 mg×kg⁻¹×d⁻¹)group (n = 12), STZ+ apoE(-/-)+Bex 30 (30 mg×kg⁻¹×d⁻¹) group (n = 12). Diabetic apoE(-/-) animal model was established by intraperitoneal injection of STZ. Blood glucose was determined by glucose oxidase method. Patch area in thoracic aorta was measured by HE staining. Western blotting was used to determine the RXR and gp91(phox) protein level in thoracic aorta. Reactive oxygen species (ROS) level in blood and thoracic aorta homogenates was detected by Fenton and Griess method.</p><p><b>RESULTS</b>(1) Patch areas of thoracic aorta were larger in apoE(-/-) group than in C57BL/6 group [(38.40 ± 8.95)µm² vs. (0.10 ± 0.01) µm², P < 0.01], further increased in STZ+apoE(-/-) group [(94.06 ± 8.04)µm², P < 0.05 vs. apoE(-/-) group] and significantly reduced in STZ+apoE(-/-)+Bex 10 group [(78.72 ± 4.62)µm², P < 0.05 vs. STZ+apoE(-/-) group] and further educed in STZ+apoE(-/-)+Bex 30 group [(46.13 ± 7.56)µm², P < 0.05 vs. STZ+apoE(-/-)+Bex 10 group]. (2) Blood glucose level, TG, TC, LDL-C, thoracic aorta gp91(phox) protein level and ROS level in blood and thoracic aorta homogenates were significantly higher in STZ+apoE(-/-) group than in apoE(-/-) group (all P < 0.05). Blood glucose level and TG, TC, LDL-C levels were similar between STZ+apoE(-/-)+Bex10 and STZ+apoE(-/-) group. Thoracic aorta gp91(phox) protein level and ROS level in blood and thoracic aorta homogenates were lower in STZ+apoE(-/-)+Bex 10 group than in STZ+apoE(-/-) group (P < 0.05). Blood glucose level, TG, TC, LDL-C levels, gp91(phox) expression in thoracic aorta, ROS level in blood and thoracic in STZ+apoE(-/-)+Bex 30 group were lower than in STZ+apoE(-/-) group (all P < 0.05).</p><p><b>CONCLUSION</b>Bexarotene treatment could attenuate arteriosclerosis progression in STZ induced diabetic apoE(-/-) mice, the underlying mechanism might be related to suppressing oxidative stress and decreasing blood glucose level and improving lipids metabolism.</p>

Advances in studies on aryltetralin lactone lignans / 中国中药杂志

Natural aryltetralin lactone lignans existed in the plants of family Berberidaceae, Acanthaceae, Burseraceae, Verbenaceae, Euphorbiaceae, etc. Due to the antineoplastic and antiviral properties, it has become a hot research topic in medicinal chemistry. This review covers extraction and isolation, biosynthesis, plant origin, and structure and spectral characteristics of natural aryltetralin lactone lignans. It will provide a useful reference for the intensive studies and rational utilization of aryltetralin lactone lignans.

Study on chemical constituents of Drosera peltata var. multisepala / 中国中药杂志

Chemical investigatation of Drosera peltata var. multisepala led to the isolation of eleven compounds using various chromatographic techniques. The structures of these compounds were elucidated as isoshinanolone-4-O-beta-D-glucoside (1), isoshinanolone (2), epi-isoshinanolone (3), plumbagin (4), droserone (5), droserone-5-O-glucoside (6), quercetin (7), kaempferol (8) , gossypetin-8-O-glucoside (9), 3,3'-dimethoxy ellagic acid (10), and ellagic acid (11) by their physicochemical properties and spectral data analysis. Compound 1 was a new compound. Compounds 3, 8, 10, and 11 were isolated from this plant for the first time.

Efficacy and safety of 24 hour rotigotine transdermal patch in the treatment of advanced Parkinson's disease: A meta-analysis

Advanced Parkinson's disease is often characterized by poor control of motor features with rapid oscillations between being on, being on with severe dyskinesias, and being off or frozen. As PD progresses, effective symptom control becomes more challenging, and a more complicated drug-regimen may be needed. OBJECTIVE: The objective was to perform a meta-analysis of randomized controlled trials of Rotigotine patch as treatment of advanced Parkinson's disease (PD). METHODS: A systemic literature search was conducted through August 2009. Both the efficacy and srlery endpoints were evaluated. RESULTS: The use of Rotigotine patch resulted in higher responder rates compared to placebo OR 0.37 (95% CI 0.35, 0.39). However, Rotigotine showed an adverse event profile similar to other dopamine agonists. CONCLUSION: The use of Rotigotine patch is an effective treatment option for the management of advanced PD but demands more study.

