ABSTRACT
Five undescribed eudesmane sesquiterpenoids, artemilavanins A-E, and one undescribed rearranged eudesmane sesquiterpenoid, artemilavanin F, were isolated from the 95% ethanol extract of the aerial parts of Artemisia lavandulaefolia DC., along with ten known compounds. The structures and configurations of undescribed compounds were mainly elucidated by spectroscopic analyses and single-crystal X-ray diffraction analysis. Among all isolated compounds, artemilavanin F exhibited inhibitory activity on PANC-1 pancreatic cancer cells with IC50 of 9.69 ± 2.39 µM. Artemilavanin F inhibited PANC-1 cell proliferation by induction of G2/M cell cycle arrest and apoptosis mediated by downregulation of cyclin-dependent kinases and accumulation of reactive oxygen species. Moreover, artemilavanin F inhibited the colony formation, cell migration and sphere formation of PANC-1 cells, indicating the suppression of stem-cell-like phenotype of PANC-1 cells. Further results confirmed that the expression of cancer stem cell markers such as Bmi1, CD44, CD133 were inhibited by artemilavanin F. Downregulation of epithelial-mesenchymal transition (EMT) markers such as N-cadherin and Oct-4 indicated the potential of artemilavanin F in prevention of metastasis.
Subject(s)
Artemisia , Pancreatic Neoplasms , Sesquiterpenes, Eudesmane , Sesquiterpenes , Artemisia/chemistry , Pancreatic Neoplasms/drug therapy , Sesquiterpenes, Eudesmane/pharmacology , Sesquiterpenes, Eudesmane/analysis , Sesquiterpenes, Eudesmane/chemistry , Plant Components, Aerial/chemistry , Sesquiterpenes/chemistry , Molecular Structure , Pancreatic NeoplasmsABSTRACT
BACKGROUND: Hyperuricemia is an important pathological basis of gout and a distinct hazard factor for metabolic syndromes and cardiovascular and chronic renal disease, but lacks safe and effective treatments currently. Paeonia × suffruticosa Andrews leaf effectively reduced serum uric acid in gout patients; however, the material foundation and the mechanism remain unclear. PURPOSE: To determine the primary active components and mechanism of P. suffruticosa leaf in hyperuricemic mice. METHODS: The chemical constituents of P. suffruticosa leaf was identified using high-performance liquid chromatographic analysis. The anti-hyperuricemic activity of P. suffruticosa leaf extract (12.5, 25, 50, 100, and 200 mg/kg) and its components was evaluated in hyperuricemic mice induced by a high purine diet for 14 days. Then, the urate-lowering effects of apigenin 7-O-glucoside (0.09, 0.18, and 0.36 mg/kg) were assessed in another hyperuricemic mice model built by administrating potassium oxonate and adenine for 4 weeks. The inhibitory effect of apigenin 7-O-glucoside on uric acid production was elucidated by investigating xanthine oxidase activity in vitro and in serum and the liver and through molecular docking. Immunofluorescence and western blot analyses of the expression of renal urate transporter 1 (URAT1), glucose transporter 9 (GLUT9), organic anion transporters 1 (OAT1), and ATP-binding cassette G member 2 (ABCG2) proteins elucidated how apigenin 7-O-glucoside promoted uric acid excretion. RESULTS: Six compounds were identified in P. suffruticosa leaf: gallic acid, methyl gallate, oxypaeoniflorin, paeoniflorin, galloylpaeoniflorin, and apigenin 7-O-glucoside. P. suffruticosa leaf extract significantly attenuated increased serum uric acid, creatinine, and xanthine oxidase activity in hyperuricemic mice. Apigenin 7-O-glucoside from P. suffruticosa leaf reduced uric acid, creatinine, and malondialdehyde serum levels, increased superoxide dismutase activity, and partially restored the spleen coefficient in hyperuricemic mice. Apigenin 7-O-glucoside inhibited xanthine oxidase activity in vitro and decreased serum and liver xanthine oxidase activity and liver xanthine oxidase protein expression in hyperuricemic mice. Molecular docking revealed that apigenin 7-O-glucoside bound to xanthine oxidase. Apigenin 7-O-glucoside facilitated uric acid excretion by modulating the renal urate transporters URAT1, GLUT9, OAT1, and ABCG2. Apigenin 7-O-glucoside protected against renal damage and oxidative stress caused by hyperuricemia by reducing serum creatinine, blood urea nitrogen, malondialdehyde, and renal reactive oxygen species levels; increasing serum and renal superoxide dismutase activity; restoring the renal coefficient; and reducing renal pathological injury. CONCLUSION: Apigenin 7-O-glucoside is the main urate-lowering active component of P. suffruticosa leaf extract in the hyperuricemic mice. It suppressed liver xanthine oxidase activity to decrease uric acid synthesis and modulated renal urate transporters to stimulate uric acid excretion, alleviating kidney damage caused by hyperuricemia.
