A series of benzamide derivatives such as 1-(1,3-benzodioxol-5-ylcarbonyl) piperidine (1-BCP) were synthesized by the reaction of substituted benzoic acids with piperidine, morpholine or pyrrolidine using a novel method. The crystals of these benzamide derivatives were obtained by recrystallization. Structures of target and intermediate compounds were determined via FT-IR, ¹H-NMR and elemental analysis and X-ray crystallography of select examples. The crystal structures of these compounds have potential applications to identify the binding site for allosteric modulators of the α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor. The anti-fatigue effects of the benzamide derivatives in weight-loaded forced swimming mice were investigated in a swimming endurance capacity test used as an indicator of fatigue. The swimming times to exhaustion were longer in the b3, d3, and e3 groups than in the caffeine group (p < 0.05). In conclusion, b3, d3 and e3 enhanced the forced swimming capacity of mice. The mechanism of the anti-fatigue effects will be studied in the future.

Pseudolarix amabilis (Nelson) Rehd, is a monotypic genus plant belonging to the family Pinaceae. The root bark , known as “Tu-Jin-Pi” has been used for the treatment of skin diseases. During our activity screening, the water-soluble part of the 70% EtOH extract of P. amabilis bark showed excellent inhibitory bioactivities on PTP1B enzyme, leading to the phytochemical isolation of the root bark of P. amabilis. Three oleanane-type compounds (1-3) and seven phenolic compounds (4-10) were isolated, in which oleanolic acid 3-O-β-D-glucuronyl-6′-ethyl ester (1) was identified as a new saponin. The chemical structures of these compounds were elucidated by 1D/2D nuclear magnetic resonance and high resolution mass spectra. In addition, their pharmacological inhibitory bioactivities on PTP1B enzyme were evaluated, and the three oleanane-type compounds 1-3 exhibited inhibitory bioactivities with IC50 values of 1.90 ± 0.37, 19.15 ± 0.10 and 10.44 ± 0.59 μM, respectively.

Background: Zhengyuan prescription (ZYP) is a Chinese herbal medicine used in clinical practice to protect against radiotherapy-induced injuries. In this study, we investigate the protective effect of ZYP against X-ray-induced injury of human umbilical vein endothelial cells (HUVECs), and we explore the mechanisms underlying this effect.Methods: After 3 h of ZYP intervention, the cells in the ZYP group were irradiated with 6 Gy X-rays and cultured for 48 h. Subsequently, the cell viability, cell morphology, mitochondrial membrane potential, and apoptosis and oxidative stress markers were observed, as well as the expressions of apoptotic and oxidative stress proteins.Results: The obtained results demonstrate that exposure to X-rays promotes cell death, reduces mitochondrial membrane potential, and induces the pirroduction of intracellular reactive oxygen species (ROS). Pretreatment with ZYP reverses these effects to a great extent. Moreover, it up-regulates the expression of the B-cell lymphoma 2 (Bcl-2) apoptosis inhibitor protein while down-regulating the expressions of Bcl-2-associated X protein (Bax), caspase-3, and caspase-9. Interestingly, ZYP can also inhibit oxidative stress injury by activating the expression of Nrf2 (Nuclear Factor E2 related factor) regulated antioxidant enzyme genes such as Heme oxygenase 1 (HO-1) and NAD(P)H:quinone oxidoreductase-1 (NQO1)Conclusions: This study is the first to demonstrate that ZYP suppresses X-ray-induced injury of HUVECs by activating the Nrf2 signaling pathway.