Journal: International journal of cancer

Article Title: Hyperforin, a bio-active compound of St. John's Wort, is a new inhibitor of angiogenesis targeting several key steps of the process.

doi: 10.1002/ijc.21246

Figure Lengend Snippet: FIGURE 1 – Chemical structure of hyperforin.

Article Snippet: Highly purified hyperforin was supplied by ChromaDex (St. Ana, CA).

Techniques:

Journal: International journal of cancer

Article Title: Hyperforin, a bio-active compound of St. John's Wort, is a new inhibitor of angiogenesis targeting several key steps of the process.

doi: 10.1002/ijc.21246

Figure Lengend Snippet: FIGURE 2 – Hyperforin inhibits in vivo angiogenesis, as determined by the CAM assay. Experiments were carried out as described in Material and Methods. Methylcellulose discs containing the substance vehicle alone (control, a), 10 (b), 20 (c) and 30 (d) nmol hyperforin. Circles show the locations of the methyl cellulose discs. Arrows point to peripheral vessels avoiding the core of the treated area, asterisks indicate disorganization of pre-existing vessels and diamonds point to tissue inflammation.

Article Snippet: Highly purified hyperforin was supplied by ChromaDex (St. Ana, CA).

Techniques: In Vivo, Chick Chorioallantoic Membrane Assay, Control

Journal: International journal of cancer

Article Title: Hyperforin, a bio-active compound of St. John's Wort, is a new inhibitor of angiogenesis targeting several key steps of the process.

doi: 10.1002/ijc.21246

Figure Lengend Snippet: FIGURE 3 – Hyperforin inhibits the growth of BAE and non-endo- thelial cells. Experiments were carried out as described in Mate- rial and Methods. Survival curves for BAE (a), MDA-MB231 (b) and NIH-3T3 (c) cells. Data are means 6 SD of 3 independent experiments, each one with quad- ruplicate samples for each tested hyperforin concentration.

Article Snippet: Highly purified hyperforin was supplied by ChromaDex (St. Ana, CA).

Techniques: Concentration Assay

Journal: International journal of cancer

Article Title: Hyperforin, a bio-active compound of St. John's Wort, is a new inhibitor of angiogenesis targeting several key steps of the process.

doi: 10.1002/ijc.21246

Figure Lengend Snippet: FIGURE 4 – Hyperforin inhibits endothelial cell tubulogenesis in vitro. BAE cells seeded on Matrigel formed tubes (a), whereas tubulo- genesis was inhibited in the presence of 2.5 lM of hyperforin (b). Cells were photographed 7 hr after seeding under an inverted micro- scope (340).

Article Snippet: Highly purified hyperforin was supplied by ChromaDex (St. Ana, CA).

Techniques: In Vitro

Journal: International journal of cancer

Article Title: Hyperforin, a bio-active compound of St. John's Wort, is a new inhibitor of angiogenesis targeting several key steps of the process.

doi: 10.1002/ijc.21246

Figure Lengend Snippet: FIGURE 5 – Hyperforin inhibits the production and secretion of endothelial cell matrix metalloproteinase-2 but not its activity. (a) Conditioned media (c.m.) and cell extracts (c.e.) from BAE cells treated for 24 hr with 10 lM hyperforin and non-treated cells (control, C) were normalized for equal cell density and used for gelatin zymog- raphy as indicated in Material and Methods. (b) Conditioned media from non-treated cells were used for gelatin zymography, revealed with substrate buffer containing 10 lM hyperforin or not (control, C). Typical results are shown.

Article Snippet: Highly purified hyperforin was supplied by ChromaDex (St. Ana, CA).

Techniques: Activity Assay, Control, Zymography

Journal: International journal of cancer

Article Title: Hyperforin, a bio-active compound of St. John's Wort, is a new inhibitor of angiogenesis targeting several key steps of the process.

doi: 10.1002/ijc.21246

Figure Lengend Snippet: FIGURE 6 – Hyperforin inhibits the production and secretion of endothelial cell urokinase. Conditioned media from BAE cells treated for 24 hr with 1 or 10 lM hyperforin and non treated cells (control, C) were normalized for equal cell density and used for zymographic detection of urokinase as indicated in Material and Methods.

Article Snippet: Highly purified hyperforin was supplied by ChromaDex (St. Ana, CA).

Techniques: Control

Journal: International journal of cancer

Article Title: Hyperforin, a bio-active compound of St. John's Wort, is a new inhibitor of angiogenesis targeting several key steps of the process.

doi: 10.1002/ijc.21246

Figure Lengend Snippet: FIGURE 7 – Hyperforin slightly inhibits the migration of BAE cells. Confluent monolayers were wounded and a wound assay was carried out as described in Material and Methods. Confluent monolayers were wounded and washed. Fresh culture medium was added, either in the absence (control, C) or presence of 10 lM hyperforin. Photographs were taken at the beginning of the assay and after 4 hr of incubation.

Article Snippet: Highly purified hyperforin was supplied by ChromaDex (St. Ana, CA).