Subject(s)
Gout , Hyperuricemia , Organic Anion Transporters , Paeonia , Mice , Animals , Hyperuricemia/drug therapy , Hyperuricemia/chemically induced , Uric Acid , Xanthine Oxidase/metabolism , Creatinine , Molecular Docking Simulation , Apigenin/pharmacology , Kidney , Organic Anion Transporters/metabolism , Superoxide Dismutase/metabolism , Glucosides/pharmacology , Malondialdehyde/metabolism , Oxonic Acid/adverse effectsABSTRACT
BACKGROUND: Many women experience menstruation-related health issues during their child-bearing years. This study aimed to evaluate women's tendency to seek Traditional Chinese Medicine (TCM) and/or Western Medicine (WM) when newly diagnosed with menstrual syndromes and to identify factors associated with their medical care-seeking behaviors. METHODS: The data of a total of 47,097 women aged between 15 and 50 years with newly diagnosed menstrual syndromes in 2005 were extracted from the Taiwan National Health Insurance Database. The follow-up period was divided equally into 6 month segments over 5 years starting with patients' first visit for obstetric/gynecologic care. Outcomes were outpatient visits and number of TCM or WM visits during each period. Patients' tendency for medical care utilization was estimated using Poisson regression analysis. RESULTS: Number of outpatient visits using TCM was 0.62 (29187/47097), and using WM was 1.67 (78697/47097) within 6 months after the first menstrual syndrome diagnosis. The tendency for TCM utilization increased as follow-up time increased after controlling for potential confounders, while WM utilization decreased as follow-up time increased. Age, economic status, infertility, value of prevention, baby delivery, and obstetric/gynecologic inpatient histories were significantly associated with patients' medical care-seeking behaviors. CONCLUSIONS: TCM and WM medical care-seeking patterns are significantly different among women with diagnoses associated with menstrual syndromes. Related factors affecting medical care-seeking behavior include age, economic status, infertility, value of prevention, childbirth and Ob/Gyn inpatient histories.
Subject(s)
Infertility , Menstruation , Humans , Female , Adolescent , Young Adult , Adult , Middle Aged , Syndrome , Medicine, Chinese Traditional , Regression AnalysisABSTRACT
INTRODUCTION: The Western Ontario and McMaster University osteoarthritis index (WOMAC) is the most commonly used indicator of disease-specific outcome in knee osteoarthritis for its convenience and reliability. It has two formats the paper-based WOMAC (p-WOMAC) and the electronic WOMAC (e-WOMAC). In China, the p-WOMAC has been widely used though e-WOMAC is yet untested. This study aims to test whether e-WOMAC is consistent with the p-WOMAC before and after the intervention. METHODS AND ANALYSIS: A total of 70 patients from Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine will be randomly assigned in two groups, named, group A and group B. This study is divided into three stages. In the first stage, patients in group A will be evaluated first by p-WOMAC and then by e-WOMAC. Patients in group B will be evaluated by e-WOMAC and then by p-WOMAC. In the second stage of the study, drug interventions will be implemented. 200 mg celecoxib will be administered orally once a day starting from the second day of enrolment for a period of 21 days. In the third stage, postintervention evaluation will be conducted after administration. Patients in group A will be evaluated first by e-WOMAC and then by p-WOMAC. Patients in group B will be evaluated first by p-WOMAC and then by e-WOMAC. In order to avoid the possible bias because of patients' potential memory, e-WOMAC and p-WOMAC will be taken for each patient at 15 min apart. The primary outcome of the study is the mean score difference in WOMAC, and the secondary outcomes are the score differences in WOMAC subscales: pain, stiffness and physical function. ETHICS AND DISSEMINATION: The protocol has been approved by the Independent Review Board of SGH (approval number: 2020-814-21-01). The results of the trial will be submitted for publication in a peer-reviewed journal. TRIAL REGISTRATION NUMBER: ChiCTR2100050914.
