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Libiguins A and B: Novel Phragmalin Limonoids Isolated from Neobeguea mahafalensis Causing Profound Enhancement of Sexual Activity
Uppsala universitet, Medicinska och farmaceutiska vetenskapsområdet, Farmaceutiska fakulteten, Institutionen för farmaceutisk biovetenskap.
Uppsala universitet, Medicinska och farmaceutiska vetenskapsområdet, Farmaceutiska fakulteten, Institutionen för farmaceutisk biovetenskap.
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2014 (Engelska)Ingår i: Planta Medica, ISSN 0032-0943, E-ISSN 1439-0221, Vol. 80, nr 4, s. 306-314Artikel i tidskrift (Refereegranskat) Published
Abstract [en]

In a screening programme directed towards the discovery of drugs that could enhance sexual activity, we found that a decoction of the root bark of Neobeguea mahafalensis displayed an extraordinarily high potency and remarkably long duration in augmenting sexual activity in male rodents. Bioassay-guided fractionation led to the isolation of two pharmacoactive constituents, which turned out to be novel 1,8,9-orthoacetate phragmalin limonoids that we named libiguins A and B, each with a C-16/30 -lactone ring. Chemical structures were established by the interpretation of their 1D and 2DNMR data. In vivo pharmacological tests showed that starting with a treatment from 0.004-0.4mg/kg/day for three consecutive days, over a 3-h sampling period, these limonoids induced a long-lasting augmentation of frequency and sustainment of mounting behaviour in male rodents, with an effect lasting for up to 11 days post-treatment. Libiguin A proved to be markedly more potent than libiguin B. This report is the first of limonoids having such an effect, and the findings could lead to novel therapies for the treatment of sexual dysfunction. Moreover, the results can serve as an opening to elucidate the central physiological control of mating behaviour, which is still not well mapped out.

Ort, förlag, år, upplaga, sidor
2014. Vol. 80, nr 4, s. 306-314
Nyckelord [en]
Neobeguea mahafalensis, Meliaceae, limonoids, libiguin, sexual enhancing activity
Nationell ämneskategori
Farmakologi och toxikologi Läkemedelskemi
Identifikatorer
URN: urn:nbn:se:uu:diva-227939DOI: 10.1055/s-0033-1360390ISI: 000332395000009OAI: oai:DiVA.org:uu-227939DiVA, id: diva2:733009
Tillgänglig från: 2014-07-07 Skapad: 2014-07-02 Senast uppdaterad: 2018-01-11Bibliografiskt granskad

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Yahorava, SviatlanaYahorau, AlehWikberg, Jarl E. S.

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