Biological Activity of Berberine—A Summary Update

Och, Anna; Podgórski, Rafał; Nowak, Renata

doi:10.3390/toxins12110713

Cited by 122 publications

(86 citation statements)

References 119 publications

(181 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Modern pharmacological studies have revealed that berberine also possesses anti-diabetic ( Yin et al, 2008 ), hypolipidemic ( Kong et al, 2004 ), anti-inflammatory ( Habtemariam, 2016 ), immunosuppressive ( Li et al, 2016 ) and anti-cancer ( Liu et al, 2019 ) activities. In addition to Asian countries, berberine has currently received great interest in European ( Och et al, 2020 ) and also gained entry in African countries as a dietary supplement ( Alolga et al, 2016 ).…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics and Excretion of Berberine and Its Nine Metabolites in Rats

Feng

Wang²,

Cao

et al. 2021

Front. Pharmacol.

View full text Add to dashboard Cite

Berberine, a well-known alkaloid, has been proved to possess various pharmacological activities. Previous studies demonstrated that berberine could be extensively metabolized and the metabolites also contributed to its therapeutic effects. However, as for berberine’s metabolites, especially phase II metabolites, pharmacokinetics and excretion studies were rarely reported. The objective of this study was to thoroughly investigate the pharmacokinetic and excretion profiles of berberine and its nine metabolites, namely, berberrubine (M1), demethyleneberberine (M2), jatrorrhizine (M3), jatrorrhizine-3-O-β-D-glucuronide (M4), jatrorrhizine-3-O-sulfate (M5), thalfendine-10-O-β-D-glucuronide (M6), berberrubine-9-O-β-D-glucuronide (M7), demethyleneberberine-2-O-sulfate (M8) and demethyleneberberine-2-O-β-D-glucuronide (M9) in rats. An accurate and reliable LC-MS/MS method was developed and validated for the determination of berberine and its nine metabolites in rat biosamples. Pharmacokinetic profiles of berberine and its nine metabolites were obtained after a single intravenous administration (4.0 mg/kg) and oral administration (48.2, 120 or 240 mg/kg) of berberine in rats. For excretion study, rats were intragastrically administered a single dose of 48.2 mg/kg berberine. Our results showed that berberine could be metabolized rapidly and all the nine metabolites could be detected in vivo. The absolute bioavailability of berberine was 0.37 ± 0.11%. As for the AUC0–48 h values, phase II metabolites were much higher than those of phase I metabolites, suggesting that phase II metabolites were the major metabolites exist in blood circulation. 18.6% of the berberine was excreted in feces as berberrubine (M1). The total recovery of berberine and its nine metabolites from urine, bile and feces was 41.2%. This is the first systematic study about the pharmacokinetics and excretion of berberine and its nine metabolites, which will be beneficial for both better understanding the clinical effects and further development of berberine.

show abstract

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics and Excretion of Berberine and Its Nine Metabolites in Rats

Feng

Wang²,

Cao

et al. 2021

Front. Pharmacol.

View full text Add to dashboard Cite

show abstract

“…BBR has a wide range of pharmacological and therapeutic effects, and BBR has been widely used for its antimicrobial and antiprotozoal activities ( 2 ). Recently, as research continues, BBR has also been found to play a role in mood disorders ( 3 ), high blood pressure ( 4 ), hypercholesterolemia ( 5 ), hyperlipidemia ( 5 ), diabetes ( 6 ), heart failure ( 7 ), colorectal cancer ( 8 ), and other diseases. Because of its many effects, BBR is as commonly used as are aspirin and metformin.…”

Section: Introductionmentioning

confidence: 99%

Berberine Suppresses Stemness and Tumorigenicity of Colorectal Cancer Stem-Like Cells by Inhibiting m6A Methylation

Zhao

Zeng

Guo³

et al. 2021

Front. Oncol.

