Identification of PD-1 small molecule inhibitors and validation in Panax ginseng / 药学学报

Tumor immune therapy has been remarkably successful in recent years and several kinds of PD-1/PD-L1 (programmed death-1/programmed death-ligand 1) antibody drugs have been approved by the FDA for treatment of advanced malignant neoplasms. However, as biomacromolecules these antibody drugs have certain drawbacks such as high cost, injection-only administration and immunogenicity; thus, we turned to small molecules that have lower immune risks and better modifiability. Considering the structural diversity of natural products, we chose to investigate the active components in Panax ginseng, a famous and highly valued traditional Chinese medicine. Nine compounds were separated and identified in this research using a HPLC-coupled MS system, and 3 PD-1 binding compounds were identified using the SPR method. The PD-1/PD-L1 inhibitory ability of ginsenoside Rg1, as a representative ginsenoside, was verified by cytopharmacological methods. This research provides a new method for the identification of immune blockade inhibitors in natural products.

Studies on chemical constituents of aerial parts of Ammopiptanthus mongolicus / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the chemical constituents of the aerial parts of Ammopiptanthus mongolicus.</p><p><b>METHOD</b>The chemical constituents were isolated by various column chromatographic methods. The structures were identified by spectral data.</p><p><b>RESULT</b>Ten compounds were isolated and identified as m-hydroxybenzoic acid (1), 1-(4-hydroxyphenyl) ethanone (2), beta-sitosterol (3), (-)-syringaresinol (4), (+)-lariciresinol (5), blumenol A (6), blumenol B (7), beta-daucosterol (8), coniferin (9), syringin (10).</p><p><b>CONCLUSION</b>The ten compounds were obtained from the genus Ammopiptanthus for the first time.</p>

Determination of cichoric acid in Echinacea purpuea / 中国中药杂志

<p><b>OBJECTIVE</b>To analyze the natural change rule of active components of E. purpuea by measuring content of cichoric acid.</p><p><b>METHOD</b>Reverse HPLC method was used.</p><p><b>RESULT</b>The maximum cichoric acid content of the roots occured in seedling age of May, and that of the flowers occured in blooming stage of mid July, but cichoric acid in stems was generally low anyway. The maximum content of cichoric acid in the plant above ground occured in the blooming stage of mid July.</p><p><b>CONCLUSION</b>The measuring method of content of cichoric acid is successful and reliable. The optimum stage of harvest in Echinacea purpuea should be guided by natural change rule of cichoric acid content.</p>

Variation of endogeneous ET, CGRP and NO in myocardial ischemia in rats and the regulatory effect of xinshuping / 中国中药杂志

<p><b>OBJECTIVE</b>To observe the variation of ET and CGRP contents in ischemic heart, and NO level in serum of myocardial damaged rats, and their regulation when with the protection of Xinshuping, a traditional Chinese medicine compound.</p><p><b>METHOD</b>The models of myocardial ischemia were prepared by subcutaneous injection of isoproterenol or by ligation of coronary artery.</p><p><b>RESULT</b>ET content in myocardium was significantly increased (P < 0.01), and CGRP content as well as NO level in serum was not changed obviously in the model induced by isoproterenal. However, NO level in serum of rats treated with Xinshuping (ig bid x 2.5 d) was markedly raised (P < 0.01), neither ET not CGRP contents were affected by it. LDH and CK levels in serum of rats were evidently lowered by Xinshuping treatment. S-T segment's elevation of ECG was significantly inhibited and myocardial infarction size was reduced markedly by Xinshuping treatment in rats subjected to coronary artery ligature.</p><p><b>CONCLUSION</b>ET, CGRP or NO is involved in myocardial infarction caused by isoproterenol. The ischemic damage or dysfunction in different models is obviously protected by Xinshuping. The promotion of NO release from vascular endothelium is probably related with this protective effect.</p>