• The Korean Journal of Physiology and Pharmacology
• /
• v.23 no.5
• /
• pp.393-402
• /
• 2019

Aurora kinases inhibitors, including ZM447439 (ZM), which suppress cell division, have attracted a great deal of attention as potential novel anti-cancer drugs. Several recent studies have confirmed the anti-cancer effects of ZM in various cancer cell lines. However, there have been no studies regarding the cardiac safety of this agent. We performed several cytotoxicity, invasion and migration assays to examine the anti-cancer effects of ZM. To evaluate the potential effects of ZM on cardiac repolarisation, whole-cell patch-clamp experiments were performed with human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs) and cells with heterogeneous cardiac ion channel expression. We also conducted a contractility assay with rat ventricular myocytes to determine the effects of ZM on myocardial contraction and/or relaxation. In tests to determine in vitro efficacy, ZM inhibited the proliferation of A549, H1299 (lung cancer), MCF-7 (breast cancer) and HepG2 (hepatoma) cell lines with $IC_{50}$ in the submicromolar range, and attenuated the invasive and metastatic capacity of A549 cells. In cardiac toxicity testing, ZM did not significantly affect $I_{Na}$, $I_{Ks}$ or $I_{K1}$, but decreased $I_{hERG}$ in a dose-dependent manner ($IC_{50}$: $6.53{\mu}M$). In action potential (AP) assay using hiPSC-CMs, ZM did not induce any changes in AP parameters up to $3{\mu}M$, but it at $10{\mu}M$ induced prolongation of AP duration. In summary, ZM showed potent broad-spectrum anti-tumor activity, but relatively low levels of cardiac side effects compared to the effective doses to tumor. Therefore, ZM has a potential to be a candidate as an anti-cancer with low cardiac toxicity.

• Journal of Pharmacopuncture
• /
• v.6 no.3
• /
• pp.57-63
• /
• 2003

Background : This study was to investigate existing studies on the mushroom Phellinus linteus for possible applications in treating hard to cure diseases and uses in herbal acupuncture as the above is known to have an anti-cancer effects and stimulating the immune system. Results : Based on the literary consideration, the following results were obtained : 1. Proteins and polysaccharides of the Class Basidiomycetes activate the host immune system for anti-cancer action without known side effects, thus it can be given for the prevention and treatment of cancer as a supplement. Phellinus linteus mushroom showed the most significant effects. 2. The Phellinus linteus mushroom is a fungi in the family Hymenochaetaceae and Phellinus, under the class Basidiomycetes. Phellinus linteus can be often found on the trunk of mulberry trees and other latifoliate trees. 3. The characteristics of Phellinus linteus are sweet, neutral in temperature, non-toxic, dissipate the stagnated blood, stop bleeding, invigorate the blood circulation and remove stasis, and nourish qi. It has been used for treating continuous menstrual discharge among the female patients and removing masses in the abdomen to name a few. 4. Phellinus linteus contains agaric acid, fatty acid, C23 and other numerous enzymes. 5. Phellinus linteus is known to have anti-cancer and anti-oxidant effects, stimulation of the immune system, as well as anti-inflammatory effects, inhibition of angiogenesis, and analgesic actions.

• International Journal of Oral Biology
• /
• v.40 no.2
• /
• pp.85-91
• /
• 2015

Quercetin is a natural flavonoid phytochemical that is extracted from various plants. Having an advantages due to its varied biological properties, such as anti-inflammatory, anti-viral, anti-oxidant, and anti-cancer effects, quercetin is used to treat many diseases. Recently, it has been reported that autophagy inhibition may play a key role in anti-cancer therapy. Therefore, in this study, we investigated the molecular mechanisms and anti-cancer effects of quercetin in human osteosarcoma cells via autophagy inhibition. We ascertained that quercetin inhibited cell proliferation and induced cell death, these process is demonstrated that apoptosis via the mitochondrial pathway and the caspase cascade. Quercetin also induced autophagy which was inhibited by 3-MA, autophagy inhibitor and the blockade of autophagy promoted the quercetin-induced apoptosis, confirming that autophagy is a pro-survival process. Thus, these findings demonstrate that quercetin is an effective anti-cancer agent, and the combination of quercetin and an autophagy inhibitor should enhance the effect of anti-cancer therapy.

