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Chemical Constituents Of Antinociceptive And Anticancer Activities Of Caragana Microphylla Lam. Seeds

Posted on:2007-03-23Degree:MasterType:Thesis
Country:ChinaCandidate:Y HuoFull Text:PDF
GTID:2144360182991598Subject:Pharmacognosy
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In accordance with the International Association for the Study of Pain, pain has been defined as an unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage. The pain appears widely in various kinds of diseases in clinic. Thousands of patients with intense and unrelenting pain need effective and potent analgesic agents. So it is very important to use analgesic exactly to control pain effectively, cause it can make the patient release their pain, improve their life quality, at the same moment give them a comfort and extra confidence to fight with diseases.According to the mechanism of pharmacological effect, analgesic agents are generally divided into opioid analgesics, such as alkaloid morphine, and non-steroidal anti-inflammatory drugs (NSAID), like aspirin. The opioid analgesics have some side effects such as addiction or respiratory depression and the NSAID has side effects to damage gastrointestinal tract. So it is necessary to search for new effective and nontoxic analgesics in plant-derived secondary metabolites. The antinociceptive substances obtained includealkaloids, terpenoids and flavonoids recently.Caragana microphylla Lam., a plant of Caragana genus (Leguminosae family), is widely distributed in the North and West parts of China. Its roots and seeds have been used to heal swollen and painful throat in folk medicine. And it is also used by the native farmers to prevent sand erosion thus making it stationary.The main compounds in Caragana microphylla Lam. were reported as flavonoids, oligomeric stilbenes, triterpene and alkaloids, but the active components reflecting clinical effectiveness were still unknown. 75% ethanol extraction of the seeds, collected from Huhehaote City of Inner-Mongolia Autonomous Region, People's Republic of China, in July, 2004, was partitioned into five fractions as petroleum spirit, chloroform, acetic ether, n-butanol and water portion. Guided with initial pharmacological activities test on mice stretching model, petroleum and chloroform fractions were showed to have obvious analgesic action on reducing the times of mice writhing reaction caused by acetic acid.Twenty components were obtained from the chloroform fraction using column chromatography of silica gel, Sephadex LH-20, ODS and HPLC. Sixteen of them were identified on the basis of spectral analysis (UV, IR, EI-MS, FAB-MS, ^-NMR, 13C-NMR, 2D-NMR) and phytochemical properties, and we identified eighteen of them. Among them main components were flavonoids, triterpene and alkaloids. A new compound was elucidated and eleven compounds were isolated from Caragana microphylla Lam. for the first time. And we also identified twenty five compound of the petroleum fraction by GC-MS for the first time. The main compound of it is the linoleic acid (50.64%), oleic acid (17.43%) and palmitic acid (11.67%).The total alkaloids and the five alkaloids were essayed by the mice stretching model. We found that the total alkaloids and some alkaloids showed strong analgesia activity. And according to the traditional use, we also essayed the cytotoxicity activity of all the fractions and compounds in vitro and some compounds showed significant cytotoxicity activity. The results of the essay notified us that the seeds of Caragana microphylla Lam. may become the resource of antinociceptive and anticancer drugs.
Keywords/Search Tags:Antinociceptive
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