• Archives of Pharmacal Research
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• 제25권3호
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• pp.258-269
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• 2002

2-Thiouracil-5-sulfonylchloride 1 reacted with a series of aromatic and heterocyclic amines to give 2a-j. The same compound 1 was reacted with a series of sulphonamides giving different sulphonamides of type 3a-e. On the other hand compound 1 was allowed to react with p-aminoacetophenone givining compound 4 which in turn was allowed to react with derivatives of alkyl thiosemicarbazides to give thiosemicarbazones of type 5a-e, also compound 4 was monobrominated to give compound 6 which in turn was reacted thiosemicarbazones of some aldehydes to give the corresponding thiazole derivatives 7a-f. In the same time compound 4 was reacted with a series of aromatic and heterocyclic aldehydes givining chalcones 8a-g (Claisen-Schemidt reaction). Also compound 4 was allowed to react with a series of aromatic and heterocyclic aldehydes, ethyl cyano acetate and/or malononitrile, and ammonium acetate giving pyridine derivatives 9a-d and 10a-e respectively. The biological effects of some of the new synthesized compounds was also investigated.

• Biomolecules & Therapeutics
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• 제32권1호
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• pp.38-55
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• 2024

Cancer is a global health challenge with high morbidity and mortality rates. However, conventional cancer treatment methods often have severe side effects and limited success rates. In the last decade, extensive research has been conducted to develop safe, and efficient alternative treatments that do not have the limitations of existing anticancer medicines. Plant-derived compounds have shown promise in cancer treatment for their anti-carcinogenic and anti-proliferative properties. Rosmarinic acid (RA) and carnosic acid (CA) are potent polyphenolic compounds found in rosemary (Rosmarinus officinalis) extract. They have been extensively studied for their biological properties, which include anti-diabetic, anti-inflammatory, antioxidant, and anticancer activities. In addition, RA and CA have demonstrated effective anti-proliferative properties against various cancers, making them promising targets for extensive research to develop candidate or leading compounds for cancer treatment. This review discusses and summarizes the anti-tumor effect of RA and CA against various cancers and highlights the involved biochemical and mechanistic pathways.

• 한국자원식물학회지
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• 제33권6호
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• pp.597-603
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• 2020

Red ginseng marc (RGM) has been used on primary industries using fertilizer or forage, and it mostly has been dumped. To improve utilization of RGM, the biological activities of RGM were examined. RGM was extracted and fractionated using various solvents and their biological activities were compared. The hexane fraction from the methanol extract of RGM (RGMMH) showed strong anti-cancer activity (58.56 ± 6.04% at 100 ㎍/mL) and anti-inflammatory effect (65.72 ± 1.33% at 100 ㎍/mL). But, oil extract of RGM extracted with hexane (RGMH) showed low activities (anti-cancer: 16.42 ± 3.33%, at 100 ㎍/mL, anti-inflammatory activity: 29.46 ± 2.10%, at 100 ㎍/mL). Their metabolites were analyzed using HPLC. Panaxydol known as anti-cancer compound of RGM was one of major compounds in RGMMH. Meanwhile, panaxydol was detected in trace amount in red ginseng marc oil (RGMH). In addition, RGMMH and RGMH showed big differences in HPLC profiling. This research suggests optimal extraction method of RGM oil.

• KSBB Journal
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• 제25권6호
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• pp.507-512
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• 2010

In this study, we investigated the ability of luteolin, a plant derived flavonoid on hepatocarcinoma cell growth using HepG2 cell culture system. We found that luteolin increased the Smac/DIABLO releases, a mitochondrial protein that potentiates apoptosis. Luteolin also induced either transcriptional activity or expression of PPAR-gamma, a target of cancer growth that PPAR-gamma agonist sensitizes to apoptosis in certain cancer types. To find the possible upstream target molecules of PPAR-gamma activated by luteolin treatment, we used compound C, a specific inhibitor of AMP-activated protein kinase. Pre-treatment of Compound C significantly restored the activation or expression of PPAR-gamma stimulated by luteolin. This result indicated that AMPK signaling might be involved in the activation or expression of PPAR-gamma signaling pathway stimulated by luteolin. Moreover, we also found that luteolin inhibited the insulin-stimulated Akt phosphorylation as well as AICAR, a specific AMPK activator. These results propose that luteolin significantly induces cancer cell death through modulating survival signal pathways such as PPAR-gamma and Akt. AMPK signaling pathway may be an upstream regulator for survival signal pathways such as PPAR-gamma and Akt stimulated by luteolin.

• Asian Pacific Journal of Cancer Prevention
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• 제16권13호
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• pp.5325-5329
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• 2015

Farnesiferol C is a natural compound with various anti-cancer properties that belongs to the class of sesquiterpene coumarins. However, the low bioavailability of farnesiferol C limits its therapeutic potential. Here, we overcame this problem utilizing dendrosome nano-particles and evaluated the anti-cancer effect of dendrosomal farnesiferol C (DFC) on the AGS gastric cancer cell line. The 3-(4,5-dimethyl-thiazol-2yl)-2,5- diphenyl tetrazolium bromide (MTT) assay and reverse transcriptase-polymerase chain reaction (RT-PCR) were respectively used to detect the anti-proliferative properties of DFC and expression ratio of Bax/Bcl-2 as a hallmark of apoptosis. Compared to the void farnesiferol C (FC), our data showed that DFC significantly suppresses the proliferation of AGS cells in a time- and dose-dependent manner (P<0.01). Also, DFC meaningfully increased the expression ratio of Bax/Bcl-2 in AGS cells (P<0.01). The findings demonstrate that our nano-based formulation of farnesiferol C could be considered as a potential therapeutic agent in cancer targeting.

