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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

Suppression of testosterone-induced sebum synthesis of hamster sebocytes by pentagalloyl glucose, a main active constituent of BK. Hamster-derived sebaceous gland cells (Ha-SE) were precultured until confluent in the presence of epidermal growth factor and further treated with the indicated concentrations of pentagalloyl glucose or bokusoku (BK) (30 μg/mL) and a differentiation factor, 10 μmol/L testosterone or 10 μg/mL insulin. Eight days later, the sebum synthesis was determined using a lipogenesis detecting assay kit. N = 3.
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fig5: Suppression of testosterone-induced sebum synthesis of hamster sebocytes by pentagalloyl glucose, a main active constituent of BK. Hamster-derived sebaceous gland cells (Ha-SE) were precultured until confluent in the presence of epidermal growth factor and further treated with the indicated concentrations of pentagalloyl glucose or bokusoku (BK) (30 μg/mL) and a differentiation factor, 10 μmol/L testosterone or 10 μg/mL insulin. Eight days later, the sebum synthesis was determined using a lipogenesis detecting assay kit. N = 3.

Mentions: Finally, we investigated whether pentagalloyl glucose, the most active and abundant in BK, suppressed testosterone- or insulin-induced lipogenesis in Ha-SE cells. As shown in Figure 5, pentagalloyl glucose significantly downregulated the lipogenesis of both differentiation factors at concentrations of 10 and 30 μmol/L, as well as BK (30 μg/mL) did.


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)

Suppression of testosterone-induced sebum synthesis of hamster sebocytes by pentagalloyl glucose, a main active constituent of BK. Hamster-derived sebaceous gland cells (Ha-SE) were precultured until confluent in the presence of epidermal growth factor and further treated with the indicated concentrations of pentagalloyl glucose or bokusoku (BK) (30 μg/mL) and a differentiation factor, 10 μmol/L testosterone or 10 μg/mL insulin. Eight days later, the sebum synthesis was determined using a lipogenesis detecting assay kit. N = 3.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig5: Suppression of testosterone-induced sebum synthesis of hamster sebocytes by pentagalloyl glucose, a main active constituent of BK. Hamster-derived sebaceous gland cells (Ha-SE) were precultured until confluent in the presence of epidermal growth factor and further treated with the indicated concentrations of pentagalloyl glucose or bokusoku (BK) (30 μg/mL) and a differentiation factor, 10 μmol/L testosterone or 10 μg/mL insulin. Eight days later, the sebum synthesis was determined using a lipogenesis detecting assay kit. N = 3.
Mentions: Finally, we investigated whether pentagalloyl glucose, the most active and abundant in BK, suppressed testosterone- or insulin-induced lipogenesis in Ha-SE cells. As shown in Figure 5, pentagalloyl glucose significantly downregulated the lipogenesis of both differentiation factors at concentrations of 10 and 30 μmol/L, as well as BK (30 μg/mL) did.

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