Synthesis and Pharmacological Activity of Alkaloids from Embryo of Lotus, <i>Nelumbo nucifera</i>

Abstract

Bisbenzylisoquinoline alkaloid, nelumboferine which was recently isolated from the embryo of Nelumbo nucifera, and stereoisomers of neferine, which is a major alkaloid of the embryo of N. nucifera, were stereo selectively synthesized. Pharmacological activity of nelumboferine, stereoisomers of neferine, liensinine, iso liensinine, and Omethylneferine were evaluated.

Serotonergic mechanisms are involved in antidepressant-like effects of bisbenzylisoquinolines liensinine and its analogs isolated from the embryo of Nelumbo nucifera Gaertner seeds in mice

“…Liensinine showed significant antidepressant effects at lower doses than those of isoliensinine and neferine. Our previous report demonstrated that liensinine and isoliensinine decreased locomotor activity over 30 min but did not increase general activity [11]. Therefore, it is unlikely that liensinine and isoliensinine elicit anti‐immobility effects by enhancing locomotor activity.…”

“…Figure shows the effects of liensinine, isoliensinine, neferine and imipramine on the time of immobility of mice. Anti‐immobility effects of liensinine, isoliensinine and neferine were examined 30 min after administration based on previous studies on its sedative effects and anxiolytic effects of neferine [7,11]. Liensinine elicited apparent antidepressant‐like effects at 10, 25 and 50 mg/kg.…”

“…Isoliensinine has been shown to inhibit bleomycin‐induced pulmonary fibrosis in mice [10]. Recently, we found that liensinine and isoliensinine reduce locomotor activity (i.e., have sedative effects) in mice [11]. These results raise the possibility that liensinine and isoliensinine may have antidepressant effects similar to those of neferine.…”

“…We reported that the other alkaloids from the embryos of the seeds of Nelumbo nucifera Gaertner liensinine and isoliensinine have sedative effects in mice [11]. However, it was not clear whether liensinine and isoliensinine are effective against depression.…”

In vitro characterization of ABC transporters involved in the absorption and distribution of liensinine and its analogs

“…However, evidence of P-gp-facilitated neferine transport has not been shown in cell models. To our knowledge, researchers have focused on the synthesis and metabolism of isoliensinine (Zhou et al, 2012;Nishimura et al, 2013), but the interaction between isoliensinine and ABC transporters remains unclear. This prompted us to investigate and identify the relevant ABC transporters involved in regulation of the cellular levels of liensinine and its analogs.…”