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Aderans Research & Development

Research on cepharanthine and what is fullerene with antioxidant properties?

Biotechnology companies are successful in discovering a new substance useful for hair growth or restoration with their accumulated technologies and research.
We had an interview with Dr. Inui who is engaged in research on hair science on the front line.

In recent years, research on hair science has leapt onto the center stage of dermatology. A secret of “Why is your hair losing?” has been elucidated for the last 10 years utilizing molecular biology techniques and thus research on rational treatment has been rapidly progressed.

As a result, androgenic alopecia can now be treated at the hospital as a dermatological disease. Specifically, you can now purchase a “topical agent”, hair restoration product or hair growth product which contains active ingredients for hair thinning as typified by minoxidil at the pharmacy.

You can take an “oral drug”, finasteride, which blocks a causative substance of androgenic alopecia, 5-alpha reductase, by asking your doctor to prescribe it. Most recently, research on androgenic alopecia has been conducted from all angles of hair science. Of all, Dr. Shigeki Inui, Associate Professor of Department of Regenerative Dermatology, Osaka University Graduate School of Medicine is known to be involved in several interesting researches on hair. We listened to the details of his research in “Aderans Plus” Vol.1. In the research, he has found that special narrow-band red LED light reaches dermal papilla and helps facilitate hair growth. Biotechnology companies are successful in discovering a new substance useful for hair growth or restoration with their accumulated technologies and research and frequently ask Dr. Inui to perform research on the substance from the scientific point of view.

The interview with Dr. Inui who is engaged in hair science on the front line about “cepharanthine”, “fullerene” and “novel treatment” is as follows:

Historical cepharanthine revives with new evidence

What kind of substance is cepharanthine?

Cepharanthine is an alkaloids* xtracted from menispermaceous plant, Stephania cepharantha. Stephania cepharantha which is native to China and Taiwan had been used as an indigenous medicine. Bunzo Hayata, a botanist of Taipei Imperial University reported it under the binomial nomenclature of Stephania cepharantha Hayata for the first time in 1914. Then, Heisaburo Kondo, Doctor of Pharmacy, purified its active ingredient in 1934 and named it “cepharanthine “after its binomial nomenclature. Originally, Chinese and Taiwanese seemed to take it as indigenous medicine or Chinese herbal medicine.

Menispermaceous plant, Stephania cepharantha, which is native to China and Taiwan had been used as an indigenous medicine.
Bulk powder of cepharanthine extracted from Stephania cepharantha

It is a plant known for a long time, isn’t it? How was it used in Japan?

Cepharanthine was initially used for the treatment of tuberculosis or leprosy.Later, with the advancement of research in the substance, the drug was demonstrated to have biomembrane stabilizing activity, antiallergic action and immunoregulatory activity. Then, it has long been used as an oral drug listed in the NHI (National Health Insurance) drug price standard for the treatment of radiation-induced leukopenia, alopecia areata, alopecia pityroides, exudative otitis media and viper bite.

What made you pay attention to cepharanthine?

Cepharanthine had already been covered by health insurance as a treatment of alopecia areata and the strength of recommendation for its oral drug was C1 (=may consider performing it) in “Clinical Practice Guideline on Alopecia Areata 2010”. However, the topical drug of cepharanthine was rated as C2 (=do not recommend because of no evidence) in the “Clinical Practice Guideline on Androgenic Alopecia 2010”. Clinical practice guidelines require articles published by academic societies. The Guideline Committee makes a judgment whether to recommend or not based on the presence or absence of articles with evidence-based data. Thus, if there is no article showing how effective it is, it is unable to make a recommendation. Thus, it is rated as being unable to make a recommendation because it has no evidence showing that it is effective. After that, topical lotion of cepharanthine, Crow® (Kakenshoyaku), commercially available went out of production and thus topical treatment with cepharanthine is no longer available.

However, there have been voices from many clinicians, “It is effective in some cases”. Some of my patients used the topical one. It is true that there are some patients whom it is effective. Not everyone says “very effective”, but almost everyone says “moderately effective”. When I asked a dermatologist, he said to me, “It is effective in some cases”. Just because it had no medical evidence, it became no longer available.

You started research on cepharanthine in response to those voices, didn’t you?

