• Archives of Pharmacal Research
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• v.29 no.9
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• pp.721-727
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• 2006

To continue exploration of structure activity relationship of novel 1-(indoline-5-sulfonyl)-4-phenylimidazolidinones (1) reported as anticancer agent with broad spectrum, three 1-(arylsulfonyl)-4-vinylimidazolidinones (2) were synthesized from methyl serinate (3) in 8 steps. Reaction of intermediate 2-phenoxycarbonylaminobut-3-enyl p-toluenesulfonate (10) with arylsulfonamide in the presence of potassium carbonate produced corresponding 2 and N-(4-vinyloxazolidin-2-yl)arylsulfonamide 11 in approximately equal ratio. This reaction is believed to undergo through urea intermediate 16 as shown in scheme 3. 1-Arylsufonyl-4-vinylimidazolidinones 2 show much reduced activity against human colon carcinoma (Colo205), human chronic myelogenous leukemia (K562), and human ovarian adenocarcinoma (SK-OV-3) and compatible activity against human lung carcinoma (A549) compared to 1. Therefore phenyl at 4-position should be the optimum planar motif for the activity of 1.

• Asian Pacific Journal of Cancer Prevention
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• v.14 no.11
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• pp.6653-6656
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• 2013

Background: The single most common proto-oncogene change in human neoplasms is a point mutation in RAS genes. A wide range of variation in frequency of KRAS mutations has been seen in hematologic malignancies. Despite this, RAS roles in leukemogenesis remain unclear. The frequency of KRAS mutations in CML has been reported to be between zero an 10%. Many attempts have been done to develop an anti-RAS drug as a therapeutic target. Materials and Methods: This cross sectional study was performed in Mashhad University of Medical Sciences, Mashhad, Iran from 2010-2012. In 78 CML patients (diagnosed according to WHO 2008 criteria) in chronic or accelerated phases, KRAS mutations in codons 12 and 13 were analyzed using a modified PCR-restriction fragment length polymorphism (RFLP) method. Results: We did not detect any KRAS mutations in this study. Conclusions: KRAS mutations are overall rare in early phase CML and might be secondary events happening late in leukemogenesis cooperating with initial genetic lesions.

• The Korean Journal of Nuclear Medicine
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• v.35 no.4
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• pp.286-287
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• 2001

A 44 year-old male patient was undergoing diagnosis and therapy for acute myelogenous leukemia (AML, M2). On physical examination a thyroid mass was palpated in the left lower lobe. He had palpitation and intolerance to heat. Thyroid function tests revealed hyperthyroidism; T3: 150ng/dl (N:60-90), fT4: 2.26 ng/dl (N:0.70-1.80), TSH: 0.01 ulU/ml (N:0.25-5.00). Ultrasonography demonstrated a hypoechoic mass with scattered calcifications measuring 2.55 2.03 3.64 cm in size. F-18 FDG camera-based PET scan performed as a follow-up study of AML revealed a focal increased uptake in the left neck, where an autonomous nodule was detected on Tc-99m thyroid scan. After the diagnosis of toxic autonomous nodule, Goetz disease, he underwent surgical nodulectomy. Microscopically, the nodule contained follicular proliferation with degenerative change but without evidence of thyroid carcinoma. Focal uptake in autonomous thyroid nodules is due to increased glycolysis within the nodules.

• The Journal of Korean Medicine
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• v.18 no.1
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• pp.157-168
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• 1997

The purpose of this study is the separation of biologically active ingredients from Coptidis Rhizoma which has been widely used as one of oriental herbal medicine for body fever. In this study, berberine-type alkaloids were tested on their biological activities in the aspect of antibacterial, antitumor, anti-herpetic and anti-HIV activity. Contents of five major alkaloids for the various origin of Coptidis Rhizoma were assayed by HPLC. As the results, the content of berberine from Coptis chinensis and Coptis japonica were 6.78% and 7.09%, respectively. The contents of coptisine, jatrorrhizine, berberastine from Coptis chinensis were higher than those of Coptis japonica. The amount of palmatine from both species were almost the same. Surprisingly for antitumor experiment, all compounds have been shown remarkable activity, especially against SNU-l(human stomach cancer) cell line. Among the compounds purified through column chromatography, palmatine, coptisine, and jatrorrhizine inhibited the growth of K-562(human chronic myelogenous leukemia) cell line whereas jatrorrhizine has been shown the effective inhibition of A-549 (human lung) cell line at the same time.

• Archives of Pharmacal Research
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• v.18 no.6
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• pp.396-401
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• 1995

As a part of trials to develop the antitumor agent from tannins isolated from plants, the antitumor activity of peduculagin, an ellagitannin, isolated from Alnus hirsuta var. microphylla was examined in vitro and in vivo. In vitro, the cytotoxicity was determined by 0.4% typanblue dye exclusion method. peduculagin showed the dose-dependent cytotoxicity against human chronic myelogenous leukemia (K-562), human promyelocytic leukemia (HL-60), mouse lymphoid neoplasm (P388), mouse lymphocytic leukemia (L1210) and mouse sarcoma 180(S180) cell lines. $ED_{50}\; values\; (ED_{50})$ of each cell line were 5.30, 0.92, 2.78, 9.35 and $1.38 \mug/ml$ respectively. The most sensitive cell line was HL-60. In vivo, pedunculagin was administered to ICR mouse with the doses of 50 and $100{\;}{\mu}g/ml$intraperitoneally once at 20 days before S180 inoculation. peduculagin showed the antitumor activity and its T/C ratio (%) was 120.82% in the group of both concentrations.

