• Title/Summary/Keyword: Anticancer agent

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Preparation and Characterization of Deoxycholic Acid-Grafted Hyaluronic Acid as a Durg Carrier (약물전달체로서 디옥시콜산이 결합된 히알루론산의 제조와 특성)

  • Choi, Chang-Yong;Park, Jun-Kyu;Kim, Won-Suk;Jang, Mi-Kyeong;Nah, Jae-Woon
    • Polymer(Korea)
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    • v.35 no.2
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    • pp.119-123
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    • 2011
  • To develop hyaluronic acid (HA)-based anticancer agent carrier, hyaluronic acid was chemically modified with the hydrophobic group of deoxycholic acid(DA). The physicochemical properties of the deoxycholic acid-conjugated HA (HADA) were investigated by using $^1H$ NMR, FTIR spectrophotometer and TEM. Paclitaxel (Tx)-loaded HADA nanoparticles were prepared by a dialysis method. The loading efficiency of drug and drug contents of Tx-loaded HADA nanoparticles (HADA-Tx) were measured by HPLC. The anticancer activity of HADA-Tx was investigated by its cytotoxicity against KB cell in vitro. The HADA-Tx was shown to have the superior potential for the anticancer drug delivery.

AMP-activated protein kinase determines apoptotic sensitivity of cancer cells to ginsenoside-Rh2

  • Kim, Min-Jung;Yun, Hee;Kim, Dong-Hyun;Kang, Insug;Choe, Wonchae;Kim, Sung-Soo;Ha, Joohun
    • Journal of Ginseng Research
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    • v.38 no.1
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    • pp.16-21
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    • 2014
  • Ginseng saponins exert various important pharmacological effects with regard to the control of many diseases, including cancer. In this study, the anticancer effect of ginsenosides on human cancer cells was investigated and compared. Among the tested compounds, ginsenoside-Rh2 displays the highest inhibitory effect on cell viability in HepG2 cells. Ginsenoside-Rh2, a ginseng saponin isolated from the root of Panax ginseng, has been suggested to have potential as an anticancer agent, but the underlying mechanisms remain elusive. In the present study, we have shown that cancer cells have differential sensitivity to ginsenoside-Rh2-induced apoptosis, raising questions regarding the specific mechanisms responsible for the discrepant sensitivity to ginsenoside-Rh2. In this study, we demonstrate that AMP-activated protein kinase (AMPK) is a survival factor under ginsenoside-Rh2 treatment in cancer cells. Cancer cells with acute responsiveness of AMPK display a relative resistance to ginsenoside-Rh2, but cotreatment with AMPK inhibitor resulted in a marked increase of ginsenoside-Rh2-induced apoptosis. We also observed that p38 MAPK (mitogen-activated protein kinase) acts as another survival factor under ginsenoside-Rh2 treatment, but there was no signaling crosstalk between AMPK and p38 MAPK, suggesting that combination with inhibitor of AMPK or p38 MAPK can augment the anticancer potential of ginsenoside Rh2.

The Role of HS-1200 Induced Autophagy in Oral Cancer Cells

  • Jang, Nam-Mi;Oh, Sang-Hun;Kim, In-Ryoung;Park, Hae-Ryoun;Park, Bong-Soo
    • International Journal of Oral Biology
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    • v.38 no.3
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    • pp.93-100
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    • 2013
  • Bile acids and synthetic bile acid derivatives induce apoptosis in various kinds of cancer cells and thus have anticancer properties. Recently, it has been suggested that autophagy may play an important role in cancer therapy. However, few data are available regarding the role of autophagy in oral cancers and there have been no reports of autophagic cell death in OSCCs (oral squamous cell carcinoma cells) induced by HS-1200, a synthetic bile acid derivative. We thus examine whether HS-1200 modulates autophagy in OSCCs. Our findings indicate that HS-1200 has anticancer effects in OSCCs, and we observed in these cells that autophagic vacuoles were visible by monodansylcadaverine (MDC)and acridine orange staining. When we analyzed HS-1200-treated OSCC cells for the presence of biochemical markers, we observed that this treatment directly affects the conversion of LC-3II, degradation of p62/SQSTM1 and full-length beclin-1, cleavage of ATG5-12 and the activation of caspase. An autophagy inhibitor suppressed HS-1200-induced cell death in OSCCs, confirming that autophagy acts as a pro-death signal in these cells. Furthermore, HS-1200 shows anticancer activity against OSCCs via both autophagy and apoptosis. Our current findings suggest that HS-1200 may potentially contribute to oral cancer treatment and thus provide useful information for the future development of a new therapeutic agent.

