• 동의생리병리학회지
• /
• 제24권1호
• /
• pp.55-60
• /
• 2010

Caesalpinia sappan L. (C. sappan) has long been used in traditional medicine as an emmenagogue, hemostatic and anti-inflammatory agent. The present study investigated the effects of water extract of C. sappan in human lymphoma U937 cells. The proliferation of U937 cells was decreased by C. sappan in a dose-dependently manner. Anti-proliferative effect of C. sappan on U937 cells was associated with G2/M phase arrest, which was mediated by regulating the expression of p21 protein. Moreover, phosphorylation of JNK and p38 was increased by C. sappan. Blockade of JNK and p38 was significantly inhibited C. sappan-induced G2/M phase arrest. Taken together, these results suggest that Anti-proliferative effect of C. sappan on U937 is assocated with G2/M phase cell cycle arrest by expression of p21 protein and, JNK and p38 activation.

• 동의생리병리학회지
• /
• 제17권6호
• /
• pp.1524-1527
• /
• 2003

In this study, we demonstrated the antioxidant effect of the Caesalpinia sappan L. extract through the scavenging effect against 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical and the protective effect on protein damage and PC12 cells against cupric ion/hydrogen peroxide. Its IC/sub 50/ value of the scavenging effect against DPPH radical was 7.7 ㎍. Protection of its extract against oxidative bovine serum albumin (BSA)damage induced by hydrogen peroxide was more effective than that of vitamin C. The protective effect on PC12 cells by hydrogen peroxide was shown to be more potent in is extract than in vitamin C. DNA fragmentation analysis also supports this result.

• 약학회지
• /
• 제46권2호
• /
• pp.137-142
• /
• 2002

Caesalpinia sappan L. has long been commonly used as emmenagogue, analgesic, and a cure for contusion and sprain as well as a remedy for thrombosis in the Oriental medicine. The main constituent of C. sappan is brazilein, which is an antioxidative substance that has a flavonoid structure. In this study, we examined the effect of butanol extract of C. sappan on proliferation and melanogenesis in B16/F10 melanoma cells. After 48h treatment of cells with various concentrations of butanol extract, the cells exhibited a dose-dependent inhibition in their proliferation without apotosis. Therefore, the growth retardation by the extract may be due to the cell arrest, not due to the cell death induced by cytotoxicity. We also estimated total melanin contents as a final product and activity of tyrosinase, a key enzyme, in melanogenesis of B16/F10 melanoma cells. Our result showed that the melanin contents and tyrosinase activity were decreased in butanol extract-treated cells in a dose dependent manner compared to control group. In conclusion, it was observed that butanol extract of C. sappan inhibited melanization of these cells and therefore butanol extract could be developed as skin whitening components of cosmetics.

• 치위생과학회지
• /
• 제12권2호
• /
• pp.155-162
• /
• 2012

본 연구는 소목(Caesalpinia sappan L.)의 6가지 유기용매 분획물 중 IP-3의 항균활성을 및 부착능을 측정하고 다음과 같은 결과를 얻었다. 1. Methanol에 의해 분리된 소목의 항균 물질 수율은 총 4.8%로 나타났으며, 여러 분획물 가운데 EtOAc 분획물(IP-3)에서 3.94%로 가장 높은 수율을 보였다. 2. 소목의 EtOAc 분획물에서 최종 정제된 활성물질은 UV 288.3 nm에서 최대 흡수피크를 나타내었으며, NMR spectrum을 통해 brazilin(($C_{16}H_{14}O_5$)으로 확인되었다. 3. S. mutans에 대한 소목의 EtOAc 분획물의 항균 활성은 최소억제농도(MIC) 3.1 mg/ml에서 균의 생장을 억제하였다. 4. S. mutans 부착억제효과는 하이드록시아파타이트(HA)를 S. mutans와 24 시간 동안 함께 배양한 대조군은 균 부착률이 높게 관찰되었으나, 소목의 EtOAc 분획물을 처리한 군에서는 HA에 S. mutans의 부착이 매우 적게 나타났다. 이상의 결과를 통해, 소목에서 추출된 EtOAc 분획에 존재하는 brazilin이 구강 내 우식원성세균에 강한 항균력을 가지고 있는 것으로 판단되며, 특히 S. mutans의 부착 억제능이 확인되어 우식원성 균주에 대한 생약치료제로 활용이 가능할 것으로 사료된다.