Subject(s)
Osteoarthritis, Knee , Humans , Reproducibility of Results , Universities , Ontario , China , Osteoarthritis, Knee/drug therapy , Electronics , Treatment Outcome , Randomized Controlled Trials as TopicABSTRACT
Nonalcoholic fatty liver disease (NAFLD) is the most common liver disease that may progress to nonalcoholic steatohepatitis (NASH), hepatic tissue fibrosis, liver cirrhosis, and hepatocellular carcinoma. In this study, we investigated the effects of Pien Tze Huang (PTH), a well-known traditional Chinese herbal formula with liver protective effect, in methionine-choline deficient diet (MCD)- and high-fat diet (HFD)-induced NASH mouse models. Our results showed that PTH could exert hepatoprotective effects by improving liver weight and steatosis and reducing the fibrosis and serum levels of alanine transaminase (ALT) and aspartate transaminase (AST) in both animal models. The effects of PTH was accompanied with the reduction of infiltrated macrophages, the inhibition of the expression of cytokines, and the induction of adiponectin expression. Mechanistically, we found that PTH could inhibit the activation of proinflammatory transcription factor nuclear factor-κB (NF-κB) by preventing the degradation of inhibitor of κBα (IκBα). These results demonstrate that PTH can improve NAFLD largely due to its suppression of the NF-κB inflammatory pathway.
Subject(s)
Drugs, Chinese Herbal , Non-alcoholic Fatty Liver Disease , Animals , Anti-Inflammatory Agents/metabolism , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Disease Models, Animal , Drugs, Chinese Herbal/metabolism , Drugs, Chinese Herbal/pharmacology , Drugs, Chinese Herbal/therapeutic use , Fibrosis , Liver , Liver Cirrhosis/metabolism , Methionine/pharmacology , Mice , Mice, Inbred C57BL , NF-kappa B/metabolism , Non-alcoholic Fatty Liver Disease/metabolismABSTRACT
Two new seco-prezizaane-type sesquiterpenes, 2ß-hydroxy-6-deoxyneoanisatin (1) and 3,4-anhydro-2-oxo-1α-hydroxy-6-deoxyneoanisatin (2), and two new prenylated C6 -C3 compounds, illilanceofunones A (3) and B (4), were obtained from the fruits of Illicium lanceolatum, along with four known prenylated C6 -C3 compounds (5-8). Their structures were proposed through HR-ESI-MS, 1 H, 13 C, and 2D NMR data interpretation. Moreover, the absolute configuration of 1 and 2 were further assigned by single-crystal X-ray diffraction analysis and electronic circular dichroism (ECD) calculations, respectively. Illihenryipyranol A (6) exhibited neuroprotective activity against MPP+ -induced PC12â cell damage in a dose-dependent manner.
