[Simultaneous determination of glucosinolates and flavonoids in leaves of Moringa oleifera by quantitative analysis of multi-components by single-marker (QAMS)].

To establish a method for simultaneously determining the content of four glucosinolates and five flavonoids in leaves of Moringa oleifera via quantitative analysis of multi-components by single-marker(QAMS) and verify the feasibility and applicability of the established method. The glucosinolates and flavonoids were analyzed via Waters Acquity UPLC HSS T_3 column(2.1 mm × 100 mm, 1.8 µm). The gradient elution was carried out with the mobile phase composed of 0.1% formic acid-acetonitrile and 0.3% formic acid at the flow rate of 0.4 mL·min~(-1) and the column temperature of 40 ℃. The wavelengths for the detection of glucosinolates and flavonoids were 225 nm and 260 nm, respectively. With 4-O-(α-L-rhamnoyloxy)-benzyl glucosinolate and vecenin-2 as internal reference substances, the relative correction factors of four glucosinolates and five flavonoids were respectively calculated for determining the content of the 9 ingredients in leaves of M. oleifera. To verify the accuracy and feasibility of QAMS, we used internal standard method(ISM) and external standard method(ESM) to determine the content of glucosinolates and flavonoids, respectively. The t-test results showed that there was no significant difference in the content of glucosinolates obtained by ISM and QAMS methods or in the content of flavonoids obtained by ESM and QAMS methods. The content of glucosinolates and flavonoids varied among M. oleifera of different varieties and from different producing areas. The total glucosinolates and total flavonoids had the highest content in the Indian variety while the lowest content in the variety ■Honghe No. 1'. The established QAMS method is rapid, simple and accurate and can be used for simultaneous determination of glucosinolates and flavonoids in the leaves of M. oleifera. This study provides experimental data for the quality control and utilization of M. oleifera leaves.

[Analysis of flavonoids from saffron floral bio-residues].

In order to better utilize saffron floral bio-residues(SFB), a qualitative and quantitative analysis of flavonoids in SFB was conducted using UPLC-MS and UPLC, respectively. On the one hand, 50 flavonols and 5 anthocyanins were putatively characte-rized by using UPLC-Q-TOF-MS. On the other hand, an UPLC method was established for determining the fingerprint of SFB as well as testing the main flavonoids kaempferol-3-O-sophoroside and delphinidin-3,5-di-O-glucoside. Contents of kaempferol-3-O-sophoroside and delphinidin-3,5-di-O-glucoside of 10 batches of samples were 44.21-58.73 mg·g~(-1) and 2.11-6.37 mg·g~(-1), respectively, and the similarities of 10 batches were more than 0.99. In addition, the color of the samples was digitized by using electronic eye technology, and it was found that the color of the samples was significantly correlated with the content of delphinidin-3,5-di-O-glucoside. The richness of flavonoids in SFB indicated its potential for development and utilization, and the large variation in anthocyanin content among samples from different regions suggested that more attention should be paid to the methods of sample pretreatment and storage.

Design, Synthesis, and Biological Activity of a Novel Series of 2-Ureidonicotinamide Derivatives Against Influenza A Virus.

BACKGROUND: Viral resistance to existing inhibitors and the time-dependent effectiveness of neuraminidase inhibitors have limited the number of antivirals that can be used for prophylaxis and therapeutic treatment of severe influenza infection. Thus, there is an urgent need to develop new drugs to prevent and treat influenza infection. OBJECTIVE: The aims of this study was to design and synthesize a novel series of 2-ureidonicotinamide derivatives and evaluate their anti-IAV activities. Furthermore, we predicted the abilities of these compounds to inhibit the PA-PB1 subunit and forecasted the docking poses of these compounds with RNA polymerase protein (PDB ID 3CM8). METHODS: The novel designed compounds were synthesized using classical methods of organic chemistry and tested in vitro for their abilities inhibiting RNP and against influenza A virus. In addition, the 23 synthesized molecules were subjected to the generated pharmacophore Hypo1 to forecast the activity target PA-PB1 subunit of RNA polymerase. The ADMET pharmacokinetic parameters were calculated by the ADMET modules in Discovery Studio 2016. The docking results helped us demonstrate the possible interactions between these compounds with 3CM8. RESULTS: The synthesized 2-ureidonicotinamide derivatives were characterized as potent anti-influenza inhibitors. The target compounds 7b and 7c demonstrated significant antiviral activities and could be considered as novel lead compounds of antiviral inhibitors. In addition, compound 7b revealed suitable ADME properties expressed and might be a significant RNA polymerase inhibitor targeting the PA-PB1 subunit based on the predictable results and the docking results. CONCLUSION: This study revealed a novel series of compounds that might be useful in the search for an effective drug against the influenza virus.