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Inhibition of Rat 5α-Reductase Activity and Testosterone-Induced Sebum Synthesis in Hamster Sebocytes by an Extract of Quercus acutissima Cortex.

Koseki J, Matsumoto T, Matsubara Y, Tsuchiya K, Mizuhara Y, Sekiguchi K, Nishimura H, Watanabe J, Kaneko A, Hattori T, Maemura K, Kase Y - Evid Based Complement Alternat Med (2015)

Bottom Line: Results.Conclusions.BK inhibited androgen-related pathogenesis of acne, testosterone conversion, and sebum synthesis, partially through 5α-reductase inhibition, and has potential to be a useful agent in the therapeutic strategy of acne.

View Article: PubMed Central - PubMed

Affiliation: Tsumura Research Laboratories, Tsumura & Co., 3586 Yoshiwara, Ami-machi, Inashiki-gun, Ibaraki 300-1192, Japan.

ABSTRACT
Objective. Bokusoku (BK) is an extract from the Quercus cortex used in folk medicine for treatment of skin disorders and convergence, and is present in jumihaidokuto, a traditional Japanese medicine that is prescribed for purulent skin diseases like acne vulgaris. The excess of sebum production induced by androgen is involved in the development of acne. Our aim is to examine whether BK and its constituents inhibit testosterone metabolism and testosterone-induced sebum synthesis. Methods. Measurements of 5α-reductase activity and lipogenesis were performed using rat liver microsomes and hamster sebocytes, respectively. Results. BK dose-dependently reduced the conversion of testosterone to a more active androgen, dihydrotestosterone in a 5α-reductase enzymatic reaction. Twenty polyphenols in BK categorized as gallotannin, ellagitannin, and flavonoid were identified by LC-MS/MS. Nine polyphenols with gallate group, tetragalloyl glucose, pentagalloyl glucose, eugeniin, 1-desgalloyl eugeniin, casuarinin, castalagin, stenophyllanin C, (-)-epicatechin gallate, and (-)-epigallocatechin gallate, inhibited testosterone metabolism. In particular, pentagalloyl glucose showed the strongest activity. BK and pentagalloyl glucose suppressed testosterone-induced lipogenesis, whereas they weakly inhibited the lipogenic action of insulin. Conclusions. BK inhibited androgen-related pathogenesis of acne, testosterone conversion, and sebum synthesis, partially through 5α-reductase inhibition, and has potential to be a useful agent in the therapeutic strategy of acne.

No MeSH data available.


Related in: MedlinePlus

Quantification of inhibitory effect of BK on rat liver microsomal 5α-reductase activity. Testosterone was incubated at a final concentration of 3.5 μmol/L for 30 min in the presence or absence of rat liver microsomes (40 μg/mL) and the cofactors. Bokusoku (BK) was added to the reactions at 3, 10, 30, or 100 μg/mL before starting the reaction. Testosterone remaining was extracted with ethyl acetate after the incubation and quantified by HPLC technique. Data are shown as relative amounts of testosterone, which are a percentage of testosterone alone control reaction. N = 3.
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fig2: Quantification of inhibitory effect of BK on rat liver microsomal 5α-reductase activity. Testosterone was incubated at a final concentration of 3.5 μmol/L for 30 min in the presence or absence of rat liver microsomes (40 μg/mL) and the cofactors. Bokusoku (BK) was added to the reactions at 3, 10, 30, or 100 μg/mL before starting the reaction. Testosterone remaining was extracted with ethyl acetate after the incubation and quantified by HPLC technique. Data are shown as relative amounts of testosterone, which are a percentage of testosterone alone control reaction. N = 3.

Mentions: Next, testosterone metabolism in the same enzymatic assay was quantified by HPLC (Figure 2). BK inhibited 5α-reductase activity at concentration-dependent manner, and the IC50 was 12.2 μg/mL. Moreover, 5α-reductase inhibitor TMF-4AS-1 also inhibited testosterone metabolism by 50% at 0.01 μmol/L and higher (data not shown).


