Gelsemine
Gelsemine is a highly toxic compound and may be a glycine receptor agonist. Gelsemine has antitumor, anti-hyperlipidemic,anti-oxidative activities,it also has marked antinociception in inflammatory, neuropathic and bone cancer pains without inducing antinociceptive tolerance.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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J Asian Nat Prod Res. 2010 Sep;12(9):731-9.
Antitumor activity of two gelsemine metabolites in rat liver microsomes.[Pubmed:
20839118]
Gelsemine is one of the major alkaloids from Gelsemium elegans Benth., which has been used as an antitumor remedy in clinic.
METHODS AND RESULTS:
In this paper, metabolism of Gelsemine has been investigated in vitro in phenobarbital-treated rat liver microsomes. The metabolites of Gelsemine were separated and evaluated using the flash silica gel column, preparative HPLC, using NMR and MS methods. According to the spectral data, two metabolites, M1 and M2, were identified as 4-N-demethylGelsemine and 21-oxoGelsemine, respectively. By the MTT method in vitro, the antitumor activities between Gelsemine and its metabolites were compared in the HepG2 and HeLa cell lines. Moreover, the main metabolic pathway was further proposed.
Cell Biochem Biophys. 2015 Jan;71(1):337-44.
Anti-hyperlipidemic and anti-oxidative effects of gelsemine in high-fat-diet-fed rabbits.[Pubmed:
25213292]
The present study investigated the anti-hyperlipidemic proprieties of a natural alkaloid, Gelsemine, in a high-fat-fed rabbit model.
METHODS AND RESULTS:
Animals were randomly divided into five groups and fed normal diet, hypercholesterolemic diet (1% cholesterol), or hypercholesterolemic diet (1% cholesterol) supplemented with Gelsemine (1, 5, or 25 mg/kg). After 60 days, serum concentrations of total cholesterol (TC), LDL-C, HDL-C, triglycerides, apolipoproteins A and B, SGOT, SGPT, glucose, and insulin were measured in all experimental groups. Hypercholesterolemic diet resulted in significantly elevated levels of TC, TG, LDL-C, SGOT, and SGPT, and reduced HDL-C compared to the normocholesterolemic diet group. Gelsemine treatment significantly improved lipid profile parameters, affected by hyperlipidemia, while having no effect on the levels of apolipoproteins, glucose, and insulin. Furthermore, Gelsemine treatment decreased hyperlipidemia-induced oxidative stress in a dose-dependent manner, as indicated by the increased activity of superoxide dismutase and catalase, and reduction in serum nitric oxide, and malondialdehyde concentrations in hyperlipidemic animals that received Gelsemine supplementation.
CONCLUSIONS:
Dietary supplementation with Gelsemine may, therefore, reverse the effect of the lipogenic diet on lipid profile and hepatic enzymes in hyperlipidemic rabbits, and protect tissues from oxidative stress, caused by high-fat diet.
Org Lett. 2008 Nov 6;10(21):4747-50.
A concise approach to a gelsemine core structure using an oxygen to carbon bridge swapping strategy.[Pubmed:
18837555]
A tricyclic core structure 2 related to Gelsemine 1 was synthesized from an oxabicyclo[3.2.1]octanone 4 by a three-step bridge swapping strategy involving elimination of the bridging ether oxygen and intramolecular Michael addition of a tethered cyanoacetamide unit.
