Protosappanin A increases the sensitivity of gastric cancer SGC-7901 cells to radiotherapy / 实用肿瘤学杂志

Objective In this study,Protosappanin A,Caesalpinia Sappan L extract and Cisplatin were combined with radiotherapy in gastric cancer cell SGC-7901 to investigate whether the Protosappanin A could in-crease radiosensitivity( SER) in gastric cancer SGC-7901 cells. This will be medication to create new areas of in-novation in the future. Methods The cell proliferation of SGC-7901 cells was detected by MTT assay. The rela-tionship between the effect of the Protosappanin A on cell proliferation and the time of action was determined. Caesalpinia Sappan L extract and Cisplatin were as controls. The fitted cell survival curve and clonal formation as-says were used to determine the SER to analyze the sensitizative effect of Protosappanin A. Results Protosappa-nin A could inhibit the growth of SGC-7901 cells,and its inhibitory effect is relatively weak. Its cytotoxicity has a time-and concentration-dependent manner. Cellular morphological changes were observed accompanying with increased concentrations and time treatments of Protosappanin A. Clonal formation experiment showed that the Protosappanin A significantly increased the radiosensitivity of SGC-7901 cells when compared to the radioactive group. They showed a statistically difference. Conclusion The inhibitory effect of the Protosappanin A on SGC-7901 cells in a concentration and time-dependent manner. Protosappanin A combined radiotherapy can improve the radiosensitization of cells,both of which may have synergistic anti-tumor effect.

Protosappanin A exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia / 中国天然药物

Microglial activation and resultant neuroinflammatory response are implicated in various brain diseases including Alzheimer's disease and Parkinson's disease. Treatment with anti-neuroinflammatory agents could provide therapeutic benefits for such disorders. Protosappanin A (PTA) is a major bioactive ingredient isolated from Caesalpinia sappan L.. In this work, the anti-neuroinflammatory effects of PTA on LPS-stimulated BV2 cells were investigated and the underlying mechanisms were explored. Results showed that PTA significantly inhibited the production of TNF-α and IL-1β in LPS-activated BV2 microglia. Moreover, the mRNA expressions of IL-6, IL-1β, and MCP-1 were reduced by PTA in a dose-dependent manner. Furthermore, PTA suppressed JAK2/STAT3-dependent inflammation pathway through down-regulating the phosphorylation of JAK2 and STAT3, as well as STAT3 nuclear translocation against LPS treatment. These observations suggested a novel role for PTA in regulating LPS-induced neuroinflammatory injuries.

Chemical constituents from ethyl acetate extract of Sappan Lignum / 中草药

Objective: To study the chemical constituents in Sappan Lignum (the core material of Caesalpinia sappan). Methods: The chemical constituents of Sappan Lignum were isolated by different column chromatographic techniques, including silica gel and Sephadex LH-20 columns. The structures of these compounds were identified by a comprehensive analysis on the spectroscopic data. Results: Fifteen compounds were isolated from the EtOAc extract of Sappan Lignum. The compounds were identified as protosappanin A (1), 3,7-dihydroxychroman-4-one (2), 7,3',4'-trihydroxy-3-benzyl-2H-chromene (3), bonducellin (4), 3'-deoxysappanol (5), 3'-deoxy-4-O-methylepisappanol (6), 3-deoxysappanchalcone (7), 3,8,9-thihydroxy-6H-benzo[c] chromen- 6-one (8), 3,9-dihydroxy-8-methoxydibenzo [b, d] pyran-6-one (9), (-)-syringaresinol (10), dibutyl phthalate (11), β-sitosterol (12), β-daucosterol (13), stigmasterol (14), and 1-heneicosanol (15). Conclusion: Compounds 9, 11, and 12 are first isolated from the plants of Caesalpinia Linn. and compound 4 is first isolated from this plant.