derivatives geniposide  (MedChemExpress)

Journal: bioRxiv

Article Title: High-throughput drug screening for inhibition of influenza A virus infection based on human SIRT1 promoter and Genipin suppressing influenza A virus by activation of AMPK-SIRT1-PGC-1α signaling pathway

doi: 10.1101/2024.07.10.602919

Figure Lengend Snippet: The effects of Genipin and its derivatives on the pSIRT1 luc reporter and IAV infection in vitro . ( A ) MTT assay was used to determine the cytotoxicity of Gardenia jasminoides Ellis extract on A549 cells. ( B ) The inhibitory effect of Gardenia jasminoides Ellis extract on IAV (PR8) infection in vitro . ( C ) The structure of Genipin and its derivatives. ( D ) MTT assay was used to determine the cytotoxicity of Genipin on A549 cells. ( E ) The stimulating effect of Genipin and its derivatives on the pSIRT1 luc reporter. All groups were co-transfected with pSIRT1 luc and pRL-TK plasmids. Except for the control group (BG), all other groups were infected with IAV (MOI=0.01). The negative group (NG) and positive control group (PC) were treated with 0.5% DMSO and 50 μmol resveratrol (Res), respectively. All other groups were given Genipin and its derivatives at a dose of 50 μ mol. The data is expressed as the ratio of luciferase activity to its internal control. ( F, G, H and I ) The inhibitory effect of Genipin and its derivatives on IAV (PR8) infection. The negative control (NC) A549 cells were only infected with IAV (MOI=0.01) and treated with DMSO (0.5%, v/v). In the PC, Genipin, and their derivatives groups, A549 cells infected with IAV were treated with ribavirin (20 μg/mL), Genipin, and Genipin derivatives (6.25, 12.5, 25, 50 μmol), respectively. After 48 hours, collect the supernatant and measure the titer using the TCID50 method. The data were the mean ± standard deviation of three independent experiments. * Compared with the NC group, P<0.05.

Article Snippet: Genipin and its derivatives (Geniposide, Genipin 1-β-D-gentiobioside and Shanziside) were purchased from MedChemexpress (MCE) Co., Ltd. (New Jersey, USA).

Techniques: Infection, In Vitro, MTT Assay, Transfection, Control, Positive Control, Luciferase, Activity Assay, Negative Control, Standard Deviation

Journal: bioRxiv

Article Title: High-throughput drug screening for inhibition of influenza A virus infection based on human SIRT1 promoter and Genipin suppressing influenza A virus by activation of AMPK-SIRT1-PGC-1α signaling pathway

doi: 10.1101/2024.07.10.602919

Figure Lengend Snippet: In vivo anti IAV activity of Genipin and its derivatives. In the blank control (BC), mice were intraperitoneally treated with VGM and gavage with sterile physiological saline. In the negative control group (NC), positive control group (PC), and the treatment groups with Genipin and its derivatives, the mice were infected with 10 × MLD50 IAV (PR8), were treated with sterile physiological saline (NC group), ribavirin (50 mg/kg/d, PC group), Genipin (10mg/kg/d) and its derivatives (10mg/kg/d), respectively. (A) Monitor the survival rate for 14 days. Kaplan-Meier analysis with Log-rank and Breslow test were used to analyze the significant differences in average survival time. (B) On the 7th day, the lung virus load was detected by qPCR. (C) Evaluate lung index by measuring the percentage of lung wet weight (g) to body weight (g) on the 7th day (lung index=lung wet weight (g)/body weight (g) × 100%). (D) On the 7th day, lung cytokine levels were detected by qPCR. The data shown are the mean ± SD. Survival rate was measured in 10 mice (n=10), while lung index, lung virus load, and lung cytokine levels were measured in 6 mice (n=6). Compared with the BC group, # P<0.05, and compared with the NC group, * P<0.05.

Article Snippet: Genipin and its derivatives (Geniposide, Genipin 1-β-D-gentiobioside and Shanziside) were purchased from MedChemexpress (MCE) Co., Ltd. (New Jersey, USA).

