Jantan Ibrahim, Ilangkovan Menaga, Husain Khairana, Chan Kok Meng
Drug and Herbal Research Center, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, Kuala Lumpur, Malaysia; Falkultas Farmasi, Universitas Sumatera Utara, USU-Kampus, Medan, Indonesia.
Drug and Herbal Research Center, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, Kuala Lumpur, Malaysia.
Drug Des Devel Ther. 2016 Jun 9;10:1935-45. doi: 10.2147/DDDT.S105651. eCollection 2016.
Standardized extract of Phyllanthus amarus has previously been shown to have a strong inhibitory effect on phagocytic activity of human neutrophils. The current study was carried out to evaluate the effects of constituents of the extract of P. amarus on nitric oxide (NO) production as well as lymphocyte proliferation and cytokine release from phagocytes. Three compounds, ethyl 8-hydroxy-8-methyl-tridecanoate, 7β,19α dihydroxy-urs-12-ene, and 1,7,8-trihydroxy-2-naphtaldehyde, together with seven known compounds were isolated from the whole plant of P. amarus. The isolated compounds and reference standards, ie, gallic acid, ellagic acid, corilagin, and geraniin, which were quantitatively analyzed in the extracts, were evaluated for their effects on immune cells. Among the compounds tested, the lignans, especially phyltetralin and phyllanthin, showed strong inhibition on lymphocyte proliferation with half maximal inhibitory concentration (IC50) values of 1.07 μM and 1.82 μM, respectively. Ethyl 8-hydroxy-8-methyl-tridecanoate and 1,7,8-trihydroxy-2-naphtaldehyde exhibited strong inhibition on nitric oxide production with IC50 values of 0.91 μM and 1.07 μM, respectively. Of all the compounds, corilagin was the strongest inhibitor of tumor necrosis factor-α release with an IC50 value of 7.39 μM, whereas geraniin depicted the strongest inhibitory activity on interleukin-1β release with an IC50 value of 16.41 μM. The compounds constituting the extract of P. amarus were able to inhibit the innate immune response of phagocytes at different steps.
此前已证明，苦味叶下珠的标准化提取物对人类中性粒细胞的吞噬活性具有强烈抑制作用。本研究旨在评估苦味叶下珠提取物的成分对一氧化氮（NO）生成、淋巴细胞增殖以及吞噬细胞释放细胞因子的影响。从苦味叶下珠全株中分离出三种化合物，即8-羟基-8-甲基十三烷酸乙酯、7β,19α-二羟基乌苏-12-烯和1,7,8-三羟基-2-萘甲醛，以及七种已知化合物。对提取物中进行定量分析的分离化合物和参考标准品（即没食子酸、鞣花酸、柯里拉京和老鹳草素）的免疫细胞作用进行了评估。在所测试的化合物中，木脂素，尤其是叶下珠素和叶下珠脂素，对淋巴细胞增殖表现出强烈抑制作用，半数最大抑制浓度（IC50）值分别为1.07 μM和1.82 μM。8-羟基-8-甲基十三烷酸乙酯和1,7,8-三羟基-2-萘甲醛对一氧化氮生成表现出强烈抑制作用，IC50值分别为0.91 μM和1.07 μM。在所有化合物中，柯里拉京是肿瘤坏死因子-α释放的最强抑制剂，IC50值为7.39 μM，而老鹳草素对白细胞介素-1β释放表现出最强抑制活性，IC50值为16.41 μM。构成苦味叶下珠提取物的化合物能够在不同步骤抑制吞噬细胞的固有免疫反应。
