KR102028519B1 - Compositions for anti-parasitic activity of scutica in a cultivated fish - Google Patents

Abstract

The present invention provides a Scoochika anti-worm composition which exhibits excellent anti-worm effect against a Scoochi-kachi, which is a kind of ciliates causing parasitic diseases on the flounder.

Description

Compositions for anti-parasitic activity of scutica in a cultivated fish}

FIELD OF THE INVENTION The present invention relates to a Scoochika antiworm composition, and more particularly to a cultured fish Squatchica antiworm composition.

Scutica (scutica) is a fish disease bacterium that seriously damages domestic flounder culture. Flounder infected with Sukuchika is anemia, weight loss, color change, enteritis, excessive secretion of mucus, scaly loss, bleeding or chipped white spots and skin necrosis. It has a long-term pathological response to the organs of infection, such as the brain, eyes, muscles, gills, liver, kidneys, intestines, and stomach, leading to death. Squatch caterpillar belonging to the protozoan cilia, the polka dots are 20 ~ 40μM in size and have cilia throughout the body and are actively active in water. It is not a parasitic life, but a protozoan that resides on the bottom or wall of a tank, and large amounts of halibut are killed by administering a lot of food at the time of seedling production or by mass-modifying during overdose breeding. Representatively, it is not only induced in fish body surface and fins, but also in kidney, blood vessels, and brain tissues. Unlike parasites of fish, it is difficult to treat during infection because it invades brain tissues through blood vessels. It has been reported to kill olive flounder through tissue destruction. Once an infection has occurred, avoid overcrowding and remove organic matter from the bottom of the tank.When a Scotchworm is parasitic to the outside, such as body surface, gills and fins, 1 hour with 100 to 150 ppm formalin. If you bathe, you can easily rescue, but parasitic brain is known to be unable to rescue. In order to prevent the disease, formalin is banned due to its toxic components, and in addition, the method of bathing with toxic or irritating substances such as hydrogen peroxide, stabilized chlorine, malachite green, formaldehyde, and sulfuric copper is used. In order to solve these problems, there have been various studies on the insecticide insecticides using weak toxic ingredients to solve these problems. In this regard, Korean Registered Patent No. 0831558 discloses a succinic insecticide.

However, in the case of the prior art, there is a limit in showing a sufficient anti-worm effect for eradicating Schizka.

The present invention is to solve a number of problems, including the above problems, it is an object of the present invention to provide a cultured fish Scoochika anti-worm composition exhibiting excellent anti-worming effect against the Scoochika. However, these problems are exemplary, and the scope of the present invention is not limited thereby.

According to one aspect of the present invention, there is provided an anti-squatchworm composition comprising a compound having the following chemical formula as an active ingredient:

(Wherein R is methyl (CH _3- ), ethyl (CH ₃ CH _2- ) or propyl (CH ₃ CH ₂ CH _2- ).

According to another aspect of the invention, the fish comprising the step of administering a therapeutically effective amount of the Shuden compound having a chemical formula to a Squatch worm infected fish, or to a tank or aquaculture farm containing the fish to be cultured Provided are methods and methods for the treatment and prevention of Squatica infections in:

(Wherein R is methyl (CH _3- ), ethyl (CH ₃ CH _2- ) or propyl (CH ₃ CH ₂ CH _2- ).

According to one embodiment of the present invention made as described above, it is possible to implement an excellent anti-worm effect against the Scoochika worms that can effectively reduce the mortality of Scoochika infected fish. Of course, the scope of the present invention is not limited by these effects.

1 is a structural formula showing the structures of the Shuden compound-6, the Shuden compound-7, and the Shuden compound-8 of the present invention which exhibit excellent anti-worming effect.
Figure 2 is a photograph observing the morphological changes and motility after treatment with DMSO to Scoochica insects to confirm the anti-worm effect of the Shuden compound of the present invention.
Figure 3 is a photograph observing the morphological changes and motility after treatment with the concentration of Shuden compound-6 in the Scoochi cara.
Figure 4 is a photograph observing the morphological changes and motility after the treatment of the Sudden compound-7 in Scoochica by concentration.
Figure 5 is a photograph observing the morphological changes and motility after treatment with the concentration of Shuden compound-8 in the scotch car.
Figure 6 is a graph analyzing the anti-worm effect after the treatment of the Shudden compound-6 in Scoochica by concentration.
Figure 7 is a graph analyzing the anti-worm effect after treatment with the concentration of Shuden compound-7 in the Scoochi cara.
8 is a graph analyzing the anti-worm effect after the treatment of the Shuden compound-8 in the concentration of Scoochika.