Subject(s)
Illicium/chemistry , Neuroprotective Agents/chemistry , Sesquiterpenes/chemistry , Animals , Cell Survival/drug effects , Circular Dichroism , Fruit/chemistry , Fruit/metabolism , Illicium/metabolism , Magnetic Resonance Spectroscopy , Molecular Conformation , Neuroprotective Agents/isolation & purification , Neuroprotective Agents/pharmacology , PC12 Cells , Plant Extracts/chemistry , Prenylation , Rats , Sesquiterpenes/isolation & purification , Sesquiterpenes/pharmacology , Spectrometry, Mass, Electrospray IonizationABSTRACT
BACKGROUND Guidelines recommend a clear liquid fasting time of 2 h before surgery, which is often exceeded, leading to adverse reactions (ARs) such as discomfort, thirst, and dehydration. We assessed the gastric contents and ARs after oral glucose water administration 1 h prior to surgery in children with cyanotic congenital heart disease (CCHD). MATERIAL AND METHODS This was a non-inferiority randomized controlled trial of children with CCHD enrolled at the Fujian Medical University Union Hospital from 09/2014 to 05/2017 and randomized to receive oral glucose water (10 g of glucose in 100 ml of warm water, 5 ml/kg) 2 h (2-h group, n=174) or 1 h (1-h group, n=170) before surgery. The primary endpoint was gastric volume. Secondary endpoints included pH of gastric content, preoperative blood glucose, and risk factors for aspiration pneumonia. Pre- and intraoperative ARs were recorded. RESULTS The 1-h group showed smaller gastric content volumes (0.34±0.35 (95% CI: 0.29-0.39) vs. 0.43±0.33 (95% CI: 0.38-0.48) ml/kg, t=2.55, P<0.05) and higher blood glucose (6.21±0.78 (95% CI: 6.09-6.33) vs. 5.59±1.11 (95% CI: 5.43-5.76) mmol/L, t=-5.91, P<0.001). The 95% confidence interval of the volume difference between the 2 groups was 0.017-0.163, the upper limit value was 0.163 Subject(s)
Glucose/therapeutic use
, Preoperative Care/methods
, Administration, Oral
, Blood Glucose/analysis
, Child, Preschool
, Fasting
, Female
, Gastrointestinal Contents/drug effects
, Glucose/administration & dosage
, Heart Defects, Congenital/surgery
, Humans
, Infant
, Infant, Newborn
, Male
, Water
ABSTRACT
OBJECTIVE: To investigate the efficacy of Niao Du Kang (NDK) mixture in renal fibrosis of rats and to explore the mechanism underlying the effect of NDK on renal fibrosis. METHODS: Unilateral ureteral obstruction (UUO) was used to replicate a rat renal interstitial fibrosis model. The drug-administered groups were given 20 ml/kg (NDK-H), 10 ml/kg (NDK-M), and 5 ml/kg (NDK-L) NDK mixture once a day for 21 days beginning 48 hours after surgery. The 24-hour urine protein and serum creatinine (CR) levels in the sham group rats, UUO rats, and NDK mixture-treated rats were measured after the last administration. The pathological changes of rat kidney tissue were observed by HE staining. The degree of fibrosis was observed by Masson's staining and scored. The expression levels of TGF-ß, α-SMA mRNA, and mir-129-5p in kidney were detected by qRT-PCR. HK-2 cells were treated with 5 ng/ml TGF-ß to induce HK-2 cell fibrosis. The expression levels of TGF-ß, α-SMA mRNA, and mir-129-5p in HK-2 cells were detected by qRT-PCR. TargetScan predicted the target gene of mir-129-5p, HK-2 cells were transfected with mir-129-5p mimic, and an overexpressed mir-129-5p HK-2 cell model was constructed. qRT-PCR was used to detect the expression of PDPK1 mRNA. Western blot was used to detect the expression of PDPK1, AKT, and p-AKT in HK-2 cells induced by TGF-ß and in UUO rats. RESULTS: NDK mixture significantly reduced the 24-hour urine protein and CR levels of UUO rats. HE staining showed that the NDK mixture group exhibited a significantly reduced degree of renal interstitial fibrosis. NDK mixture also reduced the expression of TGF-ß and α-SMA, and the middle-dose group showed a better therapeutic effect. In vitro studies showed that NDK mixture-containing serum increased the expression of mir-129-5p to reduce renal fibrosis. In addition, NDK mixture increased the expression of mir-129-5p in vivo. Further studies indicated that mir-129-5p could target PDPKl to reduce its expression. The NDK-containing serum group also exhibited reduced expression of PDPK1. CONCLUSION: NDK mixture can significantly improve renal function and improve renal fibrosis in UUO model rats. Furthermore, NDK mixture can inhibit the expression of PDPK1 by upregulating the expression of mir-129-5p and then inhibiting the PI3K/AKT pathway to improve renal fibrosis.
