falciparum strain

Oxysanguinarine (Hydroxysanguinarine) possesses antiplatelet aggregation activity, it has potential inhibitory properties against the dengue virus.

LysRs-IN-2 is a lysine tRNA synthetase (KRS) inhibitor with antiparasitic activity that inhibits Plasmodium falciparum KRS (PfKRS) and Cryptosporidium minum KRS (CpKRS), and is used in the study of malaria infections.

MMV030084 is a potent PfPKG inhibitor that displays nanomolar-level activity against liver-stage Plasmodium parasites in HepG2 cells and synchronized schizont stages of both drug-sensitive and multidrug-resistant strains, selectively inhibits male gamete exflagellation, and mechanistically targets cGMP-dependent protein kinase with sub-nanomolar potency in recombinant assays, establishing MMV030084 as a valuable antimalarial lead for multistage lifecycle intervention.

MMV665916 is a quinazolinedione derivative that is an antimalarial agent. MMV665916 shows remarkable antiplasmodial activity against P. falciparum FcB1 strain with EC 50 value of 0.4 μM and presents the high selectivity index (SI>250) [1].

MMV008138 inhibits the growth of P. falciparum Dd2 strain (IC50 of 250 nM).

Antiproliferative agent-56 (Compound 31) is an antimalarial agent that inhibits the Pf3D7 strain of the malaria parasite Plasmodium falciparum with an IC50 of >12.5 (48h) and 0.03 μM (98h), displaying slow-acting characteristics.

Villalstonine, a bisindole alkaloid, exhibits a broad spectrum of bioactivities, including anticancer, antimalarial, and anti-amoebic properties. It demonstrates potent antimalarial activity against the multidrug-resistant Plasmodium falciparum K1 strain, with an IC50 value of 0.27 μM.

Cordysinin C/D (compound 9) is a potential antimalarial agent that effectively inhibits the Plasmodium falciparum 3D7 strain.

Antimalarial agent 47 (compound F14) is a chemical compound effective against Plasmodium falciparum, specifically targeting the W2 strain with an IC50 value of 235 nM.

Mer-NF5003F (Stachybotrydial; F 1839M) is a sesquiterpene isolated from Stachybotrys, effective in inhibiting avian myeloblastosis virus (AMV) protease with an IC50 of 7.8 μM. It also inhibits sialyltransferases ST6N, ST3O, and ST3N with IC50 values of 0.61, 6.7, and 10 μg/mL, respectively, and fucosyltransferase with an IC50 of 11.3 μg/mL. Additionally, Mer-NF5003F exhibits in vitro activity against herpes simplex virus HSV-1 (IC50=4.32 μg/mL) and multi-drug-resistant Plasmodium falciparum K1 strain (IC50=0.85 μg/mL).

Antiparasitic agent-22 (Compound 24) is a broad-spectrum antiparasitic compound that inhibits the procyclic form of T. brucei, L. infantum, and L. tropica with IC50 values of 2.41, 5.95, and 8.98 μM, respectively, and the amastigote form of L. infantum with an IC50 of 8.18 μM. It also shows inhibitory activity against the P. falciparum W2 strain with an IC50 of 0.155 μM. Additionally, Antiparasitic agent-22 exhibits low cytotoxicity in THP1 cells, with a CC50 of 64.16 μM.

Antimalarial agent 41 (Compound 17) exhibits antimalarial activity by inhibiting the malaria parasite Plasmodium falciparum, with IC50 values of 40 nM for NF54 strain and 76 nM for K1 strain. This compound acts as an inhibitor of P. falciparum phosphatidylinositol-4-kinase β (PfPI4K) and hERG channels, with IC50 values of 53 nM and 3 μM, respectively. Additionally, Antimalarial agent 41 shows cytotoxicity against CHO cells, with an IC50 of 34 μM. It can improve malaria infections and demonstrates favorable pharmacokinetic properties in mouse models.

WR 30090 (Compound 37) is a broad-spectrum antimalarial agent that operates independently of the classical antifolate pathway. It shows significant activity against various strains of Plasmodium falciparum, both chloroquine-sensitive and -resistant, notably effective against the highly resistant Vietnamese strain. In rodent malaria tests, WR 30090 demonstrated high activity with a minimum effective dose of 5 mg/kg and a minimum curative dose of 20 mg/kg. This compound is useful for studying acute malaria.

1. Dehydrocorydaline(DHC) not only inhibits antibody-mediated allergic reactions but also influences cell-mediated allergic reactions, and the inhibitory effect of Corydalis Tuber on allergic reactions may be partially attributed to DHC. 2. Dehydrocorydal

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 of 6-substituted indoles. J. Antibiot. (Tokyo) 55(11), 1009-1012 (2002).|2. Nkunya, M.H., Makangara, J.J., and Jonker, S.A. Prenylindoles from Tanzanian Monodora and Isolona species. Nat. Prod. Res. 18(3), 253-258 (2004).

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 µM, respectively). It is also active against P. falciparum, including chloroquine-susceptible and -resistant strains (IC50s = 0.85 and 0.63 µM, respectively).[2] It reduces parasitemia in a mouse model of nonlethal P. chabaudi chabaudi infection when administered at a dose of 7.5 mg/kg and increases survival in a mouse model of lethal P. chabaudi chabaudi infection. Violacein permeabilizes the cytoplasmic membrane of bacterial cells but does not affect the cell wall.[1]

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 inhibits proliferation of MDA-MB-231 and MCF-7 breast cancer cells (IC50s = 22.2 and 31.9 μM, respectively).1

Hex is an enolase inhibitor and antimalarial agent with Ki values of 74.4 nM and 269.4 nM against ENO2 and ENO1, respectively; its IC50 values against NfENO and TbENO are 0.14 μM and 2.1 μM, respectively. Hex exhibits antimalarial activity against Plasmodium falciparum 3D7, Naegleria fowleri trophozoites, and Plasmodium berghei ANKA strain, and also shows certain antitumor effects against intracranial tumors.

RYL-552S is a drug-resistant strain of Plasmodium falciparum that effectively kills the asexual blood stage of the parasite in vitro.

Dehatrine is from an Indonesian medical plant Beilschmiedia madang; a bisbibenzylisoquinoline alkaloid; inhibits growth of cultured Plasmodium falciparum K1 strain.

Antimalarial agent 20, exhibiting potent efficacy with an IC50 value of 0.6 nM against the P. falciparum NF54 parasite strain within the NF54 albumax assay, serves as a significant antimalarial compound.

Z-Antiepilepsirine, an amide alkaloid present in Piper capense L.f., exhibits antiplasmodial properties, demonstrating an IC50 value of 27 µM against the W2 strain of Plasmodium falciparum [1].

MMV009085 is a potent inhibitor of the Plasmodium falciparum hexose transporter (Pf HT1), with potential as an anti-malarial agent. It also inhibits the human glucose transporter, demonstrating high potency with an IC50 of 2.6 μM in glucose uptake assays and an EC50 of 1.23±0.04 μM against the 3D7 strain of the malaria parasite [1].

Compound 24 (Compound 7), an in vitro antimalarial agent, demonstrates inhibitory activity against the Plasmodium falciparum W2 strain with an IC50 of 0.81 μM and exhibits a cytotoxicity threshold (CC50) exceeding 200 μM in HepG2 cells [1].