Background <p>Drug treatment of hydatid cysts is usually carried out using benzimidazole compounds such as albendazole and mebendazole. However, limited efficacy, the need for long-term use, and side effects such as liver damage and gastrointestinal problems have made the use of these drugs challenging. The present study aimed to evaluate the antiparasitic effects of Baicalein (BC) on <i>Echinococcus granulosus</i> protoscoleces (PTS) and its inhibitory effects on the expression level of antioxidant genes.</p> Methods <p>The antiparasitic effects of BC on PTS was evaluated using eosin exclusion test. The effects of BC on the expression level of antioxidant genes glutathione glutathione S-transferase (<i>GST</i>), thioredoxin (<i>Trx</i>), and thioredoxin peroxidase (<i>TPx</i>) in PTS was performed using Real-time PCR. For cytotoxicological tests, two human cell lines including normal liver cells (THLE-2) and liver cancer cells (HepG2) were used for MTT assay.</p> Results <p>The findings demonstrated that both the lethality and subsequent mortality of <i>E. granulosus</i> PTS increased significantly with rising concentrations of BC and prolonged exposure time (<i>p</i> &lt; 0.001). Among the concentrations evaluated, BC exhibited the most pronounced antiparasitic activity against PTS at 64 and 128 µM/mL, achieving complete protoscolicidal effects after 30 and 20&#xa0;min, respectively. Furthermore, the calculated CC50 values were 161.3 µM/mL for THLE-2 cells and 75.6 µM/mL for HepG2 cells. Treatment of PTS with the BC dose-dependently reduced the relative expression level of the <i>GST</i>,<i> TRx</i>, and <i>TPx</i> genes (<i>P</i> &lt; 0.001); while significantly increased the reactive oxygen species in the PTS.</p> Conclusion <p>The results of the study showed that BC had a significant protoscolicicidal effect on <i>E. granulosus</i> PTS, which increased parasite death by reducing the expression of antioxidant genes, indicating a direct effect on their defense system and metabolic pathways. Also, BC had a favorable selective effect on HepG2 cancer cells and showed less toxicity than normal THLE-2 cells, which confirms its high selectivity index. Future studies can focus on developing novel drug delivery formulations and investigating signaling pathways related to oxidative stress and apoptosis in parasites to optimize the antiparasitic and anticancer effects of BC.</p>

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Inhibition of Antioxidant Genes Expression in Echinococcus Granulosus by Baicalein: Implications for Novel Antiparasitic Strategies

  • Hussam Saeed Al-Aredhi

摘要

Background

Drug treatment of hydatid cysts is usually carried out using benzimidazole compounds such as albendazole and mebendazole. However, limited efficacy, the need for long-term use, and side effects such as liver damage and gastrointestinal problems have made the use of these drugs challenging. The present study aimed to evaluate the antiparasitic effects of Baicalein (BC) on Echinococcus granulosus protoscoleces (PTS) and its inhibitory effects on the expression level of antioxidant genes.

Methods

The antiparasitic effects of BC on PTS was evaluated using eosin exclusion test. The effects of BC on the expression level of antioxidant genes glutathione glutathione S-transferase (GST), thioredoxin (Trx), and thioredoxin peroxidase (TPx) in PTS was performed using Real-time PCR. For cytotoxicological tests, two human cell lines including normal liver cells (THLE-2) and liver cancer cells (HepG2) were used for MTT assay.

Results

The findings demonstrated that both the lethality and subsequent mortality of E. granulosus PTS increased significantly with rising concentrations of BC and prolonged exposure time (p < 0.001). Among the concentrations evaluated, BC exhibited the most pronounced antiparasitic activity against PTS at 64 and 128 µM/mL, achieving complete protoscolicidal effects after 30 and 20 min, respectively. Furthermore, the calculated CC50 values were 161.3 µM/mL for THLE-2 cells and 75.6 µM/mL for HepG2 cells. Treatment of PTS with the BC dose-dependently reduced the relative expression level of the GST, TRx, and TPx genes (P < 0.001); while significantly increased the reactive oxygen species in the PTS.

Conclusion

The results of the study showed that BC had a significant protoscolicicidal effect on E. granulosus PTS, which increased parasite death by reducing the expression of antioxidant genes, indicating a direct effect on their defense system and metabolic pathways. Also, BC had a favorable selective effect on HepG2 cancer cells and showed less toxicity than normal THLE-2 cells, which confirms its high selectivity index. Future studies can focus on developing novel drug delivery formulations and investigating signaling pathways related to oxidative stress and apoptosis in parasites to optimize the antiparasitic and anticancer effects of BC.