50906-12-2Relevant academic research and scientific papers
Design of chromogenic probes for efficient screening and evaluation of feruloyl esterase-like activities
Gherbovet, Olga,Fauré, Régis,Ferreira, Fernando,Durand, Julien,Ragon, Mélanie,Hostyn, Guillaume,Record, Eric,Bozonnet, Sophie,O'Donohue, Michael J.
, p. 24 - 31 (2016)
Feruloyl esterases (FAEs) constitute an important sub-group of hydrolytic enzymes involved in the deconstruction of plant cell wall polysaccharides. However, in the current era of genomics and metagenomics, finding and characterizing FAEs is not straightf
Development trans-N-benzyl hydroxyl cinnamamide based compounds from cinnamic acids and characteristics anticancer potency
Agustan, Agustan,Bahriah, Bahriah,Dali, Seniwati,Firdausiah, Syadza,Rasyid, Herlina,Soekamto, Nunuk Hariani,Tahir, Dahlang,Zenta, Firdaus
, (2022/01/31)
The derivatization of three hydroxycinnamamides becomes trans-N-benzylhydroxycinnamamides, and their potential assay as anticancer agents has been carried out. N-benzyl-p-coumaramide (5a), N-benzylcaffeamide (5b), and N-benzylferulamide (5c) were obtained
Stable isotopic labelling of β-sitosteryl ferulate for use as analytical tool
Baron, Giovanna,Fumagalli, Laura,Mazzotta, Sarah
, (2022/02/01)
Rice is one of the major staple foods consumed worldwide and due to the presence of γ-oryzanol (γ-OZ) it is well-recognized as functional food. For this reason, the most appropriate varieties' identification in term of content of γ-OZ has become essential
Design, synthesis of Cinnamyl-paeonol derivatives with 1, 3-Dioxypropyl as link arm and screening of tyrosinase inhibition activity in vitro
Tang, Kai,Jiang, Yi,Zhang, Huawei,Huang, Wenli,Xie, Yundong,Deng, Chong,Xu, Hongbo,Song, Xiaomei,Xu, Hong
supporting information, (2020/12/13)
This study aimed to obtain tyrosinase inhibitors for treating hyperpigmentation. A series of cinnamyl ester analogues were designed and synthesized with cinnamic acid (CA) and peaonol compounds. The safety, melanin content and inhibitory effects of all ta
Quorum sensing and nf-κb inhibition of synthetic coumaperine derivatives from piper nigrum
Baruch, Yifat,Gopas, Jacob,Kadosh, Yael,Kumar, Rajendran Saravana,Kushmaro, Ariel,Muthuraman, Subramani,Yaniv, Karin
supporting information, (2021/05/28)
Bacterial communication, termed Quorum Sensing (QS), is a promising target for virulence attenuation and the treatment of bacterial infections. Infections cause inflammation, a process regulated by a number of cellular factors, including the transcription Nuclear Factor kappa B (NF-κB); this factor is found to be upregulated in many inflammatory diseases, including those induced by bacterial infection. In this study, we tested 32 synthetic derivatives of coumaperine (CP), a known natural compound found in pepper (Piper nigrum), for Quorum Sensing Inhibition (QSI) and NF-κB inhibitory activities. Of the compounds tested, seven were found to have high QSI activity, three inhibited bacterial growth and five inhibited NF-κB. In addition, some of the CP compounds were active in more than one test. For example, compounds CP-286, CP-215 and CP-158 were not cytotoxic, inhibited NF-κB activation and QS but did not show antibacterial activity. CP-154 inhibited QS, decreased NF-κB activation and inhibited bacterial growth. Our results indicate that these synthetic molecules may provide a basis for further development of novel therapeutic agents against bacterial infections.
