Berberine derivatives as antileishmanial drugs.
Berberine, a quaternary alkaloid, and several of its derivatives were tested for efficacy against Leishmania donovani and Leishmania braziliensis panamensis in golden hamsters. Tetrahydroberberine was less toxic and more potent than berberine against L. donovani but was not as potent as meglumine antimonate (Glucantime), a standard drug for the treatment of leishmaniasis. Only berberine and 8-cyanodihydroberberine showed significant activity (greater than 50% suppression of lesion size) against L. braziliensis panamensis.
Vennerstrom
J L
JL
Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Washington, D.C. 20307.
Lovelace
J K
JK
Waits
V B
VB
Hanson
W L
WL
Klayman
D L
DL
D000818:Animals; D000981:Antiprotozoal Agents; D001599:Berberine / Q000031:analogs & derivatives / Q000494:pharmacology / Q000627:therapeutic use*; D001600:Berberine Alkaloids / Q000627:therapeutic use*; D001835:Body Weight; D006224:Cricetinae; D007896:Leishmaniasis / Q000188:drug therapy* / Q000469:parasitology; D007897:Leishmaniasis, Mucocutaneous / Q000188:drug therapy / Q000469:parasitology / Q000473:pathology; D007898:Leishmaniasis, Visceral / Q000188:drug therapy / Q000469:parasitology / Q000473:pathology; D008099:Liver / Q000469:parasitology; D008536:Meglumine / Q000627:therapeutic use; D000077485:Meglumine Antimoniate; D008647:Mesocricetus; D009942:Organometallic Compounds / Q000627:therapeutic use; D012867:Skin / Q000473:pathology
D000981:Antiprotozoal Agents; D001600:Berberine Alkaloids; D009942:Organometallic Compounds; D001599:Berberine; D008536:Meglumine; D000077485:Meglumine Antimoniate