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Radix Ophiopogonis is often an integral part of many traditional Chinese formulas, such as Shenmai injection used to treat cardio-cerebrovascular diseases. This study aimed to investigate t...

The herb Radix Ophiopogonis (RO) has been used effectively to treat nasopharyngeal carcinoma (NPC) as an adjunctive therapy. Due to the complexity of the traditional Chinese herbs, the pharmacological mechanism of RO’s action on NPC remains unclear. To address this problem, an integrative approach bridging proteome experiments with bioinformatics prediction was employed. First, differentially expressed protein profile from NPC serum samples was established using isobaric tag for relative and absolute quantification (iTRAQ) coupled 2-D liquid chromatography (LC)-MS/MS analysis. Second, the RO putative targets were predicted using Traditional Chinese Medicines Integrated Database and known therapeutic targets of NPC were collected from Drugbank and OMIM databases. Then, a network between RO putative targets and NPC known therapeutic targets was constructed. Third, based on pathways enrichment analysis, an integrative network was constructed using DAVID and STRING database in order to identify potential candidate targets of RO against NPC. As a result, we identified 13 differentially expressed proteins from clinical experiments compared with the healthy control. And by bioinformatics investigation, 12 putative targets of RO were selected. Upon interactions between experimental and predicted candidate targets, we identified three key candidate targets of RO against NPC: VEGFA, TP53, and HSPA8, by calculating the nodes’ topological features. In conclusion, this integrative pharmacology-based analysis revealed the anti-NPC effects of RO might be related to its regulatory impact via the PI3K-AKT signaling pathway, the Wnt signaling pathway, and the cAMP signaling pathway by targeting VEGFA, TP53, and HSPA8. The findings of potential key targets may provide new clues for NPC’s treatments with the RO adjunctive therapy.

Off-line multi-hyphenated methods including affinity-ultrafiltration mass spectrometry, molecular docking, and reverse-phase high-performance liquid chromatography-fluorescence detection (RP-HPLC-FD) were used to rapidly screen and identify natural inducible nitric oxide synthase (iNOS) inhibitors isolated from Ophiopogon japonicus (Thunb.) Ker-Gawl. Ultrafiltration high-performance liquid chromatography quadrupole time-of-flight mass spectrometry was used to screen and identify the potential ligands with high binding affinity to iNOS. Seven compounds (three saponins and four flavonoids) were found in Radix Ophiopogonis. Molecular docking identified the binding sites and found that the binding affinity of the three ophiopogonis ligands was higher than that of the four homoisoflavonoids. Pre-column derivatization of l-citrulline and RP-HPLC-FD verified that the in vitro inhibition activity of the three ophiopogonis compounds was stronger than that of the four homoisoflavonoids, which was similar to the screened results. In conclusion, combining an in vitro iNOS inhibition assay and affinity-ultrafiltration mass spectrometry with molecular docking was a powerful tool for rapid screening and identification of iNOS inhibitors isolated from this traditional Chinese medicine.

This study aimed to develop a specific and reliable method to comprehensively analyze the chemical constituents in Shengmai injection (SMI) using high performance liquid chromatography coupled with tandem mass spectrometry. The qualitative analysis of SMI was achieved on a Kromasil 100-5C18 column, and the results demonstrated that a total of sixty-two compounds in SMI were unambiguously assigned or tentatively identified, and further, twenty-one compounds including fourteen saponins, six lignans and one L-borneol-7-O-[β-D-apiofuranosyl (1→6)]-β-D-gluco-pyranoside were quantified by HPLC-MS. Furthermore, L-borneol-7-O-[β-D-apio-furanosyl (1→6)]-β-D-glucopyranoside, originated from Radix ophiopogonis, was identified and quantified in SMI for the first time. The method validation results indicated that the methods were simple, specific and reliable. All the investigated compounds showed good linearity (r(2)≥0.9992) with a relatively wide concentration range and acceptable recovery at 90.13-109.09%. Consequently, the developed methods were successfully applied to ten batches of SMI samples analysis. The proposed methods may provide a useful and comprehensive reference for the quality control of SMI, and thus to provide supporting data for the quality control and application of SMI clinically.

