Antimicrobial
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Anti-mycobacterial |
Wang Y et al., 2012Wang Y, Fu H, Li Y, Jiang J, Song D. Synthesis and biological evaluation of 8-substituted berberine derivatives as novel anti-mycobacterial agents. Acta Pharm Sin B. 2012;2(6): 581-587., Mahapatra A et al., 2014Mahapatra A, Maheswari V, Kalia NP, Rajput VS and Khan IA. Synthesis and antitubercular activity of berberine derivatives. Chem Nat Compd. 2014;50(2):321-325.
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Antibacterial |
Gao WW et al., 2018Gao WW, Gopala L, Bheemanaboina YRR, Zhang GB, Li S, Zhou CH, et al. Discovery of 2-aminothiazolyl berberine derivatives as effective antibacterial agents toward clinically drug-resistant Gram-negative Acinetobacter baumanii. Eur J Med Chem. 2018;146:15-37., Sun N et al., 2014Sun N, Chan FY, Lu YJ, Neves MAC, Lui HK, Wang Y, et al. Rational Design of berberine-based FtsZ inhibitors with broad-spectrum antibacterial activity. PloS One . 2014;9(5):e97514., Jeyakkumar P et al., 2016Jeyakkumar P, Zhang L, Avula SR, Zhou CH. Design, synthesis and biological evaluation of berberine-benzimidazole hybrids as new type of potentially DNA-targeting antimicrobial agents. Eur. J Med Chem. 2016;122:205-15.
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Antifungal |
Ling Y et al., 2018Ling YA, Ling-Ling WU, Qian LI, Qin-Mei HU, ZHANG SY, Kang LI, et al. Novel berberine derivatives: Design, synthesis, antimicrobial effects, and molecular docking studies. CJNM. 2018; 16(10): 0774-0781.
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Antiprotozoal |
Bahar M et al., 2011Bahar M, Deng Y, Zhu X, He S, Pandharkar T, Drew ME, et al. Potent antiprotozoal activity of a novel semi-synthetic berberine derivative. Bioorg Med Chem Lett. 2011;21(9): 2606-2610.
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Antioxidant
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Mistry B et al., 2017Mistry B, Patel RV, Keum YS, Kim DH. Synthesis of N-Mannich bases of berberine linking piperazine moieties revealing anticancer and antioxidant effects. Saudi J Biol sci. 2017;24(1):36-44., Pongkittiphan V, Chavasiri W, Supabphol R, 2015Pongkittiphan V, Chavasiri W, Supabphol R. Antioxidant effect of berberine and its phenolic derivatives against human fibrosarcoma cells. Asian Pac J Cancer Prev. 2015;16(13): 5371-5376., Roselli M et al., 2016Roselli M, Cavalluzzi MM, Bruno C, Lovece A, Carocci A, Franchini C, et al. Synthesis and evaluation of berberine derivatives and analogs as potential antiacetylcholinesterase and antioxidant agents. Phytochem Lett. 2016;18:150-156.
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Lipid-lowering effect/atherosclerosis |
Chen J et al., 2014Chen J, Cao J, Fang L, Liu B, Zhou Q, Sun Y, et al. Berberine derivatives reduce atherosclerotic plaque size and vulnerability in apoE-/- mice. J.Transl.Med. 2014;12(1): 326-339.
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Anticancer
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Liver, breast, pancreatic cancer |
Jin X et al., 2014Jin X, Yan TH, Yan L, Li Q, Wang RL, Hu ZL, et al. Design, synthesis, and anticancer activity of novel berberine derivatives prepared via CuAAC “click” chemistry as potential anticancer agents. Drug Des Devel Ther. 2014;8:1047-1059.
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Colon cancer |
Albring KF et al., 2013Albring KF, Weidemuller J, Mittag S, Weiske J, Geroni MC, Lombardi P, et al. Berberine acts as a natural inhibitor of Wnt/β-catenin signaling-Identification of more active 13-arylalkyl derivatives. Biofactors. 2013;39(6):652-662., Guaman Ortiz LM et al., 2014Guaman Ortiz LM, Tillhon M, Parks M, Dutto I, Prosperi E, Savio M, et al. Multiple effects of berberine derivatives on colon cancer cells. Biomed Res Int. 2014;2014:1-12., Guamán Ortiz LM et al., 2015Guaman Ortiz LM, Croce AL, Aredia F, Sapienza S, Fiorillo G, Syeda TM, et al. Effect of new berberine derivatives on colon cancer cells. Acta Biochim Biophys Sin (Shanghai). 2015;47(10):824-833., |
Histone acetyltransferase (HAT) dysfunction treatment |
Yang Z et al., 2018Yang Z, Zhang Y, Chen X, Li W, Li GB, Wu Y, et al. Total Synthesis and Evaluation of B-Homo Palmatine and Berberine Derivatives as p300 Histone Acetyltransferase Inhibitors. Eur J Org. Chem. 2018;(8):1041-1052.
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G-quadruplex telomeric DNA stabilization |
Ma Y et al., 2009Ma Y, Ou TM, Tan JH, Hou JQ, Huang SL, Gu LQ, et al. Synthesis and evaluation of 9-O-substituted berberine derivatives containing aza-aromatic terminal group as highly selective telomeric G-quadruplex stabilizing ligands. Bioorg Med Chem Lett . 2009;19(13):3414-3417.