Effects of Korean Red Ginseng extract on busulfan-induced dysfunction of the male reproductive system

  • Jung, Seok-Won;Kim, Hyeon-Joong;Lee, Byung-Hwan;Choi, Sun-Hye;Kim, Hyun-Sook;Choi, Yang-Kyu;Kim, Joon Yong;Kim, Eun-Soo;Hwang, Sung-Hee;Lim, Kwang Yong;Kim, Hyoung-Chun;Jang, Minhee;Park, Seong Kyu;Cho, Ik-Hyun;Nah, Seung-Yeol
    • Journal of Ginseng Research
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    • v.39 no.3
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    • pp.243-249
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    • 2015
  • Background: Anticancer agents induce a variety of adverse effects when administered to cancer patients. Busulfan is a known antileukemia agent. When administered for treatment of leukemia in young patients, busulfan could cause damage to the male reproductive system as one of its adverse effects, resulting in sterility. Methods: We investigated the effects of Korean Red Ginseng extract (KRGE) on busulfan-induced damage and/or dysfunction of the male reproductive system. Results: We found that administration of busulfan to mice: decreased testis weight; caused testicular histological damage; reduced the total number of sperm, sperm motility, serum testosterone concentration; and eventually, litter size. Preadministration of KRGE partially attenuated various busulfan-induced damages to the male reproductive system. These results indicate that KRGE has a protective effect against busulfan-induced damage to the male reproduction system. Conclusion: The present study shows a possibility that KRGE could be applied as a useful agent to prevent or protect the male reproductive system from the adverse side effects induced by administration of anticancer agents such as busulfan.

Beta glucan: Heath benefits of optimal ingredients via the mixture ratio of rice bran and Sarcodon aspratus

  • Seo, Yu-Ri;Kim, Hye-Been;Cheong, Kyu-Min;Lim, Ki-Taek
    • Proceedings of the Korean Society for Agricultural Machinery Conference
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    • 2017.04a
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    • pp.101-101
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    • 2017
  • Beta-glucan is a polymerized polysaccharide on beta-1,3 chemical bonds. It has the main pharmacological action of various anticancer mushrooms and is colorless and odorless. In addition, it enhances phagocytosis of macrophages against mycobacterium tuberculosism and increases resistance of host against food poisoning bacteria. Owing to these advantages, beta-glucan was used in various health supplement foods such as immune boosters, hypotensive agent and hypoglycemic agent. Our study was aimed to investigate the effective components of beta-glucan, which was optimized via the contents of Sarcodon aspratus and rice bran. First, the mixture ratio condition of Sarcodon aspratus and rice bran were respectively 10:0, 7:3, 5:5, 3:7, and 0:10. The raw materials were fabricated using hot water extraction method. Distilled water of 100 mL was added to the raw material and extracted. After the extraction processed, the content of effective components was analyzed. The absorbance of beta-glucan was measured using a beta-glucan kit (Megazyme, (1-3) (1-4) BETA-D-GLUCAN ASSAY KIT). The absorbance analysis was repeated three times for accurate analysis. After the extracts were lyophilized, the yields of extracted raw materials according to the mixture ratio conditions of Sarcodon aspratus and rice bran (10:0, 7:3, 5:5, 3:7, and 0:10) were respectively 33.1%, 34.5%, 35.3%, 30.7%, and 24.3%. The absorbance was 1.52, 1.47, 1.50, 1.79, and 1.56, respectively. As a result, the optimum ratio of beta-glucan is 3:7 at Sarcodon aspratus and rice bran. This study suggested that the optimal amount of beta-glucan could be used as a health supplement foods and food additive such as immune boosters, hypotensive agent and hypoglycemic agent. However, the new condition (temperature, time) of hot water extraction to maximize the content of beta-glucan could be considered, could be necessary to compare with the existing extracts.

