Sampangine antifungal activity

In vitro antifungal activities evaluation for sampangine metabolites demonstrated comparable activities to sampangine. However, an in vivo efficacy study revealed that SAh 2 is inactive. The antifungal activity profile of sampangine metabolites led us to conclude that metabolism per se is not the cause for the in vivo inactivity of sampangine, hence, further studies on the other pharmacokinetic parameters (bioavailability, distribution, clearance, etc.) will be necessary. 

Table 1 summarizes the antifungal/antimycobacterial activities of sampangine analogs. 

Table 1. In vitro Antifungal and Antimycobacterial Activities of Sampangines...

ATCC 23068. Antifungal/antimycobacterial activity of the sampangines was enhanced by the presence of a 3-methoxy-, 3-methyl- or 4,5-benzo- group relative to that of sampangine. However, the presence of a 4-halo-, 4-alkoxy-, or 4-amino- substituent reduced the antifungal/antimycobacterial activity relative to that of sampangine. 

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