16 December 2021

Natural products: Xanthones

Xanthones are a group of naturally produced chemical compounds with a wide range of pharmacological activities


Phenols are a broad class of natural products with phenolic hydroxyl groups (phenolic acids, flavonoids, xanthones, coumarins, lignans, among others), which have antioxidant and other pharmacological activities. Xanthones are a class of simple tricyclic compounds, which are mainly secondary metabolites from plants (such as mangosteen, lichen) and microorganisms (such as bacteria and fungi). These compounds have a wide range of pharmacological activities, including antihypertensive, antioxidation, antithrombotic, and anticancer activities.

View a selection of xanthones from MedChem Express here:

Mangiferin (HY-N0290)
Activator of Nrf2 that suppresses nuclear translocation of the NF-κB subunits p65 and p50. Exhibits antioxidant, antidiabetic, antihyperuricemic, antiviral, anticancer and anti-inflammatory activities.

Mangiferin Chemical Structure (CAS: 4773-96-0)

Alpha-Mangostin (HY-N0328)
Inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM. Exerts antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects.

alpha-Mangostin Chemical Structure (CAS: 6147-11-1)

Gambogic Acid (HY-N0087)
Antagonist of antiapoptotic Bcl-2 family proteins against Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 (IC50s ranging from 0.66 to 2.02 μM). Exerts anti-cancer, anti-inflammatory, antioxidant, anti-bacterial effects.

Gambogic Acid Chemical Structure (CAS: 2752-65-0)

Garcinone D (HY-N6953)
STAT3 activator that increases the protein levels of p-STAT3, Cyclin D1, Nrf2, and HO-1.

Garcinone D Chemical Structure (CAS: 107390-08-9)

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References

  • Yu H, Hou G, Cao J, Yin Y, Zhao Y, Cheng L. Mangiferin alleviates mitochondrial ros in nucleus pulposus cells and protects against intervertebral disc degeneration via suppression of nf-κb signaling pathway. Oxid Med Cell Longev. 2021;2021:6632786.
  • He L, Bao T, Yang Y, et al. Exploring the pathogenesis of type 2 diabetes mellitus intestinal damp-heat syndrome and the therapeutic effect of Gegen Qinlian Decoction from the perspective of exosomal miRNA. J Ethnopharmacol. Published online November 8, 2021:114786.
  • Fang S, Yu X, Ding H, Han J, Feng J. Effects of intracellular iron overload on cell death and identification of potent cell death inhibitors. Biochem Biophys Res Commun. 2018;503(1):297-303.
  • Shi Y, Fan Y, Hu Y, et al. α-Mangostin suppresses the de novo lipogenesis and enhances the chemotherapeutic response to gemcitabine in gallbladder carcinoma cells via targeting the AMPK/SREBP1 cascades. J Cell Mol Med. 2020;24(1):760-771.
  • Wang LH, Li Y, Yang SN, et al. Gambogic acid synergistically potentiates cisplatin-induced apoptosis in non-small-cell lung cancer through suppressing NF-κB and MAPK/HO-1 signalling. Br J Cancer. 2014;110(2):341-352.
  • Yang X, Wang S, Ouyang Y, et al. Garcinone D, a natural xanthone promotes C17.2 neural stem cell proliferation: Possible involvement of STAT3/Cyclin D1 pathway and Nrf2/HO-1 pathway. Neurosci Lett. 2016;626:6-12.

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