ANTIMALARIAL ACTIVITY OF ARTEMISIA-ANNUA FLAVONOIDS FROM WHOLE PLANTS AND CELL-CULTURES

ANTIMALARIAL ACTIVITY OF ARTEMISIA-ANNUA FLAVONOIDS FROM WHOLE PLANTS AND CELL-CULTURES
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DOI:
10.1007/bf00236389
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发表时间:
1992-11-01
期刊:
影响因子:
6.2
通讯作者:
PHILLIPSON, JD
PHILLIPSON, JD
中科院分区:
生物学2区
文献类型:
--
作者:
LIU, KCSC;YANG, SL;PHILLIPSON, JD

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黄花蒿细胞悬浮培养物在植物细胞培养液正己烷提取物和细胞氯仿提取物中均表现出体外抗恶性疟活性。微量的抗疟疾倍半萜内酯青蒿素可以解释正己烷部分的活性,但只有甲氧基黄酮类青蒿素、大黄素甲醚、大黄花酚-D和环烯醇才能解释氯仿提取物的活性。这些纯化的黄酮体外对恶性疟原虫的IC50值为2.4-6.5×10(-5)M,而纯化的青蒿素对恶性疟原虫的IC50值约为3×10(-8)M。在5×10~(-6)M浓度下,这些黄酮类化合物对恶性疟原虫无明显抑制作用,但对青蒿素的抗疟活性有明显的选择性增强作用。
Cell suspension cultures developed from Artemisia annua exhibited antimalarial activity against Plasmodium falciparum in vitro both in the n-hexane extract of the plant cell culture medium and in the chloroform extract of the cells. Trace amounts of the antimalarial sesquiterpene lactone artemisinin may account for the activity of the n-hexane fraction but only the methoxylated flavonoids artemetin, chrysoplenetin, chrysosplenol-D and cirsilineol can account for the activity of the chloroform extract. These purified flavonoids were found to have IC50 values at 2.4 - 6.5 x 10(-5)M against P. falciparum in vitro compared with an IC50 value of about 3 x 10(-8)M for purified artimisinin. At concentrations of 5 x 10(-6)M these flavonoids were not active against P. falciparum but did have a marked and selective potentiating effect on the antiplasmodial activity of artemisinin.