Chemical constituents of Swertia patens. The whole plant of air-dried Swertia patens was extracted with 90% EtOH. The water extract was suspended in H₂O and extracted with petroleum ether, EtOAc and n-BuOH, successively. The compounds were isola- ted and purified by column chromatography from the EtOAc fraction, and identified based on spectral analyses (MS, ¹H-NMR, ¹³C- NMR). Eighteen compounds were isolated and elucidated as 3, 4-dihydro-1H,6H,8H-naptho [1,2-c:4,5-c', d'dipyrano-1, 8-dione (1), angelone (2), gentiogenal (3), erythricin (4), erythrocentaurin (5), gentianine (6), swertiakoside B (7), swertiamarin (8), 2'-O-actylswertiamarin (9), amarogentin (10), 1, 3, 5-trihydroxyxanthone (11), 1, 3-dihydroxy-5-methoxyxanthone (12), 1-hydroxy- 2, 3, 5-trimethoxyxanthone (13), gentiocrucine (14), 3-hydroxyphenylketone (15), n-hexacosyl ester 4-hydroxy-trans-cinnamate (16), n-hexacosyl ester 4-hydroxy-cis-cinnamate (17), and cholest-4-en-3-one (18). Compounds 1-7, 9-18 were obtained from S. patens for the first time.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization ; Swertia ; chemistry

This present work is to study the chemical constituents of Swertia angustifolia. The whole plants of air-dried Swertia angustifolia was extracted with 90% EtOH. The water extract was suspended in H2O and extracted with petroleum ether, EtOAc and nBuOH, successively. The compounds were isolated and purified by column chromatography from the EtOAc fraction, and identified based on spectral analyses (MS, 1H-NMR, 13C-NMR). Fourteen compounds were isolated and characterized as 1, 8-dihydroxy-3, 7-dimethoxyxanthone (1), 1, 8-dihydroxy-3, 5, 7-trimethoxyxanthone (2), 7-hydroxy-3, 8-dimethoxyxanthone-1-O-β-D-glucopyranoside (3), 8-0-[β-D-xylopyranosyl-(1-6) -β-D-glucopyranosyl] -1, 7-dihydroxy-3-methoxyxanthone (4), (+) -syringaresinol (5), ferulic acid (6), trans-coniferyl aldehyde (7), sinapaldehyde (8), trans-coniferyl alcohol (9), 3, 4-dihydroxybenzoic acid (10), 2-hydroxybenzoic acid (11), isophthalic acid (12), 2-furoic acid (13), and 2-methyl-4(3H)-quinazolinone(14). Compounds 2-14 were obtained from this plant for the first time.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Mass Spectrometry ; Molecular Structure ; Swertia ; chemistry

This study is to investigate the chemical constituents of Swertia kouitchensis. The whole plants of air-dried Swertia kouitchensis was extracted with 90% EtOH. The water extract was suspended in H2O and extracted with petroleum ether, EtOAc and n-BuOH, successively. The compounds were isolated and purified by column chromatography from the EtOAc fraction, and their structures were identified based on spectral analyses (MS, 1H-NMR, 13C-NMR). Twenty-eight compounds were obtained, and characterized as erythrocentaurin (1), erythrocentaurin dimethylacetal (2), swertiamarin (3), vogeloside (4), 2'-O- actylswertiamarin (5), swertianoside D (6), gentiocrucines A-B (7-8), gentiocrucine (9), 1-hydroxy-3, 7, 8-trimethoxyxanthone (10), 1-hydroxy-3, 5, 6-trimethoxyxanthone (11), 3-epitaraxerol (12), erythrodiol 3-O-palmitate (13), (+) -syringaresinol (14), caffeic acid (15), trans-coniferyl aldehyde (16), trans-coniferyl alcohol (17), 3, 4-dihydroxybenzoic acid (18), 4-hydroxy-3-methoxybenzoic acid (19), 3, 4-dihydroxybenzoic aldehyde (20), 2, 3-dihydroxybenzoic acid (21), 4-hydroxybenzoic acid (22), 3-acetoxybenzoic acid (23), 3-hydroxybenzoic acid (24), 3-hydroxybenzoic alcohol (25), nicotinic acid (26), 2-furoic acid (27), and uracil (28). Compounds 1-4, 6-28 were obtained from S. kouitchensis for the first time.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Magnetic Resonance Spectroscopy ; Mass Spectrometry ; Molecular Structure ; Swertia ; chemistry

