gelsemine and gelsenicine

Gelsemium, a small genus of flowering plant from the family Loganiaceae, comprises five species including the popular Gelsemium sempervirens Ait. and Gelsemium elegans Benth., which are indigenous to North America and China/East Asia, respectively. Approximately 120 alkaloids have been isolated and identified from Gelsemium, with the predominant indole alkaloids including gelsemine, koumine, gelsemicine, gelsenicine, gelsedine, sempervirine, koumidine, koumicine and humantenine. Gelsemine is the principal active alkaloid in G. sempervirens Ait., and koumine and gelsemine are the most and second-most dominant alkaloids in G. elegans Benth. Gelsemium extract and its active alkaloids serve a variety of biological functions, including neurobiological, immunosuppressive and antitumor effects, and have traditionally been used to treat pain, neuralgia, anxiety, insomnia, asthma, respiratory ailments and cancers. This review focuses on animal-based studies of Gelsemium as a pain treatment and its mechanism of action. In contrast to morphine, when administered intrathecally and systemically, koumine, gelsemine and gelsenicine have marked antinociception in inflammatory, neuropathic and bone cancer pains without inducing antinociceptive tolerance. Gelsemium and its active alkaloids may produce antinociception by activating the spinal α3 glycine/allopregnanolone pathway. The results of this review support the clinical use of Gelsemium and suggest that its active alkaloids may be developed to treat intractable and other types of pain, preferably after chemical modification. However, Gelsemium is a known toxic plant, and its toxicity limits its appropriate dosage and clinical use. To avoid or decrease the side/toxic effects of Gelsemium, an individual monomer of highly potent alkaloids must be selected, or alkaloids that exhibit greater α3 glycine receptor selectivity may be discovered or modified.

Topics: Alkaloids; Analgesics; Animals; Gelsemium; Indole Alkaloids; Mice; Molecular Structure; Pain; Pregnanolone; Rats; Receptors, Glycine

Topics: Alkaloids; Chromatography, High Pressure Liquid; Gelsemium; Humans; Indole Alkaloids; Tandem Mass Spectrometry

To establish a LC-MS/MS method which is accurate and sensitive for determination of koumine, gelsemine, and gelsenicine in biological samples and to verify the method.. Strychnine was used as internal standard. Analytes in blood, urine and liver with 1% sodium hydroxide solution were extracted by ethyl acetate. Chromatographic separation was achieved on a ZORBAX SB-C₁₈ column （150 mm×2.1 mm, 5 μm）, and gradient elution was performed with the buffer solution of methanol-20 mmol/L ammonium acetate （including 0.1% formic acid and 5% acetonitrile） as mobile phase. Qualitative and quantitative analysis was performed in the multiple reaction monitoring mode coupled with an electrospray ionization source under positive ion mode（ESI⁺）.. The method is selective, sensitive and suitable for simultaneous determination of koumine, gelsemine and gelsenicine in body fluids and tissues, which offering technical support for clinical diagnosis and treatment and forensic toxicological analysis of

Topics: Alkaloids; Chromatography, High Pressure Liquid; Chromatography, Liquid; Forensic Toxicology; Formates; Humans; Indole Alkaloids; Liver; Reproducibility of Results; Strychnine; Tandem Mass Spectrometry

To investigate the effects of alkaloid monomers from Gelsemium elegans on proliferation of HepG2 cell in vitro and the possible mechanism.. MTT assay was used to measure the inhibitory of three alkaloid monomers on HepG2 cell in vitro. The most effective fraction was chosen to test whether the effect was in time-and dose-dependent manner. The morphological changes were observed by the light microscope and the cell cycle alteration through the flow cytometric assay. The activity of Caspase-3, Caspase-8 and Caspase-9 were detected by a Caspases colorimetric assay kit.. The results showed that koumine, Gelsemine and Gelsenicine could significantly inhibit the proliferation of HepG2 cell and Gelsenicine, the most effective fraction, was clearly in dose- and time-dependent manners, while exhibited low cytotoxicity to the Vero cell. The cell treated with Gelsenicine for 48 h showed distinctive morphological changes. The cells treated with 200 and 400 microg/mL shrinked and fell off from the bottom. At the same time, the cells were arrested at S phase and the apoptosis increased apparently. The activity of Caspase-3, Caspase-8 and Caspase-9 was increased in a dose-dependent manner.. Three alkaloid monomers from Gelsemium elegans, especially Gelsenicine, could inhibit proliferation of HepG2 cell obviously. The mechanism may be related to cell cycle arrest and activation of Caspase-3, Caspase 8 and Caspase-9.

Topics: Alkaloids; Antineoplastic Agents, Phytogenic; Apoptosis; Carcinoma, Hepatocellular; Caspases; Cell Cycle; Cell Proliferation; Dose-Response Relationship, Drug; Flow Cytometry; Hep G2 Cells; Humans; Indole Alkaloids; Liver Neoplasms; Loganiaceae; Time Factors