• Journal of Applied Biological Chemistry
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• 제65권4호
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• pp.269-275
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• 2022

자작나무(Betula platyphylla) 수피 추출물에는 생리활성을 보일 수 있는 다수의 terpenoids 물질이 포함되어 있고 염증반응을 완화시키는 치료제로 사용되어 왔다. 본 연구는 탈모예방 효과를 보일 수 있는 천연 물질을 확보하기 위해 자작나무를 여러 용매에서 추출 및 분리 정제하여 몇몇 분획을 획득하였다. 이를 사용하여 사람 모낭 모유두세포(HDP)에 대한 세포 독성 및 성장촉진 효과 그리고 β-catenin, VEGF, IGF1, Cyclin D의 발현변화와 5-α-reductase activity에 미치는 영향을 평가하였다. Ethyl acetate를 이용하여 분리한 4개의 분획 중 H3-2 분획은 알려진 유효물질인 ETB, LPO와 동등수준의 모낭 모유두세포(HDP)에 대한 성장 촉진 효과를 보였고 성장에 관여하는 주요인자들의 발현을 높이는 효과를 보였다. 또한, 5-α-reductase activity에 ETB, LPO가 큰 영향을 보이지 못한 반면 최종분획물인 H3은 5-α-reductase activity 감소활성이 있음을 확인할 수 있었다.

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 춘계총회 및 학술대회
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• pp.147.1-147.1
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• 2000

• 한국미생물·생명공학회지
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• 제49권4호
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• pp.528-533
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• 2021

The microalga, Tetrathelmis tetrathele, is used in the development of products for the aquaculture, food, and nutraceutical industries. In the present study, we investigated whether the T. tetrathele ethanolic extract (TTE), which has anti-inflammatory properties, can confer protection against alopecia and improve scalp health, influence the proliferation of human keratinocytes, HaCaT cells, and human hair follicle dermal papilla cells (HFDPC), or inhibit 5α-reductase activity. We found that TTE inhibited the production of the inflammatory mediator, nitric oxide (NO), and prostaglandin E₂ (PGE₂) without cytotoxicity in LPS-stimulated RAW 264.7 cells. In addition, TTE encouraged the proliferation of HaCaT cells and HFDPC. Our results showed that TTE had anti-inflammatory activities, proliferated HaCaT cells and HFDPC, and inhibited 5α-reductase activity. Therefore, we suggest that T. tetrathele could be a potent therapeutic agent for alopecia prevention and scalp improvement.

• The Korean Journal of Physiology and Pharmacology
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• 제7권2호
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• pp.91-96
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• 2003

In Korean folk medicine, several herbs, Glycyrrhizae Radix, Persicae Semen, Salviae Radix, Angelicae Gigantis Radix, Zanthoxyli Fructus, Ginseng Radix Alba, Cnidii Rhizoma, and Carthami Flos, are known to enhance blood circulation and have wound healing or anti-inflammatory effects. These pharmacological actions prompted us to investigate whether these herbs might stimulate hair growth. Thus, using a mixture of their extracts called SPELA 707, we investigated their effects and found that SPELA 707 possessed significant hair cycle converting activity from the telogen phase to the anagen phase in C3H mice. Furthermore, we found that SPELA 707 enhanced the hair density in subjects with hair loss and also promoted the conversion of hair into the anagen phase in subjects with androgenetic alopecia. In addition, hair growth promotion effect of SPELA 707 occurred through inhibition of steroid $5{\alpha}$-reductase activity, which is known to block hair growth. Taken together, these results suggest that SPELA 707 has a potential to be used for the treatment of hair loss.

