• Archives of Pharmacal Research
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• v.19 no.6
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• pp.535-542
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• 1996

Seven isoazamitosene derivatives, mitomycin analogues, were synthesized and tested for cytotoxicities against leukemia and gastric cancer cell lines. Preparation of a pyrrolo[1, 2-a]benzimidazole (3) (azamitosene ring system) was completed by utilizing the Lewis acid-catalized cyclization, with .omicron.-chloronitrotoluene as the starting material. Nitration of 3 produced a mixtue of two isomers (5-nitro isomer (4) and 7-nitro isomer (5)) in product ratio of 36 : 52. 4 was directly converted into quinone (7) by reduction and Fremy oxidaton. Finally, quinone derivatives (8, 9, 10, and 11) were synthesized by 1, 4-addition of 7 with cyclic secondary amines. From above-mentioned 5, 8-nitro compound (15) was prepared in 4 steps. At pH 3, Fremy oxidation of 15 produced quinone (16), whereas iminoquinone derivatives (17a and 17b) at pH 7. Isoazamitosene derivatives (8, 9, 10, and 11), containing cyclic amino groups at the 7-position, showed potent cytotoxicity on P388, SNU-1, and KHH tumor cell lines. Among them, 8 had stronger cytotoxicity against SNU-1 cell line than mitomycin and adriamycin. Considering these results, isoazamitosene derivatives may had unique cytotoxicity profiles. However, isoiminoazamitosene derivatives (17a and 17b) revealed very weak cytotoxicity.

• YAKHAK HOEJI
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• v.54 no.1
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• pp.27-31
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• 2010

Xanthohumol, a prenylated chalcone of the Hop plant (Humulus lupulus L.), has been reported to suppress tumor growth. 4-hydroxychalcone and isobavachalcone are chalcone derivatives and they have similar structure with xanthohumol. In the present study, we investigated the cytotoxic activities of chalcone and its derivatives, 4-hydroxychalcone, xanthohumol, and isobavachalcone, in MCF-7 and adriamycin resistant MCF-7 (MCF-7/ADR) breast cancer cells and HT-1080 fibrosarcoma cells. In a cell viability assay using 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) reagent, chalcone and 4-hydroxychalcone decreased cell viability in HT-1080 cells, but not in MCF-7 and MCF-7/ADR cells. Isobavachalcone showed similar cytotoxicity in HT-1080 cells, and only limited cytotoxicity in MCF-7 and MCF-7/ADR cells at very high concentration (50 ${\mu}M$). In contrast, xanthohumol showed concentration-dependent cytotoxicity in MCF-7, MCF-7/ADR, and HT-1080 cancer cells. Taken together, the structure-activity relationship of chalcone and its derivatives indicate that chalcones may be valuable cytotoxic compounds against selective cancer types.

• Tuberculosis and Respiratory Diseases
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• v.69 no.2
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• pp.129-133
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• 2010

Extramedullary plasmacytoma (EMP) is a rare disorder that typically occurs in the upper airway. Although the condition rarely arises in the lungs, a few cases have been reported. Here, we report a case of pulmonary plasmacytoma in 66-year-old man, who had been treated with VAD (vincrestine, adriamycin, dexamethasone) chemotherapy for multiple myeloma. The patient had been declared clear of multiple myeloma after 4 cycles of chemotherapy. Three months later, the patient had multiple masses visible on computed tomography (CT) and on positron emission tomography-computed tomography (PET-CT) with hot uptake. Subsequent studies using CT-guided needle biopsy and immunohistochemical stain showed pulmonary plasmacytoma. Bone marrow biopsy, serum, and urine M protein tests were repeated, showing no evidence of multiple myeloma. Pulmonary plasmacytomas, as extramedullary plasmacytomas, were considered an isolated manifestation of multiple myeloma recurrence. We treated the patient with concurrent chemoradiotherapy and the pulmonary plasmacytomas regressed dramatically.

