1162008-48-1Relevant articles and documents
Antioxidant Properties of Novel Dimers Derived from Natural β-Elemene through Inhibiting H2O2-Induced Apoptosis
Chen, Jichao,Wang, Ruifan,Wang, Tianyu,Ding, Qilong,Khalil, Aliahmad,Xu, Shengtao,Lin, Aijun,Yao, Hequan,Xie, Weijia,Zhu, Zheying,Xu, Jinyi
, p. 443 - 448 (2017)
A series of novel β-elemene dimer derivatives were synthesized and evaluated for their antioxidant activities. The results indicated that most of the target compounds showed more potent cytoprotective effects than positive control vitamin E. In particular, dimer D5 exhibited the strongest antioxidant activity, which was significantly superior to the active compound D1 obtained in our previous study. Besides, D5 did not produce obvious cytotoxicity in normal human umbilical vein endothelial cells (HUVECs) and increased the viability of HUVECs injured by H2O2 in a concentration-dependent manner. Further studies suggested that the cytoprotective action of D5 might be mediated, at least in part, by increasing the intracellular superoxide dismutase activity and nitric oxide secretion as well as decreasing the intracellular malonyldialdehyde content and lactate dehydrogenase release. Furthermore, D5 observably inhibited ROS generation and prevented H2O2-induced apoptosis in HUVECs possibly via inhibiting the activation of the MAPK signaling pathway.
The protective effects of a novel synthetic β-elemene derivative on human umbilical vein endothelial cells against oxidative stress-induced injury: Involvement of antioxidation and PI3k/Akt/eNOS/NO signaling pathways
Ahmad, Khalil Ali,Ze, Hong,Chen, Jichao,Khan, Farhan Ullah,Xuezhuo, Chen,Xu, Jinyi,Qilong, Ding
, p. 1734 - 1741 (2018)
Antioxidant therapy is considered as promising strategy for treating oxidative stress-induced cardiovascular disease. Bis (β-elemene-13-yl) glutarate (BEG) is a novel β-elemene derivative. Herein, we examined the antioxidant activity of BEG on human umbil
Rational design, synthesis and biological evaluation of novel derivatives based on in vivo metabolism of natural product β-elemene
Bai, Renren,Jie, Xiaokang,Salgado, Eric,Sun, Jian,Zhu, Yao,Pickel, Thomas,Xie, Yuanyuan,Chen, Jichao,Xu, Jinyi
, p. 905 - 912 (2018/07/03)
Background: Natural products have been an exemplary source of new drugs as they have served as direct or indirect precursors for many currently available medicines. The natural product β -elemene has been used clinically in the treatment of various cancer
Discovery of novel antitumor nitric oxide-donating β-elemene hybrids through inhibiting the PI3K/Akt pathway
Chen, Jichao,Wang, Tianyu,Xu, Shengtao,Zhang, Pengfei,Lin, Aijun,Wu, Liang,Yao, Hequan,Xie, Weijia,Zhu, Zheying,Xu, Jinyi
, p. 414 - 423 (2017/05/04)
A series of novel furoxan-based NO-donating β-elemene hybrids were designed and synthesized to improve the anticancer efficacy of natural β-elemene. The bioassay results indicated that all of the target compounds exhibited significantly improved antiproliferative activities against three cancer cell lines (SGC-7901, HeLa and U87) compared to parent compound β-elemene. Interestingly, these compounds displayed excellent sensitivity to U87?cells with IC50 values ranging from 173 to 2?nM. Moreover, most compounds produced high levels of NO in?vitro, and the antitumor activity of 11a in U87?cells was markedly attenuated by an NO scavenger (hemoglobin or carboxy-PTIO). Further mechanism studies revealed that 11a caused the G2 phase arrest of the cell cycle and induced apoptosis of U87?cells by preventing the activation of the PI3K/Akt pathway. Moreover, 11a significantly suppressed the tumor growth in H22 liver cancer xenograft mouse model with a tumor inhibitory ratio (TIR) of 64.8%, which was superior to that of β-elemene (TIR, 49.6%) at the same dose of 60?mg/kg. Together, the remarkable biological profiles of these novel NO-donating β-elemene derivatives may make them promising candidates for the intervention of human cancers.
Beta-elemene derivative containing dihydropyridine structure, and preparation method and purpose thereof
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Paragraph 0051; 0052, (2017/10/13)
The invention relates to the field of new medicine research and development and tumor therapy, in particular to a novel beta-elemene derivative containing a dihydropyridine structure, particularly a derivative directly or indirectly introducing the brain-targeted dihydropyridine structure through a connecting arm in a beta-elemene 13 bit. The invention also discloses a preparation method of the beta-elemene derivative with the brain-targeted function, and a purpose of the novel derivative for treating gliomas.
Synthesis, characterization, and in vitro antiproliferative activity of novel β-elemene monosubstituted derivatives
Liu, Guifeng,Kong, Zhenwu,Shen, Yumei
, p. 3536 - 3540 (2013/07/11)
A series of β-elemene monosubstituted ester, carbamate, acylamide, and carbamidine derivatives were synthesized via intermediates, β-elemene alcohol and β-elemene amine, which were synthesized from the traditional Chinese medicine, β-elemene. The structur
