Berberine, an Epiphany Against Cancer

Ortiz, Luis Miguel Guamán; Lombardi, Paolo; Tillhon, Micol; Scovassi, Anna Ivana

doi:10.3390/molecules190812349

Cited by 227 publications

(108 citation statements)

References 114 publications

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“…Several studies on different cancer cells treated with BBR reported its ability to regulate (up/down) different proteins that trigger apoptosis or autophagy [5]. We previously found that some BBR derivatives (NAX012, NAX014, and NAX018, characterized by arylalkyl groups bonded to the C-13 position) are able to induce DNA damage and cell cycle arrest, inhibit cellular proliferation, and promote cell death through apoptosis in a p53-dependent manner [2].…”

Section: Discussionmentioning

confidence: 99%

“…Of note, the structure of BBR makes it an attractive natural lead compound for the introduction of various chemical modifications in appropriate positions of the skeleton [4]. In particular, arylalkyl derivatives of BBR characterized by aromatic groups bonded to the C-13 position of the parent BBR via a linker of variable length have been reported to have anticancer properties [1,2,5,6]. Recently, we analyzed a first set of BBR derivatives with a 13-(di) arylalkyl modification, which were demonstrated to exert anticancer effects on human p53 wt colon cancer cell lines [2].…”

Section: Introductionmentioning

confidence: 99%

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Effect of new berberine derivatives on colon cancer cells

Ortiz¹,

Croce²,

Aredia³

et al. 2015

ABBS

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The natural alkaloid berberine has been recently described as a promising anticancer drug. In order to improve its efficacy and bioavailability, several derivatives have been designed and synthesized and found to be even more potent than the lead compound. Among the series of berberine derivatives we have produced, five compounds were identified to be able to heavily affect the proliferation of human HCT116 and SW613-B3 colon carcinoma cell lines. Remarkably, these active compounds exhibit high fluorescence emission property and ability to induce autophagy.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Effect of new berberine derivatives on colon cancer cells

Ortiz¹,

Croce²,

Aredia³

et al. 2015

ABBS

Self Cite

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“…Berberine was found to inhibit tumor cell proliferation and exhibited cytotoxicity towards tumor cells [96-104]. Berberine was shown inducing autophagic and apoptotic cell death in hepatocellular carcinoma HepG2, MHCC97-1, and SMMC7721 cells, as indicated in [101].…”

Section: Anticancer Natural Compounds and Autophagymentioning

confidence: 99%

Natural Compounds As Modulators of Non-apoptotic Cell Death in Cancer Cells

Guamán-Ortiz

Orellana²,

Ratovitski³

2017

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Cell death is an innate capability of cells to be removed from microenvironment, if and when they are damaged by multiple stresses. Cell death is often regulated by multiple molecular pathways and mechanism, including apoptosis, autophagy, and necroptosis. The molecular network underlying these processes is often intertwined and one pathway can dynamically shift to another one acquiring certain protein components, in particular upon treatment with various drugs. The strategy to treat human cancer ultimately relies on the ability of anticancer therapeutics to induce tumor-specific cell death, while leaving normal adjacent cells undamaged. However, tumor cells often develop the resistance to the drug-induced cell death, thus representing a great challenge for the anticancer approaches. Numerous compounds originated from the natural sources and biopharmaceutical industries are applied today in clinics showing advantageous results. However, some exhibit serious toxic side effects. Thus, novel effective therapeutic approaches in treating cancers are continued to be developed. Natural compounds with anticancer activity have gained a great interest among researchers and clinicians alike since they have shown more favorable safety and efficacy then the synthetic marketed drugs. Numerous studies in vitro and in vivo have found that several natural compounds display promising anticancer potentials. This review underlines certain information regarding the role of natural compounds from plants, microorganisms and sea life forms, which are able to induce non-apoptotic cell death in tumor cells, namely autophagy and necroptosis.

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“…[13] For instance, the natural product berberine shows therapeutic potential in treatment of cancer and diabetes, [14] and aspergillitine, isolated from Aspergillus versicolor in marine sponge, exhibited antibacterial activity against Bacillus subtilis . [15] Fluorine incorporation into isoquinoline has been proven to reduce in vivo metabolism, [16] particularly as a bioisostere of hydrogen to block oxidation at C-4 (the major metabolism), and thus serves as a valuable fluorine-containing component in pharmaceutical design, [17] for example Glanatec ® .…”

mentioning

confidence: 99%

Efficient Pathway for the Preparation of Aryl(isoquinoline)iodonium(III) Salts and Synthesis of Radiofluorinated Isoquinolines

et al. 2016

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Iodonium compounds play a pivotal role in 18F-fluorination of radiopharmaceuticals containing non-activated arenes. However, preparation of these species is limited to oxidation conditions or exchange with organometallics that are prepared from aryl halides. Herein we describe a novel ‘one-pot’ process to assemble aryl(isoquinoline)iodonium salts in 40-94% yields from mesoionic carbene silver complex and Aryl-I-Py2(OTf)2. The method is general, practical, and compatible with well-functionalized molecules as well as useful for the preparation of a wide range of 18F-labeled isoquinolines resulting in up to 92% radiochemical conversion. As proof of concept, a fluorinated isoquinoline alkaloid, 18F-aspergillitine is prepared in 10% isolated radiochemical yield from the corresponding phenyl(aspergillitine)iodonium salt.

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Berberine, an Epiphany Against Cancer

Cited by 227 publications

References 114 publications

Effect of new berberine derivatives on colon cancer cells

Effect of new berberine derivatives on colon cancer cells

Natural Compounds As Modulators of Non-apoptotic Cell Death in Cancer Cells

Efficient Pathway for the Preparation of Aryl(isoquinoline)iodonium(III) Salts and Synthesis of Radiofluorinated Isoquinolines

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