کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8950204 | 1645767 | 2018 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Antitumor activity of BJ-1207, a 6-amino-2,4,5-trimethylpyridin-3-ol derivative, in human lung cancer
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کلمات کلیدی
EGFRDUOX1KDRRTKTgf-αc-kitSCF12-O-tetradecanoylphorbol-13-acetateVEGFR2tPADPPHHER2PI3K1,1-diphenyl-2-picrylhydrazyl - 1،1-دیفنیل-2-پریکیل هیدرازیلMAPKs - MAPK هاNOx - NOXROS - ROSAkt - آکتNADPH oxidase - اکسیداز NADPH transforming growth factor-α - تبدیل فاکتور رشد αdual oxidase 1 - دو اکسیداز 1CAM - ساخت به کمک کامپیوترNSCLC - سرطان ریوی غیر سلول کوچکNon-small cell lung cancer - سرطان غیر سلول کوچک ریهChick chorioallantoic membrane - غشای کوریوالانتانیک جوجهVascular endothelial growth factor - فاکتور رشد اندوتلیال عروقیStem Cell Factor - فاکتور سلول بنیادیphosphoinositide 3-kinase - فسفینوزیتید 3-کینازprotein kinase B - پروتئین کیناز Bmitogen-activated protein kinases - کیناز پروتئین فعال Mitogenkinase insert domain receptor - کیناز گیرنده دامنه را وارد کنیدReactive oxygen species - گونههای فعال اکسیژنReceptor Tyrosine Kinase - گیرنده تیروزین کینازHuman epidermal growth factor receptor 2 - گیرنده عامل فاکتور رشد اپیدرمی انسان 2Epidermal growth factor receptor - گیرنده فاکتور رشد اپیدرمال
موضوعات مرتبط
علوم زیستی و بیوفناوری
علوم محیط زیست
بهداشت، سم شناسی و جهش زایی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Antitumor activity of BJ-1207, a 6-amino-2,4,5-trimethylpyridin-3-ol derivative, in human lung cancer Antitumor activity of BJ-1207, a 6-amino-2,4,5-trimethylpyridin-3-ol derivative, in human lung cancer](/preview/png/8950204.png)
چکیده انگلیسی
Enhanced expression of NADPH oxidase (NOX) and the subsequent production of reactive oxygen species (ROS) are associated with lung cancer. In the present study, fifty 6-amino-2,4,5-trimethylpyridin-3-ol derivatives were screened for anticancer activity by targeting NOX2-derived ROS. The compounds suppressed ROS production and decreased cancer cell viability (R2â¯=â¯0.79). Among the derivatives, the compound coded BJ-1207, which contained a 4-(hydroxydiphenylmethyl)piperidine moiety, exhibited the most effective anticancer activity against A549 lung cancer cell line and eight other cancer cell lines, including H1299, MCF-7, MDA-MB-231, HT-29, SW620, Mia PaCa-2, PANC-1, and U937. BJ-1207 also showed significantly lower inhibitory effects on kinase insert domain receptor (KDR) and c-KIT tyrosine kinase but higher inhibitory activity on NOX than those of sunitinib, a multi-receptor tyrosine kinase (RTK) inhibitor. In addition, BJ-1207-induced inhibition of RTK-downstream signaling pathways, such as ROS production, and expression of target genes, such as stem cell factor and transforming growth factor-α, were similar to those induced by sunitinib. In the xenograft chick tumor model, BJ-1207 inhibited lung tumor growth to a similar or much greater extent than that of sunitinib or cisplatin, respectively. Overall, the present study showed that BJ-1207, a vitamin B6-derived 2,4,5-trimethylpyridin-3-ol compound with azacyclonol moiety at C (6)-position of the pyridine ring, inhibited NOX activity and that it is a promising lead compound for developing anticancer drugs against lung cancer.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Chemico-Biological Interactions - Volume 294, 1 October 2018, Pages 1-8
Journal: Chemico-Biological Interactions - Volume 294, 1 October 2018, Pages 1-8
نویسندگان
Jaya Gautam, Suhrid Banskota, Prakash Chaudhary, Sadan Dahal, Dong-Guk Kim, Han-eol Kang, Iyn-Hyang Lee, Tae-gyu Nam, Byeong-Seon Jeong, Jung-Ae Kim,