大理大学学报 ›› 2019, Vol. 4 ›› Issue (2): 1-4.

• 药学 •    下一篇

白花酸藤果及主成分信筒子醌抗疟活性研究

崔淑君,陈浩,刘健,肖朝江,沈磊,姜北   

  1. (1.大理大学药物研究所,云南大理671000;2.大理大学药学与化学学院,云南大理671000)
  • 收稿日期:2018-09-17 修回日期:2018-11-06 出版日期:2019-02-15 发布日期:2019-02-15
  • 通讯作者: 姜北,教授,博士,E-mail:jiangbei@dali.edu.cn.
  • 作者简介:崔淑君,硕士研究生,主要从事天然产物药理学研究.
  • 基金资助:
    国家自然科学基金资助项目(81460532)

Study on Antimalarial Activity of Embelia ribes and Its Main Constituent Embelin

Cui Shujun, Chen Hao, Liu Jian, Xiao Chaojiang, Shen Lei, Jiang Bei   

  1. (1. Institute of Materia Medica, Dali University, Dali, Yunnan 671000, China;2.College of Pharmacy and Chemistry, Dali University,
    Dali, Yunnan 671000, China)
  • Received:2018-09-17 Revised:2018-11-06 Online:2019-02-15 Published:2019-02-15

摘要: [摘要]目的:探索白花酸藤果及其主成分信筒子醌抗疟活性与可能的作用机制。方法:采用β-羟高铁血红素形成抑制实验
与约氏疟原虫(BY265RFP 株)感染小鼠四天抑制法相结合的形式,对白花酸藤果与信筒子醌进行体外、体内抗疟活性研
究。结果:白花酸藤果提取物、乙酸乙酯部位均显示出较好的鼠疟抗疟活性,抑制率分别达到25.25%、32.17%;信筒子醌
100 mg/(kg·d)时其抑制率为41.59%。同时白花酸藤果提取物具有一定的β-羟高铁血红素形成抑制活性(IC50 = 500.61 μg/mL),
但信筒子醌几乎无此活性(IC50 > 1 388.89 μg/mL)。结论:白花酸藤果提取物及主成分信筒子醌确实具有一定的抗疟活性,白
花酸藤果抗疟活性应该主要源自信筒子醌,但应该不是通过β-羟高铁血红素形成抑制途径而产生抗疟活性。

关键词: [关键词]抗疟活性, 白花酸藤果, 信筒子醌, 鼠疟, &beta, -羟高铁血红素形成抑制实验

Abstract: 〔Abstract〕Objective: To explore the antimalarial activity and the possible mechanism of Embelia ribes and its main constituent
embelin. Methods: The antimalarial activity of the testing samples were evaluated by in vitro and in vivo assays. And β-hematin
formation inhibitory experiment was selected as in vitro assay while 4-day suppression assay of Plasmodium yoelii(BY265RFP)in
mice was used as in vivo assay. Results: Both of the crude extract and ethyl acetate fraction of E. ribes showed good activities with the
suppression rates of 25.25% and 32.17% against P. yoelii in mice, respectively, while the suppression rate of embelin was 41.59% at
the dose of 100 mg/(kg·d). The results from the β-hematin formation inhibitory experiment indicated that the crude extract of E. ribes
had a certain activity with IC50 = 500.61 μg/mL, but embelin was almost inactive with the IC50 value much bigger than 1 388.89 μg/mL.
Conclusion: Both extract of E. ribes and its main constituent embelin do reveal certain antimalarial activity. The antimalarial activity
of E. ribes should be mainly attributed to embelin, but the antimalarial mechanism of embelin should not come from the pathway of
β-hematin formation inhibition.

Key words: 〔Key words〕antimalarial activity, Embelia ribes, embelin, rodent malaria, β-hematin formation inhibitory experiment