Study of the interaction of antiplasmodial strychnine derivatives with the glycine receptor

Abstract

Strychnos icaja and differing from strychnine only by a cycle opening, were compared in the same way. The weak interaction of protostrychnine confirms the importance of the G cycle ring structure in strychnine for its binding to the glycine receptor and its antagonist properties.

In vitro antiprotozoal, antimicrobial and antitumor activity of Pavetta crassipes K. Schum leaf extracts

“…The indolomonoterpenic alkaloids, elaeocarpidin and hydroxy-elaeocarpidin, have been reported to be present in the leaves of Pavetta crassipes (Sanon et al, 2005). The potential of indolomonoterpenic alkaloids as effective compounds for the treatment of malaria, bacterial infections and cancer have previously been described (Frédérich et al, 2003;Philippe et al, 2006Philippe et al, , 2007Balde et al, 2010). The National Cancer Institute's (NCI) recommends that a compound have an IC 50 value lower than 30 g/ml to be considered for any preliminary study (Jokhadze et al, 2007).…”

In Vivo Antimalarial Activity of Isosungucine, an Indolomonoterpenic Alkaloid from Strychnos icaja

“…Chloroquine diphosphate (97 %, Sigma C6628; Bornem, Belgium), was used as antimalarial reference. Isosungucine (1) was isolated from Strychnos icaja as previously described [11] and its purity was assessed by HPLC (> 95 %). Stock solutions (1 mM) were prepared with 5 % DMSO (final concentration for in vitro assays maximum 0.5 %).…”

“…Compound 1 exhibited 7-35-fold higher activity against P. falciparum strains compared with human cancer cell lines (depending on Plasmodium strains and human cell lines), thus indicating selectivity [10]. Very recently, it was shown that the bisindole alkaloids from S. icaja possessing antiplasmodial properties were practically devoid of strychnine-like activity in vitro [11]. The objective of the present investigation was to demonstrate the in vivo antimalarial activity of isosungucine (1, Fig.…”

Assessment of the in vitro and in vivo genotoxicity of extracts and indole monoterpene alkaloid from the roots of Galianthe thalictroides (Rubiaceae)

“…b Including rare flr 3 single spots; c Considering mwh clones from mwh single and twin spots. According to the literature, indole monoterpene alkaloids have potential for the treatment of malaria, infectious diseases and cancer (Frédérich et al, 2003;Philippe et al, 2006Philippe et al, , 2007. So, this is the first study assessing the genotoxic activity of extracts and secondary metabolites isolated from G. thalicthroides.…”