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Objective To investigate the main chemical constituents of the low polarity extracts from pinusmassoniana Lamb. leaves and their synergetic activity with fluconazole against fluconazole-resistant Candida albicans. Methods The pinusmassoniana leaves were extracted with 80% ethanol, and then the extracts were extracted by petroleum ether to obtain the low polarity extracts. The chemical components were detected by GC-MS and elucidated by the comparison with the standard mass spectral data. The relative contents in percentage were calculated using the area normalization method. The minimal inhibitory concentrations (MIC80) of fluconazole-resistant Candida albicans strains by the low polarity extracts in combination with fluconazole were determined by checkerboard microdilution assay. Results 30 components were detected from the low polarity extracts, and 17 components were identified. The minimum inhibitory concentration (MIC80) of the 80% ethanol extracts, the low polarity extracts and the petroleum ether extracts from the pinusmassoniana leaves combined with fluconazole against fluconazole-resistant Candida albicans were 7.81 μg/ml, 31.25 μg/ml and >250 μg/ml, respectively. Conclusion The 80% ethanol extracts of pinusmassoniana leaves and its low polarity extracts have synergistic activity combined with fluconazole onfluconazole-resistant Candida albicans. The diterpenoids (53.99%) may be the effective components of the low polarity extracts.
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Herba Monochasmae savatii, whole plant of the Monochasma savatier Franch. or Monochasma sheareri Franch. ex Maxim., scrophulariaceae, was first found in "Zhiwu Mingshi Tukao". It has the effects of clearing heat and detoxicating, dispelling wind and relieving pain, cooling the blood and stopping bleeding, etc. This review used Monochasma savatier Franch. or Monochasma sheareri Franch. ex Maxim. as the subject term to search CNKI, PubMed and SciFinder, and reviewed the classification of medicinal material, medicinal standards, chemical components, biological activities and pharmacological effects of Herba Monochasmae savatii in recent years to provide a basis for the research, development and clinical rational application.
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Objective To establish a HPLC method for simultaneous determination of quercitrin, luteoloside, rutin and 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside in Yangxue Anshen syrup. Methods Waters symmetry C18 column (250 mm×4.6 mm, 5 μm) was used with 0.1% acetic acid (A) and methanol (B) as the mobile phase. Gradient elution was performed at a flow rate of 1.0 ml/min, 0-15 min, 95%-90%A; 15-35 min, 90%-70%A; 35-55 min, 70%-60%A; 55-85 min, 60%-50%A; 85-95 min, 10%A. The detection wavelengths were 256 nm and 320 nm. Column temperature was 30 ℃ and the injection volume was 10 μl. Results Quercitrin, luteoloside, rutin and 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside showed good linear relationship within the range of 10-300, 5.0-150.0, 5.0-150.0, 20.0-600.0 µg/ml(r≥0.9989), respectively. The average recovery was (96.75±1.41)%, (99.61±1.01)%, (97.18±1.96)% and(99.12±0.97)% (n=6), respectively. Conclusion The established method is simple, accurate and stable, which can be used for the simultaneous determination of 4 components in Yangxue Anshen syrup.
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Objective To explore the potential mechanism of Jiangzhihugan capsule (JZHG) for fatty liver (FL), and to provide a theoretical guideline for the clinical application of JZHG. Methods TCMSP and TCMID databases were used to search for the active components and targets of JZHG. GeneCards and OMIM database were used to search the FL related targets. The intersection method was used to identify the common targets of JZHG and FL. Cytoscape software was applied for the construction of active compounds-targets network map. Protein-protein interaction network was constructed by STRING software. Gene ontology functional enrichment analysis and KEGG pathway enrichment analysis were conducted with Bioconductor database and R software. Results 46 potential active components were screened out from JZHG. 7406 targets were retrieved through GeneCard and OMIM database. 118 genes were obtained from the intersection of component-target and disease-target. These genes were mainly involved with the response to oxidative stress, apoptosis, inflammatory response, hormone resistance and other biological processes. The mechanism was related to PI3K-Akt signaling pathway, human cytomegalovirus infection, microRNAs in cancer, etc. Conclusion The mechanism of active ingredients for FL in JZHG may be due to improving lipid metabolism and reducing liver fat accumulation through anti-oxidative stress and anti-inflammatory effects.
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Objective To design and synthesize schisandrone derivatives for the therapy of disease like AD,and to meas-ure their anti-oxidation activity.Methods Ten compounds were synthesized,and seven of them were first reported.The influ-ence all the compounds on SOD from the mouse serum were measured to evaluate anti-oxidation activity.Structure-activity rela-tionship(SARs)were also discussed.Results Compounds 2,3,5 and 8 could increase the activity of SOD in mouse serum.Fur-thermore,Compounds 2,3 and 5 showed better activities than schisandrone.Conclusion Synthesized schisandrone derivatives showed anti-oxidation activity.The SARs demonstrated the carbonyl of C-1 position and the methyls of C-2 and 3 had no influ-ences to the anti-oxidant activity.
