The air-dried aerial part of
Epilobium angustifolium
is a very popular recreational tea in the Eastern edge of Europe. Studies have found that the extract of
E. angustifolium
has strong ...anti-inflammatory effects, and the oenothein B contained therein is speculated the main anti-inflammatory component. In this study, a fraction without oenothein B from the ethanol extract of
E. angustifolium
exhibited a much stronger anti-inflammatory activity than that of the oenothein B. Guided by rapid characterization of the chemical compositions based on UPLC–Orbitrap–MS/MS, a total of 39 compounds, including 20 flavonoids and 19 other phenolic acids were identified in the active fraction, based on the accurate mass within 3 ppm error. Further investigation resulted in the isolation and identification of 10 compounds, one of which was a new compound, and four known compounds were identified in
E. angustifolium
for the first time. All isolated compounds exhibited significant inhibitory activity on nitric oxide (NO) production in lipopolysaccharide (LPS)-activated RAW 264.7 cells. This study indicated that the anti-inflammatory active ingredients in
E. angustifolium
were mainly concentrated in the 30% ethanol eluted fraction obtained over macroporous adsorption resin. In addition to the oenothein B, there are a large number of other more effective anti-inflammatory components in
E. angustifolium
.
Iron deficiency is a major global agricultural problem. Siderophores can help organisms to uptake iron in form of siderophore-Fe
3+
complexes and then in the cell cytosol, iron is reducted and ...released in ferrous form. This research aimed to obtain some efficient siderophore-producing bacterial strains and evaluate their plant growth-promoting effects in the iron-deficit environment. Two strains,
Brucella
sp. E7 and
Pseudomonas brassicae
W7, were isolated from rhizosphere soil. Both strains could produce maximum siderophores under the optimal conditions. Plant promoting experiment showed that many indicators of
Vigna radiata
seedling were all increased significantly by strain E7/W7 or the consortium of E7 + W7. Under no-iron and high iron stress, the inoculation treatment also showed growth promotion effects on both
Vigna radiata
and
Lolium multiflorum
. These results indicated that the potential ability of strain E7 and W7 in increasing agricultural production as a growth-promoting agent in iron-deficit soil.
The immunomodulatory and antioxidant activities of crude polysaccharides extracted from Gynostemma pentaphyllum Makino (GPMPP) were investigated. GPMPP was composed of rhamnose, arabinose, xylose, ...mannose, glucose and galactose in the molar ratio of 1.39:3.76:1.00:1.64:4.98:5.88. In vivo studies showed GPMPP significantly increased the spleen and thymus indices, activated the macrophage phagocytosis and NK cells, and exhibited activity on none or Con A/LPS-stimulated splenocytes in a dose-dependent manner in C57BL/6 mice. Moreover, GPMPP elevated CD4⁺ T lymphocyte counts as well as the CD4⁺/CD8⁺ ratio dose-dependently, and it increased IL-2 level in the sera and spleen of Cy-immunosuppressed mice. Furthermore, GPMPP significantly increased the SOD, GSH-Px, T-AOC, GSH and CAT level, and decreased the MDA level. The results showed that GPMPP might play an important role in prevention of oxidative damage in immunological system. These findings indicate GPMPP has immunomodulatory activity in vivo and seems to be an effective natural immunomodulatory agent.
is a kind of edible fungus widely grows in the north temperate zone, which shows various medicinal properties. Due to the complexity of chemical constitutes of this species, few investigations have ...acquired a comprehensive configuration for the chemical profile of it. In this study, a strategy based on ultra-high performance liquid chromatography (UPLC) combined with Orbitrap mass spectrometer (MS) was established for rapidly characterizing various chemical components in
. Through the summarized MS/MS fragmentation patterns of reference compounds and systematic identification strategy, a total of 110 components attributed to six categories were identified for the first time. Moreover, allergic rhinitis (AR) is a worldwide inflammatory disease seriously affecting human health, and the development of drugs to treat AR has been a topic of interest. It has been reported that the extracts of
showed obvious inhibitory effects on degranulation of mast cell- and allergen-induced IgE and proinflammatory mediators, but the active components and specific mechanism were still not clear. Src family kinases (SFKs) participate in the initial stage of allergy occurrence, which are considered the targets of AR treatment. Herein, on the basis of that self-built chemical database, virtual screening was applied to predict the potential SFKs inhibitors in
, using known crystal structures of Hck, Lyn, Fyn, and Syk as receptors, followed by the anti-inflammatory activity evaluation for screened hits by intracellular calcium mobilization assay. As results, sparoside A was directly confirmed to have strong anti-inflammatory activity with an IC
value of 5.06 ± 0.60 μM. This study provides a useful elucidation for the chemical composition of
, and demonstrated its potential inhibitory effects on AR, which could promote the research and development of effective agents from natural resources.