This work aimed to achieve long-lasting delivery of radix ophiopogonis polysaccharide (ROP) by sucrose acetate isobutyrate (SAIB)-based in situ forming systems (ISFSs) alone or combined with mono-PEGylation of ROP. When the ‘90%SAIB/10% solvent’ system was used, the mean residence time (MRT) of ROP was prolonged by 4.3 5 ∼ 7.00 times and the initial release rate was reduced significantly. However, this system was only suitable for days-long sustained release of ROP in short-term therapy. As to the ‘SAIB/additives/solvent’ system containing mono-PEGylated ROP, the results indicated that SAIB/poly(d,l-lactide-co-glycolide) (PLGA)/N-methyl-2-pyrrolidone (NMP) was superior to SAIB/polylactic acid (PLA)/NMP and SAIB/PLA/ethanol in controlled release. Moreover, weeks- to months-long (16–60 d) smooth release of ROP could be achieved by varying the concentration (10–30%) and molecular weight (MW) of PLGA (10–50 kDa) or by employing a moderate MW of PEGylated ROP (∼20 or ∼30 kDa). With further increasing the conjugate MW to ∼40 kDa, the contribution of drug elimination to its plasma retention seemed to surpass that of the SAIB-based system, resulting in that the system no longer had an obvious influence on the in vivo behavior of the conjugate. Besides, the results of host response confirmed that with less solvent being used, the SAIB-based systems showed a higher biocompatibility than the PLGA-based systems, suggesting that they could be freely chosen in the prevention and/or cure of chronic diseases.

Environmentally friendly natural dye-sensitized solar cells based on TiO2 nanorod arrays are sensitized using extracts of Radix Ophiopogonis fruits and Chinese purple yams as natural sensitizers. Compared with conventional natural dye-sensitized solar cells based on nanoporous TiO2 anodes, improved short-circuit photocurrent densities are recorded (from 3.5 mA/cm 2 to 5 mA/cm 2 and from 2.7 mA/cm 2 to 5.2 mA/cm 2 respectively) for solar cells using the TiO2 nanorod arrays. The best power conversion efficiencies obtained are 1.2% and 1.15% for solar cells sensitized by extracts of Radix Ophiopogonis fruits and Chinese purple yams, indicating increases of 155% and 91% compared with those based on nanoporous TiO2 films. These results indicate that the combination of TiO2 nanorod arrays and natural dyes may provide an efficient and stable structure for natural dye-sensitized solar cell applications.

We studied the action of the herb, Ophiopogon root (OR) in a epithelial injury model, hypothesizing that it may have beneficial effects on mucociliary transport following injury to the palate induced by sodium metabisulphite (MB) which releases SO(2) on contact with water. OR (extract from 1g of root/ml)-incubated palates and non-incubated palates were compared to assess the effect of MB on mucociliary clearance on the bull frog palate. MB 10(-1) M, acutely increased mucociliary clearance time (MCT) by 254.5 +/- 57.3% in untreated and 243.3 +/- 98.5% in OR-incubated palates, (over all significance assessed by one-way ANOVA, F = 12.82, p < 0.001, df = 8,54 for MB and F = 10.56, p < 0.001, df = 8,54 for OR). MCT returned to normal during recovery in OR-treated palates following MB. In untreated palates, MCT did not return to control values during a similar recovery period. ANOVA comparing MCTs in the recovery period in untreated vs OR-treated palates was significantly different (F = 2.92, p < 0.03, df = 5,36). SEM images of epithelial tissue, analyzed by morphometry, showed a 25 +/- 12% loss of ciliated cells in untreated palates and little or no damage to cilia in OR-treated palates. Intact groups of ciliated cells were found in SEM micrographs of mucus from MB-treated palates. We conclude that the loss of cilia or ciliated cells prevented full recovery of MCT after MB in untreated palates. In OR-incubated palates, mucociliary transport was completely restored within 20 min after topical application of MB, possibly through a protective action on the extra-cellular matrix.

A two-year survey on the residues of heavy metals in four Chinese crude drugs and their cultivated soils was conducted. Targeted heavy metals were copper (Cu), arsenic (As), lead (Pb), nickel (Ni), and cadmium (Cd). Herbs surveyed include White Peony Root (Radix Paeoniae Alba), Turmeric Root Tuber (Radix Curcumae), Thunberg Fritillary Bulb (Bulbus Fritillariae Thumbergii), and Tuber of Dwarf Lilyturf (Radix Ophiopogonis). Concentrations of all heavy metals were under the permitted levels except cadmium, which exceeded the permitted level in some samples of Thunberg Fritillary Bulb, White Peony Root, and Turmeric Root Tuber. Concentration coefficients were less than 1.0 for all heavy metals except cadmium. The concentration coefficient of cadmium in Turmeric Root Tuber was 14.0. Lower pH and high Zn concentration in the soil may facilitate the transfer of cadmium from cultivated soil into the herbs.

