Active sesquiterpene lactones against Leishmania amazonensis and Leishmania braziliensis

被引：20
作者：
Sosa, Andrea M. [1 ]
Amaya, Susana [1 ,2 ]
Salamanca Capusiri, Efrain [3 ]
Gilabert, Miguel [1 ,4 ]
Bardon, Alicia [1 ,4 ]
Gimenez, Alberto [3 ]
Vera, Nancy R. [1 ]
Borkosky, Susana A. [1 ,2 ]
机构：
[1] Univ Nacl Tucuman, Fac Bioquim Quim & Farm, San Miguel De Tucuman, Argentina
[2] Univ Nacl Catamarca, Fac Ciencias Exactas & Nat, Catamarca, Argentina
[3] Univ Mayor San Andres, Inst Investi Farmaco Bioquim, La Paz, Bolivia
[4] Consejo Nacl Invest Cient & Tecn INQUINOA CONICET, Inst Quim Noroeste Argentino, San Miguel De Tucuman, Argentina
来源：
NATURAL PRODUCT RESEARCH | 2016年 / 30卷 / 22期
关键词：
Vernonieae; sesquiterpene lactones; antileishmanial activity; Leishmania amazonensis; Leishmania braziliensis; CYTOTOXICITY RELATIONSHIPS; ANTIPROTOZOAL ACTIVITY; LOG-P;
D O I：
10.1080/14786419.2015.1126260
中图分类号：
O69 [应用化学];
学科分类号：
081704 ;
摘要：
Seventeen sesquiterpene lactones (SLs) isolated from five species of the tribe Vernonieae were evaluated for their in vitro activity against promastigotes of Leishmania amazonensis and Leishmania braziliensis. Additionally, a quantitative structure activity relationship has been made, since all these natural compounds were found to have potent to mild antileishmanial properties. The most active compounds against L. braziliensis were 16 and 17 (IC50 values 1.45 and 1.34M, respectively), followed by compound 15 with IC50 value of 1.60M against L. amazonensis. The three glaucolide-type SLs (4-6) were the least active against both parasites. The computational study allowed us to establish that lipophilicity and polarisability play an important role in the antiparasitic activity. This is the first report of the known germacradiendiolides 16 and 17 from Elephantopus mollis. The activity data of the compounds 1-17 assayed against Leishmania parasites are reported here for the first time.
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页码：2611 / 2615
页数：5
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