Objective: To observe the different effects between Mahuang (Herba Ephedra Sinicae) and Wuweizi (Fructus Schisandrae Chinensis) on the pathological changes of rats with bleomycin A(5)-induced pulmonary fibrosis. Methods: Ninety Wistar rats were randomly divided into sham operation group, model group, hydrocortisone group, Herba Ephedra Sinicae group, Fructus Schisandrae Chinensis group and Herba Ephedra Sinicae plus Fructus Schisandrae Chinensis group. There were 16 rats in each group except the sham operation group (10 rats). Pulmonary fibrosis was induced by a single intratracheal injection of bleomycin A5. Hematoxylin and eosin straining and immunohistochecical method were used after 7- and 28-day treatment to observe the pathology of lung injury, measure the inner diameter of pulmonary arterioles and the density of nuclear membrane. Results: Compared with the sham operation group at 7 and 28 d, alveolar inflammation level was significantly increased in the model group (P<0.01). Alveolar inflammation level was decreased obviously in the hydrocortisone group (P<0.05) after 7- and 28-day treatment as compared with the model group, and that in Herba Ephedra Sinicae plus Fructus Schisandrae Chinensis group was also decreased obviously (P<0.05) at 28 d. Compared with the sham operation group, nuclear density of the model group was increased, while its inner diameter was decreased (P<0.05). In the Fructus Schisandrae Chinensis group, Herba Ephedra Sinicae plus Fructus Schisandrae Chinensis group and hydrocortisone group, the nuclear density was decreased (P<0.05) as compared with the model group. Inner diameter in the Herba Ephedra Sinicae group, Herba Ephedra Sinicae plus Fructus Schisandrae Chinensis group and hydrocortisone group was higher than that in the model group (P<0.05). Microvessel density of the model group was obviously higher than that of the sham operation group (P<0.05). Compared with the model group, Herba Ephedra Sinicae plus Fructus Schisandrae Chinensis group and hydrocortisone group had lower microvessel density (P<0.05). Conclusion: Herba Ephedra Sinicae combined with Fructus Schisandrae Chinensis can restrain pulmonary artery injury. The nuclear density and microvessel density can be reduced by Fructus Schisandrae Chinensis, while Herba Ephedra Sinicae can increase the inner diameter.

Phosphatidylinositol-3-kinase (PI3K) inhibitors can increase the sensitivity of tumor cells to Poly ADP-ribose polymerase-1 (PARP-1) inhibitors. Therefore, the simultaneous inhibition of the PARP-1 and PI3K activities are expected to overcome the drug resistance of PARP-1 inhibitors.In our previous work, two compounds XW-1 and WZ-1 with excellent activities against PARP-1 and PI3K were obtained with the limitation to further study due to their poor water solubility.Therefore, XW-1 and WZ-1 were chosen as lead compounds to optimize their solubility by introducing a salt-forming site via a urea group, and 11 novel compounds were designed and synthesized. The structure of all target compounds was confirmed by 1H NMR, 13C NMR, and HRMS.The enzyme activities of the compounds against PARP-1 and PI3K were measured, and the results showed that most of the compounds demonstrated good inhibitory activities against PARP-1 and PI3K.Based on the above result, the inhibitory activities of compounds 8b, 8e, and 8f against MDA-MB-231, MDA-MB-468, HCC1937, HCT116, and olaparib-resistant HCT116R were determined by MTT, respectively.Additionally, the structure-activity relationship was discussed. The results showed that these compounds displayed excellent antiproliferation activity.Among them, compound 8f demonstrated antiproliferation remarkably against all five tumor cells, which was more potent than that of olaparib, and was comparable to that of BKM120.Furthermore, the solubility of hydrochloride salts of compound 8b and 8f was significantly improved compared to the lead compounds.The results of this study will provide a theoretical basis for the further development of PARP-1 and PI3K dual-target inhibitors with good pharmaceutical properties and strong inhibitory activities.

This paper describes the digital earth technology and its core technology-"3S" integration technology. The advance and promotion of the "3S" technology provide more favorable means and technical support for Chinese medicine resources survey, evaluation and appropriate zoning. Grid is a mature and popular technology that can connect all kinds of information resources. The author sums up the application of digital earth technology in the research of traditional Chinese medicine resources in recent years, and proposes the new method and technical route of investigation in traditional Chinese medicine resources, traditional Chinese medicine zoning and suitability assessment by combining the digital earth technology and grid.
Conservation of Natural Resources ; Medicine, Chinese Traditional ; methods ; Research ; Satellite Communications ; Technology