Aires André de Lima, Ximenes Eulália Camelo Pessoa Azevedo, Barbosa Vanessa Xavier, Góes Alexandre José da Silva, Souza Valdênia Maria Oliveira, Albuquerque Mônica Camelo Pessôa de Azevedo
Laboratório de Imunopatologia Keizo Asami (LIKA), Universidade Federal de Pernambuco, Recife, Pernambuco, Brazil; Centro de Ciências da Saúde - Departamento de Medicina Tropical, Universidade Federal de Pernambuco, Recife, Pernambuco, Brazil.
Centro de Ciências Biológicas - Departamento de Antibióticos, Universidade Federal de Pernambuco, Recife, Pernambuco, Brazil.
Phytomedicine. 2014 Feb 15;21(3):261-7. doi: 10.1016/j.phymed.2013.08.012. Epub 2013 Sep 30.
The activity of β-lapachone (3,4-dihydro-2,2-dimethyl-2H-naphthol[1,2-b]pyran-5,6-dione, β-lap) against different stages of Schistosoma mansoni was investigated in mice. Mice infected with 50 cercariae (BH strain) were intraperitoneally treated at a dose of 50 mg/kg for 5 consecutive days, starting on the 1st, 14th, 28th and 45th days after infection, to evaluate the effect of β-lap on skin schistosomula, lung schistosomula, young worms (before oviposition) and adult worms (after oviposition), respectively. All animals were euthanized 60 days after infection. β-Lap significantly reduced (p<0.001) the number of worms in 29.78%, 37.2%, 24.2% and 40.22% when administered during the phases of skin schistosomula, lung schistosomula, young worms and adult worms, respectively. Significant reduction was also achieved in terms of female burden. In all groups, there was significant reduction in the number of eggs and granulomas in the hepatic tissue. When the intervention was performed during the phase of adult worms, β-lap reduced the size of hepatic granulomas and changed the oogram pattern, lowering the percentage of immature eggs and increasing the percentage of mature and dead eggs. Our data indicate that β-lap has moderate antischistosomal properties. Its molecule may also be used as a prototype for synthesis of new naphthoquinone derivatives with potential schistosomicidal properties. Further studies with different formulations containing β-lap are needed to clearly establish the best dose and route of administration and its mechanism of action against schistosomes.
在小鼠中研究了β-拉帕醌（3,4-二氢-2,2-二甲基-2H-萘并[1,2-b]吡喃-5,6-二酮，β-lap）对曼氏血吸虫不同发育阶段的作用。用50只尾蚴（BH株）感染小鼠，从感染后的第1、14、28和45天开始，以50mg/kg的剂量连续5天腹腔注射，分别评估β-lap对皮肤期血吸虫、肺期血吸虫、幼虫（产卵前）和成虫（产卵后）的影响。感染60天后对所有动物实施安乐死。当在皮肤期血吸虫、肺期血吸虫、幼虫和成虫阶段给药时，β-lap分别使虫体数量显著减少（p<0.001），减少率分别为29.78%、37.2%、24.2%和40.22%。在雌虫负荷方面也实现了显著降低。在所有组中，肝组织中的虫卵和肉芽肿数量均显著减少。当在成虫阶段进行干预时，β-lap减小了肝肉芽肿的大小并改变了虫卵图谱模式，降低了未成熟卵的百分比，增加了成熟卵和死卵的百分比。我们的数据表明β-lap具有中等抗血吸虫特性。其分子也可作为合成具有潜在杀血吸虫特性的新萘醌衍生物的原型。需要对含有β-lap的不同制剂进行进一步研究，以明确确定最佳剂量和给药途径及其对血吸虫的作用机制。