• Archives of Pharmacal Research
• /
• 제26권2호
• /
• pp.147-150
• /
• 2003

To find anticancer agents from higher plants, DNA strand-scission assay method was employed for bioassay-guided fractionation as well as for screening the crude extracts. During the screening, an ethyl acetate extracts of the heartwood of Caesalpinia sappan L. (Leguminosae) exhibited potent DNA strand-scission activity. Therefore, the ethyl acetate extracts of the dried heartwood of C. sappan was subjected to the bioassay-guided fractionation, which led to the isolation of a known compound, brazilin (1) as the active constituent. In addition, caesalpine J (2) was also isolated as an inactive constituent.

• 산업식품공학
• /
• 제21권3호
• /
• pp.249-255
• /
• 2017

소목은 인도, 말레이시아, 중국 남부 등의 열대 아시아에 분포하는 낙엽 관목의 콩과 식물로써, 한방에서는 항통증, 항염증의 용도로 사용된다. 본 연구에서는 국내산 소목의 열수 및 에탄올 추출물의 총 폴레페놀, 총 플라보노이드의 함량 분석과 함께 항산화 및 항암활성 분석을 통해 기능성 소재로의 이용가능성을 살펴보고자 하였다. 소목 열수 추출물은 건소목 100 g에 증류수 2L를 가하여 $65^{\circ}C$의 수조에서 4시간 동안 추출하고 에탄올 추출물은 건소목 100 g에 70% 에탄올 2L를 가하여 $25^{\circ}C$, 108 rpm으로 24시간 동안 진탕 추출하였다. 추출물은 모두 여과, 농축한 후 동결 건조하여 시료로 사용되었다. 총 폴리페놀 함량은 열수 추출물 및 에탄올 추출물에서 각각 22.6 mg GAE/g과 17.6 mg GAE/g으로 나타났으며 총 플라보노이드 함량은 14.5 mg QE/g, 13.2 mg QE/g으로 에탄올 추출물에서 더 높은 함량을 보였다(p<0.05). DPPH 실험결과, 10-800 ug/mL의 농도에서 에탄올 추출물은 36.5-82.8%, 열수 추출물은 26.7-75.5%의 radical 소거능을 각각 나타내었다. DPPH실험과 동일한 농도에서 ABTS radical 소거능 측정 결과, 에탄올 추출물은 5.5-94.9%, 열수 추출물은 5.8-88.8%의 소거능을 각각 나타내었는데, 결과적으로 소목 에탄올 추출물이 열수 추출물에 비해 우수한 항산화력을 가지고 있음을 보여주었다(p<0.05). 소목의 항암 활성 측정을 위해 인체 암세포주인 A-549, HeLa, Hep3B cell에 대해 MTT assay와 SRB assay를 실시한 결과, 소목 에탄올 추출물의 농도가 증가함에 따라 각 세포주에 대한 세포 독성이 증가하는 경향을 보였다. MTT assay와 SRB assay의 모든 실험농도에서 폐암 세포인 A-549에 대해 가장 높은 세포 독성을 나타내었으며, 특히 MTT assay에서는 300 ug/mL의 소목 에탄올 추출물이 A-549 cell에 대해 90% 이상의 높은 암세포 억제효과를 보여주었다. 따라서, 우수한 항산화 활성과 항암 활성을 나타낸 소목 추출물은 향후 다양한 기능성 식품 및 의약 소재로서의 활용이 가능할 것으로 보인다.

