[Effects of Huangqin Tang on NLRP3/Caspase-1 pathway in mice model of ulcerative colitis].

The aim of this study was to explore the effects of Huangqin Tang(HQT) on the NLRP3/Caspase-1 signaling pathway in mice with DSS-induced ulcerative colitis(UC). C57BL/6J mice were randomly divided into a blank group, a model group(DSS group), and low-, medium-and high-dose HQT groups(HQT-L, HQT-M, and HQT-H), and western medicine mesalazine group(western medicine group). The UC model was induced in mice. Subsequently, the mice in the HQT-L, HQT-M, HQT-H groups, and the western medicine group were given low-, medium-, high-dose HQT, and mesalazine suspension by gavage, respectively, while those in the blank and DSS groups were given an equal volume of distilled water by gavage. After 10 days of administration, the body weight, DAI scores, and colonic histopathological score of mice in each group were determined. The levels of IL-6, IL-10, IL-1ß, and TNF-α in serum were determined by ELISA. The mRNA expression of NLRP3 and Caspase-1 in colon tissues was determined by RT-qPCR. The protein expression of NLRP3 and Caspase-1 in colon tissues was detected by immunohistochemistry. The results showed that compared with the blank group, the DSS group showed decreased body weight of mice and increased DAI scores and intestinal histopathological score. Compared with the DSS group, the HQT groups and the western medicine group showed improved DAI scores, especially in the HQT-M, HQT-H, and the western medicine groups(P<0.05). The intestinal histopathological scores of the HQT groups and the western medicine group significantly decreased, especially in the HQT-M, HQT-H, and the western medicine groups(P<0.05). In addition, compared with the blank group, the DSS group showed elevated expression of NLRP3 and Caspase-1 in colon tissues, increased serum levels of IL-6, IL-1ß, and TNF-α, and decreased IL-10 level. Compared with the DSS group, the HQT groups and the western medicine group displayed decreased expression of NLRP3 and Caspase-1 in colon tissues, reduced serum levels of IL-6, IL-1ß, and TNF-α, and increased IL-10 level. The improvement was the most significant in the HQT-H group and the western medicine group(P<0.01). In conclusion, HQT may reduce the expression of NLRP3 and Caspase-1 in colon tissues, reduce the se-rum levels of IL-6, IL-1ß, and TNF-α, and increase the expression of IL-10 by regulating the classic pyroptosis pathway of NLRP3/Caspase-1, thereby improving the symptoms of intestinal injury and inflammatory infiltration of intestinal mucosa in DSS mice to achieve its therapeutic effect.

A Novel Strategy for Screening Active Components in Cistanche tubulosa Based on Spectrum-Effect Relationship Analysis and Network Pharmacology.

Cistanche tubulosa (Schenk) R. Wight is a valuable herbal medicine in China. The study aimed to explore the potential mechanisms of C. tubulosa on antioxidant activity using spectrum-effect relationship and network pharmacology and the possibilities of utilizing herbal dregs. In this work, different extracts of C. tubulosa, including herbal materials, water extracts, and herbal residues, were evaluated using high-performance liquid chromatography (HPLC) technology. In addition, the antioxidant activities were estimated in vitro, including 2, 2-diphenyl-1-picrylhydrazyl; superoxide anion; and hydroxyl radical scavenging assays. The spectrum-effect relationships between the HPLC fingerprints and the biological capabilities were analyzed via partial least squares regression, bivariate correlation analysis, and redundancy analysis. Furthermore, network pharmacology was used to predict potential mechanisms of C. tubulosa in the treatment of antioxidant-related diseases. According to the results, eleven common peaks were shared by different extracts. Geniposidic acid, echinacoside, verbascoside, tubuloside A, and isoacteoside were quantified and compared among different forms of C. tubulosa. The spectrum-effect relationship study indicated that peak A 6 might be the most decisive component among the three forms. Based on network pharmacology, there were 159 target genes shared by active components and antioxidant-related diseases. Targets related to antioxidant activity and relevant pathways were discussed. Our results provide a theoretical basis for recycling the herbal residues and the potential mechanisms of C. tubulosa in the treatment of antioxidant-related diseases.

Inhibition of α-glucosidase by Cyclocarya paliurus based on HPLC fingerprinting integrated with molecular docking and molecular dynamics.

Cyclocarya paliurus (CP) extracts have been shown to lower sugar and lipid levels in blood, but the material basis is not clear. We analyzed CP aqueous extracts using high-performance liquid chromatography "fingerprinting", checked their pharmacological parameters using virtual screening, and undertook molecular docking and molecular dynamics simulations. Also, the inhibitory effects of CP components upon α-glucosidase in vitro were evaluated. Fingerprinting and virtual screening showed that the aqueous extract of CP contained the active components protocatechuic acid, chlorogenic acid, caffeic acid and rutin, which were safe and had no side effects in vivo. Molecular docking and molecular dynamics simulations showed that chlorogenic acid and rutin might have a potent inhibitory effect on α-glucosidase. An enzyme-activity assay in vitro showed that the half-maximal inhibitory values of chlorogenic acid and rutin were 398.9 and 351.8 µg/ml, respectively. Chlorogenic acid and rutin had an inhibitory effect on α-glucosidase. Cyclocarya paliurus could be developed as a natural α-glucosidase inhibitor.