Anti-inflammatory and antitumour activity of various extracts and compounds from the fruits of Piper longum L.
Anti-inflammatory and antitumour activity of various extracts and compounds from the fruits of Piper longum L.
复制标题
荜茇果实的各种提取物和化合物的抗炎和抗肿瘤活性。
DOI：
10.1111/jphp.13099
复制
发表时间：
2019-07-01
影响因子：
3.3
通讯作者：
Yu, Jianqing
中科院分区：
文献类型：
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作者：
Guo, Ziyan;Xu, Jie;Yu, Jianqing
目的 为探索有效的提取方法，寻找有效成分，对荜荇果实中3种提取物的生物活性进行考察，并分离出活性成分。方法分别采用回流提取、超声提取和超临界流体提取，获得3种荜荇果实提取物。通过生物测定引导的方法分离活性化合物。评估抗炎活性、抗增殖活性和细胞毒性。采用Hoechst 33258染色法检测细胞凋亡。通过蛋白质印迹分析研究相关蛋白质。主要发现 超临界流体提取物（SE）的抗炎活性和细胞毒性比其他两种提取物更强。在所有分离的化合物中，8个化合物的抗炎活性强于吲哚美辛，其中化合物8、9、11、14和15为首次发现具有抗炎作用。化合物1、2、3和14对癌细胞表现出显着的细胞毒性。 SE 和胡椒碱被发现通过增加裂解的 PARP 和 Bax/Bcl-2 的比率来减少集落形成、抑制细胞迁移并促进细胞凋亡。结论 SE的抗炎、抗肿瘤作用优于其他两种提取物。阐明了负责该活性的化合物。 SE 和胡椒碱通过细胞凋亡抑制细胞生长。
Objectives To explore effective extraction method and to find active constituents, we investigated the biological activity of three extracts and isolated active compounds from the fruits of Piper longum L. Methods Three extracts from the fruits were obtained by reflux, ultrasonic and supercritical fluid extraction, respectively. Active compounds were isolated by the bioassay-guided method. The anti-inflammatory activity, antiproliferation activity and cytotoxicity were evaluated. The apoptosis was detected by Hoechst 33258 staining assay. The relevant proteins were investigated by Western blot assay. Key findings The anti-inflammatory activity and cytotoxicity of supercritical fluid extract (SE) were stronger than those of the other two extracts. Among all isolated compounds, the anti-inflammatory activity of eight compounds was stronger than that of indomethacin, and compounds 8, 9, 11, 14 and 15 were found to possess anti-inflammatory effect for the first time. Compounds 1, 2, 3 and 14 exhibited significant cytotoxicity against cancer cells. SE and piperine were found to reduce colony formation, inhibit cell migration and promote apoptosis through increasing cleaved PARP and the ratio of Bax/Bcl-2. Conclusions The anti-inflammatory and antitumour effects of SE were better than those of the other two extracts. The compounds responsible for the activity were elucidated. SE and piperine inhibit cell growth through apoptosis.