schistosoma

Nilutamide (RU23908), an antineoplastic hormonal agent, is mainly used in the treatment of prostate Y. Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors, but not for estrogen, progestogen, or glucocorticoid receptors. Therefore, Nilutamide can block the action of androgens of testicular and adrenal origin that stimulate the growth of malignant and normal prostatic tissue. Prostate Y is mainly androgen-dependent and can be treat with chemical castration or surgical. So far, antiandrogen monotherapy has not consistently been certified to be equivalent to castration.

RR-11a analog (aza-peptide Michael acceptor, 7a) is an inhibitor of asparaginyl endopeptidase with IC50s of 4.5 nM, 4.5 nM and 31 nM for AE1 in Trichomonas Vaginalis, AE in Ixodes ricinus and AE in Schistosoma mansoni, respectively.

PHYTOL (trans-Phytol) , a diterpene alcohol from chlorophyll widely used as a food additive and in medicinal fields, shows antinociceptive and antioxidant activities as well as anti-inflammatory and antiallergic effects. It is a specific activator of PPARα.

Hycanthone (Etrenol(mesylate)) is a potent drug of antischistosomal. Hycanthone is a DNA intercalator that inhibits RNA synthesis and DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits APE1 via direct protein binding(KD: 10 nM).

Bithionol sulfoxide (Bithionoloxide) is a compound with inhibitory effects on parasites, suppressing the activity of Schistosoma japonicum and Fasciola hepatica.

Methylclonazepam is a benzodiazepine with anxiolytic properties. It inhibits the uptake of 5-hydroxytryptamine by Schistosoma mansoni, and its derivatives exhibit anti-Schistosoma mansoni activity.

Insecticidal agent 23 (compound 17) possesses anti-schistosomal properties with low toxicity. It exhibits strong in vitro activity against adult Schistosoma japonicum, with an LC50 (72 h) value of 25.31 μM.

SmCB1-IN-1 (Compound 2h) is an inhibitor of the Schistosoma mansoni cathepsin B1 (SmCB1) with a Ki of 0.05 μM. It demonstrates selectivity towards non-target human proteases, showing inhibition rates of 29% for CatB and 37% for CatL at 20 μM. At 1 μM, SmCB1-IN-1 inhibits 68% of Schistosoma mansoni.

MC3935 (Compound 19) is an LSD1 inhibitor with an IC50 of 0.52 μM for the LSD1-CoREST enzyme complex. It shows significant antischistosomal activity against newly transformed schistosomula (NTS) and adult Schistosoma mansoni, although its onset of action is delayed against larvae. MC3935 exhibits no significant toxicity to human cells and is useful for schistosomiasis research.

LSD1-IN-44 (Compound 19) is an LSD1 inhibitor with an IC50 of 0.02 μM for the LSD1-CoREST enzyme complex. It exhibits significant antischistosomal activity against newly transformed schistosomula (NTS) and adult Schistosoma mansoni, though its effect on larvae shows some delay. LSD1-IN-44 demonstrates no notable toxicity to human cells and is applicable for schistosomiasis research.

SIRT2-IN-18 (Compound 8) is a potent SIRT2 inhibitor, with IC50 values of 5.3 μM for SmSIRT2 and 12.3 μM for hSIRT2. It demonstrates strong anti-schistosomal activity against Schistosoma mansoni strains from Liberia and Puerto Rico, effectively reducing larval and adult worm pair survival, pairing, and egg production, while exhibiting low cytotoxicity to mammalian cells. Additionally, SIRT2-IN-18 enhances histone H3 hyperacetylation and induces apoptosis through cytochrome c mediation.

Teroxalene Hydrochloride is disubstituted piperazine used to treat animals with Schistosoma mansoni.

Cardol triene, a phenolic compound found in cashews, competitively and irreversibly inhibits mushroom tyrosinase (IC50=22.5 μM) and exhibits micromolar-level inhibition against Schistosoma mansoni worms. It can be used for synthesizing dibenzoxazines.

Antiparasitic agent-10 (Compound 94) is a potent anti-parasitic agent with significant anti-schistosomal activity, particularly against adult Schistosoma mansoni, making it a promising candidate for Schistosomiasis research as a treatment option [1].

HDAC8-IN-2 (compound 5o) is a potent HDAC8 inhibitor with IC50 values of 0.27 μM and 0.32 μM for smHDAC8 (Schistosoma mansoni histone deacetylase 8) and hHDAC8, respectively. It effectively kills schistosome larvae and significantly reduces egg laying in adult worm pairs [1].

Hydrolapachol is a novel potent and selective inhibitor of schistosoma mansoni dihydroorotate dehydrogenase (smdhodh)

Z-Pro-Pro-CHO acts as a prolyl oligopeptidase inhibitor with half-maximal inhibitory concentrations (IC50) of 0.16 μM for human prolyl oligopeptidase and 0.01 μM for Schistosoma mansoni prolyl oligopeptidase [1].

SjDX5-53 is a selective TLR2 inducer derived from a 3 kDa peptide found in Schistosoma japonicum eggs. This compound supports the production and inhibitory function of regulatory T cells (Tregs) by inducing tolerogenic dendritic cells (tolDCs), thereby suppressing inflammatory Th1 and Th17 responses. SjDX5-53 is primarily studied for its therapeutic potential in autoimmune and inflammatory conditions, such as colitis and psoriasis.