1.Effect of fluvastatin on expression of connective tissue growth factor in the myocardium of diabetic rats
Pengbin LAI ; Liyong YANG ; Xu LIN
Chinese Journal of Diabetes 2006;14(3):224-226
Objective To investigate the effects of fluvastatin on expression of connective tissue growth factor (CTGF)in the myocardium of diabetic rats. Methods Thirty-two Sprague-Dawley rats were randomized into four groups: normal control, untreated and STZ-induced diabetic rats, and diabetic rats treated with low-dose and high-dose fluvastatin.After 12 weeks′ intervention, body weight as well as the weights of both whole heart and its left ventricle were measured to calculate the ratio of heart weight to body weight (H/B) and the left ventricle mass index (LVMI).The mRNA expression of CTGF, transforming growth factor β1 (TGF-β1), fibronectin (FN),collagen type Ⅲ (ColⅢ) in the myocardium were detected by RT-PCR. Results Compared with the normal control group, the untreated diabetic group showed the increased (all P<0.05) H/B, LVMI and mRNA expressions of CTGF, TGF-β1, FN, and Col Ⅲ in the myocardium. In addition to the effective regulation of lipid metabolism, fluvastatin treatment could obviously reduce the increment of H/B and LVMI(P<0.05~0.01), and suppress the mRNA expressions of CTGF, TGF-β1, FN, and Col Ⅲ in the myocardium of diabetic rats(P<0.01).The down-regulation of CTGF was more significant than that of TGF-β1.All these effects were in dose dependent way. Conclusions Fluvastatin inhibits extracellular matrix accumulation in the myocardium of diabetic rat.Down-regulating the overexpression of CTGF in diabetics is an underlying mechanism of fluvastatin in the cardiac protection.
2.Study on spectrum-effect relationship based on antioxidant activity of Artemisiae Annuae Herba
Liyong LAI ; Tianshuang XIA ; Shengyan XU ; Yiping JIANG ; Xiaoqiang YUE ; Hailiang XIN
Journal of Pharmaceutical Practice and Service 2024;42(5):203-210,216
Objective To screen the pharmacodynamic material basic components of Artemisiae Annuae Herba and study its antioxidant activity in vitro by investigating the spectrum-effect relationship between the HPLC fingerprints of 11 batches of Artemisiae Annuae Herba(dried aerial part of Artemisia annua L.).Methods The determination was performed on Aglient C18 column(250 mm×4.6 mm,5 μm)with mobile phase consisted of 0.2%phosphoric acid solution-Methanol(gradient elution)at the flow rate of 1.0 ml/min.The column temperature was indoor temperature,and detection wavelength was 220 nm,with sample size of 10 μl.Using isochlorogenic acid A as reference,HPLC fingerprints of 11 batches of samples were determined.The common peaks of 11 batches of samples were identified and recorded through TCM chromatographic fingerprint similarity evaluation system(2012 edition).Using scavenging rate of DPPH and ABTS free radical as pharmacodynamic indicators of antioxidant effects,SIMCA 14.1 analysis software was used for PLSR to establish the spectra-effect relationship.Results There were 48 common peaks on 11 batches of sample,11 components were identified as scopoletin,scoparone,isochlorogenic acid B,A,C,luteolin,apigenin,chrysosplenetin,artemisinin,artemisetin and artemisinic acid.The scavenging activity of 11 batches of samples to DPPH and ABTS free radicals was detected.The spectrum-effect relationship showed that isochlorogenic acid A,B,C and scoparone were positively associated with its antioxidant capacity,and variable projection value was greater than 1.It was suggested that these components were the material basis of antioxidant effect in Artemisiae Annuae Herba.Conclusion This study investigates the antioxidant capacity of different substances in Artemisiae Annuae Herba in vitro,and proves that isochlorogenic acid A,B,C and scoparone play a major role for the antioxidant capacity.
3.Mechanism of Artemisia annua L. in GIOP with kidney-yin deficiency based on network pharmacology
Liyong LAI ; Tianshuang XIA ; Xiaoqiang YUE ; Hailiang XIN
Journal of Pharmaceutical Practice 2023;41(11):672-679
Objective To predict and preliminarily verify the potential targets and related signaling pathways of Artemisia annua L. in treating glucocorticoid-induced osteoporosis (GIOP) with kidney-yin deficiency by network pharmacology and in vitro experiments. Methods The pharmacological targets of Artemisia annua L. were obtained from TCMSP database and were converted to gene names through Uniprot database. The target genes of GIOP with kidney-yin deficiency were obtained from GeneCards database, OMIM database and Drugbank database, and the common target genes were obtained by cross analysis with drug target gene. Protein-protein interaction (PPI) network was constructed by String database, and visualization analysis and core targets screening were performed by Cytoscape 3.9.0. All common targets were analyzed by Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) functional enrichment analysis through Metascape database. Finally, the prediction results were verified by in vitro experiments. Results Ninety-eight targets of Artemisia annua L. to GIOP with kidney-yin deficiency were screened, including 17 core genes. The results of GO and KEGG functional enrichment analysis indicated that Artemisia annua L. treating GIOP with kidney-yin deficiency was related to biological processes such as hormonal response, positive regulation of cell death and extracellular stimulation response, et al, as well as signaling pathways such as PI3K/AKT, AGE/RAGE, MAPK and IL-17 et al. The number of genes enriched in PI3K/AKT signaling pathway was the largest. In vitro experiment results showed that Artemisia annua L. promoted the proliferation of osteoblasts damaged by dexamethasone (DEX), increased alkaline phosphatase activity, activated PI3K/AKT pathway, and promoted the phosphorylation of AKT. Conclusion Artemisia annua L. treating GIOP with kidney-yin deficiency has the characteristics of multi-targets and multi-pathway, which could promote the proliferation and differentiation of osteoblasts through multiple pathways. The PI3K/AKT signaling pathway is an important pathway. Artemisia annua L. treating GIOP with kidney-yin deficiency might be related to its ability to promote the PI3K/AKT signaling pathway and promote the phosphorylation of AKT.