Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Conjugate or complex
Patent
1996-12-30
2000-10-03
Kulkosky, Peter F.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Conjugate or complex
514880, 514456, A61K 706, A61K 3578
Patent
active
061269409
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a hair-growing agent comprising proanthocyanidin as the active ingredient.
BACKGROUND ART
Tannin exists broadly in the plants and has many phenolic hydroxyl groups in the molecule. Tannin is classified into a hydrolyzable tannin that is hydrolyzed with acid, alkali or tannase, and a condensed tannin that is not hydrolyzed. It is known that the condensed tannin includes a simple condensed tannin (proanthocyanidin) which is composed of constitutive flavan-3-ol units and a complex condensed tannin which is composed of constitutive units of flavan-3-ol, caffeic acid and chalcone-.beta.-ol.
It is known that such a condensed tannin has a hair-protecting effect (see Japanese Published Examined Patent Application No. 37884/90). However, the effect is exclusively exerted on the surface of hair as the effect of a cosmetic, and the hair-growing effect of the condensed tannin is unknown. Proanthocyanidin is utilized as an antioxidant (see Japanese Published Unexamined Patent Application No. 16982/86), but the hair-growing effect of proanthocyanidin is unknown.
DISCLOSURE OF THE INVENTION
The present invention relates to a hair-growing agent comprising proanthocyanidin as the active ingredient.
The present invention also relates to the use of proanthocyanidin in preparing a pharmaceutical composition for treating male pattern baldness (alopecia hereditaria). The present invention further relates to a method for treating male pattern baldness by the use of a pharmaceutical composition comprising proanthocyanidin as the active ingredient.
Proanthocyanidin indicates a group of polymer compounds composed of constitutive units of flavan-3-ol derivatives of a formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a hydrogen atom or a hydroxyl group.
Examples of the flavan-3-ol derivatives of formula (I) include catechin, epicatechin, gallocatechin, epigallocatechin, afzelechin, epiafzelechin, etc., and include all their isomers. Proanthocyanidin composed of constitutive units of epicatechin or catechin is more preferably used in the hair-growing agent of the present invention.
Any bonding mode of flavan-3-ol polymers comprising the units of formula (I) is acceptable. For example, diners to be formed by polymerization of two flavan-3-ol units may have any bonding mode of a formula (II): ##STR2## wherein R.sub.1 and R.sub.2 have the same meanings as defined above, and R.sub.3 and R.sub.4 are the same or different and each represents a hydrogen atom or a hydroxyl group. The same or different ones of such bonding modes are combined to give trimers and higher polymers.
Proanthocyanidin to be used in the present invention is a dimer or higher polymer composed of flavan-3-ol derivatives and is preferably a 2- to 10-mer, more preferably a 2- to 5-mer, even more preferably a dimer or trimer. Especially preferred examples of dimers of flavan-3-ol derivatives are epicatechin-catechin co-dimers such as epicatechin-(4.beta..fwdarw.8)-catechin, etc.; epicatechin dimers such as epicatechin-(4.beta..fwdarw.6)-epicatechin, epicatechin-(4.beta..fwdarw.8)-epicatechin, etc.; catechin dimers such as catechin-(4.alpha..fwdarw.8)-catechin, etc. Especially preferred examples of trimers of flavan-3-ol derivatives are epicatechin trimers such as epicatechin-(4.beta..fwdarw.8)-epicatechin-(4.beta..fwdarw.8)-epicatechin, epicatechin-(4.beta..fwdarw.8)-epicatechin-(4.beta..fwdarw.6)-epicatechin, etc.; catechin trimers such as catechin-(4.alpha..fwdarw.8)-catechin-(4.alpha..fwdarw.8)-catechin, etc.; epicatechin-catechin co-trimers such as epicatechin-(4.beta..fwdarw.8)-epicatechin-(4.beta..fwdarw.8)-catechin, etc.
Proanthocyanidin can be extracted and purified from various plants such as grape, kaki (Japanese persimmon), betel palm, apple, barley, Nest-leaf, rhubarb, cinnamon, adzuki bean, raspberry, etc. In addition, it can also be obtained by chemical synthesis.
To extract and purify proanthocyanidin from such plants, any known method such as that mentioned
REFERENCES:
patent: 4508714 (1985-04-01), Lecic et al.
patent: 4517175 (1985-05-01), Twabochi et al.
patent: 4530829 (1985-07-01), Abe
patent: 4698360 (1987-10-01), Masquelier
patent: 5470874 (1995-11-01), Lerner
Kamiya Toshikazu
Kawamura Michio
Kobayashi Yoshinori
Takahashi Tomoya
Tamaoki Tatsuya
Kulkosky Peter F.
Kyowa Hakko Kogyo Co. Ltd.
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