التفاصيل البيبلوغرافية
العنوان: |
Dual-Targeting Antiproliferation Hybrids Derived from 1‑Deoxynojirimycin and Kaempferol Induce MCF‑7 Cell Apoptosis through the Mitochondria-Mediated Pathway |
المؤلفون: |
Ran Zhang (117374), Yueyue Zhang (410441), Xiangdong Xin (4537408), Gaiqun Huang (8988125), Ning Zhang (23771), Qinglei Zeng (5450645), Liumei Tang (10789916), Thomas Attaribo (10789919), Kwang Sik Lee (10789922), Byung Rae Jin (10789925), Zhongzheng Gui (4537411) |
سنة النشر: |
1753 |
المجموعة: |
Smithsonian Institution: Digital Repository |
مصطلحات موضوعية: |
Biochemistry, Cell Biology, Molecular Biology, Pharmacology, Immunology, Cancer, Biological Sciences not elsewhere classified, Chemical Sciences not elsewhere classified, Bcl -2 expression, 1- deoxynojirimycin derivatives, Mitochondria-Mediated Pathway 1- De., ROS, kaempferol, reactive oxygen species, MCF -7 cells, COX, Dual-Targeting Antiproliferation Hy., compound 10, MCF -7 cell apoptosis, α- glucosidase inhibitor, compound 10 downregulated cyclooxyg., 1- deoxynojirimycin |
الوصف: |
1-Deoxynojirimycin, an α-glucosidase inhibitor, possesses various biological activities such as antitumor, antidiabetic, and antiviral effects. However, the application of 1-deoxynojirimycin is restricted by its poor lipophilicity and low bioavailability. In this study, three 1-deoxynojirimycin derivatives ( 8 – 10 ) comprising 1-deoxynojirimycin and kaempferol were designed and synthesized to modify their pharmacokinetics and improve their antitumor efficacy. Among them, compound 10 , a conjugate of 1-deoxynojirimycin and kaempferol linked through an undecane chain, exhibited excellent lipophilicity, antiproliferative effects, and α-glucosidase inhibitory activity. Compared with 1-deoxynojirimycin, kaempferol, and their combination, compound 10 downregulated cyclooxygenase-2 (COX-2) expression, arrested the cell cycle at the S phase, induced cellular apoptosis, and inhibited the migration of MCF-7 cells. Moreover, further investigation indicated that compound 10 induced MCF-7 cell apoptosis through a mitochondrial-mediated pathway via the loss of mitochondrial membrane potential. This led to increasing intracellular levels of reactive oxygen species (ROS) and Ca 2+ , the downregulation of Bcl-2 expression, and the upregulation of Bax levels. |
نوع الوثيقة: |
article in journal/newspaper |
اللغة: |
unknown |
العلاقة: |
https://figshare.com/articles/journal_contribution/Dual-Targeting_Antiproliferation_Hybrids_Derived_from_1_Deoxynojirimycin_and_Kaempferol_Induce_MCF_7_Cell_Apoptosis_through_the_Mitochondria-Mediated_Pathway/14582468Test |
DOI: |
10.1021/acs.jnatprod.1c00014.s001 |
الإتاحة: |
https://doi.org/10.1021/acs.jnatprod.1c00014.s001Test |
حقوق: |
CC BY-NC 4.0 |
رقم الانضمام: |
edsbas.CD6333C4 |
قاعدة البيانات: |
BASE |