ABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: Fufang Qiling granules (FQG), derived from the traditional Qiling Decoction with a longstanding clinical history, is utilized for the treatment of hyperuricemia (HUA). FQG is formulated with a combination of seven Chinese herbs based on the principles of traditional Chinese medicine (TCM) theories. Clinical evidence indicates that FQG exhibits favorable therapeutic effects in reducing uric acid (UA) levels and attenuating renal damage. AIM OF THIS STUDY: To elucidate the potential active components and pharmacological mechanism of FQG in the treatment of HUA, and to provide an experimental basis for the development of efficient and low-toxicity TCM for HUA treatment. MATERIALS AND METHODS: A HUA rat model induced by potassium oxonate and adenine was established to initially evaluate the hypouricemic effects of FQG. Chemical analyses were conducted using an ultra-high-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS). Network pharmacology was used to investigate the active components and mechanism of FQG in the treatment of HUA. Potential Xanthine oxidase (XOD) inhibitors were screened from FQG based on ultrafiltration liquid chromatography and mass spectrometry (UF-LC-MS). Molecular docking, surface plasmon resonance (SPR) and circular dichroism (CD) spectroscopy were applied to validate the interactions between the active components and XOD. RESULTS: In comparison to the model group, treatment with FQG significantly decreased serum UA, serum creatinine (CREA), serum blood urea nitrogen (BUN), and liver XOD activity. Additionally, the FQG administration notably ameliorated HUA-induced renal injury in rats. Through the pharmacodynamics of the HUA rat models and network pharmacology, it was found that XOD was a key pathway enzyme in UA metabolism. 18 XOD inhibitors were screened from FQG by UF-LC-MS, and 11 compounds with strong affinity were verified by SPR, molecular docking and CD spectroscopy. CONCLUSION: In summary, flavonoids, organic acids and saponins may be the active components in FQG that alleviate HUA. The primary mechanism of FQG involves inhibiting XOD enzyme activity in the plasma to reduce UA production, alleviating renal tubular epithelial cell necrosis, tubulointerstitial injury, fibrosis, and urate deposition, ultimately exerting a therapeutic effect on HUA.
ABSTRACT
Ginseng is a well-known herbal medicine that has been gaining increasingly popularity as a potential chemopreventive agent. In traditional Chinese medicine practice, white ginseng (WG), red ginseng (RG), and dali ginseng (DG) are 3 different ginseng-processed products used for different purposes. Although the morphological appearance and some constituents contained in these ginseng products are similar, their pharmacological activities are significantly different due to the varied types and quantity of ginsenosides in each product. In the present study, a practical method based on rapid liquid chromatography coupled with quadrupole time of flight mass spectrometry (LC-Q-TOF/MS) was developed to identify the chemical profiles of ginsenosides in these 3 ginseng products. The results demonstrated that a total of 55, 53, and 43 compounds were unambiguously assigned or tentatively identified in DG, WG, and RG samples, respectively. The featured compounds are mainly malonyl ginsenosides in WG, and decarboxyl products of mal-ginsenosides and the dehydrated compounds from polar ginsenosides were characteristic in RG, while DG contain some characteristic components present both in WG and RG. We presume that heating processing is the major factor affecting the chemical profile of ginseng products. The difference of chemical information revealed by LC-Q-TOF/MS could be used to discriminate the WG, RG, and DG samples.
