Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1996-03-27
1998-01-20
Dees, Jose G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514178, 552542, 552543, 552544, A61K 31575, C07J 900
Patent
active
057101434
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP94/01631 filed Sep. 30, 1994.
TECHNICAL FIELD
The present invention relates to anti-obesity agents, more specifically to anti-obesity agents which comprise as an active ingredient 3-ketosteroid compounds having ketone groups at the C.sub.3 position of the cholestane skeletons.
BACKGROUND OF THE INVENTION
Obesity is a condition under which the proliferation of tissues of body-composing lipids is increased abnormally. This abnormal condition is produced when energy intake is continuously greater than energy consumption, with the resulting excess energy being converted into neutral lipid which is accumulated in lipid tissues.
Obesity is important as a risk factor of the onset of diseases represented by geriatric diseases from hygienic and cosmetic viewpoints. Harmful influences of obesity have been recognized for a long time in advanced nations. Agents for preventing and/or treating obesity which have been developed until now have side effects or produce unsatisfactory effects.
JP A 5-170651 discloses that anti-obesity agents which comprise 4-cholestene-3-one as an active ingredient have a body lipid-inhibiting effect and present little or no toxicity. However, there still exists a need for more effective anti-obesity agents with less or no side effects and lower toxicity.
Therefore, an object of the present invention is to provide more effective anti-obesity agents with less or no side effects and lower toxicity. Another object of the present invention is to provide food products which are useful for preventing and/or treating obesity.
DISCLOSURE OF THE INVENTION
The inventors found that 3-ketosteroid compounds having ketone groups at the C.sub.3 position of the cholestane skeletons produce a high anti-obesity effect and have less or no side effects and lower toxicity. The present invention was accomplished on the basis of these findings. The present invention provides anti-obesity agents which comprise 3-ketosteroid compounds as an active ingredient. The present invention also provides food products which contain anti-obesity agents comprising 3-ketosteroid compounds as an active ingredient.
The present invention further provides pharmaceutical compositions which comprise 3-ketosteroid compounds as an active ingredient and pharmaceutically acceptable carriers.
The present invention also provides a method for preventing and/or treating obesity which comprises administering an effective amount of a 3-ketosteroid compound to a human.
The anti-obesity agents of the present invention show substantially no toxicity and hence are useful.
BRIEF DESCRIPTION OF THE DRAWINGS
FIG. 1 shows the time course of the average body weights of CDF1 mice in various experimental groups.
FIG. 2 shows the average intraperitoneal lipids in CDF1 mice in various experimental groups at the end of feeding.
FIG. 3 shows the time course of the average body weight of CDF1 mice treated with 6-hydroxy-4-cholestene-3-one.
FIG. 4 shows the average intraperitoneal lipid in 6-hydroxy-4-cholestene-3-one-treated CDF1 mice at the end of feeding.
FIG. 5 shows the time course of the average body weight of CDF1 mice treated with 4-cholestene-3,6-dione.
FIG. 6 shows the average intraperitoneal lipid in CDF1 mice treated with 4-cholestene-3,6-dione.
FIG. 7 shows the average intraperitoneal lipid in SD rats treated with 5-cholestene-3-one.
BEST MODE FOR CARRYING OUT THE INVENTION
The anti-obesity agents of the present invention comprise 3-ketosteroid compounds as an active ingredient. Any 3-ketosteroid compounds can be used, provided that they have an anti-obesity effect. Preferred is at least one compound selected from the group consisting of 5-cholesten-3-one, 5 .beta.-cholestan-3-one, cholesta-4,6-dien-3-one, 6 .beta.-bromo-4-cholesten-3-one, 6-hydroxy-4-cholesten-3-one and 4-cholestene-3,6-dione. 5-Cholesten-3-one, 6-hydroxy-4-cholesten-3-one and 4-cholestene-3,6-dione are more preferred as having a higher anti-obesity effect.
5-Cholesten-3-one, 5 .beta.-cholestan-3-one, cholesta-4,6-dien-3-one, 6 .be
REFERENCES:
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G.B. Forbes et al., Hormonal Response to Overfeeding, Am. J. Clin. Nutr. 49:608-11, (1989).
L. Abrahamsson & H. Hackl, Catabolic Effects and the Influence on Hormonal Variables Under Treatment with Gynodian-Depot.RTM. or Dehydroepiandrosterone (DHEA) Oenanthate, Maturitas, 3:225-234, (1981).
K. Kusuhara et al., The Pathogenesis of Amenorrhea Related with Simple Weight Loss, Jpn. J. Fertil. Steril., 26:7-15 (1981). (In Japanese with English language summary).
European Search Report, Apr. 25, 1997.
Enomoto Kotaro
Nakata Tadashi
Shimizu Takeshi
Suzuki Kunio
Badio Barbara
Dees Jos,e G.
Institute of Physical and Chemical Research
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