Corynantheine
Corynantheine shows pronounced activity against Leishmania major promastigotes
(IC50 at the micromolar level) but no significant in vitro antiplasmodial activity (against chloroquinesensitive Plasmodium falciparum).
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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Planta Medica, 2014 , 66 (6) :531-6.
Leishmanicidal, Antiplasmodial and Cytotoxic Activity of Indole Alkaloids from Corynanthe pachyceras[Reference:
WebLink]
METHODS AND RESULTS:
Five indole alkaloids, corynantheidine, Corynantheine, dihydroCorynantheine, -yohimbine and corynanthine were isolated from bark of Corynanthe pachyceras K. Schum. (Rubiaceae). The structures were established by spectroscopic methods, inlcuding previously unreported assignment of all 1 HNMR resonances by COSY and NOESY experiments. These and related alkaloids showed pronounced activity against Leishmania major promastigotes (IC50 at the micromolar level) but no significant in vitro antiplasmodial activity (against chloroquinesensitive Plasmodium falciparum).
CONCLUSIONS:
Cytotoxicity assessed with drug sensitive KB-3-1 and multidrug-resistant KB-V1 cell lines was low; the alkaloids are apparently not substrates for the Pglycoprotein (P-170) efflux pump.
J Org Chem. 2001 Apr 6;66(7):2217-21.
Conformational analysis of indole alkaloids corynantheine and dihydrocorynantheine by dynamic 1H NMR spectroscopy and computational methods: steric effects of ethyl vs vinyl group.[Pubmed:
11281758]
METHODS AND RESULTS:
1H NMR (400 MHz) spectra of the indole alkaloid dihydroCorynantheine recorded at room temperature show the presence of two conformers near coalescence.In contrast to dihydroCorynantheine, the corresponding rotamers of Corynantheine are in the fast exchange limit at room temperature. The activation parameters determined for Corynantheine were DeltaH(double dagger) = 60 +/- 6 kJ/mol and DeltaS(double dagger) = 24 +/- 6 J/mol.K, with DeltaG degrees = 1.3 kJ/mol at -45 degrees C. The difference in the exchange rates of the rotamers of Corynantheine and dihydroCorynantheine (respectively, 350 s(-1) and 9 s(-1) at 0 degrees C) reflects the difference in the steric bulk of the vinyl and the ethyl group.
CONCLUSIONS:
The conformational equilibria involving the side chain rotation as well as inversion of the bridgehead nitrogen in Corynantheine and dihydroCorynantheine was studied by force-field (Amber and MMFF) and ab initio (density-functional theory at the B3LYP/6-31G level) computational methods, the results of which were in good agreement with the 1H NMR data.
