Matches in SemOpenAlex for { <https://semopenalex.org/work/W3109583059> ?p ?o ?g. }
- W3109583059 endingPage "111050" @default.
- W3109583059 startingPage "111050" @default.
- W3109583059 abstract "Heart failure (HF) is an important and leading cause of substantial morbidity and mortality globally. The angiotensin-converting enzymatic (ACE) is the causative source for congestive heart failure. Natural products and its derivatives play a vital role in drug discovery and development owing to their efficacy and low toxicity. Pyxinol is a potent natural agent for cardiovascular disease. Thus we investigated the effect on ACE and HF of pyxinol derivatives. We designed and synthesized 32 novel fatty acid ester derivatives of pyxinol via esterification. Among them, compounds 2e (IC50=105 nM) and 3b (IC50=114 nM) displayed excellent ACE inhibitory activity in vitro, and exhibited non-toxic to H9c2 cells. The interactions between ACE and compounds were predicted by molecular docking respectively. In verapamil-induced zebrafish HF model, the activity assay showed that these two derivatives could improve cardiovascular physiological indexes including heart beats, venous congestion, heart dilation, cardiac output, ejection fraction and fractional shortening in a dose-dependent manner. A UPLC-QTOF-MS-based serum metabolomics approach was applied to explore the latent mechanism. A total of 25 differentiated metabolites and 8 perturbed metabolic pathways were identified. These results indicated that pyxinol fatty acid ester derivatives 2e and 3b might be considered as potent drug candidates against heart failure and deserved further research and development." @default.
- W3109583059 created "2020-12-07" @default.
- W3109583059 creator A5002661071 @default.
- W3109583059 creator A5023817184 @default.
- W3109583059 creator A5034597628 @default.
- W3109583059 creator A5035718600 @default.
- W3109583059 creator A5037014030 @default.
- W3109583059 creator A5042973046 @default.
- W3109583059 creator A5045991788 @default.
- W3109583059 creator A5049377516 @default.
- W3109583059 creator A5054426864 @default.
- W3109583059 creator A5055421170 @default.
- W3109583059 creator A5060093714 @default.
- W3109583059 date "2021-01-01" @default.
- W3109583059 modified "2023-09-29" @default.
- W3109583059 title "Design, synthesis and biological evaluation of novel pyxinol derivatives with anti-heart failure activity" @default.
- W3109583059 cites W1145343589 @default.
- W3109583059 cites W1967403815 @default.
- W3109583059 cites W1970857596 @default.
- W3109583059 cites W1981206665 @default.
- W3109583059 cites W1985864815 @default.
- W3109583059 cites W1988532962 @default.
- W3109583059 cites W1994034798 @default.
- W3109583059 cites W1997723283 @default.
- W3109583059 cites W1999056391 @default.
- W3109583059 cites W2004085095 @default.
- W3109583059 cites W2017120109 @default.
- W3109583059 cites W2019240682 @default.
- W3109583059 cites W2023142668 @default.
- W3109583059 cites W2033101925 @default.
- W3109583059 cites W2041247688 @default.
- W3109583059 cites W2044929196 @default.
- W3109583059 cites W2046971089 @default.
- W3109583059 cites W2050990399 @default.
- W3109583059 cites W2051383581 @default.
- W3109583059 cites W2052381458 @default.
- W3109583059 cites W2053286287 @default.
- W3109583059 cites W2062831191 @default.
- W3109583059 cites W2065017189 @default.
- W3109583059 cites W2065454100 @default.
- W3109583059 cites W2075665388 @default.
- W3109583059 cites W2088744527 @default.
- W3109583059 cites W2105668062 @default.
- W3109583059 cites W2118977816 @default.
- W3109583059 cites W2119340816 @default.
- W3109583059 cites W2125046568 @default.
- W3109583059 cites W2138203554 @default.
- W3109583059 cites W2148989249 @default.
- W3109583059 cites W214965827 @default.
- W3109583059 cites W2152704150 @default.
- W3109583059 cites W2256742438 @default.
- W3109583059 cites W2314094812 @default.
- W3109583059 cites W2337928559 @default.
- W3109583059 cites W2403966365 @default.
- W3109583059 cites W2507249427 @default.
- W3109583059 cites W2513717306 @default.
- W3109583059 cites W2548152158 @default.
- W3109583059 cites W2556132128 @default.
- W3109583059 cites W2579308973 @default.
- W3109583059 cites W2606476170 @default.
- W3109583059 cites W2699544910 @default.
- W3109583059 cites W2743613093 @default.
- W3109583059 cites W2749997931 @default.
- W3109583059 cites W2750807213 @default.
- W3109583059 cites W2752298876 @default.
- W3109583059 cites W2771687175 @default.
- W3109583059 cites W2774966343 @default.
- W3109583059 cites W2792264426 @default.
- W3109583059 cites W2792688663 @default.
- W3109583059 cites W2793621612 @default.
- W3109583059 cites W2811490671 @default.
- W3109583059 cites W2891377019 @default.
- W3109583059 cites W2892179165 @default.
- W3109583059 cites W2892254518 @default.
- W3109583059 cites W2896278453 @default.
- W3109583059 cites W2902990123 @default.
- W3109583059 cites W2904365182 @default.
- W3109583059 cites W2906081536 @default.
- W3109583059 cites W2959620596 @default.
- W3109583059 cites W2981107229 @default.
- W3109583059 cites W2987390185 @default.
- W3109583059 cites W2991855798 @default.
- W3109583059 cites W2992382265 @default.
- W3109583059 cites W2992870355 @default.
- W3109583059 cites W2993329266 @default.
- W3109583059 cites W3000555966 @default.
- W3109583059 cites W3005682838 @default.
- W3109583059 cites W3010868288 @default.
- W3109583059 cites W3015816038 @default.
- W3109583059 cites W3025303888 @default.
- W3109583059 cites W3044019810 @default.
- W3109583059 cites W3081429986 @default.
- W3109583059 cites W4211150832 @default.
- W3109583059 cites W617061922 @default.
- W3109583059 cites W940660918 @default.
- W3109583059 doi "https://doi.org/10.1016/j.biopha.2020.111050" @default.
- W3109583059 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/33378957" @default.
- W3109583059 hasPublicationYear "2021" @default.