Sheng-Mai-San (SMS), a traditional Chinese formulation used for the treatment of coronary heart disease, is comprised of Radix Ginseng, Fructus Schisandrae and Radix Ophiopogonis. Pretreatment with a lignan-enriched SMS (17 g/kg/day × 3, p.o.) was found effective in protection against isoproterenol-induced myocardial injury in rats, and in ischemia-reperfusion injury in isolated perfused hearts prepared from pretreated animals. Results obtained from pretreatment studies using extracts prepared by mixing various combinations of the three component herbs indicate that the major myocardial protective component in SMS is the lignan-enriched extract of Fructus Schisandrae.

Background. Clinical trials reveal that multiherb prescriptions of herbal medicine often exhibit pharmacological and therapeutic superiority in comparison to isolated single constituents. However, the synergistic mechanisms underlying this remain elusive. To address this question, a novel systems biology model integrating oral bioavailability and drug-likeness screening, target identification, and network pharmacology method has been constructed and applied to four clinically widely used herbs Radix Astragali Mongolici, Radix Puerariae Lobatae, Radix Ophiopogonis Japonici, and Radix Salviae Miltiorrhiza which exert synergistic effects of combined treatment of cardiovascular disease (CVD).Results. The results show that the structural properties of molecules in four herbs have substantial differences, and each herb can interact with significant target proteins related to CVD. Moreover, the bioactive ingredients from different herbs potentially act on the same molecular target (multiple-drug-one-target) and/or the functionally diverse targets but with potentially clinically relevant associations (multiple-drug-multiple-target-one-disease). From a molecular/systematic level, this explains why the herbs within a concoction could mutually enhance pharmacological synergy on a disease.Conclusions. The present work provides a new strategy not only for the understanding of pharmacological synergy in herbal medicine, but also for the rational discovery of potent drug/herb combinations that are individually subtherapeutic.

Without references the exact assignment of the various TLC- and HPLC-zones and peaks respectively is difficult. The TLC and HPLC together yield very characteristic fingerprints which differ only quantitatively in their zones- or peak-pattern.

OBJECTIVE To study the effects of soil factors on the active components in Radix Ophiopogonis. METHOD The content of polysaccharide, flavonoids, saponins, water-soluble extract and inorganic elements in Radix Ophiopogonis gathered from 7 different places were compared, physical and chemical properties and inorganic elements of soil were analyzed. The path and grey connection analysis were applied for studying the effects on the active components of Radix Ophiopogonis. RESULT AND CONCLUSION The concentrations of mineral elements in plant were mainly adjusted by active absorption. The active components in Radix Ophiopogonis was primarily effected by soil enzyme activity, the other important factors were potassium, pH, and organic matter. K, Fe, Mn, B, Ba, Zn of soil also had much influence on it then others inorganic elements.

Fungal invasion is a main factor leading to the loss of postharvest herbs during storage. To prevent fungal invasion and clarify the favorable conditions for the stability of herbs during the storage period, uniform design and three-dimensional response surfaces were applied to investigate the relationship of the mildew degree of Radix Ophiopogonis induced by prevalent fungal isolates and the storage factors including air relative humidity (X(1)), temperature (X(2)), and moisture content (X(3)), in laboratory studies. Mildew degree was evaluated by ergosterol assay of mold isolates through a high-performance liquid chromatography-diode array detector (HPLC-DAD) technique. As a result, storage conditions, which satisfied the following correlation equations established by the relationships between the storage factors and the biomass of mildew (Y), could effectively prevent fungal spoilage: Y = -0.2484084028 + 0.00030711966572 x X(3) x X(3) + 0.00018881361186 x X(1) x X(2) - 0.00029473040679 x X(2) x X(3)or= 0; Y = -0.2697457586 + 0.004127756022 x X(1) - 0.000015977780492 x X(1) x X(1) + 0.00021906984606 x X(2) x X(3)or= 0; Y = -0.325655811 + 0.015464432582 x X(2) + 0.00004779394354 x X(1) x X(1) - 0.00021743815482 x X(2) x X(2)or= 0. This compositive methodology might be useful to predict the occurrence of fungal invasion.

The effects of eight herbs of Guchi Gao on periodontal tissue cells were investigated. The results show that Herba Dendrobii, Radix Ophiopogonis, and two other herbs can significantly promote attachment of human gingival fibroblasts (HGF) and periodontal ligament cells (PDL) and enhance the proliferation of the latter. This may account for the effect of Guchi Gao and suggests a potential treatment for periodontitis in the future.