645-96-5Relevant articles and documents
Exploiting structure-activity relationships of QS-21 in the design and synthesis of streamlined saponin vaccine adjuvants
Anguita, Juan,Barriales, Diego,Corzana, Francisco,Fernández-Tejada, Alberto,Ghirardello, Mattia,Jiménez-Barbero, Jesús,Poveda, Ana,Ruiz-De-Angulo, Ane,Sacristan, Nagore
, p. 719 - 722 (2020)
We report the design, synthesis, immunological evaluation, and conformational analysis of new saponin variants as promising vaccine adjuvants. These studies have provided expedient synthetic access to streamlined adjuvant-active saponins and yielded molecular-level insights into saponin conformation that correlated with their in vivo adjuvant activities.
Synthesis of Seleno Oxindoles via Electrochemical Cyclization of N-arylacrylamides with Diorganyl Diselenides
Wang, Xin-Yu,Zhong, Yuan-Fang,Mo, Zu-Yu,Wu, Shi-Hong,Xu, Yan-Li,Tang, Hai-Tao,Pan, Ying-Ming
supporting information, p. 208 - 214 (2020/12/04)
The tandem cyclization of acrylamide with diselenides facilitated by electrochemical oxidation was successfully developed. This strategy provided an environmentally friendly method for the construction of C?Se bond. A series of seleno oxindoles with pharmacological activity were obtained by using this well-designed tandem cyclization strategy. The in vitro antitumor activity of the compounds was also screened through MTT assay. Results showed that the seleno oxindoles exhibited better antitumor activity than other oxindole derivatives. (Figure presented.).
Lysosomal Reacidification Ameliorates Vinyl Carbamate-Induced Toxicity and Disruption on Lysosomal pH
Chen, Wei,Cui, Sunliang,Hu, Dongwen,Li, Yuting,Qi, Jifeng
, p. 8951 - 8961 (2020/09/16)
Ethyl carbamate (EC) is a carcinogen toxicant, commonly found in fermented foods and beverages. The carcinogenic and toxic possibility of EC is thought to be related to its metabolite vinyl carbamate (VC). However, we found interesting mechanisms underlying VC-induced toxicity in this study, which were greatly different from EC. We first conducted a simple synthesis procedure for VC and found that VC possessed higher toxicity but failed to regulate levels of reactive oxygen species, glutathione, and autophagy. Notably, VC treatment resulted in upregulation of lysosomal pH, which was responsible for its cytotoxicity. Cyclic adenosine monophosphate (cAMP) pretreatment could enhance restoration of lysosomal acidity and ameliorate VC-induced damage. Inhibition of protein kinase A and cystic fibrosis transmembrane conductance regulator can block cAMP-induced cytoprotection. Together, our results provided the evidence for novel mechanisms of toxicity and possible protection method under VC exposure, which might give new perspectives on the study of EC-induced toxicity.
Visible-Light-Promoted Selenylative Spirocyclization of Indolyl-ynones toward the Formation of 3-Selenospiroindolenine Anticancer Agents
Zhou, Xiu-Jie,Liu, Hao-Yang,Mo, Zu-Yu,Ma, Xian-Li,Chen, Yan-Yan,Tang, Hai-Tao,Pan, Ying-Ming,Xu, Yan-Li
supporting information, p. 1536 - 1539 (2020/04/20)
A metal-free and efficient visible-light-induced spirocyclization of indolyl-ynones with diselenides at room temperature under air atmosphere to prepare 3-selenospiroindolenines in moderate to good yields has been developed. The resulting products were tested for in vitro anticancer activity by MTT assay, and compounds 3 c and 3 e showed potent cancer cell-growth inhibition activities.