Efficacy and safety of 24 hour rotigotine transdermal rotigotine patch in the treatment of early Parkinson's disease

Presently, treatment of PD focuses on symptomatic therapy, that is to control motor symptoms, at the lowest possible dose, so as nor to develop early drug resistance, and consequent extrapyramidal symtoms. However, there has been no clinical trial, to date that has provided definitive evidence of pharmacological neuroprotection. Among the drugs with possible neuroprotective effects are the dopamine agonists. OBJECTIVE: The objective of this study is to determine the efficacy and safety of Rotigotine transdermal patch in the treatment of early Parkinson's disease in terms of improvement in the functional capacity and the incidence of adverse effects in patients treatment with the said drug . METHODOLOGY: Literature search of all randomized controlled trials, published from 1999-2009 comparing rotigotine patch with placebo, in patients with Parkinson's disease. Types of outcome measures- The primary outcome studied was the number of responders described as those with> 20% decrease in UPDRS Scores. The secondary outcome include the mean change in UPDRS score and the total incidence of adverse effects on patients on rotigotine patch. RESULTS: The use of Rotigotine patch in early Parkinson's disease shows as trend toward benefit and was statistically significant (OR 0.33) in terms of number of patients who showed a significant change in UPRDS scores. In terms of UPDRS scoring, there was significant improvement for those who took Rotigotene (MD 5.2.5). However, incidence of adverse effects was higher in the Rotigotine group compared to the placebo group (OR 3.13) CONCLUSION: The evidence from this review supports the use of Rorigotine patch for the treatment of early Parkinson's disease. This has shown to produce clinical improvement in parkinsonian symptoms as measured by the significant decrease in the UPDRS Scores on follow-up. However, adverse events were similar to those found with other dopamine agonists.

Chemical composition fluctuations in roots of Plumbago scandens L. in relation to floral development

Plumbago scandens L. is a Brazilian tropical/subtropical species that occurs along the coast. Chemically it is mainly represented by naphthoquinones, flavonoids, terpenoids and steroids. The aim of the present work is to study quantitative changes in the root metabolic production of Plumbago scandens during different physiologic developmental stages relative to floration. The results indicated the presence of four substances in the extracts: plumbagin, epi-isoshinanolone, palmitic acid and sitosterol, independent on developmental stage. The naphthoquinone plumbagin has always showed to be the major component of all extracts. Naphthoquinones exhibited their highest content during floration, while the content of the two others components decreased during this stage, revealing an inverse profile. The chemical composition changed depending on the plant requirements.

Plumbago scandens L. é uma espécie brasileira tropical/subtropical que ocorre ao longo da costa. Quimicamente, é principalmente representada por naftoquinonas, flavonóides, terpenóides e esteróides. objetivo do presente trabalho é estudar mudanças quantitativas da produção metabólica nas raízes de Plumbago scandens durante diferentes estágios de desenvolvimento fisiológico, relativos à floração. Os resultados indicaram a presença de quatro substâncias nos extratos: plumbagina, epi-isoshinanolona, ácido palmítico e sitosterol, independente do estágio de desenvolvimento. A naftoquinona plumbagina tem sempre mostrado ser o componente majoritário de todos os extratos. Naftoquinonas exibiram seus maiores conteúdos durante a floração, enquanto o conteúdo dos dois outros componentes decresceu durante este estágio, revelando um perfil inverso. A composição química modificou dependendo das necessidades da planta.

Characterization of chemical components of essential oil from flowers of Chrysanthemum morifolium produced in Anhui province / 中国中药杂志

<p><b>OBJECTIVE</b>To analyze the chemical components of the essential oil extracted from six cultivars' Juhua (Zaogongju, Wangongju, Huangyaoju, Chuju, Xiaoboju and Daboju) produced in Anhui province of China, which were breed from Chrysanthemum morifolium, and to provide scientific basis for quality control.</p><p><b>METHOD</b>The essential oils of the six cultivars'Juhua were extracted by water-steam distillation and separated by GC capillary column chromatography. The components were quantitatively determined with normalization method, and identified by GC-MS.</p><p><b>RESULT</b>From Zaogongju, Wangongju, Huangyaoju, Chuju, Xiaoboju and Daboju, 247, 226, 246, 182, 216 and 122 chromatographic peaks were detected, among them 75, 54, 78, 50, 53 and 43 components were identified,which were composed of 85.67%, 82.80%, 81.38%, 73.22%, 71.51% and 72.87% of the total essential oil, respectively.</p><p><b>CONCLUSION</b>Monoterpenoid compounds were higher more than sesquiterpenoid compounds in the five juhua except for Chuju. There was no difference in the constituents of essential oil of Zaogongju and Wangongju. And verbenyl acetate was the main chemical constituent and composed of 32.10% and 37.85% of the total essential oil, respectively. (1R)-Camphor and bisabolol oxide A were the main chemical constituents in Huangyaoju, which were composed of 28.70% and 12.58% of the total essential oil, respectively. beta-Selinene and borneol were the main chemical constituents in Chuju, which were composed of 17.85% and 12.84% of the total essential oil, respectively. Eucalyptol was the main chemical constituent in Xiaoboju, which were composed of 21.33%. Verbene oxides and chrysanthenone were composed of 25.32% and 8.26% of the total essential oil, respectively, in the Daboju. The common chemical constituents were camphene, borneol, bornyl aceate, (1R)-camphor, (-)-4-terpineol, alpha-terpineol, eucalyptol, cis-caryophyllene, caryophyllene oxide, juniper camphor, beta-sesquiphellandrene, alpha-curcumene and beta-farnesene in the six cultivars' Juhua produced in Anhui province of China. The resultant data provided the further evidences to distinguish Juhua' cultivars and scientific basis for quality control of Juhua.</p>

