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11

抑制剂 & 化合物

10

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12084	MMV008138	Others	Others
	MMV008138 inhibits the growth of P. falciparum Dd2 strain (IC50 of 250 nM).
T70034	Dehatrine
	Dehatrine is from an Indonesian medical plant Beilschmiedia madang; a bisbibenzylisoquinoline alkaloid; inhibits growth of cultured Plasmodium falciparum K1 strain.
T62600	RYL-552S
	RYL-552S 是一种可杀死恶性疟原虫 Plasmodium falciparum 的耐药菌株，其可在体外有效杀灭无性血内阶段的寄生虫。
T72396	Antimalarial agent 20
	Antimalarial agent 20 是一种抗疟剂，在 NF54 蛋白测定中对P. falciparumNF54 寄生菌株的IC50为 0.6 nM。
T35485	6-Prenylindole
	6-Prenylindole is a bacterial metabolite that has been found in Streptomyces and has antifungal and antimalarial properties.1 It is active against A. brassicicola strain TP-F0423 and F. oxysporum f. sp. tulipae TU-4-2 (15 and 30 μg/disc in the paper disc assay), and also drug-resistant P. falciparum strain K1 (IC50 = 21 μg/ml).2 \|1. Sasaki, T., Igarashi, Y., Ogawa, M., et al. Identification of 6-prenylindole as an antifungal metabolite of Streptomyces sp. TP-A0595 and synthesis and bioactivity o...
T78951	Antimalarial agent 24	Parasite	Microbiology/Virology
	Antimalarial agent 24（Compound 7）是一种抗疟化合物，具有显著的体外（in vitro）活性。针对P. falciparum W2菌株，其IC50值为0.81 μM。同时，Antimalarial agent 24展现在HepG2细胞上的CC50值高于200 μM，表明其对宿主细胞具有较高安全性。
T116970	TLC3407-3786
	MMV665916 是一种喹唑啉二酮衍生物，是一种抗疟药。MMV665916 对恶性疟原虫 FcB1 菌株具有显著的抗疟原虫生长抑制活性，EC50值为 0.4 μM，并呈现出高选择性指数 (SI>250)。
T78184	MMV009085
	MMV009085是一种针对恶性疟原虫己糖转运体PfHT1的特异性抑制剂，具有潜在的抗疟效果。它同时抑制人葡萄糖转运蛋白，强效抑制葡萄糖吸收（IC50：2.6 μM）及恶性疟原虫3D7株的生长（EC50：1.23±0.04 μM）。
T79632	Antileishmanial agent-21	Parasite	Microbiology/Virology
	Antileishmanial agent-21 (compound 4e)，是靶向利什曼原虫蝶啶还原酶1 (Lm-PTR1) 的抗利什曼虫试剂。该化合物通过抗叶酸机制发挥作用，且其抗利什曼活性能被叶酸和亚叶酸逆转。Antileishmanial agent-21 还能抑制对 Chloroquine 抗性的恶性疟原虫菌株 (RKL9)，IC50 范围为0.0198-0.096 μM。
T83899	N-didesmethyl Loperamide R 21345
	N-didesmethyl Loperamide是loperamide的一个活性代谢产物，属于周围μ1-阿片受体激动剂。它能抑制孤立的豚鼠肠膜丛中由电刺激引起的收缩(IC50 = 370 nM)。N-didesmethyl Loperamide还能增强对氯喹产生抗药性的P. falciparum菌株对氯喹的敏感性(EC50 = 482 nM)，同时在A-10血管平滑肌细胞中未引起毒性(IC50 = >10,000 nM)。
T83044	Antimalarial agent 33	Parasite	Microbiology/Virology
	Antimalarial agent 33 (compound 5g) 显示针对红细胞期和肝期疟原虫的抗活性，特别是对 K1 恶性疟原虫株，其EC50为1.1 μM。Antimalarial agent 33 还展示出提升的微粒体稳定性（T1/2=29分钟），并且对原代肝细胞未表现出明显的细胞毒效应。

