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Objective:To evaluate the effect of parecoxib sodium on phenotypic transformation of alveolar macrophages in a mouse model of ventilator-associated lung injury (VALI).Methods:Forty-five SPF healthy adult male C57BL/6J mice, weighing 22-30 g, aged 8-12 weeks, were divided into 3 groups ( n=15 each) using a random number table method: sham operation group (S group), VALI group (V group) and parecoxib sodium group (P group). Lipopolysaccharide 20 ng was intraperitoneally injected, and 2 h later the animals were mechanically ventilated (tidal volume 30 ml/kg, respiratory rate 70 breaths/min, inspiratory/expiratory ratio 1∶2, fraction of inspired oxygen 21%, positive end-expiratory pressure 0) for 4 h to establish the model of VALI.Parecoxib sodium 30 mg/kg was intravenously injected at 1 h prior to mechanical ventilation in group P. The mice were sacrificed at 4 h of ventilation, the right lung was lavaged and the broncho-alveolar lavage fluid (BALF) was collected for determination of interleukin-6 (IL-6), IL-10 and tumor necrosis factor-alpha (TNF-α) concentrations (by enzyme-linked immunosorbent assay), expression of inducible nitric oxide synthase (iNOS) and arginase-1(Arg-1) in BALF and expression of phosphorylated Janus kinase 2 (p-JAK2) and phosphorylated signal transduction and transcription activator 3 (p-STAT-3) (by Western blot). The left lung was removed for determination of the wet/dry weight ratio (W/D ratio) and for examination of the pathological changes which were scored. Results:Compared with group S, the lung injury score, W/D ratio, concentrations of IL-6, IL-10 and TNF-α in BALF, and expression of iNOS, Arg-1, p-JAK2 and p-STAT-3 were significantly increased in V and P groups ( P<0.05). Compared with group V, the concentration of IL-10 in BALF and expression of Arg-1, p-JAK2 and p-STAT-3 were significantly increased, and the lung injury score, W/D ratio, concentrations of IL-6 and TNF-α in BALF and expression of iNOS were decreased in group P ( P<0.05). Conclusion:Parecoxib sodium promotes phenotypic transformation of alveolar macrophages from M1 subtype to M2 subtype and inhibits inflammatory responses, thus alleviating VALI, which may be related to activating JAK2/STAT-3 signaling pathway in mice.
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@#This study aimed to investigate the protective effects of Baibu Tang on bleomycin-induced pulmonary fibrosis in mice. After intratracheally giving bleomycin(3. 5 mg/kg), mice were orally administered Baibu Tang once a day for 14 consecutive days, takingnintedanib as a positive control. The anti-fibrotic effects were assessed by the hydroxyproline level and the histopathological changes in H&E or Masson stained lung tissues. The results revealed that the lung coefficient, hydroxyproline content, inflammation and collagen deposition were increased significantly in the lung tissue of the model mice. Both ethanol and water extracts of Baibu Tang significantly improved all the pathological indexes in mice, but the effect of the ethanol extract was better than that of the water extract. Baibu Tang with Baibu(root of Stemona tuberosa)containing different components(neotuberostemonine, tuberostemonine and stemoninine, respectively)could significantly reduce hydroxyproline level and collagen deposition in the lung tissue of bleomycin-induced mice, and there was no significant difference in their activity. This result showed that the changes in the chemical composition of Stemona tuberosa(Baibu, monarch drug for Baibu Tang)have little effect on the anti-fibrosis activity of Baibu Tang, and its mechanism and material basis need further investigation.