Studies on diterpenoids from Andrographis paniculata / 中国中药杂志

<p><b>OBJECTIVE</b>To study the diterpenoids in the 85% ethanol extract of the aerial parts of Andrographis paniculata.</p><p><b>METHOD</b>Fourteen diterpenoids from the 85% EtOH extract were isolated by the silica gel, Sephadex LH-20, ODS column chromatography and HPLC, and their structures were identified by the spectal analyses and chemical evidences.</p><p><b>RESULT</b>The 14 compounds were obtained and identified as neoandrographolide (1), 3, 14-di-deoxyandrographolide (2), andrographolide (3), 14-deoxy-11, 12-didehydroandrographolide (4), 19-hydroxy-8 (17), 13-labdadien-15, 16-olide (5), 14-deoxy-andrographolide (6), 3-oxo-14-deoxy-andrographolide (7), isoandrographolide, (8), bisandrographolide (9, 10, 11), deoxyandrographiside (12), 14-deoxy-11, 12-didehydroandrographiside (13), andrographiside (14), respectively.</p><p><b>CONCLUSION</b>Compound 7 was a new natural product, and compound 5 was obtained for the first time from the Andrographis species.</p>

Synthesis of new pyridine, pyrazole and pyrimidine derivatives of potential antimicrobial effect

Reaction of 2- acetyl tetralin [1] with some aldehydes was conducted in presence of malononitrile and/or ethylcyanoacetate and ammonium acetate, yielded tetrahydronaphthalenyl nicotinonitrile of types 2 and 3. Condensation of 1 with aromatic aldehydes afforded the respective chalcones 4a, b, which yielded pyrazolines 5a, b, phenyl pyrazolines 6a, b, 2-pyrimidinones 7a, b and 2-thiopyrimidines 8a, b upon reaction with hydrazine, phenyl hydrazine, urea, and thiourea, respectively. Some of the synthesized compounds have been screened for their antimicrobial activity against various strains of bacteria and fungi

Effect of SR 58611A, a beta-3 receptor agonist, against experimental gastro-duodenal ulcers.

The present study was designed to study the effect of SR 58611A, a selective beta 3-adrenoceptor agonist against gastric ulcers: pylorus ligation, water immersion plus restraint stress (WIRS), ethanol, aspirin-induced and on cysteamine-induced duodenal ulcers, in rats. SR 58611A (10 mg/kg, p.o.) was found to be effective in attenuating gastric ulceration and the results were comparable with those from standard cimetidine-treated group. Apart from reducing ulcer index, SR 58611A significantly decreased total acidity and thereby exhibited antisecretory activity in pylorus ligation model. SR 58611A showed significant reduction in ulcer index alongwith significant rise in the gastric wall mucus content in WIRS model. Further it showed significant cytoprotective activity against ethanol insult, that was evident from significant reduction in ulcer index. It showed significant reduction in gastric ulceration in aspirin-treated rats. The drug was found to be ineffective in inhibiting the cysteamine-induced duodenal ulcers as evident from the ulcer index and total lesion area parameters. It is concluded that SR 586111A possesses significant gastroprotective activity. This activity could be attributed to the inhibition of gastric acidity, increase in gastric wall mucus content and the reversal of gastric microvascular injury resulting into protection of the vascular integrity.

Reactions of, B-spiroepoxy-alkannans part IV+ New and facile synthesis of tetrahydric-naphthalin-2-01 derivatives for biological evaluation

Spirooctanones II react with acetoacetanilide to form tetrahydro-naphthalene derivatives IIIa,b, which react with phosphorus oxychloride to give the corresponding chloro derivatives IV. Compounds IV react with hydrazine hydrate, aniline, and hydroxylamine to give the corresponding compounds V, VI and VII, respectively. Compounds V condensed with aromatic aldehydes to give the corresponding hydrazones VIII

Ceanofendl in pentatate: a new aryltetralin from ceanothus Fendleri

A new aryltetrahydronaphthalene derivative, 4-[2',4',6'- triacetoxyphenyl]-5,6,7-trimethyl-1 alpha, 2 beta- diacetoxy-4-hydroxy-1,2,3,4-tetrahydronaphthalene, ceanofendlin pentaacetate, was isolated from the acetylated ethyl acetate extract of Ceanothus fendleri, Rhamnaceae. The known flavonoids kaempferol, kaempferol-3-O-beta-D-glucopyranoside-7-O-alpha-L-rhamnopyranoside, kaempferol-3-O-rutinoside, quercetin-3-O-rutinoside [rutin] and quercetin-3-O-alpha-L-rhamnopyranosyl-[1-6]-O-beta-D-galactopyranoside were also obtained. The structural characteristics of these compounds were confirmed by spectroscopic methods