1.Flavonoids from Corn Silk (Zea mays L.) and its pharmacological effects
Licheng ZHOU ; Yiming OU ; Yuan WANG
Journal of Pharmaceutical Practice and Service 2025;43(2):51-58
Corn silk, a Traditional Chinese Medicine, has the effect of calming liver, cholagogue, detumescence and diuresis. Corn silk is also widely used as tea and functional food. Natural flavonoids have multiple biological activities, which are also the main bioactive components of corn silk. In the past decade, many new advances have been made in the chemistry, analysis, pharmacology, pharmacokinetics, and safety evaluation of corn silk flavonoids. The chemical composition research of flavonoids has enriched the variety of flavonoids in corn silk. Pharmacological studies have confirmed and expanded the efficacy of corn silk flavonoids. And safety evaluation has provided a theoretical basis for the safe application of corn silk flavonoids. Through literature search, the extraction, separation, compositional analysis, content determination, pharmacological effect, pharmacokinetics, and safety research progress of corn silk flavonoids in the past ten years were reviewed in this paper.
2.Preparation of Phellodendrine-11-O-β-D-Glucuronide and Its Effects on Glycolipid Metabolism in Insulin-Resistant HepG2 Cells
Peisi OU ; Minghe GU ; Aihua LIN ; Yiming LIU
Journal of Nanjing University of Traditional Chinese Medicine 2025;41(7):926-935
OBJECTIVE To establish a preparation method for Phellodendrine-11-O-β-D-glucuronide(M1),a metabolite of Phellodendrine(PHE),and to evaluate its regulatory effects on glycolipid metabolism disorder in insulin-resistant HepG2(IR-HepG2)cells.METHODS The preparation,extraction,separation,purification and identification of M1 were completed by in vitro incuba-tion of intestinal microsomes combined with liquid phase,mass spectrometry and NMR.With Metformin as positive control,IR-HepG2 cells were treated with low(25 μmol·L-1),medium(50 μmol·L-1)and high(100 μmol·L-1)doses of M1 for 24 h.Glucose con-sumption,glucose uptake,triglyceride(TG),total cholesterol(TC),high density lipoprotein cholesterol(HDL-C)and low density lipoprotein cholesterol(LDL-C)were quantified.The binding ability of M1 to the key targets INSR,IRS1,PI3K and AKT2 in the IRS1/PI3K/AKT pathway was explored through molecular docking technology.The effects of M1 on the mRNA and protein expression of these key targets in the IRS1/PI3K/AKT pathway were detected by qPCR and Western blot,respectively.RESULTS The purified product was confirmed by NMR as Phellodendrine-11-O-β-D-glucuronide(95%purity).Compared to the model group,all M1 do-ses significantly enhanced glucose consumption(P<0.01,P<0.001)and uptake(P<0.001)in IR-HepG2 cells,outperforming PHE(P<0.001).At medium and high doses,it could significantly reduce the content of TG and TC in cells(P<0.001),and its improve-ment effect at the TG level was better than that of PHE(P<0.01);while all concentrations decreased LDL-C(P<0.001)and in-creased HDL-C(P<0.01,P<0.001).Molecular docking revealed strong binding interactions between M1 and INSR,IRS1,PI3K,and AKT2.Compared with the model group,M1 administration group increased the expression of INSR,IRS1,PI3K,AKT2,and GLUT2 mRNA to varying degrees,downregulated the protein expression of p-IRS1/IRS1(P<0.001),and upregulated the protein ex-pression of PI3K,p-AKT/AKT,and p-GSK3β/GSK3β.CONCLUSION The established protocol enables high purity M1 prepara-tion.M1 alleviates IR by regulating IRS1/PI3K/AKT signaling pathway to improve the disorder of glycolipid metabolism.
