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Steroids 2021 Apr 6:108830. Epub 2021 Apr 6.

Department of Pharmacology, Shantou University Medical College, Shantou 515041, Guangdong, China. Electronic address:

To identify new potential anti-inflammatory agents, we herein report the synthesis of novel steroidal chalcones with 3β-pregnenolone esters of cinnamic acid derivatives using pregnenolone as the starting material. The structures of the newly synthesised compounds were confirmed by H-NMR, C-NMR, HRMS and infrared imaging. All the derivatives were examined to determine their in vitro anti-inflammatory profiles against LPS-induced inflammation in RAW 264. Read More

Nucleic Acids Res 2021 Apr 9. Epub 2021 Apr 9.

Institute of New Drug Development, China Medical University, Taichung 406, Taiwan.

Mammalian cyclic GMP-AMP synthase (cGAS) and its homologue dinucleotide cyclase in Vibrio cholerae (VcDncV) produce cyclic dinucleotides (CDNs) that participate in the defense against viral infection. Recently, scores of new cGAS/DncV-like nucleotidyltransferases (CD-NTases) were discovered, which produce various CDNs and cyclic trinucleotides (CTNs) as second messengers. Here, we present the crystal structures of EcCdnD, a CD-NTase from Enterobacter cloacae that produces cyclic AMP-AMP-GMP, in its apo-form and in complex with ATP, ADP and AMPcPP, an ATP analogue. Read More

Curr Med Mycol 2020 Sep;6(3):9-14

Amity Institute of Biotechnology, Amity University Haryana, Gurugram (Manesar)-122413, India.

Background And Purpose: The increment in fungal infections, particularly due to species, is alarming due to the emergence of multidrug resistance (MDR). Hence, the identification of novel drug targets to circumvent the problem of MDR requires immediate attention. The metabolic pathway, such as glyoxylate cycle (GC), which utilizes key enzymes (isocitrate lyase [ICL] and malate synthase [MLS]), enables to adapt under glucose-deficient conditions. Read More

Evid Based Complement Alternat Med 2021 24;2021:6676470. Epub 2021 Mar 24.

Chongqing Academy of Chinese Materia Medica, No. 34 Nanshan Road, Nan'an District, Chongqing 400065, China.

Sesquiterpene pyridine alkaloids are a large group of highly oxygenated sesquiterpenoids, which are characterized by a macrocyclic dilactone skeleton containing 2-(carboxyalkyl) nicotinic acid and dihydro--agarofuran sesquiterpenoid, and are believed to be the active and less toxic components of . In this study, 55 sesquiterpene pyridine alkaloids from were subjected to identification of pharmacophore characteristics and potential targets analysis. Our results revealed that the greatest structural difference of these compounds was in the pyridine ring and the pharmacophore model-5 (Pm-05) was the best model that consisted of three features including hydrogen bond acceptor (HBA), hydrogen bond donor (HBD), and hydrophobic (HY), especially hydrophobic group located in the pyridine ring. Read More

Drug Des Devel Ther 2021 31;15:1441-1457. Epub 2021 Mar 31.

Chongqing Collaborative Innovation Center for Functional Food, Chongqing University of Education, Chongqing, 400067, People's Republic of China.

Aim: White tip silver needle, a slightly fermented white tea, is abundant in flavonoids, and it has great significance in terms of D-galactose/lipopolysaccharide-induced aging in mice.

Methods: We analyzed the antioxidant capacity of white tip silver needle flavonoids (WTSNF) in vitro, assessed the effects of WTSNF on organ indexes, pathological changes, liver function indexes, biochemical indicators, molecular biological indicators, and genes related to oxidation and inflammation.

Results: Ultra-high performance liquid chromatography-tandem mass spectrometry results showed that WTSNF contained baicalin, kaempferol, kaempferide, quercetin, isorhamnetin, lespenephryl, and rutin. Read More