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1
In vitro activities of the biguanide PS-15 and its metabolite, WR99210, against cycloguanil-resistant Plasmodium falciparum isolates from Thailand.双胍类药物PS - 15及其代谢产物WR99210对泰国环氯胍耐药恶性疟原虫分离株的体外活性。
Antimicrob Agents Chemother. 1997 Oct;41(10):2300-1. doi: 10.1128/AAC.41.10.2300.
2
The antimalarial triazine WR99210 and the prodrug PS-15: folate reversal of in vitro activity against Plasmodium falciparum and a non-antifolate mode of action of the prodrug.抗疟三嗪WR99210和前药PS-15：叶酸对恶性疟原虫体外活性的逆转作用及前药的非抗叶酸作用模式。
Am J Trop Med Hyg. 1999 Jun;60(6):943-7. doi: 10.4269/ajtmh.1999.60.943.
3
Activity of PS-15 and its metabolite, WR99210, against Plasmodium falciparum in an in vivo-in vitro model.
Trans R Soc Trop Med Hyg. 1996 Sep-Oct;90(5):568-71. doi: 10.1016/s0035-9203(96)90326-0.
4
PS-15: a potent, orally active antimalarial from a new class of folic acid antagonists.PS - 15：一种新型叶酸拮抗剂类强效口服抗疟药。
Am J Trop Med Hyg. 1993 Jul;49(1):121-6. doi: 10.4269/ajtmh.1993.49.121.
5
The activity of PS-15 in combination with sulfamethoxazole.
Trop Med Parasitol. 1994 Jun;45(2):136-7.
6
Effects of folic and folinic acids in the activities of cycloguanil and WR99210 against Plasmodium falciparum in erythrocytic culture.叶酸和亚叶酸对环氯胍及WR99210在红细胞培养物中抗恶性疟原虫活性的影响。
Ann Trop Med Parasitol. 1997 Jan;91(1):17-23. doi: 10.1080/00034983.1997.11813107.
7
Cycloguanil and its parent compound proguanil demonstrate distinct activities against Plasmodium falciparum malaria parasites transformed with human dihydrofolate reductase.环氯胍及其母体化合物氯胍对用人类二氢叶酸还原酶转化的恶性疟原虫表现出不同的活性。
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8
Effects of dual combinations of antifolates with atovaquone or dapsone on nucleotide levels in Plasmodium falciparum.抗叶酸药物与阿托伐醌或氨苯砜的双重组合对恶性疟原虫核苷酸水平的影响。
Biochem Pharmacol. 1997 Apr 4;53(7):943-50. doi: 10.1016/s0006-2952(96)00835-0.
9
Phenoxypropoxybiguanides, prodrugs of DHFR-inhibiting diaminotriazine antimalarials.苯氧丙氧基双胍，二氢叶酸还原酶抑制性二氨基三嗪抗疟药的前药。
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Transformation with human dihydrofolate reductase renders malaria parasites insensitive to WR99210 but does not affect the intrinsic activity of proguanil.用人类二氢叶酸还原酶进行转化会使疟原虫对WR99210不敏感，但不会影响氯胍的内在活性。
Proc Natl Acad Sci U S A. 1997 Sep 30;94(20):10931-6. doi: 10.1073/pnas.94.20.10931.

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efficacy of next-generation dihydrotriazines and biguanides against babesiosis and malaria parasites.新一代二氢三嗪和双胍类药物抗巴贝斯虫和疟原虫的疗效。
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Functional analysis of Plasmodium vivax dihydrofolate reductase-thymidylate synthase genes through stable transformation of Plasmodium falciparum.通过稳定转化恶性疟原虫对间日疟原虫二氢叶酸还原酶-胸苷酸合成酶基因进行功能分析。
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Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.利用疟原虫裂殖子外质体转染系统定义恶性疟原虫二氢叶酸还原酶-胸苷酸合成酶基因突变的作用。
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Probing the role of parasite-specific, distant structural regions on communication and catalysis in the bifunctional thymidylate synthase-dihydrofolate reductase from Plasmodium falciparum.探究恶性疟原虫双功能胸苷酸合酶-二氢叶酸还原酶中寄生虫特异性的远距离结构区域在通讯和催化中的作用。
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Targeting purine and pyrimidine metabolism in human apicomplexan parasites.针对人类顶复门寄生虫中的嘌呤和嘧啶代谢
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本文引用的文献

