JPH0621064B2 - Antiparasitic agent containing xanthocillin X monomethyl ether - Google Patents

Description

The present invention relates to a known antibiotic represented by the following chemical structural formula,
It relates to the use of xanthocillin X monomethyl ether. More specifically, it relates to an anthelmintic agent for parasites such as livestock and poultry containing xanthocillin X monomethyl ether.

BACKGROUND ART A large number of compounds having anthelmintic activity are known, and as a substance having anthelmintic activity in a microbial product such as this substance,
Destomycin, hygromycin, avermectin and the like can be mentioned.

Problems to be Solved by the Invention Although a large number of anthelmintic agents are known as described above, parasitic disease is caused in domestic animals such as pigs, horses, cows, sheep, goats, dogs, cats, and poultry animals such as chickens. It is still in fashion and is a serious economic problem.

Infection of parasites causes anemia, malnutrition, weakness, weight loss, damage to the stomach, intestinal wall and other tissues and organs, which is one of the causes of reduced feed efficiency and reduced productivity. The economic loss is large. Therefore, providing a new anthelmintic agent is always a challenge.

Means for Solving the Problems In order to solve the above-mentioned problems, the present invention provides xanthocillin X monomethyl ether [1- (p-hydroxyphenyl)-
2,3-diisocyano-4- (p-methoxyphenyl) -but-1,3-diene] is provided. Xanthocillin X monomethyl ether is K. Ando et al.
(J. Antibiotics 21 , 582-587, 1968), a known antibiotic that has already been reported by Dichotomomyces albus, Aspergis.
llus sp.) and other fungal culture solutions.

This substance has antibacterial activity against Gram-positive and negative bacteria,
It is known to have antiviral activity against Newcastle disease virus, herpes virus, etc., as well as activities such as prostaglandin synthesis inhibition and platelet aggregation inhibition.

However, we have now discovered that the substance has anthelmintic activity against animal parasites.

Animals to which xanthocillin X monomethyl ether is applied as an anthelmintic agent are pigs, horses, rabbits, cows, sheep, goats, chickens,
Examples thereof include domestic animals such as ducks, turkeys, twentieth mice, daikoku rats, guinea pigs, monkeys, dogs, cats, small birds, poultry, laboratory animals, and pets. Examples of parasites of these animals include dogs, cats, cows, goats, horses, chicken tapeworms, horses, pigs, dogs, cats, roundworms of horses, pinworms of horses, horses, pigs,
Sheep, goat rodworm, pig, sheep, dog whipworm, horse roundworm, cow,
Pig, sheep, goat intestinal tuberculosis, cow, sheep, dog's duodenum (hookworm), cow, pig, sheep, goat's hairy nematode, cow, horse, sheep, goat's gastropod, chicken, turkey, Duck caterpillars and cecal worms, cattle,
Horses, sheep, goats, worms of dogs, cows, horses, sheep, goats, pigs,
Various parasites are known, such as flukes that parasitize the livers of dogs and cats, and flukes such as double-mouth flukes that parasitize the fire extinguisher system.

Xanthocillin X monomethyl ether can be used for the treatment and prevention of parasitic infections. The administration method for treatment includes an oral or parenteral method. When administered orally, it is suitable for forced administration of liquid preparations using an administration device such as a gastric tube, administration by mixing with normal feed or drinking water, or ordinary oral administration There is a method of administration in a dosage form such as tablets, capsules, pellets, boluses, powders or soft capsules. When administered parenterally, a water-insoluble formulation such as peanut oil or soybean oil, or a water-soluble formulation such as glycerol or polyethylene glycol is administered subcutaneously, intramuscularly, intravenously, intraperitoneally, etc. by injection. In addition, the general method of administration for the prevention of parasites is to mix it with a commonly used feed and administer it orally. The administration period is not particularly limited for prevention, but it is usually about 2 months for meat chickens,
For pigs, 5 months is often sufficient.

