Berberine and derivatives

Berberine is an alkaloid compound isolated from medicinal herbs and exhibits extensive pharmacological activity. Although the molecular basis of its biological activity is still the subject of debate, information on the alkaloid continues to accumulate, data that can be used for future clinical applications. Among the therapeutic applications that have opened greater expectations and interest among researchers, are those related to cardiovascular disease, metabolic syndrome and cancer.  However, their low absorption and bioavailability limit their therapeutic use, and in recent years derivatives have been designed to improve their pharmacological properties for clinical use.

Relevant publications in the topic


Berberine targets KIF20A and CCNE2 to inhibit the progression of nonsmall cell lung cancer via the PI3K/AKT pathway.

Wang Q, Wu H, Wu Q, Zhong S. 
Drug Dev Res. Aug 2023. doi: 10.1002/ddr.22061.

Nonsmall cell lung cancer (NSCLC) is the main type of lung cancer, accounting for approximately 85%. Berberine (BBR), a commonly used traditional Chinese medicine, has been reported to exhibit a potential antitumor effect in various cancers. In this... see publication


Berberine-mediated Ferroptosis through System Xc-/GSH/GPX4 Axis Inhibits Metastasis of Nasopharyngeal Carcinoma.

Wu Y, Jia Q, Tang Q, Deng H, He Y, Tang F. 
J Cancer. 2024. doi: 10.7150/jca.90574.

Nasopharyngeal carcinoma (NPC) is a malignant tumor that is highly prevalent in Southeast China, and its metastasis remains an unresolved clinical problem. Ferroptosis, a type of nonapoptotic cell death, is a critical pathway in tumor metastasis.... see publication


Antitumor Effect of Berberine Analogs in a Canine Mammary Tumor Cell Line and in Zebrafish Reporters via Wnt/β-Catenin and Hippo Pathways.

Sammarco A, Beffagna G, Sacchetto R, Vettori A, Bonsembiante F, Scarin G, Gelain ME, Cavicchioli L, Ferro S, Geroni C, Lombardi P, Zappulli V. 
Biomedicines. Dec 2023.

The heterogeneous nature of human breast cancer (HBC) can still lead to therapy inefficacy and high lethality, and new therapeutics as well as new spontaneous animal models are needed to benefit translational HBC research. Dogs are primarily investigated... see publication


Clonal gene signatures predict prognosis in mesothelioma and lung adenocarcinoma.

Lin Y, Burt BM, Lee HS, Nguyen TT, Jang HJ, Lee C, Hong W, Ripley RT, Amos CI, Cheng C. 
NPJ Precis Oncol. Feb 2024.

Malignant pleural mesothelioma (MPM) is a rare but lethal pleural cancer with high intratumor heterogeneity (ITH). A recent study in lung adenocarcinoma has developed a clonal gene signature (ORACLE) from multiregional transcriptomic data and demonstrated... see publication


Berberine improved the microbiota in lung tissue of colon cancer and reversed the bronchial epithelial cell changes caused by cancer cells.

Yang W, Yang T, Huang B, Chen Z, Liu H, Huang C. 
Heliyon. Jan 2024.

The lung is a common organ for colon cancer metastasis, and the objective of this experiment was to explore the protective effect of berberine on lung tissue or alveolar epithelial cells induced by colon cancer.Thirty-six BALB/c nude mice were used... see publication


Cancer Pathways Targeted by Berberine: Role of microRNAs.

Ali M, Mishra D, Singh RP. 
Curr Med Chem. Jan 2024. doi: 10.2174/0109298673275121231228124031.

Cancer is a complex and heterogeneous malignant disease. Due to its multifactorial nature, including progressive changes in genetic, epigenetic, transcript, and protein levels, conventional therapeutics fail to save cancer patients. Evidence indicates... see publication


Identification of Autophagy-Related Targets of Berberine against Non-Small Cell Lung Cancer and Their Correlation with Immune Cell Infiltration By Combining Network Pharmacology, Molecular Docking, and Experimental Verification.

Xu L. 
Crit Rev Immunol. 2023. doi: 10.1615/CritRevImmunol.2023049923.

Non-small cell lung cancer (NSCLC) is the most common lung cancer type with high incidence. This study aimed to reveal the anti-NSCLC mechanisms of berberine and identify novel therapeutic targets.Berberine-related targets were acquired from SuperPred,... see publication


Multiomic analysis of malignant pleural mesothelioma identifies molecular axes and specialized tumor profiles driving intertumor heterogeneity.