• Bulletin of the Korean Chemical Society
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• v.32 no.3
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• pp.947-955
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• 2011

The complexes [Pd(bpy)(Hex-dtc)]$NO_3$ and [Pt(bpy)(Hex-dtc)]$NO_3$ (bpy is 2,2'-bipyridine and Hex-dtc is hexyldithiocarbamato ligands) were synthesized and characterized by elemental analysis and spectroscopic studies. The cytotoxicity assay of the complexes has been performed on chronic myelogenous leukemia cell line, K562, at micromolar concentration. Both complexes showed cytotoxic activity far better than that of cisplatin under the same experimental conditions. The binding parameters of the complexes with calf thymus DNA (CT-DNA) was investigated using UV-visible and fluorescence techniques. They show the ability of cooperatively intercalating in CT-DNA. Gel filtration studies demonstrated that platinum complex could cleave the DNA. In the interaction studies between the Pd(II) and Pt(II) complexes with CT-DNA, several binding and thermodynamic parameters have been determined, which may provide deeper insights into the mechanism of action of these types of complexes with nucleic acids.

• YAKHAK HOEJI
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• v.42 no.4
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• pp.345-352
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• 1998

Praecoxin A, an ellagitannin, purified from Alnus hirsuta var.microphlla was evaluated on the antitumor activity. Praecoxin A had the significant cytotoxicity to s ix tumor cell lines: human chronic myelogenous leukemia K-562, human promyelocytic leukemia HL-60, mouse leukemia P388, mouse lymphocytic leukemia L-1210, sarcoma-l8O, mouse lymphoma L5178Y except L-1210. And the most sensitive cell line was K-562 ($ED_{50}=2.43{\mu}g/ml$). The $ED_{50} of praecoxin A against HL-60, P388, L-1210, sarcoma7l8O and L5178Y were 6.28, 8.66, 10.00, 7.01, $9.32{\mu}g/ml$, respectively. Praecoxin A showed the increasing effect in life span by 36.8% on the 1st day after treatment of 10mg/kg in mice bearing sarcoma-180 tumor cells (ascitic form) via NCI (National Cancer Institute, U.S.A.) protocol in vivo assay. As a result, praecoxin A is considered to show the antitumor activity.

• Journal of the East Asian Society of Dietary Life
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• v.11 no.1
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• pp.19-25
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• 2001

This study was performed to examine the antimutagenic and cytotoxic effects of potato vinegar and commercial vinegars(cider, brown rice, persimmon vinegars) on Salmonella typhimurium TA98, TA100 and cancer cell lines using Ames test and cytotoxicity assay, respectively. In Ames test, all vinegars did notexhibit any mutagenicity , but showed substantial inhibitory effects against N- methyl - N -nitro - N- nitrosog -uanidine(MNNG) , 4-nitroquinoline-1-oxide(4NQO), 3-amino-1,4-dimethyl-5H-pyrido(4,3-b)indol(Trp-P-1)and benzo( $\alpha$ )pyrene(B( $\alpha$ )P). The number of revertants per plate decreased significantly when these vinegars(80 ug/plate) were added to the assay system using TA100 strain. Especially, potato vinegar(80 ug/plate) showed high inhibition rate of 69.9% against mutagenicity of B( $\alpha$ )P on TA100 strain. In the cytotoxicity assay, these vinegars also showed prominent cytotoxic activity against human cancer cell lines. Potato vinegar(10 ug/well) showed the strongest cytotoxic effect against HT1080 (fibrosacoma cell) andK562 ( myelogenous leukemia) at the same concentration when compared with other vinegars.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2003.04a
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• pp.102-102
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• 2003

The present study has been undertaken to characterize availability of camellia(Camellia japonica L.) as a medicinal plant with antineoplastic and chemosensitizing activities. The crude extracts from fresn camellia flower, young leaves and nutraceutical tea of camellia leaf and flower buds were evaluated on their potential activities against various human cancer cells and multidrug resistance to cancer cells in vitro. The range of cytotoxicity displayed from 120$\mu\textrm{g}$/mL to 200$\mu\textrm{g}$/mL. Catemix 1(CT-1) mixed with camellia and green tea showed high toxicity(respectively IC$\sub$50/=l16$\mu\textrm{g}$/mL, 129$\mu\textrm{g}$/mL) against AML-2/WT, acute myelogenous leukemia cell and MCF-7, brest adenocarcinoma pleual effusion cell. Generally camellia tea mixed with green tea showed higher cytotoxicity than the other camellia teas mixed with some herbs(CH). Methanol extract of steamed camellia tea and roasted camellia tea had a chemosensitizing effect to reverse Pgp-mediated MDR. In addition, camellia flower tea of insignificant cytotoxicity, chemosensitizing effect were increased remarkably chemosensitizing effect in mixed flower tea with some herbs.

• Hip & pelvis
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• v.35 no.3
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• pp.147-156
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• 2023

Osteonecrosis of the femoral head (ONFH), a condition characterized by the presence of a necrotic bone lesion in the femoral head, is caused by a disruption in the blood supply. Its occurrence is more common in young and middle-aged adults and it is the main reason for performance of total hip arthroplasty in this age group. Its incidence is increasing along with increased use of glucocorticoids for management of adjuvant therapy for treatment of leukemia as well as organ transplantation and other myelogenous diseases. Current information on etiology and pathogenesis, as well as natural history, stage system, and treatments is provided in this review. A description of the Association Research Circulation Osseous (ARCO) criteria for classification of glucocorticoids-and alcohol-associated ONFH, 2019 ARCO staging system, and 2021 ARCO classification using computed tomography for the early stages of ONFH is also provided.