3.Preparation of Phellodendrine-11-O-β-D-Glucuronide and Its Effects on Glycolipid Metabolism in Insulin-Resistant HepG2 Cells
Peisi OU ; Minghe GU ; Aihua LIN ; Yiming LIU
Journal of Nanjing University of Traditional Chinese Medicine 2025;41(7):926-935
OBJECTIVE To establish a preparation method for Phellodendrine-11-O-β-D-glucuronide(M1),a metabolite of Phellodendrine(PHE),and to evaluate its regulatory effects on glycolipid metabolism disorder in insulin-resistant HepG2(IR-HepG2)cells.METHODS The preparation,extraction,separation,purification and identification of M1 were completed by in vitro incuba-tion of intestinal microsomes combined with liquid phase,mass spectrometry and NMR.With Metformin as positive control,IR-HepG2 cells were treated with low(25 μmol·L-1),medium(50 μmol·L-1)and high(100 μmol·L-1)doses of M1 for 24 h.Glucose con-sumption,glucose uptake,triglyceride(TG),total cholesterol(TC),high density lipoprotein cholesterol(HDL-C)and low density lipoprotein cholesterol(LDL-C)were quantified.The binding ability of M1 to the key targets INSR,IRS1,PI3K and AKT2 in the IRS1/PI3K/AKT pathway was explored through molecular docking technology.The effects of M1 on the mRNA and protein expression of these key targets in the IRS1/PI3K/AKT pathway were detected by qPCR and Western blot,respectively.RESULTS The purified product was confirmed by NMR as Phellodendrine-11-O-β-D-glucuronide(95%purity).Compared to the model group,all M1 do-ses significantly enhanced glucose consumption(P<0.01,P<0.001)and uptake(P<0.001)in IR-HepG2 cells,outperforming PHE(P<0.001).At medium and high doses,it could significantly reduce the content of TG and TC in cells(P<0.001),and its improve-ment effect at the TG level was better than that of PHE(P<0.01);while all concentrations decreased LDL-C(P<0.001)and in-creased HDL-C(P<0.01,P<0.001).Molecular docking revealed strong binding interactions between M1 and INSR,IRS1,PI3K,and AKT2.Compared with the model group,M1 administration group increased the expression of INSR,IRS1,PI3K,AKT2,and GLUT2 mRNA to varying degrees,downregulated the protein expression of p-IRS1/IRS1(P<0.001),and upregulated the protein ex-pression of PI3K,p-AKT/AKT,and p-GSK3β/GSK3β.CONCLUSION The established protocol enables high purity M1 prepara-tion.M1 alleviates IR by regulating IRS1/PI3K/AKT signaling pathway to improve the disorder of glycolipid metabolism.
4.Viral load and neutralizing activity of plasma from HIV-1 chronic infected former blood donors in Anhui province, China
Yan JI ; Liying MA ; Shuiling OU ; Lin YUAN ; Jianping SUN ; Pengfei MA ; Quanbi ZHAO ; Yang HUANG ; Jianghong HUANG ; Yiming SHAO
Chinese Journal of Microbiology and Immunology 2008;28(9):787-790
Objective To explore the association among viral load,CD4 count and neutralizing ac-tivity of plasma from chronic HIV-1 infected former blood donors in Anhui province, China. Methods 294 chronically HIV-1 B' infected individuals from former blood donors in Anhni province were enrolled, whose plasma and peripheral blood mononuelnar cells (PBMC) were isolated. The viral load and CD4 were detec-ted, and the neutralization activity of plasma against primary virus (1597) and lab-adapted strain (SF33) was detected by Luciferase Assay System based on TZM cell line, and 50% neutralizing level was calculated by the Reed-Mueneh method. Results Neutralizing activity responding against SF33 strain was higher than 1597 (P<0.05). There was a positive correlation between neutralizing concentration of plasma against SF33 and viral load (1g) (r = 0.191, P = 0.001), but there was no correlation between neutralizing concen-tration of plasma against 1597 and viral load(lg) (r = 0.097, P = 0.096). Conchtsion In chronic HIV-1 infectious people, neutralizing level against SF33 increases with viral replication, however, there is no asso-ciation of plasma neutralizing against 1597 replication with viral load.

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