chloroquine

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

Chloroquine phosphate (Aralen phosphate) is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs).

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.

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]

Chloranthalactone C, a natural sesquiterpene from Chloranthus serratus, has an IC50 >25 nM against Chloroquine-resistant Plasmodium falciparum DD2.

Warangalone is an anti-malarial compound that inhibits the growth of Plasmodium falciparum strains 3D7 (chloroquine-sensitive) and K1 (chloroquine-resistant) with IC50 values of 4.8 μg mL and 3.7 μg mL, respectively.

Canophyllal shows antiplasmodial activity against the W2 strain of Plasmodium falciparum which is resistant to chloroquine and other antimalarial drugs.

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

Dehydroabietinol (Pomiferin A) inhibits growth of chloroquine-sensitive as well as chloroquine-resistant strains of Plasmodium falciparum cultivated in erythrocytes in vitro (IC 50 26-27 microM).

Magnolioside has anti-plasmodial activity, shows notable growth inhibitory activity against chloroquine-sensitive strains of P. falciparum. It also shows a moderate antibacterial activity against Staphylococcus aureus CIP 53.154.Magnolioside exhibits significant neuroprotective activities against glutamate-induced toxicity.

19,20-Epoxycytochalasin D is a fungal metabolite that has been found in the endophytic fungus Nemania sp. UM10M. It is active against the chloroquine-sensitive and -resistant strains of P. falciparum (MIC = 0.4 ng/ml for both) without inducing cytotoxicity in Vero cells. It is cytotoxic to BT-549, LLC-PK11, and P388 cells (IC50s = 7.84, 8.4, and 0.16 µM, respectively) but not SK-MEL, KB, or SKOV3 cells up to a concentration of 10 µM.

(-)-Heraclenol shows in vitro anti-plasmodial activity against chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum.(-)-Heraclenol has moderate antibacterial and antifungal activities.

Betulinic acid methyl ester showed antiplasmodial activity against chloroquine-resistant Plasmodium falciparum parasites in vitro.It also inhibited B16 2F2 cell proliferation by induction of apoptosis.

Melicopine is an alkaloid found in Z. simulans, known for its antimalarial and anticancer properties. It inhibits P. falciparum strains, including chloroquine-sensitive 3D7 (IC50 of 29.7 µg mL) and chloroquine-resistant Dd2 (IC50 of 33.7 µg mL). Additionally, Melicopine exhibits cytotoxicity against prostate cancer cells PC-3M (IC50 of 47.9 µg mL) and LNCaP (IC50 of 37.8 µg mL), but it is inactive in non-cancerous HEK293 cells (IC50 greater than 100 µg mL). Melicopine holds potential for research in anticancer and anti-infective applications.

(-)-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.