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OBJECTIVE:To provide reference for optimizing gout drug therapy plan. METHODS:A total of 107 patients met gout clinical diagnosis criteria in the Affiliated Hospital of Putian University during Jul. 1st,2016- Jul. 1st,2017 were divided into group A and B according to carrying out HLA-B*58:01 gene detection or not. Group A was divided into positive and negative subgroup according to the results of gene detection. Positive subgroup was given febuxostat 40 mg,qd. Negative subgroup was given allopurinol 300 mg,tid with a treatment course for 2 weeks,the level of uric acid was detected after a treatment course;febuxostat was given instead if the level of uric acid was not up to the standard. Group B was given allopurinol;after a treatment course,the level of uric acid was detected;febuxostat was given instead (usage and dosage as group A) if the level of uric acid was not up to the standard. Both groups were treated for 6 months. The levels of uric acid were investigated in 2 groups before and after treatment so as to evaluate up-to-standard rate of treatment. European 5-D health scale of 2 groups were followed up with telephone to calculate therapeutic efficacy by QALY. Cost-effectiveness of 2 groups were calculated,and sensitivity analysis was conducted. RESULTS:Before treatment,there was no statistical significance in urine acid levels between 2 groups (P>0.05). After treatment,urine acid levels of 2 groups were significantly lower than before treatment with statistical significance(P<0.05). Therapeutic effectiveness was 0.818 QALY in group A and 0.808 QALY in group B,without statistical significance between 2 groups(P>0.05). The cost of group A was 3932.46 yuan,and that of group B was 2174.92 yuan. Cost-effectiveness ratio of 2 groups were 4807.41 and 2691.73,and group A was significantly higher than group B. The therapy plan of group B showed that cost-effectiveness advantage. Sensitivity analysis supported the results. There was no statistical significance in the incidence of ADR between 2 groups (P>0.05). CONCLUSIONS:It shows cost-effectiveness advantage to directly use allopurinol without gene detection in gout patients.
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@#This study aimed to investigate the protective effect of total alkaloids(TA)and one of the active components, neotuberostemonine, of Stemona tuberosa on bleomycin-induced pulmonary fibrosis in mice and to explore the mechanism by fibroblasts model. The bleomycin-induced mice were orally administered with TA(60 mg/kg)and neotuberostemonine(10, 20 mg/kg), with prednisone(6. 67 mg/kg)as a positive control. The anti-fibrotic effects were assessed by hydroxyproline content, TGF-β1 level, inflammatory score, collagen deposition and the expression of α-SMA in the lung tissues. The results revealed that TA and neotuberostemonine could significantly ameliorate the inflammation and injury, and attenuate the hydroxyproline content and collagen deposition. Moreover, neotuberostemonine treatment markedly down-regulated the α-SMA level and TGF-β1 content in bleomycin-injured mice lungs. The in vitro experiments showed that neotuberostemonine inhibited the expression of α-SMA induced by TGF-β1 in a dose-dependent manner, indicating that suppression on differentiation of fibroblasts to myofibroblasts may be one of the mechanisms for neotuberostemonine against pulmonary fibrosis.
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Objective To evaluate the preclinical safety of 2-methoxyestradiol nanosuspension. Methods The safety of 2-methoxyestradiol nanosuspension for injection was observed through vascular stimulation test of the ear vein on rabbits, hemolytic test using rabbit erythrocytes, active systemic anaphylaxis (ASA) test on guinea pigs and acute toxicity test on mice. Results 2-Methoxyestradiol nanosuspension injection had no irritating effects on vessels, and no haemocytolysis, agglutination and ASA occurred.ASA test showed no allergy symptoms such as piloerection, nose rubbing and dyspnea in guinea pigs 30 min after sensitization.Acute toxicity test revealed that no pathological changes, including black spots and hyperaemia, were visually observed on the heart, liver and lungs after 14 days of intravenous administration. Conclusion 2-Methoxyestradiol nanosuspension injection is relatively safe, with low toxicity, and no hemolytic, anaphylactic and irritating effects. It may be clinically used for injection.