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Breast cancer |
Pierpaoli E et al., 2013Pierpaol E, Arcamone AG, Buzzetti F, Lombardi P, Salvatore C, Provinciali M. Antitumor effect of novel berberine derivatives in breast cancer cells. Biofactors . 2013;39(6): 672-679.
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inhibitor of MAPK (mitogen-activated protein kinase) |
Kim N et al., 2014Kim N, Park J, Gadhe CG, Cho SJ, Oh Y, Kim D, et al. A Protoberberine derivative HWY336 selectively inhibits MKK4 and MKK7 in mammalian cells: The importance of activation loop on selectivity. PloS One . 2014;9(4):e91037.
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Skin cancer |
(Kaboli PJ, Ismail P, Ling K-H, 2018Kaboli PJ, Ismail P, Ling KH. Molecular modeling, dynamics simulations, and binding efficiency of berberine derivatives: A new group of RAF inhibitors for cancer treatment. PloS One. 2018;13(3):e0193941.) |
Cancer immunotherapy |
Wang YX et al., 2018Wang YX, Pang WQ, Zeng QX, Deng ZS, Fan TY, Jiang JD, et al. Synthesis and biological evaluation of new berberine derivatives as cancer immunotherapy agents through targeting IDO1. Eur J Med Chem . 2018;143:1858-1868.
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Antidiabetic
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Ren G et al., 2017Ren G, Wang YX, Li YH, Song DQ, Kong WJ, Jiang JD. Structure-activity relationship of berberine derivatives for their glucose-lowering activities. Int J Clin Exp Med. 2017;10(3):s5054-5060., Turner N et al., 2008Turner N, Li JY, Gosby A, To SWC, Cheng Z, Miyoshi H, et al. Berberine and its more biologically available derivative, dihydroberberine, inhibit mitochondrial respiratory complex I: a mechanism for the action of berberine to activate AMP-activated protein kinase and improve insulin action. Diabetes. 2008;57(5):1414-1418.
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Anti-inflammatory
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Wang YX et al., 2017Wang YX, Liu L, Zeng QX, Fan TY, Jiang JD, Deng HB, et al. Synthesis and identification of novel berberine derivatives as potent inhibitor against TNF-α-induced NF-κB activation. Molecules . 2017;22(8):1257-1271., Huang MY et al., 2016Huang MY, Lin J, Huang ZJ, Xu HG, Hong J, Sun PH, et al. Design, synthesis and anti-inflammatory effects of novel 9-O-substituted-berberine derivatives. MedChemComm. 2016;7(4):658-666., Chen YY et al., 2017Chen YY, Li RY, Shi MJ, Zhao YX, Yan Y, Xu XX, et al. Demethyleneberberine alleviates inflammatory bowel disease in mice through regulating NF-κB signaling and T-helper cell homeostasis. Inflamm Res. 2017;66(2):187-196., Deng X et al., 2012Deng X, Zhao X, Han J, Wang J, Huang W, Qian H, et al. Synthesis and biological evaluation of berberine derivatives as IBS modulator. Lett Drug Des Discov. 2012;9(5):489-493.
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Hepatic effects
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Wang Y et al., 2016Wang Y, Zhao Z, Yan Y, Qiang X, Zhou C, Li R, et al. Demethyleneberberine protects against hepatic fibrosis in mice by modulating NF-κB signaling. Int J Mol Sci. 2016;17(7):1036-1051., Zhang P et al., 2015Zhang P, Qiang X, Zhang M, Ma D, Zhao Z, Zhou C, et al. Demethyleneberberine, a natural mitochondria-targeted antioxidant, inhibits mitochondrial dysfunction, oxidative stress, and steatosis in alcoholic liver disease mouse model. J Pharmacol Exp Ther. 2015;352(1):139-147., Qiang X et al., 2015Qiang X, Xu L, Zhang P, Zhang Y, Zhou H, et al. Demethyleneberberine Attenuates Free Fatty Acid-And High Fat Diet-Induced Hepatic Lipotoxicity By Activating AMP-Activated Protein Kinase. FASEB J. 2015;29(1suppl):885-7., Al LX, 2016, |
Neurodegenerative diseases
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Huang L et al., 2010Huang L, Luo Z, He F, Lu J, Li X. Synthesis and biological evaluation of a new series of berberine derivatives as dual inhibitors of acetylcholinesterase and butyrylcholinesterase. Bioorg Med Chem. 2010;18(12):4475-4484., Ribaudo G et al., 2018Ribaudo G, Zanforlin E, Canton M, Bova S, Zagotto G. Preliminary studies of berberine and its semi-synthetic derivatives as a promising class of multi-target anti-parkinson agents. Nat Prod Res. 2018;32(12):1395-1401., Huang L et al., 2010Huang L, Luo Z, He F, Lu J, Li X. Synthesis and biological evaluation of a new series of berberine derivatives as dual inhibitors of acetylcholinesterase and butyrylcholinesterase. Bioorg Med Chem. 2010;18(12):4475-4484.
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Osteoporosis
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Han Y, Kim MJ, Lee KY, 2018Han Y, Kim MJ, Lee KY. Berberine derivative, Q8, stimulates osteogenic differentiation. Biochem Biophys Res. Commun. 2018;504(1):340-5.
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