• Archives of Pharmacal Research
• /
• 제28권12호
• /
• pp.1376-1380
• /
• 2005

In this study, ethanolic extracts from 18 seaweed variants were assessed for hepatoprotective activity against tacrine-induced cytotoxicity in Hep G2 cells. Only one of these, Ecklonia stolonifera Okamura (Laminariaceae), a member of the brown algae, exhibited promising hepatoprotective activity. Bioassay-guided fractionation of the active ethyl acetate (EtOAc) soluble fraction obtained from the ethanolic extract of E. stolonifera, resulted in the isolation of several phlorotannins [phloroglucinol (1), eckstolonol (2), eckol (3), phlorofucofuroeckol A (4), and dieckol (5)]. Compounds 2 and 4 were determined to protect Hep G2 cells against the cytotoxic effects of tacrine, with $EC_{50}$ values of 62.0 and 79.2 $\mu$g/mL, respectively. Silybin, a well characterized hepatoprotective agent, was used as a positive control, and exhibited an $EC_{50}$ value of 50.0 $\mu$g/mL. It has been suggested that the phlorotannins derived from marine brown algae might prove useful sources in the development of novel hepatoprotective agents.

• 생약학회지
• /
• 제40권4호
• /
• pp.345-350
• /
• 2009

Activity-guided fractionation of the EtOH extract of flowers of Bidens bipinnata L. have been furnished five flavonoids, sulfuretin(1), butein(2), 7,8,3',4'-tetrahydroxyflavanone(3), maritimetin(4) and okanin(5). All of the compounds showed significant activities on both linoleic acid peroxidation inhibition and DPPH radical scavenging effect. The evaluation for protective effect of isolated compounds against tacrine-induced cytotoxicity in human liver-derived Hep G2 cells was conducted. Compounds 1, 3, 4 and 5 showed significant protective effects with the $EC_{50}$ values of $36.1{\pm}0.9$, $23.3{\pm}0.7$, $41.0{\pm}1.0$ and $29.8{\pm}1.1{\mu}M$, respectively. Silybin, one of the well-known hepatoprotective agents, used as a positive control, and also showed protective effect with an $EC_{50}$ value of $84.3{\pm}0.7{\mu}M$.

• 생약학회지
• /
• 제44권3호
• /
• pp.209-219
• /
• 2013

Heat shock protein 90 (Hsp90) is a molecular chaperone that assists protein folding and contributes to the stability of various proteins. It also stabilizes a number of proteins involved in tumor growth to consider it as a promising target for the treatment of cancer. Natural products have been a rich source of agents of value in medicine, therefore discovering lead compounds from them is one of important strategy in the drug development. In this regard, geldanamycin, radicicol, novobiocin and celastrol have been utilized as leads for the development of Hsp90 inhibitory anticancer agents. This review summerizes recent findings of natural products as Hsp90 inhibitiors. The Hsp90 inhibitory activities, mode of actions on Hsp90 and cytotoxicities on human cancer cell lines of natural products including bulgarialactone B, curcumin, (-)-gambogic acid, quercetin, sansalvamide A, silybin, and withaferin A were discussed.

• Parasites, Hosts and Diseases
• /
• 제61권4호
• /
• pp.449-454
• /
• 2023

Free-living amoebae (FLA) rarely cause human infections but can invoke fatal infections in the central nervous system (CNS). No consensus treatment has been established for FLA infections of the CNS, emphasizing the urgent need to discover or develop safe and effective drugs. Flavonoids, natural compounds from plants and plant-derived products, are known to have antiprotozoan activities against several pathogenic protozoa parasites. The anti-FLA activity of flavonoids has also been proposed, while their antiamoebic activity for FLA needs to be emperically determined. We herein evaluated the antiamoebic activities of 18 flavonoids against Naegleria fowleri and Acanthamoeba species which included A. castellanii and A. polyphaga. These flavonoids showed different profiles of antiamoebic activity against N. fowleri and Acanthamoeba species. Demethoxycurcumin, kaempferol, resveratrol, and silybin (A+B) showed in vitro antiamoebic activity against both N. fowleri and Acanthamoeba species. Apigenin, costunolide, (-)-epicatechin, (-)-epigallocatechin, rosmarinic acid, and (-)-trans-caryophyllene showed selective antiamoebic activity for Acanthamoeba species. Luteolin was more effective for N. fowleri. However, afzelin, berberine, (±)-catechin, chelerythrine, genistein, (+)-pinostrobin, and quercetin did not exhibit antiamoebic activity against the amoeba species. They neither showed selective antiamoebic activity with significant cytotoxicity to C6 glial cells. Our results provide a basis for the anti-FLA activity of flavonoids, which can be applied to develope alternative or supplemental therapeutic agents for FLA infections of the CNS.

