• Natural Product Sciences
• /
• 제8권4호
• /
• pp.111-126
• /
• 2002

The chemistry of secondary products from Acanthopanax species and their pharmacological activities were reviewed. A nitrogenous compound, a furan compound, a quinoid, benzoids, coumarins, phenylpropanoids, lignans, flavonoids, terpenoids, phytosterols, polyacetylenes, a pyrimidine, cyclitols, monosaccharides and an aliphatic alcohol have been isolated from Acanthopanax species and have been shown to have various levels of activities such as anti-bacterial, anti-cancer, anti-gout, anti-hepatitis, anti-hyperglycemic, anti-inflammatory, anti-leishmanicidic, anti-oxidant, anti-pyretic, anti-xanthine oxidase, choleretic, hemostatic, hypocholesterolemic, immunostimulatory and radioprotectant effects, etc.

• Bulletin of the Korean Chemical Society
• /
• 제35권4호
• /
• pp.1154-1158
• /
• 2014

Hsp90 is an ubiquitous molecular chaperone protein, which plays an important role in regulating maturation and stabilization of many oncogenic proteins. Due to its potential to simultaneously disable multiple signaling pathways, Hsp90 represents great promise as a therapeutic target of cancer. In this study, we synthesized flavokawain analogues and evaluated their biological activities against drug-resistant cancer cells. The study indicated that compound 1i impaired the growth of gefitinib-resistant non-small cell lung cancer (H1975), down-regulated the expression of Hsp90 client proteins including EGFR, Her2, Met, Akt and Cdk4, and upregulated the expression of Hsp70. The result strongly suggested that compound 1i inhibited the proliferation of cancer cells through Hsp90 inhibition. Overall, compound 1i could serve as a potential lead compound to overcome the drug resistance in cancer chemotherapy.

• Biomolecules & Therapeutics
• /
• 제17권4호
• /
• pp.422-429
• /
• 2009

Invasion and metastasis is the main cause of cancer mortality. Angiogenesis is a prerequisite for the tumor growth and metastasis. Matrix metalloproteinases (MMPs) are the key enzymes playing in the invasive growth and metastasis of cancer as well as angiogenesis. Xanthohumol, a prenylated chalcone of the Hop plant (Humulus lupulus L), has been reported to suppress cancer invasion and angiogenesis. In the present study, we investigated the antiinvasive effects of xanthohumol (1) and its synthetic derivatives, 4'-O-methylxanthohumol SEM ether (2), xanthohumol C (3), and xanthohumol C MOM ether (4) in relation to MMP expression in HT-1080 human fibrosarcoma cells. The compound 1 and its derivative, 3 and 4, significantly inhibited serum-induced HT-1080 cell invasion, and 12-O-tetradecanoylphorbol-13-acetate (TPA)-enhanced activity and expression level of MMP-2 and MMP-9 in a concentration-dependant manner. In addition, they inhibited TPA-enhanced expression of MT1-MMP with relatively weak inhibition in tissue inhibitor of metalloproteinase (TIMP)-1 and TIMP-2 level. The compound 1 significantly decreased the cell viability, whereas the derivatives, 2 and 3 showed no cytotoxicity, and compound 4 showed slight cytotoxicity in the cells. Furthermore, in a chick chorioallantoic membrane (CAM) assay, the derivatives 3 and 4 dose-dependently suppressed vascular endothelial growth factor (VEGF)-induced angiogenesis, which is similar to that of compound 1. Taken together, the results indicate that compounds 3 and 4 may be valuable anti-angiogenic agents in the treatment of chronic diseases such as cancer and inflammation working through suppression of MMP-2 and MMP-9.

