Identification of actin as a direct proteomic target of berberine using an affinity-based chemical probe and elucidation of its modulatory role in actin assembly.

Despite the diverse pharmacological activities of berberine, including anti-cancer and anti-inflammatory effects, the direct proteomic targets of berberine have remained largely unknown. Here, we have identified actin as a direct proteomic target of berberine using an affinity-based chemical probe. In addition, we found that actin assembly was significantly modulated by berberine in vitro at the biochemical level and cellular level.

[1]  G. Derosa,et al.  Alkaloids in the nature: pharmacological applications in clinical practice of berberine and mate tea. , 2013, Current topics in medicinal chemistry.

[2]  P. Ismail,et al.  Targets and mechanisms of berberine, a natural drug with potential to treat cancer with special focus on breast cancer. , 2014, European journal of pharmacology.

[3]  W. Marsden I and J , 2012 .

[4]  G. Derosa,et al.  Berberine on metabolic and cardiovascular risk factors: an analysis from preclinical evidences to clinical trials , 2012, Expert opinion on biological therapy.

[5]  M. Wright,et al.  Chemical proteomics approaches for identifying the cellular targets of natural products , 2016, Natural product reports.

[6]  K. Chopra,et al.  Current knowledge and pharmacological profile of berberine: An update. , 2015, European journal of pharmacology.

[7]  F. Lu,et al.  The Effects of Berberine on Blood Lipids: A Systemic Review and Meta-Analysis of Randomized Controlled Trials , 2013, Planta Medica.

[8]  S. Maiti,et al.  Binding of berberine to human telomeric quadruplex – spectroscopic, calorimetric and molecular modeling studies , 2008, The FEBS journal.

[9]  B. Leslie,et al.  Identification of the cellular targets of bioactive small organic molecules using affinity reagents. , 2008, Chemical Society reviews.

[10]  T. Kouyama,et al.  Fluorimetry study of N-(1-pyrenyl)iodoacetamide-labelled F-actin. Local structural change of actin protomer both on polymerization and on binding of heavy meromyosin. , 2005, European journal of biochemistry.

[11]  S. Yao,et al.  Target identification of natural products and bioactive compounds using affinity-based probes. , 2016, Natural product reports.

[12]  H. Hosseinzadeh,et al.  Berberis Vulgaris and Berberine: An Update Review , 2016, Phytotherapy research : PTR.

[13]  Herbert Waldmann,et al.  Target identification for small bioactive molecules: finding the needle in the haystack. , 2013, Angewandte Chemie.

[14]  W. Ni,et al.  Berberine as a promising anti-diabetic nephropathy drug: An analysis of its effects and mechanisms. , 2015, European journal of pharmacology.

[15]  A. Catapano,et al.  Berberine, a plant alkaloid with lipid- and glucose-lowering properties: From in vitro evidence to clinical studies. , 2015, Atherosclerosis.

[16]  A. Scovassi,et al.  Berberine: new perspectives for old remedies. , 2012, Biochemical pharmacology.

[17]  Yanyun Zhao,et al.  Meta-analysis of the effect and safety of berberine in the treatment of type 2 diabetes mellitus, hyperlipemia and hypertension. , 2015, Journal of ethnopharmacology.

[18]  I. Singh,et al.  Berberine and its derivatives: a patent review (2009 – 2012) , 2013, Expert opinion on therapeutic patents.

[19]  S. Neidle,et al.  Natural and synthetic G-quadruplex interactive berberine derivatives. , 2006, Bioorganic & medicinal chemistry letters.

[20]  A. Scovassi,et al.  Berberine, an Epiphany Against Cancer , 2014, Molecules.

[21]  D. Nikolić,et al.  Metabolomic Mining of the Botanical Dietary Supplement Wild Yam (Dioscorea villosa L.) , 2013 .

[22]  M. Abdollahi,et al.  Berberine and neurodegeneration: A review of literature , 2015, Pharmacological reports : PR.

[23]  Jin Xiang,et al.  Tumor suppressor berberine binds VASP to inhibit cell migration in basal-like breast cancer , 2016, Oncotarget.

[24]  M. Yuen,et al.  Berberine and Coptidis Rhizoma as potential anticancer agents: Recent updates and future perspectives. , 2015, Journal of ethnopharmacology.

[25]  Chih-Yu Lo,et al.  Synthesis and anticancer activity of a novel series of 9-O-substituted berberine derivatives: a lipophilic substitute role. , 2013, Bioorganic & medicinal chemistry letters.

[26]  S. Saeidnia,et al.  Phytochemistry and Pharmacology of Berberis Species , 2014, Pharmacognosy reviews.

[27]  Harald Schwalbe,et al.  Spectroscopic, molecular modeling, and NMR-spectroscopic investigation of the binding mode of the natural alkaloids berberine and sanguinarine to human telomeric G-quadruplex DNA. , 2012, ACS chemical biology.

[28]  Kuang-Chi Lai,et al.  Berberine suppresses in vitro migration and invasion of human SCC-4 tongue squamous cancer cells through the inhibitions of FAK, IKK, NF-kappaB, u-PA and MMP-2 and -9. , 2009, Cancer letters.