Protein tyrosine phosphatase 1B inhibitory activity of alkaloids from Rhizoma Coptidis and their molecular docking studies

Choi, Jae Sue; Ali, Yousof; Jung, Hyun Ah; Oh, Sang Ho; Choi, Ran Joo; Kim, Eon Ji

doi:10.1016/j.jep.2015.05.020

Cited by 52 publications

(21 citation statements)

References 52 publications

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“…Anti-diabetic potential of Coptis alkaloids, including MGN, was estimated by the evaluation of the ability of these active compounds to inhibit the protein tyrosine phosphatase 1B (PTP1B) and the ONOO (-)-mediated protein tyrosine nitration by Choi and co-investigators [72]. MGN showed significant inhibitory activity against PTP1B enzyme with the IC 50 value of 28.14 µM, compared to the ursolic acid (positive control).…”

Section: The Effect On Carbohydrate-lipid Metabolismmentioning

confidence: 99%

Advances in Chemistry and Bioactivity of Magnoflorine and Magnoflorine-Containing Extracts

Okon

Kukuła-Koch

Jarząb

et al. 2020

IJMS

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The review collects together some recent information on the identity and pharmacological properties of magnoflorine, a quaternary aporphine alkaloid, that is widely distributed within the representatives of several botanical families like Berberidaceae, Magnoliaceae, Papaveraceae, or Menispermaceae. Several findings published in the scientific publications mention its application in the treatment of a wide spectrum of diseases including inflammatory ones, allergies, hypertension, osteoporosis, bacterial, viral and fungal infections, and some civilization diseases like cancer, obesity, diabetes, dementia, or depression. The pharmacokinetics and perspectives on its introduction to therapeutic strategies will also be discussed.

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Section: The Effect On Carbohydrate-lipid Metabolismmentioning

confidence: 99%

Advances in Chemistry and Bioactivity of Magnoflorine and Magnoflorine-Containing Extracts

Okon

Kukuła-Koch

Jarząb

et al. 2020

IJMS

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“…Rhizoma coptidis , commonly known as Huang Lian in China, has been one of the most important medicinal plants used for the treatment of various diseases in traditional Chinese medicine for more than 2000 years. In recent years, numerous scientific studies have demonstrated that Rhizoma coptidis and its main active constituents display a variety of activities including anti‐bacterial, anti‐cancer, anti‐hyperglycemic, anti‐hyperlipidemic, anti‐diabetic, anti‐obesity, anti‐inflammatory, radio‐protective and hepato‐protective effects . Moreover, Rhizoma coptidis and its isolated alkaloids have been reported to have cardio‐protective and neuro‐protective properties.…”

Section: Introductionmentioning

confidence: 99%

Metabolic profile of Rhizoma coptidis in human plasma determined using ultra‐high‐performance liquid chromatography coupled with high‐resolution mass spectrometry

Zhang

Wang

Han

et al. 2017

Rapid Comm Mass Spectrometry

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Rationale: Rhizoma coptidis extract and its alkaloids show various pharmacological activities, but its metabolic profile in human plasma has not been thoroughly investigated. In the present research, the metabolism of Rhizoma coptidis at a clinical dose (5 g/60 kg/day) was systematically analyzed to determine its biotransformation processes in human plasma.Methods: In this research, the metabolites of Rhizoma coptidis in human plasma after oral administration of Rhizoma coptidis extract at a clinical dose were investigated using ultrahigh-performance liquid chromatography (UHPLC) coupled with high-resolution LTQ-Orbitrap mass spectrometry. The structural elucidation of the constituents was confirmed by comparing their retention times (t R ) and MS n fragments with those of standards and literature reports.Results: In total, two prototypes and twelve metabolites were detected in human plasma. The two prototypes were confidently identified using reference standards. Of the compounds detected, M7 (berberrubinen-9-O-glucuronide) was the most abundant based on its peak area, which indicates that this compound might be a pharmacokinetic marker for Rhizoma coptidis alkaloids in humans. Based on the metabolites detected in human plasma, a possible metabolic pathway for Rhizoma coptidis in vivo was proposed. Conclusions:The results indicated that the alkaloids in Rhizoma coptidis were extensively biotransformed in vivo mainly via conjugation with glucuronic acid (GluA) or sulfuric acid (SulA) to form phase II metabolites, and the GluA metabolites are likely the dominant form in human plasma. To the best of our knowledge, this is the first in vivo evaluation of the metabolic profile of the whole Rhizoma coptidis extract in human plasma, which is essential for determining the chemicals responsible for the pharmacological activities of Rhizoma coptidis in vivo. Moreover, it would be beneficial for us to further systematically study the pharmacokinetic behavior of Rhizoma coptidis in humans.

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“…It has been used for thousands of years in Chinese traditional medicine to treat damp-heat, dysentery, jaundice, heart fire hyperactivity, carbuncles and sores [2]. Increasingly modern pharmacological investigations have demonstrated that the extracts/compounds isolated from RCC can be used to treat inflammation [3], infection [4], dysentery [5], hypertension [6], gastrointestinal cancer [7], and type 2 diabetes mellitus (T2DM) [8]. In addition, recent research has also reported that RCC contains various chemical constituents including alkaloids, polysaccharides, and organic acids [8][9][10][11].…”

Section: Introductionmentioning

confidence: 99%

“…Importantly, T2DM makes up approximately 90 % of DM cases [13]. Although insulin and other first-line drugs for treating T2DM have been widely used in clinics, some drugs involve significant adverse effects (e.g., abdominal distention, diarrhea, and flatulence) that limit their clinical popularity [8,14]. Therefore, it is important to discover more novel drugs for treating T2DM.…”

Section: Introductionmentioning

confidence: 99%

“…Therefore, it is important to discover more novel drugs for treating T2DM. Previous studies have demonstrated that RCC possesses a notable anti-diabetic effect, and alkaloids were reported to be its primary bioactive constituents [8,15]. Moreover, a water-soluble polysaccharide isolated from C. chinensis has been proven to possess significant antidiabetic and antioxidant activity [16].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Inhibitory Effects of Various Ratios of Polysaccharides/Alkaloids from Rhizome of <i>Coptis chinensis</i> Franch on α-Glucosidase

Peng¹,

Tang²,

Li³

et al. 2016

Trop. J. Pharm Res

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Protein tyrosine phosphatase 1B inhibitory activity of alkaloids from Rhizoma Coptidis and their molecular docking studies

Cited by 52 publications

References 52 publications

Advances in Chemistry and Bioactivity of Magnoflorine and Magnoflorine-Containing Extracts

Advances in Chemistry and Bioactivity of Magnoflorine and Magnoflorine-Containing Extracts

Metabolic profile of Rhizoma coptidis in human plasma determined using ultra‐high‐performance liquid chromatography coupled with high‐resolution mass spectrometry

Inhibitory Effects of Various Ratios of Polysaccharides/Alkaloids from Rhizome of <i>Coptis chinensis</i> Franch on α-Glucosidase

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