| Name | physalin F |
| Description | Physalin F is a natural blocker of CaV2.3 (R-type) and CaV2.2 (N-type) voltage-gated calcium channels.It is a secosteroid with potent anti-inflammatory and immunomodulatory activities. Physalin F induces apoptosis of PBMC, decreasing the spontaneous proliferation and cytokine production caused by Human T-lymphotropic virus type 1 (HTLV-1) infection |
| In vitro | METHODS: Three renal cancer cell lines (A498, ACHN, and UO-31) were treated with physalin F (0, 0.3, 1, 3, and 10 μg/mL, 24 h), and cell viability was determined by MTT assay.
RESULTS Physalin F inhibited cell viability in human renal cancer cell lines A498, ACHN, and UO-31 in a concentration-dependent manner with IC50 values of 1.40 μg/mL, 2.18 μg/mL, and 2.81 μg/mL, respectively. [3]
METHODS: A498 cells were incubated in the absence or presence of physalin F (10 μg/mL, 6, 12, 18, 24 hours) for the indicated time, and the cells were harvested and prepared for detection of (A) mitochondrial membrane potential using FACScan analysis; A498 cells were incubated in the presence of physalin F (10 μg/mL, 3, 6, 8, 12, 18, 24 hours) for the indicated time, and the cells were harvested and prepared for detection of pro-caspase-8, 9, caspase-3, PARP, and p53, p21 expression using Western blotting.
RESULTS The expression of Bcl-2 protein family including Bcl-2 and Bcl-xL was decreased after treatment with physalin F, and physalin F induced apoptosis of A498 cells through a mitochondria-dependent pathway; physalin F induced apoptosis by inducing p53 and p21 proteins, followed by cleavage of caspase-8/-9/-3 and PARP. [3] |
| In vivo | Physalin F is a secosteroid with potent anti-inflammatory and immunomodulatory activities.?A concentration-dependent inhibition of spontaneous proliferation of PBMC from HAM/TSP subjects was observed in the presence of physalin F, as evaluated by (3)H-thymidine uptake.?The IC50 for physalin F was 0.97 0.11 μM.?Flow cytometry analysis using Cytometric Bead Array (CBA) showed that physalin F (10 μM) significantly reduced the levels of IL-2, IL-6, IL-10, TNF-α and IFN-γ, but not IL-17A, in supernatants of PBMC cultures.?Next, apoptosis induction was addressed by using flow cytometry to evaluate annexin V expression.?Treatment with physalin F (10 μM) increased the apoptotic population of PBMC in HAM/TSP subjects.?Transmission electron microscopy analysis of PBMC showed that physalin F induced ultrastructural changes, such as pyknotic nuclei, damaged mitochondria, enhanced autophagic vacuole formation, and the presence of myelin-like figures.?In conclusion, physalin F induces apoptosis of PBMC, decreasing the spontaneous proliferation and cytokine production caused by HTLV-1 infection. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (1.9 mM), Sonication is recommended.
DMSO : 60 mg/mL (113.95 mM), Sonication is recommended.
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| Keywords | proliferation | physalin F | PBMC | Inhibitor | inhibit | inflammatory | infection | immunomodulatory | HTLV-1 | cytokine | CaV2.3 | CalciumChannel | Calcium Channel | Apoptosis |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Flubendazole | Cysteamine hydrochloride | L-Glutamic acid monosodium salt monohydrate | Sodium 4-phenylbutyrate | L-Ascorbic acid | L-Glutamic acid | Tributyrin | L-Ascorbic acid sodium salt | Alginic acid | Dextran sulfate sodium salt (MW 5000) |
| Related Compound Libraries | Anti-Tumor Natural Product Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Selected Plant-Sourced Compound Library | Anti-Viral Compound Library | Natural Product Library | Anti-Inflammatory Traditional Chinese Medicine Compound Library | Natural Product Library for HTS | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Anti-virus Traditional Chinese Medicine Monomer Library | Heat-Clearing and Detoxifying Traditional Chinese Medicine Compound Library |
United States
