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.

Dopamine Agonists ; Dyskinesias ; Parkinson Disease ; Tetrahydronaphthalenes ; Thiophenes ; Treatment Outcome

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.
Andrographis ; chemistry ; Chromatography, Liquid ; methods ; Diterpenes ; analysis ; Drug Stability ; Glucosides ; analysis ; Principal Component Analysis ; Tetrahydronaphthalenes ; analysis

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.

Human ; Dopamine Agonists ; Drug Resistance ; Neuroprotection ; Neuroprotective Agents ; Parkinson Disease ; Parkinsonian Disorders ; Tetrahydronaphthalenes ; Thiophenes ; Transdermal Patch

Airway Extubation ; adverse effects ; Bridged Bicyclo Compounds, Heterocyclic ; therapeutic use ; Endoscopy ; Humans ; Nasal Surgical Procedures ; Tetrahydronaphthalenes ; therapeutic use ; Trachea

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.
Humans ; Placebos ; Randomized Controlled Trials as Topic ; Restless Legs Syndrome ; drug therapy ; Tetrahydronaphthalenes ; therapeutic use ; Thiophenes ; therapeutic use

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.
Lactones ; chemistry ; isolation & purification ; Lignans ; biosynthesis ; chemistry ; isolation & purification ; Magnetic Resonance Spectroscopy ; Spectrophotometry, Ultraviolet ; Tetrahydronaphthalenes ; chemistry ; isolation & purification

OBJECTIVETo study the diterpenoids in the 85% ethanol extract of the aerial parts of Andrographis paniculata.

METHODFourteen 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.

RESULTThe 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.

CONCLUSIONCompound 7 was a new natural product, and compound 5 was obtained for the first time from the Andrographis species.

Andrographis ; chemistry ; Diterpenes ; chemistry ; isolation & purification ; Glucosides ; chemistry ; isolation & purification ; Molecular Structure ; Plant Components, Aerial ; chemistry ; Plants, Medicinal ; chemistry ; Tetrahydronaphthalenes ; chemistry ; isolation & purification

OBJECTIVETo 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.

METHODThe 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.

RESULTFrom 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.

CONCLUSIONMonoterpenoid 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.

Boranes ; chemistry ; Bornanes ; chemistry ; Camphor ; chemistry ; China ; Chrysanthemum ; chemistry ; Cyclohexanols ; chemistry ; Gas Chromatography-Mass Spectrometry ; Monoterpenes ; chemistry ; Oils, Volatile ; chemistry ; Sesquiterpenes ; chemistry ; Terpenes ; chemistry ; Tetrahydronaphthalenes ; chemistry

Animals ; Apoptosis ; Bridged Bicyclo Compounds, Heterocyclic/pharmacology* ; Cell Line ; Hypoxia ; MicroRNAs/genetics* ; Myocardial Reperfusion Injury/drug therapy* ; Myocytes, Cardiac ; Oxidative Stress ; Rats ; Reperfusion Injury ; Tetrahydronaphthalenes/pharmacology*

OBJECTIVETo 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.

METHODSEight 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.

RESULTS(1) Patch areas of thoracic aorta were larger in apoE(-/-) group than in C57BL/6 group [(38.40 ± 8.95)µm&sup2; vs. (0.10 ± 0.01) µm&sup2;, P < 0.01], further increased in STZ+apoE(-/-) group [(94.06 ± 8.04)µm&sup2;, P < 0.05 vs. apoE(-/-) group] and significantly reduced in STZ+apoE(-/-)+Bex 10 group [(78.72 ± 4.62)µm&sup2;, P < 0.05 vs. STZ+apoE(-/-) group] and further educed in STZ+apoE(-/-)+Bex 30 group [(46.13 ± 7.56)µm&sup2;, 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).

CONCLUSIONBexarotene 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.

Animals ; Apolipoproteins E ; genetics ; Atherosclerosis ; etiology ; metabolism ; prevention & control ; Blood Glucose ; metabolism ; Diabetes Mellitus, Experimental ; complications ; metabolism ; Male ; Mice ; Mice, Inbred C57BL ; Mice, Knockout ; Oxidative Stress ; drug effects ; Reactive Oxygen Species ; metabolism ; Retinoid X Receptors ; agonists ; metabolism ; Tetrahydronaphthalenes ; pharmacology