• Proceedings of the Plant Resources Society of Korea Conference
• /
• 2018.04a
• /
• pp.9-9
• /
• 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.

• The Journal of Internal Korean Medicine
• /
• v.26 no.2
• /
• pp.310-319
• /
• 2005

Objectives: The aim is to identify any anti-tumor effects of Duchesnea indica(Andr.) Focke on colon cancer cells. Materials & Methods: Colo201 human adenocarcinoma cells were obtained from American Type Culture Collection. The boiled extract of Duchesnea indica(Andr.) Focke was added (10 and 20 microliters) to cultures and observed at 0, 6, and 12 hours, and at 12-hour intervals thereafter. Morphological changes in colon cancer cells were observed through an inverted microscope, Destruction of colon cancer cells was measured through Trypan blue exclusion testing. Suppression of the viability of colon cancer cells were measured via MTT assay. Anti-cancer mechanisms in the cell cycle of colon cancer cells were analysed via flow cytometry. Results: After introduction of Duchesnea indica(Andr.) Focke to cultures several changes were seen. Significant atrophy of the nucleus and cytoplasm of colon cancer cells was observed, indicating cell injury. Destruction of colon cancer cells was observed in direct proportion to dosage and duration. Suppression of viability of colon cancer cells for each test group was greater than that of the control group increasingly over time(36h, 48h, 60h, 72h), which was statistical significant (p<0.05). Cell numbers of the mitosis phase of the colon cancer cell cycle reduced. Conclusions: Statistcally significant anti-tumor effects of Duchesnea indica(Andr.) Focke were observed in this in vitro experiment. Results support a role for Duchesnea indica(Andr.) Focke in treatment of colon cancer. though it will required progressive research to develop a practical treatment.

• Advances in nano research
• /
• v.10 no.2
• /
• pp.139-150
• /
• 2021

In this study, phytochemicals present in Propolis Extract (PE) were employed as reducing and stabilizing reagents to synthesize silver nanoparticles. Three propolis-reduced silver nanoparticles (P-AgNPs1-3) were synthesized using increasing amounts of PE. P-AgNPs were treated with different cancer cells-lung (A549), cervix (HeLa) and colon (WiDr) - for 24, 48 and 72 h to evaluate their anti-proliferative activities. A non-cancerous cell type (L929) was also used to test whether suppressive effects of P-AgNPs on cancer cell proliferation were due to a general cytotoxic effect. The characterization results showed that the bioactive contents in propolis successfully induced particle formation. As the amount of PE increased, the particle size decreased; however, the size distribution range expanded. The antioxidant capacity of the particles increased with increased propolis amounts. P-AgNP1 exhibited almost equal inhibitory effects across all cancer cell types; however, P-AgNP2 was more effective on HeLa cells. P-AgNPs3 showed greater inhibitory effects in almost all cancer cells compared to other NPs and pure propolis. Consequently, the biological effects of P-AgNPs were highly dependent on PE amount, NP concentration, and cell type. These results suggest that AgNPs synthesized utilizing propolis phytochemicals might serve as anti-cancer agents, providing greater efficacy against cancer cells.

• The Korea Journal of Herbology
• /
• v.29 no.1
• /
• pp.1-6
• /
• 2014

Objectives : Many of currently used anti-cancer drugs were developed to target cell death mechanisms and had serious side effects by causing damage to normal cells. Hangambujeongsan or Kangai Fuzheng Powder was a mixture based on the traditional Chinese medicine. It had been used in the local Chinese hospitals to treat cancer patients for decades and had shown a certain level of beneficial effects without major toxic effects. But its mechanism of action had not been elucidated yet. Thus this study aimed to investigate the effects of Kangai Fuzheng Powder in an in vitro experiment. Methods : Cancer lines or RAW264.7 mouse macrophage cells were treated with Kangai Fuzheng Powder. Cell viability was measured by MTT assay, and morphological observation was also performed. Gene expression of cytokines in macrophages was determined by real-time polymerase chain reaction. Phagocytic function assay was also performed in macrophage cells. Results : Kangai Fuzheng Powder had no direct detrimental effect on cancer cells. When macrophages were co-cultured with cancer cells, Kangai Fuzheng Powder had toxic effect on cancer cells. After exposing macrophages to Kangai Fuzheng Powder, macrophages transformed into activated form and the mRNA level of tumor necrosis factor-alpha, interleukin-1beta, interleukin-6, interleukin-10 and monocyte chemotactic protein-1 was significantly enhanced. Phagocytic activity of macrophages was dramatically potentiated. Conclusions : We demonstrated that anti-cancer effect of Kangai Fuzheng Powder was related to activation of macrophages including enhanced cytokine production and phagocytic function.

