Eriocalyxin B - CAS 84745-95-9
Catalog number: B0005-152588
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Eriocalyxin B, isolated from the herbs of Isodon eriocalyx, is a potent NF-kappaB inhibitor. Eriocalyxin B inhibited the NF-kappaB transcriptional activity but not that of cAMP response element-binding protein. eriocalyxin B reversibly interfered with the binding of p65 and p50 subunits to the DNA in a noncompetitive manner. Eriocalyxin B exerts potent antiinflammatory effects through selective modulation of pathogenic Th1 and Th17 cells by targeting critical signaling pathways. Besides, Eriocalyxin B induces apoptosis and cell cycle arrest in pancreatic adenocarcinoma cells through caspase- and p53-dependent pathways. Eriocalyxin B should be considered a candidate for pancreatic cancer treatment.
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1.Eriocalyxin B Inhibits STAT3 Signaling by Covalently Targeting STAT3 and Blocking Phosphorylation and Activation of STAT3.
Yu X;He L;Cao P;Yu Q PLoS One. 2015 May 26;10(5):e0128406. doi: 10.1371/journal.pone.0128406. eCollection 2015.
Activated STAT3 plays an important role in oncogenesis by stimulating cell proliferation and resisting apoptosis. STAT3 therefore is an attractive target for cancer therapy. We have screened a traditional Chinese herb medicine compound library and found Eriocalyxin B (EB), a diterpenoid from Isodon eriocalyx, as a specific inhibitor of STAT3. EB selectively inhibited constitutive as well as IL-6-induced phosphorylation of STAT3 and induced apoptosis of STAT3-dependent tumor cells. EB did not affect the upstream protein tyrosine kinases or the phosphatase (PTPase) of STAT3, but rather interacted directly with STAT3. The effects of EB could be abolished by DTT or GSH, suggesting a thiol-mediated covalent linkage between EB and STAT3. Site mutagenesis of cysteine in and near the SH2 domain of STAT3 identified Cys712 to be the critical amino acid for the EB-induced inactivation of STAT3. Furthermore, LC/MS/MS analyses demonstrated that an α, β-unsaturated carbonyl of EB covalently interacted with the Cys712 of STAT3.
2.Eriocalyxin B, a novel autophagy inducer, exerts anti-tumor activity through the suppression of Akt/mTOR/p70S6K signaling pathway in breast cancer.
Zhou X;Yue GG;Chan AM;Tsui SK;Fung KP;Sun H;Pu J;Lau CB Biochem Pharmacol. 2017 Oct 15;142:58-70. doi: 10.1016/j.bcp.2017.06.133. Epub 2017 Jun 30.
Eriocalyxin B (EriB), a natural ent-kaurane diterpenoid presented in the plant Isodon eriocalyx var. laxiflora, has been reported to diminish angiogenesis-dependent breast tumor growth. In the present study, the effects of EriB on human breast cancer and its underlying mechanisms were further investigated. The in vitro anti-breast cancer activity of EriB was determined using MCF-7 and MDA-MB-231 cell lines. MDA-MB-231 xenograft model of human breast cancer was also established to explore the anti-tumor effect in vivo. We found that EriB was able to induce apoptosis accompanied by the activation of autophagy, which was evidenced by the increased accumulation of autophagosomes, acidic vesicular organelles formation, the microtubule-associated protein 1A/1B-light chain 3B-II (LC3B-II) conversion from LC3B-I and p62 degradation. Meanwhile, EriB treatment time-dependently decreased the phosphorylation of Akt, mammalian target of rapamycin (mTOR) and ribosomal protein S6 kinase (p70S6K), leading to the inhibition of Akt/mTOR/p70S6K signaling pathway.
3.Effects of three diterpenoids on tumour cell proliferation and telomerase activity.
Yang Y;Sun H;Zhou Y;Ji S;Li M Nat Prod Res. 2009;23(11):1007-12. doi: 10.1080/14786410802295149.
Xerophilusin B (XB), macrocalin B (MB) and eriocalyxin B (EB) belong to ent-kaurene diterpenoids. The inhibition effects of three ent-kaurane compounds on the proliferation of six tumour lines (K562, HL-60, A549, MKN, HCT and CA) were estimated by methyl-thiazol-tetrazolium, and the telomerase activity in K562 cells was measured by the telomeric repeat amplification protocol-enzyme-linked immunosorbent assay. We found that XB, MB and EB could significantly inhibit the proliferation of tumour cells. Within the concentration range of 10(-4)-10(-8) mol L(-1), three ent-kaurane compounds could markedly inhibit the telomerase activity in K562 cells, and their effects on telomerase were exhibited in a dose-dependent manner. Our results demonstrate that XB, MB and EB can inhibit the proliferation of tumour cells and the telomerase activity, which provides data for developing ent-compounds as antitumour drugs.
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CAS 84745-95-9 Eriocalyxin B

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