Table 2.
In vivo antischistosomal activity of compounds isolated from natural sources.
| Molecules | Route | Dose | Main Results | References |
|---|---|---|---|---|
| Curcumin | Intraperitoneal | 400 mg/kg/day | Curcumin reduced worm and tissue egg burden, hepatic granuloma volume, and liver collagen content by 44.4%, 30.9%, 79%, and 38.6%, respectively | [50] |
| Curcumin | Oral | 300 mg/kg/day | Curcumin treatment exerted antifibrotic effects in S. mansoni-infected mice | [51] |
| Phytol | Oral | 40 mg/kg/day | A single dose of phytol (40 mg/kg) resulted in total and female worm burden reductions of 51.2% and 70.3%, respectively. Also, reduced numbers of eggs were found in feces (76.6%), with a lower frequency of immature eggs | [44] |
| Hesperidin | Intraperitoneal | 100 mg/kg/day | Reductions of 50, 45.2, 50, and 47.5% in males, females, worm pairs, and total worm burden, respectively. In addition, respective reductions, based on the number of eggs/g of tissue, of 41.5, 63.7, and 58.6% were observed in the liver, intestine, and liver/intestinal tissue combined | [43] |
| Triphenylphosphonium | Oral | 400 mg/kg/day | Triphenylphosphonium salts 10 and 11 resulted in low worm burden reductions against S. mansoni of 21.9% and 22.2%, respectively. Both compounds were well-tolerated by mice | [52] |
| Epiisopiloturine | Oral | 40, 100, and 300 mg/Kg/day | Treatment with epiisopiloturine at 40 mg/kg reduced total worm burden by 50.2%, as well as hepatosplenomegaly, egg burden in feces, and granuloma diameter. Electron microscopy revealed a loss of important features in the parasite tegument | [53] |
| Nerolidol | Oral | 100, 200, and 400 mg/kg/day | Nerolidol (100, 200, or 400 mg/kg) reduced worm burden and egg production in mice infected with adult schistosomes. Treatment with the highest concentration reduced total worms by 70.06% and immature eggs by 84.6%. Microscopic observations revealed that nerolidol-mediated worm killing was associated with tegumental damage | [54] |
| Paeoniflorin | Oral | 50 mg/kg/day | Paeoniflorin treatment decreased worm burden, as well as immature and mature eggs, with reductions in hepatic granuloma size and fibrotic areas | [55] |
| 7-epiclusianone | Oral | 100 or 300 mg/kg/day | 7-epiclusianone showed significant schistosomicidal in vivo activity following treatment with 300 mg/kg for 5 days | [56] |
| Allicin | Oral | 0.5 μM/mouse | Prophylactic administration of allicin in infected mice significantly reduced worm burden. Serum concentrations of liver fibrosis markers and proinflammatory cytokines were also reduced | [57] |
| Series of 15 chalcones | Oral | 400 mg/Kg/day | Chalcones 1 and 3 demonstrated moderate schistosomicidal activity with total worm burden significantly reduced by 32.8% and 31.8%, respectively, at a single oral dose (400 mg/kg) | [36] |
| Epiisopilosine alkaloid | Oral | 100 or 400 mg/Kg/day | A single dose of epiisopilosine significantly decreased total worm load by 57.78 and 60.61% at doses of 400 and 100 mg/Kg, respectively. In addition, epiisopilosine significantly reduced eggs number and decreased hepatosplenomegaly | [58] |
| Piplartine | Oral | 100, 200 or 400 mg/kg/day | Treatment with the highest piplartine dose (400 mg/kg) caused a significant (60.4%) reduction in total worm burden in mice harboring adult parasites. Microscopy revealed substantial tegumental alterations in parasites recovered from mice | [59] |
| Gomphoside monoacetate and Uscharin | Oral | 10 mg/kg/day | Only gomphoside monoacetate (10 mg/kg) demonstrated activity against S. mansoni, with a low worm burden reduction of 38% | [60] |
| Rotundifolone | Oral | 35.9, 70.9 and 141.9 mg/Kg/day |
Rotundifolone (141.9 mg/kg) significantly reduced fluke burden by 74.48%. Marked reductions in liver, intestinal, and fecal fluke burden, together with changes in the oogram pattern were observed. Treatment affected the viability of both mature and immature eggs | [61] |
| Licochalcone A | Oral; intraperitoneal | 1.5 or 2.5 mg/kg/day (oral); 25 mg/kg/day (intraperitoneal) | Oral treatment with L-SLNs decreased worm burden. However, under intraperitoneal administration, both free licochalcone A and L-SLNs significantly decreased worm burden and intestinal egg load | [62] |
| Carvacryl acetate | Oral | 100, 200, or 400 mg/kg/day | Carvacryl acetate (400 mg/kg) showed moderate efficacy against S. mansoni, with slightly reduced worm burden (32–40%). Egg production was markedly reduced (70–80%) | [63] |
| Cardamonin | Oral | 400 mg/kg/day | Oral treatment with cardamonin (400 mg/kg) demonstrated efficacy against S. mansoni, with decreased total worm load in 46.8% of mice and a 54.5% reduction in egg numbers | [64] |
| Asiaticoside | Oral | 400 mg/kg/day | A single oral dose (400 mg/kg) of asiaticoside presented significant in vivo antischistosomal efficacy, markedly decreasing total worm and egg burden | [65] |
| Plumbagin | Intraperitoneal | 20 mg/kg/day | Mice treated with plumbagin (20 mg/kg) showed reductions of 64.28% and 59.88% in male and female worms, respectively. Plumbagin treatment also alleviated schistosome-induced hepatosplenomegaly and reduced hepatic granuloma and liver collagen content | [66] |
| Juglone | Intraperitoneal | 2 mg/Kg/day | Treatment with the compound reduced male and female worms by 63.1% and 52.1%, respectively. The number of eggs/g of tissue in the liver and intestine were also reduced. Juglone decreased hepatic granuloma size and collagen fiber deposition. Mice treated with juglone presented significantly lower levels of IL-4, IL-13, IL-37, TNF-α, TGF-β, and IFN-γ than PZQ mice | [67] |
L-SLNs, LicoA-loaded solid lipid nanoparticles.