Abstract：
BACKGROUND: Ficus erecta, a traditional Chinese She Ethnomedicine, has been historically utilized to treat various inflammatory conditions such as arthritis, nephritis, and osteoporosis. However, the underlying mechanisms accounting for its anti-inflammatory activity, as well as its active components, largely remain elusive.
OBJECTIVE: The purpose of this research was to investigate the chemical constituents of F. erecta that contribute to its anti-inflammatory effects.
METHODS: Coumarins and flavones were obtained from the 95% EtOH extract of F. erecta using virous column chromatography and reversed-phase semipreparative HPLC. The structures of the new compounds were elucidated by extensive analysis of spectroscopic methods, including HRESIMS, 1D and 2D NMR spectra, and CD experiments. Cultured macrophage RAW264.7 cells were utilized for the anti-inflammatory experiments. MTT cell viability assay, Griess reagent method, ELISA, and Western blot experiments were employed to evaluate the anti-inflammatory activity and investigate the related mechanism.
RESULTS: Four new (1-4) and eleven previously identified (5-16) coumarins, together with one new (17) and six known flavones (18-23) were isolated from the whole plant of F. erecta. Compounds 7 and 17 significantly reduced nitric oxide (NO) and prostaglandin E2 (PGE2) production without cytotoxic effects. Furthermore, compounds 7 and 17 reduced the production of proinflammatory cytokines including tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6 in a concentration-dependent manner. Western blot analysis indicated that compounds 7 and 17 suppressed the expression of iNOS, COX-2, and p-IκBα in LPS-stimulated RAW264.7 macrophage cells.
CONCLUSIONS: The current phytochemical investigations revealed that coumarins and flavones represent the primary chemical constituents of F. erecta. Compounds 7 and 17 exhibit potent anti-inflammatory properties, linked with the inhibition of NF-κB activation by preventing the degradation of IκBα phosphorylation. These compounds may serve as promising candidates for treating or preventing certain inflammatory diseases.
OBJECTIVE: The purpose of this research was to investigate the chemical constituents of F. erecta that contribute to its anti-inflammatory effects.
METHODS: Coumarins and flavones were obtained from the 95% EtOH extract of F. erecta using virous column chromatography and reversed-phase semipreparative HPLC. The structures of the new compounds were elucidated by extensive analysis of spectroscopic methods, including HRESIMS, 1D and 2D NMR spectra, and CD experiments. Cultured macrophage RAW264.7 cells were utilized for the anti-inflammatory experiments. MTT cell viability assay, Griess reagent method, ELISA, and Western blot experiments were employed to evaluate the anti-inflammatory activity and investigate the related mechanism.
RESULTS: Four new (1-4) and eleven previously identified (5-16) coumarins, together with one new (17) and six known flavones (18-23) were isolated from the whole plant of F. erecta. Compounds 7 and 17 significantly reduced nitric oxide (NO) and prostaglandin E2 (PGE2) production without cytotoxic effects. Furthermore, compounds 7 and 17 reduced the production of proinflammatory cytokines including tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6 in a concentration-dependent manner. Western blot analysis indicated that compounds 7 and 17 suppressed the expression of iNOS, COX-2, and p-IκBα in LPS-stimulated RAW264.7 macrophage cells.
CONCLUSIONS: The current phytochemical investigations revealed that coumarins and flavones represent the primary chemical constituents of F. erecta. Compounds 7 and 17 exhibit potent anti-inflammatory properties, linked with the inhibition of NF-κB activation by preventing the degradation of IκBα phosphorylation. These compounds may serve as promising candidates for treating or preventing certain inflammatory diseases.
摘要：
背景：无花果，中国传统的她民族医学，历史上一直被用来治疗各种炎症，如关节炎，肾炎,和骨质疏松症。然而,解释其抗炎活性的潜在机制，以及它的活性成分，在很大程度上仍然难以捉摸。
目的：本研究的目的是研究有助于其抗炎作用的F.
方法：香豆素和黄酮是用活柱色谱和反相半制备型高效液相色谱法从直角杆菌的95％EtOH提取物中获得的。通过广泛的光谱分析方法阐明了新化合物的结构，包括HRESIMS,1D和2DNMR光谱，CD实验将培养的巨噬细胞RAW264.7细胞用于抗炎实验。MTT细胞活力测定，Griess试剂法,ELISA,采用Westernblot实验评价其抗炎活性并探讨其作用机制。
结果：四种新的（1-4）和十一种先前鉴定的（5-16）香豆素，与一个新的（17）和六个已知的黄酮（18-23）一起从整个植物中分离。化合物7和17显著减少一氧化氮(NO)和前列腺素E2(PGE2)的产生而没有细胞毒性作用。此外，化合物7和17减少了包括肿瘤坏死因子（TNF）-α在内的促炎细胞因子的产生，白细胞介素（IL）-1β，和IL-6呈浓度依赖性。Westernblot分析表明,化合物7和17抑制iNOS的表达,LPS刺激的RAW264.7巨噬细胞中的COX-2和p-IκBα。
结论：当前的植物化学研究表明，香豆素和黄酮代表了直角酵母的主要化学成分。化合物7和17表现出有效的抗炎特性，与通过防止IκBα磷酸化降解来抑制NF-κB激活有关。这些化合物可用作治疗或预防某些炎性疾病的有希望的候选物。
目的：本研究的目的是研究有助于其抗炎作用的F.
方法：香豆素和黄酮是用活柱色谱和反相半制备型高效液相色谱法从直角杆菌的95％EtOH提取物中获得的。通过广泛的光谱分析方法阐明了新化合物的结构，包括HRESIMS,1D和2DNMR光谱，CD实验将培养的巨噬细胞RAW264.7细胞用于抗炎实验。MTT细胞活力测定，Griess试剂法,ELISA,采用Westernblot实验评价其抗炎活性并探讨其作用机制。
结果：四种新的（1-4）和十一种先前鉴定的（5-16）香豆素，与一个新的（17）和六个已知的黄酮（18-23）一起从整个植物中分离。化合物7和17显著减少一氧化氮(NO)和前列腺素E2(PGE2)的产生而没有细胞毒性作用。此外，化合物7和17减少了包括肿瘤坏死因子（TNF）-α在内的促炎细胞因子的产生，白细胞介素（IL）-1β，和IL-6呈浓度依赖性。Westernblot分析表明,化合物7和17抑制iNOS的表达,LPS刺激的RAW264.7巨噬细胞中的COX-2和p-IκBα。
结论：当前的植物化学研究表明，香豆素和黄酮代表了直角酵母的主要化学成分。化合物7和17表现出有效的抗炎特性，与通过防止IκBα磷酸化降解来抑制NF-κB激活有关。这些化合物可用作治疗或预防某些炎性疾病的有希望的候选物。