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Objective To investigate the methods and effects of nasolabial flaps for repair of defects after skin tumor removal on midface.Methods From Augest 2012 to March 2015,the different flaps from nasolabial fold were utilized to repair 22 skin defects due to surgical removal of skin tumors on midface.There were 12 flaps with subcutaneous pedicle and 10 flaps with skin pedicle in the group.The size of the defects ranged from0.5cm × 1.0cmto4.0cm × 5.0cm.Results After operation,all flaps survived with primary healing,cosmetic results were satisfactory with conceal scar and no facial organs distortion after 1 month to 2 years following-up.No tumor recurrence occurred.Conclusions Thenasolabial flaps with appropriate pedicles could obtain the satisfactory results for the reconstruction of medium-sized skin defects on midface,especially suitable for middle-aged and elderly patients.
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<p><b>OBJECTIVE</b>To study the chemical constituents from aerial parts of Fallopia dumetosum.</p><p><b>METHOD</b>The 80% ethanol extract was separated by means of silica gel and Sephadex LH-20 column chromatography. The compounds isolated from the plant were identified by physicochemical properties and spectroscopic evidence.</p><p><b>RESULT</b>Ten compounds were obtained and identified as emodin (1), physcion (2), quercetin (3), luteolin (4), 5"- methoxy-hydnocarpin (5), ethylparaben (6), protocatechuic acid (7), (2S,3S, 4R) -sphinganine-(2'R) -delta5'6' (E) -2'-hydroxyl tetracosanoylamino (8), beta-sitosterol (9), and daucosterol (10).</p><p><b>CONCLUSION</b>Anthraquinones and flavones were the major constituents of this plant. All compounds were isolated firstly from this plant, and compounds 5, 7, and 8 were isolated from the genus Fallopia for the first time.</p>
Subject(s)
Anthraquinones , Chemistry , Flavones , Chemistry , Plant Components, Aerial , Chemistry , Plant Extracts , Chemistry , Plants, Medicinal , Chemistry , Polygonaceae , ChemistryABSTRACT
<p><b>OBJECTIVE</b>To investigate the chemical constituents of Nauclea latifolia, which is an African folk medicine and collected from Guinea.</p><p><b>METHOD</b>The chemical constituents were isolated by silica gel and Sephadex LH-20 column chromatographies, and structurally elucidated by spectral evidence together with physiochemical properties.</p><p><b>RESULT</b>Twelve compounds including 8 triterpenes and 4 sterols were isolated from the roots of N. latifolia, and their structures were defined as 24-en-cycloartenone (1), ursolic aldehyde (2), quinovic acid (3), rotundic acid (4), 3beta,19alpha,23,24-tetrahydroxyurs-12-en-28-oic acid (5), pyrocincholic acid 3beta-O-beta-D-fucopyranoside (6), quinovic acid 3beta-O-beta-D-glucopyranoside (7), quinovic acid-3b-O-D-glucopyranosyl-(28-->1)-beta-D-glucopyranosyl ester (8), beta-sitosterol (9), stigmastan-3,6-dione (10), stigmast-4-en-6beta-ol-3-one (11) and daucosterol (12) .</p><p><b>CONCLUSION</b>All compounds except for 4,9, andl2 are isolated from this plant for the fist time, while compounds 2, 6, 10, and 11 are isolated from the genus Nauclea for the first time.</p>
Subject(s)
Chromatography , Methods , Guinea , Magnetic Resonance Spectroscopy , Methods , Plant Extracts , Chemistry , Plant Roots , Chemistry , Metabolism , Plants, Medicinal , Chemistry , Rubiaceae , Chemistry , Metabolism , Sterols , Chemistry , Triterpenes , ChemistryABSTRACT
Cholangiocarcinoma is rare. It is highly malignant and early diagnosis is difficult. Various risk facts have been linked to the carcinogenesis and development of cholangiocarcinoma. Chronic inflammation and cholestasis are the two common pathways in the malignant transformation of cholangial cells. We reviewed the molecular biological researches of cholangiocarcinoma from two aspects: its risk factors and related pathomechanism.
