Application of dequalinium chloride as mouse birth control medicine

A dequinium chloride and rodent technology is applied in the field of rodent birth control drugs to achieve the effects of population control, strong affinity and high activity

Inactive Publication Date: 2015-06-10
SHANGHAI INST OF PLANNED PARENTHOOD RES +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

It has been reported that Lewis oligosaccharide X (ie Lewis X) can bind to mouse sperm, and can specifically inhibit the in vitro fertilization of mice, suggesting that the protein that recognizes Lewis X on the sperm may be involved in the reproductive isolation of mice [9] , but only a guess

Method used

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  • Application of dequalinium chloride as mouse birth control medicine
  • Application of dequalinium chloride as mouse birth control medicine
  • Application of dequalinium chloride as mouse birth control medicine

Examples

Experimental program
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Effect test

Embodiment 1

[0041] Embodiment 1: the application of dequalinium chloride as the birth control drug of mice

[0042] Experiments with different concentrations of CTBS used >50 mouse eggs for each dose, repeated 3 times, and each dose used a total of >150 eggs. The experimental results are as follows: figure 1 As shown, its half-inhibition constant is at 50nM, indicating that dequalinium chloride can well inhibit the in vitro fertilization of mice.

Embodiment 2

[0044] We found that CTBS is expressed in rodent sperm, and CTBS antibody can inhibit in vitro fertilization in mice, but this protein is not expressed in human sperm. Its experimental method is as follows:

[0045] (1) Discovery of CTBS on mouse spermatozoa:

[0046] CTBS on mouse sperm was identified by using Lewis oligosaccharide X (Lewis X, abbreviated as LeX) probe, and it was proved that CTBS can bind to mouse egg zona pellucida.

[0047] (1) First identify the Lewis X receptor, the identification process is as follows Figure 2AAs shown, it includes the identification process of lectin-like proteins that can recognize Lewis X and the identification process of endogenous proteins containing Lewis X modifications. The principle is to modify the surface of bovine serum albumin (BSA) with Lewis X to make the pseudoglycoprotein LeX-BSA, and further modify the pseudoglycoprotein with ultraviolet crosslinking reagent [6-(biotinamido)-2-( p-Azidobenzamido)caproylamino]ethyl-...

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Abstract

The invention relates to an application of dequalinium chloride as a mouse birth control medicine. Researches find that CTBS (di-N-acetylchitobiase) is a unique sperm-egg binding receptor on the sperms of rodents, the inhibitor dequalinium chloride can effectively inhibit in vitro fertilization of a mouse, the semi-inhibition constant is less than 100nM, and the toxic effect on a human body is tiny; the researches also find that the CTBS is expressed on the sperms of rodents, the CTBS antibody can inhibit in vitro fertilization of the mouse, and the protein is not expressed on the sperms of the human body. According to the application provided by the invention, dequalinium chloride is used as a mouse birth control medicine and can effectively control the sperm-egg binding of rodents to achieve the aims of controlling the population quantity of mice and realizing mouse damage control without needing pesticides; moreover, after eating the medicine, the natural enemy of the mice does not cause harm.

Description

technical field [0001] The invention relates to a birth control drug for rodents, in particular to the application of dequalinium chloride as a birth control drug for rodents. Background technique [0002] Dequalinium chloride (Dequalinium chloride, CAS#522-51-0), used as a PKC inhibitor as an anticancer drug, its IC50 is 7-18μM, and it is also a selective melittin-sensitive Potassium channel blocker with an IC50 of 1.1 μM [1，2，3，4] . Recently, it was found that dequalinium chloride can also inhibit the activity of microbial-derived chitin hydrolase at the nanomolar level [5]. Dequalinium chloride has little toxicity to the human body, does not affect human reproduction, and is irritating to the eyes and skin. The lethal dose for mice is: 150-1000 mg / kg body weight orally, 70 mg / kg body weight for subcutaneous injection, and 1.9 mg / kg body weight for intravenous injection; the lethal dose for rabbits and dogs is 500 mg / kg body weight (MSDS). [0003] Di-N-acetylchitobias...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A01N43/42A01P11/00
Inventor 顾一骅徐文平施惠娟杨军
Owner SHANGHAI INST OF PLANNED PARENTHOOD RES
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