The enhancement of cardiotoxicity that results from inhibiton of CYP 3A4 activity and hERG channel by berberine in combination with statins.

@article{Feng2018TheEO,
  title={The enhancement of cardiotoxicity that results from inhibiton of CYP 3A4 activity and hERG channel by berberine in combination with statins.},
  author={Pan-feng Feng and Lei Zhao and Fengfeng Guo and Bo Zhang and Li Fang and Ge Zhan and Xueqi Xu and Qing Fang and Zhaoguang Liang and Baoxin Li},
  journal={Chemico-biological interactions},
  year={2018},
  volume={293},
  pages={
          115-123
        }
}

Figures and Tables from this paper

Evaluation of cytochrome P450 3A4‑mediated drug‑drug interaction potential between P2Y12 inhibitors and statins.

It is demonstrated that the co‑administration of P2Y12 inhibitors with simvastatin could markedly inhibit the activity of CYP3A4, and these findings will further influence the assessment of the clinical effectiveness and safety in the clinic.

Metabolic Susceptibility of 2-Chlorothioxanthone and Its Toxic Effects on mRNA and Protein Expression and Activities of Human CYP1A2 and CYP3A4 Enzymes.

The metabolic susceptibility of residual 2-Cl-TX, the proposed metabolites and the significant toxic effect on the activities, mRNA, and protein expression of CYP1A2 and CYP3A4 are vital to the human health and safety risk assessment from this ubiquitous xenobiotic.

Research progress on the pharmacological effects of berberine targeting mitochondria

It is proposed that berberine mainly regulates glycolipid metabolism by regulating mitochondria respiratory chain function, promotes tumor cell apoptosis by regulating mitochondrial apoptosis pathway, and protects cardiac function by promoting mitophagy to alleviate mitochondrial dysfunction.

The pharmacological activity of berberine, a review for liver protection.

Discovery of 7,9-Disulfatetrahydroberberine as Novel Lipid-Lowering Agents

A new scaffold of 7,9-disulfatetrahydroberberine was discovered unexpectedly, provided with extremely low cytotoxicity and verified the feasibility of the development of BBR as a lipid-lowering drug via disubstituted modification at the 7- and 9-position.

Berberine: a Promising Natural Isoquinoline Alkaloid for Development of Hypolipidemic Drug.

The physicochemical property, the lipid-lowering mechanism, and the modification study of berberine, all are discussed in succession to promote the depth development of ber Berberine as a lipid- Lowering agent.

Influence of Gegenqinlian Decoction on Pharmacokinetics and Pharmacodynamics of Atorvastatin Calcium in Hyperlipidemic Rats

GQD combined with AC can improve the lipid-lowering effect of AC and reduce the damage of AC to the liver simultaneously, however, GQD can inhibit the activity of CYP3A2 in hyperlipidemic rats and increase the blood concentration of AC.

Berberine in Cardiovascular and Metabolic Diseases: From Mechanisms to Therapeutics

A timely overview of the pharmacological properties and therapeutic application of BBR in CVMD is provided, and recent pharmacological advances which validate BBR as a promising lead drug against CVMD are underlined.

References

SHOWING 1-10 OF 34 REFERENCES

Repeated administration of berberine inhibits cytochromes P450 in humans

Repeated administration of berberine decreased CYP2D6, 2C9, and CYP3A4 activities, and drug-drug interactions should be considered when berberines is administered.

Inhibitory effects and mechanism of dihydroberberine on hERG channels expressed in HEK293 cells

DHB acutely blocked hERG channels by binding the aromatic Tyr652 and Phe656, and forward trafficking was disrupted by impaired channel folding associated with altered interactions between hERG proteins and chaperones.

Berberine Induces hERG Channel Deficiency through Trafficking Inhibition

It is demonstrated that BBR induces hERG channel deficiency by inhibiting channel trafficking after incubation for 24h, and the ER-restricted hERG was ubiquitinized and degraded in lysosomes and proteasomes.

Rosuvastatin blocks hERG current and prolongs cardiac repolarization.

It is proposed that some patients may be at risk of rosuvastatin-induced LQTS after using in vitro, ex vivo, and in vivo models and observing genetic polymorphisms observed for BCRP, MDR1, and OATP2B1 and IC(50) determined for hERG blocking.

Charactering the metabolism of cryptotanshinone by human P450 enzymes and uridine diphosphate glucuronosyltransferases in vitro

Cryptotanshinone was extensively metabolized by UGTs following metabolism by CYPs in the liver, and it was shown that the metabolites at m/z of 473 were mediated by U GT1A9 and that the metabolites at m-Z of 489 were mediatedBy UGT 2B7 and UGT2B4.

Antidepressant-induced Ubiquitination and Degradation of the Cardiac Potassium Channel hERG*

A previously unrecognized combination of two entirely different mechanisms; desipramine increases hERG endocytosis and degradation as a consequence of drug-induced channel ubiquitination and simultaneously inhibits hERG forward trafficking from the endoplasmic reticulum are described.

Berberine is a novel cholesterol-lowering drug working through a unique mechanism distinct from statins

Findings show berberine (BBR) as a new hypolipidemic drug with a mechanism of action different from that of statin drugs.