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Coli ATCC 10536. Streptomycin was used as a positive control. Sampangine was only marginally to moderately active against S. aureus and inactive against P. aeruginosa and E. coli. Both SAMM2 and SAM MMl had no antibacterial activities. Table 5 illustrates these results. In conclusion, antifungal/antibacterial activities evaluation revealed that, sampangine metabolites have remarkable in vitro antifungal activities, whereas SAMM2 is inactive in vivo in the mouse model of cryptococcosis. This 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.
Single Crystal X-ray Analysis Single crystal X-ray analysis is considered the ultimate structure proof, particularly for the absolute stereochemistries of the sugar moiety. For this technique to be successful SAMM2, or a suitable derivative must be obtained in a suitable crystalline form. Attempted Crystallization ofSAMMl: A variety of solvents were used and afforded only solid powder. The uncrystallizability of SAMM2 was attributed to its instability, which was evident (by TLC) during these attempts.
Also it could be used to explore unanswered questions in mammalian metabolism. For example, microbial studies may reveal a previously undetected mammalian metabolite, elucidate the previously unexplored stereochemical disposition of the xenobiotic in mammalian systems, or be used to study mechanistic aspects concerning the formation of the metabolites. The Parallel Approach: This approach involves the simultaneous study of biotransformations in mammalian and microbial species. Most studies to date have been retrospective, but the trend is to make such studies more prospective.
Bioactive natural Products (Part D) by Atta-ur-Rahman