The aim of this research is to prepare a novel monoclonal antibody against granulocytes by the intraperitional routine procedure and evaluate the usefulness of (99)Tc(m) labelled anti-granulocyte monoclonal antibody (McAb) SZ-102 for the detection of experimental inflammatory areas in rabbits. It was characterized as IgG1 subclass by the double immunodiffusion analysis. The flow cytometry demonstrated that SZ-102 reacted selectively with human granulocytes, monocytes, and with their bone marrow precursors, while human lymphocytes, red blood cells and platelets remained negative. In addition, SZ-102 antigen was expressed on the macrophages of liver, lung, thymus, spleen and lymph node by immunohistochemical SP methods. It is suggested that McAb SZ-102 is mainly against granulocytes. SZ-102 was labelled with (99)Tc(m) using 2-iminothiolane modification McAb and (99)Tc(m) -glucoheptonate (GH) transchelation method. The experimental rabbit model of inflammatory areas was prepared,through injecting with (99)Tc(m)-SZ-102 by ear-edge vein, and then imaged by SPECT. (99)Tc(m) labelled murine IgG was used as a negative control. The inflammatory areas in rabbits were clearly imaged at 2 to 4 hour after injection of (99)Tc(m)-SZ-102, while the control group after injection of (99)Tc(m)-labeled murine IgG was negative. In conclusion, the McAb SZ-102 may be a potential agent for the diagnosis and localization of inflammatory areas of carcinomas and clinically concealed infectious diseases.
Animals ; Antibodies, Monoclonal ; Flow Cytometry ; Granulocytes ; immunology ; Humans ; Inflammation ; diagnostic imaging ; Mice ; Mice, Inbred BALB C ; Rabbits ; Radioimmunodetection ; Technetium

Fifteen known compounds were isolated from Swertia delavayi by silica gel, Sephadex LH-20 and Rp-18 column chromatographies. Based on extensive spectroscopic analysis (MS, 1H, 13C-NMR), their structures were identified aserythrocentaurin (1), erythrocentaurindimethylacetal (2), sweroside (3), swertiamarin (4), gentiopicroside (5), swertiakoside A (6), 2'-O-acetylswertiamarin (7), 4'-O-[(Z) -coumaroyl] swertiamarin (8), 1,5,8-trihydroxy-3-methoxyxanthone (9), 8-O-β-D-glucopyranosyl-1-hydroxy-2,3, 5-trimethoxyxanthone (10), 8-O-[β-D-xyl- opyranosyl-(1 --> 6)-β-D-glucopyranosyl]-7,8-dihydroxy-3-methoxyxanthone (11), isovitexin (12), β-sitosterol (13), daucosterol (14), and oleanolic acid (15). Among them, ten ones (14, 7-11, 13) were obtained from S. delavayi for the first time. The isolates were evaluated for their anti-HBV activities in HepG 2. 2. 15 cell line in vitro. The results showed that compound 1, 2, 6, 7, 9 and 12 exhibited significant inhibitory activity on HBV DNA replication with IC50 values from 0.05 to 1.46 mmol x L(-1).
Antiviral Agents ; chemistry ; isolation & purification ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Hepatitis B virus ; drug effects ; genetics ; Magnetic Resonance Imaging ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization ; Swertia ; chemistry

AIMTo study asymmetric total synthesis of 14-nor-huperzine A 2 and its inhibitory activity on acetylcholinesterase.

METHODSHighly enantioselective synthesis of compound 5 from beta-keto-ester 3 and 2-methylene-1,3-propanediol diacetate 4 by palladium-catalyzed bicycloannulation was carried out using new chiral ferrocenylphosphine ligands, such as 10, 11, followed by regioselective double-bond migration to produce compound 6. Optically pure 6 was obtained after enantio-enrichment recrystallization. Then, according to similar procedures of huperzine A synthesis, the target compound 14-nor-huperzine A 2 was prepared. The inhibitory activity was tested with rat erythrocyte membrame acetylcholinesterase.

RESULTSThe inhibitory activity of synthetic (-)-14-nor-huperzine A was 8 fold less potent than that of (-)-huperzine A.

CONCLUSIONA hydrogen-bond between 14-methyl group of (-) huperzine A and the main-chain oxygen of His 440 is necessary for the highly acetylcholinesterase inhibitory activity of huperzine A.

Acetylcholinesterase ; metabolism ; Alkaloids ; Alzheimer Disease ; drug therapy ; Animals ; Cholinesterase Inhibitors ; chemical synthesis ; pharmacology ; therapeutic use ; Erythrocyte Membrane ; drug effects ; enzymology ; Molecular Conformation ; Molecular Structure ; Rats ; Sesquiterpenes ; chemical synthesis ; chemistry ; pharmacology ; therapeutic use

