Plasmodium Inhibitor

5,7,3',4'-Tetramethoxyflavone, an orally active polymethoxyflavones (PMFs) that can be isolated from M. exotica, possesses various bioactivities, including anti-fungal, anti-malarial, anti-mycobacterial, and anti-inflammatory activities. 5,7,3',4'-Tetramethoxyflavone exhibits chondroprotective activity by targeting β-catenin signaling.

KDU691, an imidazopyrazine with potent anti-parasitic activity against blood stage schizonts, gametocytes and liver stages, is a Plasmodium PI4K inhibitor. KDU691 selectively inhibits dihydroartemisinin-pretreated Plasmodium falciparum ring-stage parasites.

Quassin (Nigakilactone D) is a bioactive triterpenoid from stem bark extract of Quassia amara. Quassin inhibits P. falciparum with an IC₅₀ of 0.15 μM. Quassin possesses reversible antifertility, anti-estrogenic and anti-plasmodial activity.

Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC₅₀s of 10.2 μM and 1.5 μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1.

Artelinic acid, a derivative of Artemisinin, is an antimalarial agent for the treatment of multidrug resistant strains of Plasmodium falciparum. Artelinic acid can be administered by various routes of administration, including intravenous, intramuscular and oral routes.

Ganaplacide (KAF156) hydrochloride is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide hydrochloride is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide hydrochloride is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite.

MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (K_d^app=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent.

Artemether-d₃ is the deuterium labeled Artemether. Artemether is an antimalarial for the treatment of resistant strains of falciparum malaria.

SIBA (5'-Isobutylthioadenosine) is a transmethylation inhibitor (SAH (HY-19528) analogue), with potent anti-proliferative activity. SIBA reversibly inhibits the production of HSV-1 by blocking methylation, specifically by blocking the 5' end-capping of viral mRNA. SIBA also inhibits the growth of tumour cells in vitro and metastatic spread in vivo. SIBA can be used in cancer, HSV-1 infection and anti-malaria studies.

Ursolic acid acetate (Acetylursolic acid) is a triterpenoid compound and an inhibitor of Plasmodium falciparum heat shock protein 90 (PfHsp90) with a K_D of 8.16 μM. Ursolic acid acetate is cytotoxic to KB cells, with an IC₅₀ value of 8.4 μM. Ursolic acid acetate can be used in tumor and antimalarial research.

Naphthoquine phosphate is an orally active antimalarial and antiviral agent. Naphthoquine phosphate exhibits ex vivo activity against multidrug-resistant Plasmodium falciparum and Plasmodium vivax, preferentially targeting ring-stage rather than trophozoite-stage parasites. Naphthoquine phosphate inhibits coronavirus (SARS-CoV-2, HCoV-OC43, HCoV-229E) replication by affecting viral entry and post-entry replication. Naphthoquine phosphate is used for research on malaria and Covid-19.

8-Deoxygartanin, a prenylated xanthones from G. mangostana, is a selective inhibitor of butyrylcholinesterase (BChE). 8-Deoxygartanin exhibits antiplasmodial activity with an IC₅₀ of 11.8 μM for the W2 strain of Plasmodium falciparum. 8-Deoxygartanin inhibits NF-κB (p65) activation with an IC₅₀ of 11.3 μM.

Halofuginone lactate (RU-19110 lactate), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone lactate is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone lactate is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca²⁺ channels. Halofuginone lactate has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

(2S)-2'-Methoxykurarinone (2'-O-Methylkurarinone) is a flavanone natural product found in the roots of Sophora flavescens, possessing anti-sepsis, inhibitory effects on osteoclast differentiation and bone resorption, anti-inflammatory, and anti-Plasmodium activities. (2S)-2'-Methoxykurarinone exhibits an EC₅₀ = 2.4 μM against the FCR-3 strain of Plasmodium falciparum. In sepsis models, (2S)-2'-Methoxykurarinone modulates immune cell function and inhibits inflammation and oxidative stress. In bone-related models, (2S)-2'-Methoxykurarinone blocks osteoclast differentiation and bone resorption, and inhibits RANKL-mediated Akt, p38, and JNK signaling pathways. In skin inflammation models, (2S)-2'-Methoxykurarinone inhibits NF-κB pathway activation, upregulates HO-1 expression, and suppresses CCL27 chemokine production in HaCaT cells. (2S)-2'-Methoxykurarinone is useful for research on osteoporosis, sepsis, inflammatory skin diseases (such as atopic dermatitis and allergic contact dermatitis), and malaria.

Febrifugine dihydrochloride is a quinazolinone alkaloid that inhibits P. falciparum and has antimalarial activity. Febrifugine dihydrochloride inhibits bladder cancer by inhibiting DNA synthesis, inducing apoptosis, and reducing steroids.

Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC₅₀ of 17 nM and an EC₅₀ of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage.

Kulactone, a natural bioflavonoid and an inhibitor against jRdRp, possesses antifungal, antibacterial and antiplasmodial activities. Kulactone exhibit no crossing through Blood Brain Barrier (BBB).

AQ-13 dihydrochloride is an aminoquinoline antimalarial agent that is effective against drug-resistant strains of Plasmodium falciparum.

Artefenomel (OZ439) is an orally active, synthetic anti-malarial compound containing an artemisinin pharmacophore with a mechanism of action similar to that of artemisinin. Artefenomel has antiviral activity against SARS-CoV-2.

Allosecurinine (Phyllochrysine) is a Securinega alkaloid isolated from Phyllanthus glaucus .