ABSTRACT
The ecological environment of the Yellow River Delta is fragile, and the soil degradation in the region is serious. Therefore it is important to discern the status of the soil degradation in a timely manner for soil conservation and utilization. The study area of this study was Kenli County in the Yellow River Delta of China. First, physical and chemical data of the soil were obtained by field investigations and soil sample analyses, and the hyper-spectra of air-dried soil samples were obtained via spectrometer. Then, the soil degradation index (SDI) was constructed by the key indicators of soil degradation, including pH, SSC, OM, AN, AP, AK, and soil texture. Next, according to a cluster analysis, soil degradation was divided into the following three grades: light degradation, moderate degradation, and heavy degradation. Moreover, the spectral characteristics of soil degradation were analyzed, and an estimation model of SDI was established by multiple stepwise regression. The results showed that the overall level of reflectance spectra increased with increased degree of soil degradation, that both derivative transformation and waveband reorganization could enhance the spectral information of soil degradation, and that the correlation between SDI and the spectral parameter of (Rλ2+Rλ1)/(Rλ2-Rλ1) was the highest among all the spectral parameters studied. On this basis, the optimum estimation model of SDI was established with the correlation coefficient of 0.811. This study fully embodies the potential of hyper-spectral technology in the study of soil degradation and provides a technical reference for the rapid extraction of information from soil degradation. Additionally, the study area is typical and representative, and thus can indirectly reflect the soil degradation situation of the whole Yellow River Delta.
Subject(s)
Environmental Monitoring/methods , Soil/chemistry , Spectrum Analysis/methods , China , Cluster Analysis , Environmental Monitoring/statistics & numerical data , Hydrogen-Ion Concentration , Models, Theoretical , Nitrogen/analysis , Nitrogen/chemistry , Phosphorus/analysis , Phosphorus/chemistry , Potassium/analysis , Potassium/chemistryABSTRACT
OBJECTIVE: The purpose of this study was to compare the diagnostic accuracy of lesion localization between Cyriax's functional examination and ultrasonography in participants with and without shoulder pain. METHODS: A total of 206 adults aged 20 years and older with or without shoulder pain were included. All participants received Cyriax's functional examination by the first blinded physiatrist. Within a week, ultrasonography was performed by another blinded specialist. The diagnoses made by both methods, respectively, were compared finally. Sensitivity, specificity, and positive and negative predictive values were evaluated for the diagnosis of shoulder lesions between Cyriax's functional examination and ultrasonography. RESULTS: There was no significant difference between the 2 groups regarding age, sex, and body mass index. Moderate to high sensitivity (74.1%, 76.5%, and 66.7%) and high specificity (93.0%, 99.5%, and 99.0%) were in supraspinatus, subscapularis, and infraspinatus lesions, respectively. For the subacromial-subdeltoid bursitis, high sensitivity (90.4%) and moderate to high specificity (70.3%) was found. In contrast, low sensitivity (15.0%) and high specificity (100.0%) were found in the biceps lesions. CONCLUSION: In this study, we found that Cyriax's functional examination had high sensitivity in detecting subacromial-subdeltoid bursitis and high specificity in rotator cuff lesion.