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Candicidal Action of Resveratrol Isolated from Grapes on Human Pathogenic Yeast C. albicans

  • Jung, Hyun-Jun;Seu, Young-Bae;Lee, Dong-Gun
    • Journal of Microbiology and Biotechnology
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    • v.17 no.8
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    • pp.1324-1329
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    • 2007
  • Resveratrol (3,5,4'-trihydroxystilbene) is a naturally occurring, multi-biofunctional chemical existing in grapes and various other plants as a polyphenol type, and it is one of the best known natural anticancer and antiatherosclerosis reagents. In this study, we investigated the antifungal action by resveratrol in Candida albicans, which is a human infectious fungi as an agent of candidiasis. Resveratrol displayed potent fungicidal activity in an energy-dependent manner, without any hemolytic effects against human erythrocytes. It was found that the serum-induced mycelial forms, which playa crucial role in the pathogenesis of C. albicans during host tissue invasion, were disrupted by resveratrol. To understand the correlation between lethal effects and resveratrol action, we examined the physiological changes of C. albicans. A significant accumulation of intracellular trehalose was induced by stress responses to resveratrol action, and a remarkable arrest of cell-cycle processes at the S-phase in C. albicans occured. Therefore, the fungicidal effects of resveratrol demonstrate that this compound is a potential candidate as an antifungal agent in treating infectious diseases by candidal infections.

Neuropeptide Y improves cisplatin-induced bone marrow dysfunction without blocking chemotherapeutic efficacy in a cancer mouse model

  • Park, Min Hee;Jung, In Kyung;Min, Woo-Kie;Choi, Jin Ho;Kim, Gyu Man;Jin, Hee Kyung;Bae, Jae-sung
    • BMB Reports
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    • v.50 no.8
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    • pp.417-422
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    • 2017
  • Cisplatin is the most effective and widely used chemotherapeutic agent for many types of cancer. Unfortunately, its clinical use is limited by its adverse effects, notably bone marrow suppression leading to abnormal hematopoiesis. We previously revealed that neuropeptide Y (NPY) is responsible for the maintenance of hematopoietic stem cell (HSC) function by protecting the sympathetic nervous system (SNS) fibers survival from chemotherapy-induced bone marrow impairment. Here, we show the NPY-mediated protective effect against bone marrow dysfunction due to cisplatin in an ovarian cancer mouse model. During chemotherapy, NPY mitigates reduction in HSC abundance and destruction of SNS fibers in the bone marrow without blocking the anticancer efficacy of cisplatin, and it results in the restoration of blood cells and amelioration of sensory neuropathy. Therefore, these results suggest that NPY can be used as a potentially effective agent to improve bone marrow dysfunction during cisplatin-based cancer therapy.

Reproductive Toxicity of DA-125, A New Anthracycline Anticancer Agent: Peri- and Postnatal Study in Rats (새로운 안트라사이클린계 항암제 DA-125의 생식독성연구: 랫트 주산기 및 수유기시험)