• Applied Microscopy
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• v.44 no.4
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• pp.117-122
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• 2014

We previously have reported that periglomerular calponin expression of the glomerulosclerotic glomeruli in the chronic nephropathy. To investigate the role of calponin during glomerulosclerosis, we examined the detailed localization pattern of calponin in chronic nephropathy rat model using serial morphometric analysis. Male Sprague-Dawley rats were used, and chronic nephropathy models were established at 8 and 12 weeks after single intraperitoneal injection of adriamycin (10 mg/kg body weight; n=5). In nephropathy models, 16.3% (8 weeks) and 23.4% (12 weeks) glomeruli showed calponin-positivity at glomerular area. In all these glomeruli, showing various sclerotic changes, calponin-immunoreactivities were present only both the glomerular parietal epithelial cells (PECs) and periglomerular myofibroblasts (PMFs). However, in the glomeruli with weak calponin-positive, immunoreactivity was mostly detected in PECs, suggesting that calponin may be expressed in PECs earlier than in PMFs in the glomerulosclerotic change. Some calponin-positive PECs invaded glomerular tuft with loop-shaped projection, and around this projection, nestin expression of glomerular tuft were much reduced. These results suggested that calponin-positive PECs may play a key role in the development of glomerulosclerosis, and direct contact with PECs and glomerular tuft may be more important to degenerative changes of glomeruli.

• Journal of Yeungnam Medical Science
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• v.14 no.1
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• pp.67-76
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• 1997

The occurrence of multidrug resistance (MDR) is one of the main obstacles in the successful chemotherapeutic treatment of cancer. In this study The gene expressions of multidrug resistance-associated protein (MRP), c-myc and c-fos were investigated in L1210 cells. Adriamycin- or vincristine-resistant L1210 cells, L1210AdR or L1210VcR, respectively, has been identified to overexpression of mdr1 gene. The expression leve of MRP gene in L1210AdR and L1210Cis was more decreased than that in L1210 cells. The c-myc and c-fos genes were expressed both in L1210 and resistant sublines. In L1210AdR, the expressions level of c-myc and c-fos genes were decreased than in L1210. However, in L1210VcR and L1210Cis, c-myc and c-fosgene expressionwere rather increased than L1210. These results suggested that MRP does not contribute in resistance of drug-resistant L1210 cells and there is no relations between MRP and mdr1 gene expression. The expression of c-myc and c-fos gene may be changed during transformation of L1210 to drug-resistant sublines.

• Journal of Microbiology and Biotechnology
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• v.28 no.1
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• pp.59-64
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• 2018

Listeria monocytogenes can asymptomatically inhabit the human intestine as a commensal bacterium. However, the mechanism by which L. monocytogenes is able to inhabit the intestine without pathogenic symptoms remains unclear. We compared the invasion efficiency of L. monocytogenes strains with the 268- and 385-bp-long actA gene. Clinical strains SMFM-CI-3 and SMFM-CI-6 with 268-bp actA isolated from patients with listeriosis, and strains SMFM-SI-1 and SMFM-SI-2 with the 385-bp gene isolated from carcasses, were used for inoculum preparation. The invasion efficiency of these strains was evaluated using Caco-2 cells (intestinal epithelial cell line), prepared as normal and healthy cells with tightened tight junctions and senescent cells with loose tight junctions that were loosened by adriamycin treatment. The invasion efficiency of L. monocytogenes strains with the 268-bp-long actA gene was 1.1-2.6-times lower than that of the strains with the 385-bp-long gene in normal and healthy cells. However, the invasion efficiency of both types of strains did not differ in senescent cells. Thus, L. monocytogenes strains with the 268-bp-long actA gene can inhabit the intestine asymptomatically as a commensal bacterium, but they may invade the intestinal epithelial cells and cause listeriosis in senescent cells.

• Tuberculosis and Respiratory Diseases
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• v.59 no.2
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• pp.193-197
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• 2005

The 64-year-old female patient with cough and intermittent hemoptysis of six months duration visited our hospital. On chest computed tomography, a small, ovoid, 1.3cm sized and well enhanced lesion was detected on the distal trachea. Two multiple lobulated lesions on the sigmoid and transverse colon were revealed on the colonoscopy. The histological findings showed small and medium sized lymphocytes infiltration, CD20 and CD79a positive staining and multiple lymphoepithelial lesions on the distal trachea and colon tissues. Herein, a case of primary MALT lymphoma, with involvement of the trachea and colon, which was treated with rituximab (CD20 anti-monoclonal antibody), cyclophosphamide, adriamycin, vincristine and prednisolone (CHOP regimen), is reported.

