RESUMO
Two homogeneous polysaccharides, GEP-3 and GEP-4, were purified from Gastrodia elata, a precious traditional Chinese medicine. Their structural characteristics were obtained using HPGPC, PMP-HPLC, LC/MS, FT-IR, NMR, and SEM methods. GEP-3 was 1,4-glucan with molecular weight of 20 kDa. Interestingly, GEP-4 comprised of a backbone of â[4)-α-Glcp-(1]10â[4)-α-Glcp-(1â]5[6)-ß-Glcp-(1]11â6)-α-Glcp-(3â and two branches of ß-Glcp and p-hydroxybenzyl alcohol citrate, with repeating p-hydroxybenzyl alcohol attached to the backbone chain at O-6 position of â4,6)-α-Glcp-(1â and O-1 position of â3,6)-α-Glcp-(1â. GEP-4 is a novel polysaccharide obtained and characterized for the first time. Bioactivity test indicated that both of them significantly promote the growth of Akkermansia muciniphila (Akk. muciniphila). Furthermore, GEP-3 and GEP-4 promoted the growth of Akk. muciniphila from high-fat diet (HFD) fecal microbiota. These results indicated that GEP-3 and GEP-4 were potential Akk. muciniphila growth promoters.
Assuntos
Gastrodia , Extratos Vegetais/farmacologia , Polissacarídeos/farmacologia , Akkermansia/efeitos dos fármacos , Akkermansia/crescimento & desenvolvimento , Akkermansia/isolamento & purificação , Animais , Dieta Hiperlipídica , Modelos Animais de Doenças , Fezes/microbiologia , Gastrodia/química , Microbioma Gastrointestinal , Camundongos , Estrutura Molecular , Hepatopatia Gordurosa não Alcoólica/microbiologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Polissacarídeos/química , Polissacarídeos/isolamento & purificaçãoRESUMO
A series of cinobufagin-3-yl nitrogen-containing-carbamate derivatives were designed, synthesized, and evaluated for their proliferation inhibition activities. The structure-activity relationships suggested that the substituents at C-16 was a crucial factor for the potency and that follows this trends: acetic ester â« benzoic ester ≈ hydroxy > carbamate. Compounds 3f, 3g, 3h, and 3i exhibited significant in vitro antiproliferative activities against the eight tested tumor cell lines, with IC50 values ranging from 8.1 to 237.4 nM. Furthermore, 3g tartrate (3g-TA) significantly inhibited tumor growth by 64.5%, 83.9%, and 93.0% at a doses of 4, 6, 8 mg/kg/qod by ip, respectively.