Techniques: Migration, Control, Incubation

Journal: International journal of cancer

Article Title: Hyperforin, a bio-active compound of St. John's Wort, is a new inhibitor of angiogenesis targeting several key steps of the process.

doi: 10.1002/ijc.21246

Figure Lengend Snippet: FIGURE 8 – Hyperforin inhibits BAE cell invasion. The invasion assay was carried out as described in Material and Methods. Relative velocities of invasion were determined for both control and treated (10 lM hyperforin) cells. Data are given in arbitrary units and are means 6 SD of triplicate samples in 2 independent experiments.

Article Snippet: Highly purified hyperforin was supplied by ChromaDex (St. Ana, CA).

Techniques: Invasion Assay, Control

Journal:

Article Title: St. John's wort induces hepatic drug metabolism through activation of the pregnane X receptor

doi:

Figure Lengend Snippet: Hyperforin is a potent activator of PXR. (A) CV-1 cells were transfected with expression plasmids for human PXR and the (CYP3A1)2-tk-CAT reporter. Cells were treated with extracts prepared from three different commercial preparations of St. John's wort [extract 1, Nature's Way (9 μg/ml); extract 2, Nature's Plus (75 μg/ml); extract 3, Solaray (7 μg/ml)] or with 10 μM of the indicated pure compounds, except for hyperforin, which was tested at 1 μM. Hyperforin was toxic to cells at concentrations >1 μM. Cell extracts subsequently were assayed for CAT activity. Data represent the mean of assays performed in quadruplicate ± SE and are plotted as -fold activation relative to transfected cells treated with vehicle alone. (B) Chemical structure of hyperforin. (C) CV-1 cells were transfected as in A and treated with increasing concentrations of hyperforin (squares) or rifampicin (circles). Data points represent the mean of assays performed in triplicate.

Article Snippet: Chemicals and their sources are as follows: hyperforin (Apin Chemicals Limited, Abingdon, Oxon, U.K.); amentoflavone and isoquercitrin (Indofine Chemical Company, Belle Mead, NJ); hyperoside (Research Plus, Bayonne, NJ); kaempferol, luteolin, myricetin, quercetin, quercitrin, rifampicin, β-sitosterol (from soybeans), scopoletin, and umbelliferone (Sigma); rutin (Acros Organics, subsidiary of Fisher Scientific); hypericin and pseudohypericin (Calbiochem); and SR12813 was synthesized in house.

Techniques: Transfection, Expressing, Activity Assay, Activation Assay

Journal:

Article Title: St. John's wort induces hepatic drug metabolism through activation of the pregnane X receptor

doi:

Figure Lengend Snippet: Hyperforin binds to PXR with high affinity. Competition binding assays were performed with purified human PXR LBD and 10 nM of the high-affinity PXR radioligand [3H]SR12813 in the presence of the indicated concentrations of hyperforin (squares), SR12813 (circles), or umbelliferone (triangles). Each data point represents the mean of assays performed in triplicate. The Ki value of hyperforin was calculated to be 27 nM by nonlinear regression analysis.

Article Snippet: Chemicals and their sources are as follows: hyperforin (Apin Chemicals Limited, Abingdon, Oxon, U.K.); amentoflavone and isoquercitrin (Indofine Chemical Company, Belle Mead, NJ); hyperoside (Research Plus, Bayonne, NJ); kaempferol, luteolin, myricetin, quercetin, quercitrin, rifampicin, β-sitosterol (from soybeans), scopoletin, and umbelliferone (Sigma); rutin (Acros Organics, subsidiary of Fisher Scientific); hypericin and pseudohypericin (Calbiochem); and SR12813 was synthesized in house.

Techniques: Binding Assay, Purification

Journal:

Article Title: St. John's wort induces hepatic drug metabolism through activation of the pregnane X receptor

doi:

Figure Lengend Snippet: St. John's wort extracts and hyperforin induce CYP3A4 expression in human hepatocytes. Northern blot analysis was performed with total RNA (10 μg) prepared from primary cultures of human hepatocytes treated for 30 h with extracts prepared from three different commercial preparations of St. John's wort [extract 1, Nature's Way (9 μg/ml); extract 2, Nature's Plus (75 μg/ml); extract 3, Solaray (7 μg/ml)], 1 μM hyperforin, or vehicle alone (0.1% ethanol). The blot was probed sequentially with 32P-labeled fragments of CYP3A4 and β-actin.

Article Snippet: Chemicals and their sources are as follows: hyperforin (Apin Chemicals Limited, Abingdon, Oxon, U.K.); amentoflavone and isoquercitrin (Indofine Chemical Company, Belle Mead, NJ); hyperoside (Research Plus, Bayonne, NJ); kaempferol, luteolin, myricetin, quercetin, quercitrin, rifampicin, β-sitosterol (from soybeans), scopoletin, and umbelliferone (Sigma); rutin (Acros Organics, subsidiary of Fisher Scientific); hypericin and pseudohypericin (Calbiochem); and SR12813 was synthesized in house.

Techniques: Expressing, Northern Blot, Labeling