• 한방안이비인후피부과학회지
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• 제15권1호
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• pp.96-126
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• 2002

In the course of screening natural extracts for hair growth, we found that the extract of dried root of Sophora flavescens has the prominent hair growth promoting effect. After topical application of Sophora flavescens extract to the back of C57BL/6 mice, the earlier conversion of telogen-to-anagen phase was induced. In addition, the Sophora flavescens extract revealed to possess potent inhibitory effect on $5{\alpha}$-reductase Ⅰ and Ⅱ activity. The growth of dermal papilla cells and mouse vibrissae hair follicle cultured in vitro, however, was not affected by Sophora flavescens extract treatment. RT-PCR analysis showed that Sophora flavescens extract induced mRNA levels of growth factors such as insulin-like growth factor-Ⅰ and keratinocyte growth factor in dermal papilla cells, suggesting hair growth promoting effect of Sophora flavescens extract is mediated through inhibition of $5{\alpha}$-reductase type Ⅱ activity and the regulation of growth factors in dermal papilla cells. Furthermore, Sophora flavescens extract also showed anti-bacterial effect on Propionibacterium acnes. These results suggest that Sophora flavescens can be used as a potent treatment agent for helping hair growth stimulation and acne inhibition.

• 동의생리병리학회지
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• 제33권1호
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• pp.63-67
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• 2019

Interaction between epidermis and dermis plays an important role in wound healing and hair follicle formation. This study focused on investigating the potency of ethanol extract of Puerariae Radix (EPR) as cosmetic ingredient using human dermal fibroblasts (hDFn). Our results revealed that EPR suppressed collagenase activity dose-dependently. EPR inhibited activity of $5{\alpha}$-reductase I and II at the final concentration of $25{\mu}g/ml$ in hDFn cells. Also, EPR promoted the proliferation and the ERK activation of cells. ERK phosphorylation by EPR was blocked by specific inhibitor of ERK, PD98059. EPR-induced cell proliferation was blocked by PD98059. This means that EPR could promote the proliferation of hDFn cells via the activation ERK. Collectively, these results suggest that EPR may be used as a new cosmetic ingredient.

• Toxicological Research
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• 제18권3호
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• pp.249-257
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• 2002

Cytochrome P450 3As such as 3A4 and 3A5 metabolize a wide range of pharmaceutical compounds. The vectors for the expression of fusion protein containing an N-terminal human P450 3A4 or P450 3A5 sequences and a C-terminal rat NADPH-cytochrome P450 reductase moiety were constructed. These plasmids were used to express the fusion protein in Escherichia coli DH5$\alpha$ cells. High levels of expression were achieved (100~200 nmol/liter) and the expressed fusion protein in E. coli membranes were catalytically active for nifedipine oxidation, a typical enzymatic activity of P450 3A4. The NADPH-P450 reductase activities of these fusion protein were also determined by measuring reduction of cytochrome c. To fine a specific Inhibitor of P450 3A4 from naturally occurring chemicals, a series of isothiocyanate compounds were evaluated for the inhibitory activity of P450 using the fusion proteins in E. coli membranes. Of the five isothiocyanates (phenethyl isothiocyanate, phenyl isothiocyanate, benzol isothiocyanate, benzoyl isothiocyanate and cyclohexyl isothiocyanate) tested, benzoyl isothiocyanate showed a strong inhibition of P450 3A4 with an $IC_{50}$value of 2.8 $\mu\textrm{M}$. Our results indicate that the self-sufficient fusion protein will be very useful tool to study the drug metabolism and benzyl isothiocyanate may be valuable for characterizing the enzymatic properties of P450 3A4.

• 생약학회지
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• 제17권2호
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• pp.178-183
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• 1986