• 치위생과학회지
• /
• 제7권1호
• /
• pp.31-35
• /
• 2007

Caesalpinia sappan L. (Leguminosae) is an oriental medicinal herb distributed in China and Taiwan, and its heartwood has been traditionally used as an analgesic, a therapy for thrombosis or tumor. This study was to investigate the proliferation and inhibition effects of Caesalpinia sappan extracts against human epithelial cell and cancer cell lines. The methanol extract of dried C. sappan heartwood was evaporated (KS-6), and then sequentially extracted by hexane (KS-01), chloroform (KS-02), ethyl acetate (KS-03), n-butanol (KS-04), and water (KS-05). After 48 hr of exposure, these fractions at a concentration of $50{\mu}g/ml$ significantly increased, and reduced cell proliferation in both human normal epithelial and cancer cell lines. The ethyl acetate fraction (KS-03) among organic solvent fractions was 120.2% of the most proliferation activity ($50{\mu}g/ml$) against HaCaT human epithelial cell. However, fractions from chloroform, butanolic and methanolic extract had 7.2, 28.7 and 20.8% of antiproliferative effect on HaCaT cell, respectively. In cell proliferation effects of C. sappan extract on HeLa, SiHa and C33A human cervical cancer cells, chloroform fraction (KS-2) was the most antiproliferative activity, its antiproliferative rate (dosage, $50{\mu}g/ml$) relative to control was 25.8, 12.2 and 17.4% for SiHa, HeLa and C33A, respectively. The results indicated that the six extract fractions could induce cell cycle stimulate or arrest in some way. Finally, further investigation is needed to assess the molecular mechanisms mediated anticancer activities of this plant.

• Journal of Microbiology and Biotechnology
• /
• 제16권10호
• /
• pp.1591-1596
• /
• 2006

Acaricidal effects of materials derived from Caesalpinia sappan heartwoods against Dermatophagoides farinae and D. pteronyssinus were assessed and compared with those evidenced by commercial benzyl benzoate and DEET. The observed responses varied according to dosage and mite species. The $LD_{50}$ values of the methanol extracts derived from C. sappan heartwoods were 6.13 and $5.44{\mu}g/cm^3$ against D. farinae and D. pteronyssinus, respectively. Furthermore, the ethyl acetate fraction derived from the methanol extract was approximately 8.71 more toxic than DEET against D. farinae, and 4.73 times more toxic against D. pteronyssinus. The biologically active constituent from the ethyl acetate fraction of C. sappan heartwood extract was purified via silica gel chromatography and high-performance liquid chromatography. The structure of the acaricidal component was analyzed by $GC-MS,\;^1H-NMR,\;^{13}C-NMR,\;^1H-^{13}C\;COSY-NMR$, and DEPT-NMR spectroscopy, and identified as juglone (5-hydroxy-l,4-naphthoquinone). Based on the $LD_{50}$ values of juglone and its derivatives, the most toxic compound against D. farinae was juglone ($0.076{\mu}g/cm^3$), followed by benzyl benzoate ($9.143{\mu}g/cm^3$) and 2methyl-l,4-naphthoquinone ($40.0{\mu}g/cm^3$). These results indicate that the acaricidal activity of C. sappan heartwoods is likely to be the result of the effects of juglone. Additionally, juglone treatment was shown to effect a change in the color of the cuticles of house dust mites, from colorless-transparent to dark brownish-black. Accordingly, as a naturally occurring acaricidal agent, C. sappan heartwood-derived juglone should prove to be quite 'useful as a potential control agent, lead compound, and house dust mite indicator.