A Series of Ferulic Acid Amides Reveals Unexpected Peroxiredoxin 1 Inhibitory Activity with in vivo Antidiabetic and Hypolipidemic Effects
Yasmin, Sabina,Cerchia, Carmen,Badavath, Vishnu Nayak,Laghezza, Antonio,Dal Piaz, Fabrizio,Mondal, Susanta K.,Atl?, ?zlem,Baysal, Merve,Vadivelan, Sankaran,Shankar,Siddique, Mohd Usman Mohd,Pattnaik, Ashok Kumar,Singh, Ravi Pratap,Loiodice, Fulvio,Jayaprakash, Venkatesan,Lavecchia, Antonio
, p. 484 - 498 (2020/11/02)
Insulin resistance is a major pathophysiological feature in the development of type 2 diabetes (T2DM). Ferulic acid is known for attenuating the insulin resistance and reducing the blood glucose in T2DM rats. In this work, we designed and synthesized a library of new ferulic acid amides (FAA), which could be considered as ring opening derivatives of the antidiabetic PPARγ agonists Thiazolidinediones (TZDs). However, since these compounds displayed weak PPAR transactivation capacity, we employed a proteomics approach to unravel their molecular target(s) and identified the peroxiredoxin 1 (PRDX1) as a direct binding target of FAAs. Interestingly, PRDX1, a protein with antioxidant and chaperone activity, has been implied in the development of T2DM by inducing hepatic insulin resistance. SPR, mass spectrometry-based studies, docking experiments and in vitro inhibition assay confirmed that compounds VIe and VIf bound PRDX1 and induced a dose-dependent inhibition. Furthermore, VIe and VIf significantly improved hyperglycemia and hyperlipidemia in streptozotocin-nicotinamide (STZ-NA)-induced diabetic rats as confirmed by histopathological examinations. These results provide guidance for developing the current FAAs as new potential antidiabetic agents.
Ferulic acid amide derivative, and synthesis method and application thereof
-
, (2021/06/13)
The invention provides a ferulic acid amide derivative represented by the following general formula IV, wherein R represents phenyl, p-methoxyphenyl, 4-aminodiphenyl ether, 4-trifluoromethoxyphenyl, 4-(trifluoromethyl)phenyl, 3-aminobenzene isopropyl ethe
Design, synthesis, and bioassay of 4-thiazolinone derivatives as influenza neuraminidase inhibitors
Xiao, Mengwu,Xu, Lvjie,Lin, Ding,Lian, Wenwen,Cui, Manying,Zhang, Meng,Yan, Xiaowei,Li, Shuishi,Zhao, Jun,Ye, Jiao,Liu, Ailin,Hu, Aixi
, (2021/02/09)
A series of 4-thiazolinone derivatives (D1-D58) were designed and synthesized. All of the derivatives were evaluated in vitro for neuraminidase (NA) inhibitory activities against influenza virus A (H1N1), and the inhibitory activities of the five most pot
Cinnamate derivatives and application of cinnamate derivatives as tyrosinase inhibitors and gels
-
Paragraph 0077-0079; 0081, (2020/08/02)
The invention discloses cinnamate derivatives and application of the cinnamate derivatives as tyrosinase inhibitors and gels, and the structural general formula of the cinnamate derivatives is shown in the specification, in the formula, X and Y independently represent any one of O, S and NH, wherein R1 and R2 independently represent any one of H, OH, methoxy, allyl and acetyl; R3 and R4 respectively and independently represent any one of H, OH, methoxy, tert-butyl dimethyl siloxy and carbethoxy, and R3 and R4 are not tert-butyl dimethyl silyl at the same time; and n is an integer from 2 to 5.The cinnamate derivatives disclosed by the invention have obvious inhibitory activity on the activity of mushroom tyrosinase diphenolic enzyme and the content of tyrosinase and melanin in melanoma cells of B16F10 mice, and can be used for preparing the tyrosinase inhibitors. Meanwhile, the cinnamate derivatives can form stable gels in olive oil and can be used as micromolecular gels for cosmeticsand the like.
Thiourea derivatives, and preparation method and application thereof
-
, (2020/06/05)
The invention relates to thiourea derivatives represented by formula I, pharmaceutically acceptable salts thereof and a pharmaceutical composition thereof, and an application of the thiourea derivatives in the preparation of an influenza virus neuraminida