It was our working hypothesis that introduction of 11-keto groups to 12-oleanene/ursene series of triterpenoids should endow them with corticoid-like activities, since pharmacological actions of glycyrrhetinic acid (GA) are known to be caused by inhibition on $corticoid-{\delta}^4-reductase$. 11-Keto-triterpenoids derived artificially in these studies, such as 11, 19-diketo-18, 19-secoursolic acid methyl ester(I), $11-keto-{\beta}-boswellic$ acid derivatives (IIa-IIc), 11-Keto-presenegenin dimethyl ester (III), II-keto-oleanolic acid derivatives (IVa-IVd) and 11-keto-hederagenin (V) possess the fundamental functions of ${\alpha},\;{\beta}-unsaturated$ ketone on C-11 and hydroxyl group on C-3, as like GA (VI). Additionally, they involve the carboxyl groups on rings A (II, III), D (I, III, IV, V) and E (VI), and the hydroxyl groups on rings A (III, V) and C (III). All the compounds competitively inhibited $corticoid-5{\beta}-reductase$, and the highest inhibitory potency appeared in I. All of them except $3,\;11-diketo-{\beta}-boswellic$ acid methyl ester (IIc) were more effective about five times to twice than GA. On carrageenin-induced edema test, compounds I and IVa-IVd showed anti-inflammatory activities, but III enhanced rather edema. Structure-activity relations were found in the aspects of hydrophilicity of ring A and hydrophobicity of rings C/D. The more they were hydrophilic in ring A and hydrophobic in rings C/D, the more they inhibited the enzyme. And the more they were hydrophobic in rings C/D, the more they exhibited antiiflammatory activities. However, the increased hydrophilicity in ring A resulted in increasing edema, probably due to a nonspecific inhibition on $aldosterone-5{\beta}-reductase$.

• 한국식품영양과학회지
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• 제43권4호
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• pp.507-515
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• 2014

본 연구는 전립선암세포주인 LNCaP 세포주와 테스토스테론으로 유도된 전립선비대 백서모델에서 복분자 추출물의 전립선비대 억제 효과를 조사하였다. 첫째, 전립선암 세포주(LNCaP)에서 복분자 미숙과 추출물의 안드로겐 관련 전립선비대 유전자 억제 효과를 조사한 결과 미숙과 50% 에탄올 추출물은 안드로겐 수용체(AR)뿐만 아니라 전립선특이항원(PSA)과 5-알파 환원 효소 type 2(5AR2)의 발현을 가장 높게 억제하였다. 또한 LNCaP 세포에 DHT로 안드로겐 관련 유전자를 유도한 후 복분자 미숙과 50% 에탄올 추출물을 처리한 결과 AR과 PSA mRNA의 발현이 억제됨을 확인하였다. 둘째, 테스토스테론을 이용하여 전립선비대를 유도한 동물모델에서 복분자 미숙과 50% 에탄올 추출물을 6주간 투여한 후 전립선비대 개선 효과를 조사한 결과, 전립선비대유발군에 복분자 미숙과 추출물을 투여한 군에서 전립선 무게, 전립선 소포의 상피세포 두께 및 면적이 감소함을 확인할 수 있었고, 전립선비대 유발 호르몬인 DHT level이 감소함을 확인할 수 있었다.

• 생명과학회지
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• 제21권6호
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• pp.775-782
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• 2011

본 연구에서는 파파야씨의 메탄올 추출몰과 분획물을 이용하여 항산화 활성 및 quinone reductase (QR) 활성을 측정하였다. 파파야씨의 추출물 및 분획물의 총 폴리페놀 함량은 17.74~125.99 ${\mu}g/mg$이며, 총 플라보노이드 함량은 1.60~32.69 ${\mu}g/mg$으로 나타났으며, ethyl acetate (EtOAc) 분획층의 총 폴리페놀 및 플라보노이드 함량이 다른 분획층과 비교했을 때 가장 높은 것으로 나타났다. ${\alpha}$,${\alpha}$-Diphenyl-${\beta}$-picrylhydrazyl (DPPH) radicals, 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) and hydrogen peroxide를 이용하여 파파야씨 메탄올 추출물 및 분획물의 항산화 활성을 조사한 결과, EtOAc 분획층에서 가장 높은 free radical 억제능을 보였다. 또한 EtOAc 분획층 12.5~50 ${\mu}g/ml$의 농도에서 QR의 유도활성을 조사한 결과, 50 ${\mu}g/ml$의 농도에서 3.3배 정도의 QR 유도능을 보였다. 따라서 파파야씨의 EtOAc 분획층에 존재하는 물질들은 QR inducer 로써의 역할이 기대된다.