Bioactivity-Guided High Performance Counter-Current Chromatography and Following Semi-Preparative Liquid Chromatography Method for Rapid Isolation of Anti-Inflammatory Lignins from Dai Medicinal Plant, Zanthoxylum acanthopodium var. timbor.

The development of Dai medicine is relatively slow, and Zanthoxylum has great economic and medicinal value. It is still difficult to obtain medicinal components from the low-polarity parts of Zanthoxylum belonging to Dai medicine. In this study, we introduced one simple and quick strategy of separating target compounds from the barks of Z. acanthopodium var. timbor by high-performance countercurrent chromatography (HPCCC) with an off-line anti-inflammatory activity screening mode. The development of this strategy was based on the TLC-based generally useful estimation of solvent systems (GUESS) method and HPCCC in combination. This paper presented a rapid method for obtaining target anti-inflammatory compounds. Three lignins were enriched by HPCCC with an off-line inhibition mode of nitric oxide production in lipopolysaccharide-stimulated RAW264.7 macrophage cells, using petroleum ether-ethyl acetate-methanol-water (3:2:3:2) as the solvent system. The results showed that this method was simple and practical and could be applied to trace the anti-inflammatory components of the low-polarity part in Dai medicine.

Neuroprotective and Anti-Inflammatory Effects of Diphenylheptanes from the Fruits of Amomum tsaoko, a Chinese Spice.

Two novel diphenylheptanes, 2,3- dihydro-2 - (4' - hydroxy-phenylethyl) - 6 - [(3″,4″ - dihydroxy-5" - methoxy) phenyl] -4 - pyrone (CG-A) and 4 - dihydro-2 - (4' - hydroxy-phenylmethyl) -6 - [(3",4″ - dihydroxy-5″ - methoxyphenyl) methylene]-pyran-3, 5 - dione (CG-B), were isolated from the dried fruits of Amomum tsaoko, a commercially important spice. This study was designed to investigate their protective effects against H2O2-induced nerve injury, using PC-12 cells to determine the cell cytotoxicity and cell viability. The inhibitory effect on (nitric oxide) NO production was also determined in (lipopolysaccharide) LPS-stimulated macrophage RAW 264.7 cells. The results showed that CG-A and CG-B displayed significant neuroprotective effect and exhibited anti-inflammatory activity in a dose-dependent manner. These findings suggest that CG-A and CG-B are very important nutritional ingredients responsible for the neuroprotective and anti-inflammatory health benefits of A. tsaoko.

Optimization of astilbin extraction from the rhizome of Smilax glabra, and evaluation of its anti-inflammatory effect and probable underlying mechanism in lipopolysaccharide-induced RAW264.7 macrophages.

Astilbin, a dihydroflavonol derivative found in many food and medicine plants, exhibited multiple pharmacological functions. In the present study, the ethanol extraction of astilbin from the rhizome of smilax glabra Roxb was optimized by response surface methodology (RSM) using Box-Behnken design. Results indicated that the obtained experimental data was well fitted to a second-order polynomial equation by using multiple regression analysis, and the optimal extraction conditions were identified as an extraction time of 40 min, ethanol concentration of 60%, temperature of 73.63 °C, and liquid-solid ratio of 29.89 mL/g for the highest predicted yield of astilbin (15.05 mg/g), which was confirmed through validation experiments. In addition, the anti-inflammatory efficiency of astilbin was evaluated in lipopolysaccharide (LPS)-induced RAW 264.7 cells. Results showed that astilbin, at non-cytotoxicity concentrations, significantly suppressed the production of nitric oxide (NO) and tumor necrosis factor-α (TNF-α), as well as the mRNA expression of inducible nitric oxide synthase (iNOS) and TNF-α in LPS-induced RAW 264.7 cells, but did not affect interleukin-6 (IL-6) release or its mRNA expression. These effects may be related to its up-regulation of the phosphorylation of p65, extracellular signal-regulated kinases 1/2 (ERK1/2) and c-Jun N-terminal kinase (JNK).