• 대한한의학방제학회지
• /
• 제29권4호
• /
• pp.267-275
• /
• 2021

Objectives : Previously, we reported that compound K isolated from fermented ginseng by Aspillus oryzae has a wide biochemical and pharmacological effect, including anti-cancer activity in prostate cancer PC-3 cells. Despite these findings, its signaling pathway and gene expression pattern are not clearly understood. Methods : To confirm the gene expression study of treated with compound K in PC-3 cells, a cDNA microarray chip composed of 44K human cDNA probes was used. MTT assay, western blot analysis, propidium iodide staining, and annexin V/propidium iodide staining were analyzed. Results : We confirmed the differences of gene expression profiles. Then, we analyzed with the cell cycle arrest, cell death and cell proliferation related genes using DAVID database. Conclusions : Our finding should be useful for understanding genome-wide expression patterns of compound K-mediated cell cycle arrest toward induction of cell death and be helpful for finding future cancer therapeutic targets for prostate cancer cells.

• Journal of the Korean Association of Oral and Maxillofacial Surgeons
• /
• 제34권1호
• /
• pp.1-10
• /
• 2008

Oral squamous cell carcinoma (OSCC) is the most frequent form of oral cancer and holds the eighth position in the cancer incidence ranking. OSCC patients are treated by classical therapeutic modalities consisting of surgery, radiotherapy, and/or chemotherapy. But OSCC still shows significant mortality rates. Thus, new therapeutic approaches have been investigated and the most promising one is naturally acquired agents with known anti-cancer effects. Genistein is a compound extracted from soy bean. Its anti-cancer effect on breast cancer is well established now and it is investigated whether it has similar effect on OSCC. It inhibited the growth and invasive-ness of OSCC cells in vitro, but these effects did not work in living animals in vivo. Catechin is a compound from green tea and its anti-cancer effect on OSCC is known better than other agents. Catechin showed its anti-cancer effect in vitro via induction of apoptosis, cell cycle arrest, inhibition of growth, and down-regulation of invasion/metastasis. These effects were confirmed in vivo with mouse model. Cordycepin is one of major pharmacologically important components in Cordyceps Militaris and may exert its anti-cancer effect as an adenosine receptor agonist. In recent study, it inhibited the proliferation of OSCC cells via A3 adenosine receptor. But because there is very scarce evidence on this effect, more researches are needed on this theme.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
• /
• pp.256.1-256.1
• /
• 2002

We investigated the anti-proliferative effects of a new compound. ircinin-1. from the sponge Sarcotragus sp. on SK-MEL -2 human skin cancer cells. From the data of MTT assay, cell viability was decreased by ircinin-1 in a dose-dependent manner. We observed that the anti-proliferative effect of ircinin-1 was due to the induction of apoptosis, which was confirmed by observing the morphological changes. the increased ratio of pro-apoptotic protein Bax to anti-apoptotic protein Bcl-2, and cleavage of poly(ADP-ribose) polymerase protein, via activation of caspase-3. (omitted)

• Asian Pacific Journal of Cancer Prevention
• /
• 제14권5호
• /
• pp.3041-3044
• /
• 2013

Background: The non-steroidal anti-inflammatory drug (NSAID) aspirin (acetylsalicylic acid) is an inhibitor of cyclooxygenase enzymes. Recent studies have shown that aspirin could be used as an anti-tumor drug. Triptolide, the major compound extracted from the Chinese herb Tripteryglum wilfordii Hook.f, has now been shown that it can inhibit tumor growth. The aim of this study was to analyze the anti-tumor efficiency of aspirin and triptolide in cervical cancer cells. Methods: Viability of cervical cancer cell lines was assessed by the MTT method at various concentrations of aspirin and triptolide. Siha and HeLa cell apoptotic analysis was performed by flow cytometry. Real time-PCR and Western Blotting were used to analyze the expression of Bcl-2/Bax, Cyclin D1 and p16. Results: Viability in the combination group was significantly decreased as compared with either drug used alone. Expression change of Bcl-2/Bax, CyclinD1 and p16 appeared to play an important role in the synergistic killing effect on cervical cancer cell apoptosis. Conclusion: Aspirin and triptolide combination treatment may have synergistic anti-tumor effects on cervical cancer cells.