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<p><b>OBJECTIVE</b>To investigate the chemical constituents of the flower buds of Tussilago farfara.</p><p><b>METHOD</b>The chemical constituents were isolated by silica gel and Sephadex LH-20 column chromatography, and structurally elucidated by spectral evidence together with physiochemical properties.</p><p><b>RESULT</b>Seven flavonoids, quercetin (1), quercetin-3-O-beta-D-glucopyranoside (2), quercetin-4'-O-beta-D-glucopyranoside (3), hyperoside (4), rutin (5), kaempferol (6), kaempferol-3-O-alpha-L-rhamnopyranosyl-(1-6)-beta-D-glucopyranoside (7), together with eight phenolic acid derivatives, caffeic acid (8), methyl caffeate (9), ethyl caffeate (10), (E)-2,5-dihydroxycinnamic acid (11), 3,4-di-O-caffeoylquinic acid (12), 4,5-di-O-caffeoylquinic acid (13), methyl4,5-di-O-caffeoylquinate (14) and chlorogenic acid (15) were isolated from the flower buds of Tussilago farfara.</p><p><b>CONCLUSION</b>Compounds 7, 9-14 are isolated from this plant, also from this genus, for the first time.</p>
Subject(s)
Flavonoids , Flowers , Chemistry , Hydroxybenzoates , Plant Extracts , Tussilago , ChemistryABSTRACT
<p><b>OBJECTIVE</b>To investigate the chemical constituents in the herbs of Fallopia convolvulus.</p><p><b>METHOD</b>Its 80% ethanol extract was separated by means of silica gel and Sephadex LH-20 column chromatography to give twelve compounds, whose structures were identified by physicochemical properties and spectroscopic evidence.</p><p><b>RESULT</b>Twelve compounds were isolated and identified as: quercetin (1), luteolin (2), chrysoeriol (3), apigenin (4), kaempferol-3-O-beta-D-glucoside (5), quercetin-3-O-rhamnoside (6), N-trans-coumaroyl tyramine (7), loliolide (8), ethylparaben (9), beta-sitosterol (10), daucosterol (11), n-hexadecanoic acid (12).</p><p><b>CONCLUSION</b>All these compounds were isolated firstly from this plant, compounds 6-9 were obtained from this genus for the first time.</p>
Subject(s)
Chromatography , Plant Components, Aerial , Chemistry , Plant Extracts , Polygonaceae , ChemistryABSTRACT
<p><b>OBJECTIVE</b>To develop an HPLC method for the determination of alisol A, alisol F, alisol A 24-acetate and alisol B 23-acetate in the rhizome of Alisma orientalis.</p><p><b>METHOD</b>The separation was performed on a Shim-Pack CLC-ODS a C18 column (6 mm x 150 mm, 5 microm) eluted with the mobile phases of acetonitrile (A)-water (B) in gradient elution. The absorbance was monitored at 210 nm. Orthogonal test was adopted to optimize the extraction conditions of the four alisols.</p><p><b>RESULT</b>The correlation coefficients of the four alisols were higher than 0.999 and the average recoveries were 99.23%, 96.67%, 97.30% and 99.61%, respectively. All the RSDs were less than 3%.</p><p><b>CONCLUSION</b>The validation data demonstrated that the method was accurate and repeatable, and can be used to measure the four alisols in Rhizoma Alismatis.</p>
Subject(s)
Alisma , Chemistry , Cholestenones , Chromatography, High Pressure Liquid , Methods , Chromatography, Reverse-Phase , Methods , Reproducibility of Results , Rhizome , Chemistry , Time Factors , TriterpenesABSTRACT
