ABSTRACT
OBJECTIVE: To screen for influenza virus neuraminidase inhibition and to provide a reference for the clinical treatment of influenza using traditional Chinese medicines (TCM). In this study, 421 crude extracts (solubilized with petroleum ether, ethanol, ethyl acetate, and aqueous solvents) were obtained from 113 TCM. The medicine extracts were then reacted with oseltamivir, using 2'-(4-methylumbelliferyl)-α-D-N-acetylneuraminic acid (MUNANA) as the substrate, to determine influenza virus neuraminidase activity using a standard fluorimetric assay. It was found that Chinese medicine extracts from Pyrola calliantha, Cynanchum wilfordii, Balanophora involucrata and Paeonia delavayi significantly inhibited neuraminidase activity at a concentration of 40 µg/mL. Dose-dependent inhibitory assays also revealed significant inhibition. The IC50 range of the TCM extracts for influenza virus neuraminidase was approximately 12.66-34.85 µg/mL, respectively. Some Chinese medicines have clear anti-influenza viral effects that may play an important role in the treatment of influenza through the inhibition of viral neuraminidase. The results of this study demonstrated that plant medicines can serve as a useful source of neuraminidase (NA) inhibitors and further investigation into the pharmacologic activities of these extracts is warranted.
Subject(s)
Drugs, Chinese Herbal/chemistry , Enzyme Inhibitors/chemistry , Neuraminidase/antagonists & inhibitors , Viral Proteins/antagonists & inhibitors , Drugs, Chinese Herbal/therapeutic use , Enzyme Inhibitors/therapeutic use , Humans , Influenza, Human/drug therapy , Medicine, Chinese TraditionalABSTRACT
Paeonia delavayi, an endemic species in southwestern China, has been widely used as a traditional remedy for cardiovascular, extravasated blood, stagnated blood and female diseases in traditional Chinese medicine (TCM). However, there are no reports on the anti-influenza virus activity of this species. Here, the anti-influenza virus activity of P. delavayi root extracts was first evaluated by an influenza virus neuraminidase (NA) inhibition assay. Meantime, constituents in the active extracts were identified using ultra-high performance liquid coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) and seven major identified constituents were used to further evaluate the NA inhibitory activity. The results showed that the ethyl acetate fraction (EA) and the ethanol fraction (E) of P. delavayi both presented strong NA inhibitory activity with IC50 values of 75.932 µg/mL and 83.550 µg/mL, respectively. Twenty-seven constituents were characterized in these two active extracts by UPLC-Q-TOF-MS analysis, and seven major identified constituents exhibited high activity against the influenza virus. Among them, Benzoylpaeoniflorin (IC50 = 143.701 µM) and pentagalloylglucose (IC50 = 62.671 µM) exhibited the highest activity against the influenza virus, even far stronger than oseltamivir acid (IC50 = 281.308 µM). This study indicated that P. delavayi was a strong NA inhibitor, but cell-based inhibition, anti-influenza virus activity in vivo and anti-influenza virus mechanism still need to be tested and explored.
Subject(s)
Antiviral Agents , Drugs, Chinese Herbal , Enzyme Inhibitors , Influenza A virus/enzymology , Neuraminidase/antagonists & inhibitors , Paeonia/chemistry , Viral Proteins/antagonists & inhibitors , Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Drugs, Chinese Herbal/chemistry , Drugs, Chinese Herbal/pharmacology , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Female , Humans , Male , Neuraminidase/chemistry , Viral Proteins/chemistryABSTRACT
Objective: To compare the contents of iridoid glycosides in Qingyedan medicinal materials,and to provide the scientific basis for using resources of Qingyedan and rationality of original plant medicinal. Methods: The contens of three iridoid glycosides,including swertiamarin,gentiopicroside and sweroside in Qingyedan medicinal materials were determined by HPLC. Results: The constituents of 30 samples in nine species were significant difference. And the contents of iridoid glycosides in Swertia bimaculata,Swertia tenuis and Swertia pubescens were reported for the first time. Conclusion: The results show that the contents of iridoid glycosides in Qingyedan medicinal materials have a significant difference due to the different species and producing areas. Therefore, these medicinal plants should not be used as alternative medicines for clinical application. Swertiamarin and sweroside can be selected as quality control components, this method is an effective method to identify and control the quality of Qingyedan materials.