Objective:To investigate the therapeutic effects of noninvasive ventilation on heart failure(HF)after acute myocardial infarction(AMI)in rats.Methods:A rat model of HF after AMI was established by ligation of the left ventricular branch.Thirty male Wistar rats were randomly divided into three groups according to the random number table method: sham operation group, non-treatment group and noninvasive ventilation treatment group(n=30, each group). Echocardiography was performed on the third day after surgery, and parameters including left atrial diameter(LAD), left ventricular end diastolic diameter(LVEDD), interventricular septum thickness(IVS)and left ventricular ejection fraction(LVEF)were recorded.Serum levels of brain natriuretic peptide 45(BNP45), tumor necrosis factor α(TNF-α), matrix metalloproteinase-2(MMP-2), matrix metalloproteinase-9(MMP-9), and heat-shock protein 70(HSP70)were measured at day 3 after operation by enzyme-linked immunosorbent assays(ELISA). Morphological changes of myocardial tissue were analyzed with hematoxylin-eosin(HE)staining, and cardiomyocyte apoptosis was detected by terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling(TUNEL).Results:Compared with the non-treatment group, LVEDD decreased[(153.9±8.1)mm/m 2vs.(164.7±10.4)mm/m 2, P<0.05]and LVEF increased[(63.9±7.6) % vs. (54.4±9.4) %, P<0.05]in the noninvasive ventilation group .Compared with the non-treatment group, serum levels of BNP45[(0.65±0.07) % vs. (0.73±0.07) μg/L, P<0.05], TNF-α(361.5±13.1) μg/L vs. (399.1±12.6) μg/L( P<0.05), MMP-2(6 892.8±530.2) μg/L vs. (7 406.0±667.5) μg/L( P<0.05)and MMP-9(143.8±5.9) μg/L vs. (151.1±8.3) μg/L( P<0.05)decreased and levels of HSP70[(1.7±0.1)μg/L vs.(1.4±0.1)μg/L, P<0.05]increased in the noninvasive ventilation group.HE staining showed focal accumulation of neutrophils in the epicardium, loss of muscle striation, disorganized cell polarity and enlarged nuclei in the non-treatment group.Meanwhile, alleviated inflammation, scattered neutrophils between cardiomyocytes and misaligned muscle striation were observed in the noninvasive ventilation group.TUNEL results showed that the myocardial apoptotic index was lower in the noninvasive ventilation group than in the non-treatment group( P<0.05). Conclusions:Noninvasive ventilation can effectively improve heart function, reduce inflammatory response and cardiomyocyte apoptosis in rats with AMI-induced HF and may be an effective treatment for HF after AMI.

OBJECTIVE: To explore the effect of Twist gene on the migration and invasion of human gastric carcinoma cells. METHODS: MKN28 cells, a human gastric carcinoma cell line, were transfected with PcDNA3.1-Twist plasmid by lipofectamine transfecting technique. The transfected cells were selected with geneticin. Expressions of Twist,ecadherin and vimentin protein were detected by Western blot in cells transfected Twist gene. Matrigel invision chambers were performed to analyse the cell migration and invasion. RESULTS: MKN28 cells transfected with PcDNA3.1-Twist plasmid showed stronger intracellular expression of Twist protein than MKN28 cells transfected with PcDNA3.1 and MKN28 cells without transfection. The expression of ecadherin protein in MKN28 cells transfected with PcDNA3.1-Twist plasmid was significantly decreased compared with that in MKN28 cells transfected with PcDNA3.1 and MKN28 cells without the transfection. However, The expression of vimentin protein in MKN28 cells transfected with PcDNA3.1-Twist plasmid was significantly increased compared with that in MKN28 cells transfected with PcDNA3.1 and MKN28 cells without transfection. The migration and invasion ability of Twist+ - MKN28 cells were stronger than that of MKN28 cells transfected with PcDNA3.1 and MKN28 cells without transfection. CONCLUSION Twist gene may promote the migration and invasion ability of gastric carcinoma cells through epithelial mesenchymal transition.
Cadherins ; biosynthesis ; Cell Movement ; genetics ; Humans ; Neoplasm Invasiveness ; Neoplasm Metastasis ; Stomach Neoplasms ; genetics ; metabolism ; pathology ; Transfection ; Tumor Cells, Cultured ; Twist-Related Protein 1 ; biosynthesis ; genetics ; Vimentin ; biosynthesis

