Mitochondrial-Respiration-Improving Effects of Three Different Gardeniae Fructus Preparations and Their Components.

The processing method for Chinese traditional herbal medicine is "Pao Zhi" in Chinese. This study examined the efficacy of the Pao Zhi on the preparations of Gardeniae Fructus (GF) on a mitochondrial respiratory function in rats. To determine the efficacy of Pao Zhi, we investigated the effects of GF heat processing on mitochondrial respiratory function. To test the GF components, the rats were randomly divided into a geniposide-alone group, crocin-alone group, and combination groups and treated with geniposide and crocin at different ratios. The results showed that a high dose, raw GF was more effective in improving the neurological function, mitochondrial respiratory function, and activities of Na+-K+-ATPase and Ca2+-Mg2+-ATPase than the preparations that underwent heating. Moreover, mitochondrial ROS production was the lowest in the raw GF-treated group. In addition, treatments with crocin and GC3 were more effective than geniposide in improving the functional deficit in MCAO rats. In conclusion, our results suggest that raw GF is the most suitable preparation for the treatment of cerebral ischemia, and its underlying mechanisms may be associated with the improvement of mitochondrial respiratory function, increased activities of Na+-K+-ATPase and Ca2+-Mg2+-ATPase, and reduced oxidative stress in mitochondria. Our findings suggest that raw GF, especially crocin, could be an ideal therapeutic agent for ischemic stroke.

Treatment Mechanism of Gardeniae Fructus and Its Carbonized Product Against Ethanol-Induced Gastric Lesions in Rats.

Gardeniae Fructus (GF) and carbonized GF (GFC) have been shown to exert a gastrointestinal protective effect and are frequently used in clinical practice for the treatment of hemorrhage and brown stool. In this study, we employed a combination of pharmacological methods and metabolomics in a rat model of ethanol-induced acute stomach ulcer to investigate the gastroprotective effect of GF and GFC water extracts and the potential mechanism involved in this process. The levels of nitric oxide (NO) and interleukin 6 (IL-6) in the plasma of rats were determined. The results showed that both GF and GFC reduced the ethanol-induced gastric lesions and expression of NO and IL-6 in these rats. Of note, 16 and 11 feature metabolites were filtered and identified in the GF and GFC groups, respectively. Both GF and GFC act by restoring the biosynthesis of valine, leucine, and isoleucine, and the metabolism of glycerophospholipids. Moreover, histological evaluation revealed that heat processing of GF to create GFC enhanced the gastric mucosa protective effect. Furthermore, heat processing converted the main pathway from alanine, aspartate, and glutamate metabolism, associated with GF, to histidine metabolism, associated with GFC. GF and GFC ameliorated gastric mucosa lesions in rats via reductions in NO production and inflammatory cytokine secretion, and the induction of prostaglandin E2.

The Potential Antipyretic Mechanism of Gardeniae Fructus and Its Heat-Processed Products With Plasma Metabolomics Using Rats With Yeast-Induced Fever.

Gardeniae Fructus (GF), prepared GF (GFP), and carbonized GF (GFC) are widely used in China for the treatment of fever. However, the involved antipyretic mechanism has not been fully elucidated. In this study, rectal temperature and pyrogenic cytokines were used to evaluate the antipyretic effect of raw and processed GF in rats with dry-yeast-induced pyrexia. Reverse phase and hydrophilic interaction liquid chromatography and ultra-high-performance liquid chromatography/mass spectrometry were used to acquire the metabolomics profile of GF, GFP, and GFC in rats with pyrexia. The results showed that the rectal temperature of rats treated with GF, GFP, and GFC was suppressed after 6 h (P < 0.05), compared with that observed in pyrexia model rats. The enzyme-linked immunosorbent assay showed that the expression of tumor necrosis factor α and interleukin 6 were suppressed by GF, GFP, and GFC. Moreover, GFC suppressed the expression of interleukin 6 significantly (P < 0.01). Of note, 11, 15, and 25 feature metabolites were identified in the GF, GFP, and GFC groups. Pathway analysis showed that GF mainly regulated the biosynthesis of valine, leucine, and isoleucine. Notably, GFP was involved in glycerophospholipid metabolism, while GFC was linked to glycerophospholipid and sphingolipid metabolism. These results suggested that GF, GFP, and GFC maintained their antipyretic effect despite heat processing. However, heat processing altered endogenous feature metabolites and certain pathways of GF, GFP, and GFC in rats with yeast-induced pyrexia to exert an antipyretic effect.

[UPLC-Q-TOF/MS for rapid analysis of chemical constituents in Sanhuang tablets].

The qualitative analysis method of ultra performance liquid chromatography tandem quadrupole time of flight mass spectrometry (UPLC-Q-TOF-MS/MS) was established for the chemical constituents in Sanhuang tablets. Waters ACQUITY BEH C18 (2.1 mm×100 mm, 1.7 µm) column was used with 0.1% formic acid solution (A)-0.1% formic acid acetonitrile (B) as the mobile phase for gradient elution. The flow rate was 0.2 mL•min⁻¹; the sample volume was 1 µL and the column temperature was 30 ℃. The high-resolution quadrupole time-flight mass spectrometry was used as detector with electrospray ion source in both positive and negative models, and the dry gas temperature was 325 ℃. Based on the analysis of mass spectrometry and literature reports, 38 compounds were confirmed, including 1 alkaloid, 1 dianthrone compound, 6 tannins, 7 anthraquinone glycosides, 6 anthraquinones and 17 flavonoids. Liquid chromatography-mass spectrometry method is simple, reliable and rapid to identify the chemical compositions of Sanhuang tablets, and it is helpful to reveal its chemical constituents and pharmacodynamic substances.