• Archives of Pharmacal Research
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• v.17 no.1
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• pp.11-16
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• 1994

Cis-dichlorodiammineplatinum(II)(cisplatin) is one of the most effective antitumor agents currently available for cancer therapy. However, its clinical use has been limited by its severe side effects, especially nephrotoxicity. To evaluate the effect or radical scavengers on cisplatin nephrotoxicity in rats, cisplatin and Vitamin C were given intraperitoneally. Remarkable protective effects of Vitamin C against nephrotoxicity of cisplatin were observed when Vitamin C was administered to rats 1hr before cisplatin injection. hepatotoxicity induced by combination treament of cisplatin and Vitamin C was evaluated by measuring serum glutamic pyruvate transmainase(sGPT) and serum glutamic oxalate transminase(sGOT). Combination treatment did not affect the levels of sGPT and sGOT, and any combination treatment did not induce metallothionein biosynthesis in kidny, Vitamin C which has radical scavenging effect induce metallothionein biosynthesis in kidney. Vitamin C which has radical scavenging effect directly reduced nephrotoxicity of cisplatin in vivo. Thus, it seems that free radical is the cause of cisplatin nepthrotoxicity. Also, combination treatment did not reduce anticancer activity of cisplatin. The present results indicate that Vitamin C, when it is given with cisplatin, may provide protection against cisplatin nephrotoxicity without reducing anticancer activity.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.2
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• pp.585-588
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• 2014

Colorectal cancer is one of the most prevalent diseases all over the world. Early screening and start of chemotherapy is effective in decreasing mortality. This type of cancer can be controlled to some extent via a healthy diet rich in fruit and vegetables. Ginseng is a plant which has been consumed as a herbal medicine for thousands of years in Asian countries. Several in vitro and in vivo studies have shown that this plant not only reduces the incidence of colorectal cancer, but also improves patient's status by enhancing the effects of chemotherapy drugs. However, further studies are needed to prove this relationship. We briefly review ginseng and its components such as ginsenosides reported anticancer effects and their mechanisms of action. Understanding these relationships may produce insights into chemical and pharmacological approaches for enhancing the chemo preventive effects of ginsenosides and for developing novel anticancer agents.

• Journal of the Korean Society of Food Science and Nutrition
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• v.30 no.4
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• pp.732-738
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• 2001

This study was attempted to isolate and identify the anticancer compounds from Eucommia ulmoides leaves using a human colon cancer cell line HCT-116. The petroleum ether extracts with anticancer activity was chromatographed on silica gel TLC and finally anticancer compounds was purified by HPLC. Their chemical structures were roughly elucidate by UV-VIS absorption spectral data HPLC elution pattern and FAM/MS spectroscopy. From this study these compounds were suspected to be pheophytin a formed by the removal of $Mg^{2+}$ from chlorophyll a and pyropheophytina formed by the removal of acetate group from pheophytin a respectively. To confirm the anticancer effects against HCT-116 cancer cell petroleum ether extract fractions of column chromatography and fractions separated on TLC were tested. All samples tested including the extract of petroleum ether fractions of column chromatograph and three bands (0.13,0.19,0.25) of TLC appeared to inhibit the growth of HCT-116 cancer cell however especially 0.19 and 0.25 fractions separated on TLC plate revealed the strongest effect. These results suggest that chlorophyll derivatives in Eucommia ulmoides may be potential anticancer agents against a human colon cancer cell HCT-116.

• Mycobiology
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• v.51 no.4
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• pp.256-263
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• 2023

Species in the genus Trametes (Basidiomycota, Polyporales) have been used in natural medicine for a long time. Many studies reported that mycelia or fruiting bodies of Trametes spp. exhibited effects of antioxidant, anti-inflammatory, anticancer, and antimicrobial activities. However, comparative analysis in this genus is scarce due to limitation of morphological identification and the sample number. In this study, the 19 strains of seven Trametes species were chosen to generate a five-gene-based phylogeny with the 31 global references. In addition, 39 culture extracts were prepared for 13 strains to test for anticancer and antibacterial activities. Strong anticancer activities were found in several extracts from T. hirsuta and T. suaveolens. Anticancer activities of T. suaveolens, T. cf. junipericola and T. trogii were first described here. The antibacterial ability of T. versicolor and T. hirsuta extracts has been confirmed. The antibacterial activities of T. suaveolens have been reported at the first time in this study. These results suggest an efficient application of the genus Trametes as the drug resources especially for anticancer agents.

• Bulletin of the Korean Chemical Society
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• v.32 no.spc8
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• pp.3009-3016
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• 2011

To investigate the possible isosteric replacement of imidazolidinone moiety in 4-phenyl-N-arylsulfonylimidazolidinone for broad and potent anticancer agents, a series of 4-phenyl-l(N)-arylsulfonylimidazolidinones 6a-k, imidazolidinethione analogs 7a-i, and imidazolidine oxime analogs 8a-c were prepared and evaluated for their in vitro anticancer activity against four human cancer cell lines (human lung A549, human colon COLO205, human leukemia K562, human ovary SK-OV-3). Among all the derivatives of N-arylsulfonylimidazolidinone 6a-k, compounds 6f and 6g showed the best inhibition comparable to doxorubicin against all cancer cell lines. Increasing the carbon chain on alkyl moieties of carbamates as shown in 6c-g did not alter the activity. The imidazolidinethione analogs 7a-i and imidazolidin-2-one oxime derivatives 8a-c did not possess any good activity. Therefore, imidazolidinone moiety is the best pharmacophore among the 4-phenyl-Narylsulfonylimidazolidinone derivatives.

