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Rosa laevigata Michx., a member of the Rosaceae family, is a famous traditional Chinese medicine and edible food in Asian countries. The major active ingredient is triterpenoid, which has anti‐Alzheimer's Disease (AD), antioxidant and neuroprotection properties. However, the properties of "multi‐component structure" and "multi‐directional target" make it impossible to explain the molecular mechanism by conventional ways. The present study aimed to predict the multi‐target mechanisms of triterpenoids in R. laevigata against AD using high performance liquid chromatography equipped with quadrupole time‐of‐flight mass spectrometer (HPLC‐Q‐TOF MS) approach, network pharmacology analysis, dynamics simulation (MDs) and validation of the predicted results with straight‐target tests as well as neuroprotection model. Firstly, bioassay‐guided fractionation of R. laevigata integrated with LC‐MS/MS analysis of the most prospective enriched fractions in terms of anti‐AD efficacy was commenced. Subsequently, multi‐level network model of "multi components‐multi‐targets‐multiple pathways" was established based on the identification of 69 triterpenoids. Complementarily, 64 AD‐related targets were identified through various databases. Network structure analysis illuminated that the intricate pharmacological mechanisms improving cognitive dysfunction of AD was superiorly combined with the crucial targets of APP, APOE, VEGFA, IL1B, MAPT, PSEN1 and BACE and further regulation of principal pathways as HIF‐1 and Calcium signaling pathways. In addition, AChE, BChE and BACE inhibitory activities in vitro showed that nine compounds exhibited potential inhibitory activities. The neuroprotective effects also had a similar effect on H2O2‐induced SH‐SY5Y cell injury. The results show that R. laevigata and its bioactive triterpenoids can pave the way for potential application as inhibitors for treatment of AD. [ABSTRACT FROM AUTHOR]

A set of conditions for the Strecker reaction of formaldehyde, amines, and TMSCN that affords three‐component coupling adducts as the major products is reported. HCOOH and TBAF are used as cocatalysts and the TMSCN functions as both cyanide source and protecting reagent for amines. As a result, the side reactions were suppressed efficiently and a broad range of aromatic and aliphatic amines were mono‐cyanomethylated in 52–99% yield. Furthermore, this protocol was successfully applied toward the synthesis of meta‐diamide insecticides. [ABSTRACT FROM AUTHOR]

Summary: Considering the medicinal and edible properties of Physalis pubescens L. fruit, the plant has a long history of cultivation in China. In the current study, a novel polysaccharide (PPL‐1) was successfully obtained from P. pubescens fruits using multi‐column techniques. The chemical characterisation of the polysaccharide was achieved by acid hydrolysis, determination of weight average molecular mass, thermogravimetric and Smith degradation analyses, in addition to ultraviolet, Fourier transform infrared spectroscopy, one‐ and two‐dimensional nuclear magnetic resonance spectroscopy. According to the structural analyses, PPL‐1 consisted of rhamnose, arabinose, fructose, mannose and glucose with a relative molar ratio of 0.39:0.12:0.02:0.03:0.44. The average molecular weight of PPL‐1 was 7.3 kDa and it was mainly composed of (1 → 3) and (1 → 6) linkages. PPL‐1 exhibited not only scavenging effects on 2,2‐diphenyl‐1‐picrylhydrazyl and 2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulfonic acid) free radicals but also hydrogen peroxide‐induced oxidative stress in SH‐SY5Y cells effectively by decreasing malondialdehyde content and increasing total antioxidant capacity, superoxide dismutase and glutathione peroxidase activity levels. [ABSTRACT FROM AUTHOR]

Front Cover Picture: Strecker Reactions of Formaldehyde with TMSCN, Catalyzed by TBAF and Formic Acid: N-Monocyanomethylation of Primary Amines (Adv. Strecker reaction, formaldehyde, TMSCN, N-monocyanomethylation, meta-diamide insecticides Keywords: Strecker reaction; formaldehyde; TMSCN; N-monocyanomethylation; meta-diamide insecticides EN Strecker reaction formaldehyde TMSCN N-monocyanomethylation meta-diamide insecticides 1 1 1 01/20/23 20230110 NES 230110 The front cover picture illustrates the Strecker reaction of formaldehyde, primary amines and TMSCN. [Extracted from the article]