查看更多>>摘要：? 2022 Phytochemical Society of EuropeGlobally, non-alcoholic fatty liver disease (NAFLD) has become the most common chronic liver disease, and has attracted considerable research traction in the literature. However, no effective drugs have yet been approved by the Food and Drug Administration. In this study, a new isoxazole derivative (1), which activated AMPK and reduced gluconeogenesis levels, was evaluated in HFD-induced obese mice for NAFLD treatment. Our results showed that 1 reduced body weight gain and attenuated metabolic disorder in these mice. Underlying mechanisms revealed that 1 alleviated hepatic steatosis by activating AMPK, and inflammatory responses by inhibiting NF-κB. Our study suggested that 1 may be clinically valuable as an NAFLD therapeutic candidate.
查看更多>>摘要：? 2022 Phytochemical Society of EuropeA total synthesis of four flavans with a furan ring in different positions (1–4) was achieved successfully. The flavan was synthesized from flavanone by reduction and followed by deoxygenation steps. The synthesized compound 2 was confirmed as the naturally occurring moracinflavan E based on the comparison of their NMR spectral data.
查看更多>>摘要：? 2022Methodologies for the synthesis of C10-C-unsaturated clarithromycin congeners have been developed from corresponding C10-methyl erythromycin A ketolides. Activation of the unreactive C10-methyl group and subsequent Pd-catalyzed cross-coupling reactions afford novel C-10-unsaturated clarithromycins for antibacterial screening programs. By related methodology azides can be prepared and used for the preparation of corresponding 1,2,3-triazoles by click chemistry. The work demonstrates the importance of transition metal catalysis in natural product semi-synthesis and potential SAR studies. The in vitro MIC values from screening the products against strains of respiratory pathogens of S. pneumoniae and S. aureus indicate that the new antibacterials are close to equipotent with the clarithromycin reference compound.
查看更多>>摘要：? 2022 Phytochemical Society of EuropeTwo new sesquiterpene phenol trimers, tridysoxyphenols A (2) and B (3), along with two known compounds, namely a sesquiterpene phenol, (+)-7-hydroxycalamenene (1), and a tetralone derivative, 4-hydroxy-4,7-dimethyl-α-tetralone (4), were isolated from the leaves of Dysoxylum parasiticum (Osbeck) Kosterm. The structures of 2 and 3 were elucidated using nuclear magnetic resonance (NMR) spectroscopy, ultraviolet (UV) spectroscopy, infrared (IR) spectroscopy, high-resolution electrospray ionization time-of-flight mass spectrometry (HR-ESI/TOF-MS), and time-dependent density functional theory (TDDFT) calculations of the electronic circular dichroism (ECD) spectroscopic data. No cytotoxic activity was observed for any of the isolated compounds at low concentrations, although compound 1 suppressed the viability of HL60 cells at 119.85 ± 10.03 μM.
查看更多>>摘要：? 2022 Phytochemical Society of EuropeThree undescribed jatrophane diterpenoids, named euphpepluones P-R (1–3), were isolated from the whole plant Euphorbia peplus. The structures of these compounds were elucidated by spectroscopic methods. The absolute configuration of 1 was further assigned by X-ray crystallographic analysis. All compounds were evaluated for bioactivity towards autophagic flux by flow cytometry using HM mCherry-GFP-LC3 cells. Compounds 2 and 6 exhibited significant inhibition of autophagic flux.
NSTL
Elsevier