N-desethyl Amodiaquine (hydrochloride) (DEAQ) is the major metabolite of the antimalarial compound aminodiaquine, produced by the action of cytochrome P450 isoform 2C8 [1]. N-desethyl Amodiaquine (hydrochloride) is an antiparasitic agent that is highly active against Plasmodium falciparum and can synergize with amodiaquine[2]. N-desethyl Amodiaquine (hydrochloride) has inhibitory effects against strains V1/S and 3D7 with IC50 values of 97 nM and 25 nM, respectively [3]. This product is provided as N-desethyl Amodiaquine hydrochloride.
In vitro, treatment with N-desethyl Amodiaquine (hydrochloride) significantly blocked viral replication in both Huh 7 and Vero E6 cell lines infected with Ebola virus, with IC50 values in the low μM range [4]. Treatment of RAW264.7 cells with N-desethyl Amodiaquine (hydrochloride) (4, 8, 16, 33, 66 μM) for 1 h inhibited proteinase B activity in a dose-dependent manner[5].
References:
[1] Li X Q, Björkman A, Andersson T B, et al. Amodiaquine clearance and its metabolism ton-desethylamodiaquine is mediated by CYP2C8: a new high affinity and turnover enzyme-specific probe substrate[J]. Journal of Pharmacology and Experimental Therapeutics, 2002, 300(2): 399-407.
[2] Mariga S T, Gil J P, Sisowath C, et al. Synergism between amodiaquine and its major metabolite, desethylamodiaquine, against Plasmodium falciparum in vitro[J]. Antimicrobial agents and chemotherapy, 2004, 48(11): 4089-4096.
[3] Sasi P, Abdulrahaman A, Mwai L, et al. In vivo and in vitro efficacy of amodiaquine against Plasmodium falciparum in an area of continued use of 4-aminoquinolines in East Africa[J]. The Journal of infectious diseases, 2009, 199(11): 1575-1582.
[4] DeWald L E, Johnson J C, Gerhardt D M, et al. In vivo activity of amodiaquine against Ebola virus infection[J]. Scientific Reports, 2019, 9(1): 20199.
[5] Zilbermintz L, Leonardi W, Jeong S Y, et al. Identification of agents effective against multiple toxins and viruses by host-oriented cell targeting[J]. Sci Rep. 2015.
N-desethyl Amodiaquine (hydrochloride)（DEAQ）是抗疟化合物氨基地喹（aminodiaquine）的主要代谢物，由细胞色素P450亚型2C8的作用产生[1]。N-desethyl Amodiaquine (hydrochloride)是一种抗寄生虫药，对恶性疟原虫具有高度活性，并可与阿莫地喹产生协同作用[2]。N-desethyl Amodiaquine (hydrochloride)对菌株V1/S和3D7具有抑制作用，IC50 值分别为97 nM和25 nM[3]。本产品以N-desethyl Amodiaquine盐酸盐形式提供。
在体外，N-desethyl Amodiaquine (hydrochloride)处理感染了埃博拉病毒的Huh 7和Vero E6细胞系，均能显著阻断病毒复制，IC50 在低μM范围内[4]。N-desethyl Amodiaquine (hydrochloride)（4, 8, 16, 33, 66μM）处理RAW264.7细胞1h，以剂量依赖性方式抑制了蛋白酶B酶活性[5]。