Use of oligosaccharides molecule in preparing contraceptive medicament

A technology of contraceptives and oligosaccharides, which is applied in the field of medicine to achieve the effect of improving the quality of life and health index, with small side effects and simple structure

Inactive Publication Date: 2009-01-28
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, contraceptives are not without contraindications and side effects. Patients with severe cardiovascular diseases, liver nephritis, endocrine diseases, tumors or blood diseases should not take them. Side effects such as dizziness, nausea, vomiting, and menstrual cycle disorders will also be accompanied by improper medication or the type of medication. produce

Method used

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  • Use of oligosaccharides molecule in preparing contraceptive medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1 Structural simulation experiment

[0016] The present invention adopts the homology modeling (Modeller8.0 program) method to obtain the three-dimensional structure of LYC3 protein, and uses the Gromacs program to perform 3ns molecular dynamics simulation, further optimizes the modeled structure, and finally uses the Ramachandran diagram to evaluate the amino acid side chain, All residues except glycine were found to be within reasonable range. The simulation results show that most of the oligosaccharides that can be combined with the LYC3 protein structure are the C 4 -C 20 , Sugar molecules with a degree of polymerization of 1-1000. Since LYC3 is considered to be an indispensable protein in the process of sperm-egg binding in sperm, these sugars as LYC3 inhibitors have the potential to be prepared as contraceptive drugs.

Embodiment 2

[0017] Embodiment 2 Molecular interaction experiment

[0018] The present invention further uses BIACore3000 macromolecule interaction instrument (Biacore AB, Uppsala, Sweden) to investigate the binding strength between the two. First, the LYZ3 protein storage solution was prepared into 80ul of 20-50ug / ml solution with sodium acetate buffer solution (acetic acid-sodium acetate) with pHs of 5.5, 5.0, 4.5, and 4.0, respectively, and their comparison with the CM5 standard sensor chip (research Level, molecular interaction instrument, Biacore AB, Uppsala, Sweden, 1161036) pre-binding test, the results found that the binding amount and kinetics were the best when the pH was 5.0, so this condition was used for protein coupling. The standard amino coupling kit of Biacore Company was used for coupling, that is, NHS / EDC (N-succinimide / [1-ethyl-3-(3-dimethylaminopropyl)-formyl di amine hydrochloride]) to activate the surface of the chip, control the time and flow rate so that the amoun...

Embodiment 3

[0019] Embodiment 3 sperm-egg combination experiment

[0020] First, the present invention prepares the antibody of LYC3: five adult female rabbits are used to produce the antibody against human LYZ3 gene. The pre-immune serum was first obtained by heart puncture, and then each rabbit was injected with 50-200ug / 0.2ml purified recombinant SLLP1 protein emulsified with an equal volume of complete Freund's adjuvant emulsion, and injected with the same antigen emulsified with incomplete Freund's adjuvant emulsion 14 days later to boost immunity. A booster immunization was given at least twice every 14 days. For each immunization, half of the antigen was injected intramuscularly in the leg of the rabbit, and the other half was injected subcutaneously on both sides of the back. On the 9th day after the last immunization injection, the post-immunization serum was obtained by cardiac puncture, and the antiserum obtained by centrifuging at 1750×g for 10 min in a separation tube (Bect...

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Abstract

The invention belongs to the field of medicine, and more particularly relates to the new usage of oligosaccharide molecule in the preparation of combined oral contraceptive pill. Although various kinds of combined oral contraceptive pills exist, the patients who have serious angiocardiopathy, hepatonephritis, endocrine disease, tumour or hematonosis are not fit for taking the combined oral contraceptive pills, and the side effects such as dizziness, nauseation, vomit and irregular menstrual period can be generated along with the unsuitable dose or the sorts of medicine. The invention provides the new usage of oligosaccharide molecule in the preparation of combined oral contraceptive pill, the degree of polymerization of oligosaccharide which is the sugar component of C4-C20 is 1-1000. The oligopolymerization micromolecule sugar is native compound, has low molecular weight and simple structure, and the combined oral contraceptive pill prepared by the oligosaccharide molecule has high efficiency, good water-solubility, low cost and convenient (external) use; furthermore, the hormone or physiological structure is not changed, the side effects for the human body are low, and the living quality and health index of people are further improved.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the new application of oligosaccharide molecules in the preparation of contraceptive drugs. Background technique [0002] As the name suggests, the contraceptive pill is a drug used to prevent pregnancy and control birth. It was first developed in 1954. Contraceptives are widely used, mainly for women, including intravaginal suppositories, jelly, foams, etc., and oral or injectable contraceptives, such as estrogen and progesterone preparations. Tens of millions of people in the world are using oral contraceptives for women now, and their efficacy is very high, generally up to 99%. Long-term contraceptives are made of long-acting estrogen and synthetic progesterone. It is absorbed from the stomach and intestines and stored in fat tissue for slow release to play a long-term contraceptive effect. Taking the medicine once can prevent pregnancy for one month, and the effective rat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7004A61K31/7016A61K31/702A61K31/715A61P15/18
Inventor 余龙胡海荣唐丽莎
Owner FUDAN UNIV
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