We investigated its effects on hair growth using ADS cepharanthine, cepharanthine incorporated in liposomes basically and clinically.

growth using ADS cepharanthine, cepharanthine incorporated in liposomes basically and clinically. First, cepharanthine 0.1 μg/mL was administered to cultured dermal papilla cells with androgenic alopecia and the level of IGF-ImRNA, growth factor which activates the action of hair matrix cells, was increased. When administered orally cepharanthine 10 mg in adult patients, the blood concentration of cepharanthine was 1 ng/mL, which was markedly lower than when administered topically. This result indicates that topical cepharanthine with higher local concentrations is a promising one because it is expected to facilitate hair growth induced by IGF-I.

Then, we performed a 6-month clinical study on topical application of ADS cepharanthine lotion in 22 adult men with androgenic alopecia and found that the lotion tended to increase the number of hairs and the diameter of hair (p<0.1) and significantly increased the speed of hair growth (p<0.01). These findings indicated that ADS cepharanthine could be a novel hair care ingredient for androgenic alopecia.

An old drug called as cepharanthine is expected to bring about a renaissance of hair care which went into decline once by new evidence.

Is cepharanthine externally applied as a topical preparation? How about is the drug as an oral one?

It can be possible as orally or by injection but I think it is not used now. Topical cepharanthine was provided for adexperimental purposes this time last year. When applying it to the back skin of mice in order to observe the induction of hair growth phase, we obtained data showing that the hair growth phase was induced earlier in mice treated with cepharanthine.

Have you finished preparing an article on the research?

Now, I am in the process of preparing a manuscript based on these data.

What is fullerene which protects scalp and hair by its antioxidant properties?

This issue introduces Vitamin C60 BioResearch Corporation which deals with fullerene(refer to page 11). When did you start research on fullerene?

It was quite a long time ago. I started the research around in 2000 just after returning from study abroad. More than ten years have passed since I started.

What antioxidant properties do fullerene have?

Reactive oxygen species are also known to be free radicals, an oxygen molecule with an extra electron which causes cell damage. Free radicals are generally treated as a villain, while they also have positive effects such as bactericidal action in the body. Thus, it is not that everything about free radicals is bad. However, if they exert their effects too much, they may damage themselves. Thus, it is difficult to deal with. It is antioxidants that play an active role when free radicals exert their effects too much.

I hear that beauty care for maintaining healthy skin, that is, antiaging treatment, using fullerene has a good reputation.

The reason why ultraviolet light causes age spots, wrinkles and inflammation is that ultraviolet light induces free radical formation in skin. Free radicals induce oxidative stress leading to stimulation of melanin-producing melanocytes, which causes the formation of age spots.This is why eliminating free radicals can block the formation of melanin causing age spots. As fullerene has strong antioxidant properties, I think it has effects to eliminate free radicals. Regarding fullerene, its skin whitening effect was initially published in an article. There are some cases where facial pores are conspicuous by pigmentation. When applied fullerene to the facial skin, the amount of melanin is reduced. There are a variety of skin whitening products. Products containing fullerene have a good reputation.

How is a skin whitening product involved in hair growth?

We conducted a study in which men applied the product to their scalp in order to investigate hair growth and found that it helped speed up hair growth. We infer from the study results that the product may have an effect of protecting cells. Based on the results from the study conducted with a South Korean study group, it may inhibit the stimulation of factors involved in the hair growth suppression. Potent drugs containing fullerene having the similar effects as Propecia may emerge. In that case, it is necessary to investigate their efficacy and safety basically and clinically.

It is an era when the combination of treatments can be possible according to hair conditions.

I guess that substances such as cepharanthine or fullerene which have protecting effects of scalp from which hair is falling out and hair will attract attention in the future. What kind of treatment do you look forward to?

It will be something which can be added on an oral drug. For example, if a person takes already Propecia, finasteride, an add-on therapy is better. I think that combining a treatment such as LED irradiation with an oral drug freely based on the patient’s hair conditions will be a reasonable hair growth therapy.

It is more effective to combine an oral drug with LED irradiation than irradiating LED to the site where a topical drug is applied. This means that a person taking an oral drug like Propecia and receiving hair treatment at the beauty salon or doing self-treatment undergoes LED irradiation.

Interviewer/writer: Akiyoshi Sato Photographer: Naoyuki Tamura

History of development, products and services based on research of Aderans
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