Anti-inflammatory activity of extracts of Bushen-Qiangdu-Zhilv decoction, a Chinese medicinal formula, in M1-polarized RAW264.7.

BACKGROUND: Bushen-Qiangdu-Zhilv Decoction (BQZ) is one of famous traditional Chinese medical formula for treating ankylosing spondylitis (AS). However, the mechanisms underlying effects of BQZ remains unknown. Pro-inflammatory cytokines, tumor necrosis factor (TNF)-α and interleukin (IL)-1, play an important role in AS. We therefore evaluated if BQZ could affect the expression of these cytokines. METHODS: Crude extracts were prepared and fractioned with petroleum ether (PE), ethyl acetate (EA), n-butanol (BU) and finally water (ACE). The stability of the extracts was confirmed by high-pressure liquid chromatography (HPLC) analysis. M1-polarized RAW264.7 was induced and subsequently treated with BQZ extracts. Quantitative real-time PCR experiments were performed to measure mRNA expression of TNF-α and IL-1. RESULTS: It was found that TNF-α could be significantly suppressed by ACE extracts, whereas IL-1 was dramatically inhibited by BU extracts, which was further confirmed by dose-dependent experiments. Importantly, MTS assays showed that both ACE and BU extracts had a low cytotoxicity. CONCLUSION: Altogether, our study indicates that BQZ decoction exerts anti-AS effects via its anti-inflammatory activity and may have a low side-effect. Further analysis of the extracts of BQZ decoction could lead to a discovery of some novel drugs adding to therapeutic strategy for AS patients.

A flavonoid 8-C-glycoside and a triterpenoid cinnamate from Nervilia fordii.

One new flavonoid glycoside (1) and one new triterpenoid cinnamate (2) were isolated from Nervilia fordii. The structures of 1 and 2 were determined by extensive NMR and HRESIMS to be 7-O-ß-d-glucopyranosylapigenin-8-C-ß-d-glucopyranosyl-(1 â†’ 2)-ß-d-glucopyranoside and 24(S/ß)-dihydrocycloeucalenol-3-(Z)-p-hydroxycinnamate, respectively.

Evaluation of multi-activities of 14 edible species from Zingiberaceae.

Fourteen Zingiberaceae species, widely used in China for both food and medicine, were selected to evaluate and compare their antioxidant, antimicrobial and cytotoxic activities. Results indicated that seven species displayed high antioxidant activity, while eight species exhibited different degrees of antimicrobial activities (minimum inhibitory concentrations were 2.00-40.00 µg/ml), and six species exhibited cytotoxicity on the SMMC-7721 cells. Alpinia officinarum and Alpinia oxyphylla showed a broader antimicrobial spectrum, while Curcuma phaeocaulis and Zingiber officinale displayed specific inhibition on Escherichia coli. Amomum villosum showed strong radical scavenging capacity. Amomum kravanh and Curcuma longa exhibited significant cytotoxicity. Overall, the antioxidant, antimicrobial and cytotoxic activities of the 14 species showed obvious diversities. It is hoped that, from the results, the biological activity of ginger plants can be used more rationally and effectively in future.

Chemical compositions extracted from Wikstroemia indica and their multiple activities.