Techniques: In Vivo, Activity Assay, Control, Sterility, Saline, Negative Control, Positive Control, Infection, Virus

Journal: bioRxiv

Article Title: High-throughput drug screening for inhibition of influenza A virus infection based on human SIRT1 promoter and Genipin suppressing influenza A virus by activation of AMPK-SIRT1-PGC-1α signaling pathway

doi: 10.1101/2024.07.10.602919

Figure Lengend Snippet: The effect of Genipin and its derivatives on pathological changes in mouse lung tissue. The treatment method for mice was shown in . On the 7th day, 6 mice in each group were euthanized. Then perform H&E staining on the right lung. (A) the blank control group (BC), (B) the negative control group (NC), (C) the positive drug control group (PC), (D) Genipin treatment group, (E) Geniposide treatment group, (F) Genipin 1-β -D-gentiobioside treatment group, (G) Shanzisaide treatment group, (H) histopathological evaluation. (→) alveolar wall, (△) inflammatory exudation, (▾) bleeding. The magnification was 200 times.

Article Snippet: Genipin and its derivatives (Geniposide, Genipin 1-β-D-gentiobioside and Shanziside) were purchased from MedChemexpress (MCE) Co., Ltd. (New Jersey, USA).

Techniques: Staining, Control, Negative Control

Journal: bioRxiv

Article Title: High-throughput drug screening for inhibition of influenza A virus infection based on human SIRT1 promoter and Genipin suppressing influenza A virus by activation of AMPK-SIRT1-PGC-1α signaling pathway

doi: 10.1101/2024.07.10.602919

Figure Lengend Snippet: An antagonistic experiment on the effect of Genipin. The blank control group (BC), negative control group (NC), positive drug control group (PC), and genipin (12.5 μ mol) treatment group were the same as . In pharmacological antagonistic experiments, SIRT1 antagonist nicotinamide (NAM, 10mM) or PGC-1 alpha antagonist SR-18292 (15 μ M) were added together with Genipin. 48 hours later, TCID50 method was used to detect virus titer ( A ), and ELISA method was used to detect cytokine levels ( B ). In the siRNA antagonist assay, SIRT1 siRNA, PGC-1 α siRNA, or control siRNA were transfected with GoldenTran mRNA siRNA transfection reagents (Changchun Jinchuan Technology Co., Ltd.). After 24 hours, cells were infected with IAV (MOI=0.001) and treated with corresponding drugs. After 24 hours, Western blotting was used to determine the knockout effect of siRNA ( C and D ), TCID50 method was used to measure virus titer ( E ), and ELISA method was used to measure cytokine production ( F ). The data shown were the mean ± standard deviation of three independent experiments. Compared with the Genipin treatment group, * P <0.05.

Article Snippet: Genipin and its derivatives (Geniposide, Genipin 1-β-D-gentiobioside and Shanziside) were purchased from MedChemexpress (MCE) Co., Ltd. (New Jersey, USA).

Techniques: Control, Negative Control, Virus, Enzyme-linked Immunosorbent Assay, Transfection, Infection, Western Blot, Knock-Out, Standard Deviation

Journal: bioRxiv

Article Title: High-throughput drug screening for inhibition of influenza A virus infection based on human SIRT1 promoter and Genipin suppressing influenza A virus by activation of AMPK-SIRT1-PGC-1α signaling pathway

doi: 10.1101/2024.07.10.602919

Figure Lengend Snippet: The effects of Genipin and its derivatives on the pSIRT1 luc reporter and IAV infection in vitro . ( A ) MTT assay was used to determine the cytotoxicity of Gardenia jasminoides Ellis extract on A549 cells. ( B ) The inhibitory effect of Gardenia jasminoides Ellis extract on IAV (PR8) infection in vitro . ( C ) The structure of Genipin and its derivatives. ( D ) MTT assay was used to determine the cytotoxicity of Genipin on A549 cells. ( E ) The stimulating effect of Genipin and its derivatives on the pSIRT1 luc reporter. All groups were co-transfected with pSIRT1 luc and pRL-TK plasmids. Except for the control group (BG), all other groups were infected with IAV (MOI=0.01). The negative group (NG) and positive control group (PC) were treated with 0.5% DMSO and 50 μmol resveratrol (Res), respectively. All other groups were given Genipin and its derivatives at a dose of 50 μ mol. The data is expressed as the ratio of luciferase activity to its internal control. ( F, G, H and I ) The inhibitory effect of Genipin and its derivatives on IAV (PR8) infection. The negative control (NC) A549 cells were only infected with IAV (MOI=0.01) and treated with DMSO (0.5%, v/v). In the PC, Genipin, and their derivatives groups, A549 cells infected with IAV were treated with ribavirin (20 μg/mL), Genipin, and Genipin derivatives (6.25, 12.5, 25, 50 μmol), respectively. After 48 hours, collect the supernatant and measure the titer using the TCID50 method. The data were the mean ± standard deviation of three independent experiments. * Compared with the NC group, P<0.05.