• 대한의생명과학회지
• /
• 제17권3호
• /
• pp.177-184
• /
• 2011

Potassium cyanate (KOCN) is an inorganic compound and induces the carbamylation of proteins with cytotoxic effects on human cells. Although there is a potential cytotoxic molecule, the role of KOCN on the apoptosis of cancer cell is not well understood. The present study investigated the effects of KOCN on the human colorectal cancer cell line, HCT 116 cells. To understand the anti-cancer effect of KOCN on HCT 116 cells, we examined alteration of apoptosis, the intracellular $Ca^{2+}$ concentration, the intracellular signaling pathway and generation of reactive oxygen species (ROS) in these cells treated with KOCN. The apoptosis of HCT 116 cells was induced by KOCN in a dose-dependent manner at 24 hours and 48 hours, respectively. The apoptosis was processed via the cleavage of poly ADP-ribose polymerase (PARP) and activation of caspase 3 in HCT 116 cells. KOCN induced the elevation of intracellular $Ca^{2+}$ concentration and changed the expressions of Bcl-2 family proteins. The pro-apoptotic Bax was continuously up-regulated, and the anti-apoptotic Bcl-2 was down-regulated by KOCN. KOCN also induced the hyperpolarization of mitochondria and the generation of ROS in HCT 116 cells. Taken together, these results indicate that KOCN induces the apoptosis of HCT 116 cells by disruption of $Ca^{2+}$ homeostasis and via mitochondrial pathway. This study provides the compound that may be used as a potent agent for the treatment of colorectal cancer.

• 디지털융복합연구
• /
• 제15권11호
• /
• pp.285-295
• /
• 2017

본 연구에서는 증폭시킨 홍삼으로부터 분리한 ginsenoside Rh2(Rh2)와 compound K(CK)의 융복합적 항염증 및 항암효과를 연구하여 홍삼 내 유용한 기능성분에 대한 기초 자료를 제공하고자 한다. 이에 Hep3B에서의 세포독성과 IL-6 유도 STAT3 루시퍼라아제 활성, B16F10과 Hacat 세포의 생존 농도를 측정하였고 Apoptosis와 관련된 분자의 발현양상을 확인하기 위해 FAC (fluorescence activated cell sorting) 분석을 수행하였다. 실험결과 Rh2, CK mixture가 10 ug/ml일 때 Hep3B 세포에서 세포독성이 없고 IL-6 감소율이 102%로 항염증 효과가 있는 것으로 나타났다. 또한 Rh2, CK mixture 50 uM에서 melanoma 세포인 B16F10과 human keratinocyte인 Hacat에서 독성을 보여 사멸하는 것을 관찰하였다. FACS 분석 결과 annexin V가 발현되지 않고 흑색종 세포와 keratinocyte가 탈착되면서 사멸되는 것을 확인하였다. 이러한 현상을 통하여 사멸되는 메카니즘이 anoikis 방식의 세포사멸로 인한 것으로 추정할 수 있으며 그것에 대한 명확한 세포사 신호 체계 규명을 위하여 향후 세포부착 단백질의 변화에 대한 연구가 필요할 것으로 판단된다.

• Asian Pacific Journal of Cancer Prevention
• /
• 제17권9호
• /
• pp.4199-4204
• /
• 2016

Cancer is a complex disease caused by a progressive accumulation of multiple genetic mutations. Consumption of fruits is associated with lower risk of several cancers, which is mainly associated to their phytochemical content. The use of functional foods and chemopreventive compounds seems to contribute in this process, acting by mechanisms of antioxidant, anti-inflammatory, anti-angiogenic and hormonal. The Psidium Guajava has high potential functional related to pigments who are involved in the process of cancer prevention by having antioxidant activity. The aim of the present review is to expose some chemical compounds from P. Guajava fractions and their association with anti-carcinogenic function. The evidences supports the theory of anticancer properties of P. Guajava, although the mechanisms are still not fully elucidated, but may include scavenging free radicals, regulation of gene expression, modulation of cellular signalling pathways including those involved in DNA damage repair, cell proliferation and apoptosis.