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 2018년도 춘계학술발표회
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• pp.9-9
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• 2018

Arctii Fructus (AF), which contains arctigenin (ARC) as a major constituent, is traditionally used as an anti-inflammatory medicine to treat inflammatory sore throat. Although several studies have proven its anti-inflammatory effects, there have been no reports on its use in inflammation related disorders such as obesity, cancer metastasis, and allergic responses. This study investigated the anti-obesity effect and anti-metastasis effect of AF and ARC. AF and ARC inhibited weight gain by reducing the mass of white adipose tissue in high fat diet (HFD)-induced obese mice. Serum cholesterol levels were also improved by AF and ARC. In in vitro experiments, AF and ARC decreased differentiation of white adipocytes. Furthermore, AF induced differentiation of brown adipocytes, which are able to consume surplus energy through non-shivering thermogenesis. Also, AF and ARC inhibited colon cancer and lung metastasis of colon cancer. They suppressed not only colorectal cancer cell progression by inhibiting cell growth, but also prohibited lung metastasis by regulating epithelial-mesenchymal transition (EMT), migration, and the invasion. These effects were confirmed in an experimental metastasis mouse model. In addition, AF and ARC inhibited mast cell mediated allergic responses. Collectively, our study suggests that AF and ARC might show inhibitory effects on inflammation related diseases, including obesity, cancer, cancer metastasis, and allergic responses.

• BMB Reports
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• 제46권2호
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• pp.97-102
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• 2013

The use of various cancer cell lines can recapitulate known tumor-associated mutations and genetically define cancer subsets. This approach also enables comparative surveys of associations between cancer mutations and drug responses. Here, we analyzed the effects of ~40,000 compounds on cancer cell lines that showed diverse mutation-dependent sensitivity profiles. Over 1,000 compounds exhibited unique sensitivity on cell lines with specific mutational genotypes, and these compounds were clustered into six different classes of mutation-oriented sensitivity. The present analysis provides new insights into the relationship between somatic mutations and selectivity response of chemicals, and these results should have applications related to predicting and optimizing thera-peutic windows for anti-cancer agents.

• 한국식품영양과학회지
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• 제36권1호
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• pp.8-13
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• 2007

황기를 이용하여 황기균사체를 접종, 배양하여 얻어진 황기균사체 추출액의 간암세포, 유방암세포, 자궁경부암세포 그리고 고형암의 증식에 미치는 영향을 조사하였다. 3가지 암세포의 형태변화 및 증식억제에 미치는 영향은 황기균사체 추출물이 황기추출물보다 효과적인 것으로 나타났으며, 황기균사체를 간암세포에 3 mg/mL로 처리했을 때 65.23%, 유방암세포에 5 mg/mL로 처리했을 때 69.42%의 높은 암세포 증식 억제 효과가 있었다. 자궁경부암세포에서는 황기균사체를 3 mg/mL로 처리했을 때 황기를 처리했을 때보다 암세포 증식억제효과가 23.82%더 높았다. 특히 간암세포와 유방암세포에서 황기균사체 추출물을 처리하였을 때 강력한 암세포 증식억제효과가 있는 것으로 나타났다. 고형암 억제효과에서도 대조군에 비해 황기균사체 추출물이 47%의 고형암 억제효과가 있었고, 황기추출물보다 고형암 억제 효과 10% 더 높았다. 히스타민 유리 억제효과를 측정한 결과 compound 48/80 처리군에 비해 황기추출물은 7.6%, 황기균사체 추출물은 44.6%의 히스타민 분비 억제효과가 있는 것으로 나타났다. 이상의 결과로 볼 때 한방기능성 소재에 균사체 배양기법의 접목으로 효능의 상승과 복합기능을 기대할 수 있겠다.

• 생약학회지
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• 제39권2호
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• pp.150-154
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• 2008

Butein is a one of polyphenolic compound widely available in numerous plants. It has broad biological activities including antioxidant and anti-inflammatory activities, which contributed to its protective effects against cancer. Evidences that butein influence proliferation of tumor cells make it important to determine how butein affects cell death of various cancers. In this study, we show that butein, a phenolic compound, induces apoptosis in human T lymphoma jurkat cells. We found that treatment of cells with butein increased apoptosis in a dose- and time- dependent manner as determined by staining cells with Annexin V and 7AAD. There was no significant apoptotic cell death when normal lymphocytes and monocytes from healthy donor were treated with butein. We also found caspase-3 activity was increased during butein-induced apoptosis. The buteininduced apoptotic cell death was blocked by the treatment of cells with caspase-3 inhibitor. These results indicate that butein has the potential to provide an effective strategy against cancer with the advantage of being widely avalible.

• Asian Pacific Journal of Cancer Prevention
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• 제17권2호
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• pp.667-671
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• 2016

Oridonin, an ent-kaurane diterpenoid compound isolated from the traditional Chinese herb Rabdosia rubescens, has shown various pharmacological and physiological effects such as anti-tumor, anti-bacterial, and anti-inflammatory properties. However, the effect of oridonin on human ovarian cancer cell lines has not been determined. In this study, we demonstrated that oridonin inhibited ovarian cancer cell proliferation, migration and invasion in a dose-dependent manner. Furthermore, we showed oridonin inhibited tumor growth of ovarian cancer cells (SKOV3) in vivo. We then assessed mechanisms and found that oridonin specifically abrogated the phosphorylation/activation of mTOR signaling. In summary, our results indicate that oridonin is a potential inhibitor of ovarian cancer by blocking the mTOR signaling pathway.