Inhibition of Rat 5α-Reductase Activity and Testosterone-Induced Sebum Synthesis in Hamster Sebocytes by an Extract of Quercus acutissima Cortex.

Koseki J, Matsumoto T, Matsubara Y, Tsuchiya K, Mizuhara Y, Sekiguchi K, Nishimura H, Watanabe J, Kaneko A, Hattori T, Maemura K, Kase Y - Evid Based Complement Alternat Med (2015)

Quantification of inhibitory effect of BK on rat liver microsomal 5α-reductase activity. Testosterone was incubated at a final concentration of 3.5 μmol/L for 30 min in the presence or absence of rat liver microsomes (40 μg/mL) and the cofactors. Bokusoku (BK) was added to the reactions at 3, 10, 30, or 100 μg/mL before starting the reaction. Testosterone remaining was extracted with ethyl acetate after the incubation and quantified by HPLC technique. Data are shown as relative amounts of testosterone, which are a percentage of testosterone alone control reaction. N = 3.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4325551&req=5

fig2: Quantification of inhibitory effect of BK on rat liver microsomal 5α-reductase activity. Testosterone was incubated at a final concentration of 3.5 μmol/L for 30 min in the presence or absence of rat liver microsomes (40 μg/mL) and the cofactors. Bokusoku (BK) was added to the reactions at 3, 10, 30, or 100 μg/mL before starting the reaction. Testosterone remaining was extracted with ethyl acetate after the incubation and quantified by HPLC technique. Data are shown as relative amounts of testosterone, which are a percentage of testosterone alone control reaction. N = 3.
Mentions: Next, testosterone metabolism in the same enzymatic assay was quantified by HPLC (Figure 2). BK inhibited 5α-reductase activity at concentration-dependent manner, and the IC50 was 12.2 μg/mL. Moreover, 5α-reductase inhibitor TMF-4AS-1 also inhibited testosterone metabolism by 50% at 0.01 μmol/L and higher (data not shown).

Bottom Line: Results.Conclusions.BK inhibited androgen-related pathogenesis of acne, testosterone conversion, and sebum synthesis, partially through 5α-reductase inhibition, and has potential to be a useful agent in the therapeutic strategy of acne.

View Article: PubMed Central - PubMed

Affiliation: Tsumura Research Laboratories, Tsumura & Co., 3586 Yoshiwara, Ami-machi, Inashiki-gun, Ibaraki 300-1192, Japan.

ABSTRACT
Objective. Bokusoku (BK) is an extract from the Quercus cortex used in folk medicine for treatment of skin disorders and convergence, and is present in jumihaidokuto, a traditional Japanese medicine that is prescribed for purulent skin diseases like acne vulgaris. The excess of sebum production induced by androgen is involved in the development of acne. Our aim is to examine whether BK and its constituents inhibit testosterone metabolism and testosterone-induced sebum synthesis. Methods. Measurements of 5α-reductase activity and lipogenesis were performed using rat liver microsomes and hamster sebocytes, respectively. Results. BK dose-dependently reduced the conversion of testosterone to a more active androgen, dihydrotestosterone in a 5α-reductase enzymatic reaction. Twenty polyphenols in BK categorized as gallotannin, ellagitannin, and flavonoid were identified by LC-MS/MS. Nine polyphenols with gallate group, tetragalloyl glucose, pentagalloyl glucose, eugeniin, 1-desgalloyl eugeniin, casuarinin, castalagin, stenophyllanin C, (-)-epicatechin gallate, and (-)-epigallocatechin gallate, inhibited testosterone metabolism. In particular, pentagalloyl glucose showed the strongest activity. BK and pentagalloyl glucose suppressed testosterone-induced lipogenesis, whereas they weakly inhibited the lipogenic action of insulin. Conclusions. BK inhibited androgen-related pathogenesis of acne, testosterone conversion, and sebum synthesis, partially through 5α-reductase inhibition, and has potential to be a useful agent in the therapeutic strategy of acne.

No MeSH data available.


Related in: MedlinePlus