Mangiante L, Alcala N, Sexton-Oates A, Di Genova A, Gonzalez-Perez A, Khandekar A, Bergstrom EN, Kim J, Liu X, Blazquez-Encinas R, Giacobi C, Le Stang N, Boyault S, Cuenin C, Tabone-Eglinger S, Damiola F, Voegele C, Ardin M, Michallet MC, Soudade L, Delhomme TM, Poret A, Brevet M, Copin MC, Giusiano-Courcambeck S, Damotte D, Girard C, Hofman V, Hofman P, Mouroux J, Cohen C, Lacomme S, Mazieres J, de Montpreville VT, Perrin C, Planchard G, Rousseau N, Rouquette I, Sagan C, Scherpereel A, Thivolet F, Vignaud JM, Jean D, Ilg AGS, Olaso R, Meyer V, Boland-Auge A, Deleuze JF, Altmuller J, Nuernberg P, Ibáñez-Costa A, Castaño JP, Lantuejoul S, Ghantous A, Maussion C, Courtiol P, Hernandez-Vargas H, Caux C, Girard N, Lopez-Bigas N, Alexandrov LB, Galateau-Salle F, Foll M, Fernandez-Cuesta L. 
Nat Genet. Mar 2023. doi: 10.1038/s41588-023-01321-1.

Malignant pleural mesothelioma (MPM) is an aggressive cancer with rising incidence and challenging clinical management. Through a large series of whole-genome sequencing data, integrated with transcriptomic and epigenomic data using multiomics factor... see publication


Multi-Target Potential of Berberine as an Antineoplastic and Antimetastatic Agent: A Special Focus on Lung Cancer Treatment

Achi IT, Sarbadhikary P, George BP, Abrahamse H. 
Cells. Oct 2022.

Despite therapeutic advancements, lung cancer remains the principal cause of cancer mortality in a global scenario. The increased incidence of tumor reoccurrence and progression and the highly metastatic nature of lung cancer are of great concern... see publication


Berberine Inhibits FOXM1 Dependent Transcriptional Regulation of POLE2 and Interferes With the Survival of Lung Adenocarcinoma.

Ni L, Sun P, Fan X, Li Z, Ren H, Li J. 
Front Pharmacol. 2021. doi: 10.3389/fphar.2021.775514.

Background: Berberine is one of the most interesting and promising natural anticancer drugs. POLE2 is involved in many cellular functions such as DNA replication and is highly expressed in a variety of cancers. However, the specific molecular mechanism... see publication


APR-246—The Mutant TP53 Reactivator—Increases the Effectiveness of Berberine and Modified Berberines to Inhibit the Proliferation of Pancreatic Cancer Cells

McCubrey JA, Abrams SL, Steelman LS, Cocco L, Ratti S, Martelli AM, Lombardi P, Gizak A, Duda P. 
Biomolecules. Feb 2022.

Pancreatic ductal adenocarcinoma (PDAC) is the most common form of pancreatic cancer. In ~75% of PDAC, the tumor suppressor TP53 gene is mutated. Novel approaches to treat cancer involve compounds called mutant TP53 reactivators. They interact with... see publication


Effects of the MDM2 inhibitor Nutlin-3a on sensitivity of pancreatic cancer cells to berberine and modified berberines in the presence and absence of WT-TP53.

Abrams SL, Akula SM, Steelman LS, Follo ML, Cocco L, Ratti S, Martelli AM, Libra M, Falzone L, Candido S, Montalto G, Cervello M, Lombardi P, McCubrey JA. 
Adv Biol Regul. Jan 2022.

Approaches to improve pancreatic cancer therapy are essential as this disease has a very bleak outcome. Approximately 80% of pancreatic cancers are pancreatic ductal adenocarcinomas (PDAC). A key regulatory gene frequently mutated (∼75%) in PDAC... see publication


An insight into the medicinal attributes of berberine derivatives: A review

Gaba S, Saini A, Singh G, Monga V. 
Bioorg Med Chem. 05 2021.

In the last few decades, traditional natural products have been the center of attention for the scientific community and exploration of their therapeutic abilities is proceeding perpetually. Berberine, with remarkable therapeutic diversity, is a plant... see publication


Enhanced Clearance of Neurotoxic Misfolded Proteins by the Natural Compound Berberine and Its Derivatives.

Rusmini P, Cristofani R, Tedesco B, Ferrari V, Messi E, Piccolella M, Casarotto E, Chierichetti M, Cicardi ME, Galbiati M, Geroni C, Lombardi P, Crippa V, Poletti A. 
Int J Mol Sci. May 2020.

Accumulation of misfolded proteins is a common hallmark of several neurodegenerative disorders (NDs) which results from a failure or an impairment of the protein quality control (PQC) system. The PQC system is composed by chaperones and the degradative... see publication


Abilities of berberine and chemically modified berberines to inhibit proliferation of pancreatic cancer cells.

Abrams SL, Follo MY, Steelman LS, Lertpiriyapong K, Cocco L, Ratti S, Martelli AM, Candido S, Libra M, Murata RM, Rosalen PL, Montalto G, Cervello M, Gizak A, Rakus D, Mao W, Lombardi P, McCubrey JA. 
Adv Biol Regul. 01 2019.

