Intersci Conf Antimicrob Agents Chemother. 1998 Sep 24-27;38:281 (abstract no. F-188). Unique Identifier : AIDSLINE AIDS/20710752
McDevitt JT; Schneider DM; Katiyar SK; Edlind TD; MEDEX, PRM Pharmaceuticals, Philadelphia, PA.
Abstract: Berberine is a quaternary plant alkaloid in development for the treatment of chronic diarrhea in AIDS patients. Berberine has both antisecretory and antimicrobial properties and has been used to successfully treat a variety of gastrointestinal conditions caused by bacteria or protozoa. No currently available drug is completely effective against microsporidia or cryptosporidia, the intracellular protozoa whose presence in the GI tract often correlates with AIDS related diarrhea. Previously, we reported that berberine showed in vitro efficacy against the microsporidium E. intestinalis (IC50 =5.5micrograms/ml). We are now investigating the antimicrobial profile of berberine in combination with albendazole, another drug which has been examined as an antimicrosporidial agent. E. intestinalis was isolated from the urine of AIDS patients and passaged in supplemented MEM media to maintain a high rate of spore infectivity. African Green Monkey kidney (Vero) cells were exposed to E. intestinalis spores (3-4/cell) and then the compounds to be tested were added. In this system, a suboptimal concentration of berberine (3 micrograms/ml) reduced spore production on average by -5% relative to control. Albendazole alone, at the suboptimal concentration of 3ng/ml, produced a similar result. At these same suboptimal concentrations, berberine in combination with albendazole was more than twice as effective as either drug alone; reducing growth by -0-70%. Although both drugs are generally well tolerated, neutropenia and liver function abnormalities have been associated with albendazole administration. Co-administration of berberine with albendazole may optimize the antimicrobial efficacy of both drugs while allowing a reduction in dose.
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