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As one of the major active components of Qizhiweitong (QZWT) prescription, corydalis alkaloid (CA) has been reported to have noticeable effect of anti-inflammation in pharmacological studies. However, the anti-inflammatory function and potential mechanism of CA in anti-inflammation remain to be clarified. Hence, the aim of this study was to investigate the anti-inflammation efficacy and potential mechanism of CA in anti-inflammation by metabonomic approach coupled with related gene analyzes in vivo and in vitro. Mice acute inflammation was induced by subcutaneous injection of formalin in hind paws, and evaluated the anti-inflammatory effect of CA via detecting the index of paw edema. The results indicated that CA has an anti-inflammatory effect on mice through alleviating the paw edema significantly. Moreover, metabolic profiling was performed by high performance liquid chromatography quadrupole-time-of-flight mass spectrometer (HPLC-QTOF-MS) combined with multivariate data analysis, such as principal component analysis (PCA) and partial least-squares discriminant analysis (PLS-DA). Thirteen metabolic targets (including lysophosphatidylcholine (LysoPC), choline, arachidonic acid, phosphodimethylethanolamine) and related pathways of the cholinergic anti-inflammatory and arachidonic acid (AA) metabolism were identified, Meanwhile, the relevant target genes, like iNOS, NF-κB, TNF-α, were detected and verified in vitro. The results indicated that CA has a good pharmacological effect of anti-inflammation through regulating multiple disordered targets and metabolic networks, which provides a theoretical basis for further research on CA. Furthermore, there is a great potential for the development of CA to be a new anti-inflammatory drug with high effective activities, little side effects and weak drug resistance.

Inflammation is an important immune response; however, excessive inflammation causes severe tissue damages and secondary inflammatory injuries. The long-term and ongoing uses of routinely used drugs such as non-steroidal anti-inflammatory drugs (NSAIDS) are associated with serious adverse reactions, and not all patients have a well response to them. Consequently, therapeutic products with more safer and less adverse reaction are constantly being sought. Radix Bupleuri, a well-known traditional Chinese medicine (TCM), has been reported to have anti-inflammatory effects. However, saikosaponins (SS) as the main pharmacodynamic active ingredient, their pharmacological effects and action mechanism in anti-inflammation have not been reported frequently. This study aimed to explore the anti-inflammatory activity of SS and clarify the potential mechanism in acute inflammatory mice induced by subcutaneous injection of formalin in hind paws. Paw edema was detected as an index to evaluate the anti-inflammatory efficacy of SS. Then, a metabolomic method was used to investigate the changed metabolites and potential mechanism of SS. Metabolite profiling was performed by high-performance liquid chromatography combined with quadrupole time-of-flight mass spectrometry (HPLC-Q-TOF-MS). The detection and identification of the changed metabolites were systematically analyzed by multivariate data and pathway analysis. As a result, 12 different potential biomarkers associated with SS in anti-inflammation were identified, including nicotinate, niacinamide, arachidonic acid (AA), and 20-carboxy-leukotriene B4, which are associated with nicotinate and nicotinamide metabolism and arachidonic acid metabolism. The expression levels of biomarkers were effectively modulated towards the normal range by SS. It indicated that SS show their effective anti-inflammatory effects through regulating nicotinate and nicotinamide metabolism and arachidonic acid metabolism.

One new and three known steroidal glycosides were isolated from the ethyl acetate extract of the roots of Cynanchum wallichii Wight. Their structures were characterized as qinyangshengenin-3-O-α-Lcymaropyranosyl-(1→4)-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-β-Ddigitoxopyranoside (1), otophylloside A (2), otophylloside B (3), and cynanauriculoside A (4).

A new alkaloid, speradine B (1), together with griseofulvin (2), epigriseofulvin (3), and isogriseofulvin (4), was purified from the extracts of Penicillium dipodomyicola isolated from Clerodendrum inerme, a tree from the intertidal zone of Nanhai. Their structures were elucidated on basis of extensive spectroscopic analysis.

Four steroids were isolated from the ethyl acetate extract of the roots of Cynanchum otophyllum. Their structures were identified as qinyangshengenin-3-O-β-D-oleandropyranosyl-(1→4)-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-β-D-cymaropyranoside (1), gagamine (2), otophylloside B (3), and caudatin (4). Compound 1 is a new steroidal glycoside, and the structures of these compounds were established on the basis of chemical and spectroscopic methods.