Endophytic fungi have been shown in recent years to produce a series of bioactive secondary metabolites. Several endophytic fungi were isolated from the fresh wild body of
Phellinus igniarius
, and ...initially evaluated for their antimicrobial activity. Among which, Shm-1 extract showed moderate inhibitory activity against
Clavibacter michiganense
and the fungus was identified to be
Alternaria alternata
Shm-1 through the comparison of morphological characteristics and the sequence of the rDNA ITS with those of other
Alternaria
species. A new 2
H
-benzindazole derivative, alterindazolin A (
1
), has been isolated from cultures of the endophyte
Alternaria alternata
Shm-1. Its structure was characterized as 1-benzyl-5-
p
-hydroxy-phenyloxygen-benz
e
indazole by spectroscopic data analysis including 1D NMR, 2D NMR and MS spectrum.
Toll-like receptors (TLRs) recognize microbial pathogens and trigger immune response, but their regulation by neuropeptide-vasoactive intestinal peptide (VIP) in weaned piglets infected by ...enterotoxigenic Escherichia coli (ETEC) K88 remains unexplored. Therefore, the study was conducted to investigate its role using a model of early weaned piglets infected by ETEC K88. Male Duroc × Landrace × Yorkshire piglets (n = 24) were randomly divided into control, ETEC K88, VIP, and ETEC K88+VIP groups. On the first three days, ETEC K88 and ETEC K88+VIP groups were orally administrated with ETEC K88, other two groups were given sterile medium. Then each piglet from VIP and ETEC K88+VIP group received 10 nmol VIP intraperitoneally (i.p.) once daily, on day four and six. On the seventh day, the piglets were sacrificed. The results indicated that administration of VIP improved the growth performance, reduced diarrhea incidence of ETEC K88 challenged pigs, and mitigated the histopathological changes of intestine. Serum levels of IL-2, IL-6, IL-12p40, IFN-γ and TNF-α in the ETEC K88+ VIP group were significantly reduced compared with those in the ETEC group. VIP significantly increased IL-4, IL-10, TGF-β and S-IgA production compared with the ETEC K88 group. Besides, VIP could inhibit the expression of TLR2, TLR4, MyD88, NF-κB p65 and the phosphorylation of IκB-α, p-ERK, p-JNK, and p-38 induced by ETEC K88. Moreover, VIP could upregulate the expression of occludin in the ileum mucosa compared with the ETEC K88 group. Colon and caecum content bacterial richness and diversity were lower for pigs in the ETEC group than the unchallenged groups. These results demonstrate that VIP is beneficial for the maturation of the intestinal mucosal immune system and elicited local immunomodulatory activities. The TLR2/4-MyD88 mediated NF-κB and MAPK signaling pathway may be critical to the mechanism underlying the modulatory effect of VIP on intestinal mucosal immune function and bacterial community.
, an important medicinal plant, is widely used as a traditional Chinese medicine and spice. Using cytotoxicity-guided fractionation, nine new lignans
⁻
and ten known analogues
⁻
were obtained from ...the EtOH extract of the twigs of
. Their structures were assigned by extensive 1D- and 2D-NMR experiments, and the absolute configurations were resolved by specific rotation and a combination of experimental and theoretically calculated electronic circular dichroism (ECD) spectra. In the cytotoxicity assay, 7',9-epoxylignans with feruloyl or cinnamoyl groups (compounds
⁻
,
and
) were selectively cytotoxic against NCI-H1650 cell line, while the dibenzylbutyrolactone lignans
⁻
exerted cytotoxicities against HCT-116 and A2780 cell lines. The results highlighted the structure-activity relationship importance of a feruloyl or a cinnamoyl moiety at C-9' or/and C-7 ketone in 7',9-epoxylignans. Furthermore, compound
was moderate active toward protein tyrosine phosphatase 1B (PTP1B) with an IC
value of 13.5 μM, and compounds
⁻
,
and
displayed inhibitory activity against LPS-induced NO production in RAW264.7 macrophages, with IC
values of 46.8, 50.1, 58.6, 47.5, and 66.5 μM, respectively.
