Four ursane type triterpenes have been isolated from the methanolic extract of the aerial parts of Agrimonia pilosa Ledeb. (Rosaceae) through repeated silica gel and reverse-phase C-18 column chromatography. Their chemical structures were elucidated as ursolic acid (1), pomolic acid (2), tormentic acid (3), and corosolic acid (4) on the basis of their MS, , and spectral data. Compounds 2 and 4 were isolated from the genes of Agrimonia for the first time.
Patridoids I, II and IIA, are new iridoids isolated from the whole plants of Patrinia saniculaefolia. These compounds were examined by assessing their effects on the production of tumor necrosis factor-α (TNF-α) as well as by investigating the expression of two enzymes, inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), in the lipopolysaccharide (LPS)-stimulated murine macrophage-like cell line, Raw 264.7. Among them, patridoid II consistently inhibited nitric oxide (NO) and TNF-α production in a dose-dependent manner, with IC50 values of 14.1 and 17.6 μM, respectively. Western Blotting probed with specific anti-iNOS antibodies showed that the decrease in the quantity of the NO product was accompanied by a decrease in the iNOS protein level. However, all three patridoids did not affect the COX-2 protein expression level in the LPS-stimulated macrophages. In addition, the C-5 isomer of patridoid II, patridoid I, only slightly affected the production of NO. Moreover, the C-3 isomer of patridoid II, patridoid IIA, did not inhibit proinflammatory cytokines and NO production. These results suggest that the orientations of the C-3 and C-5 methoxy groups in the patridoids have a significant role in the expression of their biological activity.
The genus Epilobium consists of approximately 200 species that are distributed worldwide. Some of these herbs have been used for the treatment of diarrhea, infection, irritation, and other disorders associated with inflammation. Unlike that of other Epilobium species, there is little scientific understanding of the pharmacological effect of Epilobium amurense subsp. cephalostigma (Hausskn.) C. J. Chen, Hoch & P. H. Raven. In this study, we demonstrated the anti-inflammatory and antioxidative properties of an E. amurense 95% ethanol extract (EACEE) in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages, and observed the underlying mechanism of this effect. We measured the productions of nitric oxide (NO) and reactive oxygen species, and examined the actions of EACEE on transcription factors in the macrophages. EACEE reduced NO production and inducible nitric oxide synthase protein levels via the inhibition of the nuclear factor (NF)-κB pathway. Additionally, EACEE suppressed redundant reactive oxygen species production and regulated nuclear factor erythroid 2-related factor 2/heme oxygenase-1 (Nrf2/HO-1) signaling. Furthermore, EACEE significantly inhibited the phosphorylation of p38 mitogen-activated protein kinase (MAPK). Overall, these results indicate that EACEE exerts anti-inflammatory and antioxidant effects via the activation of Nrf2/HO-1 and inhibition of NF-κB/p38 MAPK signaling.
Cortex Moutan (the dried root bark of Paeonia Suffruticosa Andrew, CM) extracts have shown potent tumor inhibitory activity, suggesting CM might be a good source of tumor inhibitors. The aim of the study was to identify compounds in CM extracts with tumor inhibitory activities and evaluate their effect on different tumor cells as well as elucidating the underlying mechanisms of inhibition. A total of twenty-four compounds were identified in CM, including eleven mono-phenols (1–11), seven terpenoids (12–18), three flavonoids (19–21), two sterols (22 and 23) and one coumarin (24). After administration, both CM extracts and compounds can inhibit tumor cell growth. The most potent tumor inhibitor was identified as kalopanaxsaponin A (compound 16). Kalopanaxsaponin A increased the apoptosis of tumor cells by inhibiting the expression of MMP-2 and HIF-1α. Therefore, CM might be used as novel tumor inhibitor in functional foods or other dietary products.
Two flavonoids, 4,2′,5′-trihydroxy-4′-methoxychalcone (1) and (2S)-6,7,4′-trihydroxyflavan (2), along with fourteen known flavonoids and two other known arylbenzofurans were isolated from the heartwood of Dalbergia odorifera. The structure of compounds 1 and 2 were established by spectroscopic (NMR and MS) analyses. Of the isolates, eight compounds (1, 4, 7, 10, 12, 14, 15, 17) were found to have potent protective effect on glutamate-induced oxidative injury in HT22 cells.
Nardostachin, which is an iridoid isolated from Patrinia saniculaefolia, was examined by assessing its effect on the production of tumor necrosis factor-α (TNF-α) and expression of 2 enzymes, inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), in lipopolysaccharide (LPS)-stimulated Raw264.7 macrophages. This compound consistently inhibited the production of nitric oxide (NO) and TNF-α production in a dose-dependent manner, with respective IC50 values of 12.3 and 16.2 μM. The decrease in quantity of NO products was accompanied by a decrease in the iNOS protein level, as assessed by Western blotting probed with specific anti-iNOS antibodies. In addition, this compound also reduced the COX-2 protein expression level and the attendant PGE2 production in LPS-stimulated macrophages. These results suggest that nardostachin may be useful for inhibiting the production of inflammatory mediators such as TNF-α, NO and PGE2 in inflammatory diseases.