Portet Bénédicte, Fabre Nicolas, Roumy Vincent, Gornitzka Heinz, Bourdy Geneviève, Chevalley Séverine, Sauvain Michel, Valentin Alexis, Moulis Claude
UMR 152, IRD - Université Paul Sabatier Toulouse 3, Faculté des Sciences Pharmaceutiques, 31062 Toulouse Cedex 09, France.
Phytochemistry. 2007 May;68(9):1312-20. doi: 10.1016/j.phytochem.2007.02.006. Epub 2007 Mar 29.
The bioassay-guided purification of an n-hexane extract from the leaves of Piper hostmannianum var. berbicense led to the isolation of four monoterpene or prenyl-substituted dihydrochalcones (1a, 1b, 2, 3) as well as the known compounds 2',6'-dihydroxy-4'-methoxydihydrochalcone (4), linderatone (5), strobopinin (6), adunctin E (7) and (-)-methyllinderatin (8). Their structures were established on the basis of NMR and X-ray analysis. (-)-Methyllinderatin, linderatone and 2',6'-dihydroxy-4'-methoxydihydrochalcone exhibited the most potent antiplasmodial activity with IC50 values of 5.64, 10.33 and 12.69 microM, respectively against both chloroquine-sensitive and resistant strains of Plasmodium falciparum (F32,FcB1). The activity of (-)-methyllinderatin was confirmed in vivo against Plasmodium vinckei petteri in mice (80% of reduction of parasitemia) at a dose of 20 mg/kg/day.
对胡椒属植物霍氏胡椒变种（Piper hostmannianum var. berbicense）叶片的正己烷提取物进行生物测定导向的纯化，得到了四种单萜或异戊烯基取代的二氢查耳酮（1a、1b、2、3）以及已知化合物2',6'-二羟基-4'-甲氧基二氢查耳酮（4）、乌药酮（5）、紫茎女贞素（6）、附加素E（7）和（-）-甲基乌药素（8）。它们的结构通过核磁共振和X射线分析得以确定。（-）-甲基乌药素、乌药酮和2',6'-二羟基-4'-甲氧基二氢查耳酮表现出最强的抗疟活性，对恶性疟原虫（F32、FcB1）的氯喹敏感株和耐药株的IC50值分别为5.64、10.33和12.69微摩尔。（-）-甲基乌药素在体内对小鼠文氏疟原虫彼得氏亚种的活性得到证实（在剂量为20毫克/千克/天时，寄生虫血症降低80%）。