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Objective A series of 4 substituted salidroside derivatives were designed and synthesized .Their anti-fatigue effects were investigated .Methods With five-acetyl glucose and different 4-substituted benzyl tyrosols as the starting materi-als ,salidroside derivatives were synthesized through glycosidation and deacetylation reactions .The exercise exhaustive mice model was used to study the anti-fatigue effects of those synthesized derivatives by comparing the loading swimming time of mice .Results 10 novel salidroside derivatives were synthesized .The loading swimming tests showed that the swimming time of the mice in the positive group (salidroside) and 3a-1 group (phenethyl-β-D-glucoside) was longer than that in the control group with statistically significant difference(P<0 .05) .The swimming times for other groups were similar to control group with no statistically significant difference .Conclusion This synthetic method for salidroside derivatives was convenient and feasible for large production .The 4-hydroxyl groups on the benzene ring of salidroside and its derivatives may be the active site responsible for their anti-fatigue activity .
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Objective To develop a HPLC method for determination of baicalin .Methods The separation was carried out on a Waters XBridge C18 column(4 .6 mm × 250 mm ,5μm) ,the mobile phase was composed of acetonitrile and 0 .8% for-mic acid (25∶75) ,the detection wavelength was set at 276 nm ,the flow rate was 1 .0 ml/min ,the column temperature was 30 ℃ and the injection volume was 10 μl .Results The linearity was obtained over 1 .25-40 μg/ml(r=0 .999 9) for baicalin . The RSD of precision were less than 2% .The average recovery was between 95% and 100% .Conclusion This HPLC method was simple ,accuracy and suitable for the quality control of Biyanling capsule .
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BACKGROUND: Morphine is the first choice for the pain of medium and advanced degrees due to cancer. This is advocated in the Pain Relieving Guide of the WHO. Controlled-release morphine sulfate tablets(CRM) and sustained-release morphine sulfate tablets (SRM) all belong to oral long-acting morphine. It plays an important role in relieving cancer pain effectively and improving their quality of life(QOL).OBJECTIVE: To observe the analgesic effect of CRM and SRM and to observe how they improve the QOL of the cancer patients with severe cancer pain.SETTING: Department of oncology, department of surgery, department of internal medicine and department of traditional chinese medicine in the first affiliated hospital of a university.PARTICIPANTS: During October 1995 to June 1998, all inpatients that were pathologically proved to suffer from malignant tumor with severe pain were recruited into our study.METHODS: There were 182 patients with severe pain due to advanced cancers pathologically proven. They all met the entry criterion of the study. Totally 95 patients were treated with CRM, of which 12 cases were lost in follow-up due to side effects, death, or discharge from the hospital, and the rest 83 cases entered the stage of clinical trial. Eighty-seven patients were treated with SRM. Of them 25 cases were lost in follow-up due to side effects, death, or discharge from the hospital, and the rest 62 cases entered the stage of clinical trial. The recommended initial dosage of CRM or SRM was 30 mg every 12 hours for all patients, and then the dosage was regulated according to the effects until the ideal anesthesia was achieved.MAIN OUTCOME MEASURES: Assessments included pain severity, the effective rate, complete remission rate, remission time, adverse reactions, and the QOL before and after the treatment.RESULTS: The effective rates of CRM and SRM were 95% and 94%respectively. The complete remission rates were 82% and 80% respectively, and the remission time was(9.1 ±4.1) hours and (8.7±4.4)hours respectively. Statistically, there was no significant difference in analgesic effect and remission time between CRM and SRM. QOL was elevated for a higher degree in 62(75% ) and 47(76% ) patients after the treatment. QOL scores of CRM were (34.6 ± 11.5 ) points before treatment and (52.6 ± 13.0) points after the treatment( P = 0. 000), while QOL scores of SRM were(37.7 ± 9.7) points before the treatment and points (49.8 ± 12.9) points after the treatment (P = 0. 000). There was significant difference in QOL after the treatment. They could relicve osteocope,visceral pain, soft tissue infiltrative pain more effectively than they do about neurological pain.CONCLUSION: Oral treatment with CRM and SRM for the patients with server cancer pain shows a similar analgesic effect. They are effective, safe,and convenient, and can improve the QOL.
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Objective To study indole alkaloids of Ervatamia hainanensis. Methods The compounds were separated and purified by column chromatography with silica gel and Sephadex LH-20. The structures were identified by IR, MS, and NMR. Results Seven alkaloids were identified as: hainanervatasine (Ⅰ), hainanervatacine (Ⅱ), vobasine (Ⅲ), coronaridine (Ⅳ), 3-hydroxyl coronaridine (Ⅴ), 3-(2-oxopropyl) coronaridine (Ⅵ), and tabernamine (Ⅶ), respectively. Conclusion Compounds Ⅰ and Ⅱ are new compounds. Compounds Ⅳ and Ⅵ are isolated from this plant for the first time.