Lee K H, Tani S, Imakura Y
Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill 27514.
J Nat Prod. 1987 Sep-Oct;50(5):847-51. doi: 10.1021/np50053a012.
The quassinoids bruceoside-A [1], brusatol [2], and bruceolide [3] were tested for antimalarial activity in vitro against the chloroquine-resistant (Smith) isolates of Plasmodium falciparum. Compound 2 was quite active, 1 was not active, and 3 showed only a trace of activity. The fact that 15 [(E)-non-2-enoyl] bruceolide [7] synthesized from 2 was eight times less active than 2 would indicate that the requirement of a C-15 ester moiety for enhanced antimalarial activity among brusatol related quassinoids could be quite specific.
测试了苦木素类化合物布鲁斯苷 -A [1]、鸦胆子醇 [2] 和布鲁斯内酯 [3] 对恶性疟原虫氯喹抗性（史密斯株）分离株的体外抗疟活性。化合物2活性相当高，1无活性，3仅显示出微量活性。由2合成的15 -[(E)-壬-2-烯酰基]布鲁斯内酯 [7] 的活性比2低八倍，这一事实表明，在与鸦胆子醇相关的苦木素类化合物中，增强抗疟活性对C-15酯部分的要求可能相当特殊。