• BMB Reports
• /
• v.53 no.10
• /
• pp.512-520
• /
• 2020

T-cell-based cancer immunotherapies, such as immune checkpoint blockers (ICBs) and chimeric antigen receptor (CAR)-T-cells, have significant anti-tumor effects against certain types of cancer, providing a new paradigm for cancer treatment. However, the activity of tumor infiltrating T-cells (TILs) can be effectively neutralized in the tumor microenvironment (TME) of most solid tumors, rich in various immunosuppressive factors and cells. Therefore, to improve the clinical outcomes of established T-cell-based immunotherapy, adjuvants that can comprehensively relieve multiple immunosuppressive mechanisms of TME are needed. In this regard, recent studies have revealed that metformin has several beneficial effects on anti-tumor immunity. In this mini-review, we understand the immunosuppressive properties of TME and how metformin comprehensively enhances anti-tumor immunity. Finally, we will discuss this old friend's potential as an adjuvant for cancer immunotherapy.

• The Korea Journal of Herbology
• /
• v.22 no.4
• /
• pp.187-199
• /
• 2007

Objectives : The present study purposed to compare the antioxidant effect, anti inflammatory effect and cancer cell multiplication inhibition effect of Fructificatio Inonoti Obliqui aqueous extract according to extraction temperature. Methods : We medicated animal models, which had experimental oxidation, with Fructificatio Inonoti Obliqui total extract and $50^{\circ}C$ low temperature leachate, and performed hematological analysis and blood chemical analysis with measuring SOD, GSH, catalase, NO and MDA content in the liver. In addition, we made comparative observation of anti inflammatory effect and anti-cancer effect. Results : Compared to the control group, both the group medicated with Fructificatio Inonoti Obliqui total extract and with $50^{\circ}C$ low-temperature leachate were found to decrease the number of thrombocytes in blood plasma and NO content while to increase SOD activity and catalase activity significantly. Both groups also showed anti-inflammatory effect against THP-1 cells and a multiplication inhibition effect against liver cancer cells and stomach cancer cells significantly. Conclusions : Both Fructificatio Inonoti Obliqui total extract and Fructificatio Inonoti Obliqui $50^{\circ}C$ low-temperature leachate have significant antioxidant effect, anti inflammatory effect and anti cancer effect.

• The Journal of Internal Korean Medicine
• /
• v.28 no.2
• /
• pp.294-303
• /
• 2007

Objectives : We are aimed to identify anti-tumor effects of realgar on some kinds of cancer cells through molecular biologic methods. Materials & Methods : We used 5 kinds of cancer cell lines: lung cancer cells(A549). stomach cancer cells(KATO) and neuroglioma cells(SUN-1118. U-87MG, U-373MG). We injected the boiled extracts of realgar $50{\mu}g$. $100{\mu}g$ to cultural media( ml )for 24 hours. We measured the killing effects on 5 kinds of cancer cells through inverted and fluorescence microscope, the suppressive effects on viability of those cells via XTT assay and the effects on the revelation of Bax and Bcl-2 proteins related to apoptosis by western blotting. Results : In the changes of morphology, the extracts of realgar showed more significant killing effects on all cancer cells. especially KATO, SNU-1118, U-87MG, U-373MG, than the control group with dose dependence, which was statistically significant. In XTT assay, the extracts of realgar showed more suppressive effects on viability of all cancer cells, especially KATO and U-373MG, than the control group with dose dependence, which was statistically significant. In the revelation of proteins related to apoptosis, the extracts of realgar increased the level of Bax and decreased that of Bcl-2 in all cancer cells with dose dependence. Conclusions : We identified that realgar had more anti-tumor effects on stomach cancer and neuroglioma than on lung cancer in the experiments above. However, these basic experiments were performed in vitro. We hope the anti-tumor effects of realgar will be practically identified through more progressive research.