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Background   Zanthoxylum zanthoxyloides  and  Z. leprieurii  fruits are commonly used in traditional system of medicine for diarrhea, pain, wound healing, etc. in Cameroon, Africa.  Z. leprieurii  fruits have been chemically studied for its bioactive compounds whereas the investigation on  Z. zanthoxyloides  fruits is lacking.    Results  After a detailed chemical analysis of the fruits of  Z. leprieurii  and  Z. zanthoxyloides , a series of new acridone alkaloids, namely, 3-hydroxy-1,5,6-trimethoxy-9-acridone ( 1 ), 1,6-dihydroxy-3-methoxy-9-acridone ( 2 ), 3,4,5,7-tetrahydroxy-1-methoxy-10-methyl-9-acridone ( 3 ), 4-methoxyzanthacridone ( 8 ), 4-hydroxyzanthacridone ( 9 ), 4-hydroxyzanthacridone oxide (2,4’) ( 10 ) have been isolated. The known acridones which have been characterized are, helebelicine A ( 4 ), 1-hydroxy-3-methoxy-10-methyl-9-acridone ( 5 ) ,  1,3-dihydroxy-4-methoxy-10-methyl-9-acridone ( 6 ) and tegerrardin A ( 7 ). The i n vitro  antibacterial and cytotoxic screening of these acridones reveal that compound  3  has a moderate antibacterial activity (MIC 125 μg/mL) against  Micrococcus luteus  and  Pseudomonas aeruginosa  while compound  1  shows a moderate cytotoxic effect (IC 50  of 86 μM) against WRL-68 (liver cancer cell line). Furthermore, the molecular modeling of these acridones predicted the structural basis for their mode of action and binding affinity for aromatase, quinone reductase and WAAG, a glycosyltransferase involved in bacterial lipopolysaccharide synthesis. Computational approaches, quantitative SAR and modeling studies predicted that acridones  1, 2, 3, 4, 9  and  10  were the inhibitors of glycosyltransferase while  1 ,  8, 9  and  10,  the inhibitors of aromatase.    Conclusions  A total of 10 acridones have been isolated out of which 6 are new ( 1 ,  2 ,  3 ,  8 ,  9  and  10 ). Alkaloids  8 ,  9  and  10 , having novel tetracyclic acridone structure with new carbon skeleton, have now been named as zanthacridone. The quantitative SAR and molecular modeling studies suggested that the compounds  1 ,  9  and  10  are inhibitors of both aromatase and glycosyltransferase.

Aromatase and glycosyl transferase inhibiting acridone alkaloids from fruits of Cameroonian Zanthoxylumspecies