Subject(s)
Bursitis/diagnosis , Physical Examination/methods , Rotator Cuff Injuries/diagnosis , Shoulder Pain/etiology , Female , Humans , Male , Middle Aged , Predictive Value of Tests , Prospective Studies , Sensitivity and Specificity , Shoulder Joint/diagnostic imaging , UltrasonographyABSTRACT
The new and rapid advancement in the complexity of biologics drug discovery has been driven by a deeper understanding of biological systems combined with innovative new therapeutic modalities, paving the way to breakthrough therapies for previously intractable diseases. These exciting times in biomedical innovation require the development of novel technologies to facilitate the sophisticated, multifaceted, high-paced workflows necessary to support modern large molecule drug discovery. A high-level aspiration is a true integration of "lab-on-a-chip" methods that vastly miniaturize cellulmical experiments could transform the speed, cost, and success of multiple workstreams in biologics development. Several microscale bioprocess technologies have been established that incrementally address these needs, yet each is inflexibly designed for a very specific process thus limiting an integrated holistic application. A more fully integrated nanoscale approach that incorporates manipulation, culture, analytics, and traceable digital record keeping of thousands of single cells in a relevant nanoenvironment would be a transformative technology capable of keeping pace with today's rapid and complex drug discovery demands. The recent advent of optical manipulation of cells using light-induced electrokinetics with micro- and nanoscale cell culture is poised to revolutionize both fundamental and applied biological research. In this review, we summarize the current state of the art for optical manipulation techniques and discuss emerging biological applications of this technology. In particular, we focus on promising prospects for drug discovery workflows, including antibody discovery, bioassay development, antibody engineering, and cell line development, which are enabled by the automation and industrialization of an integrated optoelectronic single-cell manipulation and culture platform. Continued development of such platforms will be well positioned to overcome many of the challenges currently associated with fragmented, low-throughput bioprocess workflows in biopharma and life science research.
Subject(s)
Automation , Biological Products , Drug Discovery , Lab-On-A-Chip Devices , HumansABSTRACT
A rare carotane-type sesquiterpenoid, forkienin A (1), a new eudesmane-type sesquiterpenoid, forkienin B (2), and a new natural eudesmane-type sesquiterpenoid, forkienin C (3), were isolated from the twigs and leaves of Fokienia hodginsii, along with eight known sesquiterpenoids. The structures of the new compounds were elucidated on the basis of their spectroscopic analysis, including 1D and 2D NMR methods. All compounds were evaluated for cytotoxicity against HL-60, SMMC-7721, A-549, MCF-7, and SW480 cell lines.
Subject(s)
Antineoplastic Agents, Phytogenic/isolation & purification , Plant Leaves/chemistry , Plant Stems/chemistry , Sesquiterpenes, Eudesmane/isolation & purification , Sesquiterpenes/isolation & purification , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Drug Screening Assays, Antitumor , Drugs, Chinese Herbal/chemistry , HL-60 Cells , Humans , Molecular Structure , Sesquiterpenes/chemistry , Sesquiterpenes/pharmacology , Sesquiterpenes, Eudesmane/chemistry , Sesquiterpenes, Eudesmane/pharmacologyABSTRACT
Five cassane diterpenes were isolated from the 95% ethanol extract of the seeds of Caesalpinia bonduc (Leguminosea) by a combination of various chromatographic methods, including silica gel, Sephadex LH-20, and semi-preparative HPLC. On the basis of spectroscopic techniques, their structures were identified as 3ß-acetoxy-cassa-12,14(17),15-trien-7ß-ol (1), caesalmin C (2), caesall E (3), caesalpinin MJ (4), and 1-deacetylcaesalmin C (5). Among them, compound 1 is a new compound and 2, 4, 5 were isolated from the plant for the first time.