Objective:To investigate the impact of QiliQiangXin Capsules on ventricular remodeling and cardiac contraction and relaxation function in aging rats with heart failure following myocardial infarction.Methods:From August 2022 to August 2023, a total of 30 old rats were randomly assigned to three groups: sham-operated group, model group, and treatment group, with 10 rats in each group selected through a digital lottery method.The model and treatment groups were created by ligating the anterior descending branch of the left coronary artery.The rats in the treatment group received daily administration of Astragalosa hebecarpa Drabanemerosa Strong Heart Capsule(1.0 g/kg)via gavage after 4 weeks.After the 4-week drug administration period, echocardiography was performed to measure various parameters including left ventricular end-diastolic internal diameter(LVIDd), left ventricular end-systolic internal diameter(LVIDs), left ventricular ejection fraction(LVEF), left ventricular anterior wall myocardial thickness(LVAWd), mitral valve early diastolic peak flow velocity(E peak), and early diastolic velocity of mitral annulus(e peak)detected by tissue Doppler(TDI). The E/e value was calculated based on these measurements.Additionally, serum levels of B-type brain natriuretic peptide(BNP), matrix metalloproteinase 2(MMP-2), matrix metalloproteinase 9(MMP-9), and tumor necrosis factor(TNF-α)were measured using enzyme-linked immunosorbent assay(ELISA). Hematoxylin-eosin(HE)staining was employed to observe the morphological changes in myocardial tissue.Results:Compared to rats in the model group, rats in the treatment group exhibited lower left ventricular internal dimension at end-diastole(LVIDd)(9.1±0.6 mm vs.11.4±0.8 mm, P<0.01), lower left ventricular internal dimension at end-systole(LVIDs)(5.9±0.8 mm vs.8.7±0.9 mm, P<0.01), lower E/e ratio(13.4±2.0 vs.16.3±2.8, P<0.05), higher left ventricular ejection fraction(LVEF)(68.8±7.1% vs.52.0±8.4%, P<0.01), and elevated left ventricular anterior wall thickness at end-diastole(LVAWd)(1.5±0.2 mm vs.1.2±0.3 mm, P<0.05). In addition, compared to rats in the model group, the treatment group showed a decrease in brain natriuretic peptide(BNP)(0.26±0.04 μg/L vs.0.34±0.05 μg/L, P<0.01), decreased matrix metalloproteinase-2(MMP-2)(3697.0±857.7 μg/L vs.4719.5±703.5 μg/L, P<0.01), decreased matrix metalloproteinase-9(MMP-9)(87.3±13.8 μg/L vs.116.5±9.6 μg/L, P<0.01), decreased tumor necrosis factor-alpha(TNF-α)(165.3±36.9 μg/L vs.269.8±35.0 μg/L, P<0.01), and lower TNF-α levels(165.3±36.9 μg/L vs.269.8±35.0 μg/L, P<0.01). Histological examination using hematoxylin and eosin(HE)staining revealed that the treatment group had less severe cardiac myocyte arrangement disorder and inflammatory reaction compared to the model group. Conclusions:Qiliqiangxin Capsules were found to effectively delay ventricular remodeling and improve myocardial contraction and relaxation function in aging rats with heart failure after acute myocardial infarction.

OBJECTIVETo evaluate the effect of comprehensive control strategy of schistosomiasis with emphasis on infection source control in Anhui province.

METHODSForty endemic villages in Guichi district, Chizhou city, Anhui province were selected as national pilot villages in the years from 2006 to 2008, and another 10 provincial pilot villages were respectively selected from 10 highly endemic villages in 7 cities in 2007. The comprehensive infection source control measures, including "replace cattle with machines", "raise livestock in pens", "improve the sanitary toilets", "supply safe water " and so on were carried out among the above pilot villages. At the end of 2008, 13 national pilot villages and 6 provincial pilot villages were selected to investigate the popularity of schistosomiasis, and the effect of the comprehensive control strategy in those villages were compared.

RESULTSAfter implementing the comprehensive control strategy, the infectious rate of schistosomiasis in national pilot villages decreased from 4.57% (487/10 659) to 1.76% (147/8370), with the reduction rate at 61.49%, whose difference showed statistical significance (χ(2) = 115.16, P < 0.01); and the density of infected snails decreased from 0.0067/0.1 m(2) to 0.0008/0.1 m(2), the infectious rate of snails decreased from 0.28% to 0.04%, whose reduction rates were 88.06% and 85.71% respectively. While as to the provincial pilot villages, the infectious rate of schistosomiasis decreased from 1.27% (54/4254) to 0.21% (14/6592), with the reduction rate at 83.46%, whose difference showed statistical significance (χ(2) = 94.57, P < 0.01); and the density of infected snails decreased from 0.0025/0.1 m(2) to 0.0003/0.1 m(2), the infection rate of snails decreased from 0.13% to 0.05%, whose reduction rates were 88.00% and 61.54% respectively.

CONCLUSIONThe comprehensive control strategy with emphasis on infection source control implemented in marshland and lake regions can effectively control the transmission of schistosomiasis.

Animals ; China ; epidemiology ; Disease Reservoirs ; parasitology ; Humans ; Infection Control ; methods ; Livestock ; Pilot Projects ; Rural Health ; Schistosomiasis ; epidemiology ; parasitology ; prevention & control ; Snails ; parasitology