Safety evaluation of main alkaloids from Rhizoma Coptidis

Yi, Jae-Seon; Yang, Xiaoli; Wang, Dezhen; He, Kai; Yang, Yong; Liu, Xujing; Li, Xuegang

doi:10.1016/j.jep.2012.10.062

Cited by 123 publications

(64 citation statements)

References 24 publications

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“…The IC 50 of BBR is 48 ug/ml and 41 µg/ml, respectively, in HepG2 cells and 3T3-L1 adipocytes (Yi et al 2013). This is in the order of 120-140 µM.…”

Section: Safety and Tolerability Of Berberinementioning

confidence: 89%

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Berberine as a therapy for type 2 diabetes and its complications: From mechanism of action to clinical studies

Chang

Chen

Hatch

2015

Biochem. Cell Biol.

129

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The incidence of type 2 diabetes is increasing rapidly worldwide, and the development of novel anti-diabetic drugs is emerging. However, most anti-diabetic drugs cannot be used in patients with hepatic dysfunction, renal disease, and heart disease, which makes pharmacological therapy of type 2 diabetes complicated. Despite continued introduction of novel agents, the search for an ideal drug that is useful as both a hypoglycemic agent and to reduce diabetes-related complications remains elusive. Berberine is an isoquinoline alkaloid extract that has shown promise as a hypoglycemic agent in the management of diabetes in animal and human studies. Mechanistic studies have revealed beneficial effects of berberine on diabetes-related complications. Although there have been few clinical reports of the anti-diabetic effects of berberine, little documentation of adverse effects in humans positions it as a potential candidate drug to treat type 2 diabetes. In the present review, the anti-diabetic mechanism of berberine, its effect on diabetes-related complications, and its recent use in human clinical studies is highlighted. In addition, we summarize the different treatments for type 2 diabetes in adults and children.

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“…The IC 50 of BBR is 48 ug/ml and 41 µg/ml, respectively, in HepG2 cells and 3T3-L1 adipocytes (Yi et al 2013). This is in the order of 120-140 µM.…”

Section: Safety and Tolerability Of Berberinementioning

confidence: 89%

“…However, no mortality has been observed in rats treated with BBR at 521 mg/kg/day for 3 months (Yi et al 2013). The effective antihyperglycemic dose of BBR is generally no more than 100 mg/kg/day in rats (Chang et al 2012).…”

Section: Safety and Tolerability Of Berberinementioning

confidence: 99%

Berberine as a therapy for type 2 diabetes and its complications: From mechanism of action to clinical studies

Chang

Chen

Hatch

2015

Biochem. Cell Biol.

129

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“…It was also found that the toxicity of Pal was the minimal among the four major C . chinensis alkaloids (berberine, coptisine, palmatine and epiberberine), while berberine was relatively more toxic in both in vitro and in vivo assays [33]. In our previous investigation, the IC 50 of berberine against HPU and JBU was 10.20 ± 1.10 mM and above 13.00 mM, respectively [8], indicating the anti-urease activity of berberine was weaker as compared with that of Pal.…”

Section: Discussionmentioning

confidence: 99%

Inhibition of Helicobacter pylori and Its Associated Urease by Palmatine: Investigation on the Potential Mechanism

Zhou

Tan

et al. 2017

PLoS ONE

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In this paper, we evaluated the anti-Helicobacter pylori activity and the possible inhibitory effect on its associated urease by Palmatine (Pal) from Coptis chinensis, and explored the potential underlying mechanism. Results indicated that Pal exerted inhibitory effect on four tested H. pylori strains (ATCC 43504, NCTC 26695, SS1 and ICDC 111001) by the agar dilution test with minimum inhibitory concentration (MIC) values ranging from 100 to 200 μg/mL under neutral environment (pH 7.4), and from 75 to 100 μg/mL under acidic conditions (pH 5.3), respectively. Pal was observed to significantly inhibit both H. pylori urease (HPU) and jack bean urease (JBU) in a dose-dependent manner, with IC50 values of 0.53 ± 0.01 mM and 0.03 ± 0.00 mM, respectively, as compared with acetohydroxamic acid, a well-known urease inhibitor (0.07 ± 0.01 mM for HPU and 0.02 ± 0.00 mM for JBU, respectively). Kinetic analyses showed that the type of urease inhibition by Pal was noncompetitive for both HPU and JBU. Higher effectiveness of thiol protectors against urease inhibition than the competitive Ni2+ binding inhibitors was observed, indicating the essential role of the active-site sulfhydryl group in the urease inhibition by Pal. DTT reactivation assay indicated that the inhibition on the two ureases was reversible, further supporting that sulfhydryl group should be obligatory for urease inhibition by Pal. Furthermore, molecular docking study indicated that Pal interacted with the important sulfhydryl groups and inhibited the active enzymatic conformation through N-H ∙ π interaction, but did not interact with the active site Ni2+. Taken together, Pal was an effective inhibitor of H. pylori and its urease targeting the sulfhydryl groups, representing a promising candidate as novel urease inhibitor. This investigation also gave additional scientific support to the use of C. chinensis to treat H. pylori-related gastrointestinal diseases in traditional Chinese medicine. Pal might be a potentially beneficial therapy for gastritis and peptic ulcers induced by H. pylori infection and other urease-related diseases.

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“…Earlier studies reported in literature analyzed cytotoxic effects of the different alkaloids in HepG2 cells. IC 50 values of chelidonine were 34.50 M (12.19 g/ml) after 24 h (El-Readi et al, 2013), the corresponding IC 50 values of berberine and coptisine were 129.56 M (48.17 g/ml) and 202.33 M (64.81 g/ml), respectively (Yi et al, 2013). Sanguinarine and chelerythrine showed IC 50 values between 5 and 10 M (24 h) (Zdarilova et al, 2006), while protopine did not show a significant change in relation to the control at a concentration of 75 M after 24 h (Vrba et al, 2011).…”

Section: Discussionmentioning

confidence: 99%

Combining metabolomic analysis and microarray gene expression analysis in the characterization of the medicinal plant Chelidonium majus L

Orland¹,

Knapp²,

König³

et al. 2014

Phytomedicine

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Safety evaluation of main alkaloids from Rhizoma Coptidis

Cited by 123 publications

References 24 publications

Berberine as a therapy for type 2 diabetes and its complications: From mechanism of action to clinical studies

Berberine as a therapy for type 2 diabetes and its complications: From mechanism of action to clinical studies

Inhibition of Helicobacter pylori and Its Associated Urease by Palmatine: Investigation on the Potential Mechanism

Combining metabolomic analysis and microarray gene expression analysis in the characterization of the medicinal plant Chelidonium majus L

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