CONTEXT: The rhizome of Wikstroemia indica (L.) C. A. Mey (Thymelaeaceae) is widespread in China which has been widely used in China as folk medicine for the treatment of syphilis, arthritis, whooping cough, and cancer. Due to its multiactivities, its extract has an attractive potential as a promising natural agent in the pharmaceutical industries. OBJECTIVE: Aims of this study were to optimize the extraction process of the flavonoids from W. indica, and evaluate its multiple activities. MATERIALS AND METHODS: An orthogonal test design was employed to optimize the extraction procedure of flavonoids from W. indica. And multichromatography and spectroscopy were used to study the chemical compounds of W. indica, while several bioactivity assays were used to evaluate the antibacterial, anti-inflammatory, and antitumor activities of W. indica. RESULTS: Optimal extraction conditions were determined: ethanol concentration was 60%; extraction time was 60 min; liquid-solid ratio was 16:1 and the power of ultrasonic instrument was 160 W. Four compounds: daphnoretin, chrysophanol, myricitrime and rutin were purified from W. indica, and chrysophanol was identified from this plant for the first time. The extract of W. indica displayed significant antimicrobial and anti-inflammatory activities. Daphnoretin showed a significant inhibition effect on CNE cells and HeLa cells lines at the concentrations ranging from 15.6 to 125 µg/mL, the tendency of antitumor effect was displayed in a concentration-dependent manner. DISCUSSION AND CONCLUSIONS: Extracts of W. indica could potentially be used as a promising natural agent in the pharmaceutical industries.

Anti-hyperglycaemic effect of labdane diterpenes isolated from the rhizome of Amomum maximum Roxb., an edible plant in Southwest China.

Amomum maximum Roxb. rhizome is a fork medicine mainly used in South and Southeast Asia. In present study, the hypoglycaemic effects of the ethanolic extract of A. maximum rhizome were demonstrated both on α-glucosidase assay in vitro and streptozotocin (STZ)-induced postprandial hyperglycaemia in mice. Furthermore, six labdane diterpenes, amoxanthin A (1), ottensinin (2), coronarin D (3), coronarin D methyl ether (4), isocoronarin D (5), and zerumin (6), were isolated from its ethyl acetate sub-fraction with the guidance of α-glucosidase inhibitory activity. Among these compounds, 2 and 6 exhibited significant inhibitory effect on α-glucosidase, as well as on STZ-induced high postprandial blood glucose levels in mice. Additionally, molecular docking analysis revealed that 2 and 6 could firmly bind to the active sites of α-glucosidase. These results suggest that compounds 2 and 6 are the main anti-hyperglycaemic agents present in A. maximum, which may demonstrate potential beneficial effects in diabetes management.

Aspidopterys obcordata vine inulin fructan affects urolithiasis by modifying calcium oxalate crystallization.

Aspidopterys obcordata vine is a Chinese Dai ethnic herb used to treat urolithiasis. However, the material basis and underlying mechanisms remain undefined. In this study, a 2.3 kD inulin-like A. obcordata fructan (AOFOS) was isolated by size exclusion column chromatography and characterized by ultrahigh-performance liquid chromatography-ion trap-time of flight mass spectrometry (UPLC-IT-TOF-MS), nuclear magnetic resonance (NMR) spectroscopy, gas chromatography mass spectrometry (GC-MS) and high-performance gel permeation chromatography (HGPC). In addition, AOFOS showed unique anti-urolithiasis activity in Drosophila kidney stone models. Mechanism study indicated that AOFOS reduced the size of calcium oxalate crystals by inhibiting the formation of large size crystals and the generation rate of calcium oxalate crystals as well as the crystal form conversion from calcium oxalate monohydrate (COM) to calcium oxalate dihydrate (COD).

Proteomics and syndrome of Chinese medicine.

Syndrome of Chinese medicine is an understanding of the regularity of disease occurrence and development and its performance of symptoms. Syndrome is the key to recognize diseases and the foundation to treat them. However, because of the complexity of the concept and the limitation of present investigations, the research of syndrome is hard to go further. Proteomics has been received extensive attention in the area of medical diagnosis and drug development. In the holistic and systemic context, proteomics have a convergence with traditional Chinese medicine (TCM) syndrome, which could overcome the one-sidedness and singleness of TCM and avoid the complication and tedious processes. Chinese medicine has a wealth of experience and proteomics has a substantial research potential, the integration of the two aspects will bring a great enhancement of our knowledge of disease.