Berberine (BBR) is a common nutraceutical consumed by millions worldwide. BBR has many different effects on human health, e.g., diabetes, diarrhea, inflammation and now more recently it has been proposed to have potent anti-cancer effects. BBR has... see publication


Abilities of berberine and chemically modified berberines to interact with metformin and inhibit proliferation of pancreatic cancer cells.

Akula SM, Candido S, Libra M, Abrams SL, Steelman LS, Lertpiriyapong K, Ramazzotti G, Ratti S, Follo MY, Martelli AM, Murata RM, Rosalen PL, Bueno-Silva B, Matias de Alencar S, Montalto G, Cervello M, Gizak A, Rakus D, Mao W, Lin HL, Lombardi P, McCubrey JA. 
Adv Biol Regul. 08 2019.

Pancreatic cancer is devastating cancer worldwide with few if any truly effective therapies. Pancreatic cancer has an increasing incidence and may become the second leading cause of death from cancer. Novel, more effective therapeutic approaches are... see publication


Janus nanocarrier-based co-delivery of doxorubicin and berberine weakens chemotherapy-exacerbated hepatocellular carcinoma recurrence

Zhang F, Jia Y, Zheng X, Shao D, Zhao Y, Wang Z, Dawulieti J, Liu W, Sun M, Sun W, Pan Y, Cui L, Wang Y, He K, Zhang M, Li J, Dong WF, Chen L. 
Acta Biomater. Sep 2019.

Despite the rapid progress which has been made in hepatocellular carcinoma (HCC) chemotherapeutics, recurrence of liver cancer still remains a barrier to achieve satisfying prognosis. Herein, we aimed to decipher the role of berberine (BER) in chemotherapy-exacerbated... see publication


Effects of berberine, curcumin, resveratrol alone and in combination with chemotherapeutic drugs and signal transduction inhibitors on cancer cells-Power of nutraceuticals

McCubrey JA, Abrams SL, Lertpiriyapong K, Cocco L, Ratti S, Martelli AM, Candido S, Libra M, Murata RM, Rosalen PL, Lombardi P, Montalto G, Cervello M, Gizak A, Rakus D, Steelman LS. 
Adv Biol Regul. Jan 2018.

Over the past fifty years, society has become aware of the importance of a healthy diet in terms of human fitness and longevity. More recently, the concept of the beneficial effects of certain components of our diet and other compounds, that are consumed... see publication


Role of 13-(di)phenylalkyl berberine derivatives in the modulation of the activity of human topoisomerase IB.

Vieira S, Castelli S, Falconi M, Takarada J, Fiorillo G, Buzzetti F, Lombardi P, Desideri A. 
Int J Biol Macromol. 2015.

Topoisomerases IB are anticancer and antimicrobial targets whose inhibition by several natural and non-natural compounds has been documented. The inhibition effect by berberine and some 13-(di)phenylalkyl berberine derivatives has been tested towards... see publication


Multiple effects of berberine derivatives on colon cancer cells.

Guamán Ortiz LM, Tillhon M, Parks M, Dutto I, Prosperi E, Savio M, Arcamone AG, Buzzetti F, Lombardi P, Scovassi AI. 
Biomed Res Int. 2014.

The pharmacological use of the plant alkaloid berberine is based on its antibacterial and anti-inflammatory properties; recently, anticancer activity has been attributed to this compound. To exploit this interesting feature, we synthesized three berberine... see publication


Berberine acts as a natural inhibitor of Wnt/β-catenin signaling--identification of more active 13-arylalkyl derivatives.

Albring KF, Weidemüller J, Mittag S, Weiske J, Friedrich K, Geroni MC, Lombardi P, Huber O. 
Biofactors 2013.

Aberrant activation of the canonical Wnt/β-catenin signaling pathway has been reported for numerous tumors of different origins. In most cases, mutations in components of the Wnt signaling pathway or in β-catenin itself were detected which ultimately... see publication


Antitumor effect of novel berberine derivatives in breast cancer cells.

Pierpaoli E, Arcamone AG, Buzzetti F, Lombardi P, Salvatore C, Provinciali M. 
Biofactors 2013.

Breast cancer is the most common malignancy and the most common cause of cancer death in elderly women. Chemoprevention with dietary compounds and their synthetic analogs has emerged as an attractive strategy to prevent carcinogenic progression to... see publication


Berberine: new perspectives for old remedies.

Tillhon M, Guamán Ortiz LM, Lombardi P, Scovassi AI. 
Biochem Pharmacol. 2012.

Chemical compounds derived from plants have been used since the origin of human beings to counteract a number of diseases. Among them, the natural isoquinoline alkaloid berberine has been employed in Ayurvedic and Chinese Medicine for hundreds of... see publication

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