| Description: |
Orobol is an inhibitor of tyrosine-specific protein kinase and phosphatidylinositol turnover, it has sensitization effect, it can produce produced cisplatin (DDP) sensitivity in human ovarian carcinoma cells by inducing apoptosis through the MT-dependent signaling pathway. Orobol and platelet derived growth factor (PDGF) regulate paclitaxel (PX) sensitivity by reciprocally altering the proportion of tubulin isotype expression and PX-induced apoptotic signaling. Orobol exhibits antiviral effects against some animal viruses, addition of the compound after virus entry inhibits the appearance of late viral protein synthesis in Vesicular Stomatitis Virus, influenza, or vaccinia virus-infected cells, but has no effect on poliovirus protein synthesis. |
| Targets: |
PI3K | Caspase | Bcl-2/Bax | Calcium Channel | Antifection | Influenza virus |
| In vitro: |
| Biochem Biophys Res Commun. 1992 Jan 31;182(2):894-9. | | Isoflavonoids, genistein, psi-tectorigenin, and orobol, increase cytoplasmic free calcium in isolated rat hepatocytes.[Pubmed: 1734888] |
METHODS AND RESULTS:
Isoflavonoid compounds, genistein, psi-tectorigenin and orobol have been implicated as inhibitors of tyrosine-specific protein kinase and phosphatidylinositol turnover. These compounds have been frequently used as a pharmacological tool to assess signal transduction pathways in various cell systems. In the course of analyzing signaling pathways in rat hepatocytes, we obtained an unexpected finding that these compounds transiently increase cytoplasmic free calcium. Since the Ca2+ mobilizing effect was observed in 1 microM calcium containing buffer, the source of the Ca2+ may be intracellular stores.
CONCLUSIONS:
Thus, when interpreting data obtained using these compounds, caution is needed. |
|
| In vivo: |
| Pharmaceutics . 2020 Sep 3;12(9):845. | | Lipid Nanoparticles for Enhancing the Physicochemical Stability and Topical Skin Delivery of Orobol[Pubmed: 32899309] | | Abstract
Orobol is one of the major soy isoflavones, and has been reported to have various pharmacological activities, including an anti-skin-aging effect. However, since it has low solubility in water and physicochemical instability, the formulation of orobol for delivery into the dermal layer of the skin could be challenging. The objective of this study was to prepare lipid nanoparticles formulations of orobol to enhance its stability as well as its deposition into the skin. Formulations of orobol-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were characterized in terms of their mean particle size, entrapment efficiency, and morphology. The nano-sized spherical NLCs formulations maintained the stability of orobol for up to 28 days. Moreover, the NLCs formulation significantly increased the in vitro deposition of orobol into both Strat-M membranes and human cadaver skin compared with the other formulations. Additionally, the NLCs formulation did not cause significant skin irritation in clinical study. These results demonstrate that a shea butter-based NLC formulation could be a promising and safe carrier system for improving the stability of orobol and enhancing its topical skin delivery.
Keywords: Strat-M membrane; human cadaver skin; nanostructured lipid carrier (NLC); orobol; physicochemical stability; skin irritation; topical skin delivery. |
|
Cell. 2018 Jan 11;172(1-2):249-261.e12. doi: 10.1016/j.cell.2017.12.019.IF=36.216(2019)
Cell Metab. 2020 Mar 3;31(3):534-548.e5. doi: 10.1016/j.cmet.2020.01.002.IF=22.415(2019)
Mol Cell. 2017 Nov 16;68(4):673-685.e6. doi: 10.1016/j.molcel.2017.10.022.IF=14.548(2019)
ACS Nano. 2018 Apr 24;12(4): 3385-3396. doi: 10.1021/acsnano.7b08969.IF=13.903(2019)
Nature Plants. 2016 Dec 22;3: 16206. doi: 10.1038/nplants.2016.205.IF=13.297(2019)
Sci Adv. 2018 Oct 24;4(10): eaat6994. doi: 10.1126/sciadv.aat6994.IF=12.804(2019)
