| In vivo: |
| J Pharm Pharmacol. 1998 Aug;50(8):949-54. | | A comparative study of the effects of sparteine, lupanine and lupin extract on the central nervous system of the mouse.[Pubmed: 9751462] | Lupin is toxic because of its alkaloid content, sparteine and lupanine in particular. Although the pharmacological properties of sparteine are well known those of lupanine have not been much studied.
METHODS AND RESULTS:
This paper reports procedures for extraction, purification and crystallization of lupanine, and methods for the preparation of an extract for injection of Lupinus mutabilis Sweet, and for the determination of the acute toxicity and maximum non-lethal dose (DL0) of lupanine, sparteine and lupin extract in the mouse. The three substances were tested on the central nervous system (CNS) for locomotor activity, for interaction with specific drugs used for treatment of the CNS (the stimulant drugs amphetamine and pentetrazol and the depressant drugs pentobarbital and chlorpromazine) and for analgesic activity.
CONCLUSIONS:
The results indicate that lupanine and lupin extract are less toxic than sparteine and that at the doses studied the three products have a weak sedative effect on the CNS. | | Molecules. 2015 Oct 20;20(10):19085-100. | | Lupanine Improves Glucose Homeostasis by Influencing KATP Channels and Insulin Gene Expression.[Pubmed: 26492234 ] | The glucose-lowering effects of lupin seeds involve the combined action of several components. The present study investigates the influence of one of the main quinolizidine alkaloids, Lupanine, on pancreatic beta cells and in an animal model of type-2 diabetes mellitus.
METHODS AND RESULTS:
In vitro studies were performed with insulin-secreting INS-1E cells or islets of C57BL/6 mice. In the in vivo experiments, hyperglycemia was induced in rats by injecting streptozotocin (65 mg/kg body weight). In the presence of 15 mmol/L glucose, insulin secretion was significantly elevated by 0.5 mmol/L Lupanine, whereas the alkaloid did not stimulate insulin release with lower glucose concentrations. In islets treated with l-arginine, the potentiating effect of Lupanine already occurred at 8 mmol/L glucose. Lupanine increased the expression of the Ins-1 gene. The potentiating effect on secretion was correlated to membrane depolarization and an increase in the frequency of Ca(2 ) action potentials. Determination of the current through ATP-dependent K⁺ channels (KATP channels) revealed that Lupanine directly inhibited the channel. The effect was dose-dependent but, even with a high Lupanine concentration of 1 mmol/L or after a prolonged exposure time (12 h), the KATP channel block was incomplete. Oral administration of Lupanine did not induce hypoglycemia. By contrast, Lupanine improved glycemic control in response to an oral glucose tolerance test in streptozotocin-diabetic rats.
CONCLUSIONS:
In summary, Lupanine acts as a positive modulator of insulin release obviously without a risk for hypoglycemic episodes. |
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