• 한국식품영양과학회지
• /
• 제45권7호
• /
• pp.1026-1034
• /
• 2016

본 실험은 식용 가능한 약용식물을 대상으로 하여 항균 활성을 검색하였다. 미생물에 대하여 약용 식물을 50 mg/mL, 100 mg/mL, 200 mg/mL의 농도로 하여 paper disc agar diffusion assay로 항균 활성을 검색한 결과 소목 추출물에서 가장 높은 항균 활성을 나타내었다. 이에 따라 소목의 에탄올 추출물과 열수 추출물을 각각 200 mg/mL, 100 mg/mL, 50 mg/mL의 농도로 하여 paper disc agar diffusion assay로 항균 활성을 검색한 결과 소목 추출물은 그람 양성균에서 높은 항균 활성을 나타내었고, 소목의 에탄올 추출물이 소목의 열수 추출물보다 높은 항균 활성을 나타내었다. 소목 에탄올 추출물과 열수 추출물의 각 분획물을 50 mg/mL의 농도로 하여 paper disc agar diffusion assay로 항균 활성을 검색한 결과 그람 양성균은 클로로포름, 에틸아세테이트, 부탄올 층에서 항균 활성을 나타내었고, 그람 음성균은 항균 활성을 나타내지 않았다. 소목의 항균 물질로 추정되는 brazilin은 주로 에틸아세테이트 분획층에 존재하므로 소목 에탄올 추출물에서 클로로포름, 에틸아세테이트, 부탄올의 항균 활성이 유사한 점으로 미루어 brazilin 외에도 다양한 항균 물질이 존재하여 이들이 복합적으로 작용하여 항균 활성을 나타내는 것으로 생각한다. 현재까지 가장 강력한 항생제로 알려진 vancomycin과의 항균 활성을 비교한 결과 50 mg/mL 농도에서 소목 75% 에탄올 추출물의 항균 활성은 vancomycin 2.5 mg/mL를 사용하였을 때와 유사한 항균 활성을 나타내었다. 소목의 추출물을 가지고 미생물에 대한 최소저해농도를 측정한 결과 C. difficile KCTC 5009, L. monocytogens ATCC 19115의 최소저해농도는 0.06 mg/mL였고, S. aureus KCTC 1916에 대한 최소저해농도는 0.03 mg/mL였다. Vancomycin의 유효혈청농도는 0.005~0.04 mg/mL로 견줄만한 항균 활성을 나타내었다. 소목추출물을 가지고 열 및 pH 안정성을 측정한 결과는 항균력은 C. difficile KCTC 5009, L. monocytogens ATCC 19115, S. aureus KCTC 1916에서 모두 대조구와 비슷하게 억제환이 생성되어 소목 추출물의 항균성 물질은 열 및 pH에 대체로 안정한 결과를 보여주었다. 상기 결과들을 종합해 볼 때 소목 에탄올 추출물이 그람 양성균에 대해 항균활성이 뛰어난 것으로 보아 소목을 그람 양성의 병원성 미생물을 억제하기 위한 항균제제 및 기능성 식품의 소재로써 활용할 수 있다고 판단된다.

• 생약학회지
• /
• 제33권2호통권129호
• /
• pp.130-136
• /
• 2002

Melanogenesis is a physiological process resulting in the synthesis of melanin pigments, which play a crucial protective role against skin photocarcinogenesis. The heart wood of Caesalpinia sappan L.(C. sappan) has long been commonly used in Oriental folk medicines to promote blood circulation, and as an emmenagogue, analgesic or anti-inflammatory agent as well as a remedy for thrombosis. From the heartwood, many constituents have been purified and among them, brazilin and hematoxylin are two of the most abundant. This present study was designed to investigate the inhibitory effect of butanol extract from C. sappan on proliferation and melanogenesis in Melan-a cells. After 48 h treatment of these cells with various concentrations of butanol extract, the cells showed a dose-dependent inhibition in their proliferation without apoptotic cell death. Therefore, the growth retardation by the extract may be due to the cell arrest or cell differentiation. We also estimated total melanin content as a final product and activity of tyrosinase, a key enzyme, of melanogenesis in Melan-a cells. The melanin content and tyrosinase activity were deσeased in extract-treated cells in a dose dependent manner compared to control group. The butanol extract also resulted in a decrease of melanin content in ${\alpha}-melanocyte-stimulating$ hormone (MSH)-induced melanogenesis, indicating that butanol extract of C. sappan could be developed as skin whitening components of cosmetics.