Article Snippet: Genipin and its derivatives (Geniposide, Genipin 1-β-D-gentiobioside and Shanziside) were purchased from MedChemexpress (MCE) Co., Ltd. (New Jersey, USA).

Techniques: Infection, In Vitro, MTT Assay, Transfection, Control, Positive Control, Luciferase, Activity Assay, Negative Control, Standard Deviation

Journal: bioRxiv

Article Title: High-throughput drug screening for inhibition of influenza A virus infection based on human SIRT1 promoter and Genipin suppressing influenza A virus by activation of AMPK-SIRT1-PGC-1α signaling pathway

doi: 10.1101/2024.07.10.602919

Figure Lengend Snippet: In vivo anti IAV activity of Genipin and its derivatives. In the blank control (BC), mice were intraperitoneally treated with VGM and gavage with sterile physiological saline. In the negative control group (NC), positive control group (PC), and the treatment groups with Genipin and its derivatives, the mice were infected with 10 × MLD50 IAV (PR8), were treated with sterile physiological saline (NC group), ribavirin (50 mg/kg/d, PC group), Genipin (10mg/kg/d) and its derivatives (10mg/kg/d), respectively. (A) Monitor the survival rate for 14 days. Kaplan-Meier analysis with Log-rank and Breslow test were used to analyze the significant differences in average survival time. (B) On the 7th day, the lung virus load was detected by qPCR. (C) Evaluate lung index by measuring the percentage of lung wet weight (g) to body weight (g) on the 7th day (lung index=lung wet weight (g)/body weight (g) × 100%). (D) On the 7th day, lung cytokine levels were detected by qPCR. The data shown are the mean ± SD. Survival rate was measured in 10 mice (n=10), while lung index, lung virus load, and lung cytokine levels were measured in 6 mice (n=6). Compared with the BC group, # P<0.05, and compared with the NC group, * P<0.05.

Article Snippet: Genipin and its derivatives (Geniposide, Genipin 1-β-D-gentiobioside and Shanziside) were purchased from MedChemexpress (MCE) Co., Ltd. (New Jersey, USA).

Techniques: In Vivo, Activity Assay, Control, Sterility, Saline, Negative Control, Positive Control, Infection, Virus

Journal: bioRxiv

Article Title: High-throughput drug screening for inhibition of influenza A virus infection based on human SIRT1 promoter and Genipin suppressing influenza A virus by activation of AMPK-SIRT1-PGC-1α signaling pathway

doi: 10.1101/2024.07.10.602919

Figure Lengend Snippet: The effect of Genipin and its derivatives on pathological changes in mouse lung tissue. The treatment method for mice was shown in . On the 7th day, 6 mice in each group were euthanized. Then perform H&E staining on the right lung. (A) the blank control group (BC), (B) the negative control group (NC), (C) the positive drug control group (PC), (D) Genipin treatment group, (E) Geniposide treatment group, (F) Genipin 1-β -D-gentiobioside treatment group, (G) Shanzisaide treatment group, (H) histopathological evaluation. (→) alveolar wall, (△) inflammatory exudation, (▾) bleeding. The magnification was 200 times.

Article Snippet: Genipin and its derivatives (Geniposide, Genipin 1-β-D-gentiobioside and Shanziside) were purchased from MedChemexpress (MCE) Co., Ltd. (New Jersey, USA).

Techniques: Staining, Control, Negative Control