کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10584924 | 981355 | 2012 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants
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کلمات کلیدی
PDAdeferoxamine mesylateDCFH-DAMPAdihydroartemisininCDDP2′,7′-dichlorofluorescin diacetate - 2 '، 7'-dichlorofluorescin diacetateMAPK - MAPKROS - ROSphoto diode array - آرایه دیود عکسArtemisinin - آرتمیسینینApoptosis - خزان یاختهایDHA - دوکوساهگزائنوئیک اسیدdihydroethidium - دی هیدروتیدیمCarbon-centered radical - رادیکال محور کربنHL60 cells - سلول های HL60mycophenolic acid - مایکوفنولیک اسید، مایکوفنولاتART - هنرmitogen-activated protein kinase - پروتئین کیناز فعال با mitogenReactive oxygen species - گونههای فعال اکسیژن
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A bisabolane sesquiterpene endoperoxide compound, 3,6-epidioxy-1,10-bisaboladiene (EDBD), was isolated from edible wild plants grown in the northern area of Japan, Cacalia delphiniifolia and Cacalia hastata, using a mutant yeast (cdc2-1 rad9Î). It showed cytotoxicity at IC50 = 3.4 μM and induced apoptosis against the human promyelocytic leukemia cell line HL60 through a new stable rearrangement product (1) when in the presence of FeSO4. This conversion mechanism is different from another sesquiterpene endoperoxide lactone compound, dihydroartemisinin (DHA), which is an anti-malarial drug. The cytotoxicity of EDBD decreased in the presence of the ferrous ion chelating drug deferoxamine mesylate (DFOM), and this suggested that the structural change of the drug caused by Fe2+ may be responsible for its biological activities. EDBD induced apoptosis via phosphorylation of p38 mitogen-activated protein kinase (MAPK) in HL60 cells, and was detected by Western blot. EDBD resulted in an immediate increase in DCF fluorescence intensity in HL60 cells using DCFH-DA (2â²,7â²-dichlorofluorescin diacetate) assay. The in vitro reaction of EDBD with FeSO4 also increased DCF fluorescence intensity in a dose dependent manner. These results showed that the biological activity of EDBD involves an unstable carbon-centered radical intermediate. Furthermore, there was no similarity between the JFCR39 fingerprints of EDBD and DHA (correlation coefficient on COMPARE Analysis γ = 0.158). EDBD showed anti-tumor effects against a xenograft of Lox-IMVI cells in vivo.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 12, 15 June 2012, Pages 3887-3897
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 12, 15 June 2012, Pages 3887-3897
نویسندگان
Ken-ichi Kimura, Yoshimi Sakamoto, Nozomi Fujisawa, Shota Uesugi, Nobuhiro Aburai, Manabu Kawada, Shun-ichi Ohba, Takao Yamori, Eiko Tsuchiya, Hiroyuki Koshino,