Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Molecules. 2013 Sep 2;18(9):10599-608. doi: 10.3390/molecules180910599.
Five xanthone derivatives and one flavanol were isolated from the dichloromethane extract of Garcinia mangostana. Dichloromethane, ethyl acetate extract and the major xanthone (α-mangostin) were evaluated in vitro against erythrocytic schizonts of Plasmodium falciparum, intracellular amastigotes of Leishmania infantum and Trypanosoma cruzi and free trypomastigotes of T. brucei. The major constituent α-mangostin was also checked for antimicrobial potential against Candida albicans, Escherichia coli, Pseudomonas aeruginosa, Bacillius subtilis, Staphylococcus aureus, Mycobacterium smegmatis, M. cheleneoi, M. xenopi and M. intracellulare. Activity against P. falciparum (IC₅₀ 2.7 μg/mL) and T. brucei (IC₅₀ 0.5 μg/mL) were observed for the dichloromethane extract, however, with only moderate selectivity was seen based on a parallel cytotoxicity evaluation on MRC-5 cells (IC₅₀ 9.4 μg/mL). The ethyl acetate extract was inactive (IC₅₀ > 30 µg/mL). The major constituent α-mangostin showed rather high cytotoxicity (IC₅₀ 7.5 µM) and a broad but non-selective antiprotozoal and antimicrobial activity profile. This in vitro study endorses that the antiprotozoal and antimicrobial potential of prenylated xanthones is non-conclusive in view of the low level of selectivity.
从藤黄科植物藤黄中分离得到五种酮衍生物和一种黄烷醇。评估了二氯甲烷提取物、乙酸乙酯提取物和主要的酮（α-倒捻子素）对恶性疟原虫红内期裂殖体、婴儿利什曼原虫和克氏锥虫游离滋养体的体外活性。主要成分α-倒捻子素也被检查了对白色念珠菌、大肠杆菌、铜绿假单胞菌、枯草芽孢杆菌、金黄色葡萄球菌、耻垢分枝杆菌、胞内分枝杆菌、偶发分枝杆菌和胞内分枝杆菌的抗菌潜力。二氯甲烷提取物对恶性疟原虫（IC₅₀ 2.7 μg/mL）和克氏锥虫（IC₅₀ 0.5 μg/mL）具有活性，但基于对 MRC-5 细胞的平行细胞毒性评估，仅观察到中等选择性（IC₅₀ 9.4 μg/mL）。乙酸乙酯提取物无活性（IC₅₀ > 30 µg/mL）。主要成分α-倒捻子素表现出相当高的细胞毒性（IC₅₀ 7.5 µM），具有广泛但非选择性的抗原生动物和抗菌活性谱。这项体外研究表明，鉴于低选择性，芳基化黄烷酮的抗寄生虫和抗菌潜力尚无定论。
