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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 primary sebocytes by BK treatment. 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 bokusoku (BK) 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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fig3: Suppression of testosterone-induced sebum synthesis of hamster primary sebocytes by BK treatment. 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 bokusoku (BK) 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: To confirm that BK can regulate sebum synthesis, BK was evaluated in testosterone- or insulin-induced lipogenesis assays using Ha-SE cells. As shown in Figure 3, testosterone and insulin increased sebaceous lipogenesis. BK tested at 10 and 30 μg/mL significantly suppressed testosterone-induced sebum accumulation. On the other hand, BK suppressed the insulin-induced lipogenesis at 30 μg/mL with a lower inhibition compared with the action in testosterone-induced lipogenesis. Moreover, BK dramatically decreased number of sebum-producing cells 8 days after stimulating with the differentiation factor, especially testosterone (data not shown); however, BK did not exert a cytotoxic activity against undifferentiated Ha-SE cells (Supplementary Figure S1). Representative images in Figure 4 show that BK impeded the formation of sebum at 10 μg/mL in sebocytes treated with testosterone.


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 primary sebocytes by BK treatment. 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 bokusoku (BK) 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

fig3: Suppression of testosterone-induced sebum synthesis of hamster primary sebocytes by BK treatment. 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 bokusoku (BK) 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: To confirm that BK can regulate sebum synthesis, BK was evaluated in testosterone- or insulin-induced lipogenesis assays using Ha-SE cells. As shown in Figure 3, testosterone and insulin increased sebaceous lipogenesis. BK tested at 10 and 30 μg/mL significantly suppressed testosterone-induced sebum accumulation. On the other hand, BK suppressed the insulin-induced lipogenesis at 30 μg/mL with a lower inhibition compared with the action in testosterone-induced lipogenesis. Moreover, BK dramatically decreased number of sebum-producing cells 8 days after stimulating with the differentiation factor, especially testosterone (data not shown); however, BK did not exert a cytotoxic activity against undifferentiated Ha-SE cells (Supplementary Figure S1). Representative images in Figure 4 show that BK impeded the formation of sebum at 10 μg/mL in sebocytes treated with testosterone.

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