t. b. brucei

Acoziborole (SCYX-7158), a derivative of benzoxaborole, is a safe, effective and structurally novel antigen-worm agent for human African trypanosomiasis (HAT) studies. The MIC value of Acoziborole for T. b. brucei S427 was 0.6 µg/mL.

ML251 is a potent novel nanomolar inhibitor of T. brucei and T. cruzi phosphofructokinase[1]. ML251 inhibits T. brucei PFK (IC50=0.37 μM) and T. cruzi PFK (IC50=0.13 μM). ML251 can be used for the research of parasite[1].

Antitrypanosomal agent 1 is a potent and selective trypanothione reductase (TR) inhibitor (IC50: 3.3 μM) that also inhibits glutathione reductase (IC50: 64.8 μM) and T. brucei (EC50: 1 μM).

1. Xanthatin has cytotoxic activity. 2. Xanthatin has antibacterial and antifungal activies against MRSA. 3. Xanthatin may have therapeutic potential against NSCLC. 4. Xanthatin can inhibit murine melanoma B16-F1 cell proliferation possibly associated wit

Tuberculosis inhibitor 1 is a potent, non-cytotoxic inhibitor of Trypanosoma brucei growth [EC50: 5 nM].

Hygrolidin is a macrocyclic lactone originally isolated from S. hygroscopicus. It inhibits proliferation of a variety of cancer cell lines, including DLD-1 colon cancer, LNCaP prostate cancer, and K562 leukemia cells (IC50s = 2.9, 5.2, and 33 ng/ml, respectively). Hygrolidin induces the expression and levels of p21 in DLD-1 cells, but not WI-38 fibroblasts, and leads to cell accumulation in the G1 and S phases without inducing apoptosis. It has antiparasitic activity against T. cruzi, L. donovani, and T. b. brucei but also induces cytotoxicity in HepG2 cells (IC50s = 1.1, 72.5, 77, and 24.5 nM, respectively).

Orfamide A, a lipopeptide biosurfactant isolated from P. protegens, exhibits multifaceted bioactivity. With an LC50 of 34.5 μg/ml, it significantly increases mortality in adult green peach aphids. Additionally, at a concentration of 50 μM, Orfamide A inhibits appressoria formation in M. oryzae isolates and decreases the prevalence of sporulating blast lesions in M. oryzae-infected plants. Furthermore, it demonstrates efficacy against T. b. brucei, with an IC50 value of 6 µM.

Antitrypanosomal agent 9 is a potent compound with inhibitory activity against T. b. brucei, exhibiting an IC50 of 1.15 μM. It is utilized in research for human African trypanosomiasis (HAT).

Salviandulin E, a diterpenoid isolated from Salvia leucantha CAV., exhibits antitrypanosomal activity against T. b. brucei GUTat 3.1 parasites, demonstrating an IC50 value of 0.72 µg/mL [1] [2].

Antitrypanosomal agent 4 (compound 19) is a potent antitrypanosomal compound that crosses the blood-brain barrier and exhibits strong resistance to Trypanosoma cruzi and T. b. brucei with IC50 values of 1.2 μM and 70 nM, respectively.

Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα but exhibits anti-parasite activity and is a potent activator of PKA, binding to the R site (PKAR) with an EC50 of 6.5 nM and a Kd of 8 nM in Trypanosoma brucei.

NPD-2975 (compound 30) is an orally active antitrypanosomal agent effective against Human African Trypanosomiasis (HAT), demonstrating acceptable metabolic stability and low toxicity potential in human MRC-5 lung fibroblasts, as well as in an acute mouse model of T. b. brucei infection. It exhibits an in vitro IC50 of 70 nM against T. b. brucei and IC50 values of 0.16 μM and 0.42 μM against CYP1A2 and CYP2C19 enzymes, respectively [1].

20S Proteasome-IN-4 (Compound 7) is an orally active inhibitor of the 20S proteasome, selectively targeting the parasite form and demonstrating brain penetration capabilities. It exhibits a potent IC50 value of 6.3 nM against the T. b. brucei 20S proteasome, making it suitable for human African trypanosomiasis (HAT) research [1].

PEX5-PEX14 PPI-IN-1 (Compound 8) is a PEX14-PEX5 protein-protein interaction (PPI) inhibitor with an inhibitory constant (Ki) of 53 μM that disrupts the interaction between PEX5 and TbPEX14. It effectively inhibits the bloodstream form of Trypanosoma brucei brucei with a half-maximal effective concentration (EC50) of 5 μM [1].

SPR7 is a potent and selective rhodesain inhibitor (Ki: 0.51 nM). SPR7 exhibited antiparasitic effects against T. b. brucei (EC50: 1.65 μM).

Compound 12, also known as PEX5-PEX14 PPI-IN-2, is a PEX14-PEX5 protein-protein interaction (PPI) inhibitor with half-maximal effective concentration (EC50) values of 5 µM in T. b. brucei and 17 µM in HepG2 cells. It is utilized in the study of diseases associated with trypanosome infection [1].