• Archives of Craniofacial Surgery
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• v.11 no.2
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• pp.99-102
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• 2010

Purpose: Primary malignant lymphomas of the salivary glands are uncommon, representing only 1.7% to 3.1% of all salivary neoplasms and 0.6% to 5% of all tumors and tumor-like lesions of the parotid gland. Lymphomas of the parotid glands are usually manifestations of a systemic disease process but primary lymphomas of the parotid glands are rare. Most of these lesions are classified as extranodal non-Hodgkin's lymphoma. We report the clinicopathological features of primary malignant lymphoma of the parotid gland based on an analysis of our cases. Methods: The subject was a 48-year-old male patient with a malignant lymphoma originating in the parotid gland, which had been slowly increasing in size over previous 6 months. The diagnosis was established by MRI and a superficial lobectomy. After diagnosis, the patient was referred to an oncologist for staging and medical treatment. Results: The stage was IIIA. The patient was treated with chemotherapy following surgery with rituximab and CHOP (Cyclophosphamide, Adriamycin, Vincristine, Prednisolone). The tumor was controlled successfully by chemotherapy. The patient was followed up for 1 year with no relapse. Conclusion: A case of primary non-Hodgkin's lymphoma of the parotid gland was treated with a superficial parotidectomy and chemotherapy. The disease was well controlled after a 1 year follow-up.

• The Journal of the Korean bone and joint tumor society
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• v.2 no.1
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• pp.27-32
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• 1996

Recent advances in imaging techniques, surgery and combination anti-cancer chemotherapy have brought high survival rates in osteosarcoma. To investigate the survival rate, local recurrence and complications in treatment, we analysed 25 osteosarcoma cases who had been treated with preoperative neo-adjuvant chemotherapy, surgery and post operative chemotherapy at Department of Orthopedic Surgery, Catholic University. From May 1988 to April 1995, 42 cases of stage IIB osteosarcoma were admitted in Department of Orthopedic Surgery. Among them, 17 cases who didn't follow our treatment guidance were excluded in this study. The average age were 19 years. There were 21 males and 4 females. The involved sites were 4 humerus, 10 femur, 10 tibia and 1 talus. Eleven cases had received intraarterial cisplatin and intravenous adriamycin chemotherapy, and 7 T-10 protocol and 7 intravenous ifosfamide, ADR, methotrexate, cisplatin. Twenty-three cases were treated with limb salvage surgery, and 2 amputation. The average follow-up was 35 months(3~82). There were 14 cases of continuous disease free, 9 cases of died of disease, 1 case of alive with disease, and 1 case of no evidence of disease at final follow-up. There were three cases of local recurrence at 6,8 and 12 months after operation. The estimated Kaplan-Meier's 5 year survival rates for all, ADR-cisplatin group, T-10 protocol group, and ifosfamide regimen group were 6%, 73%, 44% and 72%, respectively.

• Korean Journal of Pharmacognosy
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• v.31 no.1
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• pp.72-76
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• 2000

This study was carried out to evaluate cytotoxic effects of Ajuga multiflora Bunge extracts on murine leukemia tumor $(P388D_1)$ cell lines. Disruptions in cell organelles were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide (MTT) assay. The comparison of $IC_{50}$ values of Ajuga multiflora Bunge extracts in L1210 and $P388D_1$ cell lines showed that their susceptibility to these extracts decreased in the following order: Adriamycin>methanol extract>chloroform extract>ethyl acetate extract>hexane extract>water extract by the MTT assay. In order to develop an antimicrobial agent, dried Ajuga multiflora Bunge was extracted with several solvents, and then antimicrobial activity was investigated. The minimal inhibitory concentration (MIC) of the extract against microorganisms were also examined. Antimicrobial activities of amocla and ketoconazole as references were compared to those of extracts of $H_2O$, n-hexane, chloroform, ethyl acetate and methanol. The antimicrobial activity of all extracts from the sample had growth inhibition activity against gram-negative bacteria, gram-positive bacteria and fungi $(MIC>200\;{\mu}g/ml)$. These results suggest that the methanol soluble extract of Ajuga multiflora Bunge may be a valuable choice for the studies on the treatment of murine leukemia tumor cell lines.