Subject(s)
Caesalpinia/chemistry , Diterpenes/chemistry , Seeds/chemistry , Diterpenes/isolation & purification , Molecular Structure , Plant Extracts/chemistryABSTRACT
Phytochemical investigation of the flowers of Inula japonica led to isolation of nine sesquiterpenoids, inujaponins A-I, as well as eighteen known ones. These sesquiterpenoids belong to six skeletal-types, including eudesmane, 1,10-seco-eudesmane, germacrane, guaiane, 4,5-seco-guaiane, and pseudoguaiane sesquiterpenoids. Their structures were established by extensive spectroscopic analysis. The absolute configurations of inujaponin A, eupatolide, and deacetylovatifolin were determined by Cu-Kα X-ray crystallographic analysis. Most of the isolated compounds exhibited potent cytotoxicity against HL-60, SMMC-7721, A-549, MCF-7, and SW-480 cancer cell lines, with IC50 values ranging from 1.57 to 22.58 µM. Some selected compounds also possessed significant inhibitory activity against LPS-induced NO production in RAW264.7 macrophages with IC50 values ranging from 1.42 to 8.99 µM.
Subject(s)
Flowers/chemistry , Inula/chemistry , Sesquiterpenes, Eudesmane/isolation & purification , Animals , Crystallography, X-Ray , HL-60 Cells , Humans , Inhibitory Concentration 50 , Lipopolysaccharides/pharmacology , Macrophages/drug effects , Mice , Molecular Conformation , Molecular Structure , Nitric Oxide/biosynthesis , Sesquiterpenes/chemistry , Sesquiterpenes/isolation & purification , Sesquiterpenes/pharmacology , Sesquiterpenes, Eudesmane/chemistry , Sesquiterpenes, Eudesmane/pharmacology , Sesquiterpenes, Guaiane/chemistry , Sesquiterpenes, Guaiane/isolation & purification , Sesquiterpenes, Guaiane/pharmacologyABSTRACT
Objective: To study the chemical constituents of Inula japonica. Methods: Silica gel, Sephadex LH-20,MCI and semipreparative HPLC were used to isolate and purify the constituents of Inula japonica,and the chemical structures were elucidated by chemical properties, MS and NMR analysis. Results: 14 compounds were isolated and their structures were identified as ivangustin( 1),1-acetoxy-6α-hydroxyeriolanolide( 2), 1ß-hydroxyalantolactone( 3),tomentosin( 4),11,13-dihydroinuchinenolide B( 5), britanlin A( 6),vomifoliol( 7), 17-hydroxy-16α-ent-kauran-19-oic acid( 8), 12-hydroxygeranylgeraniol ( 9), dihydroquercetin( 10), kaempferol( 11), quercetin( 12), dihydroconiferyl alcohol( 13) and fareanol( 14). Conclusion: Compounds 5,6,9,13 and 14 are isolated from this plant for the first time.
Subject(s)
Inula , Diterpenes, Kaurane , Drugs, Chinese Herbal , Kaempferols , Lactones , Magnetic Resonance Spectroscopy , SesquiterpenesABSTRACT
OBJECTIVE: To study the chemical compositions of Eucommia ulmoides. METHODS: The compounds were isolated and purified from Eucommia ulmoides by silica gel column chromatography, Sephadex LH-20, MPLC packed with MCI gel and semi-preparative HPLC. The structures of these compounds were established on the basis of spectral analyses (1H-NMR, 13C-NMR and MS). RESULTS: Thirteen compounds were obtained,and their structures were identified as betulin (1), syringin (2), pervoside A (3), glucosyringic acid (4), vanillic acid-beta-glucoside (5), geniposide acid (6), aucubin (7), geniposide (8), pinoresinol-4,4'-di-O-beta-D-glucopyranoside (9), syringaresinol di-O-beta-D-glucopyranoside (10), medioresinol di-O-beta-D-glucopyranoside (11), sucrose (12), and ethyl beta-glucopyranoside (13) on the basis of physical characteristics and spectral data. CONCLUSION: Compounds 3 - 5, 12 and 13 are isolated from this plant for the first itme.