Antimicrobial peptides represent an emerging category of therapeutic agents with remarkable structural and functional diversity. Modified vasoactive intestinal peptide (VIP) (VIP analogue 8 with ...amino acid sequence "FTANYTRLRRQLAVRRYLAAILGRR") without haemolytic activity and cytotoxicity displayed enhanced antimicrobial activities against
(
) ATCC 25923 and
(
) ATCC 25922 than parent VIP even in the presence of 180 mM NaCl or 50 mM MgCl₂, or in the range of pH 4-10. VIP analogue 8 was expressed as fusion protein thioredoxin (Trx)-VIP8 in
BL21(DE) at a yield of 45.67 mg/L. The minimum inhibitory concentration (MIC) of the recombinant VIP analogue 8 against
ATCC 25923 and
ATCC 25922 were 2 μM. These findings suggest that VIP analogue 8 is a promising candidate for application as a new and safe antimicrobial agent.
The main constituents of a typical medicinal herb, Polygonum multiflorum （Heshouwu in Chinese）, that induces idiosyncratic liver injury remain unclear. Our previous work has shown that cotreatment ...with a nontoxic dose of lipopolysaccharide （LPS） and therapeutic dose of Heshouwu can induce liver injury in rats, whereas the solo treatment cannot induce observable injury. In the present work, using the constituent ＂knock-out＂ and ＂knock-in＂ strategy, we found that the ethyl acetate （EA） extract of Heshouwu displayed comparable idiosyncratic hepatotoxicity to the whole extract in LPS-treated rats. Results indicated a significant elevation of plasma alanine aminotransferase, aspartate aminotransferase, and liver histologic changes, whereas other separated fractions failed to induce liver injury. The mixture of EA extract with other separated fractions induced comparable idiosyncratic hepatotoxicity to the whole extract in LPS-treated rats. Chemical analysis further revealed that 2,3,5,4＇-tetrahydroxy trans-stilbene-2-O-p-glucoside （trans-SG） and its cis-isomer were the two major compounds in EA extract. Furthermore, the isolated cis-, and not its trans-isomer, displayed comparable idiosyncratic hepatotoxicity to EA extract in LPS-treated rats. Higher contents of cis-SG were detected in Heshouwu liquor or preparations from actual liver intoxication patients associated with Heshouwu compared with general collected samples. In addition, plasma metabolomics analysis showed that cis-SG-disturbing enriched pathways remarkably differed from trans-SG ones in LPS-treated rats. All these results suggested that cis-SG was closely associated with the idiosyncratic hepatotoxicity of Heshouwu. Considering that the cis-trans isomerization oftrans- SG was mediated by ultraviolet light or sunlight, our findings serve as reference for controlling photoisomerization in drug discovery and for the clinical use of Heshouwu and stilbene-related medications.
(
) has a potential antihyperglycemic effect, but it is unclear what bioactive components play a key role. According to the
-glucosidase inhibition activity, three new taraxastane-type triterpenoids ...of 3
-hydroxy-30-hydroperoxy-20-taraxastene (
), 3
-hydroxy-22
-methoxy-20-taraxastene (
), and 30-nor-3
,22
-dihydroxy-20-taraxastene (
), as well as five known taraxastane triterpenoids of 3
,22-dihydroxy-20-taraxastene (
), 20-taraxastene-3,22-dione (
), 3
-acetoxy-20-taraxasten-22-one (
), 3
-hydroxy-20-taraxasten-22-one (
), and 30-nor-3
-hydroxy-20-taraxastene (
) were obtained from the petroleum ether-soluble portion of the ethanol extract from
. All chemical structures of the compounds were elucidated by spectroscopic data analysis and compared with literature data. Compounds
-
were identified for the first time from this plant, and compounds
,
,
and
exhibited more potent
-glucosidase inhibitory activity-with IC
values of 18.34 ± 1.27, 26.98 ± 0.89, 17.49 ± 1.42, and 22.67 ± 0.25 μM, respectively-than acarbose did (positive control, IC
42.52 ± 0.32 μM).
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