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A new nitrogen-containing iridoid glycoside, named (7 R,3���R)-lonijapospiroside A (1), together with thirteen known iridoid glycosides, were isolated from the flower buds of Lonicera macranthoides. The structures of these compounds were established on the basis of spectroscopic analyses. Among them, compounds 1-4 are four diastereoisomers, and their absolute configurations were accurately established by the NOE spectra as well as comparison of their experimental and calculated ECD spectra. The anti-inflammatory activities of all isolates were evaluated by measuring their inhibitory effects on NO, IL-6, and TNF-�� production in LPS stimulated RAW 264.7 macrophages. Compound 14 exhibited anti-inflammatory activities by inhibiting IL-6 with an IC50 value of 54.70 ��M, comparable to that of the positive control (hydrocortisone, IC50: 62.6 �� 1.7 ��M).

Cimicifuga dahurica (Turcz.) Maxim, which is also regarded as the main origin of "shengma" in Chinese Pharmacopoeia, has been used as cooling and detoxification agents for thousands of years. Our previous phytochemical investigations of C. dahurica extracts (CDEs) led to the isolation of a series of 9, 19-cycloalkane triterpenoids and phenolic acids showing a potential anti-inflammatory activity. However, the chemical profiling of CDEs and the material basis of its anti-inflammatory effect in vivo has not been clarified. In the present study, the CDEs chemical profile and prototype components in rat plasma were identified via ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q/TOF-MS). As a result, a total of 106 components were identified or tentatively characterized in CDEs, including 54 triterpenoids, 35 phenolic acids, eight amides and nine other type constituents (39 compounds were confirmed with the reference standards). And 20 prototype components (15 triterpenoids and five phenolic acids) were identified in rat plasma, which potentially related to the anti-inflammatory effects of CDEs. Moreover, the anti-inflammatory activities of the main prototype components were further evaluated by their inhibitory effects on the production of NO, as well as the expressions of iNOS and COX-2 in lipopolysaccharide (LPS)-stimulated RAW264.7 cells, which indicated that 9, 19-cycloalkane triterpenoids may play an anti-inflammatory role by down-regulating the expression of iNOS.

Jin-hong tablets (JHT), a well-known Traditional Chinese Patent Medicine (TCPM), has been effectively used for the treatment of chronic superficial gastritis (CSG) in clinic. The metabolic profile of TCPMs is the key part of discovering their bioactive components. In this study, a five-step strategy based on ultra-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry (UPLC-Q/TOF-MS) and metabolynxTM software combined with mass defect filter (MDF) technique was developed to delineate the metabolic profile of JHT in vivo. As a result, a total of 163 JHT-related xenobiotics (38 prototypes and 125 metabolites) were identified or tentatively characterized in rat biological samples, and the phase I and II metabolism process mainly included demethylation, hydroxylation, sulfation and glucuronidation. In addition, after oral administration of JHT, a large amount of alkaloids-related ingredients were detected in rat plasma samples, indicating that alkaloids may play an important role in the treatment of CSG with JHT. This study is beneficial for understanding of JHT's in vivo metabolic profiles and characteristics, which helps to reveal its in vivo effective components and provides a solid basis for further studies on its functional mechanism.

Two new iridoid glycosides, 2'

Chronic superficial gastritis (CSG) is a common disease of the digestive system that possesses a serious pathogenesis. Jinhong tablet (JHT), a traditional Chinese medicine (TCM) prescription, exerts therapeutic effects against CSG. However, the molecular basis of its therapeutic effect has not been clarified. Herein, we employed UPLC-Q/TOF-MS-based chemical profile identification to determine the chemical components in JHT. Further, we applied network pharmacology to illustrate its molecular mechanisms. A total of 96 chemical constituents were identified in JHT, 31 of which were confirmed using reference standards. Based on the bioinformatics analysis performed using the symptom-guided pharmacological networks of “chi,” “blood,” “pain,” and “inflammation,” and a target screening based on the interaction probabilities between compounds and targets, MMP2, DRD2, and AKR1B1 were identified as key targets in the therapeutic effect exhibited by JHT against CSG. Moreover, according to the inhibitory activities presented in the literature and binding mode analysis, the structural types of alkaloids, flavonoids, organic acids, including chlorogenic acid (10), caffeic acid (13), (-)-corydalmine (33), (-)-isocorypalmine (36), isochlorogenic acid C (38), isochlorogenic acid A (41), quercetin-3-O-α-L-rhamnoside (42), isochlorogenic acid B (47), quercetin (63), and kaempferol (70) tended to show remarkable activities against CSG. Owing to the above findings, we systematically identified the chemical components of JHT and revealed its molecular mechanisms based on the symptoms associated with CSG.

A new nitrogen-containing iridoid glycoside, named (7

Ten cycloart-7-ene triterpenoid glycosides, including three new compounds (

Two new iridoid glycosides, 2′-O-cis-coumaroylgardoside (1), and 6′-O-caffeoylioxide (2), were isolated from the fruit of Gardenia jasminoides. The structures of these compounds were elucidated based on spectroscopic analysis (HR-ESI-MS, NMR) and chemical methods. The anti-inflammatory activities of the isolates were evaluated by measuring their inhibitory effects on PGE2 production in LPS stimulated RAW 264.7 macrophages, compounds 1 and 2 could reduce PGE2 levels in LPS-activated RAW 264.7 macrophages with IC50 values of 121.4 and 83.38 μM, respectively.

Ten cycloart-7-ene triterpenoid glycosides, including three new compounds (1–3), were isolated from the roots of Cimicifuga dahurica. Their structures were elucidated on the basis of extensive spectroscopic analyses, chemical methods and comparison with literatures. In addition, the isolates were evaluated for their inhibitory effects on the production of NO, as well as the expressions of iNOS and COX-2 in LPS-stimulated RAW 264.7 macrophages. The results showed that compounds 3, 5, 6, 7 and 8 can reduce the release of NO in a dose-dependent manner. Mechanistically, Western blot analysis indicated that the NO inhibitory effects relied on down-regulating the expression of iNOS, and partially associated with lowering the expression of COX-2.