Subject(s)
Drugs, Chinese Herbal/chemistry , Eucommiaceae/chemistry , Plants, Medicinal/chemistry , Benzoates/chemistry , Benzoates/isolation & purification , Chromatography, High Pressure Liquid/methods , Coumaric Acids/chemistry , Coumaric Acids/isolation & purification , Drugs, Chinese Herbal/isolation & purification , Glucosides/chemistry , Glucosides/isolation & purification , Molecular Structure , Plant Bark/chemistryABSTRACT
Tussilagone (TSL) and its allied sesquiterpenoids were considered as the main active principles of the flower buds of Tussilago farfara, which has been widely used in China as an antitussive herbal medicine. Six new bisabolane-type sesquiterpenoids, tussfararins A-F (1-6), along with 12 known sesquiterpenoids, were isolated from the flower buds of T. farfara. Structures of the new compounds were elucidated by extensive spectroscopic analysis. The biological analysis showed that compounds 1, 3, 6, and 7 inhibited nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells with IC50 values of 13.6-24.4 µM.
Subject(s)
Antitussive Agents/isolation & purification , Drugs, Chinese Herbal/isolation & purification , Lipopolysaccharides/adverse effects , Nitric Oxide/metabolism , Sesquiterpenes/isolation & purification , Tussilago/chemistry , Animals , Antitussive Agents/chemistry , Antitussive Agents/pharmacology , Cell Line, Tumor , Drugs, Chinese Herbal/chemistry , Drugs, Chinese Herbal/pharmacology , Flowers/chemistry , Inhibitory Concentration 50 , Magnetic Resonance Spectroscopy , Mice , Molecular Structure , Plants, Medicinal , Sesquiterpenes/chemistry , Sesquiterpenes/pharmacologyABSTRACT
OBJECTIVE: To compare the effects of intra-articular hyaluronic acid (HA; ARTZ) and transcutaneous electric nerve stimulation (TENS) in the treatment of patients with knee osteoarthritis. DESIGN: A prospective, randomized controlled trial. SETTING: Rehabilitation clinic of a teaching hospital. PARTICIPANTS: Patients with knee osteoarthritis (N=50; aged 51-80y) were randomly assigned to the HA group (n=27) or the TENS group (n=23). INTERVENTIONS: The HA group received intra-articular HA injection into the affected knee once a week for 5 consecutive weeks, and the TENS group received a 20- minute session of TENS 3 times a week for 4 consecutive weeks. MAIN OUTCOME MEASURES: The primary outcome measures used were the visual analog scale (VAS) for pain and the Lequesne index. The secondary outcome measures were range of motion of the knee, walking time, pain threshold, patient global assessment, and disability in activities of daily living. All subjects were assessed at baseline, and at 2 weeks, 2 months, and 3 months after the treatments were completed. RESULTS: The TENS group exhibited a significantly greater improvement in VAS than the HA group at 2 weeks' follow-up (4.17 ± 1.98 vs 5.31 ± 1.78, respectively; P=.03). In addition, the TENS group also exhibited a significantly greater improvement in the Lequesne index than the HA group at 2 weeks' follow-up (7.78 ± 2.08 vs 9.85 ± 3.54, respectively; P=.01) and at 3 months' follow-up (7.07 ± 2.85 vs 9.24 ± 4.04, respectively; P=.03). CONCLUSIONS: TENS with silver spike point electrodes was observed to be more effective than intra-articular HA injection for patients with knee osteoarthritis in improving the VAS for pain at 2 weeks' follow-up as well as the Lequesne index at 2 weeks' and 3 months' follow-up.
Subject(s)
Hyaluronic Acid/therapeutic use , Osteoarthritis, Knee/therapy , Transcutaneous Electric Nerve Stimulation , Viscosupplements/therapeutic use , Aged , Aged, 80 and over , Cohort Studies , Female , Humans , Injections, Intra-Articular , Male , Middle Aged , Osteoarthritis, Knee/physiopathology , Range of Motion, Articular/physiology , Treatment Outcome , Walking/physiologyABSTRACT
A new tigliane diterpenoid, acerifolin A (1), and a new isopimarane diterpenoid, acerifolin B (2), together with two known compounds, were isolated from Excoecaria acerifolia. Their structures were elucidated on the basis of their spectroscopic methods, including 1D and 2D NMR techniques. All of the compounds were evaluated for cytotoxicity against five human cancer cell lines with cisplantin as a positive control.