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Young-Jin Chun Young-Kun Oh Beom Joon Kim Donghak Kim Sung Su Kim Hyung-Kyoon Choi Mie-Young Kim 《Toxicology letters》2009
Human cytochrome P450 1B1 (CYP1B1) is found mainly in extrahepatic tissues and is overexpressed in a variety of human tumors. Metabolic activation of 17β-estradiol (E2) to 4-hydroxy E2 by CYP1B1 has been postulated to be an important factor in mammary carcinogenesis. The inhibition of recombinant human CYP1B1 by 2,2′,4,6′-tetramethoxystilbene (TMS) was investigated using either the Escherichia coli membranes of recombinant human CYP1B1 coexpressed with human NADPH-P450 reductase or using purified enzyme. 2,2′,4,6′-TMS showed potent and selective inhibition of ethoxyresorufin O-deethylation (EROD) activity of CYP1B1 with IC50 values of 2 nM. 2,2′,4,6′-TMS exhibited 175-fold selectivity for CYP1B1 over CYP1A1 (IC50, 350 nM) and 85-fold selectivity for CYP1B1 over CYP1A2 (IC50, 170 nM). However, inhibition of human NADPH-P450 reductase activity by 2,2′,4,6′-TMS was negligible. The modes of inhibition by 2,2′,4,6′-TMS were noncompetitive for CYP1A1 and CYP1B1. Moreover, 2,2′,4,6′-TMS significantly suppressed EROD activity and 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD)-induced CYP1A1 or CYP1B1 gene expression in human tumor cells such as HepG2 and MCF-10A. Taken together, our results indicate that 2,2′,4,6′-TMS is a potently selective inhibitor of human CYP1B1 as well as a suppressor of CYP1B1 expression and may be a valuable tool for determining enzyme properties of human CYP1B1. 相似文献
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Xu-Feng Qi Dong-Heui Kim Yang-Suk Yoon Jian-Hong Li Dan Jin Young-Kun Deung Kyu-Jae Lee 《Journal of ethnopharmacology》2009
Ethnopharmacological relevance
Bambusae caulis in Liquamen (BCL) is a nutritious liquid extracted from heat-treated fresh bamboo stems. It is an important traditional herbal medicine used to treat coughs and asthma in East Asia. In recent years, it has been studied for its anti-inflammatory, anti-allergenic, and immune-regulating properties.Aim of the study
To examine whether BCL suppresses the development of 2,4-dinitrochlorobenzene (DNCB)-induced atopic dermatitis (AD)-like skin lesions in hairless mice.Materials and methods
The effects of BCL were analyzed by measuring transepidermal water loss (TEWL), melanin content, and erythema in the skin, leukocyte numbers and IgE levels in the serum, and mRNA expression of relevant cytokines in the spleen.Results
The transdermal administration of BCL to hairless mice inhibited the development of DNCB-induced AD-like skin lesions by suppressing TEWL, melanin production and erythema of skin, the number of leukocytes and the level of IgE in serum, and the mRNA expression of IL-4, IL-13, and TNF-α in the spleen. However, BCL administration increased the expression of IFN-γ in the spleen.Conclusions
These findings indicate that BCL suppresses the development of DNCB-induced AD-like skin lesions in hairless mice, suggesting that BCL may be a potential therapeutic agent for AD in a clinical setting. 相似文献4.
Since the Gordius worm is a parasite of crickets and several arthropods, cases of humans infected with this worm have been rare and accidental. A Gordius worm was obtained from a three-year-old girl who consulted a local clinic in Gwangju, Kyunggi-do, Korea. She lived in a rural area, and had eaten an insect that looked like a cricket. She expelled the worm in vomitus 15 minutes later; in fact, she expelled two worms, but one was discarded. The worm had a grayish white color and an intact outer surface. It was 16 cm in length and 0.6 cm wide. The posterior end of the worm was spirally enrolled and furcated into two caudal lobes, which were nearly cylindrical but showed a somewhat concave medio- ventral surface. The cloacal aperture was round and situated anterior to the point of bifurcation of the lobes. The cloacal aperture was encircled by a dark ring, which was a little removed from the aperture. The crescent fold was reddish brown, and no hairs were noticed over the entire body surface. The worm had the morphological features of a male Gordius. Accidental human cases involving the Gordius worm are rare and this is the first such case in Korea. 相似文献
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Prognostic value of vascular endothelial growth factor in Stage IB carcinoma of the uterine cervix 总被引:13,自引:0,他引:13
Lee IJ Park KR Lee KK Song JS Lee KG Lee JY Cha DS Choi HI Kim DH Deung YK 《International journal of radiation oncology, biology, physics》2002,54(3):768-779
PURPOSE: To clarify the role of vascular endothelial growth factor (VEGF) expression as an independent prognostic factor in Stage IB cervical cancer. METHODS AND MATERIALS: A total of 117 patients with Stage IB cervical cancer who had undergone radical hysterectomy and pelvic lymph node dissection with complete histopathologic examination were included. Eighty-eight (75.2%) patients received postoperative radiotherapy and/or chemotherapy. VEGF expression was examined using immunohistochemistry. RESULTS: Of 117 patients, 35 (29.9%) showed high-intensity VEGF expression and 69 (59%) had a high score for area of VEGF expression. Strong correlations were found between high VEGF intensity and both deep stromal invasion (p = 0.01) and positive pelvic lymph nodes (p = 0.03). The area of VEGF expression was significantly associated with tumor size (p = 0.02). In a multivariate analysis, high VEGF intensity (p = 0.009) and tumor size (p = 0.01) were significant prognostic factors for overall survival and disease-free survival (p = 0.001 and p = 0.003, respectively). However, the area of VEGF expression was not a prognostic factor for overall survival or disease-free survival. CONCLUSION: Our findings on the correlation between VEGF expression and prognosis were conflicting. Functional and quantitative tools to assess tumor angiogenesis in addition to the expression of VEGF need to be developed and would be helpful to support the finding that tumor angiogenesis correlates significantly with prognosis in early-stage cervical cancer. 相似文献
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