a Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine , Wrocław University of Environmental and Life Sciences , Wrocław , Poland.
b Department of Bioorganic Chemistry, Faculty of Chemistry , Wrocław University of Technology , Wrocław , Poland.
Immunopharmacol Immunotoxicol. 2019 Apr;41(2):231-241. doi: 10.1080/08923973.2019.1578972. Epub 2019 May 6.
Leaf extracts of plants of the genus have traditionally been used as diuretic, anti-rheumatic and diaphoretic preparations. One of the main active ingredients of bark is betulin, lupane-type triterpene alcohol, with multiple biological activities. The aim of this study was to investigate and immunomodulatory effects of a newly synthesized ester of betulin: 28--phosphatidylbetulin [28--(1,2-diacyl--glycero-3-phospho)-betulin, DAPB] in comparison with betulin in mice. Cytotoxic activity of DAPB or betulin was tested against non-cancer (D10.G4.1 and J774E.1) and cancer (GL-1; CL-1 and Jurkat) cell lines. The part assessed total lymphocyte count, weight ratio and subsets of lymphocytes in the lymphatic organs, and humoral immune response to sheep erythrocytes (SRBC). assay showed that DAPB, contrary to betulin, had no antiproliferative activity. Exposure to four doses of DAPB increased the absolute count of immature CD4CD8 thymic cells as well as the percentage and absolute count of mature CD4 and CD8 thymocytes. DAPB enhanced the percentage or absolute count of CD3 cells in spleen and lymph nodes with corresponding decrease in the percentage and/or absolute count of CD19 cells. Both DAPB and betulin enhanced the percentage and absolute count of CD8 lymphocytes in lymph nodes. In SRBC-immunized mice, betulin contrary to DAPB enhanced the number of splenocytes producing anti-SRBC antibodies (PFC). Both DAPB and betulin increased the level of total (IgM + IgG) and IgG titers. Despite the lack of cytotoxic activity, DAPB shows valuable immunomodulatory properties.
植物属的叶提取物传统上被用作利尿剂、抗风湿和发汗剂。树皮的一种主要活性成分是白桦脂醇，一种具有多种生物活性的羽扇烷型三萜醇。本研究旨在研究一种新合成的白桦脂醇酯：28--磷酸酯桦木醇[28--（1,2-二酰基-甘油-3-磷酸）桦木醇，DAPB]与白桦脂醇在小鼠体内的免疫调节作用。用 DAPB 或白桦脂醇对非癌细胞（D10.G4.1 和 J774E.1）和癌细胞（GL-1；CL-1 和 Jurkat）细胞系进行细胞毒性试验。采用体内法评估总淋巴细胞计数、淋巴器官重量比和淋巴细胞亚群以及对绵羊红细胞（SRBC）的体液免疫反应。结果表明，DAPB 与白桦脂醇相反，没有抗增殖活性。暴露于四种剂量的 DAPB 增加了不成熟 CD4CD8 胸腺细胞的绝对计数以及成熟 CD4 和 CD8 胸腺细胞的百分比和绝对计数。DAPB 增强了脾和淋巴结中 CD3 细胞的百分比或绝对计数，同时降低了 CD19 细胞的百分比和/或绝对计数。DAPB 和白桦脂醇均增强了淋巴结中 CD8 淋巴细胞的百分比和绝对计数。在 SRBC 免疫的小鼠中，与 DAPB 相反，白桦脂醇增强了产生抗 SRBC 抗体的脾细胞数量（PFC）。DAPB 和白桦脂醇均增加了总（IgM+IgG）和 IgG 滴度。尽管缺乏细胞毒性活性，DAPB 仍显示出有价值的免疫调节特性。