Definition of Terms:

The term "scutica" as used in this document is a disease mainly caused by ulcers caused by Scutica parasites in the epithelial cells (lower layer) of the flounder. It is causing the most serious damage in the domestic flounder culture. Recently, about 20 species of schizocci are caused by schizocaries, and the species that are particularly problematic in domestically raised flounder are known as Philasterides dicentrarchi, Miamiensis avidus, and Uronema marinμM . It often occurs in fry.

As used herein, the term "pseudane" refers to a hydroquinoline derivative having the general formula of 2-n-alkyl-4-hydroxyquinoline with whitening activity secreted by Pseudomonas bacteria.

Detailed description of the invention:

According to one aspect of the present invention, there is provided an anti-squatchworm composition comprising a compound having the following chemical formula as an active ingredient:

(Wherein R is methyl (CH _3- ), ethyl (CH ₃ CH _2- ) or propyl (CH ₃ CH ₂ CH _2- ).

In the composition, the compound may be sudden-VI (2-hexyl-4 (1H) -quinolinone), Ⅶ (2-heptyl-4 (1H) -quinolinone), or Ⅷ (2-octyl-4 (1H)- quinolinone).

According to another aspect of the invention, the fish comprising the step of administering a therapeutically effective amount of the Shuden compound having a chemical formula to a Squatch worm infected fish, or to a tank or aquaculture farm containing the fish to be cultured Provided are methods and methods for the treatment and prevention of Squatica infections in:

(Wherein R is methyl (CH _3- ), ethyl (CH ₃ CH _2- ) or propyl (CH ₃ CH ₂ CH _2- ).

The pharmaceutical composition of the present invention may comprise a pharmaceutically acceptable carrier. The composition comprising a pharmaceutically acceptable carrier may be a variety of oral or parenteral formulations, but is preferably a parenteral formulation. When formulated, diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrating agents, and surfactants are usually used. Solid preparations for oral administration include tablets, pills, powders, granules, capsules and the like, and such solid preparations contain at least one excipient such as starch, calcium carbonate, sucrose or lactose, gelatin, or the like in one or more compounds. Mix is prepared. In addition to simple excipients, lubricants such as magnesium stearate, talc and the like can also be used. Liquid preparations for oral administration include suspensions, liquid solutions, emulsions, and syrups, and various excipients such as wetting agents, sweeteners, fragrances, and preservatives, in addition to commonly used simple diluents such as water and liquid paraffin, may be included. have. Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, lyophilized preparations, suppositories. As the non-aqueous solvent and the suspension solvent, propylene glycol, polyethylene glycol, vegetable oil such as olive oil, injectable ester such as ethyl oleate, and the like can be used. As the base of the suppository, witepsol, macrogol, tween 61, cacao butter, laurin butter, glycerogelatin and the like can be used.

The pharmaceutical composition is any one selected from the group consisting of tablets, pills, powders, granules, capsules, suspensions, solutions, emulsions, syrups, sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, lyophilized preparations and suppositories. It can have one formulation.

The pharmaceutical composition of the present invention may be administered orally or parenterally. When administered parenterally, it is possible to administer via various routes such as intravenous injection, intranasal inhalation, intramuscular administration, intraperitoneal administration, and transdermal absorption. .

The composition of the present invention is administered in a pharmaceutically effective amount.

As used herein, the term “pharmaceutically effective amount” means an amount sufficient to treat a disease at a reasonable benefit / risk ratio applicable to medical treatment, with an effective dose level of the subject type and severity, age, sex, drug Can be determined according to the activity of the drug, the sensitivity to the drug, the time of administration, the route of administration and the rate of release, the duration of treatment, factors including the drug used concurrently and other factors well known in the medical arts. The pharmaceutical composition of the present invention may be administered at a dose of 0.1 mg / kg to 1 g / kg, more preferably at a dose of 1 mg / kg to 500 mg / kg. On the other hand, the dosage may be appropriately adjusted according to the age, sex and condition of the patient.