View full text Add to dashboard Cite

BackgroundCancer stem cells (CSCs) are able to survive after cancer therapies, resulting in tumor progression and recurrence, as is seen in colorectal cancer. Therapies targeting CSCs are regarded as novel and promising strategies for efficiently eradicating tumors. Berberine, an isoquinoline alkaloid extracted from the Chinese herbal medicine Coptis chinensis, was found to have antitumor activities against colorectal cancer, without knowing whether it exerts inhibitory effects on colorectal CSCs and the potential mechanisms.MethodsIn this study, we examined the inhibitory roles of Berberine on CSCs derived from HCT116 and HT29 by culturing in serum-free medium. We also examined the effects of Berberine on m6A methylation via regulating fat mass and obesity-associated protein (FTO), by downregulating β-catenin.ResultsWe examined the effects of Berberine on the tumorigenicity, growth, and stemness of colorectal cancer stem-like cells. The regulatory effect of Berberine on N6-methyladenosine (m6A), an abundant mRNA modification, was also examined. Berberine treatment decreased cell proliferation by decreasing cyclin D1 and increasing p27 and p21 and subsequently induced cell cycle arrest at the G1/G0 phase. Berberine treatment also decreased colony formation and induced apoptosis. Berberine treatment transcriptionally increased FTO and thus decreased m6A methylation, which was reversed by both FTO knockdown and the addition of the FTO inhibitor FB23-2. Berberine induced FTO-related decreases in stemness in HCT116 and HT29 CSCs. Berberine treatment also increased chemosensitivity in CSCs and promoted chemotherapy agent-induced apoptosis. Moreover, we also found that Berberine treatment increased FTO by decreasing β-catenin, which is a negative regulator of FTO.ConclusionsOur observation that Berberine effectively decreased m6A methylation by decreasing β-catenin and subsequently increased FTO suggests a role of Berberine in modulating stemness and malignant behaviors in colorectal CSCs.

show abstract

“…Berberine, a well-known isoquinoline alkaloid of the protoberberine type, is distributed among the Berberidaceae, Papaveraceae, and Ranunculaceae plant families and mostly isolated from different Berberis species [ 20 , 21 ]. Berberine is known for its proapoptotic and autophagic potential against many types of cancer but also for its chemosensitizing properties suggesting its use in combination therapy [ 21 , 22 , 23 ]. With regard to MM, berberine downregulated miRNA-21 expression and significantly upregulated programmed cell death 4 (PDCD4) leading to apoptosis and G2 phase cell cycle arrest in RPMI8226 cells [ 17 ].…”

Section: Resultsmentioning

confidence: 99%

Multiple Myeloma Inhibitory Activity of Plant Natural Products

Jöhrer

Ҫiҫek

2021

Cancers

View full text Add to dashboard Cite

A literature search on plant natural products with antimyeloma activity until the end of 2020 resulted in 92 compounds with effects on at least one human myeloma cell line. Compounds were divided in different compound classes and both their structure–activity-relationships as well as eventual correlations with the pathways described for Multiple Myeloma were discussed. Each of the major compound classes in this review (alkaloids, phenolics, terpenes) revealed interesting candidates, such as dioncophyllines, a group of naphtylisoquinoline alkaloids, which showed pronounced and selective induction of apoptosis when substituted in position 7 of the isoquinoline moiety. Interestingly, out of the phenolic compound class, two of the most noteworthy constituents belong to the relatively small subclass of xanthones, rendering this group a good starting point for possible further drug development. The class of terpenoids also provides noteworthy constituents, such as the highly oxygenated diterpenoid oridonin, which exhibited antiproliferative effects equal to those of bortezomib on RPMI8226 cells. Moreover, triterpenoids containing a lactone ring and/or quinone-like substructures, e.g., bruceantin, whitaferin A, withanolide F, celastrol, and pristimerin, displayed remarkable activity, with the latter two compounds acting as inhibitors of both NF-κB and proteasome chymotrypsin-like activity.

show abstract

Biological Activity of Berberine—A Summary Update

Cited by 122 publications

References 119 publications

Pharmacokinetics and Excretion of Berberine and Its Nine Metabolites in Rats

Pharmacokinetics and Excretion of Berberine and Its Nine Metabolites in Rats

Berberine Suppresses Stemness and Tumorigenicity of Colorectal Cancer Stem-Like Cells by Inhibiting m6A Methylation

Multiple Myeloma Inhibitory Activity of Plant Natural Products

Contact Info

Product

Resources

About