• Asian Pacific Journal of Cancer Prevention
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• 제13권7호
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• pp.3519-3528
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• 2012

Inhibitory effects of Maclura amboinenesis Bl, one plant used traditionally for the treatment of cancers, on metastatic potential of highly metastatic B16F10 melanoma cells were investigated in vitro. Cell proliferation was assessed using the MTT colorimetric assay. Details of metastatic capabilities including invasion, migration and adhesion of B16F10 melanoma cells were examined by Boyden Chamber invasion and migration, scratch motility and cell attachment assays, respectively. The results demonstrated that n-hexane and chloroform extracts exhibited potent anti-proliferative effects (p<0.01), whereas the methanol and aqueous extracts had less pronounced effects after 24 h exposure. Bioactivity-guided chromatographic fractionation of both active n-hexane and chloroform extracts led to the isolation of two main prenylated xanthones and characterization as macluraxanthone and gerontoxanthone-I, respectively, their structures being identified by comparison with the spectral data. Interestingly, both exhibited potent effective effects. At non-toxic effective doses, n-hexane and chloroform extracts (10 and $30{\mu}g/ml$) as well as macluraxanthone and gerontoxanthone-I (3 and $10{\mu}M$) significantly inhibited B16F10 cell invasion, to a greater extent than $10{\mu}m$ doxorubicin, while reducing migration of cancer cells without cellular cytotoxicity. Moreover, exposure of B16F10 melanoma cells to high concentrations of chloroform ($30{\mu}g/ml$) and geratoxanthone-I ($20{\mu}M$) for 24 h resulted in delayed adhesion and retarded colonization. As insights into mechanisms of action, typical morphological changes of apoptotic cells e.g. membrane blebbing, chromatin condensation, nuclear fragmentation, apoptotic bodies and loss of adhesion as well as cell cycle arrest in the G1 phase with increase of sub-G1 cell proportions, detected by Hoechst 33342 staining and flow cytometry were observed, suggesting DNA damage and subsequent apoptotic cell death. Taken together, our findings indicate for the first time that active n-hexane and chloroform extracts as well as macluraxanthone and gerontoxanthone-I isolated from Maclura amboinensis Bl. roots affect multistep of cancer metastasis processes including proliferation, adhesion, invasion and migration, possibly through induction of apoptosis of highly metastatic B16F10 melanoma cells. Based on these data, M. amboinensis Bl. represents a potential candidate novel chemopreventive and/or chemotherapeutic agent. Additionally, they also support its ethno-medicinal usage for cancer prevention and/or chemotherapy.

• Bulletin of the Korean Chemical Society
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• 제29권3호
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• pp.615-619
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• 2008

Eight triterpenoids, six lanostanes 1-6, one lupenane 7, and one oleanane 8, were isolated by bioactivity-guided fractionation of the ethylacetate extract from roots of Glycine max (L.) Merr. All isolated compounds were examined for their inhibitory activities against human ACAT-1 (hACAT-1) and human ACAT-2 (hACAT-2). Among them, three triterpenoids showed potent hACAT inhibitory activities, (24R)-ethylcholest-5-ene-3,7-diol (1) and 3b -hydroxylup-20(29)-en-28-oic acid (7) exhibited more potent inhibitory activity against hACAT-1 (1: IC50 = 25.0 1.2 and 7: IC50 = 11.5 0.4 m M) than hACAT-2 (1: IC50 = 102.0 5.4 and 7: IC50 = 33.9 3.7 m M), respectively. Interestingly, 5a ,8a -epidioxy-24(R)-methylcholesta-6,22-diene-3b -ol (4) has proven to be a specific inhibitor against hACAT-1 (IC50 = 38.7 0.8 m M) compared to hACAT-2 (IC50 >200). In conclusion, this is the first study to demonstrate that triterpenoids of G. max have potent inhibitory activities against hACAT-1 and hACAT-2.

• Journal of Applied Biological Chemistry
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• 제59권4호
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• pp.323-330
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• 2016

반하(Pinellia ternata Breitenbach)는 천남성과(Araceae)의 약용 식물로 동아시아 일대가 원산지이며, 유럽과 북아메리카 일부 지역에도 널리 분포하고 있는 식물이다. 반하의 괴경(tuber)은 약재로 사용되어 구토, 염증, 외상을 치료하는 목적으로 사용되고 있다. 보고된 약리학적 작용으로는 항경련, 항종양, 살충, 세포독성 등이 있는 것으로 알려져 있다. 반하는 약리학적으로 유용한 약용식물로 잘 알려져 있음에도 불구하고, 원산지를 판별할 수 있는 신뢰성이 있고 표준화된 방법이 없는 실정이다. 이를 위한 한국산과 중국산 반하를 판별할 수 있는 유의적인 화합물을 탐색하기 위해 UPLC-PDA와 QTof-MS에 기반을 둔 대사체 표지법을 이용하였다. 한국산으로부터 원산지 판별 화합물로 예상되는 화합물을 반복적인 역상 칼럼크로마토그래피에 기반을 둔 활성유도 분획법을 통해 분리하였다. 그리고, NMR과 MS를 포함한 물리화학적, 분광학적 정보의 결과를 토대로 [6]-gingerol이라는 화합물의 구조를 동정하였다. [6]-gingerol은 원산지를 판별할 수 있는 능력과 melanin 생합성 저해 활성을 지닌 기능성 화장품 소재로서 가치가 있다고 판단되어짐에 따라 유효성분 원산지 판별 화합물로 Fingerprint법에 의해 선정되었다. 더욱이, 한국산과 중국산 반하 유래 [6]-gingerol의 함량 비교를 위해, 유효성이 검증된 분석법을 이용하여 이에 대한 검량곡선을 작성하여 그 함량을 비교하였다. 이것은 한국산 반하판별을 위한 화합물 선정과 성공적인 유효성 검증을 다룬 최초의 보고이다.