The pharmaceutical composition of the present invention may be administered at a dose of 0.1 mg / kg to 1 g / kg, more preferably at a dose of 0.1 mg / kg to 500 mg / kg. On the other hand, the dosage may be appropriately adjusted according to the age, sex and condition of the patient.

Hereinafter, the present invention will be described in more detail with reference to Examples. However, the present invention is not limited to the embodiments disclosed below, but can be implemented in various forms, and the following embodiments are intended to complete the disclosure of the present invention, the scope of the invention to those skilled in the art It is provided to inform you completely.

Example 1 Synthesis of Shudene Compound

According to one embodiment of the invention Pseudoalterompmas sp. Pseudane (Group A) was commissioned to Wuxi, China, to obtain 1 g of each Pseudane family (VI, VII, and VIII) compound by organic synthesis, using HR-MS and NMR. The structure of the compound was verified (FIG. 1).

Example 2: Microscopic Method

In order to prepare a Squawka anti- worm composition of the present invention, after infecting 1/10 Scubachi (Scutica, Uronema marinum ) worms in HINAE cells and 100 μl aliquots in 96-well plate after Shuden compound-6, Shuden compound-7 , And 100 μl of Shudene Compound-8 were added according to the concentration, and the control was treated with DMSO (100 μl) and then incubated at 20 ° C. for 1 to 2 hours. After incubation, the morphological changes and the motility changes of the Schizocara were observed at a magnification of the reverse phase microscope (Carl zeiss, DE / Axio vert. A1) at X200 magnification.

As a result, in the experimental group treated with Shudene compound-6 468 μM, Shudene compound-7 117 μM, Shudene compound-8 117 μM or more compared with the control, it was confirmed that the scotch caries swelled elliptically and the mobility was also reduced (Fig. 2 to Fig. 2). 5).

Example 3 Quantification of the Antiworm Effect of Sudden Compounds

The WST-1 cell proliferation assay system was used to quantify the anti-parasitic activity of the Shuden compound of the present invention. First, after treatment with Shudene compound-6, Shudene compound-7, and Shudene compound-8 in Scoochika, 10 μl of Primx WST-1 was added per well after 1 to 2 hours, and absorbance (450 nm) was obtained using an ELISA reader. Measured.

As a result, Shudene Compound-6 treated with 468 μM of at least 98% antiviral efficacy (1.5% survival), Shudene Compound-7 treated with 117 μM of 80% or more potency (17% survival), and Shudene Compound-8 treated with 117 μM 90% or more (survival rate of 6.3%) was shown (see FIGS. 6 to 8 and Tables 1 to 3). The results were confirmed to have an excellent anti-worm effect as a result almost the same as the microscopic observation of Example 1.

Survival rate (%) Control (DMSO) 100 117 μM 44.2 234 μM 16.7 468 μM 1.5 936 μM 2.4 1.872 μM 4.0

Survival rate (%) Control (DMSO) 100 58.5 μM 59.4 117 μM 17 234 μM 8.3 468 μM 0.2 936 μM 0

Survival rate (%) Control (DMSO) 100 58.5 μM 99.8 117 μM 6.3 234 μM 4.8 468 μM 3.2 936 μM 0

In conclusion, the pseudane compound of the present invention can be utilized for the productivity improvement of the flounder fish farming because it exhibits an excellent anti-inflammatory effect against Scoochi caterpillar, a type of ciliates that cause parasitic diseases on the flounder.

Although the present invention has been described with reference to the above-described embodiments, these are merely exemplary, and it will be understood by those skilled in the art that various modifications and equivalent other embodiments are possible. Therefore, the true technical protection scope of the present invention will be defined by the technical spirit of the appended claims.

Claims (3)

An anti-squatchworm composition containing a compound having the following chemical formula as an active ingredient:

(Wherein R is methyl (CH _3- ), ethyl (CH ₃ CH _2- ) or propyl (CH ₃ CH ₂ CH _2- ). The method of claim 1,
Wherein said compound is Shuden-VI, VIII, or VIII A method of treating and preventing Squatic arachnid infection, comprising administering a therapeutically effective amount of a Shuden compound having a chemical formula to a Squatch arachnid infected fish, or treating a fish or aquaculture farm containing the fish to be cultured. :

(Wherein R is methyl (CH _3- ), ethyl (CH ₃ CH _2- ) or propyl (CH ₃ CH ₂ CH _2- ).

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