1
Activity of PS-15 and its metabolite, WR99210, against Plasmodium falciparum in an in vivo-in vitro model.
Trans R Soc Trop Med Hyg. 1996 Sep-Oct;90(5):568-71. doi: 10.1016/s0035-9203(96)90326-0.
2
Anti-Pneumocystis carinii activity of PS-15, a new biguanide folate antagonist.新型双胍类叶酸拮抗剂PS - 15对卡氏肺孢子虫的活性
Antimicrob Agents Chemother. 1993 Jul;37(7):1417-9. doi: 10.1128/AAC.37.7.1417.
3
PS-15: a potent, orally active antimalarial from a new class of folic acid antagonists.PS - 15：一种新型叶酸拮抗剂类强效口服抗疟药。
Am J Trop Med Hyg. 1993 Jul;49(1):121-6. doi: 10.4269/ajtmh.1993.49.121.
4
The antimalarial activity of N-benzyl-oxydihydrotriazines. IV. The development of resistance to BRL 6231 (4,6-diamino-1,2-dihyydro-2-,2-dimethyl-1-(2,4,5-trichloropropyloxy)-1,3,5 triazine hydrochloride) by Plasmodium berghei.N-苄基-氧化二氢三嗪的抗疟活性。IV. 伯氏疟原虫对BRL 6231（4,6-二氨基-1,2-二氢-2,2-二甲基-1-(2,4,5-三氯丙氧基)-1,3,5-三嗪盐酸盐）的抗性发展
Ann Trop Med Parasitol. 1982 Feb;76(1):9-14.
5
The antimalarial activity of N-benzyl-oxydihydrotriazines. III. The activity of 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(2,4,5,-trichloropropyloxy)-1,3,5-triazine hydrobromide (BRL 51084) and hydrochloride (BRL 6231).N-苄基氧化二氢三嗪的抗疟活性。III. 4,6-二氨基-1,2-二氢-2,2-二甲基-1-(2,4,5-三氯丙氧基)-1,3,5-三嗪氢溴酸盐（BRL 51084）和盐酸盐（BRL 6231）的活性
Ann Trop Med Parasitol. 1982 Feb;76(1):1-7.
6
Resistance of ten Thai isolates of Plasmodium falciparum to chloroquine and pyrimethamine by in vitro tests.通过体外试验检测十株泰国恶性疟原虫分离株对氯喹和乙胺嘧啶的耐药性。
Trans R Soc Trop Med Hyg. 1981;75(2):271-3. doi: 10.1016/0035-9203(81)90333-3.
7
In vitro activities of and mechanisms of resistance to antifol antimalarial drugs.抗叶酸抗疟药物的体外活性及耐药机制
Antimicrob Agents Chemother. 1985 Apr;27(4):525-30. doi: 10.1128/AAC.27.4.525.
8
Antimalarial drug susceptibility testing of Plasmodium falciparum in Thailand using a microdilution radioisotope method.采用微量稀释放射性同位素法对泰国恶性疟原虫进行抗疟药物敏感性测试。
Am J Trop Med Hyg. 1985 Mar;34(2):228-35. doi: 10.4269/ajtmh.1985.34.228.
9
Analogues of N-benzyloxydihydrotriazines: in vitro antimalarial activity against Plasmodium falciparum.N-苄氧基二氢三嗪类似物：对恶性疟原虫的体外抗疟活性
Ann Trop Med Parasitol. 1986 Apr;80(2):177-81. doi: 10.1080/00034983.1986.11812002.
10
Plasmodium falciparum: cloning by single-erythrocyte micromanipulation and heterogeneity in vitro.恶性疟原虫：通过单个红细胞显微操作进行克隆及体外异质性研究
Exp Parasitol. 1988 Jun;66(1):86-95. doi: 10.1016/0014-4894(88)90053-7.

双胍类药物PS - 15及其代谢产物WR99210对泰国环氯胍耐药恶性疟原虫分离株的体外活性。

In vitro activities of the biguanide PS-15 and its metabolite, WR99210, against cycloguanil-resistant Plasmodium falciparum isolates from Thailand.

作者信息

Edstein M D, Bahr S, Kotecka B, Shanks G D, Rieckmann K H

机构信息

Australian Army Malaria Institute, Brisbane.

出版信息

Antimicrob Agents Chemother. 1997 Oct;41(10):2300-1. doi: 10.1128/AAC.41.10.2300.

DOI:10.1128/AAC.41.10.2300
PMID:9333069
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC164114/
Abstract

The in vitro activities of the new biguanide PS-15 and its putative active metabolite, WR99210, were determined against seven different isolates or clones of Plasmodium falciparum. The mean 50% inhibitory concentrations of PS-15 and WR99210 were 1,015 and 0.06 ng/ml, respectively. WR99210 was up to 363 times more potent than cycloguanil, the active metabolite of proguanil, against cycloguanil-resistant parasites. The pronounced activity of WR99210 against multidrug-resistant P. falciparum indicates that further studies are required to determine the value of the prodrug, PS-15, as an antimalarial agent.

摘要

测定了新型双胍类药物PS - 15及其假定的活性代谢物WR99210对七种不同的恶性疟原虫分离株或克隆的体外活性。PS - 15和WR99210的平均50%抑制浓度分别为1015和0.06纳克/毫升。在对抗环氯胍耐药寄生虫方面，WR99210的效力比氯胍的活性代谢物环氯胍高363倍。WR99210对多重耐药恶性疟原虫具有显著活性，这表明需要进一步研究来确定前药PS - 15作为抗疟药物的价值。