<p><b>OBJECTIVE</b>To investigate the chemical constituents in herbs of Polygonum jucundum.</p><p><b>METHOD</b>The 85% ethanol extract was separated by means of silica gel and Sephadex LH-20 column chromatography. The compounds isolated from the plant were identified by physicochemical properties and spectroscopic evidence.</p><p><b>RESULT</b>Eight compounds were isolated and identified as: quercetin-3'-O-beta-D-galactoside (1), 8-methoxyquercetin (2), pigenin (3), luteolin (4), quercetin (5), 3,5,7-trihydroxychromone (6), p-hydroxybenzaldehyde (7), beta-sitosterol (8).</p><p><b>CONCLUSION</b>All compounds were isolated from this plant for the first time, compounds 5- 8 were isolated from the genus Polygonum for the first time.</p>
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Drugs, Chinese Herbal , Chemistry , Polygonum , ChemistryABSTRACT
<p><b>OBJECTIVE</b>To investigate the chemical constituents with immunosuppressive function from Alisma orientalis.</p><p><b>METHOD</b>The chemical constituents were isolated and purified by kinds of column chromatography and its structures were elucidated by NMR spectra and physicochemical properties. Its immunocompentence of lymphocytes taken from spleen of mouse were examined by MTT assay.</p><p><b>RESULT</b>Twelve compounds were isolated and identified as clovandiol (1), orientalol E (2), alismoxide (3), alismol (4), 4alpha, l0alpha-dihydroxy-5beta-H-guaj-6-en (5), alismorientols A (6), alisol F (7), alisol A (8), 13beta,17beta-epoxy alisol A (9), alisol B 23-acetate (10), 1H-indole-3-carboxylic acid (11) and cuccinic acid (12). Compounds 9, 10 and alisol A 24-acetate showed immunosuppressive function.</p><p><b>CONCLUSION</b>Compounds 1, 5, 11 and 12 were isolated firstly from this genus,and the NMR spectra data of 1 were corrected firstly, some protostan-type triterpenoids may be developed as new drug with immunosuppressive function.</p>
Subject(s)
Animals , Mice , Alisma , Chemistry , Cells, Cultured , Cholestenones , Chemistry , Pharmacology , Drugs, Chinese Herbal , Chemistry , Pharmacology , Immunosuppressive Agents , Chemistry , Pharmacology , Indoles , Chemistry , Pharmacology , Magnetic Resonance Spectroscopy , Mice, Inbred C57BL , Sesquiterpenes , Chemistry , Pharmacology , T-Lymphocytes , Cell Biology , Triterpenes , Chemistry , PharmacologyABSTRACT
One new quinoline alkaloid and seven known bisabolane sesquiterpenes: 2-(2'-methyl-1'-propenyl)-4, 6-dimethyl-7-hydroxyquinoline(1), 2, 5-dihydroxybisabola-3, 10-diene(2), 4, 5-dihydroxybisabola-2, 10-diene(3), turmeronol A(4), bisacurone(5), bisacurone A(6), bisacurone B(7), bisacurone C(8), as well as dehydrozingerone(9) and zingerone(10) were isolated from the root tuber of Curcuma longa. Their structures were identified by spectral evidence. Compound 1 is a new compound, compounds 6-8 were isolated from this plant for the first time and compounds 9-10 from Curcuma for the first time.
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Aim To study the chemical constituents of the underground part of Ligularia pleurocaulis (Franch.) Hand-Mazz.. Methods The dried roots and rhizomes of L.pleurocaulis were extracted with methanol. Isolation and purification were performed by silica gel column chromatography and recrystallization etc. Structures of the pure compounds were established on basis of spectral analysis. Results Twelve compounds were obtained from L.pleurocaulis, they were 6-angeloyloxy-furanoligu-larenone (1), 2-oxo-3-hydroxy-eremophila-1(10),3,7(11),8-tetraen-8,12-olide (2), tiglic acid (3), oleanolic acid (4), lupeol (5), β-sitosterol (6), daucosterol (7), caffeic acid (8), emodin (9), 7-methoxy-coumarin (10), ferulic acid (11) and 4-hydroxy-2,5-dimethoxy-benzaldehyde (12). Conclusion Compound 1 is a new eremophilane and compound 2 is a new natural compound. All above compounds were obtained for the first time from L.pleurocaulis.