《中国畜牧兽医》 ›› 2018, Vol. 45 ›› Issue (12): 3587-3593.doi: 10.16431/j.cnki.1671-7236.2018.12.033

• 基础兽医 • 上一篇    下一篇

莫西菌素在畜牧业中的应用研究进展

李娇, 李庆山, 徐凤波   

  1. 南开大学化学学院元素有机化学国家重点试验室, 天津 300071
  • 收稿日期:2018-04-16 出版日期:2018-12-20 发布日期:2018-12-21
  • 通讯作者: 徐凤波 E-mail:xufb@nankai.edu.cn
  • 作者简介:李娇(1992-),女,河北保定人,硕士,研究方向:阿维菌素系列药物衍生化,E-mail:lijiao@mail.nankai.edu.cn
  • 基金资助:

    南开大学校企合作项目(2014061)

Research Progress of Moxidectin in Animal Husbandry

LI Jiao, LI Qingshan, XU Fengbo   

  1. State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, China
  • Received:2018-04-16 Online:2018-12-20 Published:2018-12-21

摘要:

莫西菌素(moxidectin,MOX)是由链霉菌发酵产生的奈马菌素经衍生化得到,具有良好的驱虫活性且对哺乳动物安全,主要应用于畜牧业。莫西菌素相较于其他阿维菌素类药物具有更好的脂溶性和水溶性,在动物体内脂肪组织中分布最高。莫西菌素通过与γ-氨基丁酸(GABA)结合,使Cl-大量内流造成神经膜电位超极化,导致虫体麻痹死亡。给药途径和动物生理状况的不同会影响其峰血浆浓度和药物半衰期。莫西菌素在牛、羊、犬等动物体内具有很好的驱虫活性,其应用范围从哺乳动物逐渐扩展到鸟类,防治对象从线虫逐渐扩展到螨虫和部分病原菌,研究方向也从驱虫活性延伸至治疗人类疾病。随着莫西菌素应用范围的扩大和时间的延长,耐药性开始出现,可以采用莫西菌素和其他药剂混合等方式降低耐药性的产生速度。探究其更广泛的作用,需要不同研究领域研究人员的共同努力。

关键词: 莫西菌素; 药代动力学; 药效学; 耐药性

Abstract:

Moxidectin (MOX) is derived from derivatization of nemadectin produced by Streptomyces (Cyanneogrisens noncyanogenus),which has good insect repellent activity and is safe for mammals,and it is mainly used in animal husbandry.Moxidectin has better fat-soluble and water-soluble than other avermectin drugs,and has the highest distribution in adipose tissues of animals.Moxidectin binds to GABA,and neural membrane potential hyperpolarization is caused by massive influx of Cl-,resulting in the death due to the insect's body paralysis.Differences in the route of administration and the physiological condition of animals would affect the peak concentration and depletion half-lives.Moxidectin has good insect repellent activity in animals such as cattle,sheep and dogs.The application range of moxidectin gradually expands from mammals to birds,and the control objects gradually extend from nematodes to mite and several kinds of germs.The research direction extends from anthelmintic activity to the treatment of human diseases.With the increase of the application range of moxidectin and the prolongation of time,the drug resistance began to appear,and the rate of drug resistance could be reduced by the combination of moxidectin and other agents.Exploring the wider role of moxidectin requires the efforts of researchers in different fields.

Key words: moxidectin; pharmacokinetics; pharmacodynamics; drug resistance

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