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从毒鼠树和垂花螺旋籽中分离得到的两种双苄基异喹啉对映体生物碱的体外抗疟活性及氯喹增效作用

In vitro antimalarial activity and chloroquine potentiating action of two bisbenzylisoquinoline enantiomer alkaloids isolated from Strychnopsis thouarsii and Spirospermum penduliflorum.

作者信息

Ratsimamanga-Urverg S, Rasoanaivo P, Ramiaramanana L, Milijaona R, Rafatro H, Verdier F, Rakoto-Ratsimamanga A, Le Bras J

机构信息

Institut Malgache de Recherches Appliquees, Antananarivo, Madagascar.

出版信息

Planta Med. 1992 Dec;58(6):540-3. doi: 10.1055/s-2006-961545.

DOI:10.1055/s-2006-961545
PMID:1484894
Abstract

The bisbenzylisoquinolines 7-O-demethyltetrandrine and limacine, respectively, isolated from Strychnopsis thouarsii Baill. and Spirospermum penduliflorum Thou. were evaluated for their intrinsic antimalarial activity in vitro and chloroquine potentiating action against the chloroquine-resistant Plasmodium falciparum FCM 29 originating from Cameroon. They both showed significant antiplasmodial potency in vitro with very similar IC50 values of respectively, 740 nM and 789 nM (IC50 = 214 nM for chloroquine used as standard drug), which demonstrated that the stereochemistry of the C-1 and C-1' configuration likely plays a role in the chloroquine potentiating effect of these drugs. If confirmed in vivo, these results may account for the traditional use of the two plants as antimalarials and adjuvant to chloroquine in Madagascan folklore remedies.

摘要

分别从毒鼠树(Strychnopsis thouarsii Baill.)和垂花螺旋籽(Spirospermum penduliflorum Thou.)中分离得到的双苄基异喹啉类化合物7-O-去甲基粉防己碱和轮环藤宁,对其体外抗疟活性以及对源自喀麦隆的氯喹抗性恶性疟原虫FCM 29的氯喹增效作用进行了评估。它们在体外均显示出显著的抗疟效力,IC50值非常相似,分别为740 nM和789 nM(用作标准药物的氯喹的IC50 = 214 nM),这表明C-1和C-1'构型的立体化学可能在这些药物的氯喹增效作用中发挥作用。如果在体内得到证实,这些结果可能解释了这两种植物在马达加斯加民间疗法中作为抗疟药和氯喹佐剂的传统用途。

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Bisbenzylisoquinolines as modulators of chloroquine resistance in Plasmodium falciparum and multidrug resistance in tumor cells.双苄基异喹啉作为恶性疟原虫氯喹抗性和肿瘤细胞多药抗性的调节剂。
Antimicrob Agents Chemother. 1996 Jun;40(6):1476-81. doi: 10.1128/AAC.40.6.1476.