The dose of xanthocillin X monomethyl ether varies depending on the type of target animal and parasite or the administration method. For example, when a liquid preparation is orally administered using a gastric tube to control Ascaris suum, 5 mg / kg or more, preferably 5 mg / kg to 20 mg / kg is administered. In addition, the dose for prevention is preferably 5ppm or more in the feed and 5ppm to 20p.
Administer continuously at a concentration of pm.

Example 1 The following is an example in which xanthocillin X monomethyl ether was orally administered once to a chicken which had already been confirmed to have Ascaridia galli infection to treat the Ascaris suum infection.

Twelve chicks weighing around 60 g per bird were orally infected with about 200 Ascaris suum eggs. Five weeks after the infection with Ascaris, the egg count (EPG) in 1 g of chicken feces was examined to confirm that the eggs were excreted, and the eggs were divided into 4 groups of 3 birds.
The 4th group is xanthocillin X monomethyl ether 5mg /
kg administration group, 10 mg / kg administration group, 20 mg / kg administration group, remaining 1
The group was a non-administration control group to which no xanthocillin X monomethyl ether was administered. Xanthocillin X monomethyl ether was weighed in a dose exactly calculated from the body weight of each chicken, filled into a gelatin capsule, and this was forcibly orally administered by a gastric tube. Each of these chickens is placed in a wire cage bird cage, the excrement that falls from the wire mesh floor is received in a stainless steel saucer, and the larvae excreted every day for 7 days from the day when the drug is started are carefully treated. At the same time as counting, the weight and general condition were observed, and all chickens were dissected on the day of the end of the observation and all internal parasites in the digestive tract were measured to determine the number of remaining worms, and the number of offspring excreted in 7 days In addition, the insecticidal rate was calculated. The results are shown in Tables 1 and 2.

In other words, the excretion rate is regarded as an index that directly expresses the anthelmintic effect of the administered drug. Therefore, first, looking at the excretion rate, the non-administration control group did not have three coexisting insects, and the number of residual insect bodies. Since the rate was 0%, it was 0%.
8% on average in the 5 mg / kg administration group, average in the 10 mg / kg administration group
In the 69.7% and 20 mg / kg administration groups, 100% of the animals were completely eradicated, and most of the medicated groups excreted most of the larvae within 2 days after the administration. That is, a remarkable effect was obtained at a dose of 10 mg / kg or more.

Next, looking at the change in body weight, the weight gain calculated from the difference in body weight between the start and end of the study was 22.4% on average in the administration control group, while it was 20.6% on average in the 5 mg / kg administration group. mg / kg
Mean 21.7% in the administration group, average 24.3% in the 20 mg / kg administration group
The increase in body weight was not significantly different from that in the untreated control group, and there was no significant change in general condition.

Therefore, in this anthelmintic test, a reliable anthelmintic effect of xanthocillin X monomethyl ether was confirmed at a dose of 10 mg / kg to 20 mg / kg.

EFFECTS OF THE INVENTION As shown in Tables 1 and 2, the anthelmintic agent containing xanthocillin X monomethyl ether has a simple and reliable anthelmintic effect against parasites of livestock in an extremely small amount as compared with conventional anthelmintic agents.

 ─────────────────────────────────────────────────── ─── Continuation of the front page (72) Inventor Tadaaki Okada 760 Shimooka-cho, Kohoku-ku, Yokohama-shi, Kanagawa Meiji Seika Co., Ltd. Pharmaceutical Research Laboratory (72) Inventor Taka Shomura 760, Shimo-oka-cho, Kohoku-ku, Yokohama, Kanagawa Haruka Seika Co., Ltd., Pharmaceutical Research Laboratory (72) Inventor, Shoji Sezaki, 760, Shimooka-cho, Kohoku-ku, Yokohama, Kanagawa Meiji Seika Chemicals Laboratory, (72) Inventor, Naoshi Akai, 760, Shimooka-cho, Kohoku-ku, Yokohama-shi, Kanagawa (72) Inventor Shigeharu Inoue, 760 Shimooka-cho, Kohoku-ku, Yokohama-shi, Kanagawa Meiji Confectionery Co., Ltd.

Claims (1)

[Claims] 1. An anthelmintic agent for animals, which comprises xanthocillin X monomethyl ether as an active ingredient.