• 한국식품과학회지
• /
• 제35권1호
• /
• pp.138-143
• /
• 2003

쑥갓의 total methanol 추출물이 galactosamine으로 독성을 유발시킨 흰쥐의 일차배양 간세포에서 유리되는 GPT의 활성을 유의성 있게 감소시켜 간세포 보호활성을 보임을 알 수 있었다. Total methanol 추출물을 다시 $CHCl_3$, n-buthanol, $H_2O$ 분획으로 나누어 galactosamine 독성에 의한 간세포 보호작용을 재검색한 결과, 50 ppm의 농도에서 간세포 보호작용을 가지는 대조약물 silybin의 41.3% 보호효과에 비하여 각각 51.2%, 10.6%, 23.1%의 보호활성을 나타내었다. 이 중 가장 활성이 큰 $CHCl_3$, 분획을 가지고 활성의 추적 분리 방법으로 소분획 CH-II, V, VI의 활성 subfraction을 얻고 이를 다시 TLC와 활성검색을 병용하여 CH-(V+VI)-d, -e, -j의 sub-subfraction을 얻을 수 있었으며 이들은 50 ppm의 농도에서 각각 41.3%, 51.3%, 47.3%의 보호활성을 보였다. 활성 소분획 CH-II, V, VI는 모두 $[^3H]-uridine$ uptake 시험을 통한 RNA 생합성에는 영향을 미치지 않았으나 total GSH 값은 간세포 보호약물인 silymarin 대조구 $100\;{\mu}M$ 농도에서의 59.7% 수준의 회복효과에 비하여 각각 49.8%, 43.9%, 47.5%의 회복효과를 보였다. 또한 (reduced GSH)/(total GSH) 값도 silymarin $100\;{\mu}M$에서의 0.850에 비하여 각각 0.871, 0.863, 0.872로 유사한 수치를 타나내었다. 이 연구결과로 쑥갓의 간세포 보호작용을 처음으로 검색, 확인하였으며 컬럼 크로마토그래피를 이용하여 활성이 있는$CHCl_3$ 소분획을 분리하였으므로 이들 소분획으로 부터 더욱 활성물질을 순수분리하여 그 구조를 밝히고 간세포 보호활성의 기전에 대하여도 다양한 방향의 연구가 수행되어야 할 것이다.

