• Title/Summary/Keyword: Solid Cancer

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Synthesis and Evaluation of Antitumor Activity of 2- and 6-[(1,3- Benzothiazol-2-yl)aminomethyl]-5,8-dimethoxy-1,4-naphthoquinone Derivatives

  • Chung, Yong-Seog;Shin, Young-Kook;Zhan, Chang-Guo;Lee, Sung-Duck;Cho, Hoon
    • Archives of Pharmacal Research
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    • v.27 no.9
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    • pp.893-900
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    • 2004
  • 2- or 6-Substituted BZT-N derivatives were synthesized, and their cytotoxic activity against can-cer L1210 and SNU-1 cells was examined. The antitumor action was also assessed in mice bearing S-180 cells in peritoneal cavity. In a comparison, it was found that 6-substituted BZT-N derivatives exhibited higher potencies in both bioactivities than 2-substituted BZT-N derivatives against L1210 cells in in vitro and S-180 in vitro tests exception of compound 36. Interestingly, it was observed that 2-substituted compound 36, which has methyl group at RI position, exhib-ited a better antitumor activity than 6-substituted compounds against L1210 and SNU-1 in vitro. The EDso value of 2-substituted compound 36 against L1210 was found to be comparable to the EDso value of adriamycin and was even better against the solid cancer cell line SNU-1. It was also observed that 2-substituted compound 36 showed better antitumor activity in mice bearing S-180 cells in the peritoneal cavity. The T/C (%) value of 2-substituted compound 36 was simi-lar to that of adriamycin. Quantitative structure-activity relationship (QSAR) tests reveal that the experimental E $D_{50}$ values against SNU-1 closely correlate with both the calculated HOMO ener-gies ( $E_{HOMO}$) and the measured H-NMR chemical shift of 3-H ($\delta$$_{H}$). The results suggests that a compound having higher $E_{HOMO}$ and $\delta$$_{H}$ values usually should have a lower E $D_{50}$ (SNU-1) value.lue.lue.lue.

Assessment of free-radical-scavenging and antibacterial activities, and brine shrimp toxicity of Scutellaria pinnatifida (Lamiaceae)

  • Sauvage, Severine;Samson, Emilie;Granger, Melanie;Majumdar, Anisha;Nigam, Poonam;Nahar, Lutfun;Celik, Sezgin;Sarker, Satyajit D.
    • Advances in Traditional Medicine
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    • v.10 no.4
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    • pp.304-309
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    • 2010
  • Scutellaria pinnatifida A. Hamilt. (Lamiaceae) is an endemic Turkish herb. This plant is also endemic to Iran, and grows abundantly in other central and western Asian countries. Several species of the Scutellaria are known for their traditional uses in the treatment of hypertension, arteriosclerosis, inflammatory diseases, hepatitis, allergy, cancer and diarrhoea. Free-radical-scavenging property, antibacterial activity and brine shrimp toxicity of the n-hexane, dichloromethane (DCM) and methanol (MeOH) extracts of S. pinnatifida were assessed using the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) assay, the resazurin microtitre plate based assay, and the brine shrimp lethality assay, respectively. The DCM and MeOH extracts exhibited free-radical-scavenging property, with the $RC_{50}$ values of 0.362 and 0.127 mg/ml, respectively. Among the solid-phase extraction fractions of the MeOH extract, the 50% aqueous-MeOH fraction showed the highest level of free-radicalscavenging activity ($RC_{50}$ = 0.039 mg/ml). While the DCM extract showed low level of antibacterial activity against Bacillus subtilis and ampicillin-resistant Escherichia coli, the MeOH extract was active against B. cereus, B. subtilis, E. coli and ampicillin-resistant E. coli. However, the minimum inhibitory concentrations (MIC) of the MeOH extract against these bacterial strains were >10 mg/ml. None of the extracts showed any significant toxicity towards brine shrimps ($LD_{50}$ = > 1.00 mg/ml).

