Multi-level chemical characterization and anti-inflammatory activity evaluation of the polysaccharides from Prunella vulgaris.

Prunella vulgaris (PV) is a medicine and food homologous plant, but its quality evaluation seldom relies on the polysaccharides (PVPs). In this work, we established the multi-level fingerprinting and in vitro anti-inflammatory evaluation approaches to characterize and compare the polysaccharides of P. vulgaris collected from the major production regions in China. PVPs prepared from 22 batches of samples gave the content variation of 5.76-24.524 mg/g, but displayed high similarity in the molecular weight distribution. Hydrolyzed oligosaccharides with degrees of polymerization 2-14 were characterized with different numbers of pentose and hexose by HILIC-MS. The tested 22 batches of oligosaccharides exhibited visible differences in peak abundance, which failed to corelate to their production regions. All the PVPs contained Gal, Xyl, and Ara, as the main monosaccharides. Eleven batches among the tested PVPs showed the significant inhibitory effects on NO production on LPS-induced RAW264.7 cells at 10 µg/mL, but the exerted efficacy did not exhibit correlation with the production regions. Conclusively, we, for the first time, investigated the chemical features of PVPs at three levels, and assessed the chemical and anti-inflammatory variations among the different regions of P. vulgaris samples.

Characterization and comparison of cardiomyocyte protection activities of non-starch polysaccharides from six ginseng root herbal medicines.

Ginseng is rich of polysaccharides, however, the evidence supporting polysaccharides to distinguish various ginseng species is rarely reported. Focusing on six root ginseng (e.g., Panax ginseng-PG, P. quinquefolius-PQ, P. notoginseng-PN, red ginseng-RG, P. japonicus-PJ, and P. japonicus var. major-PJM), the contained non-starch polysaccharides (NPs) were structurally characterized and compared by both the chemical and biological evaluation. Holistic fingerprinting at three levels (the NPs and the acid hydrolysates involving oligosaccharides and monosaccharides) utilized various chromatography methods, and the treatment of H9c2 cells with the NPs by OGD and H2O2-induced injury models was used to assess the protective effect. NPs from six Panax herbal medicines occupied about 20 % of the total polysaccharides, which were of the highest content in RG and the lowest in PN. NPs from six ginseng exhibited weak differentiations in the molecular weight distribution, while marker oligosaccharides were found to distinguish PN and RG from the others. Glc and GalA were more abundant in the NPs for PG and RG, respectively. NPs from PQ (100/200 µg/mL) showed significant cardiomyocyte protection effect by regulating the mitochondrial functions. This work further testifies the role of polysaccharides in quality control of herbal medicine, with new markers discovered beneficial to distinguish the ginseng.

Aptamer-conjugated and doxorubicin-loaded grapefruit-derived nanovectors for targeted therapy against HER2+ breast cancer.

Increased human epidermal growth factor receptor 2 (HER2) expression is a hallmark of HER2+ breast cancer. HER2 promotes the growth of cancer cells and makes them particularly aggressive. Currently, trastuzumab is the only HER2-targeted therapeutic agent approved by the FDA for HER2-overexpressing breast cancer treatment. However, clinical efficacy of trastuzumab is limited greatly by the occurrence of drug resistance. In this study, an aptamer (HA1) specific for HER2-overexpressing breast cancer cells was selected using Cell-SELEX. This allowed the development of grapefruit-derived nanovectors (GNVs) conjugated with HA1 that targeted specifically HER2+ breast cancer cells. In vitro experiments demonstrated that HA1 effectively promoted the internalisation of GNVs into cancer cells and tumour spheroids. In vivo data showed that drug delivery to tumour tissues and antitumor activities were dramatically enhanced by conjugating HA1 with drug-loaded GNVs. This study indicates that aptamers mediating targeted drug delivery by GNVs represent a promising strategy for HER2+ breast cancer therapy.

Comparative evaluation of cultivars of Chrysanthemum morifolium flowers by HPLC-DAD-ESI/MS analysis and antiallergic assay.

A multicomponent quantification fingerprint based on HPLC coupled with diode array detection and electrospray ionization tandem mass spectrometry (HPLC-DAD-ESI/MS) technique has been established for the analysis of phenolic compounds in 12 samples originated from 5 different cultivars of Chrysanthemum morifolium flowers in China. Four caffeoylquinic acids and 15 flavonoids in the capitulum were identified by comparing the retention times and ultraviolet spectra as well as the mass spectrum and/or matching the empirical molecular formula with that of reference compounds, and the contents of these compounds have been determined simultaneously. The samples from three medicinal cultivars significantly differed in the quality and quantity of flavonoid aglycones and glycosides compared with those from two edible cultivars, which allows the possibility of showing the chemical distinctness of these cultivars and may be useful in their standardization. Moreover, the antiallergic effects of these cultivars were comparatively assayed for the first time. A representative medicinal cultivar, 'huaiju', showed potential activity on the inhibition of antigen-induced degranulation from RBL-2H3 cells and compound 48/80-induced scratching in mice, whereas the in vitro and in vivo antiallergic activities of two edible cultivars were weak. The results suggested that the quality and quantity of some active flavonoid aglycones should be responsible for the pharmacological profiles of these cultivars.