Question
Asked 16 July 2014

Do you know of any research on helleborus pharmacological properties for mental disorders?

Several ancient authors (i.e. Hippocrates, Dioscorides etc) describe the use of Helleborus for mental disorders, but I couldn't find any current research explaining it. Searching for Helloborus I read that helleborine may be a compuond with narcotic and sedative effect. Has anyone have any reference about that?

Most recent answer

Dear Dr. Brückner
thank you very much for your recommendation. Yes, this manuscript was published in Journal of the History of Neurosciences 2017, 26, 193-215. You can find it here and at my researchgate.net account:
thank you for the citations and the article recommendation...
Sincerely yours
Andreas J. Kesel
Pharmacist

All Answers (8)

in my archive there is the first isolation of hellebrin described by Walter Karrer in 1943. There he gave a German reference dealing with the use of Helleborus niger for treating mental disorders: H. Fischer, Helleborus im Altertum und bei Paracelsus, Schweizerische medizinische Wochenschrift 1936, 66, 484. To my best knowledge there is no reference available for explaining possible effects of helleborus on mental disorders. However, the bufadienolides of Helleborus niger are cytotoxic against normal cells and cancer cells. Maybe this could be an explanation by assuming that helleborus bufadienolides inhibit cell division. I have attached the original paper of Karrer from 1943, the paper on the structure confirmation of hellebrin in 1995, and a paper describing the antimitotic action of hellebrin and hellebrigenin.
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Hi Ali & Francesco
wheanwhile I also found some new aspects regarding the psychopharmacological effects of Helleborus species. Certain cardiac glycosides, the bufadienolides, are obviously known to occasionally act strongly sedative, for example daigremontianin and bersaldegenin 1,3,5-orthoacetate from Kalanchoe daigremontiana (kindly see attached papers from Prof. em. Dr. Hildebert Wagner). These sedative CNS effects may be mediated by the neurosteroid allosteric binding site of GABAA receptors (GABA = gamma-aminobutyric acid), but I found no reference for this hypothesis. Maybe hellebrin enhances GABA action in brain by acting as positive allosteric modulator at GABAA receptors. Also attached is an article dealing with Helleborus species biology in general.
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Francesco Saettini
Università degli Studi di Milano-Bicocca
Andreas and Ali
thank you so much for your help. I can finally imagine why Helleborus was so used in the past for mental disorders. I have another question though:
In Duke, James A. (1992)  "Handbook of Phytochemical Constituents of GRAS Herbs and other Economic Plants (Boca Raton, FL, CRC Press) " I read
"Helleborin is a potent narcotic "
while in Maior et al. Helleborin is not mentioned whereas "(anemonin and protoanemonin) have a sedative effect"
Do you have any idea why?
Dear Francesco
"helleborin" is a complex steroid saponin mixture from Helleborus roots (kindly see attached paper from 2014) now called hellebosaponins. Previously I thought helleborin is an old name for hellebrin, the principal cardiac glycoside from Helleborus species. But the name interchange is widely in use because of existing confusion in old literature. Nowadays hellebrin stands for the cardiac glycoside, and helleborin for the complex hellebosaponin steroid saponin mixture.
Protoanemonin/anemonin are widely distributed in the plant family Ranunculaceae, and are of chemotaxonomic value for defining affiliation to Ranunculaceae. They can be found also in Ranunculus acris, and are known to act sedative.
1 Recommendation
Francesco Saettini
Università degli Studi di Milano-Bicocca
Hello everybody
even though it's not strictly pertinent, this is the first part of the research me and Andreas started from this discussion.
Hope you find interesting
Francesco
Dear Dr. Brückner
thank you very much for your recommendation. Yes, this manuscript was published in Journal of the History of Neurosciences 2017, 26, 193-215. You can find it here and at my researchgate.net account:
thank you for the citations and the article recommendation...
Sincerely yours
Andreas J. Kesel
Pharmacist

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