RESUMO
Apocynum venetum is a promising species to remediate an emerging environmental contaminant lithium (Li). However, no research has been conducted so far relating Li tolerance mechanism. In order to improve the understanding of Li transportation and detoxification, subcellular accumulation and distribution of different chemical forms of Li was studied in Apocynum venetum. Subcellular Li compartmentalization analysis showed that majority of Li was located in vacuole (45.52-72.65%) and cell wall (14.84-29.02%) under Li treatment. Furthermore, water soluble and ethonal extracted Li (inorganic Li) are the main chemical forms of Li taken up by A. venetum. With the increase of Li concentration in the medium, Li content in all subcellular fractions and proportion of F-ethanol form with high mobility increased. The greatest amount of Li was found in soluble fraction in leaves at 25â¯mgâ¯L-1 Li treatment, followed by soluble fraction in leaves at 2.5â¯mgâ¯L-1. These results suggest that Li compartmentation in leaf vacuoles is important in Li detoxification and Li accumulation of A. venetum.
Assuntos
Apocynum/metabolismo , Lítio/química , Lítio/metabolismo , Apocynum/efeitos dos fármacos , Lítio/farmacologia , Folhas de Planta/efeitos dos fármacos , Folhas de Planta/metabolismo , Raízes de Plantas/efeitos dos fármacos , Raízes de Plantas/metabolismo , Caules de Planta/efeitos dos fármacos , Caules de Planta/metabolismo , Frações Subcelulares/metabolismoRESUMO
Nine new derivatives (6-14) of the eremophilane sesquiterpene 07H239-A (5) were designed and semisynthesized with two types of R-groups by amidation. Most of them were active against five human tumor cell lines, and compounds 6-10 were more potent than the natural product 5. In particular, compounds 6 and 9 exhibited the strongest cytotoxic activity against MDA-MB-435 with IC50 values of 0.91 and 0.96 µM, respectively. Preliminary structure-activity relationships (SARs) analysis indicated that the 14-carboxyl in 5 was an ideal target for chemical modification, and the side chain of 5 might play a necessary role in facilitating their cytotoxic potencies.