Urinary Concentrations of Benzophenones in University Students and Association with Cosmetics Habits (대학생들의 화장습관에 따른 소변 중 벤조페논 농도 비교)

  • Oh, Seungeun;Ho, Sungwook;Kim, Hyunsuk;Lee, Sehoon;Park, Nayeon;Kho, Younglim
    • Journal of Environmental Health Sciences
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    • v.39 no.6
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    • pp.505-512
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    • 2013
  • Objectives: Ultraviolet (UV) radiation may cause skin cancer, photo-ageing, erythema, and sunburn. Benzophenone (BP) is commonly used to protect skin from UV radiation. In Korea, sunscreen, sunblock, socalled 'blemish balm' (BB) and 'color correcting' (CC) creams, and foundation may contain from 0.5 to 5% benzophenone in order to protect skin from UV radiation. The purpose of this study is to understand the levels of benzophenone derivatives in urine among a group of university students and identify the contribution of cosmetics use. Methods: Forty volunteers (20 women and 20 men) were asked about skin type, frequency of use of cosmetics, and recognition of related health effects, etc. in a survey. Subjects were divided into several subgroups and were compared for concentration of benzophenone-1 (BP-1) and benzophenone-3 (BP-3). Their urine was pretreated with enzyme hydrolysis and solid phase extraction. Determinations of BP-1 and BP-3 in the urine were made with LC-MS/MS. Results: Among the study subjects, 82.5% used basic cosmetics at least once per day, and 77.5% used sunscreens at least once per day. The concentrations of BP-1 and BP-3 of the males were 4.36 ng/mL and 9.16 ng/mL, respectively. Those of the females were 3.98 ng/mL and 5.07 ng/mL, respectively. The use of cosmetics was positively related to urinary benzophenone levels. Conclusions: BP-1 and BP-3 were widely detected among the university students. Cosmetic use was identified as a potential source. Implications of such exposure deserve further investigation.

A Case of Delayed Severe Hypersensitivity Reaction during $Genexol-PM^{(R)}$ Infusion (Genexol-$PM^{(R)}$ 항암치료 중 발생한 지연성 중증 과민성반응 1예)

  • Kim, Hyun-Kyung;Kim, Su-Woo;Kang, Hye-Won;Kwon, Kyoung-Joo;Park, Hye-Sung;Ryu, Yon-Ju;Lee, Jin-Hwa;Chun, Eun-Mi;Cho, Young-Joo;Chang, Jung-Hyun
    • Tuberculosis and Respiratory Diseases
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    • v.68 no.5
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    • pp.294-297
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    • 2010
  • Although $Taxo^{(R)}$ is one of the most successful drugs in current cancer chemotherapy against solid tumors, a major problem is hypersensitivity reactions that arises as a consequence of activation of the complement (C) system, "C activation-related pseudo-allergy". Most severe hypersenstivity reactions occur within the first few minutes of $Taxo^{(R)}$ administration, usually after the first or second dose. Here we report a case of a severe hypersensitivity reaction in a 72-year-old man undergoing $Genexol-PM^{(R)}$ infusion. Hypotension and polymorphic pruritic skin rash appeared 2 hours after the start of $Genexol-PM^{(R)}$ infusion (with an appropriate premedication). Treating with methylprednisolone, epinephrine and inotropic agents, reduced the hypotension and the skin rash disappeared. We report this case with a review of the literature.

Development of Dose Verification Method for In vivo Dosimetry in External Radiotherapy (방사선치료에서 투과선량을 이용한 체내선량 검증프로그램 개발)

  • Hwang, Ui-Jung;Baek, Tae Seong;Yoon, Myonggeun
    • Progress in Medical Physics
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    • v.25 no.1
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    • pp.23-30
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    • 2014
  • The purpose of this study is to evaluate the developed dose verification program for in vivo dosimetry based on transit dose in radiotherapy. Five intensity modulated radiotherapy (IMRT) plans of lung cancer patients were used in the irradiation of a homogeneous solid water phantom and anthropomorphic phantom. Transit dose distribution was measured using electronic portal imaging device (EPID) and used for the calculation of in vivo dose in patient. The average passing rate compared with treatment planning system based on a gamma index with a 3% dose and a 3 mm distance-to-dose agreement tolerance limit was 95% for the in vivo dose with the homogeneous phantom, but was reduced to 81.8% for the in vivo dose with the anthropomorphic phantom. This feasibility study suggested that transit dose-based in vivo dosimetry can provide information about the actual dose delivery to patients in the treatment room.