化合物

Cat.No: T12084

Target: Others

Cat.No: T70034

Cat.No: T62600

Antimalarial agent 20

Cat.No: T72396

Cat.No: T35485

Antimalarial agent 24

Cat.No: T78951

Target: Parasite

Cat.No: T116970

Cat.No: T78184

Antileishmanial agent-21

Cat.No: T79632

Target: Parasite

N-didesmethyl Loperamide

Cat.No: T83899

Synonym: R 21345

Antimalarial agent 33

Cat.No: T83044

Target: Parasite

Cat. No.	Product Name	Target	Signaling Pathways
TN2027	Oxysanguinarine 8-Oxosanguinarine,氧化血根碱,Hydroxysanguinarine	Parasite	Microbiology/Virology
	Oxysanguinarine (Hydroxysanguinarine) 是一种来自Meconopsis simplicifolia 的小檗生物碱，具有抗疟和抗血小板聚集活性，对登革热病毒具有潜在的抑制作用。
TCS2070	Homogentisic acid 高龙胆酸,2,5-dihydroxyphenylacetic acid,Homogentisinic Acid,Melanic acid	Antioxidant; Endogenous Metabolite	Metabolism; oxidation-reduction
	Homogentisic acid (2,5-dihydroxyphenylacetic acid) 是一种尿液和血清代谢物中的特定代谢物，可用于尿黑酸尿症的诊断。
T2S2362	Dehydrocorydaline nitrate 去氢延胡索甲素硝酸盐,硝酸脱氢紫堇碱	BCL; Others; PARP; p38 MAPK; Caspase; Parasite; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; MAPK; Microbiology/Virology; Others; Proteases/Proteasome
	Dehydrocorydaline nitrate 是生物碱。Dehydrocorydaline 调节 Bax，Bcl-2蛋白表达，激活 caspase-7，caspase-8，并使 PARP 失活。它能增强 p38 MAPK 活化，具有抗炎、抗癌、抗疟疾等功效。
TN3583	Canophyllal	Antifection	Microbiology/Virology
	Canophyllal shows antiplasmodial activity against the W2 strain of Plasmodium falciparum which is resistant to chloroquine and other antimalarial drugs.
TN4717	Oplopanone	Antifection	Microbiology/Virology
	Oplopanone exhibits noteworthy anti-plasmodial activity against Plasmodium falciparum strain.
T75568	Z-Antiepilepsirine
	Z-Antiepilepsirine 是一种酰胺生物碱，存在于 Piper capense L.f 中。Z-Antiepilepsirine 显示抗疟原虫活性，对 PlasmodiumfalciparumW2 菌株的 IC50值为 27 µM。
TN4113	Garcinone E	Antifection	Microbiology/Virology
	Garcinone E is active constituents in the anticomplement assay used. Garcinone E exhibits potent activity in vitro against Plasmodium falciparum chloroquine-resistant strain W2, with IC50 values below 3 µM. It has potent cytotoxic effect on all hepatocellular carcinomas cell lines as well as on the other gastric and lung cancer cell lines included in the screen, may be potentially useful for the treatment of certain types of cancer.
TN4449	Longistylin C	Antifection	Microbiology/Virology
	Longistylin A and longistylin C show some cytotoxic effects, with IC(50) values of 0.7-14.7 microM against the range of cancer cell lines. Longistylin A and longistylin C, and betulinic acid show a moderately high in vitro activity against the chloroquine
T35758	Butyrolactone V
	Butyrolactone V is a fungal metabolite that has been found in A. terreus and has antiprotozoal, antioxidant, and anticancer activities.1,2,3 It is active against the P. falciparum strain K1 (IC50 = 7.9 μg/ml) and L. amazonensis promastigotes (IC50 = 23.7 μM).2,1 Butyrolactone V (227 and 454.1 μM) is also active against adult S. mansoni worms.1 It scavenges 2,2-diphenyl-1-picrylhydrazyl and ABTS radicals with IC50 values of 20.7 and 3.7 μM, respectively, in cell-free assays.3 Butyrolactone V also...
T35751	Violacein
	Violacein is a bacterial metabolite originally isolated from C. violaceum that has antibacterial and antiprotozoal activities.[1] [2] It is produced by C. violaceum as a purple pigment in response to N-hexanoyl homoserine lactone , a property that has been modified to create a strain of C. violaceum used in detecting quorum-sensing molecules.[3] Violacein is active against Gram-positive bacteria, including B. subtilis and S. aureus (MICs = 0.8 and 1.6 &#181M, respectively). It is also active aga...

天然产物

Oxysanguinarine

Cat.No: TN2027

Synonym: 8-Oxosanguinarine,氧化血根碱,Hydroxysanguinarine

Target: Parasite

Homogentisic acid

Cat.No: TCS2070

Synonym: 高龙胆酸,2,5-dihydroxyphenylacetic acid,Homogentisinic Acid,Melanic acid

Target: Antioxidant, Endogenous Metabolite

Dehydrocorydaline nitrate

Cat.No: T2S2362

Synonym: 去氢延胡索甲素硝酸盐,硝酸脱氢紫堇碱

Target: BCL, Others, PARP, p38 MAPK, Caspase, Parasite, Autophagy

Cat.No: TN3583

Target: Antifection

Cat.No: TN4717

Target: Antifection

Z-Antiepilepsirine

Cat.No: T75568

Cat.No: TN4113

Target: Antifection

Cat.No: TN4449

Target: Antifection

Butyrolactone V

Cat.No: T35758

Cat.No: T35751

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