• Archives of Pharmacal Research
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• v.13 no.1
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• pp.19-23
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• 1990

A series of hexahydro-s-triazine derivative were prepard. Cytotoxic activity testing using mouse leukemia cells (p 388) and antimicrobial testing indicated that the compounds which contain isoxazolyl moiety higher activity than those containing other hetercyclic moieties.

• Journal of Microbiology and Biotechnology
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• v.14 no.6
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• pp.1176-1181
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• 2004

The cytotoxic activities of Cinnamomum cassia (Blume) bark-derived materials toward six human HeLa epithelioid cervix, A549 lung, SK-OV-3 ovarian, SK-MEL-2 melanoma, XF-498 central nerve system, and HCT-15 colon tumor cell lines were evaluated by using sulforhodamine B assay and compared to those of the anticancer agents, cisplatin and mitomycin C. The biologically active constituent of the Cinnamomum bark was characterized as trans­cinnamaldehyde by spectroscopic analysis. The cytotoxic activity of cinnamaldehyde against HeLa, SK-MEL-2, and HCT -15 cell lines was comparable to that of cisplatin and mitomycin C. The compound showed lower activity against A549, SK-OV-3, and XF-498 cell lines than the anticancer agents. Eugenol exhibited moderate activity against SK-OV­3, XF-498, and HCT-15 tumor cells, and trans-cinnamic acid, cinnamyl alcohol, $\alpha-pinene,\;and\;\beta-pinene$ showed little or no activity against model tumor cells. Cinnamaldehyde was not mutagenic against four strains (TA 98, TA 100, TA 1535, and TA 1537) of Salmonella typhimurium (Castel and Chalm). These results indicate at least one pharmacological action of C. cassia.

• YAKHAK HOEJI
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• v.52 no.1
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• pp.67-72
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• 2008

The use of doxorubicin, which is one of the most effective anticancer agents, is often limited by occurrence of acquired resistance in tumor cells. GSH has been shown to be involved in the development of this drug resistance. Transcription factor Nrf2 governs the expression of GSH synthesizing glutamylcysteine ligase (GCL), as well as multiple phase 2 detoxifying enzymes. Here we show that Nrf2 is one of factors determining doxorubicin sensitivity. Nrf2-deficient fibroblasts (murine embryonic fibroblasts, MEF) were more susceptible to doxorubicin mediated cell death than wild-type cells. Doxorubicin treatment elevated levels of Nrf2-regulated genes including NAD(P)H: quinone oxidoreductase (Nqo1) and GCL in wild-type fibroblasts, while no induction was observed in Nrf2-deficient cells. Doxorubicin resistance in human ovarian SK-OV cells was reversed by treatment with L-buthionine-sulfoxamine (BSO), which is depleting intracellular GSH. Finally, transfection of SK-OV cells with Nrf2 siRNA resulted in exacerbated cytotoxicity following doxorubicin treatment compared to scrambled RNA control. These results indicate that the Nrf2 pathway, which plays a protective role in normal cells, can be a potential target to control cancer cell resistance to anticancer agents.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.7
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• pp.2807-2811
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• 2015

Scorpion venom peptides recently have attracted attention as alternative chemotherapeutic agents that may overcome the limitations of current drugs, providing specific cytotoxicity for cancer cells with an ability to bypass multidrug-resistance mechanisms, additive effects in combination therapy and safety. In the present study, BmKn-2 scorpion venom peptide and its derivatives were chosen for assessment of anticancer activities. BmKn-2 was identified as the most effective against human oral squamous cells carcinoma cell line (HSC-4) by screening assays with an $IC_{50}$ value of $29{\mu}g/ml$. The BmKn-2 peptide killed HSC-4 cells through induction of apoptosis, as confirmed by phase contrast microscopy and RT-PCR techniques. Typical morphological features of apoptosis including cell shrinkage and rounding characteristics were observed in treated HSC-4 cells. The results were further confirmed by increased expression of pro-apoptotic genes such as caspase-3, -7, and -9 but decrease mRNA level of anti-apoptotic BCL-2 in BmKn-2 treated cells, as determined by RT-PCR assay. In summary, the BmKn-2 scorpion venom peptide demonstrates specific membrane binding, growth inhibition and apoptogenic activity against human oral cancer cells.

• Journal of Microbiology and Biotechnology
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• v.30 no.5
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• pp.733-738
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• 2020

Glucose deprivation and hypoxia frequently occur in solid tumor cells, including pancreatic cancer cells. Glucose deprivation activates the unfolded protein response (UPR) and causes the up-regulation of glucose-regulated protein 78 (GRP78). Induction of GRP78 has been shown to protect cancer cells. Therefore, shutting down of GRP78 expression may be a novel strategy in anticancer drug development. Based on this understanding, a screening system established for anticancer agents that exhibit selective cytotoxicity on pancreatic cancer cells under glucose-deprived conditions. To test this hypothesis, the new compounds isolated, pancastatin A (PST-A) and B (PST-B), from Ponciri Fructus. PST-A and B were identified as glabretal triterpenoid moieties by electrospray ionization mass spectrometry and nuclear magnetic resonance spectroscopic methods. PST-A and B suppressed the accumulation of the UPR hallmark gene, GRP78, during glucose deprivation. Furthermore, PST-A and B showed selective cytotoxicity on PANC-1 pancreatic cancer cells under glucose deprivation. Interestingly, PST-A and B had no effect on these cells under normal growth conditions. Our results suggest that PST-A and B act as novel therapeutic agents to induce selective cell death in glucose-deprived pancreatic cancer cells.