Xanthogranulomatous Pancreatitis Mimicking a Pancreatic Cancer on CT and MRI: a Case Report and Literature Review

  • Park, Jong Min;Cho, Seung Hyun;Bae, Han-Ik;Seo, An Na;Kim, Hye Jung;Lee, So Mi;Yi, Jae Hyuck;Lim, Jae-Kwang;Cho, Chang Min
    • Investigative Magnetic Resonance Imaging
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    • v.20 no.3
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    • pp.185-190
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    • 2016
  • Xanthogranulomatous inflammation is a rare benign condition involving various organs. However, its pancreas involvement is very rare. To the best of our knowledge, only 17 cases have been described in the literature. Interestingly, all reported 17 cases due to various causes underwent surgical resection. Here, we present a case of xanthogranulomatous pancreatitis in a 63-year-old man. He presented with epigastric pain and solid mass mimicking ductal adenocarcinoma in the body and tail of pancreas on magnetic resonance imaging. The patient was diagnosed as xanthogranulomatous pancreatitis via endoscopic ultrasound-guided fine needle aspiration. After that, he was followed up and monitored without any surgical treatment. Here, we show imaging findings and serial image changes of xanthogranulomatous pancreatitis for this case.

Antitumor and Immunomodulatory Effects of Dangguihwalhyultang on Murine Melanoma-induced Lung Metastasis (당귀활혈탕(當歸活血湯)의 폐전이억제(肺轉移抑制) 및 면역조절작용(免疫調節作用)에 의한 항암효과(抗癌效果))

  • Ko, Eun-Tae;Ha, Jee-Yong;Lee, Seon-Goo;You, Byeong-Gil
    • THE JOURNAL OF KOREAN ORIENTAL ONCOLOGY
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    • v.6 no.1
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    • pp.29-45
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    • 2000
  • In order to investigate the antitumor effect by Dangguihwalhyultang after B-l6 cells were transplanted in C57BL/6 mice, and the immune responses in mice induced by methotrexate, the extract of Dangguihwalhyultang was orally administered to the ICR mice. Experimental studies were performed for measurance of metastasis, cell cytotoxicity in vitro, life extention, weight of cancer, natural killer cell activity. productivity of interleukin-2. The results were summarized as follows: 1. Mean survival time in Dangguihwalhyultang-treated group was prolonged, as compared with control group(14.63%) significantly(P<0.05). 2. Inhibition of metastasis in Dangguihwalhyultang-treated group was higher than control group with significance on 14th day(P<0.05). 3. On the weight of solid tumor. Dangguihwalhyultang-treated group was less than control group with significance(P<0.05). 4. On the MTT assay. Dangguihwalhyultang concentration inhibited cell viability was $368.8{\mu}g/well$. 5. Natural killer cell activity in Dangguihwalhyultang-treated group was significantly increased on 100:1, 50:1 E/T(effect cell/target cell) ratio(P<0.05). 6. Production of interleukin-2 in Dangguihwalhyultang-treated group was significantly increased(P<0.05).

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Exposure to Bisphenol A through Contact with Thermal Receipts among Service Industry Workers (서비스직 근로자들의 영수증 접촉 정도에 따른 비스페놀A 노출량 조사)

