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BCI induces apoptosis via generation of reactive oxygen species and activation of intrinsic mitochondrial pathway in H1299 lung cancer cells

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Science China(Life Sciences) 2018年第10期61卷 1243-1253页

作者： Jong-Woon Shin Sae-Bom Kwon Yesol Bak Sang-Ku Lee Do-Young Yoon Department of Bioscience and Biotechnology Konkuk University Targeted Medicine Research Center Korea Research Institute of Bioscience and Biotechnology (KRIBB)

The compound(E)-2-benzylidene-3-(cyclohexylamino)-2,3-dihydro-1 H-inden-1-one(BCI) is known as an inhibitor of dual specific phosphatase 1/6 and mitogen-activated protein kinase. However, its precise anti-lung cancer mechanism remains unknown. In this study, the effects of BCI on the viability of non-small cell lung cancer cell lines NCI-H1299, A549, and NCI-H460 were evaluated. We confirmed that BCI significantly inhibited the viability of p53(-) NCI-H1299 cells as compared to NCI-H460 and A549 cells, which express wild-type p53. Furthermore, BCI treatment increased the level of cellular reactive oxygen species and pre-treatment of cells with N-acetylcysteine markedly attenuated BCI-mediated apoptosis of NCI-H1299 cells. BCI induced cellular morphological changes, inhibited viability, and produced reactive oxygen species in NCI-H1299 cells in a dose-dependent manner. BCI induced processing of caspase-9, caspase-3, and poly ADP-ribose polymerase as well as the release of cytochrome c from the mitochondria into the cytosol. In addition, BCI downregulated Bcl-2 expression and enhanced Bax expression in a dose-dependent manner in NCI-H1299 cells. However, BCI failed to modulate the expression of the death receptor and extrinsic factor caspase-8 and Bid, a linker between the intrinsic and extrinsic apoptotic pathways in NCI-H1299 cells. Thus, BCI induces apoptosis via generation of reactive oxygen species and activation of the intrinsic pathway in NCI-H1299 cells.

关键词： non-small cell lung cancer apoptosis BCI cytotoxicity anticancer ROS

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Roles of hepatocyte nuclear factors in hepatitis B virus infection

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World Journal of Gastroenterology 2016年第31期22卷 7017-7029页

作者： Doo Hyun Kim Hong Seok Kang Kyun-Hwan Kim Department of Pharmacology and Center for Cancer Research and Diagnostic Medicine IBST School of Medicine Konkuk University KU Open Innovation Center Konkuk University Research Institute of Medical Science Konkuk University

Approximately 350 million people are estimated to be persistently infected with hepatitis B virus(HBV) worldwide. HBV maintains persistent infection by employing covalently closed circular DNA(ccc DNA), a template for all HBV RNAs. Chronic hepatitis B(CHB) patients are currently treated with nucleos(t)ide analogs such as lamivudine, adefovir, entecavir, and tenofovir. However, these treatments rarely cure CHB because they are unable to inhibit ccc DNA transcription and inhibit only a late stage in the HBV life cycle(the reverse transcription step in the nucleocapsid). Therefore, an understanding of the factors regulating ccc DNA transcription is required to stop this process. Among numerous factors, hepatocyte nuclear factors(HNFs) play the most important roles in ccc DNA transcription, especially in the generation of viral genomic RNA, a template for HBV replication. Therefore, proper control of HNF function could lead to the inhibition of HBV replication. In this review, we summarize and discuss the current understanding of the roles of HNFs in the HBV life cycle and the upstream factors that regulate HNFs. This knowledge will enable the identification of new therapeutic targets to cure CHB.

关键词： Hepatitis B virus Hepatocyte nuclear factor Covalently closed circular DNA Replication

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Investigation of anticancer potencies of newly generated Schiff base imidazolylphenylheterocyclic-2-ylmethylenethiazole-2-amines

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Chinese Chemical Letters 2017年第3期28卷 602-606页

作者： Nikhil M. Parekh Bhupendra M. Mistry Muthuraman Pandurangan Surendra K. Shinde Rahul V. Patel Department of Mathematics Science & Humanities Shroff S. R. Rotary Institute of Chemical Technology Valia 393135 India Organic Research Laboratory Department of Bioresources and Food Sdence College of Life and Environmental Sciences Konkuk University Seoul 143 701Republic of Korea College of Life Science and Biotechnology Department of Biological and Environmental Science Dongguk University 32 llsandong-gu Goyang-siGyeonggi-do 410-820 Republic of Korea Department of Food Science and Biotechnology Dongguk University-Seoul llsandong-gu Goyang-si Gyeonggi-do 410-820 Republic of Korea

A new series of multi-heterocyclic Schiff base was constructed starting from 4＇-（imidazol-1-yl[56_TD$IF]）-acetophenone which was converted to its 2-bromoethanone precursor which on cyclic condensation with thiourea yielded final thiazol-2-amine intermediate（3） to be reacted with substituted aldehydes to generate final imidazolylphenylheterocyclic-2-ylmethylenethiazole-2-amines（4a–4i）. New Schiff base was investigated for their in vitro cytotoxic efficacies against a panel of three human cancer cell lines namely, MCF7（human breast cancer）, HCT116（human colon cancer）, and DU145（human prostate cancer） and one normal skin fibroblast（SF）. Most of these synthetic derivatives shown important cytotoxic actions against individual carcinoma cell line collections, but weak actions against SF, which is as anticipated. Observations of SAR suggested that the difference in the characteristics of substituents attached to the Schiff base function leads to the interesting variations within pharmacological effects of resultant molecular systems. Structural analysis performed using FT-IR,~1H NMR,^（13）C NMR spectroscopy and CHN analysis for final potent anticancer Schiff base, which warrant further investigations.

关键词： Schiff Base Imidazole Thiazole Anticancer Drug designing SAR

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Primary Torsion of Lesser Omentum Presented with Acute Abdomen and Successfully Managed with Laparoscopic Surgery

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Chinese Medical Journal 2016年第13期129卷 1625-1626页

作者： Jun-Sik Yu Woo-Surng Lee Yong-Hun Kim Department of General Surgery School of Medicine Konkuk University Chungju Hospital Chungju-si Chungbuk 380-704 Korea Department of Thoracic and Cardiovascular Surgery School of Medicine Konkuk University Chungju Hospital Chungju-si Chungbuk 380-704 Korea

To the Editor： Omental torsion can be classified as primary or secondary according to etiology and may be localized in the greater or lesser omentum. Primary torsion of the omentum is characterized with the absence of associated intra-abdominal pathology; however, secondary torsion of the omentum can be associated with underlying factors.

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Rhabdomyolysis from spinning exercise and ephedra-contained herbal medicine

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Journal of Sport and Health Science 2016年第2期5卷 248-249页

作者： Hoyoung Ryu Hong Sup Kim Heejung Choi Jooyoung Kim Dong Jun Sung Division of Sport Science College of Science and Technology Konkuk University Department of Urology Konkuk University Hospital Department of Nephrology Konkuk University Hospital Health and Rehabilitation Major Kookmin University

Dear editor, Frequent participation in physical activity has a positive impact on individual physical and psychological well-being, and the effect of physical activity and exercise varies according to individual physical fitness level, the environment, and drug intake. Particularly, severe exercise that exceeds the individual physical fitness level may result in musculoskeletal injury or damage,1 and rhabdomyolysis is a pathological condition of the musculoskeletal system that can be complicated by acute renal failure, compartment syndrome, and hepatitis.2 People who fail to receive proper management for rhabdomyolysis may face life-threatening conditions, even death.

关键词：旋转运动横纹肌麻黄草药溶解

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