• 대한한의학방제학회지
• /
• 제16권1호
• /
• pp.117-130
• /
• 2008

Korean traditional medicine has been used for the treatment of the various diseases based on both oriental medicinal theory and clinical trials. Thus, the prescriptions of Korean traditional medicine would be useful for the development of new therapeutics. This research focuses on the fundamental study in Korean traditional prescriptions for the development of new hepatoprotective agents. We found two prescriptions. Injinho-Tang and Osumogwa-Tang, showed the significant DPPH free radical scavenging and hepatoprotective effect, respectively. It is well-known that free radical scavenging effect is related to the prevention of various pathological events including liver injury. This paper deals with hepatoprotective effects on tacrine-induced cytotoxicity in Hep G2 cells, free radicals scavenging on both DPPH and superoxide of above two prescriptions. Hot water extract of Injinho-Tang did not show the significant hepatoprotective effect on tacrine-induced cytotoxicity in Hep G2 cells, however, it shows the significant scavenging effects for both DPPH and superoxide radicals. On the other hand, all of the hot water extracts of constituent herbal drugs in Injinho-Tang exhibited the promising protective effect on tacrine-induced cytotoxicity in Hep G2 cells. Of these, water extract of Rhei Rhizoma showed the most prominent effect on tacrine-induced cytotoxicity in Hep G2 cells. Bioassay-guided fractionation of Rhei Rhizoma extract has furnished four compounds, and their chemical structures have been identified by comparison of their spectral data with those of literature as chrysophanol (1), emodin (2), 3,5-dihydroxy-4'- methoxystilbene (3), and rhapontigenin (4), respectively. Among the isolated compounds, compounds 2-4 revealed the significant hepatoprotective effect in vitro when their $EC_{50}$ values compare with that of silybin, as a positive control. It also exhibited that emodin possessed the most hepatoprotective effect among these active compounds. In case of Osumogwa-Tang, its hot water extract showed the moderate protective effect on tacrine-induced cytotoxicity in Hep G2 cells. Hot water extract of Chaenomelis Fructus, one of the constituent herbal drug of this prescription, exhibited the significant hepatoprotective effect with $EC_{50}$ value of $7.8{\pm}0.1\;{\mu}g/ml$, however, it showed strong cytotoxicity in Hep G2 cells above the concentration of $25\;{\mu}g/ml$. It was revealed that both hot water extract of Evodiae Fructus and its butanol soluble fraction showed the moderate hepatoprotective effect but concentration-dependent activity in Hep G2 assay system. Two quinolone alkaloids, evocarpine and dihydroevocarpine, also tested for their hepatoprotective effects on tacrine-induced cytotoxicity in Hep G2 cells, however, these two compounds derived from the Evodiae Fructus as the major constituents did not show in vitro hepatoprotective effect. From these results, it would be necessary to further isolation of its hepatoprotective compounds from the butanol soluble fraction of the hot water extract of Evodiae Fructus.

• 생명과학회지
• /
• 제27권4호
• /
• pp.442-449
• /
• 2017

엉겅퀴(C. japonicum) 부위별 추출물을 기능성 식품소재로 활용가능성을 알아보기 위해서 총 페놀 및 silymarin 화합물의 함량분석, 항산화 및 간 보호효과를 서양엉겅퀴와 비교하였다. 엉겅퀴의 총 페놀함량은 지상부($97.22{\pm}5.51mg/g$)가 지하부($85.32{\pm}3.06mg/g$)보다 많았으며, 서양엉겅퀴의 전초보다 다소 낮은 함량을 보였다. 엉겅퀴의 silymarin 화합물의 총 함량은 서양엉겅퀴의 55.56%이었으며, 지하부($0.47{\pm}0.03mg/g$)는 지상부($0.18{\pm}0.02mg/g$)보다 많이 함유되어 있었다. 또한 지상부에서는 silychristin, silydianin이, 지하부에서는 silychristin, silydianin, silybin B, isosilybin B 등이 검출되었다. 엉겅퀴의 항산화활성은 대체로 서양엉겅퀴보다는 약간 낮았고, 지하부가 지상부보다 높은 활성을 보였다. 엉겅퀴 추출물을 1 mg/ml 농도로 처리하였을 때, DPPH 활성은 지상부와 지하부에서 각각 $83.76{\pm}0.60%$, $88.28{\pm}0.17%$의 활성을 나타났으며, FRAP 활성은 지상부와 지하부에서 각각 $77.63{\pm}0.70$, $82.83{\pm}0.39%$로 나타났다. ABTS 활성도 엉겅퀴 추출물을 0.1 mg/ml 농도로 처리하였을 때, 지하부와 지상부에서 각각 $68.60{\pm}1.24%$와 $63.41{\pm}0.57%$로 나타났다. 엉겅퀴 추출물의 간 보호효과는 지하부에서 지상부보다 다소 높은 활성이 나타났으나 서양엉겅퀴 지상부의 활성보다는 낮았다. t-BHP, $H_2O_2$ 및 Ethanol의 처리에 따른 손상된 간세포에 엉겅퀴 추출물을 0.2 mg/ml씩 처리하였을 때, 세포생존율은 각각 $49.58{\pm}0.34$, $76.87{\pm}1.10$ 및 $71.73{\pm}0.58%$로서 추출물을 처리하지 않았을 때보다 각각 24.78, 61.32 및 38.04%씩 높아졌다. 이와 같은 결과로 볼 때, 본 연구에서는 국내산 엉겅퀴의 간 보호효과를 활용한 기능성 식품의 개발이 가능할 것으로 생각되었다.