21505-18-0Relevant articles and documents
PEG-derivatized embelin as a dual functional carrier for the delivery of paclitaxel
Huang, Yixian,Lu, Jianqin,Gao, Xiang,Li, Jiang,Zhao, Wenchen,Sun, Ming,Stolz, Donna Beer,Venkataramanan, Raman,Rohan, Lisa Cencia,Li, Song
, p. 1443 - 1451 (2012/10/08)
Embelin, identified primarily from the Embelia ribes plant, has been shown to be a natural small molecule inhibitor of X-linked inhibitor of apoptosis protein (XIAP). It is also a potent inhibitor of NF-κB activation, which makes it a potentially effective suppressor of tumor cell survival, proliferation, invasion, angiogenesis, and inflammation. However, embelin itself is insoluble in water, which makes it unsuitable for in vivo applications. In this work, we developed a novel micelle system through conjugating embelin to a hydrophilic polymer, poly(ethylene glycol) 3500 (PEG3.5K) through an aspartic acid bridge. The PEG3.5k-embelin2 (PEG 3.5k-EB2) conjugate readily forms micelles in aqueous solutions with a CMC of 0.0205 mg/mL. Furthermore, PEG3.5k-EB 2 micelles effectively solubilize paclitaxel (PTX), a model hydrophobic drug used in this study. Both drug-free and drug-loaded micelles were small in size (20-30 nm) with low polydispersity indexes. In vitro cytotoxicity studies with several tumor cell lines showed that PEG 3.5k-EB2 is comparable to embelin in antitumor activity and synergizes with PTX at much lower doses. Our results suggest that PEG-derivatized embelin may represent a novel and dual-functional carrier to facilitate the in vivo applications of poorly water-soluble anticancer drugs such as PTX.
New Sesamol Ethers as Pyrethrum Synergists
Devakumar, C.,Saxena, V. S.,Mukerjee, S. K.
, p. 725 - 730 (2007/10/02)
Several new methylenedioxyphenyl (MDP) ethers were synthesised from sesamol and methoxy substituted sesamols and screened as pyrethrum synergists.In general, the synergistic activity increased with the methoxyl substituents and decreased in the corresponding alkenyl analogs.The synergistic activity of alkyl ethers was found to vary with the alkyl chain, n-propyl ethers showing the maximum.In the case of alkenyl ethers, the activity followed the order γ,γ-dimethyl allyl > β-methallyl > allyl and showed no correlation between Rm and synergistic activity.