Eleutheroside K isolated from Acanthopanax henryi (Oliv.) Harms suppresses methicillin resistance of Staphylococcus aureus.

Acanthopanax (A.) henryi (Oliv.) Harms contain many bioactive compounds commonly used in traditional Chinese medicine. The objective of the present study was to investigate the antibacterial activity of the single constituent, Eleutheroside K (ETSK) isolated from the leaves of A. henryi (Oliv.) Harms, against methicillin-resistant Staphylococcus (S.) aureus (MRSA). Broth microdilution assay was used to measure the minimal inhibitory concentration (MIC) and the MIC values of ETSK against eight clinical S. aureus strains were all 50 µg ml-1 . At sub-inhibitory concentrations, a synergistic effect between oxacillin (OXA) and ETSK was confirmed using checkerboard dilution assay and time-kill curve analysis. The bacteriostatic effect became more pronounced when ETSK was used in combination with detergent (Triton X-100) or ATPase inhibitor (N, N'-dicyclohexylcarbodiimide). According to western blot analysis, the down-regulated expression of Penicillin-binding protein 2a (PBP2a) further validated that the bacterial activity was inhibited when treated with ETSK in a dose-dependent manner. Results based on our study verified that ETSK significantly suppressed MRSA infections and emphasized the potential application of ETSK as a novel anti-MRSA natural drug.

Chemical constituents from stems of Acanthopanax henryi / 中草药

Objective To study the chemical constituents from stems of Acanthopanax henryi based on LPS-induced macrophages RAW264.7 and microglia BV2 as the bioactivity guided model. Methods The compounds were isolated and purified by silica gel and Sephadex LH-20 column chromatography, as well as Prep-TLC and recrystallization methods. Their structures were identified on the basis of their physicochemical properties and spectroscopic data. Results Eighteen compounds were obtained from A. henryi and their chemical structures were identified as p-hydroxybenzoic acid (1), trans-p-hydroxycinnamic acid (2), (E)-caffeic acid methyl ester (3), caffeic acid (4), trans-coniferyl aldehyde (5), syringaldehyde (6), vanillin (7), 6-methoxy-7-hydroxycoumarin (8), trans-sinapaldehyde (9), undecane-1,11-dioic acid monomethyl ester (10), (-)-sesamin (11), 3-O-caffeoyl-quinic acid (12), 5-O-caffeoyl-quinic acid (13), 1,3-di-O-caffeoyl-quinic acid (14), 1,4-di-O-caffeoyl-quinic acid (15), 1,5-di-O-caffeoyl-quinic acid (16), stigmasterol (17), and β-sitosterol (18), respectively. Conclusion To the best of our knowledge, compound 10 was isolated from Araliaceae for the first time. Except compounds 12, 14, 17, and 18, all of other compounds were obtained from this species for the first time.

Purification of total flavonoids from leaves of Acanthopanax henryi / 中草药

Objective To optimize the purification technology of total flavonoids from the leaves of Acanthopanax henryi by macroporous resin. Methods Using the purity and yield of total flavonoids as indexes, the single factor experiment combined with response surface methodology (RSM) was used to optimize the purification technology. Results It showed that D101 macroporous resin had good adsorption and desorption effects. The optimal purification conditions were as follows: diameter height ratio was 1:10, the loading amount was 750 mg each 25 g D101 macroporous resin, the flow rate was 5 mL/min, and eluted by 130 mL 50% ethanol. Under the proposed conditions, the experimental purity of total flavonoids reached 75.87%, which was well matched with the predictive purity of 75.69%. And the yield of total flavone was 30.13%. Conclusion The results proved that D101 macroporous resin can purify the total flavonoids from the leaves of A. henryi and RSM could optimize the purification technology effectively.

Anti-adipogenic effect of Glycoside St-E2 and Glycoside St-C1 isolated from the leaves of Acanthopanax henryi (Oliv.) Harms in 3T3-L1 cells.

Acanthopanax henryi (Oliv.) Harms has been used in the treatment of arthritis, rheumatism, and abdominal pain. This study evaluated whether natural compounds isolated from the leaves of A. henryi (Oliv.) Harms could inhibit adipocyte differentiation by regulating transcriptional factors such as peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT/enhancer-binding protein α (C/EBPα). AMP-activated protein kinase (AMPK) activity was also evaluated. Among the several compounds isolated from the leaves of A. henryi (Oliv.) Harms, Glycoside St-C1 and Glycoside St-E2 significantly decreased lipid accumulation and the expressions of PPARγ and C/EBPα. Glycoside St-C1 and Glycoside St-E2 were found to activate AMPK when they regulated PPARγ and C/EBPα. Results confirmed that Glycoside St-C1 and Glycoside St-E2 isolated from the leaves of A. henryi (Oliv.) Harms can inhibit adipogenesis through the AMPK-PPARγ-C/EBPα mechanism. Thus, this study suggests that Glycoside St-C1 and Glycoside St-E2 have a therapeutic effect due to activation of the AMPKα.

Cytotoxicity and anti-inflammatory effects of root bark extracts of Acanthopanax henryi.

AIM: To investigate the cytotoxicity, anti-inflammatory activity, and action mechanism of root bark extracts of Acanthopanax henryi. METHOD: The hot methanol extract of the root bark of A. henryi was subjected to XAD-4 column chromatography eluting with a gradient of methanol in water. The cytotoxicity and anti-inflammatory effects of the MeOH fractions were evaluated on the inhibition on lipopolysaccharide (LPS)-induced nitric oxide, prostaglandin E2, interleukin-1ß, and interleukin-6 production in RAW 264.7 macrophages. RESULTS: The 80% MeOH fraction was a better inhibitor of LPS-induced NO, PGE2, IL-1ß, and IL-6 production, and expression of inducible nitric oxide synthase (iNOS) at the protein levels in a concentration-dependent manner. CONCLUSION: The 80% MeOH fraction of A. henryi root bark has significant anti-inflammatory activity. This provides a pharmacological basis for clinical application for the treatment of inflammation.

Cytotoxicity and anti-inflammatory effects of root bark extracts of Acanthopanax henryi / 中国天然药物

AIM@#To investigate the cytotoxicity, anti-inflammatory activity, and action mechanism of root bark extracts of Acanthopanax henryi.@*METHOD@#The hot methanol extract of the root bark of A. henryi was subjected to XAD-4 column chromatography eluting with a gradient of methanol in water. The cytotoxicity and anti-inflammatory effects of the MeOH fractions were evaluated on the inhibition on lipopolysaccharide (LPS)-induced nitric oxide, prostaglandin E2, interleukin-1β, and interleukin-6 production in RAW 264.7 macrophages.@*RESULTS@#The 80% MeOH fraction was a better inhibitor of LPS-induced NO, PGE2, IL-1β, and IL-6 production, and expression of inducible nitric oxide synthase (iNOS) at the protein levels in a concentration-dependent manner.@*CONCLUSION@#The 80% MeOH fraction of A. henryi root bark has significant anti-inflammatory activity. This provides a pharmacological basis for clinical application for the treatment of inflammation.