  • Lee, Yuna;Lee, Yujin;Jang, Jiwon;Han, Gaeul;Kho, Younglim
    • Journal of Environmental Health Sciences
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    • v.40 no.6
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    • pp.435-441
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    • 2014
  • Objectives: Bisphenol A, or BPA, is a chemical component in polycarbonate plastic with which many people come into contact every day. A great deal of controversy has arisen over its safety since this material, which is known to disrupt the human endocrine system and cause neurological difficulties and cancer, is commonplace in beverage containers, food can liners, and receipt paper rolls. In this study, we determined the levels of exposure to BPA of workers in the service industry depending on the number of receipts contacted. Methods: The participants were 16 male and 18 female workers employed in the service industry. Using a questionnaire, we investigated general and job characteristics. Urine samples were collected and analyzed by the LC-MS/MS technique after enzymatic hydrolysis and solid phase extraction (SPE). Results: The geometric mean (GM) concentration of urinary BPA from all subjects was 1.02 ng/ml. Workers were exposed significantly to more BPA according to the number of receipts they contacted, their work experience, and working hours per day. The BPA concentration of those who touched more than 100 receipts per day was 3.09 ng/ml, while that of the other participants was 0.61 ng/ml. It was shown that wearing gloves can protect from BPA exposure. Conclusion: We determined the urinary BPA concentrations of workers in service industry and found that the contact with receipts could increase the BPA exposure of service workers.

Oral bisphosphonates induced osteonecrosis of the mandible : A case report

  • Son, Hyo-Jeong;Jang, Ho-Yeol;Keum, Yun-Seon;Lee, Jang-Yeol;Kim, Hyoun-Chull;Lee, Sang-Chull
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • v.35 no.2
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    • pp.106-111
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    • 2009
  • Bisphosphonates have been approved for Paget's disease, cancer-related hypercalcemia, bone involvement in multiple myeloma or solid tumors and osteoporosis. Although, underlying pathophysiological mechanisms remain unclear, it seems that bisphosphonates inhibit osteoclast precursor cells, modulate migratory and adhesive characteristics and induce apoptosis of osteoclasts. Furthermore impacts on angiogenesis, microenvironment and signal transduction between osteoclasts and osteoblasts. In this report, we present a case of oral bisphosphonates induced osteonecrosis of the mandible in a 84-year-old patient who received for two years. Two tapered screw vent implants(Zimmer, USA) were placed in the area of first and second molar. Two weeks later after crowns restored, some inflammatory signs and symptoms were observed on the second molar area. Sequestrum was formed and the sequestrum was removed with the implant. Frequent follow-up checks and oral hygiene maintenances were done and the first molar implant was restored. There is insufficient evidence suggests that duration of oral bisphosphonate therapy correlates with the development and severity of osteonecrosis. Therefore, dentists should not overlook the possibility of development of bisphosphonate induced osteonecrosis in patients who have taken oral forms of medication for less than three years.

Mechanism of gemcitabine-induced apoptosis (Gemcitabine의 세포사멸 기전 연구)

  • Seol, Jae-Won;Lee, You-Jin;Kang, Dong-Won;Kang, Hyung-Sub;Kim, Nam-Soo;Kim, In-Shik;Park, Sang-Youel
    • Korean Journal of Veterinary Research
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    • v.45 no.4
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    • pp.495-500
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    • 2005
  • The nucleoside analogue gemcitabine (2', 2-difluorideoxycytide) is potential against a wide variety of solid tumors and considered to be one of the most active drugs in the treatment of non-small cell lung cancer (NSCLC). In this study, we investigated the signals of gemcitabine-induced apoptosis, especially in point of caspase pathway in A549. We exposed A549 cells to gemcitabine for dose/time dependent manner and the results showed that gemcitabine induced apoptotic cell death in a time/dose-dependent manner. We also treated to gemcitabine and Z-VAD-fmk as a pan-caspase inhibitor for 24 hours. Gemcitabine alone induced 35.3% cell death, and co-treatment with gemcitabine and Z-VAD-fmk induced 15.1% apoptotic cell death. Our results demonstrated that Z-VAD-fmk as a pan-caspase did not completely block the gemcitabine-induced apoptosis. Western blotting analysis showed that gemcitabine increased caspase-3, active caspase-8, p21 and p53 protein expressions in A549. Co-treatment with Z-VAD-fmk completely blocked caspase-3 and active caspase-8 protein expressions, but did not change the level of p21 and p53 protein expressions. Our data indicate that gemcitabine induced apoptosis through caspase-dependent and -independent pathways in A549.