RESUMO
A series of pentacyclic triterpenoids similar to glycyrrhetinic acid were designed and synthesized via the combination of chemical modification and microbial catalysis. All products were screened for the glycogen phosphorylases inhibitory activities in vitro. Within this series of derivatives, compound 5 displayed good inhibitory activities with IC50 value of 27.7 µM, which is better than that of the other derivatives and glycyrrhetinic acid. Structure-activity relationship (SAR) analysis of these inhibitors was also discussed.
Assuntos
Aspergillus ochraceus/metabolismo , Glicogênio Fosforilase/antagonistas & inibidores , Ácido Oleanólico , Streptomyces griseus/metabolismo , Biotransformação , Inibidores Enzimáticos/química , Inibidores Enzimáticos/metabolismo , Ácido Glicirretínico/análogos & derivados , Ácido Glicirretínico/química , Concentração Inibidora 50 , Estrutura Molecular , Ácido Oleanólico/biossíntese , Ácido Oleanólico/síntese química , Ácido Oleanólico/química , Ácido Oleanólico/metabolismo , Relação Estrutura-AtividadeRESUMO
The natural crosslinking agent genipin has been applied widely in biomedicines and foods nowadays. Because of the special hemiacetal ring structure in its molecule, it can only be prepared by hydrolysis of geniposide according to biocatalysis. In this research, strategies including aqueous-organic biphasic catalysis and substrate fed-batch mode were adopted to improve the biocatalysis process of genipin. A 10 L ethyl acetate-aqueous biphasic system with geniposide fed-batch led to a satisfying genipin yield. With Fusarium solani ACCC 36223, 15.7 g/l genipin in the ethyl acetate phase was obtained, corresponding to space-time yields of 0.654 g l(-1) h(-1).
Assuntos
Reagentes de Ligações Cruzadas/metabolismo , Fusarium/metabolismo , Iridoides/metabolismo , Técnicas de Cultura Celular por Lotes , Meios de Cultura/química , Fusarium/crescimento & desenvolvimento , HidróliseRESUMO
The tomato iron transporter gene (LeIRT2) was introduced to Malus robusta Rehd. via Agrobacterium-mediated transformation to produce iron-deficiency tolerant apple rootstock. A total of 19 putative transformants were obtained, 11 of which were verified by PCR amplification to carry a fragment of the transgene. Among them, nine were confirmed to carry the transgene by Southern blot analysis with one to three copies of the transgene integrated into the plant genome. Two transgenic plants, one carrying one copy and the other three copies of the transgene, were hydroponically cultured to test their tolerance to iron-deficiency, which was found only in the transgenic plant with a single copy, which weighted 21%-4% greater than those of the control plants.
