Gamabufotalin - CAS 465-11-2
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Not Intended for Therapeutic Use. For research use only.
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Gamabufotalin is a major bufadienolide of Chansu and has been used for cancer therapy due to its desirable metabolic stability and less adverse effect.
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1.Gamabufotalin, a bufadienolide compound from toad venom, suppresses COX-2 expression through targeting IKKβ/NF-κB signaling pathway in lung cancer cells.
Yu Z, Guo W, Ma X1, Zhang B, Dong P, Huang L, Wang X, Wang C, Huo X, Yu W, Yi C, Xiao Y, Yang W, Qin Y, Yuan Y, Meng S, Liu Q, Deng W. Mol Cancer. 2014 Aug 31;13:203. doi: 10.1186/1476-4598-13-203.
BACKGROUND: Gamabufotalin (CS-6), a major bufadienolide of Chansu, has been used for cancer therapy due to its desirable metabolic stability and less adverse effect. However, the underlying mechanism of CS-6 involved in anti-tumor activity remains poorly understood.
2.Pharmacokinetics and tissue distribution of five bufadienolides from the Shexiang Baoxin Pill following oral administration to mice.
Huang H1, Yang Y2, Lv C3, Chang W3, Peng C4, Wang S5, Ge G6, Han L5, Zhang W7, Liu R8. J Ethnopharmacol. 2015 Feb 23;161:175-85. doi: 10.1016/j.jep.2014.07.056. Epub 2014 Sep 6.
ETHNOPHARMACOLOGICAL RELEVANCE: Shexiang Baoxin Pill (SBP) is a well-known composite formula of traditional Chinese medicine (TCM), widely used to treat cardiovascular diseases such as angina pectoris and myocardial infarction. Bufadienolides are major active compounds of Venenum Bufonis, which is one of the seven materiamedicas that comprise the Shexiang Baoxin Pill. Previous pharmacokinetics studies of bufadienolides have typically used a single medicinal material delivered to rats. In this study, we have chosen the mouse, a more proper animal model than the rat, to investigate the in vivo pharmacokinetics and tissue distribution of bufadienolides from the Shexiang Baoxin Pill.
3.Mutations to the cardiotonic steroid binding site of Na(+)/K(+)-ATPase are associated with high level of resistance to gamabufotalin in a natricine snake.
Mohammadi S1, Brodie ED Jr2, Neuman-Lee LA3, Savitzky AH2. Toxicon. 2016 May;114:13-5. doi: 10.1016/j.toxicon.2016.02.019. Epub 2016 Feb 21.
Although toads are defended by bufadienolide toxins, some snakes have evolved resistance to bufadienolides and feed heavily on toads. We compared resistance in Nerodia rhombifer, which possesses mutations that confer target-site resistance, to Pituophis catenifer, which lacks those mutations. Even at the highest dosage tested, Nerodia showed no effects, whereas the lowest dose was lethal to Pituophis. Our results demonstrate a striking level of resistance to bufadienolides in a species possessing the mutations for resistance.
4.Gamabufotalin, a major derivative of bufadienolide, inhibits VEGF-induced angiogenesis by suppressing VEGFR-2 signaling pathway.
Tang N1, Shi L2, Yu Z1,3, Dong P1, Wang C1, Huo X1, Zhang B1, Huang S1, Deng S1, Liu K1, Ma T4, Wang X3, Wu L3, Ma XC1,3. Oncotarget. 2016 Jan 19;7(3):3533-47. doi: 10.18632/oncotarget.6514.
Gamabufotalin (CS-6), a main active compound isolated from Chinese medicine Chansu, has been shown to strongly inhibit cancer cell growth and inflammatory response. However, its effects on angiogenesis have not been known yet. Here, we sought to determine the biological effects of CS-6 on signaling mechanisms during angiogenesis. Our present results fully demonstrate that CS-6 could significantly inhibit VEGF triggered HUVECs proliferation, migration, invasion and tubulogenesis in vitro and blocked vascularization in Matrigel plugs impregnated in C57/BL6 mice as well as reduced vessel density in human lung tumor xenograft implanted in nude mice. Computer simulations revealed that CS-6 interacted with the ATP-binding sites of VEGFR-2 using molecular docking. Furthermore, western blot analysis indicated that CS-6 inhibited VEGF-induced phosphorylation of VEGFR-2 kinase and suppressed the activity of VEGFR-2-mediated signaling cascades. Therefore, our studies demonstrated that CS-6 inhibited angiogenesis by inhibiting the activation of VEGFR-2 signaling pathways and CS-6 could be a potential candidate in angiogenesis-related disease therapy.
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CAS 465-11-2 Gamabufotalin

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