  • 정문구;이순복;한상섭;노정구
    • Biomolecules & Therapeutics
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    • v.3 no.1
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    • pp.38-46
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    • 1995
  • DA-125, a new anthracycline antitumor antibiotic, was administered at dose levels of 0, 0.04, 0.2 and 1.0 mg/kg/day intravenously to pregnant and subsequently delivered Sprague-Dawley rats from day 17 of gestation to day 21 of lactation. Effects of test agent on general toxicity of dams and growth, behaviour and mating performance of F1 offspring were examined. At 1 mg/kg, one out of the twentytwo dams showed difficult delivery, characterized by a stillbirth. Reduction in body weight, loss in food intake, and decrease in spleen weight were also observed in dams. In addition, the lower rates of successful performances in memory test (28.6%) and necrosis of tail end (9.5%) were seen in F1 offspring. At 0.04 and 0.2 mg/kg, no toxic effect on dams and F1 offspring was observed. There were no malformed Fl and F2 fetuses in all groups. The results indicate that the no effect dose levels(NOELs) of DA-125 are 0.2 mg/kg/day for dams and Fl offspring, and over 1 mg/kg/day for F2 fetuses.

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Somatic Embryogenesis and Plant Regeneration from Stem Tissues of Orostachys japonicus A. Berger

  • Song, Min-Jung;Park, Young-Goo
    • Journal of Plant Biotechnology
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    • v.34 no.3
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    • pp.181-187
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    • 2007
  • Orostachys japonicus A. Berger is a Perennial herbaceous plant which has been traditionally used as an anti-inflammatory agent to treat hepatitis and as an anticancer agent. The objective of this study was 1) to establish and proliferate in vitro plant of O. japonicus 2) to induce indirect somatic embryogenesis from O. japonicus. General calli and embryogenic calli in all ranges of 2,4-D and BA combination, were induced and were best at 22% (embryogenic cell) in 5.0 mg/L 2,4-D and 0.5 mg/L BA combination. Embryogenic cell line was maintained by subculture at 2 week intervals and transferred to solid and liquid medium for embryo formation. In solid medium culture, globular and heart shaped embryos were observed in MS medium containing 5.0 mg/L 2,4-D and 0.5 mg/L BA combination. The number of embryos was 6.5 per 0.5 g cell, and then the immature embryos transferred to MS basal medium for embryo development. In a suspension culture of embryogenic cells, globular and heart shaped embryos were emerged in MS medium supplemented with 3.0 mg/L 2,4-D and 0.3 mg/L BA combination after 10 days of incubation. The embryo formation rate was about 33% by suspension culture. The ratio of embryo germination was 60.9%, on the other side, the root formation rate was 74.3% in 1/2 MS continuously.

Deoxyribonucleic Acid Was Responsible for the Anticoagulatory Effect of an Earthworm, Lumbricus rubellus

  • Paik, Seung-R.;Woo, Jeong-Im;Kim, Gyoung-Mi;Cho, Jin-Mo;Yu, Kyoung-Hee;Chang, Chung-Soon
    • BMB Reports
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    • v.30 no.1
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    • pp.37-40
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    • 1997
  • Earthworm extracts are known for anti-inflammatory, analgesic. antipyretic, and anticancer effects but can also influence blood circulation. It was previously shown that an earthworm, Lumbricus rubelius. contained a water-extractable anticoagulant which was a heat- and acid-stable molecule with hydrophilic property. In order to uncover the biochemical nature of this molecule, the anticoagulant was processed with various hydrolases such as trypsin, DNase, RNase. and lysozome. When the digested samples were analyzed with an in vitro coagulation test measuring activated partial thromboplastin time (APTT) and agarose gel electrophoresis, the anticoagulant proved to be a relatively homogeneous DNA fragment with relative molecular size around 72 base pairs. Interestingly, the activity was further stimulated with a trypsin digestion. RNA. on the other hand, did not prolong the APTT. It was also demonstrated that the DNA accelerated the antithrombin III (AT-III) inhibition of thrombin from $IC_{50}$ of 0.34 to 0.16 unit determined with S-2238 as a substrate, whereas heparin, a popular anticoagulant. shifted the value to 0.05. Therefore, it is suggested that the DNA could be considered as an alternative antithrombotic agent to heparin, which would exhibits bleeding side effects.

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