Discovery of novel berberine imidazoles as safe antimicrobial agents by down regulating ROS generation

Wen, Siqi; Jeyakkumar, Ponmani; Avula, Srinivasa Rao; Zhang, Ling; Zhou, Cheng‐He

doi:10.1016/j.bmcl.2016.04.070

Cited by 95 publications

(33 citation statements)

References 40 publications

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“…Berberine is a yellow plant isoquinoline alkaloid isolated from herb medicine Coptidis Rhizom, Hydrastis canadensis, and berberis that plays an important role in neuroprotection against pro-inflammatory responses and escape from apoptotic signals ( Refaat et al, 2013 ). A large number of pharmacological and biological properties of berberine have been identified including anti carcinogenic ( Lu et al, 2016 ), anti-inflammatory ( Guo et al, 2016 ; Woo et al, 2016 ), anti-microbial ( Wen et al, 2016 ), antihypertensive ( Saki et al, 2016 ) and cholesterol lowering effects ( Wang et al, 2014 ).…”

Section: Introductionmentioning

confidence: 99%

Berberine confers neuroprotection in coping with focal cerebral ischemia by targeting inflammatory cytokines

Maleki

Aboutaleb

Souri

2018

Journal of Chemical Neuroanatomy

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Section: Introductionmentioning

confidence: 99%

Berberine confers neuroprotection in coping with focal cerebral ischemia by targeting inflammatory cytokines

Maleki

Aboutaleb

Souri

2018

Journal of Chemical Neuroanatomy

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“…BBR is widely used for gastrointestinal infections and various inflammations in Asian countries [ 12 ]. It has many pharmacological actions, including activity against tumors [ 13 , 14 ], microbe [ 15 ], inflammation [ 15 , 16 ], neurodegenerative disease [ 17 , 18 ] and other diseases. Recent studies have found that BBR exerts cytotoxicity and inhibits telomerase and topoisomerase, promotes the proliferation apoptosis in human leukemia cells by specifically binding to oligonucleotides or polymorphic nucleic acid and by stabilizing DNA triplexes or G-quadruplexes; the electrostatic interactions may be quantified in terms of the Hill model of cooperative interactions [ 19 – 22 ].…”

Section: Introductionmentioning

confidence: 99%

Self-nanoemulsifying system improves oral absorption and enhances anti-acute myeloid leukemia activity of berberine

Yang

Shen

et al. 2018

J Nanobiotechnol

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BackgroundRecently, we found that berberine (BBR) exerts anti-acute myeloid leukemia activity, particularly toward high-risk and relapsed/refractory acute myeloid leukemia MV4-11 cells in vitro. However, the poor water solubility and low bioavailability observed with oral BBR administration has limited its clinical use. Therefore, we design and develop a novel oil-in-water self-nanoemulsifying system for BBR (BBR SNE) to improve oral bioavailability and enhance BBR efficacy against acute myeloid leukemia by greatly improving its solubility.ResultsThis system (size 23.50 ± 1.67 nm, zeta potential − 3.35 ± 0.03 mV) was prepared with RH40 (surfactant), 1,2-propanediol (co-surfactant), squalene (oil) and BBR using low-energy emulsification methods. The system loaded BBR successfully according to thermal gravimetric, differential scanning calorimetry, and Fourier transform infrared spectroscopy analyses. The release profile results showed that BBR SNE released BBR more slowly than BBR solution. The relative oral bioavailability of this novel system in rabbits was significantly enhanced by 3.41-fold over that of BBR. Furthermore, Caco-2 cell monolayer transport studies showed that this system could help enhance permeation and prevent efflux of BBR. Importantly, mice with BBR SNE treatment had significantly longer survival time than BBR-treated mice (P < 0.001) in an MV4-11 engrafted leukemia murine model.ConclusionsThese studies confirmed that BBR SNE is a promising therapy for acute myeloid leukemia.Electronic supplementary materialThe online version of this article (10.1186/s12951-018-0402-x) contains supplementary material, which is available to authorized users.

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“…BBH has a variety of pharmacological activities such as antitumor (James et al, 2011;Tan et al, 2011;Cheng et al, 2015), antimicrobial (Zhang et al, 2010;Sun et al, 2014;Wen et al, 2016), antiinflammation (Lee et al, 2007;Wen et al, 2016), and reduce irritable bowel syndrome (Chen et al, 2015;Habtemariam, 2016). However, oral administration of BBH exhibited low bioavailability and poor stability (Tan et al, 2011;Liu et al, 2014) mainly due to its hydrophobic properties resulted from the chemical structure, which contains two methoxy groups and a quaternary ammonium cation.…”

Section: Introductionmentioning

confidence: 99%

Nanoemulsion-based delivery system for enhanced oral bioavailability and Caco-2 cell monolayers permeability of berberine hydrochloride

Lü

et al. 2017

Drug Delivery

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Berberine hydrochloride (BBH) has a variety of pharmacological activities such as antitumor, antimicrobial, anti-inflammation, and reduce irritable bowel syndrome. However, poor stability and low oral bioavailability limited its usage. Herein, an oil-in-water nanoemulsion system of BBH was developed to improve its stability and oral bioavailability. The pseudoternary phase diagrams were constructed for the determination of composition of various nanoemulsions. The nanoemulsions of BBH composed of Labrafil M 1944 CS (oil phase), RH-40 (surfactant), glycerin (co-surfactant), and water (aqueous phase). The O/W nanoemulsion of BBH showed a relative bioavailability of 440.40% compared with unencapsulated BBH and was stable in our 6-month stability study. Further, there was a significant increase in intestinal permeability of BBH as assessed by Caco-2 cell monolayers and a significant reduction in efflux of BBH by the multidrug efflux pump P-glycoprotein. This study confirmed that the nanoemulsion formulation could be used as an alternative oral formulation of BBH to improve its stability, oral bioavailability and permeability.ARTICLE HISTORY

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Discovery of novel berberine imidazoles as safe antimicrobial agents by down regulating ROS generation

Cited by 95 publications

References 40 publications

Berberine confers neuroprotection in coping with focal cerebral ischemia by targeting inflammatory cytokines

Berberine confers neuroprotection in coping with focal cerebral ischemia by targeting inflammatory cytokines

Self-nanoemulsifying system improves oral absorption and enhances anti-acute myeloid leukemia activity of berberine

Nanoemulsion-based delivery system for enhanced oral bioavailability and Caco-2 cell monolayers permeability of berberine hydrochloride

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