antiplasmodial

CV-6209 is a potent antagonist of the platelet-activating factor (PAF) receptor.

Jatrorrhizine (neprotin) is a protoberberine alkaloid isolated from Enantia chlorantha (Annonaceae) and other species. It was found to have antimicrobial and antifungal activity. It binds and noncompetitively inhibits monoamine oxidase (IC50 4 micromolar for MAO-A and 62 for MAO-B).

Desethyl chloroquine diphosphate, the active metabolite of Desethylchloroquine, is a cross-placental and orally available inhibitor of toll-like receptors (TLRs) with antiplasmodial activity and inhibition of autophagy.

Guanfu base H is a diterpenoid alkaloid isolated from Aconitum coreanum. It has antiplasmodial activity against the malarial Plasmodium falciparum strains TM4 8.2 (wild type) and K1CB1 (IC50s: 4 μM and 3.6 μM).

Isochondodendrine has strong antiplasmodial activity against Plasmodium falciparum. Isochondrodendrine is a class of bisbenzylisoquinoline alkaloid isolated from Isolona ghesquiereina.

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].

Laetanine, exhibits antiplasmodial activity, a noraporphine alkaloid from Litsea laeta.

Bis-propargyl-PEG3 is a PEG-based PROTAC linker utilized for the synthesis of PROTACs. It is also employed in the synthesis of antiplasmodial zinc-dipicolylamine (ZnDPA) complexes[1] [2].

Fagaramide possesses Antiplasmodial activity.

Jatrorrhizine hydrochloride is a compound extracted from the roots of Berberis vulgaris with neuroprotective, antimicrobial, antiplasmodial, and antioxidant activities.Jatrorrhizine hydrochloride is an orally active and selective inhibitor of acetylcholinesterase (AChE), which inhibits norepinephrine (NE) uptake. It inhibits the uptake of norepinephrine (NE).

3-Isomangostin is a potent human aldose reductase inhibitor with an IC50 of 3.48 uM; it is also an acetylcholinesterase selective inhibitor. 3-Isomangostin has free radical scavenging activity; it shows antiplasmodial activity with IC50 values in the rang

Beauvericin A is a cyclodepsipeptide and derivative of beauvericin originally isolated fromB. bassianathat has diverse biological activities.1,2,3It is active againstM. tuberculosis(MIC = 25 μg/ml) andP. falciparum(IC50= 12 μg/ml).2Beauvericin A is toxic to brine shrimp (LD100= 32 μg/ml).3 1.Gupta, S., Montillor, C., and Hwang, Y.-S.Isolation of Novel Beauvericin Analogues from the Fungus Beauveria bassianaJ. Nat. Prod.58(5)733-738(1995) 2.Nilanonta, C., Isaka, M., Kittakoop, P., et al.Antimycobacterial and antiplasmodial cyclodepsipeptides from the insect pathogenic fungus Paecilomyces tenuipes BCC 1614Planta Med.66(8)756-758(2000) 3.Shi, S., Li, Y., Ming, Y., et al.Biological activity and chemical composition of the endophytic fungus Fusarium sp. TP-G1 obtained from the root of Dendrobium officinale Kimura et MigoRec. Nat. Prod.12(6)549-556(2018)

(-)-Catechin gallate ((-)-Catechin 3-O-gallate) displays inhibition of 6PGD, IDH. (-)-Catechin gallate ((-)-Catechin 3-O-gallate) displays inhibition of human Beta-secretase. (-)-Catechin gallate ((-)-Catechin 3-O-gallate) possesses antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 and chloroquine-resistant Plasmodium falciparum K1.

5,7-Dihydroxycoumarin, a coumarin isolated from the inflorescences of Macaranga triloba, exhibits antibacterial activities[1][2]. [1]. Ishak Zakaria, et al. Flavonoids with antiplasmodial and cytotoxic activities of Macaranga triloba. Fitoterapia. 2012 Jul;83(5):968-72. [2]. Yi-Ping Chin, et al. Synthesis and evaluation of antibacterial activities of 5,7-dihydroxycoumarin derivatives. Arch Pharm (Weinheim). 2011 Jun;344(6):386-93.

11-O-Galloylbergenin is isolated from of Mallotus philippinensis with antioxidant and antiplasmodial activities.

Jatrorrhizine chloride (Neprotine chloride) is a potent and orally active uptake-2 transporter inhibitor. It exhibits a critical neuroprotective role in H2O2-induced apoptosis via inhibition of the MAPK pathway in HT22 hippocampal neurons.

Anticancer agent 75 has good antiplasmodial activity. Anticancer agent 75 is a potent anticancer agent with cytotoxicity and selectivity in cancer cell lines. The cytotoxicity of Anticancer agent 75 to normal human kidney cell lines is at least 35 times lower than that of the Doxorubicin standard [1].

9-O-Demethyltrigonostemone is a natural IDO1 inhibitor, cytotoxic and antiplasmodial agent from the Roots of Strophioblachia fimbricalyx.

Jatrorrhizine hydroxide, an alkaloid derived from Coptis chinensis, exhibits a range of biological activities including neuroprotective, antimicrobial, antiplasmodial, and antioxidant properties [1]. It acts as a potent and orally active inhibitor of acetylcholinesterase (AChE) with an IC50 value of 872 nM, demonstrating over 115-fold greater selectivity for AChE compared to butyrylcholinesterase (BuChE) [2]. Additionally, Jatrorrhizine hydroxide impedes the uptake of serotonin (5-HT) and norepinephrine (NE) by inhibiting uptake-2 transporters, further contributing to its pharmacological profile [3].

Koshidacin B, a cyclic tetrapeptide, exhibits potent antiplasmodial activity, evidenced by its ability to inhibit Plasmodium falciparum strains FCR3 and K1 with IC50 values of 0.89 μM and 0.83 μM, respectively. It has been shown to effectively suppress malaria parasites in vivo and has potential applications in parasitic infection research [1].

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].

Thalifendine chloride, a Berberine metabolite, exhibits antiplasmodial and antiamoebic properties. It effectively inhibits P. falciparum and E. histolytica, with IC50 values of 7.91 μM and 116 μM, respectively [1] [2].

Antimalarial agent 28 (Compound 2i) is an antiplasmodial agent that inhibits P. berghei with IC50 values of 0.561 μM for the liver stage, 0.14 μM for early gametocytes, and 4.34 μM for the ring stages of P. falciparum [1].

Cycleanine has potent antibacterial, antifungal, antiplasmodial, and cytotoxic activities.